Norman T R, Burrows G D
Department of Psychiatry, University of Melbourne, Austin Hospital, Heidelberg, Victoria, Australia.
Drug Saf. 1995 Jan;12(1):46-54. doi: 10.2165/00002018-199512010-00004.
Moclobemide, a novel benzamide, is a reversible inhibitor of monoamine oxidase-A (RIMA). It has been extensively evaluated in the treatment of a wide spectrum of depressive disorders. Comparative studies have shown that the drug is more effective than placebo and as effective as other antidepressants. In terms of efficacy, moclobemide offers no more benefits than do existing agents. On the other hand, moclobemide is better tolerated than tricyclic antidepressants and, unlike irreversible monoamine oxidase inhibitors, has a much lower propensity to cause a 'cheese reaction' (a potentially fatal syndrome caused by an interaction with tyramine-rich foods). These are significant clinical benefits, particularly in elderly patients. Furthermore, moclobemide lacks significant effects on psychomotor performance and cognitive function, has few clinically important drug interactions and is safe on overdose. The drug has a relatively short plasma elimination half-life, a property that allows a change to an alternative agent within 24 hours in cases of nonresponse. Since it is well tolerated, therapeutic dosages can often be achieved from the onset of treatment. These benefits need to be considered against the potential risks of moclobemide therapy. To date, the most significant hazards of therapy appear to arise from drug interactions with clomipramine or selective serotonin (5-hydroxytryptamine; 5-HT) reuptake inhibitors, where the occurrence of the serotonin syndrome is potentially fatal. Similarly, in preclinical tests moclobemide has been shown to potentiate the effects of pethidine (meperidine) and dextropropoxyphene, so that combined use of moclobemide is a useful addition to the therapeutic agents used for depressive disorders.(ABSTRACT TRUNCATED AT 250 WORDS)
吗氯贝胺是一种新型苯甲酰胺,是单胺氧化酶-A(RIMA)的可逆抑制剂。它已被广泛评估用于治疗多种抑郁症。比较研究表明,该药物比安慰剂更有效,且与其他抗抑郁药效果相当。在疗效方面,吗氯贝胺并不比现有药物更具优势。另一方面,吗氯贝胺的耐受性优于三环类抗抑郁药,并且与不可逆单胺氧化酶抑制剂不同,它引起“奶酪反应”(一种因与富含酪胺的食物相互作用导致的潜在致命综合征)的倾向要低得多。这些都是显著的临床优势,尤其是在老年患者中。此外,吗氯贝胺对精神运动表现和认知功能影响不大,几乎没有重要的临床药物相互作用,过量服用也安全。该药物的血浆消除半衰期相对较短,这一特性使得在无反应的情况下可在24小时内更换为其他药物。由于耐受性良好,通常从治疗开始就能达到治疗剂量。这些益处需要与吗氯贝胺治疗的潜在风险相权衡。迄今为止,治疗中最显著的风险似乎源于与氯米帕明或选择性5-羟色胺再摄取抑制剂的药物相互作用,其中5-羟色胺综合征的发生可能是致命的。同样,在临床前试验中,吗氯贝胺已被证明可增强哌替啶(度冷丁)和右丙氧芬的作用,因此吗氯贝胺联合使用是用于治疗抑郁症的治疗药物中的有益补充。(摘要截选至250字)