Clozapine-induced agranulocytosis

Clozapine currently remains the gold standard for treatment-resistant schizophrenia, but only under an adequate hematological monitoring, because it is associated with agranulocytosis. Clozapine is metabolized to produce pharmacologically active N-desmethylclozapine, inactive clozapine N-oxide and r...

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Bibliographic Details
Authors: Luque Espino, Julio César, Oscanoa Espinoza, Teodoro Julio
Format: article
Status:Published version
Publication Date:2020
Country:Perú
Institution:Universidad de San Martín de Porres
Repository:Horizonte médico
Language:Spanish
OAI Identifier:oai:horizontemedico.usmp.edu.pe:article/1197
Online Access:https://horizontemedico.usmp.edu.pe/index.php/horizontemed/article/view/1197
Access Level:Open access
Keyword:Clozapine
Antipsychotic agents
Agranulocytosis
Neutropenia
Pharmacovigilance
Clozapina
Antipsicóticos
Agranulocitosis
Farmacovigilancia
Description
Summary:Clozapine currently remains the gold standard for treatment-resistant schizophrenia, but only under an adequate hematological monitoring, because it is associated with agranulocytosis. Clozapine is metabolized to produce pharmacologically active N-desmethylclozapine, inactive clozapine N-oxide and reactive oxygen species (nitrenium ion). A neutrophil count < 1000 cells/mm3 corresponds to a state of neutropenia. Agranulocytosis is a severe state of neutropenia with an absolute neutrophil count < 500 cells/mm3. Clozapine is associated with agranulocytosis in approximately 0.8 % of the patients, with an increased risk in older people and women. There are two mechanisms that explain the clozapine-induced agranulocytosis: immunological (response mediated by the immune system against haptenized neutrophils) and toxic (by the action of the metabolites N-desmethylclozapine and nitrenium ion). Pharmacogenetics represents a valuable tool to achieve the so-called personalized medicine by adapting and individualizing the treatment based on the genetic markers of each patient. Several studies have shown a potential association of clozapine-induced agranulocytosis with certain HLA haplotypes (HLA-B38, DR4, DQw3 and DQB1). After a patient has presented agranulocytosis, three mechanisms of clozapine rechallenge are known: simple, with lithium and with factors that stimulate granulocyte colonies. Due to the risk of agranulocytosis, clozapine formulations are available only through a controlled distribution, with a detailed record of the patients, and with a mandatory and systematized pharmacovigilance.