buprenorphine indications/contra

Stem definitionDrug idCAS RN
opioid receptor antagonists/agonists, morphinan derivates 434 52485-79-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • buprenorphine
  • buprenorfine
  • norspan
  • buprenorphine hydrochloride
  • buprenorphine HCl
A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.
  • Molecular weight: 467.65
  • Formula: C29H41NO4
  • CLOGP: 3.99
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 62.16
  • ALOGS: -4.44
  • ROTB: 5

Drug dosage:

DoseUnitRoute
1.20 mg P
1.20 mg SL
1.20 mg TD
8 mg SL
8 mg SL

Approvals:

DateAgencyCompanyOrphan
Dec. 29, 1981 FDA RECKITT BENCKISER

FDA Adverse Event Reporting System

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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
Application site pruritus 2105.94 33.90 373 7357 1089 3377040
Product adhesion issue 1650.51 33.90 310 7420 1360 3376769
Application site erythema 1426.32 33.90 284 7446 1783 3376346
Application site rash 1222.67 33.90 226 7504 885 3377244
Drug withdrawal syndrome 1096.55 33.90 321 7409 11464 3366665
Inadequate analgesia 990.76 33.90 193 7537 1056 3377073
Drug abuse 948.93 33.90 319 7411 18011 3360118
Foetal exposure during pregnancy 918.32 33.90 299 7431 15252 3362877
Drug withdrawal syndrome neonatal 888.62 33.90 195 7535 2055 3376074
Application site pain 888.51 33.90 185 7545 1482 3376647
Application site vesicles 852.74 33.90 155 7575 537 3377592
Nausea 794.48 33.90 509 7221 129136 3248993
Exposure during pregnancy 744.13 33.90 297 7433 27266 3350863
Toxicity to various agents 728.16 33.90 342 7388 46712 3331417
Application site burn 713.20 33.90 122 7608 263 3377866
Intentional product misuse 691.85 33.90 230 7500 12471 3365658
Substance abuse 674.03 33.90 139 7591 1053 3377076
Drug ineffective 663.47 33.90 437 7293 115653 3262476
Maternal exposure during pregnancy 635.92 33.90 205 7525 10066 3368063
Wrong technique in product usage process 570.48 33.90 214 7516 16537 3361592
Overdose 549.39 33.90 255 7475 33723 3344406
Vomiting 541.79 33.90 350 7380 89181 3288948
Off label use 502.99 33.90 279 7451 53698 3324431
Drug dependence 489.77 33.90 138 7592 4238 3373891
Product preparation error 455.65 33.90 93 7637 663 3377466
Application site irritation 428.97 33.90 90 7640 746 3377383
Hyperhidrosis 414.94 33.90 188 7542 23422 3354707
Drug effect decreased 389.23 33.90 148 7582 11821 3366308
Pain 371.86 33.90 255 7475 71302 3306827
Product use issue 367.65 33.90 154 7576 15847 3362282

Pharmacologic Action:

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SourceCodeDescription
ATC N02AE01 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Oripavine derivatives
ATC N07BC01 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
DRUGS USED IN ADDICTIVE DISORDERS
Drugs used in opioid dependence
ATC N07BC51 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
DRUGS USED IN ADDICTIVE DISORDERS
Drugs used in opioid dependence
FDA EPC N0000175689 Partial Opioid Agonist
FDA MoA N0000175685 Partial Opioid Agonists
MeSH PA D000700 Analgesics
MeSH PA D000701 Analgesics, Opioid
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D009292 Narcotic Antagonists
MeSH PA D009294 Narcotics
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
CHEBI has role CHEBI:35482 opioid analgesic
CHEBI has role CHEBI:55322 mu-opioid receptor agonist
CHEBI has role CHEBI:59282 kappa-opioid receptor agonist
CHEBI has role CHEBI:59283 delta-opioid receptor antagonist

