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).
May impair ability to drive or operate machinery. Avoid exposing the patch to external heat.
Monitoring Parameters
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: Mechanism of Action: 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
Buprenorphine Source: National Center for Biotechnology Information. PubChem Database. Buprenorphine, CID=644073, https://pubchem.ncbi.nlm.nih.gov/compound/Buprenorphine (accessed on Jan. 22, 2020)
Storage
Store between 15-30°C. Protect from prolonged exposure to light. Avoid freezing.
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.
References
Anon. Buprenorphine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/01/2016.Buckingham R (ed). Buprenorphine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/01/2016.McEvoy GK, Snow EK, Miller J et al (eds). Buprenorphine Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 06/01/2016.Subutex Sublingual Tablet. U.S. FDA. https://www.fda.gov/. Accessed 06/01/2016.
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