Usage
This combination medication is prescribed for the management of pain and inflammation associated with various conditions, including:
- Rheumatoid arthritis
- Osteoarthritis
- Low back pain
- Periarthritis of the shoulder
- Cervicobrachial syndrome
- Postoperative pain
- Post-trauma pain
- Post-dental extraction pain
Pharmacological Classification:
- Zaltoprofen: Non-steroidal anti-inflammatory drug (NSAID)
- Paracetamol: Analgesic and antipyretic
Mechanism of Action:
Zaltoprofen inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, thereby mitigating pain and inflammation. Paracetamol’s mechanism is not fully understood, but it is thought to inhibit prostaglandin synthesis in the central nervous system, providing analgesic and antipyretic effects. The combination provides synergistic pain relief.
Alternate Names
Zaltoprofen + Paracetamol is marketed under various brand names such as Zott P, ZALTOP-P, REDUCIN-A, and TROPOZAL P.
How It Works
Pharmacodynamics:
Zaltoprofen exerts its anti-inflammatory and analgesic effects primarily through the inhibition of COX enzymes. This inhibition leads to a decrease in prostaglandin production, which plays a key role in inflammation and pain signaling. Paracetamol’s mechanism of action is not fully elucidated but involves inhibition of COX enzymes, predominantly in the CNS. It also has antipyretic effects by acting on the hypothalamic heat-regulating center.
Pharmacokinetics:
- Absorption: Both drugs are rapidly and almost completely absorbed from the gastrointestinal tract. Zaltoprofen’s absorption is enhanced when taken with food.
- Metabolism: Zaltoprofen is primarily metabolized in the liver by CYP2C9 and UGT2B7 enzymes. Paracetamol is metabolized in the liver via glucuronidation, sulfation, and oxidation pathways.
- Elimination: Zaltoprofen metabolites are primarily excreted in urine and bile. Paracetamol is primarily excreted in urine as conjugated metabolites.
Mode of Action:
Zaltoprofen binds to and inhibits COX enzymes, reducing prostaglandin synthesis at peripheral inflammation sites. Paracetamol’s action may involve central inhibition of COX and additional mechanisms not fully characterized.
Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation:
Zaltoprofen inhibits COX-1 and COX-2 enzymes. Paracetamol’s mechanism is less clear but possibly involves COX inhibition and other pathways.
Elimination Pathways:
Zaltoprofen is eliminated via hepatic metabolism and renal excretion. Paracetamol undergoes hepatic metabolism and subsequent renal elimination.
Dosage
Standard Dosage
Adults:
One tablet three times a day. Each tablet typically contains 80mg Zaltoprofen and 325mg Paracetamol. The maximum daily dose of Paracetamol should not exceed 4000mg.
Children:
The safety and efficacy haven’t been established in children under 18. Use with extreme caution and under strict medical supervision if deemed necessary by a physician. Pediatric dosages should be adjusted based on weight and age.
Special Cases:
- Elderly Patients: Administer with caution due to age-related decline in renal and hepatic function. Lower initial doses and close monitoring are advisable.
- Patients with Renal Impairment: Exercise caution. Dosage adjustments might be necessary depending on the degree of impairment. Close monitoring of renal function is crucial.
- Patients with Hepatic Dysfunction: Use with caution. Dosage adjustments might be necessary depending on the degree of impairment. Close monitoring of liver function is recommended.
- Patients with Comorbid Conditions: Consider comorbidities such as diabetes, cardiovascular disease, and gastrointestinal disorders. Dosage adjustments or closer monitoring may be required.
Clinical Use Cases
Specific dosage recommendations for clinical use cases like Intubation, Surgical Procedures, Mechanical Ventilation, ICU Use, and Emergency Situations are not explicitly defined for this combination. These should be determined by the attending physician based on individual patient needs and specific circumstances.
Dosage Adjustments
Dose modifications may be necessary based on patient-specific factors such as renal or hepatic dysfunction, metabolic disorders, or genetic polymorphisms that affect drug metabolism.
Side Effects
Common Side Effects
Nausea, drowsiness, dizziness, headache, gastrointestinal discomfort (stomach pain, diarrhea, heartburn).
Rare but Serious Side Effects
Gastrointestinal bleeding, peptic ulcers, severe allergic reactions (anaphylaxis), liver damage, kidney dysfunction, blood disorders (leukopenia, thrombocytopenia, anemia), cardiac arrhythmias, pancreatitis, hypersensitivity reactions (rashes, itching, swelling).
Long-Term Effects
Chronic kidney disease, gastrointestinal issues.
Adverse Drug Reactions (ADR)
Anaphylaxis, Stevens-Johnson syndrome, toxic epidermal necrolysis, hepatotoxicity.
