Direct acting parasympathomimetics – Acetylcholine MCQs With Answer
Direct acting parasympathomimetics, especially acetylcholine and its analogs, are central to cholinergic pharmacology taught in B. Pharm courses. This introduction covers mechanisms, receptor selectivity (muscarinic vs nicotinic), receptor subtypes (M1–M5, Nn, Nm), structure–activity relationships, pharmacokinetics, clinical uses (glaucoma, urinary retention, xerostomia), and common adverse effects. Key drugs include acetylcholine, bethanechol, carbachol, methacholine, pilocarpine and nicotine. Understanding these agents helps you predict physiological responses, contraindications (asthma, peptic ulcer), and therapeutic rationale. The following set of focused, exam-style Acetylcholine MCQs is tailored for B. Pharm students to deepen learning and improve exam readiness. Now let’s test your knowledge with 50 MCQs on this topic.
Q1. Which best describes the primary action of acetylcholine when administered as a direct agonist?
- Blocks acetylcholinesterase
- Activates both muscarinic and nicotinic receptors
- Only activates muscarinic receptors
- Only activates nicotinic receptors
Correct Answer: Activates both muscarinic and nicotinic receptors
Q2. Which direct-acting parasympathomimetic is most commonly used topically to treat glaucoma?
- Bethanechol
- Pilocarpine
- Neostigmine
- Atropine
Correct Answer: Pilocarpine
Q3. Which cholinergic agonist is resistant to hydrolysis by acetylcholinesterase?
- Methacholine
- Acetylcholine
- Carbachol
- Pilocarpine
Correct Answer: Carbachol
Q4. Which direct-acting muscarinic agonist is used to stimulate bladder contraction in urinary retention?
- Bethanechol
- Pilocarpine
- Carbachol
- Nicotine
Correct Answer: Bethanechol
Q5. Which property explains why bethanechol has limited central nervous system effects?
- It is a lipophilic tertiary amine
- It is a quaternary ammonium poorly penetrating the BBB
- It is extensively metabolized by liver P450 enzymes
- It is rapidly deactivated by monoamine oxidase
Correct Answer: It is a quaternary ammonium poorly penetrating the BBB
Q6. Bronchoconstriction produced by muscarinic agonists is primarily mediated by which receptor subtype?
- M1
- M2
- M3
- M4
Correct Answer: M3
Q7. Which muscarinic receptor subtype predominates at the sinoatrial node and slows heart rate?
- M1
- M2
- M3
- M5
Correct Answer: M2
Q8. One recognized therapeutic use of acetylcholine in surgery is:
- Systemic treatment of asthma
- To induce muscle paralysis
- To produce rapid miosis during cataract surgery
- Long-term control of hypertension
Correct Answer: To produce rapid miosis during cataract surgery
Q9. Which direct-acting cholinergic agonist is approved to treat xerostomia (dry mouth) in Sjögren’s syndrome?
- Carbachol
- Methacholine
- Pilocarpine
- Bethanechol
Correct Answer: Pilocarpine
Q10. Which of the following is a common adverse effect of muscarinic agonists that limits their use in asthma patients?
- Hypertension
- Mydriasis
- Bronchospasm
- Dry mouth
Correct Answer: Bronchospasm
Q11. Which muscarinic receptor subtype is primarily responsible for stimulating exocrine gland secretions?
- M1
- M2
- M3
- M4
Correct Answer: M3
Q12. Which statement best describes bethanechol’s pharmacologic action?
- It is a muscarinic antagonist used for peptic ulcers
- It is a selective muscarinic agonist acting on urinary bladder smooth muscle
- It is a nicotinic agonist used for smoking cessation
- It inhibits acetylcholinesterase at synapses
Correct Answer: It is a selective muscarinic agonist acting on urinary bladder smooth muscle
Q13. Which cholinergic agonist is commonly used in a bronchial challenge test to diagnose airway hyperresponsiveness?
- Carbachol
- Methacholine
- Pilocarpine
- Bethanechol
Correct Answer: Methacholine
Q14. Which direct-acting agent primarily stimulates autonomic ganglia and adrenal medulla?
- Pilocarpine
- Nicotine
- Bethanechol
- Atropine
Correct Answer: Nicotine
Q15. Which structural feature is essential for classical acetylcholine-like muscarinic agonist activity?
- An aromatic ring and a tertiary alcohol
- A positively charged nitrogen and an ester separated by two carbon atoms
- A sulfhydryl group and a long alkyl chain
- A bulky lipophilic side chain and halogen atom
Correct Answer: A positively charged nitrogen and an ester separated by two carbon atoms
Q16. Which drug is most appropriate for treating postoperative urinary retention by stimulating detrusor contraction?
