STIMULATORS OF INSULIN RELEASE (Insulin Secretagogues) – increase insulin secretion from the pancreas1 |
SULFONYLUREAS (SFUs) |
Tolbutamide
- Orinase®
- various generics
|
1957 |
500 mg tablets |
Initial: 1000-2000 mg daily
Range: 250-3000 mg
(seldom need >2000 mg/day)
Dose: Taken two or three times daily |
SE: hypoglycemia, weight gain
Preferred SFU for elderly
Must be taken 2-3 times daily |
Glimepiride
|
11/95 |
1 mg, 2 mg, 4 mg tablets |
Initial: 1-2 mg daily
Range: 1-8 mg
Dose: Taken once daily |
SE: hypoglycemia, weight gain
Need to take only once daily |
Glipizide
- Glucotrol®
- Glucotrol XL®
- various generics
|
5/84
4/94 |
5 mg, 10 mg tablets
ER: 2.5 mg, 5 mg, 10 mg tablets |
Initial: 5 mg daily
Range: 2.5-40 mg2 (20 mg for XL)
Dose: Taken once or twice (if >15 mg) daily |
SE: hypoglycemia, weight gain
Preferred SFU for elderly
ER = extended release/take once a day |
Glyburide
- Micronase®, DiaBeta®
- various generics
|
5/84 |
1.25 mg, 2.5 mg, 5 mg tablets |
Initial: 2.5-5 mg daily
Range: 1.25-20 mg2
Dose: Taken once or twice daily |
SE: hypoglycemia, weight gain |
Glyburide, micronized
- Glynase PresTab®
- various generics
|
3/92 |
1.5 mg, 3 mg, 4.5 mg, 6 mg
micronized tablets |
Initial: 1.5-3 mg daily
Range: 0.75-12 mg
Dose: Taken once or twice (if >6 mg) daily |
SE: hypoglycemia, weight gain |
GLINIDES |
Repaglinide
|
12/97 |
0.5 mg (white), 1 mg (yellow), 2 mg
(red) tablets |
Initial: 1-2 mg daily
(0.5 mg if A1C <8%)
Range: 0.5-16 mg
Max dose per meal is 4 mg
Dose: Taken two, three, or four times daily |
SE: hypoglycemia
Safe for elderly
Duration of action is only 4 hours
Take within 15-30 minutes of meal |
Nateglinide
|
12/00 |
60 mg (pink), 120 mg (yellow) tablets |
Initial: 120 mg three times daily
(if A1C close to goal, use 60 mg)
<pRange: 180-360 mg
Dose: Taken three times daily
</p |
SE: hypoglycemia
Safe for elderly
Duration of action is only 2 hours
Take within 30 minutes of meal |
EUGLYCEMICS: Medicines that bring the blood glucose into the normal range. These medicines should not cause hypoglycemia.3 |
BIGUANIDES: decreases glucose release from liver; decreases intestinal absorption of glucose; improves insulin sensitivity (increases glucose uptake and utilization) |
Metformin
- Glucophage®
- Extended release (ER):
- Glucophage XR®
- Fortamet®
- Glumetza
- Riomet® (liquid, 500 mg/5ml)
|
12/94
10/00 |
Glucophage: 500 mg, 850 mg, 1000 mg tablets
Glucophage XR: 500 mg, 750 mg tablets
Fortamet: 500 mg, 1000 mg tablets
Glumetza: 500 mg, 1000 mg tablets
Generic metformin ER: 500 mg, 750 mg tablets |
Initial: 500 mg twice daily or 850 mg once daily
Range: 500-2550 mg
Dose: Taken two or three times daily
ER: Initial: 500 mg once daily
Range: 500-2000 mg
Dosed once daily |
SE: Gastrointestinal symptoms (diarrhea, nausea, upset stomach), metallic taste (3%),
lactic acidosis (0.03 cases/1000 people)4,5
Take with meals (ER with evening meal)
Cannot use if have liver or kidney problems, take a drug to treat heart failure, or drink alcohol excessively |
ALPHA-GLUCOSIDASE INHIBITORS: STARCH BLOCKERS – delay digestion and absorption of carbohydrates |
Acarbose
- Precose®
- various generics
|
9/95 |
25 mg, 50 mg, 100 mg tablets |
Initial: 25 mg three times daily
Range: 75-300 mg
(max 150 mg if <60 kg)
Dose: Taken three times daily |
