Parker R B, McCollam P L
University of Georgia College of Pharmacy, Athens.
Clin Pharm. 1990 Apr;9(4):261-71.
The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of adenosine in the treatment of episodes of paroxysmal supraventricular trachycardia (PSVT) are reviewed. Adenosine is an endogenous adenine nucleoside that markedly decreases heart rate and prolongs atrioventricular (AV)-nodal conduction. Adenosine is rapidly cleared from plasma by the cellular elements of the blood and by vascular endothelial cells and subjected to enzymatic metabolism. The drug has a half-life of 0.6 to 10 seconds. In noncomparative clinical trials, adenosine terminated 85% to 100% of induced or spontaneous episodes of PSVT involving the AV node in the reentrant circuit. In patients with arrhythmias that do not involve the AV node in the reentrant circuit, adenosine produces AV block and does not restore sinus rhythm. Prospective, randomized trials comparing adenosine with verapamil in adults have not yet been performed. The adverse effects of adenosine include flushing, dyspnea, headache, cough, chest pain, sinus bradycardia, atrial fibrillation, ventricular arrhythmias, and various degrees of AV block. Because of the short half-life of adenosine, these effects are transient and well tolerated. The initial dose of adenosine in treating acute PSVT is 6 mg given by rapid i.v. bolus injection, followed in one to two minutes by up to two additional 12-mg boluses if necessary. Adenosine has been found to be effective in terminating PSVT and thus offers an alternative to verapamil. Prospective, randomized trials comparing adenosine with verapamil are needed to definitively establish adenosine's role in the therapy of PSVT.
本文综述了腺苷治疗阵发性室上性心动过速(PSVT)发作时的药理学、药代动力学、临床疗效、不良反应以及剂量和用法。腺苷是一种内源性腺嘌呤核苷,可显著降低心率并延长房室(AV)结传导时间。腺苷可被血液中的细胞成分和血管内皮细胞迅速从血浆中清除,并进行酶代谢。该药物的半衰期为0.6至10秒。在非对照临床试验中,腺苷可终止85%至100%的由折返环路中AV结参与的诱发性或自发性PSVT发作。对于折返环路中不涉及AV结的心律失常患者,腺苷会导致AV阻滞,且不能恢复窦性心律。尚未进行比较腺苷与维拉帕米在成人中的前瞻性、随机试验。腺苷的不良反应包括潮红、呼吸困难、头痛、咳嗽、胸痛、窦性心动过缓、心房颤动、室性心律失常以及不同程度的AV阻滞。由于腺苷半衰期短,这些效应是短暂的且耐受性良好。治疗急性PSVT时,腺苷的初始剂量为6mg,通过快速静脉推注给药,如有必要,在1至2分钟后可追加最多两次12mg的推注。已发现腺苷在终止PSVT方面有效,因此可作为维拉帕米的替代药物。需要进行比较腺苷与维拉帕米的前瞻性、随机试验,以明确腺苷在PSVT治疗中的作用。