The dose-response relationship Flashcards
(23 cards)
What is pharmacology
the branch of medicine and biology concerned with the study of drug action
What is an agonist
A drug or endogenous hormone that occupies and activates a receptor to produce a biological response
What is a drug (2)
- A substance that causes a change in the biological functions of cells and tissues through its actions
- The majority of drugs work on receptors
What is affinity
the tendency of the drug/hormone to bind to the receptor to form a Drug-Receptor Complex
What is efficacy/intrinsic activity
the ability of the drug to trigger a pharmacological response after forming a Drug-Receptor Complex
What effect does a full agonist have on affinity and intrinsic activity
High Affinity & High Intrinsic Activity
What effect does a partial agonist have on affinity and intrinsic activity (3)
- Low Affinity & High Intrinsic Activity
- High Affinity & Low Intrinsic Activity
- Low Affinity & Low Intrinsic Activity
What effect does an antagonist have on affinity and intrinsic activity
High Affinity & No Intrinsic Activity
What is the receptor theory
The magnitude of the biological response to a drug (agonist) is proportional to the number of drug-receptor interactions that occur
What is the dose-response relationship (2)
- As a dose increases, the concentration of drug able to interact with the receptor increases
- the maximum biological response occurs when all receptors that can be occupied are occupied by a drug
What is drug efficacy (2)
- Maximum response a drug can produce
- Emax
What is drug potency (3)
- Measure of drug needed for a biological response
- Half the maximum biological response
- ED50
What effect do partial agonists have on Emax
Produces biological response but not 100% of it even at high doses
What impact do agonists have on receptor activity
has independent impact on receptor activity
What impact do antagonists have on receptor activity
impacts receptor activity in the presence of agonist
What impact do inverse agonists have on receptor activity (2)
- Independent impact on receptor activity
- Produces opposite effect to agonist
What is an antagonist
A drug that occupies a receptor but does NOT produce a biological response (may block or hinder the action of agonists)
What are the 2 types of antagonists (2)
- Competitive (reversible)
- Non-competitive (irreversible)
How do competitive antagonists work (2)
- Compete with agonists for the same receptor
- Make agonists look less potent
How do non-competitive antagonists work (3)
- Bind to receptors permanently (covalent)
or - Block the agonist binding site
- Reduce Emax that an agonist can produce
What is the therapeutic index (3)
- Measure of drug safety
- higher therapuetic index is safet than low
- LD50 is the dose that kills 50% of animals receiving it (lethal dose )
What are examples of drugs with a low therapeutic index (3)
- Lithium
- Digoxin
- Warfarin
What does it mean if a drug is more potent than the other (2)
- The drug has a lower ED50
- meaning less drug is needed to reach half Emax than the other