- Overview
- Properties
- Genetics
- Related Genes
- Related Drugs
- Related Diseases
- Datasets
- Downloads/LinkOuts
Overview
| Generic Names: | Ziprasidone hydrochloride; Ziprasidone mesylate trihydrate |
|---|---|
| Trade Names: | Geodon; Zeldox |
| PharmGKB Accession Id: | PA451974 |
Description
Ziprasidone (marketed as Geodon, Zeldox) was the fifth atypical antipsychotic to gain FDA approval (February 2001). Ziprasidone is Food and Drug Administration (FDA) approved for the treatment of schizophrenia, and the intramuscular injection form of ziprasidone is approved for acute agitation in schizophrenic patients. Ziprasidone has also received approval for acute treatment of mania associated with bipolar disorder. Wikipedia (source: Drug Bank)
Indication
For the treatment of schizophrenia (source: Drug Bank)
ATC Therapeutic Category
- N05AE:Indole derivatives
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
The mechanism of action of Ziprasidone, as with other drugs used to treat schizophrenia, is unknown. Ziprasidone exhibited high in vitro binding affinity for the dopamine D2 and D3, the serotonin 5HT2A, 5HT2C, 5HT1A, 5HT1D and alpha 1-adrenergic receptors, and moderate affinity for the histamine H1 receptor. However, it has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of dopamine Type 2 (D2) and serotonin Type 2 (5HT<sub>2</sub>) receptor antagonism. (source: Drug Bank)
Pharmacology
Ziprasidone is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Ziprasidone is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), dopamine Type 2 (D2), 1 and 2 adrenergic, and H1 histaminergic receptors. Ziprasidone acts as an antagonist at other receptors, but with lower potency. Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of Ziprasidone. Ziprasidone's antagonism of muscarinic M1-5 receptors may explain its anticholinergic effects. Ziprasidone's antagonism of histamine H1 receptors may explain the somnolence observed with this drug. Ziprasidone's antagonism of adrenergic a1 receptors may explain the orthostatic hypotension observed with this drug. Ziprasidone functions as an antagonist at the Dopamine D2 , 5HT-2A , and 5HT-1D receptors, and as an agonist at the 5HT-1A receptor. Ziprasidone also inhibits synaptic reuptake of serotonin and norepinephrine. (source: Drug Bank)
Food Interactions
Avoid alcohol. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (source: Drug Bank)
Protein Binding
99% (source: Drug Bank)
Absorption
~60% (source: Drug Bank)
Isomeric SMILES Code:
c1ccc2c(c1)c(ns2)N3CCN(CC3)CCc4cc5c(cc4Cl)NC(=O)C5 (source: Drug Bank)
Curated Annotations (
)
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rs951439
at chr1:161300315
in
RGS4
This variant is associated with differential antipsychotic treatment response in individuals of african descent. Patients with african descent and rs951439 genotype CC responded better to perphenazine treatment compared with ziprasidone or quetiapine treatments. Patient with European descent and rs951439 TT genotype responded better to risperidone than those with CC genotype. However, no association was find between this variant and incidence or age at onset in schizophrenia as well as treatment responses in Finnish patients.- Related Drugs:
- perphenazine, quetiapine, risperidone, ziprasidone
- Related Diseases:
- Schizophrenia
- Evidence:
-
PMID:16604300
PMID:17588543
PMID:18204343
-
rs2661319
at chr1:161306401
in
RGS4
This variant is associated with differential antipsychotic treatment response in individuals of african descent and chinese descent.- Related Drugs:
- perphenazine, quetiapine, risperidone, ziprasidone
- Related Diseases:
- Schizophrenia
- Evidence:
-
PMID:17588543
PMID:18204343
-
rs2842030
at chr1:161307119
in
RGS4
This variant is associated with differential antipsychotic treatment response in individuals of african descent. Patient with rs2842030 TT genotype responded better to perphenazine treatment than by quatiapine, risperidone or ziprasidone. Patient with European descent and rs2842030 GG genotype responded better to risperidone than those with TT genotype.No association was found between this variant and increased susceptibility to the etiology of schizophrenia in Han Chinese.- Related Drugs:
- perphenazine, quetiapine, risperidone, ziprasidone
- Related Diseases:
- Schizophrenia
- Evidence:
-
PMID:16904822
PMID:17588543
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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CYP2D6 |
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Publications |
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CYP3A |
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Publications |
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CYP3A4 |
|
Publications |
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CYP3A5 |
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Publications |
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DRD2 |
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Publications |
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DRD4 |
|
Publications |
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HRH1 |
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Publications |
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KCNH2 |
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Publications |
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RGS4 |
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Variants |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| HTR1A |
|
(source: Drug Bank) |
| HTR1D |
|
(source: Drug Bank) |
| HTR2A |
|
(source: Drug Bank) |
| HTR2C |
|
(source: Drug Bank) |
| HTR7 |
|
(source: Drug Bank) |
| ADRA1A |
|
(source: Drug Bank) |
| ADRB1 |
|
(source: Drug Bank) |
| DRD2 |
|
(source: Drug Bank) |
| DRD3 |
|
(source: Drug Bank) |
| DRD4 |
|
(source: Drug Bank) |
| HRH1 |
|
(source: Drug Bank) |
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
|
|
tamoxifen |
|
Publications |
A list of non-curated publications that mention this drug along with other drugs is available.
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
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Body Weight Changes |
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Publications |
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Psychotic Disorders |
|
Publications |
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Schizophrenia |
|
Publications, Variants |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
Search PubMed
Search Medline Plus
Search PubChem
Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.