Anticholinesterase Drugs

Question 1

Neostigmine

Answer 1

therapeutic anti cholinesterase agents; AChE Inhibitors

Question 2

Neostigmine

Answer 2

muscarinic and neuromuscular responses

Question 3

Neostigmine

Answer 3

low doses = increased force of contraction

high doses = reduced force of contraction

Question 4

Neostigmine

Answer 4

inhibitor but ALSO an AGONIST at NMJ nicotinic receptors

Question 5

Therapeutic uses for neostigmine:

Answer 5

myasthenia gravis = autoimmune disorder; antibodies attack Nm receptors to reduce their numbers; increases strength of muscle contractions by increasing ACh levels at NMJ

Question 6

Symptoms of neostigmine:

Answer 6

muscle weakness and fatigue (ptosis, difficulty swallowing)

Question 7

Reversal of competitive neuromuscular blockage:

Answer 7

tubocurarine

Question 8

Adverse effects and contraindications:

Answer 8

excessive muscarinic stimulation = nausea/vomitting, GI cramping, bradycardia - treat with atropine; neuromuscular blocks; respiratory depression at toxic doses

Question 9

Neostigmine:

Answer 9

contraindications are similar to those of muscarinic agonists

Question 10

AChE Inhibitors:

Answer 10

Physostigmine, donepezil

Question 11

Physostigimine:

Answer 11

crosses BBB and NO direct agonist activity; action similar to neostigmine

Question 12

What is physostigmine used for?

Answer 12

treat poisoning by atropine that causes central peripheral muscarinic blockade

Question 13

Donepezil:

Answer 13

selective inhibition of AChE iso form expressed in the CNS

Question 14

What is Donepezil used for?

Answer 14

treat cognitive decline in Alzheimer disease

Question 15

How does donepezil work in Alzheimer patients?

Answer 15

alzheimer’s patients have reduced cortical ACh synthesis and impaired cholinergic function; AChEIs elevate cerebral ACh levels

Question 16

T/F. Donepezil can help improve cognition but is not disease-modifying.

Answer 16

TRUE.

Question 17

Irreversible inhibitors (anticholinesterase):

Answer 17

malathion

Question 18

Characteristics of malathion:

Answer 18

highly lipid-soluble; absorbed from all routes including the skin

Question 19

which drug is a common for accidental and agricultural poisoning:

Answer 19

malathion

Question 20

Therapeutic use for malathion:

Answer 20

treatment of head lice and their ova

Question 21

Drug where agents of the class are used in chemical warfare:

Answer 21

malathion

Question 22

Diagnosis and treatment of organophosphate poisoning:

Answer 22

muscarinic: produse sweating, salivation, miosis, involuntary urination and defecation
nicotinic: muscle weakness, paralysis (apnea)

Question 23

Antidotes of organophosphate poisoning:

Answer 23

atropine (antagonize muscarinic effects), pralidoxime (reactivates AChE ONLY at the neuromuscular junction – most be administered before “aging” occurs)