Desmethylclozapine

Desmethylclozapine (also known as N-desmethylclozapine or norclozapine) is a major metabolite of the antipsychotic drug clozapine. It is primarily produced in the liver through the enzymatic process of N-demethylation.

Pharmacology

Desmethylclozapine is an active metabolite, meaning it has its own pharmacological effects separate from those of clozapine. It acts as an antagonist at the serotonin 2A receptor (5-HT2A receptor), and as a partial agonist at the dopamine D2 receptor (D2 receptor). This combination of actions is believed to contribute to its antipsychotic effects.

Clinical significance

The levels of desmethylclozapine in the blood can be used as a marker of clozapine metabolism. This can be useful in monitoring patient compliance with medication, and in adjusting dosages to achieve optimal therapeutic effects. However, the relationship between clozapine and desmethylclozapine levels is complex, and can be influenced by a variety of factors including genetic variations in the enzymes responsible for clozapine metabolism.

Side effects

Like clozapine, desmethylclozapine can cause a range of side effects. These can include sedation, weight gain, constipation, and drooling. It can also cause more serious side effects such as agranulocytosis (a potentially life-threatening decrease in white blood cells), seizures, and myocarditis (inflammation of the heart muscle).

See also

• Clozapine
• Antipsychotic
• Metabolite
• Pharmacology