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Naloxone
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Administration
Monitoring Parameters
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(nal OKS one)

U.S. Brand Names
Narcan® Injection

Generic Available

Yes


Synonyms
N-allylnoroxymorphine Hydrochloride; Naloxone Hydrochloride

Pharmacological Index

Antidote


Use

Dental: Reverses CNS and respiratory depressant effects of fentanyl and meperidine during I.V. conscious state

Medical:

Complete or partial reversal of opioid depression, including respiratory depression, induced by natural and synthetic opioids, including propoxyphene, methadone, and certain mixed agonist-antagonist analgesics: nalbuphine, pentazocine, and butorphanol

Diagnosis of suspected opioid tolerance or acute opioid overdose

Adjunctive agent to increase blood pressure in the management of septic shock

Unlabeled use: PCP and alcohol ingestion


Pregnancy Risk Factor

B


Contraindications

Hypersensitivity to naloxone or any component


Warnings/Precautions

Due to an association between naloxone and acute pulmonary edema, use with caution in patients with cardiovascular disease or in patients receiving medications with potential adverse cardiovascular effects (eg, hypotension, pulmonary edema or arrhythmias). Excessive dosages should be avoided after use of opiates in surgery, because naloxone may cause an increase in blood pressure and reversal of anesthesia; may precipitate withdrawal symptoms in patients addicted to opiates, including pain, hypertension, sweating, agitation, irritability; in neonates: shrill cry, failure to feed. Recurrence of respiratory depression is possible if the opioid involved is long-acting; observe patients until there is no reasonable risk of recurrent respiratory depression.


Adverse Reactions

Cardiovascular: Hypertension, hypotension, tachycardia, ventricular arrhythmias, cardiac arrest

Central nervous system: Irritability, anxiety, narcotic withdrawal, restlessness, seizures

Gastrointestinal: Nausea, vomiting, diarrhea

Neuromuscular & skeletal: Tremulousness

Respiratory: Dyspnea, pulmonary edema, runny nose, sneezing

Miscellaneous: Diaphoresis


Overdosage/Toxicology

Naloxone is the drug of choice for respiratory depression that is known or suspected to be caused by an overdose of an opiate or opioid


Drug Interactions

Decreased effect of narcotic analgesics


Stability

Protect from light; stable in 0.9% sodium chloride and D5W at 4 mcg/mL for 24 hours; do not mix with alkaline solutions


Mechanism of Action

Pure opioid antagonist that competes and displaces narcotics at opioid receptor sites


Pharmacodynamics/Kinetics

Onset of effect: Endotracheal, I.M., S.C.: Within 2-5 minutes; I.V.: Within 2 minutes

Duration: 20-60 minutes; since shorter than that of most opioids, repeated doses are usually needed

Distribution: Crosses the placenta

Metabolism: Primarily by glucuronidation in the liver

Half-life: Neonates: 1.2-3 hours; Adults: 1-1.5 hours

Elimination: In urine as metabolites


Usual Dosage

I.M., I.V. (preferred), intratracheal, S.C.:

Opiate intoxication:

Birth (including premature infants) to 5 years or <20 kg: 0.1 mg/kg; repeat every 2-3 minutes if needed; may need to repeat doses every 20-60 minutes

>5 years or greater than or equal to 20 kg: 2 mg/dose; if no response, repeat every 2-3 minutes; may need to repeat doses every 20-60 minutes

Continuous infusion: I.V.: Children and Adults: If continuous infusion is required, calculate dosage/hour based on effective intermittent dose used and duration of adequate response seen, titrate dose 0.04-0.16 mg/kg/hour for 2-5 days in children, up to 0.8 mg/kg/hour in adults; alternatively, continuous infusion utilizes 2/3 of the initial naloxone bolus on an hourly basis; add 10 times this dose to each liter of D5W and infuse at a rate of 100 mL/hour; 1/2 of the initial bolus dose should be readministered 15 minutes after initiation of the continuous infusion to prevent a drop in naloxone levels; increase infusion rate as needed to assure adequate ventilation

Narcotic overdose: Adults: I.V.: 0.4-2 mg every 2-3 minutes as needed; may need to repeat doses every 20-60 minutes, if no response is observed after 10 mg, question the diagnosis. Note: Use 0.1-0.2 mg increments in patients who are opioid dependent and in postoperative patients to avoid large cardiovascular changes.


