Indirect Acting Cholinomimetic Drugs (Cholinomimetic Drugs)

Question 1

What are indirect cholinomimetic drugs?

Answer 1

Cholinesterase inhibitors (anti-ChEs)

Question 2

What is the MOA of direct acting muscarinic agonists?

Answer 2

Blockade of AChE –> increases ACh

Question 3

What are the clinical uses of indirect acting cholinomimetic drugs?

Answer 3

Glaucoma
Alzheimer’s disease (deficit in cholinergic neurons involved)
Treatment of mAChR antagonist toxicity
Myasthenia gravis
Insecticide

Question 4

What are the adverse effects of indirect acting cholinomimetic drugs?

Answer 4

General increased cholinomimetic effects:
* GIT: diarrhea, abdominal cramps, nausea/vomiting
* Urinary urgency
* Vision problems
* Musculoskeletal effects: muscle cramps, myalgia

Question 5

What are contraindications of indirect acting cholinomimetic drugs?

Answer 5

Asthma/ COPD
Urinary or GI tract obstruction

Question 6

What is the clinical presentation of someone with anti-ChE intoxication?

Answer 6

DUMMBBELLSS
Diarrhea (M3)
Urination (M3)
Miosis (M3)
Muscle weakness, paralysis (NM)
Bradycardia (M2)
Bronchoconstriction (M3)
Excess bronchial secretion (M3)
Lacrimation (M3)
Lousy for vision (M3)
Salivation (M3)
Sweating (M3; sympathetic cholinergic NEJs)

Cause of Death: Respiratory failure (peripheral respiratory paralysis, bronchoconstriction, increased bronchosecretions)

Question 7

What type of therapy is used for anti-ChE intoxication?

Answer 7

mAChR antagonist (Atropine) to control signs of muscarinic excess
AChE reactivator (Pralidoxime)
- Used for intoxication with organophosphates
- No effect if phosphorylated AChE has “aged”