Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1   Pharmacodynamic properties
Pharmacotherapeutic group: anti-inflammatory and anti-rheumatic products, non-steroids, propionic acid derivative; ATC code: M01AE01

Ibuprofen is a NSAID that has demonstrated its efficacy in the common animal experimental inflammation models by inhibition of prostaglandin synthesis. In humans, ibuprofen reduces inflammatory pain, swellings and fever. Furthermore, ibuprofen reversibly inhibits platelet aggregation.

The clinical efficacy of ibuprofen has been demonstrated in fever and in pain associated with headache, toothache and dysmenorrhoea. Furthermore it has been demonstrated in patients with pain and fever associated with cold and flu and in pain models such as sore throat, muscular pain, soft tissue injury, backache.

Experimental data suggest that ibuprofen may inhibit the effect of low dose aspirin on platelets aggregation when they are dosed concomitantly. In one study, when a single dose of ibuprofen 400mg was taken within 8 h before or within 30 min after immediate release aspirin (81mg), a decreased effect of aspirin on the formation of thromboxane or platelet aggregation occurred. However, the limitations of these data and the uncertainties regarding extrapolation of ex vivo data to the clinical situation imply that no firm conclusions can be made for regular ibuprofen use, and no clinically relevant effect is considered to be likely for occasional ibuprofen use.

Pharmacokinetic Properties

5.2     Pharmacokinetic properties

After rectal administration, ibuprofen is absorbed quickly and almost completely, and is rapidly distributed throughout the whole body. Median peak plasma concentrations are seen 0.75 hours after use Nurofen for children suppository.

Ibuprofen is extensively bound to plasma proteins.

Ibuprofen is metabolised in the liver to two major inactive metabolites and these, together with unchanged ibuprofen, are excreted by the kidney either as such or as conjugates. Excretion by the kidney is both rapid and complete. The elimination half life is approximately 2 hours.

No special pharmacokinetic studies have been carried out in children. However, pharmacokinetic parameters of ibuprofen in children are comparable with those in adults.