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study of the biochemical and physiologic effects of drugs and the molecular mechanisms by which those effects are produced.
Dose Response Relationship
relationship between the size of an administered dose and the intensity of the response produced
What does it mean that the dose response relationship is "graded?"
patients response gets more intense with increased dosage
largest effect a drug can produce
- the amount of drug given to elicit an effect
- a potent drug gives its effects in low doses
- Drug A can be more effective than drug B even though drug B may be more potent.
What are arguably the most important receptors?
hormones, neurotransmitters, and other regulatory molecules.
What are the 4 primary receptor families?
- 1,Cell membrane–embedded enzyme.
- 2, Ligand-gated ion channel.
- 3, G protein–coupled receptor system (G = G protein).
- 4, Transcription factor.
highly desirable characteristic of a drug, in that the more selective a drug is, the fewer side effects it will produce
What are 2 instances that a drug will be non selective?
- when a drug interacts with a receptor type that regulates multiple processes
- when a drug interacts with multiple receptors
- Strength of attraction between its drug and receptor
- *drugs with high affinity are very potent
- *drugs with high affinity are effective in low doses
- ability of a drug to activate its receptor upon binding
- *Drugs with high intrinsic activity have high maximal efficacy
- Drugs that mimic the body's own regulatory molecules
- agonists activate the receptor
- have high affinity
- have high intrinsic activity
- Drugs that block the actions of endogenous regulators are called antagonists.
- Lack of intrinsic activity results in lack of receptor activity
The effect of a antagonist is determined by
how much agonist is present
What are competitive antagonists?
- produce a receptor blockade by competing with agonists.
- the receptor is occupied by whichever agent is in higher concentration.
- an agonist with moderate intrinsic activity.
- Maximal effect is lower than a full agonist
- can act as agonists (if no full agonist is present) & antagonists (if a full agonist is present)
(Refractoriness) results from continuous exposure of cell receptors to an agonist
Results from continuous exposure of cell receptors to antagonist
Average effective dose
(ED 50) dose required to produce a defined therapeutic response in 50% on the population.
ED50:LD50 ratio between average effective dose & average lethal dose
Wide Therapeutic Index
Narrow Therapeutic Index