Meloxicam

Approved Indications:

• Osteoarthritis (OA): Relief of signs and symptoms.
• Rheumatoid Arthritis (RA): Relief of signs and symptoms.
• Juvenile Idiopathic Arthritis (JIA): Treatment of signs and symptoms in children aged ≥2 years.

Clinically Accepted Off-Label Uses:

• Ankylosing Spondylitis (AS): Management of pain and inflammation.
• Acute musculoskeletal pain.
• Postoperative pain management.
• Dysmenorrhea: As an alternative NSAID when preferred.

Route of Administration: Oral (tablet, capsule, suspension), Parenteral (intramuscular/intravenous injection).

Adults:

• Osteoarthritis or Rheumatoid Arthritis:
  Oral: 7.5 mg once daily; may increase to 15 mg once daily if necessary.
  Maximum dose: 15 mg/day.
• Ankylosing Spondylitis:
  Oral: 7.5 mg once daily; may increase to 15 mg daily based on response.

Pediatrics (≥2 years):

• Juvenile Idiopathic Arthritis:
  Oral suspension: 0.125 mg/kg once daily.
  Maximum dose: 7.5 mg/day.

Elderly:

• Initiate with 7.5 mg/day; adjust cautiously to minimize GI, renal, and cardiovascular risks.

Renal Impairment:

• No dose adjustment in mild to moderate renal impairment.
• Avoid in patients with severe renal impairment not undergoing dialysis.

Hepatic Impairment:

• Use with caution; monitor liver function.

Parenteral Use:

• Intramuscular or intravenous: 15 mg once daily, used short-term when oral administration is not feasible.

Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) with preferential inhibition of cyclooxygenase-2 (COX-2) over COX-1. It inhibits the synthesis of prostaglandins, which are mediators of inflammation, pain, and fever. By selectively inhibiting COX-2, meloxicam reduces the risk of gastrointestinal side effects commonly associated with non-selective NSAIDs, while effectively decreasing inflammation and providing analgesia.

• Absorption: Well absorbed orally; bioavailability approximately 89%.
• Time to Peak Concentration: 4 to 5 hours (oral); ~60 minutes (parenteral).
• Distribution: Highly protein-bound (~99%).
• Metabolism: Hepatic via CYP2C9 (major) and CYP3A4 (minor).
• Elimination Half-Life: Approximately 15 to 20 hours.
• Excretion: ~60% via feces, ~40% via urine (as metabolites).

• Pregnancy:
• First and Second Trimesters: Use only if clearly needed; may impair fetal renal function.
• Third Trimester: Contraindicated due to risk of premature closure of the ductus arteriosus and oligohydramnios.
• Lactation:
• Limited data suggest minimal excretion into breast milk.
• Use with caution; monitor infant for adverse effects.

• Class: Nonsteroidal Anti-inflammatory Drug (NSAID)
• Subclass: Preferential COX-2 Inhibitor

• Hypersensitivity to meloxicam or other NSAIDs.
• History of asthma, urticaria, or allergic-type reactions after NSAID use.
• Active peptic ulcer or gastrointestinal bleeding.
• Severe hepatic impairment.
• Severe renal impairment (unless on dialysis).
• Pregnancy (third trimester).
• Perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.

• Cardiovascular Risk: Increased risk of serious thrombotic events, including myocardial infarction and stroke.
• Gastrointestinal Risk: Risk of GI bleeding, ulceration, and perforation.
• Renal Risk: May cause renal toxicity, especially in volume-depleted or elderly patients.
• Hepatotoxicity: Periodic liver function monitoring recommended.
• Skin Reactions: May cause serious reactions such as Stevens-Johnson syndrome.
• Fluid Retention and Edema: Use with caution in heart failure and hypertension.
• Elderly: Higher risk of GI bleeding and renal dysfunction.

Common:

• Gastrointestinal: Nausea, dyspepsia, abdominal pain, diarrhea.
• Central Nervous System: Dizziness, headache.
• General: Edema, flu-like symptoms.

Serious:

• Gastrointestinal ulceration or bleeding.
• Myocardial infarction, stroke.
• Acute kidney injury.
• Hepatotoxicity.
• Severe skin reactions (e.g., Stevens-Johnson syndrome, toxic epidermal necrolysis).

• Warfarin and other anticoagulants: Increased risk of bleeding.
• ACE inhibitors, ARBs, and diuretics: Risk of renal dysfunction.
• Methotrexate: May increase methotrexate toxicity.
• Lithium: May increase serum lithium levels.
• Corticosteroids or other NSAIDs: Additive GI toxicity.
• Metabolic Pathway: CYP2C9 (major) and CYP3A4 (minor)

• FDA Safety Communications (latest): Reinforces cardiovascular and gastrointestinal risk warnings for NSAIDs including meloxicam.
• Clinical Guidelines (EULAR, ACR): Recommend meloxicam as a second-line NSAID in patients at moderate GI risk due to its relative COX-2 selectivity.

• Oral Forms: Store at 20°C to 25°C (68°F to 77°F); protect from light and moisture.
• Suspension: Shake well before use; do not freeze.
• Injection: Store between 20°C and 25°C; do not refrigerate or freeze.