Peringatan Keamanan

The most common adverse reactions reported with ziprasidone include somnolence, respiratory tract infections, extrapyramidal symptoms, dizziness, akathisia, abnormal vision, asthenia, vomiting, headache and nausea. L7342

Ziprasidone

DB00246

small molecule approved

Deskripsi

Disorders such as schizophrenia and bipolar disorder can significantly impair mood, cognition, and behavior.A190525 These mental illnesses can often be accompanied by comorbidities such as depression and substance abuse, and can significantly impact the quality of life of patients and caregivers.A190525 Luckily, several treatment options for psychotic disorders have been introduced to market since the realization of chlorpromazine's antipsychotic properties in 1952.A190525

Second generation antipsychotics (commonly referred to as atypical antipsychotics) include clozapine, quetiapine, olanzapine, aripiprazole and ziprasidone among others, and are generally thought to be as efficacious as first generation antipsychotics but differ in their adverse effect profiles.A190525,A190534 First generation antipsychotics are associated with extrapyramidal adverse effects while atypical antipsychotics are linked to weight gain, impaired glucose tolerance and metabolic syndrome.A190534,A190537

Ziprasidone is used to treat schizophrenia and bipolar disorder.A180748 It can effectively reduce the rate and time of relapses in schizophrenia, and can be used to treat manic episodes in bipolar disorder although the mechanism of action is unknown.A180748 Although ziprasidone is classified as an atypical antipsychotic, it appears to have a lower incidence of metabolic adverse effects compared to other medications in the same class.A190525

Struktur Molekul 2D

Berat 412.936
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of ziprasidone is 6-7 hours.[A174562]
Volume Distribusi The mean apparent volume of distribution of Ziprasidone is 1.5 L/kg.[L7342]
Klirens (Clearance) The mean apparent systemic clearance is 7.5 mL/min/kg.[L7342]

Absorpsi

In the absence of food, ziprasidone's oral bioavailability is 60%, and absorption may reach 100% if ziprasidone is taken with a meal containing at least 500 kcal. The difference in bioavailability has little to do with the fat content of the food and appears to be related to the bulk of the meal since more absorption occurs the longer ziprasidone remains in the stomach.A174562

Metabolisme

Ziprasidone is heavily metabolized in the liver with less than 5% of the drug excreted unchanged in the urine.A174277 The primary reductive pathway is catalyzed by aldehyde oxidase, while 2 other less prominent oxidative pathways are catalyzed by CYP3A4.A174277 Ziprasidone is unlikely to interact with other medications metabolized by CYP3A4 since only 1/3 of the antipsychotic is metabolized by the CYP3A4 system.A174277 There are 12 identified ziprasidone metabolites (abbreviations italicized): Ziprasidone sulfoxide, ziprasidone sulfone, (6-chloro-2-oxo-2,3-dihydro-1H-indol-5-yl)acetic acid (OX-COOH), OX-COOH glucuronide, 3-(piperazine-1-yl)-1,2-benzisothiazole (BITP), BITP sulfoxide, BITP sulfone, BITP sulfone lactam, S-Methyl-dihydro-ziprasidone, S-Methyl-dihydro-ziprasidone-sulfoxide, 6-chloro-5-(2-piperazin-1-yl-ethyl)-1,3-dihydro-indol-2-one (OX-P), and dihydro-ziprasidone-sulfone.A190558 As suggested by the quantity of metabolites, ziprasidone is metabolized through several different pathways. Ziprasidone is sequentially oxidized to ziprasidone sulfoxide and ziprasidone sulfone, and oxidative N-dealkylation of ziprasidone produces OX-COOH and BITP.A190558 OX-COOH undergoes phase II metabolism to yield a glucuronidated metabolite while BITP is sequentially oxidized into BITP sulfoxide, BITP sulfone, then BITP sulfone lactam.A190558 Ziprasidone can also undergo reductive cleavage and methylation to produce S-Methyl-dihydro-ziprasidone and then further oxidation to produce S-Methyl-dihydro-ziprasidone-sulfoxide.A190558 Finally dearylation of ziprasidone produces OX-P, and the process of hydration and oxidation transforms the parent drug into dihydro-ziprasidone-sulfone.A190558 Although CYP3A4 and aldehyde oxidase are the primary enzymes involved in ziprasidone metabolismA174277, the pathways associated with each enzyme have not been specified.

Rute Eliminasi

Ziprasidone is extensively metabolized after oral administration with only a small amount excreted in the urine (<1%) or feces (<4%) as unchanged drug.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with food.

