Acemetacin

Oral
Low back pain, Osteoarthritis, Postoperative inflammation, Postoperative pain, Rheumatoid arthritis

Severe: Contraindicated.

Severe: Contraindicated.

Should be taken with food. Take w/ or immediately after meals.

Hypersensitivity to acemetacin or indometacin, previous hypersensitivity reactions (e.g. asthma, urticaria) to aspirin or other NSAIDs (e.g. ibuprofen). 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 existing or history of bronchial asthma; rhinitis, swollen nasal mucosae, chronic respiratory disease, uncontrolled hypertension, oedema, CHF, established ischaemic heart disease, peripheral arterial disease, cerebrovascular disease, risk factors for CV disease (e.g. hyperlipidaemia, diabetes mellitus, smoking), increased haemorrhagic tendency, history of gastrointestinal ulcers, ulcerative colitis, Crohn's disease, SLE, mixed connective tissue disorders, hypovolaemia, dehydration, epilepsy, Parkinson's disease or parkinsonism, inducible porphyria, psychiatric disorders, varicella zoster viral infection (e.g. chickenpox, herpes zoster). Patient undergoing surgeries. Avoid concomitant use with other NSAIDs. Consider discontinuation in females who have difficulties conceiving or those undergoing infertility investigation. 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. Concomitant use with oral corticosteroids, anticoagulants, SSRI, antiplatelet agents.

Significant: Hypersensitivity or anaphylactoid reactions, bronchospasm (in patients with bronchial asthma), renal papillary necrosis (prolonged use), decreased prostaglandin synthesis (dose-related), Na and fluid retention, oedema, decreased platelet aggregation and adhesion, prolonged bleeding time, anaemia, elevated transaminases, may mask signs and symptoms of infection, vision disturbances (e.g. retinal changes, corneal opacification), impaired female fertility; aggravation of psychiatric disorders, epilepsy or parkinsonism; CNS effects (e.g. drowsiness, dizziness). Rarely, severe blood dyscrasias (e.g. agranulocytosis, aplastic anaemia, leucopenia, thrombocytopenia), severe hepatic reactions (e.g. fulminant hepatitis, hepatic failure, hepatic necrosis).
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: Gastrointestinal bleeding, ulceration or perforation, CV thrombotic events (e.g. MI, stroke). Rarely, serious skin reactions (e.g. toxic epidermal necrolysis, Stevens-Johnson syndrome, exfoliative dermatitis).

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

Monitor blood pressure; CBC with differential (during prolonged use); renal function (BUN, serum creatinine, urine output), liver function. Observe for gastrointestinal effects (e.g. abdominal pain, bleeding, dyspepsia) and bleeding. Perform ophthalmologic exams periodically during prolonged use.

Symptoms: Nausea, vomiting, epigastric pain, gastrointestinal bleeding, diarrhoea (rare), headache, disorientation, excitation, drowsiness, dizziness, fainting, tinnitus, convulsion, acute renal failure, liver damage, or coma. Management: Symptomatic treatment. Consider administration of activated charcoal or performing gastric lavage within 1 hour of ingestion. Ensure good urine output. Closely monitor renal and hepatic function. In case of frequent or prolonged convulsions, administer IV diazepam. Observe patient for at least 4 hours following ingestion.

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. Plasma levels of cardiac glycosides (e.g. digoxin) may be increased when used concomitantly with acemetacin. Reduced elimination of phenytoin, lithium, and methotrexate. May delay penicillin elimination. Increased risk of nephrotoxicity with ciclosporin or tacrolimus. Risk of haematological toxicity is increased when used concomitantly with zidovudine. Reduced elimination with probenecid or sulfinpyrazone. Enhanced drowsiness with haloperidol. May reduce 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 glycolic acid ester of indometacin. Its exact mechanism is not yet known but its pharmacological activity is stated to be due to the presence of both acemetacin and indometacin. Unlike other NSAIDs, it is believed to be a weak inhibitor of prostaglandin synthetase.
Pharmacokinetics:
Absorption: Well absorbed from the gastrointestinal tract. Bioavailability: 100% (immediate release; after 10 days of therapy). Time to peak plasma concentration: Acemetacin: 2.6 ± 2.3 hours (immediate release); 6 hours (extended release). Indometacin: 3.1 ± 0.4 hours.
Distribution: Accumulated in inflamed regions. Higher concentrations in synovial fluid, synovial membrane, musculature, and bones.
Metabolism: Metabolised in the liver to indometacin (major metabolite).
Excretion: Via faeces (50%; as metabolite); urine (40%; as inactive metabolites); liver. Elimination half-life: Acemetacin: 1.1 ± 0.6 hours (immediate release); 1.8 hours (extended release). Indometacin: 7.07 ± 1.8 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 1981, Acemetacin. https://pubchem.ncbi.nlm.nih.gov/compound/Acemetacin. Accessed June 24, 2021.

Store below 25°C.

Thuốc kháng viêm không steroid

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

Acemet Capsules 60 mg (Synmosa Biopharma Corporation). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 04/05/2021.

Acemet Retard Capsules 90 mg (Synmosa Biopharma Corporation). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 04/05/2021.

Anon. Acemetacin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/05/2021.

Buckingham R (ed). Acemetacin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/05/2021.