Oral Drugs for Treating Hyperglycemia

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(Tables 27-7, 27-8, and 27-9.) The drugs for treating type 2 diabetes fall into three categories: (1) Drugs that primarily stimulate insulin secretion: Sulfonylureas remain the most widely prescribed drugs for treating hyperglycemia. The meglitinide analog repaglinide and the d-phenylalanine derivative nateglinide also bind the sulfonylurea receptor and stimulate insulin secretion. (2) Drugs that alter insulin action: Metformin works primarily in the liver. The thiazolidinediones appear to have their main effect on skeletal muscle and adipose tissue. (3) Drugs that principally affect absorption of glucose: The Α-glucosidase inhibitors acarbose and miglitol are such currently available drugs.

Table 27-7. Oral antidiabetic drugs that stimulate insulin secretion.

Drug	Tablet Size	Daily Dose	Duration of Action	Cost per Unit	Cost for 30 Days Treatment Based on Maximum Dosage1
Sulfonylureas
Tolbutamide (Orinase)	250 and 500 mg	0.5-2 g in 2 or 3 divided doses	6-12 hours	$0.28/500 mg	$33.60
Tolazamide (Tolinase)	100, 250, and 500 mg	0.1-1 g as single dose or in 2 divided doses	Up to 24 hours	$0.77/250 mg	$83.40
Acetohexamide (Dymelor)2	250 and 500 mg	0.25-1.5 g as single dose or in 2 divided doses	8-24 hours	$1.34/500 mg	$120.60
Chlorpropamide (Diabinese)2	100 and 250 mg	0.1-0.5 g as single dose	24-72 hours	$0.67/250 mg	$40.20
Glyburide         (Dia&bgr;eta, Micronase)	1.25, 2.5, and 5 mg	1.25-20 mg as single dose or in 2 divided doses	Up to 24 hours	$0.78/5 mg	$93.60
(Glynase)	1.5, 3, and 6 mg	1.5-18 mg as single dose or in 2 divided doses	Up to 24 hours	$1.07/6 mg	$96.30
Glipizide         (Glucotrol)	5 and 10 mg	2.5-40 mg as single dose or in 2 divided doses on an empty stomach	6-12 hours	$0.59/10 mg	$70.80
(Glucotrol XL)	5 and 10 mg	Up to 20 or 30 mg daily as a single dose	Up to 24 hours	$0.81/10 mg	$72.90
Gliclazide (not available in the US)	80 mg	40-80 mg as single dose; 160-320 mg as divided dose	12 hours	-	-
Glimepiride (Amaryl)	1, 2, and 4 mg	1-4 mg as single dose	Up to 24 hours	$1.31/4 mg	$39.30
Meglitinide analogs
Repaglinide (Prandin)	0.5, 1, and 2 mg	4 mg in two divided doses given 15 minutes before breakfast and dinner	3 hours	$1.29/2 mg	$77.40
d-Phenylalanine derivative
Nateglinide (Starlix)	60 mg and 120 mg	60 or 120 mg 3 times a day before meals	1.5 hours	$1.29/120 mg	$116.10

¹Average wholesale price (AWP, for AB-rated generic when available) for quantity listed. Source: Red Book Update, Vol. 24, No. 4, April 2005. AWP may not accurately represent the actual pharmacy cost because wide contractual variations exist among institutions.
²There has been a decline in use of these formulations. In the case of chlorpropamide, the decline is due to its numerous side effects (see text).

Table 27-8. Oral antidiabetic drugs that are insulin-sparing.

Drug	Tablet Size	Daily Dose	Duration of Action	Cost per Unit	Cost for 30 Days Treatment Based on Maximum Dosage1
Biguanides
Metformin (Glucophage)	500, 850, and 1000 mg	1-2.5 g; one tablet with meals 2 or 3 times daily	7-12 hours	$1.46/850 mg	$131.40
Extended-release metformin (Glucophage XR)	500 mg	500-2000 mg once a day	Up to 24 hours	$0.88/500 mg	$105.60
Thiazolidinediones
Rosiglitazone (Avandia)	2, 4, and 8 mg	4-8 mg daily (can be divided)	Up to 24 hours	$5.59/8 mg	$167.70
Pioglitazone (Actos)	15, 30, and 45 mg	15-45 mg daily	Up to 24 hours	$6.28/45 mg	$188.42
a-Glucosidase inhibitors
Acarbose (Precose)	50 and 100 mg	75-300 mg in 3 divided doses with first bite of food	4 hours	$0.99/100 mg	$89.10
Miglitol (Glyset)	25, 50, and 100 mg	75-300 mg in 3 divided doses with first bite of food	4 hours	$0.97/100 mg	$87.30

¹Average wholesale price (AWP, for AB-rated generic when available) for quantity listed. Source: Red Book Update, Vol. 24, No. 4, April 2005. AWP may not accurately represent the actual pharmacy cost because wide contractual variations exist among institutions.

Table 27-9. Combination oral antidiabetic drugs.

Drug	Tablet Size	Daily Dose	Duration of Action	Cost per Unit	Cost for 30 Days Treatment Based on Maximum Dosage1
Glyburide/metformin (Glucovance)	1.25 mg/250 mg 2.5 mg/500 mg 5 mg/500 mg	Maximum daily dose of 20 mg glyburide/2000 mg metformin	See individual drugs2	$1.13/5/500 mg	$135.60
Rosiglitazone/metformin (Avandamet)	1 mg/500 mg 2 mg/500 mg 4 mg/500 mg	Maximum daily dose of 8 mg rosiglitazone/2000 mg metformin	See individual drugs2	$1.75/2/500 mg	$210.00

¹Average wholesale price (AWP, for AB-rated generic when available) for quantity listed. Source: Red Book Update, Vol. 24, No. 4, April 2005. AWP may not accurately represent the actual pharmacy cost because wide contractual variations exist among institutions.
²Glyburide, Table 27-7; metformin, Table 27-8; and rosiglitazone, Table 27-8.