Abstract

ANTIBACTERIAL PREDRUGS-FROM 1899 TILL 2015

Sabrin Elayyan, Donia Karaman, Gennaro Mecca, Laura Scrano, Sabino A. Bufo, Rafik Karaman*

ABSTRACT

The predrug (prodrug) term involves chemically modified inert compound which upon an administration releases the active parent drug to elicit its pharmacological response within the body. For many years, the predrug strategy has been extensively developed to solve many unwanted drug properties. This approach has several advantages over conventional drug administration and it has the potential to be quite effective method for the treatment of diseases in the future. In this mini-review we describe a number of antibacterial agents‘ predrugs, and the ways by which predrug strategy was exploited to overcome many pharmaceutical and pharmacokinetic problems that the parent active antibacterial drugs suffer from such as, low bioavailability by increasing or decreasing lipophilicity, site selectivity for higher absorption and less toxicity, short duration of action to increase patient compliance, rapid metabolism to increase oral bioavailability and masking bitter sensation which is crucial for geriatric and pediatric patient compliance.

Keywords: Predrugs, Prodrugs, Antibacterials predrugs, Antibacterial agents, Predrug chemical approach, Intramolecular process, Bitter sensation.