Oxaceprol

Usage

• Oxaceprol is prescribed for the treatment of osteoarthritis, a degenerative joint disease. It helps to relieve symptoms such as pain, swelling, and stiffness. It can also be used for inflammatory connective tissue diseases and superficial burns (topical application).
• Pharmacological Classification: Non-steroidal anti-inflammatory drug (NSAID). Also classified as a disease-modifying osteoarthritis drug (DMOAD).
• Mechanism of Action: Oxaceprol inhibits the accumulation of leukocytes (white blood cells) in the affected joints, thereby reducing inflammation. While its exact mechanism is not fully understood, it appears to influence connective tissue metabolism and may stimulate the uptake of glucosamine and proline in chondrocytes, contributing to cartilage regeneration. It does not inhibit prostaglandin synthesis in vitro.

Alternate Names

• No widely recognized alternate names are listed in the provided sources. Regional variations may exist.
• Brand Names: Iboxa, Oxuba, Lupoxa, Aksiprol, Uceprol, Oxamac, Oxuba OD Tablet SR, Trueceprol, Oxashine, Lupoxa OD, OXAPROCT, StayHappi, Zextra

How It Works

• Pharmacodynamics: Oxaceprol reduces inflammation in joints by inhibiting leukocyte accumulation. This leads to a decrease in pain, swelling, and stiffness. It may also promote cartilage repair.

• Pharmacokinetics:

  • Absorption: Absorbed within 3.5 hours after oral administration, permeating into synovial fluid. Bioavailability is approximately 30%.
  • Metabolism: Metabolized in the liver. Limited information is available on specific metabolic pathways or CYP enzyme involvement.
  • Elimination: Excreted primarily via urine, unchanged and complete. Elimination half-life is approximately 2.2 hours.

• Mode of Action: Inhibits leukocyte extravasation and adhesion to capillaries in the affected joints, thus reducing inflammation. In vitro studies suggest it stimulates the uptake of glucosamine and proline by chondrocytes.

• Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: The provided sources do not detail specific receptor binding, enzyme inhibition, or neurotransmitter modulation. It does not inhibit prostaglandin synthesis in vitro.

Dosage

Standard Dosage

Adults:

• Oral: 200 mg three times daily. In severe cases, the initial dose can be increased to 400 mg three times daily. Tablets/capsules should be taken before meals, unchewed. Alternatively, 1200 mg once daily can be administered. Maximum dose generally does not exceed 1800mg/day, although doses up to 2400mg/day are mentioned.
• Topical (10% cream): Apply once daily for superficial burns.

Children:

• Pediatric dosing varies by weight, age, and indication. Consultation with a doctor is essential for determining the appropriate dose.
• For juvenile rheumatoid arthritis:

  • 55 kg: 1200 mg once daily

  • 32-54 kg: 900 mg once daily
  • 22-31 kg: 600 mg once daily
• For osteoarthritis and rheumatoid arthritis: Dosage to be determined by doctor.
• Below age 6: Safety and efficacy not established.

Special Cases:

• Elderly Patients: Dose reduction is recommended due to potential sensitivity to side effects.
• Patients with Renal Impairment: Use with caution; dosage adjustment may be necessary. In severe renal impairment or patients on dialysis, 600 mg once daily is recommended; this may be increased to 1200 mg/day with close monitoring.
• Patients with Hepatic Dysfunction: Use with caution in patients with severe liver impairment; dosage adjustment may be necessary.
• Patients with Comorbid Conditions: Use with caution in patients with stomach ulcers, as Oxaceprol may worsen the condition. Also use with caution in patients with liver or kidney impairment.

Clinical Use Cases

• The primary clinical use case is the management of osteoarthritis. Limited information is available regarding specific dosage recommendations for other clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.

Dosage Adjustments

• Dose modifications are necessary based on renal and hepatic function, age, and other patient-specific factors.

Side Effects

Common Side Effects

• Nausea, vomiting, diarrhea, stomach pain, constipation, indigestion, bloating, dizziness, headache, skin rashes.

Rare but Serious Side Effects

• Allergic reactions (rash, itching).

