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Naloxone is a drug used to counter the effects of opioid overdose, for example heroin and morphine overdose. Specifically, naloxone is used in opioid overdoses for countering life-threatening depression of the central nervous system and respiratory system. It is marketed under trade names including Narcan, Nalone, and Narcanti and has sometimes been mistakenly called "naltrexate."
The drug is derived from thebaine and has an extremely high affinity for μ-opioid receptors in the central nervous system. Naloxone is a μ-opioid receptor competitive antagonist, and its rapid blockade of those receptors often produces rapid onset of withdrawal symptoms. Naloxone also has an antagonist action, though with a lower affinity, at κ- and δ-opioid receptors. Structurally, Naloxone can be described as a substituted oxymorphone—here the tertiary amine methyl substituent is replaced with prop-2-enyl.
Naloxone is injected, usually initially intravenously for fastest action. The drug acts after about two minutes, and its effects may last about 45 minutes. Other routes, including intramuscular injection and intranasal injection (use of a wedge device attached to the syringe to create a mist delivering the drug to the nasal mucosa) may also be utilized, although these are more likely in the prehospital setting.
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Naloxone and buprenorphine - Familydoctor.org - Information for patients in English and Spanish.
