Peringatan Keamanan

The oral TDLO in mice is 1000mg/kg and in rats is 2000mg/kg.L7423,L7426 In humans the TDLO for men is 10mg/kg/2W and for women is 1mg/kg/1D.L7441

Symptoms of overdose are likely to include hypotension, tachycardia, or bradycardia due to vagal stimulation.L7423,L7426 Supportive treatment should be instituted for symptomatic hypotension.L7423,L7426 Hemodialysis will not remove losartan or its active metabolite due to their high rates of protein binding.L7423,L7426

Losartan

DB00678

small molecule approved

Deskripsi

Losartan is an angiotensin II receptor blocker (ARB) used to treat hypertension.L7423 Angiotensin-converting enzyme (ACE) inhibitors are used for a similar indication but are associated with a cough.L7423 When patients with ACE inhibitor associated coughs are switched to ARBs like losartan, they have an incidence of cough similar to placebo or hydrochlorothiazide.L7423 Losartan is available as losartan potassium oral tablets as well as a combination tablet of losartan potassium and hydrochlorothiazide.L7423,L7426 Patients taking losartan should have their renal function and potassium levels monitored.L7423 Losartan was granted FDA approval on 14 April 1995.L7423

Struktur Molekul 2D

Berat 422.911
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half life of losartan is 1.5-2.5 hours while the active metabolite has a half life of 6-9 hours.[A1033]
Volume Distribusi The volume of distribution of losartan is 34.4±17.9L and 10.3±1.1L for the active metabolite (E-3174).[A1033]
Klirens (Clearance) Losartan has a total plasma clearance of 600mL/min and a renal clearance of 75mL/min.[A1033] E-3174, the active metabolite, has a total plasma clearance of 50mL/min and a renal clearance of 25mL/min.[A1033]

Absorpsi

Losartan is approximately 33% orally bioavailable.A1033,L7423,L7426 Losartan has a Tmax of 1 hour and the active metabolite has a Tmax of 3-4 hours.A1033,L7423,L7426 Taking losartan with food decreases the Cmax but does only results in a 10% decrease in the AUC of losartan and its active metabolite.A1033,L7423,L7426 A 50-80mg oral dose of losartan leads to a Cmax of 200-250ng/mL.A1033

Metabolisme

Losartan is metabolized to an aldehyde intermediate, E-3179, which is further metabolized to a carboxylic acid, E-3174, by cytochrome P450s like CYP2C9.A1033 Losartan can also be hydroxylated to an inactive metabolite, P1.A1033 Approximately 14% of losartan is metabolized to E-3174.A1033 Losartan can be metabolized by CYP3A4, CYP2C9, and CYP2C10.A1033 Losartan can also be glucuronidated by UGT1A1, UGT1A3, UGT1A10, UGT2B7, and UGT 2B17.A415

Rute Eliminasi

A single oral dose of losartan leads to 4% recovery in the urine as unchanged losartan, 6% in the urine as the active metabolite.L7423,L7426 Oral radiolabelled losartan is 35% recovered in urine and 60% in feces.L7423,L7426 Intravenous radiolabelled losartan is 45% recovered in urine and 50% in feces.L7423,L7426

Interaksi Makanan

2 Data
  • 1. Take at the same time every day.
  • 2. Take with or without food. Food delays absorption, but does not affect the extent of absorption.

