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Home / Thiazolidinediones - Doses, Usage, and Side Effects

Thiazolidinediones - Doses, Usage, and Side Effects

Thiazolidinediones are used to treat type 2 diabetes. They are a kind of oral hypoglycemic medication (lowers blood sugar levels). Thiazolidinediones (TZDs) help to lower blood sugar by improving the sensitivity of the muscle, fat, and liver to insulin.

The FDA (Food and Drug Administration) has currently approved the use of two thiazolidinediones, rosiglitazone and pioglitazone, either alone or in combination with metformin or sulfonylureas, to treat type 2 diabetes mellitus.

Additionally, thiazolidinediones may be used to treat polycystic ovarian syndrome by improving endothelial function, improving ovulation, and reducing insulin resistance. In individuals with nonalcoholic steatohepatitis (NASH), pioglitazone specifically lowers hepatic fat and may improve liver fibrosis; however, other factors and dangers need to be assessed in NASH patients. As monotherapy, TZDs do not cause hypoglycemia and are not contraindicated in patients with renal disease.

Don't stop taking the medication if you don't see a change in your blood sugar level straight away because it can take TZDs several weeks to start functioning.

Type 2 diabetes can be managed by lifestyle changes and medications. Thiazolidinediones is one of them, used in type 2 diabetes. At Specialty Care Clinics we will assist you with proper medication and guidelines that will help you manage diabetes.

Mechanism of Action of Thiazolidinediones

Thiazolidinediones (TZDs) is insulin sensitizers that improve insulin action and raise insulin sensitivity in vital tissues by acting on intracellular metabolic pathways.

In addition to increasing adiponectin levels, TZDs decrease hepatic gluconeogenesis and increase insulin-dependent glucose uptake in muscles and fat. Adiponectin, a cytokine released by fat tissue, raises insulin sensitivity, while TZD therapy raises fatty acid oxidation.


How Thiazolidinediones should be taken?

With or without food, thiazolidinediones (TZDs) are given orally once daily. Liver function tests and HbA1C levels should be monitored before starting therapy and occasionally while going through it. Due to a delayed onset of action via modification of gene expression, the maximum glucose-lowering benefits of TZDs are not observed for six weeks to six months. TZDs can be used in combination with biguanides, sulfonylureas, and insulin injectables to manage type 2 diabetes. They should also be taken in conjunction with lifestyle changes such as diet, exercise, and weight reduction..

  •    Pioglitazone is taken once daily with doses of 15, 30, or 45mg
  •    In general, rosiglitazone is taken once or twice daily, starting at 2-4 mg once or twice daily and up to a daily maximum of 8 mg.

Rosiglitazone, one of the thiazolidinediones, has been linked to an increased risk of heart disease. The American Food and Drug Administration has restricted the use of this prescription to those who are already taking it, those who have tried other treatments but failed, and those who refuse to take pioglitazone.

Avoid taking thiazolidinediones, if you have congestive heart failure or liver or kidney problems.

What are the side effects of thiazolidinediones?

There have been variable side effects between the particular medications within the class since TZDs target an essential receptor that activates a wide range of different genes. Common side effects of thiazolidinediones include:

  •    Fluid retention
  •    Weight gain
  •    Eyesight problems
  •    Anemia
  •    Congestive heart failure
  •    Increase risk of heart disease
  •    Bone fractures in women
  •    Allergic skin reactions
  •    Liver failure

What should be monitored during medication?

The patient should have their liver function tests checked both before and regularly throughout TZD medication. Don’t start or should be stopped TZD medication if the liver function test is greater or equal to three times the upper limit. Additionally, hepatic injury symptoms such as jaundice or dark urine should also be monitored.

Clinicians must keep track of the patient’s body weight to identify any signs of fluid overload. Close observation is required in cases where there are indications of fluid overload or heart failures such as fast weight gain, peripheral edema, dyspnea, S3 heart sounds, or a decreased ejection fraction. The HbA1c should be checked at least twice a year for glycemic control and dosage adjustments.

Thiazolidinediones should not be used in the following situations:

  •    Heart Failure (New York Heart Association class III, IV): Due to the danger of fluid retention and diastolic cardiac malfunction, the American Heart Association and the American Diabetes Association have recommended that patients with New York Heart Association classes III and IV symptomatic heart failure use TZD at the lowest effective dose or not at all.
  •    Hepatic impairment: Due to hepatotoxicity, troglitazone was taken off the market. Rosiglitazone or pioglitazone doesn’t show the same effect, it is still advised that patients have a baseline and periodic liver function testing.
  •    Bladder cancer: Patients who have bladder cancer should avoid taking TZD medication. Before beginning pioglitazone therapy in individuals with a history of bladder cancer, it is important to weigh the benefits of glycemic control against the risk of recurrence.
  •    Pregnancy: Patients should switch to another insulin sensitizer, such as metformin if they are pregnant.
  •    Risk of fractures: People who are at high risk of fracture should avoid taking TZD medication.

Thiazolidinediones is used in the treatment of type 2 diabetes, which is manageable as compared to type 1 diabetes. There are various ways that are helpful along with medication under the supervision of a specialist. Connect Specialty Care Clinics at 469-545-9983 if you have diabetes.