Buprenorphine

Buprenorphine sublingual tablet contains buprenorphine, a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor.

• Buprenorphine sublingual tablet is indicated for the treatment of opioid dependence and is preferred for induction. Buprenorphine sublingual tablet should be used as part of a complete treatment plan to include counseling and psychosocial support.ICD-10: F11.20

• Buprenorphine sublingual tablet is contraindicated in patients with a history of hypersensitivity to buprenorphine, as serious adverse reactions, including anaphylactic shock, have been reported [see Warnings and Precautions (5.9)]. Hypersensitivity to buprenorphine.contraindicated

Administer buprenorphine sublingual tablet sublingually as a single daily dose. (2.1) Strongly consider prescribing naloxone at the time buprenorphine sublingual tablet is initiated or renewed because patients being treated for opioid use disorder have the potential for relapse, putting them at risk for opioid overdose. (2.2) To avoid precipitating withdrawal, induction with buprenorphine sublingual tablet should be undertaken when objective and clear signs of withdrawal are evident. (2.3) Buprenorphine and naloxone sublingual film or buprenorphine and naloxone sublingual tablet is generally initiated after two days of buprenorphine sublingual tablet titration. (2.4) Administer buprenorphine sublingual tablets as directed in the Full Prescribing Information. (2.3, 2.4, 2.5) Buprenorphine sublingual tablet must be administered whole. Do not cut, chew, or swallow buprenorphine sublingual tablets. (2.5) When discontinuing treatment, gradually taper to avoid signs and symptoms of withdrawal. (2.9) 2.1 Important Dosage and Administration Instructions Buprenorphine sublingual tablet is administered sublingually as a single daily dose. Buprenorphine sublingual tablet does not contain naloxone and is preferred for use only during induction. Following induction, buprenorphine and naloxone sublingual film or buprenorphine and naloxone sublingual tablet is preferred due to the presence of naloxone when clinical use includes unsupervised administration.

Addiction, Abuse, and Misuse: Buprenorphine can be abused in a similar manner to other opioids. Monitor patients for conditions indicative of diversion or progression of opioid dependence and addictive behaviors. Multiple refills should not be prescribed early in treatment or without appropriate patient follow-up visits. (5.1) Respiratory Depression: Life-threatening respiratory depression and death have occurred in association with buprenorphine use. Warn patients of the potential danger of self-administration of benzodiazepines or other CNS depressants while under treatment with buprenorphine sublingual tablets. (5.2, 5.3) Unintentional Pediatric Exposure : Store buprenorphine sublingual tablet safely out of the sight and reach of children. Buprenorphine can cause severe, possibly fatal, respiratory depression in children. (5.4) Neonatal Opioid Withdrawal Syndrome : Neonatal opioid withdrawal syndrome (NOWS) is an expected and treatable outcome of prolonged use of opioids during pregnancy. (5.5) Adrenal Insufficiency: If diagnosed, treat with physiologic replacement of corticosteroids, and wean patient off of the opioid. (5.6) Risk of Opioid Withdrawal with Abrupt Discontinuation : If treatment is temporarily interrupted or discontinued, monitor patients for withdrawal and treat appropriately. (5.7) Risk of Hepatitis, Hepatic Events : Monitor liver function tests prior to initiation and during treatment and evaluate suspected hepatic events.

The following serious adverse reactions are described elsewhere in the labeling: • Addiction, Abuse, and Misuse [see Warnings and Precautions (5.1)] • Respiratory and CNS Depression [see Warnings and Precautions (5.2, 5.3)] • Neonatal Opioid Withdrawal Syndrome [see Warnings and Precautions (5.5)] • Adrenal Insufficiency [see Warnings and Precautions (5.6)] • Opioid Withdrawal [see Warnings and Precautions (5.7, 5.10)] • Hepatitis, Hepatic Events [see Warnings and Precautions (5.8)] • Hypersensitivity Reactions [see Warnings and Precautions (5.9)] • Orthostatic Hypotension [see Warnings and Precautions (5.16)] • Elevation of Cerebrospinal Fluid Pressure [see Warnings and Precautions (5.17)] • Elevation of Intracholedochal Pressure [see Warnings and Precautions (5.18)] Adverse events commonly observed with administration of buprenorphine are oral hypoesthesia, glossodynia, oral mucosal erythema, headache, nausea, vomiting, hyperhidrosis, constipation, signs and symptoms of withdrawal, insomnia, pain, and peripheral edema. ( 6 )To report SUSPECTED ADVERSE REACTIONS, contact Sun Pharmaceutical Industries, Inc. at 1-800-818-4555 or FDA at 1-800-FDA-1088, or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

