Generic
Carisoprodol
5 brands available in the market
At a glance
Carisoprodol is a muscle relaxant used to relieve discomfort associated with acute, painful musculoskeletal conditions such as muscle rigidity, tension, stiffness, and spasms. It works by reducing impulses from the brain and spinal cord to the muscle, causing muscle relaxation.
Description
Carisoprodol is a muscle relaxant used to relieve discomfort associated with acute, painful musculoskeletal conditions. It acts as an indirect GABA-A receptor agonist with CNS chloride channel conductance effects. GABA receptor agonists typically produce sedative effects and may also cause anxiolytic, anticonvulsant, and muscle relaxant effects.
The metabolite of Carisoprodol, Meprobamate, has anxiolytic and sedative properties. It decreases impulses from the brain and spinal cord to the muscle, causing muscle relaxation and reducing spasms. It has no direct action on the muscle itself.
Carisoprodol is indicated for the relief of discomfort associated with acute, painful musculoskeletal conditions in adults, sedation and decrease of anxiety in patients with severe pain, and as an adjunct in physical therapy in injuries.
Indications
- Relief of discomfort associated with acute, painful musculoskeletal conditions
- Sedation and decrease of anxiety in patients with severe pain
- Adjunct in physical therapy in injuries
Therapeutic class
Locally acting Skeletal Muscle Relaxants
Pharmacological class
Skeletal Muscle Relaxant / Carbamate
Pharmacology
Carisoprodol is an indirect GABA-A receptor agonist with CNS chloride channel conductance effects. GABA receptor agonists typically produce sedative effects and may also cause anxiolytic, anticonvulsant, and muscle relaxant effects. The metabolite of Carisoprodol, Meprobamate, has anxiolytic and sedative properties. It decreases impulses from the brain and spinal cord to the muscle, causing muscle relaxation and reducing spasms. It has no direct action on the muscle itself.
Mechanism of action
Carisoprodol blocks interneuronal synaptic activity in the descending reticular formation and spinal cord, resulting in skeletal muscle relaxation. It activates GABA-A receptors, increasing inhibitory effects in the CNS, which reduces muscle tension and spasms.
Dosage
Adults (18 years and older): 250-350 mg three times daily and at bedtime, for up to 2-3 weeks.
Elderly: Half of the usual dose.
Children (16 years): 250-350 mg every 8 hours and at bedtime.
Renal and hepatic impairment: Caution required; caution also in patients with reduced CYP2C19 activity.
Note: Use the lowest effective dose; do not exceed 2-3 weeks of use.
Administration
Take with or without food, preferably at a fixed time each day. Swallow tablets whole; do not chew, crush, or break. Follow the dose and duration as advised by your physician.
Missed dose
If you miss a dose, take it as soon as you remember. Skip the missed dose if it is almost time for your next dose. Do not double the dose.
Side effects
Common side effects: Sleepiness, drowsiness, dizziness, headache.
Serious (rare): Drug dependence, withdrawal symptoms, seizures, respiratory depression (especially with overdose), hypotension, coma.
Most side effects are mild and transient.
Precautions & warnings
- May cause drowsiness; caution when driving or operating machinery.
- Additive sedative effects with alcohol and other CNS depressants.
- Long-term use may lead to drug dependence, withdrawal, and abuse.
- Do not stop suddenly (withdrawal symptoms may occur with long-term use).
- Use during pregnancy only if clearly needed (Category C).
- Caution during breastfeeding; monitor infant for excessive sleepiness.
- Avoid in acute intermittent porphyria or hypersensitivity to carbamates.
Contraindications
- Acute intermittent porphyria
- Hypersensitivity to carbamates such as meprobamate
- Lactation
Drug interactions
- Alcohol and other CNS depressants (benzodiazepines, opioids, tricyclic antidepressants): Additive sedative effects (potentially fatal).
- CYP2C19 inhibitors (omeprazole, fluvoxamine): May increase Carisoprodol exposure.
- CYP2C19 inducers (rifampin): May decrease Carisoprodol exposure.
Food interactions
Alcohol consumption is unsafe (may cause excessive drowsiness and CNS depression).
Use in pregnancy
May be unsafe during pregnancy (Category C). Limited human studies available; animal studies have shown harmful effects on the developing baby. Use during pregnancy only if clearly needed and under medical supervision.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Probably safe during breastfeeding (if prescribed). Limited human data suggests the drug does not pose significant risk to the baby. Monitor the infant for excessive sleepiness.
Pediatric use
Children (16 years): 250-350 mg every 8 hours and at bedtime. Safety in children under 16 years has not been established.
Geriatric use
Elderly: Half of the usual dose.
Renal / hepatic impairment
Hepatic impairment: Limited information; caution required.
Caution is also advised in patients with reduced CYP2C19 activity.
Overdose effects
Overdose symptoms: CNS depression (drowsiness, coma), respiratory depression, hypotension, seizures, death. Treatment: Basic life support, gastric lavage (within 1 hour), IV fluids and vasopressors, IV benzodiazepines or phenobarbital for seizures, tracheal intubation for severe CNS depression.
Storage conditions
Store in a cool and dry place at 20-25°C, away from direct light. Keep out of reach of children.
Chemical structure
Carisoprodol (Carbamate Skeletal Muscle Relaxant)