Most Importante drugzz (A-topiczz) Flashcards

Question

A6: DIGOXIN (cardiotonic)

Answer 1

GROUP: Cardiotonic (from the digitalis lanata plant) MOA: They inhibit the Na+/K+ ATPase enzyme which is responsible for Na+ efflux and K+ influx -> increased contractility of the heart -> Positive inotropic effect PK: - Positive inotropic effect → improves the renal blood flow → increases water and Na+ excretion, given orally, excretion via kidney SE: Cardiac arrythmias and bradycardia, hypokalemia and extracardial signs are GI-signs like vomiting. It has a narrow therapeutic index INDICATION: Prolong survival time in heart failure, supraventricular tachyarrhytmias (it increases contractility) CONTRAINDICATION: Should not be given with NSAIDs, glucocorticoids or Furosemide as they will compete for the protein albumin and it should not be used in patients with renal failure ANTIDOTE: Digibind

Answer 2

GROUP: Phosphidiesterase inhibitor MOA: Inhibits the PDE3 enzyme in the heart muscle → accumulation of cAMP → increase in calcium concentration → Positive inotropic effect PK: Given orally, one hour before meals, as feeding decrease its absorption and causes vomiting SE: Very rare, mainly GI related (vomiting and diahrrea) INDICATION: - Prolong survival time in heart failure - Supraventricular tachyarrhytmias CONTRAINDICATION: Outflow obstruction (HCM, stenosis) i.e. must perform an ultrasound before administration

Answer 3

GROUP: ACE-inhibitor MOA: ACE inhibitors cause vasodilation → decrease afterload Diuretic effect: Increases water excretion → decrease preload. It is good in heart failure PK: Good absorption, lasts 12-24 hrs, metabolism: Benazepril -> Benazeprilat, excretion via kidney and bile (do not decrease dose in renal failure patients) SE: -Azotaemia --> urea creatinine levels rise, LD50 is very high i.e. safe INDICATIONS: - Heart failure (species!) - Hypertension - Proteinuria (Increase heart performance and decrease blood pressure, but not alter contractility) DOSE: Dog/Cat: PO 0.25-0.5 mg/kg

Answer 4

GROUP: ACE-inhibitor MOA: ACE inhibitors cause vasodilation → decrease afterload Diuretic effect: Increases water excretion → decrease preload. It is good in heart failure PK: Good absorption, lasts 12-24 hrs, metabolism: Ramipril → Ramiprilat Excretion: Via urine SE: Azotaemia --> urea creatinine levels rise, LD50 is very high i.e. safe INDICATIONS: - Heart failure (species!) - Hypertension - Proteinuria (Increase heart performance and decrease blood pressure, but not alter contractility) DOSE: Excreted via the urine. When we are treating proteinuria, usually renal failure → dose should be decreased.

Answer 5

GROUP: Angiotensin II receptor blocker (ARB) MOA: Directly antagonise angiotensin II PK: Oral administration → good absorption, duration of action: 12-24 hours, excretion via urine SE: None?? INDICATION: For hypertension and proteinuria, advantages more effective no bradykinin activation

Answer 6

GROUP: (Vasodilator and class IV antiarrhythmic) and calcium channel blocker) MOA: Increasing blood flow and variably decreasing the heart rate via strong depression of A-V node conduction. It is a negative inotrope PK: Well absorbed from the GI SE: Rare, but vomiting and anorexia have been observed in cats INDICATION: Hypertension and angina

Answer 7

GROUP: Phosphidiesterase inhibitor MOA: Inhibits the PDE3 enzyme in the heart muscle → accumulation of cAMP → increase in calcium concentration → Positive inotropic effect PK: Given orally, one hour before meals, as feeding decrease its absorption and causes vomiting SE: Very rare, mainly GI related (vomiting and diahrrea) INDICATION: - Prolong survival time in heart failure - Supraventricular tachyarrhytmias CONTRAINDICATION: Outflow obstruction (HCM, stenosis) i.e. must perform an ultrasound before administration NOTE: Much safer than digoxin

Answer 8

GROUP: Opiate, antitussive, narcotic analgesic MOA: GABAa, decrease Ca2+ accumulation --> inhibits the release of stimulatory neurotransmitters PK: Poor bioavailability in dogs (4-7%), half-life is 1.2-1.5hrs SE: Constipation, drowsiness, mild itching INDICATION: For mild pain DOSE: Ca: PO:1-2 mg/kg

Answer 9

GROUP: Opioid MOA: It acts on the µ, receptors. - In the presynaptic nerve ending these receptors decrease Ca2+ influx prevents release of neurotransmitters from the nerves PK: High bioavailability in cats, highly lipophilic, less in dog and horse, duration 4-6 hours, partial agonist SE: Rare, constipation, nausea, drowsiness INDICATION: Antitussive effect in cats, treat mild pain, calming DOSAGE: Dog: PO: 4-6 mg/kg IV: 2 mg/kg Cat: PO: 2-4 mg/kg IV: 2 mg/kg Horse: PO: 4-10 mg/kg SCHEDULE 4 DRUG

Answer 10

GROUP: Opioid (Acts mainly on the κ- receptor: - Analgesia - Decrease GI motility and secretion - Increase appetite) PK: Highly lipophilic, poor bioavailability (first pass metabolism), administered 6-12 hrs , faster onset of action SE: Sedation, possible emesis, dizziness, hyperthermia, constipation, mydriasis in cats INDICATION: Analgesic, antitussive, good in horses DOSAGE: Ca/fe: IV, IM, SC: 0.2-0.5 mg/kg Eq: IV, IM, SC: 0.01-0.1 mg/kg

Answer 11

GROUP: Antitussive MOA: An agonist of NMDA and sigma-1 receptors PK: Non analgesic, non- addictive, given PO/IM/SC INDICATION: Against cough, safe in cats

Answer 12

GROUP: Mucolytic MOA: Breaking up disulphide bonds in mucoproteins → dissolution of viscous mucus PK: Given PO -> Inhalation, has bad taste / odour INDICATION: Dissolve mucous in the respiratory tract NOTE: It is used as an antidote for paracetamol

Answer 13

GROUP: Expectorant MOA: 1. breaking up mucopolysaccharides, dissolving mucus 2. increasing secretion of serous glands 3. enhancing ciliary movement PK: ?? SE:?? INDICATION: Rhinitis, sinusitis, tracheobronchitis

Answer 14

GROUP: Bronchodilator, β-adrenoceptor agonist and selective sympathomimetic MOA: Agonism of the β(2) receptor stimulates adenylyl cyclase activity which ultimately leads to downstream effects of smooth muscle relaxation in the bronchioles PK: Given PO SE: Tachycardia, tremors and a decreased uterine contraction → decreased by inhalation INDICATION: Used primarily for the treatment of recurrent airway obstruction (RAO) in horses, feline asthma bronchitis, broncho-pneumonia, tracheal hypoplasia, tracheal collapse CONTRAINDICATIONS: Contraindicated in heart failure, arrhythmia and decreased mast cell degranulation - Not used in racehorses (because it is a doping agent) - Not used in food producing animals -> cause meat to have less fat content NOTE: Longer-Acting β2-Specific Drug

Answer 15

GROUP: Bronchodilator, β-adrenoceptor agonist and selective sympathomimetic MOA: Agonism of the β (2) receptor stimulates adenylyl cyclase activity which ultimately leads to downstream effects of smooth muscle relaxation in the bronchioles PK: Given PO SE: - Tachycardia, tremors and a decreased uterine contraction → decreased by inhalation INDICATION: Used primarily for the treatment of recurrent airway obstruction (RAO) in horses, feline asthma bronchitis, broncho-pneumonia, tracheal hypoplasia, tracheal collapse CONTRAINDICATIONS: Contraindicated in heart failure, arrhythmia and decreased mast cell degranulation NOTE: It is a short-acting specific sympathomimetic

Answer 16

GROUP: Bronchodilator, β-adrenoceptor agonist and selective sympathomimetic MOA: Agonism of the β(2) receptor stimulates adenylyl cyclase activity which ultimately leads to downstream effects of smooth muscle relaxation in the bronchioles PK:Can be given SC and IV INDICATIONS: - Horse RAO - Feline asthma bronchitis- Broncho-pneumonia - Tracheal hypoplasia - Tracheal collapse CONTRAINDICATION: Should be used cautiously in animals with diabetes, high blood pressure, overactive thyroid gland (hyperthyroidism) NOTES: Longer-Acting β2-Specific drug. Less specific though!Given to dogs, cats and horses

Answer 17

GROUP: Bronchodilator, β-adrenoceptor agonist and selective sympathomimetic MOA: Agonism of the β(2) receptor stimulates adenylyl cyclase activity which ultimately leads to downstream effects of smooth muscle relaxation in the bronchioles PK: Can be given SC and IV INDICATIONS: - Horse RAO - Feline asthma bronchitis - Broncho-pneumonia - Tracheal hypoplasia - Tracheal collapse NOTE: Most specific and most expensive

Answer 18

GROUP: Methylxanthine derivatives MOA: PDE inhibitors i.e. cAMP level increases → bronchodilation PK: Good absorption and enterohepatic circulation, metabolised in liver SE: Small TI → CV and GI diuresis, can affect CNS at higher doses, given IV or PO INDICATIONS: Given to dogs, cats and horses against: - Horse RAO - Feline asthma bronchitis - Broncho-pneumonia - Tracheal hypoplasia - Tracheal collapse NOTES: Metabolism of theophylline may be inhibited by erythromycin, fluoroquinolone antibiotics (for example, enrofloxacin), and cimetidine

Answer 19

GROUP: Theophylline derivative MOA: PDE inhibitors i.e. cAMP level increases → bronchodilation PK: Good absorption and enterohepatic circulation, metabolised in liver SE: Arrhythmias, vomiting and GIT bleeding. Given IV or PO INDICATION: Given to dogs, cats and horses against: - Horse RAO - Feline asthma bronchitis - Broncho-pneumonia - Tracheal hypoplasia - Tracheal collapse DOSE: Dog: PO, IM 10 mg/kg TID

Answer 20

GROUP: Parasympatholytics MOA: Antagonist of the muscarinic acetylcholine receptor PK: Inhalational administration, safe, very low BBB- penetration, metabolised in the GI tract, excreted in urine INDICATION: Horse RAO (recurrent airway obstruction) = COPD (chronic obstructive pulmonary disease) and human (feline) asthma

Answer 21

GROUP: Short-acting, non-specific bronchodilator MOA: It produces pronounced vasopressive and cardiac effects. PK: Short duration of action SE: May cause tremors, vomiting, high blood pressure or heart rhythm irregularities INDICATION: Is considered the drug of choice for the emergency treatment of life-threatening bronchoconstriction, such as during an anaphylactic reaction DOSAGE: Dogs, cats: IV, IT, 0.01-0.2 mg/kg Horse: IV 0.01-0.02 mg/kg

Answer 22

GROUP: Leukotriene antagonist MOA: They block the cysteinyl leukotriene receptor which is responsible for the bronchoconstriction PK: Given PO INDICATION: Allergic bronchitis, RAO, and Feline asthma

Answer 23

GROUP: Serotonin antagonist and modest antagonist for histamine MOA: Produce some benefit against smooth muscle constriction, vasodilation, increased vascular permeability, and inflammatory cell influx SE: Nausea, vomiting, mydriasis, hypersalivation, and hyperthermia INDICATION: Allergic bronchitis, RAO, and Feline asthma

Answer 24

GROUP: Inhalational glucocorticoid MOA: Decrease mucus production, increase eosinophil diameter → eosinophil apoptosis PK: There are extensive first-pass effects and high plasma protein binding preventing activity of systemic blood concentrations if it is swallowed after delivery INDICATION: Allergic bronchitis, RAO, and Feline asthma

Answer 25

GROUP: A2 agonist (emetic) MOA: They penetrate the BBB and enter the chemoreceptor trigger zone (CTZ) which influence emesis and consists of dopamine and serotonin. PK: Fast absorption, Good distribution (crosses BBB), metabolize in liver, excretion in urine, works within few mins iv and 10-15 mins im SE: Emetic in cats and some dogs, sedation, hypotension, bradycardia INDICATION: Inducing emesis (mostly in cats) and in about 30% of dogs (for example after poisoning or to remove foreign body) CONTRAINDICATION: Boxers/rottweilers, and horse! And in cases of sharp foreign body, seizures, pulmonary edema, pregnant animals etc.. DOSE: Normally Ca and Fe: IM, IV, SC; 1-4 mg/kg Bo: IV, IM: 0.05- 1mg/kg Eq: 0.5-1mg/kg BUT in emesis it is 0.4-0.5 mg/kg iv/im in cats

Answer 26

GROUP: Dopamine agonist MOA: By agonising dopamine receptors, emesis can be induced (which happens in this case) PK: Works after 10 mins, can be re-administered after 20-30 mins SE: Tachycardia and tremor can occur "ANTIDOTE": Metoclopramide INDICATION: Induce emesis (good for dogs)

Answer 27

GROUP: Opioid derivative (emetic agent) MOA: Acts by stimulating CTZ and induce vomiting. After a while it will inhibit CTZ and block the emesis (do not re-administer) PK: Can be given orally but usually given SC, where it will work after 10 mins. Also given as eye drop. SE: Excitation and dysmorphia in cats (so therefore it is better in dogs) INDICATION: Induce emesis in cats and dogs CONTRAINDICATION: Should avoid use in cats if possible due to its side effects

Answer 28

GROUP: Dopamine antagonist (and prokinetic agent) MOA: The cardia will be constricted, the pylorus will be released, the stomach motility will favour the aboral direction and the duodenum motility will be increased. PK: Can be administered orally or i/v but, if given orally, the bioavailability is halved in comparison to the i/v route i.e., the oral dose is double the i/v dose. SE: Excitation and seizures INDICATION: Against vomiting, disturbances with gastric emptying (e.g brachiocephalic dogs and Siamese cats) and reflux disorder CONTRAINDICATION: Do NOT give with phenothiazines, in cases with gastric/duodenal disorders and in animals with MDR1 gene mutation as it will lead to toxicosis DOSE: Ca/fe: IV, SC, PO 0.2-0.5 mg/kg TID Eq: IV 0.04 mg/kg/h (motility increase)

Answer 29

GROUP: Serotonin antagonist MOA: These were developed against the chemotherapeutics as they easily induce vomiting via serotonin release (so it inhibits serotonin relase and prevent vomiting) PK: Orally (double dose needed) or IV. They have excellent efficacy against other origins of emesis and are the most potent antiemetic agent INDICATION: Used in chemotherapeutic induced emesis DOSE: Ca/fe: IV, SC, PO 0.2-0.5 mg/kg TID Horse: IV 0.04 mg/kg/h (motility increase)

Answer 30

GROUP: Neurokinin-1 antagonist MOA: Act on the neurokinin-1 receptor, where the P-substance also acts PK: Injection only (SC or IV), bioavailability is quartered if given orally, quick action and reach max. plasma conc. after 40 mins, long half-life SE: Pain during injection, mild analgesic and anti-inflammatory effects, reduction of iso-and sevoflurane INDICATION: Any kind of emesis

Answer 31

GROUP: Dopamine antagonist (and prokinetic agent) MOA: The cardia will be constricted, the pylorus will be released, the stomach motility will favour the aboral direction and the duodenum motility will be increased. Central and peripheral effect PK: Can be administered orally or i/v but, if given orally, the bioavailability is halved in comparison to the i/v route i.e., the oral dose is double the i/v dose. SE: Excitation and seizures INDICATION: Against vomiting, disturbances with gastric emptying (e.g brachiocephalic dogs and Siamese cats) and reflux disorder CONTRAINDICATION: Do NOT give with phenothiazines, in cases with gastric/duodenal disorders and in animals with MDR1 gene mutation as it will lead to toxicosis DOSE: Dog/ cat: IV, SC, PO 0.2-0.5 mg/kg TID Horse: IV 0.04 mg/kg/h (motility increase)

Answer 32

GROUP: Serotonin agonist (prokinetic agent) MOA: Can effect the whole GI tract, increasing the motility PK: Does not cross BBB (I think) INDICATION: Against vomiting, disturbances with gastric emptying (e.g brachiocephalic dogs and Siamese cats) and reflux disorder (better than cisapride)

Answer 33

GROUP: Antiulcer agent (and coating agent) MOA: The sucrose octasulfate is a coating agent but it has a lot of side chains in the molecule which can bind the damaged proteins to form a layer (coating effect) and inactivate pepsin and bile acids slightly PK: Give at least one hour before feed (needs acidic PH), absorption may be decreased SE: Rare, but Al(OH)3 can cause constipation INDICATION: Used against gastric ulcers (by decreasing HCL)

Answer 34

GROUP: H2 antagonist MOA: Competitive antagonists of histamine on H2 receptors on parietal cells -> decrease of HCL production PK: Good absorption, longest half-life. Given orally and IV. Oral bioavailability is lower than injection SE: Tolerance can be formed (rebound effect) if used for more than 2 weeks. Slow discontinuation!! CONTRAINDICATION: Can be used for treatment only, not yet for prevention DOSE: Dog/cat: PO, IV 0.5-1 mg/kg SID, BID (cats, long term: BID every second day)

Answer 35

GROUP: Proton pump inhibitor MOA: Prodrugs --> Activates in acidic PH. Given orally--> absorbed in intestines, through blood stream they go back into the stomach and destroys the proton pump inhibitor. For treatment AND prevention of gastric ulcers. PK: Should be given orally (before or after the meal)--> absorbed in intestines. Give with coating (GI resistant) to protect the active susbtance so it does not dissolve before being absorbed. Reach max effect after 3-4 days SE: CYP enzyme inhibition, rebound effect after 2 weeks, dysbacteriosis (due to increased PH) INDICATION: Against gastric ulcers. CONTRAINDICATION: Do NOT give with antacids (as these increases gastric PH) DOSE: Dog/cat: PO 0.5-1 mg/kg SID, BID Horse: PO 2-4 mg/kg SID

Answer 36

GROUP: Proton pump inhibitor MOA: Prodrugs --> Activates in acidic PH. Given orally--> absorbed in intestines, through blood stream they go back into the stomach and destroys the proton pump inhibitor. For treatment AND prevention of gastric ulcers. PK: Should be given orally (before or after the meal)--> absorbed in intestines. Give with coating (GI resistant) to protect the active susbtance so it does not dissolve before being absorbed. Reach max effect after 3-4 days SE: CYP enzyme inhibition, rebound effect after 2 weeks, dysbacteriosis (due to increased PH) INDICATION: Against gastric ulcers. CONTRAINDICATION: Do NOT give with antacids (as these increases gastric PH)

Answer 37

GROUP: Choleretic MOA: Hydrophilic bile acid that dissolves hydrophobic bile acids and decrease their viscosity, to allow them to flow out of the liver PK: Given orally as liquid or a tablet. SE: ?? INDICATION: used for chronic liver disease, biliary cirrhosis, and cholangitis (frequent in cats) CONTRAINDICATIONS: In post-hepatic bile duct obstruction e.g. a tumor or stone in the bile duct that blocks it, because the bile acid cannot flow out of the liver.

Answer 38

GROUP: Liver protectants, originating from milk thistle. Complex of drugs (flavonolignans) MOA: Neutralize free radicals as well as decreasing lipid peroxidation. Aids in the reactivation of the glutathione system which leads to an antioxidant effect. It has a cytoprotective agent i.e. it is a membrane stabiliser and decreases the penetration of the toxins into the liver cells. PK: Given orally SE: ?? INDICATION: Death cap poisoning, not just in horses but in dogs aslo. Acute and chronic liver failure, cirrhosis and fibrosis i.e. against hepatotoxic substances e.g. anticonvulsant drugs.

Answer 39

GROUP: Lipotropic agents (liver protectants) MOA: Methyl donors, which help in lipid movement from the liver cells i.e. they aid in hepatic lipidosis (fatty liver disease) which is mainly seen in cats or in ruminants during parturition. SAMe: S-ADENOSYLMETHIONINE is a methionine derivative which acts as an antioxidant and hepatoprotectant. It has a SH functional group, which is good for reactivation of gluathione system. It is activated by B-vitamins METIONIN: Has SH functional group, but is not as potent. It is a hepatoprotectant and mild choleretic CHOLINE: No functional group (not choleretic). It removes lipids from liver and increase lipoprotein synthesis and convert lipids to phospholipids

Answer 40

GROUP: Loop diuretics MOA: Inhibit the NKCC2 channel which reabsorbs one Na+ ion, one K+ ion, and two Cl- ions: Na+ excreted in the urine and prevents the reabsorption of water K+ is also excreted in the urine Mg2+ and Ca2+ excreted → when used for a long time, produce magnesium-containing uroliths (struvite stones) or calcium-containing uroliths (calcium oxalate stones) → rare Aldosterone is released, so aldosterone antagonists should be given in combo with these drugs PK: Good oral absorption SE: Hyperkalaemia, alkalosis, hypertension in cats, ototoxicity INDICATIONS: Primary drug for the treatment of heart failure. Can be used in dogs, cats, horses and humans. Acute renal failure when Mannitol is not working but must first ensure rehydration. DOSE: Dog: IV, IM, PO 1-5 mg/kg BID, TID Cat: IV, IM 1-2 mg/kg BID, TID, PO 0.5-2.5 mg/kg BID, TID Horse: IV 0.5-1 mg/kg BID

Answer 41

GROUP: Aldosterone antagonist MOA: Inhibit potassium excretion PK: Extremely safe drugs SE: ?? INDICATION: Long-term treatment of heart failure combined with an ACE inhibitor or Furosemide Dog with heart failure: Combine PIMOBENDAN (longer survival) with FUROSEMIDE and SPIRONOLACTONE Cat: Only furosemide

Answer 42

GROUP: Osmotic diuretic (sugar alcohol) MOA: Enter the glomerulus via the fenestrated capillaries and are filtered into the kidney tubules, it cannot be reabsorbed and is excreted in the urine PK: Given IV, cannot cross biological membranes SE: ?? INDICATION: Brain and lung edema, acue renal failure with anti-freeze poisoning, babesiosis, glaucoma (decrease IOP) CONTRAINDICATIONS: use of mannitol in patients with ongoing intracranial hemorrhage, anuric renal failure, severe dehydration, or pulmonary congestion or edema is contraindicated

Answer 43

GROUP: Cardiotonic (from the digitalis lanata plant) MOA: They inhibit the Na+/K+ ATPase enzyme which is responsible for Na+ efflux and K+ influx -> increased contractility of the heart -> Positive inotropic effect PK: - Positive inotropic effect → improves the renal blood flow → increases water and Na+ excretion, given orally, excretion via kidney SE: Cardiac arrythmias and bradycardia, hypokalemia and extracardial signs are GI-signs like vomiting. It has a narrow therapeutic index INDICATION: Prolong survival time in heart failure, supraventricular tachyarrhytmias (it increases contractility) CONTRAINDICATION: Should not be given with NSAIDs, glucocorticoids or Furosemide as they will compete for the protein albumin and it should not be used in patients with renal failure ANTIDOTE: Digibind

Answer 44

GROUP: Methylxanthine derivatives MOA: PDE inhibitors i.e. cAMP level increases → bronchodilation PK: Good absorption and enterohepatic circulation, metabolised in liver SE: Small TI → CV and GI diuresis, can affect CNS at higher doses, given IV or PO INDICATIONS: Given to dogs, cats and horses against: - Horse RAO - Feline asthma bronchitis - Broncho-pneumonia - Tracheal hypoplasia - Tracheal collapse NOTES: Metabolism of theophylline may be inhibited by erythromycin, fluoroquinolone antibiotics (for example, enrofloxacin), and cimetidine

Answer 45

GROUP: Methylxanthines MOA: PDE inhibitors i.e. cAMP level increases → bronchodilation PK: PK: Good absorption and enterohepatic circulation, metabolised in liver SE: Small TI → CV and GI diuresis, can affect CNS at higher doses, given IV or PO INDICATIONS: Given to dogs, cats and horses against: - Horse RAO - Feline asthma bronchitis - Broncho-pneumonia - Tracheal hypoplasia - Tracheal collapse

Answer 46

GROUP: ACE-inhibitor and cardiac diuretic MOA: ACE inhibitors cause vasodilation → decrease afterload Diuretic effect: Increases water excretion → decrease preload. It is good in heart failure PK: Good absorption, lasts 12-24 hrs, metabolism: Benazepril -> Benazeprilat, excretion via kidney and bile (do not decrease dose in renal failure patients) SE: -Azotaemia --> urea creatinine levels rise, LD50 is very high i.e. safe INDICATIONS: - Heart failure (species!) - Hypertension - Proteinuria (Increase heart performance and decrease blood pressure, but not alter contractility) DOSE: Dog/Cat: PO 0.25-0.5 mg/kg

Answer 47

GROUP: ACE-inhibitor MOA: ACE inhibitors cause vasodilation → decrease afterload Diuretic effect: Increases water excretion → decrease preload. It is good in heart failure PK: Good absorption, lasts 12-24 hrs, metabolism: Ramipril → Ramiprilat Excretion: Via urine SE: Azotaemia --> urea creatinine levels rise, LD50 is very high i.e. safe INDICATIONS: - Heart failure (species!) - Hypertension - Proteinuria (Increase heart performance and decrease blood pressure, but not alter contractility) DOSE: Excreted via the urine. When we are treating proteinuria, usually renal failure → dose should be decreased.

Answer 48

GROUP: Gonadotropin-Releasing Hormone MOA: GnRH stimulates the synthesis and release of gonadotropins by binding to the GnRH receptor, a G protein-coupled receptor linked to the IP3-Ca2+ signal transduction pathway. If given continuous: desensitisation/down-regulation of GnRH receptors in pituitary gland → suppression of gonadotropins, basis of medical castration. Effect on FSH/LH of animal: depends on the dose and route of administration, and the endocrine status of the animal. PK: Short half-life (2-4 min), intermittent release, SC, IM (equine IV), SE: Hyperthermia, fever and luteal body cysts INDICATION: → Follicular cysts in cattle → Infertility in cattle → Decreased pregnancy rates in cattle → Induce ovulation in mares, pigs, and rabbits → Facilitate stripping and to induce mortality due to egg binding in rainbow trout CONTRAINDICATION: Pregnancy (embryo transfer) and in starved, cachexia animals

Answer 49

GROUP: Gonadotropin-Releasing Hormone analogue MOA: GnRH stimulates the synthesis and release of gonadotropins by binding to the GnRH receptor, a G protein-coupled receptor linked to the IP3-Ca2+ signal transduction pathway. If given continuous: desensitisation/down-regulation of GnRH receptors in pituitary gland → suppression of gonadotropins, basis of medical castration. Effect on FSH/LH of animal: depends on the dose and route of administration, and the endocrine status of the animal. PK: Short half-life (2-4 min), intermittent release, SC, IM (equine IV), SE: Hyperthermia, fever and luteal body cysts INDICATION: Infertility therapy: Induce ovulation in cattle and horses Pulse dosing to induce estrus in dogs and cats Increase fertility rate in sows and fur-producing farmed animals

Answer 50

GROUP: Gonadotropin-Releasing Hormone analogue MOA: GnRH stimulates the synthesis and release of gonadotropins by binding to the GnRH receptor, a G protein-coupled receptor linked to the IP3-Ca2+ signal transduction pathway. If given continuous: desensitisation/down-regulation of GnRH receptors in pituitary gland → suppression of gonadotropins, basis of medical castration. Effect on FSH/LH of animal: depends on the dose and route of administration, and the endocrine status of the animal. PK: Short half-life (2-4 min), intermittent release, SC, IM (equine IV), SE: Hyperthermia, fever and luteal body cysts INDICATION: Cystic ovaries therapy in cattle: Therapy → GnRH analogues mimic the effect of LH surge and causes ovulation of follicular cyst. Also used in ferrets to terminate estrus

Answer 51

GROUP: Gonadotropin-Releasing Hormone analogue (superagonist) MOA: Stimulate the synthesis and secretion of FSH and LH by interacting with GnRH receptors on the pituitary gonadotropes. PK: SC implant in horses and dogs or injection. Long-acting SE: ?? INDICATION: Indications: → Chemical castration in males → Contraceptive in females → SC implant → 1 year duration of action

Answer 52

GROUP: Gonadotropin MOA: Large glycoprotein, secreted from the endometrial cups of pregnant mares in early pregnancy in order to maintain a luteotrophic (CL stimulatory) effect upon the primary and secondary CL in the mare PK: Long half-life (2-5 days) SE: Anaphylactic reaction INDICATION: → Advance onset of follicular growth and ovulation → Alone or after pre-treatment of progesterones in: cow, goat, ewe → In combination with hCG and estrogen in: sow, ancestry bitches → Superovulation: increase litter size, embryo transfer → Stimulates spermatogenesis and libido CONTRAINDICATION: Pregnancy

Answer 53

GROUP: Human Chorionic Gonadotropin MOA: Is produced only in primates and is synthesized by syncytiotrophoblast cells of the placenta. PK: Half life is 12-24hrs SE: Anaphylactic reaction INDICATION: → Supplement/replace LH in ovulation failure/delay → Oestrus synchronization → Ovulation in mare at time of breeding → Nymphomania due to cystic ovaries (induce luteinizing and then ovulation) → Ovarian stimulation → Cryptorchidism (males) CONTRAINDICATION: Pregnancy

Answer 54

GROUP: Prostaglandin (synthetic) analogue MOA: Local hormones -> produced by the endometrium. It is released in late diestrus and near term in all pregnant animals. It is released near term in all pregnant animals. PGF2α mediates a decrease in circulating progesterone via luteolysis (corpus luteum regression) at the end of the cycle and pregnancy. PK: Onset is approx 2-5 days and it should not be given IV but rather IM(?) SE: Colic disorders, nausea, vomiting, diarrhoea, bronchoconstriction, abortion INDICATION: Used for estrous synchronization, – to induce parturition (sows, mares, cows with glucocorticoid) – for abortion – for treatment of pyometra They cause premature luteolysis, thus decreasing estrous cycle length and thereby hastening the onset of estrus CONTRAINDICATION: Pregnant animals

Answer 55

GROUP: Prostaglandins MOA: Local hormones -> produced by the endometrium. It is released in late diestrus and near term in all pregnant animals. It is released near term in all pregnant animals. PGF2α mediates a decrease in circulating progesterone via luteolysis (corpus luteum regression) at the end of the cycle and pregnancy PK: Highest potency, it works 2-5 days after cycle, more resistant to metabolism than dinoprost SE: Abortion, diarrhea, abdominal discomfort, bronchoconstriction, and increase in blood pressure. INDICATION: Used for estrous synchronization, – to induce parturition (sows, mares, cows with glucocorticoid) – for abortion – for treatment of pyometra They cause premature luteolysis, thus decreasing estrous cycle length and thereby hastening the onset of estrus CONTRAINDICATION: Pregnant animals

Answer 56

GROUP: Piperazines (1st gen antihistamine) MOA: They are inverse agonists. that are considered to have a "negative efficacy", so rather than simply blocking activity at a receptor they actively dampen its activity. PK: Well absorbed and quickly metabolized, crosses BBB. Given PO and IM (and IV during emergency) SE: Rapid IV injection can cause CNS depression, cardiac toxicity and appetite supressing INDICATION: Atopic dermatitis

Answer 57

GROUP: 1st gen antihistamines (ethanolamine) MOA: They are inverse agonists. that are considered to have a "negative efficacy", so rather than simply blocking activity at a receptor they actively dampen its activity. PK: Well absorbed and quickly metabolized, crosses BBB. Given PO. SE: Rapid IV injection can cause CNS depression, cardiac toxicity and appetite supressing INDICATION: Against vaccine allergy (give 30 mins prior)

Answer 58

GROUP: 1st gen antihistamines (ethanolamine) MOA: They are inverse agonists. that are considered to have a "negative efficacy", so rather than simply blocking activity at a receptor they actively dampen its activity. PK: Well absorbed and quickly metabolized, crosses BBB. Given PO. SE: Rapid IV injection can cause CNS depression, cardiac toxicity and appetite supressing INDICATION: Against vaccine allergy (give 30 mins prior)

Answer 59

GROUP: 2nd gen antihistamine MOA: They are inverse agonists. that are considered to have a "negative efficacy", so rather than simply blocking activity at a receptor they actively dampen its activity. PK: Do not cross BBB (ionised form in the blood), metabolized in liver. Given PO. SE: Safe drugs, can cause sedation (due to CNS depression), but they have low efficacy INDICATION: Allergic reactions. They are used in anaphylactic reactions in combination with adrenaline and glucocorticoids (antihistamines will not be enough)

Answer 60

GROUP: Leukotriene antagonist MOA: They block the cysteinyl leukotriene receptor which is responsible for the bronchoconstriction PK: Given PO INDICATION: Allergic bronchitis, RAO, and Feline asthma

Answer 61

GROUP: JAK- inhibitor MOA: It inhibits cytokines involved with pruritus in dogs that are dependent on the Janus kinase (JAK) enzyme. It inhibits preferentially the JAK1 enzyme activity. Of significance for atopic and allergic dermatitis treatment is that oclacitinib inhibits the IL-31 cytokine function and reduces IL-31 induced pruritus in dogs. It also may inhibit the function of other proinflammatory cytokines such as IL-2, IL-4, IL-6, and IL-13 that may be involved with allergy PK: Good oral absorption (89% bioavailability), half-life is approx 3-5 hours in dogs, metabolized in liver. SE: Rare but vomiting and diarrhea can occur INDICATION: Atopic dermatitis CONTRAINDICATION: Oncological patients

Answer 62

GROUP: Immunology product (NOT a drug) MOA: It is an IL-31 monoclonal antibody (MAB) and targets the IL-31 which is the primary cause of itching in atopic dermatitis. PK: Given SC and works approx. 4 weeks. SE: Rare, vomiting, diarrhea and sleepiness can occur INDICATION: Treat itchiness in dogs CONTRAINDICATION: Use in dog only, not other animals as it can cause anaphylactic reactions

Answer 63

GROUP: Anti-NGF MOA: NGF is a factor for the development of sensory and sympathetic neurons. In adults the main role is the modulation of nociceptive neuronal activity. It is a biosynthetic mAB produced in Chinese hamster ovary (CHO) cells PK: Given as injection, elimination half-life is 12 days SE: Rare, anaphylaxis, swelling at injection site INDICATION: Alleviation of osteoarthritis pain in dogs – species-specific!

Answer 64

GROUP: Salicylates (classical NSAID's) MOA: It suppresses the production of prostaglandins and thromboxanes is due to its irreversible inactivation of the cyclooxygenase (COX) 1 and 2 enzyme (unsafe). PK: Used short-term. Generally good oral bioavailability in monogastric animals, penetrates BBB, metabolized in liver, excretion in urine SE: Irritating the stomach (vomiting), delayed healing, ren-and hepatotoxicity (it is considered an unsafe drug as it inhibit COX 1 and 2) INDICATION: Platelet aggregation inhibition (in thrombosis), analgesic and antipyretic CONTRAINDICATION: Do not use in cats, and after surgery

Answer 65

GROUP: Propionic acids MOA: Inhibition of the COX-2 enzyme, which is the enzyme responsible for inflammation PK: Can be given with and without food (PO) and as injection, long action in cattle, high binding to albumin, cross the BBB. It has a very long wp for meat in cattle. SE: Infrequent idiosyncratic reactions, GI ulcertaion, kidney damage INDICATION: Against inflammation, pain and fever CONTRAINDICATION: Labradors and golden retrievers. Should not be given with other hepatotoxic drugs (e.g phenobarbital) DOSE: Dog: 4.4 mg/kg loading dose, 2.2 mg/kg maintenance dose Cat: IV, SC, 4 mg/kg once Cattle: IV, SC 1.4 mg/kg SID Horse: IV 0.7 mg/kg SID

Answer 66

GROUP: Anthranilic acid MOA: It is an antiendotoxin which stops endotoxins from being released into the body after death of bacteria PK: High Vd, short elimination half-life SE: Enhances bleeding (not good after surgery) INDICATION: Used as an endotoxin, spasmolytic agent, in thrombosis (platelet aggregation inhibition), mostly used horse and cattle) CONTRAINDICATION: Not use after surgery.

Answer 67

GROUP: Oxicam MOA: 2nd generation COX inhibitor. It inhibits the COX-2 inflammatory enzyme. PK: Can be given with or without food, high albumin binding, metabolized in liver, crosses BBB, and it can be given as an injection or PO. SE: GI ulceration, kidney damage and hepatoxicity INDICATION: Used as an antiendotoxin, can be used before and after parturition, to inhibit inflammation. Works good in cats (safe in all species)and in general it does not cause cartilage damage DOSE: Dog: SC, PO 0.2 mg/kg SID on first day, then 0.1 mg/kg SID Cat: SC, PO 0,1 mg/kg SID first day, then 0.05 mg/kg SID Cattle: IV, SC 0.5 mg/kg SID Swine: IM 0.4 mg/kg SID Horse: IV 0.6 mg/kg SID

Answer 68

GROUP: Pyrazoline MOA: Non-specific, COX-3 inhibitor. Mainly acts in the brain and because it has a very low activity on COX-1 and COX-2 PK: Very safe to use, good absorption, high albumin binding, metabolized in liver SE: Rare, no effect on stomach or kidney, but can cause excitation and salivation in cats INDICATION: Spasmolytic, antipyretic and analgesic effect CONTRAINDICATION: Cats

Answer 69

GROUP: Coxibs (3rd gen NSAID) MOA: Specific COX-2 inhibitor. COX-2 is the enxyme responsible for inflammation in the body (inhibit COX-2 100x more than COX-1) PK: Given PO SE: Rare (normally no GI ulceration or antiplatelet effects) INDICATION: Anti-inflammatory and antipyretic treatment in dogs and horses CONTRAINDICATION: Cats

Answer 70

GROUP: Coxibs MOA: Specific COX-2 inhibitor. COX-2 is the enxyme responsible for inflammation in the body (inhibit COX-2 100x more than COX-1) PK: Given as injection only, works good in cats, low Vd SE: Rare INDICATION: Used in cats (and dogs) as an analgesic and anti-inflammatory agent. In cats it is used in postoperative pain (after castration, ovariohysterectomy)

Answer 71

GROUP: Coxibs MOA: Specific COX-2 inhibitor. COX-2 is the enxyme responsible for inflammation in the body (inhibit COX-2 100x more than COX-1) PK: Long half-life in dogs, duration of action is 3-4 weeks. Higher bioavailability if given with food. It is given PO. SE: Rare (it is a safe drug) INDICATION: Analgesic and anti-inflammatory agent used in dogs (degenerative joint disease) CONTRAINDICATION: Cats

Answer 72

GROUP: Glucocorticoid MOA: Repressing COX-2 gene and enzyme expression, repressing the expression of cytokines that activate COX-2, limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase A2. PK: Good absoprtion, wide distribution, half-life is 1-2 days, metabolism in liver and excretion is mainly via urine, given in single large doses. SE: Inhibits functions like wound healing, immunosuppressive effect, catabolic effects (osteoporosis, muscle waste), effects on minerals (Na, K, Ca) INDICATION: Shock (adrenaline + crystalloid infusion), oedema, allergy, autoimmune diseases, ketosis, lymphoid tumors CONTRAINDICATION: Pre-existing renal impairment,infection and do not use with NSAIDs DOSE: Dogs: PO, IM 0.5-1 mg/kg (anti-inflammatory) PO 1-2 mg/kg BID (immunosuppression)

Answer 73

GROUP: Glucocrticoid MOA: Repressing COX-2 gene and enzyme expression Repressing the expression of cytokines that activate COX-2 Limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase 2. It's activity is enchanced by C6 methyl group PK: Good absoprtion, wide distribution, half-life is 1-2 days, metabolism in liver and excretion is mainly via urine, given in single large doses. SE: Inhibits functions like wound healing, immunosuppressive effect, catabolic effects (osteoporosis, muscle waste), effects on minerals (Na, K, Ca) INDICATION: Shock (adrenaline + crystalloid infusion), oedema, allergy, autoimmune diseases, ketosis, lymphoid tumors CONTRAINDICATION: Pre-existing renal impairment,infection and do not use with NSAIDs

Answer 74

GROUP: Glucocorticoids MOA: Repressing COX-2 gene and enzyme expression, repressing the expression of cytokines that activate COX-2, limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase 2. PK: Good absoprtion, wide distribution, long half-life (>2 days), metabolism in liver and excretion is mainly via urine. SE: Inhibits functions like wound healing, immunosuppressive effect, catabolic effects (osteoporosis, muscle waste), effects on minerals (Na, K, Ca) INDICATION: Shock (adrenaline + crystalloid infusion), oedema, allergy, autoimmune diseases, ketosis, lymphoid tumors, asthma, Addison's disease (+ fludrocortisone) CONTRAINDICATION: Pre-existing renal impairment,infection and do not use with NSAIDs DOSE: Dog: IM 0.1 mg/kg (anti-inflammatory) IV 0.3-0.5 mg/kg (immunosuppression) Cattle/swine/horse: IM 0.06 mg/kg

Answer 75

GROUP: Glucocorticoid MOA: Repressing COX-2 gene and enzyme expression, repressing the expression of cytokines that activate COX-2, limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase 2. PK: Good absoprtion, wide distribution, long half-life (>2 days), metabolism in liver and excretion is mainly via urine. SE: Inhibits functions like wound healing, immunosuppressive effect, catabolic effects (osteoporosis, muscle waste), effects on minerals (Na, K, Ca) INDICATION: Shock (adrenaline + crystalloid infusion), oedema, allergy, autoimmune diseases, ketosis, lymphoid tumors, asthma, Addison's disease (+ fludrocortisone) CONTRAINDICATION: Pre-existing renal impairment,infection and do not use with NSAIDs

Answer 76

GROUP: Synthetic glucocorticoid MOA: Repressing COX-2 gene and enzyme expression, repressing the expression of cytokines that activate COX-2, limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase 2 PK: Inhalational glucocorticoid, high potency. SE: No significant adverse effects INDICATION: Treatment of feline asthma (and horses too?)

Answer 77

GROUP: Synthetic glucocorticoid MOA: Repressing COX-2 gene and enzyme expression, repressing the expression of cytokines that activate COX-2, limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase 2 PK: Inhalational glucocorticoid, very potent SE: Rare, cough, difficulty, trouble swallowing, swollen gland in the neck INDICATION: Asthma and skin disease (applied topically)

Answer 78

GROUP: Synthetic glucocorticoid MOA: Repressing COX-2 gene and enzyme expression, repressing the expression of cytokines that activate COX-2, limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase 2. PK: Given orally, undergoes first-pass metabolism, 15x more potent than prednisolone SE: Inhibits functions like wound healing, immunosuppressive effect, catabolic effects (osteoporosis, muscle waste), effects on minerals (Na, K, Ca) INDICATION: Given to dogs and cats primarily for treatment of inflammatory bowel disease CONTRAINDICATION: Pre-existing renal impairment, infection and do not use with NSAIDs

Answer 79

GROUP: Glucocorticoid MOA: Repressing COX-2 gene and enzyme expression, repressing the expression of cytokines that activate COX-2, limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase A2. PK: Good absoprtion, wide distribution, half-life is 1-2 days, metabolism in liver and excretion is mainly via urine, given in single large doses. SE: Inhibits functions like wound healing, immunosuppressive effect, catabolic effects (osteoporosis, muscle waste), effects on minerals (Na, K, Ca) INDICATION: Shock (adrenaline + crystalloid infusion), oedema, allergy, autoimmune diseases, ketosis, lymphoid tumors CONTRAINDICATION: Pre-existing renal impairment,infection and do not use with NSAIDs DOSE: Dogs: PO, IM 0.5-1 mg/kg (anti-inflammatory) PO 1-2 mg/kg BID (immunosuppression)

Answer 80

GROUP: Glucocrticoid MOA: Repressing COX-2 gene and enzyme expression Repressing the expression of cytokines that activate COX-2 Limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase 2. It's activity is enchanced by C6 methyl group PK: Good absoprtion, wide distribution, half-life is 1-2 days, metabolism in liver and excretion is mainly via urine, given in single large doses. SE: Inhibits functions like wound healing, immunosuppressive effect, catabolic effects (osteoporosis, muscle waste), effects on minerals (Na, K, Ca) INDICATION: Shock (adrenaline + crystalloid infusion), oedema, allergy, autoimmune diseases, ketosis, lymphoid tumors CONTRAINDICATION: Pre-existing renal impairment,infection and do not use with NSAIDs

Answer 81

GROUP: Glucocorticoids MOA: Repressing COX-2 gene and enzyme expression, repressing the expression of cytokines that activate COX-2, limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase 2. PK: Good absoprtion, wide distribution, long half-life (>2 days), metabolism in liver and excretion is mainly via urine. SE: Inhibits functions like wound healing, immunosuppressive effect, catabolic effects (osteoporosis, muscle waste), effects on minerals (Na, K, Ca) INDICATION: Shock (adrenaline + crystalloid infusion), oedema, allergy, autoimmune diseases, ketosis, lymphoid tumors, asthma, Addison's disease (+ fludrocortisone) CONTRAINDICATION: Pre-existing renal impairment,infection and do not use with NSAIDs DOSE: Dog: IM 0.1 mg/kg (anti-inflammatory) IV 0.3-0.5 mg/kg (immunosuppression) Cattle/swine/horse: IM 0.06 mg/kg

Answer 82

GROUP: Glucocorticoid MOA: Repressing COX-2 gene and enzyme expression, repressing the expression of cytokines that activate COX-2, limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase 2. PK: Good absoprtion, wide distribution, long half-life (>2 days), metabolism in liver and excretion is mainly via urine. SE: Inhibits functions like wound healing, immunosuppressive effect, catabolic effects (osteoporosis, muscle waste), effects on minerals (Na, K, Ca) INDICATION: Shock (adrenaline + crystalloid infusion), oedema, allergy, autoimmune diseases, ketosis, lymphoid tumors, asthma, Addison's disease (+ fludrocortisone) CONTRAINDICATION: Pre-existing renal impairment,infection and do not use with NSAIDs

Answer 83

GROUP: Synthetic glucocorticoid MOA: Repressing COX-2 gene and enzyme expression, repressing the expression of cytokines that activate COX-2, limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase 2 PK: Inhalational glucocorticoid, high potency. SE: No significant adverse effects INDICATION: Treatment of feline asthma (and horses too?)

Answer 84

GROUP: Synthetic glucocorticoid MOA: Repressing COX-2 gene and enzyme expression, repressing the expression of cytokines that activate COX-2, limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase 2 PK: Inhalational glucocorticoid, very potent SE: Rare, cough, difficulty, trouble swallowing, swollen gland in the neck INDICATION: Asthma and skin disease (applied topically)

Answer 85

GROUP: Synthetic glucocorticoid MOA: Repressing COX-2 gene and enzyme expression, repressing the expression of cytokines that activate COX-2, limiting the available pool of COX-2 substrate (arachidonic acid) by indirectly blocking phospholipase 2. PK: Given orally, undergoes first-pass metabolism, 15x more potent than prednisolone SE: Inhibits functions like wound healing, immunosuppressive effect, catabolic effects (osteoporosis, muscle waste), effects on minerals (Na, K, Ca) INDICATION: Given to dogs and cats primarily for treatment of inflammatory bowel disease CONTRAINDICATION: Pre-existing renal impairment, infection and do not use with NSAIDs

Answer 86

GROUP: Purine analogue MOA: Will interfere with transcription and reduce proliferation of the cells. PK: Slow release (2 weeks), given IV and PO SE: Cause DNA damage, vomiting, diahrrea, anaemia, lymphocytopenia and thrombocytopenia INDICATION: Immune-mediated hemolytic anaemia, cancer, inflammatory bowel disease, lupus CONTRAINDICATION: Pregnant and breeding animals (it damages the gonads)

Answer 87

GROUP: Purine analogues MOA: It will inhibit inosine monophosphate dehydrogenase which is necessary to have purine. The consequence of this is that there will be a reduction in T and B cell proliferation. PK: Faster onset of action, usually taken in combo with cyclosporine, given orally SE: Not as common as in azathioprine, but liver toxicity, vomero suppression, effect on bone marrow, and acute pancreatitis can occur INDICATION: Best choice of drug in the case of autoimmune glomerulonephritis, used in cats too.

Answer 88

GROUP: Calcineurin inhibitors MOA: Works primarily to interfere with T-lymphocyte activation and proliferation by inhibiting the production of IL-2. PK: Given orally, low bioavailability (so it is given as microemulsion), local application is possible and it is given in a higher dose to cats. SE: Vomiting and emesis INDICATION: Autoimmune diseases: lupus, pemphigus, KCS (applied locally), AIHA (autoimmune mediated hemolytic anaemia); atopic dermatitis and IBD (inflammatory bowel disease) DOSE: Dog: PO 5 mg/kg SID Cat: PO 7 mg/kg SID

Answer 89

GROUP: Narrow spectrum penicillin STRUCTURE: Beta lactam ring (determines PK) and thiazolidine ring (determining antimicrobial spectrum) MOA: Inhibits peptidoglycan cell wall synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-dependent bactericidal RESISTANCE: - Ab ovo: Mycoplasma, Pseudomonas aeruginosa, Brucella, Chlamydia - Beta lactamase production: Staphylococcus and all gram- bacteria - PBP Gene Mutation: S. Aureus and S. Intermedius ANTIMICROBIAL SPECTRUM: Many Gram positive bacteria: - Bacillus, Clostridium, Streptococcus, Erysipelothrix, Corynebacterium, Arcanobacterium pyogenes, Actinomyces, ListeriaFastidious Gram negative bacteria: - Pasteurella, Haemophilus, Actinobacillus, Mannheimia, BibersteiniaSome Spirochaetes: - Leptospira, Borrelia PK: Duration of action 24 hours; IM/SC only; hydrophilic; badmoderate distribution; minimal metabolism; d not cross BBB, excreted via the kidney in the urine SE: Allergy, Dysbacteriosis in Eq/Rabbits/Herbivore Rodents, Ataxia, Movement Disorders, Tremors INDICATION: Respiratory Tract Infections, Swine Erysipelas, Anthrax, Tetanus, Necrotic Enteritis, Metritis, Streptococcosis, Strangles, Skin Diseases, Pharyngitis ( Often combined with Benzathine Benzylpenicillin & Dihydrostreptomycin) CONTRAINDICATION: Do not combine with bacteriostatic agents

Answer 90

GROUP: Narrow spectrum penicillin STRUCTURE: Beta lactam ring (determines PK) and thiazolidine ring (determining antimicrobial spectrum) MOA: Inhibits peptidoglycan cell wall synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-dependent bactericidal RESISTANCE: - Ab ovo: Mycoplasma, Pseudomonas aeruginosa, Brucella, Chlamydia - Beta lactamase production: Staphylococcus and all gram- bacteria - PBP Gene Mutation: S. Aureus and S. Intermedius ANTIMICROBIAL SPECTRUM: Many Gram positive bacteria: - Bacillus, Clostridium, Streptococcus, Erysipelothrix, Corynebacterium, Arcanobacterium pyogenes, Actinomyces, ListeriaFastidious Gram negative bacteria: - Pasteurella, Haemophilus, Actinobacillus, Mannheimia, BibersteiniaSome Spirochaetes: - Leptospira, Borrelia PK: Duration of action 72- 96 hours; IM/SC only; hydrophilic; badmoderate distribution; minimal metabolism; excreted via the kidney SE: Allergy, Dysbacteriosis in Eq/Rabbits/Herbivore Rodents INDICATION: Respiratory Tract Infections, Swine Erysipelas, Anthrax, Tetanus, Necrotic Enteritis, Metritis, Streptococcosis, Strangles, Skin Diseases, Pharyngitis ( Often combined with Benzathine Benzylpenicillin & Dihydrostreptomycin) CONTRAINDICATION: Do not combine with bacteriostatic agents

Answer 91

GROUP: Narrow spectrum penicillin STRUCTURE: Beta lactam ring (determines PK) and thiazolidine ring (determining antimicrobial spectrum) MOA: Inhibits peptidoglycan cell wall synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-dependent bactericidal RESISTANCE: - Ab ovo: Mycoplasma, Pseudomonas aeruginosa, Brucella, Chlamydia - Beta lactamase production: Staphylococcus and all gram- bacteria - PBP Gene Mutation: S. Aureus and S. Intermedius ANTIMICROBIAL SPECTRUM: Many Gram positive bacteria: - Bacillus, Clostridium, Streptococcus, Erysipelothrix, Corynebacterium, Arcanobacterium pyogenes, Actinomyces, ListeriaFastidious Gram negative bacteria: - Pasteurella, Haemophilus, Actinobacillus, Mannheimia, BibersteiniaSome Spirochaetes: - Leptospira, Borrelia PK: Given PO to poultry in drinking water; half life of 2-3 hours; hydrophilic; bad- moderate distribution; minimal metabolism; excreted via the kidney in the urine SE: Allergy, Dysbacteriosis in Eq/Rabbits/Herbivore Rodents INDICATION: Clostridium perfringensnecrotic enteritis in poultry CONTRAINDICATION: Do not combine with bacteriostatic agents

Answer 92

GROUP: Penicillinase/ lactamase stable penicillin STRUCTURE: Beta lactam ring (determines PK) and thiazolidine ring (determining antimicrobial spectrum) MOA: Inhibits peptidoglycan cell wall synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-dependent bactericidal RESISTANCE: - Ab ovo: Mycoplasma, Pseudomonas aeruginosa, Brucella, Chlamydia - Beta lactamase production: Staphylococcus and all gram- bacteria - PBP Gene Mutation: S. Aureus and S. Intermedius ANTIMICROBIAL SPECTRUM: Many Gram positive bacteria: - Bacillus, Clostridium, Streptococcus, Staphylococcus, Erysipelothrix, Corynebacterium, Arcanobacterium pyogenes PK: Unreliable oral absorption and irritant; intramammary infusion most common; more lipophilic than oxacillin so better distribution SE: Irritant INDICATION: Mastitis in cattle and dermatitis in cat and dog CONTRAINDICATION: Do not combine with bacteriostatic NOTE: Acid resistant; Chlorinated

Answer 93

GROUP: Broad spectrum penicillin STRUCTURE: Beta lactam ring (determines PK) and thiazolidine ring (determining antimicrobial spectrum) MOA: Inhibits peptidoglycan cell wall synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-dependent bactericidal RESISTANCE: - Ab ovo: Mycoplasma, Pseudomonas aeruginosa, Brucella, Chlamydia - Beta lactamase production: Staphylococcus and all gram- bacteria - PBP Gene Mutation: S. Aureus and S. Intermedius ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus, Enterococcus, Erysipelothrix, Corynebacterium, Arcanobacterium pyogenes, Actinomyces, Listeria Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, BibersteiniaEnterobacteriaceae: E. coli, Salmonella, KlebsiellaAnaerobics: Bacteroides, Fusobacterium, ProteusSome Spirochaetes: Leptospira, Borrelia PK: Good-excellent oral absorption (100% in Hu, 80% in Ca/Fe, 60% in poultry, 30% in Su, 1% in Eq); not affected by feed; sensitive to Beta Lactamase so must be combined with lactamase inhibitors for Staphylococcus and E. coli infections; SE: Dysbacteriosis in Eq/Rabbits/Herbivore Rodents INDICATION: Respiratory Tract Infections, Swine Erysipelas, Anthrax, Tetanus, Necrotic Enteritis, Mastitis, , Metritis, Streptococcosis, Strangles, Lyme Disease, Pharyngitis, UTIs; Combination with Lactamase Inhibitors: Soft Tissue Infections, Osteomyelitis, Oral Cavity & Bite Wounds, Dermatitis CONTRAINDICATION: Do not combine with bacteriostatic agents, also prohibited to use in horse NOTE: Combined with clavulanic acid

Answer 94

GROUP: Broad spectrum penicillin STRUCTURE: Beta lactam ring (determines PK) and thiazolidine ring (determining antimicrobial spectrum) MOA: Inhibits peptidoglycan cell wall synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-dependent bactericidal RESISTANCE: - Ab ovo: Mycoplasma, Pseudomonas aeruginosa, Brucella, Chlamydia - Beta lactamase production: Staphylococcus and all gram- bacteria - PBP Gene Mutation: S. Aureus and S. Intermedius ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus, Enterococcus, Erysipelothrix, Corynebacterium, Arcanobacterium pyogenes, Actinomyces, ListeriaFastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, BibersteiniaEnterobacteriaceae: E. coli, Salmonella, KlebsiellaAnaerobics: Bacteroides, Fusobacterium, Proteus Some Spirochaetes: Leptospira, Borrelia PK: Weak-moderate oral absorption; feed reduces absorption; sensitive to Beta Lactamase so must be combined with lactamase inhibitors for Staphylococcus and E. coli infections SE: Dysbacteriosis in Eq/Rabbits/Herbivore Rodents INDICATION: Respiratory Tract Infections, Swine Erysipelas, Anthrax, Tetanus, Necrotic Enteritis, Mastitis, , Metritis, Streptococcosis,Strangles, Lyme Disease, Pharyngitis, UTIs; Combination with Lactamase Inhibitors: Soft Tissue Infections, Osteomyelitis, Oral Cavity & Bite Wounds, Dermatitis CONTRAINDICATION: Do not combine with bacteriostatic agents, also prohibited to use in horse NOTE: Combined with sulbactam

Answer 95

GROUP: Penicillin against Pseudomonas spp. STRUCTURE: Beta lactam ring (determines PK) and thiazolidine ring (determining antimicrobial spectrum) MOA: Inhibits peptidoglycan cell wall synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-dependent bactericidal RESISTANCE: - Ab ovo: Mycoplasma, Pseudomonas aeruginosa, Brucella, Chlamydia - Beta lactamase production: Staphylococcus and all gram- bacteria - PBP Gene Mutation: S. Aureus and S. Intermedius ANTIMICROBIAL SPECTRUM: Pseudomnas spp: P. Aeruginosa Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus, Enterococcus, Erysipelothrix, Corynebacterium, Arcanobacterium pyogenes, Actinomyces, Listeria Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Bibersteinia Enterobacteriaceae: E. coli, Salmonella, Klebsiella Anaerobics: Bacteroides, Fusobacterium, ProteusSome Spirochaetes: Leptospira, Borrelia PK: IV/IM only INDICATION: Life-threatening anaerobic infections, intestinal perforation, peritonitis, Pseudomonas infections CONTRAINDICATION: Do not combine with bacteriostatic agents NOTE: Combined with tazobactam

Answer 96

GROUP: Beta-lactamase inhibitor MOA: It binds to the enzyme and inactivates the enzyme i.e. it sacrifices itself to the enzyme and keeps amoxicillin alive ANTIMICROBIAL SPECTRUM: It has no antibacterial action on its own, but in combo (e.g w/ amoxicillin or ticarcillin): Gram+: Staphylococcus, Gram-: E. coli - except UTI E. coli, Bordetella spp, Pseudomonas spp PK: very similar to amoxicillin - it has similar absorption, distribution, and excretion. SE: Rare, but vomiting and diarrhoea can happen in some instances. It is a little more irritant to the GI tract than amoxicillin on its own.

Answer 97

GROUP: 1st gen cephalosporin MOA: Inhibits Peptidoglycan Cell Wall Synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-Dependent Bactericidal ; causes bacteriolysis during division RESISTANCE: Ab ovo: Mycoplasma (no cell wall),Pseudomonas aeruginosa (no porins), Brucella, Chlamydia, Mycobacteria (thick acid fast cell walls) PBP Gene Mutation: Some Escherichia coli strains are resistant to cephalosporins by this mean ANTIMICROBIAL SPECTRUM: Mostly used against Gram positive bacteria - Bacillus, Clostridium, Staphylococcus, Streptococcus, Erysipelothrix, Corynebacterium, Arcanobacterium pyogenes, Actinomyces, Listeria PK: IM/SC; mostly eliminated by the kidneys in an active form; 15-20 mg/kg BID SE: Allergy, Dysbacteriosis in Eq/Rabbits/Herbivore Rodents, Tissue Irritation, Mild Nephrotoxicity, Eosinophilia, Neutropenia, Thrombocytopenia, Fever, Diarrhea, Electrolyte disturbances INDICATION: Mastitis, Dermatitis, Soft tissue infections, Respiratory infections, UTIs, Meningitis, Encephalitis, Preoperative and Postoperative Prophylaxis CONTRAINDICATION: Much more resistant to Beta Lactamase and thus rarely combined with Beta Lactamase Inhibitors; never combine with bacteriostatic agents

Answer 98

GROUP: 1st gen cefalosporin MOA: Inhibits Peptidoglycan Cell Wall Synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-Dependent Bactericidal ; causes bacteriolysis during division RESISTANCE: Ab ovo: Mycoplasma (no cell wall),Pseudomonas aeruginosa (no porins), Brucella, Chlamydia, Mycobacteria (thick acid fast cell walls) PBP Gene Mutation: Some Escherichia coli strains are resistant to cephalosporins by this mean ANTIMICROBIAL SPECTRUM: Mostly used against Gram positive bacteria - Bacillus, Clostridium, Staphylococcus, Streptococcus, Erysipelothrix, Corynebacterium, Arcanobacterium pyogenes, Actinomyces, Listeria PK: IM/SC; mostly eliminated by the kidneys in an active form; 15-20 mg/kg BID SE: Allergy, Dysbacteriosis in Eq/Rabbits/Herbivore Rodents, Tissue Irritation, Mild Nephrotoxicity, Eosinophilia, Neutropenia, Thrombocytopenia, Fever, Diarrhea, Electrolyte disturbances INDICATION: Mastitis, Dermatitis, Soft tissue infections, Respiratory infections, UTIs, Meningitis, Encephalitis, Preoperative and Postoperative Prophylaxis CONTRAINDICATION: Much more resistant to Beta Lactamase and thus rarely combined with Beta Lactamase Inhibitors; never combine with bacteriostatic agents

Answer 99

GROUP: 1st gen cefalosporin MOA: Inhibits Peptidoglycan Cell Wall Synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-Dependent Bactericidal ; causes bacteriolysis during division RESISTANCE: Ab ovo: Mycoplasma (no cell wall),Pseudomonas aeruginosa (no porins), Brucella, Chlamydia, Mycobacteria (thick acid fast cell walls) PBP Gene Mutation: Some Escherichia coli strains are resistant to cephalosporins by this mean ANTIMICROBIAL SPECTRUM: Mostly used against Gram positive bacteria - Bacillus, Clostridium, Staphylococcus, Streptococcus, Erysipelothrix, Corynebacterium, Arcanobacterium pyogenes, Actinomyces, Listeria PK: PO; mostly eliminated by the kidneys in an active form; 15-20 mg/kg BID SE: Allergy, Dysbacteriosis in Eq/Rabbits/Herbivore Rodents, Tissue Irritation, Mild Nephrotoxicity, Eosinophilia, Neutropenia, Thrombocytopenia, Fever, Diarrhea, Electrolyte disturbances INDICATION: Mastitis, Dermatitis, Soft tissue infections, Respiratory infections, UTIs, Meningitis, Encephalitis, Preoperative and Postoperative Prophylaxis CONTRAINDICATION: Much more resistant to Beta Lactamase and thus rarely combined with Beta Lactamase Inhibitors; never combine with bacteriostatic agents

Answer 100

GROUP: 2nd gen cefalosporin MOA: Inhibits Peptidoglycan Cell Wall Synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-Dependent Bactericidal ; causes bacteriolysis during division RESISTANCE: Ab ovo: Mycoplasma (no cell wall),Pseudomonas aeruginosa (no porins), Brucella, Chlamydia, Mycobacteria (thick acid fast cell walls) PBP Gene Mutation: Some Escherichia coli strains are resistant to cephalosporins by this mean ANTIMICROBIAL SPECTRUM: Gram positive bacteria - Bacillus, Clostridium, Staphylococcus, Streptococcus, Erysipelothrix, Corynebacterium, Arcanobacterium pyogenes, Actinomyces, Listeria Fastidious Gram negative bacteria - Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Bibersteinia Enterobacteriaceae - E. coli, Salmonella, Klebsiella Anaerobics - Bacteroides, Fusobacterium, Proteus Some Spirochaetes - Leptospira, Borrelia PK: IM/SC; mostly eliminated by the kidneys in an active form; 15-20 mg/kg BID SE: Allergy, Dysbacteriosis in Eq/Rabbits/Herbivore Rodents, Tissue Irritation, Mild Nephrotoxicity, Eosinophilia, Neutropenia, Thrombocytopenia, Fever, Diarrhea, Electrolyte disturbances INDICATION: Mastitis, Dermatitis, Soft tissue infections, Respiratory infections, UTIs, Meningitis, Encephalitis, Preoperative and Postoperative Prophylaxis CONTRAINDICATION: Much more resistant to Beta Lactamase and thus rarely combined with Beta Lactamase Inhibitors; never combine with bacteriostatic agents

Answer 101

GROUP: 3rd gen cefalosporin MOA: Inhibits Peptidoglycan Cell Wall Synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-Dependent Bactericidal ; causes bacteriolysis during division RESISTANCE: Ab ovo: Mycoplasma (no cell wall),Pseudomonas aeruginosa (no porins), Brucella, Chlamydia, Mycobacteria (thick acid fast cell walls) PBP Gene Mutation: Some Escherichia coli strains are resistant to cephalosporins by this mean ANTIMICROBIAL SPECTRUM: Fastidious Gram negative bacteria - Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Bibersteinia Bordetella bronchiseptica & Pseudomonas aeruginosa Enterobacteriaceae - E. coli, Salmonella, Klebsiella Anaerobics - Bacteroides, Fusobacterium, Proteus Some Spirochaetes - Leptospira, Borrelia PK: IM/SC/intramammary/IV; high level of metabolism in the liver and elimination in the bile; 15-20 mg/kg BID SE: Allergy, Dysbacteriosis in Eq/Rabbits/Herbivore Rodents, Tissue Irritation, Mild Nephrotoxicity, Eosinophilia, Neutropenia, Thrombocytopenia, Fever, Diarrhea, Electrolyte disturbances INDICATION: Mastitis (very common!!), Dermatitis, Soft tissue infections, Respiratory infections, UTIs, Meningitis, Encephalitis, Preoperative and Postoperative Prophylaxis CONTRAINDICATION: Much more resistant to Beta Lactamase and thus rarely combined with Beta Lactamase Inhibitors; never combine with bacteriostatic agents

Answer 102

GROUP: 3rd gen cephalosporin MOA: Inhibits Peptidoglycan Cell Wall Synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-Dependent Bactericidal ; causes bacteriolysis during division RESISTANCE: Ab ovo: Mycoplasma (no cell wall),Pseudomonas aeruginosa (no porins), Brucella, Chlamydia, Mycobacteria (thick acid fast cell walls) PBP Gene Mutation: Some Escherichia coli strains are resistant to cephalosporins by this mean ANTIMICROBIAL SPECTRUM: Fastidious Gram negative bacteria - Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Bibersteinia Bordetella bronchiseptica & Pseudomonas aeruginosa Enterobacteriaceae - E. coli, Salmonella, Klebsiella Anaerobics - Bacteroides, Fusobacterium, Proteus Some Spirochaetes - Leptospira, Borrelia PK: IM 1-2 mg/kg; mostly eliminated by the kidneys in an active form (desfuroyl ceftiofur); Ceftiofur Na is short-acting and given BID; Ceftiofur hydrochloride is medium-acting and given SID; Ceftiofur crystalline free acid form (CCFA) is given as one injection every three days SE: Allergy, Dysbacteriosis in Eq/Rabbits/Herbivore Rodents, Tissue Irritation, Mild Nephrotoxicity, Eosinophilia, Neutropenia, Thrombocytopenia, Fever, Diarrhea, Electrolyte disturbances INDICATION: Mastitis, Dermatitis, Soft tissue infections, Respiratory infections, UTIs, Meningitis, Encephalitis, Preoperative and Postoperative Prophylaxis (almost exclusively used for GI tract and respiratort tract in large animals) CONTRAINDICATION: Much more resistant to Beta Lactamase and thus rarely combined with Beta Lactamase Inhibitors; never combine with bacteriostatic agents

Answer 103

GROUP: 3rd gen cefalosporin MOA: Inhibits Peptidoglycan Cell Wall Synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-Dependent Bactericidal ; causes bacteriolysis during division RESISTANCE: Ab ovo: Mycoplasma (no cell wall),Pseudomonas aeruginosa (no porins), Brucella, Chlamydia, Mycobacteria (thick acid fast cell walls) PBP Gene Mutation: Some Escherichia coli strains are resistant to cephalosporins by this mean ANTIMICROBIAL SPECTRUM: Fastidious Gram negative bacteria - Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Bibersteinia Bordetella bronchiseptica & Pseudomonas aeruginosa Enterobacteriaceae - E. coli, Salmonella, Klebsiella Anaerobics - Bacteroides, Fusobacterium, Proteus Some Spirochaetes - Leptospira, Borrelia PK: SC 8 mg/kg; mostly eliminated by the kidneys in active form; half life of 5 days in Ca (7 days in Fe); 2 week action with PAE SE: Allergy, Dysbacteriosis in Eq/Rabbits/Herbivore Rodents, Tissue Irritation, Mild Nephrotoxicity, Eosinophilia, Neutropenia, Thrombocytopenia, Fever, Diarrhea, Electrolyte disturbances INDICATION: Mastitis, Dermatitis, Soft tissue infections, Respiratory infections, UTIs, Meningitis, Encephalitis, Preoperative and Postoperative Prophylaxis (Used almost exclusively for dermatitis and oral cavity infections in small animals) CONTRAINDICATION: Much more resistant to Beta Lactamase and thus rarely combined with Beta Lactamase Inhibitors; never combine with bacteriostatic agents

Answer 104

GROUP: 4th gen cefalosporin MOA: Inhibits Peptidoglycan Cell Wall Synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-Dependent Bactericidal ; causes bacteriolysis during division RESISTANCE: Ab ovo: Mycoplasma (no cell wall),Pseudomonas aeruginosa (no porins), Brucella, Chlamydia, Mycobacteria (thick acid fast cell walls) PBP Gene Mutation: Some Escherichia coli strains are resistant to cephalosporins by this mean ANTIMICROBIAL SPECTRUM: Most Gram positive bacteria - Bacillus, Clostridium, Staphylococcus, Streptococcus, Erysipelothrix, Corynebacterium, Arcanobacterium pyogenes, Actinomyces, Listeria Fastidious Gram negative bacteria - Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Bibersteinia, Bordetella bronchiseptica & Pseudomonas aeruginosa Enterobacteriaceae - E. coli, Salmonella, Klebsiella Anaerobics - Bacteroides, Fusobacterium, Proteus Some Spirochaetes - Leptospira, Borrelia PK: IM 1-2 mg/kg SID SE: Allergy, Dysbacteriosis in Eq/Rabbits/Herbivore Rodents, Tissue Irritation, Mild Nephrotoxicity, Eosinophilia, Neutropenia, Thrombocytopenia, Fever, Diarrhea, Electrolyte disturbances; not to be administered to animals with a body weight less than 1.25 kg INDICATION: Bovine Respiratory Disease caused by Mannheimia haemolytica and Pasteurella multocida; acute E. coli mastitis, dermatitis, infectious ulbar necrosis, and interdigital necrobacillosis; in calves, E. coli septicaemia; in pigs, respiratory disease caused by P. multocida, Haemophilus parasuis, Actinobacillus pleuropneumoniae, and Streptococcus suis; mastitis-metritis-agalacti syndrome involved with E. coli, Staphylococcus, Streptococcus, etc

Answer 105

GROUP: Carbapenems STRUCTURE: Beta lactam ring and carbocyclic ring MOA: Inhibits Peptidoglycan Cell Wall Synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-Dependent Bactericidal RESISTANCE: Klebsiella pneumoniae has resistant strains and these drugs are not highly active against MRSA or enterococcal infections ANTIMICROBIAL SPECTRUM: Active against almost all known pathogenic bacteria PK: IM/IV SE: Allergy, Dysbacteriosis and Seizures INDICATION: Last resort antibiotics for multi-drug resistant strains and nosocomial respiratory infections CONTRAINDICATIONS/NOTES: Combination therapy, typically with an aminoglycoside, is recommended for Pseudomonas infections to avoid resistance development during treatment; never combine with valproic acid

Answer 106

GROUP: Monobactams STRUCTURE: Unfused bactam ring MOA: Inhibits Peptidoglycan Cell Wall Synthesis by inhibition of transpeptidase and carboxypeptidase enzymes MODA: Time-Dependent Bactericidal RESISTANCE: Ab ovo: Gram positive bacteria are resistant ANTIMICROBIAL SPECTRUM: Aerobic Gram negative bacteri: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Bibersteinia, E. coli, Salmonella, Klebsiella PK: IM/IV SE: Allergy and acute hepatitis INDICATIONS: Primary UTIs; Campylobacter, Bordetella bronchiseptica, Leptospira, Borrelia, Pseudomonas aeruginosa, Brachyspira hyodysenteriae infections

Answer 107

GROUP: Aminoglycoside STRUCTURE: Aminated sugar derivative MOA: Inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Concentration- Dependent Bactericidal RESISTANCE: Ab ovo: Shown by anaerobic bacteria and Streptococci. Plasmids: E. coli can develop resistance via plasmids. Degrading Enzymes in the periplasmic space. Altering Enzymes in the periplasmic space Reduced Permeability of the Cell Wall. One way cross resistance develops so if one aminoglycoside is ineffective you move to a stronger drug. ANTIMICROBIAL SPECTRUM: Predominantly Aerobic Bacteria, Staphylococcus, Mycobacteria Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Bibersteinia, Bordetella bronchiseptica, Pseudomonas aeruginosa, Enterobacteriaceae: E. coli, Salmonella, Klebsiella Leptospira: (some Proteus species) PK: Absorption is poor per os, hence PO usage is only for GI infections; IM/SC/parenteral use for other indications includes intramammary, intrauterine and intraabscess; topical application can be toxic, especially in Fe where it cannot be used; poor crossing of BBB and accumulates in kidney, excretion is in its active form hence these drugs are good for UTIs; SE: Nephrotoxic and ototoxic due to binding to phosphatidyl inositol in tubular cell membranes in the kidney. Drugs inhibit acetylcholine release and can cause neuromuscular blockade INDICATION: Respiratory infections, GI infections, UTIs, Mastitis, Dermatitis, Septicaemia CONTRAINDICATION: Never combine with cephalosporins; severe hepatotoxicity results; synergistic with lincomycin; never combine with tetracyclines NOTES: Most commonly combined with procaine or benzathine penicillin to include action against Streptococci; Used to treat microbacterial infections

Answer 108

GROUP: Aminoglycoside STRUCTURE: Aminated sugar derivative MOA: Inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Concentration- Dependent Bactericidal RESISTANCE: Ab ovo: Shown by anaerobic bacteria and Streptococci. Plasmids: E. coli can develop resistance via plasmids. Degrading Enzymes in the periplasmic space. Altering Enzymes in the periplasmic space Reduced Permeability of the Cell Wall. One way cross resistance develops so if one aminoglycoside is ineffective you move to a stronger drug. ANTIMICROBIAL SPECTRUM: Predominantly Aerobic Bacteria, Staphylococcus, Mycobacteria Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Bibersteinia, Bordetella bronchiseptica, Pseudomonas aeruginosa, Enterobacteriaceae: E. coli, Salmonella, Klebsiella Leptospira: (some Proteus species) PK: Absorption is poor per os, hence PO usage is only for GI infections; IM/SC/parenteral use for other indications includes intramammary, intrauterine and intraabscess; topical application can be toxic, especially in Fe where it cannot be used; poor crossing of BBB and accumulates in kidney, excretion is in its active form hence these drugs are good for UTIs; SE: Nephrotoxic and ototoxic due to binding to phosphatidyl inositol in tubular cell membranes in the kidney. Drugs inhibit acetylcholine release and can cause neuromuscular blockade INDICATION: Respiratory infections, GI infections, UTIs, Mastitis, Dermatitis, Septicaemia CONTRAINDICATION: Never combine with cephalosporins; severe hepatotoxicity results; synergistic with lincomycin; neverc ombine with tetracyclines NOTES: Very toxic (LD50=200 mg/kg) but not absorbed PO so can be used effectively for GI tract infections and mastitis treatment

Answer 109

GROUP: Aminoglycoside STRUCTURE: Aminated sugar derivative MOA: Inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Concentration- Dependent Bactericidal RESISTANCE: Ab ovo: Shown by anaerobic bacteria and Streptococci. Plasmids: E. coli can develop resistance via plasmids. Degrading Enzymes in the periplasmic space. Altering Enzymes in the periplasmic space Reduced Permeability of the Cell Wall. One way cross resistance develops so if one aminoglycoside is ineffective you move to a stronger drug. ANTIMICROBIAL SPECTRUM: Predominantly Aerobic Bacteria, Staphylococcus, Mycobacteria Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Bibersteinia, Bordetella bronchiseptica, Pseudomonas aeruginosa, Enterobacteriaceae: E. coli, Salmonella, Klebsiella Leptospira: (some Proteus species) PK: Absorption is poor per os, hence PO usage is only for GI infections; IM/SC/parenteral use for other indications includes intramammary, intrauterine and intraabscess; topical application can be toxic, especially in Fe where it cannot be used; poor crossing of BBB and accumulates in kidney, excretion is in its active form hence these drugs are good for UTIs; SE: Nephrotoxic and ototoxic due to binding to phosphatidyl inositol in tubular cell membranes in the kidney. Drugs inhibit acetylcholine release and can cause neuromuscular blockade INDICATION: Respiratory infections, GI infections, UTIs, Mastitis, Dermatitis, Septicaemia CONTRAINDICATION: Never combine with cephalosporins; severe hepatotoxicity results; synergistic with lincomycin; never combine with tetracyclines NOTES: Used alone for the treatment of mastitis but can be used as a combination with amoxicillin and clavulanic acid in life-threatening infections

Answer 110

GROUP: Aminoglycoside STRUCTURE: Aminated sugar derivative MOA: Inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Concentration- Dependent Bactericidal RESISTANCE: Ab ovo: Shown by anaerobic bacteria and Streptococci. Plasmids: E. coli can develop resistance via plasmids. Degrading Enzymes in the periplasmic space. Altering Enzymes in the periplasmic space Reduced Permeability of the Cell Wall. One way cross resistance develops so if one aminoglycoside is ineffective you move to a stronger drug. ANTIMICROBIAL SPECTRUM: Predominantly Aerobic Bacteria, Staphylococcus, Mycobacteria Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Bibersteinia, Bordetella bronchiseptica, Pseudomonas aeruginosa, Enterobacteriaceae: E. coli, Salmonella, Klebsiella Leptospira: (some Proteus species) PK: Absorption is poor per os, hence PO usage is only for GI infections; IM/SC/parenteral use for other indications includes intramammary, intrauterine and intraabscess; topical application can be toxic, especially in Fe where it cannot be used; poor crossing of BBB and accumulates in kidney, excretion is in its active form hence these drugs are good for UTIs; SE: Nephrotoxic and ototoxic due to binding to phosphatidyl inositol in tubular cell membranes in the kidney. Drugs inhibit acetylcholine release and can cause neuromuscular blockade INDICATION: Respiratory infections, GI infections, UTIs, Mastitis, Dermatitis, Septicaemia CONTRAINDICATION: Never combine with cephalosporins; severe hepatotoxicity results; synergistic with lincomycin; never combine with tetracyclines NOTES: Most active in the group, toxic with strong hearing and vestibular side effects; Frequently used in pseudomonas infections

Answer 111

GROUP: Aminoglycoside STRUCTURE: Aminated sugar derivative MOA: Inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Concentration- Dependent Bactericidal RESISTANCE: Ab ovo: Shown by anaerobic bacteria andStreptococci. Plasmids: E. coli can develop resistance via plasmids. Degrading Enzymes in the periplasmic space. Altering Enzymes in the periplasmic space. Reduced Permeability of the Cell Wall. One way cross resistance develops so if one aminoglycoside is ineffective you move to a stronger drug. ANTIMICROBIAL SPECTRUM: Predominantly Aerobic Bacteria, Staphylococcus, Mycobacteria Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Bibersteinia, Bordetella bronchiseptica, Pseudomonas aeruginosa, Enterobacteriaceae: E. coli, Salmonella, Klebsiella Leptospira: (some Proteus species) PK: Absorption is poor per os, hence PO usage is only for GI infections; IM/SC/parenteral use for other indications includes intramammary, intrauterine and intraabscess; topical application can be toxic, especially in Fe where it cannot be used; poor crossing of BBB and accumulates in kidney, excretion is in its active form hence these drugs are good for UTIs; SE: Nephrotoxic and ototoxic due to binding to phosphatidyl inositol in tubular cell membranes in the kidney. Drugs inhibit acetylcholine release and can cause neuromuscular blockade INDICATION: Respiratory infections, GI infections, UTIs, Mastitis, Dermatitis, Septicaemia CONTRAINDICATION: Never combine with cephalosporins; severe hepatotoxicity results; synergistic with lincomycin; never combine with tetracyclines NOTES: Good against MRSA, MRSP & Pseudomonas infections

Answer 112

GROUP: Aminoglycoside STRUCTURE: Aminocyclitol MOA: Inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Concentration- Dependent Bacteriostatic RESISTANCE: Ab ovo: Shown by anaerobic bacteria and Streptococci. Plasmids: E. coli can develop resistance via plasmids. Degrading Enzymes in the periplasmic space. Altering Enzymes in the periplasmic space. Reduced Permeability of the Cell Wall. One way cross resistance develops so if one aminoglycoside is ineffective you move to a stronger drug. ANTIMICROBIAL SPECTRUM: Predominantly Aerobic Bacteria, Staphylococcus, Mycobacteria Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Bibersteinia, Bordetella bronchiseptica, Pseudomonas aeruginosa, Enterobacteriaceae: E. coli, Salmonella, Klebsiella Leptospira: (some Proteus species) PK: Absorption is poor per os, hence PO usage is only for GI infections; IM/SC/parenteral use for other indications includes intramammary, intrauterine and intraabscess; topical application can be toxic, especially in Fe where it cannot be used; poor crossing of BBB and accumulates in kidney, excretion is in its active form hence these drugs are good for UTIs; SE: Nephrotoxic and ototoxic due to binding to phosphatidyl inositol in tubular cell membranes in the kidney. Drugs inhibit acetylcholine release and can cause neuromuscular blockade INDICATION: Respiratory infections, GI infections, UTIs, Mastitis, Dermatitis, Septicaemia CONTRAINDICATION: Never combine with cephalosporins; severe hepatotoxicity results; synergistic with lincomycin; never combine with tetracyclines NOTE: Least toxic aminoglycoside, only good antibiotic against Mycoplasma in the group

Answer 113

GROUP: Tetracyclines (short-acting) STRUCTURE: Linear fused tetracyclic nucleus MOA: Passively diffuse through porin channels in the bacterial membrane and inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration it is bactericidal RESISTANCE: Ab ovo: Pseudomonas aeruginosa. Acquired: E. coli, Salmonella, Pasteurella multocida, Mannheimia haemolytica, Staphylococcus aureus, Streptococci ANTIMICROBIAL SPECTRUM: Intracellular bacteria: Chlamydophilae, Rickettsia, Ehrlichia, Lawsonia, etc. Mycoplasma haemofelis, Bordetella bronchiseptica, Wolbachia, Plasmodium & Entamoeba histolytica. Almost all Gram positive Bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus etc... Enterobacteriaceae: E. coli, Salmonella, Klebsiella Anaerobics: Bacteroides, Fusobacterium, Proteus Spirochaetes: Leptospira, Borrelia PK: Lipophilic with excellent pharmacokinetics, penetrating inside all cells and crossing all biological membranes and barriers SE: Tissue irritant, vomiting, diarrhea, hepatoxicity, impairment of bone growth in very young animals INDICATION: General infections, most respiratory infections, bronchopneumonia, foot diseases, metritis, mastitis, Mycoplasma respiratory infections in Ru/Su/Av, Infectious keratoconjunctivitis in Bo CONTRAINDICATIONS: Never combine with aminoglycosides NOTES: Normal for human use

Answer 114

GROUP: Tetracyclines (short-acting) STRUCTURE: Linear fused tetracyclic nucleus MOA: Passively diffuse through porin channels in the bacterial membrane and inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration it is bactericidal RESISTANCE: ab ovo: Pseudomonas aeruginosa. Acquired: E. coli, Salmonella, Pasteurella multocida, Mannheimia haemolytica, Staphylococcus aureus, Streptococci ANTIMICROBIAL SPECTRUM: Intracellular bacteria: Chlamydophilae, Rickettsia, Ehrlichia, Lawsonia, etc. Mycoplasma haemofelis, Bordetella bronchiseptica, Wolbachia, Plasmodium & Entamoeba histolytica. Almost all Gram positive Bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus etc... Enterobacteriaceae: E. coli, Salmonella, Klebsiella Anaerobics: Bacteroides, Fusobacterium, Proteus Spirochaetes: Leptospira, Borrelia PK: Lipophilic with excellent pharmacokinetics, penetrating inside all cells and crossing all biological membranes and barriers SE: Tissue irritant, vomiting, diarrhea, hepatoxicity, impairment of bone growth in very young animals INDICATION: General infections, most respiratory infections, bronchopneumonia, foot diseases, metritis, mastitis, Mycoplasma respiratory infections in Ru/Su/Av, Infectious keratoconjunctivitis in Bo CONTRAINDICATIONS: Never combine with aminoglycosides NOTE: Naturally occuring

Answer 115

GROUP: Tetracyclines (short-acting) STRUCTURE: Linear fused tetracyclic nucleus MOA: Passively diffuse through porin channels in the bacterial membrane and inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration it is bactericidal RESISTANCE: ab ovo: Pseudomonas aeruginosa. Acquired: E. coli, Salmonella, Pasteurella multocida, Mannheimia haemolytica, Staphylococcus aureus, Streptococci ANTIMICROBIAL SPECTRUM: Intracellular bacteria: Chlamydophilae, Rickettsia, Ehrlichia, Lawsonia, etc. Mycoplasma haemofelis, Bordetella bronchiseptica, Wolbachia, Plasmodium & Entamoeba histolytica. Almost all Gram positive Bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus etc... Enterobacteriaceae: E. coli, Salmonella, Klebsiella Anaerobics: Bacteroides, Fusobacterium, Proteus Spirochaetes: Leptospira, Borrelia PK: Lipophilic with excellent pharmacokinetics, penetrating inside all cells and crossing all biological membranes and barriers SE: Tissue irritant, vomiting, diarrhea, hepatoxicity, impairment of bone growth in very young animals INDICATION: General infections, most respiratory infections, bronchopneumonia, foot diseases, metritis, mastitis, Mycoplasma respiratory infections in Ru/Su/Av, Infectious keratoconjunctivitis in Bo

Answer 116

GROUP: Tetracyclines (long-acting) STRUCTURE: Linear fused tetracyclic nucleus MOA: Passively diffuse through porin channels in the bacterial membrane and inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration it is bactericidal RESISTANCE: ab ovo: Pseudomonas aeruginosa. Acquired: E. coli, Salmonella, Pasteurella multocida, Mannheimia haemolytica, Staphylococcus aureus, Streptococci ANTIMICROBIAL SPECTRUM: Intracellular bacteria: Chlamydophilae, Rickettsia, Ehrlichia, Lawsonia, etc. Mycoplasma haemofelis, Bordetella bronchiseptica, Wolbachia, Plasmodium & Entamoeba histolytica. Almost all Gram positive Bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus etc... Enterobacteriaceae: E. coli, Salmonella, Klebsiella Anaerobics: Bacteroides, Fusobacterium, Proteus Spirochaetes: Leptospira, Borrelia. Toxoplasmosis! PK: More lipophilic with excellent absorption, penetrate bone, low degree of metabolism and mainly excreted via the large intestine in the bile SE: Tissue irritant, vomiting, diarrhea, hepatoxicity, impairment of bone growth in very young animals INDICATION: General infections, most respiratory infections, bronchopneumonia, foot diseases, metritis, mastitis, Mycoplasma respiratory infections in Ru/Su/Av, Infectious keratoconjunctivitis in Bo NOTES: First choice against Lyme disease, lethal proliferative enteropathy in horse

Answer 117

GROUP: Macrolides STRUCTURE: Weakly basic macrocyclic lactone rings with attached sugar moieties MOA: Inhibit 50S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration bactericidal RESISTANCE: Resistance is via decreased permeability and hence impaired uptake, degrading enzymes and modifications to the 50S binding site ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Anaerobic & Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Brachyspira hyodysenteriae, Lawsonia intracellularis, Bordetella, Mycoplasma, Chlamydophila, Rickettsia, Borrelia, Rhodococcus equi PK: Macrolides are lipophilic and reach very high intracellular concentrations; never give IV, given PO to Ca/Fe/Eq; macrolides reach the bones, placenta and prostate but will not cross the BBB, macrolides are CYP450 enzyme inhibitors SE: Tissue irritation, serious risk of dysbacteriosis and fatal enterocolitis in adult horses, rabbits and herbivorous rodents INDICATION: Mycoplasma, Pasteurella and other fastidious bacterial respiratory infections, foot rot, oral cavity infections & bite wounds. CONTRAINDICATION: Never combine with other 50S inhibitors (lincosamides, pleuromutilins, phenicols) NOTES: Semisynthetic azalide used to treat Campylobacter enteritis and Rhodococcus equi

Answer 118

GROUP: Macrolides STRUCTURE: Weakly basic macrocyclic lactone rings with attached sugar moieties MOA: Inhibit 50S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration bactericidal RESISTANCE: Resistance is via decreased permeability and hence impaired uptake, degrading enzymes and modifications to the 50S binding site ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Anaerobic & Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Brachyspira hyodysenteriae, Lawsonia intracellularis, Bordetella, Mycoplasma, Chlamydophila, Rickettsia, Borrelia, Rhodococcus equi PK: Macrolides are lipophilic and reach very high intracellular concentrations; never give IV, given PO to Ca/Fe/Eq; macrolides reach the bones, placenta and prostate but will not cross the BBB, macrolides are CYP450 enzyme inhibitors SE: Tissue irritation, serious risk of dysbacteriosis and fatal enterocolitis in adult horses, rabbits and herbivorous rodents INDICATION: Mycoplasma, Pasteurella and other fastidious bacterial respiratory infections, foot rot, oral cavity infections & bite wounds. CONTRAINDICATION: Never combine with other 50S inhibitors (lincosamides, pleuromutilins, phenicols) NOTES: Semisynthetic macrolide used to treat Campylobacter enteritis and Rhodococcus equi

Answer 119

GROUP: Macrolide (older veterinary drug) STRUCTURE: Weakly basic macrocyclic lactone rings with attached sugar moieties MOA: Inhibit 50S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration bactericidal RESISTANCE: Resistance is via decreased permeability and hence impaired uptake, degrading enzymes and modifications to the 50S binding site ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Anaerobic & Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Brachyspira hyodysenteriae, Lawsonia intracellularis, Bordetella, Mycoplasma, Chlamydophila, Rickettsia, Borrelia, Rhodococcus equi PK: Macrolides are lipophilic and reach very high intracellular concentrations; never give IV, given PO to Ca/Fe/Eq; macrolides reach the bones, placenta and prostate but will not cross the BBB, macrolides are CYP450 enzyme inhibitors SE: Tissue irritation, serious risk of dysbacteriosis and fatal enterocolitis in adult horses, rabbits and herbivorous rodents INDICATION: Mycoplasma, Pasteurella and other fastidious bacterial respiratory infections, foot rot, oral cavity infections & bite wounds. CONTRAINDICATION: Never combine with other 50S inhibitors (lincosamides, pleuromutilins, phenicols) NOTES: (Lawsonia intracellularis) in Su (NOT in Eq), used in Ru/Su/Av to treat respiratory tract infections and necrotic enteritis

Answer 120

GROUP: Macrolide (older veterinary drug) STRUCTURE: Weakly basic macrocyclic lactone rings with attached sugar moieties MOA: Inhibit 50S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration bactericidal RESISTANCE: Resistance is via decreased permeability and hence impaired uptake, degrading enzymes and modifications to the 50S binding site ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Anaerobic & Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Brachyspira hyodysenteriae, Lawsonia intracellularis, Bordetella, Mycoplasma, Chlamydophila, Rickettsia, Borrelia, Rhodococcus equi PK: Macrolides are lipophilic and reach very high intracellular concentrations; never give IV, given PO to Ca/Fe/Eq; macrolides reach the bones, placenta and prostate but will not cross the BBB, macrolides are CYP450 enzyme inhibitors SE: Tissue irritation, serious risk of dysbacteriosis and fatal enterocolitis in adult horses, rabbits and herbivorous rodents INDICATION: Mycoplasma, Pasteurella and other fastidious bacterial respiratory infections, foot rot, oral cavity infections & bite wounds. CONTRAINDICATION: Never combine with other 50S inhibitors (lincosamides, pleuromutilins, phenicols) NOTES: Never in goats; highly cardiotoxic in all other species

Answer 121

GROUP: Macrolide STRUCTURE: Weakly basic macrocyclic lactone rings with attached sugar moieties MOA: Inhibit 50S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration bactericidal RESISTANCE: Resistance is via decreased permeability and hence impaired uptake, degrading enzymes and modifications to the 50S binding site ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Anaerobic & Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Brachyspira hyodysenteriae, Lawsonia intracellularis, Bordetella, Mycoplasma, Chlamydophila, Rickettsia, Borrelia, Rhodococcus equi PK: Macrolides are lipophilic and reach very high intracellular concentrations; never give IV, given PO to Ca/Fe/Eq; macrolides reach the bones, placenta and prostate but will not cross the BBB, macrolides are CYP450 enzyme inhibitors SE: Tissue irritation, serious risk of dysbacteriosis and fatal enterocolitis in adult horses, rabbits and herbivorous rodents INDICATION: Mycoplasma, Pasteurella and other fastidious bacterial respiratory infections, foot rot, oral cavity infections & bite wounds. CONTRAINDICATION: Never combine with other 50S inhibitors (lincosamides, pleuromutilins, phenicols) NOTES: Against Brachyspira hyodysenteriae (3rd choice drug), Lawsonia intracellularis and mycoplasmae

Answer 122

GROUP: Macrolide STRUCTURE: Weakly basic macrocyclic lactone rings with attached sugar moieties MOA: Inhibit 50S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration bactericidal RESISTANCE: Resistance is via decreased permeability and hence impaired uptake, degrading enzymes and modifications to the 50S binding site ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Anaerobic & Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus, Mannheimia, Brachyspira hyodysenteriae, Lawsonia intracellularis, Bordetella, Mycoplasma, Chlamydophila, Rickettsia, Borrelia, Rhodococcus equi PK: Macrolides are lipophilic and reach very high intracellular concentrations; never give IV, given PO to Ca/Fe/Eq; macrolides reach the bones, placenta and prostate but will not cross the BBB, macrolides are CYP450 enzyme inhibitors SE: Tissue irritation, serious risk of dysbacteriosis and fatal enterocolitis in adult horses, rabbits and herbivorous rodents INDICATION: Mycoplasma, Pasteurella and other fastidious bacterial respiratory infections, foot rot, oral cavity infections & bite wounds. CONTRAINDICATION: Never combine with other 50S inhibitors (lincosamides, pleuromutilins, phenicols) NOTE: Outstanding cellular and respiratory concentrations against fastidious bacteria and mycoplasmae

Answer 123

GROUP: Phenicols STRUCTURE: Halogenated arylamides; small lipophilic molecules MOA: Inhibit 50S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic RESISTANCE: Ab ovo: Pseudomonas spp. Resistant bacteria often possess acetyltransferases which inactivate phenicols; Yet, resistance is uncommon compared to tetracyclines ANTIMICROBIAL SPECTRUM: Very broad spectrum; almost all Gram positive and negative aerobes and anaerobes; Mycoplasma, Chlamydophila and Rickettsia susceptible PK: Excellent pharmacokinetics with 80-100% absorption PO/IM/SC; crosses all barriers and enters bone, placenta, prostate and cells; metabolised in the liver and excreted mostly in the bile SE: Dose-dependent anaemia is seen after 7- 10 days, mostly in liver failure patients, due to protein synthesis inhibition INDICATION: Florfenicol is the only drug in the group permitted in large animals; used to treat: Bovine Respiratory Disease (BRD), Swine Respiratory Disease (SRD), Mycoplasma and fastidious Gram negative infections, foot diseases, infectious keratoconjunctivitis, Aeromonas and Vibrio infections. In Small Animals: Eye Infections, Prostatitis, Meningitis, MRSA & MRSP Infections CONTRAINDICATION: Never combine with other 50S inhibitors (lincosamides, pleuromutilins, macrolides); contraindicated in patients with liver disease NOTE: Naturally occurring from Streptomyces venezuelae; strictly banned in food-producing animals; WEAR GLOVES APPLYING

Answer 124

GROUP: Phenicols STRUCTURE: Halogenated arylamides; small lipophilic molecules MOA: Inhibit 50S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic RESISTANCE: Ab ovo: Pseudomonas spp. Resistant bacteria often possess acetyltransferases which inactivate phenicols; Yet, resistance is uncommon compared to tetracyclines ANTIMICROBIAL SPECTRUM: Very broad spectrum; almost all Gram positive and negative aerobes and anaerobes; Mycoplasma, Chlamydophila and Rickettsia susceptible PK: Excellent pharmacokinetics with 80-100% absorption PO/IM/SC; crosses all barriers and enters bone, placenta, prostate and cells; metabolised in the liver and excreted mostly in the bile SE: Dose-dependent anaemia is seen after 7- 10 days, mostly in liver failure patients, due to protein synthesis inhibition INDICATION: Florfenicol is the only drug in the group permitted in large animals; used to treat: Bovine Respiratory Disease (BRD), Swine Respiratory Disease (SRD), Mycoplasma and fastidious Gram negative infections, foot diseases, infectious keratoconjunctivitis, Aeromonas and Vibrio infections. In Small Animals: Eye Infections, Prostatitis, Meningitis, MRSA & MRSP Infections CONTRAINDICATION: Never combine with other 50S inhibitors (lincosamides, pleuromutilins, macrolides); contraindicated in patients with liver disease NOTE: Used to treat Vibrio anguillarum and Aeromonas salmonicida

Answer 125

GROUP: Lincosamides STRUCTURE: Pyrrolidine ring linked to a pyranose moiety via an amide bond MOA: Pyrrolidine ring linked to a pyranose moiety via an amide bond MODA: Bacteriostatic RESISTANCE: Exhibit cross resistance with macrolides and phenicols; fastidious Gram negative bacteria are ab ovo resistant ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus, Enterococcus etc.. Anaerobic Gram negative bacteria: Proteus, Bacteroides, Fusobacterium, Campylobacter, Brachyspira hyodysenteriae, Lawsonia intracellularis, Mycoplasma PK: Good absorption, excellent distribution and especially good at reaching the bones; does not cross the BBB but achieves very high intracellular concentrations; metabolised in the liver and excreted via the bile and urine SE: Severe tissue irritation, most toxic antibiotics for intestinal flora and cause dysbacteriosis and fatal enterocolitis in adult horses, rabbits and herbivorous rodents (guinea pigs, chinchillas, hamsters, gerbils) INDICATION: Osteomyelitis cases after bone surgery, Bone Marrow infections (often Staphylococcus aureus), moderate effectiveness against Mycoplasma infections CONTRAINDICATION: Never combine with other 50S inhibitors (macrolides, pleuromutilins, phenicols); these drugs may never be used in Eq, rabbits and herbivorous rodents (v. toxic); not to be used to treat UTIs NOTES: Synergistic with spectinomycin; in combination called Lincospectin and very effective against mycoplasmae; drug), mainly used in food producing animals and is used against foot rot, wound infections, mastitis, metritis,and proliferative enteropathy in Su

Answer 126

GROUP: Lincosamides STRUCTURE: Pyrrolidine ring linked to a pyranose moiety via an amide bond MOA: Pyrrolidine ring linked to a pyranose moiety via an amide bond MODA: Bacteriostatic RESISTANCE: Exhibit cross resistance with macrolides and phenicols; fastidious Gram negative bacteria are ab ovo resistant ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus, Enterococcus etc.. Anaerobic Gram negative bacteria: Proteus, Bacteroides, Fusobacterium, Campylobacter, Brachyspira hyodysenteriae, Lawsonia intracellularis, Mycoplasma PK: Good absorption, excellent distribution and especially good at reaching the bones; does not cross the BBB but achieves very high intracellular concentrations; metabolised in the liver and excreted via the bile and urine SE: Severe tissue irritation, most toxic antibiotics for intestinal flora and cause dysbacteriosis and fatal enterocolitis in adult horses, rabbits and herbivorous rodents (guinea pigs, chinchillas, hamsters, gerbils) INDICATION: Osteomyelitis cases after bone surgery, Bone Marrow infections (often Staphylococcus aureus), moderate effectiveness against Mycoplasma infections CONTRAINDICATION: Never combine with other 50S inhibitors (macrolides, pleuromutilins, phenicols); these drugs may never be used in Eq, rabbits and herbivorous rodents (v. toxic); not to be used to treat UTIs NOTES: More active than Lincomycin and mostly used PO in companion animals to treat oral cavity infections, especially anaerobic infections; also used against Gram positive dermatitis and to treat abscesses, osteomyelitis and anal sacculitis

Answer 127

GROUP: Pleuromutilin STRUCTURE: Bridged tricyclic diterpenoid MOA: Inhibit 50S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic RESISTANCE: Exhibit cross resistance with lincosamides, macrolides and phenicols ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus, Enterococcus etc.. Fastidious Gram negative bacteria: Pasteruella, Brachyspira hyodysenteriae, Lawsonia intracellularis, Mycoplasma PK: Good absorption, excellent distribution, metabolised in the liver and excreted via the bile and urine SE: Skin erythema and vulvar edema is common INDICATION: Swine Dysentery (Brachyspira hyodysenteriae), Proliferative Enteropathy in Su (Lawsonia intracellularis), Mycoplasmosis & Respiratory Infections in Su/Av CONTRAINDICATION: Never combine with other 50S inhibitors (macrolides, lincosamides, phenicols), never combine with monensin or other ionopohores NOTES: PO/IM/SC; outstanding against Brachyspira hyodysenteriae

Answer 128

GROUP: Pleuromutilin STRUCTURE: Bridged tricyclic diterpenoid MOA: Inhibit 50S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic RESISTANCE: Exhibit cross resistance with lincosamides, macrolides and phenicols ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus, Enterococcus etc.. Fastidious Gram negative bacteria: Pasteruella, Brachyspira hyodysenteriae, Lawsonia intracellularis, Mycoplasma PK: Good absorption, excellent distribution, metabolised in the liver and excreted via the bile and urine SE: Skin erythema and vulvar edema is common INDICATION: Swine Dysentery (Brachyspira hyodysenteriae), Proliferative Enteropathy in Su (Lawsonia intracellularis), Mycoplasmosis & Respiratory Infections in Su/Av CONTRAINDICATION: Never combine with other 50S inhibitors (macrolides, lincosamides, phenicols), never combine with monensin or other ionopohores NOTES: PO only and only used in food producing animals, outstanding against Brachyspira hyodysenteriae

Answer 129

GROUP: Polypeptide antibiotic STRUCTURE: Mixture of related cyclic peptides MOA: Inhibits bacterial cell wall synthesis by interfering with the dephosphorylation of C55- isoprenyl pyrophosphate MODA: Bacteriostatic RESISTANCE: Narrow spectrum and gram negative bacteria are ab ovo resistant ANTIMICROBIAL SPECTRUM: Some Gram positive bacteria: Clostridium, Staphylococcus, Streptococcus Haemophilus PK: PO or topical application SE: Allergy INDICATION: Topical and local infections of the mouth, nose, eye skin and mammary gland; oral premixes for prevention of necrotic enteritis in rabbits (Clostridium perfringens) CONTRAINDICATION: Contraindicated for systemic use due to nephrotoxicity NOTES: Often combined with polymyxins or neomycin

Answer 130

GROUP: Polypeptides STRUCTURE: Cationic basic polypeptides MOA: Act as detergents to disrupt the cell membrane functions of Gram negative bacteria, break down the cell wall of Gram negative bacteria and neutralise LPS endotoxin MODA: Concentration- Dependent Bactericidal RESISTANCE: Ab ovo: Gram positive bacteria are resistant as their peptidoglycan wall is too thick. Resistance is otherwise uncommon and mainly chromosomedependent, although colistin is plasmid encoded ANTIMICROBIAL SPECTRUM: Gram negative bacilli - Enterobacter, Klebsiella, Salmonella, Pasteurella, Bordetella, Shigella, E. coli AND Pseudomonas PK: Poorly absorbed and poorly distributed in tissues; administered topically and PO for skin and GI infections SE: Intense pain at site of injection, hypersensitivity reactions, kidney damage, nervous system damage INDICATION: Oral, ophthalmic, otic, intramammary or topical treatments of GI infections, pyoderma, otitis externa & mastitis; parenteral use only for life-threatening Gram negative bacillus infections, especially Pseudomonas CONTRAINDICATION: Nephrotoxic and neurotoxic with toxicity increasing from polymyxin B to E to M; act synergistically when combined with tetracyclines, potentiated sulfonamides, penicillins, aminoglycosides and fluoroquinolones NOTE: Frequently combined topically with bacitracin, neomycin or both

Answer 131

GROUP: Polypeptides STRUCTURE: Cationic basic polypeptides MOA: Act as detergents to disrupt the cell membrane functions of Gram negative bacteria, break down the cell wall of Gram negative bacteria and neutralise LPS endotoxin MODA: Concentration- Dependent Bactericidal RESISTANCE: Ab ovo: Gram positive bacteria are resistant as their peptidoglycan wall is too thick. Resistance is otherwise uncommon and mainly chromosomedependent, although colistin is plasmid encoded ANTIMICROBIAL SPECTRUM: Gram negative bacilli - Enterobacter, Klebsiella, Salmonella, Pasteurella, Bordetella, Shigella, E. coli AND Pseudomonas PK: Poorly absorbed and poorly distributed in tissues; administered topically and PO for skin and GI infections SE: Intense pain at site of injection, hypersensitivity reactions, kidney damage, nervous system damage INDICATION: Oral, ophthalmic, otic, intramammary or topical treatments of GI infections, pyoderma, otitis externa & mastitis; parenteral use only for life-threatening Gram negative bacillus infections, especially Pseudomonas CONTRAINDICATION: Nephrotoxic and neurotoxic with toxicity increasing from polymyxin B to E to M; act synergistically when combined with tetracyclines, potentiated sulfonamides, penicillins, aminoglycosides and fluoroquinolones

Answer 132

GROUP: Glycopeptides (1st gen) STRUCTURE: Glycosylated cyclic or polycyclic non ribosomal peptide MOA: Inhibit peptidoglycan synthesis by binding tightly to the D-Ala-DAla terminus of the murein monomer MODA: Time-dependent Bactericidal BUT bacteriostatic against enterococci RESISTANCE: Gram-negative rods are resistant; the VanA gene cluster confers vancomycin resistance and in vancomycinintermediate- resistant S. aureus strains (VISA) a thicker murein layer acts as a decoy target for vancomycin ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus, Enterococcus PK: Administered BID; does not distribute into the CSF; 90% excreted in urine so can accumulate in patients with renal failure; IV/IM for systemic infections and PO for GI infections SE: Tissue necrosis and phlebitis at the injection site if given too quickly; pain at site of injection; idiosyncratic reaction to IV bolus caused by histamine release; interstitial nephritis; renal failure; blood disorders INDICATION: Toxic drugs for use only in life-threatening cases; nosocomial infections; antibiotic-associated enterocolitis, particularly Clostridium difficile GI infections; MRSA infections CONTRAINDICATION: Contraindicated in renal failure or kidney disease patients NOTES: Usually given IV

Answer 133

STRUCTURE: Glycosylated cyclic or polycyclic non ribosomal peptide MOA: Inhibit peptidoglycan synthesis by binding tightly to the D-Ala-DAla terminus of the murein monomer MODA: Time-dependent Bactericidal BUT bacteriostatic against enterococci RESISTANCE: Gram-negative rods are resistant; the VanA gene cluster confers vancomycin resistance and in vancomycinintermediate- resistant S. aureus strains (VISA) a thicker murein layer acts as a decoy target for vancomycin ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus, Enterococcus PK: Administered BID; does not distribute into the CSF; 90% excreted in urine so can accumulate in patients with renal failure; IV/IM for systemic infections and PO for GI infections SE: Tissue necrosis and phlebitis at the injection site if given too quickly; pain at site of injection; idiosyncratic reaction to IV bolus caused by histamine release; interstitial nephritis; renal failure; blood disorders INDICATION: Toxic drugs for use only in life-threatening cases; nosocomial infections; antibiotic-associated enterocolitis, particularly Clostridium difficile GI infections; MRSA infections CONTRAINDICATION: Contraindicated in renal failure or kidney disease patients NOTES: 50-100 times more lipophilic than vancomycin

Answer 134

GROUP: Rifamycins STRUCTURE: Polyketide antibiotics with macrocyclic amide structure including a naphthoquinone core MOA: Inhibit bacterial DNA- dependent RNA polymerase, hence acting as RNA synthesis inhibitors MODA: Bactericidal; kills both intracellular and extracellular pathogens RESISTANCE: Develops rapidly due to decreased affinity of RNA polymerase ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria - Bacillus, Clostridium, Staphylococcus, Streptococcus, Enterococcus, Mycobacteria Rhodococcus equi & Neisseria PK: Highly selective activity against bacterial polymerases; widely distributed even into the CSF; induce liver microsomal enzymes including CYP450 and enhance the metabolism of other drugs, including anticoagulants SE: Rash, fever, nausea, vomiting, jaundice, red-orange discolouration of faeces, urine, tears and sweat. INDICATION: Treatment of tuberculosis and other Mycobacteria infections, prophylaxis of meningococcal disease CONTRAINDICATION: In liver failure patients or patients with impaired liver function

Answer 135

GROUP: Miscellaneous STRUCTURE: Fatty acid ester of substituted tetrahydropyran MOA: Reversibly inhibits isoleucyl tRNA synthetase resulting in reduced protein synthesis in Gram positive cocci. MODA: Bacteriostatic REISTANCE: Resistance due to mutations in the wildtype isoleucyl tRNA synthetase ANTIMICORBIAL SPECTRUM: Gram positive cocci: Staphylococcus, Streptococcus, Enterococcus PK: Used topically against Staphylococcus aureus and intranasally against MRSA strains postoperatively SE: Rash, pain at site of application INDICATION: Dermal or Nasal Staphylococcus aureus infections

Answer 136

GROUP: Sulphonamides (sytemic short-acting) STRUCTURE: Para -Aminosulfonamides with poor solubility in acids and often administered as alkaline sodium salts (except for sulfacetamide which can be used in native form) MOA: Inhibit bacterial dihydropteroate synthetase by competing with PABA MODA: Bacteriostatic RESISTANCE: Ab ovo resistant : Mycobacteria, Mycoplasma, Coxiella, Clostridia, Rickettsiae, Pseudomonas aeruginosa, Leptospira, Borrelia, Brachyspira, Treponema, Peptostreptococcus, Chromosomal mutation, plasmid and integronmediated resistance, decreased penetration, PABAspecific enzyme mutation and overproduction of PABA are all mechanisms of resistance ANTIMICROBIAL SPECTRUM: Most susceptible: Bacillus, Brucella, Erysipelothrix, Listeria, Nocardia, Streptococcus, Chlamydophilae & Coccidia, Toxoplasma, Sarcocystis, Pneumocystis and Cryptosporidium spp. Moderately susceptible: Staphylococcus, Enterococcus, E. coli, Klebsiella, Proteus, Actinobacillus, Haemophilus PK: Administered as feed additives, PO, topically, intrauterine, IM/SC; good absorption after PO administration, penetrates BBB well; inhibited by purulent materials; can form crystalline metabolites in the kidneys and urinary tracts of cats, excreted via the kidney both in active and metabolised forms, 20% absorbed PO SE: Crystalluria, haematuria, crystal nephrosis (especially in Fe), idiosyncratic immune reactions, idiosyncratic hepatotoxicity, allergy (especially in Doberman Pinschers), keratoconjunctivitis sicca INDICATION: Systemic and Organ Infections, Respiratory Infections by Bordetella bronchiseptica & Actinobacillus pleuropneumoniae, GI infections (E. coli, Salmonella), UTIs, Metritis, Mastitis, Agalactia, Foot Rot, Prostatitis, Meningitis and toxoplasmosis CONTRAINDICATION: Very large MIC compared to antibiotics

Answer 137

GROUP: Sulphonamides (systemic short-acting) STRUCTURE: Para -Aminosulfonamides with poor solubility in acids and often administered as alkaline sodium salts (except for sulfacetamide which can be used in native form) MOA: Inhibit bacterial dihydropteroate synthetase by competing with PABA MODA: Bacteriostatic RESISTANCE: Ab ovo resistant : Mycobacteria, Mycoplasma, Coxiella, Clostridia, Rickettsiae, Pseudomonas aeruginosa, Leptospira, Borrelia, Brachyspira, Treponema, Peptostreptococcus, Chromosomal mutation, plasmid and integronmediated resistance, decreased penetration, PABAspecific enzyme mutation and overproduction of PABA are all mechanisms of resistance ANTIMICROBIAL SPECTRUM: Most susceptible: Bacillus, Brucella, Erysipelothrix, Listeria, Nocardia, Streptococcus, Chlamydophilae & Coccidia, Toxoplasma, Sarcocystis, Pneumocystis and Cryptosporidium spp. Moderately susceptible: Staphylococcus, Enterococcus, E. coli, Klebsiella, Proteus, Actinobacillus, Haemophilus PK: Administered as feed additives, PO, topically, intrauterine, IM/SC; good absorption after PO administration, penetrates BBB well; inhibited by purulent materials; can form crystalline metabolites in the kidneys and urinary tracts of cats, excreted via the kidney both in active and metabolised forms SE: Crystalluria, haematuria, crystal nephrosis (especially in Fe), idiosyncratic immune reactions, idiosyncratic hepatotoxicity, allergy (especially in Doberman Pinschers), keratoconjunctivitis sicca INDICATION: Systemic and Organ Infections, Respiratory Infections by Bordetella bronchiseptica & Actinobacillus pleuropneumoniae, GI infections (E. coli, Salmonella), UTIs, Metritis, Mastitis, Agalactia, Foot Rot, Prostatitis, Meningitis and toxoplasmosis CONTRAINDICATION: Very large MIC compared to antibiotics

Answer 138

GROUP: Sulphonamides (systemic short-acting) STRUCTURE: Para -Aminosulfonamides with poor solubility in acids and often administered as alkaline sodium salts (except for sulfacetamide which can be used in native form) MOA: Inhibit bacterial dihydropteroate synthetase by competing with PABA MODA: Bacteriostatic RESISTANCE: Ab ovo resistant : Mycobacteria, Mycoplasma, Coxiella, Clostridia, Rickettsiae, Pseudomonas aeruginosa, Leptospira, Borrelia, Brachyspira, Treponema, Peptostreptococcus, Chromosomal mutation, plasmid and integronmediated resistance, decreased penetration, PABAspecific enzyme mutation and overproduction of PABA are all mechanisms of resistance ANTIMICROBIAL SPECTRUM: Most susceptible: Bacillus, Brucella, Erysipelothrix, Listeria, Nocardia, Streptococcus, Chlamydophilae & Coccidia, Toxoplasma, Sarcocystis, Pneumocystis and Cryptosporidium spp. Moderately susceptible: Staphylococcus, Enterococcus, E. coli, Klebsiella, Proteus, Actinobacillus, Haemophilus PK: Administered as feed additives, PO, topically, intrauterine, IM/SC; good absorption after PO administration, penetrates BBB well; inhibited by purulent materials; can form crystalline metabolites in the kidneys and urinary tracts of cats, excreted via the kidney both in active and metabolised forms, 50% PO absorption SE: Crystalluria, haematuria, crystal nephrosis (especially in Fe), idiosyncratic immune reactions, idiosyncratic hepatotoxicity, allergy (especially in Doberman Pinschers), keratoconjunctivitis sicca INDICATION: Systemic and Organ Infections, Respiratory Infections by Bordetella bronchiseptica & Actinobacillus pleuropneumoniae, GI infections (E. coli, Salmonella), UTIs, Metritis, Mastitis, Agalactia, Foot Rot, Prostatitis, Meningitis and toxoplasmosis CONTRAINDICATION: Very large MIC compared to antibiotics

Answer 139

GROUP: Sulphonamides (systemic short-acting) STRUCTURE: Para -Aminosulfonamides with poor solubility in acids and often administered as alkaline sodium salts (except for sulfacetamide which can be used in native form) MOA: Inhibit bacterial dihydropteroate synthetase by competing with PABA MODA: Bacteriostatic RESISTANCE: Ab ovo resistant : Mycobacteria, Mycoplasma, Coxiella, Clostridia, Rickettsiae, Pseudomonas aeruginosa, Leptospira, Borrelia, Brachyspira, Treponema, Peptostreptococcus, Chromosomal mutation, plasmid and integronmediated resistance, decreased penetration, PABAspecific enzyme mutation and overproduction of PABA are all mechanisms of resistance ANTIMICROBIAL SPECTRUM: Most susceptible: Bacillus, Brucella, Erysipelothrix, Listeria, Nocardia, Streptococcus, Chlamydophilae & Coccidia, Toxoplasma, Sarcocystis, Pneumocystis and Cryptosporidium spp. Moderately susceptible: Staphylococcus, Enterococcus, E. coli, Klebsiella, Proteus, Actinobacillus, Haemophilus PK: Administered as feed additives, PO, topically, intrauterine, IM/SC; good absorption after PO administration, penetrates BBB well; inhibited by purulent materials; can form crystalline metabolites in the kidneys and urinary tracts of cats, excreted via the kidney both in active and metabolised forms SE: Crystalluria, haematuria, crystal nephrosis (especially in Fe), idiosyncratic immune reactions, idiosyncratic hepatotoxicity, allergy (especially in Doberman Pinschers), keratoconjunctivitis sicca INDICATION: Systemic and Organ Infections, Respiratory Infections by Bordetella bronchiseptica & Actinobacillus pleuropneumoniae, GI infections (E. coli, Salmonella), UTIs, Metritis, Mastitis, Agalactia, Foot Rot, Prostatitis, Meningitis and toxoplasmosis CONTRAINDICATION: Very large MIC compared to antibiotics

Answer 140

GROUP: Sulphonamides (systemic short-acting) STRUCTURE: Para -Aminosulfonamides with poor solubility in acids and often administered as alkaline sodium salts (except for sulfacetamide which can be used in native form) MOA: Inhibit bacterial dihydropteroate synthetase by competing with PABA MODA: Bacteriostatic RESISTANCE: Ab ovo resistant : Mycobacteria, Mycoplasma, Coxiella, Clostridia, Rickettsiae, Pseudomonas aeruginosa, Leptospira, Borrelia, Brachyspira, Treponema, Peptostreptococcus, Chromosomal mutation, plasmid and integronmediated resistance, decreased penetration, PABAspecific enzyme mutation and overproduction of PABA are all mechanisms of resistance ANTIMICROBIAL SPECTRUM: Most susceptible: Bacillus, Brucella, Erysipelothrix, Listeria, Nocardia, Streptococcus, Chlamydophilae & Coccidia, Toxoplasma, Sarcocystis, Pneumocystis and Cryptosporidium spp. Moderately susceptible: Staphylococcus, Enterococcus, E. coli, Klebsiella, Proteus, Actinobacillus, Haemophilus PK: Administered as feed additives, PO, topically, intrauterine, IM/SC; good absorption after PO administration, penetrates BBB well; inhibited by purulent materials; can form crystalline metabolites in the kidneys and urinary tracts of cats, excreted via the kidney both in active and metabolised forms SE: Crystalluria, haematuria, crystal nephrosis (especially in Fe), idiosyncratic immune reactions, idiosyncratic hepatotoxicity, allergy (especially in Doberman Pinschers), keratoconjunctivitis sicca INDICATION: Systemic and Organ Infections, Respiratory Infections by Bordetella bronchiseptica & Actinobacillus pleuropneumoniae, GI infections (E. coli, Salmonella), UTIs, Metritis, Mastitis, Agalactia, Foot Rot, Prostatitis, Meningitis and toxoplasmosis CONTRAINDICATION: Very large MIC compared to antibiotics

Answer 141

GROUP: Diaminopyrimidines STRUCTURE: Aryl substituted diaminopyrimidines which are weak bases and poorly soluble in water MOA: Inhibit bacterial dihydrofolate reductase and thus halt bacterial tetrahydrofolate synthesis MODA: Bacteriostatic RESISTANCE: Ab ovo resistant: Mycobacteria, Mycoplasma, Clostridia, Peptostreptococcus, Fusobacterium, Proteus, Bacteroides Chromosomal mutation to produce resistant reductase enzyme, plasmid and integron mediated resistance, multiple resistance common ANTIMICROBIAL SPECTRUM: Most susceptible: Bacillus, Brucella, Erysipelothrix, Listeria, Nocardia, Streptococcus & Coccidia, Toxoplasma, Sarcocystis, Pneumocystis and Cryptosporidium spp. Moderately susceptible: Staphylococcus, Enterococcus, E. coli, Klebsiella, Proteus etc.. PK: Well absorbed PO; excellent distribution and good penetration through blood-prostate, blood-milk and bloodbrain barriers (BBB); partly metabolised in the liver so excreted partly (40%) in the bile and the remaining (60%) in the urine via the kidney mainly in active form SE: Folic acid deficiency symptoms (fatigue, lethargy, anaemia, dyspnoea etc.) at high concentrations INDICATIONS: Systemic and Organ Infections, Respiratory Infections by Bordetella bronchiseptica & Actinobacillus pleuropneumoniae, GI infections (E. coli, Salmonella), UTIs, Metritis, Mastitis, Agalactia, Foot Rot, Prostatitis, Meningitis and toxoplasmosis

Answer 142

GROUP: Fluoroquinolones (2nd gen) STRUCTURE: Cyclopropyl MOA: Bactericidal (inhibit the activities mainly of topoisomerase IV. This is more pronounced in G-positives) MODA: Bactericidal, concentration dependent + Post- Antibacterial Effect RESISTANCE: Significant & frequent, chromosomal mutation and resistance (E. coli, P. aeruginosa, Salmonella, and Campylobacter strains) ANTIMICROBIAL SPECTRUM: Gram-negatives: Enterobacteria, Klebsiella spp P. aeruginosa → pronounced, Histophilus, Mycoplasma spp, Chlamydia spp Pseudomonas spp, Brucella spp Aeromonas spp. (fish farming) Gram positives: Staphylococcus spp. (S. aureus) Mycobacterium PK: Cat B (restrict), Excellent absorption after PO, Excellent distribution, very high Vd, high concentrations in bile, urine, prostate. Appear in milk. Good penetration through special barriers, partially metabolised, elimination mainly through kidneys SE: Inhibition of cartilage development, retinopathy in cats, dysbacteriosis INDICATION: Only use if no other AB is available: -Urinary tract infection, Respiratory infections, Mycoplasma, Soft tissues infection, Osteomyelitis, Prostatitis, Eye infections CONTRAINDICATIONS: Animals with asthma or epilepsy. Antagonistic reactions with: Chloramphenicol and rifampin. NOTES: Clinical use (EU): Human and off label use in small animals.

Answer 143

GROUP: Fluoroquinolone STRUCTURE: Quinoline monocarboxylic acid MOA: Bactericidal (inhibit the activities mainly of topoisomerase IV. This is more pronounced in G-positives) MODA: Bactericidal, concentration dependent + Post- Antibacterial Effect RESISTANCE: Significant & frequent, chromosomal mutation and resistance (E. coli, P. aeruginosa, Salmonella, and Campylobacter strains) ANTIMICROBIAL SPECTRUM: Gram-negatives: Enterobacteria, Klebsiella spp P. aeruginosa → pronounced, Histophilus, Mycoplasma spp, Chlamydia spp Pseudomonas spp, Brucella spp Aeromonas spp. (fish farming) Gram positives: Staphylococcus spp. (S. aureus) Mycobacterium PK: Cat B (restrict), Excellent absorption after PO, Excellent distribution, very high Vd, high concentrations in bile, urine, prostate. Appear in milk. Good penetration through special barriers, partially metabolised, elimination mainly through kidneys SE: Inhibition of cartilage development, retinopathy in cats, dysbacteriosis INDICATION: Only use if no other AB is available: Urinary tract infection, Respiratory infections, Mycoplasma, Soft tissues infection, Osteomyelitis, Prostatitis, Eye infections CONTRAINDICATION: In dogs and cats who are hypersensitive to quinolones. NOTE: Clinical use in (EU): Lactating cows, Swine, Poultry, Small animals Off label: In horses

Answer 144

GROUP: Fluoroquinolone STRUCTURE: Carboxylic acid MOA: Bactericidal (inhibit the activities mainly of topoisomerase IV. This is more pronounced in G-positives) MODA: Bactericidal, concentration dependent + Post- Antibacterial Effect RESISTANCE: Significant & frequent, chromosomal mutation and resistance (E. coli, P. aeruginosa, Salmonella, and Campylobacter strains) ANTIMICROBIAL SPECTRUM: Gram-negatives: Enterobacteria, Klebsiella spp P. aeruginosa → pronounced, Histophilus, Mycoplasma spp, Chlamydia spp Pseudomonas spp, Brucella spp Aeromonas spp. (fish farming) Gram positives: Staphylococcus spp. (S. aureus) Mycobacterium PK: Cat B (restrict), Excellent absorption after PO, Excellent distribution, very high Vd, high concentrations in bile, urine, prostate. Appear in milk. Good penetration through special barriers, partially metabolised, elimination mainly through kidneys SE: Inhibition of cartilage development, retinopathy in cats, dysbacteriosis INDICATION: Only use if no other AB is available: Urinary tract infection, Respiratory infections, Mycoplasma, Soft tissues infection, Osteomyelitis, Prostatitis, Eye infections CONTRAINDICATION: In dogs and cats who are hypersensitive to quinolones. NOTE: Clinical use in (EU): Large animals (only injection), pets Off label: HORSES

Answer 145

GROUP: Fluoroquinolone (3rd gen) STRUCTURE: Carboxylic acid MOA: Bactericidal (inhibit the activities mainly of topoisomerase IV. This is more pronounced in G-positives) MODA: Bactericidal, concentration dependent + Post- Antibacterial Effect RESISTANCE: Significant & frequent, chromosomal mutation and resistance (E. coli, P. aeruginosa, Salmonella, and Campylobacter strains) ANTIMICROBIAL SPECTRUM: Gram-negatives: Enterobacteria, Klebsiella spp P. aeruginosa → pronounced, Histophilus, Mycoplasma spp, Chlamydia spp Pseudomonas spp, Brucella spp Aeromonas spp. (fish farming) Gram positives: Staphylococcus spp. (S. aureus) Mycobacterium AND streptococci and atypical pathogens PK: Cat B (restrict), Excellent absorption after PO, Excellent distribution, very high Vd, high concentrations in bile, urine, prostate. Appear in milk. Good penetration through special barriers, partially metabolised, elimination mainly through kidneys SE: Inhibition of cartilage development, retinopathy in cats, dysbacteriosis INDICATION: Meningitis, meningoencephalitis, peritonitis, Gingivitis, periodontitis Against Staphylococcus aureus: Combine with Oxacillin

Answer 146

GROUP: Fluoroquinolone (3rd gen) STRUCTURE: Carboxylic acid MOA: Bactericidal (inhibit the activities mainly of topoisomerase IV. This is more pronounced in G-positives) MODA: Bactericidal, concentration dependent + Post- Antibacterial Effect RESISTANCE: Significant & frequent, chromosomal mutation and resistance (E. coli, P. aeruginosa, Salmonella, and Campylobacter strains) ANTIMICROBIAL SPECTRUM: Gram-negatives: Enterobacteria, Klebsiella spp P. aeruginosa → pronounced, Histophilus, Mycoplasma spp, Chlamydia spp Pseudomonas spp, Brucella spp Aeromonas spp. (fish farming) Gram positives: Staphylococcus spp. (S. aureus) Mycobacterium AND streptococci and atypical pathogens PK: Cat B (restrict), Excellent absorption after PO, Excellent distribution, very high Vd, high concentrations in bile, urine, prostate. Appear in milk. Good penetration through special barriers, partially metabolised, elimination mainly through kidneys SE: Inhibition of cartilage development, retinopathy in cats, dysbacteriosis INDICATION: Meningitis, meningoencephalitis, peritonitis, Gingivitis, periodontitis Against Staphylococcus aureus: Combine with Oxacillin CONTRAINDICATION: Withdrawn from US market due to high risk of phototoxicity (not sure if this is for animals/humans)

Answer 147

GROUP: Fluoroquinolone (4th gen) STRUCTURE: Carboxylic acid derivatives MOA: Bactericidal (inhibit the activities mainly of topoisomerase IV. This is more pronounced in G-positives) MODA: Bactericidal, concentration dependent + Post- Antibacterial Effect RESISTANCE: Significant & frequent, chromosomal mutation and resistance (E. coli, P. aeruginosa, Salmonella, and Campylobacter strains) ANTIMICROBIAL SPECTRUM: Gram-negatives: Enterobacteria, Klebsiella spp P. aeruginosa → pronounced, Histophilus, Mycoplasma spp, Chlamydia spp Pseudomonas spp, Brucella spp Aeromonas spp. (fish farming) Gram positives: Staphylococcus spp. (S. aureus) Mycobacterium, Methicillinsusceptible and resistant Staphylococcus aureus, AND streptococci and atypical pathogens PK: Cat B (restrict), Excellent absorption after PO, Excellent distribution, very high Vd, high concentrations in bile, urine, prostate. Appear in milk. High bioavailablity: >95%. Good penetration through special barriers, partially metabolised, elimination mainly through kidneys SE: Inhibition of cartilage development, retinopathy in cats, dysbacteriosis INDICATION: Meningitis, meningoencephalitis, peritonitis, Gingivitis, periodontitis NOTES: Use in EU: Small animals (only oral formulation)

Answer 148

GROUP: Fluoroquinolone (4th gen) STRUCTURE: Carboxylic acid derivatives MOA: Bactericidal (inhibit the activities mainly of topoisomerase IV. This is more pronounced in G-positives) MODA: Bactericidal, concentration dependent + Post- Antibacterial Effect RESISTANCE: Significant & frequent, chromosomal mutation and resistance (E. coli, P. aeruginosa, Salmonella, and Campylobacter strains) ANTIMICROBIAL SPECTRUM: Gram-negatives: Enterobacteria, Klebsiella spp P. aeruginosa → pronounced, Histophilus, Mycoplasma spp, Chlamydia spp Pseudomonas spp, Brucella spp Aeromonas spp. (fish farming) Gram positives: Staphylococcus spp. (S. aureus) Mycobacterium, Methicillinsusceptible and resistant Staphylococcus aureus, AND streptococci and atypical pathogens PK: Cat B (restrict), Excellent absorption after PO, Excellent distribution, very high Vd, high concentrations in bile, urine, prostate. Appear in milk. High bioavailablity: >95%. Good penetration through special barriers, partially metabolised, elimination mainly through kidneys SE: Inhibition of cartilage development, retinopathy in cats, dysbacteriosis SE: Inhibition of cartilage development, retinopathy in cats, dysbacteriosis INDICATION: Meningitis, meningoencephalitis, peritonitis, Gingivitis, periodontitis CONTRAINDICATION: Do not combine with NSAIDS

Answer 149

GROUP: Nitrofuranes STRUCTURE: Synthetic derivative of imidazolidin edione MODA: Bactericidal (high con.). Nitrofuranreductase ➔ toxic metabolite ➔ destroys DNA, ribosome RESISTANCE: ? ANTIMICROBIAL SPECTRUM: Relatively broad spectrum, mainly Gram-negatives, coliforms, Salmonella spp. Mycoplasma spp., Coccidia species PK: Well absorbed, quick excretion in urine SE: Low TI, GI-irritation, neurotoxic, mutagenic, potentially carcinogenic INDICATIONS: UTI's and skin formulation CONTRAINDICATION: Food producing animals: Table 2 drug! D (Prudence) category

Answer 150

GROUP: Nitroimidazoles STRUCTURE: Nitroimidazole derivative MOA: In anaerobic conditions toxic metabolites (nonenzymatic reduction of the nitro group) destroy the DNA of bacteria or protozoa ANTIMICROBIAL SPECTRUM: Obligate anaerobic bacteria: Clostridium spp.Bacteroides spp. Fusobacterium spp. Brachyspira hyodysenteriae. Protozoa: Trichomonas spp. Histomonas spp. Giardia spp. Amoeba spp. PK: Excellent absorption, tissue penetration, CSF, prostate, metabolisation in liver, elimination via kidney SE: Stomach pain, breathing difficulty, pounding heartbeat INDICATION: Gingivitis, paradontitis, periodontitis, oral cavity infections, Anal sacculitis, Pseudomembranous colitis! (Cl. difficile, Cl. perfringens), Trichomonas, Giardiosis! Histomonosis CONTRAINDICATIONS: Banned for Swine dysentery prevention, D (Prudence) category

Answer 151

GROUP: Fosfomycins STRUCTURE: Phosphonic acid derivatives MOA: Inhibition of the synthesis of peptidoglycan MODA: Bactericidal (conc. and/or time dependent) RESISTANCE: Acquired resistance develops rapidly during treatment (selection) ANTIMICROBIAL SPECTRUM: Relatively wide G+ and G-, incl. VRE, MRSA PK: Fp.o.=0.35 (in dog 0.7) , t1/2el= 5-6 hrs. No metabolism Distribution: Moderate. Excretion: Via faeces and kidneys (good for UTI) SE: Orally is safe with few transient side effects INDICATION: Mainly given p.o for urinary tract infections iv., sc. internal organ infections, septicaemia NOTES: Category C (caution)

Answer 152

GROUP: Anticoccidials (monovalent ionophore) STRUCTURE: Monoglycoside (lipophilic) MOA: able to transport cations across lipid membranes of cells in an electroneutral (i.e. nondepolarizing) exchange, playing an important role as an Na+/H+ antiporter. RESISTANCE: Develops slowly. Crossresistance among monovalent ionophores ANTIMICROBIAL SPECTRUM: Eimeria spp. (mainly against extracellular sporozoites, merozoites, 1. schizonts) and toxoplasmas, Some G-positive bacteria, Gram+ cocci, Clostridia plus B. hyodysenteriae and Campylobacter spp. PK: Absorption from GI tract is rapid and complete. (Ru 50%). Rapidly and extensively metabolized by liver P450 enzymes. Very low plasma tissue levels. Excretion: Bile and faeces SE: Results include skeletal muscle and cardiac muscle dysfunction, anorexia, ataxia, diarrhoea, sudden death. INDICATION: For chemoprophylaxis (CHPR) of coccidiosis by continuous administration in feed for broilers, turkeys, rabbits. Prevention of ketosis CONTRAINDICATION: Inhibition of P450 enzymes by tiamulin and certain macrolides decreases hepatic detoxification and can lead to ionophore poisoning

Answer 153

GROUP: Anticoccidials (monovalent ionophore) STRUCTURE: Monoglycoside (lipophilic) MOA: able to transport cations across lipid membranes of cells in an electroneutral (i.e. nondepolarizing) exchange, playing an important role as an Na+/H+ antiporter. RESISTANCE: Develops slowly. Crossresistance among monovalent ionophores ANTIMICROBIAL SPECTRUM: Eimeria spp. (mainly against extracellular sporozoites, merozoites, 1. schizonts) and toxoplasmas, Some G-positive bacteria, Gram+ cocci, Clostridia plus B. hyodysenteriae and Campylobacter spp. PK: Absorption from GI tract is rapid and complete. (Ru 50%). Rapidly and extensively metabolized by liver P450 enzymes. Very low plasma tissue levels. Excretion: Bile and faeces SE: Results include skeletal muscle and cardiac muscle dysfunction, anorexia, ataxia, diarrhoea, sudden death. INDICATION: For chemoprophylaxis (CHPR) of coccidiosis by continuous administration in feed for broilers, rabbits. Lowest LD50 value CONTRAINDICATION: Inhibition of P450 enzymes by tiamulin and certain macrolides decreases hepatic detoxification and can lead to ionophore poisoning

Answer 154

GROUP: Anticoccidials (monovalent ionophore) STRUCTURE: Monoglycoside (lipophilic) MOA: able to transport cations across lipid membranes of cells in an electroneutral (i.e. nondepolarizing) exchange, playing an important role as an Na+/H+ antiporter. RESISTANCE: Develops slowly. Crossresistance among monovalent ionophores ANTIMICROBIAL SPECTRUM: Eimeria spp. (mainly against extracellular sporozoites, merozoites, 1. schizonts) and toxoplasmas, Some G-positive bacteria, Gram+ cocci, Clostridia plus B. hyodysenteriae and Campylobacter spp. PK: Absorption from GI tract is rapid and complete. (Ru 50%). Rapidly and extensively metabolized by liver P450 enzymes. Very low plasma tissue levels. Excretion: Bile and faeces SE: Results include skeletal muscle and cardiac muscle dysfunction, anorexia, ataxia, diarrhoea, sudden death. INDICATION: For chemoprophylaxis (CHPR) of coccidiosis by continuous administration in feed for broilers. Medium toxicity. CONTRAINDICATION: Inhibition of P450 enzymes by tiamulin and certain macrolides decreases hepatic detoxification and can lead to ionophore poisoning

Answer 155

GROUP: Anticoccidial (divalent ionophore) STRUCTURE: Monoglycoside (lipophilic) MOA: able to transport cations across lipid membranes of cells in an electroneutral (i.e. nondepolarizing) exchange, playing an important role as an Na+/H+ antiporter. RESISTANCE: Develops slowly. Crossresistance among monovalent ionophores ANTIMICROBIAL SPECTRUM: Eimeria spp. (mainly against extracellular sporozoites, merozoites, 1. schizonts) and toxoplasmas, Some G-positive bacteria, Gram+ cocci, Clostridia plus B. hyodysenteriae and Campylobacter spp. PK: Absorption from GI tract is rapid and complete. (Ru 50%). Rapidly and extensively metabolized by liver P450 enzymes. Very low plasma tissue levels. Excretion: Bile and faeces SE: Results include skeletal muscle and cardiac muscle dysfunction, anorexia, ataxia, diarrhoea, sudden death. INDICATION: For chemoprophylaxis (CHPR) of coccidiosis by continuous administration in feed for broilers, turkeys, game birds. Low LD50 value. Can be combined with tiamulin CONTRAINDICATION: Inhibition of P450 enzymes by tiamulin and certain macrolides decreases hepatic detoxification and can lead to ionophore poisoning

Answer 156

GROUP: Anticoccidial (divalent ionophore) STRUCTURE: Monoglycoside (lipophilic) MOA: able to transport cations across lipid membranes of cells in an electroneutral (i.e. nondepolarizing) exchange, playing an important role as an Na+/H+ antiporter. RESISTANCE: Develops slowly. Crossresistance among monovalent ionophores ANTIMICROBIAL SPECTRUM: Eimeria spp. (mainly against extracellular sporozoites, merozoites, 1. schizonts) and toxoplasmas, Some G-positive bacteria, Gram+ cocci, Clostridia plus B. hyodysenteriae and Campylobacter spp. PK: Absorption from GI tract is rapid and complete. (Ru 50%). Rapidly and extensively metabolized by liver P450 enzymes. Very low plasma tissue levels. Excretion: Bile and faeces SE: Results include skeletal muscle and cardiac muscle dysfunction, anorexia, ataxia, diarrhoea, sudden death. INDICATION: For chemoprophylaxis (CHPR) of coccidiosis by continuous administration in feed for broilers, turkeys. High LD50 value. CONTRAINDICATION: Inhibition of P450 enzymes by tiamulin and certain macrolides decreases hepatic detoxification and can lead to ionophore poisoning

Answer 157

GROUP: Coccidiostat (quinazoline derivative) STRUCTURE: Halogenated semisynthetic derivative of Febrifugin. MOA: Unknown MODA: ? ANTIMICROBIAL SPECTRUM: Active against asexual stages of all avian coccidia. SE: Causes skin tear in chickens (collagen synthesis ↓) INDICATION: For prevention in chickens and turkeys. Calves: therapy (prevention) of cryptosporidiosis. CONTRAINDICATION: Small margin of safety. Layers, waterfowls are sensitive

Answer 158

GROUP: Triazine derivative (antiprorozoal) MODA: It is active against all intracellular stages, asexual stages of coccidia by inhibiting nuclear division of schizonts and microgamonts and by inhibiting the wall-forming bodies of macrogamonts. Inhibits sporulation. ANTIMICROBIAL SPECTRUM: Active against asexual stages of all avian coccidia. PK: Symmetrical triazinone, soluble in water, persist a long time in tissues, long wp ( 2 weeks in chicken and 11 weeks in pigs), but it is a safe drug SE: Causes skin tear in chickens (collagen synthesis ↓) INDICATION: Mainly for treatment of coccidiosis in chickens, turkeys, pigs, puppies, calves, and lambs. Metaphylactic use in chicken

Answer 159

GROUP/ STRUCTURE: Antiprotozoal, Carbanilide derivatives (monovalent) MOA: Unknown PK: The agents are absorbed separately from the digestive tract SE: Reduced egg production, egg weight, hatchability, growth INDICATION: For coccidiosis prevention, used in broilers CONTRAINDICATION: Should be used in starting period only(?) NOTES: Combination with Narasin or with Semduramicin

Answer 160

GROUP: Pyridinol (anticoccidial) RESISTANCE: Slight/rare PK: Water insoluble INDICATION: Active against the sporozoite stage, allowing host cell penetration but not parasite development. It also has activity against second-generation schizogony, gametogony, and sporulation. It is used as an prophylactic agent in cheickens and turkeys. NOTE: 5 day wp, transmitted to eggs of hens

Answer 161

GROUP: Lincosamides STRUCTURE: Pyrrolidine ring linked to a pyranose moiety via an amide bond MOA: Pyrrolidine ring linked to a pyranose moiety via an amide bond MODA: Bacteriostatic RESISTANCE: Exhibit cross resistance with macrolides and phenicols; fastidious Gram negative bacteria are ab ovo resistant ANTIMICROBIAL SPECTRUM: Almost all Gram positive bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus, Enterococcus etc.. Anaerobic Gram negative bacteria: Proteus, Bacteroides, Fusobacterium, Campylobacter, Brachyspira hyodysenteriae, Lawsonia intracellularis, Mycoplasma PK: Good absorption, excellent distribution and especially good at reaching the bones; does not cross the BBB but achieves very high intracellular concentrations; metabolised in the liver and excreted via the bile and urine SE: Severe tissue irritation, most toxic antibiotics for intestinal flora and cause dysbacteriosis and fatal enterocolitis in adult horses, rabbits and herbivorous rodents (guinea pigs, chinchillas, hamsters, gerbils) INDICATION: Osteomyelitis cases after bone surgery, Bone Marrow infections (often Staphylococcus aureus), moderate effectiveness against Mycoplasma infections and toxoplasmosis CONTRAINDICATION: Never combine with other 50S inhibitors (macrolides, pleuromutilins, phenicols); these drugs may never be used in Eq, rabbits and herbivorous rodents (v. toxic); not to be used to treat UTIs NOTES: More active than Lincomycin and mostly used PO in companion animals to treat oral cavity infections, especially anaerobic infections; also used against Gram positive dermatitis and to treat abscesses, osteomyelitis and anal sacculitis

Answer 162

GROUP: Sulphonamides (systemic short-acting) STRUCTURE: Para -Aminosulfonamides with poor solubility in acids and often administered as alkaline sodium salts (except for sulfacetamide which can be used in native form) MOA: Inhibit bacterial dihydropteroate synthetase by competing with PABA MODA: Bacteriostatic RESISTANCE: Ab ovo resistant : Mycobacteria, Mycoplasma, Coxiella, Clostridia, Rickettsiae, Pseudomonas aeruginosa, Leptospira, Borrelia, Brachyspira, Treponema, Peptostreptococcus, Chromosomal mutation, plasmid and integronmediated resistance, decreased penetration, PABAspecific enzyme mutation and overproduction of PABA are all mechanisms of resistance ANTIMICROBIAL SPECTRUM: Most susceptible: Bacillus, Brucella, Erysipelothrix, Listeria, Nocardia, Streptococcus, Chlamydophilae & Coccidia, Toxoplasma, Sarcocystis, Pneumocystis and Cryptosporidium spp. Moderately susceptible: Staphylococcus, Enterococcus, E. coli, Klebsiella, Proteus, Actinobacillus, Haemophilus PK: Administered as feed additives, PO, topically, intrauterine, IM/SC; good absorption after PO administration, penetrates BBB well; inhibited by purulent materials; can form crystalline metabolites in the kidneys and urinary tracts of cats, excreted via the kidney both in active and metabolised forms SE: Crystalluria, haematuria, crystal nephrosis (especially in Fe), idiosyncratic immune reactions, idiosyncratic hepatotoxicity, allergy (especially in Doberman Pinschers), keratoconjunctivitis sicca INDICATION: Systemic and Organ Infections, Respiratory Infections by Bordetella bronchiseptica & Actinobacillus pleuropneumoniae, GI infections (E. coli, Salmonella), UTIs, Metritis, Mastitis, Agalactia, Foot Rot, Prostatitis, Meningitis and toxoplasmosis CONTRAINDICATION: Very large MIC compared to antibiotics

Answer 163

GROUP: Tetracyclines (long-acting) STRUCTURE: Linear fused tetracyclic nucleus MOA: Passively diffuse through porin channels in the bacterial membrane and inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration it is bactericidal RESISTANCE: ab ovo: Pseudomonas aeruginosa. Acquired: E. coli, Salmonella, Pasteurella multocida, Mannheimia haemolytica, Staphylococcus aureus, Streptococci ANTIMICROBIAL SPECTRUM: Intracellular bacteria: Chlamydophilae, Rickettsia, Ehrlichia, Lawsonia, etc. Mycoplasma haemofelis, Bordetella bronchiseptica, Wolbachia, Plasmodium & Entamoeba histolytica. Almost all Gram positive Bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus etc... Enterobacteriaceae: E. coli, Salmonella, Klebsiella Anaerobics: Bacteroides, Fusobacterium, Proteus Spirochaetes: Leptospira, Borrelia. Toxoplasmosis! PK: More lipophilic with excellent absorption, penetrate bone, low degree of metabolism and mainly excreted via the large intestine in the bile SE: Tissue irritant, vomiting, diarrhea, hepatoxicity, impairment of bone growth in very young animals INDICATION: General infections, most respiratory infections, bronchopneumonia, foot diseases, metritis, mastitis, Mycoplasma respiratory infections in Ru/Su/Av, Infectious keratoconjunctivitis in Bo NOTES: First choice against Lyme disease, lethal proliferative enteropathy in horse

Answer 164

GROUP: Benziimidazole (carbamate) STRUCTURE: Synthetic benzimidazole derivative MOA: Inhibition of tubulin polymerization -- > binding to colchicine sensitive site of tubulin RESISTANCE: Recently more frequent. Ruminants, GI roundworms, frequently as multiple resistance against BZs. In horse: Large strongyles, and in swine: Oesophago-stomum spp ANTIHELMNINTIC SPECTRUM: Antinematodal effect (AN): Broad spectrum of activity against roundworms. It also has larvicidal and ovicidal effect. Anticestodal effect (AC): Against tapeworms Antitrematodal effect (AT): Dicrocoelium, Paramphistomum spp.) (only for adult stages) PK: Absorption from GI, reversibly oxidized to its sulphoxide (which gives poor binding to parasite β-tubulin. Excretion in bile and elimination via faeces SE: PO relatively safe, teratogenicity, hepatotoxicity, neurotoxicity INDICATION: Given PO as a suspension, paste, bolus or premix in slow release capsule (105 days in ruminants), other uses: Antitumor, antifungal, antiviral, antiparasitic. NOTES: Has been shown to inhibit the enzyme fumarate reductase, which is helminth specific. WP is 8-14 days for meat, except boluses which are more than 3 months.

Answer 165

GROUP: Proenzimidazole (prodrug) and banzimidazole carbamate STRUCTURE: Benzimidazole carbamate MOA: Inhibition of tubulin polymerization -- > binding to colchicine sensitive site of tubulin RESISTANCE: Recently more frequent. Ruminants, GI roundworms, frequently as multiple resistance against BZs. In horse: Large strongyles, and in swine: Oesophago-stomum spp ANTIHELMNINTIC SPECTRUM: Antinematodal effect (AN): Broad spectrum of activity against roundworms. It also has larvicidal and ovicidal effect. Anticestodal effect (AC): Against tapeworms PK: Limited absorption from GI. Excretion in bile and elimination via faeces SE: PO relatively safe, teratogenicity, hepatotoxicity, neurotoxicity INDICATION: Given PO as a suspension, paste, bolus or premix in slow release capsule (140 days in sheep and goat), other uses: Antitumor, antifungal, antiviral, antiparasitic. NOTES: High levels and repeated administration may be necessary in horse. WP is 8-14 days for meat, except boluses which are more than 3 months.

Answer 166

GROUP: Probenzimidazole (prodrug) STRUCTURE: Halogenated benzimidazole carbamate MOA: Inhibition of tubulin polymerization -- > binding to colchicine sensitive site of tubulin RESISTANCE: Recently more frequent. Ruminants, GI roundworms, frequently as multiple resistance against BZs. In horse: Large strongyles, and in swine: Oesophago-stomum spp ANTIHELMNINTIC SPECTRUM: Antinematodal effect (AN): Broad spectrum of activity against roundworms. It also has larvicidal and ovicidal effect. Anticestodal effect (AC): Against tapeworms PK: Limited absorption from GI. Excretion in bile and elimination via faeces SE: PO relatively safe, teratogenicity, hepatotoxicity, neurotoxicity INDICATION: Given PO as a suspension, paste, bolus or premix to horse, cats, dogs and ruminants, other uses: Antitumor, antifungal, antiviral, antiparasitic. CONTRAINDICATION: Might be necessary with off-label use in horse and WP is 8-14 days for meat, except boluses which are more than 3 months.

Answer 167

GROUP: Benzimidazole carbamate STRUCTURE: Halogenated benzimidazole carbamate MOA: Inhibition of tubulin polymerization -- > binding to colchicine sensitive site of tubulin RESISTANCE: Recently more frequent. Ruminants, GI roundworms, frequently as multiple resistance against BZs. In horse: Large strongyles, and in swine: Oesophago-stomum spp ANTIHELMNINTIC SPECTRUM: Antinematodal effect (AN): Broad spectrum of activity against roundworms. It also has larvicidal and ovicidal effect. Anticestodal effect (AC): Against tapeworms PK: Limited absorption from GI. Excretion in bile and elimination via faeces SE: PO relatively safe, teratogenicity, hepatotoxicity, neurotoxicity INDICATION: They are given PO as a suspension, paste, bolus or premix to cats and dogs (roundworms, hookworms and tapeworms), swine (nematodes) and poultry (GI and respiratory nematodes). Other effects: antitumor, antifungal, antiviral and anti-parasitic. CONTRAINDICATION: WP is 8-14 days for meat, except boluses which are more than 3 months.

Answer 168

GROUP: Benzimidazole carbamate STRUCTURE: Halogenated benzimidazole carbamate MOA: Inhibition of tubulin polymerization -- > binding to colchicine sensitive site of tubulin RESISTANCE: Recently more frequent. Ruminants, GI roundworms, frequently as multiple resistance against BZs. In horse: Large strongyles, and in swine: Oesophago-stomum spp ANTIHELMNITIC SPECTRUM: Anti-trematodal: Only effective in liver fluke (Fasciola hepatica), effective against both immature and adult flukes PK: Limited absorption from GI. Excretion in bile and elimination via faeces SE: PO relatively safe, teratogenicity, hepatotoxicity, neurotoxicity INDICATION: They are given PO as a suspension, paste, bolus or premix to cats and dogs (roundworms, hookworms and tapeworms), swine (nematodes) and poultry (GI and respiratory nematodes). Other effects: antitumor, antifungal, antiviral and anti-parasitic. CONTRAINDICATION: WP is 8-14 days for meat, except boluses which are more than 3 months.

