Buprenorphine

DEA Class; Rx

Common Brand Names; Buprenex

Semisynthetic mixed opiate agonist-antagonist; partial mu-receptor agonist with a ceiling to its pharmacological effects
Immediate-release parenteral form used for moderate to severe pain; transdermal and buccal forms used for continuous therapy for chronic severe pain
Sublingual tablets, dermal implant, and extended-release subcutaneous injection are used for opioid dependence in conjunction with the Drug Addiction Treatment Act (DATA)

Indicated for the treatment of severe pain requiring an opioid analgesic and for which alternative treatments are inadequate.

Hypersensitivity

Significant respiratory depression

Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment

Known or suspected gastrointestinal obstruction, including paralytic ileus

• Headache (29.1-30%)
• Pain (18.4-24%)
• Withdrawal syndrome (18.4-22%)
• Insomnia (21.4%)
• Infection (20%)
• Asthenia (14%)
• Back pain (7.8-14%)
• Nausea (10-13.6%)
• Sweating (12-12.6%)
• Abdominal pain (11.7%)
• Infection (11.7%)
• Constipation (7.8-11%)
• Nausea
• Dizziness/vertigo
• Sweating
• Headache
• Hypotension
• Nausea/vomiting
• Hypoventilation
• Miosis
• Rhinitis (9.7%)
• Chills (6-7.8%)
• Vomiting (5-7.8%)
• Flu syndrome (6%)
• Nervousness (6%)
• Runny eyes (5%)
• Diarrhea (4.9-5%)
• Asthenia (4.9%)
• Vasodilation (3.9%)
• Fever (3%)
• Dyspepsia (3%)
• Accidental injury (2-3%)
• Abscess (2%)

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 (see Black Box Warnings)

Serious, life-threatening, or fatal respiratory depression reported; may occur more frequently in elderly or debilitated patients, or in conditions associated with hypoxia or hypercapnia (even moderate therapeutic doses) (see Black Box Warnings)

Neonatal opioid withdrawal syndrome reported with long-term use during pregnancy (see Black Box Warnings)

Do not abruptly discontinue buprenorphine in a patient physically dependent on opioids; when discontinuing therapy, in a physically dependent patient, gradually taper the dosage; rapid tapering in a patient physically dependent on opioids may lead to a withdrawal syndrome and return of pain

Accidental exposure reported, including fatalities (see Black Box Warnings)

May impair mental or physical abilities needed to perform potentially hazardous activities (eg, driving a car, operating machinery)

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 history of long QT syndrome or coadministration with class IA (eg, quinidine, procainamide, disopyramide) or class III (eg, sotalol, amiodarone, dofetilide) antiarrhythmics

Respiratory depressant effects of opioids may include carbon dioxide retention and lead to elevated CSF pressure

Data in pregnancy are limited; however, these data do not indicate an increased risk of major malformations specifically due to buprenorphine exposure

Data on two studies in 13 lactating women receiving therapy where the drug and it metabolite were present in low levels in human milk did not show adverse reactions in breastfed infants