basics of pharmacology (schmidt) Flashcards
pharmacodynamics
analysis of the biological effect, what the drug does to the body
pharmacokinetics
analysis of their fate in the body, what the body does to the drug
topical administration
local administration at a specific site
polarity and charge determine:
central effect (blood brain barrier can be crossed), peripheral effect (blood brain barrier cannot be crossed)
albumin
albumin slows down drug release by binding to it
pre-systemic elimination
first-pass effect, causes low systemic load
digoxin
steroid backbone, in the plasma membrane, treating heart failure
atropine
most important competitive antagonist of the muscarinic ACh receptors
concentration binding curves
the curve decreases in steepness because less binding sites are available when more drug is bound
agonist
mimetic drug that has intrinsic activity, induces a biological response
antagonist
blocker, lytic drug and has no intrinsic activity, occupies receptor
intrinsic activity
causes higher efficacy of a drug, so full agonist has higher efficacy
functional antagonism
two agonists induce an opposite effect via activation of different receptors
competitive antagonism
two agonists compete for the same receptor (atropine and propranolol)
M3 receptor
muscarinic receptor, can bind Gq
Gq protein
can bind to a receptor, activating PLC
Phospholipase C (PLC)
activated by Gq protein and causes generation of IP3 and DAG from PIP2.
calmodulin
changes when binding CA2+ allowing it to regulate the activity of many target proteins
DAG
lipid produced by the cleavage of inotisol phospholipids in response to extracellular signals. helps activate PKC
PKC
activated by DAG and an increase in the concentration of cytosolic CA, once activated phosphorylates target proteins
cAMP
activator of PKA upon ATP binding, causing relaxation
ion channels
act very fast, causes hyperpolarisation or depolarisation, depending on the ion
G protein coupled receptors
g proteins activate or inhibit, slower than ion channels because conformational change happens
hyperpolarisation
potassium is leaving the cell, which decreases its activity