Peringatan Keamanan

The oral TDLO in humans is 30mg/kg/6W.L7477

Symptoms of overdose include hypotension and tachycardia or bradycardia.L7456,L7459 Terlipressin may be given to treat hypotension and tachycardia if conventional vasopressors fail to control blood pressure.A181171

Irbesartan

DB01029

small molecule approved investigational

Deskripsi

Irbesartan is an angiotensin receptor blocker (ARB) indicated to treat hypertension or diabetic nephropathy.L7456,L7459 It can also be used as part of a combination product with hydrochlorothiazide for patients not well controlled or not expected to be well controlled on monotherapy.L7459 Unlike angiotensin converting enzyme inhibitors, ARBs are not associated with a dry cough.L7456,L7459

Irbesartan was granted FDA approval on 30 September 1997.L7456,L7459

Struktur Molekul 2D

Berat 428.5294
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 irbesartan is 11-15 hours.[L7456,L7459]
Volume Distribusi The volume of distribution of irbesartan is 53-93L.[L7456,L7459]
Klirens (Clearance) Total plasma clearance of irbesartan is 157-176mL/min while renal clearance is 3.0-3.5mL/min.[L7456,L7459]

Absorpsi

Irbesartan is 60-80% bioavailable with a Tmax of 1.5-2hours.L7456,L7459 Taking irbesartan with food does not affect the bioavailability.L7456,L7459 In one study, healthy subjects were given single or multiple oral doses of 150mg, 300mg, 600mg, and 900mg of irbesartan.A181165 A single 150mg dose resulted in an AUC of 9.7±3.0µg\•hr/mL, a Tmax of 1.5 hours, a half life of 16±7 hours, and a Cmax of 1.9±0.4µg/mL.A181165 A single 300mg dose resulted in an AUC of 20.0±5.2µg\•hr/mL, a Tmax of 1.5 hours, a half life of 14±7 hours, and a Cmax of 2.9±0.9µg/mL.A181165 A single 600mg dose resulted in an AUC of 32.6±11.9µg\•hr/mL, a Tmax of 1.5 hours, a half life of 14±8 hours, and a Cmax of 4.9±1.2µg/mL.A181165 A single 900mg dose resulted in an AUC of 44.8±20.0µg\•hr/mL, a Tmax of 1.5 hours, a half life of 17±7 hours, and a Cmax of 5.3±1.9µg/mL.A181165 Multiple 150mg doses resulted in an AUC of 9.3±3.0µg\•hr/mL, a Tmax of 1.5 hours, a half life of 11±4 hours, and a Cmax of 2.04±0.4µg/mL.A181165 Multiple 300mg doses resulted in an AUC of 19.8±5.8µg\•hr/mL, a Tmax of 2.0 hours, a half life of 11±5 hours, and a Cmax of 3.3±0.8µg/mL.A181165 Multiple 600mg doses resulted in an AUC of 31.9±9.7µg\•hr/mL, a Tmax of 1.5 hours, a half life of 15±7 hours, and a Cmax of 4.4±0.7µg/mL.A181165 Multiple 900mg doses resulted in an AUC of 34.2±9.3µg\•hr/mL, a Tmax of 1.8 hours, a half life of 14±6 hours, and a Cmax of 5.6±2.1µg/mL.A181165

Metabolisme

Irbesaran is largely metabolized by glucuronidation and oxidation in the liver.L7456,L7459 The majority of metabolism occurs through the action of CYP2C9 with a negligible contribution from CYP3A4.L7456,L7459 Some hydroxylation also occurs in irbesartan metabolism.A181114 Irbesartan can be glucuronidated by UGT1A3 to the M8 metabolite, oxidized to the M3 metabolite, or hydroxylated by CYP2C9 to one of the M4, M5, or M7 metabolites.A415,A181114 The M4, M5, and M7 metabolites are all hydroxylated to become the M1 metabolite, which is then oxidized to the M2 metabolite.A415,A181114 The M4 metabolite can also be oxidized to the M6 metabolite before hydroxylation to the M2 metabolite.A415,A181114 Finally, the minor metabolite SR 49498 is generated from irbesartan by an unknown mechanism.A415,A181114

