Usage
- This combination medication is primarily prescribed for the relief of pain and inflammation associated with various conditions like osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, muscle pain, tooth pain, bone and joint pain, headache, menstrual pain, ear pain, and fever. It also offers gastroprotective benefits.
- Pharmacological Classification: Non-steroidal anti-inflammatory drug (NSAID) + H2 receptor antagonist + Analgesic/Antipyretic.
- Mechanism of Action: Diclofenac and paracetamol reduce pain and inflammation by inhibiting cyclooxygenase (COX) enzymes, thus decreasing prostaglandin synthesis. Famotidine reduces stomach acid production by blocking histamine H2 receptors, mitigating potential gastrointestinal side effects caused by diclofenac.
Alternate Names
- No internationally recognized non-proprietary name exists for this specific combination. The components are referred to individually as Diclofenac, Famotidine, and Paracetamol (or Acetaminophen in some regions).
- Brand Names: While several brand names exist internationally depending on the region and specific formulation, it is important to refer to local formularies for accurate brand information. One example found is “Diclosef”.
How It Works
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Pharmacodynamics: Diclofenac inhibits COX-1 and COX-2 enzymes, reducing prostaglandin synthesis and thereby decreasing pain and inflammation. Paracetamol’s exact mechanism is not fully understood, but it is thought to inhibit COX enzymes, particularly a variant in the central nervous system, providing analgesic and antipyretic effects. Famotidine competitively inhibits histamine at H2 receptors of the gastric parietal cells, reducing gastric acid secretion.
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Pharmacokinetics:
- Diclofenac: Rapidly absorbed following oral administration, but subject to first-pass metabolism. Peak plasma concentration reached in 1-2 hours (can vary depending on formulation). Metabolized primarily in the liver by CYP2C9. Excreted mainly through urine (65%) and bile (35%).
- Paracetamol: Almost completely absorbed following oral administration. Peak plasma concentrations reached in 30-60 minutes. Metabolized primarily in the liver. Excreted in the urine mainly as glucuronide and sulfate conjugates.
- Famotidine: Incompletely absorbed following oral administration (40-50% bioavailability). Peak plasma concentration in 1-3 hours. Partially metabolized in the liver. Excreted primarily in the urine (65-70%) and feces (30-35%).
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Elimination Pathways: Diclofenac is eliminated primarily by hepatic metabolism followed by renal and biliary excretion. Paracetamol is mainly eliminated through hepatic metabolism followed by renal excretion. Famotidine is primarily eliminated unchanged through renal excretion, with some hepatic metabolism.
Dosage
Standard Dosage
Adults:
Specific dosing information for this particular combination product requires consultation with local formularies and product information. However, based on the individual components: Diclofenac (standard preparations): 25-50 mg orally 2-4 times daily, adjusted to individual response. Paracetamol: 325-1000 mg orally every 4-6 hours as needed, maximum 4000 mg/day. Famotidine: 20-40 mg orally once or twice daily.
Children:
The safety and efficacy of this combination have not been established in children, hence, use is generally not recommended. Dosage information for individual components in pediatric populations should be consulted in standard pediatric references.
Special Cases:
- Elderly Patients: Initiate therapy at the lowest effective dose. Close monitoring for adverse effects is essential.
- Patients with Renal Impairment: Dose adjustment of diclofenac and famotidine might be required. Individualized dosing based on renal function is recommended.
- Patients with Hepatic Dysfunction: Dose adjustment might be necessary for all three components, particularly diclofenac and paracetamol.
- Patients with Comorbid Conditions: Caution should be exercised in patients with cardiovascular disease, gastrointestinal ulcers, or bleeding disorders.
Clinical Use Cases
Due to the lack of specific clinical data for this fixed-dose combination in the provided contexts, it is advisable to consult specialists and refer to protocols for such settings. Individual components of this combination may have established uses within these contexts, hence reference to clinical guidelines focusing on those is recommended.
Dosage Adjustments
Dose adjustments should be made based on individual patient characteristics, including renal function, hepatic function, age, and concomitant medications.
Side Effects
Common Side Effects
Nausea, vomiting, stomach pain, diarrhea, dizziness, loss of appetite.
