Zaltoprofen

Usage

• Zaltoprofen is prescribed for pain and inflammation associated with conditions like rheumatoid arthritis, osteoarthritis, low back pain, periarthritis of the shoulder (frozen shoulder), cervicobrachial syndrome (neck-shoulder-arm syndrome), and post-surgical/trauma/tooth extraction pain.
• Pharmacological classification: Non-Steroidal Anti-Inflammatory Drug (NSAID) and analgesic
• Mechanism of Action: Zaltoprofen primarily inhibits cyclooxygenase (COX) enzymes, particularly COX-2. COX enzymes catalyze the formation of prostaglandins, which are mediators of pain and inflammation. By inhibiting COX, Zaltoprofen reduces prostaglandin production, thereby alleviating pain and inflammation. Zaltoprofen also exhibits some selectivity for COX-2 over COX-1, which may contribute to a lower risk of gastrointestinal side effects compared to non-selective NSAIDs. Additionally, it inhibits bradykinin release, further reducing pain and inflammation.

Alternate Names

• No alternate generic names were found in the provided sources.
• Brand Names: Zalto, Zaltokin, Zaltop-80, Zott P (in combination with paracetamol)

How It Works

• Pharmacodynamics: Zaltoprofen reduces pain and inflammation by inhibiting COX enzymes and bradykinin release.
• Pharmacokinetics:
  • Absorption: Well absorbed orally (82%).
  • Metabolism: Primarily metabolized by CYP2C9 and UGT2B7 in the liver to various metabolites (S-oxide Zaltoprofen (M-2), 10-hydroxy Zaltoprofen (M-3) and S-oxide-10-hydroxy-Zaltoprofen (M-5)).
  • Elimination: Primarily via renal excretion (62% as conjugates, 3% as unchanged drug); some hepatic excretion. Biphasic elimination with half-lives of approximately 0.9 hours (alpha phase) and 9 hours (beta phase). The elimination half-life of Zaltoprofen is approximately 2.8 hours after a single dose.
• Mode of Action: Inhibits COX enzymes, reducing prostaglandin synthesis, thus decreasing pain and inflammation. Also inhibits bradykinin release.
• Receptor Binding/Enzyme Inhibition: Binds to and inhibits COX enzymes, especially COX-2.
• Elimination Pathways: Primarily renal excretion of metabolites; some hepatic excretion.

Dosage

Standard Dosage

Adults:

• 80 mg three times daily. The total daily dose can range from 80 mg to 240 mg, divided into 2-3 doses, adjusted based on patient response and tolerance.

Children:

• Safety and efficacy in children have not been established, and therefore use is not recommended.

Special Cases:

• Elderly Patients: Start with a lower dose and adjust as needed due to potential age-related decline in renal and hepatic function.
• Patients with Renal Impairment: Reduce dose in patients with moderate to severe renal impairment.
• Patients with Hepatic Dysfunction: Reduce dose and monitor closely.
• Patients with Comorbid Conditions: Caution is advised in patients with underlying health conditions like asthma, hypertension, and cardiovascular disease.

Clinical Use Cases

• Specific dosage recommendations for clinical scenarios like intubation, surgical procedures, mechanical ventilation, ICU use, and emergency situations were not found in the provided sources. Dosing should be based on clinical judgment and patient-specific factors.

Dosage Adjustments

• Dose adjustments may be required based on renal/hepatic function, other medical conditions, and drug interactions.

Side Effects

Common Side Effects:

• Gastrointestinal: Nausea, vomiting, dyspepsia, abdominal pain, diarrhea, stomach heaviness, heartburn, stomatitis, loss of appetite.
• Central Nervous System: Dizziness, headache, drowsiness, fatigue.
• Dermatological: Photosensitivity, rash, skin eruption, eczema, itch, edema.
• Other: Dry mouth, fever, loss of appetite, sleepiness.

Rare but Serious Side Effects:

• Gastrointestinal bleeding, peptic ulcer, small/large intestine ulcer, hemorrhagic colitis.
• Blood disorders: Agranulocytosis, thrombocytopenia (indicated by fever, sore throat, headache, nosebleeds, or gum bleeding).
• Hepatic dysfunction: Jaundice.
• Renal impairment.
• Hypersensitivity reactions: Rash, itching, angioedema.

Long-Term Effects:

• Chronic use can lead to gastrointestinal complications like ulcers and bleeding, especially in patients with risk factors.
• Renal impairment can occur with long-term use, especially in patients with pre-existing renal disease.

Adverse Drug Reactions (ADR):

• Serious gastrointestinal bleeding, severe allergic reactions, blood dyscrasias, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Contraindications

• Hypersensitivity to zaltoprofen or other NSAIDs.
• Active peptic ulcer or gastrointestinal bleeding.
• History of peptic ulcer disease or GI bleeding associated with NSAID use.
• Severe heart failure, hepatic impairment, or renal impairment.
• Ulcerative colitis or Crohn’s disease.
• Aspirin-induced asthma or allergic reactions to other NSAIDs.
• Third trimester of pregnancy.

