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What Is A Drug?: Chapter 1: Drugs and Drug Targets - Overview

This document provides an overview of drugs and drug targets. It defines a drug as any compound that interacts with a biological system to produce a biological response. The main molecular targets for drugs are proteins and nucleic acids. Drugs bind to these macromolecules through transient intermolecular interactions like hydrogen bonding, electrostatic interactions, and Van der Waals forces, or through covalent bonds. The energy required for a drug to displace water molecules and bind to its target must be lower than the energy gained from binding interactions, otherwise the drug may not be effective. Pharmacokinetics studies how the body affects a drug, while pharmacodynamics studies how drugs interact with their targets.

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35 views1 page

What Is A Drug?: Chapter 1: Drugs and Drug Targets - Overview

This document provides an overview of drugs and drug targets. It defines a drug as any compound that interacts with a biological system to produce a biological response. The main molecular targets for drugs are proteins and nucleic acids. Drugs bind to these macromolecules through transient intermolecular interactions like hydrogen bonding, electrostatic interactions, and Van der Waals forces, or through covalent bonds. The energy required for a drug to displace water molecules and bind to its target must be lower than the energy gained from binding interactions, otherwise the drug may not be effective. Pharmacokinetics studies how the body affects a drug, while pharmacodynamics studies how drugs interact with their targets.

Uploaded by

koji
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Chapter 1: Drugs and Drug Targets Overview

What is a drug?
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Drug: Any compound that interacts with a biological system to create a biological response
Heroine is used as a medication under diamorphine; reduces pain to tolerable levels and produces
euphoric effect to counteract depression
There is no such thing as good and bad drugs, it all depends on the dosage. i.e., arsenic is well
known as a poison, however in the correct dosages it is used as antifungal/antiprotozoal agent
Therapeutic Index: Measure of the drugs beneficial effects at a low dose versus its harmful effects
at a high dose
Tubocurarine is the active ingredient in curare that is used to relax muscles in surgical operations
ACE inhibitors are cardiovascular drugs that are derived from snake venom

Cell Structure
-

The outer cell membrane consists of phosphatidylcholine whereas the inner cell membrane
consists of phosphatidylethanolamine, phosphatidylserine, and phosphatidylinositol

Drug Targets
-

The main molecular targets for drugs are proteins (enzymes, receptors, transport proteins) and
nucleic acids (DNA and RNA)
Drugs bind to macromolecules at binding sites through transient intermolecular interactions,
whereas some become permanently attached through covalent bonds (200-400kJ/mol)
Pharmacodynamics: The study of how drugs interact with their targets through binding
interactions and produce a pharmacological effect

Intermolecular Bonds:
-

Electrostatic (20-40kJ/mol) > Hydrogen (16-60kJ/mol) > Van der Waals (2-4kJ/mol) > Dipoles

The Role of Water and Hydrophobic Interactions


-

The energy required to desolvate both the drug and the binding site must be lower than the
stabilization energy gained by the binding interactions, otherwise the drug may be ineffective
This can be accomplished by removing polar groups, which lowers the energy of desolvation
In other cases, polar groups are added to increase the water solubility of certain drugs, but are
positioned in such a way that they protrude from the binding site when the drug binds, resulting in
no energy penalty

Pharmacokinetics

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