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Mefenamic Acid is an anti-inflammatory and analgesic drug with antipyretic, analgesic and anti-inflammatory effects. The analgesic effect is strong and the antipyretic effect is long-lasting, but the anti-inflammatory effect is not as good as that of Baotaisong and flufenamic acid.
Mefenamic acid is a nonsteroidal anti-inflammatory drug (NSAID) belonging to the fenamate class. It is primarily used for its analgesic, anti-inflammatory, and antipyretic properties.
– Inhibits cyclooxygenase (COX-1 and COX-2), reducing prostaglandin synthesis.
– Modulates pain and inflammation by blocking prostaglandin-mediated effects.
– Pain Relief: Effective for mild to moderate pain (e.g., headaches, dental pain, dysmenorrhea).
– Inflammatory Conditions: Used in rheumatoid arthritis and osteoarthritis (though less common than other NSAIDs).
– Menstrual Pain (Primary Dysmenorrhea):** One of its key indications due to strong prostaglandin inhibition.
– Absorption: Rapidly absorbed after oral administration (~50% bioavailability).
– Metabolism: Hepatic metabolism via CYP2C9.
– Excretion:Primarily renal (urine), with a half-life of **2–4 hours**.
– Common: GI disturbances (nausea, diarrhea, dyspepsia), dizziness, headache.
– Serious:
– GI ulcers/bleeding (higher risk than some NSAIDs).
– Renal impairment (especially in dehydrated or elderly patients).
– Hypersensitivity reactions (rash, Stevens-Johnson syndrome).
– Hepatotoxicity (rare but reported).
– Anticoagulants (e.g., warfarin): ↑ Bleeding risk.
– Diuretics/ACE inhibitors:Reduced efficacy due to fluid retention.
– Other NSAIDs/aspirin: ↑ GI toxicity.
– Contraindicated in:
– Peptic ulcer disease.
– Severe renal/hepatic impairment.
– Asthma/NSAID-induced hypersensitivity.
– Use with caution in:
– Elderly patients.
– Cardiovascular disease (may ↑ BP).
– Short-term use preferred (due to higher GI toxicity risk).
– Avoid in pregnancy (3rd trimester)—risk of premature ductus arteriosus closure.
Mefenamic acid is effective for acute pain and dysmenorrhea but carries significant GI and renal risks. Should be used at the **lowest effective dose for the shortest duration.
| Property | Specification | Test Method |
|---|---|---|
| Chemical Name | 2-[(2.3-Dimethylphenyl)amino]benzoic acid | IUPAC nomenclature |
| Molecular Formula | C₁₅H₁₅NO₂ | Elemental analysis |
| Molecular Weight | 241.29 g/mol | Mass spectrometry |
| Appearance | White to pale yellow crystalline powder | Visual inspection |
| Solubility (25°C) | Practically insoluble in water, soluble in ethanol, acetone | USP <911> |
| Melting Point | 230–235°C | DSC analysis |
| Parameter | Value/Description | Reference Standard |
|---|---|---|
| Mechanism of Action | Non-selective COX inhibitor | FDA label |
| Bioavailability | ~90% (oral) | Clinical studies |
| Half-life (t₁/₂) | 2–4 hours | Pharmacokinetic data |
| Protein Binding | >90% | In vitro studies |
| Metabolism | Hepatic (CYP2C9-mediated) | EMA assessment report |
| Medical Condition | Recommended Dosage | Maximum Daily Dose |
|---|---|---|
| Mild to moderate pain | 500 mg initial dose, then 250 mg every 6h | 1.500 mg |
| Primary dysmenorrhea | 500 mg loading dose, then 250 mg every 6h | 1.500 mg |
| Rheumatoid arthritis | 250–500 mg three times daily | 1.500 mg |
| Standard | Requirement | Compliance Status |
|---|---|---|
| USP-NF | Meets monograph standards | Compliant |
| Ph. Eur. | Conforms to EP 10.0 | Compliant |
| BP 2023 | Meets British Pharmacopoeia | Compliant |
| ICH Q3D (Impurities) | Heavy metals <20 ppm | Compliant |
| Residual Solvents | Class 2/3 limits per ICH Q3C | Compliant |
| Parameter | Specification |
|---|---|
| Storage temperature | 15–30°C (controlled room temp) |
| Shelf life | 36 months (unopened) |
| Light sensitivity | Protect from light |
| Packaging | HDPE bottles with desiccant |
| Regulatory status | FDA/EMA-approved prescription drug |
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