Peringatan Keamanan

No lethality was observed in acute toxicity studies in mice, rats and dogs given single oral doses of up to 2000 mg/kg of candesartan cilexetil or in rats given single oral doses of up to 2000 mg/kg of candesartan cilexetil in combination with 1000 mg/kg of hydrochlorothiazide. In mice given single oral doses of the primary metabolite, candesartan, the minimum lethal dose was greater than 1000 mg/kg but less than 2000 mg/kg.

Candesartan cilexetil

DB00796

small molecule approved

Deskripsi

Candesartan is an angiotensin-receptor blocker (ARB) that may be used alone or with other agents to treat hypertension. It is administered orally as the prodrug, candesartan cilexetil, which is rapidly converted to its active metabolite, candesartan, during absorption in the gastrointestinal tract. Candesartan lowers blood pressure by antagonizing the renin-angiotensin-aldosterone system (RAAS); it competes with angiotensin II for binding to the type-1 angiotensin II receptor (AT1) subtype and prevents the blood pressure increasing effects of angiotensin II. Unlike angiotensin-converting enzyme (ACE) inhibitors, ARBs do not have the adverse effect of dry cough. Candesartan may be used to treat hypertension, isolated systolic hypertension, left ventricular hypertrophy and diabetic nephropathy. It may also be used as an alternative agent for the treatment of heart failure, systolic dysfunction, myocardial infarction and coronary artery disease.

Struktur Molekul 2D

Berat 610.671
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Approximately 9 hours.
Volume Distribusi * 0.13 L/kg
Klirens (Clearance) * 0.37 mL/min/kg

Absorpsi

Following administration of the candesartan cilexetil prodrug, the absolute bioavailability of candesartan was estimated to be 15%. Food with a high fat content has no effect on the bioavailability of candesartan from candesartan cilexetil.

Metabolisme

The prodrug candesartan cilexetil undergoes rapid and complete ester hydrolysis in the intestinal wall to form the active drug, candesartan. Elimination of candesartan is primarily as unchanged drug in the urine and, by the biliary route, in the feces. Minor hepatic metabolism of candesartan (<20%) occurs by O-deethylation via cytochrome P450 2C9 to form an inactive metabolite. Candesartan undergoes N-glucuronidation in the tetrazole ring by uridine diphosphate glucuronosyltransferase 1A3 (UGT1A3). O-glucuronidation may also occur. 75% of candesartan is excreted as unchanged drug in urine and feces.

Rute Eliminasi

When candesartan is administered orally, about 26% of the dose is excreted unchanged in urine. Candesartan is mainly excreted unchanged in urine and feces (via bile).

