Vol 6 n° 1
- Predictors of Response to Treatment in Neuropsychiatry
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7 1
P h a r m a c o l o g i c a l a s p e c t s
Differing response to antipsychotic therapy
in schizophrenia: pharmacogenomic aspects
Manfred Ackenheil, MD; Klaus Weber, MPharm
Keywords:
antipsychotic; pharmacogenomics; pharmacokinetics; nonresponse;
schizophrenia
Author affiliations:
Psychiatric Hospital of the University of Munich, Munich,
Germany
Address for correspondence:
Psychiatric Hospital of the University of
Munich, Nussbaumstrasse 7, D-80336 Munich, Germany
(e-mail: Manfred.Ackenheil@med.uni-muenchen.de)
Copyright © 2004 LLS SAS. All rights reserved
www.dialogues-cns.org
onresponse is a frequent phenomenon in both
somatic and psychiatric pharmacotherapy. A consider-
able number of drugs have become available for the
treatment of various psychiatric diseases since the dis-
covery of chlorpromazine 50 years ago.
1
Despite all the
progress in this field, there are still many patients who
do not respond to treatment, so-called
nonresponders
.
Around 20% to 30% of the patients with schizophrenia
are thought to be nonresponders to one or more psy-
chotropic drugs.
Several reasons for nonresponse to treatment have been
considered.The main issue is the heterogeneity of schiz-
ophrenic disorders, which can result in different clinical
pictures. The existing theories discussed for schizophre-
nia
(Figure 1)
may be only a small part of the existing
mechanisms causing schizophrenia. Consequently, the
research strategy is to focus on the effects of alterations
N
Treatment-resistance in schizophrenia remains a public health problem: about 20% to 30% of patients do not respond
to antipsychotic therapy. Clozapine has been shown to be effective in about one-third of patients, but the medical
risks and weekly blood tests limit its broad application. While the heterogeneity of the disease and the duration of
untreated psychosis are important, pharmacogenomic aspects must also be considered. Pharmacogenomic investiga-
tions offer the opportunity to individualize antipsychotic therapy according to the growing knowledge of the func-
tion and effect of the genetic polymorphisms that affect the pharmacokinetics and pharmacodynamics of antipsy-
chotics. On the pharmacokinetic level, polymorphic phase I and II drug-metabolizing enzymes and transport proteins
affect drug concentration at the target structure. The cytochrome P450 enzymes,
N
-acetyltransferase, and multidrug
resistance protein (MDR1) particularly influence this parameter. Genetic alterations affecting drug pharmacodynamic
properties have an impact on therapeutic outcome that is generally independent of the applied dosage regimen. A
combined analysis of genetic polymorphisms in the dopaminergic and serotonergic receptors, neurotransmitter trans-
porters, and other target structures involved in psychiatric disorders is already a powerful predictor of therapeutic out-
come. An understanding of other factors influencing gene expression and protein production will facilitate individ-
ualized therapy in the future.
© 2004, LLS SAS
Dialogues Clin Neurosci
. 2004;6:71-77.