丹曲林临床应用的研究进展

丹曲林是目前惟一被证实治疗恶性高热(malignant hyperthermia,MH)的特效药物.丹曲林药动学特性为二房室模型,血浆消除半衰期约为10 h,稳态分布容积为26.14L.最近的研究证实ryanodine受体(RYR)为丹曲林的结合部位,阻断该受体抑制Ca2+从肌浆网内释放,从而抑制肌肉收缩和其他的钙依赖胞质代谢过程是其分子作用基础.丹曲林除了用于治疗恶性高热外,临床上还可用于抗精神病药物恶性综合征(neuroleptic malignant syndrome,NMS)、痉挛状态和摇头丸(3,4-亚甲基二氧去氧麻黄碱,MDMA)中毒等的治疗.

Advance in clinical application of dantrolene

Dantolene is the only available drug which has been proven effective and specific for the treatment of malignant hyperthermia. The pharmacokinetics profile of dantrolene is adequately described by a two-compartment model. The plasma elimina-tion half-life time is about 10 h and distribution volume at steady-state is 26.14 L. Recent studies have identified that ryanodine re-ceptor is dantrolene-binding site. Inhibition of ryanodine receptor, blockade of calcium release from the sarcoplasmic reticulum and inhibition of muscle contraction and other calcium-dependent cytoplasmic metabolic processes is thought to be fundamental in the molecular action of dantrolene. Dantrolene has been used for the treatment of neuroleptic malignant syndrome, spasticity and Ecstasy intoxication besides malignant hyperthermia.