Peringatan Keamanan

Side effects include fluid retention, congestive heart failure (CHF), liver disease

Rosiglitazone

DB00412

small molecule approved investigational

Deskripsi

Rosiglitazone is an anti-diabetic drug in the thiazolidinedione class of drugs. It is marketed by the pharmaceutical company GlaxoSmithKline as a stand-alone drug (Avandia) and in combination with metformin (Avandamet) or with glimepiride (Avandaryl). Like other thiazolidinediones, the mechanism of action of rosiglitazone is by activation of the intracellular receptor class of the peroxisome proliferator-activated receptors (PPARs), specifically PPAR?. Rosiglitazone is a selective ligand of PPAR?, and has no PPAR?-binding action. Apart from its effect on insulin resistance, it appears to have an anti-inflammatory effect: nuclear factor kappa-B (NF?B) levels fall and inhibitor (I?B) levels increase in patients on rosiglitazone. Recent research has suggested that rosiglitazone may also be of benefit to a subset of patients with Alzheimer's disease not expressing the ApoE4 allele. This is the subject of a clinical trial currently underway.

Struktur Molekul 2D

Berat 357.427
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 3-4 hours (single oral dose, independent of dose)
Volume Distribusi * 17.6 L [oral volume of distribution Vss/F] * 13.5 L [population mean, pediatric patients]
Klirens (Clearance) * Oral clearance (CL) = 3.03 ± 0.87 L/hr [1 mg Fasting] * Oral CL = 2.89 ± 0.71 L/hr [2 mg Fasting] * Oral CL = 2.85 ± 0.69 L/hr [8 mg Fasting] * Oral CL = 2.97 ± 0.81 L/hr [8 mg Fed] * 3.15 L/hr [Population mean, Pediatric patients]

Absorpsi

The absolute bioavailability of rosiglitazone is 99%. Peak plasma concentrations are observed about 1 hour after dosing. Administration of rosiglitazone with food resulted in no change in overall exposure (AUC), but there was an approximately 28% decrease in Cmax and a delay in Tmax (1.75 hours). These changes are not likely to be clinically significant; therefore, rosiglitazone may be administered with or without food. Maximum plasma concentration (Cmax) and the area under the curve (AUC) of rosiglitazone increase in a dose-proportional manner over the therapeutic dose range.

Metabolisme

Hepatic. Rosiglitazone is extensively metabolized in the liver to inactive metabolites via N-demethylation, hydroxylation, and conjugation with sulfate and glucuronic acid. In vitro data have shown that Cytochrome (CYP) P450 isoenzyme 2C8 (CYP2C8) and to a minor extent CYP2C9 are involved in the hepatic metabolism of rosiglitazone.

Rute Eliminasi

Following oral or intravenous administration of 14Crosiglitazone maleate, approximately 64% and 23% of the dose was eliminated in the urine and in the feces, respectively.

