Pioglitazone Mechanism of Action

Diabetes mellitus (DM) is curbing the normal lifestyle and is one of the leading cause of mortality around the world. Along with many other comorbidities, it also brings a huge healthcare burden on society.

During the last three decades, due to the sedentary lifestyle and increasing obesity, the prevalence of DM has faced a tremendous increment. The major factor responsible for such an enormous increase is the ignorance towards a healthy and active lifestyle.

DM is classified broadly into:

Insulin-dependent DM (Type 1): Insulin therapy is necessary

Non-insulin Dependent DM (Type 2): Oral anti-diabetic drugs are mostly sufficient with lifestyle modifications

Here we’ll talk about Type 2 DM!

Type 2 DM (T2DM) is a chronic condition and needs life long medical treatment, which brings the enormous cost of treatment. Along with the medications, T2DM management includes necessary lifestyle modifications like quitting smoking and alcohol, including regular exercise and a balanced diet.

T2DM is the mother of many other diseases. Too much glucose (sugar) in the blood can lead to several health complications like eye problems (loss of vision), kidney damage, nerve damage, foot, and dental complications. It increases the risk of cardiovascular diseases like myocardial infarction, stroke and other heart diseases.

In the following part, we will discuss three-decade-old potent medicine, which is still one of the first line choices for the management of T2DM.

Pioglitazone is an anti-diabetic drug which decreases insulin resistance and improves glycemic control. It is also the drug with some unique benefits, one of them is that there is no risk of kidney damage and nerve problems. Moreover, it is not associated with the risk of hypoglycemia (low blood sugar levels).

Let’s understand how Pioglitazone is useful in controlling diabetes.

Pioglitazone belongs to thiazolidinedione (Glitazones) class. It is used along with proper diet and exercise to control the blood glucose level.

It improves insulin sensitivity leading to better glycaemic control and dyslipidemia. It leads to the utilization of glucose in peripheral organs and decreases gluconeogenesis (production of sugar inside the body) in the liver; thereby, it reduces insulin resistance.

How does it work?

• Pioglitazone works by increasing the body’s sensitivity to the insulin produced by the body and reduces insulin resistance. It facilitates the glucose intake to the cells.
• Pioglitazone is an activator for peroxisome proliferator-activated receptors (PPARs), the receptors which are responsible for the carbohydrate
• (sugar) and lipid (fat) metabolism.
• The interaction between Pioglitazone and these receptors result in the decrease in glucose levels, free fatty acids and reduces tumor necrosis factor alpha, which is a chemical mediator of inflammation.

Advantages of Pioglitazone

• Pioglitazone (thiazolidinedione derivative) which controls high blood sugar levels in patients with type 2 diabetes.
• There is no risk of kidney damage and nerve problems.
• There is no risk of hypoglycemia when used alone.
• It also decreases the risk of heart attack and stroke.
• Pioglitazone increases the HDL level (High-density lipoprotein), which is good cholesterol and decreases fasting triglycerides as well as free fatty acids.
• Coadministration with an insulin secretagogue (help your pancreas to make and secrete insulin) like sulfonylurea decreases the dose of insulin secretagogue by 10-25%.

Dosage of Pioglitazone

• Pioglitazone is a prescription drug which is used either alone or in combination with other anti-diabetic medications like metformin or glyburide.
• These are available in the form of tablets with a convenient once in a day dosing schedule.
• The dose for Pioglitazone is 15-30 mg with a meal daily. With careful monitoring, the dose is increased by up to 45 mg.
• Coadministration with gemfibrozil (potent CYP2C8 inhibitors) reduces the dose of Pioglitazone to 15 mg daily.

Side effects of Pioglitazone:

The side effects of Pioglitazone includes mild muscle, abdominal, back pain, sore throat, headache and loss of appetite.

Precautions:

• Never take Pioglitazone without physician consultation.
• In case of any severe unusual effects consult the doctor immediately. Also, if the signs and symptoms of heart failure are observed, one should inform their doctor without wasting any time.
• Always take your medicine on time or as prescribed by the physician.
• It is contraindicated if the patient is suffering from diabetic ketoacidosis, moderate to severe hepatic impairment, chronic heart disease and bladder cancer.

We hope now you all are aware of the beneficial effects of Pioglitazone. It is a drug which is needed daily for a better life of diabetic patients.

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