Buprenorphine Buccal

Buprenorphine buccal is a prescription medication used for the management of severe chronic pain.

• Buprenorphine buccal is available under the following different brand names: Belbuca

Adult dosage

Buccal film: Schedule III

• 75mcg
• 150mcg
• 300mcg
• 450mcg
• 600mcg
• 750mcg
• 900mcg

Chronic Severe Pain

Adult dosage

Opioid-naïve

• Initiate with 75 mcg film once daily or, if tolerated, every 12 hours for at least 4 days, then increase the dose to 150 mcg every 12 hours
• Conversion from other opioids
• Following analgesic taper, base the starting dose on the patient’s daily opioid dose before taper, as described
  • Oral morphine equivalent  to less than 30 mg/day: Initiate with 75 mcg once daily or once every 12 hours
  • Oral morphine equivalent 30-89 mg/day: Initiate with 150 mcg once every 12 hours
  • Oral morphine equivalent 90-160 mg/day: Initiate with 300 mcg every 12 hours
  • Oral morphine equivalent more than 160 mg/day: Consider alternate analgesic
  • Buprenorphine buccal doses of 600 mcg, 750 mcg, and 900 mcg are only for use following titration from lower doses of buprenorphine buccal
  • Individual titration should proceed in increments of 150 mcg every 12 hours, no more frequently than every 4 days

Titration and maintenance dose

• Individual titration should proceed in increments that do not exceed 150 mcg every 12 hours
• Maximum dose: 900 mcg every 12 hours; do not exceed this dose because of potential for QTc interval prolongation

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

Common side effects of Buprenorphine buccal include:

• nausea,
• constipation,
• headache,
• vomiting,
• dizziness,
• drowsiness,
• fatigue,
• diarrhea,
• dry mouth,
• upper respiratory tract infection,
• anemia,
• abdominal pain,
• swelling of the extremities,
• fever,
• urinary tract infection,
• runny or stuffy nose,
• sinus infection,
• bronchitis,
• loss of appetite,
• muscle spasm,
• back pain,
• anxiety,
• insomnia,
• depression,
• sore throat,
• increased sweating,
• itching,
• rash,
• hot flashes, and
• high blood pressure.

Serious side effects of Buprenorphine buccal include:

• swelling of the face, arms, hands, ankles or feet,
• blood in the urine,
• blurred vision,
• cough,
• diarrhea,
• abdominal pain,
• difficulty breathing,
• dizziness,
• fever,
• frequent urination,
• headache,
• loss of appetite,
• back pain,
• mouth pain,
• nausea,
• nervousness,
• pale skin,
• pounding in the ears,
• rapid weight gain,
• slow or fast heartbeats,
• stomach pain,
• chest pain or pressure,
• tingling in the hands or feet,
• tiredness or weakness,
• unusual bruising or bleeding,
• irregular heartbeat,
• chills,
• drowsiness,
• agitation,
• confusion,
• darkening of the skin,
• lightheadedness,
• hives,
• rash,
• depression,
• shallow breathing,
• breathing that stops in your sleep,
• pale skin,
• loss of coordination,
• swelling around the eyes, lips, or tongue,
• restlessness,
• extreme excitement,
• tremors,
• muscle spasms, and
• vomiting.

Rare side effects of Buprenorphine buccal include:

• none 

This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Buprenorphine buccal has severe interactions with the following drug:
  • alvimopan
• Buprenorphine buccal has serious interactions with at least 53 other drugs.
• Buprenorphine buccal has moderate interactions with at least 218 other drugs.
• Buprenorphine buccal has minor interactions with the following drugs:
  • brimonidine
  • dextroamphetamine
  • elvitegravir
  • eucalyptus
  • lidocaine
  • sage
  • ziconotide

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns.

Contraindications

• Significant respiratory depression
• Acute or severe bronchial asthma in an unmonitored setting or the absence of resuscitative equipment
• Known or suspected gastrointestinal obstruction, including paralytic ileus
• Hypersensitivity (e.g., anaphylaxis) to buprenorphine

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Buprenorphine buccal?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Buprenorphine buccal?”

