Troglitazone

Troglitazone (brand name: Rezulin) was the inaugural thiazolidinedione introduced for treatment in the United States for managing type 2 diabetes. It was greenlit by the FDA in 1997. However, due to subsequent concerns and findings regarding its potential to cause liver injury and the incidences of acute liver failure, the drug was officially withdrawn from the market in 2000.

Mechanism of Action[edit | edit source]

Troglitazone functions as an insulin-sensitizing agent. Its primary mechanism revolves around the activation of PPAR-γ (Peroxisome proliferator-activated receptor gamma) receptors. Activation of these receptors triggers the expression of numerous genes that play pivotal roles in the metabolic processes of glucose and fatty acids. Clinical trials conducted on the drug demonstrated its efficacy in reducing both blood glucose and HbA1c levels. Moreover, when combined with antidiabetic agents like sulfonylureas and metformin, troglitazone was shown to have synergistic effects.

FDA Approval and Withdrawal[edit | edit source]

After its FDA approval in 1997, Troglitazone emerged as a promising agent in the arsenal against type 2 diabetes. It could be administered as a standalone treatment or paired with other antidiabetic medications to bolster its effects. Nevertheless, its promise was short-lived. Only a few years after its widespread commercial release, there was a surge in reports indicating severe liver injuries associated with Troglitazone usage, including some fatal instances of acute liver failure. The alarming rate and severity of these reports hastened the drug's withdrawal in 2000.

Dosage and Administration[edit | edit source]

Troglitazone was commercialized in the form of 400 mg tablets. The prescribed dosage for patients typically ranged from 400 to 800 mg, taken once daily. It could be prescribed as a sole therapeutic agent or in conjunction with other medications such as metformin, sulfonylureas, or insulin, based on the individual's glycemic control requirements.

See also[edit | edit source]

Thiazolidinedione Type 2 diabetes FDA Metformin Sulfonylureas Liver failure PPAR-γ receptors Antidiabetics

Alpha-Glucosidase Inhibitors
- Acarbose
- Miglitol
Incretin-Based Drugs
- Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
- Glucagon-Like Peptide-1 (GLP-1) Analogues
Insulin
Metformin
Metiglinide Analogues
- Nateglinide
- Repaglinide
Pramlintide
Sodium Glucose Cotransporter-2 (SGLT-2) Inhibitors
Sulfonylureas
- First Generation Sulfonylureas
  - Acetohexamide
  - Chlorpropamide
  - Tolazamide
  - Tolbutamide
- Second Generation Sulfonylureas
  - Gliclazide
  - Glimepiride
  - Glipizide
  - Glyburide (Glibenclamide)
Thiazolidinediones

Troglitazone Resources
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