酒石酸布托啡诺的研究进展

Progress in Butorphanol Tartrate

酒石酸布托啡诺属于混合型阿片受体激动-拮抗药，主要激动κ和σ受体，拮抗μ受体。该药能有效地减轻中度及重度疼痛，镇痛效价约为吗啡的5-8倍，肌肉注射2mg可维持镇痛3-4小时。同时具有镇静作用，很少出现欣快及不愉快感觉。可静脉注射、肌肉注射和经鼻粘膜给药。血浆中药物峰值浓度在肌注和鼻粘膜给药后0.5-1小时出现，半衰期约3小时，血浆蛋白结合率约为80%。经鼻给药的常用剂量为1或2mg，给药方便，起效迅速。酒石酸布托啡诺主要用于急性偏头痛和严重头痛发作、手术后中度和重度疼痛，同时还作为要前或麻醉前用药。其副作用主要有嗜睡、头晕、恶心和/或呕吐。布托啡诺的成瘾性和滥用性较低。

Butorphanol tarate is a mixed opioid receptor agorast/antagonist, which agonist κ- receptor and σ-receptor, partly antagonist μ-recepor. It is an effective analgesic used for the relief of moderate to severe pain Its analgesic effect is as 5 to 8 times as morphine. Intramuscularly injection of 2 mg butorphanol tartrate may keep analgesia for about 3 to 4 hours. It has the sedation profiles with rare euphoda or discomfortable sense Butorphanol tartrate is usually given through the way of intravascutar injection or intranasal admission. Peak plasma concentrations occur 0.5 to 1 beur after intramuscular or nasal doses and 1 to 1.5 hours after oral doses Butarphanol has a plasma elimination half-life of about 3 hours. About 80% is bound to plasma proteins. Butorphanol tartrate is available as a nasal spray formulation, normally taken as a 1 or 2 mg dose, which provides ease for the patient and rapid relief of pain symptoms. Butorphanol tartrate has mainly been applied in migraine attacks or severe headaches or moderate to severe postoperative pain .It is also given for premedication before surgery or anesthesia The most common side effects are drowsiness, dizziness, nausea and/or vomiting. The dependence or abuse liability of butsrphanct is low.