BUPRENORPHINE 8 mg Tablet, 30-count
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Partial Opioid Agonist class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Buprenorphine and the combination of buprenorphine and naloxone are used to treat opioid dependence (addiction to opioid drugs, including heroin and narcotic painkillers). Buprenorphine is in a class of medications called opioid partial agonist-antagonists and naloxone is in a class of medications called opioid antagonists. Buprenorphine alone and the combination of buprenorphine and naloxone work to prevent withdrawal symptoms when someone stops taking opioid drugs by producing similar effects to these drugs.
Read the full MedlinePlus article ↗- Buprenorphine helps your body and brain stabilize after opioid dependence. It works by partially activating the same receptors in the brain that opioids like heroin or prescription...
- What exactly is buprenorphine supposed to do for me?
- No — and this part really matters. You place the tablet under your tongue and let it fully dissolve there. Don't chew it, cut it, or swallow it whole. The medication is designed to...
- How do I take this tablet — do I just swallow it?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Buprenorphine — tap one for details:
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💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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UNII XF417D3PSL
Anhydrous citric acid is a sour, crystalline powder derived from citric acid with water removed. In medicines, it acts as a buffer to control pH, adds tartness to improve taste, and helps tablets disintegrate.
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UNII 2S7830E561
Crospovidone is a synthetic polymer derived from povidone. It acts as a disintegrant, helping the tablet or capsule break apart quickly in the stomach so the active ingredient can be absorbed.
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UNII EWQ57Q8I5X
Lactose monohydrate is a natural sugar derived from milk. It serves as a filler and binder in tablets and capsules, helping create the proper size, texture, and consistency of the medicine.
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UNII 70097M6I30
Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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UNII 3OWL53L36A
A natural sugar alcohol derived from seaweed or synthesized in the lab. It's used as a filler to add bulk, a sweetener in sugar-free formulas, and a disintegrant to help tablets break apart in the stomach.
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UNII U725QWY32X
Povidone K30 is a synthetic polymer made from petroleum. It acts as a binder to hold tablet ingredients together and as a disintegrant to help the tablet break apart in the stomach so the medicine can be absorbed.
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UNII O8232NY3SJ
A plant-based carbohydrate derived from corn kernels. It acts as a filler to add bulk, a binder to hold ingredients together, and a disintegrant to help the tablet break apart in your stomach for absorption.
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UNII B22547B95K
A salt derived from citric acid that helps maintain the proper acid-base balance in the medicine. It's used as a buffer to keep the product stable and at the right pH level.
8 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $0.568 | $17.03 / 30 tablets |
| Medicaid paysCMS SDUD · 12 mo | $0.9626 | $28.88 / 30 tablets |
| Medicare drug plans payPart D · Q2 2026 | $0.4294 | $12.88 / 30 tablets |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Buprenorphine 8 mg 00054-0177-13 | Hikma | 30 tablets | $0.568 | AB | Availability likely | — |
| buprenorphine hydrochloride 8 mg 00121-2038-30 | PAI | 30 tablets | $0.568 | AB | Availability likely | — |
| Buprenorphine 8 mg 00228-3153-03 | Actavis | 30 tablets | $0.568 | AB | Availability likely | — |
| Buprenorphine HCl 8 mg 00406-7018-03 | SpecGx | 30 tablets | $0.568 | AB | Availability likely | — |
| Buprenorphine 8 mg 00904-7155-04 | Major | 30 tablets | $0.568 | AB | Availability likely | — |
| Buprenorphine HCl 8 mg 31722-0871-30 | Camber | 30 tablets | $0.568 | AB | Availability likely | — |
| Buprenorphine 8 mgthis 42858-0502-03 | Rhodes | 30 tablets | $0.568 | AB | Availability likely | — |
| Buprenorphine 8 mg 50268-0129-15 | AvPAK | 50 tablets | $0.568 | AB | Availability likely | — |
| Buprenorphine 8 mg 60687-0492-21 | American | 30 tablets | $0.568 | AB | Availability likely | — |
| buprenorphine hydrochloride 8 mg 72888-0183-30 | Advagen | 30 tablets | $0.568 | — | Availability likely | — |
| Buprenorphine 8 mg 50090-5805-00 | A-S | 30 tablets | — | AB | FDA listed | — |
| buprenorphine hydrochloride 8 mg 50090-7559-00 | A-S | 30 tablets | — | AB | FDA listed | — |
| Buprenorphine HCl 8 mg 58118-0177-08 | Clinical | 30 tablets | — | AB | FDA listed | — |
| Buprenorphine 8 mg 58118-0460-08 | Clinical | 30 tablets | — | AB | FDA listed | — |
| Buprenorphine 8 mg 58118-0502-08 | Clinical | 30 tablets | — | AB | FDA listed | — |
