Ibuprofen: pharmacology, efficacy and safety

Abstract

This assessment of the safety and benefits of ibuprofen can be summarized thus: (1) Ibuprofen at OTC doses has low possibilities of serious GI events, and little prospect of developing renal and associated CV events. Ibuprofen OTC does not represent a risk for developing liver injury especially the irreversible liver damage observed with paracetamol and the occasional liver reactions from aspirin. (2) The pharmacokinetic properties of ibuprofen, especially the short plasma half-life of elimination, lack of development of pathologically related metabolites (e.g. covalent modification of liver proteins by the quinine-imine metabolite of paracetamol or irreversible acetylation of biomolecules by aspirin) are support for the view that these pharmacokinetic and notably metabolic effects of ibuprofen favour its low toxic potential. (3) The multiple actions of ibuprofen in controlling inflammation combine with moderate inhibition of COX-1 and COX-2 and low residence time of the drug in the body may account for the low GI, CV and renal risks from ibuprofen, especially at OTC doses.

Sensibilidade espécie-específica aos anti-inflamatórios não esteroidais: humanos X animais de companhia

“…Além disso, o diclofenaco está entre os medicamentos mais consumidos pelo brasileiro (Frutuoso, 2004), enquanto o ibuprofeno é um dos AINES de venda livre mais consumido no mundo (Rainsford, 2009 Em humanos, a meia-vida do diclofenaco é de duas horas, e de duas a quatro horas tanto para o cetoprofeno como para o ibuprofeno (Olson, 2007). Para cães, a meia-vida do cetoprofeno é de quatro horas, enquanto para gatos é de 1,1 a duas horas (Talcott, 2006;Xavier et al, 2008), e a do ibuprofeno varia entre 2,5 e 5,8 horas, para ambas as espécies (Fitzgerald et al, 2006).…”

Case Files of the University of California, San Francisco Medical Toxicology Fellowship: Seizures and a Persistent Anion Gap Metabolic Acidosis

“…The patient's serum ibuprofen concentration on arrival to the hospital was quantified at 641.5 μg/mL. Maximum therapeutic serum concentrations of ibuprofen are reported from 6.1 to 47.7 μg/mL with peak levels 1-3 h after ingestion, depending upon formulation [46].…”

The Meaning of Fever in Children

“…Вместе с тем в некоторых исследованиях установлена низкая вероятность развития гастроинтестинальных, ренальных, а также нежелательных явлений со стороны сердечно-сосудистой системы при приеме ибупрофена. Кроме того, лечение ибупрофеном не было сопряжено с риском повреждения печени, описанным для других жаропонижающих (включая парацетамол) и нестероид-ных противовоспалительных средств [28,29].…”