SE: flatulence
Take with first bite of meal
Start with low dose and slowly to minimize GI intolerance. |
THIAZOLIDINEDIONES (Glitazones or TZDs): decrease insulin resistance in the body (muscle and fat tissues) |
Pioglitazone (preferred over rosiglitazone)
|
7/99 |
15 mg, 30 mg, 45 mg
(white to off-white) tablets |
Initial: 15-30 mg daily
Range: 15-45 mg
Dose: Taken once daily |
SE: anemia, swelling (edema) from fluid retention, weight gain, macular edema (in eye), bone loss and fractures in women
May cause or worsen heart failure
Cannot use if have liver problems or severe heart failure
Requires liver monitoring6 |
Rosiglitazone
|
5/99 |
2 mg (pink), 4 mg (orange), 8 mg
(red-brown) tablets |
Initial: 4 mg daily
Range: 4-8 mg
Dose: Taken once or twice daily |
SE: anemia, swelling (edema) from fluid retention, weight gain, macular edema (in eye), bone loss and fractures in women
May increase risk of heart problems such as heart-related chest pain (angina) or heart attack (myocardial infarction)
May cause or worsen heart failure
Cannot use if have liver problems or severe heart failure
Requires liver monitoring6 |
GLP-1 ANALOGS: increase insulin secretion, reduce glucose release from liver after meals, delay food emptying from stomach and promote satiety |
Exenatide
|
4/05 |
5 mcg per dose and 10 mcg per dose
Injected under the skin (subcutaneous/SQ)
Available as a pen device |
Initial: 5 mcg SQ twice daily
Range: up to 10 mcg SQ twice daily
Dose: Taken twice daily |
SE: nausea, headache, hypoglycemia (when used with insulin secretagogues)
Rare reports of sudden pancreatitis (inflammation of pancreas)
May cause mild weight loss |
Liraglutide
|
01/10 |
3 mL pen that delivers doses of 0.6 mg, 1.2 mg, or 1.8 mg
Injected under the skin (subcutaneous/SQ)
Available as a pen device |
Initial: 0.6 mg SQ once daily
Range: up to 1.8 mg SQ once daily
Dose: Taken once daily |
SE: nausea, headache, diarrhea, hypoglycemia (when used with insulin secretagogues)
Rare reports of sudden pancreatitis (inflammation of pancreas). Cannot be used if have history of medullary thyroid cancer |
Albiglutide
|
04/14 |
30mg or 50mg per dose
Injected under the skin (subcutaneous/SQ)
Requires reconstitution
Available in dose-specific single-dose pen
devices |
Initial: 30mg once weekly
Range: can increase to 50mg once weekly
if inadequate response |
SE: injection site reaction, nausea, diarrhea, upper respiratory
infection.
Rare reports of pancreatitis (inflammation of pancreas);
cannot be used if have history of medullary thyroid cancer. |
Dulaglutide
|
09/14 |
0.75 mg or 1.5 mg per dose
Injected under the skin (subcutaneous/SQ)
Available in dose-specific, single-dose pen devices. |
Initial: 0.75 mg once weekly
Range: may increase up to 1.5 mg once
weekly if inadequate response |
SE: nausea, diarrhea, vomiting, abdominal pain
Cannot use if family history of medullary thyroid carcinoma
(MTC) or if have multiple endocrine neoplasia syndrome type
2 (MEN2)
Rare reports of pancreatitis (inflammation of pancreas);
cannot be used if have history of medullary thyroid cancer |
DPP-4 INHIBITORS: increase insulin secretion, reduce glucose release from liver after meals |
Alogliptin
|
01/13 |
6.25mg (light pink), 12.5mg (yellow), 25mg
(light red) tablets |
25mg PO daily.
