Monday, 29 January 2024

Dapagliflozin

Category/Class :  Sodium Glucose Co-transporter 2 (SGLT2) Inhibitors 

Mechanism of Action :  Ninety percent of the glucose re-absorption occurs through SGLT2 in the proximal convoluted tubule 

Inhibition of SGLT2: result in glucose excretion of only 30–50% of the amount filtered 

Drugs: dapagliflozin, canagliflozin, empagliflozin 

Pharmacokinetics : 

  • A: rapidly absorbed by the GI tract.

  • elimination half-life of dapagliflozin is 10–12 hours

  • E: 70% of the given dose is excreted in the urine in the form of 3-O-glucuronide 

 

Contraindications : not recommended in patients with more severe renal failure or advanced liver disease  


Drug interaction : 

  • Angiotensin II has been shown to induce SGLT2 production via the AT1 receptor. Thus, blockade of the renin-angiotensin- aldosterone axis may result in lower SGLT2 availability.

  • Concomitant rifampin administration reduces the total exposure to dapagliflozin by 22%

 

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