Dantrolene – A review of its pharmacology, therapeutic use and new developments

摘要: Human malignant hyperthermia is a life-threatening genetic sensitivity of skeletal muscles to volatile anaesthetics and depolarizing neuromuscular blocking drugs occurring during or after anaesthesia. The muscle relaxant dantrolene the only currently available drug for specific effective therapy this syndrome in man. After its introduction, mortality decreased from 80% 1960s < 10% today. It was soon discovered that depresses intrinsic mechanisms excitation-contraction coupling muscle. However, precise mechanism action molecular targets are still incompletely known. Recent studies have identified ryanodine receptor as dantrolene-binding site. A direct indirect inhibition receptor, major calcium release channel sarcoplasmic reticulum, thought be fundamental decreasing intracellular concentration. Dantrolene not used treatment hyperthermia, but also management neuroleptic syndrome, spasticity Ecstasy intoxication. main disadvantage poor water solubility, hence difficulties experienced rapidly preparing intravenous solutions emergency situations. Due economic considerations, no other similar been introduced into routine clinical practice.