Aceclofenac

Chemical formula: C₁₆H₁₃Cl₂NO₄  Molecular mass: 354.18 g/mol  PubChem compound: 71771

Pharmacodynamic properties

Aceclofenac is a non-steroidal agent with marked anti-inflammatory and analgesic properties.

The mode of action of aceclofenac is largely based on the inhibition to prostaglandin synthesis. Aceclofenac is a potent inhibitor of the enzyme cyclo-oxygenase, which is involved in the production of prostaglandins.

Pharmacokinetic properties

After oral administration, aceclofenac is rapidly and completely absorbed as unchanged drug. Peak plasma concentrations are reached approximately 1.25 to 3.00 hours following ingestion. Aceclofenac penetrates into the synovial fluid, where the concentrations reach approximately 57% of those in plasma. The volume of distribution is approximately 25 L.

The mean plasma elimination half-life is around 4 hours. Aceclofenac is highly protein- bound (>99%). Aceclofenac circulates mainly as unchanged drug. 4'hydroxyaceclofenac is the main metabolite detected in plasma. Approximately two thirds of the administered dose is excreted via the urine, mainly as hydroxymetabolites.

No changes in the pharmacokinetics of aceclofenac have been detected in the elderly.

Preclinical safety data

The results from preclinical studies conducted with aceclofenac are consistent with those expected for NSAIDs. The principal target organ was the gastro-intestinal tract.

No unexpected findings were recorded.

Aceclofenac was not considered to have any mutagenic activity in three in vitro studies and an in vivo study in the mouse.

Aceclofenac was not found to be carcinogenic in either the mouse or rat.

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