Peringatan Keamanan

The reported LD50 of olmesartan in dogs was reported to be greater of 1500 mg/kg. Overdose is expressed as hypotension, tachycardia, and bradycardia when there is parasympathetic stimulation. In case of overdose, supportive treatment is recommended.FDA label

Olmesartan was shown to be safe on carcinogenic and fertility studies. However, in in vitro mutagenic studies showed a potential to induce chromosomal aberrations in cells and it tested positive for thymidine kinase mutations in the mouse lymphoma assay.FDA label

Olmesartan

DB00275

small molecule approved investigational

Deskripsi

Olmesartan belongs to the angiotensin II receptor blocker (ARB) family of drugs, which also includes telmisartan, candesartan, losartan, valsartan, and irbesartan. ARBs selectively bind to angiotensin receptor 1 (AT1) and prevent the protein angiotensin II from binding and exerting its hypertensive effects, which include vasoconstriction, stimulation and synthesis of aldosterone and ADH, cardiac stimulation, and renal reabsorption of sodium, among others. Overall, olmesartan's physiologic effects lead to reduced blood pressure, lower aldosterone levels, reduced cardiac activity, and increased excretion of sodium.

Olmesartan also affects the renin-angiotensin aldosterone system (RAAS), which plays an important role in hemostasis and regulation of kidney, vascular, and cardiac functions. Pharmacological blockade of RAAS via AT1 receptor blockade inhibits negative regulatory feedback within RAAS, which is a contributing factor to the pathogenesis and progression of cardiovascular disease, heart failure, and renal disease. In particular, heart failure is associated with chronic activation of RAAS, leading to inappropriate fluid retention, vasoconstriction, and ultimately a further decline in left ventricular function. ARBs have been shown to have a protective effect on the heart by improving cardiac function, reducing afterload, increasing cardiac output and preventing ventricular hypertrophy and remodelling.A174154

By comparison, the angiotensin-converting enzyme inhibitor (ACEi) class of medications (which includes drugs such as ramipril, lisinopril, and perindopril) inhibit the conversion of angiotensin I to angiotensin II through inhibition of the ACE enzyme. However, this does not prevent the formation of all angiotensin II within the body. The angiotensin II receptor blocker (ARB) family of drugs unique in that it blocks all angiotensin II activity, regardless of where or how it was synthesized.

Olmesartan is commonly used for the management of hypertension and Type 2 Diabetes-associated nephropathy, particularly in patients who are unable to tolerate ACE inhibitors. ARBs such as olmesartan have been shown in a number of large-scale clinical outcomes trials to improve cardiovascular outcomes including reducing risk of myocardial infarction, stroke, the progression of heart failure, and hospitalization.A174124,A178153,A173869,A185324,A185327,A185333,A185342,A185345 Like other ARBs, olmesartan blockade of RAAS slows the progression of diabetic nephropathy due to its renoprotective effects.A185906,A185909,A185912

Orally available olmesartan is produced as the prodrug olmesartan medoxomil which is rapidly converted in vivo to the pharmacologically active olmesartan.A175330 It was developed by Daiichi Sankyo Pharmaceuticals and approved in 2002.A175345, L12882

Struktur Molekul 2D

Berat 446.5016
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean plasma olmesartan half-life is reported to be from 10-15 hours after multiple oral administration.[A175330]
Volume Distribusi 17 L[L5566]
Klirens (Clearance) Total plasma clearance is 1.3 L/h and the renal clearance is 0.6 L/h.[L5566]

Absorpsi

When taken orally, the prodrug olmesartan medoxomil is rapidly absorbed in the gastrointestinal tract and metabolized to olmesartan. The esterification with medoxomil was created with the intention of increasing olmesartan bioavailability from 4.5% to 28.6%.A175330 Oral administration of 10-160 mg of olmesartan has been shown to reach peak plasma concentration of 0.22-2.1 mg/L after 1-3 hours with an AUC of 1.6-19.9mgh/L.A175342 The pharmacokinetic profile of olmesartan has been observed to be nearly linear and dose-dependent under the therapeutic range.A175330 The steady-state level of olmesartan is achieved after once a day dosing during 3 to 5 days.L5566

Metabolisme

Olmesartan medoxomil is rapidly and completely bioactivated by ester hydrolysis to olmesartan during absorption from the gastrointestinal tract. This rapid first-pass metabolism was confirmed by the lack of measurable amounts of olmesartan medoxomil in plasma or excreta.A175330 This first-pass metabolism is not driven by cytochrome enzymes and hence it is not expected to interact with other drugs via this mechanism.A175342 The pharmacologically active moiety does not appear to undergo further metabolism.A175330,L12882

