naloxone Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
opioid receptor antagonists/agonists related to normorphine 1878 465-65-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • naloxone hydrochloride dihydrate
  • naloxone hydrochloride hydrate
  • naloxone hydrobromide
  • evzio
  • naloxone
  • l-naloxone
  • (-)-Naloxone
  • naloxone hydrochloride
  • naloxone HCl
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
  • Molecular weight: 327.38
  • Formula: C19H21NO4
  • CLOGP: 0.16
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 70
  • ALOGS: -1.76
  • ROTB: 2

Drug dosage:

DoseUnitRoute
75 mg O

Approvals:

DateAgencyCompanyOrphan
April 13, 1971 FDA ADAPT

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Toxicity to various agents 329.17 52.52 103 597 71937 4566355
Overdose 212.86 52.52 66 634 43493 4594799
Drug abuse 195.65 52.52 56 644 27891 4610401
Unresponsive to stimuli 120.86 52.52 31 669 10062 4628230
Drug withdrawal syndrome 113.87 52.52 31 669 12641 4625651
Pulmonary oedema 108.72 52.52 31 669 14955 4623337
Miosis 105.50 52.52 22 678 2868 4635424
Somnolence 97.48 52.52 37 663 43623 4594669
Cardio-respiratory arrest 95.94 52.52 30 670 19792 4618500
Agitation 70.49 52.52 25 675 24175 4614117
Depressed level of consciousness 69.33 52.52 22 678 15132 4623160
Cardiac arrest 69.23 52.52 27 673 33980 4604312
Drug withdrawal syndrome neonatal 67.73 52.52 14 686 1738 4636554
Mental status changes 65.11 52.52 20 680 12356 4625936
Respiratory arrest 63.51 52.52 20 680 13400 4624892
Hypotension 57.33 52.52 29 671 67371 4570921
Exposure during pregnancy 52.63 52.52 22 678 32949 4605343

Pharmacologic Action:

SourceCodeDescription
ATC A06AH04 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR CONSTIPATION
DRUGS FOR CONSTIPATION
Peripheral opioid receptor antagonists
ATC N02AA53 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Natural opium alkaloids
ATC N02AA55 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Natural opium alkaloids
ATC V03AB15 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Antidotes
CHEBI has role CHEBI:35488 central nervous system depressant
CHEBI has role CHEBI:90755 antidote to opioid poisoning
MeSH PA D002491 Central Nervous System Agents
MeSH PA D009292 Narcotic Antagonists
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
FDA EPC N0000175691 Opioid Antagonist
FDA MoA N0000000154 Opioid Antagonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Pain indication 22253000
Opioid dependence indication 75544000 DOID:2559
Poisoning by opiate analgesic drug indication 241749009
Prevention of opioid abuse indication 426928008
Opiate-Induced Respiratory Depression indication
Suicidal thoughts contraindication 6471006
Dependent drug abuse contraindication 6525002
Alcohol withdrawal delirium contraindication 8635005
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Asthenia contraindication 13791008
Constipation contraindication 14760008 DOID:2089
Chronic disease of respiratory system contraindication 17097001
Mood swings contraindication 18963009
Inflammatory bowel disease contraindication 24526004 DOID:0050589
Alcohol intoxication contraindication 25702006
Shock contraindication 27942005
Orthostatic hypotension contraindication 28651003
Hypercapnia contraindication 29596007
Torsades de pointes contraindication 31722008
Dehydration contraindication 34095006
Disorder of gallbladder contraindication 39621005 DOID:0060262
Hypothyroidism contraindication 40930008 DOID:1459
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Bradycardia contraindication 48867003
Paralytic ileus contraindication 55525008 DOID:8442
Chronic type B viral hepatitis contraindication 61977001
Ulcerative colitis contraindication 64766004 DOID:8577
Substance abuse contraindication 66214007
Benign intracranial hypertension contraindication 68267002 DOID:11459
Urethral stricture contraindication 76618002
Decreased respiratory function contraindication 80954004
Injury of head contraindication 82271004
Cor pulmonale contraindication 83291003 DOID:8515
Opioid withdrawal contraindication 87132004
Pulmonary emphysema contraindication 87433001
Kidney disease contraindication 90708001 DOID:557
Disorder of biliary tract contraindication 105997008 DOID:9741
Prolonged QT interval contraindication 111975006
Acute abdominal pain contraindication 116290004
Neoplasm of brain contraindication 126952004 DOID:1319
Chronic hepatitis C contraindication 128302006
Seizure disorder contraindication 128613002
Liver function tests abnormal contraindication 166603001
Drug-induced psychosis contraindication 191483003 DOID:1742
Disease of liver contraindication 235856003 DOID:409
Morbid obesity contraindication 238136002 DOID:11981
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Exacerbation of asthma contraindication 281239006
Lesion of brain contraindication 301766008
Coma contraindication 371632003
Primary adrenocortical insufficiency contraindication 373662000
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Operation on gastrointestinal tract contraindication 386621005
Hypoxia contraindication 389086002
Respiratory insufficiency contraindication 409623005
Central nervous system depression contraindication 418072004
Dysfunction of sphincter of Oddi contraindication 430887001
Congenital long QT syndrome contraindication 442917000
Kyphoscoliosis with Respiratory Compromise contraindication
Pain in Opioid Naive Patients contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.31 acidic
pKa2 7.47 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 0.3MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 7579019 Jan. 22, 2020 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 0.7MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 7579019 Jan. 22, 2020 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 1MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 7579019 Jan. 22, 2020 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
10MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 8969369 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
10MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9056051 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
10MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9084729 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
10MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9161937 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
10MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9168252 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
10MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9283216 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
10MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9283221 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
10MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9345701 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
10MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9511066 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE BY PROVIDING AN ABUSE-DETERRENT ORAL CONTROLLED RELEASE COMBINATION DRUG PRODUCT
20MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 8969369 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
20MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9056051 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
20MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9084729 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
20MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9161937 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
20MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9168252 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
20MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9283216 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
20MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9283221 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
20MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9345701 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
20MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9511066 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE BY PROVIDING AN ABUSE-DETERRENT ORAL CONTROLLED RELEASE COMBINATION DRUG PRODUCT
5MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 8969369 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
5MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9056051 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
5MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9084729 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
5MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9161937 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
5MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9168252 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
5MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9283216 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
5MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9283221 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
5MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9345701 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
5MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9511066 May 10, 2022 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE BY PROVIDING AN ABUSE-DETERRENT ORAL CONTROLLED RELEASE COMBINATION DRUG PRODUCT
10MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9555000 April 4, 2023 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
10MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9907793 April 4, 2023 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
5MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9555000 April 4, 2023 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
5MG TARGINIQ PURDUE PHARMA LP N205777 July 23, 2014 DISCN TABLET, EXTENDED RELEASE ORAL 9907793 April 4, 2023 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
EQ 0.5MG BASE SUBOXONE INDIVIOR INC N022410 Aug. 30, 2010 RX FILM BUCCAL, SUBLINGUAL 8603514 April 3, 2024 TREATMENT OF OPIOID DEPENDENCE/SUBLINGUAL OR BUCCAL APPLICATION
EQ 1MG BASE SUBOXONE INDIVIOR INC N022410 Aug. 10, 2012 RX FILM BUCCAL, SUBLINGUAL 8603514 April 3, 2024 TREATMENT OF OPIOID DEPENDENCE/SUBLINGUAL OR BUCCAL APPLICATION
EQ 2MG BASE SUBOXONE INDIVIOR INC N022410 Aug. 30, 2010 RX FILM BUCCAL, SUBLINGUAL 8603514 April 3, 2024 TREATMENT OF OPIOID DEPENDENCE/SUBLINGUAL OR BUCCAL APPLICATION
EQ 3MG BASE SUBOXONE INDIVIOR INC N022410 Aug. 10, 2012 RX FILM BUCCAL, SUBLINGUAL 8603514 April 3, 2024 TREATMENT OF OPIOID DEPENDENCE/SUBLINGUAL OR BUCCAL APPLICATION
0.4MG/0.4ML (0.4MG/0.4ML) EVZIO KALEO INC N205787 April 3, 2014 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 9724471 May 23, 2027 METHOD FOR CONFIRMING DOSE DELIVERY
2MG/0.4ML (2MG/0.4ML) EVZIO (AUTOINJECTOR) KALEO INC N209862 Oct. 19, 2016 RX SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 9724471 May 23, 2027 METHOD FOR CONFIRMING DOSE DELIVERY
EQ 0.3MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 8147866 July 23, 2027 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 0.3MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 9655843 July 23, 2027 TREATMENT OF OPIOID DEPENDENCE
EQ 0.7MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 8147866 July 23, 2027 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 0.7MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 9655843 July 23, 2027 TREATMENT OF OPIOID DEPENDENCE
EQ 1MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 8147866 July 23, 2027 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 1MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 9655843 July 23, 2027 TREATMENT OF OPIOID DEPENDENCE
EQ 0.18MG BASE ZUBSOLV OREXO US INC N204242 Oct. 4, 2016 RX TABLET SUBLINGUAL 8658198 Dec. 3, 2027 SUBLINGUAL OR BUCCAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 0.36MG BASE ZUBSOLV OREXO US INC N204242 July 3, 2013 RX TABLET SUBLINGUAL 8658198 Dec. 3, 2027 SUBLINGUAL OR BUCCAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 0.71MG BASE ZUBSOLV OREXO US INC N204242 June 4, 2015 RX TABLET SUBLINGUAL 8658198 Dec. 3, 2027 SUBLINGUAL OR BUCCAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 1.4MG BASE ZUBSOLV OREXO US INC N204242 July 3, 2013 RX TABLET SUBLINGUAL 8658198 Dec. 3, 2027 SUBLINGUAL OR BUCCAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 2.1MG BASE ZUBSOLV OREXO US INC N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 8658198 Dec. 3, 2027 SUBLINGUAL OR BUCCAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 2.9MG BASE ZUBSOLV OREXO US INC N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 8658198 Dec. 3, 2027 SUBLINGUAL OR BUCCAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 0.5MG BASE SUBOXONE INDIVIOR INC N022410 Aug. 30, 2010 RX FILM BUCCAL, SUBLINGUAL 9687454 Aug. 7, 2029 TREATMENT OF OPIOID DEPENDENCE/SUBLINGUAL OR BUCCAL APPLICATION
EQ 1MG BASE SUBOXONE INDIVIOR INC N022410 Aug. 10, 2012 RX FILM BUCCAL, SUBLINGUAL 9687454 Aug. 7, 2029 TREATMENT OF OPIOID DEPENDENCE/SUBLINGUAL OR BUCCAL APPLICATION
EQ 2MG BASE SUBOXONE INDIVIOR INC N022410 Aug. 30, 2010 RX FILM BUCCAL, SUBLINGUAL 9687454 Aug. 7, 2029 TREATMENT OF OPIOID DEPENDENCE/SUBLINGUAL OR BUCCAL APPLICATION
EQ 3MG BASE SUBOXONE INDIVIOR INC N022410 Aug. 10, 2012 RX FILM BUCCAL, SUBLINGUAL 9687454 Aug. 7, 2029 TREATMENT OF OPIOID DEPENDENCE/SUBLINGUAL OR BUCCAL APPLICATION
