Source: Medicines Authority (MT) Revision Year: 2022 Publisher: LABORATORIO DE APLICACIONES FARMACODINÁMICAS, S.A. – FARDI, Grassot, 16 – 08025-Barcelona (Spain) <u>Local representative:</u> Europharma Ltd, Catalunya Buildings, Psaila Street, Birkirkara. BKR 9076. ...
Pharmacotherapeutic group: Non-steroidal anti-inflammatory drug. Propionic acid derivatives; ibuprofen
ATC Code: M01AE01
Ibuprofen is an active ingredient with notable analgesic, anti-inflammatory and antipyretic properties. Its mechanism of action may be due to inhibition of prostaglandin synthesis. Prostaglandins play an essential role in the appearance of fever, pain and inflammation.
Experimental data suggest that ibuprofen may competitively inhibit the effect of low doses of acetylsalicylic acid on platelet aggregation when administered concomitantly. Some pharmacodynamic studies showed that when a single 400 mg dose of ibuprofen was administered within the 8 hours before or 30 minutes following an 81 mg dose of immediate-release acetylsalicylic acid, there was a decrease in the effect of acetylsalicylic acid on thromboxane formation or platelet aggregation. Although there are uncertainties regarding the extrapolation of these data to clinical situations, the possibility that regular long-term use of ibuprofen could reduce the cardioprotective effect of low doses of acetylsalicylic acid cannot be excluded. It is considered probable that there is no clinically relevant effect with the occasional use of ibuprofen (see section 4.5).
Ibuprofen is an active ingredient with linear pharmacokinetics.
Ibuprofen is well absorbed through the gastrointestinal tract. Publications establish that the peak plasma concentration of ibuprofen is reached 1-2 hours after administration of acid ibuprofen. The peak plasma concentration of the active isomer of ibuprofen is reached 30 minutes (Tmax) after the administration of this ibuprofen (lysine) suspension, compared to 80 minutes (Tmax) for the oral suspension of acid ibuprofen.
The degree of binding to plasma proteins is 90-99%. Its plasma half-life is approximately 2 hours. It diffuses well and passes into the synovial fluid, crosses the placental barrier and reaches very low concentrations in breast milk.
Ibuprofen is extensively metabolised in the liver by hydroxylation and carboxylation of the isobutyl group through CYP2C9 and CYP2C8. Its metabolites have no pharmacological activity.
Ibuprofen is largely eliminated through the kidneys and its excretion is virtually complete after 24 hours. Approximately 10% is eliminated unaltered and 90% is eliminated in the form of inactive metabolites, mainly glucuronides.
Ibuprofen was not teratogenic in different animal species. Furthermore, it showed no mutagenic or carcinogenic potential.
In some animal reproduction studies, an increase in labour dystocia or delays in birth have been observed, which are related to the inhibition of prostaglandin synthesis by NSAIDS.
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