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Nalmefene Hcl (nalmefene HCl)

Opioid Antagonists Injection Vial (Ml)

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Nalmefene hydrochloride is a synthetic opioid antagonist.

Nalmefene hydrochloride is a long-acting opioid antagonist at opioid receptors. Nalmefene antagonizes the effects of natural and synthetic opioids, including respiratory depression, sedation, and hypotension. Nalmefene possesses no opioid agonist activity and does not produce tolerance, physical dependence, or have abuse potential.

In patients who have notrecently received opioids, nalmefene exerts no pharmacologic effect. Nalmefene may produce withdrawal symptoms in patients who are opioid dependent.

Nalmefene is completely bioavailable following IM (101.5%) or SUBQ (99.7%) administration. The bioavailability of a single dose of nalmefene administered by either auto-injector or by nasal spray is comparable to that administered by IM injection. Following IV administration, nalmefene is rapidly distributed, blocking more than 80% of opioid receptors in the brain within 5 minutes of administration after a 1-mg dose.

When given as a single 1-mg dose by the IM or SUBQ route, therapeutic plasma concentrations are likely to be reached within 5-15 minutes. Nalmefene exhibits dose-proportional pharmacokinetics following IV administration. The duration of action of nalmefene is generally as long as most opioid analgesics.

The apparent duration of action of nalmefene will vary depending on the half-life and plasma concentration of the opioid being reversed, the presence or absence of other drugs that affect the brain or muscles of respiration, and the dose of nalmefene administered. Partial reversal doses of nalmefene (1 mcg/kg) lose their effect as the drug is redistributed through the body, and the effects of these low doses may not last more than 30-60 minutes in the presence of persistent opioid effects. Full reversal doses of nalmefene (1 mg/70 kg) have been shown to last many hours in both experimental and clinical studies, but may complicate the management of patients who are in pain, at high cardiovascular risk, or who are physically dependent on opioids.

Nalmefene is 45% bound to plasma proteins. Nalmefene is metabolized by the liver, primarily by glucuronide conjugation; metabolites are either inactive or have minimal pharmacologic activity. Nalmefene is excreted in the urine (<5% as the unchanged drug) and feces (17%).

After IV administration, plasma concentrations of nalmefene decline biexponentially with a redistribution and elimination half-life of 41 minutes and 10.8 hours, respectively. When administered by an auto-injector or nasal spray, the terminal elimination half-life of nalmefene is approximately 9.1 hours and 11.4 hours, respectively. There is no difference in plasma clearance, steady-state volume of distribution, or half-life in geriatric patients compared to younger adults.

In patients with hepatic impairment, plasma clearance is reduced by 28.3% and the elimination half-life is increased to 11.9 hours compared to healthy adults. In patients with end-stage renal disease, plasma clearance is reduced by 27% during interdialysis and 25% during intradialysis; the elimination half-life is prolonged to 26.1 hours compared to healthy adults.

Generic name: nalmefene HCl
Drug class: Opioid Antagonists
Therapeutic class: Antidotes and other Reversal Agents

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

Today’s intelligence on Nalmefene Hcl

Intelligence content is not available yet.

Indications

The following indications are listed for Nalmefene Hcl:

  • Opioid Overdose
  • Opioid-Induced Respiratory Depression

Also known as: Opiate-Induced Respiratory Depression, Opioid Agonist Overdose, Opioid-Induced Inadequate Ventilation.

Dosing

Dosage of nalmefene hydrochloride is expressed in terms of nalmefene.

Titrate dosage to reverse undesired opioid-induced effects. When adequate opioid reversal has been established, additional doses of nalmefene are not required and may cause unwanted reversal of analgesia or precipitate withdrawal.

Drug interactions

There is no enhanced messaging for this drug.

Contraindications

*Known hypersensitivity to nalmefene hydrochloride or any ingredient in the formulation.

Adverse reactions

The most common adverse effects of nalmefene hydrochloride injection (>=5% of patients) include nausea, vomiting, tachycardia, hypertension, feeling hot, headache, dizziness, chills, allodynia, palpitations, tinnitus, ear discomfort, feeling abnormal, burning sensation, hot flush, and irritability.

