Pharmacodynamics Flashcards
Action of DRUG on the body
Pharmacodynamics
Maximal effect an agonist can produce if the dose is taken to very high levels
Maximal Efficacy (Emax)
determined by the NATURE of receptor
Denotes the amount of drug needed to produce a given effect
Dose that produces in 50% of the max effect
Potency (EC50
determined by the AFFINITY of the receptor
Drug concentration VS response
Graph of DOSE VS EFFECT
GRADED dose response
Emax
EC50
Drug concentration VS fraction POPULATION that responds at each dose against log of dose administered
Graph of DOSE VS response in a POPULATION
QUANTAL dose response
ED50 (therapeutic effect)
TD50 (toxic effect)
LD50 (lethal effect)
Measure which relates the DOSE of DRUG required to produced a DESIRED EFFECT to that which produces an undesired effect
Therapeutics Index = TD50/ED50
Drug capable of fully activating the effector system when it binds to the receptor
Full Agonist
Acts as inhibitor in the presence of an agonist
Partial Agonist
Blocks or dampens drug response in the presence of an agonist
Antagonist
Antagonist Classification
Pharmacologic
- Competitive (reversible)
- Non-competitive (irreversible)
Physiologic
Chemical
Bind to receptor very close to the agonist receptor site without activating the effector
Competitive or Reversible Antagonist
Atenolol and Salbutamol
Acts at an ALLOSTERIC STE of the receptor
Binds to different receptor
Alters the configuration of the agonist receptor
Non-competitive or Irreversible Antagonist
Inhibition by DIRECT interaction with a drug
Does NOT depend on interaction with receptors
Chemical Antagonists
Dimercaprol for lead poisoning
Pralidoxime for organophosphate poisoning
Binds to a different receptor that has the capacity of producing an effect opposite to that produced by the drug that it is antagonizing
Physiologic Antagonist
Histamine and Epinephrine
TACHYPHYLAXIS
frequent or continuous exposure to agonists often results in SHORT TERM DIMINUTION of the receptor response
Metoclopramide Ephedrine Dobutamine LSD Calcitonin Nitroglycerin Nicotine Hydralazine Desmopressin