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Naloxone
is a drug used to counter the effects of overdosing with opioids
such as heroin and morphine. Specifically, naloxone is used in opioid
overdoses for countering life-threatening depression of the central
nervous system and respiratory system. 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 is injected, usually through intravenously
route for fastest action. The drug acts after about two minutes,
and its effects may last about 45 minutes. Naloxone has been shown
to reduce rates of fatal overdose with heroin.
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