BIOPRECURSOR PRODRUGS PDF

THE DIFFERENT KINDS OF PRODRUGS A. Defi nitions and classifi cations B. The carrier prodrug principle C. The bioprecursor-prodrug principle D. Other. Bioprecursor Prodrugs. Phosphorylation example –. Bioprecursor Prodrugs. We have already seen 2 examples of this: Sulfasalazine – an azo compound. Bioprecursor Prodrugs: Molecular Modification of the Active Principle Keywords: Bioprecursor prodrugs, active metabolites, oxidative activation, glucuronic.

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Identify how biooprecursor approach can be used to overcome certain issues with a drug candidate 4. Share buttons are a little bit lower. 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: Prodrugs to encourage patient acceptance clindamycin antibacterial. 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 prodruugs of excretion Ideal situation is VERY complex to achieve Example: Disposition of Chemical Compounds.

You are a scientist wanting to formulate this drug for parenteral administration. N-Oxidation pralidoxime acetylcholine esterase activator e. Prodrugz may be helpful for biopercursor bioavailability, or also if the drug itself is nonspecific in its action. Phenyl carbamates are rapidly cleaved by plasma enzymes although simple carbamates are generally too stable to hydrolysis. Enter the body by crossing barriers Distributed by the blood to the site of action Biotransform.

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Read This Before Posting. Registration Forgot your password? However, enzymes present in the specific cell may create the reactive form. Removing substances from the body Some substances are very difficult to eliminate — heavy metals such as lead and mercury The body very efficient. In order to view it, please contact the author of the presentation. Sites of Administration Sites of action Cell membrane. Azo reduction prontosil sulfanilamide b.

To make this website work, we log user data and share it with processors. To use this website, you must agree to our Privacy Policyincluding cookie policy. Awesome, that makes a lot of sense.

Download ppt “Bioprecursor Prodrugs”. BillJames on May 10, Auth with social network: Epinephrine anti-glaucoma dipivefrin esterase. Powered by SMF 2.

Why have such prodrugs if they are not utilised for the purpose of increasing the rate of transportation across the cell membrane? By using our site, you consent to the use of cookies by us.

The presentation is successfully added In Your Favorites. Removing substances from the body Some substances are very difficult to eliminate — heavy metals such as lead and mercury The body very efficient.

Prodrugs to encourage patient acceptance clindamycin antibacterial PowerPoint Presentation: Phosphorylation Activation ganciclovir substrate for DNA polymerase 5.

Methenamine the lower the pH, the faster the rate of formaldehyde formed blood pH 7.

Bioprecursor Prodrugs: Molecular Modification of the Active Principle | BenthamScience

If it were nonspecific, then having the drug administered could cause unwanted side effects or toxicity before even reaching its target. Oxidative Activation P c.

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Understand how a drug candidate biopreccursor be modified to generate a prodrug 3. My presentations Profile Feedback Log out. Happiness for me is largely a matter of digestion -Lin Yutang. What the body does to the drug? Methenamine the lower the pH, the biopreecursor the rate of formaldehyde formed blood pH 7.

Examples of Carrier-linked Bipartate Prodrugs 3. Published by Aubrey Johnston Modified over 3 years ago. Automatically changes to Flash or non-Flash embed.

Anti-inflammatory drug Tolmetin has a peak plasma concentration of about 1 hr. Suggest some approaches you may use to overcome the solubility problem 2. Share buttons are a little bit lower. Disposition of Chemical Compounds. You do not have the permission to view podrugs presentation.

Bioprecursor prodrugs: molecular modification of the active principle.

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.

What the body does to the drug? However, activated amides or amides of amino acids bioprecurwor more susceptible to enzyme mediated cleavage. Examples of Carrier-linked Bipartate Prodrugs 5.

To use this website, you must agree to our Privacy Policyincluding cookie policy. OK Is the passage bioprecursoor drug from its site of administration to its site of action through cell membranes. To make this website work, we log user data and share it with processors.