Naloxone

Identification

Summary

Naloxone is an opioid receptor antagonist used to rapidly reverse an opioid overdose. Also included in some drug formulations as an abuse deterrent to prevent injection.

Brand Names
Bunavail, Evzio, Kloxxado, Narcan, Suboxone, Targin, Targiniq, Zubsolv
Generic Name
Naloxone
DrugBank Accession Number
DB01183
Background

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.3 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.3 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.3,13 If untreated, this can progress to vomiting, absent pulse and breathing, loss of consciousness, and even death.13 Naloxone is indicated for the rapid reversal of these symptoms of central nervous system depression in opioid overdose.2 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.14,16 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.15 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.

When injected intramuscularly (IM), naloxone acts within 3-5 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.2 Common symptoms of opioid withdrawal include nausea, vomiting, sweating, runny nose, aches, and diarrhea.2 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.2

Naloxone is also available within the combination product Suboxone with the opioid medication buprenorphine.11,12 Suboxone is used for the maintenance treatment of opioid dependence and addiction.11,12 When taken orally, naloxone has no pharmacological effect and does not reduce the effectiveness of the opioid effect of buprenorphine.11,12 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.11,12

Naloxone was granted FDA approval on 13 April 1971.10

Type
Small Molecule
Groups
Approved, Vet approved
Structure
Thumb
Weight
Average: 327.3743
Monoisotopic: 327.147058165
Chemical Formula
C19H21NO4
Synonyms
  • (−)-naloxone
  • 1-N-Allyl-14-hydroxynordihydromorphinone
  • 17-allyl-3,14-dihydroxy-4,5α-epoxymorphinan-6-one
  • Nalossone
  • Naloxona
  • Naloxone
  • Naloxonum
External IDs
  • EN 1530 Base

Pharmacology

Indication

Naloxone nasal sprays are indicated for the emergency treatment of an opioid overdose or suspected opioid overdose.7 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.16

Sublingual tablets and films are formulated with buprenorphine for the treatment of opioid dependence.11,12 Naloxone is also formulated with pentazocine as an oral tablet for severe pain.17

Naloxone has been used off-label for the treatment of neuraxial opioid-induced pruritus.5

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Naloxone is an opioid receptor antagonist indicated in the reversal of opioid overdoses.7 Naloxone has a shorter duration of action than opioids and multiple doses may be required.3,7 The therapeutic window of naloxone is wide, as it has no effect if a patient has not taken opioids.4,7 Patients treated with naloxone may experience opioid withdrawal and a person administering naloxone should be aware that reversal of opioid overdoses may not resolve all the symptoms a patient is experiencing if other drugs are involved.7

Mechanism of action

Naloxone is a competitive inhibitor of the µ-opioid receptor.7,12 Naloxone antagonizes the action of opioids, reversing their effects.7 If a patient has not taken opioids, naloxone does not have a significant effect on patients.13

TargetActionsOrganism
AMu-type opioid receptor
antagonist
Humans
ADelta-type opioid receptor
antagonist
Humans
AKappa-type opioid receptor
antagonist
Humans
NCyclic AMP-responsive element-binding protein 1
other/unknown
Humans
NEstrogen receptor alpha
antagonist
other/unknown
Humans
UToll-like receptor 4
inhibitor
Humans
ULiver carboxylesterase 1
binder
Humans
Absorption

An intranasal dose of naloxone is 42-47% bioavailable.7 An 8 mg dose of nasal naloxone reaches a Cmax of 12.3-12.8 ng/mL, with a Tmax of 0.25 hours, and an AUC of 16.7-19.0 h*ng/mL.7 A 0.4 mg intramuscular dose reaches a Cmax of 0.876-0.910 ng/mL, with a Tmax of 0.25 hours, and an AUC of 1.94-1.95 h*ng/mL.7 A 2 mg intravenous dose reaches a Cmax of 26.2 ng/mL with an AUC of 12.8 h*ng/mL.7

Volume of distribution

The volume of distribution of naloxone is 200 L.3 Naloxone distributes into tissues rapidly.7 It can also cross the placenta and blood-brain barrier.7

Protein binding

Naloxone is approximately 45% bound to albumin, but there is significant binding to other proteins.7,12

Metabolism

Naloxone primarily undergoes glucuronidation to form naloxone-3-glucuronide.7 Naloxone is also N-dealkylated to noroxymorphone or undergoes 6-keto reduction to naloxol.1

