Anticholinesterase Antagonists

Question 1

RVC drugs

Answer 1

Edrophonium

Donepezil

Question 2

RC drugs

Answer 2

Neostigminee

Physostigmine

Question 3

IC drugs

Answer 3

Malathion

Question 4

Edrophonium uses

Answer 4

Diagnosis MG

Tensilon test: distinguish myasthenic crisis from cholinergic crisis

Question 5

SE of edrophonium

Answer 5

Only improves myasthenic symptoms

Worsens cholinergic crisis (desensitization, flaccid paralysis)

Question 6

MOA edrophonium

Answer 6

• Quat ammonium
• bound AChE by weak H and ionic bonds

Does NOT cross BBB
Short Doa (5-10 mint)

Question 7

Donepezil MOA

Answer 7

Lipid soluble

Can cross BBB

Question 8

Use of donepezil

Answer 8

Cognitive decline in AD

Increase cognition, but NOT disease progression

Question 9

SE donepezil

Answer 9

Mild diarrhea
N/V
Bradycardia

Question 10

MOA neostigmine

Answer 10

• quat ammonium
• some lipid solubility
• bound to AChE by ionic and reversible covalent bonds

DOA 2 hours
- does NOT cross BBB

Question 11

What is the only inhibitor that is also an agonist at NMJ N receptors??

Answer 11

Neostigmine

Question 12

Low neostigmine doses

Answer 12

Increase force of contraction

Therapeutic

Question 13

High doses of neostigmine

Answer 13

Decrease force of contraction (desensitization)

Toxic

Question 14

Neostigmine use

Answer 14

MG therapy

Postop urinary retention
Reverse competitive neuromusclar blockade after surgery

Question 15

SE of neostigmine

Answer 15

Excessive M stimulation (N/V, GI cramping, bradycardia) d

Neuromusclar blockade: paralysis of diaphragm at toxic doses

Question 16

What can neostigmine be treated with?

Answer 16

Atropine

Question 17

Physostigmine MOA

Answer 17

Crosses BBB

Not direct cholinergic agonist

Question 18

Use of physostigmine

Answer 18

Treat poisoning by atropine & related drugs that block M blockade

Reverses both peripheral & CNS effects

Question 19

SE of physostigmine

Answer 19

Blurred vision
Photophobia
Increase IOP

Question 20

Malathion MOA

Answer 20

DOA >50h
Prodrug converted to active
Highly toxic metabolite

OP insecticides

Question 21

Use of malathion

Answer 21

Head lice

Question 22

SE malathion

Answer 22

Common source of accidental and agricultural poisoning

Question 23

Pralidoxime MOA

Answer 23

Must be administered before aging occurs

Question 24

Use of pralidoxime

Answer 24

Reactivates AChE ONLY at neuromuscular junction