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naloxone (Narcan, Evzio, ReVive)

Tradename: Narcan, Evzio. 1st generic approved April 2019. [14] Indications: - opioid overdose - opioid-induced respiratory depression - opioid abuse - patients taking > 50 mg equivalents of morphine/day - clonidine overdose - alcohol-induced coma - acute ethanol intoxication (lethargy, respiratory depression) Dosage: - 0.01 mg/kg or 0.4-2.0 mg or more IV/IM/SC/ET - start 0.4 mg - increase to 1.0 mg in a few minutes if response inadequate - escalate dose every few minutes as needed [5,6] Injection: 0.4 mg/mL (1.0 mL), 1 mg/mL (2 mL) Injection (neonatal): 0.02 mg/mL (2 mL) Autoinjector: Evzio; 0.4 mg - dispensed as kit with two auto-injectors & 1 trainer Nasal spray [11] not as effective as intramuscular injections [17] - NEJM video on intranasal naloxone admininstration [18] - ReVive nasal spray, 3 mg OTC [20] Storage: 1-2 year expiration date unfounded; good for 20 years [16] Pharmacokinetics: 1) minimal activity when given orally 2) onset of action a) 1-2 minutes when given IV b) 2-3 minutes when given SC or IM 3) 1/2life 60 minutes 4) metabolized by the liver 5) eliminated in the urine Adverse effects: - common (1-10%) - sweating, hypotension, hypertension, tachycardia, ventricular arrhythmias, insomnia, irritability, anxiety,rash, nausea/vomiting, blurred vision, narcotic withdrawal tremor, mydriasis Laboratory: - naloxone in serum/plasma - naloxone in urine Mechanism of action: - competitive antagonist of - mu opioid receptor - delta opioid receptor - kappa opioid receptor Notes: - information on prescribing naloxone & nalxone rescue kits [8] - user friendly naloxone FDA-approved for use by caregivers [9] - 2014 cost of autoinjector kit Evzio = $600 - laws allowing pharmacists to directly distribute naloxone may reduce fatal opioid overdoses, but may increase in emergency department visits for nonfatal opioid overdoses [15]

General

morphinan opioid receptor antagonist or narcotic antagonist

Properties

INHIBITS: opiate MISC-INFO: elimination route LIVER KIDNEY 1/2life 1 HOUR pregnancy-category B safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill, pg 515
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. Medical Knowledge Self Assessment Program (MKSAP) 16, 18 American College of Physicians, Philadelphia 2012, 2018.
  6. Dahan A, Aarts L, Smith TW. Incidence, Reversal, and Prevention of Opioid-induced Respiratory Depression. Anesthesiology. 2010 Jan;112(1):226-38 PMID: 20010421
  7. Deprecated Reference
  8. Prescribe to Prevent. Prescribe Naloxone, Save a life. http://prescribetoprevent.org/
  9. FDA News Release: April 3, 2014 FDA approves new hand-held auto-injector to reverse opioid overdose. First naloxone treatment specifically designed to be given by family members or caregivers. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm391465.htm
  10. Prescriber's Letter 21(7): 2014 New Naloxone Auto-Injector (Evzio) for Suspected Opioid Overdose Detail-Document#: 300719 (subscription needed) http://www.prescribersletter.com
  11. Brown T FDA Approves Narcan Nasal Spray to Treat Opioid Overdose. Medscape Oncology. Mov 18, 2015 http://www.medscape.com/viewarticle/854716
  12. NEJM Knowledg+ Question of the Weeks. Dec 11, 2018 https://knowledgeplus.nejm.org/question-of-week/4142/
  13. Brooks M FDA Moves to Fast-Track OTC Naloxone for Opioid Overdose. Medscape - Jan 17, 2019. https://www.medscape.com/viewarticle/907885
  14. FDA News Release. April 19, 2019 FDA approves first generic naloxone nasal spray to treat opioid overdose. https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm636333.htm
  15. Abouk R, Pacula RL, Powell D. Association between state laws facilitating pharmacy distribution of naloxone and risk of fatal overdose. JAMA Intern Med 2019 May 6 PMID: 31058922 https://jamanetwork.com/journals/jamainternalmedicine/fullarticle/2732118
  16. Pruyn S, Frey J, Baker B et al Quality Assessment of Expired Naloxone Products from First-Responders' Supplies. Prehosp Emerg Care. 2019 Sep-Oct;23(5):647-653. PMID: 30596290
  17. Dietze P, Jauncey M, Salmon A et al Effect of Intranasal vs Intramuscular Naloxone on Opioid Overdose. A Randomized Clinical Trial. JAMA Netw Open. 2019;2(11):e1914977 PMID: 31722024 https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2755306
  18. Ortega R, Nozari A, Baker W et al Videos in Clinical Medicine: Intranasal Naloxone Administration. N Engl J Med 2021; 384:e44. March 25 PMID: 33761209 https://www.nejm.org/doi/full/10.1056/NEJMvcm2020745
  19. AMA Morning Rounds. March 30, 2023 American Medical Association - DePeau-Wilson M FDA OKs First OTC Product for Reversing Opioid Overdoses. Make the product accessible with "an affordable price," says FDA Commissioner. MedPage Today March 29, 2023 https://www.medpagetoday.com/publichealthpolicy/fdageneral/103767 - Ault A FDA Approves OTC Naloxone, but Will Cost Be a Barrier? Medscape. March 29, 2023 https://www.medscape.com/viewarticle/990249
  20. FDA News Release. July 28, 2023 FDA Approves Second Over-the-Counter Naloxone Nasal Spray Product https://www.fda.gov/news-events/press-announcements/fda-approves-second-over-counter-naloxone-nasal-spray-product
  21. U.S. Department of Health & Human Services. December 2018. Naloxone: the opioid reversal drug that saves lives. How healthcare providers and patients can better utilize this life-saving drug. https://www.hhs.gov/opioids/sites/default/files/2018-12/naloxone-coprescribing-guidance.pdf.

Component-of

buprenorphine/naloxone (Bunavail, Suboxone) naloxone/oxycodone (Targiniq ER) naloxone/pentazocine (Talwin NX)