Brainscape's Knowledge GenomeTM

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


See full index

Pharmacology > 7 > Flashcards

7 Flashcards

1
Q

Cholinergic Receptors Come in Two Types:

A

Nicotinic and Muscarinic

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

Nicotinic AcCHRs

A
  1. Bind nicotine
  2. Ligand activated ion channel (local depolarization at post synaptic membrane due to Na+ influx)
  3. Receptors contain 5 subunits and bind two molecules of agonist
  4. Skeletal muscle nACCh R molecular biology fairly simple.
  5. CNS ACCh R molecular biology complicated.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Muscarinic AcCHRs

A
  1. Bind muscarine
  2. G protein coupled receptors (really neuromodulators)
  3. There are 5 different muscarinic receptors (M1 through M5). M1 through M4 are better appreciated than M5.
  4. M1, M3, M5 are linked to Gaq (Activate DAG and IP3 signaling). M2 and M4 are linked to Gai (inhibit adenylate cyclase).
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Can usually figure out whether an aceylcholine receptor is of the nicotinic or muscarinic type by asking whether we want to

A

depolarize across a membrane (nicotinic) or activate a G protein coupled receptor (muscarini

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

Cholinergic agonists

Direct Acting:

A

bind to muscarinic or nicotinic AcCh receptor or both

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

Cholinergic agonists

Indirect acting:

A

cholinesterase inhibitor

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

-zosin

A

drug is alpha 1 adrenergic receptor blocker

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

-olol

A

beta adrenergic receptblocker

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

-ilol, -alol

A

beta andrenergic blocker with alpha 1 activity

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

Acetylcholine: hydrolyzed

A

rapidly, shortest duration of action

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

Methacholine: hydrolyzed

A

slower, somewhat longer duration of action

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

Carbachol*, bethanechol, cevimeline, alkaloids: not

A

hydrolyzed, longer duration of action

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

Carbachol: favors ——— receptors

A

nicotinic

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

Methacholine, bethanechol, muscarine, cevimeline, pilocarpine: ——- selective

A

muscarinic

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

Muscarinic agonists much more

A

clinically relevant

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

Neuromuscular transmission

A
  1. Activation of nicotinic AcCh Receptors depolarizes post-synaptic membrane 2. Local depolarization leads to action potential
  2. Post-synaptic depolarization leads to release of Ca++ from the sarcoplasmic reticulum
  3. Release of Ca++ from the sarcoplasmic reticulum leads to muscle contraction
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Odd numbered muscarinic receptors activate

A

phospholipase C and promote Ca++release

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

Even numbered muscarinic receptors inhibit

A

adenylcyclase

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

M3 muscarinic receptors on the sphincter muscle mediate

A

pupil contraction.

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

M3 receptors on ciliary muscle also mediate

A

muscle contraction. This increases drainage by the trabecular network and reduces ocular pressure.

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

Cardiac muscle contains M2 receptors and parasympathetic innervation. Activation of these receptors reduce

A

cardiac output

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

Most arteries and veins in the body are innervated by

A

sympathetic adrenergic nerves

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

Some blood vessels are innervated by

A

parasympathetic cholinergic or sympathetic cholinergic nerves.
These nerves release acetylcholine as their neurotransmitter. Coronary arteries are a prominent example.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

vascular endothelial cells express —- receptors. Activation of these receptors produce ———–

A

M3

vasodilation

25
Q

Activation of M3 receptors increase

A

Ca++ in endothelial cells

26
Q
  1. Ca++/calmodulin activates
A

NOS to produce NO.

27
Q
  1. NO travels to the smooth muscle cell, enhances —– production, leading to
A

cGMP

muscle relaxation (enhances myosin light chain phosphatase activity).

28
Q

M3 muscarinic receptors on the bronchial muscle mediate

A

muscle contraction.

29
Q

Gastrointestinal Effects Mostly, ————–. However sphincter muscle

A

contractile responses

M2 mediated) relaxes.

30
Q

Secretory Glands

A

(M3 receptor)

Ca++ stimulates release of glandular contents from secretory glands (including salivary glands)

31
Q

M3 muscarinic receptors mediate

A

detrusor muscle contraction. Aids in voiding the bladder

32
Q

Increased risk of adverse response to muscarinic agonists:

A

Patients with asthma (bronchoconstriction), Cardiovascular disease (vasodilation, reduced cardiac output), ulcer (lacrimation

33
Q

SLUD response:

A

Salivation, Lacrimation, Urination, Defecation

34
Q

Muscarinic agonists:

Intravenous, intramuscular routes generally

A

avoided (because of cardiopulmonary effects).

Topical routes favored, if possible

35
Q

Acetylcholinesterase drugs actby

A

inhibiting acetylcholinesterase, which increases acetylcholine in synapse

36
Q

Some “reversible” anticholinesterases are slowly hydrolyzed by

A

cholinesterase

37
Q

Some anticholinesterases act in

A

a rapidly reversible manner (they are not hydrolyzed at all). Only used to kill stuff.

38
Q
  1. In general anticholinesterases produce effects that are similar to the
A

direct acting cholinergic agonists.

In effect, increase the concentration of acetylcholine at effector site.

39
Q

The greater the cholinergic stimulation at the site, the

A

greater the effect.

Smooth muscle of ocular system, GI tract, urinary bladder major sites.

40
Q

. Anticholinesterases do not produce

A

muscarinic receptor mediated vasodilation (Why not).

Not much parasympathetic innervation of vascular endothelium.

41
Q

anticholinesterases Can also produce———— through ———–.
Initially prolong duration and then promote desensitization of nAcCH R (will get to this later).

A

vasodilatory effects

autonomic ganglia

42
Q

Physostigmine (tertiary amine) can produce

A

vasodilatory effects through action in the CNS.

43
Q

Anticholinesterases used to terminate the

A

neuromuscular block of curare-like agents (coming soon) in general anesthesia.

44
Q

Anticholinerases that cross the blood brain barrier (donepezil, rivastigmine, galantamine) are used to improve

A

cognitive function in Alzheimer’s patients.

45
Q

In general, treatment with an anti-muscarinic drug places the target under control by the

A

sympathetic nervous system

46
Q

sweat gland , where signals from the

A

sympathetic and parasympathetic systems act upon muscarinic receptors at the target and are both blocked by the anti-msucarinic.

47
Q

Anti-muscarinics will cause

A

pupil dilation and paralysis of accommodation*. Intraocular pressure not significantly affected except in the case of narrow angle glaucoma, in which anti-muscarinics could cause a serious rise in pressure.

48
Q

Anti-muscarinics are used to produce

A

bronchodilation and diminish mucus production to treat COPD.

49
Q

Anti-muscarinics inhibit

A

Anti-muscarinics inhibit sweating and can elevate body temperature.

50
Q

Anti-muscarinics generally inhibit ——–. Only inhibit gastric secretions at

A

Anti-muscarinics generally inhibit motility. Only inhibit gastric secretions at very high concentrations (not useful).

51
Q

Anti-muscarinics block

A

parasympathetic mediated secretion.

52
Q

Therapeutic Uses of Anti-muscarinics

A
  1. Dilate pupils for opthalmologic procedures.
  2. Treatment of COPD (quarternary amines, administered by inhalation)
  3. Diminish salivary secretion before oral procedures
  4. Anti-spasmodics, and anti-ulcer agents (not very useful because of side effects)*.
  5. Antidote to anti-cholinesterases
53
Q

Transmission of sympathetic and parasympathetic nerve impulses mediated by

A

nicotinic AcCh receptors

54
Q

Nicotinic AcCh receptors are important mediators in the

A

Nicotinic AcCh receptors are important mediators in the CNS

55
Q

Post synaptic transmission of nerve impulse at skeletal muscle mediated by

A

nicotinic AcCh receptors

56
Q

Ganglionic AcCh blockers

A

Ganglionic blockers rarely used: too many side effects.

57
Q

Ganglionic AcCh blockers

A

Ganglionic blockers rarely used: too many side effects.

58
Q

Post synaptic transmission of nerve impulse at skeletal muscle mediated by

A

nicotinic AcCh receptors

Pharmacology (19 decks)

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