Class: Skeletal muscle relaxant, centrally acting
- Tablets 250 mg
- Tablets 350 mg
Produces skeletal muscle relaxation, probably as result of its sedative properties.
Mean T max is 1.5 to 2 h. C max following oral administration of 250 and 350 mg is 1.2 and 1.8 mcg/mL, respectively.
Metabolized in the liver, primarily by CYP2C19, to form meprobamate.
t ½ is approximately 2 h.
Eliminated by renal and nonrenal routes.
4 to 6 h.
Special PopulationsRenal Function Impairment
Pharmacokinetics have not been evaluated.Hepatic Function Impairment
Pharmacokinetics have not been evaluated.Gender
Carisoprodol exposure is 30% to 50% higher in women than men; however, meprobamate exposure is not affected by gender.Race
Individuals with reduced CYP2C19 activity have a 4-fold increase in carisoprodol exposure and a 50% reduced exposure to meprobamate compared with normal CYP2C19 metabolizers. Prevalence of poor metabolizers in white and black patients is approximately 3% to 5% and in Asian patients approximately 15% to 20%.
Indications and Usage
Relief of discomfort associated with acute, painful musculoskeletal conditions in adults.
Acute intermittent porphyria; hypersensitivity to related compounds, such as meprobamate.
Dosage and AdministrationAdults
PO 250 to 350 mg 3 times a day and at bedtime.
- Recommended maximum duration of administration is 2 to 3 wk.
Store at 59° to 86°F.
Drug InteractionsAlcohol and other CNS depressants
May cause additive CNS depression.CYP2C19 inducers (eg, rifampin, St. John's wort)
May decrease carisoprodol exposure and increase meprobamate, a metabolite of carisoprodol, exposure.CYP2C19 inhibitors (fluvoxamine, omeprazole)
May increase exposure to carisoprodol and decrease exposure to meprobamate.
Laboratory Test Interactions
None well documented.
Facial flushing, postural hypotension, syncope, tachycardia (postmarketing).
Drowsiness (17%); dizziness (8%); headache (5%); agitation, ataxia, depressive reactions, insomnia, irritability, seizures, tremor, vertigo (postmarketing).
Epigastric discomfort, nausea, vomiting (postmarketing).
Leukopenia, pancytopenia (postmarketing).
Monitor for the following signs of idiosyncratic response: agitation, ataxia, disorientation, dizziness, euphoria, extreme weakness, impaired verbal communication, transient quadriplegia, vision disturbances. These reactions may appear within minutes or hours of first dose. Symptoms usually subside over several hours. If such reactions occur, withhold drug.
Category C .
Excreted in breast milk.
Safety and efficacy not established in children younger than 16 yr of age.
Safety and efficacy not established in patients older than 65 yr of age.
Use with caution.
Use with caution.
Administer with caution to patients with history of drug abuse.
Use with caution in addiction-prone patients.
Drug may impair mental and physical abilities required for performance of potentially hazardous tasks such as driving a motor vehicle or operating machinery.
Withdrawal symptoms have been reported.
Blurred vision, CNS depression, coma, death, delirium, dystonic reactions, euphoria, hallucinations, headache, hypotension, muscular incoordination, mydriasis, nystagmus, respiratory depression, rigidity, seizures.
- Instruct patient to take last daily dose at bedtime.
- Tell patient to take medication with meals if GI upset occurs.
- Instruct patient to report these symptoms to health care provider: ataxia, hiccough, palpitations, tremors.
- Advise patient to avoid intake of alcoholic beverages or other CNS depressants.
- Caution patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.
Copyright © 2009 Wolters Kluwer Health.
More about carisoprodol
- Other brands: Soma