Naslov
Dizajniranje i primjena prolijekova
(Design and Application of Prodrugs)

Autori
Jadrijević-Mladar Takač, Milena ; Branka, Zorc

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, pregledni

Izvornik
Knjiga sažetaka, Treći hrvatski kongres farmacije s međunarodnim sudjelovanjem / Zorc, Branka - Zagreb : Farmaceutsko-biokemijski fakultet Sveučilišta u Zagrebu, 2005, 30-30

Skup
Treći hrvatski kongres farmacije s međunarodnim sudjelovanjem

Mjesto i datum
Cavtat, Hrvatska, 27.04.2005. - 30.04.2005

Vrsta sudjelovanja
Pozvano predavanje

Vrsta recenzije
Domaća recenzija

Ključne riječi
Prodrug design; Drug; Prodrug; Drug rational design; Prodrug approach

Sažetak
Prodrug design comprises an area of drug research, which is concerned with the optimization of drug delivery. A prodrug is pharmacologically inactive derivative of a parent molecule, which requires spontaneous, i.e. non-enzymatic, or enzymatic transformation within the body in order to release the active drug. A prodrug has improved delivery properties over the parent drug molecule. A molecule with optimal structural configuration and physico-chemical properties for eliciting the desired therapeutic response at its target site, does not necessarily posses the best molecular form and properties for its delivery to its site of ultimate action. Prodrugs are designed to overcome pharmaceutically and/or pharmacokinetically based problems associated with the parent drug molecule, which otherwise would be of limited clinical use. In the pharmacokinetic phase, i.e. the absorption, distribution, metabolism and excretion of the drug, major barriers, which may limit the usefulness of a drug, are: incomplete absorption of the drug across biological membranes (GI mucosa or the blood-brain barrier), incomplete systemic bioavailability of a drug due to presystemic metabolism, too rapid absorption or excretion of the drug when a longer duration of action is desired, toxicity problems, poor site-specificity of the drug. The rational design of prodrugs can be divided into three basic steps: - identification of the drug delivery problem, - identification of the physico-chemical properties required for maximum efficacy or delivery, and - selection of a prodrug derivative which has the proper physico-chemical properties and which can be cleaved in the desired biological compartment. The prodrug approach has been successfully applied to a wide variety of drugs. Most of the applications have involved enhancement of bioavailability and passage through various biological barriers, increased duration of pharmacological effects, increased site-specificity, decreased toxicity and adverse reactions, improvement of organoleptic properties and improvement of stability and solubility properties.

Izvorni jezik
Engleski

Znanstvena područja
Farmacija

POVEZANOST RADA