Product Information
Registration Status: ActiveFORXIGA TABLET 10MG is approved to be sold in Singapore with effective from 2014-04-28. It is marketed by ASTRAZENECA SINGAPORE PTE LTD, with the registration number of SIN14542P.
This product contains Dapagliflozin 10mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by Bristol-Myers Squibb Manufacturing Company in UNITED STATES,AstraZeneca Pharmaceuticals LP in PUERTO RICO,Bristol-Myers Squibb S.R.L (Primary and Secondary packager) in ITALY, andAstraZeneca Pharmaceutical Co. Ltd (Primary and Secondary packager) in CHINA.
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
Dapagliflozin is indicated for the management of diabetes mellitus type 2, and functions to improve glycemic control in adults when combined with diet and exercise. Dapagliflozin is a sodium-glucose cotransporter 2 inhibitor, which prevents glucose reabsorption in the kidney. Using dapagliflozin leads to heavy glycosuria (glucose excretion in the urine), which can lead to weight loss and tiredness. Dapagliflozin was approved by the FDA on Jan 08, 2014. Dapagliflozin is not recommended for patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis.
Indication
Dapagliflozin is indicated for adjunct management of glycemic control in patients with type 2 diabetes mellitus, in combination with diet and exercise.
Mechanism of Action
A competitive inhibitor of the sodium-glucose transport subtype 2 protein, dapagliflozin blocks glucose reabsorption into the kidney, resulting in the elimination of blood glucose through the urine.
Pharmacokinetics
- Absorption
- Cmax is about 1 hour. (Obtained from 6 adult men in a fasted state administered a 50mg dose). 1.6% of unchanged dapagliflozin was found in the urine. A high-fat meal (52% caloric content) had no significant effect on previous pharmacokinetic parameters.
- Distribution
- Metabolism
- Dapagliflozin 3-O-glucuronide is the primary metabolite of dapagliflozin, with 61% of the dapagliflozin dose recovered in the urine as this metabolite. The metabolism of dapagliflozin is primarily mediated by UGT1A9-dependent glucuronide conjugation. The major metabolite, dapagliflozin 3-O-glucuronide, is not an SGLT2 inhibitor.
- Elimination
Clearance
Oral plasma clearance of 4.9 mL/min/kg, and a renal clearance of 5.6 mL/min.
Toxicity
Compared to placebo-treated patients, patients with moderate renal impairment treated with dapagliflozin did not have improvement in glycemic control and had more renal-related adverse reactions and more bone fractures; therefore, dapagliflozin should not be initiated in this population. Based on its mechanism of action, dapagliflozin is not expected to be effective in patients with severe renal impairment (eGFR less than 30 mL/min/1.73 m2) or ESRD.
Active Ingredient/Synonyms
(2S,3R,4R,5S,6R)-2-(4-Chloro-3-(4-ethoxybenzyl)phenyl)-6- (hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol | Dapagliflozin |
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.