Acemetacin

Acemetacin is a non-steroidal anti-inflammatory drug (NSAID) primarily used for its potent anti-inflammatory, analgesic, and antipyretic effects. It is indicated for the relief of pain, swelling, and inflammation in a range of acute and chronic musculoskeletal and joint disorders.

✅ Approved Indications:

• Rheumatoid Arthritis (RA)
  For the management of pain, stiffness, and swelling in patients with active rheumatoid arthritis.
• Osteoarthritis (OA)
  Used to relieve joint pain, tenderness, and reduced mobility in degenerative joint disease.
• Ankylosing Spondylitis
  Indicated for relieving spinal stiffness and inflammation in patients with ankylosing spondylitis.
• Acute Gout Attacks
  Provides effective pain and inflammation relief during acute episodes of gouty arthritis.
• Periarticular and Soft Tissue Disorders
  Such as bursitis, tendinitis, and tenosynovitis.
• Post-Traumatic and Postoperative Inflammation
  For the management of pain and swelling following soft tissue injuries, fractures, or orthopedic surgeries.
• Other Musculoskeletal Conditions
  Where inflammation and pain relief are desired, including back pain, sprains, and strains.

• Adults:
  The usual recommended dose is 60 to 120 mg daily, taken in divided doses (e.g., 60 mg twice daily or 120 mg once daily), depending on the severity of symptoms and patient response.
• Administration Instructions:
• Take with or after meals to reduce gastrointestinal side effects.
• Swallow the capsule or tablet whole with water; do not crush or chew.
• Use the lowest effective dose for the shortest possible duration to control symptoms.
• Elderly:
• Use with caution. Start at the lower end of the dosing range due to the increased risk of adverse effects, especially gastrointestinal bleeding and renal impairment.
• Children:
• Not recommended for use in pediatric patients, as safety and efficacy have not been established.
• Renal or Hepatic Impairment:
• Use with extreme caution and under close monitoring. Dose adjustments may be necessary based on clinical assessment.

Acemetacin is a nonsteroidal anti-inflammatory drug (NSAID) that acts as a prodrug of indometacin. After administration, it is converted into indometacin, which works by inhibiting cyclooxygenase (COX-1 and COX-2) enzymes. These enzymes are essential for the biosynthesis of prostaglandins, which mediate inflammation, pain, and fever. By reducing prostaglandin production, acemetacin provides anti-inflammatory, analgesic, and antipyretic effects.

• Absorption:
  Acemetacin is well absorbed after oral administration. Peak plasma concentrations are usually reached within 2 hours.
• Prodrug Conversion:
  It is rapidly converted to its active metabolite, indometacin, in the body, which is responsible for the drug’s therapeutic effects.
• Distribution:
  Both acemetacin and its active metabolite are highly protein-bound and widely distributed in body tissues, including inflamed areas.
• Metabolism:
  Metabolized in the liver primarily to indometacin, and further metabolized into inactive forms via hepatic enzymes.
• Elimination:
  Excreted mainly through the urine (as metabolites) and to a lesser extent via bile/feces. The elimination half-life ranges from 4 to 6 hours.

• Anticoagulants (e.g., warfarin):
  May increase the risk of bleeding due to inhibition of platelet function and potential GI ulceration. Monitor INR and bleeding risk closely.
• Other NSAIDs or Corticosteroids:
  Concurrent use increases the risk of gastrointestinal ulceration or bleeding. Avoid combination unless absolutely necessary.
• Antihypertensives (e.g., ACE inhibitors, ARBs, diuretics):
  NSAIDs may reduce their antihypertensive effect and increase the risk of renal impairment, especially in elderly or dehydrated patients.
• Lithium:
  May increase serum lithium levels, leading to toxicity. Monitor lithium levels regularly.
• Methotrexate:
  May reduce methotrexate clearance, increasing the risk of toxicity. Use with caution and monitor renal function.
• Cyclosporine and Tacrolimus:
  Increased risk of nephrotoxicity when used together with NSAIDs.
• Digoxin:
  May raise serum digoxin levels, requiring monitoring of digoxin concentrations and clinical status.
• Alcohol:
  Increases the risk of GI bleeding. Patients should avoid alcohol while taking acemetacin.

• Known hypersensitivity to acemetacin, indometacin, or other NSAIDs.
• History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs.
• Active or recurrent peptic ulcer, gastrointestinal bleeding, or perforation.
• Severe hepatic, renal, or cardiac impairment.
• Third trimester of pregnancy, due to risk of fetal harm and closure of the ductus arteriosus.
• Cerebrovascular bleeding or any other active bleeding disorders.
• Use in children and adolescents is not recommended, as safety and efficacy are not established.
• Inflammatory bowel diseases such as Crohn’s disease or ulcerative colitis (may worsen symptoms).
• History of gastrointestinal perforation related to previous NSAID therapy.

Common side effects:

• Gastrointestinal: Nausea, abdominal pain, indigestion, diarrhea, flatulence, and occasional vomiting.
• Central nervous system: Headache, dizziness, fatigue, and somnolence.
• Skin: Rash or pruritus.

Less common but serious side effects:

• Gastrointestinal bleeding, ulceration, or perforation (more likely with prolonged use).
• Hepatotoxicity, including elevated liver enzymes and rare cases of hepatitis.
• Renal impairment, particularly in patients with pre-existing kidney disease.
• Cardiovascular risks, such as hypertension, fluid retention, or increased risk of thrombotic events with long-term use.
• Hypersensitivity reactions, including anaphylaxis, angioedema, or bronchospasm.
• Blood disorders, such as thrombocytopenia or agranulocytosis (rare).

• Pregnancy:
  Acemetacin is contraindicated during the third trimester of pregnancy due to the risk of premature closure of the ductus arteriosus, delayed labor, and fetal renal impairment. Use during the first and second trimesters should be avoided unless absolutely necessary, and only under close medical supervision.
• Lactation:
  There is limited data on the excretion of acemetacin in human breast milk. Although small amounts may pass into milk, the potential risk to a nursing infant is uncertain. Therefore, use during breastfeeding should be avoided or used with caution. If therapy is essential, consider discontinuing breastfeeding temporarily.

Nonsteroidal Anti-inflammatory Drug (NSAID), Aryl Acetic Acid Derivative.

Store below 25°C in a cool, dry place, away from heat, moisture, and direct sunlight.
Keep out of reach of children.