Bieck P R
Humanpharmakologisches Institut CIBA-GEIGY GmbH, Tübingen.
Psychiatr Prax. 1989 Aug;16 Suppl 1:25-31.
Healthy ambulatory subjects took 6 different MAO inhibitors (MAOIs) orally for 2 to 4 weeks. The new reversible MAO-A inhibitors brofaromine and moclobemide were compared with the irreversible MAOIs clorgyline, selegiline, phenelzine and tranylcypromine. Pressor responsiveness to oral tyramine was assessed before, during and after treatment. In unmedicated subjects, doses of tyramine to raise systolic blood pressure by at least 30 mmHg (PD30) ranged between 200 and 800 mg. During treatment with MAOIs, the PD30 decreased. The ratio of median effective doses (ED50) of tyramine (pre- vs post-treatment) was: selegiline 5, moclobemide 7, brofaromine 10, clorgyline 10, phenelzine 13 and tranylcypromine 55. Pressor responsiveness normalized within 8 days after stopping the reversible MAOIs and 30 days after tranylcypromine. The increased sensitivity after phenelzine persisted for longer than 8 weeks and after clorgyline for longer than 15 weeks. The results suggest that the two reversible MAO-A inhibitors moclobemide and brofaromine carry a much reduced liability to tyramine-related hypertensive reactions.
健康的非卧床受试者口服6种不同的单胺氧化酶抑制剂(MAOIs),持续2至4周。将新型可逆性单胺氧化酶A抑制剂溴法罗明和吗氯贝胺与不可逆性MAOIs氯吉兰、司来吉兰、苯乙肼和反苯环丙胺进行比较。在治疗前、治疗期间和治疗后评估口服酪胺后的升压反应性。在未用药的受试者中,使收缩压升高至少30 mmHg的酪胺剂量(PD30)在200至800 mg之间。在用MAOIs治疗期间,PD30降低。酪胺的半数有效剂量(ED50)(治疗前与治疗后)之比为:司来吉兰5、吗氯贝胺7、溴法罗明10、氯吉兰10、苯乙肼13和反苯环丙胺55。停用可逆性MAOIs后8天内以及反苯环丙胺后30天内,升压反应性恢复正常。苯乙肼后敏感性增加持续超过8周,氯吉兰后敏感性增加持续超过15周。结果表明,两种可逆性单胺氧化酶A抑制剂吗氯贝胺和溴法罗明与酪胺相关的高血压反应的风险大大降低。