Antihypertensive agents – classification, SAR, mechanism, uses MCQs With Answer

Antihypertensive agents are drugs used to manage high blood pressure and reduce cardiovascular risk. This module covers classification, structure–activity relationships (SAR), mechanisms of action, therapeutic uses, adverse effects, and key drug interactions—essential for B. Pharm students. You will study major classes: diuretics, beta‑blockers, ACE inhibitors, ARBs, calcium channel blockers, and vasodilators, plus prototypes like enalapril, losartan, propranolol, amlodipine, and furosemide. Important SAR concepts include the aryloxypropanolamine template of beta‑blockers, dihydropyridine core of vascular CCBs, and the carboxylate/tetrazole motifs in ACE inhibitors and ARBs. Emphasis is on mechanism-based selection, monitoring, and contraindications. Now let’s test your knowledge with 30 MCQs on this topic.

Q1. Which class of antihypertensive agents primarily acts by inhibiting the angiotensin‑converting enzyme (ACE)?

  • Beta‑blockers
  • ACE inhibitors
  • Calcium channel blockers
  • Loop diuretics

Correct Answer: ACE inhibitors

Q2. Which structural feature is characteristic of dihydropyridine (DHP) calcium channel blockers?

  • Aryloxypropanolamine side chain
  • Biphenyl‑tetrazole moiety
  • Dihydropyridine ring
  • Sulfhydryl group

Correct Answer: Dihydropyridine ring

Q3. Which antihypertensive drug is most commonly associated with a persistent dry cough as a side effect?

  • Losartan
  • Lisinopril
  • Amlodipine
  • Furosemide

Correct Answer: Lisinopril

Q4. The SAR of classical beta‑blockers is centered on which pharmacophore?

  • Diaryl ether core
  • Aryloxypropanolamine
  • Dihydropyridine nucleus
  • Carboxylate ester

Correct Answer: Aryloxypropanolamine

Q5. Which diuretic class acts by inhibiting the Na+/Cl− symporter in the distal convoluted tubule?

  • Loop diuretics
  • Thiazide diuretics
  • Carbonic anhydrase inhibitors
  • Potassium‑sparing diuretics

Correct Answer: Thiazide diuretics

Q6. Losartan belongs to which antihypertensive class and what is the key SAR motif in many ARBs?

  • ACE inhibitors; sulfhydryl group
  • Calcium channel blockers; dihydropyridine ring
  • Angiotensin II receptor blockers; biphenyl‑tetrazole
  • Beta‑blockers; aryloxypropanolamine

Correct Answer: Angiotensin II receptor blockers; biphenyl‑tetrazole

Q7. Which mechanism best describes how loop diuretics like furosemide lower blood pressure?

  • Block L‑type calcium channels in vascular smooth muscle
  • Inhibit NKCC2 in the thick ascending limb to increase natriuresis
  • Antagonize aldosterone receptors in collecting tubule
  • Inhibit ACE, reducing angiotensin II formation

Correct Answer: Inhibit NKCC2 in the thick ascending limb to increase natriuresis

Q8. Which antihypertensive is a prodrug that is converted to an active carboxylate form in vivo?

  • Captopril
  • Enalapril
  • Losartan
  • Propranolol

Correct Answer: Enalapril

Q9. Which calcium channel blocker class is more selective for vascular smooth muscle than for cardiac tissue?

  • Non‑dihydropyridines (verapamil, diltiazem)
  • Dihydropyridines (nifedipine, amlodipine)
  • Benzothiazepines
  • Phenylalkylamines

Correct Answer: Dihydropyridines (nifedipine, amlodipine)

Q10. Which antihypertensive causes hyperkalemia by antagonizing aldosterone receptors?

  • Spironolactone
  • Hydrochlorothiazide
  • Propranolol
  • Nifedipine

Correct Answer: Spironolactone

Q11. In the SAR of ACE inhibitors, which functional group enhances binding to the zinc ion in the ACE active site?

  • Carboxylate or sulfhydryl group
  • Tetrazole ring
  • Dihydropyridine ring
  • Aryloxy group

Correct Answer: Carboxylate or sulfhydryl group

Q12. Which antihypertensive drug should be avoided in asthma due to bronchoconstrictive risk?

  • Propranolol
  • Atenolol
  • Amlodipine
  • Enalapril

Correct Answer: Propranolol

Q13. Which drug class reduces peripheral resistance mainly by blocking alpha‑1 adrenergic receptors on vascular smooth muscle?

  • Alpha‑1 blockers (e.g., prazosin)
  • ACE inhibitors
  • Beta‑blockers
  • Thiazide diuretics

Correct Answer: Alpha‑1 blockers (e.g., prazosin)

Q14. Which experimental SAR observation is true for beta‑adrenergic blockers regarding stereochemistry?

  • R enantiomers are generally more potent than S for beta antagonism
  • S enantiomers are usually more potent as beta antagonists
  • Stereochemistry has no effect on beta‑blocker activity
  • Only racemic mixtures are active

Correct Answer: S enantiomers are usually more potent as beta antagonists

Q15. Which antihypertensive class can cause gingival hyperplasia and constipation as notable adverse effects?

