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Autonomic Drugs- Part 1
Pharm, Module 3
97
Medical
Graduate
06/30/2009

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Cards

Term
What are the 2 main parts of the ns?
Definition
cns, pns
Term
The autonomic ns is divided into what 2 categories?
Definition
sns, parasympathetic ns
Term
How long are the pre and post ganglionic neurons in the psns?
Definition
long preganglionic short postganglionic
Term
How long are the pre and post ganglionic neurons in the sns?
Definition
short preganglionic, long postganglionic
Term
Where do sns nerves arise?
Definition
thoracic and lumbar region of spinal cord
Term
How does the sns discharge?
Definition
as a unit producing diffuse activation of target organs
Term
What is the principal post-ganglionic neurotransmitter of the sns?
Definition
norepinephrine; fight or flight
Term
From where do nn arise in psns?
Definition
from cranial and sacral region of spinal cord
Term
In the psns, are the ganglia in organ systems or spinal cord?
Definition
organ systems, not in spinal cord
Term
How does the psns activate target tissues?
Definition
discretely
Term
What is the principle post-ganglionic neurotransmitter of the psns?
Definition
acetylcholine- rest and digest
Term
Which ans branch causes smooth mm contraction?
Definition
psns
Term
What are the primary neurotransmitters in ans and somatic ns?
Definition
acetylcholine, norepinephrine, epinephrine- released from adrenal gland
Term
What type of drugs activate or block receptors? This is the method of action of most autonomic drugs.
Definition
direct acting drugs
Term
What are 2 types of acetylcholine receptors (cholinergic)?
Definition
muscarinic, nicotinic
Term
Which type of acetylcholine receptor acts at neuroeffector junctions?
Definition
muscarinic
Term
Which acetylcholine receptor acts at all autonoomic ganglia and somatic neuromuscular jcts?
Definition
nicotinic
Term
What are 2 types of norepinephrine and epinephrine receptors (adrenergic)?
Definition
alpha and beta adrenergic receptors
Term
What baroreceptor reflex receptors are situated in the aortic arch and carotid sinus and are activated w/increased aa pressure?
Definition
stretch receptors
Term
Which cholinergic receptor is present at neuroeffector junctions (site of action)?
Definition
muscarinic (primarily, most drugs work here)
Term
Which cholinergic receptor is present at *all* autonomic ganglia- leads to postganglionic release of neurotransmitters at neuroeffector junctions?
Definition
nicotinic
Term
In which autonomic ganglia are nicotinic cholinergic receptors present?
Definition
all autonomic ganglia
Term
Are there many or few primary uses for direct acting agonists?
Definition
relatively few
Term
What direct-cholinergic agonist is used to stimulate bladder or intestinal tract w/o having cardiac effects?
Definition
bethanechol
Term
What direct-cholinergic agonist is a topical agent for glaucoma?
Definition
carbachol
Term
What direct-cholinergic agonist is a topical agent for glaucoma and oral agent for xerostomia (dry mouth)?
Definition
pilocarpine
Term
What direct-cholinergic agonist is an oral, nasal, or transdermal product to assist in smoking cessation?
Definition
nicotine
Term
What direct-cholinergic agonist is a new synthetic direct agonist for xerostomia and dry eyes indicated after xrt tx or for pts w/sjogren's syndrome?
Definition
cevimeline
Term
What is an autoimmune disease producing Abs against *nicotinic* receptors in skeletal mm that results in severe mm weakness?
Definition
myasthenia gravis
Term
Against what receptors in skeletal mm do Abs in Myasthenia gravis act?
Definition
nicotinic receptors
Term
What type of cholinesterase drugs are used in myasthenia gravis?
Definition
reversible cholinesterase inhibitors
Term
What is a short acting agent to dx myasthenia gravis?
Definition
edrophonium
Term
What are quaternary amines (so the doesn't cross the bbb) that are antidotes for neuromuscular blocking drugs such as d-tubocurarine? They are used in tx of myasthenia gravis?
Definition
neostigmine and pyroidostigmine
Term
What are 3 reversible cholinesterase inhibitors used in tx of alzheimer's disease?
Definition
donepezil (aricept)- qd. galantamine (rizatidine). rivastigmine (exelon).
