Buprenorphine Hydrochloride

Trade Names:
Buprenex
- Injection 0.324 mg (equiv. to 0.3 mg buprenorphine)/mL

Trade Names:
Subutex
- Tablets, sublingual 2 mg (as base)
- Tablets, sublingual 8 mg (as base)

Mechanism of Action

Pharmacology

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

Pharmacokinetics

Absorption

C _max is approximately 5.47 ng/mL (16 mg SL dose). AUC is approximately 32.63 h•ng/mL (16 mg SL dose).

Distribution

Approximately 96% protein bound.

Metabolism

Undergoes CYP3A4-mediated N-dealkylation to norbuprenorphine (active) and glucuronidation.

Elimination

30% is excreted in the urine and 69% in the feces. The t _½ is 37 h.

Onset

15 min (IM).

Peak

1 h (IM).

Duration

At least 6 h (IM).

Indications and Usage

Treatment of opioid dependence.

Relief of moderate to severe pain.

Contraindications

Standard considerations.

Dosage and Administration

SL (Use limited to health care providers who meet certain qualifications and have notified the Health and Human Services of their intent to prescribe.) 12 to 16 mg/day.

IM/IV 0.3 mg deep IM or slow IV (over at least 2 min) at up to 6 h intervals, as needed. May repeat once (up to 0.3 mg) 30 to 60 min after initial dosage, if required.

General Advice

• Tablets
• For SL use 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.

• Injection
• For deep IM or slow IV (over at least 2 min) administration only. Not for intradermal, SC, or intra-arterial administration.

Storage/Stability

Store tablets at controlled room temperature (59° to 86°F). Store injection at controlled room temperature (59° to 86°F). Avoid freezing or exposure to excessive heat (over 104°F). Protect from prolonged exposure to light.

Drug Interactions

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

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

Increased CNS depression may occur.

May reduce buprenorphine plasma levels, decreasing the efficacy.

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

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension; hypertension; tachycardia; bradycardia.

CNS

Sedation; dizziness/vertigo; headache; confusion; dreaming; psychosis; euphoria; weakness/fatigue; malaise; hallucinations; depersonalization; coma; tremor; dysphoria; agitation; convulsions; lack of muscle coordination; insomnia.

Dermatologic

Sweating; pruritus; injections site reaction; rash; pallor; urticaria.

EENT

Miosis.

GI

Nausea; vomiting; constipation; dry mouth; dyspepsia; flatulence; loss of appetite; diarrhea; abdominal pain.

Hepatic

Hepatitis and hepatitis with jaundice.

Respiratory

Hypoventilation.

Miscellaneous

Chronic and acute hypersensitivity; infection.

Precautions

Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established in children under 13 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, 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, biliary tract dysfunction.

Abdominal conditions

May obscure diagnosis or clinical course of patients with acute abdominal conditions.

Dependency

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

Head injury or increased intracranial pressure

Use with caution; drug can increase CSF pressure.

Narcotic dependent patients

Use in physically dependent individuals may result in withdrawal effects.

Overdosage

Symptoms

Respiratory depression, pinpoint pupils, sedation, hypotension, death.

Patient Information

• Injection
• Advise patient, family, or caregiver that medication is used to control pain and will be prepared and administered by a health care provider in a medical setting.

• SL tablets
• 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 one 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 overdose 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 they experience dizziness or lightheadedness when standing.
• Advise patient to contact health care provider if experiencing the following side effects: headache, insomnia, nausea, vomiting, or abdominal pain.

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