Naloxone

Naloxone
Chemical Nomenclature
Common names	Naloxone, Narcan, Evzio
Substitutive name	1-N-Allyl-14-hydroxynordihydromorphinone
Systematic name	(4R,4aS,7aR,12bS)-4a,9-Dihydroxy-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one
Class Membership
Psychoactive class	Opioid (Antagonist)
Chemical class	Morphinan
Routes of Administration
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section. ⇣ Oral Dosage Threshold 4 mg Light 4 - 8 mg Common 8 - 16 mg Strong 16 - 28 mg Heavy 28 mg + Duration Total 1 - 2 hours Onset 5 - 15 minutes Come up 20 - 40 minutes Peak 1 - 2 hours Offset 30 - 60 minutes After effects 1 - 12 hours ⇣ Insufflated Dosage Common 1 - 4 mg Duration Total 30 - 60 minutes Onset 0 - 10 minutes ⇣ Intramuscular Dosage Common 0.4 - 2 mg Duration Total 30 - 60 minutes Onset 0.25 - 2 minutes ⇣ Intravenous Dosage Common 0.4 - 2 mg Duration Total 30 - 60 minutes Onset 0.25 - 2 minutes DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.
Interactions

Summary sheet: Naloxone

Naloxone, commonly sold under the brand names Narcan and Evzio, is an opioid antagonist used to reverse the effects of an opioid overdose. Like many substances that act on the opioid receptors, naloxone has a morphinan backbone. Naloxone is used be emergency responders and law enforcement to immediately reverse the effects of opioid overdoses. Naloxone is sold under the brand name Narcan as a nasal spray and Evzio as an auto-injector with voice instructions. Nalaxone and naltrexone have also bee researched in the treatment of depersonalization disorder with promising results.

Naloxone has been credited with saving an unprecedented number of opioid overdose victims. This is partially due to naloxone programs in several countries to give naloxone to people who use opioids, and the rapid deployment of naloxone by law enforcement agencies and emergency medical services.

Chemistry

Chemically, naloxone is similar in structure or many opiates and semi-synthetic opioids. Naloxone is extremely similar in structure to oxymorphone. Whereas oxymorphone has methyl group bonded to the nitrogen, naloxone has an allyl group, which is a moiety that often makes opioid agonists into opioid antagonist. The chemical formula of naloxone is C₁₉H₂₁NO₄ and has a molar mass of 327.38g per mole.

Pharmacology

Naloxone acts as a potent μ-opioid receptor inverse agonist. Because of its high affinity for the μ-opioid receptor, it knocks other ligands out of the receptor. Naloxone also has a lower affinity as a κ-opioid receptor and δ-opioid receptor. If naloxone is administered without previous administration of opioids, it has few biological effects, notably a lower pain threshold. Naloxone has two isomers, (+)naloxone and (-)naloxone, with the latter being active. Naloxone is metabolized by the liver. Naloxone has very low oral bioavailability which is why it is administered intravemously, intramuscularly or intranasally. Small amounts of naloxone are often added to opioids like buprenorphine and pentazocine to prevent abuse. Naloxone ha been noted to block a placebo based analgesic effect. For example, if an individual has been administered something that they were told was morphine and had a analgesic response to it, naloxone will block that response.

Subjective effects

This subjective effects section is a stub. As such, it is still in progress and may contain incomplete or wrong information. You can help by expanding or correcting it.

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.

When taken by itself without the presence of other substances or an opioid overdose, nalaxone induces relatively comfortable sedating effects and general emotion suppression.

Physical effects

• Sedation - Nalaxone is considerably sedating. It can result in the user feeling sleepy and having difficulty keeping their eyes open.

Cognitive effects

• Emotion suppression - The emotion suppression found on nalaxone is noticeably similar to the same experience found within antipsychotics although without the accompanying analysis suppression and thought deceleration.
• Identity alteration - Nalaxone has been demonstrated by a pilot study to signifigantly reduce the symptoms of chronic long term depersonalization. Within this study, 11 patients received single doses (1.6 or 4 mg i.v.) and three others received multiple infusions, with the maximal dosage being 10 mg, and the effect of naloxone on symptom severity was then measured and determined. In most cases, the first signs of improvement were recorded soon after the naloxone infusions (within 20–40 min) and the patients’ perception of the world was marked by greater brightness. A complete reduction or disappearance of depersonalization occurred within the interval of 1–4 h and, in some patients, continued for as long as 12–24 h. This was followed by some deterioration, although the depersonalization never recurred to the initial level. Five patients showed evidence of a stable improvement.

Toxicity and harm potential

Naloxone in the form it is used by emergency medical services and law enforcement.

Naloxone is not known to be addictive or cause psychological or physical dependence. When naloxone is administered in an opioid overdose, the individual will go through immediate withdrawal. Opioid withdrawal may be life threatening in serious cases. Symptoms of opioid withdrawal may include, but are not limited to agitation, nausea, psychosis, temperature regulation suppression, anxiety, physical fatigue, excessive yawning, sweating, dehydration, and pupil dilation. It has been noted that naloxone may be needed in higher dosages depending on the opioid that was consumed. It is not uncommon for several doses of naloxone in cases of fentanyl or acetylfentanyl overdoses. If an individual does not have opoioids in their system when naloxone is administered, naloxone may rarely cause dehydration and nausea.

It is strongly recommended that one use harm reduction practices when using this drug.

Legal issues

Throughout the world, naloxone is not considered a controlled substance. In most countries, it is a prescription drug.

• Australia: In Australia, naloxone is considered an over the counter drug and is available at most pharmacies
• Canada: In Canada, naloxone kits are distributed at many emergency rooms and clinics.
• United States: At a federal level, naloxone is a prescription drug. Many states have programs that make naloxone over the counter and available at request at most pharmacies. In the United States, most jurisdictions have programs to deploy naloxone to law enforcement and fire and rescue services.
• United Kingdom: In the United Kingdom, naloxone is considered a Prescription Only Medicine.

See also

• Responsible use
• Heroin
• Fentanyl
• Opioids
• Codeine
• Morphine