Drug targets Flashcards
what are pharmacokinetics
what the body does to the drug
what are 4 aspects of pharmacokinetics
Absorption, Distribution, Metabolism, Excretion
what are pharmacodynamics
what the drug does to the body - drug action
4 aspects that keep a drug in plasma
- large
- charged
- bind to plasma proteins
- transported by passive diff
2 aspects of drugs that get into extracellular compartments
- small
2. polar
type of drugs that get into cells
hydrophobic
how do most drugs work
bind to cell surface receptors
5 protein drug targets
- ion channels
- membrane bound receptors
- enzymes
- intracellular receptors
- pumps and transporters
3 non-protein drug targets
- lipids
- ions
- water
rank bond strengths
van de waals<covalent
3 features of covalent bonding drugs
- share e pair
- irreversible
- effects last long time after drug taken
what is an agonist
- affinity for receptor that causes cell changes
2. intrinsic activity
what is antagonist
- affinity for receptor but doesn’t make change
- no intrinistc effects
- make change by attenuating agonist effects
4 major receptor families
- ligan gated ion channel- lets ions in
- GCPR - 2ndry messenger system
- enzyme linked
- intracellular receptor
what is fastest mech
ion channels
how does ion channel receptor work
- ligand bind
- confomational change in protein lets in ions
- changes actions within cell
second fastest and why
GPCR - has a couple more steps
how do enzyme linked receptors work
- have cystolic enzyme activity, so when bound create more or less of an enzyme
duration of enzyme drugs
minutes to hours
how do intracellular receptors work
- hydrophobic ligands enter the cell
- binds to receptor and moves to DNA
- binding to specific DNA sequence leads to changes in DNA transcription
onset and duration of intracellular
onet in 30mins, hour to days of duration
2 types of binding
reverssible or irreversible
