Peringatan Keamanan

Symptoms of overdose are extensions of its dose-limiting pharmacologic effects and include flushing, headache, hypotension, nausea, vomiting, and diarrhea. Most events were self-limiting and resolved with reduction or withholding of epoprostenol. Single intravenous doses at 10 and 50 mg/kg (2703 and 27,027 times the recommended acute phase human dose based on body surface area) were lethal to mice and rats, respectively. Symptoms of acute toxicity were hypoactivity, ataxia, loss of righting reflex, deep slow breathing, and hypothermia.

Epoprostenol

DB01240

small molecule approved

Deskripsi

A prostaglandin that is a powerful vasodilator and inhibits platelet aggregation. It is biosynthesized enzymatically from prostaglandin endoperoxides in human vascular tissue. The sodium salt has been also used to treat primary pulmonary hypertension.

Struktur Molekul 2D

Berat 352.4651
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The in vitro half-life of epoprostenol in human blood at 37°C and pH 7.4 is approximately 6 minutes; the in vivo half-life of epoprostenol in humans is therefore expected to be no greater than 6 minutes.
Volume Distribusi * 357 mL/kg
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Epoprostenol is metabolized to 2 primary metabolites: 6-keto-PGF1α (formed by spontaneous degradation) and 6,15-diketo-13,14-dihydro-PGF1α (enzymatically formed), both of which have pharmacological activity orders of magnitude less than epoprostenol in animal test systems. Fourteen additional minor metabolites have been isolated from urine, indicating that epoprostenol is extensively metabolized in humans.

Rute Eliminasi

Epoprostenol is metabolized to 2 primary metabolites: 6-keto-PGF1? (formed by spontaneous degradation) and 6,15-diketo-13,14-dihydro-PGF1? (enzymatically formed), both of which have pharmacological activity orders of magnitude less than epoprostenol in animal test systems. Fourteen additional minor metabolites have been isolated from urine, indicating that epoprostenol is extensively metabolized in humans.

