NALMEFENE HYDROCHLORIDE

NALMEFENE HYDROCHLORIDE is an FDA-registered drug product whose active ingredient is NALMEFENE HYDROCHLORIDE. It is labelled by Knoa Pharma LLC taken by intramuscular and marketed as a human prescription drug product. Identifiers on file: NDC 59011-960, application ANDA212955, label effective 20260501. It is one of 2 FDA drug label records sharing the active ingredient NALMEFENE HYDROCHLORIDE. This page reproduces the FDA-approved label text so you can check what a product is, who makes it and how it is supplied before discussing it with a pharmacist or prescriber.

Across FDA labelling, products containing NALMEFENE HYDROCHLORIDE are most often described in connection with: nalmefene hydrochloride, injection indicated, complete partial, reversal opioid, drug effects, including respiratory, depression induced, either natural. Wording differs between labels, and the full indications section on this page takes precedence when it is present.

INDICATIONS AND USAGE Nalmefene hydrochloride injection is indicated for the complete or partial reversal of opioid drug effects, including respiratory depression, induced by either natural or synthetic opioids. Nalmefene hydrochloride injection is indicated in the management of known or suspected opioid overdose.

DOSAGE AND ADMINISTRATION Important Information - Dosage Form Nalmefene hydrochloride injection is supplied in a 2 mL vial as a 1 mg/mL concentration suitable for the management of overdose. Proper steps should be taken to prevent use of the incorrect concentration. General Principles Nalmefene hydrochloride injection should be titrated to reverse the undesired effects of opioids. Once adequate reversal has been established, additional administration is not required and may actually be harmful due to unwanted reversal of analgesia or precipitated withdrawal. Duration of Action The duration of action of nalmefene hydrochloride injection is as long as most opioid analgesics. The apparent duration of action of nalmefene hydrochloride injection will vary, however, depending on the half-life and plasma concentration of the narcotic being reversed, the presence or absence of other drugs affecting the brain or muscles of respiration, and the dose of nalmefene hydrochloride injection administered. Partially reversing doses of nalmefene hydrochloride injection (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 to 60 minutes in the presence of persistent opioid effects. Fully reversing doses (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. The recommended doses represent a compromise between a desirable controlled reversal and the need for prompt response and adequate duration of action. Using higher dosages or shorter intervals between incremental doses is likely to increase the incidence and severity of symptoms related to acute withdrawal such as nausea, vomiting, elevated blood pressure, and anxiety. Patients Tolerant to or Physically Dependent on Opioids Nalmefene hydrochloride injection may cause acute withdrawal symptoms in individuals who have some degree of tolerance to and dependence on opioids. These patients should be closely observed for symptoms of withdrawal following administration of the initial and subsequent injections of nalmefene hydrochloride injection. Subsequent doses should be administered with intervals of at least 2 to 5 minutes between doses to allow the full effect of each incremental dose of nalmefene hydrochloride injection to be reached. Management of Known or Suspected Opioid Overdose The recommended initial dose of nalmefene hydrochloride injection for non-opioid dependent patients is 0.5 mg/70 kg. If needed, this may be followed by a second dose of 1 mg/70 kg, 2 to 5 minutes later. If a total dose of 1.5 mg/70 kg has been administered without clinical response, additional nalmefene hydrochloride injection is unlikely to have an effect. Patients should not be given more nalmefene hydrochloride injection than is required to restore the respiratory rate to normal, thus minimizing the likelihood of cardiovascular stress and precipitated withdrawal syndrome. If there is a reasonable suspicion of opioid dependency, a challenge dose of nalmefene hydrochloride injection 0.1 mg/70 kg should be administered initially. If there is no evidence of withdrawal in 2 minutes, the recommended dosing should be followed. Nalmefene hydrochloride injection had no effect in cases where opioids were not responsible for sedation and hypoventilation. Therefore, patients should only be treated with nalmefene hydrochloride injection when the likelihood of an opioid overdose is high, based on a history of opioid overdose or the clinical presentation of respiratory depression with concurrent pupillary constriction. Repeated Dosing Nalmefene hydrochloride injection is the longest acting of the currently available parenteral opioid antagonists. If recurrence of respiratory depression does occur, the dose should again be titrated to clinical effect using incremental doses to avoid over-reversal. Hepatic and Renal Disease Hepatic disease and renal failure substantially reduce the clearance of nalmefene (see Pharmacokinetics ). For single episodes of opioid antagonism, adjustment of nalmefene hydrochloride injection dosage is not required. However, in patients with renal failure, the incremental doses should be delivered slowly (over 60 seconds) to minimize the hypertension and dizziness reported following the abrupt administration of nalmefene to such patients. Loss of Intravenous Access Should intravenous access be lost or not readily obtainable, a pharmacokinetic study has shown that a single dose of nalmefene hydrochloride injection should be effective within 5 to 15 minutes after intramuscular or subcutaneous doses of 1 mg (see Pharmacokinetics ).

CONTRAINDICATIONS Nalmefene hydrochloride injection is contraindicated in patients with a known hypersensitivity to the product.

