Oral Therapies for Type 2 Diabetes

Drug

Daily dose

Reduction in HbA1c

Side effects

Contraindications

Metformin (500, 850, 1,000 mg. Extended-release: 500/750 mg, 1,000 mg)

Initial small dose and titrate. Max 2,550 mg/day

1–2 %

Nausea, vomiting, flatulence, anorexia, abdominal pain, diarrhea

congestive heart failure (class 3 or 4), serum creatinine ≥1.5 mg/dl (man) ≥ 1.4 mg/dl (woman), impaired hepatic function, acute myocardial infarction, septicemia

Chlorpramida (Diabinese) 100, 250 mg

Initial: 250 mg. Max: 750 mg

1–2 %

Hypoglycemia, weight gain, photosensitivity

Type 1 diabetes; pregnancy and nursing

Glimepiride (Amaryl) 1, 2, 4 mg

Initial: 1–2 mg. Max: 8 mg

Glyburide (Diabeta) 1.25, 2.5, 5 mg

Initial: 2.5–5 mg. Max: 20 mg

Glipzide 5, 10 mg. Extended-release 2.5, 5, 10 mg

Initial: 5 mg. Max: 20 mg

Pioglitazone (Actos) 15, 30, 45 mg

Initial: 15–30 mg. Max: 45 mg

0,5–1,5 %

Weight gain, osteoporosis/fracture, bladder cancer (pioglitazone), cardiovascular event (rosiglitazone)

Heart failure NYHA class III and IV

Rosiglitazone (Avandia) 2, 4, 8 mg

Initial: 2 mg bid or 4 mg qd. Max: 8 mg

Acarbose (Precose) 25, 50, 100 mg

Initial: 25 mg tid. Max: >60 kg–100 mg tid; <60 kg–50 mg tid

0.4–1.0 %

flatulence, abdominal distention, diarrhea. If in combination with other drug and patient develop mild hypoglycemia, use dextrose, not sucrose (cane sugar) to treat.

Renal failure (Clearance Cr < 25 ml/min or creatinine > 2 mg/dl. Ketoacidosis, bowel disease, colonic ulceration

Miglitol (Glyset) 25, 50, 100 mg

Initial: 25 mg tid. Max: 100 mg tid

Nateglinide (Starlix) 60, 120 mg

Initial/Max: 120 mg tid

0.7–1.5 %

Hypoglycemia, headache, arthralgia, nausea, upper respiratory infections, constipation

Children, pregnancy, nursing, type 1 diabetes, ketoacidosis

Repaglinide (Prandin) 0.5, 1, 2 mg

Initial (depends on HbA1c): 0.5–1mg tid. Max: 16 mg/day

Bromocriptine (Cycloset) 0.8 mg

Initial: 0.8 mg 2 h after waking in the morning. Max: 4.8 mg.

0.4–0.8 %

Nausea, fatigue, constipation, dizziness, rhinitis, headache.

Renal and hepatic failure, psychosis, type 1 diabetes, syncopal attacks, migraine headache.

References

UKPDS Group. Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33). UK Prospective Diabetes Study (UKPDS) Group. Lancet. 1998. 352(9131):837–53

ACCORD Study Group. Effects of Intensive Glucose Lowering in Type 2 Diabetes. N Engl J Med. 2008. 358(24):2545–59

Gaziano JM, Cincotta AH, O’Connor CM, Ezrokhi M, Rutty D, Ma ZJ, et al. Randomized clinical trial of quick-release bromocriptine among patients with type 2 diabetes on overall safety and cardiovascular outcomes. Diabetes Care. 2010 Jul;33(7):1503–8.PubMedCrossRef

Holman RR, Cull CA, Turner RC. A randomized double-blind trial of acarbose in type 2 diabetes shows improved glycemic control over 3 years (U.K. Prospective Diabetes Study 44). Diabetes Care. 1999 Jun;22(6):960–4.PubMedCrossRef

Bolinder J, Ljunggren O, Kullberg J, Johansson L, Wilding J, Langkilde AM, et al. Effects of dapagliflozin on body weight, total fat mass, and regional adipose tissue distribution in patients with type 2 diabetes mellitus with inadequate glycemic control on metformin. J Clin Endocrinol Metab. 2012 Mar;97(3):1020–31.PubMedCrossRef

Nathan DM, Buse JB, Davidson MB, Ferrannini E, Holman RR, Sherwin R, et al. Medical management of hyperglycemia in type 2 diabetes: a consensus algorithm for the initiation and adjustment of therapy: a consensus statement of the American Diabetes Association and the European Association for the Study of Diabetes. Diabetes Care. 2009 Jan;32(1):193–203.PubMedCrossRef

Handelsman Y, Mechanick JI, Blonde L, Grunberger G, Bloomgarden ZT, Bray GA, et al. American Association of Clinical Endocrinologists Medical Guidelines for Clinical Practice for developing a diabetes mellitus comprehensive care plan. Endocr Pract. 2011;17 Suppl 2:1–53.PubMedCrossRef

Viollet B, Guigas B, Sanz Garcia N, Leclerc J, Foretz M, Andreelli F. Cellular and molecular mechanisms of metformin: an overview. Clin Sci (Lond). 2012 Mar;122(6):253–70.CrossRef

Bailey CJ. Biguanides and NIDDM. Diabetes Care. 1992 Jun;15(6):755–72.PubMedCrossRef

10.

Libby G, Donnelly LA, Donnan PT, Alessi DR, Morris AD, Evans JM. New users of metformin are at low risk of incident cancer: a cohort study among people with type 2 diabetes. Diabetes Care. 2009 Sep;32(9):1620–5.PubMedCrossRef

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