• Lactation: Buprenorphine passes into mother’s milk. ( 8.2 ) • Geriatric Patients: Monitor for sedation or respiratory depression. ( 8.5 ) • Severe Hepatic Impairment: Consider reducing the starting and titration incremental dose by half and monitor for signs and symptoms of toxicity or overdose. ( 8.6 ) 8.1 Pregnancy Risk Summary The data on use of buprenorphine, the active ingredient in buprenorphine sublingual tablets, in pregnancy, are limited; however, these data do not indicate an increased risk of major malformations specifically due to buprenorphine exposure. There are limited data from randomized clinical trials in women maintained on buprenorphine that were not designed appropriately to assess the risk of major malformations [see Data]. Observational studies have reported on congenital malformations among buprenorphine‐exposed pregnancies, but were also not designed appropriately to assess the risk of congenital malformations specifically due to buprenorphine exposure [see Data]. Reproductive and developmental studies in rats and rabbits identified adverse events at clinically relevant and higher doses. Embryofetal death was observed in both rats and rabbits administered buprenorphine during the period of organogenesis at doses approximately 6 and 0.3 times, respectively, the human sublingual dose of 16 mg/day of buprenorphine.

Metabolism

Absorption Plasma levels of buprenorphine increased with the sublingual dose of buprenorphine sublingual tablet (Table 3). There was wide inter-patient variability in the sublingual absorption of buprenorphine, but within subjects the variability was low.

Clinical Presentation The manifestations of acute overdose include pinpoint pupils, sedation, hypotension, hypoglycemia, respiratory depression, and death. Treatment of Overdose In the event of overdose, the respiratory and cardiac status of the patient should be monitored carefully. When respiratory or cardiac functions are depressed, primary attention should be given to the re-establishment of adequate respiratory exchange through provision of a patent airway and institution of assisted or controlled ventilation. Oxygen, IV fluids, vasopressors, and other supportive measures should be employed as indicated. In the case of overdose, the primary management should be the re-establishment of adequate ventilation with mechanical assistance of respiration, if required. Naloxone may be of value for the management of buprenorphine overdose. Higher than normal doses and repeated administration may be necessary. The long duration of action of buprenorphine sublingual tablet should be taken into consideration when determining the length of treatment and medical surveillance needed to reverse the effects of an overdose. Insufficient duration of monitoring may put patients at risk.

• Jun 3, 1996ANDAANDA074137Hospira
• Mar 2, 2005ANDAANDA076931Hikma
• Jun 30, 2010NDANDA021306Knoa Pharma
• Aug 30, 2010NDANDA022410Indivior
• Jul 3, 2013NDANDA204242Edenbridge Pharms
• Oct 23, 2015NDANDA207932Bdsi
• Nov 30, 2017NDANDA209819Indivior
• May 23, 2023NDANDA210136Braeburn

Recent PubMed references pinned to Buprenorphine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Should We Consider the Use of Buprenorphine for Pain Management in Nonsurgical Candidates With End-stage Osteoarthritis? A Case Report.
  WMJ : official publication of the State Medical Society of Wisconsin · 2026 · Licata T, Clements A
  PMID 42258666
• Investigating craving as an indicator of early response to buprenorphine treatment among adults with opioid use disorder.
  Journal of consulting and clinical psychology · 2026 · Votaw VR, London Z, Bailey AJ, et al.
  PMID 42241061DOI 10.1037/ccp0001013
• Buprenorphine transdermal patch induced intractable vomiting in a low backache patient. Are unmonitored patches safe?
  The National medical journal of India · 2026 · Khandelwal A, Bhattacharjee A, Ahmed KA, et al.
  PMID 42240492DOI 10.25259/NMJI_829_2024
• Emergency Department-initiated standard versus high-dose buprenorphine induction (ENVISION): a randomised clinical trial protocol.
  BMJ open · 2026 · Hawk K, Herring A, Chawarski M, et al.
  PMID 42236100DOI 10.1136/bmjopen-2025-113762
• Street Pharmacology: The Mechanistic Basis of Clinical Pharmacology Underlying the Microdosing Method of Buprenorphine-Naloxone With a Focus on the Unhoused Population.
  Journal of clinical pharmacology · 2026 · Lehmann DF, Tanner O, Pepple E, et al.
  PMID 42227733DOI 10.1002/jcph.70213
• Buprenorphine extended-release (Ethiqa XR) impacts the immunological response in mice exposed to aerosolized Burkholderia pseudomallei or Yersinia pestis.
  Frontiers in immunology · 2026 · Rodriguez CI, Klimko CP, Davies ML, et al.
  PMID 42212153DOI 10.3389/fimmu.2026.1823747
• High-Deductible Health Plan Enrollment and Buprenorphine Dispensing.
  JAMA network open · 2026 · Chua KP, Bohnert AS, Conti RM, et al.
  PMID 42207512DOI 10.1001/jamanetworkopen.2026.15550
• Brain white matter microstructural integrity differences between pre-post buprenorphine-naloxone treated individuals with opioid use disorder: Evidence from a DTI study.
  Psychiatry research. Neuroimaging · 2026 · Kaur S, Verma A, Ghosh A, et al.
  PMID 42191416DOI 10.1016/j.pscychresns.2026.112248

