Common Oral Agents for Treating Type 2 Diabetes

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Common Oral Agents for Treating Type 2 Diabetes
*Drugs that can cause hypoglycemia*
Generic name
Dosage
Glyburide
(Diabeta)
2.5- 20 mg/day
daily or split BID with meals
Gliclazide
(Diamicron)
or Diamicron
MR)
Reg: 80-320 mg/day in 2
divided doses before meals
MR: 30-120 mg once daily
Glimepiride
(Amaryl)
Repaglinide
(GlucoNorm)
1-8 mg once daily
0.5-4 mg tid taken just
before meals. Titrate to
desired response (max 16
mg/day). Wait 1 week
before dose change
Note: Do not use more than one drug from each class
Action
Instructions for patients
Side effects
Insulin Secretagogues: Stimulate the pancreas to secrete insulin
Acts for 8-24 hours.
Take with meal (usually breakfast and supper)
Can cause low blood sugar if a meal is missed or
Eat regular meals and snacks
delayed, if more activity than usual, or if dose is
Glimepiride and gliclazide may also reduce
Carry a source of sugar to treat hypoglycemia
inadequate
insulin resistance. May combine with other
(such as glucose tablets, juice, candy, sugar)
Glimepiride and gliclazide are associated with less
classes of oral agents or basal insulin.
Do not take with alcohol as flushing may occur
hypoglycemia than glyburide
Short acting, taken just before or with meals to
provide lower blood sugar levels after eating.
Hold if meal skipped. May combine with other
classes of oral agents or basal insulin.
Main Contraindications

Can cause GI symptoms and headache
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Take just before or with meals
Skip dose if skipping meal.
Carry a source of sugar to treat hypoglycemia
(such as glucose tablets, juice, candy, sugar)
Low blood sugar possible, but less frequent than
with glyburide or gliclazide.
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Instructions for patients
Side effects
Other side effects are not usual.
Pregnancy (glyburide may be used
in the treatment of gestational
diabetes when insulin can’t be
used, but not recommended for the
treatment of Type 2 diabetes in
pregnancy)
Type 1 diabetes
Severe liver or kidney disease
Type 1 diabetes
Pregnancy
Dosage and interval may need
adjustment in renal or liver disease
60-180 mg tid taken just
before main meals
Nateglinide
(Starlix)
*Drugs that do not usually cause hypoglycemia*
Generic name
Metformin
(Glucophage)
Metformin
extended release
(Glumetza)
Dosage
Reg: 500 mg to max. 2500
mg/day, usually in divided
doses
ER: 1000-2000 mg with
evening meal ( titrate in 500
mg increments)
May take up to 2 weeks to
see full effect
Action
Biguanides: Help reduce release of sugar from the liver
May make cells more responsive to insulin so
Take with food to reduce GI side effects
Nausea, gas, abdominal pain, diarrhea (may subside
that they can use sugar more efficiently. May
with time). Used alone, very unlikely to cause low
combine with other classes of oral agents or
blood sugar levels. Hold before tests using contrast
basal insulin.
dyes, surgery or if severe infection
* May improve fertility in women
Main Contraindications