Interaksi Makanan

1 Data
  • 1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Interaksi Obat

1501 Data
Apixaban Apixaban may increase the anticoagulant activities of Epoprostenol.
Dabigatran etexilate Dabigatran etexilate may increase the anticoagulant activities of Epoprostenol.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Epoprostenol.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Epoprostenol is combined with Deferasirox.
Edoxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Epoprostenol.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Epoprostenol.
Rivaroxaban Epoprostenol may increase the anticoagulant activities of Rivaroxaban.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Epoprostenol is combined with Sugammadex.
Tibolone Tibolone may increase the anticoagulant activities of Epoprostenol.
Urokinase Urokinase may increase the anticoagulant activities of Epoprostenol.
Vorapaxar The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Epoprostenol.
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Epoprostenol is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Epoprostenol is combined with Levodopa.
Risperidone Epoprostenol may increase the hypotensive activities of Risperidone.
Ursodeoxycholic acid The risk or severity of adverse effects can be increased when Epoprostenol is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of adverse effects can be increased when Epoprostenol is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of adverse effects can be increased when Epoprostenol is combined with Cholic Acid.
Glycocholic acid The risk or severity of adverse effects can be increased when Epoprostenol is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of adverse effects can be increased when Epoprostenol is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of adverse effects can be increased when Epoprostenol is combined with Taurocholic acid.
Obeticholic acid The risk or severity of adverse effects can be increased when Epoprostenol is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of adverse effects can be increased when Epoprostenol is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of adverse effects can be increased when Epoprostenol is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of adverse effects can be increased when Epoprostenol is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of adverse effects can be increased when Epoprostenol is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of adverse effects can be increased when Epoprostenol is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of adverse effects can be increased when Epoprostenol is combined with Hyodeoxycholic Acid.
Glucosamine Glucosamine may increase the antiplatelet activities of Epoprostenol.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Epoprostenol is combined with Ibritumomab tiuxetan.
Obinutuzumab The risk or severity of adverse effects can be increased when Epoprostenol is combined with Obinutuzumab.
Tipranavir Tipranavir may increase the antiplatelet activities of Epoprostenol.
Vitamin E Vitamin E may increase the antiplatelet activities of Epoprostenol.
Alfuzosin Alfuzosin may increase the hypotensive activities of Epoprostenol.
Amifostine Epoprostenol may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Epoprostenol.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Epoprostenol.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Epoprostenol.
Rituximab Epoprostenol may increase the hypotensive activities of Rituximab.
Phentermine Phentermine may decrease the antihypertensive activities of Epoprostenol.
Midodrine Midodrine may decrease the antihypertensive activities of Epoprostenol.
Eletriptan Eletriptan may decrease the antihypertensive activities of Epoprostenol.
Isoetharine Isoetharine may decrease the antihypertensive activities of Epoprostenol.
Methysergide Methysergide may decrease the antihypertensive activities of Epoprostenol.
Cabergoline Cabergoline may decrease the antihypertensive activities of Epoprostenol.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Epoprostenol.
Dihydroergotamine Dihydroergotamine may decrease the antihypertensive activities of Epoprostenol.
Protriptyline Protriptyline may decrease the antihypertensive activities of Epoprostenol.
Methylergometrine Methylergometrine may decrease the antihypertensive activities of Epoprostenol.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Epoprostenol.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Epoprostenol.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Epoprostenol.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Epoprostenol.
Promazine Promazine may decrease the antihypertensive activities of Epoprostenol.
Droperidol Droperidol may decrease the antihypertensive activities of Epoprostenol.
Nortriptyline Nortriptyline may decrease the antihypertensive activities of Epoprostenol.
Amoxapine Amoxapine may decrease the antihypertensive activities of Epoprostenol.
Doxapram Doxapram may decrease the antihypertensive activities of Epoprostenol.
Atropine Atropine may decrease the antihypertensive activities of Epoprostenol.
Lisuride Lisuride may decrease the antihypertensive activities of Epoprostenol.
Metaraminol Metaraminol may decrease the antihypertensive activities of Epoprostenol.
Epinephrine Epinephrine may decrease the antihypertensive activities of Epoprostenol.
Ergotamine Ergotamine may decrease the antihypertensive activities of Epoprostenol.
Nicergoline Nicergoline may decrease the antihypertensive activities of Epoprostenol.
Methoxamine Methoxamine may decrease the antihypertensive activities of Epoprostenol.
Trimipramine Trimipramine may decrease the antihypertensive activities of Epoprostenol.
Propiomazine Propiomazine may decrease the antihypertensive activities of Epoprostenol.
Alfentanil Alfentanil may decrease the antihypertensive activities of Epoprostenol.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Epoprostenol.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Epoprostenol.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Epoprostenol.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Epoprostenol.
Benzphetamine Benzphetamine may decrease the antihypertensive activities of Epoprostenol.
Ritodrine Ritodrine may decrease the antihypertensive activities of Epoprostenol.
Flupentixol Flupentixol may decrease the antihypertensive activities of Epoprostenol.
Bitolterol Bitolterol may decrease the antihypertensive activities of Epoprostenol.
Oxymetazoline Oxymetazoline may decrease the antihypertensive activities of Epoprostenol.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Epoprostenol.
Salmeterol Salmeterol may decrease the antihypertensive activities of Epoprostenol.
Naratriptan Naratriptan may decrease the antihypertensive activities of Epoprostenol.
Formoterol Formoterol may decrease the antihypertensive activities of Epoprostenol.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Epoprostenol.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Epoprostenol.
Ergoloid mesylate Ergoloid mesylate may decrease the antihypertensive activities of Epoprostenol.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Epoprostenol.
Arbutamine Arbutamine may decrease the antihypertensive activities of Epoprostenol.
Dutasteride Dutasteride may decrease the antihypertensive activities of Epoprostenol.
Propafenone Propafenone may decrease the antihypertensive activities of Epoprostenol.
Pergolide Pergolide may decrease the antihypertensive activities of Epoprostenol.
Finasteride Finasteride may decrease the antihypertensive activities of Epoprostenol.
Ergometrine Ergometrine may decrease the antihypertensive activities of Epoprostenol.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Epoprostenol.
Fenoterol Fenoterol may decrease the antihypertensive activities of Epoprostenol.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Epoprostenol.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Epoprostenol.
Ephedrine Ephedrine may decrease the antihypertensive activities of Epoprostenol.
Mephentermine Mephentermine may decrease the antihypertensive activities of Epoprostenol.
Procaterol Procaterol may decrease the antihypertensive activities of Epoprostenol.
Yohimbine Yohimbine may decrease the antihypertensive activities of Epoprostenol.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Epoprostenol.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Epoprostenol.

Target Protein

Prostacyclin synthase PTGIS
P2Y purinoceptor 12 P2RY12
Prostacyclin receptor PTGIR

Referensi & Sumber

Synthesis reference: Nagesh R. Palepu, "NOVEL EPOPROSTENOL FORMULATION AND METHOD OF MAKING THEREOF." U.S. Patent US20090088468, issued April 02, 2009.

Contoh Produk & Brand

Produk: 21 • International brands: 0
Produk
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    Powder, for solution • 1.5 mg / vial • Intravenous • Canada • Approved
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    Powder, for solution • 0.5 mg / vial • Intravenous • Canada • Approved
  • Epoprostenol
    Powder, for solution • 1.5 mg/5mL • Intravenous • US • Approved
  • Epoprostenol
    Injection, powder, lyophilized, for solution • 0.5 mg/10mL • Intravenous • US
  • Epoprostenol
    Injection, powder, lyophilized, for solution • 1.5 mg/10mL • Intravenous • US
  • Epoprostenol
    Injection, powder, lyophilized, for solution • 0.5 mg/10mL • Intravenous • US • Generic • Approved
  • Epoprostenol
    Injection, powder, lyophilized, for solution • 1.5 mg/10mL • Intravenous • US • Generic • Approved
  • Epoprostenol
    Injection, powder, lyophilized, for solution • 0.5 mg/10mL • Intravenous • US • Generic • Approved
Menampilkan 8 dari 21 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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