Receptor Theory

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Receptor Theory

Safety

Certain safety factor

Therapeutic Index

Desensitization

physiological adaptation

altered drug metabolism

exhaustion of mediators

translocation of receptors

altered conformation of receptors

tolerance

Combinations

synergistic/potentiating

additive

Antagonism

chemical

physiological

signaling blockade

pharmacokinetic

allosteric

Potency

effective concentration

effective dose

Quantitative aspects

Drug Receptor interaction

equilibrium dissociation constant

logarithmic

linear

Drug-receptor binding

Activation

governed by efficacy

Occupation

governed by affinity

Drug targets

enzymes

carriers/transport molecules

Ion channels

Membrane receptors

Specificity defined by:

site specificity

ligand specificity

High structural conservation

Paul Ehrlich proposed:

Drugs don’t have any supernatural properties by which their mere presence causes an effect

A drug will not work unless it is bound

Drugs require direct interaction with tissue