Thiazolidinediones – Pioglitazone MCQs With Answer

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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