Buprenorphine, sold under the brand name Subutex, among others, is an opioid used to treat opioid use disorder, acute pain, and chronic pain. It can be used under the tongue, in the cheek, by injection, as a skin patch, or as an implant. Wikipedia
Elimination half-life: 37 hours (range 20–70 hours)
Onset of action: Within 30 min
Duration of action: Up to 24 hrs
Excretion: Biliary and kidney
- Buprenorfina [INN-Spanish]
- Buprenorphinum [INN-Latin]
- DEA No. 9064
- RX 6029M
- EINECS 257-950-6
- Temgesic (TN)
- Buprenorphine (JAN/INN)
- Buprenorphine [INN:BAN:JAN]
- Buprenorphine (BN)
- Sixmo (buprenorphine hydrochloride)
- [5?,7?(S)]-?-tert-butyl-17-(cyclopropylmethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-?-methyl-6,14-ethenomorphinan-7-methanol hydrochloride;[5a,7a(S)]-a-tert-butyl-17-(cyclopropylmethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-a-methyl-6,14-ethenomorphinan-7-methanol hydrochloride;Buprenorphine hydrochloride
- 6,14-Ethenomorphinan-7-methanol, 17-(cyclopropylmethyl)-alpha-(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-alpha-methyl-, (5-alpha,7-alpha-(S))-
- 6,14-ethenomorphinan-3-ol, 17-(cyclopropylmethyl)-4,5-epoxy-18,19-dihydro-7-[(1S)-1-hydroxy-1,2,2-trimethylpropyl]-6-methoxy-, (5alpha,7alpha)-
- 6,14-Ethenomorphinan-7-methanol, 17-(cyclopropylmethyl)-alpha-(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-alpha-methyl-,
- 6,14-Ethenomorphinan-7-methanol, 17-(cyclopropylmethyl)-alpha-(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-alpha-methyl-, (alphaS,5alpha,7alpha)- (9CI)
DEA Controlled Substances
|Synonym(s)||Buprenex, Temgesic, Subutex, Suboxone|
|DEA Controlled Substances Code Number||9064|
|Controlled Substances Act Schedule||Schedule III – Substances in the DEA Schedule III have a potential for abuse less than substances in Schedules I or II and abuse may lead to moderate or low physical dependence or high psychological dependence.|
Why is this medication prescribed?
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.
How should this medicine be used?
Buprenorphine (BYOO-pre-NOR-feen) (‘bu-pre-‘nor-feen) is an opioid medication used to treat opioid addiction in the privacy of a physician’s office. 1. Buprenorphine can be dispensed for take home use, by prescription. (source)
Buprenorphine comes as a sublingual tablet. The combination of buprenorphine and naloxone comes as a sublingual tablet (Zubsolv) and as a sublingual film (Suboxone) to take under the tongue and as a buccal film (Bunavail) to apply between the gum and cheek. After your doctor determines an appropriate dose, these products are usually taken once a day. To help you remember to take or apply buprenorphine or buprenorphine and naloxone, take or apply it around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand.
Take or apply buprenorphine or buprenorphine and naloxone exactly as directed. Do not take or apply more or less of it or take or apply it more often than prescribed by your doctor.
Your doctor may decide to start your treatment with buprenorphine, which you will take in the doctor’s office. You will start on a low dose of buprenorphine and your doctor will increase your dose for 1 or 2 days before switching you to buprenorphine and naloxone. Depending on the type of opioid that you were taking, a different option that your doctor may choose is to start you on treatment with buprenorphine and naloxone right away. Your doctor may increase or decrease your buprenorphine and naloxone dose depending on your response.
If you are taking the sublingual tablets, place the tablets under your tongue until they completely melt. If you are taking more than two tablets, either place them all under your tongue at the same time or place them under your tongue up to two at a time. Do not chew the tablets or swallow them whole. Do not eat, drink, or talk until the tablet dissolves completely.
If you are using the buccal film, use your tongue to wet the inside of your cheek or rinse your mouth with water before you apply the film. Apply the film with a dry finger against the inside of the cheek. Then remove your finger and the film will stick to the inside of your cheek. If you are to use two films, place another film on the inside of your other cheek at the same time. Do not apply films on top of each other and do not apply more than two films to the inside of the mouth at one time. Leave the film(s) in the mouth until they dissolve. Do not cut, tear, chew, swallow, touch or move the film while it dissolves. Do not eat or drink anything until the film dissolves completely.
If you are using the sublingual film, rinse your mouth with water before you place the film. Place the film with a dry finger under your tongue to the right or left of the center and hold the film in place for 5 seconds. If you are using two films, place the other one on the opposite side under the tongue. Do not put the films on top of or near each other. Do not use more than two films at one time. Do not cut, tear, chew, swallow, touch or move the film while it dissolves. Do not eat or drink anything until the film dissolves completely.
If you need to switch from one buprenorphine or buprenorphine and naloxone product to another, your doctor may need to adjust your dose. Each time you receive your medication, check to be sure that you have received the buprenorphine product that was prescribed for you. Ask your pharmacist if you have are not sure that you received the right medication.
Do not stop taking or using buprenorphine or buprenorphine and naloxone without talking to your doctor. Stopping buprenorphine or buprenorphine and naloxone too quickly can cause withdrawal symptoms. Your doctor will tell you when and how to stop taking or using buprenorphine or buprenorphine and naloxone. If you suddenly stop taking or using buprenorphine or buprenorphine and naloxone, you may experience withdrawal symptoms such as hot or cold flushes, restlessness, teary eyes, runny nose, sweating, chills, muscle pain, vomiting, or diarrhea.
What side effects can this medication cause?
Buprenorphine or buprenorphine and naloxone may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
- stomach pain
- difficulty falling asleep or staying asleep
- mouth numbness or redness
- tongue pain
- blurred vision
- back pain
Some side effects can be serious. If you experience any of these symptoms or those listed in the IMPORTANT WARNINGS or SPECIAL PRECAUTIONS sections, call your doctor immediately:
- difficulty breathing or swallowing
- swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
- agitation, hallucinations (seeing things or hearing voices that do not exist), fever, sweating, confusion, fast heartbeat, shivering, severe muscle stiffness or twitching, loss of coordination, nausea, vomiting, or diarrhea
- nausea, vomiting, loss of appetite, weakness, or dizziness
- inability to get or keep an erection
- irregular menstruation
- decreased sexual desire
- slowed breathing
- upset stomach
- extreme tiredness
- blurred vision
- slurred speech
- unusual bleeding or bruising
- lack of energy
- pain in the upper right part of the stomach
- yellowing of the skin or eyes
- dark-colored urine
- light-colored stools
Buprenorphine or buprenorphine and naloxone may cause other side effects. Call your doctor if you have any unusual problems while taking or using this medication.
If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088). (source)
Opioid Use Disorder
Buprenorphine is used to treat people with opioid use disorder. The combination formulation of buprenorphine/naloxone is generally preferred as naloxone, an opioid antagonist, has a higher bioavailability intravenously and results in acute withdrawal if the formulation is crushed and injected. Prior to starting buprenorphine, individuals should wait long enough after their last dose of opioid until they have some withdrawal symptoms to allow for the medication to bind the receptors, but if taken too soon, buprenorphine can displace other opioids bound to the receptors and precipitate an acute withdrawal. The dose of buprenorphine is then adjusted until symptoms improve, and individuals remain on a maintenance dose through treatment.
In case of emergency/overdose
In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can’t be awakened, immediately call emergency services at 911.
Symptoms of overdose may include the following:
- pinpoint pupils
- extreme drowsiness
- blurred vision
- slowed breathing
SUBUTEX sublingual tablet, contains buprenorphine, a partial opioid agonist, and is indicated for the treatment of opioid dependence and is preferred for. induction. Prescription use of this product is limited under the Drug. Addiction Treatment Act.
SUBUTEX (buprenorphine) sublingual tablet is an uncoated oval white flat bevelled edged tablet, debossed with an alphanumeric word identifying the product and strength on one side. It contains buprenorphine HCl, a partial agonist at the mu-opioid receptor, and is 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). Each tablet also contains lactose, mannitol, cornstarch, povidone K30, citric acid, sodium citrate and magnesium stearate.
