Brainscape's Knowledge GenomeTM

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


See full index

PHRM 825 > ANS-4 > Flashcards

ANS-4 Flashcards

1
Q

What are the 2 types of cholinesterases

A

acetylcholinesterase and plasma cholinesterase

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

Acetylcholinesterases are located in _____

A

synapses

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

Plasma cholinesterases are located in ____

A

plasma (non-neuronal)

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

Acetylcholinesterases are selective for the transmitter ____

A

ACh

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

Plasma Cholinesterases are selective for ____, ______, and ______

A
  • ACh
  • succinylcholine
  • local anesthetics (procaine)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

T or F: Plasma cholinesterases are more selective than acetylcholinesterases

A

False

Acetylcholinesterases are more selective (only ACh)

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

Why is AChE really cool?

A

it has the highest turnover rate out of all enzymes

hydrolyzes ACh 5,000 times per second

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

What molecule is required to reactivate AChE?

A

H2O

nucleophilic attack

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

Hydrolysis of ACh: What 3 amino acids form the catalytic triad (esteric site)?

A
  • Ser203
  • His440
  • Glu327
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Hydrolysis of ACh: What amino acids form the anionic site?

A

Phe338 and Trp86

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

ACh is hydrolyzed into what?

A

acetic acid and choline

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

AChE Agents: Indirectly-Acting Cholinoceptor Stimulants -
Reversible (Alcohol)

A

Edrophonium

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

AChE Agents: Indirectly-Acting Cholinoceptor Stimulants - Reversible (Carbamates)

A
  • Physostigmine
  • Neostigmine
  • Pyridostigmine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

AChE Agents: Indirectly-Acting Cholinoceptor Stimulants - Reversible (hope you didn’t forget lol)

A

Donepezil (Aricept)

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

AChE Agents: Indirectly-Acting Cholinoceptor Stimulants - Irreversible (Organophosphates)

A
  • Echothiophate (used in glaucoma)
  • Sarin (nerve gas/chemical warfare)
  • Malathion (pesticide; head lice)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

AChE inhibitor: Tetra-alkylammonium
Ion Characteristics

A
  • Simplest structures
  • Bind to anionic site and block ACh
  • Reversible
  • Non-covalent (no ester)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

AChE inhibitor: Alcohol Characteristics

A

Example: Edrophoium (Tensilon)
* quaternary ammonium alcohol
* simplest structures
* bind to anionic site and block ACh
* reversible
* non-covalent

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

AChE inhibitors: Carbamates Characteristics

A

Examples: Neostigmine (Prostigmin), Pyridostigmine (Mestinon), Physostigmine (Antilirium)
* Quarternary or tertiary ammonium groups
* reversible
* covalent modifcation to AChE (Ser203)
* hydrolyzed slower than ACh

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

What is this?

A

Edrophoium (Tensilon)

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

What is this?

A

Neostigmine (Prostigmin)

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

What is this?

A

Pyridostigmine (Mestinon)

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

What is this?

A

Physostigmine (Antilirium)

Not intrinsically positive. Protonated at physiological pH.

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

T or F: reversible means non-covalent

A

False

covalent modification to AChE can occur AND be reversible

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

Clinical Use: Edrophonium - Time: ____-acting (unit?); diagnosis of _____

A

Short-acting (minutes), Myasthenia Gravis (MG)

MG - skeletal muscle weakness due to loss of Nm receptors because of autoimmune disease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Clinical Use: Pyridostigmine - Used in treatment of ____ by reversing ______________,
pretreatment for potential ______ exposure (occupy AChE so that it has nowhere to go)

A

MG, nondepolarazing neuromuscular blockade, nerve gas

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Clinical Use: Neostigmine -Used for ____, reversal of _____, post-op _____ retention

A

MG, nondepolarizing neuromuscular blockade, urinary

27
Q

What is the problem with AChE Inhibitors?

A

Excessive cholinergic receptor activation

ACh not broken down, so more receptor activation

28
Q

Clinical Use: Physostigmine - Can cross ___: Antidote to ___
poisoning

A

BBB, antimuscarinic

29
Q

Clinical Use: Physostigmine - Can cross ___: Antidote to ___
poisoning

A

BBB, antimuscarinic

30
Q

T or F: Stigmines are hydrolyzed faster than ACh

A

False

Stigmines are hydrolyzed more slowly due to covalent bond

31
Q

AChE Inhibitor: Organophosphates (Glaucoma) Characteristics

A

Examples: Isofluorophate; DFP (Floropryl), Echothiophate (Phospholine Iodine)
* irreversible
* covalent modification to AChE
* longer acting

32
Q

AChE Inhibitor: Organophosphates (Nerve Gases) Characteristics

A

Examples: Sarin and Soman
* irreversible
* covalent modification to AChE

33
Q

T or F: Most organophosphates are TOXIC

A

True

34
Q

AChE Inhibitor: Organophosphates (Insecticides) Characteristics

A

Examples: Malathion, Diazinon
* irreversible
* covalent modification to AChE
* rapidly inactivated in mammals

35
Q

How do insecticides (Malathion and Diazinon) not harm mammals?

