Opioid antagonists (centrally active)
- Block central opioid receptors
- Naloxone: rapid overdose reversal
- Naltrexone: OUD/AUD relapse prevention
- Nalmefene has prolonged antagonist action
- Can precipitate abrupt withdrawal
- Naltrexone requires opioid-free interval
- No analgesia while receptor blockade is active
Class at a glance
- Block central opioid receptors
Members / distinctions
- Naloxone: rapid overdose reversal
- Naltrexone: OUD/AUD relapse prevention
Pharmacology
- Nalmefene has prolonged antagonist action
- No analgesia while receptor blockade is active
Practical pearls
- Naltrexone requires opioid-free interval
Other practical pearls
- Can precipitate abrupt withdrawal
Self-check
- What interval is required before naltrexone?
An opioid-free interval. - What distinguishes Nalmefene?
Prolonged antagonist action.
Drugs in this class (4)
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