OZOBAX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OZOBAX (OZOBAX).
OZOBAX (carisoprodol) is a centrally acting skeletal muscle relaxant that does not directly relax skeletal muscle. Its mechanism of action is thought to be related to its sedative properties and its metabolite, meprobamate, which has anxiolytic and sedative effects. Carisoprodol acts as a GABA-A receptor agonist and may also inhibit interneuronal activity in the spinal cord and reticular formation.
| Metabolism | Carisoprodol is metabolized in the liver via CYP2C19 to its active metabolite, meprobamate. Both carisoprodol and meprobamate are further metabolized by other pathways. |
| Excretion | Primarily renal excretion of unchanged drug (approximately 70-80% of the dose) with minor biliary/fecal elimination (10-15%). |
| Half-life | Terminal elimination half-life is approximately 12-15 hours in adults with normal renal function. This supports twice-daily dosing in most patients. |
| Protein binding | Approximately 95% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is about 0.8-1.2 L/kg, indicating distribution into total body water with some tissue binding. |
| Bioavailability | Oral bioavailability is approximately 80-90% due to extensive absorption and minimal first-pass metabolism. |
| Onset of Action | Oral: Onset of analgesia occurs within 1-2 hours; peak effect at 3-5 hours. Intravenous: Onset within 5-15 minutes. |
| Duration of Action | Duration of analgesia is approximately 8-12 hours for oral and 6-10 hours for intravenous administration, depending on dose and patient factors. |
OZOBAX (baclofen) oral: Initial 5 mg three times daily, may increase by 5 mg per dose every 3 days to max 80 mg/day (20 mg four times daily). Intrathecal: Test dose 50-100 mcg, then continuous infusion via pump 22-900 mcg/day.
| Dosage form | SOLUTION |
| Renal impairment | CrCl <30 mL/min: Reduce dose by 50% or increase interval. Use with caution; avoid in severe impairment. |
| Liver impairment | Child-Pugh Class B or C: No specific guidelines; use with caution due to potential CNS accumulation. |
| Pediatric use | Children 2-7 years: Initial 2.5-5 mg orally twice daily, increase slowly to max 40 mg/day (divided 4 times). Children 8-12 years: Initial 5 mg twice daily, max 60 mg/day. Intrathecal: Not recommended in pediatric patients. |
| Geriatric use | Start at lower end of dosing range (5 mg twice daily), increase slowly. Monitor for sedation, confusion, and falls. Adjust for renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OZOBAX (OZOBAX).
| Breastfeeding | Omeprazole: excreted in breast milk in small amounts (M/P ratio 0.5-0.6); considered compatible with breastfeeding. Sodium bicarbonate: excreted in milk; no known adverse effects. Clarithromycin: excreted in breast milk; unknown M/P ratio; monitor infant for diarrhea or rash. Use caution and consider alternatives. |
| Teratogenic Risk | OZOBAX is a combination product containing omeprazole, sodium bicarbonate, and clarithromycin. Omeprazole: No evidence of teratogenicity in animal studies; human data limited but not suggestive of major malformations. Sodium bicarbonate: No known teratogenic risk. Clarithromycin: Animal studies show embryofetal toxicity at high doses; human data are conflicting but generally considered low risk; avoid in first trimester if possible. Overall, risk is low but use only if clearly needed. |
■ FDA Black Box Warning
WARNING: RISKS FROM CONCOMITANT USE WITH OPIOIDS; ABUSE, MISUSE, AND ADDICTION; AND DEPENDENCE AND WITHDRAWAL. Concomitant use of opioids with benzodiazepines or other CNS depressants, including carisoprodol, may result in profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing for patients for whom alternative treatment options are inadequate. Limit dosages and durations to the minimum required. Follow patients for signs and symptoms of respiratory depression and sedation. Carisoprodol is subject to abuse, misuse, and addiction. Abuse and misuse of carisoprodol can result in overdose and death, especially when used in combination with other CNS depressants. Patients should be assessed for risk before prescribing and monitored regularly for these behaviors and conditions. Physical dependence can occur with prolonged use; abrupt discontinuation may result in withdrawal symptoms, including anxiety, insomnia, vomiting, hallucinations, and seizures.
| Serious Effects |
["Hypersensitivity to carisoprodol, meprobamate, or any component of the formulation","Acute intermittent porphyria","Concomitant use with other CNS depressants (e.g., opioids, benzodiazepines) except when alternative options are inadequate","History of drug abuse or addiction (relative contraindication due to abuse potential)"]
| Precautions | ["Risks from concomitant use with opioids: profound sedation, respiratory depression, coma, and death","Abuse, misuse, and addiction: can occur even at recommended doses","Dependence and withdrawal: abrupt discontinuation may cause withdrawal symptoms","CNS depression: may impair mental/physical abilities; advise against driving or hazardous tasks","Seizures: may occur, especially with abuse or withdrawal","Concomitant use with alcohol or other CNS depressants: additive effects","Renal/hepatic impairment: use with caution","Pregnancy: may cause neonatal withdrawal syndrome with prolonged use"] |
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| Fetal Monitoring | Monitor maternal renal function, electrolytes (especially bicarbonate and potassium), and liver function tests. Assess for signs of infection (clarithromycin-related). In pregnancy, monitor fetal growth and well-being via ultrasound if prolonged use. For clarithromycin, monitor for QT prolongation if concomitant risk factors. |
| Fertility Effects | No evidence that OZOBAX components impair fertility in humans. Animal studies with clarithromycin showed reduced fertility at high doses. Omeprazole and sodium bicarbonate are not associated with fertility impairment. |