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Dr.Munir Al Assad
HMO,
Dept. of Cardiology
CMCH
 Introduction
 History
 Chemical structure
 Pharmacodynamics
 Pharmacokinetics
 Indications
 Limitation of use
 Adverse reactions
 Drug interaction
 Cardiovascular outcome
 Empagliflozin belongs to sodium glucose co-
transporter 2 inhibitor group.
 Other drugs belonging to this group are
dapagliflozin , sergliflozin , remogliflozin ,
canagliflozin
 It was developed by Boehringer Ingelheim
& Eli Lilly and company
 It was approved by FDA in august 2014
 It was approved for medical use in the US
in 2014
 A month supply in the UK costs the NHS
about 36.59 £ as of 2019.
 In the US the wholesale cost of this
amount is about US $ 442 .
 In the 2016 it was the 289th most
prescribed medication in the US with more
than a million prescription.
 C23H27CLO7
 Molecular weight :450.91
Empagliflozin
Inhibits SGLT2 at PCT
in kidney
Prevention of
reabsorption of glucose
Excretion of glucose in
urine
Reduction of blood
glucose
 Tablets available as :
Starting dose 10mg ,
Maximum dose 25mg ,
Once daily in the morning .
 May be taken with or without food.
 Route by oral.
 Absorption :
no clinically relevant effects of food.
 Distribution : Vd 73.8L
Steady state 5-6 days
37% in RBC and
63% in plasma protein bound
 Metabolism :
primary route of metabolism is hepatic
glucuronidation by uridine 5’
diphosphoglucuronosyltransferase.
 Excretion :
half life is 12.4 hr.
Clearance 10.6l/hr.
41% eliminated in feces.
54%eliminated in urine.
 As an adjunct to diet & exercise to improve
glycemic control in adults with type 2 DM.
 To reduce the risk of cardiovascular death
in adult patients with type 2DM &
established cardiovascular disease.
 Good second line option in obese patients
with type 2 DM.
 Patients with renal impairment (GFR
greater than or equal to 45ml/min/1.73m².
 Type 2 DM with hepatic impairment.
 Second line medications after Metformin
for type 2 DM in people with heart failure or
CKD.
 Type 1 DM
 GFR <45ml/min/1.73m2
 History of hypersensitivity reaction to
Empagliflozin
 Diabetic ketoacidosis
 Severe renal impairment , ESRD or
dialysis
 Urinary tract infections
 Genital mycotic infections
 Hypotension
 Diabetic ketoacidoss
 Urosepsis & pyelonephritis
 Hypoglycemia with concomitant use with
insulin & insulin secretagogues
 Pruritus
 AKI and impairment in renal function.
 Diuretics + Empagliflozin
Increased urine volume & frequency
 Insulin or insulin secretagogues +
Empagliflozin
Increased risk of hypoglycemia
 Amlodipine + Empagliflozin
May potentiate hypotension
SGLT2 inhibitors
Glycosuria
Net calorie loss of approximately
200-300kilocalories per day
Weight loss
SGLT2
inhibitors
Glycosuria
Glucose acts as
osmotic diuretic
Dehydration
Blood pressure
reduction
 Reduction in intravascular volume ( preload)
 Improvement in arterial pressure & aortic
stiffness (after load)
 Improve ventricular function & myocardial
oxygen demand , this could be an especially
attractive option for patients with reduced EF
& heart failure
 The effect of empagliflozin on
cardiovascular risk in adult patients with
type 2 DM & established, stable,
atherosclerotic cardiovascular disease was
evaluated in the EMPA-REG OUTCOME
study.
 The EMPA-REG Outcomes trial has the
potential to change dramatically the way
these drugs are now used.
 The empagliflozin cardiovascular outcome
event trial in type 2 DM patients-Removing
Excess Glucose(EMPA-REG) Outcomes
trial evaluated 7028 patients with T2DM
and high risk of cardiovascular events to
empagliflozin standards of care versus
placebo standard of care..
 Over a median follow up of 3.1 years,
treatment with empagliflozin reduced the
primary composite outcome (death from
cardiovascular causes ,non fatal MI , or
nonfatal stroke) from 12.1% to 10.5%.
 A decrease in cardiovascular mortality from
5.9% to 3.7% was noted in the treatment
group along with a remarkable 35%
relative risk reduction in hospitalization for
heart failure.
 Empagliflozin also causes small reduction
in weight, waist circumference , uric acid
level, blood pressure and reduction in
cardiovascular events.
 ADA & EASD guideline 2019.
 Davidson's Principles and Practice of
Medicine( 23rd edition).
 Drugs for the heart.
 Manual of Cardiovascular Medicine( 5th
Edition).
