- Molecular NameDantrolene
- SynonymDantrolene Sodium; Dantroleno [INN-Spanish]; Dantrolenum [INN-Latin]
- Weight314.257
- Drugbank_IDDB01219
- ACS_NO7261-97-4
- Show 2D model
- LogP (experiment)1.4
- LogP (predicted, AB/LogP v2.0)2.31
- pka7.5
- LogD (pH=7, predicted)2.16
- Solubility (experiment)0.146 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-5.36
- LogSw (predicted, AB/LogsW2.0)0.02
- Sw (mg/ml) (predicted, ACD/Labs)0.0
- No.of HBond Donors1
- No.of HBond Acceptors9
- No.of Rotatable Bonds4
- TPSA123.74
- StatusFDA approved
- AdministrationN/A
- PharmacologyA muscle relaxant that acts by abolishing excitation-contraction coupling in muscle cells, probably by action on the ryanodine receptor. It is the only specific and effective treatment for malignant hyperthermia, a rare, life-threatening disorder triggered by general anesthesia. It is also used in the management of neuroleptic malignant syndrome, muscle spasticity (e.g. after strokes, in paraplegia, cerebral palsy, or patients with multiple sclerosis), ecstasy intoxication, serotonin syndrome, and 2,4-dinitrophenol poisoning.
- Absorption_value80.0
- Absorption (description)Slowly and incompletely absorbed after oral administration.
- Caco_2N/A
- Bioavailability70.0
- Protein bindingN/A
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmMetabolised by oxidation to 5-hydroxydantrolene, which is active, and by reduction followed by acetylation to form the p-acetamido derivative.
- Half lifedantrolene 4~22 h (mean 9), 5-hydroxydantrolene 8~29 h (mean 16).
- ExcretionAbout 20% of an oral dose is excreted in the urine as metabolites, mainly the 5-hydroxy derivative; less than 5% of a dose is excreted in the urine as unchanged drug; up to about 50% of a dose may be excreted in the bile.
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityFatalities due to liver damage have been reported.
- LD50 (rat)7400 mg/kg
- LD50 (mouse)N/A