Most Importante drugzz (A-topiczz) Flashcards
The most important drugs from all the A-topics
A1: ACEPROMAZINE (neuroleptic)
GROUP: Phentothiazine
MOA: Sedation by inhibiting postsynaptic central dopaminergic receptors (alpha 1 receptor)
PK: Large Vd, slow elimination, long wp, metabolise in liver, excretion in urine, bioavailability: PO: 20%. Better rectal or buccal absorption.
SE: Penile prolapse and hypertension in eq, third eyelid prolapse in ca and fe, constipation, and dry mouth, paradoxical reactions, issues with temperature regulation.
INDICATION: Calming, sedation, muscle relaxation, premedication. Catalepsy like immobilization (not really asleep) also antihistaminic activity
CONTRAINDICATION: Food producing , epileptic or pseudopregnant animals. Boxers may be oversensitive
DOSE: Dog: PO: 1-2 mg/kg , IM/IV: 0.2-0.3 mg/kg
Horse: PO: 0.1-0.4 mg/kg , IM/IV: 0.03-0.1 mg/kg
A1: CHLORPROMAZINE (neuroleptic)
GROUP: Phentothiazine
MOA: Block postsynaptic dopamine receptors
SE: Muscle necrosis when given IM. Cause excitation and tachycardia in eq.
INDICATION: Psychotic disorders
CONTRAINDICATION: Not recommended in horses due to extreme ataxia and altered mentation. Avoid use in patients that are dehydrated, hypovolemic, bleeding, or in shock because of the drugs effect on vessel tone (vasodilation).
A1: AZAPERONE (neuroleptic)
GROUP: Butyrophenone
MOA: Dopamine and nor-adrenaline inhibition, anticholinergic effect on CNS
PK: Duration of action 2-4hrs in pigs, longer in older pigs. 13% biotransformed in liver
SE: Penile prolapse in boar, hypothermia
INDICATIONS: Stress reliever, sedation in pigs
A2: XYLAZINE (sedato-hypnotics)
GROUP: A2 agonist
MOA: Presynaptic binding of α2-adrenergic receptors –> decreased release of norepinephrine PK: Fast absorption, good distribution (crosses barriers), metabolize in liver, excretion in urine, works within few mins IV and 10-15 mins IM
SE: Emetic in cats and some dogs, penile prolapse in horse
INDICATION: Provide sedation, chemical restraint, analgesia, used against hyperglycemia and glaucoma CONTRAINDICATION: Boxers/rottweilers
DOSAGE: Dogs and cats: IM, IV, SC; 1-4 mg/kg
Cattle: IV, IM: 0.05- 1mg/kg
Horse: IV 0.5-1mg/kg
A2: DETOMIDINE (sedato-hypnotic)
GROUP: a2 agonist
MOA: Presynaptic binding of α2-adrenergic receptors –> decreased release of norepinephrine
PK: Fast absorbtion, good distribution, IV: immediately, IM: few mins, metabolize in liver, excretion in urine, high bioavailability in cattle (less in eq)
SE: Penile prolapse in eq, hypothermia, diuresis
INDICATION: Provide sedation, chemical restraint, analgesia, good premedication, used in hyperglycemia
IN COMBINATION: With thiopentone, ketamine or opioids
CONTRAINDICATION: Food producing animals
A2: DEXMEDETOMIDINE (sedato-hypnotic)
GROUP: a2 agonist
MOA: Presynaptic binding of α2-adrenergic receptors –> decreased release of norepinephrine
PK: Fast absorbtion, good distribution, IV: immediately, IM: few mins, metabolize in liver, excretion in urine
SE: Vomiting, thermoregulatory issues, constipation, bradychardia
INDICATION: Provide sedation, chemical restraint, analgesia, good premedication, used in hyperglycemia
IN COMBINATION: With thiopentone, ketamine or opioids
CONTRAINDICATION: Food producing animals
DOSE:
Dog: IM, IV 5-10 μg/kg (pre-anaesthesia)
IM, IV 10-20μg/kg (sedation + analgesia)
