Etazocine

Etazocine

Etazocine is a benzomorphan derivative drug invented by Pfizer in the 1960s. It is most commonly classified as an opioid analgesic, but it is not a true opioid as its chemical structure is significantly different from that of opioids.

Chemistry

Etazocine is a member of the benzomorphan class of opioids. It is structurally related to morphine but its chemical structure is significantly different. The benzomorphan structure of etazocine is based on a 2-azabicyclo[2.2.2]octane nucleus. The difference between this and the structure of morphine is the replacement of the six-membered morphinan ring of morphine by a seven-membered norbornane ring.

Pharmacology

Etazocine is a potent analgesic. It acts as a partial agonist at the mu-opioid receptor and as an antagonist at the kappa-opioid receptor. This combination of actions provides analgesic activity with less risk of side effects such as respiratory depression and physical dependence that are commonly associated with full opioid agonists.

Clinical Use

Etazocine was initially developed as a potent analgesic for use in the treatment of severe pain. However, its clinical use has been limited due to its side effects, which include dysphoria, hallucinations, and severe nausea and vomiting. These side effects are thought to be due to its kappa-opioid receptor antagonist activity.

Legal Status

In the United States, etazocine is classified as a Schedule I controlled substance, meaning it has a high potential for abuse and no accepted medical use. In other countries, it may be classified differently depending on local drug laws.

See Also

• Benzomorphan
• Opioid
• Analgesic
• Mu-opioid receptor
• Kappa-opioid receptor