Cholinergeics

Question 1

Acetylycholine

Answer 1

No systemic applications due to many actions and rapid hydrolysis.
Used to obtain rapid miosis in cataract surgery

Question 2

Bethanechol

Answer 2

Muscarinic agonist
Postoperative and postpartum urinary retention
Atony of the urinary bladder

Question 3

Carbachol

Answer 3

Muscarinic and nicotinic agonist
Miosis during surgery
Reduces intraocular pressure in cataract surgery

Question 4

Methacholine

Answer 4

Muscarinic agonist

Diagnostic of bronchial airway hyperreactivity in patients with asthma

Question 5

Pilocarpine

Answer 5

Natural Alkaloid
Partial muscarinic agonist
Tertiary amine
Stable to hydrolysis by acetylcholinesterase
Second line agent in glaucoma
Treatment for dry mouth caused by head and neck surgery and Sjogren’s Snydorme

Question 6

AE of Muscarinic agonists

Answer 6

Sweating, Salivating, Flushing, Low BP, Nausea, Abdominal Pain, Diarrhea, Brochospasm

Question 7

Nicotine

Answer 7

Tertiary amine, selective agonist of the nicotine receptor
Depolarizes autonomic ganglia first causing stimulation then paralysis
CV system: Sympathomimetic effects, Inc. HR/BP due to catecholamine release in adrenal medulla
Gi/Urinary system: Parasympathomimetic, nausea, vomiting, diarrhea, voiding of urine
Secretions: Stimulation of salivary and bronchial secretions
High doses: ganglionic and neuromuscular blockade

Question 8

Anticholinesterases

Answer 8

Edrophonium, Carbamates, Organophosphates

Inhibit acetylcholinesterase. Inc concentration of endogenous acetylcholine

Question 9

Edrophonium

Answer 9

Binds Reversibly to the active site of acetylchoineesterase. Short lived
Does not enter CNS
Used to diagnose myasthenia gravis and reverse non depolarizing neuromuscular blocker

Question 10

Carbamates

Answer 10

Physostigmine, Neostigmine, Pyridostigmine

Form a covalent bond with acetylcholineesterase

Question 11

Organophosphates

Answer 11

Echothiophate, Parthion/melathion(insecticides), Sarin
Phosphorylate acetylcholineesterase. Extremely stable covalent bond that hydrolyzes slowly
Can undergo a process called aging that strengthens the bond
many are toxic

Question 12

Acetylcholineesterase CNS effects

Answer 12

Low concentration causes CNS activation

Higher concentration convulsions, followed by coma and respiratory arrest

Question 13

Acetylcholineesterase eye, urinary, GI, respiratory effects

Answer 13

Act as Cholinomimetics

Question 14

Acetylcholineesterase CV effects

Answer 14

Modest Bradycardia, fall in cardiac output, inceased vascular resistance, increase in blood pressure
Toxic doses causes bradycardia, decrease in cardiac output and hypotension

Question 15

Acetylcholineesterase Neuromuscualar effects

Answer 15

Increase strenght of contraction

Used to reverse action of nondepolarizing neuromuscular blockers and myasthenia gravis

Question 16

Physostigmine

Answer 16

Tertiary amine
Can stimulate CNS
Treatment for overdoses of anticholenergics

Question 17

Neostigmine

Answer 17

Quarternary ammonium, does not enter CNS
Postoperative urinary retention
Reverse effects of nondepolarizing neuromuscular blocker
Treatment for myasthenia gravis

Question 18

Pyridostigmine

Answer 18

Quarternary ammonium, does not enter CNS

Treats myasthenia gravis

Question 19

Donepezil

Answer 19

AChE inhibitors used in ALzhiemers

Question 20

Rivastigmine

Answer 20

AChE inhibitors used in ALzhiemers

Question 21

Galantamine

Answer 21

AChE inhibitors used in ALzhiemers

Question 22

Pralidoxime

Answer 22

Reactivator of AChE, used inpoisoning from organophosphates insecticides