Cat: IM, IV 40 μg/kg (both doses)
A2: ATIPAMEZOLE (sedato-hypnotics)
GROUP: a2- antagonist
MOA: Competitively binding to the α2-adrenergic receptor (preventing activation)
PK: Highest preference for ɑ2- over ɑ1-receptors, rapid onset (IM:10 mins), first-pass metabolism in liver, excretion in urine
SE: Vomiting, hypersalivation, diarrhea
INDICATIONS: Reverse effect of dexmedetomidine and other toxicities
CONTRAINDICATION: Ketamin-medetomidine
A2: DIAZEPAM (sedato-hypnotics)
GROUP: Benzodiazepines
MOA: Activation of the benzodiazepine binding site on GABAA, which lead to hyperpolarization of the postsynaptic neuron producing decreased neuronal transmission
PK: Highly lipid soluble, good oral absorption, long onset of action IM but fast onset IV and PO, excretion via kidney
SE: Alone: Paradoxical excitement, agitation, vocalization, and dysphoria may be seen after IV or IM administration
INDICATIONS: Epilepsy, anaesthetic induction, muscle relaxants, appetite stimulant in cats, can be used in heart patients
IN COMBINATION: Ketamine and etomidate
CONTRAINDICATION:
- Paradoxical reaction (cat, greyhound)
- Aminoglycosides (inhibition of respiration)
DOSAGE:
Ca: IV: 0.5-2 mg/kg
Fe: IV: 0.5-2 mg/kg
A2: ALPRAZOLAM (sedato-hypnotic)
GROUP: Benzodiazepine
MOA: Amplify inhibitory effects of GABA, nerve inhibtion by allowing Cl- into cell.
PK: Metabolism in liver, more potent than diazepam
SE: Alone: Paradoxical excitement, agitation, vocalization, and dysphoria may be seen after IV or IM administration
INDICATION: Anxiety and panic attacks
A2: MIDAZOLAM (sedato-hypnotic)
GROUP: Benzodiazepines
MOA: Amplify inhibitory effects of GABA, nerve inhibtion by allowing Cl- into cell.
PK: Metabolized in liver, can be absorbed intranasally, no first pass effect, shorter and less sedation than diazepam. Water soluble, but becomes lipid soluble in the body
SE: Decrease respiratory rate, ataxia, weakness
INDICATIONS: Pre-anastethic (w/ ketamine), anti-epileptic (status epilepticus), muscle relaxant
CONTRAINDICATION: Food producing animals and new borns (high liver toxicity)
A2: PHENOBARBITAL (sedato-hypnotic)
GROUP: Barbiturate
MOA: GABAa, decrease Ca2+ accumulation –> inhibits the release of stimulatory neurotransmitters
PK: Respiratory depression, re-distribution in fat and muscle, accumulation in fat, excreted in urine
SE: Respiratory and cardiovascular depression, tissue irritation, liver insufficiency
INDICATION: Epilepsy in dogs (both long- and short term), membrane stabilization, pre-anasthetic, given orally, used in agressive patients and against tetanus in eq
CONTRAINDICATION: Greyhounds
DOSAGE:
Dog: PO: 1.5 -5 mg/kg BID
A2: PENTOBARBITAL (sedato-hypnotic)
GROUP: Barbiturate
MOA: GABAa, decrease Ca2+ accumulation –> inhibits the release of stimulatory neurotransmitters
PK: Respiratory depression, re-distribution in fat and muscle, accumulation in fat, excreted in urine
SE: Respiratory and cardiovascular depression, tissue irritation, liver insufficiency
INDICATION: Good muscle relaxant, combination anesthesia, tetanus in horse, epilepsy in dogs (long-acting)
CONTRAINDICATION: Greyhounds are oversensitive
A3: MORPHINE (opioids)
GROUP: Opioids (full agonist)
MOA: It acts on the µ receptor. In the presynaptic nerve ending these receptors decrease Ca2+ influx prevents release of neurotransmitters from the nerves
PK: Non- water soluble.
