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Systems Pharmacology II
B-Blockers
26
Biology
Graduate
02/21/2012

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Term
MOA
Definition
-competitively block effects of endogenous NE and Epi at the B-receptors
-inhibits the normal sympathetic effects that act thru B receptors
Term
general considerations
Definition
-bind both b1 and b2
-some selective
-some ISA
-some membrane stabilizing activity
-hydro/lipophilicity influece duration of action, elimination and SE
Term
ISA
Definition
-intrinsic sympathomimetic activity
-ability of b-blocker to stimulate b-adrenergic receptors weakly
-provides background of sympathetic activity while preventing normal activity
-inhibit activation of B receptors when SNS is stimulated
-useful in pts who become bradycardic or bronchoconstriction while on full antagonist
Term
MSA
Definition
-membrane stabilizing activity
-MSA block myocyte sodium channels
-prevents proper cardiac conduction
-no therapeutic role in HTN
-seizures more commonly onserved in drugs with MSA
-b-blockers with MSA are associared with largest proportion of fatalities at toxic doses
Term
lipophilic
Definition
-interpatient variability
-drug drug interactions
-CNS SE
Term
hydrophilic
Definition
-not much inter-patient variability
-less drug drug interactions
-less CNS SE
Term
therapeutic indications
Definition
-HT
-angina
-post MI
-arrhythmias
-heart failure
Term
how b-blockers reduce BP
Definition
Term
why taper off b-blocker therapy
Definition
Term
nonselective general
Definition
-CNS SE most common here
-1st generation
-bind both b1 and b2
-HR not affected
Term
*Propanolol
Definition
-1st clinically active b-blocker
-lipophilic
-IV and PO
Term
nonselective
Definition
-propanolol
-nadolol
-timolol
Term
*nadolol
Definition
-45 hour half life in end stage renal disease
-PO
Term
timolol
Definition
-indication-open angle glaucoma
-PO, opthalmic solution, gel-forming solution
Term
B1 selective general
Definition
-cardioselectivity is NOT associated with a difference in lowering BP lowering effect
-all b-blockers are non selective at high doses
Term
b1-selective
Definition
-acebutolol
-atenolol
-betaxolol
-bisoprolol
-esmolol
-metoprolol
-nebivolol
Term
acebutolol
Definition
-ISA and MSA
-hydrophilic
-PO
Term
*atenolol
Definition
-excreted largely unchanged
-use caution with people with reduced renal function
-PO
Term
betaxolol
Definition
-one of most potent b-blocker
-preferred for pts with bronchospastic pulmonary disease
-indications-HTN,glaucoma,ocular HTN
Term
*bisoprolol
Definition
PO
Term
Esmolol
Definition
-only in ER setting due to extremely short half life
-continuous IV
Term
*metoprolol
Definition
-PO and IV
-succinate
-B1
Term
nebivolol
Definition
-most b-1 selective
-vasodilatory properties due to NO modulation
-PO
Term
mixed b and a antagonists
Definition
-labetalol
-carvedilol
Term
labetalol
Definition
-antagonist at b1 b2 and a1
-PO and IV
Term
*carvedilol
Definition
-*antagonist at b1 b2 a1
-PO
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