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Pharmacology - Exam II
Drugs, Classes/Receptors/Mechanisms - Watters
60
Veterinary Medicine
Professional
03/12/2013

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Cards

Term
Drug
Definition
Receptor/Mechanism
Term
Carbachol
Definition
Parasympathomimetic: a synthetic choline ester that is more resistant to AChE and is more selective for mAChRs; Use for ruminal atony, to induce GI motility, and empty bladder
Term
Bethanechol
Definition
Parasympathomimetic: more resistant to AChE and more selective for mAChRs
Term
Muscarine
Definition
Parasympathomimetic: mAChR agonist - natural alkaloid; active ingredient of some poisonous mushrooms
Term
Pilocarpine
Definition
Parasympathomimetic: mAChR agonist - natural alkaloid; used to treat glaucoma (caues miosis)
Term
Atropine
Definition
Parasympathomimetic: mAChR antagonist - belladonna alkaloids; BLOCK PS stimulation; high potency in heart, intestines, bronchioles; increases HR/BP; tx for sinus rhythm bradycardia, GI/urinary muscle spasms, ophthalmology procedures, organophosphate poison tx
Term
Homatropine
Definition
Parasympathomimetic: mAChR antagonist - belladonna alkaloid; lower potency than atropine - tx for sinus rhythm bradycardia, GI/urinary muscle spasms, ophthalmology procedures, organophosphate poison tx
Term
Edrophonium
Definition
Parasympathomimetic: anticholinesterase; short acting/reversible; used to dx myasthenia gravis
Term
Physostigmine & Neostigmine
Definition
Parasympathomimetic: anticholinesterase; long acting/reversible; carbamylated intermediate; if used with Ach - potentiates effects - large dec. in BP/HR; tx for glaucoma, GI atony, Myasthenia gravis
Term
Organophosphate compounds
Definition
Parasympathomimetic: anticholinesterase; irreversible - phosphorylates AChE; highly lipophilic/able to cross BBB and absorbed by lungs, mucous membranes, skin
Term
2-PAM
Definition
AChE reactivator - facilitates the removal of phosphate groups from AChE as long as "aging" has not occurred; give in combo with Atropine to combat organophosphate poisoning
Term
Ivermectin
Definition
Stimulates release of GABA and potentiates inhibitory signaling (removes PS inhibition) - result: tachycardia; mild salivation; mydriasis - tx by giving Neostigmine
Term
Epinephrine
Definition
Direct sympathomimetic: Nonselective adrenergic receptor agonist: used with local anesthetics (alpha-1), tx anaphylaxis/asthma (beta-2), cardiac arrest (beta-1)
Term
Norepinephrine
Definition
Direct sympathomimetic: Nonselective adrenergic receptor agonist: low affinity for beta-2; causes vasoconstriction (alpha-1); increased HR (beta-1); decrease NE relase form terminals (alpha-2)
Term
Pheylephrine
Definition
Direct sympathomimetic: Selective alpha-1-agonist - used to tx hypotension w/o cardiac stimulation
Term
Clonidine
Definition
Direct sympathomimetic: Selective alpha-2-agonist - used to tx hypertension - decreases NE release - decreases vasoconstriction/decreases BP
Term
Isoproterenol
Definition
Direct sympathomimetic: Non-selective beta agonist - used to tx cardiac arrythmias (beta-1 increases contractilty/HR) and acute bronchospasm (beta-2 bronchodilates)
Term
Dobutamine
Definition
Direct sympathomimetic: Selective beta-1 agonist: ICU tx for cardiac arrythmias
Term
Terbutaline, albuterol, clenbuterol
Definition
Direct sympathomimetic: Selective beta-2 agonists: tx for bronchial asthmas and airway obstruction
Term
Phentolamine, tolazoline
Definition
Sympatholytics - adrenergic blocking drug: Non-selective COMPETITIVE alpha antagonists - used to tx hypertension
Term
Phenoxybenzamine, dibenamine
Definition
