Oxymorphazone

Oxymorphazone is a potent opioid analgesic drug related to morphine. It is a selective mu-opioid receptor agonist that has a particularly long duration of action, lasting several days after a single dose. It was developed in the 1970s by a team of researchers at Hoffmann-La Roche.

Chemistry

Oxymorphazone is a derivative of morphine, being the 3,6-diacetyl derivative. It is more potent than morphine but has similar effects. Like other opioids, it is a tertiary amine. The chemical name of oxymorphazone is 3,6-diacetyloxymorphone.

Pharmacology

Oxymorphazone acts as a potent agonist at the mu-opioid receptor, which is the main site of action for the most commonly used opioids. Its long duration of action is due to its high lipophilicity, which allows it to accumulate in fatty tissues and slowly release over time.

Clinical Use

While oxymorphazone has been studied in the context of pain management, it is not currently marketed for medical use. Its long duration of action could potentially make it useful for the treatment of chronic pain conditions, but further research is needed to fully understand its efficacy and safety profile.

Side Effects

Like other opioids, oxymorphazone can cause a range of side effects, including respiratory depression, constipation, nausea, and dependence. Due to its potency and long duration of action, it also has a high potential for abuse.

See Also

• Opioid
• Morphine
• Mu-opioid receptor
• Hoffmann-La Roche