Naloxone Hydrochloride

Naloxone, sold under the brandname Narcan among others, is a medication used to block the effects of opioids, especially in overdose. Naloxone may be combined with an opioid (in the same pill) to decrease the risk of opioid misuse. When given intravenously, naloxone works within two minutes, and when injected into a muscle, it works within five minutes; it may also be sprayed into the nose. The effects of naloxone last about half an hour to an hour. Multiple doses may be required, as the duration of action of most opioids is greater than that of naloxone.Naloxone is useful both in acute opioid overdose and in reducing respiratory or mental depression due to opioids. Whether it is useful in those in cardiac arrest due to an opioid overdose is unclear.Naloxone is pregnancy category B or C in the United States. Studies in rodents given a daily maximum dose of 10 mg naloxone showed no harmful effects to the fetus, although human studies are lacking and the drug does cross the placenta, which may lead to the precipitation of withdrawal in the fetus. In this setting, further research is needed before safety can be assured, so naloxone should be used during pregnancy only if it is a medical necessity.Naloxone has little to no effect if opioids are not present. In people with opioids in their system, it may cause increased sweating, nausea, restlessness, trembling, vomiting, flushing, and headache, and has in rare cases been associated with heart rhythm changes, seizures, and pulmonary edema.Naloxone is a lipophilic compound that acts as a non-selective and competitive opioid receptor antagonist. The pharmacologically active isomer of naloxone is (−)-naloxone. Naloxone's binding affinity is highest for the μ-opioid receptor, then the δ-opioid receptor, and lowest for the κ-opioid receptor; naloxone has negligible affinity for the nociceptin receptor.Naloxone, also known as N-allylnoroxymorphone or as 17-allyl-4,5α-epoxy-3,14-dihydroxymorphinan-6-one, is a synthetic morphinan derivative and was derived from oxymorphone (14-hydroxydihydromorphinone), an opioid analgesic. Oxymorphone, in turn, was derived from morphine, an opioid analgesic and naturally occurring constituent of the opium poppy. Naloxone is a racemic mixture of two enantiomers, (–)-naloxone (levonaloxone) and (+)-naloxone (dextronaloxone), only the former of which is active at opioid receptors. The drug is a highly lipophilic, allowing it to rapidly penetrate the brain and to achieve a far greater brain to serum ratio than that of morphine. Opioid antagonists related to naloxone include cyprodime, nalmefene, nalodeine, naloxol, and naltrexone.Naloxone was patented in 1961 by Mozes J. Lewenstein, Jack Fishman, and the company Sankyo. It was approved for opioid abuse treatment in 1971 by the FDA with opioid abuse kits being distributed by many states to medically untrained people beginning in 1996. From the period of 1996 to 2014, the CDC estimates over 26,000 cases of opioid overdose have been reversed using the kits.Naloxone is the generic name of the drug and its INN, BAN, DCF, DCIT, and JAN, while naloxone hydrochloride is its USAN and BANM.