Empagliflozin

BRAND NAMES:

Glyxambi – These are the combination of empagliflozin and linagliptin available in the form of Glyxambi empagliflozin and linagliptin tablets 10mg/5mg and 25mg/5mg. It helps in lowering the blood sugar of type 2 diabetes in adults.

Jardiance – It is a Jardiance empagliflozin tablet 10mg/25mg available in the market and used in reducing the death caused by cardiovascular failure with type 2 diabetes and also reducing the risk of kidney diseases.

Synjardy –  These are available in the market in the form of empagliflozin and metformin Hcl tablets 5mg/850mg, 5mg/1000mg, 12.5mg/850mg, and 12.5mg/1000mg.

Trijardy XR -  These are a combination of empagliflozin, linagliptin, and metformin Hcl extended-release tablets available in the composition with 25mg/5mg/1000mg, 12.5mg/2.5mg/1000mg, 10mg/5mg/1000mg and 5mg/12.5mg/1000mg.

MECHANISM OF ACTION:

Empagliflozin inhibits the sodium-glucose co-transporter-2 (SGLT-2) in the kidney's proximal tubules. It lowers renal reabsorption of glucose and increases urine excretion of glucose by inhibiting SGLT2. The drug's glucose-lowering action is insulin-independent. In type 2 diabetic patients, urine glucose excretion rose by approximately 64 grams per day with 10 mg of empagliflozin and 78 grams per day with 25 mg. Empagliflozin decreases salt and volume load, inducing intravascular contraction due to its diuretic and natriuretic effects. Empagliflozin is connected with weight loss and lower blood pressure without raising the risk of heart failure. 

PHARMACOKINETICS:

Absorption: Peak plasma concentrations occur around 1.5 hours after oral dosing. Empagliflozin absorption is not considerably affected when administered with meals.

Distribution: The anticipated steady-state volume for distribution is 73.8 L.

Metabolism: Empagliflozin has negligible metabolism. It is largely metabolised by glucoronidation by 5'-diphospho-glucarnosyltransferases 2B7, 1A3, 1A8, and 1A9, which produces three glucoronide metabolites: 2-O-, 3-O-, and 6-O-glucuronide. No metabolite accounted for more than 10% of all drug-related material.

Excretion: Following oral administration of radiolabeled empagliflozin, about 41.2% of the given dosage was excreted in feces and 54.4% in urine. The parent medicine accounted for the bulk of radioactivity in feces and around half in urine.

PHARMACODYNAMICS:

By preventing glucose reabsorption in the kidneys and enhancing glucose excretion in the urine, empagliflozin decreases blood glucose levels. It simply has to be taken once a day and has a rather lengthy duration of effect. Regardless of blood glucose level, patients should be routinely checked for diabetic ketoacidosis signs and symptoms since empagliflozin can induce the condition even when hyperglycemia is not present. Because empagliflozin's mode of action depends on the kidneys' ability to excrete glucose, it should be avoided in cases of acute kidney impairment and stopped in cases of chronic renal illness. 

Both male and female patients are more susceptible to urogenital infections due to the sugar-rich urogenital environment caused by excessive glucose excretion; keep an eye out for symptoms. 

DRUG STRENGTH AND ADMINISTRATION: 

Empagliflozin pills are available in 10mg and 25mg dosages. Oral administration, with or without food, as prescribed by your physician. 

Advise the patient to drink enough fluids to reduce the risk of hypotension. 

CONTRAINDICATIONS: 

Empagliflozin should not be used if your GFR is less than 45 ml/min or in the second and third trimesters of pregnancy. Other contraindications include end-stage renal illness, dialysis, or a severe allergic reaction to empagliflozin. It may be utilized in the presence of hepatic impairment. It is not suitable for persons with type 1 diabetes or diabetic ketoacidosis.

DRUG INTERACTIONS:

• Although certain medications should never be combined, two separate medications may be combined even if an interaction occurs. 
• Agmatine: When coupled with Empagliflozin, the risk or severity of hypoglycemia may rise.
• Salicylic acid may enhance the hypoglycemic properties of empagliflozin. 
• Empagliflozin's therapeutic efficacy may be reduced when used with niacin. 
• Gallopamil: When used in combination with Empagliflozin, the risk of severe hypoglycemia increases. 

FOOD INTERACTIONS: 

Consume with or without food. Co-administration with food changes pharmacokinetics slightly, but not significantly.

SIDE EFFECTS: 

• Low blood sugar symptoms include headaches, hunger, weakness, perspiration, disorientation, irritability, dizziness, and a high heart rate. 
• Dizziness, confusion, extreme thirst, and reduced urine output are all signs of dehydration. 
• Bladder infections are identified by painful or scorching urination, blood in the urine, and pelvic or back pain. 

OVERDOSE:

Empagliflozin overdose might cause difficulty breathing or passing out. Toxicity: The most often reported adverse effects included urinary tract infections, genital mycotic infections, and dyslipidemia. Dehydration, hypotension, and syncope have all been recorded as a result of the diuretic effects caused by volume depletion.

STORAGE:

Store at 25°C, with excursions permissible to 15-30°C. Store at room temperature, away from light and moisture.