BISPHOSPHONATES – IMPORTANT ANTIRESORPTIVE AGENTS FOR BONE DISEASES.
LĂCRĂMIOARA OCHIUZ, ELIZA GAFIŢANU
Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, University of Medicine and Pharmacy „Gr. T. Popa” Iaşi, str. Universităţii nr. 16, 700115

Abstract:

The bisphosphonates comprise a class of drugs that has been developed over the last 30 years, primarily as antiresorptive agents capable of treating diseases related to bone remodeling. Chemically, the bisphosphonates are analogs of pyrophosphates and show different antiresorptive potencies in in vitro studies that vary over several orders of magnitude, depending on the nature of the alkyl substituents R1 and R2. Although the precise mechanism of action is not completely understood, these agents strongly inhibit osteoclast mediated bone resorption. Bisphosphonates have become a first line treatment for diseases that involve excessive osteoclast mediated bone resorption, such as Paget's disease, tumoral osteolysis and osteoporosis. The major disadvantage of the clinically utilized bisphosphonates is their poor absorption from the GI tract to below 1 % for the newer ones.
In present, the research on this class of therapeutical agents aim mainly to the synthesis of new chemical compounds or the achievement of some differences on pharmaceutical-technological factors in the formulation and preparation of new pharmaceutical forms. The research aims to increase both the gastrointestinal tolerability and the bioavailability of the compounds already used in therapeutics as well as the widening of the therapeutical domain of this class of antiresorptive agents.

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