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Basic Clinical Pharmacology Bertram, Katzung 15th Edition Summary - Chapter 1 and Chapter 2 $10.49
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Basic Clinical Pharmacology Bertram, Katzung 15th Edition Summary - Chapter 1 and Chapter 2

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Basic Clinical Pharmacology Bertram, Katzung 15th Edition Summary - Chapter 1: Introduction: the nature of drugs & drug development & regulation Chapter 2: Drug receptors & pharmacodynamics

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  • October 11, 2021
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  • 2021/2022
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PHARMACOLOGY
11th October 2021
CHAPTER 1: INTRODUCTION: THE NATURE
OF DRUGS & DRUG DEVELOPMENT &
REGULATION
 Pharmacology can be defined as the study of substances that interact with living
systems through chemical processes.
 Medical pharmacology, which is often defined as the science of substances used to
prevent, diagnose, and treat disease.
 Toxicology is the branch of pharmacology that deals with the undesirable effects of
chemicals on living systems.
 Pharmacogenomics—the relation of the individual’s genetic makeup to his or her
response to specific drugs.


GENERAL PRINCIPLES OF PHARMACOLOGY:
THE NATURE OF DRUGS:
 Drug may be defined as any substance that brings about a change in biologic function
through its chemical actions.
 The drug molecule interacts as an agonist (activator) or antagonist (inhibitor) with a
specific target molecule called (receptor).
 Chemical antagonists may interact directly with other drugs.
 Osmotic agents interact almost exclusively with water molecules.
 Hormones are drugs that are synthesized within the body
 Xenobiotics are chemicals not synthesized in the body
 Poisons are drugs that have almost exclusively harmful effects
 Toxins are poisons of biologic origin

The Physical Nature of Drugs:

 a drug molecule must have the appropriate size, electrical charge, shape, and atomic
composition to be able to interact with its target receptor.
 A useful drug must be able to be transported from its site of administration to its site of
action efficiently

,  A useful drug must be inactivated or excreted from the body at a reasonable rate after
its appropriate action
 Many organic drugs are weak acids and bases
 pH differences in different parts of the body alters the degree of ionization of weak
acids and bases

Drug Size:

 most drugs have molecular weights between 100 and 1000
 To fit only to one type receptor, a drug must be in unique shape, charge and other
properties, and it should be at least 100 MW units in size.
 Drugs larger than 1000 MW do not diffuse readily between body compartments
 Large drugs (e.g., proteins) must be administered directly into the compartment where
they have their effect.

Drug Reactivity & Drug-Receptor Bonds:

 Drugs interact with receptors by means of covalent, electrostatic, and hydrophobic
forces.
o Highly reactive strong covalent bond-forming examples:
 acetylsalicylic acid (aspirin) + cyclooxygenase: in platelets
 DNA-alkylating agents used in cancer chemotherapy
o Electrostatic bond-forming examples:
 Permanently charged ionic molecules
 Weak hydrogen bonds
 Dipole interactions (e.g., Van der Waals forces)
o Hydrophobic bond-forming examples:
 Interactions of highly lipid-soluble drugs
 Interaction of drugs with walls of receptors (pockets)

Drug Shape:

 chirality (stereoisomerism): more than half of all useful drugs are chiral molecule
 because enzymes are usually stereoselective, one drug enantiomer is often more
susceptible than the other to drug- metabolizing enzymes

Rational Drug Design:

 Rational design of drugs implies the ability to predict the appropriate molecular
structure of a drug on the basis of information about its biologic receptor




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