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Pharmacology > Cholinesterase Inhibitors > Flashcards

Cholinesterase Inhibitors Flashcards

1
Q

Cholinesterase inhibitors (CI) effects

A

skeletal muscles, brain, and autonomic system

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2
Q

CI enhance acton of Ach at

A

muscarinic and nicotinic receptors

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3
Q

What are the two binding sites of Cholinesterase

A

anionic (binding) and esteratic (hydrolysis)

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4
Q

Anionic site of acetylcholine esterase

A

formed by ring system of Trp and Phe, which bind Ach

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5
Q

Esteratic site of acetylcholine esterase

A

formed by Ser, His, and Glu, which hydrolyses

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6
Q

Affects of neostigmine on esterase

A

neostigmine is hydrolyzed by esterase but the carabamate portion remains on the Ser to block further hydrolysis for a few hours

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7
Q

Edrophonium

A

simple quaternary alcohol
binds to anionic site and prevents interaction with Ach
duration: few minutes

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8
Q

How do organophosphates effect Achase

A

Bind to esteratic site of Achase, which results in increase of cholinesterase synthesis

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9
Q

medical use of cholinesterase inhibitors

A

Alzheimers
Increase GI activity post op
Myasthenia gravis

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10
Q

What is Alzheimer’s

A

most common cause of dementia old age
improper processing beta amyloid protein
loss of cholinergic neurons in brain
Tx: Donepezil

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11
Q

What do you use to increase GI activity post op

A

neostigmine

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12
Q

What is myasthenia gravis

A

disease characterized by skeletal muscle weakness
autoimmune loss of receptors (loss of 2/3 receptors results in symptoms)
Neostigmine is effective
More common in women (3:2)

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13
Q

Drugs used in Myasthenia gravis

A

edrophonium for diagnosis
pyridostigmine orally for treatment

myasthenia crisis  (low Ach) gets better with edrophonium 
cholinergic crisis (high Ach) gets worse with edrophonium
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14
Q

Catatonic (act on anionic site) Cholinesterase inhibitors

A

edrophonium

donepezil

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15
Q

Carbamate esters cholinesterase inhibitors

A

rivastigmine
physostigmine
neostigmine
pyridostigmine

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16
Q

Irreversible cholinesterase inhibitors

A

insecticides (organophosphates)

17
Q

Non-medical cholinesterase inhibitors

A

Insecticides: chlorpyrifos and malathion

Nerve gases: soman

18
Q

Toxicology of cholinesterase inhibitors

A

death due to asphyxia: bronchoconstriction, increased secretions, skeletal muscle paralysis, CNS depression

19
Q

What does DUMBELS stand for

A 
Diarrhea
Urination
Muscle weakness, miosis
Bronchoconstriction 
Excitation 
Lacrimation 
Seizures, sweat, salivation
20
Q

Treatment for intoxication by Achesterase inhibitors

A

atropine (no effect on skeletal muscle paralysis)
pralidoxime (no effect on CNS depression)

Initiate therapy quickly

21
Q

Malathion is specific for

A

insects and head lice (pediculosis capitis)

Pharmacology (11 decks)

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