Excellent , potent first-pass metabolism, metabolize in liver (morphine–> morphine-glucuronide), TI at 70
SE: Respiratory depression, emesis, excitation/dysphoria, histamine release (should be given with acepromazine), constipation and hyperthermia in cats
INDICATION: Sedation, pain relief (e.g in amputation), antitussive, antidiarrheal.
CONTRAINDICATION: CNSexcitation in swine
ANTIDOTES: Buprenorphine in respiratory depression, tramadol in emesis
DOSE: Dog:
IV, IM: 0.3-0.8 mg/kg
Cat:
IV, IM: 0.1-0.4 mg/kg
Horse:
IV, IM: 0.1mg/kg
SCHEDULE 1 DRUG!!
A3: FENTANYL (opioid)
GROUP: Opioids and narcotic analgesics (full agonist)
MOA: It acts on the µ receptor
- In the presynaptic nerve ending these receptors decrease Ca2+ influx prevents release of neurotransmitters from the nerves
PK: Lipophilic (transdermal patches), onset of action is 3 mins, metabolize in liver: Fentanyl–> Remifentanyl by plasma esterase, can be used in liver failure patients
SE: Respiratory depression, emesis, excitation/ dysphoria, constipation
INDICATION: Long term pain relief
CONTRAINDICATION: Excitation i horses
ANTIDOTES: Buprenorphine in respiratory depression, tramadol in emesis
DOSAGE:
Dog/Cat:
IV:1-5 µg/kg
Horse:
IV: 6-8 µg/kg
SCHEDULE 2 DRUG!!
A3: TRAMADOL (opioid)
GROUP: Opioid (full agonist)
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!
A3: BUPRENORPHINE (opioid)
GROUP: Opioid (partial agonist)
MOA: Acts mainly on the µ- receptor, antagonist of of κ - receptor:
- Respiratory depression
- Decrease GI motility and secretion
- Sedation
- Euphoria
- Decrease uterine contractions
PK: High affinity to receptor, highly lipophilic, works as an antidote for fentanyl and morphine, duration is less than 4hrs in cats, low oral bioavailability due to first pass metabolism, excretion in bile and delayed onset of action in cats
SE: Hyperthermia and nausea
INDICATION: Analgesic, respiratory depression, used in castration
SCHEDULE 3 DRUG!
A3: BUTORPHANOL (opioid)
GROUP: Opioid (partial agonist)
MOA: 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:
Dog and cat:
IV, IM, SC: 0.2-0.5 mg/kg
Horse:
IV, IM, SC: 0.01-0.1 mg/kg
SCHEDULE 4 DRUG!!
A3: NALOXONE (opioid)
GROUP: Opioid (antagonist)
MOA: Interacts at GABA receptors as antagonist, mainly of µ- receptor
PK: Highly lipophilic, can cross BBB, administration is mainly IV
SE: Nausea, vomiting, diahrrea, body aches, pain
INDICATIONS: Reverse side effects and analgesics of opioids
SCHEDULE 2 DRUG!!
A4: ISOFLURANE (inhalational anaesthetics)
GROUP: Inhalational anaesthetic
MOA: Act on the lipid matrix of the neuronal cell membrane, which results in disruption of neuronal transmission.
PK: Degraded by baralyme, end products are inorganic fluoride and trifluoroacetic acid
SE: Cardiovascular and respiratory depression, malignant hyperthermia
INDICATION: Induction and maintaining general anasthesia, anticonvulsant effect
CONTRAINDICATION: Younger, pregnant, lactating animals, susceptibility to malignant hyperthermia.
