Exam 1 Cholinergic Drugs Flashcards

1
Q

Muscarinic agonist drug classes

A

-choline esters
-alkaloids

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2
Q

Muscarinic agonist drugs

A

-Ach
-Methacholine
-Carbachol
-Bethanechol
-muscarine
-pilocarpine

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3
Q

Indirect cholinergic agonists

A

-endorphonium
-physostigmine
-neostigmine
-organophosphates

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4
Q

Choline esters (M agonists)

A

-Ach
-methacholine
-carbochol
-bethanechol

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5
Q

Methacholine structure

A

-Ach with B substitution
-reduced N selectivity
-more AChE resistant

-cholinergic

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6
Q

Carbachol structure

A

-carbamate group instead of acetyl
-resistant to AChE
-active at both N and M receptors

-cholinergic

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7
Q

Methacholine use

A

-test for hyperactive airways

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8
Q

Carbachol use

A

occular

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9
Q

Bethanechol structure

A

-carbamate AND B substitution
-NO effect on N receptor

-cholinergic

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10
Q

Bethanechol use

A

-GI stimulation
-urinary retention

-cholinergic

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11
Q

Alkaloids

A

-muscarine
-pilocarpine

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12
Q

Muscarine effect

A

-BRADYcardia
-nausea, cramps
-bronchoCONSTRICTION
-salivation
-visual disturbances

-sweating
-hypotension

-cholinergic

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13
Q

Pilocarpine effect

A

-promote sweating, salivation, urination

-cholinergic

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14
Q

Pilocarpine use

A

-glaucoma
-xerostomia (dry mouth)
-sjorgen’s syndrome (not enough saliva)

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15
Q

Glaucoma containdication

A

-antimuscarinic drugs

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16
Q

Side effects of cholinergics

A

-DUMBBELSS
-diarrhea
-urination
-miosis
-BRADYcardia
-BronchoCONSTRICTION
-Lacrimation
-Salivation + Sweating

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17
Q

Cholinergics caution

A

-not for patients with astma, coronary insufficiency or peptic ulcer

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18
Q

Reversible indirect cholinergics

A

-Edrophonium
-physostigmine, neostigmine, pyridostigmine
-donepezil

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19
Q

Irreversible indirect cholinergics

A

-organophosphates

-echothiopate
-sarin
-malathion

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20
Q

Problems with indirect cholinergics

A

-excessive receptor activation
-miosis

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21
Q

Edrophonium mech

A

-indirect cholinergic
-AChE inhibitor
-REVERSIBLE
-NON-covalent
-bind to anionic site

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22
Q

Edrophonium structure

A

-quarternary ammonium alcohol
-idk 4’ N on a phenol ring

-indirect cholinergic

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23
Q

Edrophonium use

A

-very short acting
-diagnosis of myasthenia gravis

-indirect cholinergic

24
Q

indirect cholinergic carbamates

A

-Pyridostigmate
-neostigmine
-physostigmine

25
Q

indirect cholinergic carbamate structure

A

-benzene ring with carbamate (O-C=O with 3’ or 4’ Nitrogen

26
Q

indirect cholinergic carbamate mech

A

-REVERSIBLE
-COVALENT
-AChE inhibitor
-more slowly hydrolyzed than ACh
-carbamate binds ESTERATIC site of AChE

27
Q

Pyridostigmate use

A

-treat MG
-reverse nondepolarizing neuromuscular blockade
-pretreatment for nerve gas exposure by occupying AChE so gas can’t bind

-indirect cholinergic

28
Q

Pyridostigmate structure

A

-indirect cholinergic carbamate

29
Q

Neostigmine use

A

-MG
-reverse nondepolarizing neuromuscular blockade
-post-op urinary retention

-indirect cholinergic

30
Q

Neostigmine structure

A

-indirect cholinergic carbamate

31
Q

Physostigmine

A

-antidote to ANTIMUSCARINIC poisoning
-CAN CROSS BBB

32
Q

Organophosphates

A

-Echothiopate
-Sarin
-Malathion

-most are toxic
-indirect cholinergic

33
Q

Organophosphate mech

A

-IRREVERSIBLE
-COVALENT
-longer acting

34
Q

Organophosphate structure

A

-phosphate group
-S or F

35
Q

Echothiopate mech

A

-long acting
-increase ACh
-enhance M activation

36
Q

Echothiopate uses

A

-treat glaucoma
-not used tho bc other drugs are better

37
Q

Sarin uses

A

-nerve gasses

38
Q

Malathion

A

-insecticides
-mammals can rapidly inactivate it with carboxyesterase

39
Q

Pralidoxime Chloride use

A

-antidote for insecticide or gas poisoning
-reverses aging
-give before exposure

40
Q

Pralidoxime chloride structure

A

-ring with N in
-double bonded nitrogen off the ring

41
Q

Pralidoxime chloride mech

A

-strong nucleophile
-hydrolyzes organophosphate
-does NOT cross BBB
-must be taken with ATROPINE

42
Q

Alzheimer drugs

A

-Donepezil
-Rivastigmine
-Galantamine
-Memantine

-AChE inhibitors except memantine

43
Q

Donepezil mech

A

-bind to ANIONIC site
-REVERSIBLE
-NON-covalent

-indirect cholinergic

44
Q

Donepezil use

A

-enhance cognitive ability
-all stages of alzheimers
-cannot slow disease

45
Q

Rivastigmine mech

A

-REVERSIBLE
-COVALENT
-carbamate

46
Q

Rivastigmine use

A

-increase cognitive ability in alzheimers
-not for later stages

47
Q

Rivastigmine problems

A

-lose effectiveness as disease progresses
-nausea, vomiting, anorexia, weight loss

-indirect cholinergic

48
Q

Galantaime mech

A

-REVERSIBLE
-COMPETITIVE
-might be an N agonist

49
Q

Galantamine use

A

-Alzheimers
-lose effectiveness tho
-increase bioavailability with P450 inhibitors

50
Q

Memantine mech

A

-NMDA ANTAgonist
-may slow progression of alzheimers by inhibiting glutamate activity

51
Q

Cholinergic side effects

A

-DUMBBELS
-decrease HR
-CNS activation

52
Q

Miosis

A

-pupils CONSTRICT

53
Q

cholinergic contraindication with ashma/copd

A

-bronchoCONSTRICTION

54
Q

cholinergic contraindication with coronary deficiency

A

-decreases HR

55
Q

cholinergic contraindication with peptic ulcer

A

-increases acid secretions

56
Q

cholinergic contraindication with obstruction of GI/urinary tract

A

-if increased contraction does not remove obstruction

57
Q

cholinergic contraindication with epilepsy

A

-M1 receptors
-CNS penetrable drugs (pilocarpine and physostigmine)