Stevenson I H, Browning M, Crooks J, O'Malley K
Br Med J. 1972 Nov 11;4(5836):322-4. doi: 10.1136/bmj.4.5836.322.
The influence of the newer, non-barbiturate hypnotics Mandrax (diphenhydramine-methaqualone) and nitrazepam on drug-metabolizing capacity was assessed and compared with the effect of amylobarbitone, a known inducer of drug-metabolizing enzymes. Plasma antipyrine and phenylbutazone half-lives and urinary output of 6beta-hydroxycortisol were used as indices. Volunteer subjects were exposed to therapeutic amounts of these agents and, in the case of Mandrax and barbiturates, further studies were carried out in dependent patients.Mandrax but not nitrazepam increased the rate of drug metabolism, presumably by enzyme induction. The degree of induction was comparable with that produced by hypnotic doses of amylobarbitone. The Mandrax-dependent and barbiturate-dependent patients were the fastest metabolizers studied. It is concluded that drug interactions resulting from interference with drug metabolism are as likely to occur with Mandrax as with barbiturates. On the other hand, it is unlikely that such drug interactions would occur with nitrazepam.
评估了新型非巴比妥类催眠药眠尔通(苯海拉明-甲喹酮)和硝西泮对药物代谢能力的影响,并与已知的药物代谢酶诱导剂戊巴比妥的作用进行了比较。以血浆安替比林和保泰松半衰期以及6β-羟基皮质醇的尿排出量作为指标。让志愿者受试者接触这些药物的治疗剂量,对于眠尔通和巴比妥类药物,还对成瘾患者进行了进一步研究。眠尔通而非硝西泮增加了药物代谢速率,推测是通过酶诱导作用。诱导程度与催眠剂量的戊巴比妥所产生的程度相当。眠尔通成瘾者和巴比妥类药物成瘾者是所研究的代谢最快的人群。得出的结论是,与巴比妥类药物一样,眠尔通也很可能因干扰药物代谢而导致药物相互作用。另一方面,硝西泮不太可能发生此类药物相互作用。