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7/24/2019 5 Autonomic Drugs
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Mosby items and derived items 2007 by Mosby, Inc., an affiliate of Elsevier Inc.
Chapter 5Chapter 5
Atonomic !r"sAtonomic !r"s
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Atonomic #harmacolo"yAtonomic #harmacolo"y
Atonomic $ervos %ystemAtonomic $ervos %ystem &his system is divided into t'o separate&his system is divided into t'o separate
systems.systems.
&hese systems are called the parasympathetic&hese systems are called the parasympatheticnervos system and the sympathetic nervosnervos system and the sympathetic nervos
system.system.
&hese systems often prodce opposite effects.&hese systems often prodce opposite effects.
!r"s in this "rop are desi"ned to either!r"s in this "rop are desi"ned to eitherenhance or mimic the atonomic nervos systemenhance or mimic the atonomic nervos system
or to bloc( the effects of the nerotransmitters ator to bloc( the effects of the nerotransmitters at
their receptor sites.their receptor sites.
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Atonomic $ervos %ystemAtonomic $ervos %ystem
#arasympathetic $ervos %ystem#arasympathetic $ervos %ystem &his system is concerned 'ith the&his system is concerned 'ith the
conservation of the body processes.conservation of the body processes.
Its main nerotransmitter is acetylcholine.Its main nerotransmitter is acetylcholine. Its receptors are mscarinic, nicotinic, and theIts receptors are mscarinic, nicotinic, and the
somatic)s(eletal mscles.somatic)s(eletal mscles.
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Atonomic $ervos %ystemAtonomic $ervos %ystem
%ympathetic $ervos %ystem%ympathetic $ervos %ystem &his nervos system is desi"ned to cope 'ith&his nervos system is desi"ned to cope 'ith
emer"ency sitations.emer"ency sitations.
&his is commonly (no'n as the +fri"ht or fli"ht&his is commonly (no'n as the +fri"ht or fli"htresponse.response.
Its nerotransmitters are epinephrine andIts nerotransmitters are epinephrine and
norepinephrine.norepinephrine.
Its receptors are theIts receptors are the --andand receptors.receptors.
/
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Atonomic #harmacolo"yAtonomic #harmacolo"y
Choliner"ic or #arasympathomimetic !r"sCholiner"ic or #arasympathomimetic !r"s &hese dr"s are classified as either direct or indirect&hese dr"s are classified as either direct or indirect
actin" a"ents.actin" a"ents.
!irect actin" dr"s act directly on the!irect actin" dr"s act directly on theparasympathetic receptors.parasympathetic receptors.
Indirect actin" dr"s 'or( by either of t'o methods.Indirect actin" dr"s 'or( by either of t'o methods.
&hey can case the release of the nerotransmitter&hey can case the release of the nerotransmitter
'hich then "oes to the receptor site or they inhibit the'hich then "oes to the receptor site or they inhibit theenyme cholinesterase.enyme cholinesterase.
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Atonomic #harmacolo"yAtonomic #harmacolo"y
Choliner"ic #harmacolo"yCholiner"ic #harmacolo"y CardiovasclarCardiovasclar
1 !irect effects inclde ne"ative chronotropic and!irect effects inclde ne"ative chronotropic and
inotropic actions.inotropic actions.
1 ela3ation of smooth mscles cases a decrease inela3ation of smooth mscles cases a decrease intotal peripheral resistance.total peripheral resistance.
1 Indirect effects inclde increased heart rate andIndirect effects inclde increased heart rate andcardiac otpt.cardiac otpt.
1 &he resltin" effect depends pon the dose sed.&he resltin" effect depends pon the dose sed.1 4sally, the patient e3periences bradycardia and a4sally, the patient e3periences bradycardia and a
decrease in blood pressre and cardiac otpt.decrease in blood pressre and cardiac otpt.
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Atonomic #harmacolo"yAtonomic #harmacolo"y
Choliner"ic #harmacolo"yCholiner"ic #harmacolo"y 6astrointestinal6astrointestinal
1 &hese dr"s e3cite the smooth mscle of the&hese dr"s e3cite the smooth mscle of the
"astrointestinal tract and case an increase in"astrointestinal tract and case an increase inactivity, motility, and secretion.activity, motility, and secretion.
EyeEye
1 &hese dr"s case miosis and cyclople"ia.&hese dr"s case miosis and cyclople"ia.
1 &hey case a decrease in intraoclar pressre.&hey case a decrease in intraoclar pressre.
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Atonomic #harmacolo"yAtonomic #harmacolo"y
Adverse eactionsAdverse eactionsAdverse reactions are an e3tension of theAdverse reactions are an e3tension of the
dr"s pharmacolo"ic effects.dr"s pharmacolo"ic effects.