Interaksi Obat

2137 Data
Buprenorphine Ziprasidone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Hydrocodone Ziprasidone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Ziprasidone can be increased when used in combination with Magnesium sulfate.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Ziprasidone.
Suvorexant Ziprasidone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Ziprasidone.
Thalidomide Ziprasidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Ziprasidone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Ziprasidone.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Ziprasidone.
Everolimus The metabolism of Everolimus can be decreased when combined with Ziprasidone.
Flibanserin The metabolism of Flibanserin can be decreased when combined with Ziprasidone.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Ziprasidone.
Ivabradine The metabolism of Ivabradine can be decreased when combined with Ziprasidone.
Ivacaftor The metabolism of Ivacaftor can be decreased when combined with Ziprasidone.
Naloxegol The metabolism of Naloxegol can be decreased when combined with Ziprasidone.
Olaparib The metabolism of Olaparib can be decreased when combined with Ziprasidone.
Sonidegib The metabolism of Sonidegib can be decreased when combined with Ziprasidone.
Avanafil The metabolism of Avanafil can be decreased when combined with Ziprasidone.
Eplerenone The metabolism of Eplerenone can be decreased when combined with Ziprasidone.
Aclidinium The risk or severity of adverse effects can be increased when Ziprasidone is combined with Aclidinium.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Ziprasidone is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Ziprasidone.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Ziprasidone.
Tiotropium The risk or severity of adverse effects can be increased when Ziprasidone is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Ziprasidone is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Ziprasidone is combined with Umeclidinium.
Desmopressin The risk or severity of hypertension can be increased when Desmopressin is combined with Ziprasidone.
Icosapent The risk or severity of hypertension can be increased when Icosapent is combined with Ziprasidone.
Mesalazine The risk or severity of hypertension can be increased when Mesalazine is combined with Ziprasidone.
Indomethacin The risk or severity of hypertension can be increased when Ziprasidone is combined with Indomethacin.
Ketorolac The risk or severity of hypertension can be increased when Ziprasidone is combined with Ketorolac.
Tenoxicam The risk or severity of hypertension can be increased when Ziprasidone is combined with Tenoxicam.
Tolmetin The risk or severity of hypertension can be increased when Ziprasidone is combined with Tolmetin.
Piroxicam The risk or severity of hypertension can be increased when Ziprasidone is combined with Piroxicam.
Doxapram The risk or severity of hypertension can be increased when Ziprasidone is combined with Doxapram.
Fenoprofen The risk or severity of hypertension can be increased when Ziprasidone is combined with Fenoprofen.
Sulindac The risk or severity of hypertension can be increased when Ziprasidone is combined with Sulindac.
Flurbiprofen The risk or severity of hypertension can be increased when Ziprasidone is combined with Flurbiprofen.
Etodolac The risk or severity of hypertension can be increased when Ziprasidone is combined with Etodolac.
Mefenamic acid The risk or severity of hypertension can be increased when Ziprasidone is combined with Mefenamic acid.
Sulfasalazine The risk or severity of hypertension can be increased when Ziprasidone is combined with Sulfasalazine.
Carprofen The risk or severity of hypertension can be increased when Ziprasidone is combined with Carprofen.
Phenmetrazine The risk or severity of hypertension can be increased when Ziprasidone is combined with Phenmetrazine.
Diflunisal The risk or severity of hypertension can be increased when Ziprasidone is combined with Diflunisal.
Salicylic acid The risk or severity of hypertension can be increased when Ziprasidone is combined with Salicylic acid.
Meclofenamic acid The risk or severity of hypertension can be increased when Ziprasidone is combined with Meclofenamic acid.
Acetylsalicylic acid The risk or severity of hypertension can be increased when Ziprasidone is combined with Acetylsalicylic acid.
Dopamine The risk or severity of hypertension can be increased when Ziprasidone is combined with Dopamine.
Oxaprozin The risk or severity of hypertension can be increased when Ziprasidone is combined with Oxaprozin.
Ketoprofen The risk or severity of hypertension can be increased when Ziprasidone is combined with Ketoprofen.
Balsalazide The risk or severity of hypertension can be increased when Ziprasidone is combined with Balsalazide.
Lumiracoxib The risk or severity of hypertension can be increased when Ziprasidone is combined with Lumiracoxib.
Magnesium salicylate The risk or severity of hypertension can be increased when Ziprasidone is combined with Magnesium salicylate.
