Exam 1; Autonomic Drugs Flashcards
This nervous system has short preganglia and long postganglia which allow the activation of other systems
sympathetic
This nervous system originates in the CNS or sacral spinal roots and has long preganglionic and short postganglionic
parasympathetics
All preganglionic neurons use this as a neurotransmitter
ACh
sympathetic postganglionic neurons use this a a neurotransmitter
NE
parasympathetic postganglionic neuros use this as a neurotransmitter
ACh
What two effects does the sympathetic system have on the eye
far focus
contraction of radial muscle = pupil enlargement “mydnasis”
What three effects does the parasympathetic system have on the eye
contracts the circular sphincter for pupil constriction (myosis)
contraction of cilliary muscle for accommodation; close focus
increased tear production
What three effects does the sympathetic system have on the digestive system
decreased secretions
decreased gastric motility
decreased sphincter tone
What three effects does the parasympathetic system have on the digestive system
increased salivary and digestive secretions
increased motility
increased sphincter tone
What two effects does the sympathetic nervous system have on the heart
increased heart rate
increased contractile force
What two effects does the parasympathetic system have on the heart
decreased rate
decreased force of contraction
What two effects does the sympathetic nervous system have on the blood vessels
muscle vessels relax
skin and gut vessels contract
What effect does the parasympathetic system have on the blood vessels
relaxes most blood vessels
What effect does the sympathetic system have on the lung
relaxation of bronchial smooth muscle
What effect does the parasympathetic system have on the lungs
constricts bronchial smooth muscle
What two effects does the sympathetic system have on the reproductive system
relaxation of the bladder
ejaculation
What two effects does the parasympathetic system have on the reproductive system
contraction of the bladder
erection
What effect does the sympathetic system have on metabolism
increase in blood glucose
What type of receptor does ACh bind to
cholinergic
This type of neurotransmitter receptor activation leads to altered ion channels
nictonic receptors
This type of neurotransmitter receptor activation leads to altered metabolism
muscarinic
Niconitic receptors are used by what portions of the autonomic nervous system
preganglionic of both
Muscarinic receptors are used by what portions of the autonomic nervous system
postganglionic parasympathetic
Adrenergic receptors are used by what portions of the autonomic nervous system
postganglionic sympathetic
These act on ACh receptors
cholinergic agents
What is the effect of cholinergic agents
increase in parasympathetic activity
myosis, increased GI motility, increased sweat/tears/saliva, constriction of bronchial SM, decrease in HR and contraction
What is the mechanism of direct acting cholinergic agonists
bind and cause activation
These three drugs are muscarinic agonists
muscarine
pilocarpine
bethanechol
These two drugs are nicotinic agonists
nicotine
succinylcholine
This is a partial nicotinic agonist; binds, but does not fully activate; ACh cannot bind
varenicline
These two drugs are agonists that act at both nicotinic and muscarinic receptors
acetylcholine
carbachol
What is the mechanism behind indirect-active cholinergic agonists
all agents which inhibit AChE; prevents the breakdown of ACh
These indirect-active cholinergic agonists have an effect that lasts several hours
physostigmine
neostigmine
demecarium
This is an indirect-active cholinergic agonists which is reversible and has a short duration of action
edrophonium
This is an indirect-active cholinergic agonists which phosphorylates AChE and may inhibit for hundreds of hours
echothiophate
indirect-active cholinergic agonists may also affect cholinoreceptors of the muscles; need for these three thigns
Glaucoma
Mysathenia gravis
Sjogren’s syndrome
What two indirect-active cholinergic agonists are used to treat Azheimer’s
donepezil
tacrine
This indirect-active cholinergic agonist, if given early, can reduce any permanent damage caused by organophosphate AChE inhibitors
pralidoxime
What are two non-medical indirect-active cholinergic agonists which are irreversible AChE inhibitors
malathion (insecticide)
sarin (nerve gas)
What are the toxicities of cholinergic agonists
Diarrhea Urination Miosis Bradycardia (slow HR) Broncoconstriction Excitation (CNS); paralysis, ataxia, seizures, amnesia Lacrimation Sweating
This blocking agent reversibly blocks the muscarinic receptor
cholinoceptor
*This antimuscarinic agent lasts 7-10 days
atropine
This antimuscarinic agent lasts 3-7 days
scopolamine
These four drugs have short term effects; as in dilating the pupil
homatropine
cyclopentolate
tropicamide
ipratropium
Following an overdose of antimuscarinic agents, what are some minor side effects (8)
pupil size increases inhibits ciliary muscle (virtually blind) decreased tear production bronchodilation dry mouth decreased gastric motility and secretions urinary retention decreased sweating
What are the two major side effects follow an overdose of antimuscarinic agents
increased HR
CNS effects including psychosis
What are the four clinical uses of antimuscarinic agents
used to treat urinary incotinence
motion sickness
GI hyperactivity
asthma
This depolarizing anti nicotinic blocker has a long duration of action; it initially activated the receptor, eventually there is muscle hyper polarization which leads to paralysis
succinylcholine
These are three non-depolarizing antinictonic skeletal muscle ACh receptor blockers; all derived from curare
pancuronium
atracurium
rocurorium (most common)
This reverses the blockade by rocuronium by binding it directly
sugammadex
This muscle paralytic agent is an inhibitor of ACh releaseq
botulinum toxin type A
Botox is used cosmetically but it was originally developed to treat what three conditions
cerebral palsy
tics
strabissmus and mystaganus (eye muscle issues)
This sympathetic adrenoreceptor subtype can contract vascular smooth muscle; heart rate increases
α1
This sympathetic adrenoreceptor subtype can act on presynaptic nerve terminals in CNS
α2
This sympathetic adrenoreceptor subtype increases heart rate and contraction force
β1
This sympathetic adrenoreceptor subtype causes relaxation and vascular smooth muscle
β2
*This adrenergic agonist acts on all adrenergic receptors (α and β) and it stimulates the receptor
epinephrine
These three adrenergic agonists activate α1 receptors; they decease congestion
phenylephrine
tetrahydrozoline
naphazoline
These two adrenergic agonists activate α2 receptors; they decrease sympathetic outflow from the CNS; used to treat hypertension and other analogs treat glaucoma
clonidine
α methyl norepinephrine
These adrenergic agonist activate β1 receptors
norepinephrine
dobutamine
These four adrenergic agonists activate β2 receptors; cause bronchodilation
metalproternol terbutaline fenoterol albuterol (the -nols and -rols)
These are four indirect acting amine, which induce the release of NE from nerve terminals; doesn’t directly affect the receptors
amphetamine, methamphetamine
tyramine
phenylpropanolamine
pseudoephedrine
These two adrenergic antagonists are α1 receptor blockers
prazosin
phenoybenzamine
This α1 receptor blocker drug is used as an anti-hypertensive and also used to treat benign prostatic hypertrophy (BPH)
prazosin
This is an adrenergic antagonist that blocks α1 and α2 receptors
phentolamine
This is an adrenergic antagonists that blocks α2 receptors
tolazoline
These are five adrenergic antagonists that block β1 receptors; decrease heart rate
metoprolol acebutolol alprenolol atenolol esmolol ( the -olols)
These are five adrenergic antagonists that block both β1 and β2 receptors
propanolol timolol levobunolol carteolol metipranolol
