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naloxone (Narcan, Evzio)

 

Classes: Opioid Reversal Agents; Opioid Antagonists

Dosing and uses of Narcan, Evzio (naloxone)

 

Adult dosage forms and strengths

injectable solution

  • 0.4mg/mL
  • 1mg/mL

IM/SC auto-injector

  • 0.4mg/0.4mL (2 auto-injectors/package)

 

Opioid Overdose

Indicated for the complete or partial reversal of opioid depression (including respiratory depression) induced by natural and synthetic opioids

0.4-4 mg IV/IM/SC; repeat q2-3min PRN; not to exceed 10 mg (0.01 mg/kg)

Consider other causes of respiratory depression if desired response not achieved after 0.8 mg totaL

Endotracheal: 2-2.5 times (0.8-1 mg) initial IV dose

For chronic opioid abuse, use smallest doses (0.1-0.2 mg) and titrate to reversal of respiratory depression

Continuous IV infusion

  • For use in patients exposed to long acting opioids (eg, methadone), sustained release products
  • Calculate dose/hr based on effective intermittent dose used and duration of adequate response seen
  • Alternatively, use two-thirds of initial effective naloxone bolus on an hourly basis (0.25-6.25 mg/hr); administer one-half of initial bolus dose 15 min after initiating continuous IV infusion to prevent drop in naloxone levels

Evzio Auto-Injector

  • Indicated for immediate administration as emergency treatment of known or suspected opioid overdose, as manifested by respiratory and/or central nervous system depression
  • 0.4 mg or 2 mg IM/SC into anterolateral aspect of the thigh (through clothing if necessary)
  • Seek emergency medical care immediately after use
  • Additional doses may be administered q2-3min until EMS arrives

Dosing considerations (Evzio)

  • Take-home, single-use auto-injector with visual and voice instruction for guidance
  • May be prescribed to a family member or caregiver
  • Compact size for portability with retractable needle system
  • Intended for immediate administration as emergency therapy in settings where opioids may be present
  • Not a substitute for emergency medical care
  • Also see Administration

 

Pediatric dosage forms and strengths

injectable solution

  • 0.4mg/mL
  • 1mg/mL

IM/SC auto-injector

  • 0.4mg/0.4mL (2 auto-injectors/package)

 

Opioid Reversal

Postanesthesia (acute) opioid reversaL

  • Neonates: 0.01 mg/kg IV into umbilical vein/IM/SC; give subsequent dose of 0.1 mg/kg if needed
  • Children: 0.01 mg/kg IV x1; may repeat with 0.1 mg/kg

Therapeutic opioid dosing

  • 0.00-0.015 mg/kg/dose IV/IM/SC/ET; may repeat PRN

Acute opioid overdose

  • ≤20 kg or <5 years: 0.1 mg/kg/dose IV/IM/SC/ET; if needed, repeat q2-3min PRN; not to exceed 2 mg/dose
  • >20 kg or ≥5 years: 2 mg IV/IM/SC/ET; if needed, repeat q2-3min PRN

 

Opioid Overdose (Evzio Auto-Injector)

Indicated for immediate administration as emergency treatment of known or suspected opioid overdose, as manifested by respiratory and/or central nervous system depression

0.4 mg or 2 mg IM/SC into anterolateral aspect of the thigh (through clothing if necessary); if child is <1 yr, pinch the thigh muscle while administering the dose

Seek emergency medical care immediately after use

Additional doses may be administered q2-3min until EMS arrives

Dosing considerations (Evzio)

  • Take-home, single-use auto-injector with visual and voice instruction for guidance
  • May be prescribed to a family member or caregiver
  • Compact size for portability with retractable needle system
  • Intended for immediate administration as emergency therapy in settings where opioids may be present
  • Not a substitute for emergency medical care
  • Also see Administration

 

Narcan, Evzio (naloxone) adverse (side) effects

Frequency not defined

Withdrawal reaction precipitated

Abrupt reversal of narcotic depression may result in nausea, vomiting, sweating, tachycardia, increased blood pressure and tremulousness

Cardiac arrest

Ventricular fibrillation

Dyspnea

Pulmonary edema

Abdominal cramps

Diarrhea

 

Warnings

Contraindications

Hypersensitivity

 

Cautions

Caution in patients with cardiovascular disease or seizures

Avoid excessive dose after use of opioids in surgery; abrupt postoperative reversal may cause nausea/vomiting, edema, tachycardia, sweating, and may unmask pain

Recurrence of respiratory depression may occur if opioid involved is long-acting or a partial agonist (eg, methadone, buprenorphine)

Opioid withdrawaL

  • Use in patients who are opioid dependent may precipitate acute abstinence syndrome
  • Syndrome characterized by body aches, diarrhea, tachycardia, fever, runny nose, sneezing, piloerection, sweating, yawning, nausea or vomiting, nervousness, restlessness, or irritability, shivering or trembling, abdominal cramps, weakness, and hypertension
  • In neonates, opioid withdrawal may be life-threatening if not recognized and properly treated and may include convulsions, excessive crying, and hyperactive reflexes

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Not known if distributed in milk; use caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Narcan, Evzio (naloxone)

Mechanism of action

Competitive opioid antagonist; synthetic congener of oxymorphone

 

Absorption

Onset: 2 min (IV); 2-5 min (IM/SC)

Duration: Depends on route of administration; generally 1-2 hr

 

Elimination

Half-life: 30-90 min (adults); 3-4 hr (neonates)

Excretion: Urine

 

Administration

IV Compatibilities

Additive: VerapamiL

Syringe: Heparin, ondansetron, dimehydrinate

Y-site: Fenoldopam, gatifloxacin, linezolid, propofoL

 

IV Incompatibilities

Syringe: Pantoprazole

Y-site: Amphotericin B cholSO4

 

IV Preparation

For infusion, dilute to 4 mcg/mL in D5W or Ns

Use within 24 hr

 

IM/SC Preparation

Before using, check to make sure the solution is not discolored

Replace if the solution is discolored or contains a precipitate

 

IM/SC Administration

For IM or SC use only

Seek emergency medical care immediately after use

Since the duration of action of most opioids exceeds that of naloxone and the suspected opioid overdose may occur outside of supervised medical settings, seek immediate emergency medical assistance, keep the patient under continued surveillance until emergency personnel arrive, and administer repeated naloxone doses as necessary

Evzio

  • Administer in anterolateral aspect of the thigh in adult and pediatric patients
  • Upon actuation, the autoinjector automatically inserts the needle IM or SC, and thereby delivers the naloxone injection, and then retracts the needle fully into its housing
  • In pediatric patients aged <1 yr, the caregiver should pinch the thigh muscle while administering the dose
  • Administer additional doses using a new auto-injector, if the patient does not respond or responds and then relapses into respiratory depression
  • Additional doses may be given q2-3min until emergency medical assistance arrive

 

Storage

Store at controlled room temperature 15-25°C (59-77°F) excursions permitted between 4-40°C (39-104°F)