MELAMISA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for MELAMISA (MELAMISA).

How it works

Meloxicam selectively inhibits cyclooxygenase-2 (COX-2), reducing the synthesis of prostaglandins involved in inflammation, pain, and fever, while sparing COX-1 activity at therapeutic doses.

What the body does with it

Metabolism	Primarily hepatic via CYP2C9 (major) and CYP3A4 (minor) isoenzymes; also undergoes glucuronidation. Less than 1% excreted unchanged in urine.
Excretion	Renal (approximately 50% as unchanged drug and metabolites), biliary/fecal (approximately 30%), with minor pulmonary elimination. Total clearance is about 1.2 mL/min/kg.
Half-life	Terminal elimination half-life is 6.5–9.8 hours in adults with normal renal function; prolonged to >24 hours in severe renal impairment (CrCl <30 mL/min), requiring dose adjustment.
Protein binding	Approximately 98% bound, primarily to serum albumin.
Volume of Distribution	Vd is 0.35–0.45 L/kg; distributed mainly in extracellular fluid, with limited CNS penetration unless meninges inflamed.
Bioavailability	Oral: 75–85% (first-pass metabolism reduces absolute bioavailability from 95% absorbed); Intramuscular: nearly 100%; Rectal: 50–70% (variable).
Onset of Action	Intravenous: 5–15 minutes; Oral: 1–2 hours (delayed if taken with food).
Duration of Action	Intravenous: 6–8 hours for antipyretic/analgesic effect; Oral: 4–6 hours. Duration may be extended with repeated dosing due to accumulation.

Classification & Brands

Dosing & administration

100 mg orally twice daily for 5 days; take with food.

Dosage form	TABLET
Renal impairment	GFR ≥ 30 mL/min: no adjustment; GFR 15-29 mL/min: 100 mg once daily; GFR < 15 mL/min or dialysis: not recommended.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: 100 mg once daily; Child-Pugh C: contraindicated.
Pediatric use	Children ≥ 2 years: 4 mg/kg orally twice daily for 5 days, max 100 mg per dose.
Geriatric use	Use with caution; consider starting at 100 mg once daily due to increased risk of adverse effects.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for MELAMISA (MELAMISA).

Breastfeeding	MELAMISA is excreted in human milk; M/P ratio approximately 0.3. Potential for serious adverse reactions in nursing infants; breastfeeding is not recommended during therapy and for at least 2 weeks after the last dose due to long half-life.
Teratogenic Risk	MELAMISA is contraindicated in pregnancy due to evidence of fetal harm. First trimester: increased risk of major congenital malformations, particularly cardiac and neural tube defects. Second and third trimesters: risk of oligohydramnios, fetal renal dysfunction, and premature closure of the ductus arteriosus.

Warnings & precautions

■ 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. This risk may occur early in treatment and may increase with duration of use. Meloxicam is contraindicated in the setting of coronary artery bypass graft (CABG) surgery.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to meloxicam, aspirin, or other NSAIDs; history of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs; peri-operative pain setting of CABG surgery; active gastrointestinal bleeding; advanced renal disease; patients with severe uncontrolled heart failure; third trimester of pregnancy.

Clinical Precautions

Precautions

Cardiovascular risk (thrombotic events, MI, stroke, hypertension); gastrointestinal risk (bleeding, ulceration, perforation); renal toxicity (especially in elderly, volume-depleted, or those with pre-existing renal impairment); hepatic effects (elevated liver enzymes); anaphylactoid reactions; fluid retention and edema; asthma exacerbation in aspirin-sensitive patients; skin reactions (including Stevens-Johnson syndrome); use in late pregnancy should be avoided due to risk of premature ductus arteriosus closure.

Clinical Tips & Counseling

Drug interactions

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MELAMISA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for MELAMISA (MELAMISA).

How it works

Meloxicam selectively inhibits cyclooxygenase-2 (COX-2), reducing the synthesis of prostaglandins involved in inflammation, pain, and fever, while sparing COX-1 activity at therapeutic doses.

What the body does with it

Metabolism	Primarily hepatic via CYP2C9 (major) and CYP3A4 (minor) isoenzymes; also undergoes glucuronidation. Less than 1% excreted unchanged in urine.
Excretion	Renal (approximately 50% as unchanged drug and metabolites), biliary/fecal (approximately 30%), with minor pulmonary elimination. Total clearance is about 1.2 mL/min/kg.
Half-life	Terminal elimination half-life is 6.5–9.8 hours in adults with normal renal function; prolonged to >24 hours in severe renal impairment (CrCl <30 mL/min), requiring dose adjustment.
Protein binding	Approximately 98% bound, primarily to serum albumin.
Volume of Distribution	Vd is 0.35–0.45 L/kg; distributed mainly in extracellular fluid, with limited CNS penetration unless meninges inflamed.
Bioavailability	Oral: 75–85% (first-pass metabolism reduces absolute bioavailability from 95% absorbed); Intramuscular: nearly 100%; Rectal: 50–70% (variable).
Onset of Action	Intravenous: 5–15 minutes; Oral: 1–2 hours (delayed if taken with food).
Duration of Action	Intravenous: 6–8 hours for antipyretic/analgesic effect; Oral: 4–6 hours. Duration may be extended with repeated dosing due to accumulation.

Classification & Brands

Dosing & administration

100 mg orally twice daily for 5 days; take with food.

Dosage form	TABLET
Renal impairment	GFR ≥ 30 mL/min: no adjustment; GFR 15-29 mL/min: 100 mg once daily; GFR < 15 mL/min or dialysis: not recommended.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: 100 mg once daily; Child-Pugh C: contraindicated.
Pediatric use	Children ≥ 2 years: 4 mg/kg orally twice daily for 5 days, max 100 mg per dose.
Geriatric use	Use with caution; consider starting at 100 mg once daily due to increased risk of adverse effects.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for MELAMISA (MELAMISA).

Breastfeeding	MELAMISA is excreted in human milk; M/P ratio approximately 0.3. Potential for serious adverse reactions in nursing infants; breastfeeding is not recommended during therapy and for at least 2 weeks after the last dose due to long half-life.
Teratogenic Risk	MELAMISA is contraindicated in pregnancy due to evidence of fetal harm. First trimester: increased risk of major congenital malformations, particularly cardiac and neural tube defects. Second and third trimesters: risk of oligohydramnios, fetal renal dysfunction, and premature closure of the ductus arteriosus.