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Opioid dependence indication 75544000 DOID:2559
Severe pain indication 76948002
Chronic pain indication 82423001
Prevention of opioid abuse indication 426928008
Acute postoperative pain indication 107401000119105
Chronic Pain with Opioid Tolerance indication
Dependent drug abuse contraindication 6525002
Alcohol withdrawal delirium contraindication 8635005
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Asthenia contraindication 13791008
Chronic disease of respiratory system contraindication 17097001
Alcohol intoxication contraindication 25702006
Orthostatic hypotension contraindication 28651003
Hypercapnia contraindication 29596007
Torsades de pointes contraindication 31722008
Hypothyroidism contraindication 40930008 DOID:1459
Paralytic ileus contraindication 55525008 DOID:8442
Chronic type B viral hepatitis contraindication 61977001
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
Disorder of biliary tract contraindication 105997008 DOID:9741
Prolonged QT interval contraindication 111975006
Chronic hepatitis C contraindication 128302006
Liver function tests abnormal contraindication 166603001
Drug-induced psychosis contraindication 191483003 DOID:1742
Disease of liver contraindication 235856003 DOID:409
Benign prostatic hyperplasia contraindication 266569009 DOID:2883
Lesion of brain contraindication 301766008
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Hypoxia contraindication 389086002
Respiratory insufficiency contraindication 409623005
Central nervous system depression contraindication 418072004
Congenital long QT syndrome contraindication 442917000
Pain in Opioid Naive Patients contraindication
Kyphoscoliosis with Respiratory Compromise contraindication
Opioid withdrawal off-label use 87132004

