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1.25 Drugs affecting parasympathetic/somatic
by Dr. Kapusta
69
Pharmacology
Professional
01/25/2012

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Term
What enzyme makes Ach? What are the substrates?
Definition
CAT (choline acetyltransferase) via acetyl CoA and choline
Term
How does ACh get into vesciles?
Definition
transported via a proton antiporter= VAT
Term
What are the two sites of AchE?
Definition
anion spot that binds to N+, and active site with serine 203
Term
What part of Ach is metabolized?
Definition
choline
Term
What drug inhibits uptake of choline by the presynaptic neuron?
Definition
Hemicholinium
Term
What drug inhibits VAT?
Definition
vesamicol
Term
How does botulinum toxin work?
Definition
prevents exocytosis of Ach
Term
What is the mechanism of black widow spider venom?
Definition
has alpha-latrotoxin which causes release of Ach
Term
Where are M1 receptors found?
Definition
neuronal CNS and ANS presynaptic
Term
What are the direct acting cholinomimetic drugs?
Definition
receptor agonists= choline esters, alkaloids
Term
What are indirect acting cholinomimetic drugs?
Definition
cholinesterase inhibitors= carbamates and organophophates
Term
Name two choline esters?
Definition
bethanechol and carbachol
Term
What is the clnical use of ACh?
Definition
there isn't one
Term
What type of drug is bethanechol?
Definition
muscarinic agonist
Term
What is bethanechol used for?
Definition
effects mostly on GI and urinary system when asdministered p.o. or S.c. and used to prevent urinary retention after surgery
Term
What type of drug is carbachol?
Definition
muscarinic and nicotinic agonist
Term
What is carbachol used for?
Definition
muscarinic and nicotinic agonist
Term
What is carbachol used for?
Definition
used to produce miosis during ocular surgery
Term
Name some muscarinic alkaloids?
Definition
muscarine, pilocarpine, and (synthetic) cevimeline
Term
What type of drug is pilocarpine?
Definition
muscarinic agonist
Term
What is pilocarpine used for clinically?
Definition
topically to treat glaucoma, orally for the treatment of zerostomia (Sjorgren's syndrome), somewhat selective for salivary glands
Term
What type of drug is cevimeline?
Definition
muscarinic agonist
Term
What is cevimeline used for?
Definition
Sjogren's syndrome
Term
What is closed (or narrow angle) glaucoma?
Definition
drainage angle of the eye becomes physically blocked by a narrow angle preventing drainage of aqueous humour slowly or suddenly
Term
What is chronic open-angle glaucoma?
Definition
the drainage angle of the eye becomes less efficient with time causing inefficient drainage of aqueous humour and increased pressure within the eye. Gradually produced optic nerve damage
Term
What is the MC type of glaucoma?
Definition
chronic, open angle
Term
Is closed angle glaucoma acute or chronic?
Definition
can be either
Term
What are the effects of PNS on the eye?
Definition
M3 contraction of iris sphincter muscle produces miosis

M3 contraction of the ciliary muscle allows near vision
Term
What is the effect of SNS on the eye?
Definition
alpha 1 contraction of iris dilator (radial) muscle causes mydriasis
beta 2 relaxation of ciliary msucle allows you to see far away
Term
What effect does the ANS have on the ciliary epithelium?
Definition
alpha2 and beta 2 mediates aqueous humor production
Term
What are the glaucoma treatments that increase outflow of aqueous humour?
Definition
mitotic agents (aprasympathomimetics; e.g. pilocarpine)
cholinesterase inhibitors (physostigmine)
prostaglandin analogs (Iatanopros, bimatoprost)
Term
What drugs treat glaucoma by decreasing ciliary body production of aqueous humour?
Definition
carbonic anhydrase inhibitors (acetazolamide); topical beta-blockers (timolol, levobunolol)
Term
What are the two types of antimuscarinic drugs?
Definition
natural alkaloids and semi-synthetic derivatives
Term
Name two natural antimuscarinicalkaloids?
Definition
atropine and scopolamine
Term
Name semi-synthetic derivatives that are antimuscarinic drugs.
Definition
ipratropium (quaternary), tiotropium (quaternary; 24h duration); glycopyrrolate; oxybutynin
Term
What are the clinical uses of the belladonna alkaloids?
Definition
preop to reduce salivations/bronchial secretions, reduce intestinal motility, prevent vagal stimulation during anesthesia and surgery, treat overactive bladder, opthalmological examinations, prevent motion sickness, treat asthma, treat AChE inhibitor poisoning
Term
What are the toxic effects of atropine or other muscarinic antagonists?