  • ACE inhibitors
  • Calcium channel blockers
  • Beta‑blockers
  • Loop diuretics

Correct Answer: Calcium channel blockers

Q16. Which mechanism explains how ARBs lower blood pressure?

  • They inhibit renin release directly from the kidney
  • They block AT1 receptors, preventing angiotensin II actions
  • They inhibit ACE to reduce angiotensin II synthesis
  • They increase urinary sodium by blocking Na+/K+ ATPase

Correct Answer: They block AT1 receptors, preventing angiotensin II actions

Q17. Which antihypertensive drug contains a sulfhydryl moiety and may cause taste disturbances and rash?

  • Captopril
  • Enalapril
  • Losartan
  • Metoprolol

Correct Answer: Captopril

Q18. Which diuretic is most potent for acute pulmonary edema due to rapid and strong natriuretic effect?

  • Hydrochlorothiazide
  • Furosemide
  • Spironolactone
  • Acetazolamide

Correct Answer: Furosemide

Q19. Which pharmacological effect primarily accounts for the antihypertensive action of beta‑1 selective blockers like metoprolol?

  • Direct vasodilation via nitric oxide release
  • Reduction of heart rate and cardiac output via β1 blockade
  • Increased renal sodium excretion via aldosterone antagonism
  • Blockade of L‑type calcium channels

Correct Answer: Reduction of heart rate and cardiac output via β1 blockade

Q20. In structure–activity relationships of ARBs, replacing a carboxyl group with a tetrazole often results in:

  • Reduced receptor affinity and potency
  • Increased lipophilicity and oral bioavailability
  • Conversion to ACE inhibitor activity
  • Marked increase in diuretic effect

Correct Answer: Increased lipophilicity and oral bioavailability

Q21. Which antihypertensive is known for causing reflex tachycardia because of potent arteriolar dilation?

  • Hydralazine
  • Propranolol
  • Enalapril
  • Hydrochlorothiazide

Correct Answer: Hydralazine

Q22. Which combination is most likely to cause symptomatic hypotension if started simultaneously in a patient with volume depletion?

  • ACE inhibitor plus thiazide diuretic
  • Beta‑blocker plus calcium channel blocker
  • ARBs plus potassium supplement
  • Loop diuretic plus NSAID

Correct Answer: ACE inhibitor plus thiazide diuretic

Q23. Which antihypertensive class often requires monitoring of serum potassium due to risk of hyperkalemia?

  • ACE inhibitors and ARBs
  • Thiazide diuretics
  • Loop diuretics
  • Calcium channel blockers

Correct Answer: ACE inhibitors and ARBs

Q24. A key therapeutic use of beta‑blockers in hypertension beyond blood pressure reduction is:

  • Prevention of migraine and control of ischemic heart disease
  • Treatment of acute pulmonary edema
  • Management of hyperkalemia
  • Direct diuresis promotion

Correct Answer: Prevention of migraine and control of ischemic heart disease

Q25. Which antihypertensive agent’s SAR shows that bulky lipophilic substituents on the aromatic ring increase vascular selectivity in DHP CCBs?

  • Verapamil
  • Nifedipine
  • Enalapril
  • Propranolol

Correct Answer: Nifedipine

Q26. Which antihypertensive class directly antagonizes mineralocorticoid receptors to reduce sodium retention?

  • ACE inhibitors
  • Mineralocorticoid receptor antagonists (e.g., spironolactone)
  • Thiazide diuretics
  • Calcium channel blockers

Correct Answer: Mineralocorticoid receptor antagonists (e.g., spironolactone)

Q27. Which adverse effect is most classically associated with thiazide diuretics?

  • Hypokalemia and hyperglycemia
  • Hyperkalemia and hyponatremia
  • Bronchospasm
  • Cough and angioedema

Correct Answer: Hypokalemia and hyperglycemia

Q28. Which antihypertensive drug works intracellularly as a potassium channel opener producing arteriolar vasodilation?

  • Minoxidil
  • Enalapril
  • Verapamil
  • Hydrochlorothiazide

Correct Answer: Minoxidil

Q29. Which drug interaction is important to consider when combining ACE inhibitors with NSAIDs?

  • NSAIDs enhance ACE inhibitor efficacy, causing hypotension
  • NSAIDs can reduce antihypertensive effect and increase risk of renal impairment
  • ACE inhibitors prevent NSAID‑induced gastric ulcers
  • No clinically relevant interaction exists

Correct Answer: NSAIDs can reduce antihypertensive effect and increase risk of renal impairment

Q30. For a B. Pharm student, which principle is most important when choosing antihypertensive therapy for a diabetic patient?

  • Avoid ACE inhibitors because they worsen renal function in all diabetics
  • Prefer ACE inhibitors or ARBs for renal protection unless contraindicated
  • Choose only beta‑blockers to control blood sugar
  • Diuretics are always the first choice regardless of comorbidities

Correct Answer: Prefer ACE inhibitors or ARBs for renal protection unless contraindicated

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