Product Information
Registration Status: InactiveSIN14929P
THIS PRODUCT HAS BEEN DEREGISTERED!
OSENI FILM COATED TABLET 12.5MG/ 15MG is approved to be sold in Singapore with effective from 2016-01-26. It is marketed by TAKEDA PHARMACEUTICALS (ASIA PACIFIC) PTE LTD, with the registration number of SIN14929P.
This product contains ALOGLIPTIN 12.5mg, and PIOGLITAZONE 15mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by Takeda Pharmaceutical Company Limited in UNITED STATES, and Osaka Plant 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.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
Alogliptin is a selective, orally-bioavailable inhibitor of enzymatic activity of dipeptidyl peptidase-4 (DPP-4). Chemically, alogliptin is prepared as a benzoate salt and exists predominantly as the R-enantiomer (>99%). It undergoes little or no chiral conversion in vivo to the (S)-enantiomer. FDA approved January 25, 2013.
Indication
Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Mechanism of Action
Alogliptin inhibits dipeptidyl peptidase 4 (DPP-4), which normally degrades the incretins glucose-dependent insulinotropic polypeptide (GIP) and glucagon like peptide 1 ( GLP-1). The inhibition of DPP-4 increases the amount of active plasma incretins which helps with glycemic control. GIP and GLP-1 stimulate glucose dependent secretion of insulin in pancreatic beta cells. GLP-1 has the additional effects of suppressing glucose dependent glucagon secretion, inducing satiety, reducing food intake, and reducing gastric emptying.
Pharmacokinetics
- Absorption
- The pharmacokinetics of NESINA was also shown to be similar in healthy subjects and in patients with type 2 diabetes. When single, oral doses up to 800 mg in healthy subjects and type 2 diabetes patients are given, the peak plasma alogliptin concentration (median Tmax) occurred 1 to 2 hours after dosing. Accumulation of aloglipin is minimal. The absolute bioavailability of NESINA is approximately 100%. Food does not affect the absorption of alogliptin.
- Distribution
- Following a single, 12.5 mg intravenous infusion of alogliptin to healthy subjects, the volume of distribution during the terminal phase was 417 L, indicating that the drug is well distributed into tissues.
- Metabolism
- Alogliptin does not undergo extensive metabolism. Two minor metabolites that were detected are N-demethylated alogliptin (
- Elimination
Clearance
Renal clearance = 9.6 L/h (this value indicates some active renal tubular secretion); Systemic clearance = 14.0 L/h.
Toxicity
Common adverse reactions (reported in ≥4% of patients treated with alogliptin 25 mg and more frequently than in patients who received placebo) are: nasopharyngitis, headache, and upper respiratory tract infection.
Active Ingredient/Synonyms
Alogliptina | Alogliptine | Alogliptinum | SYR-322 | Alogliptin |
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.
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.