BACKGROUND/AIM Switching the patient from one pharmaceutical formulation of the same drug to another, may lead to therapeutic inadequancy in some cases. To minimize the risk, careful pharmacokinetic studies are desired in the pre-registration period and afterwards. METHODS A randomized, crossover design with one-week wash-out period between each dose was applied. Serum samples, obtained befor...

Two conformational polymorphs of novel 2-[2-(3-cyano-4,6-dimethyl-2-oxo-2H-pyridin-1-yl)-ethoxy]-4,6-dimethyl nicotinonitrile have been developed. The crystal structure of both polymorphs (1a and 1b) seems to be stabilized by weak interactions. A difference was observed in the packing of both polymorphs. Polymorph 1b has a better binding affinity with the cyclooxygenase (COX-2) receptor than th...

Non-steroidal anti-inflammatory drugs (NSAIDs) and cyclo-oxygenase-2 (cox-2) inhibitors are structurally heterogeneous drugs that share similar therapeutic actions and adverse effects. Hepatotoxicity, although a relatively rare adverse effect of this class of drugs, can be severe. This has led to the withdrawal of some NSAIDs from the market. Nimesulide is an NSAID, with cox-2 preference, which...

Objective: This study aimed to verify the effect of preemptive administration dexamethasone 8 mg co-administered with paracetamol 1 g compared nimesulide 100 in surgeries for extracting third molars. Methods: A prospective, randomized, triple-blind clinical trial was conducted, allocating patients into two groups by split-mouth method: Group received and paracetamol, 2 nimesulide. Each patient ...

A double-blind, crossover clinical trial was carried out in subjects with fever, to assess the activity of three antipyretic drugs. Eighteen in-patients with body temperature (axillary) above 38 degrees C were given a single dose of nimesulide 100 mg, acetylsalicylic acid 500 mg, and dipyrone 500 mg, orally according to an incomplete balanced block design. Significant improvement was recorded w...

Madam, Nimesulide is a drug very commonly used in Pakistan. It non-steroidal anti-inflammatory (NSAID) with selectivity for cyclooxygenase-2 (COX-2) (1). as an analgesic, anti-inflammatory, and antipyretic (2). This which was first introduced Italy, has been successfully marketed more than 50 countries except the US (3). Moreover, result of its extensive rapid absorption, it allows effective pa...

Cyclo-oxygenase (COX) inhibitors may have a role in reducing inflammation in asthma and other pulmonary diseases. COX inhibitors have different selectivities for the two COX isoenzymes (COX 1 and COX 2) which vary between purified enzyme and intact cell preparations. The relative selectivity of COX inhibitors has not been studied in human airway cells. A number of COX inhibitors in cultured hum...

Westover AJ, Hooper SB, Wallace MJ, Moss TJM. Prostaglandins mediate the fetal pulmonary response to intrauterine inflammation. Am J Physiol Lung Cell Mol Physiol 302: L664–L678, 2012. First published January 27, 2012; doi:10.1152/ajplung.00297.2011.— Intra-amniotic (IA) lipopolysaccharide (LPS) induces intrauterine and fetal lung inflammation and increases lung surfactant and compliance in pre...

The aim of this study was to examine the relative contribution of both cyclooxygenase (COX) isoforms in producing the prostaglandins (PG) involved in the regulation of renal function, when nitric oxide (NO) synthesis is reduced. In anesthetized dogs with reduction of NO synthesis, the renal effects of a nonisozyme-specific COX inhibitor (meclofenamate) were compared with those elicited by a sel...