| Term | Definition |
|---|
| Alpha-methyl-para-tyrosine (metyrosine) | Competitive inhibitor of tyrosine hydroxylaseUsed to treat pheochromocytoma before surgery (prevents chance of hypertensive crisis) |
| Reserpine | VMAT-2 blockerBlocks active transport of amines into vesiclesTransient massive efflux of catecholamines followed by depletion of NE, DA, serotoninUsed in hypertension treatment, but has severe side effects (suicidal depression, hypotension, movement disorders) |
| Phenoxybenzamine | alpha-1 > alpha-2 antagonistInitially a competitive blocker, followed by irreversible block (competitive non-equilibrium).Reflex tachycardia after sympathetic response exaggerated by alpha-2A blockUsed in pheochromocytoma management and to treat Reynaud's diseaseOther effects: hypotension, miosis, nasal congestion, inh of ejactulation |
| Phentolamine | alpha-1 and alpha-2 competitive antagonistshort term control of hypertensionpheochromocytoma management |
| Alpha-1 selective blockers | low cardiac stimulation- preserve alpha-2 negative feedbackUsed for: CHF, hypertension, BPH (alpha-1A antagonists)Increase HDL/LDL ratio |
| Prazosin | alpha-1 antagonist70% bioavailablityUsed: hypertension, CHF, peripheral vascular diseases, BPH |
| Terazosin | alpha 1 antagonist.Long-lasting, little first-pass metabolismUsed: hypertension, CHF, peripheral vascular diseases, BPH |
| Tamsulosin (FLOMAX) | Alpha-1A and 1D antagonistLower incidence of orthostatic hypotension than other alpha-1 antagonistsHighly specific for alpha-1 in urinary tractSide effect: asthenia |
| Afluzosin | Alpha-1 antagonist (urinary tract selective-means little hypotensive effects)Used for BPH, once per dayHighly metabolized |
| Yohimbine | alpha-2 blocker, homeopathicstimulates male sexual performancenausea |
| Beta blockers | Decrease cardiac outputInhibit renin releaseDecrease sympathetic outflowResetting of baroreceptor |
| Propanolol | Nonselective beta blockercrosses BBB, short half life, No ISAUses (besides cardiac): migraine prophylaxis |
| Timolol | nonselective beta blockerhigh CNS penetrationUses (besides cardiac): migraine prophylaxis, open angle glaucoma |
| Pindolol | nonselective beta blockerPartial agonist (ISA): means less change in cardiac output and heart rate (less loss of exercise tolerance)ISA- inhibits endogenous response in high levels of neurotransmitter, but creates a response in low levels of endogenous neurotransmitter |
| Acebutolol | Beta-1 selective blocker (little to no bronchoconstriction)Partial agonist (ISA)Less change in CO and HR than non-ISA beta-blockers |
| Metoprolol | Beta-1 blocker (loses selectivity at higher doses)Uses CYP2D6 |
| Atenolol | Beta-1 blockerlong half life, little CNS Used: systolic hypertension in elderly |
| Bisoprolol | Beta-1 blockerStandard with ACE inhibitor and diuretic to control hypertensionNo ISA means bradycardia is potential side affect |
| Labetalol | Nonselective beta blocker and alpha blockerISA(carvedilol similar antagonist actions)B1=B2>a1>a2Potent antihypertensive (cardiac and vasoconstrictive effects blocked) |
| Beta blocker side effects | Withdrawal syndrome- due to upregulated receptors (causes tachycardia, angina, MI)Cardiac depressionAirway toxicity- bronchoconstriction (do not give to asthmatics)Caution is vasospastic patientsAugments hypoglycemia (blocks normal sympathetic response to increase blood sugar) and masks tachycardia normally associated with hypoglycemiaElevates serum lipids (LDL, TG)Fatigue, CNS depressionDecreases exercise tolerance, except in some coronary artery disease patients where it may redistribute blood flow, thus enhancing exercise tolerance |
| Beta blocker uses | Blood pressure control (cardiac, kidney)Ventricular ArrythmiasAngina (not with partial agonists)anti-anxiolytic |
| Treating Glaucoma | Muscarinic Agonist (carbachol, pilocarpine)EPIBeta (2) blockersAlpha-2 agonists (brimonidine) |
Combine with other sets
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