7/23/2019 Antidiabetes 2010 [Compatibility Mode]
1/71
Farmakologi
OBAT ANTIDIABETIK
Fathiyah Safithri
Laboratorium Farmakologi FK-UMM
2009
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om
(
http://www.novapdf.com/http://www.n/http://www.n/http://www.n/http://www.n/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
2/71
Diabetes Mellitus:a group of 'iseases harateri)e' by high le"els of bloo' gluose
resulti!g from 'efets i! i!suli! pro'utio!* i!suli! atio!* or
both
+ ,er'iri 'ari tipe$
.( ,ype . 'iabetes
2( ,ype 2 'iabetes
( /estatio!al 'iabetes
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
3/71
Diabetes Mellitus
Type 2 Diabetes Produksi insulin & pe
kerja insulin (resistansi
insulin = kadar seruminsulin N / , tp tdk bisabekerja maksimal
terdeteksi stl 40th serin dihubunkan d
obesitas! lama" aal sel beta,
sekresi insulin ##
$% : 'D
Type 1 Diabetes sel beta rusak
(autoimmun disease,
sekresi insulin () terdeteksi sblm *0th$% : insulin (insulin
dependen +% utama : Diabeti
ketoaidosis (karenao-erproduksi ketoaids(
+ Gestational Diabetes
-1 of preg!a!t wome! i! the
U 'e"elop gestatio!al 'iabetes
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
4/71
3ormal #mg%'L( /oal #mg%'L(
'merian Diabetes 'sso! .riteria
D'1$12 .'31 "000 (adapted
Action
Suggested
Prepra!'ial
gluose(average)
4 .00#whole bloo'(
50 6.20 4 50 or 7.80
e'time
gluose(average)
4 ..0#whole bloo'(
.00 - .80 4.00 or 7.:0
;b 75
=Depe!'i!g o!
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
5/71
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om
(
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
6/71
+omplikasi DM
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om
(
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
7/71
REGULASI GULA DARAH
Dilakukan a!l oleh : hati, pankreas, sel otot, lemak,adenohiposis, adrenal, tiroid
HATI) Makanan absorbsi lukosa di usus -!porta hati
sintesa likoen
) absorbsi selesai
kdr lukosa dlm sirkulasi ?
hati glikogenolisis
- ad!likoen di hati ? glukoneogenesis
PANKREAS) glukagon glikogenolisis
) insulin
SEL TT) insulin uptake lukosa ke sel otot
) kerja sik kontraksi otot lukosa lbh b5k msk ke dlm sel(tanpa bantuan insulin
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
8/71
REGULASI GULA DARAH !lanj"
ADRENAL lukokortikoid (kortisol
) hepar : sintesa likoen, lukoneoenesis
) pankreas : lukaon @ gluko!eoge!esis
67"+ ADENOI!O"ISE growth hormo! #/;(
hormo! yg mempu!yai efek berlawa!a! 'g i!suli!
me@ gula 'arah
LE#AK
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
9/71
Sli$e %
&'2 6ND62 7P, 88/"4/"009
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
10/71Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
11/71Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
12/71
PERAN INSULIN DL#
#E
KADAR GULA DARAH+
++
+
Afek akhir $ hipoglikemi 'a! me pe!yimpa!a! a'a!ga!e!ergi
Mempe!garuhi metabolisme K;* protei!* 'a! lemak
,arget Bari!ga! utama $ hepar* sel otot* sel lemak
e#ar
- Me ?gluo!eoge!esis* glyoge!olysis* ketoge!esis
- Me @ si!tesa glyoge!
Sel Otot
- me @ uptake glukosa /LU,-8 * oksi'asi glukosa si!tesaglikoge!*
- Me uptake asam ami!o si!tesa protei!- me ? glikoge!olisis release asam ami!o
Sel le$ak- me @ uptake gluose si!tesa triglyeri'e
- me ? pelepasa! FF< 'a! glyerol
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
13/71
PERAN INSULIN DL#
+
#E
KADAR GULA DARAH
%erangsang serabut otot
skeletal+
+
%erangsang sel &e#ar&
Beker'a di sel le$ak+ %eng&a$bat #roduksi eni$
tertentu&
glucoseu#take
#rotein
snt&esisa$ino acids
u#take
en$e
#roduction
glcogen
breaking
glcogen
snt&esis
*at
snt&esis
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novap/http://www.novap/http://www.novap/http://www.novap/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
14/71
Penga(u) Insulin pa$a
#etabolis*e
'! $ranspor sen5aa melalui Membran 2el tertentu(lukosa, as amino, +;, nukleosida,
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
15/71
Sekresi Insulin
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
16/71
2ekresi insulin oleh sel beta : tt kadar '$P ,ion .a
Pd kead istirahat kdr '$P intrasel betapankreas ### +; berdi
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
17/71
Glucose $etabolis$
(glucokinase)
G+,T-.
