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Pharmacology Block 1
Drug/Mechanism
55
Medical
Graduate
01/20/2008

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Cards

Term
norepinephrine
Definition
a1 (a2, ß1) vasoconstriction to increase BP; reflex bradycardia decreases HR
Term
epinephrine
Definition
ß1 increase HR and contractile force to increase CO (increase SBP); ß2 bronchodilation, hyperglycemia (increase gluconeogenesis and glycogenolysis), lipolysis, (decrease DBP so overall no BP change); (a1,a2)
Term
isoproterenol
Definition
ß1 increase HR and contractile force to increase CO (increase SBP w/relex decrease PR so overal BP decrease); ß2 bronchodilation
Term
dopamine
Definition
D1 (@low dose) renal vasodilation increase BF to kindey and increase in renal function; ß1 (@ medium dose) increase HR and contractile force to increase CO with reflex BP drop; a1 (@ high dose) vasoconstriction with increase in BP
Term
dobutamine
Definition
ß1 increase HR and contractile force to increase CO w/minimal increase in BP
Term
methyldopa
Definition
a2 in CNS, potent decrease in SNS output and BP decrease
Term
phenylephrine
Definition
a1 vasoconstriction increases BP with reflex decrease in HR, decreases BF to most vascular beds
Term
clonidine
Definition
a2 in CNS, potent decrease in SNS output and BP decrease
Term
ritodrine
Definition
ß2 uterine relaxation
Term
albuterol
Definition
ß2 bronchodilation
Term
terbutaline
Definition
ß2 bronchodilation
Term
cocaine
Definition
blocks NE re-uptake into nerve terminals by blocking UPTAKE 1
Term
tyramine
Definition
releases NE from adrenergic neurons; metabolized my MAO to inactivate
Term
amphetamine
Definition
releases NE from adrenergic neurons; weak direct a and ß agonist; weakly blocks UPTAKE 1 b/c competes for uptake
Term
ephedrine
Definition
direct ß2 agonist; releases NE
Term
pseudoephedrine
Definition
a1 agonist; slight ß2 agonist; slight NE releasing affects
Term
alpha-methyl-tyrosine
Definition
blocks tyrosine hydroxylase (rate-limiting step of NE synthesis)
Term
guanethidine
Definition
uses UPTAKE 1 to enter adrenergic neurons; initially blocks NE release by inhibiting Ca2+ channels; long term use depletes NE from storage vesicles
Term
reserpine
Definition
diffuses into adrenergic neuron; depletes NE; inhibits UPTAKE 1
Term
phenoxy-benzamine
Definition
competitive irreversible a1 and a2 antagonist
Term
phentolamine
Definition
competitive reversible a1 and a2 antagonist
Term
prazosin
Definition
selective competitive reversible a1 antagonist
Term
propranolol
Definition
non-selective competitive reversible ß1 and ß2 antagonist
Term
timolol
Definition
non-selective competitive reversible ß1 and ß2 antagonist
Term
metoprolol
Definition
selective competitive reversible ß1 antagonist
Term
esmolol
Definition
ultra-short acting selective competitive reversible ß1 antagonist
Term
carvedilol
Definition
non-selective competitive reversible ß1, ß2, and a1 antagonist; anti-oxidant properties
Term
bethanechol
Definition
muscarinic agonist resistant to degradation by acetylcholinesterase, so longer duration of action
Term
pilocarpine
Definition
constriction of circular iris m. to open up angle to canal of schlemn (narrow); constriction of ciliary m. to promote drainage by better aligning obstructed canal (wide)
Term
edrophonium
Definition
rapid onset, short duration of action
Term
physostigmine
Definition
substrate hydrolyzed at a slow rate
Term
neostigmine
Definition
substrate hydrolyzed at a slow rate
Term
sarin
Definition
organophosphate acetylcholinesterase inhibitor; phosphorylates the serine in the substrate-binding domain
Term
parathion
Definition
organophosphate acetylcholinesterase inhibitor; phosphorylates the serine in the substrate-binding domain
Term
echothiophate
Definition
organophosphate acetylcholinesterase inhibitor; phosphorylates the serine in the substrate-binding domain
Term
hemicholinium
Definition
blocks uptake of choline into nerve terminals (rate-limiting step of Ach synthesis)
Term
botulinium toxin
Definition
prevents release of Ach by cleaving vesicle/membrane tethering proteins
Term
pralidoxime
Definition
reactivates enzyme inactivated by organophosphate inhibitors
Term
atropine
Definition
reversible competitive muscarinic receptor antagonist
Term
scopolamine
Definition
reversible competitive muscarinic receptor antagonist
Term
ipratropium
Definition
reversible competitive muscarinic receptor antagonist
Term
trimethaphan
Definition
post-ganglion nerve blocker of both SNS and PNS
Term
mivacurium
Definition
non-depolarizing competitve antagonist
Term
atracurium
Definition
non-depolarizing competitve antagonist
Term
vecuronium
Definition
non-depolarizing competitve antagonist
Term
pancuronium
Definition
non-depolarizing competitve antagonist
Term
succinylcholine
Definition
depolarizing blockade b/c opens Ca2+ channels on endplate; dimer of 2 Ach molecules; produces muscle fasciculations and flaccid paralysis
Term
lysergic acid diethylamide
Definition
potent visual hallucinations
Term
sumatriptan
Definition
vasocontriction of inflammed/dilated cerebral vasculature
Term
tegaserod
Definition
GI smooth muscle constriction to stimulate motility and stimulates intestinal secrestions
Term
fluoxetine
Definition
selective serotonin reuptake inhibitor (SSRI) causing increase serotonin
Term
phenelzine
Definition
MAO inhibitor, blocks serotonin metabolism
Term
sibutramine
Definition
nonselective reuptake inhibitor (serotonin, norepinephrine, dopamine); serotonin enhances satiety, norepinephine increases metabolism
Term
cyproheptadine
Definition
also antagonizes H1 receptor
Term
ondansetron
Definition
blocks brain and GI nausea and vomiting centers
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