Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

PHA 037 - PHARMACOLOGY > SAS 9: Cholinoceptor-activating & cholinesterase-inhibiting drugs > Flashcards

SAS 9: Cholinoceptor-activating & cholinesterase-inhibiting drugs Flashcards

1
Q

What caused acetylcholine?

A

Cholinomimetics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Mimics the effects of parasympathetic
nerve discharge

A

Muscarine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is the effects of parasympathetic called?

A

Parasympathomimetic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

At low concentrations of the alkaloid stimulates autonomic ganglia and skeletal muscle neuromuscular junctions BUT NOT AUTONOMIC EFFECTOR CELLS.

A

Nicotine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What type of receptors is Cholinoceptors?

A

G-protein coupled receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is the MOA of direct-acting cholinomimetic drugs?

A

Activates muscarinic and nicotinic receptors through binding

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is the MOA of indirect-acting cholinomimetic drugs?

A

Inhibits acetylcholinesterase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What are the two direct-acting cholinomimetic drugs?

A

> esters of choline
alkaloids

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Choline esters are ____________ and __________ into CNS because they are hydrophilic

A

poorly absorbed and poorly distributed

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Acetylcholine is very rapidly hydrolyzed hence it must be administered as

A

parentally

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What are the four choline esters (quaternary ammonium structure)?

A

Acetylcholine
Methacholine
Carbachol
Bethanechol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

This 2 B-methyl group reduces the potency of the choline esters at nicotinic receptors

A

Methacholine and bethanechol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

a liquid, is sufficiently lipid-soluble to be absorbed across the skin

A

Nicotine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

A plant derivative similar to Nicotine

A

Lobeline

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Nicotine, Muscarine, and Lobeline are natural cholinomimetic alkaloids that are easily ____ and excreted chiefly by the ______

A

easily absorbed, excreted chiefly by the kidney

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are the pharmacodynamics of Acetylcholine?
/what are the steps to set effect and stop production of acetylcholine?

A

> adhering to its post-ganglion
adhering to its pre-ganglion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

It activates IP3 and DAG by adhering to these muscarinic receptors?

A

by adhering to M1, M3, M5 receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

DAG’s role to cholinergic transmission

A

stimulates opening of smooth muscle calcium channels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

IP3’s role to cholinergic transmission

A

releases calcium from endoplasmic and sarcoplasmic reticulum

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

It inhibits adenylyl cyclase activity by activation of these muscarinic receptors

A

M2,M4

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

activation of this receptor causes depolarization of the nerve cell or neuromuscular end plate membrane

A

Nicotinic receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What is the effect of cholinomimetics to eye sphincter muscle?

A

Miosis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

this relates to the effect to the eye, the contraction for near vision

A

accommodation

24
Q

what is the effect on the blood vessels if cholinomimetic drug is administered via EDRF

A

vasodilation

25
what is the effect on the blood vessels if high dose direct-acting cholinomimetic drug is given
Vasoconstriction
26
the effects to the detrusor
constriction
27
the effects to trigone
relaxation
28
the effects to the glands
secretion
29
what are the 3 groups of cholinesterase inhibitor *carbamic acid *organic derivatives of phosphoric acid
> simple alcohols bearing quaternary ammonium (reversible) > Carbamic acid esters of alcohol with quaternary or tertiary ammonium groups (2 way, reversible) > Organic derivatives of phosphoric acid (2 way, irreversible)
30
where do eDrophonium belong in cholinesterase group?
simple alcohol bearing quaternary ammonium
31
where do neostigmine belong in cholinesterase group?
carbamic acid esters of alcohol
32
where do organophosphate: eChothophate belongs to?
organic derivatives of phosphorus
33
CU: Myasthenia gravis, arrythmia, ileus D: 5-15 minutes
Edrophonium (simple alcohol)
34
CU: Myasthenia gravis, ileus D: .5-4 hours
Neostigmine ( carbamic acid esters of alcohol)
34
CU: Myasthenia gravis D: 4-6 hours
PYRIdostigmine (carbamic acid esters of alcohol)
35
-
36
this cholinesterase inhibitor has a clinical use for glaucoma and has action duration of 100 hours.
Echothiophate (organic derivative of phosphorus)
37
is an extremely potent "nerve gas"
Sarin
38
a thiocholine derivative, is of clinical value because it retains the very long duration of action of other organophosphates
Echothiophate
39
is a thiophosphate prodrug that is inactive as such; they are converted to the phosphate derivatives in animals and plants and are used as insecticides
Parathion and Malathion
40
is a large group of carbamate insecticides designed to be be highly lipid soluble
Carbaryl
41
can be used topically in the eye
Physostigmine
42
why organophosphate cholinesterase inhibitor is so dangerous EXCEPT echothiophate
as they are highly soluble to skin, lung, gut, conjunctive - and the CNS.
43
the third group forms covalent _______________ bond and hydrolyzes water in a very ______.
the third group forms covalent phosphorus-enzyme bond and hydrolyzes water in a very slow pace.
44
what is aging in the third group?
the breaking of one of the oxygen-phosphorus bonds of the inhibitor hence, strengthening the phosphorus-enzyme bond.
45
what is the drug called for its "cholinesterase regenerator" before aging action.
Pralidoxime
46
where is the prominent areas cholinoesterase act?
cardiovascular system, gastrointestinal system, eye, skeletal muscle neuromuscular junction
47
what do high concentration of cholinoesterase do the the muscle?
a period of contraction to rest
48
is used in diagnosis myasthenia gravis
Edrophonium
49
Pyridostigmine (short-acting, frequent dosing)
accompanied in the long therapy for myasthenia gravis
50
Physostigmine
counteracts the atropine toxicity
51
treatment of mild and moderate Alzheimers disease
Tacrine
52
Donepezill, galantamine, and rivastigmine
newer SELECTIVE cholinesterase inhibitor with same effect and and LESS ADVERSE EFFECT.
53
the predictable symptoms of direct-acting muscarinic stimulants
nausea, vomiting, diarrhea, urinary urgency, salivation, sweating, cutaneous vasodilation, and bronchial constriction
54
what is the fatal dose of nicotine
40mg or 1 drop of pure nicotine
55
varenicline
partial agonist of a4b2 nicotinic receptors

PHA 037 - PHARMACOLOGY (19 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions