Naltrexone (Trexan) is three to five times as potent as naloxone and has a duration of action of 24 to 72 hours, depending on the dose. It is used orally in the treatment of opioid abstinence. Naltrexone exhibits a large firstpass effect in the liver. However, the major metabolite, 6-p-naltrexol, is also a pure opioid antagonist and contributes to the potency and duration of action of nal-trexone. Administration of naltrexone orally blocks the subjective effects of abused opioids and is used to decrease the craving for opioids in highly motivated recovering addicts. However, high doses of the opioids can overcome the naltrexone blockade and lead to seizures or respiratory depression and death. In addition, it has been reported recently that naltrexone can reduce the craving for alcohol in alcoholic patients. Naltrexone also has been used with success in treating apneic episodes in children, an effect hypothesized to be due to blockade of (3-endorphin-induced respiratory depression.
Naltrexone can induce hepatotoxicity at doses only five times the therapeutic dose and should be used with care in patients with poor hepatic function or liver damage. Side effects of the use of naltrexone are more frequently observed than following naloxone administration. Such side effects include headache, difficulty sleeping, lethargy, increased blood pressure, nausea, sneezing, delayed ejaculation, blurred vision, and increased appetite.
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