| Buprenorphine 8 mg 62756-0460-64 | Sun | 30 tablets | — | AB | FDA listed | — |
| Buprenorphine 8 mg 67296-2173-03 | Redpharm | 30 tablets | — | AB | FDA listed | — |
| Buprenorphine HCl 8 mg 70518-2014-00 | REMEDYREPACK | 30 tablets | — | AB | FDA listed | — |
| buprenorphine hydrochloride 8 mg 70518-4571-00 | REMEDYREPACK | 30 tablets | — | AB | FDA listed | — |
| Buprenorphine 8 mg 71335-1154-00 | Bryant | 120 tablets | — | AB | FDA listed | — |
| Buprenorphine HCl 8 mg 71335-1163-00 | Bryant | 120 tablets | — | AB | FDA listed | — |
| Buprenorphine 8 mg 72162-1345-03 | Bryant | 30 tablets | — | AB | FDA listed | — |
| Buprenorphine Sublingual C-III 8 mg 72189-0582-60 | Direct_Rx | 60 tablets | — | AB | FDA listed | — |
| Buprenorphine 8 mg 71335-3152-00 | Bryant | 120 tablets | — | AB | FDA listed | — |
| Buprenorphine 8 mg 87441-0082-01 | Unit | 30 tablets | — | AB | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 42858-0502-03 You're viewing this | 30 TABLET in 1 BOTTLE (42858-502-03) | 2017-10-25 | Active |
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Buprenorphine Sublingual Tablets are indicated for the treatment of opioid dependence and are preferred for induction. Buprenorphine sublingual tablets should be used as part of a complete treatment plan to include counseling and psychosocial support. Buprenorphine sublingual tablets contain buprenorphine, a partial opioid agonist, and are indicated for the treatment of opioid dependence and are preferred for induction.
( 1 ) Buprenorphine sublingual tablets should be used as part of a complete treatment plan that includes counseling and psychosocial support. ( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Administer buprenorphine sublingual tablets sublingually as a single daily dose. ( 2.1 ) Strongly consider recommending or prescribing an opioid overdose reversal agent (e.g., naloxone, nalmefene) at the time buprenorphine sublingual tablets are 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 tablets should be undertaken when objective and clear signs of withdrawal are evident.
( 2.3 ) Buprenorphine and naloxone sublingual film or buprenorphine and naloxone sublingual tablets are 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 tablets 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 )
2.1Important Dosage and Administration Instructions Buprenorphine sublingual tablets are administered sublingually as a single daily dose. Buprenorphine sublingual tablets do not contain naloxone and are preferred for use only during induction. Following induction, buprenorphine and naloxone sublingual film or buprenorphine and naloxone sublingual tablets are preferred due to the presence of naloxone when clinical use includes unsupervised administration.
The use of buprenorphine sublingual tablets for unsupervised administration should be limited to those patients who cannot tolerate buprenorphine and naloxone sublingual film or buprenorphine and naloxone sublingual tablet; for example, those patients who have been shown to be hypersensitive to naloxone. Medication should be prescribed in consideration of the frequency of visits. Provision of multiple refills is not advised early in treatment or without appropriate patient follow-up visits.
2.2Patient Access to an Opioid Overdose Reversal Agent for the Emergency Treatment of Opioid Overdose Inform patients and caregivers about opioid overdose reversal agents (e.g., naloxone, nalmefene) and discuss the importance of having access to an opioid overdose reversal agent. Because patients being treated for opioid use disorder have the potential for relapse, putting them at risk for opioid overdose, strongly consider recommending or prescribing an overdose reversal agent for the emergency treatment of opioid overdose, both when initiating and renewing treatment with buprenorphine sublingual tablets.
Also consider recommending or prescribing such an agent if the patient has household members (including children) or other close contacts at risk for accidental ingestion or opioid overdose [see Warnings and Precautions (5.2) ]. Discuss the options for obtaining an opioid overdose reversal agent (e.g., prescription, over-the-counter, or as part of a community-based program) [see Warnings and Precautions (5.2) ] . There are important differences among the opioid overdose reversal agents, such as route of administration, product strength, approved patient age range, and pharmacokinetics.
Be familiar with these differences, as outlined in the approved labeling for those products, prior to recommending or prescribing such an agent. Advise patients and caregivers that opioid overdose reversal agents, such as naloxone or nalmefene, may also be administered for a known or suspected overdose with buprenorphine sublingual tablets itself. Higher than normal doses and repeated administration of an opioid overdose reversal agent may be necessary due to the long duration of action of buprenorphine sublingual tablets and its affinity for the mu receptor [see Overdosage (10) ] .
