Buprenorphine Hydrochloride	(BYOO-preh-NAHR-feen HIGH-droe-KLOR-ide)
Trade Name(s):	Buprenex   ·Injection 0.324 mg (equiv. to 0.3 mg buprenorphine)/mL   Subutex   ·Tablets, sublingual 2 mg (as base)   ·Tablets, sublingual 8 mg (as base) Indicates Canadian Trade Name.
Class:	Opioid agonist-antagonist analgesic
Action:	Analgesic effect caused by binding to opiate receptors in the CNS. Antagonist effects decrease abuse potential. 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.
	Excretion: 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:
	Tablet Treatment of opioid dependence.
	Injection Relief of moderate to severe pain.
Contraindications:	Standard considerations.
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.
Lab Test Interferences:	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:
	Monitoring: Ensure that liver enzymes and hepatic function are evaluated prior to starting therapy and periodically during treatment. Document type of opioid dependence (eg, long-, short-acting), time since last opioid use, and degree of opioid dependence prior to starting SL tablets. 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: 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:	Signs & symptoms Respiratory depression, pinpoint pupils, sedation, hypotension, death.
Patient/Family Education:	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. 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.