Chemically, buprenorphine HCl is (2S)-2-[17-Cyclopropylmethyl-4,5α-epoxy-3-hydroxy-6-methoxy6α,14-ethano-14α-morphinan-7α-yl]-3,3-dimethylbutan-2-ol hydrochloride. It has the following chemical structure:
Addiction, Abuse, And Misuse
SUBUTEX contains 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 patientâ€™s level of stability is essential. Multiple refills should not be prescribed early in treatment or without appropriate patient follow-up visits.
Risk Of Life-Threatening Respiratory And Central Nervous System (CNS) Depression
Buprenorphine has been associated with life-threating respiratory depression and death. Many, but not all, post-marketing 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 SUBUTEX.
Use SUBUTEX 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).
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. In patients who present with CSA, consider decreasing the opioid dosage using best practices for opioid taper.
Managing Risks From Concomitant Use Of Benzodiazepines Or Other CNS Depressants
Concomitant use of buprenorphine and benzodiazepines or other CNS depressants increases the risk of adverse reactions including overdose and death. Medication-assisted treatment of opioid use disorder, however, should not be categorically denied to patients taking these drugs. Prohibiting or creating barriers to treatment can pose an even greater risk of morbidity and mortality due to the opioid use disorder alone.
As a routine part of orientation to buprenorphine treatment, educate patients about the risks of concomitant use of benzodiazepines, sedatives, opioid analgesics, and alcohol.
Develop strategies to manage use of prescribed or illicit benzodiazepines or other CNS depressants at initiation of buprenorphine treatment, or if it emerges as a concern during treatment. Adjustments to induction procedures and additional monitoring may be required. There is no evidence to support dose limitations or arbitrary caps of buprenorphine as a strategy to address benzodiazepine use in buprenorphine-treated patients. However, if a patient is sedated at the time of buprenorphine dosing, delay or omit the buprenorphine dose if appropriate.
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 other CNS depressant or decreasing to the lowest effective dose may be appropriate.
For patients in buprenorphine treatment, benzodiazepines are not the treatment of choice for anxiety or insomnia. Before co-prescribing benzodiazepines, ensure that patients are appropriately diagnosed and consider alternative medications and non-pharmacologic treatments to address anxiety or insomnia. Ensure that other healthcare providers prescribing benzodiazepines or other CNS depressants are aware of the patientâ€™s buprenorphine treatment and coordinate care to minimize the risks associated with concomitant use.
In addition, take measures to confirm that patients are taking their medications as prescribed and are not diverting or supplementing with illicit drugs. Toxicology screening should test for prescribed and illicit benzodiazepines.
Unintentional Pediatric Exposure
Buprenorphine can cause severe, possibly fatal, respiratory depression in children who are accidentally exposed to it. Store buprenorphine-containing medications safely out of the sight and reach of children and destroy any unused medication appropriately
Neonatal Opioid Withdrawal Syndrome
Neonatal opioid withdrawal syndrome (NOWS) is an expected and treatable outcome of prolonged use of opioids during pregnancy, whether that use is medically-authorized or illicit. Unlike opioid withdrawal syndrome in adults, NOWS may be life-threatening if not recognized and treated in the neonate. Healthcare professionals should observe newborns for signs of NOWS and manage accordingly [see Use In Specific Populations].
Advise pregnant women receiving opioid addiction treatment with SUBUTEX of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available [see Use In Specific Populations]. This risk must be balanced against the risk of untreated opioid addiction which often results in continued or relapsing illicit opioid use and is associated with poor pregnancy outcomes. Therefore, prescribers should discuss the importance and benefits of management of opioid addiction throughout pregnancy.
Cases of adrenal insufficiency have been reported with opioid use, more often following greater than one month of use. Presentation of adrenal insufficiency may include non-specific symptoms and signs including nausea, vomiting, anorexia, fatigue, weakness, dizziness, and low blood pressure. If adrenal insufficiency is suspected, confirm the diagnosis with diagnostic testing as soon as possible. If adrenal insufficiency is diagnosed, treat with physiologic replacement doses of corticosteroids. Wean the patient off of the opioid to allow adrenal function to recover and continue corticosteroid treatment until adrenal function recovers. Other opioids may be tried as some cases reported use of a different opioid without recurrence of adrenal insufficiency. The information available does not identify any particular opioids as being more likely to be associated with adrenal insufficiency.