2.3Induction Prior to induction, consideration should be given to the type of opioid dependence (i.e., long- or sho…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Buprenorphine sublingual tablets are supplied as white to off-white, round, flat-faced, beveled edged tablets in two dosage strengths: buprenorphine 2 mg, and buprenorphine 8 mg Sublingual tablet: buprenorphine 2 mg and buprenorphine 8 mg. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS Buprenorphine sublingual tablets are 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. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS 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 tablets 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. ( 5.8 ) Precipitation of Opioid Withdrawal Signs and Symptoms : An opioid withdrawal syndrome is likely to occur with parenteral misuse of buprenorphine sublingual tablets by individuals physically dependent on full opioid agonists, or by sublingual administration before the agonist effects of other opioids have subsided. ( 5.10 ) Risk of Overdose in Opioid-Naïve Patients : Buprenorphine sublingual tablets are NOT appropriate as an analgesic.
There have been reported deaths of opioid naïve individuals who received a 2 mg sublingual dose of buprenorphine. ( 5.11 )
5.1Addiction, Abuse, and Misuse Buprenorphine sublingual tablets contain buprenorphine, a Schedule III controlled substance that can be abused in a manner similar to other opioids, legal or illicit. Prescribe and dispense buprenorphine with appropriate precautions to minimize risk of misuse, abuse, or diversion, and ensure appropriate protection from theft, including in the home. Clinical monitoring appropriate to the patient's level of stability is essential.
Multiple refills should not be prescribed early in treatment or without appropriate patient follow-up visits [see Drug Abuse and Dependence (9.2) ].
5.2Life-Threatening Respiratory Depression and Central Nervous System (CNS) Depression Buprenorphine has been associated with life-threating respiratory depression and death. Many, but not all, postmarketing reports regarding coma and death involved misuses by self-injection or were associated with the concomitant use of benzodiazepines or other CNS depressants, including alcohol. Warn patients of the potential danger of self-administration of benzodiazepines or other CNS depressants while under treatment with buprenorphine sublingual tablets [see Warning and Precautions (5.3) , Drug Interactions (7) ].
Use buprenorphine sublingual tablets with caution in patients with compromised respiratory function (e.g., chronic obstructive pulmonary disease, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression). Educate patients and caregivers on how to recognize respiratory depression and emphasize the importance of calling 911 or getting emergency medical help right away in the event of a known or suspected overdose [see Patient Counseling Information (17) ] . Opioids can cause sleep-related breathing disorders including central sleep apnea (CSA) and sleep-related hypoxemia.
Opioid use increases the risk of CSA in a dose-dependent fashion.…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS 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 Rhodes Pharmaceuticals LLC at 1-888-873-5329 or FDA at 1-800-FDA-1088, or www.fda.gov/medwatch
6.1Clinical 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. The safety of buprenorphine sublingual tablets was supported by clinical trials using buprenorphine sublingual tablets, buprenorphine and naloxone sublingual tablets, and other trials using buprenorphine sublingual solutions. In total, safety data were available from 3214 opioid-dependent subjects exposed to buprenorphine at doses in the range used in treatment of opioid addiction.
Few differences in adverse event profile were noted between buprenorphine sublingual tablets or buprenorphine administered as a sublingual solution. The following adverse events were reported to occur by at least 5% of patients in a 4-week study (Table 1). Table 1.
Adverse Events ≥ 5% by Body System and Treatment Group in a 4-week study N (%) N (%) Body System/Adverse Event (COSTART Terminology) Buprenorphine sublingual tablets 16 mg/day Placebo N=103 N=107 Body as a Whole Asthenia 5 (4.9%) 7 (6.5%) Chills 8 (7.8%) 8 (7.5%) Headache 30 (29.1%) 24 (22.4%) Infection 12 (11.7%) 7 (6.5%) Pain 19 (18.4%) 20 (18.7%) Pain Abdomen 12 (11.7%) 7 (6.5%) Pain Back 8 (7.8%) 12 (11.2%) Withdrawal Syndrome 19 (18.4%) 40 (37.4%) Cardiovascular System Vasodilation 4 (3.9%) 7 (6.5%) Digestive System Constipation 8 (7.8%) 3 (2.8%) Diarrhea 5 (4.9%) 16 (15.0%) Nausea 14 (13.6%) 12 (11.2%) Vomiting 8 (7.8%) 5 (4.7%) Nervous System Insomnia 22 (21.4%) 17 (15.9%) Respiratory System Rhinitis 10 (9.7%) 14 (13.1%) Skin and Appendages Sweating 13 (12.6%) 11 (10.3%) The adverse event profile of buprenorphine was also characterized in the dose-controlled study of buprenorphine solution, over a range of doses in four months of treatment.
