Chemical formula: C₁₃H₁₈O₂ Molecular mass: 206.281 g/mol PubChem compound: 3672
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.
Experimental data suggest that ibuprofen may inhibit the effect of low dose aspirin on platelet aggregation when they are dosed concomitantly. In one study, when a single dose of ibuprofen 400 mg was taken within 8 hours before or within 30 minutes after immediate release aspirin dosing (81 mg), 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.
Ibuprofen gel exerts its anti-inflammatory and analgesic effects directly in inflamed tissues underlying the site of application, mainly by inhibiting prostaglandin biosynthesis. Because it is formulated in an aqueous/alcoholic gel, the preparation also exerts a soothing and cooling effect when applied to the affected area.
Ibuprofen is rapidly absorbed from the gastro-intestinal tract and rapidly distributed throughout the whole body. Peak plasma concentrations occur about 1 to 2 hours after ingestion with food or in 45 minutes if taken on an empty stomach. These times may vary with different dosage forms.
The excretion is rapid and complete via the kidneys.
The elimination half-life is about 2 hours.
It is metabolized to two inactive metabolites and these are rapidly excreted in urine. About 1 percent is excreted in urine as unchanged Ibuprofen and about 14 percent as conjugated ibuprofen.
Ibuprofen is extensively bound to plasma proteins.
In limited studies, ibuprofen appears in breast milk in very low concentrations.
Specially formulated for external application, the active ingredient penetrates through the skin rapidly and extensively (approximately 22% of a finite dose within 48 hours), achieving high, therapeutically relevant local concentrations in underlying soft tissues, joints and the synovial fluid, whilst producing plasma levels that are unlikely to be sufficient to cause any systemic side-effects, other than in rare individuals who are hypersensitive to ibuprofen. Furthermore, there do not appear to be any appreciable differences between the oral and topical routes of administration regarding metabolism or excretion.
There is no new data published on the active ingredient.
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