Contraindications
- Hypersensitivity to Zaltoprofen, Paracetamol, or any component of the formulation.
- Active peptic ulcer or gastrointestinal bleeding.
- History of peptic ulcer disease or GI bleeding associated with NSAID use.
- Severe blood disorders.
- Severe liver impairment.
- Severe renal impairment.
- Severe heart failure or cardiac dysfunction.
- Ulcerative colitis or Crohn’s disease.
- Aspirin-induced asthma or allergic reactions to NSAIDs.
Drug Interactions
- Anticoagulants (e.g., warfarin): Increased risk of bleeding.
- Other NSAIDs: Increased risk of gastrointestinal side effects.
- Methotrexate: Increased methotrexate toxicity.
- Lithium: Increased lithium levels.
- Alcohol: Increased risk of liver damage.
- Quinolone antibiotics (e.g., ciprofloxacin, levofloxacin): Increased risk of seizures.
- Sulfonylurea antidiabetic agents: Increased risk of hypoglycemia.
Pregnancy and Breastfeeding
Use with caution during pregnancy and breastfeeding. Consult a physician to weigh the benefits and risks. Paracetamol is generally considered safe during pregnancy at recommended doses, but Zaltoprofen should be avoided, especially in the third trimester. Both drugs are excreted in breast milk, and their use during breastfeeding should be carefully evaluated.
Drug Profile Summary
- Mechanism of Action: Zaltoprofen inhibits COX enzymes, reducing prostaglandin synthesis. Paracetamol inhibits COX, primarily in the CNS, providing analgesia and antipyresis.
- Side Effects: Nausea, drowsiness, dizziness, headache, GI discomfort; rarely GI bleeding, ulcers, liver/kidney dysfunction.
- Contraindications: Hypersensitivity, active peptic ulcer, severe blood/liver/kidney disease, heart failure, IBD, aspirin-induced asthma.
- Drug Interactions: Anticoagulants, NSAIDs, methotrexate, lithium, alcohol, quinolones, sulfonylureas.
- Pregnancy & Breastfeeding: Use with caution; consult a physician.
- Dosage: Adults: One tablet (80mg zaltoprofen/325mg paracetamol) thrice daily; maximum 4000mg paracetamol/day. Not established for children under 18.
- Monitoring Parameters: Liver and kidney function tests, complete blood count, signs of GI bleeding.
Popular Combinations
This drug is not typically combined with other medications for synergistic effects, as the combination itself provides enhanced pain relief. Co-administration with other analgesics or NSAIDs should be done with caution to avoid potential adverse effects.
Precautions
- Pre-existing medical conditions like liver/kidney disease, heart disease, GI disorders should be evaluated before prescribing.
- In pregnant or breastfeeding women, careful risk-benefit assessment is necessary.
- Age-specific precautions are essential for children and the elderly.
- Alcohol should be avoided due to the increased risk of liver damage and GI bleeding.
- Smoking might exacerbate GI side effects.
- Monitor patients for any adverse effects.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Paracetamol + Zaltoprofen?
A: Adults: One tablet (80mg zaltoprofen/325mg paracetamol) three times a day. Maximum 4000mg of paracetamol daily. Pediatric use: Safety and efficacy not established. Use only under strict supervision with dose adjustments.
Q2: Can this combination be used in children?
A: The safety and efficacy in children under 18 years have not been established. Use with caution and strict medical supervision.
Q3: What are the common side effects?
A: Nausea, drowsiness, dizziness, headache, and gastrointestinal discomfort.
Q4: What are the serious side effects?
A: GI bleeding, liver damage, severe allergic reactions, kidney problems.
Q5: Can patients with liver disease take this medication?
A: Use with caution in patients with liver disease. Consult a physician for dose adjustments or alternatives. Close monitoring of liver function tests is necessary.
Q6: Can this medicine be taken during pregnancy?
A: Consult a physician before use during pregnancy. Zaltoprofen should be avoided, especially in the third trimester. Paracetamol is generally safe at recommended doses.
Q7: Can this medicine be taken during breastfeeding?
A: Consult a physician before use during breastfeeding, as both components are excreted in breast milk.
Q8: Are there any drug interactions I should be aware of?
A: Yes, clinically significant interactions can occur with anticoagulants, other NSAIDs, methotrexate, lithium, alcohol, quinolone antibiotics, and sulfonylureas. Provide a complete medication history to your physician.
Q9: Can I consume alcohol while taking this medication?
A: Alcohol consumption is not recommended due to an increased risk of liver damage and gastrointestinal bleeding.
Q10: What should I do if an overdose occurs?
A: Seek immediate medical attention. Liver damage is a significant risk in paracetamol overdose. Early treatment is essential.