The most common adverse effects of nalmefene hydrochloride nasal spray (>=2% of patients) include nasal discomfort, headache, nausea, dizziness, hot flush, vomiting, anxiety, fatigue, nasal congestion, throat irritation, rhinalgia, decreased appetite, dysgeusia, erythema, and hyperhidrosis.

Precautions

No enhanced messaging available.

ICD codes

CodeTypeDescription
Opioid overdose
T40.0x1AICD10CMPoisoning by opium, accidental (unintentional), initial encounter
T40.0x2AICD10CMPoisoning by opium, intentional self-harm, initial encounter
T40.0x3AICD10CMPoisoning by opium, assault, initial encounter
T40.0x4AICD10CMPoisoning by opium, undetermined, initial encounter
T40.1x1AICD10CMPoisoning by heroin, accidental (unintentional), initial encounter
T40.1x2AICD10CMPoisoning by heroin, intentional self-harm, initial encounter
T40.1x3AICD10CMPoisoning by heroin, assault, initial encounter
T40.1x4AICD10CMPoisoning by heroin, undetermined, initial encounter
T40.2x1AICD10CMPoisoning by other opioids, accidental (unintentional), initial encounter
T40.2x2AICD10CMPoisoning by other opioids, intentional self-harm, initial encounter
T40.2x3AICD10CMPoisoning by other opioids, assault, initial encounter
T40.2x4AICD10CMPoisoning by other opioids, undetermined, initial encounter
T40.3x1AICD10CMPoisoning by methadone, accidental (unintentional), initial encounter
T40.3x2AICD10CMPoisoning by methadone, intentional self-harm, initial encounter
T40.3x3AICD10CMPoisoning by methadone, assault, initial encounter
T40.3x4AICD10CMPoisoning by methadone, undetermined, initial encounter
T40.411AICD10CMPoisoning by fentanyl or fentanyl analogs, accidental (unintentional), initial encounter
T40.412AICD10CMPoisoning by fentanyl or fentanyl analogs, intentional self-harm, initial encounter
T40.413AICD10CMPoisoning by fentanyl or fentanyl analogs, assault, initial encounter
T40.414AICD10CMPoisoning by fentanyl or fentanyl analogs, undetermined, initial encounter
T40.421AICD10CMPoisoning by tramadol, accidental (unintentional), initial encounter
T40.422AICD10CMPoisoning by tramadol, intentional self-harm, initial encounter
T40.423AICD10CMPoisoning by tramadol, assault, initial encounter
T40.424AICD10CMPoisoning by tramadol, undetermined, initial encounter
T40.491AICD10CMPoisoning by other synthetic narcotics, accidental (unintentional), initial encounter
T40.492AICD10CMPoisoning by other synthetic narcotics, intentional self-harm, initial encounter
T40.493AICD10CMPoisoning by other synthetic narcotics, assault, initial encounter
T40.494AICD10CMPoisoning by other synthetic narcotics, undetermined, initial encounter
T40.601AICD10CMPoisoning by unspecified narcotics, accidental (unintentional), initial encounter
T40.602AICD10CMPoisoning by unspecified narcotics, intentional self-harm, initial encounter
T40.603AICD10CMPoisoning by unspecified narcotics, assault, initial encounter
T40.604AICD10CMPoisoning by unspecified narcotics, undetermined, initial encounter
T40.691AICD10CMPoisoning by other narcotics, accidental (unintentional), initial encounter
T40.692AICD10CMPoisoning by other narcotics, intentional self-harm, initial encounter
T40.693AICD10CMPoisoning by other narcotics, assault, initial encounter
T40.694AICD10CMPoisoning by other narcotics, undetermined, initial encounter
T50.7x1AICD10CMPoisoning by analeptics and opioid receptor antagonists, accidental (unintentional), initial encounter
T50.7x2AICD10CMPoisoning by analeptics and opioid receptor antagonists, intentional self-harm, initial encounter
