Drug intelligence / Profile preview

ziprasidone + olanzapine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Ziprasidone + olanzapine is a combination of two atypical (second-generation) antipsychotic drugs used in the management of schizophrenia and related psychotic disorders. Both agents act primarily as antagonists at dopamine D2 and serotonin 5HT2A receptors, but each has a unique receptor binding profile. Ziprasidone also inhibits norepinephrine and serotonin reuptake, while olanzapine exhibits broader antagonism across multiple dopamine, serotonin, adrenergic, histamine, and muscarinic receptors. Combination therapy may be considered for patients with inadequate response to monotherapy or to mitigate certain side effects such as metabolic syndrome associated with olanzapine alone. Clinical studies suggest that combining these agents can improve psychotic symptoms and reduce movement-related side effects without significantly increasing metabolic risk compared to monotherapy[1][4][8].

Other names
ziprasidone + olanzapine
02

Targets

DRD4 (Dopamine D4 Receptor)HTR2A (Serotonin receptor 5-HT2A)SERT (Sodium-dependent serotonin transporter)HTR2C (5-hydroxytryptamine 2C receptor)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)ADRA1A (α1A)DRD1 (Dopamine D1 Receptor)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)HTR6 (5-hydroxytryptamine receptor 6)NET (Norepinephrine Transporter)

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