AT!
K/
0a// 0a./
AT!
release
E
0a./2K/
ASK0
3D00
I!4
A0&
%.
2
so$atostatin
. NEinsulin
granule
cA%!E
/ -
/ -
-
/-
/
/ -
F
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
18/71
2timulator 2ekresi nsulin
?lukosa 'kti-itas sara< otonom : parasimpatis, simpatis @" bat : alpha)" blokers, beta)" aonist, theoph5lline,
sul
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
19/71
+ ,&u glukosa per oral
+ k k'r glukosa 'rh @ gluk msk i!trasel mel
/LU,-2* km' me!galami metab
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
20/71
Tu+uan Te(api D#
+ %engontrol &i#erglike$i dan ketoasidosis
serta $eng&indari &i#oglike$i
B hiperlikemi dapat men5ebabkan berbaaikomplikasi
B Cipolikemi dapat men5ebabkan koma dan
kerusakan sel otak!
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.nova/http://www.nova/http://www.nova/http://www.nova/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
21/71
Pen$ekatan Te(api D#
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
22/71
PRINSIP PENATALAKSANAAN D#
Pengatu(an $ietB Minum air ban5ak, susu skim dan minuman berkalori
rendah lainn5a pada aktu makanB Cindari makanan manis, orenan, biskuit, akeB Makanlah denan aktu 5an teratur
B$inkatkan asupan sa5uran dua kali tiap makanB>adikan nasi, roti, kentan, atau sereal sebaai menu utamaB Minum air atau minuman bebas ula setiap anda haus
Lati)an +as*ani+eiatan jasmani sehari B hari dan latihan jasmani teratur, * B4 %/m, selama *0 menit : jalan, bersepeda santai, join,berenan! Eatihan jasmani me dan memperbaikisensititas thd insulin, serta me uptake lukosa oleh otot(tanpa perlu bantuan insulin
,a(*akote(api
Create PDF files without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
23/71
,AR#AKTERAPI
DIA-ETES #ELLITUS
nsulin
) Pasien Diabetes $ipe 8, tidak ada
produksi insulin!) Pasien diabetes $5pe ", produksi insulin
tdk menukupi!
bat 'ntidiabetik ral
) ?ol! 2ul
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
24/71
TERAPI INSULIN
$ujuan : utk menontrol ula darahsepanjan hari dan menormalkanmetabolisme
Pemberian biasan5a dilakukan sendirioleh pasien
3eimen diberikan
) sekitar kt makan, e%erise, tidur
Faktor 5 mempenaruhi kebutuhaninsulin : e%erise, diet, stress/in
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
25/71
MAK
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
26/71
Sli$e 2.
K1 +edokteran, 88/"4/"009
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
27/71
In$ikasi Te(api Insulin
2emua penderita DM tipe
Penderita DM tipe , bila terapi jenis lain tidak
dapat menendalikan kadar lukosa darah!