Dietary Considerations

No data reported


Administration

Endotracheal: Dilute to 1-2 mL with normal saline

I.V. push: Administer over 30 seconds as undiluted preparation

I.V. continuous infusion: Dilute to 4 mcg/mL in D5W or normal saline


Monitoring Parameters

Respiratory rate, heart rate, blood pressure


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

If patient is responsive, instructions are individualized. This drug can only be administered I.V. Report difficulty breathing, palpitations, or tremors. Breast-feeding precautions: Breast-feeding is not recommended.


Nursing Implications

The use of neonatal naloxone (0.02 mg/mL) is no longer recommended because unacceptable fluid volumes will result, especially to small neonates; the 0.4 mg/mL preparation is available and can be accurately dosed with appropriately sized syringes (1 mL)


Dosage Forms

Injection, as hydrochloride: 0.4 mg/mL (1 mL, 2 mL, 10 mL); 1 mg/mL (2 mL, 10 mL)

Injection, neonatal, as hydrochloride: 0.02 mg/mL (2 mL)


References

American Academy of Pediatrics Committee on Drugs, "Naloxone Dosage and Route of Administration for Infants and Children: Addendum to Emergency Drug Doses for Infants and Children," Pediatrics, 1990, 86(3):484-5.

Bergasa NY, Alling DW, Talbot TL, et al, "Effects of Naloxone Infusions in Patients With the Pruritus of Cholestasis. A Double-Blind, Randomized, Controlled Trial," Ann Intern Med, 1995, 123(3):161-7.

Boeuf B, Gauvin F, Guerguerian AM, et al, "Therapy of Shock With Naloxone: A Meta-Analysis," Crit Care Med, 1998, 26(11):1910-6.

Chamberlain JM and Klein BL, "A Comprehensive Review of Naloxone for the Emergency Physician," Am J Emerg Med, 1994, 12(6):650-60.

Evans LE, Swainson CP, Roscoe P, et al, "Treatment of Drug Overdosage With Naloxone, a Specific Narcotic Antagonist," Lancet, 1973, 1(801):452-5.

Goldfrank L, Weisman RS, Errick JK, et al, "A Dosing Nomogram for Continuous Infusion Intravenous Naloxone," Ann Emerg Med, 1986, 15(5):566-70.

Hantson P, Evenepoel E, Ziade D, et al, "Adverse Cardiac Manifestations Following Dextropropoxyphene Overdose: Can Naloxone Be Helpful?" Ann Emerg Med, 1995, 25(2):263-6.

Hoffman RS and Goldfrank LR, "The Poisoned Patient With Altered Consciousness. Controversies in the Use of a 'Coma Cocktail'," JAMA, 1995, 274(7):562-9.

Johnson C, Mayer P, and Grosz D, "Pulmonary Edema Following Naloxone Administration in a Healthy Orthopedic Patient," J Clin Anesth, 1995, 7(4): 356-7.

Merigian KS, "Cocaine-Induced Ventricular Arrhythmias and Rapid Atrial Fibrillation Temporally Related to Naloxone Administration," Am J Emerg Med, 1993, 11(1):96-7.

O'Connor PG and Kosten TR, "Rapid and Ultrarapid Opioid Detoxification Techniques," JAMA, 1998, 279(3):229-34.

Olsen KS, "Naloxone Administration and Laryngospasm Followed by Pulmonary Edema," Intensive Care Med, 1990, 16(5):340-1.

Salvucci AA Jr, Eckstein M, and Iscovich AL, "Submental Injection of Naloxone," Ann Emerg Med, 1995, 25(5):719-20.

Storrow AB, Wians FH Jr, Mikkelsen SL, et al, "Does Naloxone Cause a Positive Urine Opiate Screen?" Ann Emerg Med, 1994, 24(6):1151-3.

Tandberg D and Abercrombie D, "Treatment of Heroin Overdose With Endotracheal Naloxone," Ann Emerg Med, 1982, 11(8):443-5.

Waters C, "Cognitive Enhancing Agents: Current Status in the Treatment of Alzheimer's Disease," Can J Neurol Sci, 1988, 15(3):249-56.


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