EMPERA

COMPOSITION:

Empera 10 :  

Each film coated tablet contains Empagliflozin 10 mg                                                          

Empera 25:   

Each film coated tablet contains Empagliflozin 25 mg                                

CLINICAL PHARMACOLOGY:

Mechanism of Action:

Empagliflozin is a potent, selective, and reversible inhibitor of sodium-glucose co-transporter 2 (SGLT2), which is primarily expressed in the kidney and plays a key role in glucose reabsorption from the glomerular filtrate. It is 5000 times more selective for SGLT2 compared to SGLT1, the major glucose transporter in the gut. In type 2 diabetes, where glucose reabsorption is elevated, empagliflozin increases urinary glucose excretion immediately after the first dose and maintains this effect continuously over a 24-hour dosing period.

Pharmacokinetics:

Absorption:Empagliflozin demonstrates favorable pharmacokinetics for managing type 2 diabetes mellitus. After oral administration, it is rapidly absorbed, reaching peak plasma concentrations (Tmax) within 1.5 hours. The drug exhibits a high oral bioavailability of approximately 78%, 

Distribution:  plasma protein binding exceeding 86%. 

Metabolism:It is metabolized minimally, primarily via glucuronidation by UGT2B7, UGT1A3, and to a lesser extent by CYP450 enzymes.

Elimination: Empagliflozin is excreted mostly unchanged in urine (approximately 50%) and feces, with a terminal half-life of 12-13 hours, supporting once-daily dosing.

INDICATIONS AND USAGE:

Type 2 diabetes mellitus

Empagliflozin is indicated for the treatment of adults with insufficiently controlled type 2 diabetes mellitus as an adjunct to diet and exercise

- as monotherapy when metformin is considered inappropriate due to intolerance

- in addition to other medicinal products for the treatment of diabetes

Heart failure

Empagliflozin is indicated in adults for the treatment of symptomatic chronic heart failure.

DOSAGE AND ADMINISTRATION:

Type 2 diabetes mellitus

The recommended starting dose is 10 mg empagliflozin once daily for monotherapy and add-on combination therapy with other medicinal products for the treatment of diabetes. In patients tolerating empagliflozin 10 mg once daily who have an eGFR ≥60 ml/min/1.73 m2 and need tighter glycaemic control, the dose can be increased to 25 mg once daily. The maximum daily dose is 25 mg.

Heart failure

The recommended dose is 10 mg empagliflozin once daily.

WARNINGS AND PRECAUTIONS:

Warning:

Empagliflozin should be used with caution in patients with a history of genital or urinary tract infections, as it may increase the risk of these conditions. It can cause volume depletion, leading to hypotension, particularly in elderly patients or those on diuretics. Ketoacidosis, including euglycemic ketoacidosis, has been reported and warrants immediate discontinuation if suspected. 

Precautions:

Renal function should be monitored regularly, as the drug may reduce glomerular filtration rate (GFR) and is not recommended for patients with severe renal impairment. Additionally, it may elevate the risk of lower limb amputations and fractures, necessitating careful patient evaluation.

ADVERSE REACTIONS:

Vaginal moniliasis, Vulvovaginitis, Urinary tract infection, Hypoglycaemia( when used with sulphonylurea or insulin), Thirst, Constipation, Pruritis , Rash, Urticaria, Angioedema, Volume depletion, Increased urination.

DRUG INTERACTIONS:

Diuretics

Empagliflozin may add to the diuretic effect of thiazide and loop diuretics and may increase the risk of dehydration and hypotension.

Insulin and insulin secretagogues

Insulin and insulin secretagogues, such as sulphonylureas, may increase the risk of hypoglycaemia. Therefore, a lower dose of insulin or an insulin secretagogue may be required to reduce the risk of hypoglycaemia when used in combination with empagliflozin.

USE IN SPECIFIC POPULATION:

Pregnancy: There are no data from the use of empagliflozin in pregnant women. As a precautionary measure, it is preferable to avoid the use of Empagliflozin during pregnancy.

Nursing Mother: No data in humans are available on excretion of empagliflozin into milk. A risk to the newborns/infants cannot be excluded. Empagliflozin should not be used during breast-feeding.

Pediatric Use: The safety and efficacy of empagliflozin in pediatric patients have not been established. It is not recommended for use in children and adolescents under 18 years of age due to a lack of clinical studies in this population. 

Geriatric Use: Empagliflozin can be used in elderly patients; however, caution is advised due to an increased risk of adverse effects such as volume depletion, hypotension, and impaired renal function. Monitoring of renal function and hydration status is essential, especially in patients aged 65 years or older. Dose adjustments may be required based on the individual's renal status and overall health condition.

CONTRAINDICATIONS:

Hypersensitivity to the active substance.

OVERDOSAGE:

In clinical studies, single doses of up to 800 mg and multiple daily doses up to 100 mg of empagliflozin showed no toxicity in healthy volunteers and patients with type 2 diabetes. Empagliflozin increased urine glucose excretion, leading to a rise in urine volume, which was not dose-dependent or clinically significant. There is no data available for doses above 800 mg in humans.

STORAGE:

Store in well-closed containers, at controlled room temperature.

PRESENTATION:

Empera 10/25: Carton containing 3 blister strips of 10 tablets each.