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FIU Beta blockers and agonists
Beta blockers and agonists
30
Pharmacology
Professional
01/03/2012

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Cards

Term
beta 2 receptor agonist PD, effect, uses
Definition
increase cAMP by activating Gs protein which decreases cytosolic Ca...also decreases histamine and LT release; relaxes smooth muscle and mild anti-inflammatory; for asthma (COPD), uterus relaxation (delays birth/also use Mg), hyperkalemia (squeezes K into cell, insulin/dextrose is first-line tx)
Term
-terol, effect
Definition
beta 2 agonists, smooth muscle relaxation
Term
Albuterol mode of action, onset/offset, use, side effect, secretion, good guy: R/S isomer?
Definition
beta-2 agonist; rapid onset/short acting (ROSA); asthma reliever (2-4 hr); tachycardia (some beta 1 action); renal secretion; R = eutomer, more affinity for beta 2 than distomer (L)
Term
levalbuterol mode of action, onset/offset, use, side effect
Definition
only eutomer version of albuterol beta-2 agonist; rapid onset/short acting (ROSA); asthma reliever (2-4 hr); less tachycardia (more selective for beta 2 than beta 1 than albuterol)
Term
ROSA beta 2 agonists, use
Definition
bambuterol -> terbutalin, fenoterol, reproterol, pirbuterol, bitolterol -> colterol (slow onset); asthma relievers (2-4 hr)
Term
Long acting beta 2 agonists, use, current trend?
Definition
salmeterol, formoterol; asthma controllers (> 10 hr), move toward anti-inflammatory steroids as controllers
Term
Salmeterol mode of action, use, onset/offset
Definition
partial beta 2 agonists, asthma controller, slow onset/long acting (SOLA)
Term
Formoterol mode of action, use, onset/offset
Definition
beta 2 agonist; asthma controller OR reliever; rapid onset/long acting (ROLA)
Term
beta 1 receptor agonist PD, effect
Definition
increase cAMP, inotropic
Term
dobutamine mode of action, effect, synthetic version of?
Definition
pseudo beta 1 agonist (alpha 1 agonist and antagonism of racemic mix cancel); inotropic used by surgeons; synthetic catecholamine
Term
dopamine dose effects: low, medium, high?
Definition
Low (D1) = renal dose, dilates renal vasculature, increased RPF/perfusion; medium (beta 1) = heart dose, increased heart rate; high (alpha 1) = increased vasoconstriction, afterload and oxygen consumption.
Term
dopexamine mode of action, effect, use, synthetic version of?
Definition
D1 and beta 2 agonists at low dose, decreases afterload (vasodilation) and O2 consumption, inotropic; synthetic catecholamine (dopamine)
Term
fenoldopam mode of action, use, equivalent to?
Definition
selective D1 agonist; anti-hypertensive; like low dose dopamine (renal dose)
Term
Isoprenaline mode of action, effect, synthetic version of?
Definition
non-selective beta agonist; inotropic and vasodilation/decrease afterload (increase in O2 consumption more moderate like PDE III inhibitors); synthetic catecholamine
Term
ISA, advantage?
Definition
Intrinsic sympathomimetic activity; less likely to overdose on beta blockers with this (blockers also partial agonists), no increase in TG, LDL or glucose
Term
selective beta 1 blockers effect, at high doses,examples?
Definition
slow heart without vascular effect; lose selectivity at high doses; metaprolol, atenolol, acebutolol
Term
Beta blocker effect, side effects? for overdose?
Definition
vasodilation; loss of ability to vasodilate (bad for asthma and COPD), increased TG, LDL and glucose (like diuretics), dreams if fat soluble (ex: diuretic propranolol); use inotropic insulin or glucagon for overdose
Term
propranolol mode of action, solubility?, metabolism? ISA?
Definition
non-selective beta and Na channel blocker; fat soluble (dreams); Hepatatic 1A and 2D6; no ISA
Term
pindolol mode of action, solubility?, metabolism? ISA?
Definition
non-selective beta and (membrane stabilizing) Na channel blocker, 5HT1a agonist; water soluble; renal excretion; strong ISA
Term
metoprolol mode of action, solubility?, metabolism? ISA?
Definition
selective beta 1 blocker; fat soluble (dreams); hepatic 2D6; no ISA
Term
atenolol mode of action, solubility?, metabolism? ISA?
Definition
selective beta 1 blocker; water soluble; renal elimination; no ISA
Term
acebutolol mode of action, solubility?, metabolism? ISA?
Definition
selective beta 1 and membrane stabilizing Na channel blocker; fat soluble; renal elimination; ISA (also less effect on metabolic profile TG, LDL)
Term
nadolol mode of action, solubility?, metabolism? ISA?
Definition
non-selective beta blocker; water soluble; renal excretion; no ISA
Term
Water soluble beta blockers?
Definition
PANS: pindolol, atenolol, nadolol, satalol
Term
esmolol mode of action, delivery?, metabolism? half life?
Definition
beta blocker; IV, plasma esterases; ultra short acting
Term
beta blockers affect on cardio depolarization
Definition
Mainly flattens phase 4 (harder to depolarize)
Term
labetalol mode of action, effect,
Definition
mixed: non-cardio selective alpha/beta blocker and more; mainly reduces afterload and bronchoconstriction (alpha blocker)
Term
carvedilol mode of action, effect
Definition
mixed non-cardioselective alpha/beta blocker; stops vasculature from contracting (alpha blocker)
Term
Nebivolol mode of action, metabolism
Definition
beta blocker with NO (an EDRF) potentiating effect; metabolism by 2D6 to active moieties. NOTE EDRF = endothelium derived relaxing factor
Term
For beta blocker overdose?
Definition
Use inotrope insulin or glucagon (can't use beta agonist because receptor blocked)
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