Which is the active metabolite of ketamine?

Which is the active metabolite of ketamine?

• A. Norketamine
• B. Noradrenaline
• C. Hydroxynorketamine
• D. Desmethylketamine

Answer: (A)

Norketamine is the active metabolite formed when ketamine is demethylated in the liver by cytochrome P450 enzymes. This N-demethylation product still blocks NMDA receptors, though it is less potent than ketamine, so it helps sustain anesthesia and analgesia as the parent drug wears off. Hydroxynorketamine is a downstream metabolite with its own activity, but the primary metabolite responsible for continuing effects is norketamine. Desmethylketamine is another name sometimes used for the same compound, but the metabolite most commonly cited as the active one is norketamine.

Norketamine is the active metabolite formed when ketamine is demethylated in the liver by cytochrome P450 enzymes. This N-demethylation product still blocks NMDA receptors, though it is less potent than ketamine, so it helps sustain anesthesia and analgesia as the parent drug wears off. Hydroxynorketamine is a downstream metabolite with its own activity, but the primary metabolite responsible for continuing effects is norketamine. Desmethylketamine is another name sometimes used for the same compound, but the metabolite most commonly cited as the active one is norketamine.