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Naloxone

From Wikipedia
naloxone
type of chemical entity
Subclass ofmorphinan alkaloid Edit
Get useMedication Edit
Stereoisomer of(+)-Naloxone, (+)-naloxone Edit
Chemical formulaC₁₉H₂₁NO₄ Edit
Canonical SMILESC=CCN1CCC23C4C(=O)CCC2(C1CC5=C3C(=C(C=C5)O)O4)O Edit
Isomeric SMILESC=CCN1CC[C@]23[C@@H]4C(=O)CC[C@]2([C@H]1CC5=C3C(=C(C=C5)O)O4)O Edit
Active ingredient inNarcan, Evzio Edit
World Health Organisation international non-proprietary namenaloxone, naloxonum Edit
Found insyd taxonPapaver somniferum Edit
Medical condition treatedopiate dependence, septic shock, opioid overdose Edit
Physically dey interact plusOpioid receptor, mu 1 Edit
Route of administrationintravenous infusion and defusion, intramuscular injection, subcutaneous injection Edit
Pregnancy categoryAustralian pregnancy category B1, US pregnancy category C Edit
Subject has roleopioid antagonist, essential medicine, antidote Edit

Naloxone, dem sell under de brand name Narcan among odas, be an opioid antagonist, a medication dem use to reverse anaa reduce de effects of opioids.[1] For example, dem dey use am to restore breathing after an opioid overdose.[1] Effects dey begin within two minutes wen dem give intravenously, five minutes wen dem inject into a muscle,[1] den ten minutes as a nasal spray.[2] Naloxone blocks the effects of opioids for 30 to 90 minutes.[3][4]

Administration to opioid-dependent individuals fi cause symptoms of opioid withdrawal, wey dey include restlessness, agitation, nausea, vomiting, a fast heart rate, den sweating.[1] To prevent dis, dem fi give small doses every few minutes til dem reach de desired effect.[1] Insyd those plus previous heart disease anaa wey dey take medications wey negatively dey affect de heart, na further heart problems occur.[1] Der be limited data on naloxone ein safety during pregnancy.[5] Naloxone be a non-selective den competitive opioid receptor antagonist.[6][7] E dey reverse de depression of de central nervous system den respiratory system wey be caused by opioids.[1][4][8]

Na dem patent naloxone insyd 1961 wey dem approve am for opioid overdose insyd de United States insyd 1971.[9][10] E dey on de World Health Organization's List of Essential Medicines.[11]

References

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  1. 1 2 3 4 5 6 7 "Naloxone Hydrochloride". The American Society of Health-System Pharmacists. Archived from the original on 2 January 2015. Retrieved 2 January 2015.
  2. ↑ McDonald R, Lorch U, Woodward J, Bosse B, Dooner H, Mundin G, Smith K, Strang J (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.
  3. ↑ "Naloxone DrugFacts". National Institute on Drug Abuse. 1 June 2021. Archived from the original on 6 January 2022. Retrieved 5 January 2022.
  4. 1 2 Saari TI, Strang J, Dale O (April 2024). "Clinical Pharmacokinetics and Pharmacodynamics of Naloxone". Clinical Pharmacokinetics. 63 (4). Springer Nature: 397–422. doi:10.1007/s40262-024-01355-6. PMC 11052794. PMID 38485851.
  5. ↑ "Naloxone and Pregnancy". MotherToBaby. Brentwood, TN: Organization of Teratology Information Specialists (OTIS). March 2024. Retrieved 25 November 2025.
  6. ↑ "Narcan- naloxone hydrochloride spray Narcan- naloxone hydrochloride spray". DailyMed. 7 October 2019. Archived from the original on 30 January 2016. Retrieved 12 May 2020.
  7. ↑ Malenka RC, Nestler EJ, Hyman SE (2009). Sydor A, Brown RY (eds.). Molecular Neuropharmacology: A Foundation for Clinical Neuroscience (2nd ed.). New York: McGraw-Hill Medical. pp. 190–191, 287. ISBN 978-0-07-148127-4. Products of this research include the discovery of lipophilic, small-molecule opioid receptor antagonists, such as naloxone and naltrexone, which have been critical tools for investigating the physiology and behavioral actions of opiates. ... A competitive antagonist of opiate action (naloxone) had been identified in early studies. ... Opiate antagonists have clinical utility as well. Naloxone, a nonselective antagonist with a relative affinity of μ > δ > κ, is used to treat heroin and other opiate overdoses.
  8. ↑ Handal KA, Schauben JL, Salamone FR (July 1983). "Naloxone". Annals of Emergency Medicine. 12 (7). Elsevier Inc.: 438–445. doi:10.1016/s0196-0644(83)80343-6. PMID 6309038.
  9. ↑ 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.
  10. ↑ 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
  11. ↑ 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.

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