. 2008 Oct;1(8):39–48.

Table 4.

Oral Antihyperglycemic Agents

Drug	Mechanism of action	Hemoglobin A_1C reduction, %	Dose range	Adverse events	Comments	Cost for 30-day supply (range)^*
*Alpha-glucosidase inhibitors*
Acarbose(Precose)	Delay complex carbohydrate absorption	0.5–0.8	25–100 mg tid w/meals	Flatulence, diarrhea, abdominal pain	Titrate slowly to minimize GI effects	$73.79-$80.99
Miglitol(Glyset)	Delay complex carbohydrate absorption	0.5–0.8	25–100 mg tid w/meals	Flatulence, diarrhea, abdominal pain	Titrate slowly to minimize GI effects	$79.99-$99.99
*Biguanides*
Metformin (Glucophage)	Decrease hepatic glucose output; increase peripheral glucose uptake	1–2	IR: 1000–2550 mg/d divided bid or tidER: 500–2000 mg/d	Nausea, vomiting, diarrhea, flatulence	Take w/meals; avoid use in patients w/renal or hepatic impairment or CHF due to increased risk of lactic acidosis	IR: $24.99-$77.99 ER: $6.33-$25.32
*Dipeptidyl peptidase-4 inhibitors*
Sitagliptin (Januvia)	Slow inactivation of incretin hormones	0.5–0.8	25–100 mg/d	Not clinically significant	Renal dose: 50 mg/d for CrCl ≥30 to <50 mL/min; 25 mg/d for CrCl <30 mL/min	$45.27-$181.09
*Nonsulfonylurea secretagogues*
Nateglinide (Starlix)	Stimulate insulin secretion from the pancreas	1–1.5	60–120 mg tid	Hypoglycemia, weight gain	Take w/meals due to rapid onset	$154.11-$164.85
Repaglinide (Prandin)	Stimulate insulin secretion from the pancreas	1–1.5	0.5–4 mg tid to qid	Hypoglycemia, weight gain	Take w/meals due to rapid onset	$164.82-$396.08
*Sulfonylureas*
First-generation
Chlorpropamide (Diabinese)	Stimulate insulin secretion from the pancreas	1–2	100–750 mg/d	Hypoglycemia, weight gain	Use of these agents has declined due to side effects and unpredictable results	$8.62-$31.49
Tolazamide (Tolinase)			100–1000 mg/d given as a single dose or divided bid if dose is >500 mg/d			$12-$69.98
Tolbutamide (Orinase)			250–3000 mg/d in divided doses			$5-$59.97
Second-generation
Glimepiride (Amaryl)			1–8 mg/d	Hypoglycemia, weight gain		$12.99-$29.98
Glipizide (Glucotrol)			IR: 2.5–40 mg/d as a single dose or divided bid ER: 2.5–20 mg/d			IR: $3-$25.99 ER: $18.99$39.98
Glyburide (Micronase, Diabeta, Glynase)			1.25–20 mg/d as a single dose or divided bid (Glynase: 0.7512 mg/d as a single dose or divided bid if dose >6 mg/d)			$12.99-$47.96 (Glynase: $4.33$109.42)
*Thiazolidinediones*
Pioglitazone (Actos)	Increase peripheral tissue insulin sensitivity	0.5–1.4	15–45 mg/d	Edema, weight gain	Black box warning: these agents can cause or exacerbate CHF; contraindicated in patients with NYHA class III or IV heart failure	$134.07-$195.99
Rosiglitazone (Avandia)	Increase peripheral tissue insulin sensitivity	0.5–1.4	4–8 mg/d as a single dose or divided bid	Edema, weight gain		$120.10-$223.49

Cost calculated from generic, if available, and lowest bottle size available. GI indicates gastrointestinal; IR, immediate release; ER, extended release; CHF, congestive heart failure; CrCl, creatinine clearance; NYHA, New York Heart Association.

Sources: Lacy CF, Armstrong LL, Goldman MP, Lance LL, eds. Drug Information Handbook. 17th ed. Hudson, OH: Lexi-Comp; 2008. McEvoy GK, ed. AHFS Drug Information. Bethesda, MD: American Society of Health-System Pharmacists; 2008. Cost: www.drugstore.com.