naloxone intranasal (Rx)

Brand and Other Names:Narcan Nasal Spray
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

intranasal solution

  • 4mg/actuation

Opioid Overdose

Indicated for emergency treatment of known or suspected opioid overdose, as manifested by respiratory and/or CNS depression

Note: Also see Administration section

Initial dosing: 1 spray delivered by intranasal administration; delivers 4 mg of naloxone HCl

Repeat dosing

  • Seek emergency medical assistance as soon as possible after administering the first dose
  • The requirement for repeat doses depends on the amount, type, and route of administration of the opioid being antagonized
  • Administer in alternate nostrils with each dose
  • If the 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 the patient
  • If the desired response is not obtained after 2-3 minutes, administer an additional dose using a new spray
  • If there is 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
  • Additional supportive and/or resuscitative measures may be helpful 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

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

Not a substitute for emergency medical care

Dosage Forms & Strengths

intranasal solution

  • 4mg/actuation

Opioid Overdose

Indicated for emergency treatment of known or suspected opioid overdose, as manifested by respiratory and/or CNS depression

Note: Also see Administration section

Initial dosing: 1 spray delivered by intranasal administration; delivers 4 mg of naloxone HCl

Repeat dosing

  • Seek emergency medical assistance as soon as possible after administering the first dose
  • The requirement for repeat doses depends on the amount, type, and route of administration of the opioid being antagonized
  • Administer in alternate nostrils with each dose
  • If the 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 the patient
  • If the desired response is not obtained after 2-3 minutes, administer an additional dose using a new spray
  • If there is 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
  • Additional supportive and/or resuscitative measures may be helpful 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

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

Not a substitute for emergency medical care

Precipitation of withdrawal in neonates

  • There may be clinical settings, particularly the postpartum period in neonates with known or suspected exposure to maternal opioid use, where it is preferable to avoid the abrupt precipitation of opioid withdrawal symptoms; in these settings, consider use of an alternative naloxone-containing product that can be titrated to effect and, where applicable, dosed according to weight

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

Precipitation of severe opioid withdrawal

Increased blood pressure

Musculoskeletal pain

Headache

Nasal dryness

Nasal edema

Nasal congestion

Nasal inflammation

Postmarketing Reports

Aggressive behavior upon abrupt reversal of an opioid overdose

Constipation

Toothache

Muscle spasms

Rhinalgia

Xeroderma

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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 (see Dosing and Administration sections)

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 (see Dosage Modifications)

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; death, coma, and encephalopathy have been reported as sequelae of these events; these events have primarily occurred in patients who had preexisting cardiovascular disorders or received other drugs that may have similar adverse cardiovascular effects
  • There may be clinical settings, particularly the postpartum period in neonates with known or suspected exposure to maternal opioid use, where it is preferable to avoid the abrupt precipitation of opioid withdrawal symptoms; in these settings, consider use of an alternative naloxone-containing product that can be titrated to effect and, where applicable, dosed according to weight
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Pregnancy

Pregnancy

The limited available data on naloxone use in pregnant women are not sufficient to inform a drug-associated risk regarding teratogenicity

Fetal/neonatal adverse reactions

  • Naloxone crosses the placenta and may precipitate withdrawal in the fetus, as well as in the opioid-dependent mother
  • The fetus should be evaluated 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

Naloxone is minimally orally bioavailable

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: 0.33-0.5 hr

Peak plasma concentration: 4.83-9.7 ng/mL

AUC: 7.87-15.3 hr·ng/mL

Distribution

Protein bound: Occurs, but is relatively weak; plasma albumin is the major binding constituent, but significant binding of naloxone also occurs to plasma constituents other than albumin

Metabolism

Metabolized in the liver, primarily by glucuronide conjugation

Metabolites: Naloxone-3-glucoronide

Elimination

Half-life: ~2 hr

Excretion in urine

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

Intranasal Administration

Because treatment of suspected opioid overdose must be performed by someone other than the patient, instruct the prescription recipient to inform those around him or her about the presence of naloxone intranasal and the Instructions for Use

Instruct the patient or caregiver to read the Instructions for Use at the time they receive a prescription for naloxone intranasal

Emphasize the following instructions

  • Administer as quickly as possible because prolonged respiratory depression may result in damage to the CNS or death
  • 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 doses of naloxone intranasal, as necessary
  • Always seek emergency medical assistance in the event of a suspected, potentially life-threatening opioid emergency after administration of the first dose of naloxone intranasal
  • Additional doses may be required until emergency medical assistance becomes available
  • 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
  • Administer according to the printed instructions on the device label and the Instructions for Use
  • Place the patient in the supine position
  • Prior to administration, be sure the device nozzle is inserted in either nostril of the patient, and provide support to the back of the neck to allow the head to tilt back
  • Do not prime or test the device prior to administration
  • To administer the dose, press firmly on the device plunger
  • Remove the device nozzle from the nostril after use
  • Turn patient on his or her side as shown in the Instructions for Use and call for emergency medical assistance immediately after administration of the first dose

Storage

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

Do not freeze

Protect from light

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Formulary

FormularyPatient Discounts

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

To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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.
  • Access your plan list on any device – mobile or desktop.

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.