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THE USE OF ANTIDIABETIC DRUGS IN HEART FAILURE
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PHARMANEWS PARO #10
THE USE OF ANTIDIABETIC DRUGS IN HEART FAILURE Keywords: SGLT2 inhibitors, Antidiabetics, Pharmacology, Mellitus diabetes, mechanism of action.
Introduction Sodium-glucose co-transporter type 2 (SGLT2) inhibitor antidiabetic drugs have been shown in many clinical studies to be very effective in reducing the risk of hospitalizations for heart failure in diabetic patients. In different settings, the relative reduction in hospitalization has been approximately 30-35% compared to the groups that did not receive an SGLT2 inhibitor. Cardiovascular studies showed that the use of SGLT2 inhibitors is associated with a reduction in new atherothrombotic events in patients in secondary prevention, however, there was also a great improvement in the reduction of traditional cardiovascular risk factors, such as weight reduction, blood pressure, glycemia. As well as there were also short-term hemodynamic benefits.
Figure
1:
kidney, majority
Glucose
Normally of
reabsorption
SGLT2
glucose
by
the
reabsorbs
the
filtered
by
the
kidney, but SGLT2 inhibitors reduce the renal reabsorption of glucose, producing an
increase
in
glucose
excretion
decrease in plasma glucose.
and
a
PHARMANEWS PARO #10
Mechanism of action SGLT2
inhibitors
reabsorption convoluted
in
reduce
the
tubule,
first
Among the most widely seen therapeutic targets is the sodium
and
segments
leading
to
of
glucose
the
glycosuria,
distal
osmotic
inhibition
exchanger
in
of the
the
sodium
heart,
and
producing
hydrogen a
ion
decrease
in
sodium cardiomyocyte concentrations, indirectly of calcium,
reducing
the
possible
toxic
effects
diuresis, and natriuresis. It was then postulated that
associated with the accumulation of cations. At the
diuresis
in
cardiac level, SGLT2 inhibitors have an inhibitory
intravascular volume, which would imply a decrease
effect on calmodulin-dependent protein kinase type
in myocardial work through a reduction in preload
II (CaMKII), which regulates calcium homeostasis
and afterload.
and can increase cell viability.
and
natriuresis
Renoprotection
decrease
have
kinase (AMPK) activity associated with the use of
mainly been in the reduction of proteinuria and in
SGLT2 inhibitors have decreased the activity of the
better preservation of the glomerular filtration rate.
multiprotein
Thus,
decreases
it
SGLT2
has
been
pathophysiological syndrome,
that
mechanism
a
a
In cardiac fibroblasts, the increase in AMP-activated
with
been
cause
in
studies
has
could
consistent
inhibitors.
postulated, complex
the
benefits
supported
called
renoprotection
for
The
finding
a
by
the
cardio-renal
may
be
improvement
of
an
the
inflammasome
complex,
inflammatory
response
which and
the
production of fibrous tissue.
indirect
ventricular
function.
Dosage and adverse effects
Also at the renal level, the increased supply of sodium to the distal segments of the nephron is a stimulus to
Dapagliflozin, 10 mg once daily, for the treatment of
cause vasoconstriction of the afferent arteriole, with
heart failure patients with reduced ejection fraction.
the consequent decrease in renal blood flow, which
The
could explain an increase in erythropoietin release. As
bacterial infections of the genito-urinary tract.
a consequence, a stimulus for erythropoiesis would occur with an increase in oxygen transport to the tissues.
Additionally,
erythropoietin
has
most
frequent
adverse
effect
is
fungal
and
Conclusion
been
associated with decreased inflammation and reduced
The discovery of its beneficial effects in heart failure
left ventricular mass.
has
allowed
an
important
change
in
its
pharmacological profile and in its clinical utility. It has been shown that alterations in cardiac ATP
This characteristic is unique since no other type of
production occur in the pathophysiology of diabetes
hypoglycemic drugs has been shown to be effective
mellitus,
ketone
in reducing the serious events associated with heart
oxidation; In these cases, ATP is covered mainly by
failure. The clinical benefits demonstrated by these
fatty acid oxidation, all these alterations are increased
antidiabetics for the treatment of heart failure with
in
reduced ejection fraction are also achieved in both
heart
which
failure,
decrease
but
can
glycolysis
be
from
reversed
by
SGLT2
inhibitors and it has been seen that ATP production mechanisms
can
have
a
positive
impact
on
diabetics and non-diabetics.
the
ventricular contractile function.
All credits of scientific information are for the authors of the scientific article creation! Scientific information reference: Quesada, D. J. (2020). El uso de los inhibidores de SGLT2 en falla cardiaca. Revista MĂŠdica PeriĂłdica, 1-4.
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