Rare but Serious Side Effects
Gastrointestinal bleeding, ulcers, hepatic dysfunction, renal impairment, allergic reactions, cardiovascular events.
Long-Term Effects
Chronic kidney disease, gastrointestinal issues.
Adverse Drug Reactions (ADR)
Anaphylaxis, Stevens-Johnson syndrome, toxic epidermal necrolysis, severe hepatotoxicity.
Contraindications
Hypersensitivity to any component of the medication, active peptic ulcer disease, severe hepatic impairment, severe renal impairment, aspirin triad (asthma, nasal polyps, and aspirin sensitivity), last trimester of pregnancy.
Drug Interactions
- Anticoagulants (warfarin, heparin), NSAIDs (aspirin, ibuprofen), corticosteroids, diuretics, lithium, methotrexate, and certain antidepressants.
- Alcohol, which might potentiate gastrointestinal side effects and increase the risk of hepatotoxicity.
Pregnancy and Breastfeeding
- Pregnancy: Contraindicated in the third trimester. Use in the first and second trimesters only if the potential benefit outweighs the risk. Diclofenac can cause premature closure of the ductus arteriosus in the fetus.
- Breastfeeding: Use with caution. Small amounts of the drugs may be excreted in breast milk. Diclofenac is generally considered compatible with breastfeeding, while famotidine is excreted in minimal amounts. Monitor the infant for any adverse reactions.
Drug Profile Summary
- Mechanism of Action: See “How It Works” Section.
- Side Effects: Nausea, vomiting, diarrhea, dizziness, gastrointestinal bleeding, hepatotoxicity, renal impairment.
- Contraindications: Hypersensitivity, active peptic ulcer, severe liver/kidney disease, third-trimester pregnancy.
- Drug Interactions: Anticoagulants, NSAIDs, corticosteroids.
- Pregnancy & Breastfeeding: Contraindicated in the third trimester. Use with caution during breastfeeding.
- Dosage: Refer to local formularies or product information for dosage specifics of this combination product.
- Monitoring Parameters: Renal function, liver function, blood pressure, complete blood count.
Popular Combinations
This specific combination (diclofenac + famotidine + paracetamol) is not widely considered a standard, “popular” combination in international clinical practice. However, combinations including two of the components are frequently used (e.g. diclofenac + paracetamol, diclofenac + famotidine). Physicians may choose to prescribe the three components separately based on the patient’s specific needs.
Precautions
- General Precautions: Assess renal and hepatic function before starting therapy. Monitor for signs of gastrointestinal bleeding.
- Specific Populations: See “Dosage” -> “Special Cases”.
- Lifestyle Considerations: Avoid alcohol consumption.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diclofenac + Famotidine + Paracetamol?
A: The recommended dosage needs to be verified via local formularies and product information. General guidance is to use the lowest effective dose for the shortest duration.
Q2: Can this combination be used in children?
A: The safety and efficacy in children have not been established. Generally, it is not recommended.
Q3: Is it safe to take this combination during pregnancy?
A: It is contraindicated in the third trimester. Consult a physician before use during the first and second trimesters.
Q4: What are the potential drug interactions?
A: Potential interactions include anticoagulants (warfarin, heparin), other NSAIDs, corticosteroids, and diuretics.
Q5: Are there any dietary restrictions while taking this medication?
A: Alcohol should be avoided due to the increased risk of gastrointestinal side effects and hepatotoxicity.
Q6: What are the monitoring parameters for patients on this combination?
A: Renal function, liver function, blood pressure, and signs of gastrointestinal bleeding should be monitored.
Q7: Can this combination be used in patients with a history of peptic ulcers?
A: It is generally contraindicated in patients with a history of active peptic ulcers.
Q8: What should be done in case of an overdose?
A: Seek immediate medical attention. Supportive care and symptomatic treatment are usually indicated.
Q9: What is the difference between diclofenac potassium and diclofenac sodium?
A: Diclofenac potassium and diclofenac sodium are different salt forms of the same drug. They have similar efficacy and safety profiles, but diclofenac potassium may have a slightly faster onset of action.
