Our website is made possible by displaying online advertisements to our visitors.
Please consider supporting us by disabling your ad blocker.
Naloxone
 | This article needs more reliable medical references for verification or relies too heavily on primary sources. (September 2023) |  |
 | |
 | |
| Clinical data | |
|---|---|
| Trade names | Narcan, others |
| Other names | EN-1530; N-Allylnoroxymorphone; 17-Allyl-4,5α-epoxy-3,14-dihydroxymorphinan-6-one, naloxone hydrochloride (USAN US) |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a612022 |
| License data | |
| Pregnancy category |
|
| Routes of administration | Intranasal, intravenous, intramuscular |
| Drug class | Opioid antagonist |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | 2% (by mouth, 90% absorption but high first-pass metabolism) 43–54% (intranasal) 98% (intramuscular, subcutaneous)[12][13] |
| Metabolism | Liver |
| Onset of action | IV: 2 min, IM: 5 min[13] |
| Elimination half-life | 1–1.5 h |
| Duration of action | IN: 30–90 min IV: 45 min IM: 30–120 min |
| Excretion | Urine, bile |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| IUPHAR/BPS | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.006.697 |
| Chemical and physical data | |
| Formula | C19H21NO4 |
| Molar mass | 327.380 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
  (what is this?) (verify) | |
Naloxone, sold under the brand name Narcan among others, is an opioid antagonist, a medication used to reverse or reduce the effects of opioids.[13] For example, it is used to restore breathing after an opioid overdose.[13] Effects begin within two minutes when given intravenously, five minutes when injected into a muscle,[13] and ten minutes as a nasal spray.[14] Naloxone blocks the effects of opioids for 30 to 90 minutes.[15]
Administration to opioid-dependent individuals may cause symptoms of opioid withdrawal, including restlessness, agitation, nausea, vomiting, a fast heart rate, and sweating.[13] To prevent this, small doses every few minutes can be given until the desired effect is reached.[13] In those with previous heart disease or taking medications that negatively affect the heart, further heart problems have occurred.[13] It appears to be safe in pregnancy, after having been given to a limited number of women.[16] Naloxone is a non-selective and competitive opioid receptor antagonist.[6][17] It reverses the depression of the central nervous system and respiratory system caused by opioids.[13]
Naloxone was patented in 1961 and approved for opioid overdose in the United States in 1971.[18][19] It is on the World Health Organization's List of Essential Medicines.[20]
- ^ "Naloxone Use During Pregnancy". Drugs.com. 2 September 2019. Archived from the original on 25 April 2020. Retrieved 13 May 2020.
- ^ Cite error: The named reference
doi 10.5694/mja15.01181was invoked but never defined (see the help page). - ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
- ^ "Frequently Asked Questions: Access to naloxone in Canada (including Narcan Nasal Spray)". Health Canada. 6 July 2016. Archived from the original on 16 August 2021. Retrieved 16 August 2021.
- ^ "Naloxone 400 micrograms/ml solution for Injection/Infusion – Summary of Product Characteristics (SmPC)". (emc). 6 February 2019. Archived from the original on 4 August 2020. Retrieved 13 May 2020.
- ^ a b Cite error: The named reference
Narcan FDA labelwas invoked but never defined (see the help page). - ^ "Evzio- naloxone hydrochloride injection, solution". DailyMed. 1 February 2018. Archived from the original on 8 October 2020. Retrieved 5 October 2020.
- ^ "Zimhi- naloxone hydrochloride injection, solution". DailyMed. 29 September 2022. Archived from the original on 7 January 2023. Retrieved 7 January 2023.
- ^ Cite error: The named reference
Kloxxado FDA labelwas invoked but never defined (see the help page). - ^ "Narcan- naloxone hydrochloride nasal spray". DailyMed. 8 August 2023. Retrieved 5 September 2024.
- ^ "Rivive- naloxone hydrochloride spray". DailyMed. 10 January 2024. Retrieved 5 September 2024.
- ^ Ryan SA, Dunne RB (May 2018). "Pharmacokinetic properties of intranasal and injectable formulations of naloxone for community use: a systematic review". Pain Management. 8 (3): 231–245. doi:10.2217/pmt-2017-0060. PMID 29683378.
- ^ a b c d e f g h i "Naloxone Hydrochloride". The American Society of Health-System Pharmacists. Archived from the original on 2 January 2015. Retrieved 2 January 2015.
- ^ McDonald R, Lorch U, Woodward J, Bosse B, Dooner H, Mundin G, et al. (March 2018). "Pharmacokinetics of concentrated naloxone nasal spray for opioid overdose reversal: Phase I healthy volunteer study". Addiction. 113 (3): 484–493. doi:10.1111/add.14033. PMC 5836974. PMID 29143400.
{{cite journal}}: CS1 maint: overridden setting (link) - ^ "Naloxone DrugFacts". National Institute on Drug Abuse. 1 June 2021. Archived from the original on 6 January 2022. Retrieved 5 January 2022.
- ^ "Prescribing medicines in pregnancy database". Australian Government. 3 March 2014. Archived from the original on 8 April 2014. Retrieved 22 April 2014.
- ^ Cite error: The named reference
NHM-Naloxone pharmacologywas invoked but never defined (see the help page). - ^ Yardley W (14 December 2013). "Jack Fishman Dies at 83; Saved Many From Overdose". The New York Times. Archived from the original on 15 December 2013. Retrieved 6 July 2015.
- ^ US patent 3493657, Jack Fishman & Mozes Juda Lewenstein, "Therapeutic compositions of n-allyl-14-hydroxy - dihydronormorphinane and morphine", published 1970-02-03, issued 1970-02-03, assigned to Mozes Juda Lewenstein Archived 7 December 2022 at the Wayback Machine
- ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
Previous Page Next Page
