Mallinger A G, Edwards D J, Himmelhoch J M, Knopf S, Ehler J
Clin Pharmacol Ther. 1986 Oct;40(4):444-50. doi: 10.1038/clpt.1986.205.
We investigated the pharmacokinetics of tranylcypromine, as well as the relationship between plasma levels of this agent and its effects on blood pressure and pulse rate. Tranylcypromine was absorbed rapidly after oral dosing, with the peak level being attained within 0.67 to 3.50 hours. Absorption was biphasic in seven of nine subjects. Elimination of tranylcypromine also was rapid, with a t 1/2 between 1.54 and 3.15 hours. From 2 to 7 hours after dosing, standing systolic and diastolic blood pressures were lowered and standing pulse was raised, compared with baseline. Onset of the effect on standing systolic blood pressure was correlated with the time of peak plasma tranylcypromine concentration. Maximum orthostatic drop of blood pressure and rise of pulse rate occurred 2 hours after dosing. Mean plasma tranylcypromine concentrations were correlated with mean orthostatic drop of systolic blood pressure and rise of pulse rate. Patients who have clinically significant hypotensive reactions to this agent may benefit from changes in their dose regimen aimed at minimizing peak tranylcypromine levels.
我们研究了反苯环丙胺的药代动力学，以及该药物的血浆水平与其对血压和脉搏率影响之间的关系。口服给药后，反苯环丙胺吸收迅速，在0.67至3.50小时内达到峰值水平。9名受试者中有7名的吸收呈双相性。反苯环丙胺的消除也很快，半衰期在1.54至3.15小时之间。给药后2至7小时，与基线相比，站立时收缩压和舒张压降低，站立时脉搏加快。对站立收缩压的影响开始时间与血浆反苯环丙胺浓度峰值时间相关。给药后2小时出现最大直立性血压下降和脉搏率升高。平均血浆反苯环丙胺浓度与平均直立性收缩压下降和脉搏率升高相关。对该药物有临床上显著低血压反应的患者，可能会从旨在尽量降低反苯环丙胺峰值水平的剂量方案改变中获益。