Drug Interactions

• Anticoagulants (e.g., warfarin): Increased risk of bleeding.
• Antiplatelet agents (e.g., aspirin): Increased risk of bleeding.
• Antihypertensives (e.g., ACE inhibitors, beta-blockers): Reduced antihypertensive effect.
• Diuretics: Increased risk of renal impairment.
• Quinolone antibiotics: Increased risk of seizures.
• Sulfonylurea antidiabetic agents: Increased risk of hypoglycemia.
• Lithium: Increased lithium levels.
• Methotrexate: Increased methotrexate toxicity.
• Other NSAIDs: Increased risk of gastrointestinal side effects.
• Alcohol: Increased risk of gastrointestinal bleeding.

Pregnancy and Breastfeeding

• Pregnancy: Zaltoprofen should be avoided during pregnancy, particularly the third trimester, due to the risk of premature closure of the ductus arteriosus in the fetus. Use in the first and second trimesters should be limited to cases where the potential benefit to the mother outweighs the risk to the fetus.
• Breastfeeding: Limited data suggest Zaltoprofen may be excreted in breast milk; therefore, it should be used with caution during breastfeeding. Consider alternative analgesics if possible.

Drug Profile Summary

• Mechanism of Action: COX inhibitor, predominantly COX-2, reducing prostaglandin synthesis; inhibits bradykinin release.
• Side Effects: Gastrointestinal issues, dizziness, headache, skin rashes; rarely, GI bleeding, blood disorders, hepatic/renal dysfunction.
• Contraindications: Hypersensitivity, active peptic ulcer/GI bleeding, severe heart/liver/renal impairment, inflammatory bowel disease, aspirin-induced asthma.
• Drug Interactions: Anticoagulants, antiplatelets, antihypertensives, diuretics, quinolones, sulfonylureas, lithium.
• Pregnancy & Breastfeeding: Avoid in the third trimester; use with caution in other trimesters and during breastfeeding.
• Dosage: 80-240 mg/day divided into 2-3 doses; adjust for elderly and patients with renal/hepatic impairment.
• Monitoring Parameters: Renal and liver function tests, complete blood count, signs of gastrointestinal bleeding.

Popular Combinations

• Paracetamol: Often combined with paracetamol (Zott P) for enhanced analgesic effects.

Precautions

• Pre-existing medical conditions: Assess for renal, hepatic, cardiovascular, and gastrointestinal conditions before initiating therapy.
• Pregnant Women: Avoid, especially in the third trimester.
• Breastfeeding Mothers: Use with caution, monitor infant.
• Children & Elderly: Not recommended for children; dose adjustment for elderly.
• Lifestyle Considerations: Limit alcohol intake to reduce the risk of GI bleeding; avoid driving or operating heavy machinery if drowsiness or dizziness occur.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Zaltoprofen?

A: The recommended adult dosage is 80-240 mg/day, divided into 2-3 doses. Dosage adjustments are necessary for elderly patients and those with renal or hepatic impairment. Pediatric use is not recommended.

Q2: What are the common side effects of Zaltoprofen?

A: Common side effects include gastrointestinal issues (nausea, vomiting, dyspepsia, abdominal pain), dizziness, headache, and skin rashes.

Q3: What are the serious side effects of Zaltoprofen?

A: Serious side effects include gastrointestinal bleeding, peptic ulcers, blood disorders (agranulocytosis, thrombocytopenia), and allergic reactions.

Q4: What are the contraindications for Zaltoprofen?

A: Contraindications include hypersensitivity to zaltoprofen or other NSAIDs, active peptic ulcer or GI bleeding, severe heart/liver/renal impairment, and aspirin-induced asthma.

Q5: How does Zaltoprofen interact with other medications?

A: Zaltoprofen can interact with anticoagulants, antiplatelets, antihypertensives, diuretics, quinolone antibiotics, and other NSAIDs. It’s important to inform your physician about all medications, including over-the-counter drugs and supplements.

Q6: Can Zaltoprofen be used during pregnancy and breastfeeding?

A: Zaltoprofen should be avoided during pregnancy, especially in the third trimester. Use during breastfeeding should be cautious, and alternative analgesics should be considered.

Q7: What are the long-term effects of Zaltoprofen use?

A: Long-term use can increase the risk of gastrointestinal problems and renal impairment. Regular monitoring is recommended.

Q8: How should Zaltoprofen be administered?

A: Zaltoprofen is administered orally, typically with food or milk to reduce gastrointestinal discomfort. Tablets should be swallowed whole and not crushed or chewed.

Q9: What should patients be advised before starting Zaltoprofen?

A: Patients should inform their doctors about their complete medical history, including any allergies, pre-existing conditions, and concomitant medications. They should also be advised about potential side effects and drug interactions. Patients should understand that Zaltoprofen primarily treats symptoms and does not cure the underlying condition. They should be advised to seek medical attention immediately if they experience any serious side effects.