Answer 169

GROUP: Imidathiazole STRUCTURE: L-isomer form MOA: As agonists at nicotinic acetylcholine receptors of nematodes they are ganglion stimulant. RESISTANCE: Frequently for GI nematodes of cattle and sheep. Nematodes resistant to Levamisole are cross-resistant to Morantel ANTIHELMNITHIC SPECTRUM: Antinematodal effect (AN): Broad spectrum of activity adulticidal (Heartworm - D. immitis). Larvicidal activity – only against migrating stage. They have no activity against hypobiotic larvae, flukes and tapeworms PK: The absorption and excretion are rapid. In cattle, peak blood levels. Excretion via urine, short WP for milk and meat SE: Lower TI, Cats, Horses, and certain dog breeds (e.g. Kuvasz) are very sensitive. Cholinergictype signs of salivation, muscle tremors, ataxia, urination, defecation. INDICATION: Lungworms, pig GI-roundworms, poultry GI- roundworms and poultry gapeworms NOTE: Antidote: Atropine

Answer 170

GROUP: Carbox-amidine MOA: Cholinomimetic activity, ganglionstimulant, interaction with parasitic nerve transmission, leading to spastic paralysis. RESISTANCE: Limited or no activity against migrating larvae, and Trichuris spp. (whipworms) ANTIHELMNITIC SPECTRUM: Antinematodal effect (AN): Broad spectrum of activity against roundworms. Adult gut worms and larval stages that dwell in the lumen or on the mucosal surface. PK: Pyrantel tartrate (or citrate) is well absorbed by pigs and dogs, less well by ruminants. The pamoate salt is poorly soluble in water; this offers the advantage of reduced absorption from the gut. Excretion: Urine, (unchanged drug is excreted in the faeces) Metabolism of pyrantel is rapid. SE: Cholinergictypes of signs. INDICATIONS: Used for parasite control: GI roundworms: Parascaris, Strongylus, Oxyuris ANTIDOTE: Atropine

Answer 171

GROUP: Macrocyclic lactone (avermectin) and endectoside MOA: Potentiation of inhibitory transmitters by binding to glutamate and GABA-gated chloride channel RESISTANCE: Spreading, cross-resistance. Multiple resistance against BZs and Levamisole ANTIHELMNITIC SPECTRUM: Adult, immature nematodes, including hypobiotic larvae, microfilariae + arthropods PK: 93% protein binding (BBB), Excreted almost exclusively in the feces, Moderately well absorbed, lipophilic compounds. Accumulation in fatty tissue, long lasting effect SE: Nervous system signs (idiosyncratic reactions) including depression, muscle weakness, blindness, coma, and death INDICATION: Both endo and ectoparasites CONTRAINDICATION: Narrow TI. Toxic in MDR-1 gene breeds

Answer 172

GROUP: Macrocyclic lactone (avermectin) and endectoside MOA: Potentiation of inhibitory transmitters by binding to glutamate and GABA-gated chloride channel RESISTANCE: Spreading, cross-resistance. Multiple resistance against BZs and Levamisole ANTIHELMNITIC SPECTRUM: Adult, immature nematodes, including hypobiotic larvae, microfilariae + arthropods PK: 93% protein binding (BBB), Excreted almost exclusively in the feces, Moderately well absorbed, lipophilic compounds. Accumulation in fatty tissue, long lasting effect, with low TI SE: Nervous system signs (idiosyncratic reactions) including depression, muscle weakness, blindness, coma, and death INDICATION: Both endo and ectoparasites

Answer 173

GROUP: Macrocyclic lactone (avermectin) and endectoside MOA: Potentiation of inhibitory transmitters by binding to glutamate and GABA-gated chloride channel RESISTANCE: Spreading, cross-resistance. Multiple resistance against BZs and Levamisole ANTIHELMNITIC SPECTRUM: Adult, immature nematodes, including hypobiotic larvae, microfilariae + arthropods PK: 93% protein binding (BBB), Excreted almost exclusively in the feces, Moderately well absorbed, lipophilic compounds. Accumulation in fatty tissue, long lasting effect, with low TI SE: Nervous system signs (idiosyncratic reactions) including depression, muscle weakness, blindness, coma, and death INDICATION: Both endo and ectoparasites

Answer 174

GROUP: Macrocyclic lactone (avermectin) and endectoside MOA: Potentiation of inhibitory transmitters by binding to glutamate and GABA-gated chloride channel RESISTANCE: Spreading, cross-resistance. Multiple resistance against BZs and Levamisole ANTIHELMNITIC SPECTRUM: Adult, immature nematodes, including hypobiotic larvae, microfilariae + arthropods PK: 93% protein binding (BBB), Excreted almost exclusively in the feces, Moderately well absorbed, lipophilic compounds. Accumulation in fatty tissue, long lasting effect, with low TI SE: Nervous system signs (idiosyncratic reactions) including depression, muscle weakness, blindness, coma, and death INDICATION: Both endo and ectoparasites

Answer 175

GROUP: Macrocyclic lactone (milbemycins) and endectoside MOA: Potentiation of inhibitory transmitters by binding to glutamate and GABA-gated chloride channel RESISTANCE: Spreading, cross-resistance. Multiple resistance against BZs and Levamisole ANTIHELMNITIC SPECTRUM: Adult, immature nematodes, including hypobiotic larvae, microfilariae + arthropods PK: 93% protein binding (BBB), Excreted almost exclusively in the feces, Moderately well absorbed, lipophilic compounds. Accumulation in fatty tissue, long lasting effect, with low TI SE: Nervous system signs (idiosyncratic reactions) including depression, muscle weakness, blindness, coma, and death INDICATION: Both endo and ectoparasites

Answer 176

GROUP: Macrocyclic lactone (milbemycins) and endectoside MOA: Potentiation of inhibitory transmitters by binding to glutamate and GABA-gated chloride channel RESISTANCE: Spreading, cross-resistance. Multiple resistance against BZs and Levamisole ANTIHELMNITIC SPECTRUM: Adult, immature nematodes, including hypobiotic larvae, microfilariae + arthropods PK: 93% protein binding (BBB), Excreted almost exclusively in the feces, Moderately well absorbed, lipophilic compounds. Accumulation in fatty tissue, long lasting effect, with low TI SE: Nervous system signs (idiosyncratic reactions) including depression, muscle weakness, blindness, coma, and death INDICATION: Both endo and ectoparasites

Answer 177

GROUP: Organophosphates STRUCTURE: Phosphate MOA: Irreversible inhibition of AChE! Muscarinic ACh receptors, Nicotinic ACh receptors. Central nervous system ANTIMICROBIAL SPECTRUM: Broad-spectrum ectoparasiticides, fleas, ticks, lice, mites, myiasis mostly for dipping PK: Highly lipophilic. Good absorption, Excellent distribution (special barriers, BBB), Metabolism (partial activation), Excretion (80% urine metabolites, 20% feces), Long half-time. Dermal absorption: Large, lipophilic molecules SE: SLUDGE (salivation, lacrimation, urination, diarrhea, GI pain, emesis), Muscle tremor, spasms (nicotinic Ach receptors) INDICATION: Against fleas, ticks, lice, mites, myiasis CONTRAINDICATION: Cats are sensitive, so be careful with the dosaging and application ANTIDOTE: Atropine

Answer 178

GROUP: Organophosphates STRUCTURE: Phosphate MOA: Irreversible inhibition of AChE! Muscarinic ACh receptors, Nicotinic ACh receptors. Central nervous system ANTIMICROBIAL SPECTRUM: Broad-spectrum ectoparasiticides, fleas, ticks, lice, mites, myiasis mostly for dipping PK: Highly lipophilic. Good absorption, Excellent distribution (special barriers, BBB), Metabolism (partial activation), Excretion (80% urine metabolites, 20% feces), Long half-time. Dermal absorption: Large, lipophilic molecules SE: SLUDGE (salivation, lacrimation, urination, diarrhea, GI pain, emesis), Muscle tremor, spasms (nicotinic Ach receptors) INDICATION: Varroosis of honey bees, vaporizers and fumigant strips CONTRAINDICATION: Cats are sensitive, so be careful with the dosaging and application ANTIDOTE: Atropine

Answer 179

GROUP: Carbamate STRUCTURE: Cyclic or aliphatic derivatives of carbamic acid MOA: Similar to organophosp hates but inhibition is by carbamylation and reaction is slowly reversible PK: Less lipophilic, so better for the skin. INDICATIONS: Fleas, ticks, come as collars, aerosol, sprays and shampoos. Much safer than organophosphates

Answer 180

GROUP: Pyrethroids (2nd gen) MOA: The main target is the gating kinetics of Na+ channels in nerves, which results in repetitive discharges or membrane depolarization and ultimately death of the ectoparasite RESISTANCE: Resistance is common in fleas and it has Poor efficacy against mange mites ANTIMICROBIAL SPECTRUM: Ticks and varroosis in honey bees PK: Dermal absoprtion is limited, lipophilic, metablized in blood and liver SE: Tremors, seizures, excitation + local irritation and allergic reactions INDICATION: Used against ticks, and has moderate efficacy against Varroa mites CONTRAINDICATION: Fish are especially sensitive and there is NO antidote available NOTE: Safe in warm-blooded animals

Answer 181

GROUP: Pyrethroids (2nd gen) MOA: The main target is the gating kinetics of Na+ channels in nerves, which results in repetitive discharges or membrane depolarization and ultimately death of the ectoparasite RESISTANCE: Resistance is common in fleas and it has Poor efficacy against mange mites ANTIMICROBIAL SPECTRUM: Ticks and varroosis in honey bees PK: Dermal absoprtion is limited, lipophilic, metablized in blood and liver SE: Tremors, seizures, excitation + local irritation and allergic reactions INDICATION: Used against ticks, and has moderate efficacy against Varroa mites CONTRAINDICATION: Fish are especially sensitive and there is NO antidote available NOTE: Safe in warm-blooded animals

Answer 182

GROUP: Pyrethroids (2nd gen) MOA: The main target is the gating kinetics of Na+ channels in nerves, which results in repetitive discharges or membrane depolarization and ultimately death of the ectoparasite RESISTANCE: Resistance is common in fleas and it has Poor efficacy against mange mites ANTIMICROBIAL SPECTRUM: Ticks and varroosis in honey bees PK: Dermal absoprtion is limited, lipophilic, metablized in blood and liver SE: Tremors, seizures, excitation + local irritation and allergic reactions INDICATION: Used against ticks, and has moderate efficacy against Varroa mites CONTRAINDICATION: Fish are especially sensitive and there is NO antidote available NOTE: Safe in warm-blooded animals

Answer 183

GROUP: Formamidine MOA: Inhibits monamine oxidase (MAO) that normally metabolize neurotransmitter amines present in the CNS of ticks and mites ANTIMICROBIAL SPECTRUM: Mange, mites, demodex and ticks. Varroa mites, sarcoptes, psoroptes, and otodectes mites. PK: Moderate absorption (p.o. 13% > dermal), Half-life: 23 hours in dogs ( dogs are very sensitive to amitraz poisoning). SE: Sedation, Bradycardia, Hypothermia, Emesis is especially seen in cats INDICATION: Mange, mites, demodex and ticks. Varroa mites, sarcoptes, psoroptes, and otodectes mites. Used as dipping solution CONTRAINDICATION: Small therapeutic index in cats, horses, chihuahua. Should be kept in a dark bottle and not be exposed to air (in a fridge) ANTIDOTE: Atipamezole

Answer 184

GROUP: Phenylpyrazole MOA: Acts on the central nervous system where it appears to be primarily effective in noncompetitively blocking the passage of chloride ions through GABA gated and glutamate gated chloride channels in ectoparasites ANTIMICROBIAL SPECTRUM: As a topical spray is effective against adult fleas, all stages of brown dog ticks, American dog tick, lone star ticks, and deer ticks. PK: Good distribution in skin, good residual activity, minimal systemic effect SE: Minimal toxicity BUT at toxic doses, it can cause hyperactivity, hyperexcitability, and convulsions. INDICATION: Spot on/ spray against ticks and fleas CONTRAINDICATION: Signs of excitation in rabbits

Answer 185

GROUP: Neonicotinoids (1st gen) STRUCTURE: Chloronicotinyls MOA: Mimics the effects of ACh by competitive inhibition at the postsynaptic nicotinic acetylcholine receptors (nAChR) ANTIMICROBIAL SPECTRUM: Fleas PK: Very safe, Topical application of imidacloprid to the skin does not result in significant dermal absorption into the blood stream, but rather surface translocation aided by body movement results in whole-body coverage, it has rapid action, lasts for about 4 weeks, SE: Tremors, seizures (?) INDICATION: Used against fleas (collar, spot on) IN COMBINATION: With PERMETHRIN = Advantix to repel and kill ticks too With FLUMETHRIN = Foresto also against ticks With MOXIDECTIN = Advocate which broadens the spectrum against worms

Answer 186

GROUP: Neonicotinoids (3rd gen) STRUCTURE: Chloronicotinyls MOA: Mimics the effects of ACh by competitive inhibition at the postsynaptic nicotinic acetylcholine receptors (nAChR) ANTIMICROBIAL SPECTRUM: Fleas PK: Very safe SE: Tremors, seizures (?) INDICATION: Used against fleas (collar, spot on)

Answer 187

GROUP: Oxadiazine STRUCTURE: Methyl ester MOA: Na+ channel blocker → hyperpolarization so an inhibition of the parasite. ANTIMICROBIAL SPECTRUM: Adult fleas, larvae, and eggs INDICATION: Adult fleas, larvae, and eggs (in cats and dogs only) PK: Once fleas are exposed to indoxacarb, it is rapidly cleaved to its decarbomethoxylated metabolite, which appears to be a potent blocker of voltage-gated sodium ion channels in fleas. It is slow-acting

Answer 188

GROUP: Isoxazolines MOA: Inhibit GABAgated chloride ion channel inhibitors with nanomolar potency ANTIMICROBIAL SPECTRUM: Against fleas and ticks, mange mites and demodex spp PK: Low systemic clearance, large Vd, long half-life, low oral bioavailability, high plasma protein binding, slow metabolism, enterohepatic circulation, accumulation in adipose tissues. Excreted in bile. SE: RARE! Although vomiting, diarrhea, lethargy, and anorexia have been observed INDICATION: and ticks, mange mites and demodex spp. Given PO (and IV?). Fluralaner is also used in Dermanyssus gallinae in poultry. CONTRAINDICATION: In MDR-1 mutant animal species. Agents have not been evaluated in pregnant or lactating animals!

Answer 189

GROUP: Isoxazolines MOA: Inhibit GABAgated chloride ion channel inhibitors with nanomolar potency ANTIMICROBIAL SPECTRUM: Against fleas and ticks, mange mites and demodex spp PK: Low systemic clearance, large Vd, long half-life, low oral bioavailability, high plasma protein binding, slow metabolism, enterohepatic circulation, accumulation in adipose tissues. Excreted in kidneys. SE: RARE! Although vomiting, diarrhea, lethargy, and anorexia have been observed INDICATION: and ticks, mange mites and demodex spp. Given PO (and IV?). Fluralaner is also used in Dermanyssus gallinae in poultry. CONTRAINDICATION: In MDR-1 mutant animal species. Agents have not been evaluated in pregnant or lactating animals!

Answer 190

GROUP: Isoxazolines MOA: Inhibit GABAgated chloride ion channel inhibitors with nanomolar potency ANTIMICROBIAL SPECTRUM: Against fleas and ticks, mange mites and demodex spp PK: Low systemic clearance, large Vd, long half-life, low oral bioavailability, high plasma protein binding, slow metabolism, enterohepatic circulation, accumulation in adipose tissues. Excreted in bile. SE: - 3x overdose: tremors, ataxia - 5x overdose: seizures, tremors, ataxia INDICATION: and ticks, mange mites and demodex spp. Given PO (and IV?). Fluralaner is also used in Dermanyssus gallinae in poultry. CONTRAINDICATION: In MDR-1 mutant animal species. Agents have not been evaluated in pregnant or lactating animals!

Answer 191

GROUP: Isoxazolines MOA: Inhibit GABAgated chloride ion channel inhibitors with nanomolar potency ANTIMICROBIAL SPECTRUM: Against fleas and ticks, mange mites and demodex spp PK: Low systemic clearance, large Vd, long half-life, low oral bioavailability, high plasma protein binding, slow metabolism, enterohepatic circulation, accumulation in adipose tissues. Excreted in bile. SE: - 3x overdose: tremors, ataxia - 5x overdose: seizures, tremors, ataxia INDICATION: and ticks, mange mites and demodex spp. Given PO (and IV?). Fluralaner is also used in Dermanyssus gallinae in poultry. CONTRAINDICATION: In MDR-1 mutant animal species. Agents have not been evaluated in pregnant or lactating animals! NOTE: Newest isoxazolines

Answer 192

GROUP: Insect growth regulators STRUCTURE: Juvenile hormone analogues MOA: Falsely signals insect to remain in immature stage. Inhibition of chitin synthesis! ANTIMICROBIAL SPECTRUM: Ticks, fleas, and flies PK: Light, residual activity: pyriproxyfen > methoprene INDICATION: Used against ticks, fleas and flies, given PO and as spot on

Answer 193

GROUP: Insect growth regulators STRUCTURE: Juvenile hormone analogues MOA: Falsely signals insect to remain in immature stage. Inhibition of chitin synthesis! ANTIMICROBIAL SPECTRUM: Ticks, fleas, and flies PK: Light, residual activity: pyriproxyfen > methoprene INDICATION: Used against ticks, fleas and flies, given PO and as spot on

Answer 194

GROUP: Allyamine (squalene epoxidase inhibitors) MOA: Squalene to ergosterol conversion is inhibited → squalene accumulation (toxic metabolite) → weakens cell membranes → prevents formation of lanosterol → fungicidal ANTIFUNGAL SPECTRUM: Dermatophytes + yeasts PK: High oral bioavailability, highly lipophilic, given PO or applied topically, local and systemic. SE: Nephrotoxicity, mild-moderate hepatotoxicity, accumulates in the skin and nails INDICATION: Dermatomycosis, onychomycosis. Microsporum spp., Trichophyton spp., Candida spp., Malassezia spp. IN COMBINATION: Itraconazole

Answer 195

GROUP: Polyene antibiotic STRUCTURE: Polyene MOA: Membrane disruption → bind to ergosterol binding site → complex-formation→ permeability changes. K+ efflux, H+ influx → acidic pH amino acids and sugars leave the cell. Fungistatic → fungicidal effect ANTIFUNGAL SPECTRUM: Yeasts, decreased against dermatophytes. Some protozoa (Leishmania spp.) RESISTANCE: Rare - develops slowly PK: Bad PO absorption INDICATION: It can be given orally as a “topical” treatment for oral and intestinal candidiasis, particularly in exotic animal species. CONTRAINDICATION: Very toxic NOTES: In veterinary medicine, it is most commonly used in combination with antibiotics (neomycin, thiostrepton) and antiinflammatory (triamcinolone) drugs in ointments

Answer 196

GROUP: Imidazole MOA: Membrane disruption: conversion of lanosterol → ergosterol is inhibited. Selective toxicity (fungal cell membrane), but to some degree cell can also be affected ANTIFUNGAL SPECTRUM: Dermatophytes, Yeasts (Malassezia spp. very sensitive) PK: Following local administration only the corium can be reached, maybe subcutaneous tissue, absorption <2% INDICATION: It has been used for treatment of nasal aspergillosis in dogs. Active ingredient of ear drops, shampoo, and topical solutions IN COMBINATION: Found in combination with gentamicin sulfate and betamethasone valerate

Answer 197

GROUP: Imidazole MOA: Membrane disruption: conversion of lanosterol → ergosterol is inhibited. Selective toxicity (fungal cell membrane), but to some degree cell can also be affected ANTIFUNGAL SPECTRUM: Dermatophytes, Yeasts (Malassezia spp. very sensitive) PK: Rapid clearance, poor oral absorption, INDICATION: In veterinary medicine, miconazole is used as a 2% cream or 1% spray or lotion for the treatment of dermatophytosis in dogs and cats. It is also commonly compounded as a 1% solution for topical treatment of keratomycosis. Active ingredient of ear drops, shampoo, and topical solutions. IN COMBINATION: Can also be found combined with chlorhexidine as a shampoo for the adjunct treatment of dermatophytosis in animals

Answer 198

GROUP: Imidazole MOA: Membrane disruption: conversion of lanosterol → ergosterol is inhibited. Selective toxicity (fungal cell membrane), but to some degree cell can also be affected ANTIFUNGAL SPECTRUM: Broad spectrum against dermatophytes and yeast. PK: Little penetration into CSF and urine SE: Causes hepatotoxicity - oral usage should be limited, and not suitable for liver insufficient patients, must always check their liver parameters before treatment. Approx 20%: Nausea and vomiting INDICATION: Cushing syndrome CONTRAINDICATION: Liver patients

Answer 199

GROUP: Triazoles MOA: Membrane disruption: conversion of lanosterol → ergosterol is inhibited. Selective toxicity (fungal cell membrane), but to some degree cell can also be affected PK: Highly lipophilic, weak base (Pka 3.7). Given PO but need acidic environment to dissolve (variable absoprtion), should be given with meal. It is also highly protein bound, and it is excreted in urine. ANTIFUNGAL SPECTRUM: Microsporum, Trichophyton, Candida, Malassezia, Sporothrix, Pythium, Histoplasma, Aspergillus, Blastomyces, Coccidioides, and Cryptococcus. It has little activity against Fusarium sp. INDICATION: Given to cats, dogs, horse (it is better tolerated in cats than ketoconazole). Itraconazole has been used to treat ocular and systemic blastomycosis in dogs, as well as aspergillosis and histoplasmosis. SE: GI effects like vomiting, and anorexia in cats

Answer 200

GROUP: Fungistatic antibiotics MOA: Once inside the cell, griseofulvin disrupts the mitotic spindle by interacting with polymerized microtubules, thus causing mitotic arrest in metaphase. This is known as the curling phenomenon. RESISTANCE: Rare/not reported ANTIFUNGAL SPECTRUM: Limited to organisms causing dermatophytosis, Microsporum spp., Trichophyton spp., and Epidermophyton. PK: Given PO as tablets or syrup in small animals and powder formulation or bolus in large animals. Distributes to keratin of skin, hair, and nails and can be detected in the stratum corneum within hours of administration. Should be given with meal (lipophilic?). It is metabolized in liver, to demethylgriseofulvin. SE: In cats: Include leukopenia, anemia, increased hepatic enzyme activity, and neurotoxicosis. INDICATION: Dermatophytosis CONTRAINDICATION: Food producing animals(?) and pregnant cats

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