Adult: For management of known or suspected cases: In non-opioid-dependent patients: Initially, 0.5 mg/70 kg, followed by 2nd dose of 1 mg/70 kg after 2-5 minutes, if needed. In opioid-dependent patients: Initially, administer a challenge dose of 0.1 mg/70 kg. If no evidence of withdrawal within 2 minutes, administer 0.5 mg/70 kg. If needed, a 2nd dose of 1 mg/70 kg may be given after 2-5 minutes. All doses may be given via IV (preferred), IM or SC inj.
Nasal Opioid overdosage
Adult: For emergency treatment of known or suspected cases as manifested by respiratory and/or CNS depression: As nasal spray: 1 spray (2.7 mg) as a single dose in 1 nostril. May repeat dose every 2-5 minutes as needed, to be given in alternate nostrils, for continued or recurrent respiratory depression until emergency medical assistance becomes available. Child: ≥12 years Same as adult dose.
Oral Adjunct in alcohol dependence
Adult: For reduction of alcohol consumption in patients who continue to have high drinking risk level 2 weeks after initial assessment, without physical withdrawal symptoms and who do not need immediate detoxification: 18 mg once daily as needed, preferably 1-2 hours before anticipated time of drinking. If a dose is not taken before alcohol intake, 1 dose must be taken as soon as possible. Max: 18 mg daily.
Renal Impairment
Oral:
Severe (eGFR <30 mL/min/1.73 m2): Contraindicated.
Hepatic Impairment
Oral:
Severe: Contraindicated.
Contraindications
Oral: Current or recent opioid addiction, acute symptoms of opioid withdrawal, suspected recent use of opioid, recent history of acute alcohol withdrawal syndrome (including hallucinations, delirium tremens and seizures). Severe renal and hepatic impairment. Concomitant use of opioid agonists (e.g. methadone, opioid analgesics) or partial opioid agonist (e.g. buprenorphine).
Special Precautions
Patient with CV disease, psychiatric disorder (e.g. major depressive disorder); history of seizure disorders, including alcohol withdrawal seizures (oral); known physical dependence on opioids (parenteral). Oral preparation of nalmefene is not indicated for use in patients needing immediate alcohol detoxification or for immediate abstinence. Temporarily discontinue oral nalmefene 1 week before the scheduled elective surgery if opioid use is anticipated. Mild to moderate renal and hepatic impairment (oral). Children (nasal) and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: May precipitate opioid withdrawal syndrome (particularly in opioid-dependent patients). Cardiac disorders: Tachycardia; palpitations (oral). Gastrointestinal disorders: Nausea, vomiting, diarrhoea, dry mouth. General disorders and administration site conditions: Fatigue, asthenia, malaise, feeling abnormal. Investigations: Weight decreased (oral). Metabolism and nutrition disorders: Decreased appetite. Musculoskeletal and connective tissue disorders: Muscle spasm (oral). Nervous system disorders: Dizziness, headache; somnolence, tremor, paraesthesia, hypoaesthesia, disturbance in attention (oral). Psychiatric disorders: Insomnia; anxiety (nasal); sleep disorder, confusional state, restlessness (oral). Rarely, hallucinations, dissociation (oral). Reproductive system and breast disorders: Decreased libido (oral). Respiratory, thoracic and mediastinal disorders: Nasal congestion, nasal discomfort, rhinalgia, dyspnoea, throat irritation, oropharyngeal pain (nasal). Skin and subcutaneous tissue disorders: Diaphoresis. Vascular disorders: Hot flushes (nasal); hypertension (IV).
Monitoring Parameters
Evaluate the patient's clinical status, alcohol dependence and level of consumption before initiating oral treatment. Monitor respiratory rate, heart rate, blood pressure, level of consciousness, arterial blood gas, and pulse oximetry. Assess for acute opioid withdrawal (e.g. pain, abnormal heartbeat, fever, sweating, gastrointestinal symptoms).
Drug Interactions
May increase exposure with UGT2B7 potent inhibitors (e.g. diclofenac, fluconazole, medroxyprogesterone, meclofenamic acid). May decrease exposure with UGT inducers (e.g. dexamethasone, rifampicin, omeprazole, phenobarbital).
Action
Description: Mechanism of Action: Nalmefene, a 6-methylene analogue of naltrexone, is a competitive opioid receptor antagonist. It reverses the respiratory depression induced by opioids. It also reduces the urge to drink, possibly by modulating the activity of opioid receptors involved in addiction. Onset: 2-5 minutes (IV); 5-15 minutes (IM, SC); 2.5-5 minutes (nasal). Duration: IV: Partially reversing doses: 30-60 minutes. Fully reversing doses: >4 hours. Pharmacokinetics: Absorption: Rapidly absorbed (oral). Bioavailability: Approx 40% (oral); approx 100% (IM, SC); approx 80% (nasal). Time to peak plasma concentration: Approx 1.5 hours (oral, SC); 2.3 hours (IM); approx 15 minutes (nasal). Distribution: Plasma protein binding: Approx 45%. Metabolism: Metabolised in the liver via glucuronide conjugation, mainly into inactive glucuronide, and to trace amounts of inactive N-dealkylated metabolite; undergoes enterohepatic recycling. Excretion: Via urine (<5% as unchanged drug); faeces (17%). Elimination half-life: Approx 10 hours (IV); 12.5 hours (oral).
Chemical Structure
Nalmefene Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5284594, Nalmefene. https://pubchem.ncbi.nlm.nih.gov/compound/Nalmefene. Accessed Mar. 26, 2025.
Storage
Tab: Store at room temperature. Solution for inj: Store between 20-25°C. Protect from light. Nasal spray: Store between 15-25°C. Do not freeze. Protect from light.
N07BB05 - nalmefene ; Belongs to the class of drugs used in the management of alcohol dependence.
References
Anon. Nalmefene. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 03/02/2025.Brayfield A, Cadart C (eds). Nalmefene. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/02/2025.Joint Formulary Committee. Nalmefene. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/02/2025.Nalmefene Hydrochloride Injection, Solution (Purdue Pharma L.P.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 17/03/2025.Nalmefene. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 03/02/2025.Opvee Spray (Indivior Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 17/03/2025.Selincro 18 mg Film-coated Tablets (Lundbeck Limited). MHRA. https://products.mhra.gov.uk. Accessed 03/02/2025.
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