T50.7x3AICD10CMPoisoning by analeptics and opioid receptor antagonists, assault, initial encounter
T50.7x4AICD10CMPoisoning by analeptics and opioid receptor antagonists, undetermined, initial encounter
Opioid-induced respiratory depression
T40.0x1AICD10CMPoisoning by opium, accidental (unintentional), initial encounter
T40.0x2AICD10CMPoisoning by opium, intentional self-harm, initial encounter
T40.0x3AICD10CMPoisoning by opium, assault, initial encounter
T40.0x4AICD10CMPoisoning by opium, undetermined, initial encounter
T40.1x1AICD10CMPoisoning by heroin, accidental (unintentional), initial encounter
T40.1x2AICD10CMPoisoning by heroin, intentional self-harm, initial encounter
T40.1x3AICD10CMPoisoning by heroin, assault, initial encounter
T40.1x4AICD10CMPoisoning by heroin, undetermined, initial encounter
T40.2x1AICD10CMPoisoning by other opioids, accidental (unintentional), initial encounter
T40.2x2AICD10CMPoisoning by other opioids, intentional self-harm, initial encounter
T40.2x3AICD10CMPoisoning by other opioids, assault, initial encounter
T40.2x4AICD10CMPoisoning by other opioids, undetermined, initial encounter
T40.3x1AICD10CMPoisoning by methadone, accidental (unintentional), initial encounter
T40.3x2AICD10CMPoisoning by methadone, intentional self-harm, initial encounter
T40.3x3AICD10CMPoisoning by methadone, assault, initial encounter
T40.3x4AICD10CMPoisoning by methadone, undetermined, initial encounter
T40.411AICD10CMPoisoning by fentanyl or fentanyl analogs, accidental (unintentional), initial encounter
T40.412AICD10CMPoisoning by fentanyl or fentanyl analogs, intentional self-harm, initial encounter
T40.413AICD10CMPoisoning by fentanyl or fentanyl analogs, assault, initial encounter
T40.414AICD10CMPoisoning by fentanyl or fentanyl analogs, undetermined, initial encounter
T40.421AICD10CMPoisoning by tramadol, accidental (unintentional), initial encounter
T40.422AICD10CMPoisoning by tramadol, intentional self-harm, initial encounter
T40.423AICD10CMPoisoning by tramadol, assault, initial encounter
T40.424AICD10CMPoisoning by tramadol, undetermined, initial encounter
T40.491AICD10CMPoisoning by other synthetic narcotics, accidental (unintentional), initial encounter
T40.492AICD10CMPoisoning by other synthetic narcotics, intentional self-harm, initial encounter
T40.493AICD10CMPoisoning by other synthetic narcotics, assault, initial encounter
T40.494AICD10CMPoisoning by other synthetic narcotics, undetermined, initial encounter
T40.5x1AICD10CMPoisoning by cocaine, accidental (unintentional), initial encounter
T40.5x2AICD10CMPoisoning by cocaine, intentional self-harm, initial encounter
T40.5x3AICD10CMPoisoning by cocaine, assault, initial encounter
T40.5x4AICD10CMPoisoning by cocaine, undetermined, initial encounter
T40.601AICD10CMPoisoning by unspecified narcotics, accidental (unintentional), initial encounter
T40.602AICD10CMPoisoning by unspecified narcotics, intentional self-harm, initial encounter
T40.603AICD10CMPoisoning by unspecified narcotics, assault, initial encounter
T40.604AICD10CMPoisoning by unspecified narcotics, undetermined, initial encounter
T40.691AICD10CMPoisoning by other narcotics, accidental (unintentional), initial encounter
T40.692AICD10CMPoisoning by other narcotics, intentional self-harm, initial encounter
T40.693AICD10CMPoisoning by other narcotics, assault, initial encounter
T40.694AICD10CMPoisoning by other narcotics, undetermined, initial encounter

ICD code information from First Databank (FDB).

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Last reviewed · Source: First Databank (FDB) drug data