Carisoprodol

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[edit] BRAND NAMES

[edit] STRUCTURE

Carisoprodol.jpg

[edit] MECHANISM OF ACTION

Carisoprodol is a centrally acting skeletal muscle relaxant that does not directly relax skeletal muscles. The pharmacological effects of carisoprodol have been attributed to its active metabolite, meprobamate, a controlled substance that produces sedation via GABAA receptors (GABAAR).

The GABAA receptor is a pentameric ligand-gated ion channel. Upon activation, it selectively conducts Cl- through its pore, resulting in hyperpolarization of the neuron which reduces cell excitability.

[edit] INDICATIONS

Carisoprodol is indicated for the relief of discomfort associated with acute, painful musculoskeletal conditions in adult. Carisoprodol should only be used for acute treatment periods up to two or three weeks

[edit] DOSAGE

Recommended dose is 250 mg to 350 mg three times a day and at bedtime

[edit] DOSAGE FORMS AND STRENGTHS

  • Tablets: 250 mg, 350 mg

[edit] CONTRAINDICATIONS

  • Acute intermittent porphyria
  • Hypersensitivity reactions to a carbamate such as meprobamate

[edit] WARNINGS AND PRECAUTIONS

  • 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 abuse, dependence, and withdrawal
  • Seizures

[edit] INTERACTIONS

  • CNS depressants (e.g., alcohol, benzodiazepines, opioids, tricyclic antidepressants): additive sedative effects

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Carisoprodol should be used during pregnancy only if the potential benefit justifies the risk to the fetus.
  • Nursing Mothers: Very limited data in humans show that Carisoprodol is present in breast milk and may reach concentrations two to four times the maternal plasma concentrations. In one case report, a breast-fed infant received about 4-6% of the maternal daily dose through breast milk and experienced no adverse effects. However, milk production was inadequate and the baby was supplemented with formula. In lactation studies in mice, female pup survival and pup weight at weaning were decreased. This information suggests that maternal use of Carisoprodol may lead to reduced or less effective infant feeding (due to sedation) and/or decreased milk production. Caution should be exercised when Carisoprodol is administered to a nursing woman

[edit] SIDE EFFECTS

Most common adverse reactions (incidence > 2%) are drowsiness, dizziness, and headache

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES