Naloxone
Narcan
- Naloxone hydrochloride injection is indicated for the complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids including natural and synthetic narcotics, propoxyphene, methadone and certain narcotic-antagonist analgesics: nalbuphine, pentazocine and butorphanol. Naloxone hydrochloride is also indicated for the diagnosis of suspected acute opioid overdosage. Naloxone hydrochloride prevents or reverses the effects of opioids, including respiratory depression, sedation, and hypotension. Also, it can reverse the psychotomimetic and dysphoric effects of agonist-antagonist such as pentazocine.
- Naloxone hydrochloride is an essentially pure narcotic antagonist, i.e., it does not possess the "agonistic" or morphine-like properties characteristic of other narcotic antagonists; naloxone does not produce respiratory depression, psychotomimetic effects or pupillary constriction.
- In the absence of narcotics or agonistic effects of other narcotic antagonists naloxone exhibits essentially no pharmacologic activity.
- Naloxone has not been shown to produce tolerance or to cause physical or psychological dependence.
- In the presence of physical dependence on narcotics, naloxone will produce withdrawal symptoms.
- While the mechanism of action of naloxone is not fully understood, the preponderance of evidence suggests that naloxone antagonizes the opioid effects by competing for the same receptor sites.
- When naloxone hydrochloride is administered intravenously the onset of action is generally apparent within two minutes; the onset of action is only slightly less rapid when it is administered subcutaneously or intramuscularly.
How supplied
| |
Multiple Dose Vials
0.4 mg/mL
1 mg/mL
Preservative-Free Ampules
0.02 mg/mL
0.4 mg/mL
1 mg/mL
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10 mL multiple dose vial-box of 1
10 mL multiple dose vial-box of 1
2 mL unit dose ampule-box of 10
1 mL unit dose ampule-box of 10
2 mL unit dose ampule-box of 10
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Naloxone Dosing for Endoscopic Sedation Adult - Initial dose: 0.1-0.2 mg
- Additional doses: 0.2-0.4 mg administered intravenously every 2-3 minutes until desired response is attained. Supplemental dose may be necessary after 20-30 minutes.
- Onset of action: 1-2 minutes
- Peak effect: 5 minutes
- Duration of effect: 30-45 minutes
Pediatric* - Children: Initial dose: 1mcg/kg
- Additional doses if no response at 90 seconds: 2 – 4 mcg/kg
- Maximum dose: 400 mcg or 1 ampule
* When using naloxone hydrochloride injection in neonates a product containing 0.02 mg/ml should be used. |
Note:
- The duration of action is dependent upon the dose and route of administration of naloxone hydrochloride. Intramuscular administration produces a more prolonged effect than intravenous administration.
- The requirement for repeat doses of naloxone will also be dependent upon the amount, type and route of administration of the narcotic being antagonized.
- There is no clinical experience with naloxone hydrochloride overdosage in humans.
- Carcinogenesis and mutagenesis: Studies have not been performed with naloxone hydrochloride. Reproductive studies in mice and rats demonstrated no impairment of fertility.
- Teratogenic effects: Pregnancy Category B. Reproduction studies performed in mice and rats at doses up to 1,000 times the human dose revealed no evidence of impaired fertility or harm to the fetus due to naloxone. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, naloxone hydrochloride should be used during pregnancy only if clearly needed.
- Nursing mothers: It is not known whether naloxone is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when naloxone is administered to a nursing woman.
- Several instances of hypotension, hypertension, ventricular tachycardia and fibrillation, and pulmonary edema have been reported. These have occurred in postoperative patients, most of whom had pre-existing cardiovascular disorders or received other drugs which may have similar adverse cardiovascular effects.
- Although a direct cause-and-effect relationship has not been established, naloxone should be used with caution in patients with pre-existing cardiac disease or patients who have received potentially cardiotoxic drugs.
- Abrupt reversal of narcotic depression may result in nausea, vomiting, sweating, tachycardia, increased blood pressure, tremulousness, seizures and cardiac arrest
- In postoperative patients, larger than necessary dosage of naloxone hydrochloride may result in significant reversal of analgesia and in excitement.
- Hypotension, hypertension, ventricular tachycardia and fibrillation, and pulmonary edema have been associated with the use of naloxone hydrochloride postoperatively.
- Naloxone hydrochloride should be administered cautiously to persons including newborns of mothers who are known or suspected to be physically dependent on opioids. In such cases an abrupt and complete reversal of narcotic effects may precipitate acute withdrawal symptoms.
- The patient who has satisfactorily responded to naloxone should be kept under continued surveillance and repeated doses of naloxone should be administered, as necessary, since the duration of action of some narcotics may exceed that of naloxone.
- Naloxone is not effective against respiratory depression due to non-opioid drugs.
- Reversal of buprenorphine-induced respiratory depression may be incomplete.
- If an incomplete reversal of respiratory depression from oipioids occurs after naloxone administration, respirations should be mechanically assisted.
- Naloxone hydrochloride injection is contraindicated in patients known to be hypersensitive to it.
SourcesCohen LB, DeLegge MH, Aisenberg J, Brill JV, Inadomi JM, et al.
AGA Institute review of endoscopic sedation. Gastroenterology. 2007 Aug;133(2):675-701.
Naloxone Hydrochloride Injection, Solution [package insert]. HOSPIRA, INC. June 2006.
http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=1281 Accessed April 20, 2008.
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