Thiazolidinediones – Pioglitazone MCQs With Answer
Thiazolidinediones (TZDs) such as pioglitazone are important oral antidiabetic agents used in Type 2 diabetes mellitus. This introduction covers pioglitazone’s mechanism as a PPARγ agonist, insulin-sensitizing effects, pharmacokinetics (CYP2C8 metabolism, active metabolites), therapeutic uses, dosing (15–45 mg), key adverse effects (fluid retention, heart failure risk, weight gain, fracture risk, bladder cancer concerns), drug interactions, monitoring (LFTs, signs of edema) and prescribing considerations. Designed for B.Pharm students, these concise points emphasize pharmacology, safety, and clinical application. Now let’s test your knowledge with 30 MCQs on this topic.
Q1. Which best describes the primary mechanism of action of pioglitazone?
- Stimulates pancreatic beta-cell insulin secretion
- Inhibits hepatic glucose absorption
- Activates PPARγ nuclear receptors to increase insulin sensitivity
- Blocks intestinal carbohydrate absorption
Correct Answer: Activates PPARγ nuclear receptors to increase insulin sensitivity
Q2. Pioglitazone belongs to which drug class?
- Sulfonylureas
- Biguanides
- Thiazolidinediones
- GLP-1 receptor agonists
Correct Answer: Thiazolidinediones
Q3. The main therapeutic effect of pioglitazone in Type 2 diabetes is:
- Increasing insulin secretion from beta cells
- Enhancing peripheral insulin sensitivity in muscle and adipose tissue
- Rapid decrease of postprandial glucose only
- Inhibiting renal glucose reabsorption
Correct Answer: Enhancing peripheral insulin sensitivity in muscle and adipose tissue
Q4. Pioglitazone’s action on adipose tissue includes:
- Decreasing adipocyte differentiation
- Increasing adipogenesis and GLUT4 expression
- Directly blocking lipogenesis enzymes
- Inhibiting fatty acid uptake into adipocytes
Correct Answer: Increasing adipogenesis and GLUT4 expression
Q5. Which lipid effect is commonly associated with pioglitazone therapy?
- Decrease in HDL cholesterol
- Increase in triglycerides
- Increase in HDL and reduction in triglycerides
- Marked reduction in LDL cholesterol only
Correct Answer: Increase in HDL and reduction in triglycerides
Q6. The most clinically important adverse effect requiring caution with pioglitazone is:
- Hypokalemia
- Fluid retention and exacerbation of heart failure
- Acute pancreatitis
- Severe hyperthyroidism
Correct Answer: Fluid retention and exacerbation of heart failure
Q7. Long-term use of pioglitazone has been associated with increased risk of:
- Osteoporosis-related fractures
- Acute kidney injury
- Parkinson’s disease
- Myasthenia gravis
Correct Answer: Osteoporosis-related fractures
Q8. Which safety concern has been specifically investigated with pioglitazone?
- Bladder cancer signal with long-term use
- Increased risk of myocardial infarction in all patients
- High risk of severe hypoglycemia as monotherapy
- Permanent alopecia
Correct Answer: Bladder cancer signal with long-term use
Q9. Pioglitazone is primarily metabolized by which cytochrome P450 enzyme?
- CYP1A2
- CYP2C8 (with contribution from CYP3A4)
- CYP2D6 exclusively
- CYP2E1 mainly
Correct Answer: CYP2C8 (with contribution from CYP3A4)
Q10. Pioglitazone is contraindicated in patients with which condition?
- Stable ischemic heart disease
- New York Heart Association (NYHA) class III or IV heart failure
- Mild controlled hypertension
- Hyperlipidemia without heart failure
Correct Answer: New York Heart Association (NYHA) class III or IV heart failure
Q11. Risk of hypoglycemia with pioglitazone monotherapy is:
- Very high
- Moderate and common
- Low unless combined with insulin or secretagogues
- Zero, it cannot cause hypoglycemia
Correct Answer: Low unless combined with insulin or secretagogues
Q12. Treatment with pioglitazone commonly causes which metabolic change?
- Weight loss
- Weight gain due to fluid retention and adiposity
- Rapid muscle wasting
- Severe hypovolemia
Correct Answer: Weight gain due to fluid retention and adiposity
Q13. Clinical onset of glycemic effect with pioglitazone is typically:
- Immediate within hours
- Within 1–2 days
- Over several weeks to months
- Only after one year of therapy
Correct Answer: Over several weeks to months
Q14. Dose adjustment of pioglitazone is usually required in renal impairment?
