Nadzhimutdinov K N, Khakimov Z Z, Kabulov Sh M
Eksp Klin Farmakol. 1992 Jan-Feb;55(1):68-71.
It is stated that phenobarbital used as the most potent inductor of the monoxygenase enzymic system of the liver in different pathologies has substantial side effects. In this connection the search of active inductive agents devoid of phenobarbital deficiencies is an important issue. Zixorene, a Hungarian drug developed to solve the problem, is weak as an inductor and has deficiencies of its own. A fitting substitute for phenobarbital is benzonal which is not inferior to phenobarbital in inductive activity but lacks its drawbacks. It is used both as a hypobilirubinemic agent and a drug restoring a disordered monohygenase system of the liver in different pathologies. Benhonal is metabolized in the gastrointestinal tract and the liver generating an active metabolite of phenobarbital. It is suggested that slow formation of phenobarbital in small quantities determines its more optimal interaction with the corresponding hepatic receptors resulting in the appearance of a marked inductive action while side effects are significantly decreased.
据说，苯巴比妥在不同病理状态下作为肝脏单加氧酶系统最有效的诱导剂，有大量副作用。因此，寻找没有苯巴比妥缺陷的活性诱导剂是一个重要问题。为解决该问题研发的匈牙利药物齐索雷纳，作为诱导剂作用较弱且自身存在缺陷。苯唑那是苯巴比妥的合适替代品，其诱导活性不低于苯巴比妥，但没有其缺点。它既用作降胆红素剂，也用作恢复不同病理状态下肝脏紊乱的单加氧酶系统的药物。苯唑那在胃肠道和肝脏中代谢，生成苯巴比妥的活性代谢物。有人认为，少量苯巴比妥的缓慢形成决定了它与相应肝受体更优化的相互作用，从而产生显著的诱导作用，同时副作用明显减少。
