Pharm Flashcards
Bethanechol drug class
cholinergic
bethanechol indications
used primary to inc bladder contractility
–acute & partial detrusor atony secondary to acute bladder overdistension and partial neurogenic lesions
Bethanechol alternative indications in horses
adjunctive prokinetic agent for tx of equine gastric ulcer syndrome (EGUS)
Bethanechol altnerative indication in ruminants
INC abomasum and duodenum contractility with healthy dairy cattle and those with left displacement of the abomasum (LDA)
Bethanechol pharmacology/actions
stimulates cholinergic receptors
**effects principally muscarinic negligible nicotinic activity
Bethanechol pharmacologic effects
- INC esophageal persistalsis and lower esophageal sphincter tone
- INC sphincter tone
- INC tone & peristatic activity of stomach and intestines
- INC gastric and pancreatic secretions
- INC tone of detrusor mm of bladder
- DEC bladder capacity
Bethanechol at high doses
INC bronchial secretions & constriction
- lacrimation
- salivation
Bethanechol contraindications
- GI or urinary tract obstructions
- bladder wall integrity is in question
Bethanechol adverse effects in horses
Salivation
lacrimation
abdominal pain (colic)
bethanechol if used IM/IV can cause
Severe cholinergic reactions
- salivation, tearing & sweating, bronchoconstriciton, bradycardia, inc GI motility, diarrhea
Metoclopramide drug class
GI prokinetic agent
Metoclopramide indications
- Stimulates upper GI motility & has anti-emetic properties
Metoclopramide pharmacological effect
(not completely known)
Sensitizes upper GI smooth mm effects of acetylcholine
–anti-cholinergic drugs will negate metoclopramides effects
Metoclopramide in CNS effects
Antagonizes dopamine (D3) at receptor sites
– weak inhibitor of 5-HT3– agonist of 5HT4 receptors
–> sedative, central anti-emetic, extrapyramidal and prolactin secretion stimulation effects
Metoclopramide contraindications
GI hemorrhage
obstruction or perforation
hypersensitivity
**relatively contraindicated: seizure disorders, pheochromocytoma
Metoclopramide adverse effects
Severe CNS effects
–>Alternating periods of sedation & excitement, beahvioral changes & abdominal pain
Omeprazole drug class
Proton pump inhibitor
Omeprazole pharmacological actions
Benzimidazole gastric acid (proton) pump inhibitor
- –> activated to sulphenamide derivative that binds at secretory surface of parietal cells to the enzyme, H-K ATPase
- inhibits strnasport of H ions into stomach
- reduces acid secretion
Omeprazole inhibits what enzyme?
Hepatic cytochrome P-450 mixed function oxidase system
Omeprazole is metabolized by what organ?
IN the liver
Sucralfate Drug Class
GI mucosal protectant
Sucralfate indications
Tx of oral, esophageal, gastric & duodenal ulcers
Sucralfate MOA
**Exact mechanism unknown
- local effect
- reacts with hydrochloric acid in stomach to form paste-like complex that will bind to proteinaceous exudates found at ulcer sites
- insoluble complex forms a barrier at site & protects ulcer from further damage caused by pepsin, acid or bile
Misoprostal drug class
Prostaglandin E1 Analog
Misoprostol indications
Treating or preventing gastric ulcers
Uterine contractibility & cervical softening/opening (pregnancy termination)
Misoprostol pharmacology actions
Direct action on parietal cells
- inhibits basal & nocturnal gastric acid secretion
- pepsin secretion decreased
- cytoprotective effect on gastric mucosa–> INC production of gastric mucus & bicarbonate, INC turnover & blood supply of gastric mucosal cells
Uterine contractions
Misoprostol contraindications
Pregnancy & nursing others
Caution: sensitivty to prostaglandins & prostaglandin analogues; pts with cerebral or coronary vascular dz
Misoprostol adverse effects
GI distress (diarrhea, adbom pain, vomiting/flatulence)
**pregnant women should handle with caution**
Cisapride drug class
Pro-motility agent
Cisapride indications
Oral GI prokinetic– used in several spp for GI stasis, reflux esophagitis & constipation/megacolon (cats)
**no longer commerically available**
Cisapride contraindications
Hypersensitivity
GI perforation or obstruction
Hemorrhage
Cisapride pharmacology actions
INC lower esophageal peristalsis & sphincter pressure
accelerates gastric emptying
–> enhances release of acetylcholine at myenteric plexues (does not induce myenetric plexus, but does not induce nicotinic or muscarinic receptor stim)
Naloxone drug class