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.97 acidic
pKa2 8.88 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 0.7MG BASE ZUBSOLV OREXO US INC N204242 Oct. 4, 2016 RX TABLET SUBLINGUAL 8454996 Sept. 24, 2019 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE
EQ 1.4MG BASE ZUBSOLV OREXO US INC N204242 July 3, 2013 RX TABLET SUBLINGUAL 8454996 Sept. 24, 2019 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE
EQ 11.4MG BASE ZUBSOLV OREXO US INC N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 8454996 Sept. 24, 2019 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE
EQ 2.9MG BASE ZUBSOLV OREXO US INC N204242 June 4, 2015 RX TABLET SUBLINGUAL 8454996 Sept. 24, 2019 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE
EQ 5.7MG BASE ZUBSOLV OREXO US INC N204242 July 3, 2013 RX TABLET SUBLINGUAL 8454996 Sept. 24, 2019 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE
EQ 8.6MG BASE ZUBSOLV OREXO US INC N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL 8454996 Sept. 24, 2019 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE
EQ 2.1MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 7579019 Jan. 22, 2020 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 4.2MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 7579019 Jan. 22, 2020 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 6.3MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 7579019 Jan. 22, 2020 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 0.075MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 7579019 Jan. 22, 2020 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 0.15MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 7579019 Jan. 22, 2020 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 0.3MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 7579019 Jan. 22, 2020 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 0.45MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 7579019 Jan. 22, 2020 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 0.6MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 7579019 Jan. 22, 2020 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 0.75MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 7579019 Jan. 22, 2020 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 0.9MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 7579019 Jan. 22, 2020 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 12MG 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 4MG 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 8MG 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 80MG BASE/IMPLANT PROBUPHINE BRAEBURN PHARMS INC N204442 May 26, 2016 RX IMPLANT IMPLANTATION 7736665 April 25, 2024 FOR OPIOID DEPENDENCE
EQ 2.1MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 8147866 July 23, 2027 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 2.1MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 9655843 July 23, 2027 TREATMENT OF OPIOID DEPENDENCE
EQ 4.2MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 8147866 July 23, 2027 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 4.2MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 9655843 July 23, 2027 TREATMENT OF OPIOID DEPENDENCE
EQ 6.3MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 8147866 July 23, 2027 MAINTENANCE TREATMENT OF OPIOID DEPENDENCE
EQ 6.3MG BASE BUNAVAIL BDSI N205637 June 6, 2014 RX FILM BUCCAL 9655843 July 23, 2027 TREATMENT OF OPIOID DEPENDENCE
EQ 0.075MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 8147866 July 23, 2027 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 0.075MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 9655843 July 23, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE.
EQ 0.15MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 8147866 July 23, 2027 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 0.15MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 9655843 July 23, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE.
EQ 0.3MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 8147866 July 23, 2027 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 0.3MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 9655843 July 23, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE.
EQ 0.45MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 8147866 July 23, 2027 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 0.45MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 9655843 July 23, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE.
EQ 0.6MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 8147866 July 23, 2027 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 0.6MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 9655843 July 23, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE.
EQ 0.75MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 8147866 July 23, 2027 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 0.75MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 9655843 July 23, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE.
EQ 0.9MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 8147866 July 23, 2027 TREATEMENT OF PAIN BY TRANSMUCOSAL DELIVERY OF BUPRENORPHINE
EQ 0.9MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL 9655843 July 23, 2027 MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE.
