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Neuro Pharm
Cholinergics
35
Pharmacology
Professional
03/17/2011

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Cards

Term
Direct-acting muscarinic agonists
Definition
Acetylcholine chloride
Methacholine
Carbachol
Bethanechol
Cevimeline
Pilocarpine
Term
Acetylcholine chloride
Definition
opthalmic
miosis, short acting
Term
Methacholine
Definition
longer duration
bronchoconstriction
Term
Carbachol
Definition
miosis
decreases intraocular press->contract ciliary m. which opens angle
Term
Bethanechol
Definition
use: excrete urine
caution: asthma (bronchoconstriction)
hyperthyroid (heart is sensitive)
peptic ulcers (acid secretion)
Term
Cevimeline
Definition
use: for drymouth, dec lacr/saliv
SE: all heart mechanisms decr
Vasodilation, reflex tachy-> stim M3 on vasculature
SLUDGE
Term
Pilocarpine
Definition
use: miosis, open angle (glaucoma)
CNS effects: can cross BBB
Term
Indirect-acting cholinergic agonists
(cholinesterase inhibitors)
Definition
keep ACh from being broken down->prolong
Term
Short-acting
Definition
Edrophonium
Tacrine
Donepezil
Rivastigmine
Galantamine
Memantine (not AChEI)
Term
Edrophonium
Definition
binds anionic site
use: Dx myasthenia gravis
Nicotinic at NMJ
Term
Tacrine
Definition
use: Alzheimer's
hepatotoxic
Term
Donepezil
Definition
Use: Alzheimer's
not short-acting
Term
Rivastigmine
Definition
SE: severe vomiting, esophageal rupture
Term
Galantamine
Definition
Use: Alzheimer's
Incr mortality rate?
Term
Memantine
Definition
not an AChEI
Use: Alzheimer's
blocks glutamate receptors->incr intracell Ca->overstim->cell death
Term
Intermediate acting
Definition
Pyridostigmine
Ambenonium
Guanidine
Term
Pyridostigmine
Definition
Carbamoylates AChE->more stable
Use: myasthenia gravis
Term
Ambenonium
Definition
accumulates in body
Use: myasthenia gravis
Term
Guanidine
Definition
Use: myasthenia Eaton-Lambert syndrome
IgG Ab to Ca channels
Mech: prolongs ACh release, slows repolar.
Term
Long acting AChEIs
Definition
Organophosphates
irreversible inhibitors->P's AChE
Rx-enzyme AGES->loses alkyl->more stable
Term
Echothiophate
Definition
binds both sites
use: glaucoma
muscarinic
Term
Malathion
Definition
lotion for head lice
binds to Sulfur in hair
Term
Organophosphate toxicity
Definition
DUMBBELSS: hyper-parasymp effects
Tx Muscarinic: atropine
Nicotinic: pralidoxime (2-PAM)
-binds P of P'ing enzyme>frees enzyme
Duodote: treats both
Must give before AGING occurs
Chronic can cause axon degen
Term
Spinosad
Definition
kills lice
excites insect CNS, exhaustion/death
Term
Antimuscarinics
Definition
blocks PSNS activity
Atropine
Scopolamine
Caution for GLAUCOMA bc it relaxes ciliary body->blocks aqueous flow
antidote for organophosphates
Term
Atropine
Definition
belladonna, deadly nightshade
used as mydriatic, cycloplegic
Term
Scopolamine
Definition
penetrates CNS better
used for motion sickness
SE: sympathetic activity
Term
Mydriatics, Cycloplegics
Definition
Cyclopentolate
Tropicamide
Term
Antispasmodic
Definition
Dicyclomine-IBS
Term
Overactive Bladder
Definition
Darifenacin
Flavoxate
Solfenacin
Term
Ganglionic Blockers
Definition
Nicotine
Varenicline
Term
Nicotine- low dose
Definition
Stim Nn receptors
causes initial incr in BP and CO
-CA release from adrenal medulla
HR incr only slightly
Stim PSNS
Term
Nicotine- high dose
Definition
Ganglionic block
decr BP, peristalsis
Incr alertness from NE in cortex
Term
Bupropion
Definition
treats nicotine addiction by inhibiting NE uptake
Term
Varenicline
Definition
partial agonist of a4B2 Nn receptor
Decr DA release
SE: nausea, HA, sleep disturbances
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