Pharmacology Flashcards
pharmacokinetics?
how the body affects the drug; Absorption, Distribution,
Metabolism and Excretion (ADME)
pharmacodynamics ?
how the drug affects the body
receptor types?
ligand gated ion channels (eg, nicotinic ACh), G coupled receptors (eg, beta adrenoceptors), kinase linked receptors (eg, GF) and cytosolic receptors (eg, steroids)
potency?
measure of how well a drug works
affinity?
how well a ligand binds to the receptor
efficacy?
how well a ligand activates the receptor?
antagonists have 0 efficacy
isoprenaline?
non-selective beta adrenoceptor agonist so it activates B1 in the heart and B2 in the lungs
salbutamol
selective B2 adrenoceptor agonist
eg of enzymes as drug targets?
NSAIDS that inactivate COX responsible for the breakdown of
arachidonic acid to prostaglandin H2
(aspirin irreversibly blocks the active site)
transporters as drug targets eg?
PPI (omeprazole) irreversibly inhibit proton pump
ion channels as drug targets eg?
CCB eg, amlodipine
bio-availability?
amount of drug taken up as a proportion of the amount
administered
aspirin in the gut?
Aspirin is acidic
• In the stomach the acidic tablet dissolves but it then becomes less
ionised due to the fact that a weak acid (such as aspirin) becomes less ionised in lower pH and movement of un-ionised aspirin across gut is rapid.
which molecules are distributed where?
Proteins/large molecules are only active in the plasma compartment (5L) eg, warfarin
- Water soluble molecules are active in plasma and interstitial compartment
(5L + 15L) eg, NSAIDS
- Lipid soluble molecules are only active in the intracellular fluid (45L) eg, paracetamol
volume of distribution equation?
Volume of distribution = Total amount of drug in body ➗ Concentration
of drug in plasma
clearance?
The volume of plasma that can be completely cleared of drug per unit
time (mls minute-1 (ml/min))
water soluble v larger molecules in kidney elimination?
Water soluble molecules which pass through the glomerular endothelia
gap are eliminated by glomerular filtration
• Larger water soluble molecules can be eliminated by active tubular
secretion
hepatic extraction ratio?
The proportion of drug removed by one passage through the liver
phase I reaction - where do they occur?
95% of phase I reactions are in liver smooth endoplasmic
reticulum
what is phase 1 reactions?
make the drug more hydrophilic so that it can be excreted by the kidneys - it does this by adding a hydroxyl group to the drug