Definition
dry, hot, red, blind, mad
Term
What effect does .5mg of atropine have?
Definition
paradoxical bradycardia; some dry mouth; inhibition of sweating
Term
1.0 mg of atropine=
Definition
increased xerostomia; thirst; mild tachycardia; mild mydriasis
Term
What are the effects of >10 mg of atropine?
Definition
rapid and weak pulse; fixed, maximally dilated pupils; blurred vision; ataxia; excitement; hallucinations and delirium; coma
Term
What is the antidote for atropine overdose?
Definition
physostigmine (by inhibiting cholinesterase)
Term
What are the three general categories of AChE inhibitors?
Definition
short acting (non-covalent), medium-duration ('reversible carbamates'); long-duration (irreversible organophosphates)
Term
How do carbamates inhibit cholinesterase?
Definition
bind to the esteratic site of AChE
Term
Which carbamates penetrate the CNS?
Definition
physostigmine (neostigmine and pyridostigmine do NOT)
Term
What is physostigmine used for?
Definition
drug of choice to treat poisoning with atropinic agents; used to treat alzheimer's and dementia
Term
Name the carbamates?
Definition
physostigmine, neostigmine, pyridostigmine
Term
What is neostigmine used to treat?
Definition
myasthenia gravis, antidote for OD of curare-like drugs, treat glaucoma
Term
What is pyridostigmine used to treat?
Definition
myasthenia gravis, glaucoma
Term
Name a short acting (noncovalent) cholinesterase inhibitor?
Definition
edrophonium
Term
What is edrophonium used for?
Definition
very short acting diagnostic agent used to test for myasthenia gravis
Term
Which cholinesterase inhibitors bind to the active 'esteratic' site versus the choline 'anionic' site?
Definition
choline 'anionic' site= edrophonium; active 'esteratic' site= physostigmine, neostigmine, pyridostigmine
Term
What is cholinesterase inhibitor acute toxicity termed?
Definition
cholinergic toxidrome
Term
What are the symptoms of cholinergic toxidrome?
Definition
M= salivation, lacrimation, urination, defecation, emesis (vomiting), bradycardia, bronchoconstriction, nausea, mental confusion, seizures
N= fasciculation, muscle cramps, weakness and paralysis of respiratory muscles
Term
What are potential nicotinic receptor effects of high dose AChE inhibitor poisoning?
Definition
Mydriasis, tachycardia, weakness, hypertension, fasciculations
Term
What is the antidote for OD of carbamate cholinesterase inhibitors?
Definition
atropine
Term
How do organophosphates inhibit acetylcholinesterase?
Definition
irreversibly phosphorylate serine hydroxyl at active site of AChE
Term
What are organophophates used for?
Definition
insecticides (malathion, parathion, diazinon), nerve gases (Sarin, soman, tabun)
Term
How do you treat cholinergic toxidrome?
Definition
atropine, 2 pralidoxime (2-PAM), Diazepam
Term
What are ganglionic blocking agents and their uses?
Definition
trimethaphan (produces controlled hypotension), hexamethonium
Term
What are ganglionic stimulating agents?
Definition
nicotine, and Varenicline (chantix)=partial agonist
Term
What are NMJ blocking agents used for?
Definition
intubation, maintain controlled ventilation, paralysis of skeletal muscle in area of surgery
Term
What are the two main categories of NMJ blocking drugs?
Definition
nondepolarizing (competative) versus depolarizing (non-competative)
Term
What are the different types of nondepolarizing (competative) NMJ blocking drugs?
Definition
long duration (tubocurarine), intermediate duration (pancuronium), short duration (mivacurium)
Term
Name a non-competative (depolarizing) NMJ blocking agent.
Definition
succinylcholine
Term
What is the effect of depolarizing (noncompetitive) NMJ blocking agents?
Definition
phase I= contraction (for a few minutes) phase II= relaxed
Term
What is the antidote to NMJ blocking agents?
Definition
nondepolarizing use neostigmine; for depolarizing (succinylcholine) DON"T USE A DRUG, just ventilate until effects wear off in a few minutes
Term
What are curare-like drugs?
Definition
nondepolarizing (comopetative) NMJ blocking drugs
Term
In susceptible patients, succinylcholine may produce what side effects?
Definition
hyperkalemia or malignant hyperthermia
Term
What causes Succinylcholine to wear off in a few minutes?
Definition
metabolized by butyrlcholinesterases
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