Acemetacin

Acemetacin belongs to the group of non-steroidal anti-inflammatory drugs. It has an anti-inflammatory, analgesic and antipyretic effect and is used for the symptomatic treatment of inflammatory rheumatic diseases such as rheumatoid arthritis, osteoarthritis or spinal disorders. The active ingredient is also used to treat low back pain and pain triggered by surgery or injury.

The antirheumatic drug was developed in 1972 by the Cologne-based drug manufacturer Tropon and is commercially available as an imitation drug. Acemetacin is now only rarely used due to its relatively strong side effects.

Pharmacodynamics

Acemetacin is the inactive precursor of indomethacin. This inhibits the enzyme COX, reducing prostaglandin synthesis. It specifically inhibits the formation of prostaglandin E2 and F2 (molecules derived from fatty acids). This allows the analgesic and anti-inflammatory effects to develop, as prostaglandins are primarily responsible for the transmission of pain to the brain.

Pharmacokinetics

Acemetacin is metabolized by esterolytic cleavage to indomethacin. The drug is strongly and almost completely bound to plasma proteins. The half-life is 4.5 hours. Acemetacin is excreted 40% by the kidney and 60% in the feces.

Contraindications

Acemetacin should not be used in case of:

• Hypersensitivity
• renal and hepatic dysfunction
• disturbance of hematopoiesis
• Heart failure
• gastric ulcer and duodenal ulcer
• Pregnancy and lactation

Side effects

Common side effects include:

• Nausea and vomiting
• abdominal pain or upper abdominal pain
• Loss of appetite
• diarrhea and constipation
• headache and dizziness
• drowsiness and fatigue
• Depression
• Tinnitus

Toxicological data

Inhibition of prostaglandin synthesis also reduces renal blood flow and glomerular filtration. Consequently, acemetacin causes decreased renal function with transient renal insufficiency and further renal and urinary disorders.