Pharmacology Flashcards
Define drug efficacy
the measure of drug response elicited by a particular drug
Define drug potency
the measure of the concentration of drug required to elicit a certain response
What characteristics would you expect of a drug with a very low volume of distribution (Vd)?
large, charged, plasma protein-bound, hydrophillic
What relative volume of distribution would you expect of a small, hydrophobic, uncharged drug?
large Vd
Are acidic or basic drugs more likely to be reabsorbed in the DCT (pH 5.4)?
With pH below 7.4, the equilibrium tends towards HA and HB+, meaning the uncharged acidic drugs are more likely to be reabsorbed
What are the main mechanisms of Phase I metabolic reactions?
Transformations into a more polar molecule; redox, hydrolysis
What are the two most important P450 oxidases in Phase I reactions?
CYP3A4 “workhorse”
CYP2D6 “bottleneck”
What are the main mechanisms of Phase II metabolic reactions?
conjugations (sulfation, methylation, acetylation, glucoronidation)
What is the main result of a drug going through a Phase II metabolic reaction?
Water soubility is typically enhanced to the point of secretion into urine and excreted from body
What are 3 examples of zero-order elimination drugs?
Aspirin, Phenytoin, Ethanol