Chlorpheniramine Maleate + Diclofenac + Magnesium Trisilicate + Paracetamol

Usage

This combination medication is primarily prescribed for the temporary relief of symptoms associated with the common cold, flu, and allergies. It addresses symptoms like fever, headache, body aches, nasal congestion, runny nose, sneezing, watery eyes, and itchy eyes. Additionally, due to the presence of diclofenac, it can provide relief from pain associated with conditions like toothache, neck pain, or arthritic pain.

• Pharmacological Classification: This is a combination product containing drugs from different classifications:

  • Analgesic (Paracetamol, Diclofenac)
  • Antipyretic (Paracetamol, Diclofenac)
  • Antihistamine (Chlorpheniramine)
  • Non-Steroidal Anti-inflammatory Drug (NSAID) (Diclofenac)
  • Antacid (Magnesium Trisilicate)

• Mechanism of Action: This combination works through multiple pathways:

  • Paracetamol reduces fever and pain by inhibiting cyclooxygenase (COX) enzymes in the central nervous system, primarily COX-3, reducing prostaglandin synthesis.
  • Diclofenac is an NSAID that inhibits both COX-1 and COX-2 enzymes, further reducing pain and inflammation.
  • Chlorpheniramine is an antihistamine that blocks the action of histamine, relieving allergy symptoms.
  • Magnesium trisilicate acts as an antacid, neutralizing excess stomach acid and providing relief from heartburn and indigestion.

Alternate Names

• Cold Relief Tablets

• Brand Names:

  • Clodip Tablet
  • Dacron Plus Tablet
  • Dolopee Tablet
  • DPC Tablet
  • Geodic MR Tablet
  • Insta Relief Tablet
  • Labdic Tablet
  • Labdic Relief Tablet
  • Paindoz Tablet
  • Paingesic Tablet

How It Works

• Pharmacodynamics: The combination exerts its effects through the combined actions of its components. Diclofenac, by inhibiting COX-1 and COX-2, reduces inflammation and pain. Paracetamol primarily affects central COX enzymes, resulting in pain and fever reduction. Chlorpheniramine antagonizes histamine H1 receptors, reducing allergy symptoms. Magnesium trisilicate neutralizes gastric acid.

• Pharmacokinetics:

  • Absorption: All components are absorbed orally, though Diclofenac absorption can be affected by food.
  • Metabolism: Primarily hepatic metabolism, mainly through the CYP450 system, especially for Diclofenac and Chlorpheniramine. Paracetamol undergoes glucuronidation and sulfation.
  • Elimination: Primarily renal excretion for all components and their metabolites.

• Mode of Action:

  • Diclofenac and Paracetamol reduce prostaglandin synthesis.
  • Chlorpheniramine competitively inhibits histamine at H1 receptors.
  • Magnesium Trisilicate chemically neutralizes stomach acid.

• Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation:

  • Diclofenac and Paracetamol: COX-1, COX-2 (Diclofenac), and COX-3 (Paracetamol) enzyme inhibition.
  • Chlorpheniramine: Histamine H1 receptor antagonist.

• Elimination Pathways: Primarily renal excretion. Hepatic metabolism plays a significant role, especially for Diclofenac, via CYP enzymes.

Dosage

Standard Dosage

Adults:

The typical adult dose is one tablet containing Diclofenac 50mg, Paracetamol 500mg, Chlorpheniramine Maleate 4mg, and Magnesium Trisilicate 100mg, taken up to three times a day.

Children: Use in children is generally not recommended without careful consideration of benefit versus risk. Specific dosing guidelines for children vary with age and weight and should be determined by a physician.

Special Cases:

• Elderly Patients: Use with caution due to increased risk of adverse effects, especially gastrointestinal issues. Dose adjustments may be necessary.

• Patients with Renal Impairment: Caution is advised. Dose adjustments may be required based on the degree of impairment.

• Patients with Hepatic Dysfunction: Use with caution, as all components undergo hepatic metabolism. Dose adjustments may be needed.

• Patients with Comorbid Conditions: Careful consideration is necessary for patients with cardiovascular disease, diabetes, or other relevant conditions.

Clinical Use Cases

This combination is not typically used in clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its primary indication is symptomatic relief of common cold and flu symptoms.

Dosage Adjustments

Adjustments based on renal/hepatic function, age, and other conditions are recommended as determined by a physician.

Side Effects

Common Side Effects:

Drowsiness, dizziness, nausea, vomiting, stomach upset, dry mouth, blurred vision, constipation, loss of appetite.

