Phenadoxone
Phenadoxone
Phenadoxone is a synthetic opioid analgesic that is used in the management of moderate to severe pain. It is chemically related to methadone and shares many of its pharmacological properties. Phenadoxone is known for its long duration of action and is used in some countries as an alternative to other opioids for pain management.
Pharmacology
Phenadoxone acts primarily as an agonist at the mu-opioid receptor, which is responsible for its analgesic effects. Like other opioids, it can produce effects such as euphoria, sedation, and respiratory depression. The drug is metabolized in the liver and excreted primarily in the urine.
Mechanism of Action
Phenadoxone binds to the mu-opioid receptors in the central nervous system, mimicking the effects of endogenous endorphins. This binding inhibits the release of neurotransmitters such as substance P and glutamate, which are involved in the transmission of pain signals.
Clinical Use
Phenadoxone is used in the treatment of chronic pain conditions where other analgesics may not be effective. It is also used in some cases for opioid substitution therapy, although this is less common compared to methadone or buprenorphine.
Side Effects
Common side effects of phenadoxone include nausea, vomiting, constipation, and drowsiness. More serious side effects can include respiratory depression, hypotension, and bradycardia.
Legal Status
The legal status of phenadoxone varies by country. In some regions, it is classified as a controlled substance due to its potential for abuse and dependence.
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Contributors: Prab R. Tumpati, MD