Peringatan Keamanan

The oral TDLo observed in mice is 24 mg/kg for 4 days and for rats is 3 mg/kg for 6 days.L11431

One instance of overdose was reported during clinical trials with pioglitazone in which a patient took an oral dose of 120mg daily for four days, followed by 180mg daily for seven daysL11416 - this patient did not report any adverse clinical symptoms during this time. In the event of overdosage, employ symptomatic and supportive measures according to the patient's clinical status.L11416

Pioglitazone

DB01132

small molecule approved investigational

Deskripsi

Pioglitazone is an antihyperglycemic used as an adjunct to diet, exercise, and other antidiabetic medications to manage type 2 diabetes mellitus.L11416,L11419,L11422,L11425 It is administered as a racemic mixture, though there is no pharmacologic difference between the enantiomers and they appear to interconvert in vivo with little consequence.L11416 The thiazolidinedione class of medications, which also includes rosiglitazone and troglitazone, exerts its pharmacological effect primarily by promoting insulin sensitivity and the improved uptake of blood glucoseL11416 via agonism at the peroxisome proliferator-activated receptor-gamma (PPAR?).A19757 PPARs are ligand-activated transcription factors that are involved in the expression of more than 100 genes and affect numerous metabolic processes, most notably lipid and glucose homeostasis.A19759

Thiazolidinediones, including pioglitazone, have fallen out of favor in recent years due to the presence of multiple adverse effects and warnings regarding their use (e.g. congestive heart failure, bladder cancer) and the availability of safer and more effective alternatives for patients with type 2 diabetes mellitus.L11461

Struktur Molekul 2D

Berat 356.439
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean serum half-life of pioglitazone and its metabolites (M-III and M-IV) range from 3-7 hours and 16-24 hours, respectively.[L11416]
Volume Distribusi The average apparent volume of distribution of pioglitazone is 0.63 ± 0.41 L/kg.[L11416]
Klirens (Clearance) The apparent clearance of orally administered pioglitazone is 5-7 L/h.[L11416]

Absorpsi

Following oral administration of pioglitazone, peak serum concentrations are observed within 2 hours (Tmax) - food slightly delays the time to peak serum concentration, increasing Tmax to approximately 3-4 hours, but does not alter the extent of absorption.L11416 Steady-state concentrations of both parent drug and its primary active metabolites are achieved after 7 days of once-daily administration of pioglitazone.L11416 Cmax and AUC increase proportionately to administered doses.L11416

Metabolisme

Pioglitazone is extensively metabolized by both hydroxylation and oxidation - the resulting metabolites are also partly converted to glucuronide or sulfate conjugates.L11416 The pharmacologically active M-IV and M-III metabolites are the main metabolites found in human serum and their circulating concentrations are equal to, or greater than, those of the parent drug.A415 The specific CYP isoenzymes involved in the metabolism of pioglitazone are CYP2C8 and, to a lesser degree, CYP3A4. There is also some evidence to suggest a contribution by extrahepatic CYP1A1.L11416

Rute Eliminasi

Approximately 15-30% of orally administered pioglitazone is recovered in the urine. The bulk of its elimination, then, is presumed to be through the excretion of unchanged drug in the bile or as metabolites in the feces.L11416

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food delays drug absorption, but not to a clinically significant extent.

