Pethidine Flashcards
1
Q
What is Pethidine
A
- Meperidine
- a synthetic opiate agonist
- kappa-opiate receptor agonist with
2
Q
What is Pethidine used for
A
- recommended for relief of moderate to severe acute pain
- local anesthetic effects
3
Q
Morphine vs Pethidine in terms of duration and onset of action
A
The onset of action is more rapid than morphine, but has a shorter duration of action.
4
Q
which one out of Morphine and Pethidine has a greater affinity for the kappa-receptor
A
Meperidine
5
Q
what are opiate receptors coupled with
A
G-protein receptors
6
Q
what do G-protein receptors activate
A
activate adenylate cyclase and the production of cAMP
7
Q
what do opioids do?
A
- Opioids decrease intracellular cAMP by inhibiting adenylate cyclase
- .the release of the nociceptive neurotransmitters substance P, GABA, dopamine, acetylcholine and noradrenaline and the hormones vasopressin, somatostatin, insulin and glucagon is inhibited
8
Q
what can receptors can opioids open and close? and what effects does this have
A
- opioids can close N-type voltage-operated calcium channels (OP2-receptor agonist)
- can open calcium-dependent
- inwardly rectifying potassium channels (OP3 and OP1 receptor agonist)
- resulting in reduced neuronal excitability.