Pioglitazone

Pioglitazone (中文：吡格列酮)

Pronunciation

Pioglitazone 30mg

Common Strengths of Pioglitazone

Pioglitazone is available in three strengths:

• 15 mg
• 30 mg
• 45 mg

Drug Trade Names of Pioglitazone

Actos is the trade name for pioglitazone. It is also sold under various brand names when combined with other medications, such as:

• Actoplus Met (pioglitazone and metformin)
• Duetact (pioglitazone and glimepiride)
• Oseni (pioglitazone and alogliptin)

Mechanism of Action

Pioglitazone is a thiazolidinedione that works by enhancing insulin sensitivity. It activates peroxisome proliferator-activated receptor-gamma (PPARγ) in fat, muscle, and liver tissues, which helps control the production of hormones and enzymes that improve insulin sensitivity, lower blood sugar, reduce glucose production in the liver, and maintain the function of pancreatic β-cells.

Route of Administration

Pioglitazone is administered orally in tablet form.

Dosages

• Normal People (without congestive heart failure)
  • Initial dose is 15 mg or 30 mg once daily. The dose can be increased up to 45 mg once daily based on glycemic response.
• Hypertension
  • No specific dosage adjustment for hypertension alone, but careful monitoring is required due to potential fluid retention.
• Heart Failure (NYHA Class I or II)
  • Initial dose is 15 mg once daily. Dose adjustments should be made cautiously with careful monitoring for signs of heart failure.
• Diabetic Kidney Disease
  • No specific dosage adjustment, but careful monitoring is required due to potential fluid retention and renal function.

Side Effects

Frequency	Adverse reactions
Very common (≥1/10)	Edema
	Weight gain
Common (≥1/100 to <1/10)	Upper respiratory tract infection
	Headache
	Sinusitis
	Myalgia
	Tooth disorder
	Pharyngitis
Uncommon (≥1/1,000 to <1/100)	Anemia
	Hypoglycemia (when used with other antidiabetic drugs)
	Increased appetite
Rare (≥1/10,000 to <1/1,000)	Liver dysfunction
	Macular edema
	Heart failure
Very Rare (<1/10,000)	Bladder cancer (long-term use)
	Severe allergic reactions

Pharmacokinetics

• Absorption
  • Well absorbed orally. Peak plasma concentrations of unchanged pioglitazone are usually achieved 2 hours after administration.
• Metabolism
  • Primarily metabolized in the liver via CYP2C8.
• Half-life
  • About 7 hours.
• Excretion
  • Mainly excreted in faeces; 15 - 30% excreted in urine.

Precautions for Use

Fluid retention and cardiac failure

Pioglitazone can cause fluid retention, which may exacerbate or precipitate heart failure. Not recommended for patients with cardiac failure (NYHA stages 1 to IV), active bladder cancer, or severe liver disease.

Pregnancy

Not recommended due to potential risks.

Breastfeeding

Not recommended.

Children and Elderly

Not recommended for children; elderly patients should be monitored closely due to increased risk of heart failure.

Renal Impairment

No specific dosage adjustment, but careful monitoring is required.

Monitoring Requirements

Regular monitoring of liver enzymes, blood glucose, and signs of heart failure is recommended.

Drug Interactions

Caution with CYP2C8 inhibitors (e.g., gemfibrozil), insulin, and other antidiabetic drugs due to increased risk of hypoglycemia.

FAQs

How should I take the tablet?

Take Pioglitazone exactly as prescribed by your doctor, usually once daily, with or without food.

What should I avoid while taking?

Avoid excessive alcohol consumption as it can increase the risk of hypoglycemia and liver damage. Avoid using Pioglitazone if you have severe heart failure or active bladder cancer.

What happens if I miss a dose?

Take the missed dose as soon as you remember, but skip it if it is almost time for your next dose. Do not take two doses at one time.

Reference

[1] https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021842s014s015lbl.pdf

[2] https://www.rxlist.com/actos-drug.htm

[3] https://www.drugs.com/availability/generic-actos.html

[4] https://www.drugs.com/actos.html

[5] https://en.wikipedia.org/wiki/Pioglitazone