Term
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Definition
• Motilide agonist at smooth muscle receptors for motilin
GI DRUG
• Stimulates motility of stomach and upper SI (no effect on colon)
• Administered IM, mostly in cattle, dogs
• Oral and perenteral forms
• Metabolized by CYP450 and eliminated in bile
• Safe in most species, but ruminants react with severe diarrhea
• Clarithromycin has fewer side effects |
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Term
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Definition
• "Benzamide" Partial agonist at serotonin receptors
GI DRUG
• Increases Ach release
• Used in cats and dogs, horses and ruminants (eliminate faster)
• Indication: chronic constipation in cats and GE reflux/delayed emptying in dogs |
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Term
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Definition
• "Benzamide" that acts on upper GI to increase amplitude and frequency of smooth muscle contractons
• Prokinetic action from blocking of D2-Dopamine receptors and increased Ach release
• Oral and parenteral
• Eliminated in urine
• Adverse effects: restlessness, neck and jaw spasms
GI DRUG |
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Term
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Definition
• Approved for dogs over 16 weeks (not established in cats)
• Oral and injectable
• Blocks G Protein coupled type 1 neurokinin substance P receptors in emetic center
• Inhibits for cancer chemo, motion sickness, parvo, GE and renal disease
CNS-acting ANTIemetic |
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Term
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Definition
• Blocks type 3 serotonin receptors
• Effective via IV in dogs with chemo
• NOT effective for motion sickness!!!
CNS-acting ANTIemetic |
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Term
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Definition
• H2-Histamine antagonist (increases cAMP)
• Decreaes acid output to lessen irritation
• Afferent neurotransmission to vomiting center decreases
Peripherally-acting emetic and histamine antagonist |
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Term
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Definition
• Potent emetic in dogs
• Produces vomiting as agonist at D2-dopamine receptors in CTZ
• Topically or parental
• Blocked by tranquilizers that are dopamine receptor antagonists, but NOT by naloxone
Centrally-acting emetic |
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Term
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Definition
• Complex of aluminum hydroxide and sucrose
• Polymerizes below pH4 to form gel and binds to ulcerated tissue to form a seal around ulcer after administration
• Stimulates prostanoid formation (PGE2 and PGI) to increase cytoprotection (INHIBITED BY ANTIINFLAMMATORIES)
• Does NOT reduce acid output!!
• Locally-acting with short duration |
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Term
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Definition
• PGE analog used in preventing ulcers in dogs on NSAIDs but NOT glucocorticoids!
• Decreases acid secretion from histamine or gastrin
• Increases gastric cytoprotection
Adverse affects: diarrhea most common |
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Term
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Definition
• PPI - Active form binds and inactivates a-subunit of H+-K+-ATPase
• Reduces acid secretion by all sources of stimulation
• Approved in horses over 4weeks old for stress ulcers (orally, works within an hour)
• Also used in dogs
• Can slow hepatic oxidation of some drugs
• Acid suppressant drugs may reduce omeprazole activity (PPI's need acid to work) |
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Term
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Definition
• Longest duration and most potent
• Oral and parental dosage forms
• NO effect on hepatic metabolism
H2-Histamine Antagonist |
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Term
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Definition
• Oral and parenteral dosages (last 8 hrs)
• Few side effects (less CYP450 inhibition)
• Has anticholinesterase activity
H2-Histamine Antagonist |
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Term
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Definition
• Oldest antagonist; low potency and short action
• Oral and parental forms (last 3-5 hrs)
• Risk of potential drug interactions due to ability for CYP450 biotransformation in liver
○ May be useful to de-activate some toxicants or delay elimination
H2-Histamine Antagonist that increases cAMP |
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Term
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Definition
Cough suppressant with NO action at opioid receptors
Safe, no adverse effects
Common for small animals, found in OTC's |
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Term
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Definition
Kappa-type opioid agonist
Some abuse liability (crosses BBB)
Used in dogs and horses |
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Term
| N-Acetylcysteine (Mucomyst) |
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Definition
• Decreases viscosity of mucus by breaking disulfide bonds b/w glycoproteins
