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Action/Kinetics:
Combines competitively with opiate receptors and blocks or reverses the action of narcotic analgesics. Since the duration of action of naloxone is shorter than that of the narcotic analgesics, the respiratory depression may return when the narcotic antagonist has worn off.
Onset: IV, 2 min;
SC, IM: <5 min.
Time to peak effect: 5-15 min.
Duration: Dependent on dose and route of administration but may be as short as 45 min.
t
1/2: 60-100 min. Metabolized in the liver to inactive products; eliminated through the kidneys.
Uses:
Respiratory depression induced by natural and synthetic narcotics, including butorphanol, methadone, nalbuphine, pentazocine, and propoxyphene. Drug of choice when nature of depressant drug is not known. Diagnosis of acute opiate overdosage. Not effective when respiratory depression is induced by hypnotics, sedatives, or anesthetics and other nonnarcotic CNS depressants. Adjunct to increase BP in septic shock.
Investigational: Treatment of Alzheimer's dementia, alcoholic coma, and schizophrenia.
Contraindications:
Sensitivity to drug. Narcotic addicts (drug may cause severe withdrawal symptoms). Use in neonates.
Special Concerns:
Safe use during lactation and in children is not established.
Side Effects:
N&V;, sweating, hypertension, tremors, sweating due to reversal of narcotic depression. If used postoperatively, excessive doses may cause
VT and fibrillation hypo- or hypertension, pulmonary edema, and
seizures (infrequent).
How Supplied:
Injection: 0.02 mg/mL, 0.4 mg/mL
Dosage
?IV, IM, SC
Narcotic overdose.
Initial: 0.4-2 mg IV; if necessary, additional IV doses may be repeated at 2- to 3-min intervals. If no response after 10 mg, reevaluate diagnosis.
Pediatric, initial: 0.01 mg/kg IV;
then, 0.1 mg/kg IV, if needed. The SC or IM route may be used if an IV route is not available.
To reverse postoperative narcotic depression.
Adults: IV, initial, 0.1- to 0.2-mg increments at 2- to 3-min intervals;
then, repeat at 1- to 2-hr intervals if necessary. Supplemental IM dosage increases the duration of reversal.
Children: Initial 0.005-0.01 mg IV at 2- to 3-min intervals until desired response is obtained.
Reverse narcotic-induced depression in neonates.
Initial: 0.01 mg/kg IV, IM, or SC. May be repeated using adult administration guidelines.