Interaksi Makanan

2 Data
  • 1. Take at the same time every day.
  • 2. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1040 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Candesartan cilexetil is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Candesartan cilexetil is combined with Levodopa.
Risperidone Candesartan cilexetil may increase the hypotensive activities of Risperidone.
Alfuzosin Alfuzosin may increase the hypotensive activities of Candesartan cilexetil.
Aliskiren The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Candesartan cilexetil.
Amifostine Candesartan cilexetil 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 Candesartan cilexetil.
Diazoxide Diazoxide may increase the hypotensive activities of Candesartan cilexetil.
Drospirenone The risk or severity of hyperkalemia can be increased when Candesartan cilexetil is combined with Drospirenone.
Semuloparin The risk or severity of hyperkalemia can be increased when Semuloparin is combined with Candesartan cilexetil.
Lithium citrate The serum concentration of Lithium citrate can be increased when it is combined with Candesartan cilexetil.
Lithium carbonate The serum concentration of Lithium carbonate can be increased when it is combined with Candesartan cilexetil.
Lithium hydroxide The serum concentration of Lithium hydroxide can be increased when it is combined with Candesartan cilexetil.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Candesartan cilexetil.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Candesartan cilexetil.
Obinutuzumab Candesartan cilexetil may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Candesartan cilexetil.
Rituximab Candesartan cilexetil may increase the hypotensive activities of Rituximab.
Tolvaptan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Candesartan cilexetil.
Trimethoprim The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Candesartan cilexetil.
Desmopressin Desmopressin may decrease the antihypertensive activities of Candesartan cilexetil.
Phentermine Phentermine may decrease the antihypertensive activities of Candesartan cilexetil.
Midodrine Midodrine may decrease the antihypertensive activities of Candesartan cilexetil.
Isoetharine Isoetharine may decrease the antihypertensive activities of Candesartan cilexetil.
Methysergide Methysergide may decrease the antihypertensive activities of Candesartan cilexetil.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Candesartan cilexetil.
Etomidate Etomidate may decrease the antihypertensive activities of Candesartan cilexetil.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Candesartan cilexetil.
Dihydroergotamine Dihydroergotamine may decrease the antihypertensive activities of Candesartan cilexetil.
Protriptyline Protriptyline may decrease the antihypertensive activities of Candesartan cilexetil.
Methylergometrine Methylergometrine may decrease the antihypertensive activities of Candesartan cilexetil.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Candesartan cilexetil.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Candesartan cilexetil.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Candesartan cilexetil.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Candesartan cilexetil.
Droperidol Droperidol may decrease the antihypertensive activities of Candesartan cilexetil.
Buspirone Buspirone may decrease the antihypertensive activities of Candesartan cilexetil.
Nortriptyline Nortriptyline may decrease the antihypertensive activities of Candesartan cilexetil.
Amoxapine Amoxapine may decrease the antihypertensive activities of Candesartan cilexetil.
Doxapram Doxapram may decrease the antihypertensive activities of Candesartan cilexetil.
Atropine Atropine may decrease the antihypertensive activities of Candesartan cilexetil.
Lisuride Lisuride may decrease the antihypertensive activities of Candesartan cilexetil.
Metaraminol Metaraminol may decrease the antihypertensive activities of Candesartan cilexetil.
Trazodone Trazodone may decrease the antihypertensive activities of Candesartan cilexetil.
Ergotamine Ergotamine may decrease the antihypertensive activities of Candesartan cilexetil.
Nicergoline Nicergoline may decrease the antihypertensive activities of Candesartan cilexetil.
Methoxamine Methoxamine may decrease the antihypertensive activities of Candesartan cilexetil.
Propiomazine Propiomazine may decrease the antihypertensive activities of Candesartan cilexetil.
Alfentanil Alfentanil may decrease the antihypertensive activities of Candesartan cilexetil.
Fentanyl Fentanyl may decrease the antihypertensive activities of Candesartan cilexetil.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Candesartan cilexetil.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Candesartan cilexetil.
Dobutamine Dobutamine may decrease the antihypertensive activities of Candesartan cilexetil.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Candesartan cilexetil.
Benzphetamine Benzphetamine may decrease the antihypertensive activities of Candesartan cilexetil.
Ritodrine Ritodrine may decrease the antihypertensive activities of Candesartan cilexetil.
Terbutaline Terbutaline may decrease the antihypertensive activities of Candesartan cilexetil.
Bitolterol Bitolterol may decrease the antihypertensive activities of Candesartan cilexetil.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Candesartan cilexetil.
Salmeterol Salmeterol may decrease the antihypertensive activities of Candesartan cilexetil.
Naratriptan Naratriptan may decrease the antihypertensive activities of Candesartan cilexetil.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Candesartan cilexetil.
Dopamine Dopamine may decrease the antihypertensive activities of Candesartan cilexetil.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Candesartan cilexetil.
Albuterol Salbutamol may decrease the antihypertensive activities of Candesartan cilexetil.
Ergoloid mesylate Ergoloid mesylate may decrease the antihypertensive activities of Candesartan cilexetil.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Candesartan cilexetil.
Arbutamine Arbutamine may decrease the antihypertensive activities of Candesartan cilexetil.
Dutasteride Dutasteride may decrease the antihypertensive activities of Candesartan cilexetil.
Nefazodone Nefazodone may decrease the antihypertensive activities of Candesartan cilexetil.
Desipramine Desipramine may decrease the antihypertensive activities of Candesartan cilexetil.
Pergolide Pergolide may decrease the antihypertensive activities of Candesartan cilexetil.
Finasteride Finasteride may decrease the antihypertensive activities of Candesartan cilexetil.
Ergometrine Ergometrine may decrease the antihypertensive activities of Candesartan cilexetil.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoterol Fenoterol may decrease the antihypertensive activities of Candesartan cilexetil.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Candesartan cilexetil.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Candesartan cilexetil.
Ephedrine Ephedrine may decrease the antihypertensive activities of Candesartan cilexetil.
Mephentermine Mephentermine may decrease the antihypertensive activities of Candesartan cilexetil.
Procaterol Procaterol may decrease the antihypertensive activities of Candesartan cilexetil.
Yohimbine Yohimbine may decrease the antihypertensive activities of Candesartan cilexetil.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Candesartan cilexetil.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Candesartan cilexetil.
Bambuterol Bambuterol may decrease the antihypertensive activities of Candesartan cilexetil.
MMDA MMDA may decrease the antihypertensive activities of Candesartan cilexetil.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Candesartan cilexetil.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Candesartan cilexetil.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Candesartan cilexetil.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Candesartan cilexetil.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Candesartan cilexetil.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Candesartan cilexetil.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Candesartan cilexetil.
Metamfetamine Metamfetamine may decrease the antihypertensive activities of Candesartan cilexetil.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Candesartan cilexetil.
Solifenacin Solifenacin may decrease the antihypertensive activities of Candesartan cilexetil.
Periciazine Periciazine may decrease the antihypertensive activities of Candesartan cilexetil.
Acepromazine Acepromazine may decrease the antihypertensive activities of Candesartan cilexetil.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Candesartan cilexetil.
Zuclopenthixol Zuclopenthixol may decrease the antihypertensive activities of Candesartan cilexetil.

