Acetylcholine Esterase Inhibitors

Question 1

Drugs that augment Acetylcholine:

Answer 1

• Sildenafil
• Tadalfil and vardenafil
• Rivastigmine and Galantamine

Mnemonic: ST(G)aRVe

Question 2

Botulinum toxin

Answer 2

1. Acetylcholine Release Inhibitor
2. Rx of wrinkles
3. Botox injection will inhibit release of Acetylcholine –> paralysis of the muscle

Question 3

Reversible Acetylcholine Esterase inhibitors (Indirect Agonists):

Answer 3

•  Edrophonium
•  Neostigmine and Pyridostigmine
•  Physostigmine
•  Donepezil

Mnemonic: Edro Stig-me and I’m Done

Question 4

Edrophonium

Answer 4

1. Reversible Acetylcholinesterase inhibitor
2. Diagnosis of Myasthenia gravis

Question 5

Physostigmine

Answer 5

1. Reversible Acetylcholinesterase inhibitor
2. Glaucoma; antidote in overdose of atropine

Note: tertiary amines (enter CNS)

Question 6

Neostigmine

Pyridostigmine

Answer 6

1. Reversible Acetylcholinesterase inhibitor
2. Myasthenia gravis, ileus, urinary retention; Reversal of non- depolarizing NM blockers

Note: quaternary amines (No CNS)

Question 7

Donepezil

Tacrine

Answer 7

1. Reversible Acetylcholinesterase inhibitor
2. Alzheimer’s disease

Question 8

Irreversible Acetylcholine esterase (Indirect Agonist) inhibitors:

Answer 8

• Ecothiophate
• Isoflurophate
• Malathion and Parathion
• Insecticides Toxicity (P450)

Mnemonic: Thion’s Fate

Question 9

Ecothiophate

Answer 9

1. Irreversible Acetylcholinesterase inhibitor
2. Glaucoma
3. Increases outflow

Note: Organophosphates

Question 10

Acetylcholine esterase inhibitors toxicity:

Answer 10

Parasympathetic stimulation:

• Bradycardia
• Bronchospasm
• Diarrhea
• Urinary incontinence
• increased sweating, salivation and lacrimation
• Muscle fasciculation and paralysis (Nm receptors)

Treatment of Toxicity: Atropine and Pralidoxime (2-PAM)

Note: Anticholinergics (Parasympatholytics) = Muscarinic receptors antagonists

Effects are opposite to Cholinergic, See below