Hover over products below to view reaction partners

Route of elimination

After oral or intravenous administration, naloxone is 25-40% eliminated in the urine within 6 hours, 50% in 24 hours, and 60-70% in 72 hours.7 The metabolites naloxone-3-glucuronide, noroxymorphone, and naloxol are all detected in the urine.1,7

Half-life

The mean half life of naloxone hydrochloride is 1.8-2.7 hours intranasally, 1.4 hours intramuscularly, and 1.2 hours intravenously.8 In neonates, the mean half life is 3.1 ± 0.5 hours.8

Clearance

The clearance of naloxone is 2500 L/day.3

Adverse Effects
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Toxicity

If a patient has not taken opioids, naloxone does not have a significant effect on patients.4,13

The oral LD50 in mice and rats is >1 g/kg.8 The intraperitoneal LD50 is 80 mg/kg in mice and 239 mg/kg in rats.8 The subcutaneous LD50 is 286 mg/kg in mice and 500 mg/kg in rats.8

Pathways
PathwayCategory
Naloxone Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Naloxone which could result in a higher serum level.
AbemaciclibThe metabolism of Abemaciclib can be decreased when combined with Naloxone.
AcalabrutinibThe metabolism of Acalabrutinib can be decreased when combined with Naloxone.
AceclofenacAceclofenac may decrease the excretion rate of Naloxone which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Naloxone which could result in a higher serum level.
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Naloxone.
AcetaminophenAcetaminophen may decrease the excretion rate of Naloxone which could result in a higher serum level.
AcetazolamideNaloxone may increase the excretion rate of Acetazolamide which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Naloxone which could result in a higher serum level.
AclidiniumNaloxone may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Interactions
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Food Interactions
  • Take separate from meals. When formulated as a buccal film or sublingual form, avoid eating or drinking until the film has completely dissolved.

