Glyxambi

Glyxambi Uses, Dosage, Side Effects, Food Interaction and all others data.

Empagliflozin is a sodium glucose co-transporter-2 (SGLT-2) inhibitor. SGLT2 co-transporters are responsible for reabsorption of glucose from the glomerular filtrate in the kidney. The glucuretic effect resulting from SGLT2 inhibition reduces renal absorption and lowers the renal threshold for glucose, resulting in increased glucose excretion. Additionally, it contributes to reduced hyperglycaemia, assists weight loss, and reduces blood pressure.

Empagliflozin lowers blood glucose levels by preventing glucose reabsorption in the kidneys, thereby increasing the amount of glucose excreted in the urine. It has a relatively long duration of action requiring only once-daily dosing. Patients should be monitored closely for signs and symptoms of ketoacidosis regardless of blood glucose level as empagliflozin may precipitate diabetic ketoacidosis in the absence of hyperglycemia. As its mechanism of action is contingent on the renal excretion of glucose, empagliflozin may be held in cases of acute kidney injury and/or discontinued in patients who develop chronic renal disease.

The overexcretion of glucose creates a sugar-rich urogenital environment which increases the risk of urogenital infections - including urosepsis, pyelonephritis, mycotic infections, and even Fournier's gangrene - in both male and female patients - monitor closely for signs and symptoms of developing infection.

Trade Name Glyxambi
Generic empagliflozin + linagliptan
Weight 10mg, 25mg, , 10mg + 5mg, 25mg + 5mg
Type Tablet, Oral Tablet
Therapeutic Class
Manufacturer Boehringer Ingelheim Limited
Available Country Australia, Canada, United Kingdom, India, United States,
Last Updated: September 19, 2023 at 7:00 am
Glyxambi
Glyxambi

Uses

Empagliflozin is used for:

  • As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus and
  • To reduce the risk of cardiovascular death in adult patients with type 2 diabetes mellitus and established cardiovascular disease

Glyxambi is also used to associated treatment for these conditions: Cardiovascular Mortality, Type 2 Diabetes Mellitus

How Glyxambi works

The vast majority of glucose filtered through the glomerulus is reabsorbed within the proximal tubule, primarily via SGLT2 (sodium-glucose linked co-transporter-2) which is responsible for ~90% of the total glucose reabsorption within the kidneys. Na+/K+-ATPase on the basolateral membrane of proximal tubular cells utilize ATP to actively pump Na+ ions into the interstitium surrounding the tubule, establishing a Na+ gradient within the tubular cell. SGLT2 on the apical membrane of these cells then utilize this gradient to facilitate secondary active co-transport of both Na+ and glucose out of the filtrate, thereby reabsorbing glucose back into the blood – inhibiting this co-transport, then, allows for a marked increase in glucosuria and decrease in blood glucose levels. Empagliflozin is a potent inhibitor of renal SGLT2 transporters located in the proximal tubules of the kidneys and works to lower blood glucose levels via an increase in glucosuria.

Empagliflozin also appears to exert cardiovascular benefits - specifically in the prevention of heart failure - independent of its blood glucose-lowering effects, though the exact mechanism of this benefit is not precisely understood. Several theories have been posited, including the potential inhibition of Na+

Dosage

Glyxambi dosage

The recommended dose of Empagliflozin is 10 mg once daily, taken in the morning, with or without food. In patients tolerating Empagliflozin, the dose may be increased to 25 mg once daily. In patients with volume depletion, correcting this condition prior to initiation of Empagliflozin is recommended.

Side Effects

The most common adverse reactions associated with Empagliflozin are urinary tract infections and female genital mycotic infections. Others common side effects includes dehydration, hypotension, weakness, dizziness and increased thirstiness.

Toxicity

Experience with empagliflozin overdose is limited - employ standard symptomatic and supportive measures, as well as gastric decontamination when appropriate. The use of hemodialysis in empagliflozin overdose has not been studied but is unlikely to be of benefit given the drug's relatively high protein-binding.

Precaution

Assessment of renal function is recommended prior to initiation of Empagliflozin and periodically thereafter. Empagliflozin should not initiated in patients with an eGFR less than 45 ml/min/1.73 m2. No dose adjustment is needed in patients with an eGFR greater than or equal to 45 ml/min/1.73 m2.

Interaction

Diuretics: Co-administration of Empagliflozin with diuretics resulted in increased urine volume.

Insulin or Insulin Secretagogues: Co-administration of Empagliflozin with insulin or insulin secretagogues increases the risk for hypoglycemia.

Positive Urine Glucose Test: Monitoring glycemic control with urine glucose tests is not recommended in patients taking SGLT2 inhibitors as SGLT2 inhibitors increase urinary glucose excretion and will lead to positive urine glucose tests. Use alternative methods to monitor glycemic control.

Interference with 1,5-anhydroglucitol (1,5-AG) Assay: Monitoring glycemic control with 1,5-AG assay is not recommended as measurements of 1,5-AG are unreliable in assessing glycemic control in patients taking SGLT2 inhibitors. Use alternative methods to monitor glycemic control.

Volume of Distribution

The estimated apparent steady-state volume of distribution is 73.8 L.

Elimination Route

Following oral administration, peak plasma concentrations are reached in approximately 1.5 hours (Tmax). At steady-state, plasma AUC and Cmax were 1870 nmol·h/L and 259 nmol/L, respectively, following therapy with empagliflozin 10mg daily and 4740 nmol·h/L and 687 nmol/L, respectively, following therapy with empagliflozin 25mg daily. Administration with food does not significantly affect the absorption of empagliflozin.

Half Life

The apparent terminal elimination half-life was found to be 12.4 h based on population pharmacokinetic analysis.

Clearance

Apparent oral clearance was found to be 10.6 L/h based on a population pharmacokinetic analysis.

Elimination Route

After oral administration of radiolabeled empagliflozin approximately 41.2% of the administered dose was found eliminated in feces and 54.4% eliminated in urine. The majority of radioactivity in the feces was due to unchanged parent drug while approximately half of the radioactivity in urine was due to unchanged parent drug.

Pregnancy & Breastfeeding use

There are no adequate and well-controlled studies of Empagliflozin in pregnant women. Empagliflozin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known if Empagliflozin is excreted in human milk. It is not recommended when breastfeeding.

Contraindication

Empagliflozin is contraindicated in patients with history of serious hypersensitivity reaction to Empagliflozin or any of its ingredients, severe renal impairment, end-stage renal disease, or dialysis.

Storage Condition

Keep in a cool & dry place (below 30° C), protected from light & moisture. Keep out of the reach of children.

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