Term
Are choline esters direct or indirect acting agents?
Definition
direct acting agents
Term
Which direct acting agent- choline ester- has no tx use, is nonselective and has short duration?
Definition
acetylcholine
Term
Which direct acting agent- choline ester- is muscarinic and has a longer duration?
Definition
methacholine
Term
Which direct acting agent- choline ester- is predominatelly nicotinic?
Definition
carbachol
Term
Which direct acting agent- choline ester- is predominately muscarinic?
Definition
bethanechol
Term
Which direct acting agent- plant alkaloid- comes from poisonous mushrooms?
Definition
muscarine
Term
Which direct acting agent- plant alkaloid- comes from tobacco?
Definition
nicotine
Term
Which direct acting agent- plant alkaloid- comes from a small shrub and is predominately muscarinic?
Definition
pilocarpine
Term
Which drugs for primary open angle glaucoma increases aq humor outflow?
Definition
prostaglandin analogs (now the most common drugs used). muscarinic receptor agonists.
Term
Which drugs for primary open angle glaucoma decrease aq humor productino?
Definition
alpha2-receptor agonists. beta-receptor antagonists. carbonic anhydrous inhibitors.
Term
What are 2 classes of muscarinic receptor antagonists?
Definition
beladonna alkaloids. semisynthetic and synthetic antagonists.
Term
What are 2 classes of nicotinic receptor antagonists?
Definition
ganglionic blocking agents. neuromuscular blocking agents.
Term
What are 2 classes of neuromuscular blocking agents?
Definition
nondepolarizing. depolarizing.
Term
What are 2 classes of cholinergic receptor antagonists?
Definition
muscarinic receptor antagonists and nicotinic receptor antagonists.
Term
What are the most common of the cholinergic drugs?
Definition
muscarinic receptor antagonists
Term
What are also known as **anticholinergic** drugs?
Definition
muscarinic receptor antagonists
Term
Muscarinic receptor antagonists are also known as what?
Definition
also known as **anticholinergic** drugs
Term
What type of antagonists are most muscarinic receptor antagonists?
Definition
competitive
Term
What are natural substances are muscarinic receptor antagonists?
Definition
belladonna alkaloids
Term
What group contains atropine from atropa belladonna (deadly nightshade)?
Definition
belladonna alkaloids
Term
What is the prototypical anticholinergic agent?
Definition
atropine, a belladonna alkaloid
Term
Atropine, scopalamine, and hyoscyamine are all part of what class of drugs?
Definition
beladonna alkaloids
Term
What is anticholinergic agents' anticipated response in the eye?
Definition
mydriasis, paralysis of accomodation
Term
What is anticholinergic agents' anticipated response regarding sweating?
Definition
blocked, increase in body temp
Term
What is anticholinergic agents' anticipated response in secretions?
Definition
drying effect
Term
What is anticholinergic agents' anticipated response in the lungs?
Definition
bronchodilation, reduced secretions
Term
What is anticholinergic agents' anticipated response in intestinal motility?
Definition
decreased
Term
What is anticholinergic agents' anticipated response in the bladder?
Definition
atony, urinary retention
Term
The clinical uses of which belladonna alkaloid includes tx of sinus bradycardia and colinesterase inhibitor overdose?
Definition
atropine
Term
The clinical uses of which belladonna alkaloid includes tx of gi spasms?
Definition
hyoscamine (L) isomer of atropine
Term
The clinical uses of which belladonna alkaloid includes a transdermal patch for motion sickness- releases 1 mg over 72 hrs?
Definition
scopalamine (transderm scop)
Term
The toxicity profile for what class of drugs includes: dry mouth, blurred vision, tachycardia, palpitations, urinary retention, delerium, and hallucinations?
Definition
toxicity profile, belladonna alkaloids
Term
What are teh relative contraindications for belladonna alkaloids?
Definition
glaucoma, prostatic hyperplasia, dementia, delerium
Term
What class of drugs includes oxybutinin, tolterodine, and solifenacin?
Definition
synthetic and semisynthetic muscarinic receptor antagonists
Term
What are 3 drugs used for hyperactive bladder?
Definition
oxybutinin (ditropan), tolterodine (detrol), solifenacin (VESIcare)
Term
What are 2 classes of nicotinic receptor antagonists?
