Usage
- Aceclofenac is prescribed for the relief of pain and inflammation in osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. It is also used for other painful conditions such as dental pain, low back pain, and periarthritis.
- Pharmacological Classification: Non-Steroidal Anti-Inflammatory Drug (NSAID).
- Mechanism of Action: Aceclofenac inhibits cyclooxygenase (COX) enzymes, primarily COX-2, which are responsible for the production of prostaglandins. Prostaglandins mediate inflammation, pain, and fever. By inhibiting COX enzymes, aceclofenac reduces prostaglandin synthesis, thus alleviating these symptoms.
Alternate Names
- International Nonproprietary Name (INN): Aceclofenac
- No significant regional variations in the name exist.
- Brand Names: Dolowin, Zerodol, Valk, Aclonac, etc. (Brand names can vary by region).
How It Works
- Pharmacodynamics: Aceclofenac exerts its analgesic and anti-inflammatory effects through the inhibition of COX enzymes, predominantly COX-2. This leads to reduced prostaglandin synthesis.
- Pharmacokinetics:
- Absorption: Aceclofenac is rapidly and completely absorbed after oral administration. Food intake can slightly delay the absorption rate but does not affect the extent of absorption.
- Metabolism: Aceclofenac undergoes hepatic metabolism, primarily via CYP2C9 enzymes. The main metabolite is 4’-hydroxyaceclofenac.
- Elimination: Aceclofenac is eliminated primarily through urine, with a small portion excreted in bile.
- Mode of Action: Aceclofenac binds to COX enzymes, particularly COX-2, and prevents the conversion of arachidonic acid to prostaglandin H2, a precursor for various pro-inflammatory prostaglandins.
- Receptor Binding/Enzyme Inhibition: Aceclofenac primarily acts through COX-2 enzyme inhibition.
- Elimination Pathways: Aceclofenac is mainly eliminated through renal excretion (urine), with minor biliary excretion. Metabolism occurs in the liver via CYP2C9 enzymes.
Dosage
Standard Dosage
Adults:
- 100 mg twice daily, one tablet in the morning and one in the evening.
- The maximum recommended dose is 200 mg/day.
Children:
- Not recommended for use in children under 18 years of age due to lack of clinical data.
Special Cases:
- Elderly Patients: Start with the lowest effective dose and monitor closely for adverse reactions. Dose adjustments might be needed based on renal function.
- Patients with Renal Impairment: Caution should be exercised in patients with mild renal impairment. Aceclofenac is contraindicated in severe renal impairment.
- Patients with Hepatic Dysfunction: Reduce the initial dose to 100 mg daily in mild to moderate hepatic impairment. Aceclofenac is contraindicated in severe hepatic impairment.
- Patients with Comorbid Conditions: Caution should be exercised in patients with cardiovascular disease, hypertension, or diabetes. Monitor these patients closely.
Clinical Use Cases
- Aceclofenac is not typically used in clinical settings like intubation, surgical procedures, mechanical ventilation, ICU, or emergency situations. It’s primarily used for chronic pain management in outpatient settings.
Dosage Adjustments
- Dose adjustments might be needed in elderly patients, those with renal or hepatic impairment, and those with certain comorbid conditions.
Side Effects
Common Side Effects
- Gastrointestinal discomfort (dyspepsia, nausea, diarrhea, abdominal pain, constipation, flatulence)
- Headache, dizziness, drowsiness
- Skin rash, itching
Rare but Serious Side Effects
- Gastrointestinal bleeding or perforation
- Allergic reactions (anaphylaxis, angioedema)
- Stevens-Johnson syndrome, toxic epidermal necrolysis
- Hepatic or renal dysfunction
- Cardiovascular events (myocardial infarction, stroke)
Long-Term Effects
- Chronic use can potentially lead to gastrointestinal issues (ulcers, bleeding), renal damage, and cardiovascular complications.
Adverse Drug Reactions (ADR)
- Severe allergic reactions, gastrointestinal bleeding, and acute renal failure require immediate medical attention.
Contraindications
- Hypersensitivity to aceclofenac or any other NSAIDs
- Active peptic ulcer or history of recurrent peptic ulcer/hemorrhage
- Severe heart failure, hepatic failure, or renal failure
- History of gastrointestinal bleeding or perforation related to previous NSAID therapy
- Active bleeding or bleeding disorders
- Third trimester of pregnancy
- Patients undergoing Coronary Artery Bypass Graft (CABG) surgery
Drug Interactions
- Other NSAIDs: Increased risk of gastrointestinal side effects
- Anticoagulants (e.g., warfarin): Increased risk of bleeding
- Antihypertensives and diuretics: Reduced effectiveness of these drugs
- Corticosteroids: Increased risk of gastrointestinal ulcers and bleeding
- Methotrexate: Increased methotrexate levels and toxicity
- Lithium and digoxin: Increased levels of these drugs
- Oral antidiabetic agents: Enhanced hypoglycemic effect
- Alcohol: Increased risk of gastrointestinal bleeding
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Contraindicated in the third trimester. Use with caution in the first and second trimesters only if clearly necessary and at the lowest effective dose for the shortest duration.
- Fetal Risks: Potential for miscarriage, cardiac malformation, and gastroschisis in early pregnancy. Premature closure of ductus arteriosus and pulmonary hypertension in the third trimester.
- Breastfeeding: Aceclofenac is not recommended during breastfeeding as it may pass into breast milk.
Drug Profile Summary
- Mechanism of Action: COX inhibitor, predominantly COX-2.
- Side Effects: GI discomfort, headache, dizziness, skin rash; rarely, GI bleeding, allergic reactions, renal/hepatic dysfunction.
- Contraindications: Hypersensitivity, peptic ulcer, severe heart/liver/kidney failure, GI bleeding history, pregnancy (3rd trimester).
- Drug Interactions: Other NSAIDs, anticoagulants, antihypertensives, corticosteroids, methotrexate, lithium, digoxin.
- Pregnancy & Breastfeeding: Contraindicated in 3rd trimester, caution in 1st and 2nd trimesters; not recommended while breastfeeding.
- Dosage: 100 mg twice daily (max 200 mg/day); adjustments needed for elderly, renal/hepatic impairment.
- Monitoring Parameters: Renal and liver function, blood pressure, signs of GI bleeding.
Popular Combinations
- Aceclofenac is sometimes combined with paracetamol (as in Zerodol-SP) or with serratiopeptidase for enhanced pain relief.
Precautions
- General Precautions: Assess for allergies, renal/hepatic function, and cardiovascular risk factors.
- Specific Populations: Monitor elderly patients and those with renal or hepatic impairment closely. Avoid use in the third trimester of pregnancy and use with caution in the first and second trimesters only if clearly necessary. Not recommended during breastfeeding. Not recommended for use in children under 18 years.
- Lifestyle Considerations: Limit alcohol intake to minimize GI risks.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Aceclofenac?
A: The standard adult dose is 100 mg twice daily. Adjustments may be necessary for the elderly and those with renal or hepatic impairment.
Q2: Can Aceclofenac be used in children?
A: Aceclofenac is not recommended for children under 18 years due to insufficient safety and efficacy data.
Q3: What are the common side effects of Aceclofenac?
A: Common side effects include gastrointestinal discomfort (nausea, dyspepsia, diarrhea), headache, and skin rash.
Q4: Can Aceclofenac be taken with other NSAIDs?
A: Combining Aceclofenac with other NSAIDs increases the risk of gastrointestinal adverse effects and is generally not recommended.
Q5: What are the contraindications for Aceclofenac?
A: Aceclofenac is contraindicated in patients with hypersensitivity to NSAIDs, active peptic ulcer disease, severe heart/liver/kidney failure, and during the third trimester of pregnancy.
Q6: How should Aceclofenac be administered?
A: Aceclofenac should be taken orally with food or after meals to minimize gastrointestinal irritation.
Q7: Does Aceclofenac interact with warfarin?
A: Yes, Aceclofenac can interact with warfarin, increasing the risk of bleeding. Close monitoring of INR is necessary when these drugs are co-administered.
Q8: What should patients be monitored for while taking Aceclofenac?
A: Patients should be monitored for signs of gastrointestinal bleeding, changes in renal and liver function, and any allergic reactions. Blood pressure should also be monitored, particularly in patients with pre-existing hypertension.
Q9: Can Aceclofenac be used during pregnancy?
A: Aceclofenac is contraindicated during the third trimester. Use during the first and second trimesters should be restricted to situations where the benefits outweigh the risks and for the shortest duration possible at the lowest effective dose.
Q10: Is Aceclofenac safe to use while breastfeeding?
A: Aceclofenac is not recommended during breastfeeding. It may pass into breast milk and potentially affect the nursing infant.
