naloxone intranasal (Rx)

Brand and Other Names:Narcan Nasal Spray, Kloxxado
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

intranasal solution (Narcan)

  • 2mg/actuation (equivalent to 1.8 mg naloxone)
  • 4mg/actuation (equivalent to 3.6 mg naloxone)

intranasal solution (Kloxxado)

  • 8mg/actuation (equivalent to 7.2 mg naloxone)

Opioid Overdose

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

Intended for immediate use as emergency therapy in settings where opioids may be present

Initial dosing

  • Narcan: 1 spray delivered by intranasal administration into 1 nostril; delivers 4 mg of naloxone HCl
  • Kloxxado: 1 spray delivered by intranasal administration into 1 nostril; delivers 8 mg of naloxone HCl

Repeat dosing

  • Seek emergency medical assistance as soon as possible after administering the first dose
  • Requirement for repeat doses depends on amount, type, and route of administration of opioid being antagonized
  • Administer in alternate nostrils with each doseDesired response is not obtained after 2-3 minutes: Administer additional dose using a new spray
  • Still no response and additional doses are available: Administer additional doses every 2-3 minutes using a new spray with each dose until emergency medical assistance arrives
  • If patient responds and relapses back into respiratory depression before emergency assistance arrives, administer an additional dose of naloxone intranasal using a new spray and continue surveillance of patient
  • Consider additional supportive and/or resuscitative measures while awaiting emergency medical assistance

Dosage Modifications

Partial opioid agonists or mixed agonist/antagonists

  • Reversal of respiratory depression by partial agonists or mixed agonist/antagonists (eg, buprenorphine, pentazocine) may be incomplete and require higher doses of naloxone or repeated administration

Dosing Considerations

Not a substitute for emergency medical care

Limitation of use

  • Restrict 2-mg dose to opioid-dependent patients expected to be at risk for severe opioid withdrawal in situations where there is a low-risk for accidental or intentional opioid exposure by household contacts

Dosage Forms & Strengths

intranasal solution (Narcan)

  • 2mg/actuation (equivalent to 1.8 mg naloxone)
  • 4mg/actuation (equivalent to 3.6 mg naloxone)

intranasal solution (Kloxxado)

  • 8mg/actuation (equivalent to 7.2 mg naloxone)

Opioid Overdose

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

Intended for immediate use as emergency therapy in settings where opioids may be present

Initial dosing

  • Narcan: 1 spray delivered by intranasal administration into 1 nostril; delivers 4 mg of naloxone HCl
  • Kloxxado: 1 spray delivered by intranasal administration into 1 nostril; delivers 8 mg of naloxone HCl

Repeat dosing

  • Seek emergency medical assistance as soon as possible after administering the first dose
  • Requirement for repeat doses depends on amount, type, and route of administration of opioid being antagonized
  • Administer in alternate nostrils with each dose
  • Desired response is not obtained after 2-3 minutes: Administer additional dose using a new spray
  • Still no response and additional doses are available: Administer additional doses every 2-3 minutes using a new spray with each dose until emergency medical assistance arrives
  • If patient responds and relapses back into respiratory depression before emergency assistance arrives, administer an additional dose of naloxone intranasal using a new spray and continue surveillance of patient
  • Consider additional supportive and/or resuscitative measures while awaiting emergency medical assistance

Dosage Modifications

Partial opioid agonists or mixed agonist/antagonists

  • Reversal of respiratory depression by partial agonists or mixed agonist/antagonists (eg, buprenorphine, pentazocine) may be incomplete and require higher doses of naloxone or repeated administration

Dosing Considerations

Not a substitute for emergency medical care

Limitation of use

  • Restrict 2-mg dose to opioid-dependent patients expected to be at risk for severe opioid withdrawal in situations where there is a low-risk for accidental or intentional opioid exposure by household contacts

Geriatric patients have a greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy; therefore, the systemic exposure of naloxone can be higher in these patients

See Adult Dosing

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Adverse Effects

Frequency Not Defined

Narcan

  • Precipitation of severe opioid withdrawal
  • Increased blood pressure
  • Musculoskeletal pain
  • Headache
  • Nasal dryness
  • Nasal edema
  • Nasal congestion
  • Nasal inflammation

Kloxxado

  • Abdominal pain
  • Asthenia
  • Dizziness
  • Headache
  • Nasal discomfort
  • Presyncope
  • Nasal irritation
  • Signs of nasal inflammation
  • Nasal congestion

Postmarketing Reports

Narcan

  • Aggressive behavior upon abrupt reversal of an opioid overdose
  • Constipation
  • Toothache
  • Muscle spasms
  • Rhinalgia
  • Xeroderma

Kloxxado

  • Hypotension
  • Hypertension
  • Ventricular tachycardia and fibrillation
  • Dyspnea
  • Pulmonary edema
  • Cardiac arrest
  • Death
  • Coma
  • Encephalopathy
  • Agitation

All routes of administration

  • Withdrawal syndrome
  • Vomiting
  • Nonresponsive to stimuli
  • Drug ineffective
  • Agitation
  • Somnolence
  • Loss of consciousness
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Warnings

Contraindications

Hypersensitivity

Cautions

Risk of recurrent respiratory and CNS depression

  • There is limited data to inform if 2 mg dose will avoid precipitation of severe opioid withdrawal in setting of opioid dependence; however, the 2 mg dose may not provide adequate and timely reversal in persons who may be exposed to overdose of potent or very high dose of opioids
  • Risk of recurrent respiratory and CNS depression exists because the duration of action of most opioids may exceed that of naloxone nasal spray
  • Seek immediate emergency medical assistance following the first dose
  • Administer additional doses and additional supportive and/or resuscitative measures while waiting for help