Salsalate The risk or severity of hypertension can be increased when Ziprasidone is combined with Salsalate.
Choline magnesium trisalicylate The risk or severity of hypertension can be increased when Ziprasidone is combined with Choline magnesium trisalicylate.
Antrafenine The risk or severity of hypertension can be increased when Ziprasidone is combined with Antrafenine.
Tiaprofenic acid The risk or severity of hypertension can be increased when Ziprasidone is combined with Tiaprofenic acid.
Epicaptopril The risk or severity of hypertension can be increased when Ziprasidone is combined with Epicaptopril.
Taxifolin The risk or severity of hypertension can be increased when Ziprasidone is combined with Taxifolin.
Oxyphenbutazone The risk or severity of hypertension can be increased when Ziprasidone is combined with Oxyphenbutazone.
1-benzylimidazole The risk or severity of hypertension can be increased when Ziprasidone is combined with 1-benzylimidazole.
Benoxaprofen The risk or severity of hypertension can be increased when Ziprasidone is combined with Benoxaprofen.
Cimicoxib The risk or severity of hypertension can be increased when Ziprasidone is combined with Cimicoxib.
Lornoxicam The risk or severity of hypertension can be increased when Ziprasidone is combined with Lornoxicam.
Aceclofenac The risk or severity of hypertension can be increased when Ziprasidone is combined with Aceclofenac.
Zaltoprofen The risk or severity of hypertension can be increased when Ziprasidone is combined with Zaltoprofen.
Saralasin The risk or severity of hypertension can be increased when Ziprasidone is combined with Saralasin.
Azapropazone The risk or severity of hypertension can be increased when Ziprasidone is combined with Azapropazone.
Salicylamide The risk or severity of hypertension can be increased when Ziprasidone is combined with Salicylamide.
Tyramine The risk or severity of hypertension can be increased when Ziprasidone is combined with Tyramine.
Kebuzone The risk or severity of hypertension can be increased when Ziprasidone is combined with Kebuzone.
Isoxicam The risk or severity of hypertension can be increased when Ziprasidone is combined with Isoxicam.
Indoprofen The risk or severity of hypertension can be increased when Ziprasidone is combined with Indoprofen.
Ibuproxam The risk or severity of hypertension can be increased when Ziprasidone is combined with Ibuproxam.
Floctafenine The risk or severity of hypertension can be increased when Ziprasidone is combined with Floctafenine.
Fenbufen The risk or severity of hypertension can be increased when Ziprasidone is combined with Fenbufen.
Etofenamate The risk or severity of hypertension can be increased when Ziprasidone is combined with Etofenamate.
Epirizole The risk or severity of hypertension can be increased when Ziprasidone is combined with Epirizole.
Benzydamine The risk or severity of hypertension can be increased when Ziprasidone is combined with Benzydamine.
Moxisylyte The risk or severity of hypertension can be increased when Ziprasidone is combined with Moxisylyte.
Dexibuprofen The risk or severity of hypertension can be increased when Ziprasidone is combined with Dexibuprofen.
Dexketoprofen The risk or severity of hypertension can be increased when Ziprasidone is combined with Dexketoprofen.
Droxicam The risk or severity of hypertension can be increased when Ziprasidone is combined with Droxicam.
Firocoxib The risk or severity of hypertension can be increased when Ziprasidone is combined with Firocoxib.
Clonixin The risk or severity of hypertension can be increased when Ziprasidone is combined with Clonixin.
Morniflumate The risk or severity of hypertension can be increased when Ziprasidone is combined with Morniflumate.
Talniflumate The risk or severity of hypertension can be increased when Ziprasidone is combined with Talniflumate.
Robenacoxib The risk or severity of hypertension can be increased when Ziprasidone is combined with Robenacoxib.
Tepoxalin The risk or severity of hypertension can be increased when Ziprasidone is combined with Tepoxalin.
Atipamezole The risk or severity of hypertension can be increased when Ziprasidone is combined with Atipamezole.
Flunixin The risk or severity of hypertension can be increased when Ziprasidone is combined with Flunixin.
Nitroaspirin The risk or severity of hypertension can be increased when Ziprasidone is combined with Nitroaspirin.
Indobufen The risk or severity of hypertension can be increased when Ziprasidone is combined with Indobufen.
Idazoxan The risk or severity of hypertension can be increased when Ziprasidone is combined with Idazoxan.
Ebselen The risk or severity of hypertension can be increased when Ziprasidone is combined with Ebselen.
Tinoridine The risk or severity of hypertension can be increased when Ziprasidone is combined with Tinoridine.
Tramazoline The risk or severity of hypertension can be increased when Ziprasidone is combined with Tramazoline.
Alclofenac The risk or severity of hypertension can be increased when Ziprasidone is combined with Alclofenac.
Fentiazac The risk or severity of hypertension can be increased when Ziprasidone is combined with Fentiazac.

Target Protein

D(2) dopamine receptor DRD2
Neuronal acetylcholine receptor subunit alpha-7 CHRNA7
5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 1D HTR1D
5-hydroxytryptamine receptor 2C HTR2C
D(1A) dopamine receptor DRD1
D(1B) dopamine receptor DRD5
D(3) dopamine receptor DRD3
D(4) dopamine receptor DRD4
5-hydroxytryptamine receptor 1B HTR1B
5-hydroxytryptamine receptor 1E HTR1E
5-hydroxytryptamine receptor 6 HTR6
5-hydroxytryptamine receptor 7 HTR7
Histamine H1 receptor HRH1
Alpha-1A adrenergic receptor ADRA1A
Alpha-1B adrenergic receptor ADRA1B
Alpha-2A adrenergic receptor ADRA2A
Alpha-2B adrenergic receptor ADRA2B
Alpha-2C adrenergic receptor ADRA2C
Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M3 CHRM3
Muscarinic acetylcholine receptor M4 CHRM4
Muscarinic acetylcholine receptor M5 CHRM5
5-hydroxytryptamine 3 receptor HTR3A
5-hydroxytryptamine receptor 5A HTR5A

Referensi & Sumber

Synthesis reference: Frank R. Busch, Carol A. Rose, "Mesylate trihydrate salt of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihy dro-2(1H)-indol-2-one (=ziprasidone), its preparation and its use as dopamine D2 antagonist." U.S. Patent US6110918, issued January, 1995.
Artikel (PubMed)
  • PMID: 14728084
    Stahl SM, Shayegan DK: The psychopharmacology of ziprasidone: receptor-binding properties and real-world psychiatric practice. J Clin Psychiatry. 2003;64 Suppl 19:6-12.
  • PMID: 11513838
    Schmidt AW, Lebel LA, Howard HR Jr, Zorn SH: Ziprasidone: a novel antipsychotic agent with a unique human receptor binding profile. Eur J Pharmacol. 2001 Aug 17;425(3):197-201.
  • PMID: 12826984
    Beedham C, Miceli JJ, Obach RS: Ziprasidone metabolism, aldehyde oxidase, and clinical implications. J Clin Psychopharmacol. 2003 Jun;23(3):229-32. doi: 10.1097/01.jcp.0000084028.22282.f2.
  • PMID: 23861634
    Mattei C, Rapagnani MP, Stahl SM: Ziprasidone hydrocloride: what role in the management of schizophrenia? J Cent Nerv Syst Dis. 2011 Feb 15;3:1-16. doi: 10.4137/JCNSD.S4138. Print 2011.
  • PMID: 28846230
    Bouchette D, Marwaha R: Ziprasidone .
  • PMID: 18568067
    Kutcher S, Brooks SJ, Gardner DM, Honer B, Kopala L, Labelle A, Lalonde P, Malla A, Milliken H, Soni J, Williams R: Expert Canadian consensus suggestions on the rational, clinical use of ziprasidone in the treatment of schizophrenia and related psychotic disorders. Neuropsychiatr Dis Treat. 2005 Jun;1(2):89-108. doi: 10.2147/nedt.1.2.89.61042.
  • PMID: 28344764
    Murray R, Correll CU, Reynolds GP, Taylor D: Atypical antipsychotics: recent research findings and applications to clinical practice: Proceedings of a symposium presented at the 29th Annual European College of Neuropsychopharmacology Congress, 19 September 2016, Vienna, Austria. Ther Adv Psychopharmacol. 2017 Mar;7(1 Suppl):1-14. doi: 10.1177/2045125317693200. Epub 2017 Mar 1.
  • PMID: 28883731
    Dayabandara M, Hanwella R, Ratnatunga S, Seneviratne S, Suraweera C, de Silva VA: Antipsychotic-associated weight gain: management strategies and impact on treatment adherence. Neuropsychiatr Dis Treat. 2017 Aug 22;13:2231-2241. doi: 10.2147/NDT.S113099. eCollection 2017.
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