A4: SEVOFLURANE (inhaltional anaesthetics)
GROUP: Inhalational anaesthetics
MOA: Decreasing gap junction channel opening times and increasing gap junction channel closing times.
PK: Less blood solubility than isoflurane, rapid anaesthetic induction, biotransformed into organic and inorganic metabolites
SE: Decrease cerebral vascular resistance and cerebral metabolic rate, muscle stiffness, slight respiratory depression, malignant hyperthermia
INDICATION: Induction and maintaining general anesthesia (higher induction and maintenance % than isoflurane)
A5: PROPOFOL
(injectable anaesthetics)
GROUP: Injectable anaesthetics
MOA: Decreases the rate of GABA dissociation from its receptors thus increasing the opening of chloride channels
PK: Milky white emulsion, fast distribution, quick hepatic metabolism (can be used in liver failure patients), excretion in urine
SE: Cardiac, respiratory and renal impairment, negative inotropic effect–> hypotension, increased ocular pressure–> not good in glaucoma
INDICATION: Induction and maintain general anaesthesia, TIVA with opioids (like fentanyl), occacionally used in epileptic seizures
DOSAGE:
Dog/ Cat:
- IV 6-8 mg/kg (without premedication)
- IV 3-4 mg/kg (with premedication)
A5: PENTOBARBITAL
(injectable anaesthetics)
GROUP: Barbiturate
MOA: GABAa, decrease Ca2+ accumulation –> inhibits the release of stimulatory neurotransmitters
PK: Lipophilic, re-distribution in fat and muscle, accumulation in fat, excreted in urine
SE: Respiratory and cardiovascular depression, tissue irritation, liver insufficiency
INDICATION: Good muscle relaxant, combination anesthesia, tetanus in horse, epilepsy in dogs (long-acting)
CONTRAINDICATION: Greyhounds are oversensitive
A5: KETAMINE
(injectable anesthetics)
GROUP: NMDAr antagonists (dissociative anaesthetics)
MOA: These drugs prevent the binding of excitatory neurotransmitters, glutamate, and glycine at the NMDA receptor, preventing conduction of ions (Na+, K+, and Ca2+).
PK: Highly lipid soluble, can also be absorbed through oral or rectal mucous membranes, elimination through urine
SE: Increased sympathetic tone → tachycardia, hyperthermia, increased IOP, salivation, hallucinations
INDICATION: Combination anaesthesia, induction, and maintenance
CONTRAINDICATION: Late pregnancy, only used in dog, cat and horse (I think??)
DOSAGE:
Dog/ Cat:
- IV, IM 5-10 mg/kg (anesthesia in combination)
- IV 10 µg/kg/min (perioperative analgesia)
Horse: IV 0.4-0.8 mg/kg/h
SCHEDULE 2 DRUG!
A5: TILETAMINE (injectable anesthetics)
GROUP: NMDAr antagonists (dissociative anaesthetics)
MOA: These drugs prevent the binding of excitatory neurotransmitters, glutamate, and glycine at the NMDA receptor, preventing conduction of ions (Na+, K+, and Ca2+).
PK: Highly lipid soluble, can also be absorbed through oral or rectal mucous membranes, elimination through urine
SE: Increased sympathetic tone → tachycardia, hyperthermia, increased IOP, salivation, hallucinations
INDICATION: Combination anaesthesia, induction, and maintenance
CONTRAINDICATION: Late pregnancy, only used in dog, cat and horse (I think??)
SCHEDULE 3 DRUG!
A6: DIGOXIN (cardiotonic)
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
A6: PIMOBENDAN (VETMEDIN) (phosphodiesterase inhibitor)
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
A7: BENAZEPRIL (ace-inhibitor)
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
A7: RAMIPRIL (ace- inhibitor)
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.
