Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

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
Q

what is the effect on the blood vessels if high dose direct-acting cholinomimetic drug is given

A

Vasoconstriction

26
Q

the effects to the detrusor

A

constriction

27
Q

the effects to trigone

A

relaxation

28
Q

the effects to the glands

A

secretion

29
Q

what are the 3 groups of cholinesterase inhibitor

*carbamic acid
*organic derivatives of phosphoric acid

A

> 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
Q

where do eDrophonium belong in cholinesterase group?

A

simple alcohol bearing quaternary ammonium

31
Q

where do neostigmine belong in cholinesterase group?

A

carbamic acid esters of alcohol

32
Q

where do organophosphate: eChothophate belongs to?

A

organic derivatives of phosphorus

33
Q

CU: Myasthenia gravis, arrythmia, ileus
D: 5-15 minutes

A

Edrophonium (simple alcohol)

34
Q

CU: Myasthenia gravis, ileus
D: .5-4 hours

A

Neostigmine ( carbamic acid esters of alcohol)

34
Q

CU: Myasthenia gravis
D: 4-6 hours

A

PYRIdostigmine (carbamic acid esters of alcohol)

35
Q

-

A
36
Q

this cholinesterase inhibitor has a clinical use for glaucoma and has action duration of 100 hours.

A

Echothiophate (organic derivative of phosphorus)

37
Q

is an extremely potent “nerve gas”

A

Sarin

38
Q

a thiocholine derivative, is of clinical value because it retains the
very long duration of action of other organophosphates

A

Echothiophate

39
Q

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

A

Parathion and Malathion

40
Q

is a large group of carbamate insecticides designed to be be highly lipid soluble

A

Carbaryl

41
Q

can be used topically in the eye

A

Physostigmine

42
Q

why organophosphate cholinesterase inhibitor is so dangerous EXCEPT echothiophate

A

as they are highly soluble to skin, lung, gut, conjunctive - and the CNS.

43
Q

the third group forms covalent _______________ bond and hydrolyzes water in a very ______.

A

the third group forms covalent phosphorus-enzyme bond and hydrolyzes water in a very slow pace.

44
Q

what is aging in the third group?

A

the breaking of one of the oxygen-phosphorus bonds of the inhibitor

hence, strengthening the phosphorus-enzyme bond.

45
Q

what is the drug called for its “cholinesterase regenerator” before aging action.

A

Pralidoxime

46
Q

where is the prominent areas cholinoesterase act?

A

cardiovascular system, gastrointestinal system, eye, skeletal muscle neuromuscular junction

47
Q

what do high concentration of cholinoesterase do the the muscle?

A

a period of contraction to rest

48
Q

is used in diagnosis myasthenia gravis

A

Edrophonium

49
Q

Pyridostigmine (short-acting, frequent dosing)

A

accompanied in the long therapy for myasthenia gravis

50
Q

Physostigmine

A

counteracts the atropine toxicity

51
Q

treatment of mild and moderate Alzheimers disease

A

Tacrine

52
Q

Donepezill, galantamine, and rivastigmine

A

newer SELECTIVE cholinesterase inhibitor with same effect and and LESS ADVERSE EFFECT.

53
Q

the predictable symptoms of direct-acting muscarinic stimulants

A

nausea, vomiting, diarrhea, urinary urgency, salivation, sweating, cutaneous vasodilation, and bronchial constriction

54
Q

what is the fatal dose of nicotine

A

40mg or 1 drop of pure nicotine

55
Q

varenicline

A

partial agonist of a4b2 nicotinic receptors

PHA 037 - PHARMACOLOGY (19 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions