mechanism of drug action Flashcards
What is an agonist?
chemical that binds to and activates a receptor to produce a biological response
What is an antagonist?
blocks the actions of an agonist
What is a quantal response?
An all or nothing response
What are constitutively active receptors?
receptors that have a background activity even when an agonist is not present
What is the Two-State Model of Receptors?
- receptors can be active or resting
- under baseline circumstances, most receptors remain in the resting state
What are some targets for drug action?
- ion channels
- enzymes
- carrier molecules
- receptors
What are some type of receptors that are targets for drug action?
- type 1: ligand gated ion channels
- type 2: G-protein coupled receptors
- type 3: enzyme-linked and related (kinase-linked)
- type 4: nuclear ‘intracellular’ receptors
Give an example of a drug that directly interacts with ion channels?
- lidocaine can block them in nerves
- local anaesthetic
How does aspirin work on enzymes to treat pain?
- enzyme cyclo-oxygenase (COX) converts arachidonic acid into prostaglandins (PGs) which mediate pain and inflammation
- aspirin (acetyl-salicylic acid) targets COX and inhibits its activity
- reduce generation of inflammatory prostaglandins
Give an example of a ‘loop-diuretic’ drug and how does it work
- furosemide used to increase urine production by blocking Na+K+2Cl- transporter
What is GABA?
- gamma-aminobutyric acid
- predominant inhibitory neurotransmitter in the brain
How does GABA inhibit things?
- interacts with GABAa receptor on Cl- channel
- allows Cl- to enter cell
- makes depolarisation difficult
- stabilises tissue
Describe the cAMP pathway in G-protein coupled receptors?
- Gs activated (Gi does opposite)
- adenylate cyclase (AC) activated, converts ATP to cAMP
- cAMP is second messenger, causes physiological response
Describe the calcium pathway in G-protein coupled receptors?
- Gq activated
- activated phospholipase C (PLC)
- activates IP3 and DAG
- they increase Ca2+ levels
What are some examples of physiological beta 2 receptor antagonists?
- noradrenaline
- adrenaline