Buprenorphine + Naloxone


Concise Prescribing Info
Indications/Uses
Opioid dependence.
Dosage/Direction for Use
Adult : Sublingual Expressed as buprenorphine: Initial: 2-4 mg once daily, may admin an additional dose of 2-4 mg on day 1. May increase in increments of 2-8 mg. Total wkly dose may be divided and given on alternate days or 3 times wkly. Max: 24 mg/day.
Dosage Details
Sublingual
Opioid dependence
Adult: Expressed as buprenorphine: Initially, 2-4 mg once daily, may admin an additional dose of 2-4 mg on day 1 depending on patient's response. Increased in increments of 2-8 mg according to response. Total wkly dose may be divided and given on alternate days or 3 times wkly. Max: 24 mg daily.
Hepatic Impairment
Severe: Contraindicated.
Administration
May be taken with or without food. Place under the tongue & allow to dissolve completely.
Contraindications
Severe resp insufficiency, acute alcoholism or delirium tremens. Severe hepatic impairment. Concomitant admin w/ opioid antagonists (naltrexone, nalmefene).
Special Precautions
Patient w/ head injury, intracranial lesions, other circumstances where cerebrospinal pressure may be increased, history of seizure; hypotension, prostatic hypertrophy, urethral stenosis; myxoedema, hypothyroidism, adrenal cortical insufficiency (e.g. Addison's disease); biliary tract dysfunction. Severe renal and moderate hepatic impairment. Debilitated patients. Pregnancy and lactation.
Adverse Reactions
Influenza, infection, pharyngitis, rhinitis, depression, anxiety, nervousness, abnormal thinking, decreased libido, migraine, hypertonia, dizziness, paraesthesia, somnolence, amblyopia, lacrimal disorder, HTN, vasodilatation, cough, diarrhoea, abdominal pain, vomiting, flatulence, dyspepsia, pruritus, urticaria, rash, back pain, arthralgia, myalgia, muscle spasms, urine abnormality, erectile dysfunction, chest pain, asthenia, pyrexia, chills, malaise, pain, peripheral oedema, abnormal LFT, decreased wt, injury.
Patient Counseling Information
This drug may cause drowsiness, dizziness or impaired thinking, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor LFTs prior to and periodically during treatment; resp and mental status, CNS depression, symptoms of withdrawal, signs of addiction.
Overdosage
Symptoms: Resp depression, amblyopia, miosis, somnolence, hypotension, nausea, vomiting, and speech disorders. Management: Supportive and symptomatic treatment. Assure a patent airway and assisted or controlled ventilation.
Drug Interactions
Concomitant admin w/ benzodiazepines may result to death due to resp depression. May increase CNS depression w/ other CNS depressants and other opioid derivatives (e.g. methadone, antitussives, analgesics), barbiturates, clonidine, neuroleptics, anxiolytics other than benzodiazepines, sedative H1-receptor antagonists, certain antidepressants. May reduce plasma levels w/ CYP3A4 inducers (e.g. phenobarbital, carbamazepine). May exaggerate effects w/ MAOIs.
Potentially Fatal: Blocked pharmacological effects w/ opioid antagonists (naltrexone, nalmefene).
Food Interaction
May enhance sedative effect w/ alcohol.
Action
Description: Buprenorphine is a partial agonist/antagonist at the µ- and kappa-opioid receptor of the brain. Its activity is attributed to its slowly reversible properties w/ the µ-opioid receptors which, over a prolonged period may minimise the need of addicted patients for drugs. Naloxone, a potent antagonist at the µ-opioid receptors, produces marked opioid antagonist effects and opioid withdrawal, thus deterring IV abuse.
Pharmacokinetics:
Absorption: Buprenorphine: Absorbed through the buccal mucosa. Time to peak plasma concentration: 90 min. Naloxone: Absorbed from the GI tract.
Distribution: Buprenorphine: It crosses the placenta, enters breast milk (small amounts). Plasma protein binding: Approx 96%. Naloxone: Extensively distributed into body tissues and fluids, particularly the brain; crosses the placenta. Plasma protein binding: Approx 32-45%.
Metabolism: Buprenorphine: Hepatically metabolised via oxidation by CYP3A4 isoenzyme to active metabolite N-dealkylbuprenorphine (norbuprenorphine), and via conjugation to glucuronide metabolites. Naloxone: Hepatically metabolised via glucuronide conjugation, w/ naloxone-3-glucuronide as major metabolite.
Excretion: Buprenorphine: Mainly via faeces (as unchanged drug); urine (as metabolites). Elimination half-life: 20 to >36 hr. Naloxone: Via urine (as metabolites).
Chemical Structure

Chemical Structure Image
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)


Chemical Structure Image
Naloxone

Source: National Center for Biotechnology Information. PubChem Database. Naloxone, CID=5284596, https://pubchem.ncbi.nlm.nih.gov/compound/Naloxone (accessed on Jan. 22, 2020)

Storage
Store between 20-25°C.
MIMS Class
ATC Classification
N07BC51 - buprenorphine, combinations ; Belongs to the class of drugs used in the management of opioid dependence.
References
Anon. Buprenorphine and Naloxone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/03/2016.

Buckingham R (ed). Buprenorphine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/03/2016.

Buckingham R (ed). Naloxone Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/03/2016.

Buprenorphine Hydrochloride and Naloxone Hydrochloride Dehydrate Tablet (Actavis Pharma, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 07/03/2016.

Joint Formulary Committee. Buprenorphine with Naloxone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/03/2016.

Disclaimer: This information is independently developed by MIMS based on Buprenorphine + Naloxone 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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