Empagliflozin

Oral
Type 2 diabetes mellitus

eGFR <60 mL/min/1.73 m²: Do not initiate therapy or reduce to 10 mg daily in patients already taking empagliflozin. eGFR <45 mL/min/1.73 m², ESRD, patient on dialysis: Contraindicated.

May be taken with or without food.

Severe renal impairment (eGFR <45 mL/min/1.73 m²), ESRD, patient on dialysis. Lactation.

Patient with history of genital mycotic infections, risk factors that may predispose ketoacidosis (e.g. pancreatic insulin deficiency, dose reduction of insulin, caloric restriction, alcohol abuse, acute febrile illness, extreme stress event). Uncircumcised males. Not intended for treatment of type 1 diabetes mellitus and diabetic ketoacidosis. Patient undergoing surgery; discontinue treatment at least 3 days prior to surgery. Renal impairment. Elderly. Pregnancy.

Significant: Bone fractures, genital mycotic infections (e.g. vulvovaginal mycotic infection, vulvovaginal candidiasis, vulvovaginitis, candida balanitis, balanoposthitis), hypersensitivity reactions (e.g. angioedema, urticaria), hypotension, acute kidney injury, UTI (including urosepsis and pyelonephritis), increased low-density lipoprotein cholesterol (LDL-C), lower limb amputation.
Investigations: Increased blood creatinine, decreased eGFR.
Metabolism and nutrition disorders: Hypoglycaemia (in combination with sulfonylurea or insulin), thirst.
Renal and urinary disorders: Increased urination.
Skin and subcutaneous tissue disorders: Pruritus, rash.
Vascular disorders: Volume depletion.
Potentially Fatal: Diabetic ketoacidosis. Rarely, necrotising fasciitis of the perineum (Fournier’s gangrene).

PO: C

Monitor blood glucose, HbA_1c (at least twice yearly in patients with stable glycaemic control; quarterly in patients not meeting treatment goals), volume status (e.g. blood pressure, haematocrit, electrolytes). Assess renal function at baseline and periodically during therapy. Monitor for UTI, genital mycotic infections; signs and symptoms of ketoacidosis (e.g. nausea, vomiting, abdominal pain, malaise, shortness of breath).

Additive diuretic effect and increased risk of dehydration and hypotension with diuretics (e.g. thiazide, loop diuretics). Increased risk of hypoglycaemia with insulin and insulin secretagogues (e.g. sulfonylureas).

May cause false-positive result for urine glucose test. May interfere with 1,5-anhydroglucitol (1,5-AG) assay.

Description: Empagliflozin is a reversible inhibitor of sodium-glucose co-transporter 2 (SGLT2), the main site of filtered glucose reabsorption in the renal proximal convoluted tubules. This reduces reabsorption of filtered glucose and lowers renal threshold for glucose, resulting in increased urinary glucose excretion, thereby reducing blood glucose concentration.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Time to peak plasma concentration: 1.5 hours.
Distribution: Volume of distribution: 73.8 L. Plasma protein binding: 86.2%.
Metabolism: Metabolised via glucuronidation by UGT2B7, UGT1A3, UGT1A8, and UGT1A9 to minor metabolites.
Excretion: Via urine (54.4%, 50% as unchanged drug); faeces (41.2%, mainly as unchanged drug). Elimination half-life: 12.4 hours.

Source: National Center for Biotechnology Information. PubChem Database. Empagliflozin, CID=11949646, https://pubchem.ncbi.nlm.nih.gov/compound/Empagliflozin (accessed on Jan. 22, 2020)

Store below 30°C.

Antidiabetic Agents

A10BK03 - empagliflozin ; Belongs to the class of sodium-glucose co-transporter 2 (SGLT2) inhibitors. Used in the treatment of diabetes.

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