NALORPHINE

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Created Aug 2020

NALORPHINE

  • [NALLINE]
  • [LETHIDRONE]

N-allylnormorphine

DEA CODE 9400: Schedule 3 Narcotic

Nalorphine has a mixed opioid agonist-antagonist properties. Nalorphine inhibits the cholinesterases of mouse brain, bovine erythrocytes and horse serum. It acts on mu-, k- and sigma-opioid receptors. Nalorfin by virtue of the agonistic effect has an analgesic effect but to a much lesser extent than morphine. Initially, before the appearance of a "pure" morphine-naloxone antagonist, nalorphine was used as an antidote for severe respiratory depression and other body function disorders caused by acute poisoning in case of an overdose of morphine, promedol, fentanyl or other narcotic analgesics, or with increased sensitivity to them. At present, nalorphine is practically not used for this purpose. It was replaced by naloxone. Large doses of nalorphine can cause nausea, cramps, drowsiness, headache, mental stimulation.

Nalorphine and Pregnancy:
USFDA pregnancy category D. Nalorphine can harm the unborn fetus. Perform pregnancy tests before using Nalorphine. Use effective contraceptive mode to prevent unintended pregnancies while taking Nalorphine

Nalorphine and Lactation:
Nursing mothers should consult the healthcare provider before Nalorphine treatment.

Nalorphine and Children:
Nalorphine is contraindicated in children

Abandoned Drug:
It was introduced in 1954 and was used as an antidote to reverse opioid overdose and in a challenge test to determine opioid dependence. Nalorphine was the second opioid antagonist to be introduced, preceded by nalodeine (N-allylnorcodeine) in 1915 and followed by naloxone in 1960 and naltrexone in 1963. Due to potent activation of the KOR, nalorphine produces side effects such as dysphoria, anxiety, confusion, and hallucinations, and for this reason, is no longer used medically.

  
Office-Based Treatment of Opiate Addiction with a Sublingual-Tablet Formulation of Buprenorphine and Naloxone - currently Reckitt Benckiser Pharmaceuticals) and the National Institute on Drug Abuse, National Institutes of Health. The data were held by the National Institute on Drug Abuse; Reckitt and Colman ...
Wednesday January 31, 2024 - nejm.org

  
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