Interaksi Obat

828 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Pioglitazone.
Insulin human The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin human.
Insulin lispro The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin lispro.
Insulin glargine The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin glargine.
Insulin pork The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin pork.
Insulin aspart The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin aspart.
Insulin detemir The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin detemir.
Insulin glulisine The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin glulisine.
NN344 The risk or severity of adverse effects can be increased when Pioglitazone is combined with NN344.
Insulin beef The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin beef.
Insulin degludec The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin degludec.
Insulin peglispro The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin peglispro.
Insulin tregopil The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin tregopil.
Insulin argine The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin argine.
Mifepristone The serum concentration of Pioglitazone 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 Pioglitazone.
Sorafenib The metabolism of Sorafenib can be decreased when combined with Pioglitazone.
Ritonavir The serum concentration of Pioglitazone can be increased when it is combined with Ritonavir.
Erlotinib The serum concentration of Pioglitazone can be increased when it is combined with Erlotinib.
Fluticasone propionate The serum concentration of Pioglitazone can be increased when it is combined with Fluticasone propionate.
Clopidogrel The serum concentration of Pioglitazone can be increased when it is combined with Clopidogrel.
Candesartan cilexetil The serum concentration of Pioglitazone can be increased when it is combined with Candesartan cilexetil.
Salmeterol The serum concentration of Pioglitazone can be increased when it is combined with Salmeterol.
Felodipine The serum concentration of Pioglitazone can be increased when it is combined with Felodipine.
Gemfibrozil The serum concentration of Pioglitazone can be increased when it is combined with Gemfibrozil.
Fluticasone furoate The risk or severity of hyperglycemia can be increased when Fluticasone furoate is combined with Pioglitazone.
Dabrafenib The serum concentration of Pioglitazone can be increased when it is combined with Dabrafenib.
Fluticasone The serum concentration of Pioglitazone can be increased when it is combined with Fluticasone.
Mometasone furoate The serum concentration of Pioglitazone can be increased when it is combined with Mometasone furoate.
Moxifloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Pioglitazone can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Pioglitazone can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Pioglitazone can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Pioglitazone can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Pioglitazone can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Epitizide.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Pioglitazone.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Pioglitazone.
Desipramine Desipramine may decrease the hypoglycemic activities of Pioglitazone.
Amineptine Amineptine may decrease the hypoglycemic activities of Pioglitazone.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Pioglitazone.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Pioglitazone.
Dosulepin Dosulepin may decrease the hypoglycemic activities of Pioglitazone.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Pioglitazone.
Opipramol Opipramol may decrease the hypoglycemic activities of Pioglitazone.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Pioglitazone.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Pioglitazone.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Pioglitazone.
Melitracen Melitracen may decrease the hypoglycemic activities of Pioglitazone.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Pioglitazone.
Iprindole Iprindole may decrease the hypoglycemic activities of Pioglitazone.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Pioglitazone.
Trimipramine Trimipramine may decrease the hypoglycemic activities of Pioglitazone.
Imipramine Imipramine may decrease the hypoglycemic activities of Pioglitazone.
Nortriptyline Nortriptyline may decrease the hypoglycemic activities of Pioglitazone.
Doxepin Doxepin may decrease the hypoglycemic activities of Pioglitazone.
Clomipramine Clomipramine may decrease the hypoglycemic activities of Pioglitazone.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Pioglitazone.
Acetohexamide The therapeutic efficacy of Acetohexamide can be increased when used in combination with Pioglitazone.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Pioglitazone.

Target Protein

Peroxisome proliferator-activated receptor gamma PPARG
Amine oxidase [flavin-containing] B MAOB

Referensi & Sumber

Synthesis reference: Chandra Khanduri, Yatendra Kumar, Atulya Panda, Suchitra Chakraborty, Mukesh Sharma, "Process for the preparation of pioglitazone." U.S. Patent US20070078170, issued April 05, 2007.
Artikel (PubMed)
  • PMID: 26940171
    Al-Majed A, Bakheit AH, Abdel Aziz HA, Alharbi H, Al-Jenoobi FI: Pioglitazone. Profiles Drug Subst Excip Relat Methodol. 2016;41:379-438. doi: 10.1016/bs.podrm.2015.11.002. Epub 2016 Feb 2.
  • PMID: 25450819
    Janani C, Ranjitha Kumari BD: PPAR gamma gene--a review. Diabetes Metab Syndr. 2015 Jan-Mar;9(1):46-50. doi: 10.1016/j.dsx.2014.09.015. Epub 2014 Oct 13.
  • 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

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