Product Information
Registration Status: ActiveACTOS TABLET 30mg is approved to be sold in Singapore with effective from 2003-10-10. It is marketed by TAKEDA PHARMACEUTICALS (ASIA PACIFIC) PTE LTD, with the registration number of SIN12442P.
This product contains Pioglitazone 30mg in the form of TABLET. It is approved for ORAL use.
This product is manufactured by TAKEDA PHARMACEUTICAL CO LTD in JAPAN.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Pioglitazone is a medication belonging to the thiazolidinedione class of drugs that are used as adjuncts to diet, exercise, and other diabetes medications to manage type 2 diabetes mellitus. The thiazolidinedione class of medications exerts its pharmacological effect primarily by promoting insulin sensitivity and the improved uptake of blood glucose. Following entry into fat cell nuclei, pioglitazone selectively binds to the Peroxisome Proliferator-Activated Receptor Gamma (PPARγ)[A19757]. PPARs are ligand-activated transcription factors that are involved in the expression of more than 100 genes, and affect numerous metabolic processes, notably lipid and glucose homeostasis [A19759]. PPARγ in particular is abundantly expressed in lipid cells (adipocytes), where it plays a central role in lipid production and regulation of lipid metabolism.
Indication
Pioglitazone is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus [FDA Label].
Mechanism of Action
Pioglitazone acts as a selective agonist at Peroxisome Proliferator Activated Receptor Gamma (PPARγ) in target tissues for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPAR-gamma receptors increases the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In this way, pioglitazone both enhances tissue sensitivity to insulin and reduces the production of glucose via the liver (hepatic gluconeogenesis). Thus, insulin resistance associated with type 2 diabetes mellitus is improved without an increase in insulin secretion by pancreatic β cells.
Pharmacokinetics
- Absorption
- Following oral administration of pioglitazone, peak concentrations of pioglitazone were observed within 2 hours. Food slightly delays the time to peak serum concentration (T max) to 3 to 4 hours, but does not alter the extent of absorption (AUC). Steady state concentrations are achieved after 7 days of once daily administration of pioglitazone [FDA Label].
- Distribution
- 0.63 ± 0.41 L/kg [FDA Label]
- Metabolism
- Pioglitazone is extensively metabolized by hydroxylation and oxidation; the metabolites also partly convert to glucuronide or sulfate conjugates. Metabolites M-III and M-IV are the major circulating active metabolites in humans. The cytochrome P450 isoforms involved are CYP2C8 and, to a lesser degree, CYP3A4 with additional contributions from a variety of other isoforms including the mainly extrahepatic CYP1A1 [FDA Label].
- Elimination
Clearance
The apparent clearance of orally administered pioglitazone is 5 - 7 L/h [FDA Label].
Active Ingredient/Synonyms
(+-)-5-((4-(2-(5-Ethyl-2-pyridinyl)ethoxy)phenyl)methyl)-2,4-thiazolidinedione | 5-{4-[2-(5-ethylpyridin-2-yl)ethoxy]benzyl}-1,3-thiazolidine-2,4-dione | Pioglitazona | Pioglitazone | Pioglitazonum | Pioglitazone |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.