A7: TELMISARTAN (angiotensin II receptor blocker)
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
A7: DILTIAZEM (Vasodilator and class IV antiarrhythmic) and calcium channel blocker)
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
A7: PIMOBENDAN (VETMEDIN) (Phosphidiesterase inhibitor)
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
A8: CODEINE (opiate, antitussive, narcotic analgesic)
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
A8: TRAMADOL (opioid)
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
A8: BUTORPHANOL (opioid and antitussive)
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
A8: DEXTROMETORPHAN (antitussive)
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
A8: ACETYLCYSTEINE (mucolytic)
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
A8: BROMHEXINE (expectorant)
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
A8: CLENBUTEROL (bronchodilator)
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
A8: SALBUTAMOL (bronchodilator)
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
A8: TERBUTALINE (bronchodilator)
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
A8: SALMETEROL (bronchodilator)
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
A8: THEOPHYLLINE
(methylxanthine derivatives)
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
A8: AMINOPHYLLINE (theophylline derivative)
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
A8: IPRATROPIUM (parasympatholytics)
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
A8: EPINEPHRINE (short-acting, non-specific bronchodilator)
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
A8: ZAFIRLUKAST (leukotriene antagonist)
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
A8: CIPROHEPTADINE (serotonin antagonist)
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
A8: FLUTICASONE (inhalational glucocorticoid)
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
A9: XYLASZINE (A2 agonist and emetic agent )
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
A9: ROPINIROL (dopamine agonist)
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)
A9: APOMORPHINE (opioid derivative)
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
A9: METOCLOPRAMIDE (dopamine antagonist)
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)
A9: ONDANSETRON (serotonin antagonist)
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)
A9: MAROPITANT (neurokinin-1 antagonist)
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
A9: METOCLOPRAMIDE ( dopamine antagonist and prokinetic agent)
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)
A9: PRUCALOPRIDE (prokinetic agent)
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)
A10: SUCRALFAT (coating- and antiulcer agent)
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)
A10: FAMOTIDINE (H2 anatgonist)
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)
A10: OMEPRAZOLE (proton pump inhibitor)
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
A10: PANTOPRAZOLE (proton pump inhibitor)
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)
A10: URSODEOXYCHOLIC ACID (choleretic)
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.
A10: SYLIMARIN/SYLIBININ (liver protectant)
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.
A10: CHOLIN, METIONIN, SAMe (lipotropic agents)
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
A11: FUROSEMIDE (loop diuretic)
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
A11: SPIRONOLACTONE (aldosterone antagonist)
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
A11: MANNITOL (sugar alcohol)
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
A11: DIGOXIN (cardial diuretic)
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
A11: THEOPHYLLINE
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
A11: THEOBROMINE (methylxantine)
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
A11: BENAZEPRIL (ace-inhibitor)
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
A11: RAMIPRIL
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.
A12: BUSERELIN (gonadotropin-releasing hormone)
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
A12: FERTIRELIN
(gonadotropin-releasing hormone analogue)
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
12: GONADORELIN (gonadotropin-releasing hormone analogue)
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
A12: DESLORELIN (gonadotropin-releasing hormone analogue)
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
A12: ECG (equine chorionic gonadotropin)
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
A12: HCG (human chorionic gonadotropin)
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
A12: DINOPROST ( prostagalandin analogue)
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
A12: CLORPROSTENOL (prostaglandin)
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
A13: HYDROXYZINE (piperazines)
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
A13: DIPHENHYDRAMINE (ethanolamine)
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)
A13: DIMENHYDRINATE ( ethanolamine)
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)
A13: CETIRIZINE ( 2nd gen antihistamine)
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)
A13: ZAFIRLUKAST (leukotriene receptor antagonist)
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
A13: OCLACITINIB (jak- inhibitor)
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
A13: LOKIVETMAB ( immunology product)
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
A13: BEDINVETMAB (anti-ngf)
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!
A14: ACETYLSALICYCLIC ACID (salicylates)
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
A14: CARPROFEN (arilproprionic acid)
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
