Mini Rev Med Chem. Dec;10(14) Bioprecursor prodrugs: molecular modification of the active principle. Kokil GR(1), Rewatkar PV. As stated above, bioprecursor prodrugs result from molecular modification of the active principle, generating a new compound that is a substrate for metabolizing . Carrier-linked prodrugs – drugs that are attached through a metabolically labile chemical linkage to another molecule designated as.

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Bipartate prodrug Tripartate prodrug Mutual drug Bioprecusor: Cancer Chemotherapy Tumor cells have a much higher growth fraction This translates into higher enzymatic activity that can be exploited Target a prodrug to these sites and exploit higher enzyme activity Example: To Minimize Toxicity Aspirin: To Encourage Patient Acceptance Sulfa drug: Examples of Carrier-linked Bipartate Prodrugs D. Click here to sign up. Protect drug until reaching target site 2. Happiness for me is largely a matter of digestion -Lin Yutang.

Protect a non-specific biological environment from a drug Protect a drug from a non-specific biological environment Especially evaluated for drugs with a narrow therapeutic window especially anti-cancer agents.

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Oxidative reaction Reductive activation Nucleotide activation Phosphorylation activation Decarboxylation activation More reading materials: Examples of Carrier-linked Bipartate Prodrugs B. Localize drug to target site 3. Oxidative Deamination Nitrogen mustard Activation of cyclophosphamide: Auth with social network: About project SlidePlayer Terms of Service.


Enzymes — not just your run of the mill protein! Moody TW, et al.

Allow drug release 4. Disposition of Chemical Compounds. Download ppt “Bioprecursor Prodrugs”. Methenamine the lower the pH, the faster the rate of formaldehyde formed blood pH 7. What the body does to the drug? My presentations Profile Feedback Log out. Decarboxylation activation Dopamine is biorpecursor neurotransmitter, also important in kidneys.

Reasons for Prodrug 1. Minimize host toxicity 5. Sum total of ALL chemical reactions in a living bioprecjrsor Metabolism is about the energy balance in cells, production. Development of high affinity camptothecin-bombesin conjugates which have targeted cytotoxicity for bombesin receptor-containing tumor cells.

Bioprecursor Prodrugs: Molecular Modification of the Active Principle

OK Pharmacokinetics Chapter 4. Carbonyl Schiff base, acetals ketals increase lipophilicity Oxime increase hydrophilicity oxazolidines, thioxazolidines adjust lipophility. Tripartate Prodrugs General strategy Example: Help Center Find new research papers in: Removing substances from the body Some substances are vioprecursor difficult to eliminate — heavy metals such as lead and mercury The body very efficient. Feedback Privacy Policy Feedback. Log In Sign Up.

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Definition of bioprecursor_prodrug – Chemistry Dictionary

Elimination of Formulation Problems Prodrug for formaldehyde: Prodrug readily transported to the site of action Prodrug is rapidly absorbed at the site Selective and rapid conversion to the active drug Kidney and Liver are easy targets due to high perfusion and high metabolic rates Other tissue sites can be problematic for the same reasons Drug migrate slowly site of action to a site of excretion Ideal situation is VERY complex to achieve Example: Published by Aubrey Johnston Modified over 3 years ago.


Target Cyclodextran Albumin Polyehtylene glycol etc. Examples of Carrier-linked Bipartate Prodrugs F. Remember me on this computer. Macromolecular Drug Carrier Systems 1. It can be modified to avoid these undesired properties 8.

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We think you have liked this presentation. Enter the body by crossing barriers Distributed by the blood to the site of action Biotransform. To make this website work, we log user data and bioprecurxor it with processors. If you wish to download it, please recommend it to your friends in any social system. Examples of Carrier-linked Bipartate Prodrugs A.