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Direct acting agonist of a1; leads to nasal vein constriction to reduce nasal congestion; also used in hypotensive emergency
Direct acting agonist on a1 and b1 has selectivity towards B1; net effect is positive inotropy; Useful in treating CHF
direct agonist of a2, long acting and is used for nasal congestion (via nasal arterioles
similar to albuterol in that it is a B2 direct acting agonist, it has a rapid onset of action
Indirect acting agonists
class of alpha beta agonists that act by increasing release of NE resulting in increased BP adn HR, sever responses, tachyphylaxis is possible;
Indirect acting agonists indications
alerting/sleep deferring, narcolepsy, appetite suppression, adhd
Indirect acting agonist of a,b; it is long acting; used to treat postural hypertension; has direct effects as well; severe toxicities including stroke, MI and death
Indirect acting agonists that has more effects on alpha rather than B than ephedrine; Tx: nasal congestion; it is a schedule II drug that can be used to make meth
reverses NE and DA reuptake; blocks NE and DE reuptake and MAO, readily enters the CNS, has a high abuse potential and is used to treat ADHD
Off market indirect acting agonist of alpha or B, it was taken off market because of hemorrhagic strokes
Phentolamine adverse effects
orthostatic hypertension, tachycardia, miosis, nasal stuffiness, inhibited ejaculation, GI disturbances - resulting from histamine release
a1>a2; nonequilibrium competitive antagonism; Inhibits ACH, 5HT, Histamine receptors, blocks NET and extraneuronal uptake; SE include Otrthostatic hypotension, tachycardia, Miosis, Nasal stuffiness. Inhibits ejaculation
Prazosin, terazosin, doxazosin, alfuzosin
a1 adrenoreceptor antagonists that are equilibrium competitive antagonists of moderate duration; Tx mild-moderate hypertension and BPH; **1st dose syncope, fewer reflex cardiac stimulation b/c it doesn't block presynaptic alpha receptors - at high doeses these are direct vasodilators; SE of residula orthostatic hypotension
Drug used for erectile dysfunction; not very affective because it mainly acts on the CNS via a2 (essentially has the opposite effects as clonodine; will increase BP and heart rate
Antagonist of a1a; Tissue specific and used to treat BPH; decrease contraction of urinary bladder, less contraction of prostate smooth muscle
B1, B2 receptor antagonist; acts by stabilizing the membrane (it is an anti-arrythmatic drug)
B1 B2 antagonist with partial agonist activity and slight membrane stabilizaiton: less decrease in BP/HR than full antagonist
nonselective antagonist of B receptors; it is a slight B2 agonist, has slight membrane stabilization; Tx: hypertension; decrease BP and inhibits the baroreceptor reflex
Useful in early CHF, a very powerful antioxidant; eases the work that the heart must perform
B1 inverse agonist, has slight membranes stabilization (antiarrythmatic) useful in HT and MI
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