Key Definitions Flashcards
Drug
The active ingredient of a medicine; any substance which interacts with a biological system and changes it
Pharmacology
The study of the mechanism of drug action
Potency
The dose of drug required to produce a specific effect of given intensity as compared to a standard reference.
Agonist
- Bind to a receptor and produce a response
* Possess affinity and efficacy:- ACh, histamine
Antagonist
- Antagonists:- Bind to a receptor but do not produce a response
- Competitive antagonists prevent agonist binding and so prevent (block)the response to an agonist
- Possess affinity but not efficacy (atrophine, mepyramine)
Affinity
•The affinity of a drug for its receptors is a measure of how well it binds to the receptor. The affinity can be measured using a drug’s dissociation constant (Kd). This is equal to the concentration at which, at equilibrium, half the receptors will be bound with a drug.
Efficacy
- Efficacy is a measure of the degree to which an agonist produces a response when binding a given proportion of receptors.
- For a full agonist, the efficacy is 1; for a partial agonist, the efficacy is less than 1 (but greater than 0)
- In some cases, it is possible to have a negative efficacy, in which case the drug is called an inverse agonist. Such drugs inhibit any intrinsic activity of a receptor that might exist in the absence of a ligand.
Inverse agonist
In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist.
Quantitative pharmacology
Based on the assumption that drugs act by entering into a simple chemical relation with certain receptors in cells and that there is a simple relation between the amount of drug fixed and by these receptors and the action produced.
Positive allosteric effect
receptor more likely to open in response to a given concentration of GABA
Pharmacokinetics
The study of the change in drug and metabolite concentrations in tissues and body fluids
Absorption
Movement of a drug from the point of administration to the plasma
Distribution
from plasma to tissues and organs. How drugs equilibrate within the body after entering the systemic circulation
Bioavailability
Fraction of unchanged drug that reaches the systemic circulation
Volume of distribution
The volume of fluid required to contain the total amount of drug in the body at the same concentration as that present in the plasma