Long-Term Effects

• No specific long-term effects are identified in the sources, although chronic use of NSAIDs carries a risk of gastrointestinal issues.

Adverse Drug Reactions (ADR)

• No specific ADRs requiring immediate intervention are noted beyond the common and rare side effects mentioned above.

Contraindications

• Hypersensitivity to Oxaceprol.
• Active peptic ulcers or gastrointestinal bleeding.
• Severely impaired liver or kidney function.

Drug Interactions

• Anticoagulants (e.g., warfarin, heparin): Increased risk of bleeding.
• Antihypertensives (e.g., atenolol, losartan): Decreased antihypertensive effect.
• Methotrexate: Increased toxicity.
• Lithium: Increased toxicity.
• NSAIDs and corticosteroids: Increased risk of gastrointestinal issues (ulcers, bleeding).
• Drugs affecting liver enzymes (CYP450 inhibitors or inducers): Altered metabolism and efficacy of Oxaceprol.

Pregnancy and Breastfeeding

• Pregnancy: Use with caution and only if clearly needed. Limited data on safety during pregnancy.
• Breastfeeding: Consult a doctor before use during breastfeeding as no information is available.

Drug Profile Summary

• Mechanism of Action: Inhibits leukocyte accumulation in joints, reducing inflammation.
• Side Effects: Nausea, vomiting, diarrhea, stomach pain, dizziness, headache, skin rash.
• Contraindications: Hypersensitivity, active peptic ulcers, severe liver/kidney impairment.
• Drug Interactions: Anticoagulants, antihypertensives, methotrexate, lithium.
• Pregnancy & Breastfeeding: Use with caution; consult a doctor.
• Dosage: Adults: 200 mg TID, up to 400 mg TID in severe cases. Pediatric: Weight-based dosing.
• Monitoring Parameters: Monitor for gastrointestinal symptoms, renal and hepatic function.

Popular Combinations

• No specific popular drug combinations are identified in the provided sources.

Precautions

• Pre-existing medical conditions (liver/kidney disease, stomach ulcers).
• Pregnant Women: Use with caution.
• Breastfeeding Mothers: Consult a doctor.
• Children & Elderly: Use with caution; dose adjustments may be required.
• Lifestyle Considerations: Limit alcohol consumption while on treatment. Avoid driving or operating heavy machinery if dizziness occurs.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Oxaceprol?

A: Adults: 200 mg three times a day, up to 400 mg three times a day in severe cases or 1200 mg once a day. Pediatric and special populations require individualized dosing; consult a physician.

Q2: What are the common side effects of Oxaceprol?

A: Common side effects include gastrointestinal issues like nausea, vomiting, diarrhea, stomach pain, and constipation. Dizziness, headache, and skin rashes can also occur.

Q3: Is Oxaceprol safe to use during pregnancy or breastfeeding?

A: Limited information is available on its safety during pregnancy and breastfeeding. Consult a doctor before use.

Q4: How does Oxaceprol work?

A: It inhibits leukocyte accumulation in the affected joints, reducing inflammation and pain. It may also contribute to cartilage repair by stimulating the production of certain components within the cartilage matrix.

Q5: What are the contraindications for Oxaceprol?

A: Contraindications include hypersensitivity to Oxaceprol, active peptic ulcers, gastrointestinal bleeding, and severe liver or kidney impairment.

Q6: Does Oxaceprol interact with other medications?

A: Yes, it can interact with anticoagulants, antihypertensives, methotrexate, lithium, and drugs affecting liver enzymes. Inform your doctor about all medications you are taking.

Q7: What should I do if I miss a dose of Oxaceprol?

A: Take the missed dose as soon as possible. If it is almost time for your next dose, skip the missed dose and continue with your regular schedule. Do not double the dose.

Q8: Can I drink alcohol while taking Oxaceprol?

A: While no direct interaction is noted, limiting alcohol consumption is advisable while on any medication.

Q9: Can I drive while taking Oxaceprol?

A: Oxaceprol may cause dizziness. Avoid driving or operating heavy machinery if you experience this side effect.

Q10: What if my pain doesn’t improve with the standard dose?

A: Consult with your physician, who may consider increasing the dose within the recommended range or exploring alternative treatment options.