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Naloxone

Generic Name
Naloxone
Brand Names
Kloxxado, Narcan, Suboxone, Targin, Targiniq, Zimhi, Zubsolv, Nyxoid
Drug Type
Small Molecule
Chemical Formula
C19H21NO4
CAS Number
465-65-6
Unique Ingredient Identifier
36B82AMQ7N

Overview

Naloxone is an opioid antagonist medication used to block or reverse the effects of opioid drugs, particularly within the setting of drug overdoses which are rapidly becoming a leading cause of death worldwide. More specifically, naloxone has a high affinity for μ-opioid receptors, where it acts as an inverse agonist, causing the rapid removal of any other drugs bound to these receptors. When taken in large quantities, opioid medications such as morphine, hydromorphone, methadone, heroin, or fentanyl are capable of causing life-threatening symptoms such as respiratory depression, reduced heart rate, slurred speech, drowsiness, and constricted pupils. If untreated, this can progress to vomiting, absent pulse and breathing, loss of consciousness, and even death. Naloxone is indicated for the rapid reversal of these symptoms of central nervous system depression in opioid overdose. It's important to note that naloxone only works on opioid receptors within the body, and is therefore not capable of reversing the effects of non-opioid medications such as stimulants like methamphetamine or cocaine, or benzodiazepines like lorazepam or diazepam. Also known as the brand name product Narcan, naloxone is currently available by intramuscular (IM) or subcutaneous (SubQ) injection, nasal spray, or intravenous (IV) infusion. Naloxone IM injections are commonly available in the form of "kits", which is ideal for making overdose treatment accessible and readily available for administration by minimally trained individuals within the community. Kits commonly include the supplies necessary to treat an overdose in a non-medical setting such as alcohol swabs, syringes, a rescue breathing mask, and instructions for use. Frequently also carried by medical and emergency personnel and at events known to be associated with heavy drug use like music festivals, naloxone kits are considered a key component of harm reduction strategies. There are over-the-counter nasal sprays available. When injected intramuscularly (IM), naloxone acts within three to five minutes. Administration of naloxone is associated with very few side effects. Notably, if injected into a person not currently using opioid medications, there would be no noticeable effects at all. However, for individuals using opioid medications or experiencing an overdose, IM injection of naloxone rapidly reverses opioid effects and can cause the injected individual to immediately experience withdrawal symptoms. Common symptoms of opioid withdrawal include nausea, vomiting, sweating, runny nose, aches, and diarrhea. Although certainly physically uncomfortable, opioid withdrawal symptoms are not life-threatening; administration of naloxone is, therefore, appropriate for any person appearing to have any symptoms of an opioid overdose. Due to its short duration of action, persons injected with naloxone should be monitored for responsiveness and potentially injected a second time or taken to the hospital. Naloxone is also available within the combination product Suboxone with the opioid medication buprenorphine. Suboxone is used for the maintenance treatment of opioid dependence and addiction. When taken orally, naloxone has no pharmacological effect and does not reduce the effectiveness of the opioid effect of buprenorphine. The primary purpose of including naloxone within Suboxone is to act as a deterrent to injection, as injected naloxone would rapidly reverse the effects of buprenorphine. Naloxone was granted FDA approval on 13 April 1971.

Indication

Naloxone nasal sprays are indicated for the reversal of an opioid overdose or suspected opioid overdose: it is intended for immediate administration as emergency therapy in settings where opioids may be present. Intramuscular, intravenous, and subcutaneous injections are indicated for complete or partial reversal of opioid depression, diagnosis of known or suspected opioid overdose, and as an adjunct therapy in the treatment of septic shock. Sublingual tablets and films are formulated with buprenorphine for the treatment of opioid dependence. Naloxone is also formulated with pentazocine as an oral tablet for severe pain. Intramuscular or subcutaneous naloxone autoinjectors are used for the emergency treatment of people 12 years of age and older where the use of high-potency opioids such as fentanyl analogues as a chemical weapon, is suspected. Naloxone has been used off-label for the treatment of neuraxial opioid-induced pruritus.

