BUPRENEX Dosage & Rx Info | Uses, Side Effects

Buprenex Generic Name & Formulations

Legal Class

CIII

General Description

Buprenorphine (as HCl) 0.3mg/mL; for IM or IV inj.

Pharmacological Class

Opioid (partial agonist-antagonist).

How Supplied

Amps (1mL)—5

Manufacturer

Indivior Inc.

Generic Availability

YES

Mechanism of Action

Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor. The principal action of therapeutic value of buprenorphine is analgesia and is thought to be due to buprenorphine binding with high affinity to opioid receptors on neurons in the brain and spinal cord.

Buprenex Indications

Indications

Management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate.

Limitations of Use

Reserve for use in patients for whom alternative treatment options are not tolerated or inadequate to provide analgesia.

Buprenex Dosage and Administration

Adult

Use lowest effective dose for shortest duration. Individualize. >12yrs: initially 0.3mg (1mL) by deep IM or slow IV (over ≥2mins) inj at up to 6hr intervals, as needed. May repeat once (up to 0.3mg), 30–60mins after initial dose. Max single dose: 0.6mg (IM only). Concomitant use or discontinuation of CYP3A4 inhibitors or inducers: monitor closely and consider dose adjustments (see full labeling).

Children

<2yrs: not recommended. 2–12yrs: 2–6micrograms/kg every 4–6hrs, depending on clinical response. Concomitant use or discontinuation of CYP3A4 inhibitors or inducers: monitor closely and consider dose adjustments (see full labeling).

Buprenex Contraindications

Contraindications

Significant respiratory depression. Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment. Known or suspected GI obstruction, including paralytic ileus.

Buprenex Boxed Warnings

Boxed Warning

Serious and life-threatening risks from use of Buprenex: Addiction, abuse, and misuse; Life-threatening respiratory depression; Risks from concomitant use with benzodiazepines or other CNS depressants; Neonatal opioid withdrawal syndrome.

Buprenex Warnings/Precautions

Warnings/Precautions

Abuse potential (monitor). Life-threatening respiratory depression; monitor within first 24–72hrs of initiating therapy and following dose increases. Sleep-related breathing disorders (including central sleep apnea (CSA), sleep-related hypoxemia); consider dose reduction if CSA develops. COPD, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression; monitor and consider non-opioid analgesics. Risk of QT prolongation (esp. in those with hypokalemia, bradycardia, recent conversion from atrial fibrillation, CHF, digitalis therapy, baseline QT prolongation, subclinical long-QT syndrome, severe hypomagnesemia). Adrenal insufficiency. Opioid-induced hyperalgesia (OIH) and allodynia; consider dose reduction of current opioid or opioid rotation if OIH is suspected. Monitor for signs of hypotension when initiating or titrating dose. Head injury. Increased intracranial pressure, brain tumors; monitor. Seizure disorders. CNS depression. Impaired consciousness, coma, shock; avoid. Biliary tract disease. Acute pancreatitis. Myxedema or hypothyroidism. Toxic psychoses. Prostatic hypertrophy. Urethral stricture. Delirium tremens. Kyphoscoliosis. Drug or alcohol abusers. Severe pulmonary, hepatic, or renal impairment. Reevaluate periodically. Avoid abrupt cessation. Children. Elderly. Cachectic. Debilitated. Labor & delivery. Pregnancy; potential neonatal opioid withdrawal syndrome during prolonged use. Nursing mothers: not recommended.

Buprenex Pharmacokinetics

Metabolism

N-dealkylation (CYP3A4 primarily) and glucuronidation.

Buprenex Interactions

Interactions

Increased risk of hypotension, respiratory depression, sedation with benzodiazepines or other CNS depressants (eg, non-benzodiazepine sedatives/hypnotics, anxiolytics, general anesthetics, phenothiazines, tranquilizers, muscle relaxants, antipsychotics, alcohol, other opioids); reserve concomitant use in those for whom alternative options are inadequate; limit dosages/durations to minimum required; monitor. Avoid concomitant Class 1A (eg, quinidine, procainamide, disopyramide) or Class III antiarrhythmics (eg, sotalol, amiodarone, dofetilide). During or within 14 days of MAOIs: not recommended. Risk of serotonin syndrome with serotonergic drugs (eg, SSRIs, SNRIs, TCAs, triptans, 5-HT3 antagonists, mirtazapine, trazodone, tramadol, cyclobenzaprine, metaxalone, MAOIs, linezolid, IV methylene blue); monitor and discontinue if suspected. Avoid concomitant mixed agonist/antagonist and partial agonist opioids (eg, butorphanol, nalbuphine, pentazocine); may reduce effects and/or precipitate withdrawal symptoms. Potentiated by CYP3A4 inhibitors (eg, macrolides, azole antifungals, protease inhibitors). Antagonized by CYP3A4 inducers (eg, rifampin, carbamazepine, phenytoin). May antagonize diuretics; monitor. Paralytic ileus may occur with anticholinergics. Chronic Buprenex treatment with concomitant NNRTIs (eg, efavirenz, nevirapine, etravirine, delavirdine); monitor. Concomitant atazanavir ± ritonavir: may need to reduce Buprenex dose.

Buprenex Adverse Reactions

Adverse Reactions

Sedation, dizziness/vertigo, nausea, vomiting, hypotension, miosis, headache, sweating, hypoventilation; respiratory depression, orthostatic hypotension, syncope, hypersensitivity reactions, OIH and allodynia.

Buprenex Clinical Trials

See Literature

Buprenex Note

Not Applicable

Buprenex Patient Counseling