Drug intelligence / Profile preview

ethoheptazine

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Ethoheptazine is a phenazepine-based opioid analgesic developed in the 1950s. It is structurally related to proheptazine and pethidine and was primarily used for the relief of mild to moderate pain. Ethoheptazine acts as an opioid analgesic, producing effects such as analgesia, sedation, dizziness, and nausea similar to other opioids. Its mechanism of action is believed to involve binding to mu-opioid receptor in the central nervous system. Ethoheptazine was marketed under the brand name Zactane and also available in combination with acetylsalicylic acid and meprobamate as Equagesic for conditions involving both pain and anxiety. The drug has been withdrawn from markets worldwide due to concerns over efficacy compared with toxicity and safer alternatives; it is no longer FDA approved or available in the United States[1][2][3][4][5][6][7].

Brand names
ZactaneEquagesic
Other names
ZactaneEquagesic
02

Targets

MOR (Mu opioid receptor)

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