Chpt 11 Adrenoceptor blocking drugs肾上腺素受体阻断药.pptVIP

Metoprolol 美托洛尔, Atenolol 阿替洛尔 --Selective for β1 receptor. --may be safer in patients who experience bronchoconstriction in response to propranolol. --may be preferable in patients with diabetes or peripheral vascular disease since β2 receptors are probably important in liver (recovery from hypoglycemia) and blood vessels (vasodilation). Specific Agents Esmolol 艾司洛尔 --is an ultra-short–acting β1-selective adrenoceptor antagonist. --has a short half-life (about 10 minutes). steady state concentrations are achieved quickly, and the therapeutic actions of the drug are terminated rapidly. Specific Agents --is potentially safer to use than longer-acting antagonists in critically ill patients. --is useful in controlling supraventricular arrhythmias, arrhythmias associated with thyrotoxicosis, perioperative hypertension, and myocardial ischemia in acutely ill patients. Specific Agents Esmolol Pindolol 吲哚洛尔, Acebutolol 醋丁洛尔 --have partial-agonist activity. --are effective in the major cardiovascular applications (hypertension and angina). --Although these partial agonists may be less likely to cause bradycardia and abnormalities in plasma lipids, the overall clinical significance of intrinsic sympathomimetic activity remains uncertain. α, β Blocker Labetalol 拉贝洛尔 block α1, β1, β2 receptors beta: alpha= 3:1 blood pressure lowered–α and β1 blocked heart rate , cardiac output no change Uses: different types of hypertension, ventricular arrhythmias, angina Side effects: dizziness, general malaise全身倦怠, nausea Contraindications -- asthma -- congestive heart failure Drug list Prototypes: ? phenoxybenzamine ?propranolol Major variants: ? phentolamine ? prazosin ?terazosin ? metoprolol ?timolol ?pindolol ?esmolol Other significant agents: ?labetalol 思考题 1.试比较酚苄明和酚妥拉明的药理学特点及临床应用。 2.与普萘洛尔相比, 噻吗洛尔、艾司洛尔、 吲哚洛尔、拉贝洛尔有哪些药理学及临床应用特点。 Scottish scientist James W. Bla