Acetylcholinesterase Inhibitors in Alzheimer’s Disease
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Questions and Answers

What is the role of acetylcholine (ACh) in Alzheimer's Disease progression?

  • It catalyzes the hydrolysis of choline to acetic acid
  • It is closely associated with early cognitive decline (correct)
  • It leads to beta-amyloid protein aggregation
  • It is responsible for mitochondrial damage in neurons

    • Which process results in the hydrolysis of acetylcholine to choline and acetic acid?

  • Acetylcholinesterase catalysis (correct)
  • Neuroinflammation
  • Beta-amyloid protein aggregation
  • Cation binding to tryptophan residue

    • Why is acetylcholine (ACh) highly prone to hydrolysis?

  • It has an electron-deficient carbon (correct)
  • It has a positively charged nitrogen
  • It forms cation-pi interactions
  • It interacts with serine amino acid residues

    • Which neurotransmitter is depleted in Alzheimer's Disease?

    <p>Acetylcholine</p> Signup and view all the answers

    What is the primary function of acetylcholinesterase (AChE) in the context of Alzheimer's Disease?

    <p>To hydrolyze acetylcholine into choline and acetic acid</p> Signup and view all the answers

    Which amino acid residue acts as a base and removes a proton during the hydrolysis process of acetylcholine by acetylcholinesterase?

    <p>Histidine</p> Signup and view all the answers

    Which medication acts on the glutamatergic system by blocking NMDA receptors?

    <p>Memantine</p> Signup and view all the answers

    Which medication is a potent allosteric potentiating ligand of human nicotinic acetylcholine receptors?

    <p>Galantamine</p> Signup and view all the answers

    Which medication is a centrally acting reversible acetylcholinesterase inhibitor with CNS selectivity?

    <p>Donepezil</p> Signup and view all the answers

    Which medication is obtained synthetically or from the bulbs and flowers of Galanthus caucasicus?

    <p>Galantamine</p> Signup and view all the answers

    Which medication shows weak competitive and reversible cholinesterase inhibition in all areas of the body?

    <p>Galantamine</p> Signup and view all the answers

    Which medication is used for the treatment of mild to moderate Alzheimer's disease and memory impairments of vascular origin?

    <p>Galantamine</p> Signup and view all the answers

    Which class of drugs is commonly used to treat Alzheimer's Disease (AD)?

    <p>Anticholinesterase drugs</p> Signup and view all the answers

    What is the primary cognitive function affected by Alzheimer's Disease (AD)?

    <p>Short-term memory</p> Signup and view all the answers

    Which of the following is NOT a non-cognitive function often affected by Alzheimer's Disease (AD)?

    <p>Headaches</p> Signup and view all the answers

    What type of drugs are carbamate cholinesterase inhibitors?

    <p>Anticholinesterase drugs</p> Signup and view all the answers

    What is the most common single cause of dementia in the ageing society?

    <p>Alzheimer's Disease (AD)</p> Signup and view all the answers

    What is the main function of anticholinesterases in alleviating symptoms of Alzheimer's Disease?

    <p>Extending the action of acetylcholine</p> Signup and view all the answers

    What is the significance of the carbamate group in AChE inhibitors like Rivastigmine?

    <p>It is essential for inhibitory properties</p> Signup and view all the answers

    Why is Rivastigmine considered a 'pseudo-irreversible' AChE inhibitor?

    <p>It mimics ACh and forms a carbamylated complex with AChE</p> Signup and view all the answers

    Why is Neostigmine preferred over Miotine despite both drugs being developed to address 'miotine problems'?

    <p>Neostigmine's permanent quaternary nitrogen prevents the formation of free base</p> Signup and view all the answers

    How do nerve agents cause death?

    <p>By permanently deactivating AChE through phosphorylated adduct formation</p> Signup and view all the answers

    What is one reason for the limited medicinal use of physostigmine?

    <p>It has serious side effects limiting its use</p> Signup and view all the answers

    Why are benzene rings considered important in AChE inhibitors like Carbamates?

    <p>For hydrophobic interactions with the active site</p> Signup and view all the answers

    'Smart drugs' are often associated with which class of compounds despite lacking evidence of general memory improvement?

    <p>'Cognitive enhancers' like Rivastigmine</p> Signup and view all the answers

    What is the role of tertiary nitrogen in AChE inhibitors such as Rivastigmine?

    <p>To bind to anionic regions of the enzyme at blood pH</p> Signup and view all the answers

    What effect does Rivastigmine have on plasma proteins?

    <p>It has no appreciable binding to plasma proteins</p> Signup and view all the answers

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