Risk Of Opioid Withdrawal With Abrupt Discontinuation
Buprenorphine is a partial agonist at the mu-opioid receptor and chronic administration produces physical dependence of the opioid type, characterized by withdrawal signs and symptoms upon abrupt discontinuation or rapid taper. The Subutex withdrawal syndrome is typically milder than seen with full agonists and may be delayed in onset [see Drug Abuse And Dependence]. When discontinuing SUBUTEX, gradually taper the dosage
Risk Of Hepatitis, Hepatic Events
Cases of cytolytic hepatitis and hepatitis with jaundice have been observed in individuals receiving buprenorphine in clinical trials and through post-marketing adverse event reports. The spectrum of abnormalities ranges from transient asymptomatic elevations in hepatic transaminases to case reports of death, hepatic failure, hepatic necrosis, hepatorenal syndrome, and hepatic encephalopathy. In many cases, the presence of pre-existing liver enzyme abnormalities, infection with hepatitis B or hepatitis C virus, concomitant usage of other potentially hepatotoxic drugs, and ongoing injecting drug use may have played a causative or contributory role. In other cases, insufficient data were available to determine the etiology of the abnormality. Withdrawal of buprenorphine has resulted in amelioration of acute hepatitis in some cases; however, in other cases no dose reduction was necessary. The possibility exists that buprenorphine had a causative or contributory role in the development of the hepatic abnormality in some cases. Liver function tests, prior to initiation of treatment is recommended to establish a baseline. Periodic monitoring of liver function during treatment is also recommended. A biological and etiological evaluation is recommended when a hepatic event is suspected. Depending on the case, SUBUTEX may need to be carefully discontinued to prevent withdrawal signs and symptoms and a return by the patient to illicit drug use, and strict monitoring of the patient should be initiated.
Cases of hypersensitivity to buprenorphine products have been reported both in clinical trials and in the post-marketing experience. Cases of bronchospasm, angioneurotic edema, and anaphylactic shock have been reported. The most common signs and symptoms include rashes, hives, and pruritus. A history of hypersensitivity to buprenorphine is a contraindication to the use of SUBUTEX.
Precipitation Of Opioid Withdrawal Signs And Symptoms
Because of the partial agonist properties of buprenorphine, SUBUTEX may precipitate opioid withdrawal signs and symptoms in individuals physically dependent on full opioid agonists if administered sublingually or parenterally before the agonist effects of other opioids have subsided.
Risk Of Overdose In Opioid NaÃ¯ve Patients
There have been reported deaths of opioid naÃ¯ve individuals who received a 2 mg dose of buprenorphine as a sublingual tablet for analgesia. SUBUTEX is not appropriate as an analgesic.
Buprenorphine / Naloxone
Buprenorphine/naloxone, sold under the brand name Suboxone among others, is a combination medication that includes buprenorphine and naloxone. In combination with counselling, it is used to treat opioid use disorder. It decreases withdrawal symptoms for about 24 hours. Wikipedia
ATC code: N07BC51 (WHO)
Naloxone: Opioid antagonist
Buprenorphine: Opioid modulator
Buprenorphine/naloxone is used for the treatment of opioid use disorder. Long term outcomes are generally better with use of buprenorphine/naloxone than attempts at stopping opioid use altogether. This includes a lower risk of overdose with medication use. Due to the high binding affinity and low activation at the opioid receptor, cravings and withdrawal for opioids are decreased while preventing a person from getting high and relapsing on another opioid. The combination of the two medications is preferred over buprenorphine alone for maintenance treatment due to the presence of naloxone in the formulation, which helps function as an abuse deterrent, especially against intravenous use.
