Usage
- This combination medication is primarily prescribed for the relief of musculoskeletal pain and spasms. It is often associated with conditions such as low back pain, sprains, strains, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and post-operative pain. It is also used to treat headache, joint pain, body pain, muscle strain, viral fever, and joint stiffness.
- Pharmacological Classification: This combination includes a Nonsteroidal anti-inflammatory drug (NSAID) - Diclofenac, an analgesic and antipyretic - Paracetamol, a muscle relaxant - Chlorzoxazone, and an H2-receptor antagonist (antacid) - Famotidine.
- Mechanism of Action: Diclofenac inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis (mediators of pain and inflammation). Paracetamol acts centrally on the brain’s pain and temperature-regulating centers. Chlorzoxazone acts centrally on the spinal cord and subcortical areas of the brain to inhibit reflexes that cause muscle spasms. Famotidine reduces gastric acid secretion, protecting the stomach lining from potential irritation caused by Diclofenac.
Alternate Names
This combination medication does not have an international nonproprietary name (INN). It is marketed under various brand names such as Dicwoz MR and Andic-MR. Other brand names may exist depending on the manufacturer.
How It Works
- Pharmacodynamics: Diclofenac reduces pain and inflammation by inhibiting COX-1 and COX-2 enzymes, thereby suppressing prostaglandin synthesis. Paracetamol is believed to inhibit COX enzymes primarily in the central nervous system, with minimal peripheral effects, and has central effects on serotonergic pathways. Chlorzoxazone depresses polysynaptic reflex arcs in the spinal cord and subcortical areas of the brain, leading to muscle relaxation. Famotidine competitively inhibits the action of histamine at the H2 receptors of the parietal cells, reducing gastric acid secretion.
- Pharmacokinetics:
- Diclofenac is well-absorbed orally but undergoes first-pass metabolism. Peak plasma levels are reached in 1-2 hours. It is metabolized in the liver and primarily eliminated through the kidneys.
- Paracetamol is rapidly absorbed orally, reaching peak plasma levels in 30-60 minutes. It is metabolized by the liver, primarily by glucuronidation and sulfation, with a small fraction undergoing CYP450-mediated oxidation to a reactive metabolite. This reactive metabolite is detoxified by conjugation with glutathione and excreted in the urine.
- Chlorzoxazone is readily absorbed from the gastrointestinal tract. Peak plasma concentration occurs in 1-2 hours. It undergoes hepatic metabolism, primarily by CYP2E1, and the metabolites are excreted in the urine.
- Famotidine is incompletely absorbed orally. Peak plasma levels occur in 1-3 hours. It undergoes minimal metabolism and is primarily eliminated unchanged in the urine, with a small amount excreted in the feces.
Dosage
The dosage of this combination medication is not standardized and varies depending on the specific product and the patient’s condition. Always adhere to the prescribing physician’s instructions or the product label. One example of dosage and strength found was: Diclofenac sodium 50 mg, paracetamol 325 mg, and chlorzoxazone 500 mg per tablet. One tablet to be taken three times a day.
Standard Dosage
Adults: One example found was 1 tablet three times a day. However, this may vary. The maximum recommended daily dose of diclofenac is 150 mg. The maximum recommended dose of paracetamol is 4 grams. The maximum dose of Chlorzoxazone is 3,000mg.
Children: This medication is generally not recommended for children under 12, as safety and efficacy have not been established in pediatric populations.
Special Cases:
- Elderly Patients: Dosage adjustments may be needed due to age-related decline in renal and hepatic function. Start with lower doses and monitor closely.
- Patients with Renal Impairment: Dose reduction may be necessary based on the degree of impairment. Monitor renal function.
- Patients with Hepatic Dysfunction: Exercise caution and adjust dosage as needed based on liver function. Close monitoring is necessary.
- Patients with Comorbid Conditions: Consider individual patient factors, such as cardiovascular disease, diabetes, and other relevant conditions, when determining the appropriate dosage and monitoring.
Clinical Use Cases
Dosage recommendations for specific medical settings (Intubation, Surgical Procedures, Mechanical Ventilation, Intensive Care Unit (ICU) Use, and Emergency Situations) are not standardized and should be determined by the treating physician based on the individual patient’s needs.
Dosage Adjustments
Dose modification may be necessary for renal/hepatic dysfunction, metabolic disorders, or genetic polymorphisms affecting drug metabolism. Closely monitor patients for adverse effects and adjust the dosage as needed.
Side Effects
Common Side Effects
Nausea, vomiting, stomach pain, loss of appetite, dizziness, drowsiness, diarrhea, heartburn, constipation, headache, mild skin rash, tiredness, and upset stomach.
Rare but Serious Side Effects
Allergic reactions (difficulty breathing, swelling of face, mouth, and throat, skin rash, itching), gastrointestinal bleeding, liver damage (jaundice, abdominal pain, dark urine), cardiovascular events (chest pain, shortness of breath), and Stevens-Johnson syndrome.