Table 2 shows adverse events reported by at least 5% of subjects in any dose group in the dose-controlled study. Table 2. Adverse Events (≥ 5%) by Body System and Treatment Group in a 16-week Study Body System/Adverse Event (COSTART Terminology) Buprenorphine Dose Sublingual solution.
Doses in this table cannot necessarily be delivered in tablet form, but for comparison purposes: "Very low" dose (1 mg solution) would be less than a tablet dose of 2 mg "Low" dose (4 mg solution) approximates a 6 mg tablet dose "Moderate" dose (8 mg solution) approximates a 12 mg tablet dose "High" dose (16 mg solution) approximates a 24 mg tablet dose Very Low (N=184) Low (N=180) Moderate (N=186) High (N=181) Total (N=731) N (%) N (%) N (%) N (%) N (%) Body as a Whole Abscess 9 (5%) 2(1%) 3 (2%) 2 (1%) 16 (2%) Asthenia 26 (14%) 28 (16%) 26 (14%) 24 (13%) 104 (14%) Chills 11 (6%) 12 (7%) 9 (5%) 10 (6%…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Table 3 includes clinically significant drug interactions with buprenorphine sublingual tablets. Table 3. Clinically Significant Drug Interactions with Buprenorphine Sublingual Tablets Benzodiazepines or other Central Nervous System (CNS) Depressants Clinical Impact: Due to additive pharmacologic effects, the concomitant use of benzodiazepines or other CNS depressants, including alcohol, can increase the risk of hypotension, respiratory depression, profound sedation, coma, and death.
Intervention: Cessation of benzodiazepines or other CNS depressants is preferred in most cases of concomitant use. In some cases, monitoring in a higher level of care for taper may be appropriate. In others, gradually tapering a patient off of a prescribed benzodiazepine or CNS depressant or decreasing to the lowest effective dose may be appropriate.
Before co-prescribing benzodiazepines for anxiety or insomnia, ensure that patients are appropriately diagnosed and consider alternative medications and non-pharmacologic treatments [see Warnings and Precautions (5.2 , 5.3) ] . If concomitant use is warranted, strongly consider recommending or prescribing an opioid overdose reversal agent, as is recommended for all patients on buprenorphine treatment for opioid use disorder [see Warnings and Precautions (5.2) ]. Examples: Benzodiazepines and other sedatives/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, gabapentinoids (gabapentin or pregabalin), other opioids, alcohol.
Inhibitors of CYP3A4 Clinical Impact: The concomitant use of buprenorphine and CYP3A4 inhibitors can increase the plasma concentration of buprenorphine, resulting in increased or prolonged opioid effects, particularly when an inhibitor is added after a stable dose of buprenorphine sublingual tablets is achieved. After stopping a CYP3A4 inhibitor, as the effects of the inhibitor decline, the buprenorphine plasma concentration will decrease [see Clinical Pharmacology (12.3) ] , potentially resulting in decreased opioid efficacy or a withdrawal syndrome in patients who had developed physical dependence to buprenorphine.
Intervention: If concomitant use is necessary, consider dosage reduction of buprenorphine sublingual tablets until stable drug effects are achieved. Monitor patients for respiratory depression and sedation at frequent intervals. If a CYP3A4 inhibitor is discontinued, consider increasing the buprenorphine sublingual tablets dosage until stable drug effects are achieved.
Monitor for signs of opioid withdrawal. Examples: Macrolide antibiotics (e.g., erythromycin), azole-antifungal agents (e.g., ketoconazole), protease inhibitors (e.g., ritonavir) CYP3A4 Inducers Clinical Impact: The concomitant use of buprenorphine and CYP3A4 inducers can decrease the plasma concentration of buprenorphine [see Clinical Pharmacology (12.3) ] , potentially resulting in decreased efficacy or onset of a withdrawal syndrome in patients who have developed physical dependence to buprenorphine. After stopping a CYP3A4 inducer, as the effects of the inducer decline, the buprenorphine plasma concentration will increase [see Clinical Pharmacology (12.3) ] , which could increase or prolong both therapeutic effects and adverse reactions and may cause serious respiratory depression.
