Tools Wisconsin Diabetes Mellitus Essential Care Guidelines • 2012 40 DIABETES MELLITUS MEDICATIONS 2012 ORAL GLUCOSE-LOWERING AGENTS RX Avail. Dosage Initial Dose Initial Dose (elderly) Dose Adjustment Schedule Usual Maint. Dosage Max. Effecttive Dose A1C Lowering Wt Renal Dosing Hepatic Dosing Lab Monitoring Common Side Effects Contraindications/ Precautions Drug Class: Sulfonyureas Actions: Stimulates insulin secretion; lowers fasting plasma glucose Indications: Type 2 diabetes as monotherapy or in combination with insulin, metformin, DPP-IV inhibitors, incretin mimetics, or TZDs Glipizide 5 mg 10 mg 5 mg 2.5 mg/day Increase by 2.5 to 5 mg (> 15 mg/day = BID) after 1-2 wks 5-15 mg/ day 20 mg/day 1.0-2% + N/A Start at 2.5 mg/ day N/A • hypoglycemia • weight gain • Use caution in people with sulfa allergies • Use glyburide with caution due to greater risk of hypoglycemia • Use caution with renal or hepatic insufficiency (glipizide or glimepiride preferred choices) • Immediate release and extended release glipizide doses are not equivivalent Glipizide ER 2.5 mg 5 mg 10 mg 5 mg/day Increase by 5 mg after 1-2 wks 5-10 mg/ day 20 mg/day Glimepiride 1 mg 2 mg 4 mg 1-2 mg 1 mg Increase by 1-2 mg after 1-2 wks 1-4 mg/ day 8 mg/day Start at 1 mg/ day and monitor Mild--start at 1 mg (monitor) Severe-- avoid Glyburide 1.25 mg 2.5 mg 5 mg 2.5-5 mg 1.25 mg/ day Increase by 2.5-5 mg after 1-2 wks 1.25-10 mg/day 10 mg/day Do NOT use if CrCl < 50 ml/min Conser- vative 1.25 mg/ day Drug Class: Biguanides Actions: Targets hepatic cells; decreases hepatic glucose production; does not stimulate insulin secretion; lowers fasting plasma glucose Indications: Type 2 diabetes as monotherapy or in combination with any other agent or insulin; overweight; dyslipidemic; children (approved for ≥ age 10) Metformin 500 mg 850 mg 1000 mg 500 mg BID Use with caution, especially if > 80 years Increase by 500 mg after 1-2 wks 1000-2000 mg/day 2550 mg/day (10-16 yo = 2000 mg/day) 1.0-2% 0/- Contrain- dicated if SCr ≥ 1.5 males, ≥ 1.4 females or eGFR < 50 Avoid due to risk of lactic acidosis BUN, Cr & CBC: prior to initiation then yearly. LFTs: prior to initiation. Vitamin B12 levels: every year for those at high risk of Vitamin. B12 deficiency • diarrhea • nausea • abdominal bloating • anorexia • Do not use with hepatic insuf- ficiency • Consult with diabetes specialist is recommended for SCr > 1.5 or eGFR < 50 • Uncompensated CHF • Excessive alcohol intake • Over age 80 (caution) • Acetazolamide • Withhold therapy for 48 hours after iodinated contrast media is used • May cause ovulation to resume in anovulatory, premenopausal women Metformin ER 500 mg 750 mg 500 mg 500-2000 mg/day 2000 mg/ day Drug Class: TZD (Thiazolidinediones) Actions: Regulates insulin responsive genes necessary for glucose and lipid metabolism; improves sensitivity to insulin in skeletal and adipose tissue Indications: Type 2 diabetes as monotherapy or in combination with any other agents; Actos is also approved for use with insulin Note: Rosiglitazone is not listed on this chart due to restricted use by FDA. For more information, see: http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm226976.htm pioglitazone (Actos) 15 mg 30 mg 45 mg 15-30 mg Same Increase by 15 mg 6-12 wks 15-45 mg/ day 45 mg/day (30 mg if on insulin) 1-1.5% + N/A Do NOT use if ALT > 2.5X ULN LFTs: prior to initiation then periodically • weight gain, edema • heart failure symptoms, macular edema • increased fracture rate • increase risk of bladder cancer • CHF III & IV or any symptomatic heart failure • Clinical evidence of liver disease or ALT > 2.5 ULN • Do not use rosiglitazone in combina- tion with insulin or nitrates (may increase risk of MI) • Use caution in females at high risk for fractures • Monitor for increase edema • May cause ovulation to resume in anovulatory, premenopausal women
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ToolsWisconsin Diabetes Mellitus Essential Care Guidelines • 2012
40
DIA
BET
ES M
ELLI
TUS
MED
ICAT
ION
S 20
12O
RA
L G
LUC
OSE
-LO
WER
ING
AG
ENTS
RX
Avai
l. D
osag
eIn
itial
Dos
eIn
itial
Dos
e (e
lder
ly)
Dos
e A
djus
tmen
t S
ched
ule
Usu
al
Mai
nt.
