[Dantrolene. Pharmacological and therapeutic aspects].

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Gerbershagen MU, Fiege M, Krause T, Agarwal K, Wappler F

[Dantrolene. Pharmacological and therapeutic aspects].

Anaesthesist. 2003 Mar;52(3):238-45.

PubMed ID

12666006 [ View in PubMed

]

Abstract

Malignant hyperthermia (MH) is a genetic, potentially life-threatening disorder of the skeletal muscle presenting during or following general anaesthesia. Trigger agents are volatile anaesthetics and depolarising muscle relaxants. Dantrolene is the only available drug for effective and specific MH therapy, which reduces significantly the mortality rate. Dantrolene is a skeletal muscle relaxant that depresses the excitation-contraction coupling,however, the specificity of action remains unknown. Recent studies identified the ryanodine receptor, the calcium release channel of the sarcoplasmic reticulum, as the direct molecular target of dantrolene. In addition to its use for MH, dantrolene is used in other disorders such as neuroleptic malignant syndrome and spasticity. Since dantrolene is weakly water soluble, the clinical preparation is time and manpower consuming. New agents have been synthesized, but because of economic considerations no registration for clinical usage has been realised.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Dantrolene	Ryanodine receptor 1	Protein	Humans	Yes	Antagonist	Details