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Naloxone

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🔗 MergedComparePsychonautWikiPharmacologyDrugCentralDailyMed

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Classification
Class / category
Also known as
NaloxoneNarcanEvzio
Safety
Addiction potentialnot habit-forming
Dose · Insufflated
Common1–4 mg
Dose · Intramuscular
Common0.4–2 mg
Dose · Intravenous
Common0.4–2 mg
Dose · Oral
Threshold4 mg
Light4–8 mg
Common8–16 mg
Strong16–28 mg
Heavy28 mg+
Duration
Onset0–10 minutes
Total30–60 minutes
After-effects1–12 hours
Pharmacology
Receptor activity
OPRD1OPRK1OPRM1ADORA3Ccr5CYP2D6
Half-lifeThe mean half life of naloxone hydrochloride is 1.8-2.7 hours intranasally, 1.4 hours intramuscularly, and 1.2 hours intravenously. In neonates, the mean half life is 3.1 ± 0.5 hours. The mean plasma half-life of naloxone was 1.28 hours following IM or subcutaneous injection of naloxone hydrochloride using an auto-injector, compared with 1.36 hours following IM or subcutaneous injection using a standard syringe. The half-life of naloxone has been reported to be 30-81 minutes in adults and about 3 hours in neonates. Plasma naloxone levels were determined by RIA over a period of 6--36 hr in three groups of neonates, (1) those given 35 microgram iv (n = 6), (2) those given 70 microgram iv (n = 6) and (3) those given 200 microgram im (n = 17) naloxone HCl within 1 min of birth. After intravenous administration of 35 and 70 microgram of naloxone peak levels of 4--15 ng/mL and 9--20 ng/mL respectively were reached in 5--40 min and the mean plasma half-life after both doses was 3.1 +/- 0.5 hr.
Protein bindingNaloxone is approximately 45% bound to albumin, but there is significant binding to other proteins.

PsychonautWiki summary

Experts now advise that anyone using street drugs—and those around them—should carry naloxone, as opioids are increasingly found contaminating the drug supply. Having naloxone on hand can save lives by reversing overdoses, even if opioids were not intentionally consumed.[1] Summary sheet: Naloxone

Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.