Cyclobenzaprine

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.