• Administration: nebulization for dogs and cats (quesitonable in horses)
• Cautions: Acute bronchoconstriction in sensitive patients, may inactivate antibiotics (ex: penicillin)
• Pharmacokinetics: nebulized drug not used is absorbed into blood and biotransformed in liver
• Non-pulmonary use: hepatotoxicoses by replacing cysteine in glutathione |
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Term
| Atropine, Glycopyrrolate, Ipratropium |
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Definition
• Muscarinic receptor blockers do NOT cross BBB
• Glycopyrrolate has slower onset, but longer duration (longer than atropine)
• Administration: low oral vioavailability; given by injection
○ Ipratropium available in aerosol
• Uses: dogs, horses with RAO
• Side effects: increased HR and decreased GI motility
Herbivores less sensitive than carnivores! |
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Term
| Aminophylline (methylzanthine) |
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Definition
• Water-soluble salt of theophylline inhibits phosphodiesterase to decrease cAMP breakdown
• Dilates airways and increases ciliary beat frequency and mucociliary clearance
• Pharmacokinetics: Orally, or injection to dogs and horses
○ Short 1/2 life (6hrs in dogs, 12hrs in horses)
○ High hepatic metabolism, and clearance varies (fast in dogs, slow in horses/cats)
○ LOW TI: leads to excitation, GI upset, arrhythmias, respiratory failure |
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Term
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Definition
B2-Adrenergic agonist bronchodilator to increase airway diameter, increase mucociliary clearance, and decrease allergic/inflammatory response
Stimulates intracellular cAMP
Used in horses and small animals |
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Term
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Definition
B2-Adrenergic agonist bronchodilator to increase airway diameter, increase mucociliary clearance, and decrease allergic/inflammatory response
Stimulates intracellular cAMP
Used in dogs and cats |
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Term
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Definition
B2-Adrenergic agonist bronchodilator to increase airway diameter, increase mucociliary clearance, and decrease allergic/inflammatory response
Stimulates intracellular cAMP
Used in horses for broncho-constrictive diseases |
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Term
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Definition
• Non-steroidal Anti-inflammatory drug decreases inflammation AND PAIN with pleuropneumonia
• Can mask signs of inflammation and cause delay in treatment |
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Term
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Definition
• Glucocorticoid decreases inflammation with RAI
• Enhances spread of infections, so use with bacteriocidal antibiotics
• Lots of side effects, particularly long-term
Anti-inflammatory used for coughing |
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Term
| Blood:gas partition coefficient from high to low (most soluble to least soluble) |
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Definition
Methoxyflurane
Halothane
isoflurane
Sevoflurane
N2O |
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Term
| Dopamine (and Dobutamine) |
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Definition
• Mainly used for AHF
• Chemically related to dopamine and NE
• Acts as agonist at B1-AR or dopamine receptors
• +inotrope with vasoconstriction at a1-AR's
• Indication: Treatment of AHF when BP is low
• Effects: Tachycardia (increases energy for heart)
• Short-lived, given IV, tolerance develops with repeated use
• LOW dose: Dilates renal vasculature at a1-AR's to maintain renal blood flow
• HIGH dose: Direct and indirect actions at B1-AR's to improve cardiac contractility
• Clinical utility is limited: short duration of action, and LOTS of side effects |
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Term
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Definition
• Used for ACUTE HF as NO donor to increase cGMP in vascular smooth muscles (venules and arerioles)
• Administration: I.V. infusion over short time periods
• Rapid tolerance development |
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Term
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Definition
• Phosphodiesterase inhibitor inhibits PDE III and V activities
• Used in dogs with CHF secondary to cardiomyopathy or mitral valve disease
• + inotrope inhibits intracellular cAMP breakdown
• ADME: Oral administration, minds to plasma proteins, hepatic biotransformation to active metabolite, lasts about 8 hours
• Effects may be reduced with use of B-AR blockers or Ca2+ blockers |
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Term
| Digitalis (Digoxin and Digitoxin) |
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Definition
• Cardiac glycosides form natural sources
○ Work by decreasing Na+-Ca2+ exchange and increases Ca2+ at contractile apparatus
○ Increases contraction amplitude ans speeds, but no change in duration or diastolic tone (mild)
○ Sensitize baroreceptors to stimulate vagus nerve and increase cholinergic transmission to heart |
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Term
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Definition
