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Talk:Clozapine: Difference between revisions
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Clozapine is classified as and was the first atypical antipsychotic agent. It binds to several types of central nervous system receptors and displays a unique pharmacological profile. It is a [[serotonin]] antagonist, with strong binding to the 5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> receptor subtypes. Clozapine has clinically significant anticholinergic activity, and this activity may make clozapine one of the few, if any other antipsychotic agents to have very low induction rates of tardive dyskinesia.<ref>Lieberman, J., Johns, C., Cooper, T., Pollack, S., & Kane, J. (1989). Clozapine pharmacology and tardive dyskinesia. Psychopharmacology, 99(1), S54-S59.</ref> | Clozapine is classified as and was the first atypical [[antipsychotic]] agent. It binds to several types of central nervous system receptors and displays a unique pharmacological profile. It is a [[serotonin]] [[antagonist]], with strong binding to the 5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> [[receptor]] subtypes.<ref name="Clozapine">Clozapine (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/mesh/68003024</ref> Clozapine has clinically significant anticholinergic activity, and this activity may make clozapine one of the few, if any other antipsychotic agents to have very low induction rates of tardive dyskinesia.<ref>Lieberman, J., Johns, C., Cooper, T., Pollack, S., & Kane, J. (1989). Clozapine pharmacology and tardive dyskinesia. Psychopharmacology, 99(1), S54-S59.</ref> | ||
It also displays a strong affinity as an antagonist to several [[dopamine|dopaminergic]] receptors, but shows only weak antagonism at the dopamine D2 receptor, which is commonly thought to modulate neuroleptic activity. | It also displays a strong affinity as an [[antagonist]] to several [[dopamine|dopaminergic]] receptors, but shows only weak antagonism at the [[dopamine]] D2 [[receptor]], which is commonly thought to modulate neuroleptic activity.<ref name="Clozapine"/> | ||
[https://en.wikipedia.org/wiki/Agranulocytosis Agranulocytosis] (severely low white blood cell count) is a major adverse effect associated with the administration of this agent.<ref>Baldessarini, R. J., & Frankenburg, F. R. (1991). Clozapine: a novel antipsychotic agent. New England Journal of Medicine, 324(11), 746-754.</ref><ref>Smits, R. A., Lim, H. D., Stegink, B., Bakker, R. A., de Esch, I. J., & Leurs, R. (2006). Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives. Journal of medicinal chemistry, 49(15), 4512-4516.</ref> | [https://en.wikipedia.org/wiki/Agranulocytosis Agranulocytosis] (severely low white blood cell count) is a major adverse effect associated with the administration of this agent.<ref>Baldessarini, R. J., & Frankenburg, F. R. (1991). Clozapine: a novel antipsychotic agent. New England Journal of Medicine, 324(11), 746-754.</ref><ref>Smits, R. A., Lim, H. D., Stegink, B., Bakker, R. A., de Esch, I. J., & Leurs, R. (2006). Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives. Journal of medicinal chemistry, 49(15), 4512-4516.</ref> | ||