Desmetramadol

Desmetramadol (also known as O-Desmethyltramadol, O-DSMT, or 1-(3-methoxyphenyl)cyclohexanol) is an opioid analgesic and the main active metabolite of tramadol. It is significantly more potent than its parent compound, making it a key player in tramadol's analgesia.

Pharmacology

Desmetramadol is a mu-opioid receptor agonist, meaning it binds to and activates these receptors in the brain to produce its analgesic effects. It is also a weak norepinephrine and serotonin reuptake inhibitor, which may contribute to its analgesic and mood-altering effects.

Metabolism

Desmetramadol is formed from tramadol in the liver via the cytochrome P450 enzyme system, specifically the CYP2D6 enzyme. This process, known as O-demethylation, removes a methyl group from tramadol, transforming it into desmetramadol.

Clinical Use

Desmetramadol is not typically used directly in clinical practice, but its formation in the body is crucial for the effectiveness of tramadol. Some individuals, known as "poor metabolizers," have a less active form of the CYP2D6 enzyme and may not experience the full analgesic effects of tramadol due to reduced formation of desmetramadol.

Side Effects

As an opioid, desmetramadol can cause a range of side effects, including nausea, vomiting, constipation, drowsiness, and respiratory depression. It also carries a risk of dependence and withdrawal if used for extended periods.

See Also

• Tramadol
• Opioid
• Analgesic
• Cytochrome P450