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Physicochemical Properties of Drugs in relation to Drug Action. Roselyn Aperocho Naranjo, RPh, MPH USPF, College of Pharmacy rose_may26@yahoo.com. Understanding the Modern Drug Design. Modern chemical techniques Recent knowledge on disease mechanisms & receptor properties

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physicochemical properties of drugs in relation to drug action

Physicochemical Properties of Drugs in relation to Drug Action

Roselyn Aperocho Naranjo, RPh, MPH

USPF, College of Pharmacy

rose_may26@yahoo.com

understanding the modern drug design
Understanding the Modern Drug Design
  • Modern chemical techniques
  • Recent knowledge on disease mechanisms & receptor properties
  • Transportation of drugs in the body
  • Distribution of drug through different compartments
  • Metabolism of drugs in the liver and other organs
  • Structural characteristics of the receptor
  • Acid-base chemistry
  • Availability of the computer software that determines the three-dimensional shape of the receptor in order to design new molecules that will give optimum fit to the receptor
history general

Crude extracts

Plant Source

Specific Plants are selected

Treatment

for medical conditions

History: General
history general4

Crude extracts

Plant Source

Specific Plants are selected

Treatment

for medical conditions

History: General

Structure of Natural products

Selective changes in the molecule

selected molecules are changed due to
Selected molecules are changed due to:
  • Reduction of undesirable pharmacologic response of the drug (side-effect)
  • Obtain better drug response
  • Alter drug’s metabolism
  • Produce more cheaper and competitive supply of the product
selected molecules are changed due to6
Selected molecules are changed due to:

Example:

Morphine

Cocaine

Addiction effect

reduced

Analgesic effect

enhanced

Local Anesthetic Effect

enhanced

CNS effects

reduced

medicinal chemistry in 1900 s
Medicinal Chemistry in 1900’s
  • Phenothiazines – first synthesized as ANTIHISTAMINES

- Careful investigation led to discover its

TRANQUILIZING PROPERTYfor the

mentally ill patient.

  • Benzodiazepines – originated from an expected ring

enlargement which resulted it to

become a CNS RELAXANT

overview

drug

receptor

Drug-receptor complex

Overview

Pharmacologic response

drug distribution
Drug Distribution
  • Oral Administration
drug distribution11
Drug Distribution
  • Oral Administration
        • Solubility depends on:
          • Chemical Structure
          • Size of particles
          • Surface area
          • Nature of crystal form
          • Type of tablet coating
          • Type of tablet matrix
drug distribution12
Drug Distribution

PRODRUG- inactive form but are easily metabolized in the liver to become active

  • Oral Administration
        • Example:
          • CHLORAMPHENICOL
  • CHLORAMPHENICOL PALMITATE
protein binding14
Protein Binding
  • Can affect the drug’s effective solubility, biodistribution, half-life in the body and interaction with other drugs.
  • Control access to certain body compartments
  • Prolong the drug’s duration of action
  • Limit the amount of drug available for biotransformation and interaction with specific receptor sites.
tissue depot
Tissue Depot
  • Fats in the body which can be a storage for drugs
  • The more Lipophilic the drug is, the more it will stay in the tissue
      • Example:
          • Thiopental
statistical prediction of pharmacological activity
Statistical Prediction of Pharmacological Activity
  • Mathematical Model will explain many chemical processes

Three goals in Drug Design

  • Predict biological activity in untested compounds
  • define the structural requirements required to fit to a specific receptor
  • design a test set of compounds

Quantitative-Structure- Activity relationship (QSAR)

slide18
QSAR
  • Proposed by Crum-Brown and Fraser in 1865 to 1870
  • Certain modification in the molecular structure of a poisonous compound produces an important differences in their action
topological descriptors
Topological Descriptors
  • Alternate method in describing molecular structure which is based on graph theory using the bonds that connects between atoms
combinatorial chemistry
Combinatorial Chemistry

…to be continued

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