• Net effect: slow heart rate, decreased AV nodal conduction, decreased ventricular response to supraventricular arrhythmias
• Decreases AP duration and ERP, but at toxic doses produces DADs and leads to ectopic pacemakers and V-fib
○ Toxic dose range: heart becomes sensitized and increases in arrhythmias
• Digoxin is safer: oral administration, lasts 24-36 hours, can use in cats, lower plasma binding for better excretion (Digitoxin not used in cats)
• Non-cardiac effects:
○ Toxic inhibition of Na+-K+-ATPase produces signs of toxicity such as:
§ GI (common): Anorexia, vomiting, diarrhea
§ CNS: ataxia, depression, convulsions, visual disturbances
• NARROW TI (2-3), so tailor dosage to individual patients
• Conditions and concurrent drugs may modify digitalis activity (ex: systolic dysfunction or A-fib respond BETTER to digitalis)
○ Action also increases with hypokalemia and hypercalcemia |
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Term
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Definition
• Non-selective B-AR Antagonist during CHR (more powerful in AHF)
• Blocks B1, B2-AR's to decrease effects of NE stimulation on failing heart (70-80% of B-AR's are B1)
• Antioxidant action beneficial in CHF
• Produces long term increased ejection fraction and decreased HR |
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Term
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Definition
• ACE inhibitor for CHRONIC HF
• Reduces conversion of AGI to AGII (vasoconstrictor)
• Inhibits breakdown of vasodilatory kinins
• Increases ejection fraction and CO (decreases afterload)
• NO tolerance development (yay, they can stay on it forever)
• Enhances diuretics and reduces aldosterone!
• Approved for dogs AND cats
• Hydrolyzed in liver to an active form of enalaprilat
• Excretion: urine
• Peak effect 4 hrs after administration; lasts 12-14 hours |
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Term
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Definition
Class I: lesion, but no signs
Class II: Signs during exercise
Class III: Signs during normal activity
Class IV: Signs even at rest |
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Term
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Definition
• Non-specific osmotic diuretic
• Inhibits water reabsorption
• Net effect: Increased water excretion; some excretion of Na+ and other ions (increased urine volume and flow)
• Absorption: NOT absorbed by GI, given i.v., filtered in glomerulus
• Excretion: Urine (no metabolism)
• Kidney indications: oligouric states (acute renal failure)
• Extra-renal indications: elevated CSF or intraocular pressure (pulls water out of interstitial fluid)
• Contraindications: edematous states, dehydration |
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Term
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Definition
• Site 4: K+-sparing diuretic
• Blocks Na+ channels in LDT and CD
• NOT dependent of aldosterone
• May slightly increase urinary pH due to H+ excretion
• Minimal effect on normal K+ excretion
• Administered: p.o. with extensive plasma protein binding
• Hepatic biotransformation; converted to active metabolites
• Elimination: Urine
• Faster onset, but shorter duration (12-16 hours)
• Indications: hypokalemia from prolonged thiazides or loop diuretics, excess mineralocorticoid activty, compromised hepatic function
• Contraindications: Kyperkalemia, hyperkalemic metabolic acidosis, renal insufficiency, diabetes mellitus |
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Term
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Definition
• Site 4: K+-sparing diuretic
• Agonist of mineralicorticoid receptors; inhibits aldosterone induction of Na+ channels
• Decreases Na+ reabsorption, reduces drive force for K+ secretion
• DEPENDENT on presence of aldosterone
• May slightly increase urinary pH due to H+ excretion
• Minimal effect on normal K+ excretion
• Administered: p.o. with extensive plasma protein binding
• Hepatic biotransformation; converted to active metabolites
• Elimination: Urine
• Slower onset and longer duration (days)
• Indications: hypokalemia from prolonged thiazides or loop diuretics, excess mineralocorticoid activty, hyperaldosteronism
• Contraindications: Kyperkalemia, hyperkalemic metabolic acidosis, renal insufficiency, diabetes mellitus |
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Term
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Definition
• Site 3: Thiazides
• Block NCC transporter in early distal tubule; decreases NaCl reabsorption; increases Na+ delivery for excretion; increases Ca++ reabsorption
• Net effect: Increased excretion of Na+, Cl-, K+, H+ and water with Ca++ reabsorption
• Administered: p.o. or parenteral
• Site of action: lumen of nephron
• Elimination: Urine
• Indications: edematous states, acute oligouria, kidney stone formation, nephrogenic diabetes insipidus, mild CHF, hypercalciuria
• Contraindications: Preexisting hyperglycemia (aggravate diabetes mellitus by decreasing K+ and pro-insulin)
• Side effects: Hypokalemic metabolic alkalosis, dilutional hyponatremia |
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Term
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Definition
• MOST COMMON diuretic
• Site 2: "loop diuretic"
• Blocks NKCC2 protein, inhibits Na/K/Cl transport in thick ascending limb = increased Na+ delivery (and water)