- Bethanechol
- Neostigmine
- Pilocarpine
- Atropine
Correct Answer: Bethanechol
Q17. Why is methacholine used diagnostically in pulmonary function testing?
- It causes bronchodilation in asthmatics
- It is a muscarinic antagonist that blocks airway receptors
- It is a muscarinic agonist causing bronchoconstriction to test hyperresponsiveness
- It acts as an acetylcholinesterase inhibitor
Correct Answer: It is a muscarinic agonist causing bronchoconstriction to test hyperresponsiveness
Q18. Which direct agonist is both muscarinic and nicotinic in action and resists breakdown by acetylcholinesterase?
- Pilocarpine
- Carbachol
- Methacholine
- Bethanechol
Correct Answer: Carbachol
Q19. Which clinical condition is a contraindication to systemic administration of muscarinic agonists?
- Peptic ulcer disease
- Asthma
- Urinary retention
- Xerostomia
Correct Answer: Asthma
Q20. Stimulation of cardiac M2 receptors produces which primary effect?
- Increased contractility
- Decrease in heart rate (negative chronotropy)
- Ventricular arrhythmias
- Systemic vasoconstriction
Correct Answer: Decrease in heart rate (negative chronotropy)
Q21. Which adverse ocular effect is least likely to occur with pilocarpine administration?
- Mydriasis
- Miosis
- Increased lacrimation
- Excessive salivation
Correct Answer: Mydriasis
Q22. How does pilocarpine produce pupillary constriction (miosis)?
- Inhibition of adrenergic receptors on the iris dilator
- Contraction of sphincter pupillae via M3 receptors
- Stimulation of sympathetic ganglia innervating the iris
- Blockade of acetylcholinesterase around the pupil
Correct Answer: Contraction of sphincter pupillae via M3 receptors
Q23. Which drug is used to stimulate salivary flow in radiation-induced xerostomia?
- Methacholine
- Pilocarpine
- Carbachol
- Neostigmine
Correct Answer: Pilocarpine
Q24. Which direct-acting parasympathomimetic is a tertiary amine and can cross the blood–brain barrier?
- Bethanechol
- Carbachol
- Pilocarpine
- Neostigmine
Correct Answer: Pilocarpine
Q25. Which of the following agents primarily stimulates autonomic ganglia and is used in smoking research and cessation therapies?
- Bethanechol
- Pilocarpine
- Nicotine
- Carbachol
Correct Answer: Nicotine
Q26. Which direct-acting cholinergic agonist is effective in lowering intraocular pressure by contracting the ciliary muscle?
- Bethanechol
- Carbachol
- Nicotine
- Morphine
Correct Answer: Carbachol
Q27. Why is acetylcholine seldom used therapeutically for systemic indications?
- It has extensive oral bioavailability
- It is rapidly hydrolyzed by acetylcholinesterase
- It selectively activates only M1 receptors
- It causes permanent receptor desensitization
Correct Answer: It is rapidly hydrolyzed by acetylcholinesterase
Q28. Which direct-acting cholinergic drug has a longer duration of action and is effective in treating urinary retention?
- Acetylcholine
- Methacholine
- Bethanechol
- Pilocarpine
Correct Answer: Bethanechol
Q29. At the neuromuscular junction, acetylcholine causes which immediate event?
- Inhibition of sodium channels
- Depolarization of motor endplate leading to muscle contraction
- Blockade of nicotinic receptors
- Activation of muscarinic receptors on skeletal muscle
Correct Answer: Depolarization of motor endplate leading to muscle contraction
Q30. Administration of muscarinic agonists is relatively contraindicated in patients with which condition?
- Glaucoma (open-angle)
- Peptic ulcer disease
- Urinary retention
- Dry mouth
Correct Answer: Peptic ulcer disease
Q31. Which muscarinic receptor subtype is most closely associated with cognitive function in the central nervous system?
- M2
- M3
- M1
- M4
Correct Answer: M1
Q32. How can you pharmacologically distinguish muscarinic from nicotinic cholinergic effects?
- Use of hexamethonium to block muscarinic receptors
- Administration of atropine abolishes muscarinic but not nicotinic responses
- Use of atropine specifically blocks nicotinic receptors
- Acetylcholinesterase inhibitors selectively block muscarinic effects
Correct Answer: Administration of atropine abolishes muscarinic but not nicotinic responses
Q33. Why do quaternary ammonium cholinergic agonists have poor central nervous system penetration?
- Their large aromatic rings impede transport
- They are highly lipophilic and sequestered in fat
- Permanent positive charge prevents crossing lipid membranes
- They are substrates for P-glycoprotein efflux in the BBB
Correct Answer: Permanent positive charge prevents crossing lipid membranes
Q34. In acute angle-closure glaucoma, which direct-acting cholinergic agonist can be used to induce miosis and open the trabecular meshwork?
- Pilocarpine
- Bethanechol
- Methacholine
- Propranolol
Correct Answer: Pilocarpine
Q35. Which muscarinic receptor subtype mediates gastric acid secretion on parietal cells?
- M1
- M2
- M3
- M5
Correct Answer: M3
Q36. Which drug can stimulate sweating (via sympathetic cholinergic fibers) and is used diagnostically in sweat testing?
- Pilocarpine
- Carbachol
- Bethanechol
- Morphine
Correct Answer: Pilocarpine
Q37. Which muscarinic receptor subtype is coupled to Gi proteins and inhibits adenylate cyclase?
- M1
- M2
- M3
- M4
Correct Answer: M2
Q38. Muscarinic agonist–induced vasodilation in intact blood vessels is mediated by which mechanism?
- Direct relaxation of vascular smooth muscle M2 receptors
- Endothelial M3 receptor–mediated nitric oxide release
- Activation of sympathetic adrenergic receptors
- Blockade of calcium channels in smooth muscle
Correct Answer: Endothelial M3 receptor–mediated nitric oxide release
Q39. Which statement correctly contrasts carbachol with acetylcholine?
- Carbachol is more rapidly hydrolyzed than acetylcholine
- Carbachol is less susceptible to cholinesterase and activates both muscarinic and nicotinic receptors
- Carbachol is a muscarinic antagonist
- Carbachol cannot be used in ophthalmic applications
Correct Answer: Carbachol is less susceptible to cholinesterase and activates both muscarinic and nicotinic receptors
Q40. Which agent is the drug of choice for diagnostic methacholine challenge testing for bronchial hyperreactivity?
- Acetylcholine
- Methacholine
- Pilocarpine
- Bethanechol
Correct Answer: Methacholine
Q41. Which direct-acting cholinergic agonist is considered relatively selective for muscarinic receptors with minimal nicotinic activity?
- Carbachol
- Bethanechol
- Nicotine
- Suxamethonium
Correct Answer: Bethanechol
Q42. Which structural modification of acetylcholine analogs increases resistance to acetylcholinesterase hydrolysis?
- Introduction of a carbamate ester replacing the acetyl group
- Addition of an aromatic benzene ring
- Converting the tertiary amine to a quaternary ammonium
- Removal of the ester linkage entirely
Correct Answer: Introduction of a carbamate ester replacing the acetyl group
Q43. Which mnemonic correctly represents common muscarinic excess symptoms (SLUDGE)?
- Somnolence, Lethargy, Urination, Diaphoresis, Gastrointestinal pain, Emesis
- Salivation, Lacrimation, Urination, Diarrhea, Gastrointestinal upset, Emesis
- Sweating, Lightheadedness, Urgency, Dry mouth, Gastric stasis, Emesis
- Seizures, Lethargy, Urination, Dyspnea, Glaucoma, Edema
Correct Answer: Salivation, Lacrimation, Urination, Diarrhea, Gastrointestinal upset, Emesis
Q44. Contraction of the ciliary muscle by muscarinic agonists produces which visual change?
- Relaxation for distant vision
- Contraction producing near vision (accommodation)
- Loss of accommodation
- Permanent mydriasis
Correct Answer: Contraction producing near vision (accommodation)
Q45. Which receptor mediates fast excitatory transmission in autonomic ganglia?
- Muscarinic M2
- Nicotinic Nn (neuronal)
- M3 muscarinic
- Beta-adrenergic
Correct Answer: Nicotinic Nn (neuronal)
Q46. Which drug is preferred to stimulate bladder emptying with minimal systemic vascular effects?
- Bethanechol
- Acetylcholine
- Pilocarpine
- Methacholine
Correct Answer: Bethanechol
Q47. Which direct-acting muscarinic agonist is used both in glaucoma therapy and to stimulate salivary secretion?
- Carbachol
- Pilocarpine
- Bethanechol
- Methacholine
Correct Answer: Pilocarpine
Q48. Excessive stimulation of cardiac M2 receptors can lead to which conduction abnormality?
- Ventricular fibrillation
- AV block
- Hypertrophic cardiomyopathy
- Atrial septal defect
Correct Answer: AV block
Q49. Which muscarinic agonist is used in pilocarpine iontophoresis to induce sweat for cystic fibrosis testing?
- Pilocarpine
- Carbachol
- Bethanechol
- Neostigmine
Correct Answer: Pilocarpine
Q50. Which direct-acting agent is commonly applied topically to the eye because it resists acetylcholinesterase and produces sustained miosis?
- Methacholine
- Carbachol
- Acetylcholine
- Pilocarpine
Correct Answer: Carbachol

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