Amaryl

[Glimepiride]

These data indicate that glimepiride did not accumulate in serum, and the pharmacokinetics of glimepiride were not different in healthy volunteers and in NIDDM patients. Oral clearance of glimepiride did not change over the 1-8-mg dose range, indicating linear pharmacokinetics.

Variability.

In normal healthy volunteers, the intra-individual variabilities of Cmax, AUC, and CL/f for glimepiride were 23%, 17%, and 15%, respectively, and the inter-individual variabilities were 25%, 29%, and 24%, respectively.

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Special Populations

Geriatric.

Comparison of glimepiride pharmacokinetics in NIDDM patients <65 years and those >65 years was performed in a study using a dosing regimen of 6 mg daily. There were no significant differences in glimepiride pharmacokinetics between the two age groups. The mean AUC at steady state for the older patients was about 13% lower than that for the younger patients; the mean weight-adjusted clearance for the older patients was about 11% higher than that for the younger patients.

Pediatric.

No studies were performed in pediatric patients.

Gender.

There were no differences between males and females in the pharmacokinetics of glimepiride when adjustment was made for differences in body weight.

Race.

No pharmacokinetic studies to assess the effects of race have been performed, but in placebo-controlled studies of AMARYL (glimepiride tablets) in patients with NIDDM, the antihyperglycemic effect was comparable in whites (n = 536), blacks (n = 63), and Hispanics(n = 63).

Renal Insufficiency.

A single-dose, open-label study was conducted in 15 patients with renal impairment. AMARYL (3 mg) was administered to 3 groups of patients with different levels of mean creatinine clearance (CLcr); (Group I, CLcr = 77.7 mL/min, n = 5), (Group II, CLcr = 27.7 mL/min, n = 3), and (Group III, CLcr = 9.4 mL/min, n = 7). AMARYL was found to be well tolerated in all 3 groups. The results showed that glimepiride serum levels decreased as renal function decreased. However, M1 and M2 serum levels (mean AUC values) increased 2.3 and 8.6 times from Group I to Group III. The apparent terminal half-life (T1/2) for glimepiride did not change, while the half-lives for M1 and M2 increased as renal function decreased. Mean urinary excretion of M1 plus M2 as percent of dose, however, decreased (44.4%, 21.9%, and 9.3% for Groups I to III).

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