Peringatan Keamanan

No maximum toxic doses have been established yet for azilsartan.A232863 There is limited human data available related to azilsartan medoxomil overdosage. In clinical trials, healthy subjects tolerated once-daily doses up to 320 mg of azilsartan medoxomil well. In the event of drug overdose, supportive measures should be initiated as azilsartan is not dialyzable.L32918

Azilsartan is a teratogenic agent with a risk of congenital abnormalities. Azilsartan and other ARB drugs are considered fetotoxic during the second and third trimesters.A232863,L32918

Azilsartan medoxomil

DB08822

small molecule approved investigational

Deskripsi

Azilsartan medoxomil is a prodrug that is broken down to azilsartan, which belongs in the angiotensin-receptor blocking (ARB) drug class. It is a selective AT1 subtype angiotensin II receptor antagonist. Azilsartan medoxomil is a relatively recently-developed antihypertensive drug that was first approved by the FDA in February 2011.A7354 Many guidelines recommend the use of ARBs as first-line therapy when initiating antihypertensive therapy and indicate that the clinical efficacy of ARBs is comparable to angiotensin-converting enzyme (ACE) inhibitors that are also used as first-line treatment for hypertension.A232863

Azilsartan medoxomil is marketed under the brand name Edarbi. It is used to treat hypertension as monotherapy or in combination with other antihypertensive drugs. It is also available in a combination product with chlorthalidone. As hypertension is a major risk factor for cardiovascular disease,A7354 early management of hypertension has several implications on patients' survival rate and quality of life in the future. Lowering blood pressure is associated with a reduced risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.L32918 Azilsartan medoxomil is thus speculated to lower mortality rates and the onset of cardiovascular disease. Although there is no clinical significance yet determined, azilsartan medoxomil may have potential off-label uses in patients with a history of myocardial infarction or heart failure.A232863

Struktur Molekul 2D

Berat 568.5336
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of azilsartan is approximately 11 hours.[L32918]
Volume Distribusi The volume of distribution of azilsartan is approximately 16 L. In rats, a minimal amount of radiolabelled drug crossed the blood-brain barrier. Azilsartan crossed the placental barrier in pregnant rats and was distributed to the fetus.[L32918]
Klirens (Clearance) Renal clearance of azilsartan is approximately 2.3 mL/min.[L32918]

Absorpsi

During absorption, azilsartan medoxomil is hydrolyzed to azilsartan. The parent drug is not detectable in plasma after oral administration. The absolute bioavailability of azilsartan is estimated to be 60%. Tmax ranges from 1.5 to three hours. Steady-state levels of azilsartan are achieved within five days, and no accumulation in plasma occurs with repeated once-daily dosing.L32918

Metabolisme

After azilsartan medoxomil is hydrolyzed into its active metabolite, azilsartan is metabolized to two primary metabolites, which are pharmacologically inactive. The major metabolite in plasma is metabolite M-II, which is formed via O-dealkylation mediated by CYP2C9. The minor metabolite is metabolite M-I, which is formed via decarboxylation mediated by CYP2C8 and CYP2B6. MII has approximately 50% systemic exposure of azilsartan, and MI has less than 1% systemic exposure of azilsartan.A232910,L32918

Rute Eliminasi

Following oral administration of 14C-labeled azilsartan medoxomil, approximately 55% of radioactivity was recovered in feces and approximately 42% in urine. Of the recovered dose in urine, about 15% was excreted as azilsartan.L32918

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food does not affect the bioavailability.

Interaksi Obat

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

Target Protein

Type-1 angiotensin II receptor AGTR1

Referensi & Sumber

Synthesis reference: Kohara Y, Kubo K, Imamiya E, Wada T, Inada Y, Naka T: Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisosteres. J Med Chem. 1996 Dec 20;39(26):5228-35.
Artikel (PubMed)
  • PMID: 22346296
    Jones JD, Jackson SH, Agboton C, Martin TS: Azilsartan Medoxomil (Edarbi): The Eighth Angiotensin II Receptor Blocker. P T. 2011 Oct;36(10):634-40.
  • PMID: 22399858
    Kurtz TW, Kajiya T: Differential pharmacology and benefit/risk of azilsartan compared to other sartans. Vasc Health Risk Manag. 2012;8:133-43. doi: 10.2147/VHRM.S22595. Epub 2012 Feb 28.
  • PMID: 30860708
    Hardin MD, Jacobs TF: Azilsartan .
  • PMID: 31885897
    Pradhan A, Tiwari A, Sethi R: Azilsartan: Current Evidence and Perspectives in Management of Hypertension. Int J Hypertens. 2019 Nov 3;2019:1824621. doi: 10.1155/2019/1824621. eCollection 2019.
  • PMID: 22661897
    De Caterina AR, Harper AR, Cuculi F: Critical evaluation of the efficacy and tolerability of azilsartan. Vasc Health Risk Manag. 2012;8:299-305. doi: 10.2147/VHRM.S22589. Epub 2012 May 14.

Contoh Produk & Brand

Produk: 46 • International brands: 0
Produk
  • Edarbi
    Tablet • 40 mg/1 • Oral • US • Approved
  • Edarbi
    Tablet • 80 mg/1 • Oral • US • Approved
  • Edarbi
    Tablet • 40 mg • Oral • Canada • Approved
  • Edarbi
    Tablet • 80 mg • Oral • Canada • Approved
  • Edarbi
    Tablet • 40 mg/1 • Oral • US • Approved
  • Edarbi
    Tablet • 80 mg/1 • Oral • US • Approved
  • Edarbi
    Tablet • 20 mg • Oral • EU • Approved
  • Edarbi
    Tablet • 20 mg • Oral • EU • Approved
Menampilkan 8 dari 46 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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