Glimepiride: evidence-based facts, trends, and observations

Figures & data

Figure 1 Management of hyperglycemia in type 2 diabetes: a patient-centered approach. Position statement of the American Diabetes Association and the European Association for the Study of Diabetes. © 2012, Springer Science and Business Media. Reproduced with kind permission from Inzucchi SE, Bergenstal RM, Buse JB, et al. Management of hyperglycaemia in type 2 diabetes: a patient-centered approach. Position statement of the American Diabetes Association (ADA) and the European Association for the Study of Diabetes (EASD). Diabetologia. 2012;55(6):1577–1596.⁹

Abbreviations: DPP-4, dipeptidyl peptidase IV; GIP, glucose-dependent insulinotropic peptide; GLP-1, glucagon-like peptide 1; NPH, neutral protamine Hagedorn; TZD, thiazolidinedione.

Figure 2 International Diabetes Federation treatment algorithm for people with type 2 diabetes.

© 2005, International Diabetes Federation. Reproduced with kind permission from International Diabetes Federation Clinical Guidelines Task Force. Global guidelines for type 2 diabetes. 2005. Available from: http://www.idf.org/Global_guideline. Accessed on March 29, 2012.¹⁰

Table 1 Comparison of oral hypoglycemic agents used in the management of type 2 diabetes mellitus

Class of hypoglycemic agents	Duration of action	Reduction in HbA1c (%)	Reduction in FPG (mg/dL)	Dosage
Sulfonylureas	12–24 hours	0.8–2.0	60–70
Glyburide	Up to 24 hours			1.25–20 mg as single dose or in two divided doses
Glipizide	6–12 hours			2.5–20 mg twice a day
Gliclazide	12 hours			40–80 mg single dose 160–320
Glimepiride	Up to 24 hours			1–4 mg once 8 mg max
Meglitinides analogues	3 hours	0.5–2.0	65–75	0.5–4 mg TDS
Biguanides	7–12 hours	1.5–2.0	50–70	1–2.5 g/day
Thiazolidinediones	Up to 24 hours	0.5–1.5	25–50	15–45 mg/day
α-Glucosidase inhibitor	4 hours	0.7–1.0	35–40	25–100 mg TDS
DDP-4 inhibitors	24 hours	0.5–1.4	–
Sitagliptin				100 mg once daily
Sexagliptin				2.5 mg/5 g once daily
Vildagliptin				50 mg once or twice daily
Linagliptin				05 mg once daily

Abbreviations: FPG, fasting plasma glucose; HbA_1c, glycosylated hemoglobin; TDS, three times daily.

Table 2 Pharmacokinetic properties of glimepiride

Absorption	Completely absorbed after oral administration within 1 hour of administration; significant absorption occurs: plasma protein binding is 99.4% and volume of distribution is 8.8 L. Accumulation does not occur after multiple doses.
Metabolism	The drug is primarily metabolized in the liver by CYP2C9 to the active M1 (hydroxyl) metabolite and then to inactive M2 (carboxy) metabolite.
Excretion	The main route of excretion is through kidneys. A total of 60% of the metabolites are excreted in urine (predominantly M1) and remainder in feces (predominantly M2).

Figure 3 Chemical structure of glimepiride.

Table 3 Comparative efficacy of glimepiride in patients with type 2 diabetes

Reference	Study design	Drug regimen (mg)	Results
Goldberg et al^Citation29	DB, R, PC 14-weeks	G 0, 1, 4 or 8 qd	Median FPG, PPG and HbA1c at all G does significantly lower than P (P < 0.05)
Sonnenberg et al^Citation30	DB, R, CO 8-weeks	G 3 bid or 6 qd	Glycemic control equivalent between qd and bid regimens
Rosenstock et al^Citation31	DB, R, PC 14-weeks	G 0 qd, 4 bid, 8 qd, 8 bid or 16 qd	Median FPG and HbA1c at all G does significantly lower than P (P < 0.001)
Draeger et al^Citation37	DB, R 52-weeks	G 1–8 qd or glyburide 2.5 to 20 qd or bid	Similar (significant) reductions in FPG and HbA1c in both groups
Dills et al^Citation36	DB, R 52-weeks	G 1–16 qd or glyburide 1.25–20 qd	Similar (significant) reduction in FPG and HbA1c in both groups; significantly lower C peptide and fasting insulin concentrations with G than with glyburide
Riddle^Citation41	DB, R, PC 24-weeks	Insulin ± G 8 bid	Significantly reduced exogenous insulin requirement with G compared with P
Schernthaner et al^Citation38	DB, R 27-weeks	G 1–6 mg or Gliclazide modified release (MR) 30–120 mg	Similar reduction in FPG and HbA1c in both groups Safety of glimepiride was better
Charpentier et al^Citation33	DB, R 20-weeks	G 1–6 mg OD M 850 tid	No difference in HbA1c or FBG with either agent as monotherapy glimepiride more effective in reducing PPBG
Jeon and Oh^Citation63	OL, R 32-weeks	V50 mg bid plus M500 mg bid or V 50 mg bid plus G 2 mg bid	Comparable efficacy of both groups in reducing HbA1c Less risk of hypoglycemia with V group

Abbreviations: bid, twice daily; DB, double-blind; FPG, fasting plasma glucose; G, glimepiride; HbA_1c, glycosylated hemoglobin; M, metformin; OL, open-label; PC, placebo-controlled; PPG, postprandial glucose; R, randomized; tid, three times daily; qd, once daily; V, vildagliptin.

InzucchiSEBergenstalRMBuseJBManagement of hyperglycaemia in type 2 diabetes: a patient-centered approach. Position statement of the American Diabetes Association (ADA) and the European Association for the Study of Diabetes (EASD)Diabetologia20125561577159622526604

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