Drugs

Question 1

Diphenhydramine

Answer 1

1st gen. H1 histamine blocker
Competitive antagonist/inverse agonist
^ free intracellular Ca2+

Question 2

Chlorpheniramine

Answer 2

1st gen. H1 histamine blocker
Competitive antagonist/inverse agonist
^ free intracellular Ca2+

Question 3

phrilamine

Answer 3

1st gen. H1 histamine blocker
Competitive antagonist/inverse agonist
^ free intracellular Ca2+

Question 4

Meclizine

Answer 4

1st gen. H1 histamine blocker
Competitive antagonist/inverse agonist
^ free intracellular Ca2+

Question 5

hydroxyzine

Answer 5

1st gen. H1 histamine blocker
Competitive antagonist/inverse agonist
^ free intracellular Ca2+

Question 6

Cetirizine

Answer 6

2nd gen H1 histamine blocker
Competitive antagonist/inverse agonist
^ free intracellular Ca2+
Pumped out of BBB by P glycoprotein

Question 7

Loratidine

Answer 7

2nd gen H1 histamine blocker
Competitive antagonist/inverse agonist
^ free intracellular Ca2+
Pumped out of BBB by P glycoprotein

Question 8

Fexofenadine

Answer 8

2nd gen H1 histamine blocker
Competitive antagonist/inverse agonist
^ free intracellular Ca2+
Pumped out of BBB by P glycoprotein

Question 9

Epinepherine

Answer 9

Functional antagonist of histamine effects
Agonizes all ARs
A: vasoconstriction –> ^ BP
B1: ^ HR and CO –> ^ systolic BP
B2: skeletal muscle vasodilation –> decreased systolic BP –> widening in pulse
Vc, decreased allergic response
Use in anaphylactic shock, heaves, hypotensive states, cardiac arrest, + hemostasis, local anesthesia, can produce cardiac dysrhythmias

Question 10

Misoprostil

Answer 10

H2-histamine antagonist, PGE derivative
Decrease acid secretion, increase GI mucosal cytoprotection, decrease mast cell degranulation
Highly effective, long lasting

Question 11

Dinoprost

Answer 11

PGF-2a derivative
Estrus synchronization
Increase uterine contractions (expel uterus pus, abortion)

Question 12

Travoprost

Answer 12

PGF-2a derivative

Glaucoma, ocular fluid drainage (decr. ocular pressure)

Question 13

latanoprost

Answer 13

PGF-2a derivative

Glaucoma, ocular fluid drainage (decr. ocular pressure)

Question 14

Carprofen

Answer 14

Proprionic acid derived
Inhibits COX-2 > COX-1
No TxA2 inhibition
Low ulcer formation
Anti-inflammatory
analgesic > aspirin, phenylbutazone

Question 15

Deracoxib

Answer 15

Coxib
Inhibits COX-2 > COX-1
No TxA2 inhibition
GI ulcers and changes in renal function at high doses

Question 16

Tepoxalin

Answer 16

Dual COX/5-LOX inhibitor (block both sides of arachadonic acid pathway)
Inhibits COX-2 > COX-1, 5-LOX, NF-kB, TxA2

Question 17

Phenylbutazone –> oxyphenbutazone

Answer 17

anti-inflammatory/analgesic
inhibits prostanoid biosynthesis, COX-1 and COX-2, and 5-LOX
Chondrodestructive effects

Question 18

Flunixin/Flunixin Meglumide

Answer 18

Non-selective COX inhibitor (both COX-1 and COX-2)
May inhibit NF-kB
anti-inflammatory, analgesic, antipyretic
Used for skeletal muscle pain (horses) and visceral pain (dogs)

Question 19

Aspirin/salicylate ions

Answer 19

Irreversibly acetylates/inhibits COX
–> decreases TxA2 formation
Can change properties of COX-2 favoring production of anti-inflammatory lipoxins
anticoagulant, analgesic, anti-pyretic, anti-inflammatory

Question 20

Cloprostenol

Answer 20

PGF-2a derivative
Estrus synchronization
Increase uterine contractions (expel uterus pus, abortion)