Reversing partial opioid agonists or mixed opioid agonist/antagonists

  • Incomplete reversal of respiratory depression may be observed when attempting to reverse partial opioid agonists or mixed opioid agonist/antagonists
  • Larger or repeat doses may be required to antagonize buprenorphine because the latter has a long duration of action owing to its slow rate of binding and subsequent slow dissociation from the opioid receptor

Precipitation of severe opioid withdrawal

  • Use in patients who are opioid dependent may precipitate opioid withdrawal 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 increased blood pressure
  • In neonates, opioid withdrawal may be life-threatening if not recognized and properly treated and may include convulsions, excessive crying, and hyperactive reflexes
  • Abrupt postoperative reversal of opioid depression may result in nausea, vomiting, sweating, tremulousness, tachycardia, hypotension, hypertension, seizures, ventricular tachycardia and fibrillation, pulmonary edema, and cardiac arrest; these events have primarily occurred in patients who had preexisting cardiovascular disorders or received other drugs that may have similar adverse cardiovascular effects
  • Consider avoiding use in certain clinical settings (eg, postpartum period in neonates with known or suspected exposure to maternal opioid use) and using an alternant naloxone-containing product that can titrate to effect
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Pregnancy

Pregnancy

Limited available data are insufficient on use in pregnant females to inform a drug-associated risk regarding teratogenicity

Fetal/neonatal adverse reactions

  • Crosses the placenta and may precipitate withdrawal in the fetus, as well as in the opioid-dependent mother
  • Evaluate fetus for signs of distress after naloxone is used
  • Careful monitoring is needed until the fetus and mother are stabilized

Animal studies

  • No embryotoxic or teratogenic effects were observed in mice and rats treated during the period of organogenesis at doses equivalent to 6-12 times a human dose of 8 mg/day

Lactation

Unknown if distributed in human breast milk

Studies in nursing mothers have shown that naloxone does not affect prolactin or oxytocin hormone levels

Minimally orally bioavailable and is unlikely to affect breastfed infants

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.

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Pharmacology

Mechanism of Action

Competitive opioid antagonist that antagonizes opioid effects by competing for the same receptor sites

It reverses the effects of opioids, including respiratory depression, sedation, and hypotension

Absorption

Peak plasma time

  • Narcan: 0.33-0.5 hr
  • Kloxxado: 0.25 hr

Peak plasma concentration

  • Narcan: 4.83-9.7 ng/mL
  • Kloxxado: 12.3-12.8 ng/mL

AUC

  • Narcan: 7.87-15.3 hr·ng/mL
  • Kloxxado: 16.7-19 hr·ng/mL

Bioavailability

  • Kloxxado: 37%

Distribution

Protein bound

  • Occurs, but is relatively weak
  • Major binding constituent: Plasma albumin, but significant binding also occurs to plasma constituents other than albumin
  • Unknown whether excreted into human milk

Metabolism

Metabolized in the liver, primarily by glucuronide conjugation

Metabolites: Naloxone-3-glucoronide

Elimination

Half-life

  • Narcan: ~2 hr
  • Kloxxado: 1.76-2.69 hr

Excretion in urine

  • 6 hr: 25-40%
  • 24 hr: 50%
  • 72 hr: 60-70 %
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Administration

Intranasal Administration

Intranasal use only

Ready for use; no additional device assembly required

Place patient in the supine position

Before administration, ensure insert device nozzle in either nostril, and provide support to back of neck to allow head to tilt back

Use each nasal spray only 1 time; do NOT test or prime before use; press firmly on device plunger to administer dose

Remove device nozzle from nostril after use

Do not attempt to reuse naloxone intranasal; each spray contains a single dose of naloxone and cannot be reused

Readminister using a new nasal spray every 2-3 minutes if the patient does not respond or responds and then relapses into respiratory depression

Administer in alternate nostrils with each dose

Turn patient on side and call for emergency medical assistance immediately after administration of first dose

Other instructions to consult patients and caregivers

  • Administer as quickly as possible because prolonged respiratory depression may result in damage to the CNS or death
  • Since duration of action of most opioids exceeds that of naloxone and suspected opioid overdose may occur outside of supervised medical settings, seek immediate emergency medical assistance, continue monitoring patient until emergency personnel arrive, and administer repeated doses of naloxone intranasal, as necessary
  • Always seek emergency medical assistance if a potentially life-threatening opioid emergency is suspected after administration of the first dose of naloxone intranasal

Storage

Protect from light

Do not freeze

Freezes at temperatures below -15ºC (5ºF); if frozen, device will not spray

If frozen and is needed in an emergency, do NOT wait to thaw; get emergency medical help right away

Narcan nasal spray

  • Store at controlled room temperature 15-25ºC (59-77ºF); excursions permitted to 4-40ºC (39-104ºF)

Kloxxado

  • Store at 20-25ºC (68-77ºF), with excursions permitted to 5-40ºC (41-104ºF)
  • Not made of rubber latex
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Images

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Formulary

FormularyPatient Discounts

Adding plans allows you to compare formulary status to other drugs in the same class.

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Adding plans allows you to:

  • View the formulary and any restrictions for each plan.
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  • Compare formulary status to other drugs in the same class.
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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.