Associated Conditions

  • Opioid Dependence
  • Opioid Overdose
  • Pruritus
  • Respiratory Depression
  • Septic Shock
  • Severe Pain
  • Moderate Pain
  • Suspected Opioid Overdose

Research Report

Published: Jul 24, 2025

Naloxone (DB01183): A Comprehensive Monograph on its Pharmacology, Clinical Utility, and Public Health Impact

Section 1: Physicochemical Properties and Molecular Identification

This section provides a definitive characterization of naloxone, detailing the fundamental chemical, regulatory, and physical data that form the basis of its pharmacological identity and clinical use. A thorough understanding of its molecular structure and physicochemical properties is essential for appreciating its mechanism of action, pharmacokinetic profile, and the pharmaceutical challenges associated with its formulation.

1.1 Chemical and Regulatory Identifiers

Naloxone is a well-characterized small molecule drug with a comprehensive set of identifiers used in regulatory, clinical, and research contexts worldwide. It is cataloged in major pharmacological databases under the DrugBank Accession Number DB01183.[1] Its unique chemical identity is universally recognized by its Chemical Abstracts Service (CAS) Number, which is 465-65-6 for the free base form of the molecule.[2] To enhance its solubility for clinical formulations, naloxone is frequently prepared as a salt; the most common of these are naloxone hydrochloride (CAS Number: 357-08-4) and naloxone hydrochloride hydrate (CAS Number: 51481-60-8).[2]

The drug is known by several synonyms and international nonproprietary names, including Naloxona, Nalossone, and Naloxonum, reflecting its global use.[1] Its chemical nomenclature includes systematic names such as (−)-naloxone and 1-N-Allyl-14-hydroxynordihydromorphinone.[1]

Continue reading the full research report

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Physicians Total Care, Inc.
54868-5707
SUBLINGUAL
2 mg in 1 1
7/27/2010
INDIVIOR INC.
12496-1202
SUBLINGUAL, BUCCAL
0.5 mg in 1 1
6/1/2022
Lannett Company, Inc.
62175-458
SUBLINGUAL
2 mg in 1 1
3/26/2024
Lannett Company, Inc.
62175-452
SUBLINGUAL
0.5 mg in 1 1
3/26/2024
Baxter Healthcare Corporation
36000-308
INTRAMUSCULAR, INTRAVENOUS, SUBCUTANEOUS
0.4 mg in 1 mL
2/3/2021
Akorn Operating Company LLC (dba Akorn)
50383-294
SUBLINGUAL
0.5 mg in 1 1
10/1/2023
Dr.Reddys Laboratories Inc
43598-579
BUCCAL, SUBLINGUAL
0.5 mg in 1 1
11/5/2019
Mylan Institutional LLC
67457-992
INTRAMUSCULAR, INTRAVENOUS, SUBCUTANEOUS
1 mg in 1 mL
10/22/2021
HF Acquisition Co. LLC, DBA HealthFirst
51662-1238
INTRAMUSCULAR, INTRAVENOUS, SUBCUTANEOUS
0.4 mg in 1 mL
12/9/2022
Quality Care Products, LLC
83008-007
NASAL
4 mg in 0.1 mL
3/3/2023

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
Authorised
9/26/2006

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
MAPIN INJECTION 0.4 mg/ml
SIN10290P
INJECTION
0.4 mg/ml
10/23/1998
TARGIN® Prolonged Release Tablets 20mg /10mg
SIN14033P
TABLET, FILM COATED, EXTENDED RELEASE
10 mg
10/19/2011
TARGIN® Prolonged Release Tablets 10mg/5mg
SIN14032P
TABLET, FILM COATED, EXTENDED RELEASE
5 mg
10/19/2011
NALOXONE HYDROCHLORIDE INJECTION USP 0.4 mg/ml
SIN05964P
INJECTION
0.4 mg/ml
5/23/1991
TARGIN® Prolonged Release Tablets 5mg/2.5mg
SIN14031P
TABLET, FILM COATED, EXTENDED RELEASE
2.5 mg
10/19/2011
Suboxone 8 mg/2 mg sublingual tablets
SIN13405P
TABLET, ORALLY DISINTEGRATING
2.44MG
1/28/2008
Suboxone 2 mg/0.5 mg sublingual tablets
SIN13404P
TABLET, ORALLY DISINTEGRATING
0.61MG
1/28/2008