Question 21

Cromoglycate

Answer 21

Mast cell stabilizer

Question 22

Mifepristone

Answer 22

GcR antagonist
Inhibits dissociation of HSP90
Changes interaction of GcR with accessory proteins to inhibit GC-GcR effects on gene transcription

Question 23

Hydrocortisone

Answer 23

Full GC agonist
Short duration
Low anti-inflammatory and Na+ retention potency
Act at GcRs and mineralocorticoid receptors

Question 24

Dexamethasone

Answer 24

Full GC agonist
Long duration
High potency
No mineralocorticoid activity

Question 25

Prednisone ( --> prednisolone)

Answer 25

Medium duration and potency Works both at GcR and MC receptors (more so at GcR) Prednisolone is more bioavailable in dogs and cats

Question 26

Triamcinolone

Answer 26

Medium duration and potency

Question 27

Aldosterone

Answer 27

High mineralocorticoid potency ^ Na+ retention and K+ secretion Can lead to hypertension and hypokalemic alkalosis

Question 28

Betamethasone

Answer 28

Long duration Highly potent GcR agonist Less mineralocorticoid effects

Question 29

Cortisone --> hydrocortisone

Answer 29

Greatest MC side effects | Binds both GcRs and MCRs

Question 30

Fludrocortisone

Answer 30

``` short duration medium potency (esp. Na+ retention potency) ```

Question 31

SEGRAs

Answer 31

Selective GcR agonists Trans-repress pro-inflammatory genes trans-activate anti-inflammatory genes no catabolism-related gene TS --> less side effects

Question 32

Cyclosporine

Answer 32

Calcineurin inhibitor: binds cyclophilin Inhibits gene transcription in activated Th cells Inhibits mast cells and eosinophils as well Uses for CsA: ocular inflammation, dry eye, atopic dermatitis, graft vs. host defense CsA increases digoxin plasma levels Most effective if given before T cell activation has occurred

Question 33

Tacrolimus

Answer 33

``` Calcineurin inhibitor: FKBP Inhibits gene transcription in activated Th cells atopic dermatitis More potent Use topically ```

Question 34

Bethanechol

Answer 34

Cholinomimetic (alkaloid) mAChR agonist (contracts smooth m.) Contract detrusor m. and relax trigone/sphincter m. GI motility

Question 35

Carbachol

Answer 35

Cholinomimetic (alkaloid) mAChR agonist (contracts smooth m) Rumen/colonic motility

Question 36

Pilocarpine

Answer 36

``` Cholinomimetic alkaloid tertiary amine - less ionized mAChR agonist (NOT nAChR) Topical (eye): pupillary constriction Glaucoma: miosis decreases intraocular P Lens ciliary m. accommodation for near vision Dry eye (KCS): increases lacrimation ```

Question 37

Edrophonium

Answer 37

Cholinesterase inhibitor Quaternary ammonium compound: N+ slowly unbinds from (-) anionic site (minutes) Increases Ach in synaptic zone Ionized - poor GI absorption

Question 38

Neostigmine

Answer 38

Carbamate: reversible carbomylates esteratic site (15-30m) Ionized: poor GI absorption Can increase Ach at NMJ and surmount nicotinic cholinergic antagonist mAChR blockers co-administered to prevent adverse muscarinic effects of ACE Potentiates relaxation of depolarizing agents like succinylcholine

Question 39

Organophosphates

Answer 39

Irreversibly phosphorylate esteratic site (must be replaced) Lipid soluble With all cholinergic agonists: watch for SLID and cardiorespiratory effects (bradycardia) Cholinergic toxidrome

Question 40

Solanaceous (belladonna)

Answer 40

mAChR antagonist alkaloid, tertiary amine ~atropine mydriasis increases ocular P, cycloplegia, decreased tear formation Increased HR and AV conduction Bronchodilation, decreased tracheobronchiolar secretions Decreased salivation, GI motility, urinary bladder relaxation and retention Antiemetic Sedation (only tertiary amines)

Question 41

Scopolamine

Answer 41

tertiary amine ~atropine mydriasis increases ocular P, cycloplegia, decreased tear formation Increased HR and AV conduction Bronchodilation, decreased tracheobronchiolar secretions Decreased salivation, GI motility, urinary bladder relaxation and retention Antiemetic Sedation (only tertiary amines)

Question 42

Tropicamide

Answer 42

shorter duration and less cycloplegic effects than atropine can use as short-acting non-cycloplegic a1-Ar agonists mydriasis increases ocular P, cycloplegia, decreased tear formation Increased HR and AV conduction Bronchodilation, decreased tracheobronchiolar secretions Decreased salivation, GI motility, urinary bladder relaxation and retention Antiemetic Sedation (only tertiary amines) Quaternary amines and atropine are more peripherally selective

Question 43

Trimethaphan

Answer 43

nN-AChR blocker (ANS ganglia, some peripheral N-terminals) Inhibits both sympathetic and parasympathetic neurotransmission Blocks ganglia without skeletal muscle paralysis Causes tachycardia, mydriasis, cycloplegia, urine retention, dry mouth, decrease in GI motility (constipation), decreased sweating, decreased cardiac contractility/CO, increased vasodilation, hypotension Use as hypotensive agent

Question 44

Pancuronium

Answer 44

nMAChR blocker (skeletal ms. endplates) Non-depolarizing NM blocker = curariform Long duration of action (>35m) Use as skeletal ms. relaxants/paralyzing agents Also blocks mAChR --> tachycardia (~atropine)

Question 45

Vecuronium

Answer 45

intermediate duration (20-30m) No CV side effects Elim in bile rather than urine

Question 46

Atracurium

Answer 46

~vecuronium | spontaneously decomposes in plasma

Question 47

Levamisole

Answer 47

non-depolarizing NM blocker = curariform | antiparasitic

Question 48

Succinylcholine

Answer 48

``` choline ester parasympathomimetic depolarizing NM blocker persistent nAChR agonist Ultra short action ACE inhibitors potentiate block Minimal effects on ganglionic nAChRs (skm selective) No antidote (atropine ineffective) ```

Question 49

Pyridostigmine

Answer 49

ACE inhibitor, reversible Dx myasthenia gravis Reverse NM blockade of curariform pancuronium/atracurium (give after atropine)

Question 50

Neostigmine

Answer 50

ACE inhibitor, reversible Dx myasthenia gravis Reverse NM blockade of curariform pancuronium/atracurium (give after atropine)

Question 51

Edrophonium

Answer 51

ACE inhibitor, reversible Dx myasthenia gravis Reverse NM blockade of curariform pancuronium/atracurium (give after atropine)

Question 52

Isoproterenol

Answer 52

B-AR agonist ==> affects heart only More potent than NE or E B1: increased HR, CO --> increased systolic BP B2: skeletal muscle vasodilation --> decreased diastolic BP --> widening in pulse P Can produce arrhythmias Uses: bronchodilator, alleviate AV block, increase BP RActopamine: turkey feed additive

Question 53

Dobutamine

Answer 53

B1 agonist short lived give IV Increases cardiac contractility --> increased HR ^ CO, ^ cAMP --> ^Na --> depolarization of RMP (makes more +) Uses: ^ CO in shock or AHF

Question 54

Albuterol

Answer 54

B2 agonist long duration give intrapulmonary to decrease side effects Relaxes bronchial, uterine, vascular smooth ms. Uses: bronchodilator, relax uterus prior to partition Use in cats/dogs

Question 55

Clenbuterol

Answer 55

B2 agonist long duration give intrapulmonary to decrease side effects Relaxes bronchial, uterine, vascular smooth ms. Uses: bronchodilator, relax uterus prior to partition Use in horses

Question 56

NE

Answer 56

A/B1-AR stimulants (less B2) A: increased BP (peripheral vasoconstriction) --> decreased HR due to baroreflex of vagal tone caused by increased BP if mAChRs blocked, NE will increase HR due to actions at B1-ARs