EQ 0.5MG BASE SUBOXONE INDIVIOR INC N022410 Aug. 30, 2010 RX FILM BUCCAL, SUBLINGUAL 8475832 March 26, 2030 THIS DRUG IS ADMINISTERED BY SUBLINGUAL ROUTE TO HUMANS FOR MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 1MG BASE SUBOXONE INDIVIOR INC N022410 Aug. 10, 2012 RX FILM BUCCAL, SUBLINGUAL 8475832 March 26, 2030 THIS DRUG IS ADMINISTERED BY SUBLINGUAL ROUTE TO HUMANS FOR MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 2MG BASE SUBOXONE INDIVIOR INC N022410 Aug. 30, 2010 RX FILM BUCCAL, SUBLINGUAL 8475832 March 26, 2030 THIS DRUG IS ADMINISTERED BY SUBLINGUAL ROUTE TO HUMANS FOR MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 3MG BASE SUBOXONE INDIVIOR INC N022410 Aug. 10, 2012 RX FILM BUCCAL, SUBLINGUAL 8475832 March 26, 2030 THIS DRUG IS ADMINISTERED BY SUBLINGUAL ROUTE TO HUMANS FOR MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 0.18MG BASE ZUBSOLV OREXO US INC N204242 Oct. 4, 2016 RX TABLET SUBLINGUAL 8470361 May 22, 2030 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 0.36MG BASE ZUBSOLV OREXO US INC N204242 July 3, 2013 RX TABLET SUBLINGUAL 8470361 May 22, 2030 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 0.71MG BASE ZUBSOLV OREXO US INC N204242 June 4, 2015 RX TABLET SUBLINGUAL 8470361 May 22, 2030 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 1.4MG BASE ZUBSOLV OREXO US INC N204242 July 3, 2013 RX TABLET SUBLINGUAL 8470361 May 22, 2030 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 2.1MG BASE ZUBSOLV OREXO US INC N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 8470361 May 22, 2030 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 2.9MG BASE ZUBSOLV OREXO US INC N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 8470361 May 22, 2030 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
0.4MG/0.4ML (0.4MG/0.4ML) EVZIO KALEO INC N205787 April 3, 2014 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10322239 Feb. 28, 2031 USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
0.4MG/0.4ML (0.4MG/0.4ML) EVZIO KALEO INC N205787 April 3, 2014 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 9474869 Feb. 28, 2031 USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
2MG/0.4ML (2MG/0.4ML) EVZIO (AUTOINJECTOR) KALEO INC N209862 Oct. 19, 2016 RX SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10322239 Feb. 28, 2031 USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
2MG/0.4ML (2MG/0.4ML) EVZIO (AUTOINJECTOR) KALEO INC N209862 Oct. 19, 2016 RX SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 9474869 Feb. 28, 2031 USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
0.4MG/0.4ML (0.4MG/0.4ML) EVZIO KALEO INC N205787 April 3, 2014 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10143972 May 24, 2031 USE OF A DELIVERY DEVICE TO DELIVER A DOSE OF NALOXONE
2MG/0.4ML (2MG/0.4ML) EVZIO (AUTOINJECTOR) KALEO INC N209862 Oct. 19, 2016 RX SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10143792 May 24, 2031 USE OF A DELIVERY DEVICE TO DELIVER A DOSE OF NALOXONE
0.4MG/0.4ML (0.4MG/0.4ML) EVZIO KALEO INC N205787 April 3, 2014 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 9517307 July 18, 2034 USE OF AN AUTO INJECTOR TO ADMINISTER NALOXONE HCL
2MG/0.4ML (2MG/0.4ML) EVZIO (AUTOINJECTOR) KALEO INC N209862 Oct. 19, 2016 RX SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 9517307 July 18, 2034 USE OF AN AUTO INJECTOR TO ADMINISTER NALOXONE HCL
2MG/SPRAY NARCAN ADAPT N208411 Jan. 24, 2017 DISCN SPRAY, METERED NASAL 9480644 March 16, 2035 USE OF NALOXONE HYDROCHLORIDE FOR EMERGENCY TREATMENT OF KNOWN OR SUSPECTED OPIOID OVERDOSE, AS MANIFESTED BY RESPIRATORY AND/OR CENTRAL NERVOUS SYSTEM DEPRESSION.
2MG/SPRAY NARCAN ADAPT N208411 Jan. 24, 2017 DISCN SPRAY, METERED NASAL 9707226 March 16, 2035 USE OF NALOXONE HYDROCHLORIDE FOR EMERGENCY TREATMENT OF KNOWN OR SUSPECTED OPIOID OVERDOSE, AS MANIFESTED BY RESPIRATORY AND/OR CENTRAL NERVOUS SYSTEM DEPRESSION.
4MG/SPRAY NARCAN ADAPT N208411 Nov. 18, 2015 RX SPRAY, METERED NASAL 10085937 March 16, 2035 USE OF NALOXONE HYDROCHLORIDE FOR EMERGENCY TREATMENT OF KNOWN OR SUSPECTED OPIOID OVERDOSE, AS MANIFESTED BY RESPIRATORY AND/OR CENTRAL NERVOUS SYSTEM DEPRESSION.
4MG/SPRAY NARCAN ADAPT N208411 Nov. 18, 2015 RX SPRAY, METERED NASAL 9468747 March 16, 2035 USE OF NALOXONE HYDROCHLORIDE FOR EMERGENCY TREATMENT OF KNOWN OR SUSPECTED OPIOID OVERDOSE, AS MANIFESTED BY RESPIRATORY AND/OR CENTRAL NERVOUS SYSTEM DEPRESSION.
