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PHRM 825 > ANS-4 > Flashcards

ANS-4 Flashcards

(64 cards)

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1
Q

What are the 2 types of cholinesterases

A

acetylcholinesterase and plasma cholinesterase

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2
Q

Acetylcholinesterases are located in _____

A

synapses

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3
Q

Plasma cholinesterases are located in ____

A

plasma (non-neuronal)

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4
Q

Acetylcholinesterases are selective for the transmitter ____

A

ACh

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5
Q

Plasma Cholinesterases are selective for ____, ______, and ______

A
  • ACh
  • succinylcholine
  • local anesthetics (procaine)
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6
Q

T or F: Plasma cholinesterases are more selective than acetylcholinesterases

A

False

Acetylcholinesterases are more selective (only ACh)

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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

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8
Q

What molecule is required to reactivate AChE?

A

H2O

nucleophilic attack

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9
Q

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

A
  • Ser203
  • His440
  • Glu327
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10
Q

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

A

Phe338 and Trp86

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11
Q

ACh is hydrolyzed into what?

A

acetic acid and choline

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12
Q

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

A

Edrophonium

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13
Q

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

A
  • Physostigmine
  • Neostigmine
  • Pyridostigmine
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14
Q

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

A

Donepezil (Aricept)

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15
Q

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

A
  • Echothiophate (used in glaucoma)
  • Sarin (nerve gas/chemical warfare)
  • Malathion (pesticide; head lice)
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16
Q

AChE inhibitor: Tetra-alkylammonium
Ion Characteristics

A
  • Simplest structures
  • Bind to anionic site and block ACh
  • Reversible
  • Non-covalent (no ester)
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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

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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

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19
Q

What is this?

A

Edrophoium (Tensilon)

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20
Q

What is this?

A

Neostigmine (Prostigmin)

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21
Q

What is this?

A

Pyridostigmine (Mestinon)

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22
Q

What is this?

A

Physostigmine (Antilirium)

Not intrinsically positive. Protonated at physiological pH.

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23
Q

T or F: reversible means non-covalent

A

False

covalent modification to AChE can occur AND be reversible

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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

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25
Clinical Use: Pyridostigmine - Used in **treatment** of ____ by reversing ______________, pretreatment for potential ______ exposure (occupy AChE so that it has nowhere to go)
MG, nondepolarazing neuromuscular blockade, nerve gas
26
Clinical Use: Neostigmine -Used for ____, reversal of _____, post-op _____ retention
MG, nondepolarizing neuromuscular blockade, urinary
27
What is the problem with AChE Inhibitors?
Excessive cholinergic receptor activation | ACh not broken down, so more receptor activation
28
Clinical Use: Physostigmine - Can cross ___: Antidote to ___ poisoning
BBB, antimuscarinic
29
Clinical Use: Physostigmine - Can cross ___: Antidote to ___ poisoning
BBB, antimuscarinic
30
T or F: Stigmines are hydrolyzed faster than ACh
False | Stigmines are hydrolyzed more slowly due to covalent bond
31
AChE Inhibitor: Organophosphates (Glaucoma) Characteristics
Examples: Isofluorophate; DFP (Floropryl), Echothiophate (Phospholine Iodine) * irreversible * covalent modification to AChE * longer acting
32
AChE Inhibitor: Organophosphates (Nerve Gases) Characteristics
Examples: Sarin and Soman * irreversible * covalent modification to AChE
33
T or F: Most organophosphates are TOXIC
True
34
AChE Inhibitor: Organophosphates (Insecticides) Characteristics
Examples: Malathion, Diazinon * irreversible * covalent modification to AChE * rapidly inactivated in mammals
35
How do insecticides (Malathion and Diazinon) not harm mammals?
Insects have a specific Cyt P450 that converts Malathion into toxic Malaoxon. Mammals metabolize Malathion into an inactive compound.
36
Organophosphate mechanism
P forms a super stable covalent bond with Ser203. Aging then occurs (irreversible and cannot be detoxified)
37
What is this?
Isofluorophate; DFP (Floropryl)
38
What is this?
Echothiophate (Phospholine Iodine)
39
What is this?
Sarin
40
What is this?
Soman
41
What is this?
Malathion
42
What is this?
Diazinon
43
What is the antidote for AChE poisioning (pesticide and nerve gas)
Pralidoxime Chloride | strong nucleophile
44
T or F: Pralidoxime must be administered before aging occurs (within a few hours of exposure)
True | once aging occurs, damage is irreversible.
45
What is this?
Pralidoxime Chloride
46
Because Pralidoxime Chloride cannot cross the BBB, it should be administered with ___ because....
Atropine; a muscarinic receptor antagonist that can cross the BBB. Blocks muscarinic receptor activity caused by excess ACh
47
Alzheimer's Disease is due to...
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
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
Anionic, ACh, cognitive
49
T or F: Donepezil slows the progression of Alzheimer's disease
False
50
What is this?
Donepezil (Aricept)
51
Alzheimer's: Mechanism of Rivastigmine (Exelon) - Reversible ____ AChE inhibitor. Enhances cognitive ability by increasing ___ function.
Carbamate, cholinergic
52
T or F: Rivastigmine loses effectiveness as Alzheimer's progresses
True
53
What are the side effects of Rivastigmine?
* nausea * vomiting * anorexia * weight loss
54
What is this?
Rivastigmine (Exelon)
55
Alzheimer's: Mechanism Galantamine (Razadyne) - Reversible ___ AChE inhibitor. Extracted from ___. May be a ___ receptor agonist. Inhibitors of Cyp ___ and ___ will increase Galantamine bioavailability.
competitive, daffodil, nicotinic, 3A4, 2D6
56
T or F: Galantamine may slow the progression of Alzheimer's
False | Like Rivastigmine, it loses effectiveness as Alzheimer's progresses
57
What is this?
Galantamine (Razadyne)
58
Alzheimer's: Memantine Mechanism - ___ receptor antagonist. These receptors are activated by ___ in the CNS in areas associated with cognition and memory.
N-methyl-D-aspartate (NDMA), glutamate
59
T or F: Memantine may slow the progression of Alzheimer's
True
60
T or F: Neuronal loss in Alzheimer's may be related to increased activity of glutamate
True
61
Because Memantine is NOT ___, it has a favorable adverse effect profile
cholinergic
62
What is this?
Memantine (Namenda)
63
What are side effects assoicated with cholinergic agonists? Hint: DUMBBELSS
diarrhea, urination, miosis, bradycardia, bronchoconstriction, emesis, lacrimation, salivation, sweating (SNS)
64
Contraindications to the use of parasympathomimetic drugs
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)

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