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Opioid antagonist
Opioid antagonist
8
Pharmacology
Graduate
06/11/2011

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Cards

Term
Opioid Antagonist characteristics:
Definition
  • Created from a minor structural changes to opioid the agonists.
  • A substitution of a alkyl group for a methly group creates an antagonist.
  • Antagonists displace opioid agonists from mu receptors.
Term
Naloxone (Narcan) characteristics:
Definition
  • Derivative of oxymorphone
  • no agonist properties
  • high antagonist affinity for the mu receptors
  • moderate antagonistic affinity for the kappa receptors.
  • Metabolized in the liver
Term
naloxone (narcan) clinical uses:
Definition
  • Tx of opioid-induced depression of ventilation
  • Tx of opioid-induced depression of ventilation in neonates.
  • Tx of pts at risk of deliberate opioid overdose
  • Used to detect suspected physical  dependence to opioids.
Term
Naloxone (Narcan) dose:
Definition

Dose: Titrate 1-4mcg/kg to desired effect

Onset of Action: IV 1-2min IM/SQ/ETT 2-5min

DOA-Short 30-45min

Clinical Implications: You may need to redose this patient r/t resp. depression and short DOA.

Term
Naloxone (Narcan) side effects:
Definition
  • Reversal of analgesia
    • titrate 40-100mcg at a time to prevent
  • N/V with rapid administration
  • Awakening
  • Sympathetic nervous system activity
  • Withdrawal syndrome
Term
Naltrexone (Revia) Uses:
Definition
Used in the treatment of chronic alcoholism
Term
Nalmefene (Revex)
Definition

Equipotent to naloxone

Dose:15-25mcg IV every 2-5min

Duration of action-longer

Side Effects- same as naloxone 

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