4MG/SPRAY NARCAN ADAPT N208411 Nov. 18, 2015 RX SPRAY, METERED NASAL 9561177 March 16, 2035 USE OF NALOXONE HYDROCHLORIDE FOR EMERGENCY TREATMENT OF KNOWN OR SUSPECTED OPIOID OVERDOSE, AS MANIFESTED BY RESPIRATORY AND/OR CENTRAL NERVOUS SYSTEM DEPRESSION.
4MG/SPRAY NARCAN ADAPT N208411 Nov. 18, 2015 RX SPRAY, METERED NASAL 9629965 March 16, 2035 USE OF NALOXONE HYDROCHLORIDE FOR EMERGENCY TREATMENT OF KNOWN OR SUSPECTED OPIOID OVERDOSE, AS MANIFESTED BY RESPIRATORY AND/OR CENTRAL NERVOUS SYSTEM DEPRESSION.
4MG/SPRAY NARCAN ADAPT N208411 Nov. 18, 2015 RX SPRAY, METERED NASAL 9775838 March 16, 2035 USE OF NALOXONE HYDROCHLORIDE FOR EMERGENCY TREATMENT OF KNOWN OR SUSPECTED OPIOID OVERDOSE, AS MANIFESTED BY RESPIRATORY AND/OR CENTRAL NERVOUS SYSTEM DEPRESSION.
0.4MG/0.4ML (0.4MG/0.4ML) EVZIO KALEO INC N205787 April 3, 2014 DISCN SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10220158 March 20, 2035 USE OF A DELIVERY DEVICE TO DELIVER A BIOEQUIVALENT DOSE OF A NALOXONE COMPOSITION VIA A NEEDLE
2MG/0.4ML (2MG/0.4ML) EVZIO (AUTOINJECTOR) KALEO INC N209862 Oct. 19, 2016 RX SOLUTION INTRAMUSCULAR, SUBCUTANEOUS 10220158 March 20, 2035 USE OF A DELIVERY DEVICE TO DELIVER A BIOEQUIVALENT DOSE OF A NALOXONE COMPOSITION VIA A NEEDLE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
1MG/ML NALOXONE HYDROCHLORIDE DR REDDYS A213209 March 16, 2020 RX INJECTABLE INJECTION Sept. 14, 2020 COMPETITIVE GENERIC THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Mu-type opioid receptor GPCR ANTAGONIST Ki 8.81 WOMBAT-PK CHEMBL
Kappa-type opioid receptor GPCR ANTAGONIST Ki 8.50 WOMBAT-PK
Cytochrome P450 2D6 Enzyme IC50 5.70 DRUG MATRIX
Adenosine receptor A3 GPCR IC50 8.80 CHEMBL
Delta-type opioid receptor GPCR ANTAGONIST Ki 7.27 WOMBAT-PK
C-C chemokine receptor type 5 GPCR Kd 7.98 CHEMBL
Kappa-type opioid receptor GPCR Ki 8.50 CHEMBL
Delta-type opioid receptor GPCR Kd 7.30 CHEMBL
Mu-type opioid receptor GPCR Ki 9.17 CHEMBL
Opioid receptor GPCR Kd 9 CHEMBL
Kappa-type opioid receptor GPCR Kd 9 CHEMBL
Delta-type opioid receptor GPCR Kd 7.74 CHEMBL
Mu-type opioid receptor GPCR IC50 8.30 CHEMBL
Mu-type opioid receptor GPCR Kd 9.40 CHEMBL
Kappa-type opioid receptor GPCR ANTAGONIST IC50 8.30 IUPHAR
Mu-type opioid receptor GPCR ANTAGONIST Ki 9 IUPHAR

External reference:

IDSource
C3819096 UMLSCUI
D01340 KEGG_DRUG
36B82AMQ7N UNII
1526 INN_ID
51481-60-8 SECONDARY_CAS_RN
89018006 SNOMEDCT_US
4019852 VANDF
7242 RXNORM
372890007 SNOMEDCT_US
d00311 MMSL
27364 MMSL
004661 NDDF
CHEMBL80 ChEMBL_ID
CHEMBL1718 ChEMBL_ID
DB01183 DRUGBANK_ID
CHEBI:7459 CHEBI
5284596 PUBCHEM_CID
D009270 MESH_DESCRIPTOR_UI
1638 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
buprenorphine hydrochloride and naloxone hydrochloride dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0054-0188 TABLET 0.50 mg SUBLINGUAL ANDA 19 sections