- Yes, reduce dose by 75%
- No, generally no adjustment needed for renal impairment
- Never use if creatinine is elevated
- Switch to IV formulation in renal disease
Correct Answer: No, generally no adjustment needed for renal impairment
Q15. Before starting pioglitazone which baseline test is recommended?
- Thyroid function tests only
- Liver function tests (LFTs)
- Routine brain MRI
- Serum amylase only
Correct Answer: Liver function tests (LFTs)
Q16. PPARγ receptors targeted by pioglitazone are located primarily where?
- Cell membrane of hepatocytes
- Nuclear receptors in adipose tissue, muscle and macrophages
- Mitochondrial matrix of pancreatic cells
- Extracellular matrix of muscle
Correct Answer: Nuclear receptors in adipose tissue, muscle and macrophages
Q17. Combining pioglitazone with insulin increases risk of:
- Hypothyroidism
- Edema and congestive heart failure
- Decreased efficacy of insulin
- Severe hyperkalemia
Correct Answer: Edema and congestive heart failure
Q18. Pioglitazone use in pregnancy is:
- Recommended as first-line therapy
- Generally not recommended; use alternatives
- Mandatory in gestational diabetes
- Safe without restrictions
Correct Answer: Generally not recommended; use alternatives
Q19. Which parameters should be monitored periodically during pioglitazone therapy?
- Complete blood count only
- Liver function tests, weight, and signs of fluid retention
- Serum uric acid only
- Ophthalmic pressure monthly
Correct Answer: Liver function tests, weight, and signs of fluid retention
Q20. Regarding metabolites of pioglitazone:
- Pioglitazone is excreted unchanged only
- It is metabolized to several active metabolites
- All metabolites are inactive and toxic
- There are no detectable metabolites
Correct Answer: It is metabolized to several active metabolites
Q21. Typical HbA1c reduction with pioglitazone monotherapy is approximately:
- 0% (no effect)
- 0.5–1.5%
- 3–4%
- Greater than 5%
Correct Answer: 0.5–1.5%
Q22. Pioglitazone is administered by which route?
- Intravenous infusion
- Oral tablets
- Subcutaneous injection
- Topical cream
Correct Answer: Oral tablets
Q23. The commonly prescribed maximum daily dose of pioglitazone is:
- 5 mg
- 15 mg
- 30 mg
- 45 mg
Correct Answer: 45 mg
Q24. Pioglitazone lowers blood glucose primarily by:
- Increasing insulin secretion from the pancreas
- Reducing alimentary carbohydrate absorption
- Enhancing insulin sensitivity, not increasing insulin secretion
- Direct renal glucose excretion
Correct Answer: Enhancing insulin sensitivity, not increasing insulin secretion
Q25. Coadministration of gemfibrozil (a CYP2C8 inhibitor) with pioglitazone will likely:
- Decrease pioglitazone plasma levels
- Increase pioglitazone plasma concentrations and effect
- Have no interaction
- Cause immediate detoxification of pioglitazone
Correct Answer: Increase pioglitazone plasma concentrations and effect
Q26. Pioglitazone is appropriate for which diabetes type?
- Type 1 diabetes mellitus as monotherapy
- Type 2 diabetes mellitus with insulin resistance
- Gestational diabetes as first choice
- All types without restriction
Correct Answer: Type 2 diabetes mellitus with insulin resistance
Q27. Activation of PPARγ by pioglitazone leads to:
- Immediate ion channel opening
- Altered gene transcription of insulin-responsive genes
- Direct enzymatic blockade of gluconeogenesis
- Destruction of pancreatic alpha cells
Correct Answer: Altered gene transcription of insulin-responsive genes
Q28. The elimination half-life of pioglitazone parent compound is approximately:
- 30 minutes
- 3–7 hours (active metabolites longer)
- 2–3 days
- Several weeks
Correct Answer: 3–7 hours (active metabolites longer)
Q29. Pioglitazone is commercially available in which pharmaceutical form?
- Injectable solution
- Oral tablets of various strengths
- Transdermal patch
- Inhalation powder
Correct Answer: Oral tablets of various strengths
Q30. Which clinical sign should prompt assessment for possible bladder cancer during pioglitazone therapy?
- Persistent cough
- Gross or microscopic hematuria (blood in urine)
- Night sweats
- Intermittent blurry vision
Correct Answer: Gross or microscopic hematuria (blood in urine)

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