Products
Dantrolene is commercially available in capsule form and as a solution for injection (dantamacrine, dantrolene). It has been approved in many countries since 1983. It was developed in the 1960s and 70s. This article refers primarily to peroral therapy.
Structure and properties
Dantrolene (C14H10N4O5, Mr = 314.3 g/mol) is present in the drug as dantrolene sodium (- 3.5 H2O), an orange powder that is sparingly soluble in water. It is a hydantoin and furan derivative.
Effects
Dantrolene (ATC M03CA01) has muscle relaxant effects on striated muscle. It inhibits calcium release from the sarcoplasmic reticulum. The effects are due to antagonism at the ryanodine receptor, being a calcium channel on the SR. The half-life is 8.7 hours.
Indications
- Severe or refractory muscle spasm after spinal cord or brain injury.
- Micturition dysfunction due to spasticity of the bladder sphincter and perineum.
- Malignant hyperthermia (parenteral).
Dosage
According to the professional information. Treatment is started gradually and the dose is adjusted individually.
Contraindications
- Hypersensitivity
- Liver disease
- Impaired lung function
- Severe myocardial damage
- Children under 5 years
- In cases where abnormal tone elevation is required to allow better motor function, upright posture or balance of movement.
- Pregnancy, lactation
Full precautions can be found in the drug label.
Interactions
Drug-drug interactions have been described with benzodiazepines, sedatives, alcohol, metoclopramide, estrogens, calcium channel blockers, and muscle relaxants, among others.
Adverse effects
The most common possible adverse effects include dizziness, lightheadedness, diarrhea, fatigue, feeling weak, and general malaise. Dantrolene has liver-toxic properties and may cause liver damage.