Product Information
Registration Status: ActiveTRAJENTA FILM-COATED TABLET 5MG is approved to be sold in Singapore with effective from 2012-08-02. It is marketed by BOEHRINGER INGELHEIM SINGAPORE PTE LTD, with the registration number of SIN14101P.
This product contains Linagliptin 5mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by Boehringer Ingelheim Roxane Inc. in UNITED STATES.
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
Linagliptin is a DPP-4 inhibitor developed by Boehringer Ingelheim for the treatment of type II diabetes. Two pharmacological characteristics that sets linagliptin apart from other DPP-4 inhibitors is that it has a non-linear pharmacokinetic profile and is not primarily eliminated by the renal system. FDA approved on May 2, 2011.
Indication
Linagliptin is used for the management of type 2 diabetes mellitus.
Mechanism of Action
Linagliptin is a competitive and reversible dipeptidyl peptidase (DPP)-4 enzyme inhibitor that slows the breakdown of insulinotropic hormone glucagon-like peptide (GLP)-1 for better glycemic control in diabetes patients. GLP and glucose-dependent insulinotropic polypeptide (GIP) are incretin hormones that increase the production and release of insulin from pancreatic beta cells and decrease the release of glucagon from pancreatic alpha cells. This results in a overall decrease in glucose production in the liver and increase an of insulin in a glucose-dependent manner.
Pharmacokinetics
- Absorption
- Cmax, 5 mg, healthy subjects = 8.32 nmol/L; Tmax, 5 mg, healthy subjects = 1.75 hours; AUC(0-24 hours), 5 mg, healthy subjects = 119 nmol · h/L; Bioavailability, healthy subjects = 30%. When a dose of 5 mg once daily is given, steady state is achieved by the third dose. Although a high fat meal reduces Cmax and increases AUC, this interaction with food is not clinically significant. Linagliptin may be administered with or without food.
- Distribution
- Vd = 1110 L
- Metabolism
- Linagliptin is not extensively metabolized, 90% of dose is excreted unchanged. The small portion of drug that is metabolized, the main metabolite is CD 1790 and is pharmacologically inactive. Glucuronidation forms some of its other minor metabolites.
- Elimination
Clearance
Renal clearance, steady state = 70 mL/min
Active Ingredient/Synonyms
(R)-8-(3-Aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methylquinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione | Trajenta | Linagliptin |
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.