kinetics/dynamics Flashcards
michaelis-Menton eq
V=(Vmax*[S])/(Km+[S])
Km (inverse of affinity/potency)
[S] at which V=1/2 Vmax. inversely related to affinity. [E[ has no effect. increased by competitive reversible inhibitors.
Vmax (efficacy)
Vmax=k2*[E]. V when [S]»»Km. [S] has no effect. decreased by competitive irreversible and non-competitive inhibitors.
Lineweaver-Burke plot
verticle: 1/Vmax
horizontal: 1/-Km or 1/[S].
inhibitors: competitive cross, noncompetitive do not.
`substrate limited
[S]c dependent, first order.
enzyme imited
[S]»>Km. con’c independent. zero order.
volume of distribution
Vd= amount of drug in body/plasma drug con’c
half life
T1/2= 0.693*Vd/ CL
Clearance
CL= rate of eliminating drug/plasma drug con’c
loading dose
=target plasma con’c * Vd/ bioavailability
maintenance dose
= target plasma con’c * CL * dosage interval / bioavailability
therapeutic index
TD50/ED50= median toxic dose/median effective dose. higher is safer.