Abstract

DICLOFENAC CODRUGS AND PRODRUGS-THREE DECADES OF DESIGN

khuloud Dweib, Salma Jumaa, Ameen Thawabteh, Laura Scrano, Sabino A. Bufo, Gennaro Mecca, Rafik Karaman*

ABSTRACT

Prodrugs or predrugs are inactive molecules which become active after in vivo conversion to release the active parent drug. The prodrug’s cleavage can be catalyzed by metabolic enzymes or can occur by chemical means without the involvement of enzymes. Prodrugs are designed to improve undesirable physicochemical and pharmacokinetic properties of their parent drugs. Non-steroidal anti-inflammatory (NSAIDs) drugs are among the most commonly used drugs for treatment of pain, inflammation and fever. Despite their frequent use, these agents suffer from gastrointestinal side effects that limit their use for those patients with gastrointestinal conditions. This mini review discusses the design, synthesis and pharmacological effects of prodrugs and codrugs of the non-steroidal anti-inflammatory (NSAIDs) Diclofenac sodium or potassium. It argues that the prodrug approach has the potential to eliminate Diclofenac associated gastrointestinal complications, increases its bioavailability and masks its bitter taste.

Keywords: Non-steroidal anti-inflammatory drugs, gastrointestinal complications, enzymatic biotransformation, Diclofenac, Prodrugs, Predrugs.