Tìm theo
Ziprasidone
Các tên gọi khác (3) :
  • Ziprasidona
  • Ziprasidone
  • Ziprasidonum
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 146939-27-7
ATC: N05AE04
ĐG : Ben Venue Laboratories Inc. , http://www.benvenue.com
CTHH: C21H21ClN4OS
PTK: 412.936
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]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H21ClN4OS
Phân tử khối
412.936
Monoisotopic mass
412.112459711
InChI
InChI=1S/C21H21ClN4OS/c22-17-13-18-15(12-20(27)23-18)11-14(17)5-6-25-7-9-26(10-8-25)21-16-3-1-2-4-19(16)28-24-21/h1-4,11,13H,5-10,12H2,(H,23,27)
InChI Key
InChIKey=MVWVFYHBGMAFLY-UHFFFAOYSA-N
IUPAC Name
5-{2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl}-6-chloro-2,3-dihydro-1H-indol-2-one
Traditional IUPAC Name
ziprasidone
SMILES
ClC1=C(CCN2CCN(CC2)C2=NSC3=CC=CC=C23)C=C2CC(=O)NC2=C1
Độ tan chảy
>300 °C
Độ hòa tan
7.18e-03 g/l
logP
3.8
logS
-4.8
pKa (strongest acidic)
13.18
pKa (Strongest Basic)
7.09
PSA
48.47 Å2
Refractivity
116.72 m3·mol-1
Polarizability
44.96 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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] Ziprasidone's antipsychotic activity is likely due to a combination of its antagonistic function at D2 receptors in the mesolimbic pathways and at 5HT2A receptors in the frontal cortex. Alleviation of positive symptoms is due to antagonism at D2 receptors while relief of negative symptoms are due to 5HT2A antagonism.
Dược Động Học :
▧ Absorption :
~60%
▧ Volume of Distribution :
* 1.5 L/kg
▧ Protein binding :
99%
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Ziprasidone is extensively metabolized after oral administration with only a small amount excreted in the urine (<1%) or feces (<4%) as unchanged drug. Approximately 20% of the dose is excreted in the urine, with approximately 66% being eliminated in the feces.
▧ Half Life :
7 hours
▧ Clearance :
* 7.5 mL/min/kg
Chỉ Định : For the treatment of schizophrenia and related psychotic disorders.
Tương Tác Thuốc :
  • Abarelix Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Amantadine The atypical antipsychotic, ziprasidone, may antagonize the effect of the dopamine agonist, amantadine. Consider alternate therapy or monitor for worsening of movement disorder.
  • Amiodarone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Amitriptyline Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Amoxapine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Apomorphine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Arsenic trioxide Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Asenapine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Azithromycin Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Bromocriptine The atypical antipsychotic, ziprasidone, may antagonize the effect of the dopamine agonist, bromocriptine. Consider alternate therapy or monitor for worsening of movement disorder.
  • Carbamazepine Increases the effect and toxicity of ziprasidone
  • Chlorpromazine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Cisapride Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Citalopram Additive QTc-prolongation may occur increasing the risk of life-threatening ventricular arrhythmias and torsade de pointes. Concomitant therapy should be avoided.
  • Clarithromycin Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Clomipramine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Dasatinib Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Desipramine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Disopyramide Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Dofetilide Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Dolasetron Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Domperidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Donepezil Possible antagonism of action
  • Doxepin Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Dronedarone Additive QTc-prolongation may occur. Concomitant therapy is contraindicated.
  • Droperidol Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Erythromycin Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Escitalopram Additive QTc-prolongation may occur increasing the risk of life-threatening ventricular arrhythmias and torsade de pointes. Concomitant therapy should be avoided.
  • Flecainide Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Fluconazole Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Fluoxetine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Flupentixol Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Foscarnet Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Galantamine Possible antagonism of action
  • Gatifloxacin Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Halofantrine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Haloperidol Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Ibutilide Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Iloperidone Additive QTc-prolongation may occur increasing the risk of life-threatening ventricular arrhythmias and torsade de pointes. Concomitant therapy should be avoided.
  • Imipramine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Indapamide Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Isradipine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Ketoconazole Ketoconazole increases the effect and toxicity of ziprasidone
  • L-DOPA The atypical antipsychotic, ziprasidone, may antagonize the effect of the dopamine agonist, levodopa. Consider alternate therapy or monitor for worsening of movement disorder.