A

Insects have a specific Cyt P450 that converts Malathion into toxic Malaoxon. Mammals metabolize Malathion into an inactive compound.

36
Q

Organophosphate mechanism

A

P forms a super stable covalent bond with Ser203. Aging then occurs (irreversible and cannot be detoxified)

37
Q

What is this?

A

Isofluorophate; DFP (Floropryl)

38
Q

What is this?

A

Echothiophate (Phospholine Iodine)

39
Q

What is this?

A

Sarin

40
Q

What is this?

A

Soman

41
Q

What is this?

A

Malathion

42
Q

What is this?

A

Diazinon

43
Q

What is the antidote for AChE poisioning (pesticide and nerve gas)

A

Pralidoxime Chloride

strong nucleophile

44
Q

T or F: Pralidoxime must be administered before aging occurs (within a few hours of exposure)

A

True

once aging occurs, damage is irreversible.

45
Q

What is this?

A

Pralidoxime Chloride

46
Q

Because Pralidoxime Chloride cannot cross the BBB, it should be administered with ___ because….

A

Atropine; a muscarinic receptor antagonist that can cross the BBB. Blocks muscarinic receptor activity caused by excess ACh

47
Q

Alzheimer’s Disease is due to…

A

Loss of cholinergic neurons in the brain caused by improper processing of B- amyloid precursor protein (B-APP) leading to toxic form (B-A42) that promotes apoptosis.

48
Q

Alzheimer’s: Mechansim of Donepezil (Aricept) - Reversibly and non-covalently binds to ___ site on AChE and blocks ___ binding. Enhances ____ ability. Approved for all stages of Alzheimers

A

Anionic, ACh, cognitive

49
Q

T or F: Donepezil slows the progression of Alzheimer’s disease

A

False

50
Q

What is this?

A

Donepezil (Aricept)

51
Q

Alzheimer’s: Mechanism of Rivastigmine (Exelon) - Reversible ____ AChE inhibitor. Enhances cognitive ability by increasing ___ function.

A

Carbamate, cholinergic

52
Q

T or F: Rivastigmine loses effectiveness as Alzheimer’s progresses

A

True

53
Q

What are the side effects of Rivastigmine?

A
  • nausea
  • vomiting
  • anorexia
  • weight loss
54
Q

What is this?

A

Rivastigmine (Exelon)

55
Q

Alzheimer’s: Mechanism Galantamine (Razadyne) - Reversible ___ AChE inhibitor. Extracted from ___. May be a ___ receptor agonist. Inhibitors of Cyp ___ and ___ will increase Galantamine bioavailability.

A

competitive, daffodil, nicotinic, 3A4, 2D6

56
Q

T or F: Galantamine may slow the progression of Alzheimer’s

A

False

Like Rivastigmine, it loses effectiveness as Alzheimer’s progresses

57
Q

What is this?

A

Galantamine (Razadyne)

58
Q

Alzheimer’s: Memantine Mechanism - ___ receptor antagonist. These receptors are activated by ___ in the CNS in areas associated with cognition and memory.

A

N-methyl-D-aspartate (NDMA), glutamate

59
Q

T or F: Memantine may slow the progression of Alzheimer’s

A

True

60
Q

T or F: Neuronal loss in Alzheimer’s may be related to increased activity of glutamate

A

True

61
Q

Because Memantine is NOT ___, it has a favorable adverse effect profile

A

cholinergic

62
Q

What is this?

A

Memantine (Namenda)

63
Q

What are side effects assoicated with cholinergic agonists? Hint: DUMBBELSS

A

diarrhea, urination, miosis, bradycardia, bronchoconstriction, emesis, lacrimation, salivation, sweating (SNS)

64
Q

Contraindications to the use of parasympathomimetic drugs

A

asthma and COPD (bronchoconstriction), coronary deficiency (further lowers HR), peptic ulcer (increases acid secretion), obstruction of urinary or GI tract (contraction does not remove obstruction), and epilepsy (M1)

PHRM 825 (49 decks)

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