Empagliflozin

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Empagliflozin

  • 1. Dr.Munir Al Assad HMO, Dept. of Cardiology CMCH
  • 2.  Introduction  History  Chemical structure  Pharmacodynamics  Pharmacokinetics  Indications  Limitation of use  Adverse reactions  Drug interaction  Cardiovascular outcome
  • 3.  Empagliflozin belongs to sodium glucose co- transporter 2 inhibitor group.  Other drugs belonging to this group are dapagliflozin , sergliflozin , remogliflozin , canagliflozin
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  • 5.  It was developed by Boehringer Ingelheim & Eli Lilly and company  It was approved by FDA in august 2014  It was approved for medical use in the US in 2014
  • 6.  A month supply in the UK costs the NHS about 36.59 £ as of 2019.  In the US the wholesale cost of this amount is about US $ 442 .  In the 2016 it was the 289th most prescribed medication in the US with more than a million prescription.
  • 8. Empagliflozin Inhibits SGLT2 at PCT in kidney Prevention of reabsorption of glucose Excretion of glucose in urine Reduction of blood glucose
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  • 10.
  • 11.  Tablets available as : Starting dose 10mg , Maximum dose 25mg , Once daily in the morning .
  • 12.  May be taken with or without food.  Route by oral.
  • 13.  Absorption : no clinically relevant effects of food.  Distribution : Vd 73.8L Steady state 5-6 days 37% in RBC and 63% in plasma protein bound
  • 14.  Metabolism : primary route of metabolism is hepatic glucuronidation by uridine 5’ diphosphoglucuronosyltransferase.
  • 15.  Excretion : half life is 12.4 hr. Clearance 10.6l/hr. 41% eliminated in feces. 54%eliminated in urine.
  • 16.  As an adjunct to diet & exercise to improve glycemic control in adults with type 2 DM.  To reduce the risk of cardiovascular death in adult patients with type 2DM & established cardiovascular disease.
  • 17.  Good second line option in obese patients with type 2 DM.  Patients with renal impairment (GFR greater than or equal to 45ml/min/1.73m².
  • 18.  Type 2 DM with hepatic impairment.  Second line medications after Metformin for type 2 DM in people with heart failure or CKD.
  • 19.  Type 1 DM  GFR <45ml/min/1.73m2  History of hypersensitivity reaction to Empagliflozin  Diabetic ketoacidosis  Severe renal impairment , ESRD or dialysis
  • 20.  Urinary tract infections  Genital mycotic infections  Hypotension  Diabetic ketoacidoss  Urosepsis & pyelonephritis
  • 21.  Hypoglycemia with concomitant use with insulin & insulin secretagogues  Pruritus  AKI and impairment in renal function.
  • 22.  Diuretics + Empagliflozin Increased urine volume & frequency
  • 23.  Insulin or insulin secretagogues + Empagliflozin Increased risk of hypoglycemia
  • 24.  Amlodipine + Empagliflozin May potentiate hypotension
  • 25. SGLT2 inhibitors Glycosuria Net calorie loss of approximately 200-300kilocalories per day Weight loss
  • 26. SGLT2 inhibitors Glycosuria Glucose acts as osmotic diuretic Dehydration Blood pressure reduction
  • 27.  Reduction in intravascular volume ( preload)  Improvement in arterial pressure & aortic stiffness (after load)  Improve ventricular function & myocardial oxygen demand , this could be an especially attractive option for patients with reduced EF & heart failure
  • 28.  The effect of empagliflozin on cardiovascular risk in adult patients with type 2 DM & established, stable, atherosclerotic cardiovascular disease was evaluated in the EMPA-REG OUTCOME study.
  • 29.  The EMPA-REG Outcomes trial has the potential to change dramatically the way these drugs are now used.
  • 30.  The empagliflozin cardiovascular outcome event trial in type 2 DM patients-Removing Excess Glucose(EMPA-REG) Outcomes trial evaluated 7028 patients with T2DM and high risk of cardiovascular events to empagliflozin standards of care versus placebo standard of care..
  • 31.  Over a median follow up of 3.1 years, treatment with empagliflozin reduced the primary composite outcome (death from cardiovascular causes ,non fatal MI , or nonfatal stroke) from 12.1% to 10.5%.
  • 32.  A decrease in cardiovascular mortality from 5.9% to 3.7% was noted in the treatment group along with a remarkable 35% relative risk reduction in hospitalization for heart failure.
  • 33.  Empagliflozin also causes small reduction in weight, waist circumference , uric acid level, blood pressure and reduction in cardiovascular events.
  • 34.
  • 35.  ADA & EASD guideline 2019.  Davidson's Principles and Practice of Medicine( 23rd edition).  Drugs for the heart.  Manual of Cardiovascular Medicine( 5th Edition).