Antidote: opiate antagonist
Naloxone pharmacologic actions
** exact mech unknown
- competitive antagonist by binding to the mu, kappa & sigmoid opioid receptor sites
- high affinity for mu receptor
Naloxone effect on horses:
low end of dosing range: limit opioid induced locomotor actiivty
Upper end of dosing range: may stimulate colonic propulsion
Flunixin meglumine drug class
Non-steroidal anti-inflammatory agent
Flunixin meglumine use caution in:
GI ulcers, renal, hepatic or hematologic dzes
–horses with colic– may mask behavioral & cardiopulmonary signs assoc with endotoxemia or intesitnal devitalization
Flunixin meglumine pharmacology/actions:
potent inhibitor of cyclooxygenase
– analagesic, anti-inflammatory & antipyretic activity
Phenylbutazone drug class
Non-steroidal anti-inflammatory agent
Phenylbutazone contraindications
known hypersensitivity
history of or pre-existing hematologic or bone marrow abnormalities pre-existing GI ulcers
Phenylbutazone pharacologic actions
inhibition of cyclooxygenase– reducing prostaglandin synthesis
Other effects: reduced renal blood flow, dec GFR, dec plt aggregation, gastric mucosal damage
Phenylbutazone adverse effects in horses
oral & GI erosions & ulcers
hypoalbuminemia
diarrhea
anorexia
renal effects
Administration of phenylbutazone intrmauscular can cause
irritating: swelling ot necrosis & sloughing
Fenbendazole indicated for removal of following parasites in horses:
large strongyles (S. edentatus, S. equinus, S. vulgaris)
Small strongyles (Cyathostomum spp., Cyclicocylus spp., Cyclicostephanus spp., Triodontroophorus spp.)
Pin worms (oxyuris equi)
Fenbendazole indicating for following parasites in cattle:
Haemonchus contortus, Ostertagia ostertagi, Trichostorngylus axei, Brunostomum phelbotomum, Nematodirus helvetianus, Cooperia spp., Trichostrongylus colubriformis, Oesophagostomum radiatum, Dictyocaulus viviparus
Acetylcystein indications
mucolytic
treatment for acetaminophen tox or other hepatotoxic conditions were glutathione syntehsis is inhibited or oxidative stress occurs
Acetylcysteine used in horses for what indication
Strangles– acetylcysteine instilled into guttural pouch used ot help break up chondroids & avoid the need for surgical removal
Meconium impaciton– foals: break up meconium refractory to repeated enemas
Acetylcystein MOA as a mucolytic
Reduces viscosity of purulent & nonpurulent secretions & expedites removal of secretions via coughing, suction or postural drainage
- free sulfhydryl group on drug reduces disulfide linkages in mucoproteins
- pronounced action at pH from 7-9
Acetylcysteine actions on liver d/t acetominophen toxicity
- reduce extent of liver injury or methemoglobemia after ingestion of acetaminophen or phenol
- provides an alterante substrate for conjugations with reactive metabolite of acetaminophen– maintaining or restoring glutathione level s
Acetylcysteine advers effect when administered into pulmonary tract
hypersensitivity
chest tightness
bronchoconstriction
bronchial or tracheal irritation
S-Adenosyl-methionine drug class
Hepatoprotectant
S-Adenosyl-methionine Pharacological action
Endogenous molecuels synthesized by cells throughout the body
- formed from amino acid methionine
- SAMe– essenital part of 3 major biochemical pathways
- beneficial effects: inc liver & rbc glutahtione levels &/or prevent its depletion; inhibts apoptosis secondary to acohol or bile acids in hepatocytes
Pentoxifylline pharmacological actions
- INC RBC flexibility by inhibiting rbc phosphodiesterase & dec rbc viscosity by dec plasma fibrinogen
- INC fibrinolytic activity
- horses– potent inihibitor of matrix metalloproteinase-9 & 2
- dec negative endotoxic effects of cytokine medators via phosphodiesterase inhibition
Pentoxifylline contraindications:
retinal or cerebral hemorrhage
intolerance or hypersensitivity to xanthines
Caution: severe hepatic or enal impairment or at risk for hemorrhage
Pentoxifylline adverse effects
GI tract (vomiting/inappetance) most common
Isoflupredone acetate uses/indications
potent glucocorticoid– anti-inflammatory or immunosuppressive effects:
- labelled indications: adjucntive in bovine ketosis, alleviating pain & lameness assoc with msc conditions, acute hypersenstiivity rxns, adjunctive tx of overwhelming infections with sevre tox, shock, supportive therapy in stress, dystocia, retained palcement, inflamm., ocular conditions, sneakbite & parturient paresis