Rute Eliminasi

20% of a radiolabelled oral dose of irbesartan is recovered in urine, and the rest is recovered in the feces.L7480 <2% of the dose is recovered in urine as the unchanged drug.L7480

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1165 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Irbesartan is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Irbesartan is combined with Levodopa.
Risperidone Irbesartan may increase the hypotensive activities of Risperidone.
Aliskiren The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Irbesartan.
Amifostine Irbesartan 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 Irbesartan.
Diazoxide Diazoxide may increase the hypotensive activities of Irbesartan.
Drospirenone The risk or severity of hyperkalemia can be increased when Irbesartan is combined with Drospirenone.
Eplerenone The risk or severity of hyperkalemia can be increased when Eplerenone is combined with Irbesartan.
Semuloparin The risk or severity of hyperkalemia can be increased when Semuloparin is combined with Irbesartan.
Lithium citrate The serum concentration of Lithium citrate can be increased when it is combined with Irbesartan.
Lithium carbonate The serum concentration of Lithium carbonate can be increased when it is combined with Irbesartan.
Lithium hydroxide The serum concentration of Lithium hydroxide can be increased when it is combined with Irbesartan.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Irbesartan.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Irbesartan.
Obinutuzumab Irbesartan may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Irbesartan.
Rituximab Irbesartan may increase the hypotensive activities of Rituximab.
Tolvaptan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Irbesartan.
Trimethoprim The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Irbesartan.
Desmopressin Desmopressin may decrease the antihypertensive activities of Irbesartan.
Midodrine Midodrine may decrease the antihypertensive activities of Irbesartan.
Isoetharine Isoetharine may decrease the antihypertensive activities of Irbesartan.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Irbesartan.
Etomidate Etomidate may decrease the antihypertensive activities of Irbesartan.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Irbesartan.
Protriptyline Protriptyline may decrease the antihypertensive activities of Irbesartan.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Irbesartan.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Irbesartan.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Irbesartan.
Droperidol Droperidol may decrease the antihypertensive activities of Irbesartan.
Amoxapine Amoxapine may decrease the antihypertensive activities of Irbesartan.
Doxapram Doxapram may decrease the antihypertensive activities of Irbesartan.
Atropine Atropine may decrease the antihypertensive activities of Irbesartan.
Metaraminol Metaraminol may decrease the antihypertensive activities of Irbesartan.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Irbesartan.
Nicergoline Nicergoline may decrease the antihypertensive activities of Irbesartan.
Methoxamine Methoxamine may decrease the antihypertensive activities of Irbesartan.
Propiomazine Propiomazine may decrease the antihypertensive activities of Irbesartan.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Irbesartan.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Irbesartan.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Irbesartan.
Dobutamine Dobutamine may decrease the antihypertensive activities of Irbesartan.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Irbesartan.
Ritodrine Ritodrine may decrease the antihypertensive activities of Irbesartan.
Terbutaline Terbutaline may decrease the antihypertensive activities of Irbesartan.
Flupentixol Flupentixol may decrease the antihypertensive activities of Irbesartan.
Bitolterol Bitolterol may decrease the antihypertensive activities of Irbesartan.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Irbesartan.
Naratriptan Naratriptan may decrease the antihypertensive activities of Irbesartan.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Irbesartan.
Dopamine Dopamine may decrease the antihypertensive activities of Irbesartan.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Irbesartan.
Albuterol Salbutamol may decrease the antihypertensive activities of Irbesartan.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Irbesartan.
Arbutamine Arbutamine may decrease the antihypertensive activities of Irbesartan.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Irbesartan.
Fenoterol Fenoterol may decrease the antihypertensive activities of Irbesartan.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Irbesartan.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Irbesartan.
Ephedrine Ephedrine may decrease the antihypertensive activities of Irbesartan.
Mephentermine Mephentermine may decrease the antihypertensive activities of Irbesartan.
Procaterol Procaterol may decrease the antihypertensive activities of Irbesartan.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Irbesartan.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Irbesartan.
Bambuterol Bambuterol may decrease the antihypertensive activities of Irbesartan.
MMDA MMDA may decrease the antihypertensive activities of Irbesartan.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Irbesartan.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Irbesartan.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Irbesartan.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Irbesartan.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Irbesartan.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Irbesartan.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Irbesartan.
Metamfetamine Metamfetamine may decrease the antihypertensive activities of Irbesartan.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Irbesartan.
Periciazine Periciazine may decrease the antihypertensive activities of Irbesartan.
Acepromazine Acepromazine may decrease the antihypertensive activities of Irbesartan.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Irbesartan.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Irbesartan.
Amineptine Amineptine may decrease the antihypertensive activities of Irbesartan.
Amibegron Amibegron may decrease the antihypertensive activities of Irbesartan.
Naluzotan Naluzotan may decrease the antihypertensive activities of Irbesartan.
Pizotifen Pizotifen may decrease the antihypertensive activities of Irbesartan.
Solabegron Solabegron may decrease the antihypertensive activities of Irbesartan.
Droxidopa Droxidopa may decrease the antihypertensive activities of Irbesartan.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Irbesartan.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Irbesartan.
Xylometazoline Xylometazoline may decrease the antihypertensive activities of Irbesartan.
Isometheptene Isometheptene may decrease the antihypertensive activities of Irbesartan.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Irbesartan.
Naphazoline Naphazoline may decrease the antihypertensive activities of Irbesartan.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Irbesartan.
Cinitapride Cinitapride may decrease the antihypertensive activities of Irbesartan.
Tyramine Tyramine may decrease the antihypertensive activities of Irbesartan.
Adrafinil Adrafinil may decrease the antihypertensive activities of Irbesartan.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Irbesartan.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Irbesartan.
Etilefrine Etilefrine may decrease the antihypertensive activities of Irbesartan.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Irbesartan.

Target Protein

Type-1 angiotensin II receptor AGTR1
Transcription factor Jun JUN

Referensi & Sumber

Synthesis reference: Gennady Nisnevich, "Novel synthesis of irbesartan." U.S. Patent US20040192713, issued September 30, 2004.
Artikel (PubMed)
  • PMID: 11565517
    Lewis EJ, Hunsicker LG, Clarke WR, Berl T, Pohl MA, Lewis JB, Ritz E, Atkins RC, Rohde R, Raz I: Renoprotective effect of the angiotensin-receptor antagonist irbesartan in patients with nephropathy due to type 2 diabetes. N Engl J Med. 2001 Sep 20;345(12):851-60.
  • PMID: 15101793
    Croom KF, Curran MP, Goa KL, Perry CM: Irbesartan: a review of its use in hypertension and in the management of diabetic nephropathy. Drugs. 2004;64(9):999-1028.
  • PMID: 9571222
    Chando TJ, Everett DW, Kahle AD, Starrett AM, Vachharajani N, Shyu WC, Kripalani KJ, Barbhaiya RH: Biotransformation of irbesartan in man. Drug Metab Dispos. 1998 May;26(5):408-17.
  • 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.
  • PMID: 9549663
    Marino MR, Langenbacher K, Ford NF, Uderman HD: Pharmacokinetics and pharmacodynamics of irbesartan in healthy subjects. J Clin Pharmacol. 1998 Mar;38(3):246-55.
  • PMID: 16548975
    McNamee JJ, Trainor D, Michalek P: Terlipressin for refractory hypotension following angiotensin-II receptor antagonist overdose. Anaesthesia. 2006 Apr;61(4):408-9. doi: 10.1111/j.1365-2044.2006.04599.x.

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