Mobic - Drug Monograph

Introduction

Mobic (meloxicam) is a nonsteroidal anti-inflammatory drug (NSAID) belonging to the enolic acid class. It is commonly prescribed for its analgesic, anti-inflammatory, and antipyretic properties. Meloxicam exhibits relative selectivity for cyclooxygenase-2 (COX-2) over COX-1 enzymes, which may contribute to a potentially improved gastrointestinal safety profile compared to some non-selective NSAIDs.

Mechanism of Action

Meloxicam works by inhibiting prostaglandin synthesis through competitive inhibition of cyclooxygenase (COX) enzymes. It demonstrates approximately 10-30 times greater selectivity for COX-2 over COX-1 isoenzymes. COX-2 is primarily responsible for synthesizing prostaglandins that mediate pain, inflammation, and fever, particularly at sites of inflammation. By preferentially inhibiting COX-2, meloxicam reduces the production of these inflammatory prostaglandins while potentially preserving the protective prostaglandins produced via COX-1 in the gastrointestinal tract.

Indications

Mobic is FDA-approved for:

• Osteoarthritis (OA)
• Rheumatoid arthritis (RA)
• Juvenile rheumatoid arthritis (JRA) in patients 2 years and older

Off-label uses may include:

• Ankylosing spondylitis
• Acute pain management
• Other inflammatory arthritic conditions

Dosage and Administration

• Osteoarthritis: 7.5 mg once daily
• Rheumatoid arthritis: 15 mg once daily
• Maximum recommended dose: 15 mg daily

• Initiate at 7.5 mg daily
• Consider renal function before dosing

• Mild to moderate impairment: Maximum 7.5 mg daily
• Severe renal impairment: Not recommended

• No dosage adjustment needed for mild to moderate impairment
• Not recommended in severe hepatic impairment

• Take with food to minimize gastrointestinal upset
• Tablets should be swallowed whole with water
• Do not crush or chew

Pharmacokinetics

• Bioavailability: ~89%
• Time to peak concentration: 4-5 hours
• Food does not significantly affect absorption

• Volume of distribution: 10-15 L
• Protein binding: >99% (primarily albumin)
• Crosses placenta and enters breast milk

• Primarily hepatic via CYP2C9 and CYP3A4
• Minor pathways: CYP2C8, peroxidases
• Forms four inactive metabolites

• Half-life: 15-20 hours
• Excretion: Urine and feces (approximately equal)
• Less than 1.5% excreted unchanged in urine

Contraindications

• Hypersensitivity to meloxicam or other NSAIDs
• History of asthma, urticaria, or allergic reactions after taking aspirin or other NSAIDs
• Peri-operative pain in coronary artery bypass graft (CABG) surgery
• Third trimester of pregnancy

Warnings and Precautions

• Increased risk of serious cardiovascular thrombotic events, including MI and stroke
• Risk may increase with duration of use
• Contraindicated in CABG surgery

• Increased risk of GI bleeding, ulceration, and perforation
• Elderly patients at higher risk
• History of GI events increases risk

• May cause renal toxicity
• Monitor patients with impaired renal function, heart failure, or liver dysfunction
• Avoid in advanced renal disease

• May cause severe hepatic reactions
• Monitor liver function tests
• Discontinue if signs or symptoms of liver disease develop

• May worsen existing hypertension or cause new-onset hypertension
• Monitor blood pressure during therapy

Drug Interactions

• Warfarin: Increased risk of bleeding (monitor INR closely)
• Aspirin: Increased GI toxicity (avoid concomitant use)
• Lithium: Increased lithium levels (monitor serum concentrations)
• Methotrexate: Increased methotrexate toxicity (monitor closely)
• Diuretics: Reduced diuretic and antihypertensive effects
• ACE inhibitors/ARBs: Reduced antihypertensive effects
• Cyclosporine: Increased nephrotoxicity risk
• SSRIs/SNRIs: Increased bleeding risk

• CYP2C9 inhibitors (fluconazole, amiodarone): May increase meloxicam levels
• CYP2C9 inducers (rifampin): May decrease meloxicam levels

Adverse Effects

• Dyspepsia (10-12%)
• Nausea (5-7%)
• Diarrhea (4-5%)
• Abdominal pain (4-5%)
• Headache (4-6%)
• Edema (3-5%)
• Upper respiratory infection (3-5%)

• GI bleeding/perforation
• Cardiovascular thrombotic events
• Hepatotoxicity
• Renal impairment/failure
• Severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis)
• Anaphylactic reactions
• Hematologic toxicity (anemia, leukopenia)

Monitoring Parameters

• Complete blood count
• Renal function (BUN, creatinine)
• Liver function tests
• Blood pressure
• GI risk assessment

• CBC every 6-12 months
• Renal function every 6-12 months
• LFTs every 6-12 months
• Blood pressure regularly
• Signs/symptoms of GI bleeding
• Efficacy assessment (pain relief, functional status)

• Elderly: More frequent renal and GI monitoring
• Patients on anticoagulants: Increased bleeding parameter monitoring
• Patients with cardiovascular risk factors: Increased cardiovascular monitoring

Patient Education

• Take with food to reduce stomach upset
• Do not exceed prescribed dose
• Report any signs of bleeding (unusual bruising, blood in stool)
• Watch for signs of allergic reaction (rash, swelling, difficulty breathing)
• Monitor for signs of heart problems (chest pain, shortness of breath)
• Report symptoms of liver problems (nausea, fatigue, jaundice)
• Avoid alcohol during treatment
• Inform all healthcare providers about Mobic use before any procedures
• Do not take other NSAIDs or aspirin unless directed by physician
• Use caution when driving or operating machinery until effects are known
• Store at room temperature away from moisture

• Pregnancy: Avoid during third trimester
• Breastfeeding: Not recommended
• Elderly: Increased risk of adverse effects
• Renal impairment: Requires dose adjustment and close monitoring

References

1. FDA Prescribing Information: Mobic (meloxicam) tablets 2. Drugs.com: Meloxicam Professional Monograph 3. UpToDate: Meloxicam drug information 4. American College of Rheumatology Guidelines for NSAID Use 5. European League Against Rheumatism (EULAR) recommendations 6. Clinical Pharmacology [Internet]. Tampa (FL): Elsevier. Meloxicam monograph 7. PubMed Central: Meloxicam clinical trials and meta-analyses 8. Manufacturer's product information and clinical studies 9. Drug Interaction Facts: Wolters Kluwer Clinical Drug Information 10. Lexicomp Online: Meloxicam monograph