Dapagliflozin

What is Dapagliflozin?

Dapagliflozin is an oral medication belonging to a class of drugs called sodium-glucose co-transporter 2 (SGLT2) inhibitors. It is primarily prescribed to help manage blood sugar levels in adults with type 2 diabetes mellitus. The medication works by blocking glucose reabsorption in the kidneys, allowing excess glucose to be eliminated through urine.

Uses

Dapagliflozin has several approved therapeutic applications:

Type 2 diabetes management: The primary use is as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes, either as monotherapy or in combination with other diabetes medications.

Heart failure with reduced ejection fraction: Used to reduce the risk of cardiovascular death and hospitalization for heart failure in adults with heart failure with reduced ejection fraction.

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Chronic kidney disease: Prescribed to reduce the risk of sustained decline in estimated glomerular filtration rate, end-stage kidney disease, cardiovascular death, and hospitalization for heart failure in adults with chronic kidney disease at risk of progression.

Heart failure with preserved ejection fraction: Helps reduce cardiovascular death and hospitalization for heart failure in adults with heart failure with mildly reduced or preserved ejection fraction.

How it works

Dapagliflozin blocks the SGLT2 protein in the proximal tubules of the kidneys, which normally reabsorbs about 90% of filtered glucose back into the bloodstream. By inhibiting this process, the medication causes excess glucose to be excreted in the urine, thereby lowering blood glucose levels. This mechanism also results in modest weight loss and blood pressure reduction due to the loss of calories and fluid through increased urination.

Side effects

Common side effects include:

• Increased urination and thirst
• Genital yeast infections
• Urinary tract infections
• Nausea
• Back pain
• Constipation
• Extremity pain
• Nasopharyngitis (common cold symptoms)

Serious side effects to watch for:

• Diabetic ketoacidosis (even with normal blood sugar levels)
• Serious urinary tract infections that may spread to kidneys
• Dehydration and low blood pressure
• Necrotizing fasciitis of the perineum (Fournier’s gangrene)
• Acute kidney injury

Warnings and precautions

Patients with severe kidney disease (eGFR less than 25 mL/min/1.73 m²) should not use dapagliflozin for diabetes management, though it may still be used for heart failure and kidney disease indications with appropriate monitoring. The medication is not recommended during pregnancy and breastfeeding due to potential risks to the developing fetus and nursing infant. Individuals with a history of diabetic ketoacidosis, frequent urinary tract infections, or genital infections should discuss these conditions with their healthcare provider before starting treatment. Patients should be counseled about maintaining adequate hydration and recognizing signs of ketoacidosis. Those scheduled for surgery or experiencing acute illness may need temporary discontinuation to reduce the risk of ketoacidosis.

Interactions

Insulin and insulin secretagogues: May increase the risk of hypoglycemia; dosage adjustments of these medications may be necessary.

Diuretics: Combined use may enhance the risk of dehydration and low blood pressure due to increased fluid loss.

Lithium: Dapagliflozin may increase lithium concentrations, requiring more frequent monitoring of lithium levels.

Digoxin: May slightly increase digoxin exposure, though dose adjustment is typically not required.

Rifampin: This antibiotic may reduce dapagliflozin effectiveness by increasing its metabolism.

Phenytoin and phenobarbital: These seizure medications may decrease dapagliflozin concentrations.

St. John’s Wort: This herbal supplement may reduce the effectiveness of dapagliflozin.

Alcohol: May increase the risk of lactic acidosis, particularly in patients with kidney problems.

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Dosage

For adults with type 2 diabetes, the typical starting dose is 5 mg once daily in the morning, which may be increased to 10 mg once daily if additional glycemic control is needed and the patient tolerates the initial dose well. For heart failure and chronic kidney disease indications, the recommended dose is 10 mg once daily. The medication can be taken with or without food. Dosage adjustments are not required for mild to moderate kidney impairment, but the drug should be discontinued if kidney function declines significantly. Healthcare providers will determine the appropriate dose based on individual patient factors, kidney function, and treatment goals.

Sources: FDA DailyMed drug labels (public domain), BNF, WHO Essential Medicines List. This article is for informational purposes only and does not constitute medical advice. Always consult your healthcare provider before starting or stopping any medication.

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