• Net effect: increased flow of hypertonic urine with Na+, Cl-, K+, Mg2+, H+, and H20
• "Loop diuretic" given p.o. or parenterally
• Binds to plasma, some excreted in urine, rest undergoes phase II glucuronidation - filtered at glomerulus
• Site of action: lumen of nephron
• Elimination: urine
• Indications: Acute pulmonary edema, acute renal failure, mild hyperkalemia, acute hypercalcemia, EIPH in horses, CHF
• Side effects: Hypokalemic metabolic alkalosis, dehydration --> circulatory shock, hyponatremia, ototoxicity (hearing loss), hyperglycemia |
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Term
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Definition
• Site 1: carbonic anhydrase inhibitor
• Non-competetive inhibition in proximal tubule
• Lowers sodium-bicarb reabsorption
• Increases H+ and K+ excretion
• Net effect: increase bicarb and K+ excretion, mild natriuresis, hyperchloremic metabolic acidosis
• Absorbed p.o., eliminated in urine, produces systemic acidosis
• Uses: Glaucoma (not used for diuresis)
• Side effects: Ca,P uroliths (CaP precipitates in alkaline urine)
• Contraindications: Sulfonamide sensitivity, acidosis, hepatic insufficiency |
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Term
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Definition
Class IV cardiac Ca2+ channel blocker
Antiarrhythmic, reduces Ca2+ entry in phase 0 |
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Term
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Definition
Class III cardiac K+ channel blocker
Antiarrhythmic, blocks outward K+ currents in phase 3
Atria: increases atrial ERP (decreases atrial conduction)
Ventricles: slow repolarization, increased AP (decreased conduction)
Can induce Torsades de Pointes by slowing repolarization of AP |
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Term
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Definition
Class II Cardiac B-Adrenergic Antagonist
Antiarrhythmic, decreases NE and EPI in heart, decreases HR and ectopic PM |
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Term
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Definition
Class I Cardiac Na+ channel blockers
3 subclasses: A, B, C
Decrease numbers of Na+ channels
Affect is decreased by hypokalemia and alkalosis
"L" treats V-tachyarrhythmias |
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Term
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Definition
Direct cholinergic agonist works on muscarinic AND nicotinic receptors
Susceptible to AChE |
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Term
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Definition
Direct cholinergic agonist
Works on BOTH receptors (muscarinic and nicotinic)
Stimulates rumen and cholonic motility |
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Term
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Definition
Direct cholinergic agonist
Muscarinic receptors ONLY
Stimulates bladder and GI motility |
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Term
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Definition
Direct cholinergic agonist
Nicotinic receptors ONLY
Neuromuscular blockade |
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Term
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Definition
Direct cholinergic agonist
Cholinomimetic alkaloid
Used for purging tapeworms |
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Term
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Definition
Direct cholinergic agonist
Cholinomimetic alkaloid
Miotic for glaucoma (increases drainage of aqueous humor via pupillary constriction) |
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Term
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Definition
Muscurinic receptor blocker
Reverses choline esters |
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Term
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Definition
Indirect cholinomimetic drug
Reversible inhibitor
Acts at anionic site
SHORT effect
Poor GI absorption - given IV |
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Term
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Definition
Indirect cholinomimetic drug
Reversible inhibitor
Acts at esteratic site
Lasts longer
Treats myasthenia gravis, reversis curariforms, stimulates GI and bladder motility
Reverses paralysis |
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Term
| Osmotic Laxatives: draw water into intestinal tract to increase intestinal motility |
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Definition
• Magnesium salts
• Sodium salts
• Sugar alcohols (mannitol, sorbitol) |
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Term
| Irritant Laxitives: stimulate enteric sensory nerves to increase intestinal motility |
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Definition
• Castor oil - used in non-ruminants
• Emodin
• Bisacodyl - effects in large intestine in cats and dogs |
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Term
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Definition
• Kaolin: aluminum silicate
• Pectin: carbohydrate from fruit rinds
• Traditional antidiarrheal treatment in pets and ruminants, but efficacy is questionable |
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Term
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Definition
