EMFLO

Each film coated tablets contains: (Empagliflozin  5mg / 10 mg / 25 mg )

Tablet for Oral Use

Empagliflozin is a highly potent, selective, competitive inhibitor of SGLT2 approved as a treatment for T2DM in patients with normal kidney function. Approximately 90 % of renal glucose reabsorption occurs in the first segment of the proximal tubule and is mediated by SGLT2, and the remaining 10 % is removed in the distal segment via SGLT1. Inhibition of SGLT2 decreases renal glucose reabsorption, promotes urinary glucose excretion (UGE) and reduces plasma glucose concentrations. Because SGLT2 inhibition occurs through an insulin-independent mechanism, the risk of hypoglycaemia is low.

Absorption: After oral administration, Empagliflozin exhibits rapid absorption, reaching peak levels 1.5 hours after a single dose.

Distribution: Empagliflozin is 86.2% protein-bound in healthy volunteers and distributed to tissues and fluids. Approximately 36.8% of Empagliflozin is partitioned into red blood cells in healthy volunteers. Empagliflozin has a population-based volume of distribution of approximately 73.8 L at steady state.

Metabolism: Empagliflozin is primarily metabolized by glucuronidation by UGT2B7, UGT1A3, UGT1A8, and UGT1A9. There are no major metabolites of Empagliflozin in the plasma; however, three conjugates were found with each metabolite, consisting of less than 10% of the total drug in circulation. Empagliflozin exerts renal excretion.

Half Life: The terminal elimination half-life (t_½) was up to 13.1 h. 

• Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes
• Also indicated to reduce the risk of cardiovascular death in adults with type 2 diabetes mellitus and cardiovascular disease
• Nephropathy (urine albumin-to-creatinine >300 mg/g)
• Indicated in adults for the treatment of symptomatic chronic heart failure with reduced ejection fraction

ADVERSE REACTION

Empagliflozin has several adverse effects including frequent urination, burning while urinating, dizziness, or lightheadedness, dehydration, hypotension, ketoacidosis, acute kidney injury, genital mycotic infections, and hypoglycemia when used with insulin, dyslipidemia, and pyelonephritis.

DOSAGE AND ADMINISTRATION:

Empagliflozin is administered at an initial dose of 10 mg orally in the morning, with a gradual increase to a maximum dose of 25 mg once daily if necessary

CONTRAINDICATIONS

Empagliflozin is contraindicated in patients with serious hypersensitivity to any components of the formulation, severe renal impairment (estimated glomerular filtration rate [eGFR] less than 30 mL/min/1.73 m²), end-stage renal disease, or dialysis. Empagliflozin should not be initiated if eGFR is less than 45 mL/min/1.73 m. Empagliflozin is not for use with patients with Type 1 diabetes or those with diabetic ketoacidosis.

WARNINGS AND PRECAUTIONS:

• Should not be used during 2^nd and 3^rd trimester of Pregenancy and Breast Feeding
• Use in caution with Older adults as they may be more sensitive to the side effects of this drug, especially dehydration, kidney problems, and dizziness/fainting 

Pregnancy Category: C

Drug Interaction:

• Coadministration of Empagliflozin with diuretics resulted in increased urine volume and frequency of voids, which might enhance the potential for volume depletion.
• Coadministration of Empagliflozin with insulin or insulin secretagogues increases the risk for hypoglycemia.