Naloxone

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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 a synthetic mu-opiod antagonist of the morphinan chemical class that is widely used to reverse the effects of an acute opioid overdose. Many emergency responders and law enforcement are trained to administer naloxone to reverse the effects of opioid overdoses immediately. Naloxone is sold under the brand name Narcan as a nasal spray and Evzio as an auto-injector with voice instructions.

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.

Besides their use in emergency medicine, both naloxone and naltrexone have also been researched in the treatment of depersonalization disorder with promising results.

Chemistry

This chemistry section is incomplete. You can help by adding to it.

On a chemical level, Naloxone is similar in structure or many opiates and semisynthetic opioids. It is extremely similar in structure to the morphinan opiod oxymorphone. Naloxone has an allyl group as opposed to a methyl group bound to the oxygen, which has been shown to be a functional group substitution that often reverses the activity of opioid agonists and turns them into antagonist instead. 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. The liver metabolizes naloxone. It has very low oral bioavailability which is why it is administered intravenously, intramuscularly or intranasally. Small amounts of naloxone are often added to opioids like buprenorphine and pentazocine to prevent abuse. Naloxone has 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

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.

It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.

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

Physical effects

• Sedation - Naloxone 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 naloxone is noticeably similar to the same experience found within antipsychotics although without the accompanying analysis suppression and thought deceleration.
• Identity alteration - Naloxone has been demonstrated by a pilot study to significantly 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 greater brightness marked the patients' perception of the world. A full 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 considered not habit-forming. 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 opioids 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 substance.

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.

Administration

When administering naloxone, it is important to understand which formulation it is coming in and what that means. In the United States, naloxone primarily comes in four formulations. Narcan is a prescription nasal spray that is inserted and administered into the nose. Evzio is an autoinjector with voice instruction capabilities similar to many epinephrine autoinjectors. Naloxone may come in a pink or orange box that reads "Naloxone Hydrochloride, INJ., USP" or a green box that reads the same thing. The main difference between these two is that the green ones come with a needle built in and is meant for intramuscular injection specifically.

Common Brands (US)

The three most common types of naloxone. Narcan, Evzio and generic orange/pink box naloxone respectively.

Narcan is one of the most common brands containing naloxone. To use it you must peel the device out of the packaging. Hold the device with your thumb on the bottom of the plunger and 2 fingers on the nozzle. Then place and hold the tip of the nozzle in either nostril until your fingers touch the bottom of the patient’s nose. Press the plunger down, which will release the medication. Narcan is not a substitute for professional medical care. On brand Narcan will deliver 4mg of naloxone. Narcan does not last as long as many opioids, so before or after administering Narcan, you should call for emergency services.

Evzio is one of the most common brands containing naloxone. Pull the device out of the case. Pull off the red safety guard. Place the black end of the device against their outer thigh. Ensure there are no solid objects between the black end and their skin, although the needle can go through clothes if necessary. Press firmly down on the device until you hear a distinct click and hold it their for 5 seconds to ensure all the naloxone is released from the device. Evzio is not a substitute for professional medical care. Evzio does not last as long as many opioids, so before or after administering Evzio, you should call for emergency services.

To use orange/pink box naloxone, take the device out of the box. If the device is not assembled, assemble it. Remove the yellow caps off the cylinder. On the narrow end, put the cylindrical cap. Take the vial of the medication and put it into the chamber, with the colored end pointing towards the patient. The dosage for adults is 2mg of naloxone and the device comes with 2mg. Put the device in either nostril and press down on the vial of medication until half of it is dispersed into that nostril. Then, take the device and put it in the other nostril and administer the rest of the medication. If the patient is under 5 years of age, only administer 1mg total, or a quarter of the total medication in each nostril. Each naloxone should be administered with the goal of restoring ventilation (breathing) but not necessarily consciousness. Naloxone should not be administered in the field to patients under 28 days of age. Boxed naloxone is not a substitute for professional medical care. Naloxone does not last as long as many opioids, so before or after administering naloxone, you should call for emergency services.

See also

• Responsible use
• Safer injection guide
• Heroin
• Fentanyl
• Opioids
• Codeine
• Morphine

External links

• Naloxone (Drugs.com)
• Combatting America's Opioid Crisis: Heroin's Antidote (Vice)