Products

Products
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Product Ingredients
IngredientUNIICASInChI Key
Naloxone hydrochlorideF850569PQR357-08-4RGPDIGOSVORSAK-STHHAXOLSA-N
Naloxone hydrochloride dihydrate5Q187997EE51481-60-8TXMZWEASFRBVKY-IOQDSZRYSA-N
Product Images
International/Other Brands
Kloxxado (Hikma Pharmaceuticals PLC) / Narcanti / Narcon
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
EvzioInjection, solution2 mg/0.4mLIntramuscular; Subcutaneouskaleo, Inc.2016-10-192021-09-30US flag
EvzioInjection, solution0.4 mg/1Intramuscular; SubcutaneousKaleo, Inc2014-04-032018-05-31US flag
EVZIO(R) NALOXONE HClInjection, solution2 mg/0.4mLIntramuscular; SubcutaneousHF Acquisition Co LLC, DBA HealthFirst2020-01-11Not applicableUS flag
Injectable Naloxone HydrochlorideSolution0.4 mg / mLIntramuscular; Intravenous; SubcutaneousOmega Laboratories Ltd2016-08-05Not applicableCanada flag
Injectable Naloxone HydrochlorideSolution1 mg / mLIntramuscular; Intravenous; SubcutaneousOmega Laboratories LtdNot applicableNot applicableCanada flag
KloxxadoSpray8 mg/0.1mLNasalHikma Specialty USA Inc.2021-04-29Not applicableUS flag
Naloxone HCl Injection - 0.4mg/ml USPLiquid0.4 mg / mLIntramuscular; Intravenous; SubcutaneousSandoz Canada Incorporated1995-12-31Not applicableCanada flag
Naloxone HCl Injection - 1mg/ml USPLiquid1 mg / mLIntramuscular; Intravenous; SubcutaneousSandoz Canada Incorporated1995-12-31Not applicableCanada flag
Naloxone HydrochlorideInjection, solution0.02 mg/1mLIntramuscular; Intravenous; SubcutaneousHospira2006-05-112006-05-11US flag
Naloxone HydrochlorideInjection, solution0.02 mg/1mLIntramuscular; Intravenous; SubcutaneousHospira2006-05-112006-05-11US flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Naloxone HciInjection, solution0.4 mg/1mLIntramuscular; Intravenous; SubcutaneousHf Acquisition Co. Llc, Dba Health First2018-08-18Not applicableUS flag
Naloxone HClInjection0.4 mg/1mLIntramuscular; Intravenous; SubcutaneousRenaissance Ssa, Llc2019-12-28Not applicableUS flag
Naloxone HydrochlorideInjection, solution0.4 mg/1mLIntramuscular; Intravenous; SubcutaneousHospira, Inc.2005-09-23Not applicableUS flag
Naloxone HydrochlorideInjection, solution0.4 mg/1mLIntramuscular; Intravenous; SubcutaneousMedical Purchasing Solutions, Llc2017-08-08Not applicableUS flag
Naloxone HydrochlorideInjection1 mg/1mLParenteralInternational Medication Systems, Limited2016-07-28Not applicableUS flag
Naloxone HydrochlorideInjection, solution0.4 mg/1mLIntramuscular; Intravenous; SubcutaneousA-S Medication Solutions2017-08-08Not applicableUS flag
Naloxone HydrochlorideInjection, solution0.4 mg/1mLIntramuscular; Intravenous; SubcutaneousAkorn, Inc.2017-02-28Not applicableUS flag
Naloxone HydrochlorideInjection, solution0.4 mg/1mLIntramuscular; Intravenous; SubcutaneousSina Health Inc1987-01-07Not applicableUS flag
Naloxone HydrochlorideInjection, solution0.4 mg/1mLIntramuscular; Intravenous; SubcutaneousHF Acquisition Co. LLC, DBA HealthFirst2018-09-03Not applicableUS flag
Naloxone HydrochlorideInjection, solution0.4 mg/1mLIntramuscular; Intravenous; SubcutaneousGeneral Injectables and Vaccines, Inc.2018-06-122021-04-30US flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
BunavailNaloxone hydrochloride dihydrate (0.7 mg/1) + Buprenorphine hydrochloride (4.2 mg/1)FilmBuccalBioDelivery Sciences International, Inc.2014-09-302021-10-31US flag
BunavailNaloxone hydrochloride dihydrate (0.3 mg/1) + Buprenorphine hydrochloride (2.1 mg/1)FilmBuccalBioDelivery Sciences International, Inc.2014-09-302021-02-28US flag
BunavailNaloxone hydrochloride dihydrate (1 mg/1) + Buprenorphine hydrochloride (6.3 mg/1)FilmBuccalBioDelivery Sciences International, Inc.2014-09-302021-07-31US flag
Buprenorphine and NaloxoneNaloxone (0.5 mg/1) + Buprenorphine hydrochloride (2 mg/1)Film, solubleBuccal; SublingualDr.Reddys Laboratories Inc2018-06-14Not applicableUS flag
Buprenorphine and NaloxoneNaloxone hydrochloride dihydrate (0.5 mg/1) + Buprenorphine hydrochloride (2 mg/1)FilmBuccal; SublingualMylan Pharmaceuticals Inc.2020-04-17Not applicableUS flag
Buprenorphine and NaloxoneNaloxone hydrochloride dihydrate (0.5 mg/1) + Buprenorphine hydrochloride (2 mg/1)TabletSublingualActavis Pharma, Inc.2013-03-04Not applicableUS flag
Buprenorphine and NaloxoneNaloxone hydrochloride dihydrate (0.5 mg/1) + Buprenorphine hydrochloride (2 mg/1)TabletSublingualTeva2014-12-102018-10-31US flag
Buprenorphine and NaloxoneNaloxone hydrochloride dihydrate (2 mg/1) + Buprenorphine hydrochloride (8 mg/1)TabletSublingualbryant ranch prepack2016-09-19Not applicableUS flag
Buprenorphine and NaloxoneNaloxone hydrochloride (0.5 mg/1) + Buprenorphine hydrochloride (2 mg/1)TabletSublingualGolden State Medical Supply, Inc.2015-10-16Not applicableUS flag
Buprenorphine and NaloxoneNaloxone hydrochloride dihydrate (2 mg/1) + Buprenorphine hydrochloride (8 mg/1)TabletSublingualREMEDYREPACK INC.2021-06-17Not applicableUS flag

