Empagliflozin


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Type 2 diabetes mellitus
Adult: As monotherapy or in combination with other antidiabetic agents: Initially, 10 mg once daily, may be increased to 25 mg daily if necessary.
Elderly: ≥85 years Not recommended.
Renal Impairment
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.
Cách dùng
May be taken with or without food.
Chống chỉ định
Severe renal impairment (eGFR <45 mL/min/1.73 m2), ESRD, patient on dialysis. Lactation.
Thận trọng
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.
Phản ứng phụ
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).
MonitoringParameters
Monitor blood glucose, HbA1c (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).
Tương tác
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).
Lab Interference
May cause false-positive result for urine glucose test. May interfere with 1,5-anhydroglucitol (1,5-AG) assay.
Tác dụng
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.
Đặc tính

Chemical Structure Image
Empagliflozin

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

Bảo quản
Store below 30°C.
Phân loại MIMS
Phân loại ATC
A10BK03 - empagliflozin ; Belongs to the class of sodium-glucose co-transporter 2 (SGLT2) inhibitors. Used in the treatment of diabetes.
References
Anon. Empagliflozin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/04/2020.

Buckingham R (ed). Empagliflozin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/04/2020.

FDA Approves Label Changes to SGLT2 Inhibitors Regarding Temporary Discontinuation of Medication Before Scheduled Surgery . U.S. FDA. https://www.fda.gov/. Accessed 02/04/2020.

Jardiance Film-Coated Tablets 10 mg and 25 mg (Boehringer Ingelheim Pharma GmbH & Co. KG). MIMS Singapore. http://www.mims.com/singapore . Accessed 02/04/2020.

Jardiance Tablet, Film Coated (Boehringer Ingelheim Pharmaceuticals, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 02/04/2020.

Jardiance Tablets (Boehringer Ingelheim International GmbH). U.S. FDA. https://www.fda.gov/. Accessed 02/04/2020.

Joint Formulary Committee. Empagliflozin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/04/2020.

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