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Rezulin

Clinical Pharmacology
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Clinical Pharmacology

Rezulin

Geriatrics: Steady-state pharmacokinetics of troglitazone, Metabolite 1 and Metabolite 3 in healthy elderly subjects are comparable to those seen in young adults.

Pediatrics: Pharmacokinetic data in the pediatric population are not available.

Gender: Plasma concentrations of troglitazone and its metabolites are similar in men and women.

Ethnicity: Pharmacokinetics of troglitazone and its metabolites are similar among various ethnic groups.

Pharmacodynamics and Clinical Effects

Clinical studies demonstrate that Rezulin improves insulin sensitivity in insulin-resistant patients. Rezulin increases insulin-dependent glucose disposal, reduces hepatic gluconeogenesis, and enhances cellular responsiveness to insulin and thus, improves dysfunctional glucose homeostasis. In patients with type II diabetes, the decreased insulin resistance produced by Rezulin causes decreases in serum glucose, plasma insulin, and hemoglobin A1C. Unlike sulfonylureas, Rezulin does not stimulate insulin secretion. Addition of Rezulin to a sulfonylurea has a synergistic effect since both agents act to improve glucose tolerance by different but complementary mechanisms. These effects occur without weight loss and persist for 52 weeks of Rezulin treatment.

In clinical trials of Rezulin as monotherapy or in combination, an increase in LDL (up to 1 3%), HDL (up to 16%), and total cholesterol (total-C) (up to 5%) occurred while total-C/ HDL and LDUHDL ratios did not change. The increase in total cholesterol is due to the increase in HDL and LDL cholesterol. Despite the observed increase in total and LDL cholesterol, fraction levels are not increased.

Patients treated with Rezulin as monotherapy or in combination with other agents exhibited a reduction in fasting (-13% to -26%) and postprandial triglyceride levels. For patients on Rezulin and insulin, reduction in insulin doses may occur following Rezulin therapy and some attenuation of the triglyceride reduction may occur.

Pharmacokinetic estimators of systemic troglitazone exposure do not improve the prediction of pharmacodynamic response beyond that obtained based upon knowledge of the administered dose.

Rezulin has only been shown to exert its antihyperglycemic effect in the presence of insulin. Because Rezulin does not stimulate insulin secretion, hypoglycemia in patients treated with Rezulin alone is not to be expected. Because of this insulin-dependent mechanism of action, Rezulin should not be used in patients with type l diabetes.

Clinical Studies

Combination With Sulfonylureas: A Q-week, double-blind, placebo-controlled study of Rezulin and 12 mg micronized glyburide, alone and in combination, was conducted in patients with type II diabetes (N= 552), who had failed to achieve adequate glycemic control (FSG of 224 mg/dL and HbA1C of 9.6%) while on maximal doses of a sulfonylurea. Patients randomized to receive micronized glyburide showed mean increases in FSG and HbA1C. Similarly, patients who switched from a sulfonylurea to Rezulin monotherapy also demons rated increases in FSG and HbA1C.

TABLE 2.

Combination Therapy With Glyburide: Mean Difference

From 12 mg Micronized Glyburide Monotherapy (1 yr)
 

200 mg Rezulin + Glyburide

400 mg Rezulin + Glyburide

600 mg Rezulin + Glyburide
FSG (mg/dL)
Mean Baseline
Brand Name: Rezulin
Generic Name: Troglitazone (removed from the US market 3/21/00)
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