The 10 most recently updated of 770 ClinicalTrials.gov registrations naming Buprenorphine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Coordinating Outpatient bupreNorphiNe for Emergency Care and Continuing Treatment
  Recruiting · Interventional · 3,492 enrolled · University of California, Davis
  NCT07024498updated 2026-06-12
• Prolonged Exposure Therapy for PTSD and Opioid Use Disorder
  Completed · Interventional · 82 enrolled · University of Vermont
  NCT04104022updated 2026-06-11
• Adaptive Decision Support for Addiction Treatment Master
  Recruiting · Interventional · 1,912 enrolled · Yale University
  NCT06799117updated 2026-06-11
• PRimary Care Opioid Use Disorders Treatment (PROUD) Trial
  Completed · Interventional · 377,373 enrolled · Kaiser Permanente
  NCT03407638updated 2026-06-11
• Enhancing Addiction Treatment Through Psychoeducation
  Not yet recruiting · Interventional · 40 enrolled · Virginia Commonwealth University
  NCT07178158updated 2026-06-09
• Improving Access to Opioid Use Disorder Treatment Among Marginalized Patients With a Tailored Telehealth Intervention
  Not yet recruiting · Interventional · 60 enrolled · University of Pennsylvania
  NCT06341608updated 2026-06-09
• Better Experiences in Substance Treatment: A Brief Alcohol-focused Intervention Tailored for Patients in Opioid Agonist Treatment
  Recruiting · Interventional · 60 enrolled · University of Notre Dame
  NCT07342504updated 2026-06-09
• Dronabinol and Epidiolex to Manage Uncontrolled Residual Symptoms of Buprenorphine Initiation Trial
  Not yet recruiting · Phase 3 · Interventional · 40 enrolled · Montefiore Medical Center
  NCT07148206updated 2026-06-09
• Buprenorphine Implementation at Syringe Service Programs to Reduce Overdoses
  Not yet recruiting · Interventional · 512 enrolled · Montefiore Medical Center
  NCT07631598updated 2026-06-08
• Outcome Inference in the Sensory Preconditioning Task in Opioid-Use Disorder
  Recruiting · Observational · 150 enrolled · National Institute on Drug Abuse (NIDA)
  NCT03745339updated 2026-06-08

CPIC-curated drug–gene pairs for Buprenorphine. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• COMTCPIC CClinPGx 3
  CYP2D6, OPRM1, COMT, and Opioids
• OPRM1CPIC CClinPGx 3
  CYP2D6, OPRM1, COMT, and Opioids

Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

• MorphineOpioid Agonist92%
• CodeineOpium alkaloids and derivatives92%
• NaltrexoneOpioid Antagonist85%
• HydromorphoneOpioid Agonist84%
• NaloxoneOpioid Antagonist84%
• HydrocodoneOpioid Agonist83%
• OxymorphoneOpioid Agonist83%
• OxycodoneOpioid Agonist83%

Frequently asked questions

How does Buprenorphine work?

Buprenorphine sublingual tablet contains buprenorphine, a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor.

What is Buprenorphine used for?

According to FDA labeling, Buprenorphine carries indications including: Buprenorphine sublingual tablet is indicated for the treatment of opioid dependence and is preferred for induction. Buprenorphine sublingual tablet should be used as part of a complete treatment plan to include counseling and psychosocial support.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Buprenorphine?

Buprenorphine is classified as Drugs used in opioid dependence, Oripavine derivatives, Partial Opioid Agonist, Opioid Antagonists, Partial Opioid Agonists, Decreased Organized Electrical Activity.

What are the brand names for Buprenorphine?

Buprenorphine is marketed under brand names including Belbuca, Brixadi, BuTrans, Bunavail, Buprenex, Simbadol, Sublocade, Suboxone.

What are the contraindications for Buprenorphine?

Buprenorphine labeling lists contraindications including: Buprenorphine sublingual tablet is contraindicated in patients with a history of hypersensitivity to buprenorphine, as serious adverse reactions, including anaphylactic shock, have been reported [see Warnings and Precautions (5.9)]. Hypersensitivity to buprenorphine.. Always consult the full prescribing information and a clinician.