Definition
ganglionic blocking agents, neuromuscular blocking agents
Term
What class of nicotinic receptor antagonists block nicotinic receptors at ganglia?
Definition
ganglionic blocking agents
Term
What class of nicotinic receptor antagonists are only useful for research b/c they block all autonomic outflow-not useful clinically anymore b/c of potential toxicity?
Definition
ganglionic blocking agents
Term
What class of nicotinic receptor antagonists inhibits neurotransmission at skeletal neuromuscular junction?
Definition
neuromuscular blocking agents
Term
What class of nicotinic receptor antagonists cause mm weakness and paralysis?
Definition
neuromuscular blocking agents
Term
How do pesticides act in the body?
Definition
*irreversible* cholinesterase inhibitors
Term
Pesticides belong to what class of drugs?
Definition
organophosphates
Term
How do indirect-acting cholinergic agonsits act on cholinesterase?
Definition
*irreversible* cholinesterase inhibitors
Term
Which indirect-acting cholinergic agonist is very lipid soluble?
Definition
isoflurophate (dfp)- *irreversible* cholinesterase inhibitor
Term
Which indirect-acting cholinergic agonist is a quaternary compound?
Definition
echothiophate, *irreversible* cholinesterase inhibitor
Term
Which indirect-acting cholinergic agonist acts on mammals and birds by inactivation by hydrolisis (insects do not- common pesticide)?
Definition
malathion- *irreversible* cholinesterase inhibitor
Term
The following s/s of organophosphate toxicity are associated with what class of drugs: bradycardia, hypotension, salivation, sweating, lacrimation, miosis?
Definition
muscarinic
Term
The following s/s of organophosphate toxicity are associated with what class of drugs: mm fibrillation, mm fasciculation, mm paralysis?
Definition
nicotinic
Term
What are the cns effects of organophosphate toxicity?
Definition
confusion, ataxia, coma, respiratory paralysis
Term
How do nondepolarizing neuromuscular blocking agents act?
Definition
*competitive* antagonists of acetylcholine at nicotine receptor, *preventing depolarization by ach*
Term
Which has greater cns effects: scopolamine or atropine?
Definition
scopalamine
Term
Which prototypical anticholinergic agent is a muscarinic antagonist, belladonna alkaloid, widely distributed, t1/2=2hrs, eye effect>72 hrs, and blocks m1, m2, and m3?
Definition
atropine
Term
What is the only agent of the depolarizing neuromuscular blocking agents?
Definition
succinylcholine
Term
What drug consists of 2 ach molecules linked together?
Definition
succinylcholine- a depolarizing neuromuscular blocking agent
Term
What is the pharmacologic antidote for succinylcholine?
Definition
no pharmacologic antidote exists. effects cannot be reversed by chlinesterase inhibitors.
Term
Which indirect-acting cholinergic agonist (reversible cholinesterase inhibitor) is a quaternary amine and is poorly absorbed?
Definition
neostigmine
Term
Which indirect-acting cholinergic agonist (reversible cholinesterase inhibitor) is a neostigmine analogue w/shorter duration and is also a quaternary amine?
Definition
edrophonium (tensilon)
Term
Which indirect-acting cholinergic agonist (reversible cholinesterase inhibitor) is an alkaloid from calabar bean (ordeal bean) and is a tertiary amine- can penetrate the cns?
Definition
physostigmine
Term
Which 3 drugs are reversible cholinesterase inhibitors that are indirect-acting cholinergic agonists?
Definition
neostigmine, edrophonium (tensilon), and physostigmine
Term
The following drugs belong to what class: neostigmine, edrophonium (tensilon), and physostigmine?
Definition
reversible cholinesterase inhibitors that are indirect-acting cholinergic agonists
Term
How do indirect-acting cholinergic agonists act?
Definition
reversible cholinesterase inhibitors
Term
How many risk points are associated w/the following drugs: amitriptyline, chlorpheniramine, diphenhydramine, and oxybutinin?
Definition
anticholinergic risk- 3 points
Term
How many risk points are associated w/the following drugs: cetirizine (zyrtec), loratidine, olanzapine, tolterodine?
Definition
anticholinergic risk- 2 pts
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