Sympatholytics - adrenergic blocking drug: Non-selective NON-COMPETITIVE alpha antagonists - tx for pheocromocytoms/hypertension
Term
Prazosin
Definition
Sympatholytics - adrenergic blocking drug: Selective alpha-1 antagonist; used to tx hypertension/adjunct therapy for CHF
Term
Yohimbine
Definition
Sympatholytics - adrenergic blocking drug: Seletive alpha-2 antagonist; reverse toxic effects of xylazine (prevents feedback inhibition from happening so more NE is released and the dog wakes up)
Term
Propranolol
Definition
Sympatholytics - adrenergic blocking drug: Non-selective beta antagonist - tx exercise - induced arrhythmias since heart is PS at rest (at rest, only see slight depression of HR, contractile force, and CO)
Term
Metoprolol
Definition
Sympatholytics - adrenergic blocking drug: Selective beta-1 antagonists; used to tx supraventricular tachycardia and PVCs (safer than propranolol because doesn't bronchoconstrict)
Term
Amitryptiline
Definition
Indirect sympathomimetic: amine transporter blocker - result: increased NE in the terminals - little effect on dopamine transporters; used to tx behavior disorders, neuropathic pain
Term
Imipramine
Definition
Indirect sympathomimetic: amine transport blocker - result: increased NE in the terminals; HAS inhibitory effect on DA transports; tx for cataplexy, narcolepsy
Term
Amphetamines
Definition
Indirect sympathomimetic: cause release of NE into synpatic cleft - causes tachyphyllaxis (type of pharmacodynamic tolerance where there is a rapid loss of response to a drug w/o a change in the R)
Term
Ephedrine
Definition
Indirect sympathomimetic: cause release NE into synpatic cleft/substitude amphetamine; used in cold medicines as a decongestant (pseudophedrine/phenylephrine) and treats urinary incontinence (agonizes alpha-1)
Term
Amphetamine
Definition
Indirect sympathomimetic: cause release of NE into synpatic cleft; can cross BBB/CNS effects; addictive to do DA release; appetite suppression due to potentiation of 5HT release
Term
Selegiline
Definition
Indirect sympathomimetic: MAOIs - NE is more availiable for action potentials because free NE is not degraded; used as an antidepressant in humans b/c interferes with DA and 5HT degradation; tx of cognitive dysfunciton in canines
Term
Reserpeine
Definition
Sympatholytics - adrenergic neuron blocking drug: impairs cytoplasmic uptake into storage vesicles, so MAOs deplete NE in the terminals
Term
Guanethidine
Definition
Sympatholytics - adrenergic neuron blocking drug: displaces NE from storage vesicles so MAOs break down NE
Term
Nicotine
Definition
Ganglionic drug: effect determined by predominant tone - potent/crosses BBB, causes release of DA, NE, 5HT and behaves like Ach
Term
DMPP
Definition
Ganglionic drug: effects determined by predominant tone
Term
Mecamylamine, Hexamethonium, Trimethapan
Definition
Ganglionic blockers: competes with Ach for binding to nAChRs (competitive antagonist) - used to treat hypertension and reduce bleeding during surgery
Term
Diazepam
Definition
GABAa channel agonist - treats epileptic seizures and muscle spasms
Term
Pentobarbital
Definition
GABAa channel agonist - anesthetic
Term
Verapamil
Definition
Voltage-gated ion channel antagonist - Ca++ channel blocker - decreases HR in patients w/supraventricular tachycardias
Term
Lidocaine
Definition
Voltage-gated ion channel antagonist - Na+ channel blocker - local anesthetic
Term
Cholera Toxin (CTX)
Definition
Ribosylates Gs so it's always on - AC constitutively activated - chronically elevated cAMP - massive efflux of water from blood to lumen
Term
Pertussis (PTX)
Definition
Ribosylates Gi so it's always off - AC always active - chronically elevated cAMP - massive efflux of water from blood to lumen
Term