Rare but Serious Side Effects: Allergic reactions (rash, itching, swelling), gastrointestinal bleeding, liver damage, kidney problems, blood pressure changes, heart problems.

Long-Term Effects: Chronic use of NSAIDs like Diclofenac can increase the risk of gastrointestinal problems. Prolonged use should be monitored.

Adverse Drug Reactions (ADR): Stevens-Johnson Syndrome (rare), toxic epidermal necrolysis (rare), severe allergic reactions.

Contraindications

• Hypersensitivity to any of the components.
• Active peptic ulcer.
• Severe liver or kidney disease.
• Asthma, urticaria, or acute rhinitis precipitated by NSAIDs.
• Third trimester of pregnancy.

Drug Interactions

• Other NSAIDs, anticoagulants, antihypertensives, diuretics, alcohol, and other CNS depressants.
• CYP450 interactions are possible, especially with Diclofenac.

Pregnancy and Breastfeeding

• Diclofenac is contraindicated in the third trimester of pregnancy. Use in other trimesters should be carefully evaluated.

• Chlorpheniramine and Paracetamol use during pregnancy should be under the guidance of a doctor.

• Limited information suggests that small amounts of Chlorpheniramine may be excreted in breast milk. It is recommended to consult a doctor regarding breastfeeding while taking this combination.

Drug Profile Summary

• Mechanism of Action: Multifaceted, addressing pain, fever, inflammation, allergy symptoms, and gastric acidity.

• Side Effects: Drowsiness, dizziness, gastrointestinal upset, rare but serious effects include organ damage and allergic reactions.

• Contraindications: Hypersensitivity, active peptic ulcer, severe liver/kidney disease, pregnancy (third trimester), specific allergies.

• Drug Interactions: NSAIDs, anticoagulants, antihypertensives, alcohol.

• Pregnancy & Breastfeeding: Diclofenac contraindicated in the third trimester; consult a doctor for use of other components.

• Dosage: Adult dose typically one tablet (specific composition above) three times daily. Adjustments needed for specific populations.

• Monitoring Parameters: Liver and kidney function, blood pressure.

Popular Combinations

This combination itself is a popular formulation. Magnesium Trisilicate is frequently included to address potential gastrointestinal side effects of Diclofenac.

Precautions

• General Precautions: Assess patient history for allergies, pre-existing conditions, and concomitant medications.

• Specific Populations:

  • Pregnant Women: Avoid in the third trimester. Consult doctor for other trimesters.
  • Breastfeeding Mothers: Consult a doctor.
  • Children & Elderly: Use with caution and dose adjustments.

• Lifestyle Considerations: Avoid alcohol and driving while taking this medication.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Chlorpheniramine Maleate + Diclofenac + Magnesium Trisilicate + Paracetamol?

A: The standard adult dose is one tablet containing 50mg Diclofenac, 500mg Paracetamol, 4mg Chlorpheniramine Maleate, and 100mg Magnesium Trisilicate, taken up to three times daily. Dosages should be adjusted for children, the elderly, and patients with renal or hepatic impairment.

Q2: What are the primary uses of this combination?

A: It’s mainly used for symptomatic relief from the common cold, flu, and allergies.

Q3: Can this combination be used during pregnancy?

A: Diclofenac is contraindicated in the third trimester. Consult a doctor regarding its use during other trimesters or for the other components.

Q4: What are the common side effects?

A: Drowsiness, dizziness, nausea, vomiting, dry mouth, and blurred vision are common.

Q5: Are there any serious side effects?

A: Yes, though rare, serious side effects can include liver or kidney problems, gastrointestinal bleeding, and allergic reactions.

Q6: Can this be taken with other medications?

A: It can interact with other NSAIDs, anticoagulants, antihypertensives, and alcohol. Consult a physician before combining with other medications.

Q7: What precautions should be taken with this medicine?

A: Avoid driving or operating heavy machinery due to potential drowsiness. Consult a doctor for dosage adjustments in elderly patients or those with liver or kidney problems.

Q8: How does magnesium trisilicate contribute to the formulation?

A: It acts as an antacid to reduce the risk of gastrointestinal side effects associated with diclofenac.

Q9: Is this combination suitable for children?

A: Use in children is generally not recommended without careful medical evaluation.

Q10: What should I do if I miss a dose?

A: If you miss a dose, take it as soon as you remember, unless it is close to the time for your next dose. Do not double the dose to catch up.