Peringatan Keamanan

Information on acute overdosage with cilostazol in humans is limited. The signs and symptoms of an acute overdose can be anticipated to be those of excessive pharmacologic effect: severe headache, diarrhea, hypotension, tachycardia, and possibly cardiac arrhythmias. The oral LD50 of cilostazol is >5.0 g/kg in mice and rats and >2.0 g/kg in dogs.

Cilostazol

DB01166

small molecule approved investigational

Deskripsi

Cilostazol is a quinolinone derivative and antiplatelet agent with vasodilating properties that has been used in the symptomatic treatment of intermittent claudication in patients with peripheral ischaemia. It is marketed under the brand name Pletal by Otsuka Pharmaceutical Co.. Cilostazol works by inhibiting both primary and secondary aggregation and reducing calcium-induced contractions.

Struktur Molekul 2D

Berat 369.4607
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 11-13 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Cilostazol is absorbed after oral administration. A high fat meal increases absorption, with an approximately 90% increase in Cmax and a 25% increase in AUC. Absolute bioavailability is not known.

Metabolisme

Hepatic. Cilostazol is extensively metabolized by hepatic cytochrome P-450 enzymes, mainly 3A4, and, to a lesser extent, 2C19, with metabolites largely excreted in urine. Two metabolites are active, with one metabolite appearing to account for at least 50% of the pharmacologic (PDE III inhibition) activity after administration of cilostazol.

Rute Eliminasi

Cilostazol is extensively metabolized by hepatic cytochrome P-450 enzymes, mainly 3A4, and, to a lesser extent, 2C19, with metabolites largely excreted in urine. Cilostazol is eliminated predominately by metabolism and subsequent urinary excretion of metabolites. The primary route of elimination was via the urine (74%), with the remainder excreted in feces (20%). No measurable amount of unchanged cilostazol was excreted in the urine, and less than 2% of the dose was excreted as 3,4-dehydro-cilostazol. About 30% of the dose was excreted in urine as 4'-trans-hydroxy-cilostazol.

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products.
  • 2. Take on an empty stomach. A high fat meal will increase absorption.

Interaksi Obat

1883 Data
Apixaban The risk or severity of adverse effects can be increased when Cilostazol is combined with Apixaban.
Dasatinib Dasatinib may increase the anticoagulant activities of Cilostazol.
Ursodeoxycholic acid The risk or severity of adverse effects can be increased when Cilostazol is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of adverse effects can be increased when Cilostazol is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of adverse effects can be increased when Cilostazol is combined with Cholic Acid.
Glycocholic acid The risk or severity of adverse effects can be increased when Cilostazol is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of adverse effects can be increased when Cilostazol is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of adverse effects can be increased when Cilostazol is combined with Taurocholic acid.
Obeticholic acid The risk or severity of adverse effects can be increased when Cilostazol is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of adverse effects can be increased when Cilostazol is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of adverse effects can be increased when Cilostazol is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of adverse effects can be increased when Cilostazol is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of adverse effects can be increased when Cilostazol is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of adverse effects can be increased when Cilostazol is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of adverse effects can be increased when Cilostazol is combined with Hyodeoxycholic Acid.
Glucosamine Glucosamine may increase the antiplatelet activities of Cilostazol.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Cilostazol is combined with Ibritumomab tiuxetan.
Ibrutinib The risk or severity of adverse effects can be increased when Ibrutinib is combined with Cilostazol.
Obinutuzumab The risk or severity of adverse effects can be increased when Cilostazol is combined with Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the antiplatelet activities of Cilostazol.
Rivaroxaban Cilostazol may increase the anticoagulant activities of Rivaroxaban.
Tipranavir Tipranavir may increase the antiplatelet activities of Cilostazol.
Urokinase Cilostazol may increase the anticoagulant activities of Urokinase.
Vitamin E Vitamin E may increase the antiplatelet activities of Cilostazol.
Methylene blue The serum concentration of Cilostazol can be increased when it is combined with Methylene blue.
Fenofibrate The serum concentration of Cilostazol can be increased when it is combined with Fenofibrate.
Fluvoxamine The serum concentration of Cilostazol can be increased when it is combined with Fluvoxamine.
Bortezomib The serum concentration of Cilostazol can be increased when it is combined with Bortezomib.
Fluconazole The serum concentration of Cilostazol can be increased when it is combined with Fluconazole.
Sildenafil The serum concentration of Cilostazol can be increased when it is combined with Sildenafil.
Ticlopidine The serum concentration of Cilostazol can be increased when it is combined with Ticlopidine.
Pantoprazole The serum concentration of Cilostazol can be increased when it is combined with Pantoprazole.
Citalopram The serum concentration of Cilostazol can be increased when it is combined with Citalopram.
Valproic acid The serum concentration of Cilostazol can be increased when it is combined with Valproic acid.
Amitriptyline The serum concentration of Cilostazol can be increased when it is combined with Amitriptyline.
Indomethacin The serum concentration of Cilostazol can be increased when it is combined with Indomethacin.
Olanzapine The serum concentration of Cilostazol can be increased when it is combined with Olanzapine.
Omeprazole The serum concentration of Cilostazol can be increased when it is combined with Omeprazole.
Clozapine The serum concentration of Cilostazol can be increased when it is combined with Clozapine.
Progesterone The serum concentration of Cilostazol can be increased when it is combined with Progesterone.
Sorafenib The serum concentration of Cilostazol can be increased when it is combined with Sorafenib.
Chloramphenicol The serum concentration of Cilostazol can be increased when it is combined with Chloramphenicol.
Lansoprazole The serum concentration of Cilostazol can be increased when it is combined with Lansoprazole.
Imipramine The serum concentration of Cilostazol can be increased when it is combined with Imipramine.
Quinine The serum concentration of Cilostazol can be increased when it is combined with Quinine.
Fluoxetine The serum concentration of Cilostazol can be increased when it is combined with Fluoxetine.
Cimetidine The serum concentration of Cilostazol can be increased when it is combined with Cimetidine.
Ritonavir The serum concentration of Cilostazol can be increased when it is combined with Ritonavir.
Mephenytoin The serum concentration of Cilostazol can be increased when it is combined with Mephenytoin.
Zafirlukast The serum concentration of Cilostazol can be increased when it is combined with Zafirlukast.
Carbamazepine The serum concentration of Cilostazol can be increased when it is combined with Carbamazepine.
Voriconazole The serum concentration of Cilostazol can be increased when it is combined with Voriconazole.
Nicardipine The serum concentration of Cilostazol can be increased when it is combined with Nicardipine.
Efavirenz The serum concentration of Cilostazol can be increased when it is combined with Efavirenz.
Nilutamide The serum concentration of Cilostazol can be increased when it is combined with Nilutamide.
Aprepitant The serum concentration of Cilostazol can be increased when it is combined with Aprepitant.
Warfarin The serum concentration of Cilostazol can be increased when it is combined with Warfarin.
Amprenavir The serum concentration of Cilostazol can be increased when it is combined with Amprenavir.
Delavirdine The serum concentration of Cilostazol can be increased when it is combined with Delavirdine.
Esomeprazole The serum concentration of Cilostazol can be increased when it is combined with Esomeprazole.
Modafinil The serum concentration of Cilostazol can be increased when it is combined with Modafinil.
Tranylcypromine The serum concentration of Cilostazol can be increased when it is combined with Tranylcypromine.
Methimazole The serum concentration of Cilostazol can be increased when it is combined with Methimazole.
Oxcarbazepine The serum concentration of Cilostazol can be increased when it is combined with Oxcarbazepine.
Phenelzine The serum concentration of Cilostazol can be increased when it is combined with Phenelzine.
Diazepam The serum concentration of Cilostazol can be increased when it is combined with Diazepam.
Ethanol The serum concentration of Cilostazol can be increased when it is combined with Ethanol.
Zonisamide The serum concentration of Cilostazol can be increased when it is combined with Zonisamide.
Buprenorphine The serum concentration of Cilostazol can be increased when it is combined with Buprenorphine.
Felbamate The serum concentration of Cilostazol can be increased when it is combined with Felbamate.
Isoniazid The serum concentration of Cilostazol can be increased when it is combined with Isoniazid.
Telmisartan The serum concentration of Cilostazol can be increased when it is combined with Telmisartan.
Azelastine The metabolism of Cilostazol can be decreased when combined with Azelastine.
Ethinylestradiol The serum concentration of Cilostazol can be increased when it is combined with Ethinylestradiol.
Ketoconazole The serum concentration of Cilostazol can be increased when it is combined with Ketoconazole.
Probenecid The serum concentration of Cilostazol can be increased when it is combined with Probenecid.
Thalidomide The serum concentration of Cilostazol can be increased when it is combined with Thalidomide.
Memantine The serum concentration of Cilostazol can be increased when it is combined with Memantine.
Dimethyl sulfoxide The serum concentration of Cilostazol can be increased when it is combined with Dimethyl sulfoxide.
Fluvastatin The serum concentration of Cilostazol can be increased when it is combined with Fluvastatin.
Sertraline The serum concentration of Cilostazol can be increased when it is combined with Sertraline.
Miconazole The serum concentration of Cilostazol can be increased when it is combined with Miconazole.
Bicalutamide The serum concentration of Cilostazol can be increased when it is combined with Bicalutamide.
Rabeprazole The serum concentration of Cilostazol can be increased when it is combined with Rabeprazole.
Moclobemide The serum concentration of Cilostazol can be increased when it is combined with Moclobemide.
Gemfibrozil The serum concentration of Cilostazol can be increased when it is combined with Gemfibrozil.
Clomipramine The serum concentration of Cilostazol can be increased when it is combined with Clomipramine.
Aminophenazone The serum concentration of Cilostazol can be increased when it is combined with Aminophenazone.
Antipyrine The serum concentration of Cilostazol can be increased when it is combined with Antipyrine.
Etoricoxib The serum concentration of Cilostazol can be increased when it is combined with Etoricoxib.
Topiroxostat The serum concentration of Cilostazol can be increased when it is combined with Topiroxostat.
Oritavancin The serum concentration of Cilostazol can be increased when it is combined with Oritavancin.
Clevidipine The serum concentration of Cilostazol can be increased when it is combined with Clevidipine.
Methsuximide The serum concentration of Cilostazol can be increased when it is combined with Methsuximide.
Abiraterone The serum concentration of Cilostazol can be increased when it is combined with Abiraterone.
Dovitinib The serum concentration of Cilostazol can be increased when it is combined with Dovitinib.
Sitaxentan The serum concentration of Cilostazol can be increased when it is combined with Sitaxentan.
Armodafinil The serum concentration of Cilostazol can be increased when it is combined with Armodafinil.
Etravirine The serum concentration of Cilostazol can be increased when it is combined with Etravirine.
Safinamide The serum concentration of Cilostazol can be increased when it is combined with Safinamide.

Target Protein

cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A PDE3A

Referensi & Sumber

Synthesis reference: Marioara Mendelovici, "Processes for preparing cilostazol." U.S. Patent US20020099213, issued July 25, 2002.

Contoh Produk & Brand

Produk: 71 • International brands: 1
Produk
  • Cilostazol
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Cilostazol
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Cilostazol
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Cilostazol
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Cilostazol
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Cilostazol
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Cilostazol
    Tablet • 50 mg/1 • Oral • US • Generic • Approved
  • Cilostazol
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 71 produk.
International Brands
  • Pletaal

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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