Peringatan Keamanan

There was no mortality in rats and mice receiving oral doses of up to 3000 mg eprosartan/kg and in dogs receiving oral doses of up to 1000 mg eprosartan/kg.

Eprosartan

DB00876

small molecule approved

Deskripsi

Eprosartan is an angiotensin II receptor antagonist used to treat hypertension. It performs 2 actions on the renin angiotensin system. By preventing the binding of angiotensin II to AT1, vascular smooth muscle relaxes and vasodilation occurs. By inhibiting norepinephrine production, blood pressure is further reduced.

Struktur Molekul 2D

Berat 424.513
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half-life of eprosartan following oral administration is typically 5 to 9 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Absolute bioavailability following a single 300 mg oral dose of eprosartan is approximately 13%. Administering eprosartan with food delays absorption.

Metabolisme

Eprosartan is not metabolized by the cytochrome P450 system. It is mainly eliminated as unchanged drug. Less than 2% of an oral dose is excreted in the urine as a glucuronide.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

874 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Eprosartan is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Eprosartan is combined with Levodopa.
Risperidone Eprosartan may increase the hypotensive activities of Risperidone.
Alfuzosin Alfuzosin may increase the hypotensive activities of Eprosartan.
Aliskiren The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Eprosartan.
Amifostine Eprosartan may increase the hypotensive activities of Amifostine.
Canagliflozin The risk or severity of hypotension, hyperkalemia, and reduced intravascular volume can be increased when Canagliflozin is combined with Eprosartan.
Diazoxide Diazoxide may increase the hypotensive activities of Eprosartan.
Drospirenone The risk or severity of hyperkalemia can be increased when Eprosartan is combined with Drospirenone.
Eplerenone The risk or severity of hyperkalemia can be increased when Eplerenone is combined with Eprosartan.
Semuloparin The risk or severity of hyperkalemia can be increased when Semuloparin is combined with Eprosartan.
Lithium citrate The serum concentration of Lithium citrate can be increased when it is combined with Eprosartan.
Lithium carbonate The serum concentration of Lithium carbonate can be increased when it is combined with Eprosartan.
Lithium hydroxide The serum concentration of Lithium hydroxide can be increased when it is combined with Eprosartan.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Eprosartan.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Eprosartan.
Obinutuzumab Eprosartan may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Eprosartan.
Rituximab Eprosartan may increase the hypotensive activities of Rituximab.
Tolvaptan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Eprosartan.
Trimethoprim The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Eprosartan.
Desmopressin Desmopressin may decrease the antihypertensive activities of Eprosartan.
Phentermine Phentermine may decrease the antihypertensive activities of Eprosartan.
Midodrine Midodrine may decrease the antihypertensive activities of Eprosartan.
Eletriptan Eletriptan may decrease the antihypertensive activities of Eprosartan.
Isoetharine Isoetharine may decrease the antihypertensive activities of Eprosartan.
Methysergide Methysergide may decrease the antihypertensive activities of Eprosartan.
Cabergoline Cabergoline may decrease the antihypertensive activities of Eprosartan.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Eprosartan.
Etomidate Etomidate may decrease the antihypertensive activities of Eprosartan.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Eprosartan.
Dihydroergotamine Dihydroergotamine may decrease the antihypertensive activities of Eprosartan.
Amitriptyline Amitriptyline may decrease the antihypertensive activities of Eprosartan.
Protriptyline Protriptyline may decrease the antihypertensive activities of Eprosartan.
Methylergometrine Methylergometrine may decrease the antihypertensive activities of Eprosartan.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Eprosartan.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Eprosartan.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Eprosartan.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Eprosartan.
Promazine Promazine may decrease the antihypertensive activities of Eprosartan.
Droperidol Droperidol may decrease the antihypertensive activities of Eprosartan.
Buspirone Buspirone may decrease the antihypertensive activities of Eprosartan.
Nortriptyline Nortriptyline may decrease the antihypertensive activities of Eprosartan.
Amoxapine Amoxapine may decrease the antihypertensive activities of Eprosartan.
Doxapram Doxapram may decrease the antihypertensive activities of Eprosartan.
Atropine Atropine may decrease the antihypertensive activities of Eprosartan.
Lisuride Lisuride may decrease the antihypertensive activities of Eprosartan.
Metaraminol Metaraminol may decrease the antihypertensive activities of Eprosartan.
Trazodone Trazodone may decrease the antihypertensive activities of Eprosartan.
Epinephrine Epinephrine may decrease the antihypertensive activities of Eprosartan.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Eprosartan.
Ergotamine Ergotamine may decrease the antihypertensive activities of Eprosartan.
Nicergoline Nicergoline may decrease the antihypertensive activities of Eprosartan.
Methoxamine Methoxamine may decrease the antihypertensive activities of Eprosartan.
Trimipramine Trimipramine may decrease the antihypertensive activities of Eprosartan.
Propiomazine Propiomazine may decrease the antihypertensive activities of Eprosartan.
Alfentanil Alfentanil may decrease the antihypertensive activities of Eprosartan.
Fentanyl Fentanyl may decrease the antihypertensive activities of Eprosartan.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Eprosartan.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Eprosartan.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Eprosartan.
Dobutamine Dobutamine may decrease the antihypertensive activities of Eprosartan.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Eprosartan.
Benzphetamine Benzphetamine may decrease the antihypertensive activities of Eprosartan.
Ritodrine Ritodrine may decrease the antihypertensive activities of Eprosartan.
Terbutaline Terbutaline may decrease the antihypertensive activities of Eprosartan.
Flupentixol Flupentixol may decrease the antihypertensive activities of Eprosartan.
Bitolterol Bitolterol may decrease the antihypertensive activities of Eprosartan.
Quinidine Quinidine may decrease the antihypertensive activities of Eprosartan.
Almotriptan Almotriptan may decrease the antihypertensive activities of Eprosartan.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Eprosartan.
Naratriptan Naratriptan may decrease the antihypertensive activities of Eprosartan.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Eprosartan.
Formoterol Formoterol may decrease the antihypertensive activities of Eprosartan.
Dopamine Dopamine may decrease the antihypertensive activities of Eprosartan.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Eprosartan.
Albuterol Salbutamol may decrease the antihypertensive activities of Eprosartan.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Eprosartan.
Ergoloid mesylate Ergoloid mesylate may decrease the antihypertensive activities of Eprosartan.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Eprosartan.
Arbutamine Arbutamine may decrease the antihypertensive activities of Eprosartan.
Dutasteride Dutasteride may decrease the antihypertensive activities of Eprosartan.
Doxepin Doxepin may decrease the antihypertensive activities of Eprosartan.
Nefazodone Nefazodone may decrease the antihypertensive activities of Eprosartan.
Desipramine Desipramine may decrease the antihypertensive activities of Eprosartan.
Pergolide Pergolide may decrease the antihypertensive activities of Eprosartan.
Finasteride Finasteride may decrease the antihypertensive activities of Eprosartan.
Ergometrine Ergometrine may decrease the antihypertensive activities of Eprosartan.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Eprosartan.
Paliperidone Paliperidone may decrease the antihypertensive activities of Eprosartan.
Arformoterol Arformoterol may decrease the antihypertensive activities of Eprosartan.
Fenoterol Fenoterol may decrease the antihypertensive activities of Eprosartan.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Eprosartan.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Eprosartan.
Ephedrine Ephedrine may decrease the antihypertensive activities of Eprosartan.
Mephentermine Mephentermine may decrease the antihypertensive activities of Eprosartan.
Procaterol Procaterol may decrease the antihypertensive activities of Eprosartan.
Yohimbine Yohimbine may decrease the antihypertensive activities of Eprosartan.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Eprosartan.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Eprosartan.

