Naloxone
Naloxone is a drug used to counter the effects of overdosing on opiates such as heroin or morphine. It is being offered under the trade names Narcan, Nalone, and Narcanti by DuPont Pharmaceuticals .The drug has an extremely high affinity for the opiate receptors on nerve cells in the brain, and blocks those receptors quickly, often throwing addicts into immediate withdrawal symptoms. It acts as a competitive antagonist, being structurally similar to morphine while lacking morphine-like effects.
Naloxone is injected, usually initially intravenously for fastest action. The drug acts after about two minutes, and its effects may last about 45 minutes.
Naloxone has been distributed as part of emergency kits to heroin addicts, which has been shown to reduce death rates.
The drug also blocks the action of pain-lowering endorphins which the body produces naturally. The likely reason for this is that these endorphins operate on the same opiate receptors. In one experiment, women treated with naloxone reported higher pain levels during childbirth than women not so treated; in another experiment, the pain lowering effect of placebos was blocked if the placebos were administered along with naloxone.
While Naloxone is still often used in emergency treatments for opiate overdose, its clinical use in ongoing treatment of users with opiate addiction is being increasingly superseded by Naltrexone. Naltrexone blocks a wider range of opiate receptors and blocks the receptors for a significantly longer time.
The patent for the drug has expired and naloxone is manufactured by various companies. It is derived from thebaine. The empirical formula for naloxone is C19H21NO4 and the technical name is 17-Allyl-6-deoxy-7,8-dihydro-14-hydroxy-6-oxo-17-normorphone. The CAS number of Naloxone is 465-65-6; the anhydrous hydrochloride salt has CAS 357-08-4 and the hydrochloride salt with 2 molecules of water has CAS 51481-60-8.
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