Rute Eliminasi

The main elimination route of olmesartan is in the unchanged form through the feces. From the systemically bioavailable dose, about 10-16% is eliminated in the urine.A175330

Interaksi Makanan

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

Interaksi Obat

814 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Olmesartan is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Olmesartan is combined with Levodopa.
Risperidone Olmesartan may increase the hypotensive activities of Risperidone.
Dipyridamole Olmesartan may decrease the excretion rate of Dipyridamole which could result in a higher serum level.
Nifedipine Olmesartan may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Erythromycin Olmesartan may decrease the excretion rate of Erythromycin which could result in a higher serum level.
Tipranavir Olmesartan may decrease the excretion rate of Tipranavir which could result in a higher serum level.
Glyburide Olmesartan may decrease the excretion rate of Glyburide which could result in a higher serum level.
Ketoconazole Olmesartan may decrease the excretion rate of Ketoconazole which could result in a higher serum level.
Ursodeoxycholic acid Olmesartan may decrease the excretion rate of Ursodeoxycholic acid which could result in a higher serum level.
Cholic Acid Olmesartan may decrease the excretion rate of Cholic Acid which could result in a higher serum level.
Pravastatin Olmesartan may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Fluvoxamine Olmesartan may decrease the excretion rate of Fluvoxamine which could result in a higher serum level.
Nelfinavir Olmesartan may decrease the excretion rate of Nelfinavir which could result in a higher serum level.
Glimepiride Olmesartan may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Indinavir Olmesartan may decrease the excretion rate of Indinavir which could result in a higher serum level.
Ranolazine Olmesartan may decrease the excretion rate of Ranolazine which could result in a higher serum level.
Diethylstilbestrol Olmesartan may decrease the excretion rate of Diethylstilbestrol which could result in a higher serum level.
Isradipine Olmesartan may decrease the excretion rate of Isradipine which could result in a higher serum level.
Flucloxacillin Olmesartan may decrease the excretion rate of Flucloxacillin which could result in a higher serum level.
Atenolol Olmesartan may decrease the excretion rate of Atenolol which could result in a higher serum level.
Terfenadine Olmesartan may decrease the excretion rate of Terfenadine which could result in a higher serum level.
Rosiglitazone Olmesartan may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Cerivastatin Olmesartan may decrease the excretion rate of Cerivastatin which could result in a higher serum level.
Loratadine Olmesartan may decrease the excretion rate of Loratadine which could result in a higher serum level.
Ritonavir Olmesartan may decrease the excretion rate of Ritonavir which could result in a higher serum level.
Atropine Olmesartan may decrease the excretion rate of Atropine which could result in a higher serum level.
Imatinib Olmesartan may decrease the excretion rate of Imatinib which could result in a higher serum level.
Nicardipine Olmesartan may decrease the excretion rate of Nicardipine which could result in a higher serum level.
Efavirenz Olmesartan may decrease the excretion rate of Efavirenz which could result in a higher serum level.
Simvastatin Olmesartan may decrease the excretion rate of Simvastatin which could result in a higher serum level.
Fluorescein Olmesartan may decrease the excretion rate of Fluorescein which could result in a higher serum level.
Nitrofurantoin Olmesartan may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.
Disulfiram Olmesartan may decrease the excretion rate of Disulfiram which could result in a higher serum level.
Cefaclor Olmesartan may decrease the excretion rate of Cefaclor which could result in a higher serum level.
Mifepristone Olmesartan may decrease the excretion rate of Mifepristone which could result in a higher serum level.
Tinidazole Olmesartan may decrease the excretion rate of Tinidazole which could result in a higher serum level.
Repaglinide Olmesartan may decrease the excretion rate of Repaglinide which could result in a higher serum level.
Ezetimibe Olmesartan may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Sulfamethoxazole Olmesartan may decrease the excretion rate of Sulfamethoxazole which could result in a higher serum level.
Felodipine Olmesartan may decrease the excretion rate of Felodipine which could result in a higher serum level.
Fenofibrate Olmesartan may decrease the excretion rate of Fenofibrate which could result in a higher serum level.
Nitrendipine Olmesartan may decrease the excretion rate of Nitrendipine which could result in a higher serum level.
Glipizide Olmesartan may decrease the excretion rate of Glipizide which could result in a higher serum level.
Atazanavir Olmesartan may decrease the excretion rate of Atazanavir which could result in a higher serum level.
