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39 terms

Pharm 4 Fedan alpha/beta agonists/antagonists

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Norepinepinephrine
direct acting agonist of a1,a2, b1; degraded by MAO and COMT
Epinephrine
direct acting agonist of a1,a2,b1,b2; degraded by MAO and COMT
Isoproteronol
Direct acting agonsit of B1 and B2
Dopamine
Direct acting agonist of B1 receptor; degraded by MAO and COMT
Phenylephrine
Direct acting agonist of a1; leads to nasal vein constriction to reduce nasal congestion; also used in hypotensive emergency
Methoxamine
direct acting agonist of a1; used in hypotensive emergency
Dobutamine
Direct acting agonist on a1 and b1 has selectivity towards B1; net effect is positive inotropy; Useful in treating CHF
Clonidine
direct acting agonist of a2, has CNS effects many side effects; used to treat HT
Oxymetazoline
direct agonist of a2, long acting and is used for nasal congestion (via nasal arterioles
Albuterol
B2 direct acting agonist, inhaled, used for broncospasm in asthma
Terbutamine
similar to albuterol in that it is a B2 direct acting agonist, it has a rapid onset of action
Ritodrine
B2 direct acting agonist administered IV, used for uterine relaxation in premature labor
Tyramine
Indirect acting agonist that increases the release of NE
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
Ephedrine
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
Pseudoephedrine
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
Amphetamine
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
Phenylpropanolamine
Off market indirect acting agonist of alpha or B, it was taken off market because of hemorrhagic strokes
Phentolamine
alpha antagonist with a1=a2
Phentolamine or phenoxybenzamine
Tx pheochromocytoma and Raynauds
Phentolamine MOA
Equilibrium competitive antagonist of a1=a2, moderate duratio
Phentolamine adverse effects
orthostatic hypertension, tachycardia, miosis, nasal stuffiness, inhibited ejaculation, GI disturbances - resulting from histamine release
Phenoxybenzamine
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
Yohimbine
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
Ergotamine
alpha antagonist Interacts with 5HT and DA receptors; used to treat MIgraines
Ergonovine
alpha antagonist; Vascoconstriction adn oxytocic; used to treat post-partum hemmorrhage
Tamsulosin
Antagonist of a1a; Tissue specific and used to treat BPH; decrease contraction of urinary bladder, less contraction of prostate smooth muscle
Propanolol
B1, B2 receptor antagonist; acts by stabilizing the membrane (it is an anti-arrythmatic drug)
Nadalol
B1 B2 antagonist
Pindolol
B1 B2 antagonist with partial agonist activity and slight membrane stabilizaiton: less decrease in BP/HR than full antagonist
TImolol
nonselective b antagonist used in treatment of open angle glaucoma
Labelatol
nonselective antagonist of B receptors; it is a slight B2 agonist, has slight membrane stabilization; Tx: hypertension; decrease BP and inhibits the baroreceptor reflex
Carvedilol
Useful in early CHF, a very powerful antioxidant; eases the work that the heart must perform
Metoprolol
B1 inverse agonist, has slight membranes stabilization (antiarrythmatic) useful in HT and MI
Acetobutolol
B1 antagonist
Esmolol
B1 antagonist that has a fast acting, short duration; this is the "tunable" B antagonist
Butoxamine
B2 antagonist that is not really used since it leads to bronchoconstriction