Ch. 5: Pharmacodynamics Flashcards
Dose-Response Relationships
- between size of an administered dose and intensity of response produced
- determines: min. amount of drug to be used, max. response a drug can elict, how much to increase dosage to produce desired increase in response
- as dosage increases, response becomes progressively largers
- treatment is tailored by increasing or decreasing dosage until desire intensitity
- 3 phases
Max Efficacy and Relative Potency
max efficacy: largest effect drug can produce (height of curve), match intensity of responses with patient’s need, very high max is not always most desirable
relative potency: amount that must be given to elict response, rarely an important characterisitic of drug, can be important if a lack of potency forces inconveniently large doses, refers to dosage needed to produce effects
Drug-Receptor Interactions
- receptor refers to body’s own receptors for hormones, neurotransmitters, and other regulatory molecules
- usually reversible
- regulated by endogenous compounds
- it will mimic or block action of endogenous regulatory molecules and increase/decrease rate normally controlled by that receptor
4 Primary Receptor Families
- cell membrane-embedded enzymes
- ligand-gated ion channels
- G protein ion channels
- transcription factors
Selectivity of Drug Action
- more selective= fewer side effects
Affinity and Intrinsic Activity
- strength of the attraction
- ability of drug to activate a receptor upon binding
Agonist, Antagonist, and Partial Antagonist
- activate receptors, endogenous regulators, have affinity and high intrinsic activity, make process go faster or slower
- preventing receptor activation by endogenous regulatory molecules and drugs, affinty but no intrinsic activity, no effects, if no agonist present an antagonist will have no observable effect
- can do both actions, moderate intrinsic activity
Noncompetive vs. Competitive Antagonist
- bind irreversibly t receptors, reduce max. response that an agonist can elicit (fewer receptors), impact not permanent (breaking down old receptors and making new ones)
- compete with agonists for receptors, bind reversibly to receptors, equal affinity= receptor occupied by whichever agent is present in the highest concentration
Regulation of Receptor Sensitivity
- continuous exposure to agonist= desensitized or refractory
- continuous exposure to antagonist= hypersensitive