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Rezulin

Clinical Pharmacology
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Discontinued Warning Icon Please Note: This drug is no longer available in the U.S.

CLINICAL PHARMACOLOGY

Rezulin

Mechanism of Action

Troglitazone is a thiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin. It has a unique mechanism of action that is dependent on the presence of insulin for activity. Troglitazone decreases hepatic glucose output and increases insulindependent glucose disposal in skeletal muscle. Its mechanism of action is thought to involve binding to nuclear receptors (PPAR) that regulate the transcription of a number of insulin responsive genes critical for the control of glucose and lipid metabolism. Unlike sulfonylureas, troglitazone is not an insulin secretagogue.

In animal models of diabetes, troglitazone reduces the hyperglycemia. hyperinsulinemia. and hypertriglyceridemia characteristic of insulin-resistant states such as type II diabetes. Plasma lactate and ketone body formation are also decreased. The metabolic changes produced by troglitazone result from the increased responsiveness of insulin-dependent tissues and are observed in numerous animal models of insulin resistance. Treatment with troglitazone did not affect pancreatic weight, islet number or glucagon content. but did increase regranulation of the pancreatic beta cells in rodent models of insulin resistance.

Since troglitazone enhances the effects of circulating insulin (by decreasing insulin resistance), it does not lower blood glucose in animal models that lack endogenous insulin.

Pharmacokinetics and Drug Metabolism

Maximum plasma concentration (Cmax) and the area under plasma concentration- time curve (AUC) of troglitazone increase proportionally with increasing doses over the dose range of 200 to 600 mg/day (Table 1). Following daily drug administration, steady-state plasma concentrations of troglitazone are reached within 3 to 5 days.

TABLE 1.

Mean(+1 SD) Steady-State Pharmacokinetics of

Troglitazone in 21 Normal Volunteers

Dose

(mg/day)

Cmax

mL

AUC (0-24)

(ug.hr/mL)

CL/F*

(mL/min)

200

0.90 (0.36)

7.4 (2.4)

500 (187)

400

1.61 (0.69)

13.4 (5.5)
Brand Name: Rezulin
Generic Name: Troglitazone (removed from the US market 3/21/00)

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