1
Q
ACh function
A
a chemical transmitter that is released from pre-synaptic nerve ending into synapse
2
Q
therapeutic use of ACh
A
some ocular surgeries to produce complete miosis within seconds
3
Q
Methacholine
A
- selective to muscarinic receptors
- S-(+)-enantimer is active
- acts as a competative inhibitor of ACh-E: longer duration of action than ACh
4
Q
Carbachol
A
- used as a muscarinic therapeutic agent
- potent cholinergic agonist: both nicotinic and muscarinic
- uses: glaucoma and miosis in ocular surgery
5
Q
Bethanechol
A
- combination of methacholine and carbachol
- potent muscarinic agent
- treat post surgical and post partum urinary retention and abdominal distention
6
Q
Pilocarpine HCl
A
- used in ophthalmic solution
- mitotic of choice for open angle glaucoma
7
Q
Nicotine
A
- classic nonendogenous agonist for nicotinic receptors
- used in nicotine replacement therapy
8
Q
Varenicline
A
- partial agonist for certain nicotinic receptor subtypes
- can reduce the feeling of craving and withdrawal
- treat tabacco dependence
9
Q
Physostigmine
A
- alkaloid
- high binding affinity
- likes to bind to AChE more than ACh
- uses: glaucoma
- antidote for overdose of antichoinergic agents
- lipophilic enough to cross BBB
- indirect cholimemetic for Alzheimers
10
Q
Neostigmine and Pyridostigmine
A
- chemically more stable with longer duration of action
- uses: myasthenia gravis, reverse effects of neuromuscular blockers
11
Q
Rivastigmine
A
- selective aryl carbamate
- able to inhibit for up to 10 hours
- pseudo-irreversible AChEI
12
Q
Donepezil
A
- centrally acting non competitive AChEI
- greater affinity for AChe in the brain than the periphery
- used: alzheimers
- adverse effects: elevated cholinergic activity - decreased HR
- metabolism: CYP metabolized to both active and inactive metabolites
- strong CYP 3A4 inhibitors
13
Q
organic phosphates
A
- phosphate esters are very stable to hydrolysis
- work by same mechanism as reversible inhibitors but leave E esterified as phosphate esters
- rate of degradation is slower
- key difference: phosphorylated E can undergo aging leading to toxicity
14
Q
isoflurophate and Echothiophate Iodide
A
- phosphate ester AChEIs
- treat open angle glaucoma
- isoflurophate: used as eye oitment when other agents fail
- EI: ophthalmic solution, most widely used AChEI for treatment of glaucoma
- decrease in intraocular pressure can last up to 4 weeks
- bc of toxicity, can not be used systemically.
15
Q
Parathione and Malathione
A
- number of lipophilic phospoesters used as insecticides
- beneficial to agricultural production
16
Q
pralidoxime Obidoxime and Asoxime
A
- antidotes for irreversible AChEIs for treatment of organophosphate poisoning
- it must be given within a short period after exposure
17
Q
Therapeutic Applications of AChEIs
A
- classified as indirect cholinomimetics
- MOA does not involve binding to cholingergic receptors
- improve muscle strength in myasthenia gravis
- open angle glaucoma
- symptoms of Alzheimers
- insecticides and chemical warfare agents
Med Chem
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