Buprenorphine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : Sublingual Moderate to severe pain 200-400 mcg 6-8 hrly as needed. Anaesth premed 400 mcg. Opioid dependence Initial: 0.8-4 mg once daily, increase as necessary. Maintenance: ≤32 mg/day. Once patient is stabilised, gradually reduce dose and may stop treatment if appropriate. Opioid-dependent addicts who have not undergone withdrawal: 1st dose should not be given until 1st signs of craving appear or until at least 6 hr after last opioid use. Patients receiving methadone: Reduce methadone dose to max 30 mg/day before starting therapy. IM Anaesth premed 300 mcg. IV Perioperative analgesia 300-450 mcg. IM/IV Moderate to severe pain 300-600 mcg 6-8 hrly. Transdermal Moderate to severe pain BuTrans (Napp, UK) Non-malignant pain: Initial: 5 mcg/hr. Replace patch every 7 days and apply new patch to a different site. Avoid using the same area of the skin for the next 3-4 wk. Transtec (Napp, UK) Cancer pain: Initial: Opioid-naive patient: 35 mcg/hr; patient receiving a strong opioid analgesic: Base dose on previous 24-hr opioid requirement. Replace patch every 96 hr at the latest and apply new patch to a different site. Avoid using the same area of the skin for at least the next 2 applications.
Dosage Details
Intramuscular
Premedication before anaesthesia
Adult: 300 mcg.

Intravenous
Perioperative analgesic supplement
Adult: 300-450 mcg.

Parenteral
Moderate to severe pain
Adult: 300-600 mcg by IM or slow IV inj repeated 6-8 hrly if needed.
Child: 6 mth to 12 yr 3-6 mcg/kg 6-8 hrly. Refractory cases: Up to 9 mcg/kg.

Sublingual
Moderate to severe pain
Adult: 200-400 mcg repeated 6-8 hrly as needed.
Child: 6-12 yr 16-25 kg: 100 mcg; >25-37.5 kg: 100-200 mcg; >37.5-50 kg: 200-300 mcg. Doses to be given 6-8 hrly.

Sublingual
Premedication before anaesthesia
Adult: 400 mcg.

Sublingual
Opioid dependence
Adult: Initially, 0.8-4 mg once daily, may increase as necessary. Maintenance: ≤32 mg daily. Once patient is stabilised, gradually reduce dose and may stop treatment if appropriate. Opioid-dependent addicts who have not undergone withdrawal: 1st dose should not be given until 1st signs of craving appear or until at least 6 hr after last opioid use. Patients receiving methadone: Reduce methadone dose to max 30 mg daily before starting therapy.
Child: ≥16 yr Same as adult dose.

