Topic (19) Prodrugs (Part -01) = Introduction, Classification and Ideal Properties of Prodrugs
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(01) Antibiotics = Historical background, Nomenclature, Stereochemistry, Structure activity relationship, Chemical degradation classification and important products of the following classes-
(02) Macrolide: Erythromycin Clarithromycin, Azithromycin.
Miscellaneous: Chloramphenicol*, Clindamycin.
(03) Prodrugs: Basic concepts and application of prodrugs design.
Antimalarials: Etiology of malaria.
(04) Quinolines: SAR, Amodiaquine,Primaquine hydrochloride, Mefloquine.
Quinine phosphate, sulphate, Pamaquine*, Chloroquine*, Quinacrine
(05) Biguanides and dihydro triazines: Cycloguanil pamoate, Proguanil.
(06) Miscellaneous: Pyrimethamine, Artesunete, Artemether, Atovoquone.
A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug.
1. Prodrugs provide possibilities for overcoming drug-delivery challenges, such as poor aqueous solubility, formulation, insufficient oral absorption, chemical instability, inadequate brain penetration, toxicity, and local irritation.
2. Prodrugs are usually used with the aim of increasing drug permeation by enhancing lipophilicity or water solubility. The prodrug must exhibit enough aqueous solubility and stability, adequate lipophilicity, sufficient safety, and reasonable conversion to the parent drug in vivo.
Classification
Prodrugs can be classified into two major types,[10] based on how the body converts the prodrug into the final active drug form:
1. Type I prodrugs are bioactivated intracellularly, which means turn into their active forms inside of cells.
Examples of these are anti-viral nucleoside analogs that must be phosphorylated and lipid-lowering statins.
2. Type II prodrugs are bioactivated extracellularly, which means turn into their active forms outside of cells, such as in blood or other fluids, especially in digestive fluids or in the body's circulatory system, particularly in the blood.
Examples of Type II prodrugs are salicin (described above) and certain antibody-, gene- or virus-directed enzyme prodrugs used in chemotherapy or immunotherapy.
Both major types can be further categorized into subtypes, based on factors such as (Type I) whether the intracellular bioactivation location is also the site of therapeutic action, or (Type 2) whether or not bioactivation occurs in the gastrointestinal fluids or in the circulation system.
An ideal ester prodrug should exhibit the following properties:
1) Weak (or no) activity against any pharmacological target
2) Chemical stability across a pH range
3) High aqueous solubility
4) Good transcellular absorption
5) Resistance to hydrolysis during the absorption phase
6) Rapid and quantitative breakdown to yield high circulating concentrations of the active component post absorption.
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