Anticholinesterases Flashcards

1
Q

What is cholinesterase?

A

enzyme that hydrolyse ACh to acetyl and choline

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2
Q

Name the 2 types of cholinesterases?

A

acetylcholinesterase (ACHE) and butyrylcholinesterase (BCHE)

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3
Q

Anticholinesterase is directly acting cholinergic drug. T/F

A

F. Indirectly acting

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4
Q

Examples of reversible anticholinesterase

A

Edrophonium , Pyridostigmine, Physostigmine

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5
Q

What is the drug name for irreversible anticholinesterase?

A

Ecothiopate

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6
Q

Why neostigmine cannot cross BBB?

A

Has quaternary ammonium group; lipid insoluble

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7
Q

Why physostigmine can cross BBB?

A

Has carbamate group but no quaternary ammonium group; lipid soluble thus can cross BBB

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8
Q

Why pyridostigmine is quite similar to neostigmine?

A

The chemical structure is similar except the quaternary amm group is incorporated into phenol ring

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9
Q

What drug is used to diagnose myasthenia gravis?

A

Edrophonium

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10
Q

What drug is used to reverse competitive neuromuscular block?

A

Neostigmine (IV)

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11
Q

What drug is used to manage myasthenia gravis?

A

Neostigmine and pyridostigmine (oral)

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12
Q

What happen if cholinergic receptors are overstimulated?

A

DUMBBELLS

Diarrhea, urination, miosis, bradycardia, bronchorrhea, emesis, lacrimation, salivation/sweating

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13
Q

What drug is used to treat paralytic ileus and atony of bladder?

A

Neostigmine

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14
Q

Why ecothiopate is used to treat glaucoma?

A

Stimulate muscarinic receptor and constrict the sphinter pupillae and ciliary muscle = miosis

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15
Q

What is the muscarinic side effects of anticholinesterase?

A

SLUDGE

Salivation, lacrimation, diaphoresis, GI upset, emesis

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16
Q

What is nicotinic s/e of anticholinesterase?

A

muscle fasciculation –> weakness –> paralysis

17
Q

What is the antidote for anticholinesterase toxicity?

A

Atropine and pralidoxime

18
Q

How atropine works to treat anticholinesterase toxicity?

A

by inhibiting muscarinic receptors

19
Q

How pralidoxime treat organophosphate poisoning?

A

A nucleophilic agent that re-activate the phosphorylated esteratic site of AChE by exerting nucleophilic attack on the phosphorus