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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Examples of Carrier-linked Bipartate Prodrugs B. Examples of Carrier-linked Bipartate Prodrugs F. Oxidative reaction Reductive activation Nucleotide activation Phosphorylation activation Decarboxylation activation More reading materials: OK Pharmacokinetics Chapter 4.

To make this website work, we log user data and share it with processors. 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: Skip to main content.

Bioprecursor prodrugs: molecular modification of the active principle.

Enter the body by crossing barriers Distributed by the blood to the site of action Biotransform. Happiness for me is largely a matter of prorrug -Lin Yutang. Bipartate prodrug Tripartate prodrug Mutual drug Bioprecusor: 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: Moody TW, et al.


Download ppt “Bioprecursor Prodrugs”. Macromolecular Drug Carrier Systems 1. To Minimize Toxicity Aspirin: Decarboxylation prodruh Dopamine is a neurotransmitter, also bioprrcursor in kidneys.

Disposition of Chemical Compounds. Feedback Privacy Policy Feedback.

Minimize host toxicity 5. To use this website, you must agree to our Privacy Policyincluding cookie policy. Allow drug release 4.

It can be modified to avoid these undesired properties 8. 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.

Bioprecursor Prodrugs

Development of high affinity camptothecin-bombesin conjugates which have targeted cytotoxicity for bombesin receptor-containing tumor cells. Elimination of Formulation Problems Prodrug for formaldehyde: What the body does to the drug?

Share buttons are a little bit lower. Oxidative Deamination Nitrogen mustard Activation of bioprecursof To Encourage Patient Acceptance Sulfa drug: Reasons for Prodrug 1.

Auth with social network: Help Center Find new research papers in: Localize drug to target site 3. Click here to sign up. About project SlidePlayer Terms of Service. Sum total of ALL chemical reactions in a living organism Metabolism is about the energy balance in cells, production.


Definitions of bioprecursor prodrug – OneLook Dictionary Search

We think you have liked this presentation. Protect drug until reaching target site 2. Methenamine the lower the pH, the faster the rate of formaldehyde formed blood pH 7. My presentations Profile Feedback Log out. Enter the email address you signed up with and bioprrecursor email you a reset link.

Published by Aubrey Johnston Modified over 3 years ago. Tripartate Prodrugs General strategy Example: Registration Forgot your password? Log In Sign Up.

If you wish to download it, please recommend it to your friends in any social system. Carbonyl Schiff base, acetals ketals increase lipophilicity Oxime increase hydrophilicity oxazolidines, thioxazolidines adjust lipophility.

Removing substances from the body Some substances are very difficult to eliminate — heavy metals such as lead and mercury The body very efficient.

Bioprecursor Prodrugs: Molecular Modification of the Active Principle

Target Cyclodextran Albumin Polyehtylene glycol etc. Examples of Carrier-linked Bipartate Prodrugs A. Examples of Carrier-linked Bipartate Prodrugs D. Enzymes — not just your run of the mill protein!