Atorvastatin Olmesartan may decrease the excretion rate of Atorvastatin which could result in a higher serum level.
Sulfinpyrazone Olmesartan may decrease the excretion rate of Sulfinpyrazone which could result in a higher serum level.
Nefazodone Olmesartan may decrease the excretion rate of Nefazodone which could result in a higher serum level.
Ofloxacin Olmesartan may decrease the excretion rate of Ofloxacin which could result in a higher serum level.
Clarithromycin Olmesartan may decrease the excretion rate of Clarithromycin which could result in a higher serum level.
Budesonide Olmesartan may decrease the excretion rate of Budesonide which could result in a higher serum level.
Saquinavir Olmesartan may decrease the excretion rate of Saquinavir which could result in a higher serum level.
Glycochenodeoxycholic Acid Olmesartan may decrease the excretion rate of Glycochenodeoxycholic Acid which could result in a higher serum level.
Taurocholic acid Olmesartan may decrease the excretion rate of Taurocholic acid which could result in a higher serum level.
Prasterone sulfate Olmesartan may decrease the excretion rate of Prasterone sulfate which could result in a higher serum level.
Indocyanine green acid form Olmesartan may decrease the excretion rate of Indocyanine green acid form which could result in a higher serum level.
Benzbromarone Olmesartan may decrease the excretion rate of Benzbromarone which could result in a higher serum level.
Pilsicainide Olmesartan may decrease the excretion rate of Pilsicainide which could result in a higher serum level.
Dihydroergocristine Olmesartan may decrease the excretion rate of Dihydroergocristine which could result in a higher serum level.
Glycyrrhizic acid Olmesartan may decrease the excretion rate of Glycyrrhizic acid which could result in a higher serum level.
Belantamab mafodotin Olmesartan may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Alfuzosin Alfuzosin may increase the hypotensive activities of Olmesartan.
Aliskiren The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Olmesartan.
Amifostine Olmesartan 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 Olmesartan.
Diazoxide Diazoxide may increase the hypotensive activities of Olmesartan.
Drospirenone The risk or severity of hyperkalemia can be increased when Olmesartan is combined with Drospirenone.
Eplerenone The risk or severity of hyperkalemia can be increased when Eplerenone is combined with Olmesartan.
Semuloparin The risk or severity of hyperkalemia can be increased when Semuloparin is combined with Olmesartan.
Lithium citrate The serum concentration of Lithium citrate can be increased when it is combined with Olmesartan.
Lithium carbonate The serum concentration of Lithium carbonate can be increased when it is combined with Olmesartan.
Lithium hydroxide The serum concentration of Lithium hydroxide can be increased when it is combined with Olmesartan.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Olmesartan.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Olmesartan.
Obinutuzumab Olmesartan may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Olmesartan.
Rituximab Olmesartan may increase the hypotensive activities of Rituximab.
Tolvaptan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Olmesartan.
Trimethoprim The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Olmesartan.
Desmopressin Desmopressin may decrease the antihypertensive activities of Olmesartan.
Phentermine Phentermine may decrease the antihypertensive activities of Olmesartan.
Midodrine Midodrine may decrease the antihypertensive activities of Olmesartan.
Eletriptan Eletriptan may decrease the antihypertensive activities of Olmesartan.
Isoetharine Isoetharine may decrease the antihypertensive activities of Olmesartan.
Methysergide Methysergide may decrease the antihypertensive activities of Olmesartan.
Cabergoline Cabergoline may decrease the antihypertensive activities of Olmesartan.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Olmesartan.
Etomidate Etomidate may decrease the antihypertensive activities of Olmesartan.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Olmesartan.
Dihydroergotamine Dihydroergotamine may decrease the antihypertensive activities of Olmesartan.
Amitriptyline Amitriptyline may decrease the antihypertensive activities of Olmesartan.
Protriptyline Protriptyline may decrease the antihypertensive activities of Olmesartan.
Methylergometrine Methylergometrine may decrease the antihypertensive activities of Olmesartan.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Olmesartan.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Olmesartan.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Olmesartan.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Olmesartan.
Promazine Promazine may decrease the antihypertensive activities of Olmesartan.
Droperidol Droperidol may decrease the antihypertensive activities of Olmesartan.
Buspirone Buspirone may decrease the antihypertensive activities of Olmesartan.

