Carisoprodol

Indications

Carisoprodol is indicated for-
  • The relief of discomfort associated with acute, painful musculoskeletal conditions in adults.
  • Sedation and decrease anxiety in patients with severe pain.
  • Used as an adjunct in physical therapy in injuries.

Pharmacology

Carisoprodol is a GABA-A receptor indirect agonist with CNS chloride channel conductance effect. GABA receptor agonists typically produce sedative effect and may also cause other effects such as anxiolytic, anticonvulsant and muscle relaxant. Metabolite of Carisoprodol, Meprobamate, has anxiolytic and sedative properties. Carisoprodol decreases the impulses from brain and spinal cord to the muscle. This causes the muscle to relax and hence decrease the spasm. It has no direct action on muscle itself.

Dosage & Administration

Adults (18 years and older): The recommended dose of Carisoprodol is 250 mg to 350 mg three times a day and at bedtime. The recommended maximum duration of Carisoprodol use is up to two or three weeks. Caution should be taken in patients with renal and hepatic impairment and also with reduced CYP2C19 activity.

Interaction

  • Caution should be exercised with patients who take other CNS depressants (eg. alcohol, benzodiazepines, opioids, tricyclic antidepressants) with Carisoprodol.
  • Co-administration of CYP2C19 inhibitors (Omeprazole, Fluvoxamine) with Carisoprodol could result in increased exposure of Carisoprodol. Co-administration of CYP2C19 inducers (Rifampin) with Carisoprodol could result in decreased exposure of arisoprodol.

Contraindications

Carisoprodol is contraindicated in patients with a history of acute intermittent porphyria or a hypersensitivity reaction to a carbamate such as meprobamate.

Side Effects

Common side effects are drowsiness, dizziness and headache.

Pregnancy & Lactation

Pregnancy category C. Maternal use of Carisoprodol may lead to reduced or less effective infant feeding (due to sedation) and/or decresed milk production. Caution should be exercised when Carisoprodol is administered to a nursing woman.

Precautions & Warnings

Due to sedative properties, may impair ability to perform hazardous tasks such as driving or operating machinery. Additive sedative effects when used with other CNS depressants including alcohol. Cases of Drug Dependence, Withdrawal, and Abuse. Seizures

Overdose Effects

Overdosage of Carisoprodol commonly produces CNS depression. Death, coma, respiratory depression, hypotension, seizures have been reported with Carisoprodol overdosage. Basic life support measures should be instituted in Carisoprodol overdose. Induced emesis is not recommended due to the risk of CNS and respiratory depression. Gastric lavage should be considered soon after ingestion (within one hour). Circulatory support should be administered with volume infusion and vasopressor agents if needed. Seizures should be treated with intravenous benzodiazepines and the reoccurrence of seizures may be treated with phenobarbital. In cases of severe CNS depression, airway protective reflexes may be compromised and tracheal intubation should be considered for airway protection and respiratory support.

Therapeutic Class

Locally acting Skeletal Muscle Relaxants

Storage Conditions

Store in cool and dry place at room temperature 20°-25°C, away from direct light. Keep out reach of children.