This document discusses prodrugs and analogues. It defines prodrugs as biologically inert derivatives of drug molecules that undergo enzymatic or chemical conversion in the body to release the active drug. The objectives of prodrug design are to improve pharmaceutical properties like solubility, stability and toxicity, as well as pharmacokinetic properties like absorption, metabolism and tissue targeting. Prodrugs are classified as Type I which activate intracellularly or Type II which activate extracellularly. Applications of prodrugs include masking taste/odour, reducing irritation and pain, improving solubility/stability, enhancing bioavailability, preventing presystemic metabolism, prolonging duration, reducing toxicity, and enabling site-specific drug delivery including for chemotherapy.

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

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. 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. 2. Classification of Prodrugs

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. 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. 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. Thanks For Listening