Lecture 5-6 Flashcards
T or F: Majority of the lipid-soluble compounds are reabsorbed in the tubular.
True. because lipid-soluble compounds can easily pass through plasma membranes.
How to calculate the total body clearance?
CL= CLrenal+CLhep+CLother
How much time it take to eliminate the biological activity of the drug?
4 times the half-life
First order kinetics
Constant fraction metabolized per unit of time.
Elimination directly proportional to its plasma concentration & dependent on its half-life.
Half-life
is 50% of the active drug that disappear from the plasma in a amount of time.
Zero order kinetics
Constant amount metabolized per unit of time.
T or F: First order kinetics will sometimes switch over to zero order kinetics.
True. Because you no longer have the spare enzymes to metabolize the drug. ex. overdose condition (enzyme are not abundant enough or too saturated)
T or F: The standard for reaching the steady state is >4 half-life.
True. it starts to cycle within a reasonable steady state. Always take the same time to plateau.
4 types of drug receptors
Ion channels
G-protein coupled receoptor
Enzyme-linked receptors (Tyrosine Kinase receptors)
intracellular receptors
T or F: GPCRs are mainly involved in drugs acting on the ANS (adrenergic receptor)
True.
LGICs and GPCRs subtypes focus on this class
LGICs: Nicotinic GABA Glutamate Serotonin
GPCRs:
Opioid
Kd is
affinity constant (concentration of drug that bind half of the receptors.)
Low Kd is high or low affinity?
High affinity (bc need least concentration of the drug to bind to the half of the receptor)
Potency vs Efficacy
Potency is the amount of drug needed to produce an effect of a given magnitude.
Efficacy is the maximal effect produced by the drug.
T or F: a partial agonist could become a full agonist if there are enough spare receptors
True.