Cautions

• Misuse, abuse, diversion: Partial agonist at the mu-opioid receptor and a schedule III controlled opioid exposes users to the risks of addiction, abuse, and misuse; there is a greater risk for overdose and death with extended-release opioids owing to the larger amount of active opioid present; screen patients for risk of substance use disorders, including opioid abuse and misuse, and warn them of risk for overdose and death associated with the use of additional CNS depressants including alcohol and illicit drugs (see Black Box Warnings)
• Life-threatening respiratory depression is more likely to occur in elderly, cachectic, or debilitated patients as they may have altered pharmacokinetics or altered clearance compared to younger, healthier patients (even to moderate therapeutic doses) (see Black Box Warnings); because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and may be useful to monitor renal function
• Neonatal opioid withdrawal syndrome reported with long-term use during pregnancy (see Black Box Warnings)
• Accidental exposure was reported, including fatalities (see Black Box Warnings)
• Interactions with CNS depressants (eg, alcohol, sedatives, anxiolytics, hypnotics, neuroleptics, other opioids) can cause additive effects and increase the risk for respiratory depression, profound sedation, and hypotension
• Risk of apnea in patients with chronic pulmonary disease; closely monitor these patients, when initiating and titrating therapy; alternatively, consider the use of alternative non-opioid analgesics in these patients (see Black Box Warnings and Contraindications)
• QTc prolongation observed in healthy individuals at 40 mcg/hr; avoid in patients with a history of long QT syndrome or coadministration with class IA (eg, quinidine, procainamide, disopyramide) or class III (eg, sotalol, amiodarone, dofetilide) antiarrhythmics
• Head injury: Respiratory depressant effects of opioids may include carbon dioxide retention and lead to elevated CSF pressure
• Hypotensive effects: Can cause severe hypotension; caution with depleted blood volume or coadministration of drugs that affect vasomotor tone (eg, phenothiazines), vasodilators, or antihypertensives
• Hepatoxicity: Cases of cytolytic hepatitis and hepatitis with jaundice observed in individuals receiving buprenorphine SL for opioid dependence treatment; increased risk for overdose with moderate or severe hepatic impairment (see Dosage Modifications)
• Anaphylactic reactions reported
• May cause sphincter of Oddi spasm and aggravate abdominal conditions, including ileus (see Contraindications)
• Similar to other opioids, may aggravate seizure disorders by lowering the seizure threshold
• Patients with cancer who have oral mucositis may absorb buprenorphine more rapidly than intended and have higher plasma levels of buprenorphine (see Dosage Modifications)
• Special risk groups may experience increased adverse reactions; caution with alcoholism, delirium tremens, adrenocortical insufficiency, CNS depression, debilitation, kyphoscoliosis associated with respiratory compromise, myxedema or hypothyroidism, prostatic hypertrophy or urethral stricture, severe impairment of hepatic, pulmonary or renal function, and toxic psychosis
• Profound sedation, respiratory depression, coma, and death may result from concomitant use with other CNS depressants (see BBW); prescribe lowest effective dosages and minimum durations of concomitant use
• If an opioid analgesic is initiated in a patient already taking a benzodiazepine or other CNS depressant, prescribe a lower initial dose of the opioid analgesic, and titrate based on clinical response; follow patients closely for signs and symptoms of respiratory depression and sedation; if concomitant use with a benzodiazepine is warranted, consider prescribing naloxone for the emergency treatment of opioid overdose
• Due to the risk of respiratory depression with concomitant use of skeletal muscle relaxants and opioids, consider prescribing naloxone for the emergency treatment of opioid overdose
• Cases of adrenal insufficiency reported with opioid use, more often following greater than one month of use; symptoms may include nausea, vomiting, anorexia, fatigue, weakness, dizziness, and low blood pressure; 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
• Chronic use of opioids may cause reduced fertility in females and males of reproductive potential; unknown whether effects on fertility are reversible
• Increased risk of dental problems
  • On January 12, 2022, FDA warned of potential dental problems associated with transmucosal buprenorphine-containing products (eg, buccal, sublingual)
  • Dental problems (ie, tooth decay, cavities, oral infections, loss of teeth), can be serious and have been reported even in patients with no history of dental issues
  • Despite these risks, buprenorphine is an important treatment option for opioid use disorder and pain, and the benefits of these medicines outweigh the risks
  • Review patient’s health before initiating transmucosal buprenorphine
  • Counsel patients regarding the potential for dental problems and the importance of taking extra steps after the medicine have completely dissolved, including gently rinsing teeth and gums with water and then swallowing; advice to wait at least 1 hour before brushing their teeth
  • Dentists treating patients taking transmucosal buprenorphine should perform a baseline dental evaluation and caries risk assessment, establish a dental caries preventive plan, and encourage regular dental checkups
• Opioid analgesic risk evaluation and mitigation strategy (REMS)
  • To ensure that the benefits of opioid analgesics outweigh the risks of addiction, abuse, and misuse, the Food and Drug Administration (FDA) has required a Risk Evaluation and Mitigation Strategy (REMS) for these products
  • Discuss the safe use, serious risks, and proper storage and disposal of opioid analgesics with patients and/or their caregivers every time these medicines are prescribed; use the following link to obtain the Patient Counseling Guide (PCG): www.fda.gov/OpioidAnalgesicREMSPCG
  • Emphasize to patients and their caregivers the importance of reading the Medication Guide that they will receive from their pharmacist every time an opioid analgesic is dispensed to them
  • Consider using other tools to improve patient, household, and community safety, such as patient-prescriber agreements that reinforce patient-prescriber responsibilities
  • To obtain further information on opioid analgesic REMS and for a list of accredited REMS CME/CE, call 1-800-503-0784, or log on to www.opioidanalgesicrems.com; the FDA Blueprint can be found at www.fda.gov/OpioidAnalgesicREMSBlueprint
• Patient access to naloxone for emergency treatment of opioid overdose
  • Assess potential need for naloxone; consider prescribing for emergency treatment of opioid overdose
  • Consult on availability and ways to obtain naloxone as permitted by individual state naloxone dispensing and prescribing requirements or guidelines
  • Educate patients regarding the signs and symptoms of respiratory depression and to call 911 or seek immediate emergency medical help in the event of a known or suspected overdose

Pregnancy and Lactation

• Opioids cross the placenta and may produce respiratory depression and psychophysiological effects in neonates; not recommended for use in women immediately before and during labor, when the use of shorter-acting analgesics or other analgesic techniques are more appropriate
• Neonates whose mothers have been taking opioids long term may also exhibit withdrawal signs, either at birth and/or in the nursery because they have developed physical dependence; neonatal opioid withdrawal syndrome, unlike opioid withdrawal syndrome in adults, may be life-threatening and should be treated according to protocols developed by neonatology experts
• Lactation
  • Caution should be exercised when therapy is administered to nursing women; the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on the breastfed child from the drug or underlying maternal condition.