General Flashcards
Define volume of distribution(VD)
Ratio of amount of drug in the body to its concentration in blood
How can a drug have VD 1600/70kg
due to lipid solubility higher concentration in extravascular tissues than blood
Examples of drug with high VD and low VD
High VD >70l/70kg- digoxin, diazepam, b blocker, morphine
Low VD- Lithium, warfarin, aspirin, antibiotics (amoxycillin, cephalexin, gentamicin) frusemide
Difference B/W Efficacy and Potency
Potency- Concentration of drug required to produce 50% of the drug effect.
Efficacy- Maximum effect of the drug regardless of dose.
Phase1 and Phase2 reaction
What organ involved
Phase1- convert the parent drug to more polar metabolite by introduction or unmasking of functional group.
e.g oxidation, reduction
requires mixed function oxidases(MFO) located ER of liver and other tissues(lung, skin).
MFO-cytochrome P450 and NADPH cytochrome P450reductase
Phase2- forms highly polar conjugate by introduction of functional group to drug. e.g Glucoronidation, sulphation
Liver lung
clearance
factors affecting drug clearance
measure of ability of body to eliminate a drug Cl= rate of elimination/concentration
Blood Flow
Specific organ function
dose and bioavailability
difference b/w capacity ltd and flow dependent elimination
Capacity ltd is saturable (zero order kinetics)
Flow dependent is non saturable(1st order)
First Pass Metabolism
Defination
Mechanism
Reduction in drug concentration reaching circulation after absorption mostly from oral route and some from rectal
occurs via liver metabolism, gut wall metabolism bile excretion, portal blood metabolism
factors affecting absorption from oral route
First pass metabolism
Transit time
Absorption
Gut bacteria metabolism
bioavailability
depends on
unchanged amount of drug reaching systematic circulation after been taken from any route.
rate of absorption
first pass metabolism
first pass metabolism
reduction in amount if drug reaching sys circulation after oral ingestion due to gut metabolism, portal blood and liver metabolism, bile excretion
half life
factors affecting
time taken for reduction of the amount of drug by one half during elimination or infusion
those that affect Vd- body mass, fat distribution, malnutrition, oedema
Those that affect CL: renal disease, cardiac disease(Co)
variables affecting drug absorption
route
blood flow
nature of absorbing surface: surface area cell membrane thickness
drug solubility- ionised(water soluble) unionised (lipid sol)
zero order kinetics
constant rate of elimination irrespective of drug concentration but saturable.e capacity limited
first order kinetics
rate of elimination is dependent on amount of drug not saturable