Nalmefene

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Latin America

Mexico: Nocarex.

Drug combinations

Chemistry

Nalmefene: C~21~H~25~NO~3~. Mw: 339.43. (1) Morphinan-3,14-diol, 17-(cyclopropylmethyl)-4,5-epoxy-6-methylene-, (5α)-; (2) 17-(Cyclopropylmethyl)-4,5α-epoxy-6-methylenemorphinan-3,14-diol. CAS-55096-26-9 (1981).

Pharmacologic Category

Opiate Antagonists. Antidotes. (ATC-Code: N07BC).

Mechanism of action

Acts as competitive antagonist at opioid receptor sites, preventing or reversing respiratory depression, sedation, and hypotension induced by opiates.

Therapeutic use

Complete or partial reversal of opioid drug effects, including respiratory depression induced by natural or synthetic opioids. Reversal of postoperative opioid depression. Management of known or suspected opioid overdose.

Pregnancy and lactiation implications

Animal studies have not demonstrated fetal harm or fertility impairment. There are no adequate, well-controlled studies in pregnant women. Use only if clearly needed. Should not be used in lactating women if possible.

Unlabeled use

Contraindications

Hypersensitivity to nalmefene or any component of the formulation.

Warnings and precautions

May precipitate symptoms of acute withdrawal in opioid-dependent patients, including pain, hypertension, sweating, agitation, and irritability. Animal studies indicate nalmefene may not completely reverse buprenorphine-induced respiratory depression. Nalmefene structurally similar to both naltrexone and naloxone (patients with hypersensitivity to these agents may also react to nalmefene). Use with caution in cardiovascular disease or in patients receiving medications with potential adverse cardiovascular effects (e.g. hypotension, pulmonary edema or arrhythmias). Pulmonary edema and cardiovascular instability, including ventricular fibrillation, reported in association with abrupt reversal when using narcotic antagonists. Use with caution in renal impairment. Concurrent use of flumazenil and nalmefene may increase risk of seizures. Patients are at greater risk of overdose when nalmefene wears off if megadosing of opiates occurred. Risk of recurrent respiratory depression if opioid involved is long-acting. Excessive dosages should be avoided after use of opiates in surgery. Abrupt postoperative reversal may result in nausea, vomiting, sweating, tachycardia, hypertension, seizures, and other cardiovascular events (including pulmonary edema and arrhythmias).

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