Dos
age
Max
. E
ffect
tive
Dos
e
A1C
Lo
wer
ing
Wt
Ren
al
Dos
ing
Hep
atic
D
osin
gLa
b M
onito
ring
Com
mon
Sid
e E
ffect
sC
ontra
indi
catio
ns/ P
reca
utio
ns
Dru
g C
lass
: Sul
fony
urea
sA
ctio
ns: S
timul
ates
insu
lin s
ecre
tion;
low
ers
fast
ing
plas
ma
gluc
ose
Indi
catio
ns: T
ype
2 di
abet
es a
s m
onot
hera
py o
r in
com
bina
tion
with
insu
lin, m
etfo
rmin
, DP
P-IV
inhi
bito
rs, i
ncre
tin m
imet
ics,
or T
ZDs
Glip
izid
e5
mg
10 m
g5
mg
2.5
mg/
day
Incr
ease
by
2.5
to 5
mg
(> 1
5 m
g/da
y =
BID
) af
ter 1
-2 w
ks
5-15
mg/
day
20 m
g/da
y
1.0-
2%+
N/A
Sta
rt at
2.
5 m
g/da
y
N/A
• hyp
ogly
cem
ia
• wei
ght g
ain
• Use
cau
tion
in p
eopl
e w
ith s
ulfa
al
lerg
ies
• Use
gly
burid
e w
ith c
autio
n du
e to
gr
eate
r ris
k of
hyp
ogly
cem
ia• U
se c
autio
n w
ith re
nal o
r hep
atic
in
suffi
cien
cy (g
lipiz
ide
or g
limep
iride
pr
efer
red
choi
ces)
• Im
med
iate
rele
ase
and
exte
nded
re
leas
e gl
ipiz
ide
dose
s ar
e no
t eq
uivi
vale
nt
Glip
izid
e E
R2.
5 m
g5
mg
10 m
g 5
mg/
day
Incr
ease
by
5 m
g af
ter 1
-2
wks
5-10
mg/
day
20 m
g/da
y
Glim
epiri
de1
mg
2 m
g 4
mg
1-2
mg
1 m
gIn
crea
se b
y 1
-2
mg
afte
r 1-2
w
ks
1-4
mg/
day
8 m
g/da
y
Sta
rt at
1
mg/
day
and
mon
itor
Mild
--st
art
at 1
mg
(mon
itor)
S
ever
e--
avoi
d
Gly
burid
e1.
25 m
g 2.
5 m
g 5
mg
2.5-
5 m
g1.
25 m
g/da
y
Incr
ease
by
2.5-
5 m
g af
ter
1-2
wks
1.25
-10
mg/
day
10 m
g/da
y
Do
NO
T us
e if
CrC
l < 5
0 m
l/min
Con
ser-
vativ
e 1.
25 m
g/da
y
Dru
g C
lass
: Big
uani
des
Act
ions
: Tar
gets
hep
atic
cel
ls; d
ecre
ases
hep
atic
glu
cose
pro
duct
ion;
doe
s no
t stim
ulat
e in
sulin
sec
retio
n; lo
wer
s fa
stin
g pl
asm
a gl
ucos
eIn
dica
tions
: Typ
e 2
diab
etes
as
mon
othe
rapy
or i
n co
mbi
natio
n w
ith a
ny o
ther
age
nt o
r ins
ulin
; ove
rwei
ght;
dysl
ipid
emic
; chi
ldre
n (a
ppro
ved
for ≥
age
10)
Met
form
in50
0 m
g85
0 m
g10
00 m
g50
0 m
g B
ID
Use
with
ca
utio
n,
espe
cial
ly if
>
80 y
ears
Incr
ease
by
500
mg
afte
r 1-2
w
ks
1000
-200
0 m
g/da
y
2550
mg/
day
(10-
16 y
o =
2000
mg/
day)
1.0-
2%0/
-
Con
train
-di
cate
d if
SC
r ≥
1.5
mal
es,
≥ 1.
4 fe
mal
es
or e
GFR
<
50
Avoi
d du
e to
risk
of
lact
ic
acid
osis
BUN, Cr & CBC: prior to initiation then yearly.LFTs: prior to initiation.Vitamin B12 levels: every year for those at high risk of Vitamin. B12 deficiency