buprenorphine hydrochloride and naloxone hydrochloride dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0054-0189 TABLET 2 mg SUBLINGUAL ANDA 19 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0228-3154 TABLET 0.50 mg SUBLINGUAL ANDA 19 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0228-3155 TABLET 2 mg SUBLINGUAL ANDA 19 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0378-8765 FILM 0.50 mg SUBLINGUAL ANDA 18 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0378-8766 FILM 1 mg SUBLINGUAL ANDA 18 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0378-8767 FILM 2 mg SUBLINGUAL ANDA 18 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0378-8768 FILM 3 mg SUBLINGUAL ANDA 18 sections
Buprenorphine HCl and Naloxone HCl HUMAN PRESCRIPTION DRUG LABEL 2 0406-1923 TABLET 0.50 mg SUBLINGUAL ANDA 18 sections
Buprenorphine HCl and Naloxone HCl HUMAN PRESCRIPTION DRUG LABEL 2 0406-1924 TABLET 2 mg SUBLINGUAL ANDA 18 sections
Buprenorphine Hydrochloride and Naloxone Hydrochloride Dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0406-8005 TABLET 0.50 mg SUBLINGUAL ANDA 19 sections
Buprenorphine Hydrochloride and Naloxone Hydrochloride Dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0406-8020 TABLET 2 mg SUBLINGUAL ANDA 19 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-1212 INJECTION, SOLUTION 0.40 mg INTRAMUSCULAR ANDA 13 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-1215 INJECTION, SOLUTION 0.40 mg INTRAMUSCULAR ANDA 13 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-1219 INJECTION, SOLUTION 0.40 mg INTRAMUSCULAR ANDA 13 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-1782 INJECTION, SOLUTION 0.40 mg INTRAMUSCULAR ANDA 13 sections
Pentazocine and naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0591-0395 TABLET 0.50 mg ORAL ANDA 15 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0641-6132 INJECTION 0.40 mg INTRAMUSCULAR ANDA 13 sections
BUPRENORPHINE AND NALOXONE HUMAN PRESCRIPTION DRUG LABEL 2 0781-7216 FILM, SOLUBLE 0.50 mg SUBLINGUAL NDA authorized generic 18 sections
BUPRENORPHINE AND NALOXONE HUMAN PRESCRIPTION DRUG LABEL 2 0781-7227 FILM, SOLUBLE 1 mg SUBLINGUAL NDA authorized generic 18 sections
BUPRENORPHINE AND NALOXONE HUMAN PRESCRIPTION DRUG LABEL 2 0781-7238 FILM, SOLUBLE 2 mg SUBLINGUAL NDA authorized generic 18 sections
BUPRENORPHINE AND NALOXONE HUMAN PRESCRIPTION DRUG LABEL 2 0781-7249 FILM, SOLUBLE 3 mg SUBLINGUAL NDA authorized generic 18 sections
Suboxone HUMAN PRESCRIPTION DRUG LABEL 2 12496-1202 FILM, SOLUBLE 0.50 mg SUBLINGUAL NDA 18 sections
Suboxone HUMAN PRESCRIPTION DRUG LABEL 2 12496-1204 FILM, SOLUBLE 1 mg SUBLINGUAL NDA 18 sections
Suboxone HUMAN PRESCRIPTION DRUG LABEL 2 12496-1208 FILM, SOLUBLE 2 mg SUBLINGUAL NDA 18 sections
Suboxone HUMAN PRESCRIPTION DRUG LABEL 2 12496-1212 FILM, SOLUBLE 3 mg SUBLINGUAL NDA 18 sections
PENTAZOCINE HCL AND NALOXONE HCL HUMAN PRESCRIPTION DRUG LABEL 2 16590-556 TABLET 0.50 mg ORAL ANDA 13 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-041 INJECTION, SOLUTION 0.40 mg INTRAVENOUS ANDA 13 sections
Naloxone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-042 INJECTION, SOLUTION 0.40 mg INTRAVENOUS ANDA 13 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 42858-601 TABLET 0.50 mg SUBLINGUAL ANDA 19 sections