Nalmexone Explained

Nalmexone (INN; also known as nalmexone hydrochloride (USAN) or by the development codes EN-1620A and UM-592) is a semisynthetic, opioid partial agonist or mixed agonist-antagonist with both analgesic and narcotic antagonist properties that was never marketed.^{[1] [2] [3] [4]} In clinical studies it was found to have comparable analgesic efficacy to morphine, though with several-fold reduced potency.^[5] In addition, nalmexone's side effects, the most common of which were sleepiness and sweating, were reported to be similar to those of morphine, albeit with a noticeably higher degree of incidence.

Synthesis

Nalmexone can be synthesized from oxymorphone:^[6]

See also

• Nalbuphine
• Oxymorphone
• Naloxone
• Naltrexone
• Pentazocine

Notes and References

1. Book: Macdonald F . Dictionary of Pharmacological Agents . 11 May 2012 . 1997 . CRC Press . 978-0-412-46630-4 . 1395.
2. Book: Casy AF, Parfitt RT . Opioid Analgesics: Chemistry and Receptors . 11 May 2012 . 1986 . Springer . 978-0-306-42130-3 . 55.
3. Loew GH, Berkowitz DS . Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics . Journal of Medicinal Chemistry . 21 . 1 . 101–106 . 1978 . 73588 . 10.1021/jm00199a018.
4. Forrest WH, Shroff PF, Mahler DL . Analgesic and other effects of nalmexone in man . Clinical Pharmacology and Therapeutics . 13 . 4 . 520–525 . 1972 . 4557582 . 10.1002/cpt1972134520 . 30780581 .
5. Book: Committee on Problems of Drug Dependence . Bulletin, problems of drug dependence . 11 May 2012 . 1969 . National Academies . 5873 . NAP:10503.
6. Lowenstein, M. J.; Fishman, J.; 1967,