Empagliflozin: Advanced Glycemic Control with Cardio-Renal Benefits
| Product dosage: 10 mg | |||
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| Product dosage: 25 mg | |||
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Synonyms | |||
Empagliflozin is a sodium-glucose cotransporter 2 (SGLT2) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It represents a significant advancement in the therapeutic landscape, offering a unique insulin-independent mechanism of action. By inhibiting SGLT2 in the proximal renal tubules, it reduces renal glucose reabsorption and increases urinary glucose excretion. Beyond its primary glucose-lowering effects, empagliflozin has demonstrated substantial benefits in reducing cardiovascular mortality and hospitalization for heart failure in patients with established cardiovascular disease, as well as slowing the progression of kidney disease.
Features
- Pharmacological Class: Sodium-glucose cotransporter 2 (SGLT2) inhibitor
- Available Formulations: Oral tablets (10 mg and 25 mg)
- Mechanism of Action: Selective and reversible inhibition of SGLT2 in the proximal convoluted tubule
- Bioavailability: Approximately 78%
- Time to Peak Plasma Concentration (Tmax): 1.5 hours
- Elimination Half-life: Approximately 12.4 hours
- Metabolism: Minimally metabolized, primarily via UGT1A3, UGT1A8, UGT1A9, and UGT2B7
- Excretion: Primarily excreted unchanged in feces (41.2%) and urine (54.4%)
Benefits
- Provides effective and sustained HbA1c reduction through an insulin-independent mechanism.
- Reduces the risk of cardiovascular death in adult patients with type 2 diabetes and established cardiovascular disease.
- Lowers the risk of hospitalization for heart failure in both diabetic and non-diabetic patient populations with heart failure.
- Slows the progression of kidney disease, including reducing the risk of sustained decline in eGFR, end-stage kidney disease, and cardiovascular death in patients with chronic kidney disease.
- Promotes modest weight loss and a reduction in systolic blood pressure.
- Lowers the risk of hyperglycemia with a minimal associated risk of hypoglycemia when not used with insulin or insulin secretagogues.
Common use
Empagliflozin is primarily prescribed for the management of type 2 diabetes mellitus in adults. Its use has been expanded based on landmark clinical trials. It is now also indicated to reduce the risk of cardiovascular death in adults with type 2 diabetes and established cardiovascular disease. Furthermore, it is approved to reduce the risk of cardiovascular death and hospitalization for heart failure in adults with heart failure (NYHA Class II-IV), regardless of ejection fraction and diabetes status. It is also indicated to reduce the risk of sustained decline in eGFR, end-stage kidney disease, cardiovascular death, and hospitalization for heart failure in adults with chronic kidney disease at risk of progression.
Dosage and direction
The recommended starting dosage is 10 mg administered orally once daily, taken in the morning, with or without food. Based on glycemic efficacy and tolerability, the dosage may be increased to 25 mg once daily. For patients with volume depletion, correcting this condition prior to initiation is recommended. In patients with chronic kidney disease with an eGFR between 20 to less than 45 mL/min/1.73m², the dose is 10 mg once daily. It is not recommended when eGFR is less than 20 mL/min/1.73m², and it is contraindicated in patients on dialysis. The tablet should be swallowed whole with a glass of water.
Precautions
- Ketoacidosis: Cases of ketoacidosis, including life-threatening and fatal cases, have been reported in patients with type 1 and type 2 diabetes receiving SGLT2 inhibitors. This may occur even with blood glucose levels below 250 mg/dL. Assess patients who present with symptoms consistent with metabolic acidosis.
- Volume Depletion: Empagliflozin can cause intravascular volume contraction which may sometimes manifest as symptomatic hypotension or acute transient changes in creatinine. Assessment of volume status and correction of volume depletion is recommended before initiation, particularly in elderly patients, those on diuretics, or with renal impairment.
- Urosepsis and Pyelonephritis: Serious urinary tract infections, including urosepsis and pyelonephritis, have been reported. Evaluate for signs and symptoms of urinary tract infections and treat promptly.
- Hypoglycemia: The risk of hypoglycemia is increased when empagliflozin is co-administered with insulin or an insulin secretagogue (e.g., sulfonylurea). A lower dose of the insulin or secretagogue may be required to reduce the risk of hypoglycemia.