Long-Term Effects
Long-term use of NSAIDs like diclofenac can increase the risk of gastrointestinal bleeding, ulcers, and cardiovascular complications. Chronic use of paracetamol, especially at high doses, can lead to liver damage.
Adverse Drug Reactions (ADR)
Clinically significant ADRs requiring immediate intervention include severe allergic reactions, gastrointestinal bleeding, signs of liver damage (jaundice, abdominal pain, dark urine), symptoms suggesting heart attack or stroke (chest pain, shortness of breath, weakness on one side of the body), blood dyscrasias (unusual bleeding or bruising), and severe skin reactions.
Contraindications
- Hypersensitivity to any component of the medication
- Active peptic ulcer or gastrointestinal bleeding
- Severe hepatic or renal impairment
- Aspirin-induced asthma or urticaria
- Last trimester of pregnancy
- Heart failure
- History of GI bleeding or perforation related to previous NSAID therapy
- Porphyria
- Intolerance to Chlorzoxazone.
Drug Interactions
This combination can interact with many drugs, including anticoagulants, antihypertensives, other NSAIDs, methotrexate, lithium, digoxin, some antibiotics, antidepressants (duloxetine), antipsychotics (lithium), cardiac glycosides (digoxin), anti-rheumatoid drugs (methotrexate), bronchodilators (albuterol), vitamin B12, potassium-sparing diuretics, and alcohol. It is always best to check for interactions with any medication or supplement before use.
Pregnancy and Breastfeeding
This combination is not recommended during pregnancy, especially in the third trimester, due to potential risks to the fetus. Caution is advised during breastfeeding. It is essential to consult with a doctor to evaluate the risks and benefits before using this medication during pregnancy or breastfeeding. The doctor will prescribe only if the benefits outweigh the risks.
Drug Profile Summary
- Mechanism of Action: See “How It Works” section
- Side Effects: See “Side Effects” section
- Contraindications: See “Contraindications” section
- Drug Interactions: See “Drug Interactions” section
- Pregnancy & Breastfeeding: Not recommended during pregnancy, especially the third trimester. Caution during breastfeeding.
- Dosage: Dosage is not standardized and varies depending on individual products and clinical needs. Consult the prescribing physician or the product label for specific instructions.
- Monitoring Parameters: Liver function tests, renal function tests, complete blood count, blood pressure.
Popular Combinations
The combination of diclofenac, paracetamol, chlorzoxazone, and famotidine is itself a common combination often prescribed for musculoskeletal pain and spasms.
Precautions
Prescreen patients for allergies, metabolic disorders, and organ dysfunction. Review patient medication history carefully to avoid harmful drug interactions. Caution should be exercised in patients with heart disease, kidney disease, or liver problems. Exercise caution when prescribing to elderly patients. This medication is typically not recommended for children.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Chlorzoxazone + Diclofenac + Famotidine + Paracetamol?
A: The dosage is not standardized. Always follow the dosage instructions on the product label or as directed by your physician. An example of a standard dosage would be 1 tablet three times daily for adults.
Q2: What are the common side effects?
A: Common side effects may include nausea, dizziness, drowsiness, constipation, diarrhea, stomach upset, and mild skin rash.
Q3: Is this combination safe to use during pregnancy?
A: It is not recommended during pregnancy, especially in the third trimester, due to potential risks to the fetus.
Q4: Are there any serious side effects I should be aware of?
A: Yes, rare but serious side effects can include allergic reactions, gastrointestinal bleeding, liver damage, cardiovascular events (such as heart attack and stroke), and blood dyscrasias. Seek immediate medical attention if any of these occur.
Q5: Can this combination be used during breastfeeding?
A: Caution is advised during breastfeeding. Consult your doctor before use.
Q6: What conditions is this medication used to treat?
A: It is primarily used to treat musculoskeletal pain and spasms associated with conditions such as low back pain, sprains, strains, osteoarthritis, and post-operative pain.
Q7: Are there any medications I should avoid while taking this combination?
A: Yes, avoid alcohol and other medications that can interact with this combination, such as anticoagulants, antihypertensives, other NSAIDs, and certain antibiotics. Consult your doctor for a complete list of interacting medications.
Q8: Can I operate machinery or drive while taking this medication?
A: Use caution, as this medication can cause dizziness and drowsiness. It is best to avoid driving or operating machinery if such effects occur.
Q9: What should I do if I miss a dose?
A: If you miss a dose, take it as soon as you remember. However, if it is close to the time of your next dose, skip the missed dose and take the next dose as scheduled. Do not double the dose.
Q10: How should this medication be stored?
A: Store this medication at room temperature away from moisture, heat, and direct light. Keep it out of the reach of children.
