Exam 1 Cholinergic Drugs Flashcards by Brooke Thornburg

Muscarinic agonist drug classes

-choline esters
-alkaloids

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Muscarinic agonist drugs

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

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Indirect cholinergic agonists

-endorphonium
-physostigmine
-neostigmine
-organophosphates

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Choline esters (M agonists)

-Ach
-methacholine
-carbochol
-bethanechol

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Methacholine structure

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

-cholinergic

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Carbachol structure

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

-cholinergic

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Methacholine use

-test for hyperactive airways

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Carbachol use

occular

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Bethanechol structure

-carbamate AND B substitution
-NO effect on N receptor

-cholinergic

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Bethanechol use

-GI stimulation
-urinary retention

-cholinergic

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Alkaloids

-muscarine
-pilocarpine

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Muscarine effect

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

-sweating
-hypotension

-cholinergic

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Pilocarpine effect

-promote sweating, salivation, urination

-cholinergic

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Pilocarpine use

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

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Glaucoma containdication

-antimuscarinic drugs

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Side effects of cholinergics

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

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Cholinergics caution

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

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Reversible indirect cholinergics

-Edrophonium
-physostigmine, neostigmine, pyridostigmine
-donepezil

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Irreversible indirect cholinergics

-organophosphates

-echothiopate
-sarin
-malathion

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Problems with indirect cholinergics

-excessive receptor activation
-miosis

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Edrophonium mech

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

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Edrophonium structure

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

-indirect cholinergic

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Edrophonium use

-very short acting
-diagnosis of myasthenia gravis

-indirect cholinergic

indirect cholinergic carbamates

-Pyridostigmate
-neostigmine
-physostigmine

indirect cholinergic carbamate structure

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

indirect cholinergic carbamate mech

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

Pyridostigmate use

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

Pyridostigmate structure

-indirect cholinergic carbamate

Neostigmine use

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

Neostigmine structure

-indirect cholinergic carbamate

Physostigmine

-antidote to ANTIMUSCARINIC poisoning -CAN CROSS BBB

Organophosphates

-Echothiopate -Sarin -Malathion -most are toxic -indirect cholinergic

Organophosphate mech

-IRREVERSIBLE -COVALENT -longer acting

Organophosphate structure

-phosphate group -S or F

Echothiopate mech

-long acting -increase ACh -enhance M activation

Echothiopate uses

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

Sarin uses

-nerve gasses

Malathion

-insecticides -mammals can rapidly inactivate it with carboxyesterase

Pralidoxime Chloride use

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

Pralidoxime chloride structure

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

Pralidoxime chloride mech

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

Alzheimer drugs

-Donepezil -Rivastigmine -Galantamine -Memantine -AChE inhibitors except memantine

Donepezil mech

-bind to ANIONIC site -REVERSIBLE -NON-covalent -indirect cholinergic

Donepezil use

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

Rivastigmine mech

-REVERSIBLE -COVALENT -carbamate

Rivastigmine use

-increase cognitive ability in alzheimers -not for later stages

Rivastigmine problems

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

Galantaime mech

-REVERSIBLE -COMPETITIVE -might be an N agonist

Galantamine use

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

Memantine mech

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

Cholinergic side effects

-DUMBBELS -decrease HR -CNS activation

Miosis

-pupils CONSTRICT

cholinergic contraindication with ashma/copd

-bronchoCONSTRICTION

cholinergic contraindication with coronary deficiency

-decreases HR

cholinergic contraindication with peptic ulcer

-increases acid secretions

cholinergic contraindication with obstruction of GI/urinary tract

-if increased contraction does not remove obstruction

cholinergic contraindication with epilepsy

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