Categories

ATC Codes
A06AH04 — NaloxoneN02AA53 — Hydromorphone and naloxoneV03AB15 — NaloxoneN02AA55 — Oxycodone and naloxone
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Phenanthrenes and derivatives
Sub Class
Not Available
Direct Parent
Phenanthrenes and derivatives
Alternative Parents
Isoquinolones and derivatives / Tetralins / Coumarans / 1-hydroxy-2-unsubstituted benzenoids / Alkyl aryl ethers / Aralkylamines / Piperidines / Tertiary alcohols / Trialkylamines / 1,2-aminoalcohols
show 7 more
Substituents
1,2-aminoalcohol / 1-hydroxy-2-unsubstituted benzenoid / Alcohol / Alkyl aryl ether / Amine / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Carbonyl group / Coumaran
show 19 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
morphinane alkaloid, organic heteropentacyclic compound (CHEBI:7459)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
36B82AMQ7N
CAS number
465-65-6
InChI Key
UZHSEJADLWPNLE-GRGSLBFTSA-N
InChI
InChI=1S/C19H21NO4/c1-2-8-20-9-7-18-15-11-3-4-12(21)16(15)24-17(18)13(22)5-6-19(18,23)14(20)10-11/h2-4,14,17,21,23H,1,5-10H2/t14-,17+,18+,19-/m1/s1
IUPAC Name
(1S,5R,13R,17S)-10,17-dihydroxy-4-(prop-2-en-1-yl)-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10-trien-14-one
SMILES
OC1=CC=C2C[C@H]3N(CC=C)CC[C@@]45[C@@H](OC1=C24)C(=O)CC[C@@]35O

References

Synthesis Reference

Bianca Brogmann, Silke Muhlau, Christof Spitzley, "Pharmaceutical preparation containing oxycodone and naloxone." U.S. Patent US20050245556, issued November 03, 2005.

