What is the role of medications in the treatment of opioid toxicity?

Updated: Jul 19, 2021
  • Author: Everett Stephens, MD; Chief Editor: Jeter (Jay) Pritchard Taylor, III, MD  more...
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Naloxone is a pure competitive antagonist of opioid receptors and lacks any agonist activity. Adverse effects are rare at therapeutic doses. Effects of withrawal may follow administration, and may be confused as adverse effects by the the layperson. Naloxone can be given by the intravenous (IV), intramuscular (IM), endotracheal (ET), subcutaneous (SC), or intranasal (IN) route. IN naloxone has the advantage of posing no risk of needlestick injury. [56]

By the IV or ET route, the onset of action of naloxone is 1-2 minutes. A second dose can be repeated every 2-3 minutes. With IM, SC, or IN administration, onset is 2-5 minutes. Discontinue treatment as soon as the desired degree of opioid reversal is achieved. Higher doses may be necessary to reverse the effects of methadone, diphenoxylate, propoxyphene, butorphanol, pentazocine, nalbuphine, designer drugs, or veterinary tranquilizers.

Nalmefene (Revex) and naltrexone are newer opioid antagonists that have longer half-lives than naloxone (4-8 h and 8-12 h vs 1 h). The routine use of a long-acting antagonist in the patient who is unconscious for unknown reasons is not recommended. In addition, the fear of precipitating prolonged opioid withdrawal likely prevents the widespread use of these antagonists for emergency reversal of opiate intoxication.

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