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PHM - Exam 2 - Drugs - Receptors; Actions
N/A
65
Medical
Graduate
06/01/2013

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Term
Phenyleprine
Definition
alpha-1 D-Ag; BP under anesthesia; short duration mydriasis; nasal decongestant; for acute hypotension
Term
Clonidine
Definition
alpha-2 D-Ag; Tx HT;opiate withdrawal; decrease BP in CNS
Term
Isoproterenol
Definition
beta-1,2 D-Ag;increase in CO + decrease in MAP; brief duration (COMT); for emergency cardiac arrest or heart block.
Term
DA
Definition
beta-1 D-Ag; D1,2 Ag; short duration (MOA; COMT) increase renal/mesenteric bld. flow; natriureisis (D1); Vomiting (D2); NE release (NET substrate); vasoconstriction (alpha-1); for cardiogenic shock
Term
Dobutamine
Definition
beta-1 D-Ag; short duration; no DA-R activation; for cardiogenic shock
Term
Terbutaline
Definition
beta-2 D-Ag; can be administered sub-q; rapid onset, short duration; delay labor
Term
Albuterol
Definition
beta-2 D-Ag; rapid onset, short duration; prevents HISTAMINE release from mast cells
Term
Salmeterol
Definition
beta-2; prophylaxis of exercise-induced asthma; slow onset, long duration
Term
Ritodrine
Definition
beta-2 D-Ag; uterine relaxant, delay labor
Term
Amphetamine
Definition
I-Ag; blocks NET; reverse NE transport; oral; BBB penetration; for narcolepsy, ADHD
Term
Methylphenidate
Definition
I-Ag; structural analog of amphetamine; for ADHD
Term
Ephedrine
Definition
I-Ag; increases NE in synapse; short t1/2; alpha-1, beta-2 D-Ag; for asthma, enuresis, nasal decongestion
Term
Pseudoephedrine
Definition
I-Ag; increases NE in synapse; alpha-1 D-Ag; for nasal decongestion
Term
Tyramine
Definition
I-Ag; releases catecholamines; in food; byproduct of Tyr metabolism; short t1/2 (MAO)
Term
Cocaine
Definition
I-Ag; blocks NET; powerful CNS stimulant; DA reuptake inhibitor;
Term
MAOi (Phenelzine); COMTi (Entacapone)
Definition
I-Ag; prevents secondary NE deamination after reuptake; for depression and Parkinson's respectively (decreases DA degradation = increased levadopa t1/2)
Term
Metyrosine
Definition
catecholamine synthesis inhibitor; inhibits Tyr hydroxylase; for pheochromocytoma
Term
Carbidopa
Definition
catecholamine synthesis inhibitor; inhibits aromatic L-amino acid decarboxylase; blocks levadopa-->DA in PNS = levadopa into CNS; + levadopa for Parkinson's
Term
Phenoxybenzamine (PBZ)
Definition
non-selective alpha Antag.; irreversible; decreases BP (reflexive tachycardia and increased CO); increses NE release; tissue responsiveness restored when new receptors made; for preoperative management of pheochromocytoma and Reynaud's
Term
Phentolamine
Definition
non-selective alpha Antag.; reversible; decreases BP (reflexive increase in CO and tachycardia); for BP control during pheochromocytoma and erectile dysfunction
Term
Prazosin
Definition
reversible alpha-1 Antag.; decreases vascular resistance (for peripheral vascular disease/Reynaud's) and venous return (for HT); relaxes prostatic sm. mm. (BPH); decreases LDLs and TGs, increases HDLs.
Term
Terazosin
Definition
reversible alpha-1 Antag.; water soluble and high bioavailability; for HT and BPH
Term
Doxasosin
Definition
reversible alpha-1 Antag.; long duration; for HT and BPH
Term
Tamsulosin
Definition
reversible alpha-1 Antag.; relaxes prostatic sm. mm; short duration;
Term
Yohimbine
Definition
reversible alpha-2 Antag. = NE release; for hypotension; reverse HT effects of clonidine; little clinical value
Term
Propranolol
Definition
non-selective beta blocker; reduces HR, BP, renin; highly lipophilic (for migraine); liver metabolized (first pass); for ischemic heart disease
Term
Timolol
Definition
non-selective beta blocker; reduces HR, BP, renin; less lipid soluble, NO local anesthetic effect; for open angle glaucoma (decreases aq. humor secretion)
Term
Labetalol
Definition
non-selective beta blocker, competitive alpha-1 Antag., beta-2 agonist; reduces HR, BP, renin; local anesthetic; for HT (alpha-1 block + beta-2 agonist = vasodilation)
Term
Carvedilol
Definition
non-selective beta blocker, alpha-1 Antag.; NO local anesthetic effect; for CHF and myocardial infarction
Term
Atenolol
Definition
beta-1 blocker; drop in HR, BP, and contractility; NO local anesthetic effect, for HT, angina and arrhythmia
Term
Metoprolol
Definition
beta-1 blocker; drop in HR, BP, and contractility; local anesthetic; first pass; for HT, heart failure, and arrythmia
Term
Esmolol
Definition
beta-1 blocker; drop in HR, BP, and contractility; short t1/2; NO local anesthetic effect; for tachycardia, arrhythmia, HT, thyroid storm
Term
ACh
Definition
direct acting cholinergic agonist; = parasympathetic stimulation; brief duration (AChE); vasodilation, miosis, near vision, glandular secretion, bronchial constriction, bradycardia, GI activity
Term
Metacholine
Definition
direct acting cholinergic agonist; less hydrolysis; cardiovascular-selective; reduces HR, contractility, contraction vel., for asthma diagnosis
Term
Bethanechol
Definition
direct acting cholinergic agonist; bladder and GI tract; mAChR-selective; very resistant to hydrolysis;
Term
Succinylcholine
Definition
direct acting cholinergic agonist; nAChR-selective; depolarizing blockade desensitization = muscle paralysis; Phase1/2 block; metabolized by pseudoChE in plasma
Term
Carbachol
Definition
direct acting cholinergic agonist; mAChR-selective; very resistant to hydrolysis; reduces HR, contractility, and conduction vel.
