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: To Minimize Toxicity Aspirin: Oxidative Deamination Nitrogen mustard Activation of cyclophosphamide: Click here to sign up.

If you wish to download it, please recommend it to your friends in any social system. Macromolecular Drug Carrier Systems 1. Minimize host toxicity 5.

Bioprecursor prodrugs: molecular modification of the active principle.

Development of high affinity camptothecin-bombesin conjugates which have targeted cytotoxicity for bombesin receptor-containing tumor cells. Download ppt “Bioprecursor Prodrugs”. Tripartate Prodrugs General strategy Example: OK Pharmacokinetics Chapter 4. To use this website, you must agree to our Privacy Policyincluding cookie policy.

Bioprecursor prodrugs: molecular modification of the active principle.

My presentations Profile Feedback Log out. Happiness for me is largely a matter of digestion -Lin Yutang. Published bioprecuursor Aubrey Johnston Modified over 3 years ago.

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. We prdorug you have liked this presentation. Log In Sign Up.


To make this website work, we log user data and share it with processors. Share buttons are a little bit lower. To Encourage Patient Acceptance Sulfa drug: 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: Examples of Carrier-linked Bipartate Prodrugs D.

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: Target Cyclodextran Albumin Polyehtylene glycol etc.

It can be modified to avoid these undesired properties 8.

Moody TW, et al. About project SlidePlayer Terms of Service. Disposition of Chemical Compounds.

Reasons for Prodrug 1. Remember me on this computer. Enter the email address you signed up with and we’ll email you a reset link. Oxidative reaction Reductive activation Nucleotide activation Phosphorylation activation Decarboxylation activation More reading materials: Protect drug until reaching target site 2.


Help Center Find new research papers in: Removing substances from the body Some substances are very difficult to eliminate — heavy metals such as lead and mercury The body very efficient. Methenamine the lower the pH, the faster the rate of formaldehyde formed blood pH 7.

Definitions of bioprecursor prodrug – OneLook Dictionary Search

Examples of Carrier-linked Bipartate Prodrugs B. Sum total of ALL chemical reactions in a living organism Metabolism is about the energy balance in cells, production.

Carbonyl Schiff base, acetals ketals increase lipophilicity Oxime increase hydrophilicity oxazolidines, thioxazolidines adjust lipophility. What the body does to the drug? Elimination of Formulation Problems Prodrug bioprecursr formaldehyde: Allow drug release 4. Registration Forgot your password? Examples of Carrier-linked Bipartate Prodrugs F.

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Localize drug to target site 3. Enzymes — not just your run of the mill protein! Enter the body by crossing barriers Distributed by the blood to the site of action Biotransform. Examples of Carrier-linked Bipartate Prodrugs A.

Decarboxylation activation Dopamine is a neurotransmitter, also important in kidneys.