WARNINGS Use of Nalmefene Hydrochloride Injection in Emergencies Nalmefene hydrochloride injection, like all drugs in this class, is not the primary treatment for ventilatory failure. In most emergency settings, treatment with nalmefene hydrochloride injection should follow, not precede, the establishment of a patent airway, ventilatory assistance, administration of oxygen, and establishment of circulatory access. Risk of Recurrent Respiratory Depression Accidental overdose with long acting opioids [such as methadone and levo -alpha-acetylmethadol (LAAM)] may result in prolonged respiratory depression. Respiratory depression in both the postoperative and overdose setting may be complex and involve the effects of anesthetic agents, neuromuscular blockers, and other drugs. While nalmefene hydrochloride injection has a longer duration of action than naloxone in fully reversing doses, the physician should be aware that a recurrence of respiratory depression is possible, even after an apparently adequate initial response to nalmefene hydrochloride injection treatment. Patients treated with nalmefene hydrochloride injection should be observed until, in the opinion of the physician, there is no reasonable risk of recurrent respiratory depression.

ADVERSE REACTIONS Adverse event information was obtained following administration of nalmefene hydrochloride injection to 152 normal volunteers and in controlled clinical trials to 1127 patients for the treatment of opioid overdose or for postoperative opioid reversal. Nalmefene was well tolerated and showed no serious toxicity during experimental administration to healthy individuals, even when given at 15 times the highest recommended dose. In a small number of subjects, at doses exceeding the recommended nalmefene hydrochloride injection dose, nalmefene produced symptoms suggestive of reversal of endogenous opioids, such as have been reported for other narcotic antagonist drugs. These symptoms (nausea, chills, myalgia, dysphoria, abdominal cramps, and joint pain) were usually transient and occurred at very low frequency. Such symptoms of precipitated opioid withdrawal at the recommended clinical doses were seen in both postoperative and overdose patients who were later found to have had histories of covert opioid use. Symptoms of precipitated withdrawal were similar to those seen with other opioid antagonists, were transient following the lower doses used in the postoperative setting, and more prolonged following the administration of the larger doses used in the treatment of overdose. Tachycardia and nausea following the use of nalmefene in the postoperative setting were reported at the same frequencies as for naloxone at equivalent doses. The risk of both these adverse events was low at doses giving partial opioid reversal and increased with increases in dose. Thus, total doses larger than 1 mcg/kg in the postoperative setting and 1.5 mg/70 kg in the treatment of overdose are not recommended. Relative Frequencies of Common Adverse Reactions with an Incidence Greater than 1% (all patients, all clinical settings) Adverse Event Nalmefene N=1127 Naloxone N=369 Placebo N=77 Nausea 18% 18% 6% Vomiting 9% 7% 4% Tachycardia 5% 8% - Hypertension 5% 7% - Postoperative pain 4% 4% N/A Fever 3% 4% - Dizziness 3% 4% 1% Headache 1% 1% 4% Chills 1% 1% - Hypotension 1% 1% - Vasodilation 1% 1% - Incidence less than 1% CARDIOVASCULAR: Bradycardia, arrhythmia DIGESTIVE: Diarrhea, dry mouth NERVOUS SYSTEM: Somnolence, depression, agitation, nervousness, tremor, confusion, withdrawal syndrome, myoclonus RESPIRATORY: Pharyngitis SKIN: Pruritus UROGENITAL: Urinary retention The incidence of adverse events was highest in patients who received more than the recommended dose of nalmefene hydrochloride injection. Laboratory findings Transient increases in CPK were reported as adverse events in 0.5% of the postoperative patients studied. These increases were believed to be related to surgery and not believed to be related to the administration of nalmefene hydrochloride injection. Increases in AST were reported as adverse events in 0.3% of the patients receiving either nalmefene or naloxone. The clinical significance of this finding is unknown. No cases of hepatitis or hepatic injury due to either nalmefene or naloxone were observed in the clinical trials.

FDA lists 2 drug label records with NALMEFENE HYDROCHLORIDE as the active ingredient. The most common dosage forms and the manufacturers with the most records are summarised below; strengths, pack sizes and inactive ingredients can still differ between apparently similar products.

What is NALMEFENE HYDROCHLORIDE used for?
INDICATIONS AND USAGE Nalmefene hydrochloride injection is indicated for the complete or partial reversal of opioid drug effects, including respiratory depression, induced by either natural or synthetic opioids. Nalmefene hydrochloride injection is indicated in the management of known or suspected opioid overdose.

Who makes NALMEFENE HYDROCHLORIDE?
Knoa Pharma LLC is the labeler of record for NALMEFENE HYDROCHLORIDE. 2 FDA label records share the active ingredient NALMEFENE HYDROCHLORIDE, so generic and branded versions may come from different companies; the manufacturer named on your pack is the one that matters for any enquiry.

What form does NALMEFENE HYDROCHLORIDE come in?
administered by intramuscular. Strengths and pack sizes vary by label, so compare the NDC on your pack with the identifier listed on this page.

Is NALMEFENE HYDROCHLORIDE prescription or over-the-counter?
The FDA label for this product is recorded as human prescription drug. Marketing status can differ between strengths and countries, so check the dispensing rules where you live.

Are there other products containing NALMEFENE HYDROCHLORIDE?
Yes. 2 FDA drug label records list NALMEFENE HYDROCHLORIDE as the active ingredient. Products with the same active ingredient can usually be substituted only when a prescriber or pharmacist confirms it is appropriate.

Has NALMEFENE HYDROCHLORIDE been recalled?
No FDA recall record in our database matches this product name or manufacturer. Recall data is updated periodically, so a very recent notice may not appear here yet.

Where does this information come from?
All content is reproduced from FDA Structured Product Labelling data via openFDA. It is provided for identification and reference only and is not medical advice.