Cholinomimetics

Question 1

Bethanecol

Answer 1

Class: Direct-acting carbamic acid ester

Mechanism of action: Direct acting muscarinic cholinomimetic

Therapeutic uses: Ileus, Urinary retention
Both bowel and urinary smooth muscle is ACh innervated.

Toxicity:
SLUDGE (Salivation, Lacrimation, Urination, Defecation, GI distress, Emesis)

Question 2

Muscarine

Answer 2

Class: Direct acting non-ester alkaloid

Mechanism of action: Direct acting muscarinic cholinomimetic

Therapeutic uses: N/A

Toxicity: SLUDGE

Question 3

Pilocarpine

Answer 3

Class: Direct acting non-ester alkaloid

Mechanism of action: Direct acting muscarinic cholinomimetic

Therapeutic uses: Glaucoma (ACh activates sphincter and ciliary muscles of the eye)

Toxicity: SLUDGE

Question 4

Cevimiline

Answer 4

Class: Direct acting non-ester alkaloid

Mechanism of action: Direct acting muscarinic cholinomimetic

Therapeutic uses: Dry mouth (Sjogrens disease and post-radiation therapy)

Toxicity: SLUDGE

Question 5

Nicotine

Answer 5

Class: Direct acting non-ester alkaloid

Mechanism of action: Direct acting nicotinic cholinomimetic.

Therapeutic uses: Smoking cessation.

Toxicities: N/A

Question 6

Neostigmine

Answer 6

Class: Indirect acting carbamate.

Mechanism of action: AChE inhibitor (short acting)

Therapeutic uses: Ileus and urinary retention
Myasthenia Gravis
Reversal of neuromuscular blockade

Toxicities: SLUDGE plus general increase in cholinergic neurotransmission
Paralysis

Miscellaneous: Lasts 0.5-2 hours

Question 7

Physostigmine

Answer 7

Class: Indirect-acting carbamate.

Mechanism of action: AChE inhibitor (short acting)

Therapeutic uses: Glaucoma (ACh activates sphincter and ciliary muscles)

Toxicities: SLUDGE plus general increase in cholinergic neurotransmission
Paralysis

Miscellaneous: Lasts 0.5-2 hours

Question 8

Donepezil

Answer 8

Class: Indirect-acting non-ester

Mechanism of action: AChE inhibitor

Therapeutic uses: Alzheimers (Amplifies endogenous ACh in the brain.

Toxicities: SLUDGE plus general increase in cholinergic neurotransmission
Paralysis

Question 9

Edrophonium

Answer 9

Class: Indirect-acting non-ester

Mechanism of action: AChE inhibitor (very short acting)

Therapeutic uses: Myasthenia Gravis (differentiates between deficiency versus ACh crisis)

Toxicities: SLUDGE plus general increase in cholinergic neurotransmission
Paralysis

Miscellaneous: Acts for 5-15 minutes.

Question 10

Echothiophate

Answer 10

Class: Indirect acting organophosphate

Mechanism of action: AChE inhibitor (long acting)

Therapeutic uses: Glaucoma (acts on sphincter and ciliary muscles)

Toxicities: SLUDGE plus general increase in cholinergic neurotransmission
Paralysis

Miscellaneous: Acts for greater than 100 hours

Question 11

Pralidoxime

Answer 11

Class: Strong nucleophile

Mechanism of action: Regenerates phosphorylated AChE

Therapeutic uses: Poisoning by nerve gas or insecticide

Toxicities: N/A

Question 12

Sarin

Answer 12

Class: Very potent indirect acting organophosphate

Mechanism of action: AChE inhibitor

Therapeutic uses: Volatile nerve gas

Toxicities:SLUDGE plus general increase in cholinergic neurotransmission
Paralysis
Death

Miscellaneous: Treat with Pralidoxime and Atropine before aging occurs