Acemetacin

Severe: Contraindicated.

Severe: Contraindicated.

Acemetacin Should be taken with food.

Hypersensitivity to acemetacin or indometacin; previous hypersensitivity reactions (e.g. asthma, urticaria) to aspirin or other NSAIDs. Severe heart failure, haematologic disorder of uncertain aetiology, history of gastrointestinal bleeding or perforation related to previous NSAID use, nasal polyps associated with angioneurotic oedema, existing or history of recurrent (≥2 episodes) peptic ulcer or haemorrhage. Severe renal and hepatic impairment. Children and adolescents. Pregnancy (3rd trimester).

Patient with CV disease or risk factors for CV disease; oedema, hypertension, established ischaemic heart disease, peripheral arterial disease, cerebrovascular disease; history of peptic ulcer disease, gastrointestinal ulcers, gastrointestinal bleeding; dehydration, hypovolaemia; systemic lupus erythematosus, mixed connective tissue disorders, other forms of asthma, Crohn's disease, ulcerative colitis, epilepsy, Parkinson's disease or parkinsonism; coagulopathy, porphyria, psychiatric disorders, varicella zoster viral infections (e.g. chickenpox, herpes zoster). Smokers. May mask the signs and symptoms of infection. Extended-release cap is not recommended for initial relief of acute pain. Mild to moderate renal and hepatic impairment. Elderly or debilitated patient. Pregnancy (1st-2nd trimester) and lactation.

Significant: Hypersensitivity, anaphylactic reactions; CNS effects (e.g. drowsiness, dizziness, blurred vision); decreased platelet adhesion and aggregation, prolonged bleeding time; anaemia, (long-term use); visual disturbances (e.g. retinal changes, corneal opacification) during prolonged use; transaminase elevations, increased risk of aseptic meningitis, severe bronchospasm. Rarely, severe blood dyscrasias (e.g. agranulocytosis, leucopenia, thrombocytopenia, aplastic anaemia); severe hepatic reactions (e.g. fulminant hepatitis, hepatic necrosis, hepatic failure).
Cardiac disorders: Cardiac failure.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain or cramps, dyspepsia, flatulence.
General disorders and administration site conditions: Malaise, fatigue.
Metabolism and nutrition disorders: Loss of appetite.
Nervous system disorders: Headache.
Psychiatric disorders: Agitation.
Skin and subcutaneous tissue disorders: Urticaria, alopecia.
Vascular disorders: Hypertension.
Potentially Fatal: CV thrombotic events (e.g. MI, stroke); gastrointestinal inflammation, ulceration, bleeding, and perforation; exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis.

This drug may cause drowsiness, dizziness, and blurred vison, if affected, do not drive or operate machinery.

Monitor renal function (e.g. urine output, serum creatinine, BUN), blood pressure, LFTs; CBC with differential, ophthalmologic exams (with prolonged therapy). Assess for bleeding, bruising, gastrointestinal effects (e.g. abdominal pain, bleeding, dyspepsia).

May increase the risk of adverse effects with other NSAIDs. Increased risk of ulceration or bleeding with oral corticosteroids, anticoagulants (e.g. warfarin), SSRI, or antiplatelet drugs (e.g. aspirin). May diminish the effect of diuretics (e.g. loop), hypertensive agents (e.g. ACE inhibitors), and mifepristone (avoid acemetacin for 8-12 days after mifepristone use). Increased excretion with furosemide. May increase the plasma levels of cardiac glycosides (e.g. digoxin). May reduce the elimination of phenytoin, lithium, and methotrexate. May delay penicillin elimination. Increased risk of nephrotoxicity with ciclosporin or tacrolimus. Increased risk of haematological toxicity with zidovudine. Reduced elimination with probenecid or sulfinpyrazone. Enhanced drowsiness with haloperidol. Reduced resorption rate with antacids.

Concomitant use with alcohol may enhance the occult blood loss from the gastrointestinal tract.

Description:
Mechanism of Action: Acemetacin is a non-steroidal anti-inflammatory drug (NSAID). Its exact mechanism is unknown but is believed to involve both acemetacin and its major metabolite, indometacin. Unlike other NSAIDs, acemetacin is a weak inhibitor of prostaglandin synthetase.
Pharmacokinetics:
Absorption: Rapidly and completely absorbed from the gastrointestinal tract. Bioavailability: 100% after 10 days of therapy (immediate-release). Time to peak plasma concentration: 2.6 ± 2.3 hours (immediate-release); 6 hours (extended-release).
Distribution: Accumulates in inflamed regions, higher levels in the synovial fluid, synovial membrane, musculature, and bones.
Metabolism: Metabolised in the liver into indometacin (major metabolite).
Excretion: Via faeces (50% as metabolite); urine (40% as inactive metabolites); liver. Elimination half-life: 1.1 ± 0.6 hours (immediate-release); 1.8 hours (extended-release).

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 1981, Acemetacin. https://pubchem.ncbi.nlm.nih.gov/compound/Acemetacin. Accessed May 27, 2025.

Store below 25°C.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

M01AB11 - acemetacin ; Belongs to the class of acetic acid derivatives and related substances of non-steroidal antiinflammatory and antirheumatic products.

Acemetacin. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 10/04/2025.

Aceo Capsules Retard 90 mg (American Taiwan Biopharm Co Ltd). MIMS Thailand. http://www.mims.com/thailand. Accessed 10/04/2025.

Brayfield A, Cadart C (eds). Acemetacin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/04/2025.