- Necrotizing Fasciitis of the Perineum (Fournier’s Gangrene): Rare but serious, life-threatening cases have been reported in patients with diabetes mellitus taking SGLT2 inhibitors. Assess patients presenting with pain or tenderness, erythema, or swelling in the genital or perineal area, along with fever or malaise.
- Genital Mycotic Infections: Empagliflozin increases the risk for genital mycotic infections. Patients with a history of chronic or recurrent infections are more susceptible.
Contraindications
Empagliflozin is contraindicated in patients with a history of serious hypersensitivity reaction to empagliflozin or any of the excipients in the formulation. It is also contraindicated in patients with severe renal impairment (eGFR less than 30 mL/min/1.73m²) for glycemic control, in patients with an eGFR less than 20 mL/min/1.73m² for any indication, and in patients on dialysis.
Possible side effect
The most common adverse reactions (≥5% incidence) are urinary tract infections and female genital mycotic infections. Other reported side effects include:
- Male genital mycotic infections (e.g., balanitis)
- Volume depletion-related events (e.g., hypotension, dizziness, orthostatic hypotension)
- Increased urination
- Dyslipidemia (increased LDL-C)
- Nausea
- Joint pain (arthralgia)
- Pruritus
- Increased thirst (polydipsia)
Serious but less common side effects include ketoacidosis, acute kidney injury, urosepsis, pyelonephritis, and Fournier’s gangrene.
Drug interaction
- Diuretics: Coadministration with diuretics may enhance the potential for volume depletion and hypotension. Monitor blood pressure and volume status.
- Insulin and Insulin Secretagogues: Coadministration increases the risk of hypoglycemia. A reduction in the dose of insulin or the secretagogue may be necessary.
- Lithium: SGLT2 inhibitors may decrease lithium concentrations. More frequent monitoring of lithium serum concentrations is recommended.
- UGT Inducers: Drugs that induce UGT enzymes (e.g., rifampin, phenytoin, ritonavir) may decrease empagliflozin exposure. Efficacy should be monitored.
- Positive Urine Glucose Tests: SGLT2 inhibitors will cause a positive test for glucose in the urine. Use alternative methods for monitoring glycemic control.
Missed dose
Instruct the patient to take the missed dose as soon as it is remembered on the same day. If the missed dose is not remembered until the next day, the patient should skip the missed dose and resume the usual dosing schedule. The patient should not take a double dose to make up for a missed one.
Overdose
There is limited experience with overdose in humans. The maximum single dose administered in clinical studies was 100 mg, which was not associated with any specific adverse reactions. In the event of a suspected overdose, contact a Poison Control Center immediately. Management should consist of general supportive measures, including monitoring of vital signs and blood glucose levels, and hydration. Empagliflozin is negligibly dialyzable; therefore, hemodialysis is not expected to enhance elimination.
Storage
Store empagliflozin tablets at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F). Keep the bottle tightly closed to protect from moisture. Keep out of reach of children and pets. Do not use after the expiration date printed on the bottle.
Disclaimer
This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content is provided on an “as is” basis.
Reviews
- “As a cardiologist, the EMPA-REG OUTCOME data was practice-changing. Empagliflozin is now a cornerstone therapy for my patients with type 2 diabetes and cardiovascular disease. The mortality benefit is undeniable.” – Dr. A. Sharma, MD, Cardiology
- “From a nephrology perspective, the EMPA-KIDNEY trial solidified the role of empagliflozin in CKD management. Its ability to slow eGFR decline and reduce renal-specific hard endpoints is a monumental achievement in our field.” – Dr. L. Chen, MD, Nephrology
- “In clinical practice, patients appreciate the once-daily dosing and the side effect of weight loss. We must remain vigilant for signs of genital infections and volume depletion, especially upon initiation, but overall, it is a well-tolerated and highly effective agent.” – C. Robinson, NP, Endocrinology
- “The paradigm shift towards organ protection in diabetes management is largely thanks to drugs like empagliflozin. It moves us beyond simple glucose-lowering to addressing the macrovascular and microvascular complications that truly impact patient morbidity and mortality.” – Dr. M. Ibrahim, MD, Endocrinology