Indications:
- Weak opioids - mild to moderate pain
- Strong opioids - Severe pain
Examples:
Weak opioid analgesics - Codeine, Dihydrocoedeine
Strong opioid analgesics - Morphine, Diamorphone, Pethidine, Fentanyl
Partial/mixed agonist opioids - Buprenorphine, pentazocine
MOA:
- Mimic endogenous opioids - Act on opioid receptors (MOP, KOP, DOP, ORL1)
- Opioids decrease neuronal transmission:
- Decrease opening of voltage dependent Ca channels
- Increase K outflow
- Decreases Ca release from intracellular stores
- Hyperpolarisation = decreased exocytosis of transmitter vesicles
Sites of CNS opioid action:
- PAG - can dampen down behaviours at this level
- Can increase activity where 5HT is being produced - increase descending inhibition
- At the brainstem and periphery - downplay pain transmission
Side effects:
- Cardinal signs - respiratory depression, conscious depression, miosis
- Constipation, nausea and vomitting, anaphylaxis, tolerance and dependancy