Introduction: Understanding drugs for Alzheimer’s disease is essential for B. Pharm students studying clinical pharmacology and therapeutics. This concise guide explains mechanisms of action, pharmacokinetics (ADME), dosing, adverse effects, monitoring, and drug interactions for cholinesterase inhibitors (donepezil, rivastigmine, galantamine), the NMDA antagonist memantine, and older agents such as tacrine. Key topics include mechanism of action, CYP-mediated metabolism (CYP2D6/CYP3A4), formulation differences (oral, transdermal), common side effects (nausea, bradycardia, dizziness), and safe dispensing and patient counseling. This resource integrates clinical pharmacology, evidence-based treatment guidelines, and practical points for B. Pharm practice. ‘Now let’s test your knowledge with 30 MCQs on this topic.’
Q1. Which drug is a reversible acetylcholinesterase inhibitor commonly used in mild to moderate Alzheimer’s disease?
- Donepezil
- Rivastigmine
- Memantine
- Tacrine
Correct Answer: Donepezil
Q2. Which agent acts primarily as an NMDA receptor antagonist to reduce excitotoxicity in Alzheimer’s disease?
- Galantamine
- Memantine
- Donepezil
- Rivastigmine
Correct Answer: Memantine
Q3. Which cholinesterase inhibitor inhibits both acetylcholinesterase and butyrylcholinesterase?
- Donepezil
- Galantamine
- Rivastigmine
- Memantine
Correct Answer: Rivastigmine
Q4. Which Alzheimer’s drug also acts as a positive allosteric modulator of nicotinic receptors in addition to inhibiting acetylcholinesterase?
- Donepezil
- Rivastigmine
- Galantamine
- Tacrine
Correct Answer: Galantamine
Q5. The most common adverse effects associated with cholinesterase inhibitors are:
- Hepatotoxicity and jaundice
- Severe hypertension
- Gastrointestinal upset (nausea, vomiting, diarrhea)
- Neutropenia
Correct Answer: Gastrointestinal upset (nausea, vomiting, diarrhea)
Q6. Memantine’s mechanism of action is best described as:
- Competitive NMDA receptor agonist
- Uncompetitive NMDA receptor antagonist (open-channel blocker)
- Acetylcholinesterase inhibitor
- Monoamine oxidase inhibitor
Correct Answer: Uncompetitive NMDA receptor antagonist (open-channel blocker)
Q7. Donepezil is mainly metabolized by which cytochrome P450 enzymes?
- CYP1A2 and CYP2E1
- CYP3A4 and CYP2D6
- CYP2C9 and CYP2C19
- Not metabolized; excreted unchanged
Correct Answer: CYP3A4 and CYP2D6
Q8. Which older Alzheimer’s drug was largely discontinued due to hepatotoxicity concerns?
- Galantamine
- Tacrine
- Memantine
- Donepezil
Correct Answer: Tacrine
Q9. Which cholinesterase inhibitor is available as a transdermal patch to improve tolerability?
- Donepezil patch
- Rivastigmine patch
- Galantamine patch
- Memantine patch
Correct Answer: Rivastigmine patch
Q10. Which cognitive scale is commonly used in clinical trials and practice to assess severity of Alzheimer’s disease?
- Glasgow Coma Scale (GCS)
- Mini-Mental State Examination (MMSE)
- Apgar Score
- Barthel Index
Correct Answer: Mini-Mental State Examination (MMSE)
Q11. A major cardiovascular contraindication to starting cholinesterase inhibitors is:
- Hypertension
- Bradycardia or heart block
- Hypercholesterolemia
- Peripheral vascular disease
Correct Answer: Bradycardia or heart block
Q12. Co-administration of which drug class can reduce the clinical effectiveness of cholinesterase inhibitors?
- Beta blockers
- Anticholinergics (e.g., oxybutynin)
- ACE inhibitors
- Statins
Correct Answer: Anticholinergics (e.g., oxybutynin)
Q13. Which acetylcholinesterase inhibitor is commonly dosed once daily at bedtime in clinical practice?
- Rivastigmine twice daily
- Donepezil once daily
- Memantine once daily
- Galantamine three times daily
Correct Answer: Donepezil once daily
Q14. The usual initial oral dose of donepezil for Alzheimer’s disease is:
- 1 mg daily
- 5 mg daily
- 10 mg twice daily
- 20 mg daily
Correct Answer: 5 mg daily
Q15. Memantine is primarily indicated for which stage of Alzheimer’s disease?
