empagliflozin

Action and Spectrum

Actions and Spectrum: 

• Glucose-lowering effect: empagliflozin lowers blood glucose levels by reducing the reabsorption of glucose in the kidneys. This effect is independent of insulin and can be used in patients with type 2 diabetes who have inadequate insulin secretion or insulin resistance. 
• Weight loss: empagliflozin has been associated with weight loss in some patients, which may be related to the increased urinary glucose excretion and reduction in calorie absorption. 
• Blood pressure-lowering effect: empagliflozin has been shown to reduce blood pressure in patients with type 2 diabetes. This effect may be related to the reduction in sodium reabsorption in the kidneys, which can lead to decreased extracellular fluid volume and reduced arterial pressure. 
• Cardiovascular benefits: In clinical trials, empagliflozin has been shown to reduce the risk of cardiovascular events, such as heart attack, stroke, and cardiovascular death, in patients with type 2 diabetes and established cardiovascular disease. 
• Renal benefits: empagliflozin has been shown to slow the progression of chronic kidney disease in patients with type 2 diabetes and established cardiovascular disease. 

Drug Interaction

Adverse Reaction

Frequency Defined 

1-10% 

Female genital mycotic infections  

Increased urination  

Dyslipidemia  

Urinary tract infection  

Upper respiratory tract infection  

Male genital mycotic infections  

Nausea  

Polydipsia 

Arthralgia  

<1% 

Decreased blood pressure 

Hypotension 

Syncope 

Hypovolemia 

Nocturia 

Dehydration 

Polyurea 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

• Type 1 diabetes: empagliflozin is not indicated for the treatment of type 1 diabetes, as it works by reducing glucose reabsorption in the kidneys, which is not the primary defect in type 1 diabetes. 
• Diabetic ketoacidosis: empagliflozin is contraindicated in patients with a history of diabetic ketoacidosis (DKA) or current DKA. This is because empagliflozin may increase the risk of developing DKA, particularly in patients with a history of DKA or those with insulin deficiency. 
• Renal impairment: empagliflozin should be used with caution in patients with moderate to severe renal impairment, as it is primarily excreted by the kidneys. The dose of empagliflozin may need to be adjusted based on the patient’s renal function. 
• Volume depletion: empagliflozin may increase the risk of volume depletion, particularly in patients taking diuretics or with a history of low blood pressure. empagliflozin should be used with caution in these patients. 
• Genital mycotic infections: empagliflozin has been associated with an increased risk of genital mycotic infections, such as vaginal candidiasis, in some patients. Patients should be advised to report any signs or symptoms of genital mycotic infections to their healthcare provider. 

Pregnancy / Lactation

Pregnancy consideration:  

It is not secure to administer empagliflozin during pregnancy. 

Breastfeeding warnings:  

No data is available about the excretion of empagliflozin in human breast milk. Avoid using in lactating women. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women.  
• Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

empagliflozin is a sodium-glucose co-transporter 2 (SGLT2) inhibitor, which works by blocking the reabsorption of glucose in the kidneys. SGLT2 is a protein responsible for glucose reabsorption in the kidney tubules. empagliflozin selectively inhibits SGLT2, leading to increased glucose excretion in the urine, and thereby reducing blood glucose levels. 

Pharmacodynamics: 

• Glucose-lowering effects: empagliflozin reduces blood glucose levels by inhibiting SGLT2 in the kidneys. By reducing glucose reabsorption, empagliflozin increases glucose excretion in the urine and reduces the amount of glucose that is reabsorbed back into the bloodstream. 
• Independent of insulin: The glucose-lowering effect of empagliflozin is independent of insulin secretion and action. This means that empagliflozin can be used in patients with type 2 diabetes who have insulin resistance or who have inadequate insulin secretion. 
• Weight loss: empagliflozin has been associated with weight loss in some patients. This effect may be related to the increased urinary glucose excretion and the reduction in calorie absorption. 
• Blood pressure-lowering effects: empagliflozin has been shown to reduce blood pressure in patients with type 2 diabetes. This effect may be related to the reduction in sodium reabsorption in the kidneys, which can lead to decreased extracellular fluid volume and reduced arterial pressure. 

Pharmacokinetics: 

Absorption 

The peak plasma concentration is 259 nmol/L (for 10 mg/day), 687 nmol/L (for 25 mg/day) and is achieved in 1.5 hours 

The area under the curve is 1870 nmol•hr/L (for 10 mg/day) and 4740 nmol•hr/L (for 25 mg/day) 

Distribution 

Bound protein is 86.2%  

Red blood cells are 36.8% partitioned 

The volume of distribution is 73.8 L 

Metabolism 

No major metabolites are formed, the mostly present metabolites are 3 glucuronide conjugates  

Each metabolite is 10% less systemically exposed 

Elimination and Excretion 

The elimination half-life is 12.4 hours 

The rate of clearance is 10.6 L/hr 

The drug is excreted 54.4% in urine and 41.2% in feces 

Adminstartion

Administration: 

• Dosage: The recommended dose of empagliflozin is 10 mg once daily, taken in the morning. The dose may be increased to 25 mg once daily in patients who need additional glycemic control. 
• Administration: empagliflozin should be taken orally, with or without food. The tablet should be swallowed whole with a glass of water and should not be crushed, chewed, or broken. 
• Timing: empagliflozin should be taken at the same time each day to maintain consistent blood levels of the medication. 
• Missed Dose: If a dose of empagliflozin is missed, it should be taken as soon as possible, unless it is almost time for the next dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. 
• Storage: empagliflozin should be stored at room temperature, away from moisture and heat, and kept out of reach of children. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: empagliflozin 

Pronounced: EM-pa-gli-FLOE-zin 

Why do we use empagliflozin? 

It is used in: 

• Lowering blood glucose levels: empagliflozin helps to lower blood glucose levels by increasing urinary glucose excretion. 
• Improving glycemic control: empagliflozin is used to improve glycemic control in patients with type 2 diabetes, particularly when other treatments have not been effective. 
• Reducing the risk of cardiovascular events: empagliflozin has been shown to reduce the risk of cardiovascular events, such as heart attack and stroke, in patients with type 2 diabetes and established cardiovascular disease. 
• Weight loss: empagliflozin has been associated with modest weight loss in some patients, which may be beneficial for those who are overweight or obese. 
• Lowering blood pressure: empagliflozin has been shown to lower blood pressure in some patients, which may be helpful for those with hypertension.