Intervention: If concomitant use is necessary, consider increasing the buprenorphine sublingual tablets dosage until stable drug effects are achieved. Monitor for signs of opioid withdrawal. If a CYP3A4 inducer is discontinued, consider buprenorphine sublingual tablets dosage reduction and monitor for signs of respiratory depression.
Examples: Rifampin, carbamazepine, phenytoin Antiretrovirals: Non-nucleoside reverse transcriptase inhibitors (NNRTIs) Clinical Impact: Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are metabolized principally by CYP3A4. Efavirenz, nevirapine, and etravirine are known CYP3A inducers, whereas delavirdine is a CYP3A inhibito…
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS 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 )
8.1Pregnancy 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. Pre- and post-natal development studies in rats demonstrated increased neonatal deaths at 0.3 times and above and dystocia at approximately 3 times the human sublingual dose of 16 mg/day of buprenorphine.
No clear teratogenic effects were seen when buprenorphine was administered during organogenesis with a range of doses equivalent to or greater than the human sublingual dose of 16 mg/day of buprenorphine. However, increases in skeletal abnormalities were noted in rats and rabbits administered buprenorphine daily during organogenesis at doses approximately 0.6 times and approximately equal to the human sublingual dose of 16 mg/day of buprenorphine, respectively. In a few studies, some events such as acephalus and omphalocele were also observed but these findings were not clearly treatment-related [see Data ] .
Based on animal data, advise pregnant women of the potential risk to a fetus. The estimated background risks of major birth defects and miscarriage for the indicated population are unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Clinical Considerations Disease-associated maternal and embryo-fetal risk Untreated opioid addiction in pregnancy is associated with adverse obstetrical outcomes such as low birth weight, preterm birth, and fetal death. In addition, untreated opioid addiction often results in continued or relapsing illicit opioid use.
Dose Adjustment during Pregnancy and the Postpartum Period Dosage adjustments of buprenorphine, such as higher doses, may be required during pregnancy, even if the patient was maintained on a stable dose prior to pregnancy. Dosing should be based on individual response, and withdrawal signs and symptoms should be monitored closely and the dose adjusted as necessary. Fetal/neonatal adverse reactions Neonatal opioid withdrawal syndrome may occur in newborn infants of mothers who are receiving treatment with buprenorphine sublingual tablets.
Neonatal opioid withdrawal syndrome presents as irritability, hyperactivity and abnormal sleep pattern, high pitched cry, tremor, vomiting, diarrhea, and/or failure to gain weight. Signs of neonatal withdrawal usually occur in the first days after birth. The duration and severity of neonatal opioid withdrawal syndrome may vary.
Observe newborns for signs of neonatal opioid withdrawal syndrome and manage accordingly [see Warnings and Precautions (5.5) ] . Labor or…
🤰 Pregnancy ▾
8.1Pregnancy 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. Pre- and post-natal development studies in rats demonstrated increased neonatal deaths at 0.3 times and above and dystocia at approximately 3 times the human sublingual dose of 16 mg/day of buprenorphine.
No clear teratogenic effects were seen when buprenorphine was administered during organogenesis with a range of doses equivalent to or greater than the human sublingual dose of 16 mg/day of buprenorphine. However, increases in skeletal abnormalities were noted in rats and rabbits administered buprenorphine daily during organogenesis at doses approximately 0.6 times and approximately equal to the human sublingual dose of 16 mg/day of buprenorphine, respectively. In a few studies, some events such as acephalus and omphalocele were also observed but these findings were not clearly treatment-related [see Data ] .
Based on animal data, advise pregnant women of the potential risk to a fetus. The estimated background risks of major birth defects and miscarriage for the indicated population are unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Clinical Considerations Disease-associated maternal and embryo-fetal risk Untreated opioid addiction in pregnancy is associated with adverse obstetrical outcomes such as low birth weight, preterm birth, and fetal death. In addition, untreated opioid addiction often results in continued or relapsing illicit opioid use.
Dose Adjustment during Pregnancy and the Postpartum Period Dosage adjustments of buprenorphine, such as higher doses, may be required during pregnancy, even if the patient was maintained on a stable dose prior to pregnancy. Dosing should be based on individual response, and withdrawal signs and symptoms should be monitored closely and the dose adjusted as necessary. Fetal/neonatal adverse reactions Neonatal opioid withdrawal syndrome may occur in newborn infants of mothers who are receiving treatment with buprenorphine sublingual tablets.
Neonatal opioid withdrawal syndrome presents as irritability, hyperactivity and abnormal sleep pattern, high pitched cry, tremor, vomiting, diarrhea, and/or failure to gain weight. Signs of neonatal withdrawal usually occur in the first days after birth. The duration and severity of neonatal opioid withdrawal syndrome may vary.
