ナロキソン

使用用途

• Opioid reversal
• Neonatal opioid reversal (following caesarian sections)
• Adjunctive treatment of hyperthermia
• Opioid overdose / reversal
• Opioid overdose / reversal
• Prolonged opioid antagonism
• Opioid reversal
• Limit increases in locomotor activity secondary to narcotic agonists
• Treatment of opioid gastrointestinal tract dysfunction
• Opioid reversal in rodents
• Opioid reversal in rabbits
• Opioid reversal in hamsters, gerbils, mice, rats, guinea pigs, chinchillas
• Opioid reversal

投与方法

考えられる副作用

• Reversal of analgesia (return of pain)
• Acute withdrawal syndrome in opioid-dependent patients
• CNS excitement (especially if used in meperidine overdose)
• Seizures (at very high doses, likely secondary to GABA antagonism)
• Acute severe discomfort or pain (due to sudden loss of analgesia)
• Antanalgesic effects in opioid-naïve subjects
• Transient elevation of unconsciousness (at low doses)

注意事項と禁忌

• Hypersensitivity to naloxone
• Indiscriminate use in animals that have undergone major surgery or trauma (due to severe pain from analgesia reversal)
• > **Important Warning:** The duration of action of naloxone (45-90 minutes) is often shorter than the opioid it is reversing. Patients may slip back into respiratory depression and require re-dosing or continuous ventilatory support. - Use with caution in animals with preexisting cardiac abnormalities. - Use cautiously in opioid-dependent animals or those that have received exceedingly large doses of narcotics, as it may precipitate an acute withdrawal syndrome. - **Meperidine Toxicity:** Naloxone is reportedly not effective for reversing meperidine-induced seizures and may elicit CNS excitement if normeperidine excitotoxicity is present. Avoid unless severe respiratory depression is present without ventilatory support. - **Buprenorphine:** Naloxone is not a good reversal agent for buprenorphine due to buprenorphine's high receptor affinity; massive doses (100X usual) may be required.

薬物相互作用

• Opioid partial-agonists (butorphanol, pentazocine, nalbuphine): Naloxone may antagonize the effects of these agents (respiratory depression, analgesia). It should not be relied upon to treat respiratory depression caused by buprenorphine.
• Clonidine: Naloxone may reduce the hypotensive and bradycardic effects of clonidine; potentially useful for clonidine overdoses.
• Yohimbine: Naloxone may increase the CNS effects of yohimbine (anxiety, tremors, nausea, palpitations) and increase plasma cortisol levels.
• Opioid Agonists (e.g., Morphine, Methadone, Fentanyl): Naloxone reverses the analgesic, sedative, and respiratory depressant effects of opioid agonists.
• Buprenorphine: Buprenorphine binds tightly to opioid receptors; naloxone may not fully reverse its effects or may require much higher doses.

よくある質問