Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names


Austria: Actos, Glustin; Belgium: Actos; Cyprus: Glustin; Czech Republic: Actos, Glustin; Denmark: Actos; Estonia: Actos, Glustin; Finland: Actos, Glustin; France: Actos; Germany: Actos, Glustin; Greece: Actos, Glustin; Hungary: Actos, Glustin; Ireland: Actos, Glustin; Italy: Actos, Glustin; Latvia: Actos, Glustin; Lithuania: Actos, Glustin; Malta: Actos, Glustin; Netherlands: Actos, Glustin; Poland: Actos, Glustin; Portugal: Actos, Glustin; Romania: Actos, Glustin; Slovakia: Actos, Glustin; Slovenia: Actos, Glustin; Spain: Actos, Glustin; Sweden: Actos, Glustin; UK: Actos.

North America

Canada: Actos, Pioglitazone; USA: Actos.

Latin America

Argentina: Actos, Cereluc, Higlucem, Pioglit, Piotamax; Brazil: Actos; Mexico: Zactos.


Japan: Actos.

Drug combinations

Pioglitazone and Glimepiride

Pioglitazone and Metformin


Pioglitazone Hydrochloride: C~19~H~20~N~2~O~3~S HCl. Mw: 392.90. (1) 2,4-Thiazolidinedione, 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-, monohydrochloride, (±)-; (2)(±)-5-[p-[2-(5-Ethyl-2-pyridyl)ethoxy]benzyl]-2,4-thiazolidinedione monohydrochloride. CAS-112529-15-4; CAS-111025-46-8 (pioglitazone)(1989).

Pharmacologic Category

Antidiabetic Agents; Thiazolidinediones. (ATC-Code: A10BG03).

Mechanism of action

Thiazolidinedione is an antidiabetic agent which lowers blood glucose by improving target cell response to insulin, without increasing pancreatic insulin secretion. Pioglitazone is a potent, selective agonist for peroxisome proliferator-activated receptor-gamma (PPARG). Activation of nuclear PPARG receptors influences production of a number of gene products involved in glucose and lipid metabolism.

Therapeutic use

Type 2 diabetes mellitus (non-insulin-dependent), monotherapy, or combination therapy with sulfonylurea, metformin, or insulin.

Pregnancy and lactiation implications

Pioglitazone is classified as pregnancy category C due to adverse effects observed in animal studies. Thiazolidinediones may cause ovulation in anovulatory premenopausal women, increasing risk of pregnancy. Maternal hyperglycemia can be associated with adverse effects in fetus, including macrosomia, neonatal hyperglycemia, and hyperbilirubinemia. Diabetes can also be associated with adverse effects in mother. Use of oral agents generally not recommended as routine management of gestational diabetes mellitus or type 2 diabetes mellitus during pregnancy. Not recommended during lactation.

Unlabeled use

Polycystic ovary syndrome.


Hypersensitivity to pioglitazone or any component of the formulation.

Warnings and precautions

Increased incidence of bone fractures in females. Thiazolidinediones, including pioglitazone, may cause or exacerbate heart failure. Not recommended for use in symptomatic heart failure. Initiation of therapy contraindicated in heart failure. Use with caution in edema (may increase plasma volume and/or cause fluid retention). May decrease hemoglobin/hematocrit (effects may be related to increased plasma volume). Dose-related weight gain observed with use (probably associated with fluid retention and fat accumulation). Use with caution in anemia (may reduce hemoglobin and hematocrit). Use in type 1 diabetes (insulin-dependent) or diabetic ketoacidosis not recommended. Use with caution in elevated transaminases (AST or ALT). Avoid use in patients who previously experienced jaundice during troglitazone therapy. Use with caution in pre-existing macular edema or diabetic retinopathy, and in premenopausal, anovulatory women (may result in resumption of ovulation, increasing risk of pregnancy).



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