Turkish Journal of Physical Medicine and Rehabilitation 2004 , Vol 50 , Num 1

Selektif Siklo-oksijenaz-2 (COX-2) İnhibitörleri:KOKSİB’ler

Canan Tıkız 1
1 Celal Bayar Üniversitesi Tıp Fakültesi, Fiziksel Tıp ve Rehabilitasyon Anabilim Dalı, Manisa, Türkiye

Nonsteroidal anti-inflammatory drugs are the most widely used medications in the world. These agents are especially preferred to treat arthritis, headache and menstrual pain because of their analgesic and anti-inflammatory properties. During their long-term use they increase the risk of gastric erosion, peptic ulcus and bleeding by inhibiting the synthesis of prostaglandins which protect the gastric mucosa.The major limitation of  these drugs is gastrointestinal (GI) toxicity occurring in 2% to 4% of patients every year. The inhibition of cyclooxygenase-1 (COX-1) is the main factor in GI toxicity which necessiated further research on selective cyclooxygenase-2 (COX-2) inhibitors. In 1990, a novel cyclooxygenase protein was identified in monocytes which was stimulated by interleukin. After this observation, next year a different gene which was quite similar to COX-1 had been identified. Identification of this gene responsible from the synthesis of COX-2 rekindled the affords of the pharmacuetical industry to produce a safer analgesic and anti-inflammatory agent by selective inhibition of COX-2. Celecoxib and rofecoxib are the first two agents introduced for clinical use in 1999. They were prescribed more than 100 million for the 12 month period ending in July 2000 in the United States. In this review, the available data about the types, structural properties, mechanism of action and side effects of selective COX-2 inhibitors were summarized.

Keywords : Selective cyclooxyegenase-2 inhibitors, coxibs