Observe newborns for signs of neonatal opioid withdrawal syndrome and manage accordingly [see Warnings and Precautions (5.5) ] . Labor or Delivery Opioid-dependent women on buprenorphine maintenance therapy may require additional analgesia during labor. Opioids cross the placenta and may produce respiratory depression and psycho-physiologic effects in neonates.
An opioid overdose reversal agent, such as naloxone or nalmefene, must be available for reversal of opioi…
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of buprenorphine sublingual tablets have not been established in pediatric patients.
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical studies of buprenorphine sublingual tablets, buprenorphine and naloxone sublingual film, or buprenorphine and naloxone sublingual tablet did not include sufficient numbers of subjects aged 65 and over to determine whether they responded differently than younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. Due to possible decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy in geriatric patients, the decision to prescribe buprenorphine sublingual tablets should be made cautiously in individuals 65 years of age or older and these patients should be monitored for signs and symptoms of toxicity or overdose.
🆘 Overdosage ▾
10 OVERDOSAGE Clinical Presentation The manifestations of acute overdose with buprenorphine sublingual tablets can include pinpoint pupils, sedation, hypotension, hypoglycemia, respiratory depression, and death. Toxic leukoencephalopathy has been reported after opioid overdose and can present hours, days, or weeks after apparent recovery from the initial intoxication. 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.
An opioid overdose reversal agent 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 tablets 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.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Buprenorphine sublingual tablets contain buprenorphine, a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor.
12.2Pharmacodynamics Subjective Effects Comparisons of buprenorphine to full opioid agonists such as methadone and hydromorphone suggest that sublingual buprenorphine produces typical opioid agonist effects which are limited by a ceiling effect. Opioid agonist ceiling-effects were also observed in a double-blind, parallel group, dose-ranging comparison of single doses of buprenorphine sublingual solution (1, 2, 4, 8, 16, or 32 mg), placebo, and a full agonist control at various doses. The treatments were given in ascending dose order at intervals of at least one week to 16 opioid-experienced subjects who were not physically dependent.
Both active drugs produced typical opioid agonist effects. For all measures for which the drugs produced an effect, buprenorphine produced a dose-related response. However, in each case, there was a dose that produced no further effect.
In contrast, the highest dose of the full agonist control always produced the greatest effects. Agonist objective rating scores remained elevated for the higher doses of buprenorphine (8 to 32 mg) longer than for the lower doses and did not return to baseline until 48 hours after drug administration. The onset of effects appeared more rapidly with buprenorphine than with the full agonist control, with most doses nearing peak effect after 100 minutes for buprenorphine compared to 150 minutes for the full agonist control.
Physiologic Effects Buprenorphine in IV (2, 4, 8, 12 and 16 mg) and sublingual (12 mg) doses have been administered to opioid-experienced subjects who were not physically dependent to examine cardiovascular, respiratory, and subjective effects at doses comparable to those used for treatment of opioid dependence. Compared to placebo, there were no statistically significant differences among any of the treatment conditions for blood pressure, heart rate, respiratory rate, O 2 saturation, or skin temperature across time.
Systolic BP was higher in the 8 mg group than placebo (3-hour AUC values). Minimum and maximum effects were similar across all treatments. Subjects remained responsive to low voice and responded to computer prompts.
Some subjects showed irritability, but no other changes were observed. The respiratory effects of sublingual buprenorphine were compared with the effects of methadone in a double-blind, parallel group, dose ranging comparison of single doses of buprenorphine sublingual solution (1, 2, 4, 8, 16, or 32 mg) and oral methadone (15, 30, 45, or 60 mg) in non-dependent, opioid-experienced volunteers. In this study, hypoventilation not requiring medical intervention was reported more frequently after buprenorphine doses of 4 mg and higher than after methadone.
Both drugs decreased O 2 saturation to the same degree. Effects on the Endocrine System Opioids inhibit the secretion of adrenocorticotropic hormone (ACTH), cortisol, and luteinizing hormone (LH) in humans [see Adverse Reactions (6.2) ] . They also stimulate prolactin, growth hormone (GH) secretion, and pancreatic secretion of insulin and glucagon.
Chronic use of opioids may influence the hypothalamic-pituitary-gonadal axis, leading to androgen deficiency that may manifest as low libido, impotence, erectile dysfunction, amenorrhea, or infertility. The causal role of opioids in the clinical syndrome of hypogonadism is unknown because the various medical, physical, lifestyle, and psychological stressors that may influence gonadal hormone levels have not been adequately controlled for in studies conducted to date. Patients presenting with symptoms of androgen deficiency should undergo laboratory evaluation.
