Nalmefene


Concise Prescribing Info
Indications/Uses
Adjunct in alcohol dependence.
Dosage/Direction for Use
Adult : PO 18 mg/day preferably at least 1-2 hr before anticipated time of alcohol drinking. If a dose has not been taken before alcohol intake, 1 dose to be taken immediately.
Dosage Details
Oral
Adjunct in alcohol dependence
Adult: 18 mg daily, preferably at least 1-2 hr before anticipated time of alcohol drinking. If a dose has not been taken before alcohol intake, 1 dose to be taken immediately.
Renal Impairment
Severe (eGFR <30 mL/min/1.73 m2): Contraindicated.
Hepatic Impairment
Severe: Contraindicated.
Contraindications
Current or recent opioid addiction, acute opioid withdrawal symptoms, history of acute alcohol withdrawal syndrome. Severe hepatic and renal impairment. Concomitant use w/ opioid agonists (e.g. opioid analgesics, methadone) or partial agonists (e.g. buprenorphine).
Special Precautions
Patient w/ psychiatric comorbidity (e.g. major depressive disorder), history of seizure disorders. Intended for use only to patient w/ high drinking risk level, at least 2 wk after assessment. Mild or moderate renal and hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Psychiatric symptoms, alcoholic psychosis, alcohol withdrawal symptoms.
Nervous: Dizziness, insomnia, headache, sleep disorder, confusional state, restlessness, somnolence, tremor, attention disturbance, paraesthesia, hypoaesthesia, fatigue, asthenia, malaise, abnormal feeling, hallucinations, dissociation.
CV: Tachycardia, palpitation.
GI: Nausea, decreased appetite, vomiting, dry mouth, diarrhoea.
Endocrine: Decreased libido, wt decreased.
Musculoskeletal: Muscle spasms.
Dermatologic: Hyperhidrosis.
Patient Counseling Information
This drug may cause dizziness and somnolence, if affected, do not drive or operate machinery.
MonitoringParameters
Assess clinical status, alcohol dependence, level of alcohol consumption before initiation of therapy.
Drug Interactions
Increased exposure w/ UGT2B7 enzyme inhibitors (e.g. diclofenac, fluconazole). Decreased exposure w/ UGT2B7 enzyme inducers (e.g. dexamethasone, phenobarbital).
Potentially Fatal: Increased risk of resp depression w/ opioids (e.g. cough medications, opioid analgesics).
Action
Description: Nalmefene is 6-methylene analogue of naltrexone, a specific opioid antagonist. It modifies cortico-mesolimbic functions of opioid receptors thereby reduces the level of alcohol consumption.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Bioavailability: Approx 40%. Time to peak plasma concentration: Approx 1.5 hr.
Distribution: Volume of distribution: Approx 3,200 L. Plasma protein binding: Approx 30%.
Metabolism: Undergoes rapid extensive first-pass metabolism in the liver into inactive nalmefene 3-O-glucuronide metabolite by UGT enzymes; small portion via sulfation into nalmefene 3-O-sulfate; and into nornalmefene by CYP enzymes and further converted to nornalmefene 3-O-glucuronide and nornalmefene 3-O-sulfate.
Excretion: Via urine (54%, as inactive metabolites); faeces (small amount). Terminal elimination half-life: Approx 12.5 hr.
Chemical Structure

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Storage
Store below 30°C.
ATC Classification
N07BB05 - nalmefene ; Belongs to the class of drugs used in the management of alcohol dependence.
Disclaimer: This information is independently developed by MIMS based on Nalmefene 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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