Peringatan Keamanan

The oral LD50 of aliskiren in rats is >2000 mg/kg.L14294 Overdose information is limited in the literature, however, an overdose with aliskiren is likely to result in hypotension. Supportive treatment should be initiated in the case of an overdose.L13994,L14297

Aliskiren

DB09026

small molecule approved investigational

Deskripsi

Aliskiren is the first drug in the renin inhibitor drug class and is used for the treatment of hypertension.A203624 It was developed by Speedel and Novartis and initially approved by the FDA in early 2007.L14018 Aliskiren has been proven to efficacious in reducing blood pressure when used alone or in conjunction with other antihypertensive agents.A203624

Struktur Molekul 2D

Berat 551.7583
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Plasma half-life for aliskiren can range from 30 to 40 hours [A214172] with an accumulation half-life of about 24 hours.[A214172]
Volume Distribusi Unchanged aliskiren accounts for about 80% of the drug found in the plasma.[A214172,L13994]
Klirens (Clearance) Aliskiren is partially cleared in the kidneys, and safety data have not been established for patients with a creatinine clearance of less than 30 mL/min.[L13994] One pharmacokinetic study revealed an average renal clearance of 1280 +/- 500 mL/hour in healthy volunteers.[A214181]

Absorpsi

Aliskiren is absorbed in the gastrointestinal tract and is poorly absorbed with a bioavailability between 2.0 and 2.5%.A204305,L13994 Peak plasma concentrations of aliskiren are achieved between 1 to 3 hours after administration.A204305,L13994 Steady-state concentrations of aliskiren are achieved within 7-8 days of regular administration.A7581

Metabolisme

About 80% of the drug in plasma following oral administration is unchanged. Two major metabolites account for about 1-3% of aliskiren in the plasma. One metabolite is an O-demethylated alcohol derivative and the other is a carboxylic acid derivative. Minor oxidized and hydrolyzed metabolites may also be found in the plasma.A214172,L13994

Rute Eliminasi

Aliskiren is mainly excreted via the hepatobiliary route and by oxidative metabolism by hepatic cytochrome enzymes.A7581 Approximately one-quarter of the absorbed dose appears in the urine as unchanged parent drug. L13994 One pharmacokinetic study of radiolabeled aliskiren detected 0.6% radioactivity in the urine and more than 80% in the feces, suggesting that aliskiren is mainly eliminated by the fecal route.A214172

Interaksi Makanan

2 Data
  • 1. Do not take with or immediately after a high-fat meal. The absorption of aliskiren is substantially reduced by taking it with high-fat meals.
  • 2. Take with or without food. Take consistently at the same time in regard to meals.

Interaksi Obat

830 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Aliskiren is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Aliskiren is combined with Levodopa.
Risperidone Aliskiren may increase the hypotensive activities of Risperidone.
Cyclosporine The serum concentration of Aliskiren can be increased when it is combined with Cyclosporine.
Alfuzosin Alfuzosin may increase the hypotensive activities of Aliskiren.
Olmesartan The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Olmesartan.
Losartan The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Losartan.
Candesartan cilexetil The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Candesartan cilexetil.
Eprosartan The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Eprosartan.
Telmisartan The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Telmisartan.
Irbesartan The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Irbesartan.
Forasartan The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Forasartan.
Saprisartan The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Saprisartan.
Tasosartan The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Tasosartan.
Saralasin The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Saralasin.
Fimasartan The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Fimasartan.
Candesartan The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Candesartan.
Amifostine Aliskiren may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Aliskiren.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Aliskiren.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Aliskiren.
Obinutuzumab Aliskiren may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Aliskiren.
Rituximab Aliskiren may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Aliskiren.
Midodrine Midodrine may decrease the antihypertensive activities of Aliskiren.
Isoetharine Isoetharine may decrease the antihypertensive activities of Aliskiren.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Aliskiren.
Etomidate Etomidate may decrease the antihypertensive activities of Aliskiren.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Aliskiren.
Protriptyline Protriptyline may decrease the antihypertensive activities of Aliskiren.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Aliskiren.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Aliskiren.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Aliskiren.
Droperidol Droperidol may decrease the antihypertensive activities of Aliskiren.
Amoxapine Amoxapine may decrease the antihypertensive activities of Aliskiren.
Doxapram Doxapram may decrease the antihypertensive activities of Aliskiren.
Atropine Atropine may decrease the antihypertensive activities of Aliskiren.
Metaraminol Metaraminol may decrease the antihypertensive activities of Aliskiren.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Aliskiren.
Nicergoline Nicergoline may decrease the antihypertensive activities of Aliskiren.
Methoxamine Methoxamine may decrease the antihypertensive activities of Aliskiren.
Propiomazine Propiomazine may decrease the antihypertensive activities of Aliskiren.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Aliskiren.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Aliskiren.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Aliskiren.
Dobutamine Dobutamine may decrease the antihypertensive activities of Aliskiren.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Aliskiren.
Ritodrine Ritodrine may decrease the antihypertensive activities of Aliskiren.
Terbutaline Terbutaline may decrease the antihypertensive activities of Aliskiren.
Flupentixol Flupentixol may decrease the antihypertensive activities of Aliskiren.
Bitolterol Bitolterol may decrease the antihypertensive activities of Aliskiren.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Aliskiren.
Naratriptan Naratriptan may decrease the antihypertensive activities of Aliskiren.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Aliskiren.
Formoterol Formoterol may decrease the antihypertensive activities of Aliskiren.
Dopamine Dopamine may decrease the antihypertensive activities of Aliskiren.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Aliskiren.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Aliskiren.
Arbutamine Arbutamine may decrease the antihypertensive activities of Aliskiren.
Dutasteride Dutasteride may decrease the antihypertensive activities of Aliskiren.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Aliskiren.
Arformoterol Arformoterol may decrease the antihypertensive activities of Aliskiren.
Fenoterol Fenoterol may decrease the antihypertensive activities of Aliskiren.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Aliskiren.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Aliskiren.
Ephedrine Ephedrine may decrease the antihypertensive activities of Aliskiren.
Mephentermine Mephentermine may decrease the antihypertensive activities of Aliskiren.
Procaterol Procaterol may decrease the antihypertensive activities of Aliskiren.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Aliskiren.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Aliskiren.
Bambuterol Bambuterol may decrease the antihypertensive activities of Aliskiren.
MMDA MMDA may decrease the antihypertensive activities of Aliskiren.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Aliskiren.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Aliskiren.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Aliskiren.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Aliskiren.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Aliskiren.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Aliskiren.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Aliskiren.
Metamfetamine Metamfetamine may decrease the antihypertensive activities of Aliskiren.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Aliskiren.
Periciazine Periciazine may decrease the antihypertensive activities of Aliskiren.
Acepromazine Acepromazine may decrease the antihypertensive activities of Aliskiren.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Aliskiren.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Aliskiren.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Aliskiren.
Amineptine Amineptine may decrease the antihypertensive activities of Aliskiren.
Amibegron Amibegron may decrease the antihypertensive activities of Aliskiren.
Naluzotan Naluzotan may decrease the antihypertensive activities of Aliskiren.
Pizotifen Pizotifen may decrease the antihypertensive activities of Aliskiren.
Solabegron Solabegron may decrease the antihypertensive activities of Aliskiren.
Droxidopa Droxidopa may decrease the antihypertensive activities of Aliskiren.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Aliskiren.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Aliskiren.
Xylometazoline Xylometazoline may decrease the antihypertensive activities of Aliskiren.
Isometheptene Isometheptene may decrease the antihypertensive activities of Aliskiren.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Aliskiren.
Naphazoline Naphazoline may decrease the antihypertensive activities of Aliskiren.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Aliskiren.

Target Protein

Renin REN

Referensi & Sumber

Synthesis reference: Hanessian S, Guesné S, Chénard E. Total synthesis of "aliskiren": the first Renin inhibitor in clinical practice for hypertension. Org Lett. 2010;12(8):1816?1819. doi:10.1021/ol100427v
Artikel (PubMed)
  • PMID: 18611061
    Vaidyanathan S, Jarugula V, Dieterich HA, Howard D, Dole WP: Clinical pharmacokinetics and pharmacodynamics of aliskiren. Clin Pharmacokinet. 2008;47(8):515-31.
  • PMID: 15723979
    Gradman AH, Schmieder RE, Lins RL, Nussberger J, Chiang Y, Bedigian MP: Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation. 2005 Mar 1;111(8):1012-8. Epub 2005 Feb 21.
  • PMID: 17055947
    Staessen JA, Li Y, Richart T: Oral renin inhibitors. Lancet. 2006 Oct 21;368(9545):1449-56.
  • PMID: 19170589
    Sanoski CA: Aliskiren: an oral direct renin inhibitor for the treatment of hypertension. Pharmacotherapy. 2009 Feb;29(2):193-212. doi: 10.1592/phco.29.2.193.
  • PMID: 17956203
    Oh BH: Aliskiren, the first in a new class of direct renin inhibitors for hypertension: present and future perspectives. Expert Opin Pharmacother. 2007 Nov;8(16):2839-49. doi: 10.1517/14656566.8.16.2839.
  • PMID: 19066408
    Buczko W, Hermanowicz JM: Pharmacokinetics and pharmacodynamics of aliskiren, an oral direct renin inhibitor. Pharmacol Rep. 2008 Sep-Oct;60(5):623-31.
  • PMID: 17510248
    Waldmeier F, Glaenzel U, Wirz B, Oberer L, Schmid D, Seiberling M, Valencia J, Riviere GJ, End P, Vaidyanathan S: Absorption, distribution, metabolism, and elimination of the direct renin inhibitor aliskiren in healthy volunteers. Drug Metab Dispos. 2007 Aug;35(8):1418-28. doi: 10.1124/dmd.106.013797. Epub 2007 May 17.
  • PMID: 17655373
    Vaidyanathan S, Bigler H, Yeh C, Bizot MN, Dieterich HA, Howard D, Dole WP: Pharmacokinetics of the oral direct renin inhibitor aliskiren alone and in combination with irbesartan in renal impairment. Clin Pharmacokinet. 2007;46(8):661-75. doi: 10.2165/00003088-200746080-00003.

Contoh Produk & Brand

Produk: 164 • International brands: 0
Produk
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