US20050245556
General References
  1. Weinstein SH, Pfeffer M, Schor JM, Indindoli L, Mintz M: Metabolites of naloxone in human urine. J Pharm Sci. 1971 Oct;60(10):1567-8. doi: 10.1002/jps.2600601030. [Article]
  2. Jordan MR, Morrisonponce D: Naloxone . [Article]
  3. Rzasa Lynn R, Galinkin JL: Naloxone dosage for opioid reversal: current evidence and clinical implications. Ther Adv Drug Saf. 2018 Jan;9(1):63-88. doi: 10.1177/2042098617744161. Epub 2017 Dec 13. [Article]
  4. Papathanasiou T, Springborg AD, Kongstad KT, Staerk D, Moller K, Taylor BK, Lund TM, Werner MU: High-dose naloxone, an experimental tool uncovering latent sensitisation: pharmacokinetics in humans. Br J Anaesth. 2019 Aug;123(2):e204-e214. doi: 10.1016/j.bja.2018.12.007. Epub 2019 Jan 18. [Article]
  5. Kumar K, Singh SI: Neuraxial opioid-induced pruritus: An update. J Anaesthesiol Clin Pharmacol. 2013 Jul;29(3):303-7. doi: 10.4103/0970-9185.117045. [Article]
  6. Link [Link]
  7. FDA Approved Drug Products: Kloxxado (Naloxone) Nasal Spray [Link]
  8. Caymen Chemical: Naloxone MSDS [Link]
  9. International Pharmacopoeia: Naloxone Hydrochloride [Link]
  10. FDA Approved Drug Products: Narcan (Naloxone) Injection (Discontinued) [Link]
  11. FDA Approved Drug Products: Suboxone (Buprenorphine, Naloxone) Sublingual, Buccal Film [Link]
  12. FDA Approved Drug Products: Zubsolv (Buprenorphine, Naloxone) Sublingual Tablet [Link]
  13. British Columbia CDC: Administration of Naloxone [Link]
  14. FDA Approved Drug Products: Narcan (Naloxone) Nasal Spray [Link]
  15. DailyMed: Lifems (Naloxone Hydrochloride) Kit [Link]
  16. Dailymed: Naloxone Hydrochloride Subcutaneous, Intramuscular, Intravenous Injection [Link]
  17. DailyMed: Naloxone and Pentazocine Oral Tablet [Link]
Human Metabolome Database
HMDB0015314
KEGG Drug
D08249
KEGG Compound
C07252
PubChem Compound
5284596
PubChem Substance
46508816
ChemSpider
4447644
BindingDB
54795
RxNav
7242
ChEBI
7459
ChEMBL
CHEMBL80
ZINC
ZINC000000389747
Therapeutic Targets Database
DAP000097
PharmGKB
PA450586
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Naloxone
MSDS
Download (74 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingHealth Services ResearchCoronavirus Disease 2019 (COVID‑19) / Human Immunodeficiency Virus (HIV) Infections / Opioid Use Disorder (OUD) / Opioids Use / Risk Reduction1
4CompletedPreventionOpioid Induced Constipation (OIC) / Postoperative pain1
4CompletedPreventionRespiratory Depression1
4CompletedSupportive CareBack Pain Lower Back1
4CompletedSupportive CareMalignancies1
4CompletedSupportive CarePain, Chronic1
4CompletedSupportive CareSpinal Disorders1
4CompletedTreatmentBack Pain Lower Back1
4CompletedTreatmentBack pain / Back Pain Lower Back / Neuropathic Pain1
4CompletedTreatmentBack pain / Osteoarthritis (OA)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Amphastar Pharmaceuticals
  • A-S Medication Solutions LLC
  • Bristol-Myers Squibb Co.
  • Bryant Ranch Prepack
  • Cardinal Health
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Endo Pharmaceuticals Inc.
  • General Injectables and Vaccines Inc.
  • Hospira Inc.
  • Lake Erie Medical and Surgical Supply
  • Letco Medical Inc.
  • Mallinckrodt Inc.
  • Mckesson Corp.
  • Nucare Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Reckitt Benckiser Inc.
  • Southwood Pharmaceuticals
  • Stat Rx Usa
Dosage Forms
FormRouteStrength
FilmBuccal
FilmBuccal; Sublingual
Film, solubleBuccal; Sublingual
Injection, solution0.4 mg/1ml
Injection, solutionIntramuscular; Subcutaneous0.4 mg/1
Injection, solutionIntramuscular; Subcutaneous2 mg/0.4mL
