N

retains high binding affinity to the receptor, but no intrinsic activity. It is used to reverse the respiratory depressant effects of opioid overdoses.

Naloxone is administered intravenously with an onset of action within 2 minutes. Because it is competing with the opioid for the receptor sites, the dose and frequency of administration will depend on the amount and type of narcotic being antagonized. Overdoses of long-acting opioids (methadone) may require multiple IV doses of naloxone or continuous infusions. Neonates born to opioid-exposed mothers may be given IV naloxone at birth to reverse the effects of opiates.

Very few metabolism studies on naloxone have been conducted, although the major metabolite found in the urine is naloxone-3-glucuronide.121,122

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