This document summarizes key information about the drug Empagliflozin. It belongs to the sodium glucose co-transporter 2 inhibitor class, which works by inhibiting glucose reabsorption in the kidney and increasing glucose excretion. The document outlines Empagliflozin's pharmacodynamics, pharmacokinetics, adverse reactions, dosage and administration, current status, and references. It provides an overview of Empagliflozin's mechanism of action, metabolism, excretion, drug interactions, efficacy, safety profile, and approved uses as monotherapy or add-on therapy for type 2 diabetes.

1. Dr Shinde Viraj Ashok
Junior resident 2
Department of Pharmacology
GMC Nagpur

2. 
Introduction
Pharmacodynamics
Pharmacokinetics
Adverse drug reaction
Current status
Overview

3. 
 Belongs to sodium glucose co- transporter inhibitor
group
 Other drugs belonging to this group are
dapagliflozin, sergliflozin , remogliflozin,
canagliflozin
Introduction

4. 
Potent highly selective Sodium Glucose Cotransporter 2
inhibitor

5. 
Drug
 Inhibits reabsorption of filtered glucose in
proximal tubule and
 Lowers renal threshold for glucose - ↑ urinary
glucose excretion
 ↓ blood glucose levels
 Dose dependent ↑ glycosuria with doses ≤ 1oomg
Pharmacodynamics

6. 
 In a study, empagliflozin resulted in
1. Improvements in β cell function and insulin
sensitivity
2. ↓ insulin secretion and tissue glucose disposal
 No clinically relevant effects of single doses of
empagliflozin 25mg and 200mg on heart rate
corrected QT interval

7. 
 No clinically relevant effects of food
 Vd - 73.8 L
 Steady state – 5 – 6 days
Pharmacokinetics

8. 
 37 % in RBC & 86 % plasma protein bound
 Primary route of metabolism – hepatic
glucuronidation (UGT)
 Excretion
 41% eliminated in faeces- majority as unchanged
 54% eliminated in urine – of which 50% was
unchanged
Contd …

9. 
 Avoid coadministration with drugs known to induce
UGT(5’ uridine diphosphoglucuronyltransferase)
enzymes ( phenytoin & carbamazepine)
 Doesn’t inhibit , inactivate or induce cytochrome
P450 enzymes
Drug interactions
Potential risk of ↓ efficacy

10. 
 Starting dose – 10mg once daily as
 Monotherapy or
 In combination with other antihyperglycaemic
agents
 Patients tolerating this dose & who require tighter
glycaemic control
 Dosage – may be ↑ to 25 mg ( maximum dose)
Dosage & administration

11. 
 Common – 1- 10% of patients
 Genital infections
 Urinary tract infections
 Pruritus
 ↑ urination
Adverse reactions

12. 
 May add to diuretic effects of thiazide & loop
diuretics - ↑ risk of dehydration & hypotension
 Frequency of minor or major hypoglycaemia was
similar to placebo recipient
 Risk of hypoglycaemia increases when
coadministered with a sulfonylurea and /or insulin

13. 
 Approved in EU and USA and based on most recent
guidelines (2013)
 First line monotherapy (though not typically first
choice) or
 Add on therapy to other antihyperglycaemic agents
(dual or triple combination)
 SGLT 2 inhibitors - associated with body weight loss
(may be used in obese patients)
Current status of
Empagliflozin

14.  Add on therapy to metformin
 Non inferior to glimepiride at 52 weeks
 Superior to glimepiride at 104 weeks in terms of
reduction of HbA1C
 In clinical trials overall number of empagliflozin
treated patients who developed kidney and bladder
cancer was low and similar to that in placebo
recipients

15. 
 Empagliflozin : A review of its use in patients with
Type 2 Diabetes Mellitus ; Drugs (2014)74 , Lesley J
Scott
 The sodium glucose cotransporter 2 inhibitor
empagliflozin does not prolong QT interval in a
thorough QT (TQT) study, Ring et al. Cardiovascular
Diabetology 2013, - bio med central
References

16. 