Methylxanthines:

Theophyllines, Aminophylline, Caffeine, Theobromine

Definition

Inhibit cAMP-phospodiesterases so cAMP is always on - Beta-1 receptor (Gs)... also antagonizes adenosine receptors that stimulate contraction (Gi);

 

main ingredient in chocolate; toxicosis - vomiting, restlessness, hyperactivity, hypotension, tachycardia;

 

results - bronchodilation, CNS/Cardiac Stimulation

Term
NO
Definition
Endogenous signaling - primary determinant of resting vascular tone; important in CNS, cardiovascular, immune system; activates Soluble Guanylate Cyclase (GC) - increases PKG which causes strong vascular/airway dilation via decreasing myosin-actin interaction, activates K+ channels, and decreases activity of proteins involved in Ca++ efflux/store release
Term
Nitroglycerin
Definition
Exogenous NO donor - alleviates angina by decreasing cardiac workload and myocardial oxygen requirement
Term
Sildenafil (Viagra), Vardenafil (Levitra), Tadalafil (Cialis)
Definition
Inhibitors of cGMP phosphodiesterases (PDEs) - tx for erectile dysfunction and pulmonary hypertension; highly specificl for PDE is vasculature (PDE 5)
Term
Mannitol & Glucose
Definition
Osmotic diuretic: Unabsorbed synthetic sugar draws water into the lumen; freely filtered by glomerulus, poorly reabsorbed by the renal tubule, relatively inert pharmacologically
Term
Furosamide (Lasix)
Definition
Loop diuretic: Inhibitor of Na+/K+/2Cl- symport in loop of Henle
Term
Hydrochlorothiazide
Definition
Thiazides: inhibitors of Na+/Cl- reabsorption in distal convoluted tubule; decrease calciuresis
Term
Spirolactone
Definition
Potassium-sparing: mineralcorticoid receptor antagonists (may oppose fibrotic effects of increased aldosterone concentration in heart and kidneys); late distal convoluted tubule and collecting duct
Term
Acetazoamide/Methazolamide
Definition
Carbonic anhydrase inhibitors in renal proximal tubule - HCO3- lost with Na+ and K+ following; used for glaucoma, hyperkalemic periodic paralysis, acute mountain sickness
Term
Phenylpropanolamine - PPA (lower urinary tract)
Definition
Alpha adrenergic agonist - increase NE release to increase internal sphincter tone (alpha)
Term
Diethylstilbestrol (lower urinary tract)
Definition
Synthetic estrogen - enhances binding of catecholamines via increased sensitivity to NE to increase internal sphincter tone (alpha-1)
Term
Penoxybenxamine (lower urinary tract)
Definition
Alpha receptor antagonist - relax urethral tone (use for urethral spasms or refractory hypertension)
Term
Prazocin (lower urinary tract)
Definition
Alpha-1 adrenergeric antagonists - relax urethral tone (urethral spasm or refractory hypertension)
Term
Benzodiazepines: Midaozlam, Diazepam, Alprazolam
Definition
Facilitates GABAa action central - central sedative, anxiolytic, anticonvulsant, skeletal muscle relaxant
Term
Bethanechol (lower urinary tract)
Definition
Cholinergic (Ach) agonist - increase detrusor tone (used for bladder atony)
Term
Oxybutynin (lower urinary tract)
Definition
Cholinergic antagonist - relax detrusor muscle (decreases bladder spasms associed with chronic inflammation/infection)
Term
Finasteride (Proscar) - prostatic disease
Definition
Inhibits 5-alpha reductase (necessary enzyme for bioactivating testosterone to a more active form - DHT)
Term
Tamsulosin (Flomax) - prostatic disease
Definition
Antagonist of alpha - 1A adrenergic receports - relaxes smooth muscles within prostatic urethra
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