Drug action Flashcards
1
Q
Examples of non-selective physicochemical drugs
A
- Bicarbonate as an antacid
- Osmotic laxatives/diuretics
2
Q
Four receotor types, from fastest to slowest
A
- Ligand gated ion channels ms
- G protein couples receptors sec-min
- Catalytic receptors min-hr
- Nuclear receptirs (hours-days)
3
Q
An example of G protein coupled receptor
A
Nicotinic receptor - fast synaptic transmission
- Acetylcholine; NAChR; Na+; depolarisation
4
Q
Other GPCR targeting drugs
A
- B-blockers
- Anti-muscarinics
- Dyspepsia (H2)
- Antipsychotics
- Anti-viral (CCR-5)
5
Q
Examples of adrenoceptor subtypes
A
6
Q
How do catalytics rceotors work
A
- Have an enzyme activated by hormone binding
- Tyrosine kinase receptors for growth factors
- A kinase phosphorylates target protein
- Adaptor proteins notice this; signals
- Tyrosine kinase receptors for growth factors
Diabetes- insulin receptor
Cancer - EGFR
7
Q
How do nuclear receptors function?
A
By transcription factors e.g. steroid hormones from oestrogen receptor activation
Asthma - corticosteroids
Cancer - tamoxifen
8
Q
A framwork for drug-receptor interactions
A
9
Q
Agonist vs Antagonist
A
10
Q
Formula for receptor occupancy
A
Where KD is dissasosciaton consant
If D equals its KD half of receptors are cocupied i.e. the KD of a drug is the concentration need to occupy 50% of receptors at equilibrium
11
Q
A
