Products
Cyclobenzaprine is commercially available in the United States and elsewhere in the form of film-coated tablets. No finished drug products containing cyclobenzaprine are currently registered in many countries.
Structure and properties
Cyclobenzaprine (C20H21N, Mr = 275.4 g/mol) is present in drugs as cyclobenzaprine hydrochloride, a white crystalline powder that is soluble in water. It is structurally closely related to the tricyclic antidepressants.
Effects
Cyclobenzaprine (ATC M03BX08) has muscle relaxant, anticholinergic, and sedative properties. It is not peripherally active but is active in the central nervous system in the brainstem. The half-life is approximately 18 hours.
Indications
For short-term treatment of muscle spasms.
Dosage
According to the professional information. The tablets are usually taken three times daily.
Abuse
Cyclobenzaprine can be abused as a depressant and relaxant intoxicant. The cocktail of medications and drugs that killed Whitney Houston contained cyclobenzaprine in addition to cocaine and central depressant medications.
Contraindications
- Hypersensitivity
- Treatment with MAO inhibitors (life-threatening).
- Recovery period after myocardial infarction.
- Cardiac arrhythmias, conduction disorders, heart failure.
- Hyperthyroidism
Full precautions can be found in the drug label.
Interactions
Drug-drug interactions have been described with MAO inhibitors, central depressant drugs, alcohol, antihypertensives, antidepressants, and tramadol.
Adverse effects
The most common possible adverse effects include drowsiness, somnolence, dry mouth, fatigue, and headache.