naloxone (Narcan, Evzio, ReVive)
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Introduction
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
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
- minimal activity when given orally
- onset of action
- 1/2life 60 minutes
- metabolized by the liver
- eliminated in the urine
elimination via liver
elimination via kidney
1/2life = 1 hour
Adverse effects
- common (1-10%)
Laboratory
Mechanism of action
- competitive antagonist of
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]
More general terms
Component of
- naloxone/oxycodone (Targiniq ER)
- naloxone/pentazocine (Talwin NX)
- buprenorphine/naloxone (Bunavail, Suboxone)
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill, pg 515
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Jump up to: 5.0 5.1 Medical Knowledge Self Assessment Program (MKSAP) 16, 18 American College of Physicians, Philadelphia 2012, 2018.
- ↑ Jump up to: 6.0 6.1 Dahan A, Aarts L, Smith TW. Incidence, Reversal, and Prevention of Opioid-induced Respiratory Depression. Anesthesiology. 2010 Jan;112(1):226-38 PMID: https://www.ncbi.nlm.nih.gov/pubmed/20010421
- ↑ Deprecated Reference
- ↑ Jump up to: 8.0 8.1 Prescribe to Prevent. Prescribe Naloxone, Save a life. http://prescribetoprevent.org/
- ↑ Jump up to: 9.0 9.1 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
- ↑ Prescriber's Letter 21(7): 2014 New Naloxone Auto-Injector (Evzio) for Suspected Opioid Overdose Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=300719&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Jump up to: 11.0 11.1 Brown T FDA Approves Narcan Nasal Spray to Treat Opioid Overdose. Medscape Oncology. Mov 18, 2015 http://www.medscape.com/viewarticle/854716
- ↑ NEJM Knowledg+ Question of the Weeks. Dec 11, 2018 https://knowledgeplus.nejm.org/question-of-week/4142/
- ↑ Brooks M FDA Moves to Fast-Track OTC Naloxone for Opioid Overdose. Medscape - Jan 17, 2019. https://www.medscape.com/viewarticle/907885
- ↑ Jump up to: 14.0 14.1 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
- ↑ Jump up to: 15.0 15.1 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: https://www.ncbi.nlm.nih.gov/pubmed/31058922 https://jamanetwork.com/journals/jamainternalmedicine/fullarticle/2732118
- ↑ Jump up to: 16.0 16.1 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: https://www.ncbi.nlm.nih.gov/pubmed/30596290
- ↑ Jump up to: 17.0 17.1 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: https://www.ncbi.nlm.nih.gov/pubmed/31722024 https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2755306
- ↑ Jump up to: 18.0 18.1 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: https://www.ncbi.nlm.nih.gov/pubmed/33761209 https://www.nejm.org/doi/full/10.1056/NEJMvcm2020745
- ↑ 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 - ↑ Jump up to: 20.0 20.1 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
- ↑ 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.