No

Analgesic, Narcotic

Management of moderate to severe pain

C-V

C

Hypersensitivity to buprenorphine or any component

May cause respiratory depression - use caution in patients with respiratory disease or pre-existing respiratory depression. Potential for drug dependency exists, abrupt cessation may precipitate withdrawal. Use caution in elderly, debilitated, or pediatric patients. Use with caution in patients with depression or suicidal tendencies, or in patients with a history of drug abuse. Tolerance, psychological and physical dependence may occur with prolonged use. Use with caution in patients with hepatic, pulmonary, or renal function impairment. May cause CNS depression, which may impair physical or mental abilities. Patients must be cautioned about performing tasks which require mental alertness (ie, operating machinery or driving). Effects with other sedative drugs or ethanol may be potentiated. Elderly may be more sensitive to CNS depressant and constipating effects. Use with caution in patients with head injury or increased ICP, biliary tract dysfunction, pancreatitis, patients with history of ileus or bowel obstruction, glaucoma, hyperthyroidism, adrenal insufficiency, prostatic hypertrophy, urinary stricture, CNS depression, toxic psychosis, alcoholism, delirium tremens, or kyphoscoliosis. Partial antagonist activity may precipitate acute narcotic withdrawal in opioid-dependent individuals.

>10%: Central nervous system: Sedation

1% to 10%:

Cardiovascular: Hypotension

Central nervous system: Respiratory depression, dizziness, headache

Gastrointestinal: Vomiting, nausea

Ocular: Miosis

Miscellaneous: Diaphoresis

<1%: Hypertension, tachycardia, bradycardia, euphoria, slurred speech, confusion, xerostomia, nervousness, depression, constipation, pruritus, urinary retention, paresthesia, blurred vision, diplopia, dyspnea, cyanosis

Symptoms of overdose include CNS depression, pinpoint pupils, hypotension, bradycardia

Treatment of an overdose includes support of the patient's airway, establishment of an I.V. line, and administration of naloxone 2 mg I.V. (0.01 mg/kg for children) with repeat administration as necessary up to a total of 10 mg

Barbiturate anesthetics may produce additive respiratory and CNS depression

Respiratory and CV collapse was reported in a patient who received diazepam and buprenorphine

Protect from excessive heat (>40°C/104°F) and light

Incompatible with diazepam, lorazepam

Buprenorphine exerts its analgesic effect via high affinity binding to m opiate receptors in the CNS; displays both agonist and antagonist activity

Onset of analgesia: Within 10-30 minutes

Duration: 6-8 hours

Absorption: I.M., S.C.: 30% to 40%

Distribution: V_d: 97-187 L/kg

Protein binding: High

Metabolism: Mainly in the liver; undergoes extensive first-pass metabolism

Half-life: 2.2-3 hours

Elimination: 70% excreted in feces via bile and 20% in urine as unchanged drug

I.M., slow I.V.:

Elderly: 0.15 mg every 6 hours; elderly patients are more likely to suffer from confusion and drowsiness compared to younger patients

Long-term use is not recommended

Pain relief, respiratory and mental status, CNS depression, blood pressure

Drowsiness is common; rare reports of euphoria

Concurrent use with benzodiazepines or barbiturates may result in CNS or respiratory depression

No information available to require special precautions

No effects or complications reported

If self-administered, use exactly as directed (do not increase dose or frequency). While using this medication, do not use alcohol and other prescription or OTC medications (especially sedatives, tranquilizers, antihistamines, or pain medications) without consulting prescriber. May cause dizziness, drowsiness, confusion, or blurred vision (use caution when driving, climbing stairs, or changing position - rising from sitting or lying to standing, or when engaging in tasks requiring alertness until response to drug is known). You may experience nausea or vomiting (frequent mouth care, small frequent meals, sucking lozenges, or chewing gum may help). Report unresolved nausea or vomiting; difficulty breathing or shortness of breath; excessive sedation or unusual weakness; rapid heartbeat or palpitations. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.

Gradual withdrawal of drug is necessary to avoid withdrawal symptoms

Injection, as hydrochloride: 0.3 mg/mL (1 mL)

"Drugs for Pain," Med Lett Drugs Ther, 1998, 40(1033):79-84.

Gal TJ, "Naloxone Reversal of Buprenorphine-Induced Respiratory Depression," Clin Pharmacol Ther, 1989, 45(1):66-71.

Harcus AH, Ward AE, and Smith DW, "Buprenorphine: Experience in an Elderly Population of 975 Patients During a Year's Monitored Release," Br J Clin Pract, 1980, 34(5):144-6.

Jain PN and Shah SC, "Respiratory Depression Following Combination of Epidural Buprenorphine and Intramuscular Ketorolac," Anaesthesia, 1993, 48(10):898-9.

Mac Evilly M and O'Carroll C, "Hallucinations After Epidural Buprenorphine," Br Med J, 1989, 298(6678):928-9.

O'Connor PG, Oliveto AH, Shi JM, et al, "A Randomized Trial of Buprenorphine Maintenance for Heroin Dependence in a Primary Care Clinic for Substance Users Versus a Methadone Clinic," Am J Med, 1998, 105(2):100-5.