Cardiac Electrophysiology Thorough QT studies with buprenorphine products have demonstrated QT prolongation ≤15 msec.
12.3 Pharmacokinetics Absorption Plasma levels of buprenorph…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Buprenorphine sublingual tablets contain buprenorphine, a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Buprenorphine Sublingual Tablets are available in the following strengths: 2 mg – White to off-white, round flat-faced beveled edged tablet debossed with "RP" on one side and "b2" on the other side (content expressed in terms of free base, equivalent to 2.16 mg buprenorphine hydrochloride USP). NDC 42858-501-03 30 tablets per bottle 8 mg – White to off-white, round flat-faced beveled edged tablet debossed with "RP" on one side and "b8" on the other side (content expressed in terms of free base, equivalent to 8.64 mg buprenorphine hydrochloride USP).
NDC 42858-502-03 30 tablets per bottle Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Store Buprenorphine Sublingual Tablets securely and dispose of properly [see Patient Counseling Information (17) ].
📦 Storage and Handling ▾
Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Store Buprenorphine Sublingual Tablets securely and dispose of properly [see Patient Counseling Information (17) ].
📋 Description ▾
11 DESCRIPTION Buprenorphine Sublingual Tablets are supplied as white to off white, round flat-faced beveled edged tablets debossed with "RP" on one side and an alphanumeric word identifying product and strength on the other side. They contain buprenorphine HCl, a partial agonist at the mu-opioid receptor, and are available in two dosage strengths, 2 mg buprenorphine and 8 mg buprenorphine (as the free base, equivalent to 2.16 mg buprenorphine hydrochloride USP and 8.64 mg buprenorphine hydrochloride USP, respectively).
Each tablet also contains lactose monohydrate, povidone K29/32, anhydrous citric acid, trisodium citrate dihydrate, corn starch, mannitol, crospovidone, and magnesium stearate. Chemically, buprenorphine HCl is (2S)-2-[17-Cyclopropylmethyl-4,5α-epoxy-3-hydroxy-6-methoxy- 6α,14-ethano-14α-morphinan-7α-yl]-3,3-dimethylbutan-2-ol hydrochloride. It has the following chemical structure: Buprenorphine HCl has the molecular formula C 29 H 41 NO 4 ∙ HCl and the molecular weight is 504.10.
It is a white or off-white crystalline powder, sparingly soluble in water, freely soluble in methanol, soluble in alcohol, and practically insoluble in cyclohexane. Chemical Structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise patients to read the FDA-approved patient labeling (Medication Guide). Storage and Disposal Because of the risks associated with accidental ingestion, misuse, and abuse, advise patients to store buprenorphine sublingual tablets securely, out of sight and reach of children, and in a location not accessible by others, including visitors to the home [see Warnings and Precautions (5.1 , 5.4) , Drug Abuse and Dependence (9.2) ] . Inform patients that leaving buprenorphine sublingual tablets unsecured can pose a deadly risk to others in the home.
Advise patients and caregivers that when medicines are no longer needed, they should be disposed of promptly. Expired, unwanted, or unused buprenorphine sublingual tablets should be disposed of by flushing the unused medication down the toilet if a drug take-back option is not readily available. Inform patients that they can visit www.fda.gov/drugdisposal for a complete list of medicines recommended for disposal by flushing, as well as additional information on disposal of unused medicines.
Safe Use Before initiating treatment with buprenorphine sublingual tablets, explain the points listed below to caregivers and patients. Instruct patients to read the Medication Guide each time buprenorphine sublingual tablets are dispensed because new information may be available. Inform patients and caregivers that potentially fatal additive effects may occur if buprenorphine sublingual tablets are used with benzodiazepines or other CNS depressants (e.g., alcohol, non-benzodiazepine sedatives/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, gabapentinoids [gabapentin or pregabalin], and other opioids).
Counsel patients that such medications should not be used concomitantly unless supervised by a health care provider [see Warnings and Precautions (5.2 , 5.3) , Drug Interactions (7) ] . Educate patients and caregivers on how to recognize respiratory depression and emphasize the importance of calling 911 or getting emergency medical help right away in the event of a known or suspected overdose [see Warnings and Precautions (5.2) ]. Patient Access to an Opioid Overdose Reversal Agent for the Emergency Treatment of Opioid Overdose Inform patients and caregivers about opioid overdose reversal agents (e.g., naloxone, nalmefene) and discuss the importance of having access to an opioid overdose reversal agent.
