Buprenorphine Hydrochloride / Naloxone Hydrochloride

Pronunciation: (BYOO-preh-NAHR-feen HIGH-droe-KLOR-ide/NAL-ox-ohn HIGH-droe-KLOR-ide)Class: Narcotic agonist-antagonist analgesic

Trade Names:Suboxone- Tablets, sublingual 2 mg buprenorphine base per 0.5 mg naloxone- Tablets, sublingual 8 mg buprenorphine base per 2 mg naloxone

Pharmacology

Buprenorphine

Analgesic effect caused by binding to opiate receptors in the CNS, while antagonist effects decrease abuse potential.

Naloxone

Possibly antagonizes opioid effects by competing for the same receptor sites.

Indications and Usage

Treatment of opioid dependence.

Contraindications

Standard consideration.

Dosage and Administration

Adults and Children (16 yr of age and older)

SL Single daily dose in the range of 12 to 16 mg of buprenorphine. The dose should be adjusted in increments or decrements of 2 or 4 mg to a level that holds the patient in treatment and suppresses opioid withdrawal effects. This is likely to range between 4 and 24 mg/day.

General Advice

• For sublingual administration only. Do not chew, crush, or swallow tablets. Place tablets under the tongue until they are dissolved. Swallowing tablets reduces effectiveness.
• Buprenorphine and buprenorphine/naloxone tablets are interchangeable.
• Do not initiate therapy until objective signs of opioid withdrawal are evident.
• For dose requiring more than 2 tablets, place all tablets under the tongue and allow to dissolve. If patient cannot fit more than 2 tablets under the tongue at one time, then place 2 tablets under the tongue at a time.

Storage/Stability

Store tablets at controlled room temperature (59° to 86°F).

Drug Interactions

Barbiturate anesthetics

May have additive effects with buprenorphine, increasing the respiratory and CNS effects.

Benzodiazepines (eg, diazepam)

Coma and death have been associated with misuse of buprenorphine and benzodiazepines.

CNS depressants (eg, alcohol, phenothiazines, sedative-hypnotics)

Increased CNS depression may occur.

CYP3A4 inducers (eg, carbamazepine, phenytoin, rifampin)

May reduce buprenorphine plasma levels, decreasing the efficacy.

CYP3A4 inhibitors (eg, erythromycin, ketoconazole, ritonavir)

May elevate buprenorphine plasma levels, increasing the risk of side effects.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Vasodilation.

CNS

Headache; insomnia; anxiety; depression; dizziness; nervousness; somnolence.

Dermatologic

Sweating.

EENT

Rhinitis; pharyngitis; runny eyes.

GI

Abdominal pain; constipation; diarrhea; nausea; vomiting; dyspepsia.

Respiratory

Increased cough.

Miscellaneous

Pain; back pain; withdrawal symptoms; abscess; asthenia; chills; fever; flu syndrome; infection; accidental injury.

Precautions

Monitor Document type of opioid dependence (eg, long-, short-acting), time since last opioid use, and degree of opioid dependence prior to starting therapy. Ensure that liver enzymes and hepatic function are evaluated prior to starting therapy and periodically during treatment. Monitor patient for respiratory depression. If noted, re-establish adequate ventilation with mechanical assistance and notify health care provider immediately. Naloxone may not be effective in reversing respiratory depression caused by this drug. Monitor patient for narcotic withdrawal symptoms, CNS, GI, and general body side effects. Report to health care provider if noted and significant.

Pregnancy

Category C .

Lactation

Buprenorphine is excreted in breast milk.

Children

Safety and efficacy not established in children below the age of 16 yr of age.

Special Risk Patients

Use with caution in elderly or debilitated patients; use with caution in patients with impaired hepatic, renal, or pulmonary function (eg, chronic obstructive pulmonary disease), myxedema or hypothyroidism, adrenal cortical insufficiency (eg, Addison disease), CNS depression or coma, toxic psychoses, prostatic hypertrophy or urethral stricture, acute alcoholism, delirium tremens or kyphoscoliosis, or biliary tract dysfunction.

Dependency

Buprenorphine has abuse potential. Psychological and physical dependence as well as tolerance may occur.

Head injury or increased IOP

Use with caution; drug can increase CSF pressure.

Withdrawal

Marked and intense withdrawal symptoms are likely to occur if misused parenterally by individuals dependent on opioid agonists; sublingual use may cause opioid withdrawal symptoms if administered before the agonist effects of the opioid have subsided.

Overdosage

Symptoms

Pinpoint pupils, sedation, hypotension, respiratory depression, death.

Patient Information

• Advise patient to take prescribed dose once daily by placing tablet under the tongue until dissolved. For dose requiring more than 2 tablets, advise patient to place all tablets under the tongue and allow to dissolve. If patient cannot fit more than 2 tablets under the tongue at 1 time, then advise patient to place 2 tablets under the tongue at a time and repeat until entire dose has been taken.
• Caution patient that swallowing tablets reduces effectiveness.
• Advise patient to not change the dose or stop taking unless advised by the health care provider.
• Caution patient to avoid alcoholic beverages and other CNS depressants (eg, narcotics, benzodiazepines) while taking this drug. Combined use may result in a serious toxicity and possibly death.
• Advise patient to inform family members that, in the event of an emergency, the treating emergency personnel should be informed that the patient is physically dependent on narcotics and is being treated with buprenorphine.
• Advise patient that drug may impair mental or physical abilities required for the performance of potentially hazardous tasks and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
• Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
• Instruct patient to lie or sit down if experiencing dizziness or lightheadedness when standing.
• Advise patient to contact their health care provider if experiencing the following side effects: headache, insomnia, nausea, vomiting, abdominal pain.

Copyright © 2009 Wolters Kluwer Health.