Isoflupredone acetate pharmacological actions
17x more potent anti-inflammatory than hydrocotisone (cortisol)
10x more potent than prednisolone
Isoflupredone acetate adverse effects
Hyperadrenocroticism
dairy cattle–hypokalemia
potential adverse effects: dec milk production, delayed wound healing, GI ulceration, INC infection rates, diabetes mellitus exacerbation/hyperglycemia, pancreatitis, hepatopathy, renal dysfunction, osteoporosis, laminitis, hypothyroidism, hyperlipidemia
Dexamethasone drug class
Glucocorticoid
Glucocorticoids: 3 braod uses/indications
- Replacement of glucocorticoid activity in patients with adrenal insuffiency
- anti-inflammatory agent
- immunosuppressive
Glucocorticoids effects on cardiovascular system
- Dec capillary permeability
- enhance vasoconstriction
- POS ionotropic (mild) (inc BP)
Glucocorticoids effects on cells
- inhibit fibroblast proliferation
- macro response to migration inhibiting factor
- sensitization of lymphocytes and cellular response to mediators of inflammation
- stabilize lysosomal membranes
Glucocorticoids effect on CNS/autonomic nervous sytem
- Lower seizure threshold
- alter mood and behavior
- diminish response to pyrogens
- stim appetite
- maintain alpha rhythm
- glucocorticoids necessary for normal adrenergic receptor sensitivity
Glucocorticoids effect on endocrine system
- suppress release of ACTH from anterior pituitary–> dec release of endogenous corticosteroids
- inihibit osteoblast function
- reduced ADH (vasopressin) activity at renal tubules & diuresis may occur
- inhibits insulin binding to insulin receptors & post-recept effects of insulin
- reduced: TSH, FSH, prolactin & LH at pharmacological doses
Glucocorticoids effect on hematopoietic system
- INC number of circulating neuts & rbcs
- plt aggregation inhibited
- dec amts of lymphocytes (peripheral), monos & eos
- removal of old red cells diminished
- can cause involution of lymphoid tissue
Glucocorticoids effects on immune system
- dec circulating levels of T lymphs
- inhibit lymphokines
- inhibit neuts, macro & mono migration
- reduce production of interferon
- inhibit phagocytosis & chemotaxis
- ag processing
- diminish intracellular killing
- antagonize complement cascade & mask clinical signs of infection
- mast cells decreased in number & histamine suppressed
Glucocorticoid effects on metabolism
- stimulate gluconeogenesis
- lipogenesis enhance in certain areas of body
- adipose tissue can be redistrubted away from extremities to trunk
- fatty acids are mobilized from tissues & their oxidation increased
- plasma triglycerides, cholesterol & glycerol increased
- protein mobilize from most areas of body
Glucocorticoid effects on musculoskeletal sys
- may cause muscular weakness, atrophy, osteoporosis
- bone growht inhibited via growth hormoen & somatomedin inihibition
- increased Ca excretion
- inhibition of Vit D activation
- resorption of bone can be enhanced
- fibrocartilage growth inhibited
Ophthalmic effects of Glucocorticoids
prolonged use (systemic/topical)–> INC intraocular pressure & glaucoma, cataracts & exopathalmus
Glucocorticoid effects on renal, fluid & electrolytes
- INC potassium & Ca excretion
- Na & Cl reabsorption
- extracellular fluid volume
- rare: hypokalemia/hypocalcemia
- diuresis
Glucocorticoid effects on skin
- thinning of dermal tissue & skin atrophy
- hair follicles can become distended & alopecia may occur
Propylene glycol base injectable production administration rapidly can cause
Hypotension
Collapse
Hemolytic Anemia
**most drug formualtions use sodiu mphosphate when givin drug intravenously**
Triamcinolone Acetonide intraarticular injeciton in horses shown to cause
- improvement clinical lamenss
- reduce articular protein, inflammatory cell infiltraiton, animal hyperplasia & subintimal fibrosis
- synovial levels of hyaluronan & glycosaminoglycan can be increased
Ivermectin is approved for control of what parasites in horses
- Large adult strongyles: strongylus vulgaris, S. Edentatus, S. Equinus Triodontophorus spp
- Small strongyles
- pinworms (adults & 4th stage larva)
- ascarids (adults)
- hair worms (adults)
- large mouth stomach worms (adults)
- beck threadworms (microfilaria)
- bots (oral & gastric stages)
- lungworms (adults & 4th stage larva0
- intestinal threadworms (adults)
- summer sores (cutaneous 3rd stage larva) econdary to Hebronema or Draschia spp.
