pharmacodynamics Flashcards
pharmacodynamics
what the drug does to the body and how they do it; the study of biochemical and physiologic actions of drugs and the molecular mechanisms by which those effects are produced.
dose response relationship
the relationship between the size of an administered dose and the intensity of the response produced; the minimum amount of drug needed to elicit a response and the maximum response a drug can elicit, how much to increase the dosage to increase the response
drug responses are…
graded-patient response gets more intense with increased dosing
efficacy
maximum efficacy: largest effect that a drug can produce
potency
amount of drug given to elicit an effect. a potent drug produces its effects at low doses
efficacy and potency
two drugs can be equally effective but have different potency
drug receptors
chemical sites in the body that drugs interact with to produce effects-make selective drug action happen. drugs either mimic or block the action of the body’s own regulatory molecules; do NOT give cells new functions; drugs produce their therapeutic effects by helping the body use its pre-existing capacities
drug receptors and selectivity: what happens when a drug interacts with one type of receptor that regulates only few processes?
the effects of the drug will be limited
drug receptors and selectivity: what happens when a drug interacts with a receptor type that regulates multiple processes?
the drug is likely to elicit a variety of responses
drug receptors and selectivity: what happens when a drug interacts with multiple receptors?
it will elicit a variety of responses
affinity
strength of attraction between a drug and its receptor
high affinity drugs have…
high affinity drugs have a strong attraction for receptor sites. they are very potent
low affinity drugs need…
low affinity drugs need to be present in high concentrations to elicit a response
intrinisic activity
the ability of a drug to activate a receptor upon binding
high intrinsic activity
drugs with high intrinsic activity have high maximal efficacy and produce and intense response
agonists
activate receptors; have high affinity and intrinsic activity. they mimic action of endogenous regulators
antagonists
they prevent receptor activity: high affinity but no intrinsic activity. they bind to receptors but do not cause receptor activation. they block actions of endogenous regulatory molecules or drugs
response to an antagonist is determined by
how much agonist is present
types of antagonists
noncompetitive antagonists and competitive antagonists
noncompetitive antagonsits
bind irreversibly to receptors and decrease the total number of receptors available for binding
competitive antagonists
produce receptor blockage by competing with agonists. if both have equal affinity then the receptor is occupied by whichever agent is higher in concentration
partial agonists
an agonist with moderate intrinsic activity. produces less effect than a full agonist
example of partial agonists
pentazocine (a partial agonist) and meperidine (a full agonist)- better pain relief with meperidine
regulation of receptor sensitivity: desensitization
desensitization (refractoriness) results from continuous exposure of cell receptors to an agonist: the cell is less responsive + implications for drug tolerance