Usage
Aceclofenac + Misoprostol is prescribed for the relief of pain and inflammation in patients with osteoarthritis or rheumatoid arthritis who are at high risk of developing NSAID-induced gastric or duodenal ulcers.
Pharmacological Classification:
- Aceclofenac: Non-Steroidal Anti-Inflammatory Drug (NSAID)
- Misoprostol: Prostaglandin Analog
Mechanism of Action: Aceclofenac inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, thereby decreasing inflammation and pain. Misoprostol, a synthetic prostaglandin E1 analog, protects the gastric mucosa by replacing depleted prostaglandins, reducing gastric acid secretion, and increasing mucus and bicarbonate production.
Alternate Names
While Aceclofenac + Misoprostol doesn’t have a universally recognized alternate name, the combination is often referred to by its components. Brand names vary by region. Some popular brand names include Arthrotec and Cytonac ER.
How It Works
Pharmacodynamics: Aceclofenac exerts analgesic and anti-inflammatory effects by inhibiting COX-1 and COX-2 enzymes. Misoprostol acts as a prostaglandin E1 analog, binding to prostaglandin receptors on parietal cells in the stomach, decreasing acid secretion. It also enhances mucosal defense by stimulating mucus and bicarbonate production.
Pharmacokinetics: Aceclofenac is well-absorbed orally, reaching peak plasma concentrations within 1-3 hours. It undergoes hepatic metabolism, primarily by CYP2C9, and is excreted mainly in urine. Misoprostol is rapidly absorbed orally, metabolized in the liver to its active metabolite, misoprostol acid, and is eliminated primarily in urine.
Elimination Pathways: Aceclofenac is primarily excreted via the kidneys, following hepatic metabolism, mainly by CYP2C9 enzymes. Misoprostol is eliminated via renal excretion following its metabolism in the liver to misoprostol acid.
Dosage
Standard Dosage
Adults:
For osteoarthritis and rheumatoid arthritis: One tablet of Aceclofenac 100mg + Misoprostol 200mcg twice daily, typically taken with food.
Children:
Use in children under 18 years of age is not recommended due to the lack of clinical safety data. Pediatric dosing has not been established.
Special Cases:
- Elderly Patients: Start with the lowest effective dose and monitor closely for adverse effects.
- Patients with Renal Impairment: Exercise caution, as dose adjustments might be necessary in cases of moderate to severe renal impairment. Start at a reduced dose and monitor renal function.
- Patients with Hepatic Dysfunction: Start with a reduced dose, usually Aceclofenac 100 mg daily, and monitor liver function regularly.
- Patients with Comorbid Conditions: Consider existing cardiovascular, gastrointestinal, or other relevant conditions when prescribing and adjust dosage or medication choice as needed.
Clinical Use Cases
The use of Aceclofenac + Misoprostol is not indicated for intubation, surgical procedures, mechanical ventilation, intensive care unit use, or emergency situations. The combination is specifically indicated for chronic conditions like osteoarthritis and rheumatoid arthritis in patients at high risk of gastrointestinal ulceration.
Dosage Adjustments
Dosage adjustments may be necessary based on patient-specific factors, such as renal or hepatic impairment, age, and the presence of other medical conditions.
Side Effects
Common Side Effects:
- Diarrhea
- Abdominal pain
- Nausea
- Indigestion
- Headache
- Dizziness
Rare but Serious Side Effects:
- Gastrointestinal bleeding or perforation
- Severe allergic reactions (e.g., anaphylaxis, angioedema)
- Stevens-Johnson syndrome
Long-Term Effects:
Long-term use of NSAIDs, including aceclofenac, can increase the risk of cardiovascular events like heart attack and stroke. Long-term use of misoprostol can potentially lead to dependence.
Adverse Drug Reactions (ADR):
Clinically significant ADRs include gastrointestinal bleeding, ulcer perforation, severe allergic reactions, and acute renal failure.