Injection, solutionParenteral
SprayNasal8 mg/0.1mL
InjectionIntramuscular; Intravenous
InjectionIntramuscular; Intravenous; Subcutaneous
SolutionIntramuscular; Intravenous; Subcutaneous0.4 mg
SolutionParenteral0.4 mg
Injection, solution
Injection, solutionIntramuscular; Intravenous; Subcutaneous
LiquidIntramuscular; Intravenous; Subcutaneous0.4 mg / mL
LiquidIntramuscular; Intravenous; Subcutaneous1 mg / mL
InjectionIntramuscular; Intravenous; Subcutaneous0.4 mg/1mL
InjectionIntramuscular; Intravenous; Subcutaneous1 mg/1mL
InjectionParenteral0.4 mg/1mL
InjectionParenteral1 mg/1mL
InjectionParenteral4 mg/1mL
Injection, solutionIntramuscular; Intravenous; Subcutaneous.4 mg/1mL
Injection, solutionIntramuscular; Intravenous; Subcutaneous0.02 mg/1mL
Injection, solutionIntramuscular; Intravenous; Subcutaneous0.4 mg/1mL
Injection, solutionIntramuscular; Intravenous; Subcutaneous1 mg/1mL
PowderNot applicable1 kg/1kg
SolutionIntramuscular; Intravenous; Subcutaneous1 mg / mL
SolutionIntramuscular; Intravenous; Subcutaneous0.4 mg / mL
SolutionIntramuscular; Intravenous; Subcutaneous4 mg / 10 mL
InjectionIntravenous0.02 mg/1mL
InjectionIntravenous0.4 mg/1mL
InjectionIntravenous1 mg/1mL
SprayNasal2 mg/0.1mL
SprayNasal4 mg/0.1mL
LiquidIntramuscular; Intravenous; Subcutaneous0.02 mg / mL
Spray, meteredNasal2 mg / 0.1 mL
Spray, meteredNasal4 mg / 0.1 mL
Solution0.4 mg/1ml
Injection
SprayNasal
Tablet, extended releaseOral
TabletOral
Film, solubleSublingual
TabletOral; Sublingual
TabletSublingual
FilmSublingual
Tablet, film coated, extended releaseOral
SolutionOral
Tablet, orally disintegratingSublingual
Prices
Unit descriptionCostUnit
Naloxone hcl powder70.9USD g
Naloxone 0.4 mg/ml vial7.07USD ml
Naloxone 0.4 mg/ml ampul4.78USD ml
Narcan 0.4 mg/ml ampul4.58USD ml
Naloxone 0.02 mg/ml vial0.84USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
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US9084729No2015-07-212022-05-10US flag
US9283216No2016-03-152022-05-10US flag
US9056051No2015-06-162022-05-10US flag
US8846090No2014-09-302023-04-04US flag
US6277384No2001-08-212018-12-22US flag
US8822487No2014-09-022018-12-22US flag
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Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)177 °CInternational Pharmacopoeia
water solubilitySolubleFDA Label
logP2.09HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility5.64 mg/mLALOGPS
logP1.47ALOGPS
logP1.62ChemAxon
logS-1.8ALOGPS
pKa (Strongest Acidic)10.07ChemAxon
pKa (Strongest Basic)7.84ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area70 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity88.72 m3·mol-1ChemAxon
Polarizability33.83 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9729
Blood Brain Barrier+0.9787
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.8788
P-glycoprotein inhibitor INon-inhibitor0.7922
P-glycoprotein inhibitor IINon-inhibitor0.8382
Renal organic cation transporterInhibitor0.5
CYP450 2C9 substrateNon-substrate0.8522
CYP450 2D6 substrateSubstrate0.5296
CYP450 3A4 substrateSubstrate0.6107
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9303
CYP450 2D6 inhibitorNon-inhibitor0.7886
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9153
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9523
Ames testNon AMES toxic0.7182
CarcinogenicityNon-carcinogens0.9583
BiodegradationNot ready biodegradable0.9968
Rat acute toxicity2.7231 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7798
hERG inhibition (predictor II)Non-inhibitor0.8641
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-004i-0139000000-e70921e0765c3389ce85

