| Term | Definition |
|---|
| 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 |
Combine with other sets
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