Question 57

Dopamine

Answer 57

D1-DAR agonist Low doses: dilates renal vasculature Higher doses: less D-AR selectivity --> interactions with adrenergic receptors B1: increased NE release to improve HR and CO A: systemic vasoconstriction --> ^ BP ^ CO, ^ cAMP --> ^Na --> depolarization of RMP (makes more +)

Question 58

Fenoldopam

Answer 58

D1 DAR selective agonist no effects on ARs dilate renal vasculature

Question 59

Amphetamines/tyramine

Answer 59

stimulate release of NE from sympathetic nerves | stimulate a-AR

Question 60

Cocaine/tricyclic antidepressants

Answer 60

decrease NE uptake into nerve terminals

Question 61

Monoamine oxidase inhibitors (MAOI)

Answer 61

Inhibit NE breakdown | antidepressant

Question 62

Phentolamine

Answer 62

blcok all a-ARs Opposite of NE decrease peripheral resistance --> hypotension Use: ST BP control in dogs with pheochromocytoma

Question 63

Prazosin

Answer 63

a1-AR antagonist: relax vascular smooth muscle --> decrease peripheral resistance and venous return to heart (cardiac preload) Tx of CHF, hypertension, FLUTD

Question 64

Atipamezole

Answer 64

a1-AR antagonist enter CNS and inhibit analgesic, muscle relaxant, and sedating effects of centrally acting a2-AR agonists (xylazine, medetomidine) antidote for amitraz toxicity

Question 65

Yohimbine

Answer 65

a1-AR antagonist enter CNS and inhibit analgesic, muscle relaxant, and sedating effects of centrally acting a2-AR agonists (xylazine, medetomidine) antidote for amitraz toxicity

Question 66

Propranolol

Answer 66

Class II non-selective B-AR antagonist decreases HR and contractility esp during high sympathetic tone (stress) --> ST decrease in CO blocks effects of NE on AV node and decreases conduction decreases activity of ectopic pacemakers

Question 67

Phenylephrine

Answer 67

a1-AR agonist Arteriolar and venous constriction --> systolic and diastolic BP reflex decrease HR (bradycardia) mydriasis (used b/c shorter duration and no cycloplegia as compared to mAChR blockers)

Question 68

Medetomidine (>xylazine)

Answer 68

a2-AR agonist in CNS w/hyperpolarizing K+ conductance in neurons --> decreases NE release and inhibits NT including central sympathetic outflow (decreases BP) sedative, analgestic, vomiting in cats reversed by a2-AR antagonists (atipamezole)

