Drug intelligence / Profile preview

ziprasidone

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

Overview

Ziprasidone is a benzisothiazolylpiperazine class atypical antipsychotic drug primarily used to treat schizophrenia and bipolar disorder (manic or mixed episodes). It acts mainly as an antagonist of dopamine D2 and serotonin 5-HT2A receptors. Additionally, it moderately antagonizes alpha-adrenergic and histamine H1 receptors. Unique among atypical antipsychotics, ziprasidone also inhibits the reuptake of norepinephrine and serotonin transporters enhancing their function similarly to tricyclic antidepressants like amitriptyline. It activates the 5-HT1A receptor subtype significantly while having minimal H1 histamine receptor antagonism. Approved by the FDA in 2001 for schizophrenia treatment in adults, it is available as oral capsules (20mg to 80mg) and intramuscular injection formulations for acute agitation in schizophrenia. Ziprasidone has a lower risk of weight gain and hyperprolactinemia compared with other atypical antipsychotics. The drug is mostly excreted unchanged via the kidneys with minimal hepatic metabolism reducing liver toxicity risk[1][4][5][6][7].

Brand names
Geodon卓乐定Zeldox
Other names
齐拉西酮ziprasidone hydrochloride
02

Targets

HTR2A (Serotonin receptor 5-HT2A)SERT (Sodium-dependent serotonin transporter)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HRH1 (Histamine H1 Receptor)HTR1D (5-hydroxytryptamine receptor 1D)ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)NET (Norepinephrine Transporter)

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