EQ 0.7MG 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 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 11.4MG 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 June 4, 2015 RX TABLET SUBLINGUAL 8658198 Dec. 3, 2027 SUBLINGUAL OR BUCCAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 5.7MG 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 8.6MG 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 12MG 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 4MG 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 8MG 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 12MG 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 4MG 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 8MG 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 0.7MG 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 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 11.4MG 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 June 4, 2015 RX TABLET SUBLINGUAL 8470361 May 22, 2030 SUBLINGUAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION COMPRISING BUPRENORPHINE AND NALOXONE
EQ 5.7MG 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 8.6MG 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
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9272044 June 6, 2031 TREATING OPIOID ADDICTION BY ADMINISTERING BUPRENORPHINE
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9272044 June 6, 2031 TREATING OPIOID ADDICTION BY ADMINISTERING BUPRENORPHINE COMPOSITION WITH 28 DAY DOSE DURATION
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9272044 June 6, 2031 TREATING OPIOID ADDICTION BY ADMINISTERING BUPRENORPHINE ONCE PER MONTH
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9272044 June 6, 2031 TREATING OPIOID ADDICTION BY SUBCUTANEOUS INJECTION OF BUPRENORPHINE
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9498432 June 6, 2031 IN SITU FORMATION OF SOLID BUPRENORPHINE COMPOSITION
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9782402 June 6, 2031 TREATING ADDICTION BY ONCE PER MONTH ADMINISTRATION OF BUPRENORPHINE
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9782402 June 6, 2031 TREATING ADDICTION BY SUBCUTANEOUS INJECTION OF BUPRENORPHINE
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9782402 June 6, 2031 TREATING ADDICTION WITH 100 MG OR 300 MG DOSE OF BUPRENORPHINE
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9782402 June 6, 2031 TREATING OPIOID ADDICTION BY ADMINISTERING BUPRENORPHINE
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9827241 June 6, 2031 TREATING OPIOID ADDICTION BY 100 MG OR 300 MG DOSE BUPRENORPHINE
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9827241 June 6, 2031 TREATING OPIOID ADDICTION BY ADMINISTRATION OF BUPRENORPHINE
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9827241 June 6, 2031 TREATING OPIOID DEPENDENCY BY ADMINISTERING BUPRENORPHINE
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9827241 June 6, 2031 TREATING OPIOID DEPENDENCY BY ADMINISTERING BUPRENORPHINE ONCE PER MONTH
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9827241 June 6, 2031 TREATING OPIOID DEPENDENCY BY SUBCUTANEOUSLY ADMINISTERING BUPRENORPHINE
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9272044 June 6, 2031 TREATING OPIOID ADDICTION BY ADMINISTERING BUPRENORPHINE
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9272044 June 6, 2031 TREATING OPIOID ADDICTION BY ADMINISTERING BUPRENORPHINE COMPOSITION WITH 28 DAY DOSE DURATION
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9272044 June 6, 2031 TREATING OPIOID ADDICTION BY ADMINISTERING BUPRENORPHINE ONCE PER MONTH
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9272044 June 6, 2031 TREATING OPIOID ADDICTION BY SUBCUTANEOUS INJECTION OF BUPRENORPHINE
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9498432 June 6, 2031 IN SITU FORMATION OF SOLID BUPRENORPHINE COMPOSITION
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9782402 June 6, 2031 TREATING ADDICTION BY ONCE PER MONTH ADMINISTRATION OF BUPRENORPHINE
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9782402 June 6, 2031 TREATING ADDICTION BY SUBCUTANEOUS INJECTION OF BUPRENORPHINE
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9782402 June 6, 2031 TREATING ADDICTION WITH 100 MG OR 300 MG DOSE OF BUPRENORPHINE
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9782402 June 6, 2031 TREATING OPIOID ADDICTION BY ADMINISTERING BUPRENORPHINE
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9827241 June 6, 2031 TREATING OPIOID ADDICTION BY 100 MG OR 300 MG DOSE BUPRENORPHINE
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9827241 June 6, 2031 TREATING OPIOID ADDICTION BY ADMINISTRATION OF BUPRENORPHINE
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9827241 June 6, 2031 TREATING OPIOID DEPENDENCY BY ADMINISTERING BUPRENORPHINE
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9827241 June 6, 2031 TREATING OPIOID DEPENDENCY BY ADMINISTERING BUPRENORPHINE ONCE PER MONTH
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 9827241 June 6, 2031 TREATING OPIOID DEPENDENCY BY SUBCUTANEOUSLY ADMINISTERING BUPRENORPHINE
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 8975270 Sept. 5, 2031 TREATING OPIOID DEPENDENCY BY ADMINISTERING BUPRENORPHINE
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 8975270 Sept. 5, 2031 TREATING OPIOID DEPENDENCY BY ADMINISTERING BUPRENORPHINE ONCE MONTHLY
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 8975270 Sept. 5, 2031 TREATING OPIOID DEPENDENCY BY ADMINISTERING BUPRENORPHINE
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 8975270 Sept. 5, 2031 TREATING OPIOID DEPENDENCY BY ADMINISTERING BUPRENORPHINE ONCE MONTHLY
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 8921387 Jan. 6, 2032 TREATING OPIOID DEPENDENCE BY ADMINISTERING BUPRENORPHINE
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 8921387 Jan. 6, 2032 TREATING OPIOID DEPENDENCY BY ADMINISTERING BUPRENORPHINE ONCE PER MONTH
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 8921387 Jan. 6, 2032 TREATING OPIOID DEPENDENCE BY ADMINISTERING BUPRENORPHINE
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS 8921387 Jan. 6, 2032 TREATING OPIOID DEPENDENCY BY ADMINISTERING BUPRENORPHINE ONCE PER MONTH

