Pharmacodynamics & Pharmacokinetics Flashcards
Bonding can occur through…
In, hydrogen, or van der waals
Acidic drugs bind to…
albumin
Alkalotic drugs bind to..
a-1 acid glycoprotein
Free drugs can
-cross cell membranes
-determine concentration available to receptor (potency)
What decreases plasma proteins
-age
-hepatic disease
-renal failure
-pregnancy
If normal free fraction of drug is 2% and 50% of plasma proteins are lost then free fraction of drug is?
4%
If poor protein binding and lipophilic will have…
-Big volume of distribution
i.e. thiophental, diazepa,
If highly protein bound then…
-low volume of distribution
ex: warfarin
Examples of active metabolites
-diazepam
-propranolol
-morphine
-codeine
How are drugs MAINLY metabolized?
Hepatic microsomal enzymes
Most common CYP 450 enzyme?
CYP3A4
Rate of drug metabolism equation
R= Q(C inflow - C outflow)
Q= cardiac output
C= concentration
Flow limited clearance
CO limits metabolic rate
Capacity limited clearance
liver’s ability to metabolize is limiting factor
Elimination 1/2 time
Time necessary to eliminate 50% of drug from plasma after bolus dose