Taken once daily. |
SE:stuffy or runny nose, sore throat, headache, upper
respiratory infection, rare severe allergic reactions (swelling of
tongue, throat, face or body; severe rash)
rare reports of
pancreatitis
No weight gain |
Sitagliptin
|
11/06 |
25 mg (pink), 50 mg (light beige),
100 mg (beige) tablets |
Initial: 100 mg daily
Range: 25-100 mg daily
Dose: Taken once daily |
SE: runny nose, upper respiratory infection, rare severe allergic reactions (swelling of tongue, throat, face or body; severe rash)
No weight gain; Lower doses used if kidney problems |
Saxagliptin
|
7/09 |
2.5 mg (pale to light yellow), 5 mg (pink) tablets |
Initial: 2.5 or 5 mg daily
Range: 2.5-5 mg daily
Dose: Taken once daily |
SE: upper respiratory infection, urinary tract infection, headache
No weight gain; Lower doses used if kidney problems |
Linagliptin
|
5/11 |
5mg (light red) tablet |
Initial: 5 mg daily
Dose: Taken once daily |
SE: runny nose, sore throat, rare reports of pancreatitis, rare severe allergic reactions, no weight gain; |
SGLT2 inhibitors: increase glucose excretion in the urine |
Canagliflozin
|
03/13 |
100mg (yellow, capsule-shaped), 300mg
(white, capsule-shaped) tablets |
Initial: 100mg daily
Range: 100-300mg daily
Dose: Taken once daily |
SE: increased urination or urgency, lower blood pressure,
dizziness, genital yeast infections, urinary tract infections
increase in blood potassium; rare severe allergic reactions
(swelling of tongue, throat, face or body; severe rash)
Cannot use if have kidney problems |
Dapagliflozin
|
01/14 |
5mg (yellow, round shaped), 10mg (yellow,
diamond shaped) tablets |
Initial: 5mg once daily
Range: up to 10mg daily |
SE: increased urination or urgency, lower blood pressure,
dizziness, genital yeast infections, urinary tract infections
increase in blood potassium; rare severe allergic reactions
(swelling of tongue, throat, face or body; severe rash)
Cannot use if have kidney problems |
Empagliflozin
|
08/14 |
10mg (pale, beige, round), 25mg (pale, beige
oblong) tablets |
Initial: 10mg once daily
Range: up to 25mg daily |
SE: increased urination or urgency, lower blood pressure,
dizziness, genital yeast infections, urinary tract infections
increase in blood potassium; rare severe allergic reactions
(swelling of tongue, throat, face or body; severe rash)
Cannot use if have kidney problems |
COMBINATION ORAL PILLS |
Alogliptin/Metformin
|
01/13 |
12.5mg/500mg (pale yellow), 12.5mg/1000mg
(pale yellow) oblong tablets |
Initial: 12.5mg/500mg once or twice daily
Range: up to 25/2000 Taken twice daily with food. |
Same as above with alogliptin and metformin |
Alogliptin/Pioglitazone
|
01/13 |
12.5mg/15mg (pale yellow), 12.5mg/30mg (pale peach),
12.5mg/45mg (pale red), 25mg/15mg (yellow), 25mg/30mg
(peach), 25mg/45mg (red) round tablets |
Initial: 12.5mg/15mg once daily
Range: up to 25/45 mg Taken once daily with or without food. |
Same as above with alogliptin and pioglitazone |
Empagliflozin/Linagliptin
|
02/15 |
10mg/5mg (pale yellow), 25mg/5mg (pale pink) triangular
tablets |
Initial: 10mg/5mg once daily
Range: up to 25mg/5mg once daily |
Same as above with empagliflozin and linagliptin |
Empagliflozin/Metformin
|
01/15 |
5mg/500mg (orange yellow), 5mg/1000mg (brownish yellow),
12.5mg/500mg (pale brownish purple), 12.5mg/1000mg (dark
brownish purple) oval film-coated tablet |
Initial: 5mg/500mg or 5mg/1000mg
Range: up to 25mg/2000mg
Taken in 2 divided doses |
Same as above with empagliflozin and
metformin |
Canagliflozin/Metformin
|
08/14 |
50mg/500mg (white), 50mg/1000mg (beige), 150mg/500mg
(yellow), 150mg/1000mg (purple) capsule-shaped film-coated
tablets |
Initial: 50mg/500mg or 50mg/1000mg
