Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1. Pharmacodynamic properties
Pharmacotherapeutic group: Propionic acid derivatives
ATC code: M01A E01

Ibuprofen is a propionic acid derivative NSAID that has demonstrated its efficacy by inhibition of prostaglandin synthesis. In humans ibuprofen reduces inflammatory pain, swellings and fever.

Furthermore, ibuprofen reversibly inhibits platelet aggregation.

Clinical evidence demonstrates that when 400 mg of ibuprofen are taken, pain relieving effects can last for up to 8 hours.

Experimental data suggest that ibuprofen may competitively inhibit the effect of low dose aspirin on platelet aggregation when they are dosed concomitantly. Some pharmacodynamic studies show that when single doses of ibuprofen 400mg were taken within 8 hours before or within 30 minutes after immediate release aspirin dosing (81mg), a decreased effect of aspirin on the formation of thromboxane or platelet aggregation occurred. Although there are uncertainties regarding extrapolation of these data to the clinical situation, (for) the possibility that regular, long-term use of ibuprofen may reduce cardioprotective effect of low-dose aspirin cannot be excluded. No clinically relevant effect is considered to be likely for occasional ibuprofen use (see section 4.5).

Pharmacokinetic Properties

5.2. Pharmacokinetic properties
After oral administration, solubilized ibuprofen (as present in Liquigel Capsules) is quickly absorbed when administered under fasting conditions. Cmax is achieved within 0.6 hours compared to conventional tablets (¾ – 1½ hours). When taken with food, peak levels are observed after 1-2 hours.

Ibuprofen protein binding is approximately 99%. After an oral dose, ibuprofen is 75 – 85% excreted in the urine during the first 24 hours (mainly in the form of two metabolites), the remainder being eliminated in the faeces following excretion in bile. Excretion is complete within 24 hours.

The half-life of ibuprofen in plasma is approximately 2 hours.

In limited studies, ibuprofen appears in the breast milk in very low concentrations.