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CHAPTER 1 (DRUG DESIGN (Able to predict the appropriate molecular…
CHAPTER 1
DRUG DESIGN
Able to predict the appropriate molecular structure of a drug on the basis of information about its biologic receptor
A constant research is underway for the development of drug which can complete the requirement of receptor
Drug were developed through random testing of chemicals or modification of already known drugs that have effects.
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DRUG DEVELOPMENT
First step in the development of new drug is the discovery of a potential new drug compound/elucidation of a new drug target
Seek an understanding of the drug's interaction with its biologic targets:
- Increased efficacy, potency and selectivity
Testing needed:
- In vitro studies, relevant biologic effects, drug metabolism, pharmacokinetic profiles, toxicological and safety characterizations in animal studies
- Approval from FDA -> Clinical trials
PHARMACOLOGY
Pharmacokinetics
- Uptake (absorption)
- Transport (distribution)
- Metabolism & Transformation
- Eliminate
- Description of what rate a chemical will enter the body and what happens to it once it is in the body
Pharmacodynamics
- Binding
- Interaction
- Induction of therapeutic effects
- Describes the dynamic interactions of drugs with biological targets and its biological effects
- What drugs does to the body
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NATURE OF DRUGS
Chemical Nature
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May be synthesized within the body. Or maybe chemicals not synthesized in the body or known as xenobiotics
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Physical Nature
May be solid at RT (aspirin), liquid (codein),
or gaseous (nitrous oxide)
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Drug Size
- Varies to very small to very large
- Common drugs between (100-1000 MW)
- Drugs larger than 1000 MW can't move
- Freely between compartments in the body
- Administered directly
Drug Shape
- To have a good fit to only 1 type of receptor, a drug
molecule must be unique in SHAPE and CHARGE
- Specific shape to permit binding to its receptor site
via the bonds
- More than half common drugs are chiral molecules
Drug Reactivity
- Drugs react with receptors by means of chemical forces or bonds:
i. Covalent
ii. Electrostatic
iii. Hydrophobic