About: Dapagliflozin     Goto   Sponge   Distinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/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. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Obermeier M, Yao M, Khanna A, Koplowitz B, Zhu M, Li W, Komoroski B, Kasichayanula S, Discenza L, Washburn W, Meng W, Ellsworth BA, Whaley JM, Humphreys WG: In vitro characterization and pharmacokinetics of dapagliflozin (BMS-512148), a potent sodium-glucose cotransporter type II inhibitor, in animals and humans. Drug Metab Dispos. 2010 Mar;38(3):405-14. doi: 10.1124/dmd.109.029165. Epub 2009 Dec 8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19996149 # Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical Pharmacokinetics and Pharmacodynamics of Dapagliflozin, a Selective Inhibitor of Sodium-Glucose Co-transporter Type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/24105299 # Kasichayanula S, Chang M, Hasegawa M, Liu X, Yamahira N, LaCreta FP, Imai Y, Boulton DW: Pharmacokinetics and pharmacodynamics of dapagliflozin, a novel selective inhibitor of sodium-glucose co-transporter type 2, in Japanese subjects without and with type 2 diabetes mellitus. Diabetes Obes Metab. 2011 Apr;13(4):357-65. doi: 10.1111/j.1463-1326.2011.01359.x. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21226818 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • 13.8 hours with the consumption of a 50 mg dose. (en)
http://linked.open...ugbank/indication
  • Dapagliflozin is indicated for adjunct management of glycemic control in patients with type 2 diabetes mellitus, in combination with diet and exercise. (en)
sameAs
Title
  • Dapagliflozin (en)
adms:identifier
http://linked.open...mechanismOfAction
  • 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. (en)
http://linked.open.../drugbank/synonym
  • (2S,3R,4R,5S,6R)-2-[4-chloro-3-(4-ethoxybenzyl)phenyl]-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol (en)
http://linked.open...drugbank/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. (en)
http://linked.open.../drugbank/mixture
http://linked.open...nk/proteinBinding
  • 91%. (en)
http://linked.open...ogy/drugbank/salt
  • (en)
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http://linked.open...ugbank/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. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 461432-26-8 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...rugbank/clearance
  • Oral plasma clearance of 4.9 mL/min/kg, and a renal clearance of 5.6 mL/min. (en)
http://linked.open...k/Bioavailability
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http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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