Ivermectin is labeled for control of what parasites in cattle
- roundworms (adults & 4th stage larva)
- lungworms (adults & 4th stage larva)
- cattle grubs (parasitic stages)
- sucking lice
- mites (scabies)
Ivermectin pharmacological actions
- enhances release of GABA at pre-synpatic neurons
- blocks postsynaptic stim of adjacent neuron in nematodes or mm fiber in athropods
- causes paralysis of parasite & eventual death
Ivermectin is ineffective against liver flukes & tapeworms because
Do not use GABA as pierpheral nerve transmitter
Amphotericin B pharmacologic actions
acts by binding sterols (primarily ergosterol) in cell membrane & alters permeability of membrane allowing intraclelular K & other cellular constituents to leak out
Amphotericin B is ineffective against rickettsia & bacteria because
has no activity against these organisms
Amphotericin B in vitro activity against what fungal organisms
- blastomyces
- aspergillus
- paracoccidioides
- coccidioides
- histoplasma
- cryptococcus
- mucor
- sporothrix
Amphotericin adverse effects in hroses
tachycardia
tachypnea
lethargy
fever
restlessness
fever
anorexia
anemia
phlebitis
polyuria
collapse
Amphotericin B nephrotoxicity
renal vasoconstriction wiht subsequent reduction in GFR
**monitor renal values aggressively during therapy**
Acyclovir tx in horses
investigated in EHV-5, lymphoma, EHV-1 myelonencephalopathy
**poor bioavailability is an issue
Acyclovir adverse effects
thrombophlebitis
acute renal failure
encephelopathologic changes (rare)
GI disturbances– oral or parenteral therapy
Class 1 Antiarrythmic agents
Na channel blockers
– block voltage gated sodium channels of myocardium
Class 1a antiarrhythmic agetns
block fast sodium channels
– prolong action potential activity– lengthening the effective refractory period
potentially proarrythmic– QT interval prolongation (promoting reentry)
Tx of supraventricular & ventricular tachyarrythmias
Class 1a antiarrhythmic agents examples
Quinidine
procainamide
Quinidine indications
atrial fibrillation
(quinidine gluconate): ventricular tachycardia (VT-) discontinued in 2017
Quinidine pharmacological actions
slow impulse conduction
prolong effective reractor period
vagolytic activity–accelerated AV nodal conudction
alpha adrenoreceptor antagonist effects: hypotension & reflex INC in sympathetic outflow (poteniates proarrhythmic effects)
Quinidine adverse effects in horses
- inappetance
- depression
- swelling of nasal mucosa
- ataxia
- diarrhea
- colic
- hypotension
- rarely: laminitis, paraphimosis & development of urticarial wheels; cardiac arrthmias: AV block, circulatory collapse & sudden death
Procainamide indications
acute management of VT (& VPCs)
acute onset AF in horses
Procainamide action
- Prolongs refractory times in both atria & ventricles
- decreases myocardial excitability
- depresses automaticity and conduction velocity
- some anticholinergic effects
Procainamide contraindicated
- myasthenia gravis
- hyerpsensitivity to drug, procaine or other chemically related drugs
- torsade de pointes
- 2nd or 3rd degree heart block (unless artificially paced)
- EXTREME CAUTION: cardiac glycoside intoxication, systemic lupus
- CAUTION: signficant hepatic, renal dz or CHF
Procainamide adverse effects
- Reported in the dog: GIT effects: anorexia, vomiting & diarrhea
- CV: weakness, hypotension, neg inotropism, widened WRS complex & QT intervals, AV block, multiform ventricular tachycardia
- profound hypotension if injected too rapidly
Class 1b anti-arrhythmic agents used for management of
Ventricular arrhythmias
- shorten action paotenial without causing QT prolongation
- preferentially bind to Na channels– act primarily on damaged mycoardial cells ot prevent reentry pathways
Class 1b anti-arrhythmic agents examples
lidocaine
phenytoin (diphenylhydantoin)
tocaindide
mexiletine