Acemetacin; Uses, Dosage, Site Effects, Interactions

Acemetacin; Uses, Dosage, Site Effects, Interactions

Acemetacin is a carboxymethyl ester of indomethacin. It is a potent non-steroidal anti-inflammatory drug, derived from the indol-3-acetic acid, whose activity is thought to be mainly through its active metabolite indomethacin. In clinical trials, acemetacin exhibits a better gastric tolerability compared to its active metabolite indometacin. It was developed by E. Merck and Company in Germany as an attempt to provide a safer drug but other than the amelioration on the gastrointestinal effects, the metabolism of acetamicin led to the formation of indomethacin and it kept the same side effects.

Acemetacin is a carboxylic ester that is the carboxymethyl ester of indomethacin. A non-steroidal anti-inflammatory drug, it is used in the treatment of rheumatoid arthritis, osteoarthritis, and low back pain, as well as for postoperative pain and inflammation. Its activity is due to both acemetacin and its major metabolite, indomethacin. It has a role as a prodrug, an EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor, a non-steroidal anti-inflammatory drug, and a non-narcotic analgesic. It is a N-acylindole, a monocarboxylic acid, a carboxylic ester, an idol-3-yl carboxylic acid and a member of monochlorobenzenes. It derives from an indometacin.

Mechanism of Action of Acemetacin

Acemetacin is a non-selective inhibitor of the production of pro-inflammatory mediators derived from the action of the enzyme COX. COX is essential for the synthesis of prostaglandin E2 and F2 which are molecules derived from fatty acids and stored in the cell membrane. Acemetacin is metabolized and forms its major metabolite indometacin which is also a non-selective inhibitor of COX and exhibits the capacity to inhibit the motility of polymorphonuclear leukocytes and decreased cerebral flow by modulating the nitric oxide pathway and vasoconstriction.
Prostaglandin-endoperoxide synthase activity. Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the generation of thromboxane A2 (TXA2), which promotes platelet activation and aggregation, vasoconstriction and proliferation of vascular smooth muscle cells

Indications of Acemetacin

Acemetacin is not FDA, Canada or EMA approved, but in the countries where it is marketed it is indicated for the symptomatic treatment of pain and swelling in acute inflammation of the joints in rheumatoid arthritis, osteoarthritis, low back pain, and post-surgical pain. It is also indicated for the treatment of chronic inflammation of the joints in presence of rheumatoid arthritis, treatment of ankylosing spondylitis, treatment of irritation in the joints and spinal column caused by degenerative disorders, treatment of inflammatory soft-tissue rheumatism syndrome and painful swelling and inflammation caused by injury.
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Contra-Indications of Acemetacin

Hypersensitivity to acemetacin tablet is a contraindication. In addition, Acemetacin should not be used if you have the following conditions

Dosage of Acemetacin

  • Strengths: 60 mg, 120 mg,

Postoperative pain; Pain and inflammation associated with musculoskeletal and joint disorders

  •  Initially, 120 mg daily in divided doses, may increase to 180 mg, based on patient response.

or

  • The recommended starting dose is 120mg/day in divided doses, increasing to 180mg/day in divided doses, depending on patient response

Side Effects of Acemetacin

The most common

More common

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Rare

Drug Interactions of Acemetacin

Acemetacin may interact with following drugs, supplements & may change the efficacy of drugs

Pregnancy and Lactation of 

FDA Pregnancy Category – C

Pregnancy 

The safety of this medicine in human pregnancy and lactation has not been established. Some animal reproduction studies showed some toxic/ teratogenic effects on the fetus. Therefore, use of this drug during pregnancy and lactation period is not recommended.

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References

 

Acemetacin

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