化合物信息

Drug Groups

approved

Description

A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202)

Indication

For the relief of discomfort associated with acute, painful, musculoskeletal conditions.

Pharmacology

Carisoprodol is used as a skeletal muscle relaxant. One of its metabolites, meprobamate, is available as an anxiolytic agent.

Toxicity

Symptoms of overdose include drowsiness, giddiness, nausea, indigestion, or rash. Other adverse effects attributed to therapeutic use of carisoprodol include dizziness, irritability, insomnia, diplopia, temporary loss of vision, ataxia, weakness, headache, and dysarthria. Non-CNS adverse effects include gastrointestinal complaints, tachycardia, and postural hypotension. Patients sensitive to sulfites or tartrazine may experience wheezing, allergic rashes including erythema multiforme, or anaphylaxis after using some preparations of carisoprodol which contain such additives

Affected Organisms

Biotransformation

Hepatic. Metabolized in the liver via the cytochrome P450 oxidase isozyme CYP2C19.

Half Life

8 hours

Protein Binding

60%

Elimination

Carisoprodol is eliminated by both renal and non-renal routes.

Clearance

* oral cl=0.772 L/hour/kg [Women]
* oral cl=0.38 L/hour/kg [Men]

References

External Links