Ethoheptazine

Ethoheptazine[1] (trade name Zactane) is an opioid analgesic from the phenazepane family. It was invented in the 1950s[2] and is related to other drugs such as proheptazine and pethidine.[3]

Ethoheptazine
Clinical data
Trade namesEquagesic
Other namesZactane
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.000.917
Chemical and physical data
FormulaC16H23NO2
Molar mass261.365 g·mol−1
3D model (JSmol)
 NY (what is this?)  (verify)

Ethoheptazine produces similar effects to other opioids, including analgesia, sedation, dizziness and nausea.[4] It was sold by itself as Zactane, and is still available as a combination product with acetylsalicylic acid and meprobamate as Equagesic, which is used for the treatment of conditions where both pain and anxiety are present.[5] It was also investigated for use as an antitussive.[6]

It is no longer prescribed, as it is no longer FDA approved, and not available for United States' Pharmacy Processing. Revocation of FDA Approved Medications Status stems from a combination of efficacy vs. toxicity, and the more-varied and historically safer Benzodiazepines Class. Only reversal of the FDA's decision, allows removing the drug from the CSD. Ethoheptazine is not listed as a controlled substance under the Controlled Substances Act, 1970 in the United States.[7] The controlled status (Schedule IV) of Equagesic was due to the meprobamate content.[8][7] Regulation elsewhere varies.

References
  1. ES 310184, "Procedure for the preparation of a new derivative of pirazolidine-hexametilenimina with therapeutic properties."
  2. Batterman RC, Golbey M, Grossman AJ, Leifer P (October 1957). "Analgesic effectiveness of orally administered ethoheptazine in man". The American Journal of the Medical Sciences. 234 (4): 413–9. doi:10.1097/00000441-195710000-00004. PMID 13469802. S2CID 32299049.
  3. Diamond J, Bruce WF, Tyson FT (January 1964). "Synthesis and Properties of the Analgesic DL-α-1,3-dimethyl-4-phenyl-4-propionoxyazacycloheptane (Proheptazine)". Journal of Medicinal Chemistry. 7: 57–60. doi:10.1021/jm00331a013. PMID 14186026.
  4. Cinelli P, Zucchini M (March 1962). "[Current pharmaco-therapeutic possiblities in the treatment of pain. Experiments with ethoeptazine]". Minerva Medica (in Italian). 53: 637–42. PMID 13879557.
  5. Scheiner JJ, Richards DJ (September 1974). "Treatment of musculoskeletal pain and associated anxiety with an ethoheptazine-aspirin-meprobamate combination (equagesic): a controlled study". Current Therapeutic Research, Clinical and Experimental. 16 (9): 928–36. PMID 4214668.
  6. Overton DA, Batta SK (November 1979). "Investigation of narcotics and antitussives using drug discrimination techniques". The Journal of Pharmacology and Experimental Therapeutics. 211 (2): 401–8. PMID 41087.
  7. "Conversion Factors for Controlled Substances". Diversion Control Division. Drug Enforcement Agency, U.S. Department of Justice.
  8. PDR 1978, pp 1618


This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.