Contraindications are severe respiratory or liver impairment and acute alcoholism. There are limited accounts of cross-reactivity with opioids, but there is a possibility. Serious central nervous system (CNS) and respiratory depression may also occur with concurrent use of CNS depressants, ingesting alcohol, or other CNS depressing factors while on buprenorphine/naloxone.(source)
SUBOXONE sublingual film is contraindicated in patients with a history of hypersensitivity to buprenorphine or naloxone as serious adverse reactions, including anaphylactic shock, have been reported
Suboxone – Drug Abuse and Dependence
SUBOXONE sublingual film contains buprenorphine, a Schedule III controlled substance under the Controlled Substances Act.
Under the Drug Addiction Treatment Act (DATA) codified at 21 U.S.C. 823(g), prescription use of this product in the treatment of opioid dependence is limited to healthcare providers who meet certain qualifying requirements, and who have notified the Secretary of Health and Human Services (HHS) of their intent to prescribe this product for the treatment of opioid dependence and have been assigned a unique identification number that must be included on every prescription.
Buprenorphine, like morphine and other opioids, has the potential for being abused and is subject to criminal diversion. This should be considered when prescribing or dispensing buprenorphine in situations when the clinician is concerned about an increased risk of misuse, abuse, or diversion. Healthcare professionals should contact their state professional licensing board or state controlled substances authority for information on how to prevent and detect abuse or diversion of this product.
Patients who continue to misuse, abuse, or divert buprenorphine products or other opioids should be provided with or referred for more intensive and structured treatment.
Abuse of buprenorphine poses a risk of overdose and death. This risk is increased with the abuse of buprenorphine and alcohol and other substances, especially benzodiazepines.
The healthcare provider may be able to more easily detect misuse or diversion by maintaining records of medication prescribed including date, dose, quantity, frequency of refills, and renewal requests of medication prescribed.
Proper assessment of the patient, proper prescribing practices, periodic re-evaluation of therapy, and proper handling and storage of the medication are appropriate measures that help to limit abuse of opioid drugs.
Buprenorphine is a partial agonist at the mu-opioid receptor and chronic administration produces physical dependence of the opioid type, characterized by moderate withdrawal signs and symptoms upon abrupt discontinuation or rapid taper. The Suboxone withdrawal syndrome is typically milder than seen with full agonists and may be delayed in onset [see Warnings and Precautions (5.7)].
The manifestations of acute overdose include pinpoint pupils, sedation, hypotension, 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 SUBOXONE sublingual film 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.
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What is buprenorphine hydrochloride?
Buprenorphine Hydrochloride is the hydrochloride salt form of buprenorphine, a synthetic phenanthrene with narcotic analgesic activity. Buprenorphine hydrochloride is a partial agonist at the mu-opioid receptor and an antagonist at the kapa-opioid receptor in the central nervous system.
What is buprenorphine used for?
Buprenorphine is used to treat dependence/addiction to opioids. Buprenorphine belongs to a class of drugs called mixed opioid agonist-antagonists. It helps prevent withdrawal symptoms caused by stopping other opioids.
What is buprenorphine and naloxone?
Buprenorphine/naloxone, sold under the brand name Suboxone among others, is a combination medication that includes buprenorphine and naloxone. In combination with counselling, it is used to treat opioid use disorder. It decreases withdrawal symptoms for about 24 hours.
What drugs contain buprenorphine?
Buprenorphine is available under the trade names Cizdol, Brixadi (weekly and monthly depot injections approved in the US by FDA for addiction treatment in 2020), Suboxone (with naloxone), Subutex (typically used for opioid use disorder), Zubsolv, Bunavail, Buvidal (weekly and monthly depot injections, approved in the UK, Europe and Australia for addiction treatment in 2018), Sublocade (monthly injection, approved in the US in 2018), Probuphine, Temgesic (sublingual tablets for moderate to severe pain), Buprenex (solutions for injection often used for acute pain in primary-care settings), Norspan and Butrans (transdermal preparations used for chronic pain
What is the difference between suboxone and subutex?
Both Subutex and Suboxone contain buprenorphine. While both drugs were developed at around the same time, Subutex was formulated first. While it was found to be relatively effective in the treatment of opiate addiction, there was still a tendency to abuse the drug. Many users sought to inject the drug intravenously in order to obtain the high they had become accustomed to with heroin or prescription painkillers. They often succeeded in doing so, giving rise to the need to develop another drug to address this issue: Suboxone.