Brands, Medical Use, Clinical Data
Drug Category
- Antinarcotic Agents
- Depressants
- Opiate Antagonists
Dosage Forms
Brands / Synonyms
EN 1530 Base; L-Naloxone; N-Allylnoroxymorphone; Nalone; Nalossone [Dcit]; Naloxona [Inn-Spanish]; Naloxone; Naloxone HCl; Naloxonum [Inn-Latin]; Narcan; Narcanti; Narcon; Narcotic Antagonist
; Pentazocine and Naloxone; Suboxone
Indications
For the complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids including natural and synthetic narcotics, propoxyphene, methadone and the narcotic-antagonist analgesics: nalbuphine, pentazocine and butorphanol.
Pharmacology
Naloxone is an opiate antagonist and prevents or reverses the effects of opioids including respiratory depression, sedation and hypotension. Also, it can reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine. Naloxone 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, it exhibits essentially no pharmacologic activity.
Mechanism of Action
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, especially the opioid mu receptor. Recently, naloxone has been shown to bind all three opioid receptors (mu, kappa and gamma) but the strongest binding is to the mu receptor.
Absorption
Well absorbed following intramuscular injection.
Toxicity
Not Available
Biotrnasformation / Drug Metabolism
Hepatic.
Contraindications
Naloxone Hydrochloride Injection is contraindicated in patients known to be hypersensitive to it.
Drug Interactions
No information provided.
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