Vildagliptine

‘islet enhancer’

dr Budi Enoch SpPD

RSUD dr Abdul Aziz
Singkawang
“Selama ini, pengobatan diabetes
hanya memperhatikan insulin
(hormon yang menurunkan kadar
glukosa darah) saja, sementara
glukagonnya (yang meningkatkan
kadar glukosa darah) belum
disentuh,”

Soewondo, Media Edukasi Penatalaksanaan Diabetes, (16/10) 2009

 incretin
• Selain kekurangan insulin, diabetesi juga
mengalami kekurangan hormon inkretin, sejenis
hormon yang disekresi saluran usus ketika
makanan masuk
• Inkretin berperan dalam memperbaiki fungsi
keseimbangan antara glukagon dan insulin
 berfungsi mengatur dan mengontrol glukosa
darah
• Kurangnya inkretin disebabkan oleh hadirnya
protein DPP-4 yang bekerja memecah inkretin.
Padahal, kurangnya hormon inkretin ini dapat
mengganggu keseimbangan antara glukagon
dan insulin
 vildagliptine
• Bertindak sebagai inhibitor protein Dipeptidyl
Peptidase-4 (DPP-4 Inh) yang poten, selektif
dan reversibel
• Bekerja dengan cara memperbaiki fungsi sel
beta pankreas (sel yang memproduksi insulin)
dan sel alfa pankeras (yang memproduksi
glukagon) serta memperbaiki sensitivitas insulin
• Dengan inhibitor (penghambat) DPP-4,
keseimbangan akan tercapai sehingga fungsi
organ pankreas pun akan meningkat
• Valdigliptin mampu meningkatkan fungsi
pankreas yakni memperbaiki sensitifitas sekresi
glukagon terhadap glukosa dan memperbaiki
sensitifitas sekresi insulin terhadap glukosa
• Dipeptidyl peptidase 4 (DPP-4) inhibitors are
a new class of drugs now available for the
treatment of type 2 diabetes mellitus (T2DM).
DPP-4 is a widely expressed serine protease
with particularly high levels of activity in the liver,
kidney,and intestine.
• Although there are numerous endogenous
peptides that may be metabolized by DPP-4, the
two best-established targets of this enzyme are
the gastrointestinal hormones glucose-
dependent insulinotropic polypeptide (GIP) and
glucagon-like peptide 1 (GLP-1) GIP and GLP-1,
collectively referred to as incretins
• Incretins are secreted during meal absorption,
stimulate insulin secretion, and are essential for
normal glucose tolerance
• DPP-4 rapidly removes the two N-terminal
amino acids from GIP and GLP-1 after their
release from intestinal endocrine cells,
abolishing their insulinotropic activity
• DPP-4 inhibitors were developed to attenuate
this process and increase the concentration of
active incretins as a means of improving glucose
metabolism
• Although many DPP-4 inhibitors are being
evaluated in clinical trials, vildagliptin and
sitagliptin are agents that have been approved
for the treatment hyperglycemia in patients with
T2DM.
• In fact, both vildagliptin and sitagliptin stimulate
postprandial insulin secretion relative to plasma
glucose and reduce plasma glucagon levels
David A. D’Alessio, J Clin Endocrinol Metab, January 2009, 94(1):81–88
 Islet Enhancer Vildagliptin
in Combination Therapy

©2009 Novartis Pharma AG, CH-4002, Basel, Switzerland. Item code:

GAL09.404, January 2009
 What is it used for?

 Type 2 diabetes (non-insulin dependent

diabetes).
• Galvus is used for people with type 2 diabetes
whose blood sugar is not sufficiently controlled
by other antidiabetic medicines. It can be added
to treatment with metformin; a sulphonylurea, for
example gliclazide; or another type of
antidiabetic medicine known as a
thiazolidinedione, for example pioglitazone or
rosiglitazone
 Warning!
 Hypoglycaemia (low blood glucose) has been
commonly reported when this medicine is used
in combination with metformin or sulphonylurea
medicines, eg glimepiride. Symptoms of
hypoglycaemia usually occur suddenly and may
include cold sweats, cool pale skin, tremor,
anxious feeling, unusual tiredness or weakness,
confusion, difficulty in concentration, excessive
hunger, temporary vision changes, headache,
nausea and palpitations. You should talk to your
doctor or diabetes specialist about this and
make sure you know what to do if you
experience these symptoms.
 * Your ability to concentrate or react may be reduced if
you have low blood sugar, and this can cause problems
driving or operating machinery. You should take
precautions to avoid low blood sugar when driving -
discuss this with your doctor.
 * This medicine may also cause dizziness or fatigue. If
affected you should take care driving or operating
machinery
 * Rare cases of inflammation of the liver (hepatitis) have
been reported in people taking this medicine. For this
reason, your liver function should be checked before
starting treatment, every three months during the first
year of treatment, and regularly thereafter. You should
consult your doctor if you develop any of the following
symptoms while taking this medicine, so that your liver
can be checked: unexplained nausea, vomiting,
abdominal pain, fatigue, loss of appetite, darkened urine
or yellowing of the eyes or skin (jaundice).
 Use with caution in

• People over 75 years of age.

• People with mild heart failure.
• People taking ACE inhibitor medicines, eg
captopril
 Not to be used in
• Type 1 diabetes.
• Diabetic ketoacidosis.
• Decreased liver function.
• Pregnancy.
• Breastfeeding.
• This medicine is not recommended for people receiving dialysis or
who have moderate to severe kidney disease.
• This medicine is not recommended for people with severe heart
failure.
• This medicine is not recommended for children and adolescents
under 18 years of age because it has not been studied in this age
group.
• This medicine contains lactose and should not be taken by people
with rare hereditary problems of galactose intolerance, the Lapp
lactase deficiency or glucose-galactose malabsorption.
This medicine should not be used if you are allergic to one or any of its
ingredients. Please inform your doctor or pharmacist if you have previously
experienced such an allergy.
If you feel you have experienced an allergic reaction, stop using this medicine
and inform your doctor or pharmacist immediately
 no,can
butyou
youcheat
can negotiate…….
death ?

Source :
Thomas Pearl, Living to 100.com
Gary E Fraser, Archives of Internal Medicine, 2001
Kay Tee Khaw et all, Plos Medicine, 2008
Daniele E Hal, Journal of the American Board of Family Medicine, 2006
• You have a blood relative who has lived to
be 95 or older + 10
• You regularly play puzzles like Scrabble,
Sodoku or Bridge game + 5
• You’re a married man + 5
• You take 81 mgr of aspirin a day + 5
• You eat five sering of fruits/vegatable daily
+ 3
• You floss daily + 2
• You regularly nosh on nuts + 2
• You regularly go to church/mosque + 1,7
• You’re a married woman + 0
• You drink more than five cups off coffee a day
- 0,5
• You get less than six to eight hours of sleep a
night - 1
• You have a family history of diabetes - 1
• You are slowly putting on weight - 5
• You frequently feel stressed out - 5
• You eat red meat more than twice a week
- 5
• You have less than 12 years of education
- 5
• You engage in unprotected sex with multiple
partner - 7
• You smoke - 15
• You use iv drugs - 15