Orange Book exclusivity data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.7MG BASE ZUBSOLV OREXO US INC N204242 Oct. 4, 2016 RX TABLET SUBLINGUAL Aug. 10, 2018 REVISIONS TO THE LABELING TO PERMIT THE USE OF ZUBSOLV AS INITIAL ('INDUCTION') TREATMENT OF OPIOID DEPENDENCE
EQ 1.4MG BASE ZUBSOLV OREXO US INC N204242 July 3, 2013 RX TABLET SUBLINGUAL Aug. 10, 2018 REVISIONS TO THE LABELING TO PERMIT THE USE OF ZUBSOLV AS INITIAL ('INDUCTION') TREATMENT OF OPIOID DEPENDENCE
EQ 11.4MG BASE ZUBSOLV OREXO US INC N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL Aug. 10, 2018 REVISIONS TO THE LABELING TO PERMIT THE USE OF ZUBSOLV AS INITIAL ('INDUCTION') TREATMENT OF OPIOID DEPENDENCE
EQ 2.9MG BASE ZUBSOLV OREXO US INC N204242 June 4, 2015 RX TABLET SUBLINGUAL Aug. 10, 2018 REVISIONS TO THE LABELING TO PERMIT THE USE OF ZUBSOLV AS INITIAL ('INDUCTION') TREATMENT OF OPIOID DEPENDENCE
EQ 5.7MG BASE ZUBSOLV OREXO US INC N204242 July 3, 2013 RX TABLET SUBLINGUAL Aug. 10, 2018 REVISIONS TO THE LABELING TO PERMIT THE USE OF ZUBSOLV AS INITIAL ('INDUCTION') TREATMENT OF OPIOID DEPENDENCE
EQ 8.6MG BASE ZUBSOLV OREXO US INC N204242 Dec. 11, 2014 RX TABLET SUBLINGUAL Aug. 10, 2018 REVISIONS TO THE LABELING TO PERMIT THE USE OF ZUBSOLV AS INITIAL ('INDUCTION') TREATMENT OF OPIOID DEPENDENCE
EQ 0.075MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL Oct. 23, 2018 NEW PRODUCT
EQ 0.15MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL Oct. 23, 2018 NEW PRODUCT
EQ 0.3MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL Oct. 23, 2018 NEW PRODUCT
EQ 0.45MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL Oct. 23, 2018 NEW PRODUCT
EQ 0.6MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL Oct. 23, 2018 NEW PRODUCT
EQ 0.75MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL Oct. 23, 2018 NEW PRODUCT
EQ 0.9MG BASE BELBUCA BDSI N207932 Oct. 23, 2015 RX FILM BUCCAL Oct. 23, 2018 NEW PRODUCT
EQ 80MG BASE/IMPLANT PROBUPHINE BRAEBURN PHARMS INC N204442 May 26, 2016 RX IMPLANT IMPLANTATION May 26, 2019 NEW PRODUCT
100MG/0.5ML (100MG/0.5ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS Nov. 30, 2020 NEW PRODUCT
300MG/1.5ML (200MG/ML) SUBLOCADE INDIVIOR INC N209819 Nov. 29, 2017 RX SOLUTION, EXTENDED RELEASE SUBCUTANEOUS Nov. 30, 2020 NEW PRODUCT