Contraindications
- Hypersensitivity to aceclofenac or misoprostol
- Active or history of recurrent peptic ulcer/gastrointestinal bleeding
- Active bleeding or bleeding diathesis
- Severe hepatic or renal failure
- Pregnancy
- Women of childbearing potential not using effective contraception
Drug Interactions
- Anticoagulants (e.g., warfarin): Increased risk of bleeding
- Corticosteroids: Increased risk of gastrointestinal ulceration
- Antihypertensives: Possible reduced antihypertensive effect
- Other NSAIDs (including Aspirin): Increased risk of adverse effects.
- Methotrexate: Increased methotrexate toxicity
Pregnancy and Breastfeeding
Aceclofenac + Misoprostol is contraindicated in pregnancy and breastfeeding. Misoprostol can cause uterine contractions and induce miscarriage or premature labor.
Drug Profile Summary
- Mechanism of Action: Aceclofenac: COX inhibitor, reducing inflammation and pain; Misoprostol: Prostaglandin analog, protects gastric mucosa.
- Side Effects: Diarrhea, abdominal pain, nausea, headache, dizziness.
- Contraindications: Pregnancy, breastfeeding, active or history of peptic ulcer disease, severe hepatic or renal impairment.
- Drug Interactions: Anticoagulants, corticosteroids, other NSAIDs.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Adults: Aceclofenac 100mg + Misoprostol 200mcg twice daily with food.
- Monitoring Parameters: Gastrointestinal symptoms, renal and hepatic function.
Popular Combinations
Aceclofenac + Misoprostol is itself a popular combination to provide pain relief while minimizing the risk of NSAID-induced gastrointestinal ulcers.
Precautions
- General Precautions: Monitor for gastrointestinal bleeding, renal and hepatic function, and cardiovascular events.
- Specific Populations: Pregnant women, breastfeeding mothers, children, and elderly require special caution.
- Lifestyle Considerations: Limit alcohol consumption and avoid driving if dizziness or drowsiness occurs.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Aceclofenac + Misoprostol?
A: The recommended adult dose is Aceclofenac 100mg + Misoprostol 200mcg twice daily, taken with food.
Q2: Can Aceclofenac + Misoprostol be used during pregnancy?
A: No, it is contraindicated in pregnancy as misoprostol can induce uterine contractions and cause miscarriage or premature labor.
Q3: What are the common side effects?
A: Common side effects include diarrhea, abdominal pain, nausea, indigestion, headache, and dizziness.
Q4: How does Aceclofenac + Misoprostol work?
A: Aceclofenac reduces pain and inflammation by inhibiting COX enzymes. Misoprostol protects the stomach lining by reducing gastric acid secretion and enhancing mucus production.
Q5: What are the contraindications for this medication?
A: Contraindications include hypersensitivity, active peptic ulcer disease, severe liver or kidney impairment, pregnancy, and breastfeeding.
Q6: Are there any drug interactions I should be aware of?
A: Yes, Aceclofenac + Misoprostol interacts with anticoagulants, corticosteroids, other NSAIDs and certain other medications. It is important to disclose all medications you are taking to your prescribing physician.
Q7: Can this medicine be taken with alcohol?
A: It’s best to avoid alcohol as it can increase the risk of stomach upset and gastrointestinal bleeding.
Q8: What should I do if I experience severe or persistent side effects?
A: Contact your doctor immediately if you experience any severe or persistent side effects, especially gastrointestinal bleeding or severe allergic reactions.
Q9: Is there any age restriction for the use of Aceclofenac + Misoprostol?
A: It is not recommended for use in patients under 18 years of age due to the lack of clinical data on its safety and effectiveness.
Q10: Are there any precautions to take while taking this medicine?
A: Yes, patients with pre-existing conditions like renal or liver problems, heart disease, high blood pressure, or asthma should be cautious when taking this medication and discuss these conditions with their doctor beforehand. Close monitoring of renal and hepatic function is recommended, especially in elderly patients.