+ebutuhan insulin me pd penderita DM d :in
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
28/71
bat 5 men5ebabkan hiperlikemi :
a! 1
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
29/71
,a(*akokinetik Insulin
Pemberian per)oral tidak eHekti< 'iberikan seara parenteral :
) s atau im) i- pd keadaan emmeren5 atau
selama operasi
$I plasma #J menit
nakti-asi oleh hepar dan injal
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf./http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf./7/23/2019 Antidiabetes 2010 [Compatibility Mode]
30/71
P(e$ileksi te*pat penyuntikan insulin
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
31/71
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
32/71
Se$iaan P(epa(at Insulin
dsr sumbern5a :
B hean (bee< or porkKLsinle)peak -!Lsinle)omponent
B Manusia (1! oli reombinant -! semi)s5ntheti modied porine
dsr ms kerja : sinkat, menenah,panjan, ampuran
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
33/71
Klasi/kasi Insulin8! Insulin ke(+a singkat 0an termasuk di sini adalah insulin reular ( .r5stal Oin nsulin /.O ! 2aat ini dikenal " maam insulin .O, 5aitu dalam bentuk asamdan netral! Preparat 5an ada antara lain : 'trapid, elosulin ,2emilente! nsulin jenis ini diberi *0 menit sebelum makan,menapai punak setelah 8B * jam! Maam dan eenis ini aal kerjan5a adalah 8!R B "!Rjam! Punakn5a terapai dalam 4 B 8R jam dan e
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
34/71
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
35/71
N21$ & DS3'2 N2SEN
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
36/71
Eek Sa*ping $an Toksisitas Insulin
$erutama berhubunan d o-erdosis
B hipolikemia! brp
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
37/71
TANDA HIPGLIKE#I
$erantun epat / tidakn5a penurunankadar lukosa dlm plasma
.epat :
kerinat dinin, takikardi, tremor, mual,lapar
Eambat :
sakit kepala, blurred -ision, binun,inkoheren speeh, kejan, koma
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
38/71
(al Anti$iabeti3s
'da R kelompok :
'! 2ul
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
39/71
#ekanis*e ke(+a
(al Anti$iabeti3s !AD"
Me absorbsi lukosa : aarbose, biuanid
Me sekresi insulin (seretaoues :sul
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
40/71
Gel&Pote!y
Sulonylu(ea 8st eneration
B tolbuta*i$e ( 3astinon, rinase
B tola4a*i$e ($olinase
B 3)lo(p(opa*i$e (Diabinese
"nd enerationB Gli3la4i$
B Glipi4i$e (Minidiab, ?luotrol
B Glybu(i$e 5 Gliben3la*i$ (Daonil, ?lulo, Prodiabet
B Gliklasi$ (Diamiron, ?lidiabet, Oumadia *rd eneration
B Gli*epi(i$e ('mar5l
=;y'roylatio! of the aromati ri!g appears to be the most fa"ore' metaboli pathway
=;y'roylate' 'eri"ati"es ha"e muh lower hypoglyemi ati"ity
Create PDFfiles without this message by purhasi!g !o"aPDF pri!ter #http$%%www&!o"ap'f&om (
http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/http://www.novapdf.com/7/23/2019 Antidiabetes 2010 [Compatibility Mode]
41/71
. I!testi!e$ gluose absorptio! 2 Musle a!' a'ipose tissue$
4 !ancreas5 insulin secretion
Sul*onlureas 5
insulin secretion
gluose uptake
I!suli! resista!e
loo' gluose
8 Li"er$ hepatigluose output
I!suli!
resista!e
2ul
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
42/71
SUL,NILUREA
#ekanis*e Ke(+a :B Menstimuli release insulin endoen dari sel beta
2ul
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
43/71
nset dan durasi ber-ariasi
) hlorpropamide durasi sanat panjan
(tI *9j, ok metab di hepar lambat!) "nd enerations lebih potent
B lipiide short hal
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
44/71
!&ar$acological co$#arison o* sul*onlureas
,olbu-
tami'e
/libe!-
/lila)i'e /lipi)i'e lami'e/lime-
piri'e
Gepa-
gli!i'e
Gelati"e pote!y 1 46 76 - 166 176 - 866 866-1666/ 866
mg%tablet
Plasma peak #h(
766
4
96
8
7-16
1
1:.7-7
4
1- 8
.:8
6:7-.
;1< - 16 .8 1< - .8 .8 .8Duratio! of atio! #h( ; 1?9?
+ % A$arl %onogra#&
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
45/71
1 - .
1
1 - .(.)
.(1)
4 - 8(4)
7(1)
Sul*onlureas 5 oglce$ic risk
elative iske#aglinide
Tolbuta$ide
Gliclaide
Gli#iide
Gli$e#iride
7/23/2019 Antidiabetes 2010 [Compatibility Mode]
46/71
Penggunaan Sulonilu(ea
ndikasi : Can5a utk DM $5pe)"
Bplg baik utk pasien Usia ; .7 t)< *en$e(ita D# = 17t)