Target Protein

Type-1 angiotensin II receptor AGTR1

Referensi & Sumber

Synthesis reference: Richard T. Matsuoka, Peng Liu, "Process for preparing eprosartan using regioselective protection of 2,4-disubstituted-imidazole intermediates." U.S. Patent US6294675, issued June, 1992.
Artikel (PubMed)
  • PMID: 11800061
    Ruilope L, Jager B, Prichard B: Eprosartan versus enalapril in elderly patients with hypertension: a double-blind, randomized trial. Blood Press. 2001;10(4):223-9.
  • PMID: 12184062
    Hedner T: The clinical profile of the angiotensin II receptor blocker eprosartan. J Hypertens Suppl. 2002 Jun;20(5):S33-8.
  • PMID: 12766389
    Puig JG, Lopez MA, Bueso TS, Bernardino JI, Jimenez RT: Clinical profile of eprosartan. Cardiovasc Drugs Ther. 2002 Dec;16(6):543-9.
  • PMID: 12517247
    Ruilope L, Jager B: Eprosartan for the treatment of hypertension. Expert Opin Pharmacother. 2003 Jan;4(1):107-14.
  • PMID: 18093407
    de la Sierra A, Ram CV: Introduction: The pharmacological profile of eprosartan--implications for cerebrovascular and cardiovascular risk reduction. Curr Med Res Opin. 2007 Nov;23 Suppl 5:S1-3. doi: 10.1185/030079907X260692.
  • PMID: 18855637
    Blankestijn PJ, Rupp H: Clinical profile of eprosartan: a different angiotensin II receptor blocker. Cardiovasc Hematol Agents Med Chem. 2008 Oct;6(4):253-7.

Contoh Produk & Brand

Produk: 17 • International brands: 3
Produk
  • Eprosartan Mesylate
    Tablet, film coated • 400 mg/1 • Oral • US • Generic • Approved
  • Eprosartan Mesylate
    Tablet, film coated • 600 mg/1 • Oral • US • Generic • Approved
  • Teveten
    Tablet • 400 mg/1 • Oral • US • Approved
  • Teveten
    Tablet • 400 mg/1 • Oral • US • Approved
  • Teveten
    Tablet • 600 mg/1 • Oral • US • Approved
  • Teveten
    Tablet • 400 mg/1 • Oral • US • Approved
  • Teveten
    Tablet • 600 mg/1 • Oral • US • Approved
  • Teveten
    Tablet • 400 mg • Oral • Canada • Approved
Menampilkan 8 dari 17 produk.
International Brands
  • Eprozar — INTAS Pharmaceuticals
  • Futuran — Merck
  • Teveten

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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