Empagliflozin

Empagliflozin is an active ingredient used to treat type 2 diabetes. The substance belongs to the class of SGLT2 inhibitors. It is also used as an adjuvant in the treatment of chronic heart failure. It can be used alone or in combination with other antidiabetic agents and is taken orally. Empagliflozin was developed by Boehringer Ingelheim and first approved in 2014.

Pharmacodynamics and mechamism of action.

Empagliflozin lowers blood glucose levels by preventing glucose uptake in the kidneys, thereby increasing the amount of glucose excreted in the urine. It has a relatively long duration of action and only needs to be taken once daily.

The majority of glucose filtered through the glomerulus is reabsorbed in the proximal tubule, primarily via the SGLT2 transporter, which is responsible for approximately 90% of total glucose reabsorption in the kidneys. SGLT2 causes the co-transport of Na+ and glucose from the filtrate back into the blood. Inhibition of this co-transport by empagliflozin allows a significant increase in glucosuria and a decrease in blood glucose levels without affecting insulin secretion.

Pharmacokinetics

After oral administration, peak plasma concentration is reached within approximately 1.5 hours (Tmax). The apparent volume of distribution is 73.8 L. Empagliflozin is approximately 86.2% protein-bound in plasma. Empagliflozin is minimally metabolized in the liver. After oral administration, approximately 45% of the administered dose is excreted in feces and 55% in urine. The elimination half-life is approximately 12.4 hours.

Drug Interactions

There are several drug interactions that must be considered when taking empagliflozin. Drugs that also lower blood glucose levels, such as insulin or sulfonylureas, should not be taken concomitantly with empagliflozin, as excessive blood glucose lowering may result. Simultaneous use with diuretics should also be avoided, as the effect of the diuretics may be increased.

Side effects

One of the most common side effects is an increased incidence of urogenital tract infections. Oversecretion of glucose leads to a sugar-rich urogenital environment, which increases the risk of urogenital infections in male and female patients. Diarrhea and dizziness due to a decrease in blood pressure are also possible side effects. In rare cases, allergic reactions or acute renal failure may also occur.

Contraindications

Since its mode of action depends on renal excretion of glucose, empagliflozin should not be used in acute renal failure or in patients suffering from chronic kidney disease. If the treated individual is suffering from ketoacidosis, the use of empagliflozin is also contraindicated.