2010肾上腺素能药物与局麻药.ppt

Adrenoceptor agonists and antagonists and local anesthetics Adrenoceptor agonists Basic actions: Excitation of smooth muscles (skin vessel and mucosal vessel) Inhibition of smooth muscles (intestine, bronchia and skeletal muscle vessel) Excitation of heart Metabolism (glycogenolysis and lipolysis) Endocrine effects (insulin↓, renin↑, etc.) CNS excitatory effects epinephrine 1, cardiovascular system Heart（β1）: HR↑, contraction↑, conductance↑, cardiac output↑, oxygen consumption↑ arrhythmia (large dose) Blood vessel（? receptors）: contraction in skin, mucus, abdominal viscera dilation in coronary and skeletal muscle vessels BP: systolic↑，diastolic, － or ↓ epinephrine Clinical uses: cardiac arrest caused by anesthesia operation drowning drug intoxication electric attack atrio-ventricular block allergic shock ephedrine adrenaline like-action facilitation of norepinephrine release （CNS PNS） central excitation weak action and long lasting Clinical uses: hypotension by anesthesia, … nasal congestion (replaced by oxymetazoline，羟甲唑啉) asthma (replaced by salbutamol, etc.) urticaria [‘??ti‘k??ri?] (荨麻疹） βadrenoceptor antagonists 1948, Ahlquist, adrenoceptor subtypes 1958, βblocker dichlorisoprenaline, potent intrinsic sympathomimetic activity 1962, James Black, pronethalol（丙萘洛尔），pure βblocker, but carcinogenic 1964, propranolol 1988, Nobel Prize for J. Black, et al. 2, intrinsic sympathomimetic activity 内在拟交感活性 of significance in reducing side effects of bronchia and heart. 3, membrane-stabilizing effects, not related to βadrenoceptor blockade, but to anesthetic action induced by sodium channel blockade; not significant clinically Pharmacokinetic property：first-pass effect；variation in blood concentration: 20 folds Clinical uses：angina pectoris, tachycardic arrhythmia, hypertension, and hyperthyroidism contraindications: asthma, A-V block clinical uses： asthma