Targets

Drugtargets
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Details
1. Mu-type opioid receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Voltage-gated calcium channel activity
Specific Function
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
Gene Name
OPRM1
Uniprot ID
P35372
Uniprot Name
Mu-type opioid receptor
Molecular Weight
44778.855 Da
References
  1. Narita M, Suzuki M, Mizoguchi H, Narita M, Yajima Y, Sakurada S, Tseng LF, Suzuki T: Up-regulation of mu-opioid receptor-mediated G-protein activation in protein kinase Cgamma knockout mice following repeated naloxone treatment. Neurosci Lett. 2003 Feb 27;338(2):103-6. [Article]
  2. Freye E, Latasch L, Von Bredow G, Neruda B: [The opioid tramadol demonstrates excitatory properties of non-opioid character--a preclinical study using alfentanil as a comparison]. Schmerz. 1998 Feb 28;12(1):19-24. [Article]
  3. Neal CR Jr, Owens CE, Taylor LP, Hoversten MT, Akil H, Watson SJ Jr: Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors. J Chem Neuroanat. 2003 Jul;25(4):233-47. [Article]
  4. Spetea M, Toth F, Schutz J, Otvos F, Toth G, Benyhe S, Borsodi A, Schmidhammer H: Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist. Eur J Neurosci. 2003 Jul;18(2):290-5. [Article]
  5. Marek GJ: Behavioral evidence for mu-opioid and 5-HT2A receptor interactions. Eur J Pharmacol. 2003 Aug 1;474(1):77-83. [Article]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  7. Helm S, Trescot AM, Colson J, Sehgal N, Silverman S: Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification. Pain Physician. 2008 Mar-Apr;11(2):225-35. [Article]
  8. Goodman AJ, Le Bourdonnec B, Dolle RE: Mu opioid receptor antagonists: recent developments. ChemMedChem. 2007 Nov;2(11):1552-70. [Article]
  9. van Dorp E, Yassen A, Dahan A: Naloxone treatment in opioid addiction: the risks and benefits. Expert Opin Drug Saf. 2007 Mar;6(2):125-32. [Article]
  10. Nazzaro C, Rizzi A, Salvadori S, Guerrini R, Regoli D, Zeilhofer HU, Calo G: UFP-101 antagonizes the spinal antinociceptive effects of nociceptin/orphanin FQ: behavioral and electrophysiological studies in mice. Peptides. 2007 Mar;28(3):663-9. doi: 10.1016/j.peptides.2006.11.004. Epub 2006 Dec 11. [Article]
  11. Economidou D, Fedeli A, Fardon RM, Weiss F, Massi M, Ciccocioppo R: Effect of novel nociceptin/orphanin FQ-NOP receptor ligands on ethanol drinking in alcohol-preferring msP rats. Peptides. 2006 Dec;27(12):3299-306. doi: 10.1016/j.peptides.2006.09.007. [Article]
  12. FDA Approved Drug Products: Zubsolv (Buprenorphine, Naloxone) Sublingual Tablet [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Opioid receptor activity
Specific Function
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...
Gene Name
OPRD1
Uniprot ID
P41143
Uniprot Name
Delta-type opioid receptor
Molecular Weight
40368.235 Da
References
  1. Moncada A, Cendan CM, Baeyens JM, Del Pozo E: Effects of serine/threonine protein phosphatase inhibitors on morphine-induced antinociception in the tail flick test in mice. Eur J Pharmacol. 2003 Mar 28;465(1-2):53-60. [Article]
  2. Kakinohana M, Marsala M, Carter C, Davison JK, Yaksh TL: Neuraxial morphine may trigger transient motor dysfunction after a noninjurious interval of spinal cord ischemia: a clinical and experimental study. Anesthesiology. 2003 Apr;98(4):862-70. [Article]
  3. Breljak D, Boranic M, Horvat S: Oligopeptide fragments of the enkephalin molecule interfere with hematopoietic cell colony formation. Int J Immunopathol Pharmacol. 2000 Jan-Apr;13(1):13-19. [Article]
  4. Chudapongse N, Kim SY, Kramer RE, Ho IK: Nonspecific effects of the selective kappa-opioid receptor agonist U-50,488H on dopamine uptake and release in PC12 cells. J Pharmacol Sci. 2003 Nov;93(3):372-5. [Article]
  5. Osman AM, Gomma M, Saad AH: A possible role for an enkephalinergic system in the internal defense mechanism of Biomphalaria alexandrina exposed to Schistosoma mansoni. J Egypt Soc Parasitol. 2003 Dec;33(3):841-61. [Article]
  6. Helm S, Trescot AM, Colson J, Sehgal N, Silverman S: Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification. Pain Physician. 2008 Mar-Apr;11(2):225-35. [Article]
  7. van Dorp E, Yassen A, Dahan A: Naloxone treatment in opioid addiction: the risks and benefits. Expert Opin Drug Saf. 2007 Mar;6(2):125-32. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Opioid receptor activity
Specific Function
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
Gene Name
OPRK1
Uniprot ID
P41145
Uniprot Name
Kappa-type opioid receptor
Molecular Weight
42644.665 Da
References
  1. Peng X, Neumeyer JL: Kappa receptor bivalent ligands. Curr Top Med Chem. 2007;7(4):363-73. [Article]
  2. van Dorp E, Yassen A, Dahan A: Naloxone treatment in opioid addiction: the risks and benefits. Expert Opin Drug Saf. 2007 Mar;6(2):125-32. [Article]
  3. Helm S, Trescot AM, Colson J, Sehgal N, Silverman S: Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification. Pain Physician. 2008 Mar-Apr;11(2):225-35. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Other/unknown
General Function
Transcriptional activator activity, rna polymerase ii transcription factor binding