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Type 1 diabetes
Hepatic failure
Kidney failure, creatinine clearance
< 30 mL/min, use with caution if
<60 mL/min
Significant CHF
Acidosis
Treating
Type 2for
Diabetes
Adapted Common
from CDA Oral
2013 Agents
Clinical for
Practice
Guidelines
the Prevention and Management of Diabetes in Canada
Note: Do not use more than one drug from each class
Revised May, 2013- prepared by Inpatient Diabetes Nursing Consult Team: Advance Practice Nurse-: Filomena De Sousa. Diabetes Nurse Specialists - Rosemary Basa, Michelle Bradley,
*Drugs that do not usually cause hypoglycemia*
Edith Cloutier, Anne Fourney,
Common Oral Agents for Treating Type 2 Diabetes
-Drug Information Pharmacist- Anne Massicotte
*Drugs that do not usually cause hypoglycemia*
Generic name
Pioglitazone
(Actos)
Dosage
15-45 mg once a day.
May take 8-12 weeks to
see maximal effect
Action
Note: Do not use more than one drug from each class
Instructions for patients
Side effects
Thiazolidindiones: Improve insulin sensitivity at the liver, fat and muscle cells
Reduces insulin resistance and improves Advise physician if any swelling or
Low blood sugar very rare. Side effects not usual but
insulin sensitivity at the liver, fat and
shortness of breath
may promote weight gain Monitor Liver function tests
muscle cells, allowing insulin to work
May induce edema and cardiac failure
more effectively. May be taken with other
* May improve fertility in women
oral agents
May increase risk fracture in women
Main Contraindications
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Rosiglitazone
(Avandia)
Acarbose
(Glucobay)
Sitagliptin
(Januvia)
Saxagliptin
(Onglyza)
Linagliptin
Trajenta)
Avandamet
Janumet
4 mg/day, taken as a
single daily dose or in 2
divided doses
After 8-12 weeks, titrate
if needed to 8 mg/day,
taken as a single daily
dose or in 2 divided
doses.
25-100 mg three times
a day with meals (start
low and increase dose
slowly every 4-8 weeks
to minimize side effects)
100 mg daily
5 mg daily
5 mg daily
Rosiglitazone/metformin
2 mg/500 mg
4 mg/500 mg
2mg/1000 mg
4mg/1000 mg
Sitagliptin/metformin
50 mg/500 mg
50 mg/850 mg
50 mg/1000 mg
Reduces insulin resistance and
improves insulin sensitivity at the liver, fat
and muscle cells, allowing insulin to work
more effectively. May be taken with other
oral agents
Advise physician if any swelling or
shortness of breath
Low blood sugar very rare. Side effects not usual but
may promote weight gain, Monitor Liver function tests
May induce edema and cardiac failure
May increase risk fracture in women
*May improve fertility in women
Black Box Warning  may increase risk of MI
Alpha-glucosidase inhibitors: Delay the absorption of glucose from the gut
Taken with the first bite of each meal.
Take with the first bite of each
Abdominal pain, gas
Reduces the rise in blood sugar after a
meal.
By itself this drug will not cause low blood sugar but may
meal. May be combined with other oral
If taking other medication that can
occur if combined with secretagogues or insulin. Treat
agents or insulin.
cause hypoglycemia treat with
lows with milk or glucose tablets or gels. With this drug,
glucose tablets, milk or honey
candy, soft drinks or juice will not raise blood sugar
quickly
DPP-4 inhibitors: Enhance action of incretins by inhibiting breakdown of endogenous GLP-1 and GIP
Incretins are gut hormones that ↑release Take daily with or without food
Low blood sugar rare
of insulin and ↓ glucagon secretion in a
Some serious allergic reactions possible
glucose dependant way. DPP-4 is an
Rare case of pancreatitis
enzyme that deactivates incretins. This
drug inhibits DPP-4 and enhances and
prolongs action of incretins
See action of rosiglitazone and metformin
Taken twice a day
See action of sitagliptin and metformin
Taken twice a day
Type 1 diabetes
Pregnancy
Significant liver disease
Avoid use in CHF
Dosage adjustment with liver impairment,
Not to be used: withCHF or as monotherapy, as part
of triple therapy, if liver enzymes 2.5 x upper limit of
normal) discuss risk with patient if CAD present
Increased risk of heart failure if given in
combination with insulin

Type 1 diabetes

Pregnancy

Dosage adjustment with liver impairment,
Not to be used:with CHF or as monotherapy, as part of
triple therapy, if liver enzymes 2.5 x upper limit of normal)
discuss risk with patient if CAD present

Increased risk of heart failure if given in
combination with insulin
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Inflammation or ulceration of the bowel
Partial bowel obstruction
Diseases affecting digestion
Kidney disorders
Large hernia
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Type 1 diabetes
Pregnancy
Serious allergic reaction to a DPP-4 inhibitor
Dose adjustment in renal failure except for
linagliptin (no dosage adjustment needed but
caution)
Combination drugs: 2 oral agents combined in one tablet
See rosiglitazone and metformin
See rosiglitazone and metformin

See rosiglitazone and metformin
See sitagliptin and metformin

See sitagliptin and metformin
See sitagliptin and metformin
Injectable Agents for Treating Type 2 Diabetes
*Drugs that do not usually cause hypoglycemia*
Generic name
Liraglutide
(Victoza)
Exenatide
(Byetta)
Dosage
Action
Note: Do not use more than one drug from each class
Instructions for patients
Side effects
Main Contraindications
Glucagon–like peptide-1 (GLP-1) Agonist: Stimulate insulin production, inhibit glucagon production and increase feelings of satiety- resistant to DPP-4 enzyme
0.6 mg SC once daily to Increases insulin production
Report to GP if nausea and
GI upset- nausea, vomiting and diarrhea usually subside
 History of pancreatitis
increase weekly if
Inhibits glucagon production
vomiting do not go away over time over time
 Moderate to severe renal disease
needed to a max dose
Slows down gastric emptying
Store unused pens in refrigerator
Pancreatitis
 Liver disease (for liraglutide only) _
of 1.8 mg SC once
Pen being used can be stored at
Weight loss
 Personal or family history of medullary thyroid
daily. To be taken
room temperature for up to 1
Hypoglycemia if taken with other drugs that can cause
carcinoma or in patients with MEN 2 (multiple
anytime of the day,
month
hypoglycemia
medullary thyroid cancer type2)
independent of meals
Always remove the injection
 Type 1 diabetes
needle after each injection
 Heart disease (precaution)
5 mcg SC bid, usually
Do not expose to extreme
 Pregnancy and breastfeeding
before morning and
temperatures (Minimum 2˚Cevening meals, within
Maximum 25-30˚C)
60 minutes before
Do not mix with insulin
meals
*patient will require teaching on SC
Increase to 10 mcg SC
injection and use of prefilled pen
bid after 1 montth of
device
therapy if needed
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