Because patients being treated for opioid use disorder are at risk for relapse, discuss the importance of having access to an opioid overdose reversal agent. Also discuss the importance of having access to an opioid overdose reversal agent if there are household members (including children) or other close contacts at risk for accidental ingestion or opioid overdose. Discuss with the patient the options for obtaining an opioid overdose reversal agent (e.g., prescription, over-the-counter (some products), or as part of a community-based program) [see Dosage and Administration (2.2) , Warnings and Precautions (5.2) ] .
There are important differences among the opioid overdose reversal agents. Be familiar with these differences, as outlined in the approved labeling for those products, prior to recommending or prescribing such an agent. Educate patients and caregivers on how to recognize the signs and symptoms of an opioid overdose.
Explain to patients and caregivers that effects of opioid overdose reversal agents like naloxone and nalmefene are temporary, and that they must call 911 or get emergency medical help right away in all cases of known or suspected opioid overdose, even if an opioid overdose reversal agent is administered. Repeat administration may be necessary, particularly for overdose involving buprenorphine [see Dosage and Administration (2.2) , Warnings and Precautions (5.2) , Overdosage (10) ]. Advise patients and caregivers: how to treat with an opioid overdose reversal agent in the event of an opioid overdose…
💬 Medication Guide ▾
MEDICATION GUIDE Buprenorphine (byoo-pre-NOR-feen) Sublingual Tablets, CIII IMPORTANT: Keep buprenorphine sublingual tablets in a secure place away from children. Accidental use by a child is a medical emergency and can result in death. If a child accidentally takes buprenorphine sublingual tablets, get emergency help or call 911 right away.
Tell your healthcare provider if you are living in a household where there are small children. What is the most important information I should know about buprenorphine sublingual tablets? Buprenorphine sublingual tablets contain a medicine called buprenorphine.
Buprenorphine is an opioid that can cause serious and life-threatening breathing problems, especially if you take or use certain other medicines or drugs. Ask your healthcare provider about medicines like naloxone or nalmefene that can be used in an emergency to reverse opioid overdose including accidental use of buprenorphine sublingual tablets by a child. If naloxone or nalmefene is given, you must call 911 or get emergency medical help right away to treat an overdose or accidental use of an opioid.
Buprenorphine sublingual tablets may cause serious and life-threatening breathing problems. Get emergency help right away if you: feel faint have blurred vision feel dizzy have slurred speech are confused are breathing slower than normal feel sleepy or uncoordinated cannot think well or clearly Do not take buprenorphine sublingual tablets with certain medicines. Taking buprenorphine sublingual tablets with other opioid medicines, benzodiazepines, gabapentinoids (gabapentin or pregabalin), alcohol, or other central nervous system depressants (including street drugs) can cause severe drowsiness, decreased awareness, breathing problems, coma, and death.
Do not inject ("shoot-up") buprenorphine sublingual tablets . Injecting buprenorphine sublingual tablets may cause life-threatening infections and other serious health problems. Do not switch from buprenorphine sublingual tablets to other medicines that contain buprenorphine without talking with your healthcare provider.
The amount of buprenorphine in a dose of buprenorphine sublingual tablets is not the same as in other medicines that contain buprenorphine. Your healthcare provider will prescribe a starting dose of buprenorphine sublingual tablets that may be different than other buprenorphine containing medicines you may have been taking. Do not stop taking buprenorphine sublingual tablets suddenly.
You could become sick and have withdrawal symptoms because your body has become used to the medicine (physical dependence). Physical dependence is not the same as drug addiction. In an emergency, have family members tell emergency department staff that you are physically dependent on an opioid and are being treated with buprenorphine sublingual tablets.
Never give anyone else your buprenorphine sublingual tablets. They could die from taking it. Selling or giving away buprenorphine sublingual tablets is against the law.
Store buprenorphine sublingual tablets securely, out of sight and reach of children, and in a location not accessible by others, including visitors to the home. What are buprenorphine sublingual tablets? Buprenorphine sublingual tablets are a prescription medicine used to treat opioid addiction in adults and is part of a complete treatment program that also includes counseling and behavioral therapy.
Who should not take buprenorphine sublingual tablets? Do not take buprenorphine sublingual tablets if you are allergic to buprenorphine. Before taking buprenorphine sublingual tablets, tell your healthcare provider about all of your medical conditions, including if you have: trouble breathing or lung problems an enlarged prostate (men) a head injury or brain problem a curve in your spine that affects your breathing problems urinating mental health problems Addison's disease liver, kidney, or gallbladder problems adrenal gland or thyroid gland problems alcoholism tooth problems, inc…