Target Protein

Type-1 angiotensin II receptor AGTR1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 11967728
    Brunner HR: The new oral angiotensin II antagonist olmesartan medoxomil: a concise overview. J Hum Hypertens. 2002 May;16 Suppl 2:S13-6. doi: 10.1038/sj.jhh.1001391.
  • PMID: 17323586
    Brunner HR: Olmesartan medoxomil: current status of its use in monotherapy. Vasc Health Risk Manag. 2006;2(4):327-40.
  • PMID: 30683835
    Gonakoti S, Khullar S, Rajkumar A: Olmesartan Associated Enteropathy: A Rare Underdiagnosed Cause of Diarrhea and Weight Loss. Am J Case Rep. 2019 Jan 26;20:111-116. doi: 10.12659/AJCR.913207.
  • PMID: 22538956
    Akazawa H, Yabumoto C, Yano M, Kudo-Sakamoto Y, Komuro I: ARB and cardioprotection. Cardiovasc Drugs Ther. 2013 Apr;27(2):155-60. doi: 10.1007/s10557-012-6392-2.
  • PMID: 19911855
    Black HR, Bailey J, Zappe D, Samuel R: Valsartan: more than a decade of experience. Drugs. 2009;69(17):2393-414. doi: 10.2165/11319460-000000000-00000.
  • PMID: 29111106
    Ezekowitz JA, O'Meara E, McDonald MA, Abrams H, Chan M, Ducharme A, Giannetti N, Grzeslo A, Hamilton PG, Heckman GA, Howlett JG, Koshman SL, Lepage S, McKelvie RS, Moe GW, Rajda M, Swiggum E, Virani SA, Zieroth S, Al-Hesayen A, Cohen-Solal A, D'Astous M, De S, Estrella-Holder E, Fremes S, Green L, Haddad H, Harkness K, Hernandez AF, Kouz S, LeBlanc MH, Masoudi FA, Ross HJ, Roussin A, Sussex B: 2017 Comprehensive Update of the Canadian Cardiovascular Society Guidelines for the Management of Heart Failure. Can J Cardiol. 2017 Nov;33(11):1342-1433. doi: 10.1016/j.cjca.2017.08.022. Epub 2017 Sep 6.
  • PMID: 28449828
    Leung AA, Daskalopoulou SS, Dasgupta K, McBrien K, Butalia S, Zarnke KB, Nerenberg K, Harris KC, Nakhla M, Cloutier L, Gelfer M, Lamarre-Cliche M, Milot A, Bolli P, Tremblay G, McLean D, Tran KC, Tobe SW, Ruzicka M, Burns KD, Vallee M, Prasad GVR, Gryn SE, Feldman RD, Selby P, Pipe A, Schiffrin EL, McFarlane PA, Oh P, Hegele RA, Khara M, Wilson TW, Penner SB, Burgess E, Sivapalan P, Herman RJ, Bacon SL, Rabkin SW, Gilbert RE, Campbell TS, Grover S, Honos G, Lindsay P, Hill MD, Coutts SB, Gubitz G, Campbell NRC, Moe GW, Howlett JG, Boulanger JM, Prebtani A, Kline G, Leiter LA, Jones C, Cote AM, Woo V, Kaczorowski J, Trudeau L, Tsuyuki RT, Hiremath S, Drouin D, Lavoie KL, Hamet P, Gregoire JC, Lewanczuk R, Dresser GK, Sharma M, Reid D, Lear SA, Moullec G, Gupta M, Magee LA, Logan AG, Dionne J, Fournier A, Benoit G, Feber J, Poirier L, Padwal RS, Rabi DM: Hypertension Canada's 2017 Guidelines for Diagnosis, Risk Assessment, Prevention, and Treatment of Hypertension in Adults. Can J Cardiol. 2017 May;33(5):557-576. doi: 10.1016/j.cjca.2017.03.005. Epub 2017 Mar 10.
  • PMID: 15520426
    Lee VC, Rhew DC, Dylan M, Badamgarav E, Braunstein GD, Weingarten SR: Meta-analysis: angiotensin-receptor blockers in chronic heart failure and high-risk acute myocardial infarction. Ann Intern Med. 2004 Nov 2;141(9):693-704. doi: 10.7326/0003-4819-141-9-200411020-00011.
Menampilkan 8 dari 16 artikel.

Contoh Produk & Brand

Produk: 493 • International brands: 6
Produk
  • Ach-olmesartan
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Ach-olmesartan
    Tablet • 40 mg • Oral • Canada • Generic • Approved
  • Ach-olmesartan Hctz
    Tablet • - • Oral • Canada • Generic • Approved
  • Ach-olmesartan Hctz
    Tablet • - • Oral • Canada • Generic • Approved
  • Ach-olmesartan Hctz
    Tablet • - • Oral • Canada • Generic • Approved
  • Ag-olmesartan
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Ag-olmesartan
    Tablet • 40 mg • Oral • Canada • Generic • Approved
  • Ag-olmesartan Hctz
    Tablet • - • Oral • Canada • Generic • Approved
Menampilkan 8 dari 493 produk.
International Brands
  • Erastapex — Apex Pharma
  • Golme — Golgi USA Research Laboratories Ltd
  • Olmy — Zydus Cadila
  • Olsar — Unichem Laboratories
  • Olvance — Ranbaxy Laboratories Ltd
  • WinBP — Abbott Healthcare Pvt Ltd

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