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Acetylcholinesterase Inhibitors in Alzheimer’s Disease

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27 Questions

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

It is closely associated with early cognitive decline

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

Acetylcholinesterase catalysis

Why is acetylcholine (ACh) highly prone to hydrolysis?

It has an electron-deficient carbon

Which neurotransmitter is depleted in Alzheimer's Disease?

Acetylcholine

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

To hydrolyze acetylcholine into choline and acetic acid

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

Histidine

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

Memantine

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

Galantamine

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

Donepezil

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

Galantamine

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

Galantamine

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

Galantamine

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

Anticholinesterase drugs

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

Short-term memory

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

Headaches

What type of drugs are carbamate cholinesterase inhibitors?

Anticholinesterase drugs

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

Alzheimer's Disease (AD)

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

Extending the action of acetylcholine

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

It is essential for inhibitory properties

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

It mimics ACh and forms a carbamylated complex with AChE

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

Neostigmine's permanent quaternary nitrogen prevents the formation of free base

How do nerve agents cause death?

By permanently deactivating AChE through phosphorylated adduct formation

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

It has serious side effects limiting its use

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

For hydrophobic interactions with the active site

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

'Cognitive enhancers' like Rivastigmine

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

To bind to anionic regions of the enzyme at blood pH

What effect does Rivastigmine have on plasma proteins?

It has no appreciable binding to plasma proteins

Learn about the drugs used to treat Alzheimer's Disease, including how anticholinesterase drugs work and the role of carbamate cholinesterase inhibitors. Explore the recent advances in drug therapy that challenge the traditional view of Alzheimer's Disease as an untreatable degenerative condition.

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