Usage
- Meloxicam is prescribed for the relief of signs and symptoms of osteoarthritis, rheumatoid arthritis, and juvenile rheumatoid arthritis (JRA) in patients 2 years and older. It can also be used for other types of pain.
- Pharmacological classification: Nonsteroidal anti-inflammatory drug (NSAID).
- Mechanism of action: Meloxicam works by inhibiting cyclooxygenase (COX) enzymes, primarily COX-2. COX enzymes produce prostaglandins, which are involved in inflammation and pain. By inhibiting COX enzymes, meloxicam reduces prostaglandin production, thereby decreasing inflammation and pain.
Alternate Names
- International and regional variations: The generic name Meloxicam is commonly used internationally.
- Brand names: Mobic, Vivlodex.
How It Works
- Pharmacodynamics: Meloxicam exerts its anti-inflammatory, analgesic, and antipyretic effects by inhibiting prostaglandin synthesis via preferential inhibition of COX-2. This leads to a decrease in inflammation and pain.
- Pharmacokinetics:
- Absorption: Meloxicam is well-absorbed orally, with an absolute bioavailability of approximately 89%. Food does not significantly affect absorption.
- Metabolism: Meloxicam is extensively metabolized in the liver, primarily by CYP2C9, to inactive metabolites.
- Elimination: Meloxicam is eliminated primarily through the kidneys (approximately 50%) and the remainder through the feces. The drug has a half-life of about 20 hours.
- Mode of Action: Meloxicam binds to COX-2 enzymes, inhibiting their activity and reducing the production of inflammatory prostaglandins. It has a preferential effect on COX-2 over COX-1, which may contribute to a lower incidence of gastrointestinal side effects compared to some other NSAIDs.
- Elimination Pathways: Meloxicam is eliminated by both renal (urine) and hepatic (bile/feces) routes after being metabolized in the liver, primarily by the CYP2C9 enzymes.
Dosage
Standard Dosage
Adults:
- Osteoarthritis and Rheumatoid Arthritis: 7.5 mg orally once a day. The dose may be increased to a maximum of 15 mg per day if needed.
- Other pain: Up to 15 mg once daily.
Children:
- JRA (2 years and older and weighing 60 kg or more): 7.5 mg orally once daily. For JRA in children under 60 kg, the recommended dose is 0.125 mg/kg orally once daily, up to a maximum of 7.5 mg per day.
- Pediatric Safety Considerations: Meloxicam is not recommended for children younger than 2 years old. Careful monitoring is necessary in pediatric patients due to potential adverse effects on growth and development.
Special Cases:
- Elderly Patients: Start with 7.5 mg orally once daily. Close monitoring for adverse effects is recommended.
- Patients with Renal Impairment: For patients with severe renal impairment or on hemodialysis, the maximum recommended dose is 7.5 mg per day.
- Patients with Hepatic Dysfunction: Use with caution. No specific dosage adjustments are provided in the available sources, but close monitoring is advised.
- Patients with Comorbid Conditions: Careful dose adjustment may be necessary in patients with diabetes, cardiovascular disease, or other relevant conditions. Consult a specialist for individualized recommendations.
Clinical Use Cases
Meloxicam is not typically used in clinical settings such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations that require rapid pain relief or control of inflammation. Other medications might be more suitable for such acute situations.
Dosage Adjustments
Dose adjustments may be needed based on patient response, renal or hepatic function, and other individual factors. Closely monitor patients for side effects and adjust the dose accordingly. Genetic polymorphisms affecting CYP2C9 may influence meloxicam metabolism, and genotyping may be considered.
Side Effects
Common Side Effects
- Gastrointestinal issues: Abdominal pain, diarrhea, indigestion, nausea, constipation, gas.
- Dizziness, headache.
- Itching, rash.
- Cold or flu symptoms.
Rare but Serious Side Effects
- Cardiovascular: Heart attack, stroke, heart failure, blood clots.
- Gastrointestinal: Ulcers, bleeding.
- Hepatic: Liver damage or dysfunction.
- Renal: Kidney failure or dysfunction.
- Hypersensitivity reactions: Anaphylaxis, angioedema.
- Hematologic: Anemia.
- Skin reactions: Stevens-Johnson syndrome, toxic epidermal necrolysis.
Long-Term Effects
Long-term use of meloxicam can increase the risk of cardiovascular and gastrointestinal complications, as well as renal and hepatic dysfunction.
Adverse Drug Reactions (ADR)
Any severe adverse reaction requires immediate medical attention and discontinuation of the drug.
Contraindications
- Hypersensitivity to meloxicam or other NSAIDs.
- History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs.
- Active peptic ulcer disease.
- Severe heart failure.
- Severe renal impairment or patients on dialysis (maximum dose 7.5 mg/day).
- History of gastrointestinal bleeding.
- Peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.
- Pregnancy (especially after 20 weeks).
