3.
Belongs to sodium glucose co- transporter inhibitor
group
Other drugs belonging to this group are
dapagliflozin, sergliflozin , remogliflozin,
canagliflozin
Introduction
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
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
No causal link has been established but concerns have been raised regarding potential ↑ risk of breast & bladder cancer occurring during clinical trials of dapagliflozin