  • Lapatinib Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Levofloxacin Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Loxapine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Maprotiline Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Mefloquine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Mesoridazine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Methadone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Methotrimeprazine Additive QTc-prolongation may occur increasing the risk of life-threatening ventricular arrhythmias and torsade de pointes. Concomitant therapy should be avoided.
  • Moxifloxacin Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Nilotinib Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Norfloxacin Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Nortriptyline Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Octreotide Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Pazopanib Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Pentamidine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Perflutren Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Pergolide The atypical antipsychotic, ziprasidone, may antagonize the effect of the dopamine agonist, pergolide. Consider alternate therapy or monitor for worsening of movement disorder.
  • Pimozide Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Pramipexole The atypical antipsychotic, ziprasidone, may antagonize the effect of the dopamine agonist, pramipexole. Consider alternate therapy or monitor for worsening of movement disorder.
  • Probucol Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Procainamide Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Propafenone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Protriptyline Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Quetiapine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Quinidine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Quinine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Ranolazine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Risperidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Romidepsin Additive QTc-prolongation may occur increasing the risk of life-threatening ventricular arrhythmias and torsade de pointes. Concomitant therapy should be avoided.
  • Ropinirole The atypical antipsychotic, ziprasidone, may antagonize the effect of the dopamine agonist, ropinirole. Consider alternate therapy or monitor for worsening of movement disorder.
  • Rotigotine The atypical antipsychotic, ziprasidone, may antagonize the effect of the dopamine agonist, rotigotine. Consider alternate therapy or monitor for worsening of movement disorder.
  • Sotalol Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Sparfloxacin Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Sunitinib Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Tacrine Tacrine, a central acetylcholinesterase inhibitor, may augment the central neurotoxic effect of antipsychotics such as Ziprasidone. Monitor for extrapyramidal symptoms.
  • Tacrolimus Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Telavancin Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Telithromycin Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Tetrabenazine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Thioridazine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Thiothixene Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Toremifene Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Trimipramine Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Triprolidine The CNS depressants, Triprolidine and Ziprasidone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Voriconazole Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Vorinostat Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Zuclopenthixol Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
Liều Lượng & Cách Dùng : Capsule - Oral
Powder, for solution - Intramuscular
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Zeldox 20 mg Capsule
    Giá bán buôn : USD >1.86
    Đơn vị tính : capsule
  • Biệt dược thương mại : Zeldox 40 mg Capsule
    Giá bán buôn : USD >2.13
    Đơn vị tính : capsule
  • Biệt dược thương mại : Zeldox 60 mg Capsule
    Giá bán buôn : USD >2.13
    Đơn vị tính : capsule
  • Biệt dược thương mại : Zeldox 80 mg Capsule
    Giá bán buôn : USD >2.13
    Đơn vị tính : capsule
  • Biệt dược thương mại : Geodon 20 mg capsule
    Giá bán buôn : USD >8.14
    Đơn vị tính : capsule
  • Biệt dược thương mại : Geodon 40 mg capsule
    Giá bán buôn : USD >8.14
    Đơn vị tính : capsule
  • Biệt dược thương mại : Geodon 60 mg capsule
    Giá bán buôn : USD >9.88
    Đơn vị tính : capsule
  • Biệt dược thương mại : Geodon 80 mg capsule
    Giá bán buôn : USD >9.88
    Đơn vị tính : capsule
  • Biệt dược thương mại : Geodon 20 mg vial
    Giá bán buôn : USD >16.22
    Đơn vị tính : vial
  • Biệt dược thương mại : Zoladex 10.8 mg Implant Syringe
    Giá bán buôn : USD >1407.72
    Đơn vị tính : syringe
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Geodon
  • Công ty :
    Sản phẩm biệt dược : Zeldox
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00246
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60854
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507627
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07568
ChemSpider
http://www.chemspider.com/Chemical-Structure.54841.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0049-3960-60
PharmGKB
http://www.pharmgkb.org/drug/PA451974
Wikipedia
http://en.wikipedia.org/wiki/Ziprasidone
RxList
http://www.rxlist.com/cgi/generic2/ziprasidone.htm
Drugs.com
http://www.drugs.com/cdi/ziprasidone.html
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