Drug Interactions
- Other NSAIDs and Aspirin: Increased risk of gastrointestinal side effects.
- Anticoagulants (e.g., warfarin): Increased risk of bleeding.
- Antihypertensives (e.g., ACE inhibitors, diuretics, beta-blockers): Reduced effectiveness of antihypertensive medication.
- Corticosteroids: Increased risk of gastrointestinal ulcers and bleeding.
- SSRIs and SNRIs: Increased risk of bleeding.
- Lithium and Methotrexate: Increased serum levels of these drugs.
- Alcohol: Increased risk of gastrointestinal side effects.
- CYP2C9 inhibitors and inducers: May affect meloxicam metabolism and require dose adjustments.
- Pemetrexed, cyclosporine, cholestyramine: May result in increased risk of toxicity.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: C (first and second trimester), D (third trimester).
- Fetal Risks: Meloxicam should be avoided during pregnancy, particularly during the third trimester, as it may cause premature closure of the ductus arteriosus and other complications. It should not be used after 30 weeks of gestation.
- Breastfeeding: Meloxicam can pass into breast milk. While it can be used with caution during breastfeeding, monitoring of the infant is necessary. It’s generally recommended to avoid using meloxicam while breastfeeding if possible.
Drug Profile Summary
- Mechanism of Action: COX-2 inhibitor, reducing prostaglandin synthesis and inflammation.
- Side Effects: Common: Gastrointestinal issues, dizziness, headache, rash. Serious: Cardiovascular events, GI bleeding, hepatic/renal dysfunction.
- Contraindications: Hypersensitivity to NSAIDs, active peptic ulcer, severe heart/renal failure, pregnancy (3rd trimester).
- Drug Interactions: Other NSAIDs, anticoagulants, antihypertensives, corticosteroids, SSRIs/SNRIs, lithium, methotrexate, alcohol.
- Pregnancy & Breastfeeding: Avoid, especially in the third trimester. Use with caution during breastfeeding.
- Dosage: Adults: 7.5-15 mg/day. Children (JRA): 7.5 mg/day or 0.125 mg/kg/day up to 7.5 mg. Special adjustments for renal impairment and elderly.
- Monitoring Parameters: Blood pressure, renal function, liver function, signs of GI bleeding.
Popular Combinations
Meloxicam is often used as monotherapy. If needed, it can be combined with non-NSAID analgesics like acetaminophen for additional pain relief. However, combining meloxicam with other NSAIDs is generally avoided due to increased risk of side effects. Always evaluate the need for combination therapy and monitor for potential drug interactions.
Precautions
- General Precautions: Evaluate patients for cardiovascular, renal, and hepatic risk factors before starting meloxicam. Monitor for signs and symptoms of gastrointestinal bleeding.
- Specific Populations: Closely monitor pregnant women (if use is unavoidable), breastfeeding mothers, children, and the elderly for adverse events.
- Lifestyle Considerations: Advise patients to limit alcohol intake and avoid smoking.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Meloxicam?
A: Adults: 7.5-15 mg orally once daily. Children (JRA): 7.5 mg once daily or 0.125 mg/kg/day, up to 7.5 mg/day.
Q2: How does Meloxicam differ from other NSAIDs?
A: Meloxicam is a preferential COX-2 inhibitor, which may be associated with a lower risk of certain gastrointestinal side effects compared to some other NSAIDs.
Q3: What are the most serious side effects of Meloxicam?
A: Cardiovascular events (heart attack, stroke), gastrointestinal bleeding, renal and hepatic dysfunction.
Q4: Can Meloxicam be used during pregnancy?
A: Meloxicam should generally be avoided during pregnancy, especially after 20 weeks, due to risks to the fetus.
Q5: What are the main drug interactions with Meloxicam?
A: Other NSAIDs, anticoagulants, antihypertensives, corticosteroids, some antidepressants (SSRIs and SNRIs), lithium, methotrexate, and alcohol.
Q6: Can I take Meloxicam with other pain relievers?
A: Combining Meloxicam with other NSAIDs like ibuprofen or aspirin is not recommended due to increased risk of side effects. Consult a physician regarding the use of acetaminophen with meloxicam.
Q7: How long does it take for Meloxicam to work?
A: Pain relief may be experienced within a few hours, but it can take several days or weeks for the full anti-inflammatory effects to be seen.
Q8: How should Meloxicam be taken?
A: Meloxicam tablets or capsules should be swallowed whole with water, with or without food. The oral suspension should be measured carefully.
Q9: What should I do if I miss a dose of Meloxicam?
A: Take the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose and return to your regular dosing schedule. Do not double the dose.
Q10: Can Meloxicam be used long-term?
A: Long-term use of Meloxicam requires careful monitoring for potential side effects, especially cardiovascular, gastrointestinal, renal, and hepatic complications. Use the lowest effective dose for the shortest duration necessary.