| Inhibits histamine release from mast cells |
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Term
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Definition
| H1-Histamine Antagonist increases intracellular Ca2+ |
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Term
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Definition
| Second generation antihistamine that cannot cross the BBB (not really used in vet med) |
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Term
| Uses of H1-Histamine antagonists |
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Definition
Allergies
Motion sickness
Conditions secondary to histamine production/release (tumors) |
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Term
Carprofen
Deracoxib
Etodolac
Firocoxib
Meloxicam
Tepoxalin |
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Definition
| NSAIDs for dogs used for inflammation, DJD, lameness |
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Term
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Definition
| Proinflammabory LTB4, can cause gastric ulcers if only COX are inhibited |
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Term
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Definition
Dual COX/LOX inhibitor, used in osteoarthritic dogs
Only weak base NSAID |
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Term
| PG's, COX, and blood clotting |
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Definition
Decreased platelet cAMP causes aggregation (COX-2)
Increased platelet cAMP reduces aggregation (COX-1/Aspirin) |
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Term
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Definition
First anticoaggulant, then analgesia, then fever, then anti-inflammatory!
Irreversible COX-1 inhibition
Don't use in food animals (use banamine)
Eliminated SLOW in cats, FAST in horses, ruminants (need higher dose)
Causes Heinz anemia in cats |
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Term
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Definition
NSAID ok for cats
COX-1 and COX-2 and NF-kB |
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Term
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Definition
Non-selective COX NSAID for dogs and horses
CAN use in beef, NOT in dairy |
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Term
| Flunixin Meglumide (Banamine) |
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Definition
Standard NSAID in cattle
Non-selective COX inhibitor |
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Term
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Definition
| Kills adrenocortical cells |
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Term
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Definition
Glucocorticoid antagonist
Inhibits dissociation of Hsp90 from GcR |
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Term
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Definition
Inhibit uptake of glucose (hyperglycemia)
Makes everything go to the liver
Increases lipolysis |
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Term
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Definition
Long duration, very potent, and NO Na+ retention
DRUG OF CHOICE |
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Term
| Prednisone (becomes prednisolone) |
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Definition
| Medium duration, potency and Na+ retention. Good for maintenance doses. |
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Term
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Definition
G-protein coupled
Stimulated by Ach and muscarine
Blocked by atropine
Located on neurons, heart... |
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Term
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Definition
Na+, K+ depolarizing ion channel
Stimulated by Ach and nicotine
Blocked by tubocurarine
Located on skeletal muscle |
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Term
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Definition
Blocks nicotinic Nm receptors on skeletal muscle endplates
Long duration of action
Low Nm sensitivity |
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Term
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Definition
| Muscarinic AND nicotinic activity |
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Term
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Definition
Depolarizes neuromuscular blockade on NICOTINIC receptors
Short acting |
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Term
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Definition
Stimulates urinary bladder motility (cats)
GI motility
acts on MUSCURINIC receptors only |
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Term
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Definition
Intermediate duration, eliminated in bile
Atracurium more selective |
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Term
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Definition
OLDEST NMJ blocker
LONG duration of action
hypotension = side effect due to histamine release |
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Term
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Definition
| Depolarizing neuromuscular blocker at nicotinic receptors in nematodes |
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