nalmefene

REMS

Emergency treatment of known or suspected overdose caused by natural or synthetic opioids and characterized by respiratory and/or CNS depression

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Known hypersensitivity.

Use Cautiously in:

Overdosage of buprenorphine (may not completely reverse respiratory depression; may required repeated doses);
Pedi: Children <12 yr (safety and effectiveness not established).

Exercise Extreme Caution in:

Patients known to be physically dependent on opioid agents or who have undergone surgery with large doses of opioid analgesics (especially those with severe cardiovascular disease or who have received cardiovascular medications) (↑ risk of withdrawal and cardiovascular complications).

Adv. Reactions/Side Effects ⬆ ⬇

CV: palpitations, hypertension, hypotension, tachycardia

Derm: hot flush, ↑sweating, erythema

EENT: nasal discomfort, tinnitus, ear discomfort, nasal congestion, oropharyngeal pain, rhinitis, throat irritation

GI: nausea, vomiting, abdominal pain, dry mouth

Metab: ↓appetite

Neuro: allodynia, dizziness, headache, irritability, agitation, anxiety, claustrophobia, dysgeusia, fatigue, insomnia, paresthesia, recurrent CNS depression

Resp: dyspnea, recurrent respiratory depression

Misc: chills, fever, postoperative pain

Interactions ⬆ ⬇

Drug-drug:

None reported.

Availability ⬆ ⬇

Nasal spray (Opvee): 2.7 mg/device
Solution for injection (single-dose autoinjectors) (Zurnai): 1.5 mg/0.5 mL

Route/Dosage ⬆ ⬇

IM SC (Adults and Children ≥12 yr): 1.5 mg as single dose; if desired response not achieved, may repeat dose every 2–5 min.
(Adults and Children ≥12 yr): One spray (2.7 mg) in one nostril; if desired response not achieved, may repeat dose every 2–5 min.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Competitively blocks the effects of opioid analgesics, including CNS and respiratory depression, without producing any agonist (opioid-like) effects.

Therapeutic effects:

Reversal of signs of opioid excess.

Classifications ⬆ ⬇

Therapeutic Classification: antidotes

Pharmacologic Classification: opioid antagonists

Pharmacokinetics ⬆ ⬇

Absorption: 82% absorbed following intranasal administration; extent of absorption following IM or SUBQ administration unknown.

Distribution: Rapidly and widely distributed to tissues.

Metabolism/Excretion: Primarily metabolized by the liver via glucuronide conjugation; <5% excreted unchanged in urine, 17% in feces. Undergoes enterohepatic recycling.

Half-Life: Intramuscular: 9 hr; Intranasal: 11.4 hr.

Time/Action Profile ⬆ ⬇

(reversal of opioid effects)

ROUTE	ONSET	PEAK	DURATION
IM, SUBQ	mins	2.5–5 min	5–15 min
Intranasal	mins	5–15 min	unknown

Patient/Family Teaching ⬆ ⬇

Explain to family and patient the rationale for use and to take only as directed. Advise to read Instructions for Use at the time of prescription.
Instruct patient and caregivers in the correct technique for use and disposal of provided device.
Advise caregiver to use as quickly as possible, always seek emergency medical care after first dose, and monitor the patient continuously.

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Indications ⬇