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Kappa-type opioid receptor GPCR ANTAGONIST Ki 9.01 WOMBAT-PK CHEMBL
Mu-type opioid receptor GPCR PARTIAL AGONIST Ki 8.29 WOMBAT-PK CHEMBL
Nociceptin receptor GPCR Ki 7.11 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.10 CHEMBL
Delta-type opioid receptor GPCR ANTAGONIST Ki 8.07 WOMBAT-PK
Mu-type opioid receptor GPCR Ki 9.40 CHEMBL
Delta-type opioid receptor GPCR Ki 9.32 CHEMBL
Mu-type opioid receptor GPCR Ki 9.89 CHEMBL
Kappa-type opioid receptor GPCR Ki 9.30 CHEMBL

External reference:

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IDSource
1670 IUPHAR_LIGAND_ID
4019644 VUID
N0000147737 NUI
C0006405 UMLSCUI
D00836 KEGG_DRUG
40D3SCR4GZ UNII
3403 INN_ID
53152-21-9 SECONDARY_CAS_RN
DB00921 DRUGBANK_ID
4019644 VANDF
N0000007417 NDFRT
N0000147737 NDFRT
27271 MMSL
004632 NDDF
1819 RXNORM
31684002 SNOMEDCT_US
387173000 SNOMEDCT_US
d00840 MMSL
257949 MMSL
CHEMBL511142 ChEMBL_ID
644073 PUBCHEM_CID
CHEMBL560511 ChEMBL_ID
CHEMBL1200401 ChEMBL_ID
D002047 MESH_DESCRIPTOR_UI
CHEMBL2368861 ChEMBL_ID
CHEBI:3216 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Buprenorphine HCl HUMAN PRESCRIPTION DRUG LABEL 1 0054-0176 TABLET 2 mg SUBLINGUAL ANDA 19 sections
Buprenorphine HCl HUMAN PRESCRIPTION DRUG LABEL 1 0054-0177 TABLET 8 mg SUBLINGUAL ANDA 19 sections
buprenorphine hydrochloride and naloxone hydrochloride dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0054-0188 TABLET 2 mg SUBLINGUAL ANDA 19 sections
buprenorphine hydrochloride and naloxone hydrochloride dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0054-0189 TABLET 8 mg SUBLINGUAL ANDA 19 sections
Buprenorphine HUMAN PRESCRIPTION DRUG LABEL 1 0093-3600 PATCH, EXTENDED RELEASE 5 ug TRANSDERMAL NDA authorized generic 21 sections
Buprenorphine HUMAN PRESCRIPTION DRUG LABEL 1 0093-3601 PATCH, EXTENDED RELEASE 10 ug TRANSDERMAL NDA authorized generic 21 sections
Buprenorphine HUMAN PRESCRIPTION DRUG LABEL 1 0093-3602 PATCH, EXTENDED RELEASE 15 ug TRANSDERMAL NDA authorized generic 21 sections
Buprenorphine HUMAN PRESCRIPTION DRUG LABEL 1 0093-3603 PATCH, EXTENDED RELEASE 20 ug TRANSDERMAL NDA authorized generic 21 sections
Buprenorphine HUMAN PRESCRIPTION DRUG LABEL 1 0093-5378 TABLET 2 mg SUBLINGUAL ANDA 19 sections
Buprenorphine HUMAN PRESCRIPTION DRUG LABEL 1 0093-5379 TABLET 8 mg SUBLINGUAL ANDA 19 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0093-5720 TABLET 2 mg SUBLINGUAL ANDA 19 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0093-5721 TABLET 8 mg SUBLINGUAL ANDA 19 sections
Buprenorphine HUMAN PRESCRIPTION DRUG LABEL 1 0228-3153 TABLET 8 mg SUBLINGUAL ANDA 19 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0228-3154 TABLET 2 mg SUBLINGUAL ANDA 19 sections
Buprenorphine and Naloxone HUMAN PRESCRIPTION DRUG LABEL 2 0228-3155 TABLET 8 mg SUBLINGUAL ANDA 19 sections
Buprenorphine HUMAN PRESCRIPTION DRUG LABEL 1 0228-3156 TABLET 2 mg SUBLINGUAL ANDA 19 sections
Buprenorphine Hydrochloride Sublingual HUMAN PRESCRIPTION DRUG LABEL 1 0378-0923 TABLET 2 mg SUBLINGUAL ANDA 19 sections
Buprenorphine Hydrochloride Sublingual HUMAN PRESCRIPTION DRUG LABEL 1 0378-0924 TABLET 8 mg SUBLINGUAL ANDA 19 sections
Buprenorphine HCl and Naloxone HCl HUMAN PRESCRIPTION DRUG LABEL 2 0406-1923 TABLET 2 mg SUBLINGUAL ANDA 19 sections
Buprenorphine HCl and Naloxone HCl HUMAN PRESCRIPTION DRUG LABEL 2 0406-1924 TABLET 8 mg SUBLINGUAL ANDA 19 sections
Buprenorphine Hydrochloride and Naloxone Hydrochloride Dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0406-8005 TABLET 2 mg SUBLINGUAL ANDA 18 sections
Buprenorphine Hydrochloride and Naloxone Hydrochloride Dihydrate HUMAN PRESCRIPTION DRUG LABEL 2 0406-8020 TABLET 8 mg SUBLINGUAL ANDA 18 sections
Buprenorphine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-2012 INJECTION, SOLUTION 0.30 mg INTRAMUSCULAR ANDA 15 sections
Buprenorphine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0517-0725 INJECTION, SOLUTION 0.32 mg INTRAMUSCULAR ANDA 13 sections
SUBLOCADE HUMAN PRESCRIPTION DRUG LABEL 1 12496-0100 SOLUTION 100 mg SUBCUTANEOUS NDA 19 sections
SUBLOCADE HUMAN PRESCRIPTION DRUG LABEL 1 12496-0300 SOLUTION 300 mg SUBCUTANEOUS NDA 19 sections
Buprenex HUMAN PRESCRIPTION DRUG LABEL 1 12496-0757 INJECTION 0.30 mg INTRAVENOUS NDA 14 sections
Suboxone HUMAN PRESCRIPTION DRUG LABEL 2 12496-1202 FILM, SOLUBLE 2 mg SUBLINGUAL NDA 18 sections
Suboxone HUMAN PRESCRIPTION DRUG LABEL 2 12496-1204 FILM, SOLUBLE 4 mg SUBLINGUAL NDA 18 sections
Suboxone HUMAN PRESCRIPTION DRUG LABEL 2 12496-1208 FILM, SOLUBLE 8 mg SUBLINGUAL NDA 18 sections