Lefetamine Explained

Lefetamine (Santenol) is a drug which is a stimulant and also an analgesic with effects comparable to codeine.

Discovery

Lefetamine-related 1,2-diphenylethylamines were invented in the 1940s and showed weak analgesic activity.[1]

It was investigated in Japan in the 1950s.[2] The L-isomer showed weak analgesic action comparable to codeine and antitussive action far weaker than codeine. The d-isomer showed no such activity but caused seizures in rats.[3] [4]

Society and culture

It was abused in Japan during the 1950s. In a small study in 1989 it showed some effect against opioid withdrawal symptoms without causing withdrawal symptoms itself. It was concluded that it may be an opioid partial agonist.[5]

It has been abused in Europe; in 1989 a small study of 15 abusers and some volunteers found that it had some partial similarity to opioids, that it produced withdrawal symptoms, and had dependence and abuse potential to a certain degree.[6]

In a small study in 1994, it was compared to clonidine and buprenorphine in the detoxification of methadone patients and found to be inferior to both of them.[7]

Regulation may vary; it does not appear as either a narcotic or non-narcotic under the US Controlled Substances Act 1970 [8]

The Canadian Controlled Drugs and Substances Act was amended in 2016 to include the substance as a Schedule III substance. Possession without legal authority can result in maximum 3 years imprisonment. Further, Health Canada amended the Food and Drug Regulations in May, 2016 to classify Lefetamine as a controlled drug.[9]

Research

Some related pyrrylphenylethanones had analgesic activity comparable to morphine.[10] Some pyrrole analogues were reported to have analgesic effects comparable to lefetamine and being devoid of neurotoxic properties.[11]

See also

Notes and References

  1. Dodds EC, Lawson W, Simpson SA, Williams PC . Testing diphenylethylamine compounds for analgesic action . The Journal of Physiology . 104 . 1 . 47–51 . June 1945 . 16991666 . 1393527 . 10.1113/jphysiol.1945.sp004105 .
  2. DE . patent . 1159958 . Verfahren zur Herstellung von antitussiv wirksamem l-1,2-Diphenyl-1-dimethylaminoaethan und dessen Salzen . 1963-12-27 . Ogyu K, Fujimura H, Yamakawa Y, Mita I . Institut Seikatsu Kagaku Kenkyusho (Scientific Research Institute for Practical Life, Kyoto) .
  3. Fujimura H, Kawai K . Pharmacological Studies on Diphenylalkylamine Derivatives. (I) . Bulletin of the Institute for Chemical Research, Kyoto University . 1961 . 39 . 1 . 67–77 . 2011-09-25 . 2012-05-01 . https://web.archive.org/web/20120501003845/http://repository.kulib.kyoto-u.ac.jp/dspace/bitstream/2433/75783/1/chd039_1_067.pdf . live .
  4. Fujimura H, Kawai K, Ohata K, Shibata S . Pharmacological Studies on Diphenylalkylamine Derivatives. (II): On the Actions of l-1,2-Diphenyl-1-dimethylaminoethane Hydrochloride (SPA) . Bulletin of the Institute for Chemical Research, Kyoto University . 1961 . 39 . 1 . 78–94 . 2012-06-30 . 2016-03-04 . https://web.archive.org/web/20160304023829/http://repository.kulib.kyoto-u.ac.jp/dspace/bitstream/2433/75782/1/chd039_1_078.pdf . live .
  5. Mannelli P, Janiri L, De Marinis M, Tempesta E . Lefetamine: new abuse of an old drug--clinical evaluation of opioid activity . Drug and Alcohol Dependence . 24 . 2 . 95–101 . October 1989 . 2571492 . 10.1016/0376-8716(89)90071-9 .
  6. Janiri L, Mannelli P, Pirrongelli C, Lo Monaco M, Tempesta E . Lephetamine abuse and dependence: clinical effects and withdrawal syndrome . British Journal of Addiction . 84 . 1 . 89–95 . January 1989 . 2917208 . 10.1111/j.1360-0443.1989.tb00555.x .
  7. Janiri L, Mannelli P, Persico AM, Serretti A, Tempesta E . Opiate detoxification of methadone maintenance patients using lefetamine, clonidine and buprenorphine . Drug and Alcohol Dependence . 36 . 2 . 139–45 . October 1994 . 7851281 . 10.1016/0376-8716(94)90096-5 .
  8. Web site: DEA Diversion Control Division . 2016-02-27 . 2016-03-02 . https://web.archive.org/web/20160302162948/http://deadiversion.usdoj.gov/quotas/conv_factor/index.html . live .
  9. Web site: Regulations Amending the Food and Drug Regulations (Parts G and J — Lefetamine, AH-7921, MT-45 and W-18) . June 2016 . 2016-11-17 . 2017-12-02 . https://web.archive.org/web/20171202203151/http://www.gazette.gc.ca/rp-pr/p2/2016/2016-06-01/html/sor-dors106-eng.php . live .
  10. Massa S, Di Santo R, Mai A, Artico M, Pantaleoni GC, Giorgi R, Coppolino MF . Pyrrylphenylethanones related to cathinone and lefetamine: synthesis and pharmacological activities . Archiv der Pharmazie . 325 . 7 . 403–9 . July 1992 . 1417455 . 10.1002/ardp.19923250707 . 22300931 .
  11. Massa S, Stefancich G, Artico M, Corelli F, Silvestri R, Pantaleoni GC, Fanini D, Palumbo G, Giorgi R . 6 . Synthesis, neuropsychopharmacological effects and analgesic-antiinflammatory activities of pyrrole analogues of lefetamine . Farmaco . 44 . 9 . 763–77 . September 1989 . 2604832 . Societa Chimica Italiana .

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