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Prodrugs and analogues

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Topic:
Prodrugs and analogues
Name:
Ali Zia
Roll No:
Bsf-1702570
Semester:
8th(Morning)

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Prodrugs
• The term prodrug, introduced in 1958 by Adrien Albert, relates to “Biologically
inert derivatives of drug molec...

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1.Objectives of Prodrug Design
• There are three basic, overlapping objectives in prodrug research:
1. 1. Pharmaceutical O...

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Prodrugs and analogues

  1. 1. Topic: Prodrugs and analogues Name: Ali Zia Roll No: Bsf-1702570 Semester: 8th(Morning)
  2. 2. Prodrugs • The term prodrug, introduced in 1958 by Adrien Albert, relates to “Biologically inert derivatives of drug molecules that undergo an enzymatic and/or chemical conversion in vivo to release the pharmacologically active parent drug.” • A class of drugs, the pharmacologic action of which results from conversion by metabolic processes within the body (biotransformation). • The idea of prodrugs in cancer therapy is to reduce unintended side effects by designing compounds that interact with specific targets.
  3. 3. 1.Objectives of Prodrug Design • There are three basic, overlapping objectives in prodrug research: 1. 1. Pharmaceutical Objectives:  To improve solubility, chemical stability, and organoleptic properties  To decrease irritation and/or pain after local administration,  To reduce problems related with the pharmaceutical technology of the active agent. 1. 2. Pharmacokinetic Objectives:  To improve absorption (oral and by non-oral routes).  To decrease presystemic metabolism to improve time profile.  To increase organ/ tissue-selective delivery of the active agent. 1. 3. Pharmacodynamic Objectives:  To decrease toxicity and improve therapeutic index.  To design single chemical entities combining two drugs (co-drugs) strategy.
  4. 4. 2. Classification of Prodrugs
  5. 5. 3. Novel Classification  Type I Prodrugs are bioactivated inside the cells (intracellularly). Examples of these are anti-viral nucleoside analogs that must be phosphorylated and the lipid-lowering statins.  Type II prodrugs are bioactivated outside cells (extracellularly), especially in digestive fluids or in the body's circulation system. Analogue • An analogue is referred to as a drug that is structurally changed. An analogue is normally accepted as being that modification which brings about a carbon-skeletal transformation or substituent synthesis. • For example: oxytetracycline, chlortetracycline etc.
  6. 6. 4. Applications of Prodrugs 1. Pharmaceutical applications Masking Taste or Odour Reduction of gastric irritation Reduction in Pain at Site of Injection Enhancement of drug solubility and dissolution rate Enhancement of chemical stability
  7. 7. 2. Pharmacokinetic Applications Improvement of Bioavailability Prevention of Presystemic metabolism Prolongation of duration of action Reduction Local and Systemic Toxicity of Drugs Site specific drug delivery Site specific Drug Delivery in Chemotherapy
  8. 8. Thanks For Listening

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