Question 69

Amitraz

Answer 69

A2-AR agonist insecticide

Question 70

lidocaine

Answer 70

``` CHF drug Na channel blocker - binds open/inactivated slows AV conduction uses: supraventricular tachyarrhythmias Ectopic pacemakers in purkinje fibers ```

Question 71

metoprolol

Answer 71

CHF drug B-AR antagonist decrease B1-AR mediated effect of NE/E on heart decrease pacemaker current --> decrease sinus rt decrease AV nodal conduction reduce ectopic automaticity in bundle of His or ventricle prolong ERP in His bundle, ventricle Uses: decrease ventricular response to supraventricular tachycardia/obstructive heart disease inhibit ventricular arrhythmias associated with high sympathetic tone ( --> sinus tachycardia) ectopic pacemakers in purkinje fibers, atrial fibrillation

Question 72

amiodarone

Answer 72

CHF drug K channel blocker - blocks/widens outward K currents in P3 of ventricular AP atria: increase atrial ERP --> decrease atrial conduction ventricle: slow repolarization of MP and increase AP duration --> decrease ventricular conduction Some secondary sites of action (C1, C2, AARD) Uses: decrease supraventricular tachyarrhythmias, ectopic pacemakers in purkinje fibers

Question 73

sotalol

Answer 73

CHF drug K channel blocker - blocks/widens outward K currents in P3 of ventricular AP atria: increase atrial ERP --> decrease atrial conduction ventricle: slow repolarization of MP and increase AP duration --> decrease ventricular conduction Some secondary sites of action (C1, C2, AARD) Uses: decrease supraventricular tachyarrhythmias, ectopic pacemakers in purkinje fibers

Question 74

diltiazem

Answer 74

CHF drug Ca channel blocker = potent vasodilators Cardiac Ca channels as anti-arrhythmics Use: supraventricular tachycardia, sinus tachycardia, atrial fibrillation (abolishes re-entry) reduce Ca entry in P0 of nodal AP --> decreased AV nodal conduction Potential bradycardic effects thru SA node Ca channels balanced by hypotensive effects of these drugs --> reflex increase in HR

Question 75

verapamil

Answer 75

CHF drug Ca channel blocker = potent vasodilators Cardiac Ca channels as anti-arrhythmics Use: supraventricular tachycardia, sinus tachycardia, atrial fibrillation (abolishes re-entry) reduce Ca entry in P0 of nodal AP --> decreased AV nodal conduction Potential bradycardic effects thru SA node Ca channels balanced by hypotensive effects of these drugs --> reflex increase in HR

Question 76

digitalis

Answer 76

CHF drug increases vagal tone of heart uses: atrial fibrillation If occurring secondary to CHF, then digoxin is preferred (increases vagal tone + inotropic effects)

Question 77

Furosemide

Answer 77

Site 2 Loop diuretic decreases cardiac load Na/K/Cl transporter inhibitor --> ^ Na in tubule ==> water excretion, decreases K, Ca, Mg abs increases Na and water excretion, reducing blood volume

Question 78

Hydrochlorothiazide

Answer 78

site 3 diuretic (early DT) thiazide diuretic decreases cardiac load blocks Na/Cl transporter in early distal tubule, decreased NaCl reabsorption, increased long-term Ca reabsorption increases Na and water excretion, reducing blood volume

Question 79

Spironolactone

Answer 79

site 4 diuretic (late DT/CD) K+ sparing antagonist of mineralocorticoid receptors and inhibits aldosterone mediated Na+ channels --> less reabsorption, lumen is more electro+ --> less K+ secretion use for hypokalemia, edema secondary to hyperaldosteronism dependent on presence of aldosterone

Question 80

Enalapril

Answer 80

CHF drug balanced vasodilator (both aa and vv) ACE inhibitor decreases A-II influence

Question 81

Amlodipine

Answer 81

CHF drug a1-AR blocker balanced vasodilator Ca channel blocker

Question 82

carvediol

Answer 82

``` 3rd generation B-AR antagonist blocks B1>B2, also a1 antioxidant increased CO decreased HR decreased adrenergic influence ```

Question 83

pimobendan

Answer 83

PDE inhibitor - increases cAMP | vasodilation, decreased pre and afterload

Question 84

digoxin

Answer 84

cardiac glycoside decrease Na/Ca exchange by inhibiting Na/K/ATPase activity, increased intracellular Na decreases, Ca pumped out use if you want decreased HR and increased contraction (just changes amplitude of contraction)

Question 85

triamterene

Answer 85

site 4 diuretic (late DT/CD) K+ sparing directly blocks epithelial Na+ channels in principal cells of late distal tubule and collecting duct to stop K excretion use for hypokalemia, edema secondary to hyperaldosteronism not dependent on aldosterone

Question 86

mannitol

Answer 86

osmotic diuretic in PT, TDL, CD creates osmotic gradient decreases water reabsorption increased flow --> less Na+ reabsorption, more urine use in acute renal failure, toxicant elimination, cerebral edema, glaucoma, osmotic laxative

Question 87

Halothane

Answer 87

anesthesia

Question 88

Isoflurane

Answer 88

anesthesia

Question 89

Sevoflurane

Answer 89

anesthesia

Question 90

Nitrous oxide

Answer 90

anesthesia highest MAC lowest blood solubility shortest induction/recovery time

Question 91

Theophylline

Answer 91

bronchodilator methylxanthine inhibits PDE activity --> decreased cAMP breakdown dilates airways increases ciliary beat frequency (mucus clearance) low therapeutic index