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

1540 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Rosiglitazone.
Insulin human The risk or severity of congestive heart failure can be increased when Insulin human is combined with Rosiglitazone.
Insulin lispro The risk or severity of congestive heart failure can be increased when Insulin lispro is combined with Rosiglitazone.
Insulin glargine The risk or severity of congestive heart failure can be increased when Insulin glargine is combined with Rosiglitazone.
Insulin pork The risk or severity of congestive heart failure can be increased when Insulin pork is combined with Rosiglitazone.
Insulin aspart The risk or severity of congestive heart failure can be increased when Insulin aspart is combined with Rosiglitazone.
Insulin detemir The risk or severity of congestive heart failure can be increased when Insulin detemir is combined with Rosiglitazone.
Insulin glulisine The risk or severity of congestive heart failure can be increased when Insulin glulisine is combined with Rosiglitazone.
NN344 The risk or severity of congestive heart failure can be increased when NN344 is combined with Rosiglitazone.
Insulin beef The risk or severity of congestive heart failure can be increased when Insulin beef is combined with Rosiglitazone.
Insulin degludec The risk or severity of congestive heart failure can be increased when Insulin degludec is combined with Rosiglitazone.
Insulin peglispro The risk or severity of congestive heart failure can be increased when Insulin peglispro is combined with Rosiglitazone.
Insulin tregopil The risk or severity of congestive heart failure can be increased when Insulin tregopil is combined with Rosiglitazone.
Insulin argine The risk or severity of congestive heart failure can be increased when Insulin argine is combined with Rosiglitazone.
Erythromycin The serum concentration of Rosiglitazone can be increased when it is combined with Erythromycin.
Reserpine Reserpine may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Chlorpromazine Chlorpromazine may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Cimetidine Cimetidine may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Bosentan Bosentan may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Ethinylestradiol Ethinylestradiol may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Fusidic acid Fusidic acid may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Simeprevir Simeprevir may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Lenvatinib Lenvatinib may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Letermovir The metabolism of Rosiglitazone can be decreased when combined with Letermovir.
Valinomycin Valinomycin may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Cyclosporine Cyclosporine may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Rosiglitazone.
Mifepristone The serum concentration of Rosiglitazone can be increased when it is combined with Mifepristone.
Pregabalin The risk or severity of weight gain and edema formation can be increased when Pregabalin is combined with Rosiglitazone.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Rosiglitazone.
Nitroglycerin The risk or severity of adverse effects can be increased when Nitroglycerin is combined with Rosiglitazone.
Isosorbide dinitrate The risk or severity of adverse effects can be increased when Isosorbide dinitrate is combined with Rosiglitazone.
Amyl Nitrite The risk or severity of adverse effects can be increased when Amyl Nitrite is combined with Rosiglitazone.
Erythrityl tetranitrate The risk or severity of adverse effects can be increased when Erythrityl tetranitrate is combined with Rosiglitazone.
Pentaerythritol tetranitrate The risk or severity of adverse effects can be increased when Pentaerythritol tetranitrate is combined with Rosiglitazone.
Isosorbide The risk or severity of adverse effects can be increased when Isosorbide is combined with Rosiglitazone.
Propatyl nitrate The risk or severity of adverse effects can be increased when Propatyl nitrate is combined with Rosiglitazone.
Methylpropylpropanediol dinitrate The risk or severity of adverse effects can be increased when Methylpropylpropanediol dinitrate is combined with Rosiglitazone.
Tenitramine The risk or severity of adverse effects can be increased when Tenitramine is combined with Rosiglitazone.
Trolnitrate The risk or severity of adverse effects can be increased when Trolnitrate is combined with Rosiglitazone.
Nitrate The risk or severity of adverse effects can be increased when Nitrate is combined with Rosiglitazone.
Cholestyramine The serum concentration of Rosiglitazone can be decreased when it is combined with Cholestyramine.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Rosiglitazone.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Rosiglitazone.
Moxifloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Epitizide.
Amineptine Amineptine may decrease the hypoglycemic activities of Rosiglitazone.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Rosiglitazone.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Rosiglitazone.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Rosiglitazone.

Target Protein

Peroxisome proliferator-activated receptor gamma PPARG
Long-chain-fatty-acid--CoA ligase 4 ACSL4
Peroxisome proliferator-activated receptor alpha PPARA
Peroxisome proliferator-activated receptor delta PPARD
Retinoic acid receptor RXR-alpha RXRA
Retinoic acid receptor RXR-beta RXRB
Retinoic acid receptor RXR-gamma RXRG

Referensi & Sumber

Synthesis reference: Manne Reddy, "Amorphous form of rosiglitazone maleate and process for preparation thereof." U.S. Patent US20040242658, issued December 02, 2004.
Artikel (PubMed)
  • PMID: 15181049
    Mohanty P, Aljada A, Ghanim H, Hofmeyer D, Tripathy D, Syed T, Al-Haddad W, Dhindsa S, Dandona P: Evidence for a potent antiinflammatory effect of rosiglitazone. J Clin Endocrinol Metab. 2004 Jun;89(6):2728-35.
  • PMID: 17145742
    Kahn SE, Haffner SM, Heise MA, Herman WH, Holman RR, Jones NP, Kravitz BG, Lachin JM, O'Neill MC, Zinman B, Viberti G: Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy. N Engl J Med. 2006 Dec 7;355(23):2427-43. Epub 2006 Dec 4.

Contoh Produk & Brand

Produk: 112 • International brands: 16
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Menampilkan 8 dari 112 produk.
International Brands
  • Blutab — Werrick
  • DH-Rosidia — Hasan
  • Diaben — Elea
  • Diaglinex — Farmindustria
  • Gaudil — Craveri
  • Gliximina — Denver
  • Naidi — Hisun
  • Rogelin — Torrent
  • Roglit — Gedeon Richter
  • Romerol — Drug International

Sekuens Gen/Protein (FASTA)

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