Toxicity, Opioids Medication

  • Author: Everett Stephens, MD; Chief Editor: Asim Tarabar, MD   more...
 
Updated: Nov 19, 2010
 

Medication Summary

Naloxone is a pure competitive antagonist of opioid receptors and lacks any agonist activity. Adverse effects are rare at therapeutic doses. Naloxone can be given IV, ET, IL, or IM. The use of intranasal naloxone has also been reported. By the ET, IV, or IL route, the onset of action of naloxone is 1-2 minutes. A second dose can be repeated every 2-3 minutes. Discontinue treatment as soon as the desired degree of opioid reversal is achieved. Higher doses may be necessary to reverse 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. In theory, nalmefene may be useful for persons with opiate addiction who accidentally overdose on heroin but refuse to stay for continued observation after an initial reversal dose of naloxone. However, this practice can be fatal to the patient who is discharged and is trying to use an excessive dose of opioids in order to overcome the effects of nalmefene and experience dysphoria. The routine use of this agent is not recommended.

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Antidotes for narcotic agonists

Class Summary

These agents reduce or eliminate the effects of opioid agents on their receptors.

View full drug information

Naloxone (Narcan)

 

Historically, the most commonly used opioid receptor antagonist in the United States. Used to reverse opioid intoxication. Prevents or reverses opioid effects (hypotension, respiratory depression, sedation), possibly by displacing opiates from their receptors. Half-life is 1 h.

If patients do not respond to multiple doses of naloxone, consider alternative causes of unconsciousness.

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Contributor Information and Disclosures
Author

Everett Stephens, MD  Assistant Clinical Professor, Department of Emergency Medicine, University of Louisville

Everett Stephens, MD is a member of the following medical societies: American Academy of Emergency Medicine

Disclosure: Nothing to disclose.

Specialty Editor Board

Mark Louden, MD, FACEP  Assistant Medical Director, Emergency Department, Duke Raleigh Hospital

Mark Louden, MD, FACEP is a member of the following medical societies: American Academy of Emergency Medicine and American College of Emergency Physicians

Disclosure: Nothing to disclose.

John T VanDeVoort, PharmD  Regional Director of Pharmacy, Sacred Heart & St. Joseph's Hospitals

John T VanDeVoort, PharmD is a member of the following medical societies: American Society of Health-System Pharmacists

Disclosure: Nothing to disclose.

Michael J Burns, MD  Instructor, Department of Emergency Medicine, Harvard University Medical School, Beth Israel Deaconess Medical Center

Michael J Burns, MD is a member of the following medical societies: American Academy of Clinical Toxicology, American College of Emergency Physicians, American College of Medical Toxicology, and Society for Academic Emergency Medicine

Disclosure: Nothing to disclose.

John D Halamka, MD, MS  Associate Professor of Medicine, Harvard Medical School, Beth Israel Deaconess Medical Center; Chief Information Officer, CareGroup Healthcare System and Harvard Medical School; Attending Physician, Division of Emergency Medicine, Beth Israel Deaconess Medical Center

John D Halamka, MD, MS is a member of the following medical societies: American College of Emergency Physicians, American Medical Informatics Association, Phi Beta Kappa, and Society for Academic Emergency Medicine

Disclosure: Nothing to disclose.

Chief Editor

Asim Tarabar, MD  Assistant Professor, Director, Medical Toxicology, Department of Emergency Medicine, Yale University School of Medicine; Consulting Staff, Department of Emergency Medicine, Yale-New Haven Hospital

Disclosure: Nothing to disclose.

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