Introduction to pharmacology Flashcards
The receptor concept
In pharmacology, anything that causes a physiological effect when interacting with a drug is a receptor. The response is a function of the number of occupied receptors.
Agonists
- bind to a receptor and produce a response
- possess affinity and efficacy
- eg. acetylcholine, histamine, TNF
Antagonists
- bind to a receptor but do not produce a response
- prevent agonist binding, blocking the effect
- possess affinity but not efficacy
- may be competitive, irreversible or other
- eg. atropine, etanercept, mepyramine (anti-histamine)
Potency
A measure of drug activity, hence related to affinity.
Affinity
The binding strength of the drug-receptor interaction.
Chemical specificity
Specificity on the side of the drug.
The lock and key hypothesis
The shape of the drug complements the shape of the receptor.
Dissociation constant (KD)
KD is the concentration of agonist at which the receptor is half-maximally saturated.
The relationship between drug concentration and response
- continuous
- saturating
- exhibits a threshold
Hyperbolic on a regular scale, sigmoidal on a logarithmic scale.