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
MAPIN INJ 0.4MG/ML
N/A
wings pharmaceutical ltd
N/A
N/A
8/18/2000

TGA Drug Approvals

Approved Product
ARTG ID
Sponsor
Registration Type
Status
Registration Date
No TGA approvals found for this drug.

Health Canada Drug Approvals

Approved Product
Company
DIN
Dosage Form
Strength
Market Date
S.O.S. NALOXONE HYDROCHLORIDE INJECTION
02453266
Solution - Intramuscular ,  Intravenous ,  Subcutaneous
1 MG / ML
N/A
TEVA-NALOXONE NASAL SPRAY
teva canada limited
02511568
Spray, Metered Dose - Nasal
4 MG / 0.1 ML
1/8/2024
TARGIN
purdue pharma
02339617
Tablet (Extended-Release) - Oral
10 MG
10/5/2010
NALOXONE HYDROCHLORIDE INJECTION USP
sterinova inc.
02548194
Solution - Subcutaneous ,  Intramuscular
0.4 MG / ML
9/26/2024
NARCAN NASAL SPRAY
emergent operations ireland limited
02458187
Spray, Metered Dose - Nasal
4 MG / 0.1 ML
7/7/2017
TARGIN
purdue pharma
02339625
Tablet (Extended-Release) - Oral
20 MG
10/5/2010
NALOXONE HYDROCHLORIDE INJECTION, USP
auro pharma inc
02515261
Solution - Intravenous ,  Subcutaneous ,  Intramuscular
0.4 MG / ML
N/A
NALOXONE HYDROCHLORIDE INJECTION, USP
eugia pharma inc.
02534967
Solution - Intravenous ,  Subcutaneous ,  Intramuscular
0.4 MG / ML
N/A
KLOXXADO
hikma canada limited
02555441
Spray, Metered Dose - Nasal
8 MG / 0.1 ML
N/A
NALOXONE HYDROCHLORIDE INJECTION, USP
auro pharma inc
02515288
Solution - Intramuscular ,  Subcutaneous ,  Intravenous
4 MG / 10 ML
N/A

CIMA AEMPS Drug Approvals

Approved Product
Company
Registration Number
Pharmaceutical Form
Prescription Type
Status
SUBOXONE 2 MG/0,5 MG COMPRIMIDOS SUBLINGUALES
06359001
COMPRIMIDO SUBLINGUAL
Diagnóstico Hospitalario. Psicótropos
Not Commercialized
SUBOXONE 8 MG/2 MG COMPRIMIDOS SUBLINGUALES
06359003
COMPRIMIDO SUBLINGUAL
Diagnóstico Hospitalario. Psicótropos
Not Commercialized
SUBOXONE 2 MG/0,5 MG COMPRIMIDOS SUBLINGUALES
106359002
COMPRIMIDO SUBLINGUAL
Diagnóstico Hospitalario. Psicótropos
Not Commercialized
SUBOXONE 8 MG/2 MG COMPRIMIDOS SUBLINGUALES
106359004
COMPRIMIDO SUBLINGUAL
Diagnóstico Hospitalario. Psicótropos
Not Commercialized

Philippines FDA Drug Approvals

Approved Product
Company
License Number
Dosage Form
Strength
Approval Date
No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

Approved Product
Company
License Number
Dosage Form
Strength
Approval Date
No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

Approved Product
Company
Registration Number
Dosage Form
Strength
Approval Date
No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

Medicine Name
MA Holder
MA Number
Pharmaceutical Form
Active Ingredient
Authorization Date
No UK EMC drug information found for this drug.

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