Endocrine System-Oral Antidiabetic drugs – Sodium glucose cotransport-2(SGLT-2) inhibitors

Endocrine System

Name of the Sodium glucose cotransport-2(SGLT-2) inhibitors Antidiabetic Drugs

Dapagliflozin
Dapagliflozin
Availability
tablet (Farxiga, generic) 5mg,10mg
Indication
To be used in the treatment of symptomatic chronic heart failure with reduced ejection fraction, with or without type 2 diabetes.
Mechanism of Action

Selective sodium-glucose transporter-2 (SGLT2) inhibitor

SGLT-2, expressed in the proximal renal tubules, is responsible for the majority of the reabsorption of filtered glucose from the tubular lumen; SGLT2 inhibitors will reduce glucose reabsorption and lower the renal threshold for glucose, thereby increasing urinary glucose excretion

Also reduces sodium reabsorption and increases the delivery of sodium to the distal tubule; this may influence several physiological functions, such as lowering both pre-and afterload of the heart and downregulating sympathetic activity

Pharmacokinetics
  • Bioavailability: 78%
  • Peak plasma time: 2 hr (fasting); ~3 hr (with high fat meal)
  • Protein bound: 91%
  • Metabolism primarily mediated by UGT1A9
  • Half-life: 12.9 hr
  • Excretion: 75% urine; 21% feces
Contraindications
  • Serious hypersensitivity to dapagliflozin (eg, anaphylaxis, angioedema)
  • Patients on dialysis

REFERENCES

  1. Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
  2. McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
  3. April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
  4. Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
  5. Nursebro.com, Search – Nursebro

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