Range: up to 300mg/2000mg
Taken in 2 divided doses |
Same as above with canagliflozin and metformin |
Dapagliflozin/Metformin XR
|
10/14 |
5mg/500mg (orange), 5mg/1000mg (pink to dark pink),
10mg/500mg (pink), 10mg/1000mg (yellow to dark yellow) oval
film-coated tablet |
Initial: base on patient’s current regimen
Range: up to 10mg/2000mg daily |
Same as above with dapagliflozin and metformin |
Glyburide/Metformin
- Glucovance®
- various generics
|
7/00 |
1.25 mg/250 mg, 2.5 mg/500 mg, 5 mg/500 mg tablets |
Initial: 1.25 mg/250 mg once or twice daily
Range: up to – 20/2000 mg
Dose: Taken once or twice daily |
Same as above with glyburide and metformin |
Glipizide/Metformin
- Metaglip®
- various generics
|
10/02 |
2.5 mg/250 mg, 2.5mg/500 mg, 5mg/500 mg tablets |
Initial: 2.5 mg/250 mg daily or 2.5mg/500 mg twice daily
Range: up to 20/2000 mg
Dose: Taken once or twice daily |
Same as above with glipizide and metformin |
Linagliptin/Metformin
|
01/12 |
2.5mg/500mg (light yellow), 2.5mg/850mg (light orange, oval),
2.5mg/1000mg (light pink) oval tablets |
Initial:2.5mg/500mg twice daily with food
Range:up to 2.5mg/1000mg twice daily with
food. |
Same as above with linagliptin and metformin |
Rosiglitazone/Metformin
- Avandamet®
- various generics
|
10/02 |
2 mg/500 mg (pale pink), 2 mg/1000 mg (yellow), 4 mg/500 mg (orange), 4 mg/1000 mg (pink) oval tablets |
Initial: 2 mg/5000 mg once or twice daily
Range: up to 8 mg/2000 mg
Dose: Taken twice daily |
Same as above with metformin and rosiglitazone |
Pioglitazone/Metformin
- ActoPlus Met®
- various generics
|
8/05 |
15 mg/500 mg, 15 mg/850 mg (white to off-white) oblong tablets |
Initial: 15 mg/500 mg or 15 mg/850 mg once or twice daily
Range: up to 45 mg/2550 mg
Dosed once or twice daily |
Same as above with metformin and pioglitazone |
Pioglitazone/Glimepiride
|
7/06 |
30 mg/2 mg, 30 mg/4 mg (white to off-white) tablets |
Initial: 30 mg/2 mg or 30 mg/4 mg once daily
Range: max of one tablet daily
Dose: Taken once daily |
Same as above with pioglitazone and glimepiride |
Rosiglitazone/Glimepiride
- Avandryl®
- various generics
|
11/05 |
4 mg/1 mg (yellow), 4 mg/2 mg (orange), 4 mg/4 mg (pink) rounded triangle tablets |
Initial: 4 mg/1 mg or 4 mg/2 mg once daily
Range: up to 8 mg/4 mg
Dose: Taken once daily |
Same as above with rosiglitazone and glimepiride |
Sitagliptin/Metformin
|
03/07 |
50 mg/500 mg (light pink), 50 mg/1000mg
(red) oblong tablets |
Initial: 50 mg/500 mg or 50 mg/1000 mg twice daily
Range: up to 100 mg/2000 mg
Dose: Taken twice daily |
Same as above/below with sitagliptin and metformin |
Sitagliptin/Metformin
|
2/12 |
50 mg/500 mg (light blue), 50 mg/1000 mg (light green),100
mg/ 1000 mg (blue) oval tablets |
Initial: 100 mg/1000 mg daily
Range: up to 100 mg/2000 mg daily
Dose: Taken once daily |
Same as above/below with sitagliptin and metformin |
Repaglinide/Metformin
|
06/08 |
1 mg/500 mg (yellow), 2 mg/500 mg (pink) tablets |
Initial: 1 mg/500 mg twice daily
Range: 10 mg/2500 mg, Max per dose
4 mg/1000 mg
Dose: Taken twice or three times daily |
Same as above with repaglinide and metformin |
Pioglitazone/Metformin XR
|
05/09 |
15 mg/1000 mg, 30 mg/1000 mg (white to off-white) round tablets |
Initial: 15 mg/1000 mg or 30 mg/1000 mg once daily
Range: up to 45 mg/2000 mg
Dose: Taken once daily |
Same as above with metformin and pioglizatone |
Saxagliptin/Metformin XR
|
11/10 |
5 mg/500 mg (light brown to brown), 5 mg/1000 mg (pink), 2.5 mg/1000 mg (pale yellow to light yellow) capsule-shaped tablets |
Initial: 5 mg/500 mg or 5 mg/1000 mg once daily
Range: up to 5 mg / 2000 mg
Dose: Taken once daily |
Same as above with metformin and saxagliptin |