Acetylcholinesterase Inhibitors

Flashcards based on Acetylcholinesterase Inhibitors lecture notes.

Acetylcholinesterase (AChE)

Breaks down acetylcholine (ACh) into acetate and choline.

Cholinomimetics

Drugs that mimic the effects of acetylcholine.

Indirect Reversible Inhibitors

Inhibitors that bind reversibly to acetylcholinesterase.

Indirect Irreversible Inhibitors

Inhibitors that bind irreversibly to acetylcholinesterase.

Electrostatic attraction

Attraction between the anionic site and the drug.

Anionic Site

Site on acetylcholinesterase that attracts acetylcholine.

Esteric Site

Site on acetylcholinesterase where acylation occurs.

Acylation

Enzymatic knife, forms covalent bond.

Deacylation

The rate-limiting step in the breakdown of acetylcholine.

Alcohols

Drug class of Edrophonium.

carbamate ester

Drug class of Neostigmine

carbamate ester

Drug class of Pyridostigmine

Carbamate Ester

Drug class of Physostigmine

Organophosphates

Drug class of Ecothiopate

Alzheimer's Drugs

Drug class of donepezil

Alzheimer's Drugs

Drug class of Galantamine

Alzheimer's Drugs

Drug class of Rivastigmine

Alzheimer's Drugs

Drug class of Tacrine

Myasthenia Gravis Diagnosis

Clinical use of Edrophonium

Treatment of Myasthenia Gravis

Clinical use of Neostigmine

Treatment of Myasthenia Gravis

Clinical use of Pyridostigmine

treating overdoses with anticholinergic drugs

Clinical use of Physostigmine

Historical use for glaucoma

Clinical use of Ecothiopate

Treatment of Alzheimer's Disease

Clinical use of Donepezil

Treatment of Alzheimer's Disease

Clinical use of Galantamine

Treatment of Alzheimer's Disease

Clinical use of Rivastigmine

Treatment of Alzheimer's Disease

Clinical use of Tacrine

Ocular

The first stage of Myasthenia Gravis.

Tensilon test

Diagnostic test using edrophonium for myasthenia gravis.

5 to 15 min

The duration of AChE inhibition for Edrophonium.

0.5 to 4 hours

The duration of AChE inhibition for Neostigmine.

4 to 6 hours

The duration of AChE inhibition for Pyridostigmine.

0.5 to 2 hours

The duration of AChE inhibition for Physostigmine.

1000+ hours

The duration of AChE inhibition for Ecothiopate.

1000+ hours

The duration of AChE inhibition for Malathion.

S

Adverse event due to acetylcholine accumulation: Salivation

L

Adverse event due to acetylcholine accumulation: Lacrimation

U

Adverse event due to acetylcholine accumulation: Urination

D

Adverse event due to acetylcholine accumulation: Defecation

G

Adverse event due to acetylcholine accumulation: Gastric upset

E

Adverse event due to acetylcholine accumulation: Emesis

M

Adverse event due to acetylcholine accumulation: Miosis

Oral treatment of choice

Clinical effect of pyridostigmine within 10-15 minutes.

Treatment for glaucoma

Historical use of physostigmine.

Selective for CNS

The selectivity of donepezil.

Aricept

Common name for Donepezil

Razadyne or Reminyl

Brand name for Galantamine

Exelon, Nimvastid, Prometax

Brand names for Rivastigmine

AChE and BuChE

Rivastigmine inhibits these two enzymes.

Ecothiopate

Last resort treatment for glaucoma due to toxicity.

4 weeks

Duration of intraocular pressure decrease with ecothiopate.

Esotropia

Inward misalignment of the eyes.

Exotropia

Outward misalignment of the eyes.

Ophthalmic administration only route

Route of administration for Echothiophate

Malathion

Insecticide for hair/scalp lice.

S-L-U-D-G-E

Toxic effects of Acetylcholine

Neostigmine

The step where Carbamoylation of serine creates bond that is more resistant to hydrolysis, extended rate limiting step 2

Donepezil

This drug crosses the blood brain barrier

Transdermal patch overcomes gastrointestinal distress

Why is Rivastigmine unique

Echothiophate and glaucoma

Binding site that leads to cataract promoting toxicity

Asthma and COPD

A contraindication for Acetylcholinesterase treatment

Cardiac Disease

A contraindication for Acetylcholinesterase treatment

U and Gl obstruction

A contraindication for Acetylcholinesterase treatment

Neostigmine

This has two steps hydrolysis like acetylcholine

Neostigmine

This is dosed by slow intravenous injection for reversal of neuromuscular blockade

Physostigmine

This is a natural alkaloid

Physostigmine

This drug lacks neuromuscular blocking action

Galantamine

This increases response to ACh

Echothiophate

This drug is absorbed systemically through conjunctiva and lacrimal drainage system

Malathion

This drug has limited toxicity to humans

Echothiophate

This is a quaternary ammonium with diethyl-thiophosphate

Pyridostigmine

This oral treatment of choice for myasthenia gravis

Pyridostigmine

This drug prophylaxis against nerve gas poisoning

Pyridostigmine

This treatment against nerve gas poisong use is supported by animal studies, but human impact not well established

Malathion

The organophosphate that should be used for hair and scalp lice according to the lecture notes

Edrophonium

This has an impact on the eyelid droop or ability to do repetitious movements

Edrophonium

This is a phenol with quaternary ammonium group

Neostigmine

This is a phenol with quaternary ammonium plus carbamic acid