Abstract

CLINICAL PHARMACOLOGY OF IBUPROFEN

Prof. Gian Maria Pacifici

ABSTRACT

Ibuprofen is the anti-inflammatory most used in the United States and is a non-selective cyclooxygenase inhibitor approved for use in treatment of symptomatic rheumatoid arthritis, juvenile arthritis, osteoarthritis, pain, ankylosing spondylitis, acute gouty, tendinitis, bursitis, headache, postoperative dental pain, swelling, and primary dysmenorrhoea. Ibuprofen is supplied in tablets, chewable tablets, capsules, geladas, oral drops, and oral suspension. An injectable formulation of ibuprofen is approved to close the patent ductus arteriosus. Ibuprofen is rapidly absorbed following oral administration and has been found efficacy and safe. The prophylaxis and the treatment with ibuprofen and the trials conducted with ibuprofen havebeen reviewed. Ibuprofen is hydrolysed into 2-hydroxy-ibuprofen and 3-hydroxy-ibuprofen and ibuprofen is also conjugated with glucuronic acid. The elimination half-life of ibuprofen is about 2.2 hours in adult healthy volunteers and is 1.4, 1.6, and 1.9 hours following the administration of ibuprofen suspension, chewable tablets, and tablets, respectively, to children with cystic fibrosis. The penetration of ibuprofen into subcutaneous tissue and skeletal muscle has been investigated following oral or topical administration of ibuprofen. Following oral administration, the peak concentration of (R)-ibuprofen and (S)-ibuprofen measured in plasma is higher than that of ibuprofen in dialysate from muscle and from dermis. Ibuprofen is a safe drug and induces toxicity only after the ingestion of large doses. The aim of this study is to review ibuprofen efficacy and safely, prophylaxis and treatment, trials conducted with ibuprofen, ibuprofen pharmacokinetics and metabolism, penetration of ibuprofen in human tissues, and ibuprofen toxicity.

Keywords: efficacy-safely, human tissues, ibuprofen, metabolism, pharmacokinetics, prophylaxis, toxicity, and treatment.