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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
ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)HRH1 (Histamine H1 Receptor)NET (Norepinephrine Transporter)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR1D (5-hydroxytryptamine receptor 1D)HTR2A (Serotonin receptor 5-HT2A)SERT (Sodium-dependent serotonin transporter)ADRA1 (Alpha-1 adrenergic receptor family)
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