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Drug-Receptor Set 1
Drugs and Receptors for Pharm Exam 1
72
Pharmacology
Graduate
11/04/2010

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Cards

Term
Phentolamine
Definition
nonselective competitive alpha antagonist - not metabolized by COMT in liver
Term
phenoxybenzamine
Definition
irreversible alpha antagonist
Term
prazosin
Definition
alpha-1 antagonist (reversible)
Term
tamsulosin
Definition
reversible alpha1 antagonist
Term
metoprolol
Definition
beta1 inhibitor (high doses beta2)
Term
atenolol
Definition
beta1 blocker
Term
propanolol
Definition
non-selective beta blocker
Term
pindolol
Definition
partial beta agonist (non selective)
Term
carvedilol
Definition
non selective beta blocker + alpha1 blcokage
Term
nebivolol
Definition
selective beta1 blocker
Term
labetolol
Definition
nonselective beta blocker (partial beta2 agonist) and alpha1 blocker
Term
timolol
Definition
nonselective beta-competitive antagonist
Term
fenoldopam
Definition
D1 receptor agonist. some alpha2 stimulation
Term
nicotine
Definition
Nicotinic muscular or neurologic receptors
Term
bethanechol
Definition

muscarinic receptor agonist (predom. M3)

crosses BBB poorly

Term
methacholine
Definition

quarternary ester - nonselective muscarinic agonist

- not a substrate for Acetylcholine esterase

Term
pilocarpine
Definition
nonselective muscarinic agonist (predom M3)
- partial agonist
Term
carbachol
Definition
quarternary ester - nonselective cholinergic agonist (N and M receptors)
cannot be digested by acetylcholinesterase
Term
atropine
Definition
nonselective muscarininc antagonist
Term
scopolamine
Definition
tertiary amine - nonselective muscarinic antagonist
Term
ipratropium
Definition
nonselective muscarinic antagonist
(inhaled - predom M3)
Term
glycopyrrolate
Definition
nonselective antimuscarinic agent
Term
oxybutynin
Definition
competitive muscarinic antagonist (mainly GI/GU M3)
Term
tolterodine
Definition
muscarinic antagonist
tertiary amine with greater selection for M3
Term
succinylcholine
Definition
Nm agonist
- not digested by acetylcholinesterase
- hydrolyzed in plasma and liver by pseudocholinesterases
- may stimulatate ganglionic nicotinic Ach-R and cardiac muscarinic Ach-R
Term
pancuronium
Definition
- partial agonist at Ach-R
- competitive antagonist of Nm
Term
atracurium
Definition
competitive Nm antagonist
- eliminated by spontaneous hydrolysis, no ganglionic block, no cardiac M2 block
Term
cisatracurium
Definition
competitive Nm antagonist
Term
Tubocurarine
Definition
competitive antagonist at Nm receptor
Term
neostigmine
Definition
carbamate inhibitor of Ach-esterase
- does not penetrate BBB
Term
pyridostigmine
Definition
carbamate acetylcholinesterase inhibitor
- does not penetrate BBB
Term
edrophonium
Definition
noncarbamate Ach-esterase inhibitor with short half life
Term
donepezil
Definition
cholinesterase inhibitor
- crosses BBB readily
Term
galantamine
Definition
minimal binding, crosses the BBB, noncovalent Ach-esterase inhibitor
Term
physostigmine
Definition
cholinesterase inhibitor - crosses the BBB
Term
sarin
Definition
organophosphate Ach-esterase inhibitor
Term
DFP (diisopropyl fluorophosphate)
Definition
organophosphate Ach-esterase inhibitor (not a drug)
Term
2-PAM (pralidoxime)
Definition
cholinesterase regenerator
- only useful in organophosphate toxicity
Term
epinephrine
Definition
direct sympathomimetic
- stimulates alphas and betas nonselectively (beta predom at low dose, alpha at high dose)
Term
norepinephrine
Definition
selectively stimulates alphas more than beta1 (but NO beta2)
Term
dopamine
Definition
stimulates D1 > beta1 > alpha1
- does not cross BBB
Term
dobutamine
Definition
stimulates beta1 >> beta2 >> alpha1=alpha2
- racemic mixture (+ goes beta1 selective, alpha1 antagonist; - is alpha1 agonist)
Term
amphetamine
Definition
causes release of endogenous norepinephrine and, at higher doses, dompamine and serotonin
Term
ephedrine
Definition
release of norepi from sympathetic neurons
- some adrenergic agonist action
- activates alphas and betas
Term
pseudoephedrine
Definition
- precursor for meth drug
- stimluates release of NE from sympathetic neurons
Term
phenylephrine
Definition
- alpha1 agonist
Term
clonidine
Definition
alpha2 agonist
- presynaptic symapthetic neurons --> decreased NE release
Term
isoproterenol
Definition
nonselective beta-agonist
- metabolism in liver and tissues by COMT
Term
albuterol
Definition
beta2 agonist
Term
salmeterol
Definition
beta2 agonist
Term
ritodrine
Definition
beta-2 agonist
Term
sumatriptan
Definition
selection serotonin agonist for 5-HT1B and 5-HT1D
Term
odansetron
Definition
selective serotonin antagonist 5-HT3
Term
alosetron
Definition
selective serotonin 5-HT3 antagonist
Term
tegaserod
Definition
5-HT4 partial agonist
Term
prochlorperazine
Definition
D2 dopamine receptor antagonist
Term
metoclopramide
Definition
D2 antagonists and weak 5-HT3 antagonist, 5-HT4 agonist
Term
cromolyn
Definition
alters chloride channels for cell stabilization
- inhibit degranulation of mast cells and eosinophils
Term
nedocromil
Definition
chloride channel alteration (cell stabilizer)
- inhibit degranulation of mast cells and eosinophils
Term
diphendyramine
Definition
inhibitor of histamine H1 receptors
- lipid soluble so can travel to CNS
Term
cyproheptadine
Definition
5-HT2 blocker and H1 blocker
Term
fexofenadine
Definition
competitive inhibitor of H1 receptors
- does not cross BBB
Term
cimetidine
Definition
inhibits H2 receptors
Term
omeprazole
Definition
inhibits H+/K+ ATPase (proton pump inhibitor)
- racemic mixture
Term
esomeprazole
Definition
S-isomer of omeprazole
- proton pump inhibitor (Na+/K+ ATPase)
Term
Cevimeline Hydrochloride
Definition
muscarinic agonist
Term
Acetylcholin
Definition
endogenous agonist
- activates cholinergic receptors
- M1, M3, M5 - Ca2+ influx (via IP3 and DAG)
- M2 & M4 - decrease cAMP and K+ channels opened
- NM and NN - depolarization due to Na+,K+ channels opening
Term
mecamylamine
Definition
ganglionic blocker of sympathetics and parasympathetics
Term
tyramine
Definition
causes NE release from adrenergic terminals
Term
serotonin
Definition
5-HT3 is ligand gated Na+, K+ channel 5-HT1-7 (except for 3) are GPCRs
Term
cisapride
Definition
5HT4 agonist, 5HT3 antagonist
Term
histamine
Definition
4 receptors
H1 - GPCR (Gq)
H2 - GPCR (Gs)
H3 - GPCR (Gi)
H4 - GPCR (Gi)
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