- Mild Alzheimer’s disease only
- Moderate to severe Alzheimer’s disease
- Preclinical Alzheimer’s disease
- Vascular dementia only
Correct Answer: Moderate to severe Alzheimer’s disease
Q16. Galantamine is metabolized predominantly by which enzymes?
- CYP2D6 and CYP3A4
- CYP1A2 and CYP2E1
- Renal excretion unchanged only
- Monoamine oxidase A and B
Correct Answer: CYP2D6 and CYP3A4
Q17. A common central nervous system adverse effect of memantine is:
- Dizziness
- Severe hepatotoxicity
- Profound neutropenia
- Paresthesia of the extremities only
Correct Answer: Dizziness
Q18. Which cholinesterase inhibitor is a carbamate-based inhibitor producing pseudo-irreversible inhibition?
- Donepezil
- Rivastigmine
- Galantamine
- Memantine
Correct Answer: Rivastigmine
Q19. The earliest cognitive deficit typically seen in Alzheimer’s disease is:
- Impaired recent (short-term) memory
- Loss of long-term procedural memory
- Visual field defects
- Motor weakness
Correct Answer: Impaired recent (short-term) memory
Q20. Which genetic allele is most strongly associated with increased risk of late-onset Alzheimer’s disease?
- ApoE2
- ApoE3
- ApoE4
- PSEN1
Correct Answer: ApoE4
Q21. Memantine is eliminated primarily by which route?
- Hepatic metabolism with biliary excretion
- Renal excretion (unchanged)
- Pulmonary exhalation
- Fecal elimination only
Correct Answer: Renal excretion (unchanged)
Q22. Which inhibitor binds reversibly and non-covalently to acetylcholinesterase?
- Rivastigmine (carbamate, pseudo-irreversible)
- Donepezil (reversible, non-covalent)
- Organophosphate (irreversible)
- Physostigmine (carbamate)
Correct Answer: Donepezil (reversible, non-covalent)
Q23. The most frequent adverse effect specific to transdermal rivastigmine patches is:
- Severe hepatotoxicity
- Skin irritation at application site
- Excessive salivation only
- Renal failure
Correct Answer: Skin irritation at application site
Q24. Overdose of cholinesterase inhibitors can precipitate a cholinergic crisis characterized by:
- Tachycardia and hypertension
- Dry mouth and mydriasis
- Excessive salivation, bradycardia, bronchospasm
- Hyperthermia and delirium only
Correct Answer: Excessive salivation, bradycardia, bronchospasm
Q25. Pharmacologic strategies targeting glutamatergic excitotoxicity in Alzheimer’s disease primarily use which class?
- Beta-blockers
- Nicotinic receptor antagonists
- NMDA receptor antagonists
- SSRIs
Correct Answer: NMDA receptor antagonists
Q26. The main reason tacrine fell out of widespread clinical use was:
- Poor oral bioavailability only
- Significant hepatotoxicity requiring frequent monitoring
- Excessive renal excretion
- High cost compared to alternatives
Correct Answer: Significant hepatotoxicity requiring frequent monitoring
Q27. Which laboratory parameter should be monitored during memantine therapy, especially in elderly patients?
- Serum transaminases only
- Renal function (serum creatinine, eGFR)
- Fasting lipid profile
- Platelet count
Correct Answer: Renal function (serum creatinine, eGFR)
Q28. Cardiovascular adverse events associated with cholinesterase inhibitors include:
- Ventricular fibrillation as the most common effect
- Bradycardia and syncope
- Systemic hypertension and stroke
- Pulmonary embolism
Correct Answer: Bradycardia and syncope
Q29. Which approved Alzheimer’s medication combines acetylcholinesterase inhibition with nicotinic receptor potentiation?
- Tacrine
- Memantine
- Galantamine
- Rivastigmine
Correct Answer: Galantamine
Q30. To minimize adverse effects, cholinesterase inhibitor therapy is usually started and adjusted by:
- High initial dose then rapid taper
- One-time loading dose
- Gradual dose titration to target dose
- Using parenteral administration only
Correct Answer: Gradual dose titration to target dose
I am a Registered Pharmacist under the Pharmacy Act, 1948, and the founder of PharmacyFreak.com. I hold a Bachelor of Pharmacy degree from Rungta College of Pharmaceutical Science and Research. With a strong academic foundation and practical knowledge, I am committed to providing accurate, easy-to-understand content to support pharmacy students and professionals. My aim is to make complex pharmaceutical concepts accessible and useful for real-world application.
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