Thiazolidinediones are a class of oral hypoglycemic agents. They are also known as glitazones. They are widely used in the treatment of diabetes mellitus. It binds to a group of molecules in the cell nucleus and activates certain genes. This leads to a decrease in insulin resistance, a decrease in leptin levels leading to an increased appetite, decreases levels of triglycerides, low density lipoproteins and an increase in high density lipoprotein which is good cholesterol. Some glitazones are known to increase the risk of heart attacks and stroke.
Various types of Thiazolidinediones:
Pioglitazone: This drug is not used in France and Germany any more as it is known to increase the risk of developing bladder cancer.
Rosiglitazone: This drug has been banned in the US market and withdrawn from the European markets as there has been an increased risk in the development of cardiovascular events and strokes following use of this drug.
Troglitazone: This drug has been associated with an increased incidence of drug induced hepatitis, hence has been withdrawn from the market.
Uses of Thiazolidinediones: It is used for the treatment of diabetes mellitus type 2. Its use in cases of polycystic ovarian disease, psoriasis, autism, ovarian hyper stimulation syndrome and nonalcoholic steatohepatitis (NASH) is under experimentation. Administration of rosiglitazone and pioglitazone has been shown to have a protective effect on the progression of microvascular and macrovascular complications of diabetes mellitus.
Side effects of Thiazolidinediones: The main side effects of troglitazone are that it causes drug induced hepatitis and can cause liver failure in approximately 1 in 20,000 individuals. Thus all patients on Troglitazone are recommended to check their liver function tests every two to three months. If there is any significant change in the liver enzymes the drug must be discontinued at once. The newer Thiazolidinediones, like rosiglitazone and pioglitazone have been free of this problem.
The main side effects of all Thiazolidinediones are water retention, leading to swelling all over the body. This side effect may be seen in less than 5 % of the individuals taking this drug. Excess fluid retention can cause severe overload on the heart and in turn lead to heart failure. Hence this drug must be used with caution in patients. Before administration of this drug, a complete health check up must be performed and the cardiac function must be checked in all patients. Once the patient is given the drug, the patient must be checked for weight gain, water retention and decreased ventricular function. Patients taking rosiglitazone and pioglitazone have an increased risk of developing coronary heart disease and heart attacks. Those patients who are diabetic and already suffering from ischemic heart disease are best, not given pioglitazone or rosiglitazone for the treatment of their diabetes. Epidemiological studies have shown that some patients taking pioglitazone developed bladder cancer. A correlation of pioglitazone and bladder cancer has been established; hence it is advisable to use this drug with great caution, especially in those patients who have a history of cancer.
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