Question 92

Atropine

Answer 92

bronchodilator muscarinic receptor blockers dilates airways decreases GI muscle spasms and secretions use for severe asthma unresponsive to other bronchodilators, anti-vomit

Question 93

glycopyrrolate

Answer 93

bronchodilator muscarinic receptor blockers quaternary ammonium (no BBB) dilates airways decreases GI muscle spasms and secretions use for severe asthma unresponsive to other bronchodilators, anti-vomit slow onset, long duration

Question 94

ipratropium

Answer 94

bronchodilator muscarinic receptor blockers quaternary ammonium (no BBB) dilates airways decreases GI muscle spasms and secretions use for severe asthma unresponsive to other bronchodilators, anti-vomit more effective and fewer side effects

Question 95

codeine

Answer 95

antitussive act on opioid receptors decrease sensitivity of cough center medulla to afferent stimuli decrease awareness of irritation use for coughing depresses respiration, blunts CO2 sensitivity

Question 96

butorphanol

Answer 96

antitussive act on opioid receptors: K-opioid R agonist decrease sensitivity of cough center medulla to afferent stimuli decrease awareness of irritation not as much respiratory depression and sedation use for coughing

Question 97

detromethorphan

Answer 97

antitussive does not act at opioid receptor; sigma agonist decrease sensitivity of cough center medulla to afferent stimuli decrease awareness of irritation use for coughing

Question 98

methoxyflurane

Answer 98

anesthesia lowest MAC highest blood solubility of inhalants longest induction/recovery time

Question 99

Acetazolamide

Answer 99

site 1 diuretic (PT) | carbonic anhydrase inhibitor --> decreased Na-bicarb reabs --> ^ urine pH --> ^ H, K, Na excretion

Question 100

famotidine>rantidine>cimetidine

Answer 100

H2-histamine antagonist highly effective, long lasting weak bases decrease acid and pepsin secretion, ^ pH

Question 101

Omeprazole

Answer 101

use for ulcers inhibits H/K ATPase irreversibly increase absorption w/increased pH --> systemic --> enter parietal cell --> stop acid secretion

Question 102

sucralfate

Answer 102

AlOH and sucrose form coating gel at low pH Low absorption binds only ulcerated tissues increases prostanoids, blood flow, GFs does not prevent ulcers/decrease acid output

Question 103

Na/Ca carbonate

Answer 103

antacid rapid onset, prolonged action acid rebound

Question 104

Mg salts

Answer 104

``` antacid intermediate laxatice longer duration ^^^ pH ```

Question 105

AlOH

Answer 105

Slowly increases prostanoids | risk of constipation

Question 106

Warm water/NaCl/3% H2O2/ipecac

Answer 106

irritates GI/distends gut --> stim. afferent nn. --> vomit

Question 107

apomorphine

Answer 107

D2-dopamine agonist in dogs

Question 108

xylazine

Answer 108

ST A2-AR at doses below sedation/hypertension

Question 109

H2 agonists

Answer 109

peripheral anti-emetic

Question 110

Metoclopramide

Answer 110

ST gastric motility prevent relaxation of sphincters block CN D2-DPA receptors and 5HT3 receptors

Question 111

Ondansetron, dolasetron

Answer 111

nlocks serotonin 5HT3 receptors

Question 112

Maropitant

Answer 112

blocks G protein coupled type 1 neurokinin (substance P)

Question 113

Cisapride

Answer 113

partial agonist at 5HT3 receptor, increased motility

Question 114

Erythromyicin

Answer 114

agonist at smooth muscle for motilitn | motility of stomach and upper SI

Question 115

Bisacodyl

Answer 115

ST enteric sensory nn, increased intestinal motility, decreased water reabsorption

Question 116

Kaolin-pectin

Answer 116

absorbs some toxins

Question 117

Bismuth subsalicylate

Answer 117

anti-inflammatory, bacteriocidal, absorb enterotoxins

Question 118

isopropamide, propantheline, n-butyl-scopolammonium bromide

Answer 118

muscarinic cholinergic antagonist quaternary ammonium inhibit intestinal mobility

Question 119

loperamide

Answer 119

opiate stimulant