Specific Function
Phosphorylation-dependent transcription factor that stimulates transcription upon binding to the DNA cAMP response element (CRE), a sequence present in many viral and cellular promoters. Transcript...
Gene Name
CREB1
Uniprot ID
P16220
Uniprot Name
Cyclic AMP-responsive element-binding protein 1
Molecular Weight
36687.86 Da
References
  1. Li J, Li YH, Yuan XR: Changes of phosphorylation of cAMP response element binding protein in rat nucleus accumbens after chronic ethanol intake: naloxone reversal. Acta Pharmacol Sin. 2003 Sep;24(9):930-6. [Article]
  2. Chartoff EH, Papadopoulou M, Konradi C, Carlezon WA Jr: Dopamine-dependent increases in phosphorylation of cAMP response element binding protein (CREB) during precipitated morphine withdrawal in primary cultures of rat striatum. J Neurochem. 2003 Oct;87(1):107-18. [Article]
  3. Gao C, Chen LW, Tao YM, Chen J, Xu XJ, Chi ZQ: Effects of ohmefentanyl stereoisomers on phosphorylation of cAMP- response element binding protein in cultured rat hippocampal neurons. Acta Pharmacol Sin. 2003 Dec;24(12):1253-8. [Article]
  4. Walters CL, Cleck JN, Kuo YC, Blendy JA: Mu-opioid receptor and CREB activation are required for nicotine reward. Neuron. 2005 Jun 16;46(6):933-43. [Article]
  5. Hawes JJ, Narasimhaiah R, Picciotto MR: Galanin attenuates cyclic AMP regulatory element-binding protein (CREB) phosphorylation induced by chronic morphine and naloxone challenge in Cath.a cells and primary striatal cultures. J Neurochem. 2006 Feb;96(4):1160-8. Epub 2006 Jan 17. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
Other/unknown
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
Gene Name
ESR1
Uniprot ID
P03372
Uniprot Name
Estrogen receptor
Molecular Weight
66215.45 Da
References
  1. Farooqui M, Geng ZH, Stephenson EJ, Zaveri N, Yee D, Gupta K: Naloxone acts as an antagonist of estrogen receptor activity in MCF-7 cells. Mol Cancer Ther. 2006 Mar;5(3):611-20. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Transmembrane signaling receptor activity
Specific Function
Cooperates with LY96 and CD14 to mediate the innate immune response to bacterial lipopolysaccharide (LPS). Acts via MYD88, TIRAP and TRAF6, leading to NF-kappa-B activation, cytokine secretion and ...
Gene Name
TLR4
Uniprot ID
O00206
Uniprot Name
Toll-like receptor 4
Molecular Weight
95679.19 Da
References
  1. Lewis SS, Loram LC, Hutchinson MR, Li CM, Zhang Y, Maier SF, Huang Y, Rice KC, Watkins LR: (+)-naloxone, an opioid-inactive toll-like receptor 4 signaling inhibitor, reverses multiple models of chronic neuropathic pain in rats. J Pain. 2012 May;13(5):498-506. doi: 10.1016/j.jpain.2012.02.005. Epub 2012 Apr 20. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Triglyceride lipase activity
Specific Function
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acy...
Gene Name
CES1
Uniprot ID
P23141
Uniprot Name
Liver carboxylesterase 1
Molecular Weight
62520.62 Da
References
  1. Bencharit S, Morton CL, Xue Y, Potter PM, Redinbo MR: Structural basis of heroin and cocaine metabolism by a promiscuous human drug-processing enzyme. Nat Struct Biol. 2003 May;10(5):349-56. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Fang WB, Chang Y, McCance-Katz EF, Moody DE: Determination of naloxone and nornaloxone (noroxymorphone) by high-performance liquid chromatography-electrospray ionization- tandem mass spectrometry. J Anal Toxicol. 2009 Oct;33(8):409-17. doi: 10.1093/jat/33.8.409. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da
References
  1. Williams JA, Hyland R, Jones BC, Smith DA, Hurst S, Goosen TC, Peterkin V, Koup JR, Ball SE: Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8. doi: 10.1124/dmd.104.000794. Epub 2004 Aug 10. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C18
Uniprot ID
P33260
Uniprot Name
Cytochrome P450 2C18
Molecular Weight
55710.075 Da
References
  1. Fang WB, Chang Y, McCance-Katz EF, Moody DE: Determination of naloxone and nornaloxone (noroxymorphone) by high-performance liquid chromatography-electrospray ionization- tandem mass spectrometry. J Anal Toxicol. 2009 Oct;33(8):409-17. doi: 10.1093/jat/33.8.409. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Fang WB, Chang Y, McCance-Katz EF, Moody DE: Determination of naloxone and nornaloxone (noroxymorphone) by high-performance liquid chromatography-electrospray ionization- tandem mass spectrometry. J Anal Toxicol. 2009 Oct;33(8):409-17. doi: 10.1093/jat/33.8.409. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. FDA Approved Drug Products: Kloxxado (Naloxone) Nasal Spray [Link]
  2. FDA Approved Drug Products: Zubsolv (Buprenorphine, Naloxone) Sublingual Tablet [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Name
SLCO1A2
Uniprot ID
P46721
Uniprot Name
Solute carrier organic anion transporter family member 1A2
Molecular Weight
74144.105 Da
References
  1. Gao B, Hagenbuch B, Kullak-Ublick GA, Benke D, Aguzzi A, Meier PJ: Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier. J Pharmacol Exp Ther. 2000 Jul;294(1):73-9. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [Article]

Drug created on June 13, 2005 13:24 / Updated on July 24, 2021 14:57