MECLOMEN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for MECLOMEN (MECLOMEN).
Meclomen (meclofenamate) is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing prostaglandin synthesis. This results in anti-inflammatory, analgesic, and antipyretic effects.
| Metabolism | Meclomen is metabolized primarily via hepatic glucuronidation. Minor involvement of cytochrome P450 (CYP) enzymes (likely CYP3A4 and CYP2C9) observed. Renal excretion of unchanged drug and metabolites. |
| Excretion | Renal (approximately 70% as metabolites, <5% unchanged); fecal/biliary (approximately 30% as metabolites). |
| Half-life | Terminal elimination half-life: 0.8–1.1 hours for meclofenamic acid; 2–4 hours for metabolites. Short half-life requires frequent dosing (e.g., every 6–8 hours) for sustained effect. |
| Protein binding | Greater than 99% bound, primarily to albumin. |
| Volume of Distribution | Approximately 0.3 L/kg; distributes into synovial fluid but low penetration into CNS. |
| Bioavailability | Oral: approximately 100% (well absorbed). |
| Onset of Action | Oral: 30–60 minutes for analgesic effect; peak plasma concentrations at 0.5–2 hours. |
| Duration of Action | Analgesic effect: 4–6 hours (short duration necessitates frequent dosing). Anti-inflammatory effect may require several days of therapy to become apparent. |
50-100 mg orally every 6-8 hours; maximum 400 mg/day.
| Dosage form | CAPSULE |
| Renal impairment | GFR 30-60 mL/min: avoid use or reduce dose; GFR <30 mL/min: contraindicated. |
| Liver impairment | Child-Pugh Class A: no adjustment; Class B: reduce dose by 50%; Class C: avoid use. |
| Pediatric use | Not recommended for children under 14 years; safety not established. |
| Geriatric use | Start at lowest effective dose; reduce dose by 50% due to increased risk of GI bleeding and renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for MECLOMEN (MECLOMEN).
| Breastfeeding | Excreted in breast milk in low amounts; M/P ratio not established. Use caution due to potential for adverse effects in infant (e.g., gastrointestinal bleeding, renal toxicity). |
| Teratogenic Risk | First trimester: Avoid due to potential for cardiovascular and neural tube defects. Second and third trimesters: Contraindicated; may cause premature closure of ductus arteriosus, oligohydramnios, and neonatal renal impairment. |
| Fetal Monitoring |
■ FDA Black Box Warning
Nonsteroidal anti-inflammatory drugs (NSAIDs) cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. Risk may increase with duration of use. Patients with cardiovascular disease or risk factors may be at greater risk. NSAIDs are contraindicated for the treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.
| Serious Effects |
Hypersensitivity to meclofenamate or any component of the formulation; history of asthma, urticaria, or allergic-type reaction after taking aspirin or other NSAIDs; perioperative pain in the setting of coronary artery bypass graft (CABG) surgery; active significant GI bleeding; moderate to severe renal impairment (CrCl <30 mL/min); advanced hepatic disease; third trimester of pregnancy (may cause premature closure of ductus arteriosus and oligohydramnios).
| Precautions | Cardiovascular thrombotic events; gastrointestinal adverse events including bleeding, ulceration, and perforation; renal toxicity (elevated serum creatinine, acute renal failure); hepatic effects (elevated liver enzymes, hepatotoxicity); anaphylactoid reactions; exacerbation of asthma; hypertension; fluid retention; serious skin reactions (e.g., Stevens-Johnson syndrome). Use with caution in elderly, patients with history of peptic ulcer disease, renal impairment, or hepatic impairment. |
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| Monitor amniotic fluid volume, ductus arteriosus patency (fetal echocardiography), and fetal renal function. Maternal monitoring of blood pressure, renal function, and gastrointestinal symptoms. |
| Fertility Effects | May impair fertility in women via inhibition of prostaglandin synthesis affecting ovulation; reversible upon discontinuation. |