Target Protein

Type-1 angiotensin II receptor AGTR1

Referensi & Sumber

Synthesis reference: Marina Etinger, Boris Fedotev, Ben-Zion Dolitzky, "Preparation of candesartan cilexetil." U.S. Patent US20050131037, issued June 16, 2005.
Artikel (PubMed)
  • PMID: 13678868
    Pfeffer MA, Swedberg K, Granger CB, Held P, McMurray JJ, Michelson EL, Olofsson B, Ostergren J, Yusuf S, Pocock S: Effects of candesartan on mortality and morbidity in patients with chronic heart failure: the CHARM-Overall programme. Lancet. 2003 Sep 6;362(9386):759-66.
  • PMID: 19563275
    Mendis B, Page SR: Candesartan: widening indications for this angiotensin II receptor blocker? Expert Opin Pharmacother. 2009 Aug;10(12):1995-2007. doi: 10.1517/14656560903092197.
  • PMID: 19436650
    Baguet JP, Barone-Rochette G, Neuder Y: Candesartan cilexetil in the treatment of chronic heart failure. Vasc Health Risk Manag. 2009;5(1):257-64. Epub 2009 Apr 8.
Textbook
  • ISBN: 978-0321556660
    Stanfield, Cindy L.;Germann, William J. (2009). Principles of Human Physiology (3rd ed.). Benjamin-Cummings Publishing Company.
  • ISBN: 9783540298328
    Bader, M. (2004). Renin-angiotensin-aldosterone system. In Encyclopedic reference of molecular pharmacology (pp. 810-814). Berlin: Springer.

Contoh Produk & Brand

Produk: 287 • International brands: 2
Produk
  • Accel-candesartan
    Tablet • 4 mg • Oral • Canada • Generic • Approved
  • Accel-candesartan
    Tablet • 8 mg • Oral • Canada • Generic • Approved
  • Accel-candesartan
    Tablet • 16 mg • Oral • Canada • Generic • Approved
  • Accel-candesartan
    Tablet • 32 mg • Oral • Canada • Generic • Approved
  • Accel-candesartan/hctz
    Tablet • - • Oral • Canada • Generic • Approved
  • Accel-candesartan/hctz
    Tablet • - • Oral • Canada • Generic • Approved
  • Accel-candesartan/hctz
    Tablet • - • Oral • Canada • Generic • Approved
  • Ach-candesartan
    Tablet • 8 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 287 produk.
International Brands
  • Amias — Eureco (Netherlands), Takeda (United Kingdom)
  • Blopress — Takeda

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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