cholinergic drugs - joshi

based on his kahoot 👉🏻👈🏻

what enzyme is responsible for the synthesis of ACh?

choline acetyltransferase

what drug is a cholinesterase inhibitor used in alzheimer’s disease?

donepezil

memantine, used in Alzheimer’s disease, acts by:

blocking NMDA receptors

what is a major side effect of cholinesterase inhibitors, like donepezil?

bradycardia

what is NOT a mechanism of action for alzheimer’s drugs?

dopamine receptor agonism

memantine is beneficial in alzheimer’s disease because it:

reduces excitotoxicity by blocking NMDA receptors

what is TRUE about cholinesterase inhibitors?

they provide symptomatic relief but do NOT halt disease progression

the use of cholinesterase inhibitors is contraindicated in patients with:

bradycardia

peptic ulcers

galantamine differs from other cholinesterase inhibitors because it:

acts as a partial nicotinic receptor agonist

what is a common side effect of donepezil?

diarrhea

why should cholinesterase inhibitors be used cautiously in pts with cardiac conditions?

can lead to bradycardia and syncope

if a pt on donepezil develops bradycardia, which medication should be avoided?

propranolol

rivastigmine differs from donepezil in that it:

inhibits both acetylcholinesterase and butyrylcholinesterase

which cholinesterase inhibitor has the highest risk of GI side effects?

rivastigmine

which side effect is most likely to occur if overdosed on cholinesterase inhibitors?

cholinergic crisis (severe n/v, increased salivation/sweating, etc.)

pts on donepezil should be monitored for:

QT prolongation

what enzymes are responsible for metabolism of ACh?

acetylcholinesterase

butyrylcholinesterase

T/F botulinum toxin and tetanus toxin block the ACh release by cleaving the VAMP

TRUE

T/F M1, M3, and M5 muscarinic receptors are coupled with Gq protein and activate phospholipase C

TRUE

which of the following cholinergic drugs is used for alzheimer’s disease?

rivastigmine

T/F anticholinesterase compound, tacrine, use is limited due to extensive hepatotoxicity

TRUE

what is the MOA of donepezil?

carbamylates the acetylcholinesterase

in what condition are the cholinergic drugs contraindicated?

asthma

T/F anticholinergic drugs are useful in dementia

FALSE

what mechanism of galantamine produces its cognitive and behavioral benefits?

inhibiting cerebral AChE

activating nicotinic receptor

what receptor is coupled with Gq protein?

M1

in what condition are anticholinergic drugs contraindicated?

closed angle glaucoma

what group of the ACh is responsible for binding to the cholinergic receptors?

ethylene chain

what anticholinesterase drug leads to the aging of the acetylcholinesterase enzyme?

echothiophate

what cholinergic drug is direct acting?

carbachol

what is the mechanism of action of anticholinesterase drugs?

increase ACh level

inhibit AChE

what is a major side effect of rivastigmine?

GI discomfort

T/F to possess cholinergic/muscarinic agonist effects, candidate drugs should have quaternary ammonium group

TRUE

what isomer is responsible for biological activity of atropine?

l-isomer

T/F there is NO NEED to take precaution if the cholinergic drug donepezil is given with beta 1 blockers

FALSE

what category of drugs may interact with cholinergic drugs and induce bradycardia?

beta 1 blockers

anti-arrhythmia drugs