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Pharmacology Exam 2 > 2 - Cholinoceptor-Activating & Cholinesterase-Inhibiting Drugs > Flashcards

2 - Cholinoceptor-Activating & Cholinesterase-Inhibiting Drugs Flashcards

1
Q

Cholinergic drugs are also known as?

A

Parasympathomimetic agents, mimic ACh actions

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2
Q

What are the 2 types of direct-acting drugs?

A

Alkaloids & Choline esters

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3
Q

What receptors do direct-acting drugs act on?

A

Muscarinic & Nicotinic receptors

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4
Q

Where are Muscarinic receptors found?

A

Nerves, Heart & smooth muscle, Glands & endothelium

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5
Q

Where are Nicotinic receptors found?

A

Neuromuscular end plate, skeletal muscle, autonomic ganglion cells

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6
Q

What are the 2 types of indirect-acting drugs?

A

Reversible & Irreversible

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7
Q

Which cholinoceptor agonist crosses the BBB?

A

Physostigmine

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8
Q

What are the 4 choline ester drugs?

A

ABCM: Acetylcholine, Bethanechol, Carbachol, Methacholine

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9
Q

What is Methacholine’s MOA?

A

Its methyl group blocks nicotinic activity

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10
Q

What is Bethanechol’s MOA?

A

Its carbamoyl group blocks hydrolysis

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11
Q

All Muscarinic receptors are ____________ receptors

A

G-protein coupled

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12
Q

What receptor activation results in electrical and ionic changes?

A

Nicotinic receptor

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13
Q

What receptor activation results in depolarization of the nerve cell or neuromuscular end plate membrane, causing a “depolarization blockade”?

A

Nicotinic receptor (abolishes the effector response)

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14
Q

What receptor activation results in prolonged agonist occupancy?

A

Nicotinic receptor

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15
Q

Which receptor activation can result in muscle paralysis?

A

Nicotinic receptor

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16
Q

What receptor activation results in activation of IP3 & DAG cascade?

A

Muscarinic receptor

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17
Q

What receptor activation results in increase of potassium flux?

A

Muscarinic receptor

18
Q

____ receptors desensitize very quickly upon excessive stimulation

A

Nicotinic

19
Q

What are the 2 classes of Cholinesterase Reversible Inhibitors?

A

Simple alcohol ester (Edrophonium) & Carbamates (pseudo-reversible)

20
Q

What is the class of Cholinesterase Irreversible Inhibitors?

A

Organophosphates

21
Q

What 2 enzymes do cholinesterase inhibitors inhibit?

A

Acetylcholinesterase (primary) & Butyrylcholinesterase

22
Q

_________ bear a quaternary ammonium group that cannot enter the CNS

A

Simple alcohols

23
Q

______ bear a quaternary ammonium group that cannot enter the CNS OR a tertiary ammonium group that CAN enter the CNS

A

Carbamic acid/Carbamate esters

24
Q

________ compete for ACh at the enzyme

A

Simple alcohols

25
Q

_______ carbamoylate the active site

A

Carbamic acid/Carbamate esters

26
Q

_______ has a tertiary ammonium group

A

Physostigmine

27
Q

_______ phosphorylate the active site

A

Organophosphates

28
Q

_______ reversibly bind to the active site

A

Quaternary alcohols

29
Q

_______ undergo a two-step hydrolysis

A

Carbamic acid/Carbamate esters

30
Q

What group causes the longest inhibition time?

A

Organophosphates

31
Q

What group causes the shortest inhibition time?

A

Quaternary alcohols

32
Q

In which 2 groups is the enzyme reactivated?

A

Carbamate esters & Organophosphates

33
Q

What organs have prominent effects from cholinesterase inhibitors?

A

Cardiovascular & GI systems, eye, skeletal muscle

34
Q

T/F: Cholinesterase inhibitors have a large effect on vascular smooth muscle & blood pressure

A

False, they have a low effect

35
Q

T/F: Cholinesterase inhibitors amplify the actions of endogenous acetylcholine

A

True

36
Q

At NMJ, what happens with low concentrations of cholinesterase inhibitors?

A

Increased force of contraction in neuromuscular junction

37
Q

At NMJ, what happens with high concentrations of cholinesterase inhibitors?

A

Depolarizing neuromuscular blockade

38
Q

Cholinesterase Inhibitors Toxicity: SLUDGE DUMBBELSS stands for?

A

Salivation, Lacrimation, Urinary incontinence, Diarrhea, GI cramps, Emesis
Diarrhea, Urination, Miosis, Bronchoconstriction, Bradycardia, Excitation/Emesis, Lacrimation, Salivation, Sweating

39
Q

Acute toxicity from cholinesterase inhibitors can be reversed by? (2)

A

Atropine (muscarinic antagonist) or pralidoxime

40
Q

M1 & M3 antagonist, used for Sjogren’s syndrome & post-radiation xerostomia (dry mouth)

A

Cevimeline

41
Q

Partial agonist of nicotine receptors, used in smoking cessation

A

Varenicline

Pharmacology Exam 2 (6 decks)

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