Interaksi Obat

1129 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Losartan is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Losartan is combined with Levodopa.
Risperidone Losartan may increase the hypotensive activities of Risperidone.
Reserpine Reserpine may increase the hypotensive activities of Losartan.
Progesterone The metabolism of Losartan can be decreased when combined with Progesterone.
Chlorpromazine Chlorpromazine may decrease the antihypertensive activities of Losartan.
Cimetidine The metabolism of Losartan can be decreased when combined with Cimetidine.
Bosentan The metabolism of Losartan can be increased when combined with Bosentan.
Glyburide The metabolism of Losartan can be decreased when combined with Glyburide.
Fusidic acid The metabolism of Losartan can be decreased when combined with Fusidic acid.
Simeprevir The metabolism of Losartan can be decreased when combined with Simeprevir.
Erythromycin The serum concentration of Losartan can be increased when it is combined with Erythromycin.
Pralsetinib The metabolism of Losartan can be decreased when combined with Pralsetinib.
Aliskiren The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Losartan.
Amifostine Losartan 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 Losartan.
Diazoxide Diazoxide may increase the hypotensive activities of Losartan.
Drospirenone The risk or severity of hyperkalemia can be increased when Losartan is combined with Drospirenone.
Eplerenone The risk or severity of hyperkalemia can be increased when Eplerenone is combined with Losartan.
Semuloparin The risk or severity of hyperkalemia can be increased when Semuloparin is combined with Losartan.
Lithium citrate The serum concentration of Lithium citrate can be increased when it is combined with Losartan.
Lithium carbonate The serum concentration of Lithium carbonate can be increased when it is combined with Losartan.
Lithium hydroxide The serum concentration of Lithium hydroxide can be increased when it is combined with Losartan.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Losartan.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Losartan.
Obinutuzumab Losartan may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Losartan.
Rituximab Losartan may increase the hypotensive activities of Rituximab.
Tolvaptan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Losartan.
Trimethoprim The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Losartan.
Desmopressin Desmopressin may decrease the antihypertensive activities of Losartan.
Midodrine Midodrine may decrease the antihypertensive activities of Losartan.
Isoetharine Isoetharine may decrease the antihypertensive activities of Losartan.
Etomidate Etomidate may decrease the antihypertensive activities of Losartan.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Losartan.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Losartan.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Losartan.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Losartan.
Doxapram Doxapram may decrease the antihypertensive activities of Losartan.
Metaraminol Metaraminol may decrease the antihypertensive activities of Losartan.
Nicergoline Nicergoline may decrease the antihypertensive activities of Losartan.
Methoxamine Methoxamine may decrease the antihypertensive activities of Losartan.
Propiomazine Propiomazine may decrease the antihypertensive activities of Losartan.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Losartan.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Losartan.
Dobutamine Dobutamine may decrease the antihypertensive activities of Losartan.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Losartan.
Ritodrine Ritodrine may decrease the antihypertensive activities of Losartan.
Bitolterol Bitolterol may decrease the antihypertensive activities of Losartan.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Losartan.
Naratriptan Naratriptan may decrease the antihypertensive activities of Losartan.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Losartan.
Dopamine Dopamine may decrease the antihypertensive activities of Losartan.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Losartan.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Losartan.
Arbutamine Arbutamine may decrease the antihypertensive activities of Losartan.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Losartan.
Fenoterol Fenoterol may decrease the antihypertensive activities of Losartan.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Losartan.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Losartan.
Ephedrine Ephedrine may decrease the antihypertensive activities of Losartan.
Mephentermine Mephentermine may decrease the antihypertensive activities of Losartan.
Procaterol Procaterol may decrease the antihypertensive activities of Losartan.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Losartan.
Bambuterol Bambuterol may decrease the antihypertensive activities of Losartan.
MMDA MMDA may decrease the antihypertensive activities of Losartan.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Losartan.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Losartan.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Losartan.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Losartan.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Losartan.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Losartan.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Losartan.
Metamfetamine Metamfetamine may decrease the antihypertensive activities of Losartan.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Losartan.
Periciazine Periciazine may decrease the antihypertensive activities of Losartan.
Acepromazine Acepromazine may decrease the antihypertensive activities of Losartan.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Losartan.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Losartan.
Amineptine Amineptine may decrease the antihypertensive activities of Losartan.
Amibegron Amibegron may decrease the antihypertensive activities of Losartan.
Naluzotan Naluzotan may decrease the antihypertensive activities of Losartan.
Pizotifen Pizotifen may decrease the antihypertensive activities of Losartan.
Solabegron Solabegron may decrease the antihypertensive activities of Losartan.
Droxidopa Droxidopa may decrease the antihypertensive activities of Losartan.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Losartan.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Losartan.
Isometheptene Isometheptene may decrease the antihypertensive activities of Losartan.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Losartan.
Naphazoline Naphazoline may decrease the antihypertensive activities of Losartan.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Losartan.
Cinitapride Cinitapride may decrease the antihypertensive activities of Losartan.
Tyramine Tyramine may decrease the antihypertensive activities of Losartan.
Adrafinil Adrafinil may decrease the antihypertensive activities of Losartan.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Losartan.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Losartan.
Etilefrine Etilefrine may decrease the antihypertensive activities of Losartan.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Losartan.
Cirazoline Cirazoline may decrease the antihypertensive activities of Losartan.
Synephrine Synephrine may decrease the antihypertensive activities of Losartan.

Target Protein

Erythropoietin receptor EPOR
Type-1 angiotensin II receptor AGTR1

Referensi & Sumber

Synthesis reference: Gordon C. Campbell, Jr., Anil M. Dwivedi, Dorothy A. Levorse, James A. McCauley, Krishnaswamy S. Raghavan, "Polymorphs of losartan and the process for the preparation of form II of losartan." U.S. Patent US5608075, issued May, 1994.
Artikel (PubMed)
  • PMID: 16029066
    Sica DA, Gehr TW, Ghosh S: Clinical pharmacokinetics of losartan. Clin Pharmacokinet. 2005;44(8):797-814.
  • PMID: 19515014
    Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1.

Contoh Produk & Brand

Produk: 985 • International brands: 1
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