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.
Indications and Dosage
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.
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Renal Impairment
Severe (eGFR <30 mL/min/1.73 m2): Contraindicated.
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Hepatic Impairment
Severe: Contraindicated.
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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).
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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.
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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.
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Monitoring Parameters
Assess clinical status, alcohol dependence, level of alcohol consumption before initiation of therapy.
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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:
Mechanism of Action: 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.
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MIMS Class
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ATC Classification
N07BB05 - nalmefene ; Belongs to the class of drugs used in the management of alcohol dependence.
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References
Anon. Pharmacotherapy for Alcohol Use Disorder. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/10/2017. Buckingham R (ed). Nalmefene. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/08/2017. Joint Formulary Committee. Nalmefene. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/08/2017. McEvoy GK, Snow EK, Miller J et al (eds). Nalmefene Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 23/08/2017.
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