Term
Muscarine
Definition
direct acting cholinergic agonist; not used clinically; toxicity if enters CNS
Term
Nicotine
Definition
direct acting cholinergic agonist; nAChR-selective; can be absorbed across skin; will desensitize; CNS stimulant
Term
Pilocarpine
Definition
direct acting cholinergic agonist; mACHR-selective; well absorbed
Term
Neostigmine
Definition
carbamate indirect cholinergic agonist; also nAChR agonist; intermediate duration of action; for Myasthenia Gravis, slow Alzheimer's
Term
Physostigmine
Definition
carbamate indirect cholinergic agonist; crosses BBB; for anticholinergic poisoning
Term
Malathion and Parathion
Definition
organophosphate indirect cholinergic agonist; irreversible conjugate with AChE (longest duration); well absorbed (skin, gut, lungs); crosses BBB; insecticides
Term
Endrophonium
Definition
simple alcohol indirect cholinergic agonist; reverses muscle weakness in pts with Myasthenia Gravis only
Term
Atropine
Definition
naturally occurring antimuscarinic; inverse agonist; well absorbed (gut and conjunctiva); crosses BBB; potent against salivary, bronchial, and sweat glands; for cholinergic poisoning, reversal of sinus bradycardia, and reduce secretions during surgery, prolonged midriasis (also cycloplegic)
Term
Scopolamine
Definition
naturally occurring antimuscarinic; fast onset; crosses skin and BBB; for motion sickness, to reduce secretions during surgery
Term
Ipratropium
Definition
synthetic antimuscarinic; for asthma and COPD
Term
Pirenzepine
Definition
synthetic antimuscarinic; for peptic ulcers (M1-selective: autonomic ganglia and CNS)
Term
Tolterodine
Definition
synthetic antimuscarinic; M3-selective (smooth mm. and glands); for urinary incontinence
Term
Apraclonidine
Definition
alpha-2 Ag.; does NOT cross BBB (minimal systemic effect); for OAG
Term
Cyclopentate
Definition
mAChR Antag.; mydriasis and cycloplegia; 1 day duration; for OAG
Term
Tropicamide
Definition
mAChR Antag.; mydriasis and cycloplegia; 5-6 hrs duration (shortest); for OAG
Term
Bromonidine
Definition
alpha-2 Ag; decrease in aq. secretion and increased outflow; crosses BBB; for OAG
Term
Trimethaphan
Definition
ganglionic blocker; inhibits autonomic postganglionic AChR (competitive); IV-admin; for hypertensive emergencies
Term
Hexamethonium
Definition
ganglionic blocker; blocks channel after opening; inhibits autonomic postganglionic R; for HT
Term
Mecamylamine
Definition
ganglionic blocker; inhibits autonomic postganglionic R; crosses BBB
Term
Tubocurarine
Definition
nondepolarizing neuromuscular blocker; Cholinergic Antag.; doesn't cross BBB; for reducing dosage of anesthesia during surgery
Term
Cisatracurium
Definition
nondepolarizing neuromuscular blocker; potent and less likely to cause histamine release; most widely used muscle relaxant; short duration (25-45 min); not dependent on renal or hepatic function; for relaxation during surgery
Term
Pancuronium
Definition
nondepolarizing neuromuscular blocker;
Term
Vecuronium
Definition
nondepolarizing neuromuscular blocker; 5x more potent than tubocurarine; elimination by liver; very short duration (35 min)
Term
Mivacurium
Definition
nondepolarizing neuromuscular blocker; rapid onset; shortest duration (10-20 min); metabolized by pseudocholinesterase
Term
Diazepam
Definition
spasmolytic; facilitates GABA binding to GABA-A-R; opens Cl- channels; inhibits SC primary afferents; for chronic spasm from cerebral palsy, muscle injury, spinal cord injury
Term
Baclofen
Definition
spasmolytic; GABA-B-receptor Ag.; increased K+ conductance, inhibits substance P release; orally active; for pain reduction (intrathecal admin., for spasticity due to cerebral palsy, MS, stroke.
Term
Dantrolene
Definition
spasmolytic; inhibits Ca2+ release; binds to ryanodine R (disrupts excitation-contraction coupling); for malignant hyperthermia
Term
Botulinum toxin
Definition
spasmolytic; inhibits ACh release at presynaptic terminals (cleaves SNARE); duration of weeks and months; for spastic disorders, face wrinkles, strabismus
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