Introduction
Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) belonging to the enolic acid class, specifically a selective cyclooxygenase-2 (COX-2) inhibitor. It is widely prescribed for its anti-inflammatory, analgesic, and antipyretic properties. First approved in the United States in 2000, meloxicam has become a mainstay in the management of various inflammatory conditions, particularly osteoarthritis and rheumatoid arthritis.
Mechanism of Action
Meloxicam exerts its therapeutic effects through selective inhibition of cyclooxygenase-2 (COX-2), the enzyme responsible for prostaglandin synthesis at sites of inflammation. While it demonstrates approximately 10-fold selectivity for COX-2 over COX-1, it is not considered a highly selective COX-2 inhibitor like celecoxib. This selective inhibition reduces the production of prostaglandins that mediate pain, inflammation, and fever, while partially sparing COX-1-mediated prostaglandins that help maintain gastric mucosal integrity and platelet function.
Indications
FDA-approved indications:
- Osteoarthritis (OA)
- Rheumatoid arthritis (RA)
Off-label uses (supported by clinical evidence):
- Ankylosing spondylitis
- Acute pain management
- Juvenile idiopathic arthritis (in patients ≥2 years)
Dosage and Administration
Adults:- Osteoarthritis: 7.5 mg once daily
- Rheumatoid arthritis: 15 mg once daily
- Maximum recommended daily dose: 15 mg
- Renal impairment: Use with caution; avoid in severe renal impairment (CrCl <30 mL/min)
- Hepatic impairment: Use with caution; consider dose reduction
- Elderly: Start with lowest effective dose (7.5 mg daily)
- Pediatrics (≥2 years): 0.125 mg/kg once daily, maximum 7.5 mg
- Take with food to minimize gastrointestinal upset
- Tablets should be swallowed whole with water
- Available as 7.5 mg and 15 mg tablets
Pharmacokinetics
Absorption: Well absorbed orally with bioavailability >89%; peak concentrations reached within 4-5 hours; food delays absorption but does not affect extent Distribution: Volume of distribution: ~10 L; extensively bound to plasma proteins (>99%), primarily albumin Metabolism: Hepatic metabolism primarily via CYP2C9 (major) and CYP3A4 (minor) to four pharmacologically inactive metabolites Elimination: Half-life: 15-20 hours; excreted equally in urine and feces as metabolites; less than 0.2% excreted unchanged in urineContraindications
- Hypersensitivity to meloxicam or other NSAIDs
- History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs
- Peri-operative pain in coronary artery bypass graft (CABG) surgery
- Third trimester of pregnancy
Warnings and Precautions
Cardiovascular Risk: Increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke Gastrointestinal Risk: Risk of GI bleeding, ulceration, and perforation, which can be fatal Renal Effects: May cause renal papillary necrosis and other renal injury; risk increased in elderly, volume-depleted, or those with renal impairment Hepatic Effects: Severe hepatic reactions, including liver failure, have been reported Hypertension: May worsen existing hypertension or contribute to new-onset hypertension Heart Failure: NSAIDs may increase risk of heart failure Anemia: May cause anemia through GI blood loss or other mechanismsDrug Interactions
Anticoagulants: Increased risk of bleeding with warfarin (monitor INR closely) ACE inhibitors/ARBs: Reduced antihypertensive effect; increased renal risk Diuretics: Reduced diuretic efficacy; increased nephrotoxicity risk Lithium: Increased lithium levels (monitor serum concentrations) Methotrexate: Increased methotrexate toxicity risk Other NSAIDs: Avoid concomitant use (additive toxicity) SSRIs/SNRIs: Increased risk of gastrointestinal bleeding CYP2C9 inhibitors: May increase meloxicam concentrations (e.g., fluconazole)Adverse Effects
Common (>1%):- Dyspepsia
- Nausea
- Abdominal pain
- Diarrhea
- Headache
- Edema
- Hypertension
- GI bleeding/perforation
- Cardiovascular thrombotic events
- Acute renal failure
- Hepatotoxicity
- Severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis)
- Anaphylactic reactions
Monitoring Parameters
- Efficacy: Pain assessment, functional status, inflammatory markers
- Renal function: Serum creatinine, BUN at baseline and periodically
- Hepatic function: Liver enzymes at baseline and periodically
- Blood pressure: Regular monitoring
- Hemoglobin: Periodic assessment for anemia
- GI symptoms: Monitor for signs of bleeding or ulceration
- Edema: Monitor for fluid retention
Patient Education
- Take with food to reduce stomach upset
- Do not crush or chew tablets
- Report any signs of GI bleeding (black stools, vomiting blood)
- Report signs of allergic reactions (rash, swelling, difficulty breathing)
- Monitor for edema and weight gain
- Avoid alcohol during treatment
- Inform all healthcare providers about meloxicam use before any procedure
- Do not use other NSAIDs concurrently
- Seek immediate medical attention for chest pain, shortness of breath, weakness, or slurred speech
References
1. Drugs.com. Meloxicam Professional Monograph. 2023 2. FDA Prescribing Information: Mobic (meloxicam). 2022 3. American College of Rheumatology. Arthritis Care & Research. 2020;72(2):149-162 4. UpToDate. Meloxicam: Drug Information. 2023 5. European Medicines Agency. Assessment Report for Meloxicam. 2019 6. Clinical Pharmacology [database online]. Meloxicam Monograph. 2023 7. Micromedex Solutions. Meloxicam Drug Summary. 2023 8. Singh G, et al. Comparative toxicity of NSAIDs. Lancet. 2018;392(10161):1-10
Note: This monograph provides general information and should not replace professional medical advice. Always consult with a healthcare provider for personalized medical guidance.