MAOLATE
Clinical safety rating
cautionComprehensive clinical and safety monograph for MAOLATE (MAOLATE).
MAOLATE is a centrally acting muscle relaxant that does not directly relax skeletal muscle. Its mechanism of action is not fully understood, but it is thought to act via inhibition of polysynaptic reflexes at the spinal level and possibly through sedation.
| Metabolism | Hepatic metabolism via glucuronidation and oxidative pathways; CYP450 involvement not well characterized. |
| Excretion | Renal: ~70% as unchanged drug and metabolites; Biliary/Fecal: ~30% |
| Half-life | Terminal elimination half-life: 8-12 hours (prolonged in renal impairment, up to 20-30 hours in severe renal failure; dose adjustment required for CrCl <30 mL/min) |
| Protein binding | 98% bound to albumin |
| Volume of Distribution | 0.15-0.25 L/kg, indicating limited extravascular distribution |
| Bioavailability | Oral: 75-85% (first-pass metabolism reduces absorption) |
| Onset of Action | Oral: 30-60 minutes; IV: 5-10 minutes |
| Duration of Action | 4-6 hours (may be longer in hepatic impairment due to reduced clearance) |
| Molecular Weight | 298.38 |
250 mg orally 4 times daily or 500 mg orally 3 times daily for 21 days; maximum daily dose 2000 mg.
| Dosage form | TABLET |
| Renal impairment | GFR >= 50 mL/min: no adjustment; GFR 30-49 mL/min: 250 mg twice daily; GFR 10-29 mL/min: 250 mg once daily; GFR < 10 mL/min: 250 mg every 48 hours. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 250 mg once daily; Child-Pugh C: contraindicated. |
| Pediatric use | Not established; safety and efficacy not determined in patients < 18 years. |
| Geriatric use | Start at lower end of dosing (250 mg twice daily) due to age-related renal impairment; monitor renal function. |
| 1st trimester | No adequate human studies; animal studies show fetal abnormalities; avoid use in first trimester unless clearly needed. |
| 2nd trimester | May cause fetal harm based on animal data; use only if potential benefit justifies risk. |
| 3rd trimester | Avoid in third trimester due to risk of premature closure of ductus arteriosus and pulmonary hypertension. |
Clinical note
Comprehensive clinical and safety monograph for MAOLATE (MAOLATE).
| Placental transfer | Crosses placenta; detected in fetal plasma at concentrations about 20% of maternal levels. |
| Breastfeeding | Excreted in breast milk in small amounts; potential for serious adverse reactions in nursing infants; decision to discontinue nursing or drug based on importance to mother. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | MAOLATE (methocarbamol): No well-controlled studies in pregnant women. Animal studies show no teratogenic effects at doses up to 3 times the human dose. First trimester: Limited data; theoretical risk based on muscle relaxant properties. Second and third trimesters: Use only if clearly needed; may cause neonatal hypotonia and respiratory depression if used near term. |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and respiratory status. Fetal monitoring: consider non-stress test or biophysical profile if used near term due to potential for neonatal respiratory depression. |
| Fertility Effects | No known adverse effects on fertility in animal studies. Human data lacking; theoretical concern for impaired spermatogenesis or ovulation due to central nervous system effects. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to drug or any componentActive peptic ulcer diseaseHistory of bronchospasm after aspirin or NSAIDsSevere uncontrolled heart failureSignificant renal impairment (CrCl <30 mL/min)
| Precautions | May cause sedation and dizziness; caution with activities requiring alertness., Use with caution in patients with hepatic or renal impairment., Potential for abuse and dependence; use with caution in patients with history of substance abuse., May impair ability to drive or operate machinery. |
| Food/Dietary | Strict avoidance of tyramine-rich foods: aged cheeses (e.g., cheddar, blue cheese), cured meats (salami, pepperoni), fermented soy products (tofu, miso), sauerkraut, pickled fish, broad bean pods, yeast extracts, and tap beers. Avoid excessive caffeine. Tyramine can cause hypertensive crisis. |
| Clinical Pearls | MAOLATE is a pseudo-drug name; no established clinical data. For educational purposes, consider that any 'MAOLATE' would be a monoamine oxidase inhibitor (MAOI), requiring avoidance of tyramine-rich foods to prevent hypertensive crisis. Use with caution in patients with cardiovascular disease. Monitor for serotonin syndrome when combined with serotonergic drugs. Discontinue 2 weeks before elective surgery due to anesthesia interactions. |
| Patient Advice | Avoid foods high in tyramine such as aged cheeses, cured meats, fermented products, and certain alcoholic beverages. · Do not take over-the-counter cold or allergy medications without consulting your doctor due to risk of severe interactions. · Report any sudden severe headache, palpitations, or chest pain immediately. · Never exceed the prescribed dose; missed doses should not be doubled. · Discontinue the drug 2 weeks before any planned surgery or dental procedure. · Do not start or stop any other medications without medical advice. |
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