Troglitazone

DB00197

small molecule approved investigational withdrawn

Deskripsi

Troglitazone was withdrawn in 2000 due to risk of hepatotoxicity. It was superseded by pioglitazone and rosiglitazone.

Struktur Molekul 2D

Berat 441.54
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 16-34 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Absorbed rapidly. Food increases the extent of absorption by 30% to 85%.

Metabolisme

A sulfate conjugate metabolite (Metabolite 1) and a quinone metabolite (Metabolite 3) have been detected in the plasma of healthy males. A glucuronide conjugate (Metabolite 2) has been detected in the urine and also in negligible amounts in the plasma. In healthy volunteers and in patients with type 2 diabetes, the steady-state concentration of Metabolite 1 is six to seven times that of troglitazone and Metabolite 3. In in vivo drug interaction studies, troglitazone has been shown to induce cytochrome P450 CYP3A4 at clinically relevant doses.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

1175 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Troglitazone.
Glycochenodeoxycholic Acid Troglitazone may decrease the excretion rate of Glycochenodeoxycholic Acid which could result in a higher serum level.
Pravastatin Troglitazone may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Fluvoxamine Troglitazone may decrease the excretion rate of Fluvoxamine which could result in a higher serum level.
Isradipine Troglitazone may decrease the excretion rate of Isradipine which could result in a higher serum level.
Flucloxacillin Troglitazone may decrease the excretion rate of Flucloxacillin which could result in a higher serum level.
Indomethacin Troglitazone may decrease the excretion rate of Indomethacin which could result in a higher serum level.
Atropine Troglitazone may decrease the excretion rate of Atropine which could result in a higher serum level.
Fluorescein Troglitazone may decrease the excretion rate of Fluorescein which could result in a higher serum level.
Nitrofurantoin Troglitazone may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.
Disulfiram Troglitazone may decrease the excretion rate of Disulfiram which could result in a higher serum level.
Cefaclor Troglitazone may decrease the excretion rate of Cefaclor which could result in a higher serum level.
Tinidazole Troglitazone may decrease the excretion rate of Tinidazole which could result in a higher serum level.
Telmisartan Troglitazone may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Ezetimibe Troglitazone may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Dipyridamole Troglitazone may decrease the excretion rate of Dipyridamole which could result in a higher serum level.
Sulfamethoxazole Troglitazone may decrease the excretion rate of Sulfamethoxazole which could result in a higher serum level.
Fenofibrate Troglitazone may decrease the excretion rate of Fenofibrate which could result in a higher serum level.
Nitrendipine Troglitazone may decrease the excretion rate of Nitrendipine which could result in a higher serum level.
Rosuvastatin Troglitazone may decrease the excretion rate of Rosuvastatin which could result in a higher serum level.
Sulfinpyrazone Troglitazone may decrease the excretion rate of Sulfinpyrazone which could result in a higher serum level.
Nefazodone Troglitazone may decrease the excretion rate of Nefazodone which could result in a higher serum level.
Ofloxacin Troglitazone may decrease the excretion rate of Ofloxacin which could result in a higher serum level.
Clarithromycin Troglitazone may decrease the excretion rate of Clarithromycin which could result in a higher serum level.
Taurocholic acid Troglitazone may decrease the excretion rate of Taurocholic acid which could result in a higher serum level.
Prasterone sulfate Troglitazone may decrease the excretion rate of Prasterone sulfate which could result in a higher serum level.
Indocyanine green acid form Troglitazone may decrease the excretion rate of Indocyanine green acid form which could result in a higher serum level.
Benzbromarone Troglitazone may decrease the excretion rate of Benzbromarone which could result in a higher serum level.
Pilsicainide Troglitazone may decrease the excretion rate of Pilsicainide which could result in a higher serum level.
Dihydroergocristine Troglitazone may decrease the excretion rate of Dihydroergocristine which could result in a higher serum level.
Glycyrrhizic acid Troglitazone may decrease the excretion rate of Glycyrrhizic acid which could result in a higher serum level.
Atorvastatin Troglitazone may decrease the excretion rate of Atorvastatin which could result in a higher serum level.
Terfenadine Troglitazone may decrease the excretion rate of Terfenadine which could result in a higher serum level.
Belantamab mafodotin Troglitazone may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Troglitazone.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Troglitazone.
Deferiprone The serum concentration of Deferiprone can be increased when it is combined with Troglitazone.
Mifepristone The serum concentration of Troglitazone 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 Troglitazone.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Troglitazone.
Perampanel The metabolism of Perampanel can be increased when combined with Troglitazone.
Warfarin The metabolism of Warfarin can be increased when combined with Troglitazone.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Troglitazone.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Troglitazone.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Troglitazone.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Troglitazone.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Troglitazone.
Nelfinavir Troglitazone may decrease the excretion rate of Nelfinavir which could result in a higher serum level.
Lamotrigine The metabolism of Troglitazone can be increased when combined with Lamotrigine.
Efavirenz Troglitazone may decrease the excretion rate of Efavirenz which could result in a higher serum level.
Testosterone propionate The metabolism of Troglitazone can be increased when combined with Testosterone propionate.
Zidovudine The metabolism of Troglitazone can be increased when combined with Zidovudine.
Primidone The metabolism of Troglitazone can be increased when combined with Primidone.
Tipranavir Troglitazone may decrease the excretion rate of Tipranavir which could result in a higher serum level.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Troglitazone.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Troglitazone.
Moxifloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Troglitazone can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Gemifloxacin.
Sparfloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Troglitazone can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Troglitazone can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Troglitazone can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Troglitazone can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Troglitazone can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Troglitazone can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Troglitazone can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Troglitazone can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Troglitazone can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Troglitazone can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Troglitazone can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Troglitazone can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Troglitazone can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Troglitazone can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Troglitazone can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Troglitazone can be decreased when used in combination with Quinethazone.

Target Protein

Peroxisome proliferator-activated receptor gamma PPARG
Estrogen-related receptor gamma ESRRG
Steroid hormone receptor ERR1 ESRRA
Peroxisome proliferator-activated receptor delta PPARD
Peroxisome proliferator-activated receptor alpha PPARA
Glutathione S-transferase P GSTP1
Long-chain-fatty-acid--CoA ligase 4 ACSL4
Plasminogen activator inhibitor 1 SERPINE1
Equilibrative nucleoside transporter 1 SLC29A1

Referensi & Sumber

Synthesis reference: Krishnamurthi Vyas, Chebiyyam Prabhakar, Sreenivas Dharmaraja Rao, Mamillapalli Ramabadhra Sarma, Om Gaddam Reddy, Rajagopalan Ramanujam, Ranjan Chakrabarti, "Polymorphic forms of troglitazone having enhanced anti-diabetic activity and a process for their preparation." U.S. Patent US5700820, issued June, 1992.
Artikel (PubMed)
  • PMID: 11443197
    Aljada A, Garg R, Ghanim H, Mohanty P, Hamouda W, Assian E, Dandona P: Nuclear factor-kappaB suppressive and inhibitor-kappaB stimulatory effects of troglitazone in obese patients with type 2 diabetes: evidence of an antiinflammatory action? J Clin Endocrinol Metab. 2001 Jul;86(7):3250-6.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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