Pioglitazone: Uses, Dosage, Side Effects, and More
1. Drug Name
Generic Name: Pioglitazone
Brand Name(s):
- Pakistan: Actos, Piozone
- India: Pioz, Glizone
- United States: Actos
- United Kingdom: Actos
2. Pharmacological Class
Class: Antidiabetic agent
Subclass: Thiazolidinedione
3. Mechanism of Action
Pioglitazone works by increasing the sensitivity of liver, fat, and muscle cells to insulin, allowing more glucose to enter cells in response to insulin. It binds to peroxisome proliferator-activated receptor-gamma (PPAR-γ) on the nuclear membrane, influencing the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization.
4. Indications
Primary Indications:
- Type 2 diabetes mellitus
Off-label Uses:
- Polycystic ovary syndrome (PCOS)
5. Dosage and Administration
Standard Dosage:
- Initial dose: 15-30 mg once daily.
- Maintenance dose: 15-45 mg once daily.
- Maximum dose: 45 mg once daily.
Route of Administration: Oral
Special Populations:
- Pediatric: Not recommended.
- Geriatric: Dose adjustments may be necessary due to increased risk of heart failure.
6. Pharmacokinetics
Absorption: Well absorbed from the gastrointestinal tract.
Distribution: Widely distributed, with 99% bound to plasma proteins.
Metabolism: Metabolized in the liver via hydroxylation and oxidation.
Excretion: Excreted primarily in the urine and feces.
Half-life: Approximately 3-7 hours.
7. Contraindications
Pioglitazone is contraindicated in patients with:
- Hypersensitivity to pioglitazone or any of its components.
- Heart failure (NYHA Class III or IV).
- Active bladder cancer.
8. Warnings and Precautions
Use caution in patients with:
- Hepatic impairment.
- Heart failure or risk of heart failure.
- Bladder cancer history.
Monitor liver enzymes before and during treatment. Watch for signs of heart failure, especially in at-risk patients.
9. Side Effects
Common Side Effects:
- Weight gain
- Edema
- Headache
- Muscle pain
Serious Side Effects:
- Heart failure
- Bladder cancer
- Fractures
- Liver failure
10. Drug Interactions
Major Interactions:
- Gemfibrozil (increases pioglitazone levels)
- Rifampin (decreases pioglitazone levels)
Moderate Interactions:
- Oral contraceptives (may reduce their efficacy)
Minor Interactions:
- Ketoconazole (may increase pioglitazone levels)
11. Pregnancy and Lactation
Pregnancy Category: C
Breastfeeding Considerations: Not recommended during breastfeeding due to the potential risk to the infant.
12. Patient Counseling Information
Key Points for Patients:
- Take pioglitazone exactly as prescribed.
- Monitor blood glucose levels regularly and keep track of results.
- Report any unusual symptoms such as rapid weight gain, shortness of breath, or blood in urine.
- Follow dietary and exercise recommendations provided by your healthcare provider.
Administration Tips:
- Take pioglitazone once daily, with or without food.
- Do not skip doses or change the dose without consulting your doctor.
- Store pioglitazone at room temperature away from moisture and heat.