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Therapeutics > Cholinesterase Inhibitors > Flashcards

Cholinesterase Inhibitors Flashcards

1
Q

Cholinesterases

A

-acetylcholinesterase
-plasma cholinesterase

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2
Q

Acetylcholinesterase

A

-located in synapses
-substrate selective for ACH

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3
Q

plasma cholinesterase

A

-located in plasma
-selective for ACH, succinylcholine, local anesthetics

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4
Q

AChE

A

-highest turnover rate of any mammalian enzyme
-hydrolyze ACH 5000x/sec

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5
Q

Hydrolysis of ACh by AChE

A

-requires water
-cleaves ester
= choline + inactivated enzyme
-attack with H20 = reactivated enzyme

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6
Q

cholinesterase inhibitors

A

-anticholinesterase agents
-reversible or irreversible
-muscarinic or nicotinic effect

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7
Q

Reversible anticholinesterase agents

A

-alcohol (edrophonium)
-carbamates (physostigmine, neostigmine, pyridostigmine)
-donepezil (aricept)

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8
Q

Irreversible anticholinesterase agents

A

-organophosphates
-echothiophate (glaucoma)
-sarin (nerve gas)
-malathion (pesticide, lice)

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9
Q

Acetylcholinesterase inhibitors

A

-quarternary ammonium alcohol
-simplest structure
-bind anionic site and block ACh binding
-reversible
-non-covalent

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10
Q

Carbamates

A

-quarternary or tertiary ammonium groups
-reversible
-covalent modification to AChE
-more slowly hydrolyzed than ACh

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11
Q

Inhibition of AChE by neostigmine

A

-positive charge binds anionic site
-ester at esteratic site
slide 21

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12
Q

Therapuetic AChE inhibitors

A

-inhibit AChE
-noncovalent reversible
-endorphonium
-pyridostigmine
-neostigmine

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13
Q

edorphonium

A

-very short acting
-diagnosis fo myathenia gravis (skeletal muscle weakness)

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14
Q

pyridostigmine

A

-used in treatment of MG
-reversal of nondepolarizing neuromuscular blockade
-pretreatment for potential nerve gas exposure (occupy AChE so nerve gas has nowhere to go)

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15
Q

neostigmine

A

-used for MG, reversal of nondepolarizing neuromuscular bloackade
-post-op urinary retention

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16
Q

Physostigmine

A

-inhibt AChE
-CAN cross BBB
-antidote to antimuscarinic poisoning

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17
Q

Problems with therapeutic AChE inhibitors

A

excessive cholinergic receptor activation

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18
Q

Isofluorophate and echothiophate (Organophosphates)

A

-irreversible
-covalent modification of AChE
-longer acting
-used in treatment of glaucoma
-most are TOXIC

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19
Q

Echothiophate

A

-therapeutic organophosphate AChE inhibitor
-long acting
-essential irreversible

20
Q

echothiopate clinical use

A

-originally for glaucoma
-better drugs now tho

21
Q

problems with organophosphate AChE inhibitor therapeutics

A

-excessive cholinergic receptor activation
-including miosis

22
Q

Sarin and Soman AChE inhibitors

A

-nerve gasses
-irreversible
-covalent modification to AChE

23
Q

Malathion and diazinon (organophophates)

A

-insecticides
-irreversible
-covalent
-rapidly inactivated in mammals

24
Q

Biotransformation of MALATHION

A

-Cyt P450 in insects to malaoxon
-carboxyesterase in mammals and birds to inactivate it

25
Q

Pralidoxamine Chloride

A

-antidote for pesticide or nerve gas poisoning (AChE poisoning)
-most effective if given within few hours of exposure

26
Q

Regeneration of AChE by Pralidoxime

A

-before aging occurs
-attack phosphate and release phosphate
-slide 37

27
Q

Pralidoxime (2-PAM)

A

-AChE inhibitor antiddote)
-hydrolyze organophosphate if treated before aging occurs
-regenerate AChE
-does not cross BBB

28
Q

Atropine

A

-block access to muscarinic receptor (ANTAGONIST)
-CANT BLOCK ACTION AT NICOTINIC RECEPTORS

29
Q

slide 39

A

slide 39

30
Q

Alzheimer’s disease

A

-atrophy of brain
-widening of sulci and thinning of gyri
-improper processing of B-amyloid precursor protein leads to toxic form that promotes apoptosis
-plaques and tangles
-loss of cholinergic neurons in brain

31
Q

Drugs to treat alzheimers

A

-donepezil
-rivastigmine
-galantamine
-memantine

32
Q

Donepezil

A

-bind to anionic site
-block ACh binding
-reversible
-non-covalent
-enhance cognitive ability
-does not slow progression

33
Q

Rivastigmine (exelon)

A

-reversible carbamate AChe inhibitor
-enhance cognitive ability by increasing cholinergic function
-lose effectiveness as disease progresses
-nausea, vomiting, anorexia
-new and better one: epastigmine

34
Q

Galantamine

A

-reversible competitive AChE inhibitor
-extract from daffodil bulbs
-lose effectiveness as disease progresses
-may be nicotinic receptor agonist
-inhibitors of P450 enzymes will increase galantamine bioavailability

35
Q

Mematine

A

-NMDA receptor antagonist
-NDMA receptors activated by glutamate in CNS
-maybe too much glutamate?
-glutamate regulators improve condition
-may slow progression of disease
-moderate to severe
-favorable adverse effect profile

36
Q

Slide 45 review

A

slide 45 review

37
Q

Cholinergic Agonist side effects

A

-DUMBBELS
-use caution in pateints with asthma, coronary insufficiency, peptic ulcer
-cardiovascular and respiratory

38
Q

Cholinergic side effects

A

-SLUD
-Salivation
-Lacrimation
-Urination
-Defecation
-also:
-increased sweating
-decreased heartrate
-pupils constrict
-CNS activation

39
Q

Astma and COPD contraindications to PSNS drugs

A

increase bronchoconstriction

40
Q

Coronary defeciency contraindications to PSNS drugs

A

further lower heart rate

41
Q

peptic ulcer contraindications to PSNS drugs

A

would increase acid secretion

42
Q

obstruction of the urinary/ GI tract contraindications to PSNS drugs

A

if increased contraction does not remove obstruction

43
Q

Epilepsy contraindications to PSNS drugs

A

-M1Rs
-CNS penetrable drugs (pilocarpine, physostigmine)

44
Q

Cholinergic receptor antagonist treatment

A

Atropine

45
Q

reversible AChE inhibitor treatment

A

2-PAM (pralidoxime)

Therapeutics (78 decks)

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