Transdermal
Moderate to severe pain
Adult: BuTrans (Napp, UK) Non-malignant pain: Initial: 5 mcg/hr. Replace patch every 7 days and apply new patch to a different site. Avoid using the same area of the skin for the next 3-4 wk. Transtec (Napp, UK) Cancer pain: Initial: Opioid-naive patient: 35 mcg/hr; patient receiving a strong opioid analgesic: Base dose on previous 24-hr opioid requirement. Replace patch every 96 hr at the latest and apply new patch to a different site. Avoid using the same area of the skin for at least the next 2 applications.
Hepatic Impairment
Sublingual:
Severe: Dose adjustment needed.
Incompatibility
Incompatible w/ amphotericin B cholesteryl sulfate complex, doxorubicin liposome.
Contraindications
Transdermal: Patient w/ known or suspected paralytic ileus, substantial resp depression or severe bronchial asthma. Management of acute, intermittent, mild, or short-term (including post-op) pain. Concomitant admin of IV buprenorphine and oral diazepam. Concurrent use or w/in 14 days of discontinuation of MAOIs.
Special Precautions
Patient w/ pulmonary impairment or compromised resp function (e.g. COPD, cor pulmonale, decreased resp reserve [e.g. asthma, severe obesity, sleep apnoea], hypoxia, hypercapnia, pre-existing resp depression). Patient w/ hypothyroidism, myxedema, adrenocortical insufficiency (e.g. Addison's disease), dysfunction of biliary tract including acute pancreatitis, acute alcoholism, delirium tremens, toxic psychoses, kyphoscoliosis, prostatic hypertrophy or urethral stricture; comatose patients. Patient w/ CNS depression, history of seizure disorders, head injury, intracranial lesions or conditions in which intracranial pressure may be increased. Patient w/ personal or family history of QT interval prolongation, hypokalaemia or unstable cardiac disease (e.g. AF, CHF, myocardial ischaemia), particularly in transdermal admin. Hepatic or renal impairment. Pregnancy and lactation.
Adverse Reactions
CNS depression, including somnolence, dizziness, alterations in judgment and levels of consciousness, including coma; sedation, dizziness, sweating, vertigo, headache; nausea, vomiting, dry mouth, constipation, dyspepsia, abdominal cramps, flatulence, diaphoresis; rash, urticaria, pruritus; miosis, blurred vision, hallucinations and other psychotomimetic effects; hypotension leading to syncope, HTN, tachycardia, bradycardia, ECG abnormalities.
Potentially Fatal: Resp depression (transdermal).
IM/IV/Parenteral/SL/Transdermal: C
Patient Counseling Information
May impair ability to drive or operate machinery. Avoid exposing the patch to external heat.
MonitoringParameters
Establish baseline liver function levels prior to therapy and periodically monitor liver function throughout therapy in patients treated for opioid dependence.
Overdosage
Symptoms: Resp depression, sedation, somnolence, nausea, vomiting, CV collapse and marked miosis. Management: Supportive treatment. May use naloxone or resp stimulants if appropriate.
Drug Interactions
Plasma-buprenorphine concentrations may be affected when co-administered w/ drugs that induce or inhibit CYP3A4 isoenzyme. Enhanced depressant effects of other CNS depressants, other opiate agonists, anaesth, antihistamines, muscle relaxants, tranquilisers (e.g. phenothiazines), sedatives and hypnotics (e.g. benzodiazepines). Increased and/or prolonged activity w/ drugs that may reduce hepatic blood flow (e.g. halothane). Receiving class IA (e.g. quinidine, procainamide) or class III (e.g. sotalol, amiodarone) antiarrhythmic agents w/ transdermal buprenorphine may increase the risk of QT interval prolongation.
Potentially Fatal: Concomitant admin of IV buprenorphine and oral diazepam may produce resp and CV collapse. MAOIs may be additive w/ or may potentiate action of CNS depressants.
Food Interaction
Increased sedative effect w/ alcohol.
Action
Description: Buprenorphine exerts its analgesic effect via high affinity binding to the mu-opioid receptors in the CNS. It displays partial mu agonist activity and weak kappa antagonist activity.
Onset: Analgesia: W/in 15 min (IM).
Duration: 6 hr (IM); 12-24 hr, or up to 72 hr for the once-wkly dosing (transdermal).
Pharmacokinetics:
Absorption: Rapidly absorbed (approx 40-90%) following IM admin; readily absorbed (approx 55%) following sublingual admin. Absolute bioavailability: Approx 15% (transdermal). Time to peak plasma concentration: 90 min (sublingual); approx 60 hr (transdermal).
Distribution: Crosses the placenta and distributed into breast milk (small amounts). Plasma protein binding: Approx 96%.
Metabolism: Undergoes hepatic metabolism via oxidation by CYP3A4 isoenzyme to the pharmacologically active metabolite N-dealkylbuprenorphine (norbuprenorphine) and via conjugation to glucuronide metabolites.
Excretion: Via faeces mainly as unchanged drug; urine as metabolites. Plasma elimination half-life: 1.2-7.2 hr (IV); 20-36 hr (sublingual or transdermal).
Chemical Structure

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Storage
Store between 15-30°C. Protect from prolonged exposure to light. Avoid freezing.
MIMS Class
ATC Classification
N07BC01 - buprenorphine ; Belongs to the class of drugs used in the management of opioid dependence.
N02AE01 - buprenorphine ; Belongs to the class of oripavine derivative opioids. Used to relieve pain.
Disclaimer: This information is independently developed by MIMS based on Buprenorphine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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