&hey inclde8&hey inclde81 %alivation%alivation1 9acrimation9acrimation1 4rination4rination1 !efecation!efecation
1 #aralysis#aralysis1 :verdose:verdose
;
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Choliner"ic #harmacolo"yCholiner"ic #harmacolo"y
ContraindicationsContraindications &he contraindications and relative cations are&he contraindications and relative cations are
a reslt of the dr"s pharmacolo"ic anda reslt of the dr"s pharmacolo"ic and
adverse effects.adverse effects. &hey inclde8&hey inclde8
1
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Choliner"ic !r"sCholiner"ic !r"s
?0
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Anticholiner"ic !r"sAnticholiner"ic !r"s
&hese dr"s prevent the action of&hese dr"s prevent the action of
acetylcholine at post"an"lionicacetylcholine at post"an"lionic
parasympathetic endin"s.parasympathetic endin"s.
Acetylcholine is released bt its receptor siteAcetylcholine is released bt its receptor site
is completely bloc(ed by anticholiner"icis completely bloc(ed by anticholiner"ic
dr"s.dr"s.
&hese dr"s only bloc( mscarinic receptors.&hese dr"s only bloc( mscarinic receptors.
??
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Anticholiner"ic !r"sAnticholiner"ic !r"s
#harmacolo"y#harmacolo"y Central $ervos %ystemCentral $ervos %ystem
1 !ependin" on the dose, these dr"s can case!ependin" on the dose, these dr"s can case
stimlation or depression.stimlation or depression. E3ocrine 6landsE3ocrine 6lands
1 &hey redce the flo' and volme of secretions in the&hey redce the flo' and volme of secretions in therespiratory, "astrointestinal, and "enitorinary tracts.respiratory, "astrointestinal, and "enitorinary tracts.
?2
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Anticholiner"ic !r"sAnticholiner"ic !r"s
#harmacolo"y#harmacolo"y %mooth Mscle%mooth Mscle
1 ela3 smooth mscles in the respiratory andela3 smooth mscles in the respiratory and
"astrointestinal tracts."astrointestinal tracts.1 &hey delay "astric emptyin" and decrease&hey delay "astric emptyin" and decrease
esopha"eal and "astric emptyin".esopha"eal and "astric emptyin".
1 &hese dr"s also case bronchial dilation.&hese dr"s also case bronchial dilation.
EyeEye
1 &hese dr"s case mydriasis and cyclople"ia.&hese dr"s case mydriasis and cyclople"ia.
?*
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Anticholiner"ic !r"sAnticholiner"ic !r"s
#harmacolo"y#harmacolo"y CardiovasclarCardiovasclar
1 @ith lar"e doses, these dr"s prodce va"al@ith lar"e doses, these dr"s prodce va"al
bloc(in" 'hich reslts in tachycardia.bloc(in" 'hich reslts in tachycardia.1
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Anticholiner"ic !r"sAnticholiner"ic !r"s
Adverse eactionsAdverse eactions &he adverse reactions are an e3tension of the&he adverse reactions are an e3tension of the
dr"s pharmacolo"ic effects.dr"s pharmacolo"ic effects.
&hey inclde8&hey inclde81 erostomiaerostomia1 ConstipationConstipation1 4rinary retention4rinary retention1
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Anticholiner"ic !r"sAnticholiner"ic !r"s
ContraindicationsContraindications Contraindications are sally de to the dr"sContraindications are sally de to the dr"s
pharmacolo"ic and adverse effects.pharmacolo"ic and adverse effects.
&hey inclde8&hey inclde81 6lacoma6lacoma
1 #rostatic hypertrophy#rostatic hypertrophy
1 Intestinal or rinary obstrction or retentionIntestinal or rinary obstrction or retention
1 Cardiovasclar diseaseCardiovasclar disease
?
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Anticholiner"ic !r"sAnticholiner"ic !r"s
4ses4ses #reoperative Medication#reoperative Medication
1 &hey inhibit salivary and bronchial secretions.&hey inhibit salivary and bronchial secretions.
1 &hey bloc( the va"al slo'in" of the heart that can&hey bloc( the va"al slo'in" of the heart that canoccr 'ith "eneral anesthesia.occr 'ith "eneral anesthesia.
6astrointestinal !isorders6astrointestinal !isorders
1 &hey decrease "astrointestinal motility and can be&hey decrease "astrointestinal motility and can besed to treat lcers, diarrhea, and hypermotility.sed to treat lcers, diarrhea, and hypermotility.
?7
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Anticholiner"ic !r"sAnticholiner"ic !r"s
4ses4ses :phthalmolo"ic E3aminations:phthalmolo"ic E3aminations
1 &opical se can case mydriasis 'hich cases a fll&opical se can case mydriasis 'hich cases a fll
visaliation of the retina.visaliation of the retina.1 Cyclople"ia rela3es the lens so that properCyclople"ia rela3es the lens so that proper
prescriptions for "lasses can be determined.prescriptions for "lasses can be determined.
#ar(inson !isease#ar(inson !isease
1 &hey redce the tremors and ri"idity associated 'ith&hey redce the tremors and ri"idity associated 'ith#ar(inson and dr")indced #ar(inson disease.#ar(inson and dr")indced #ar(inson disease.
?;
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Anticholiner"ic !r"sAnticholiner"ic !r"s
4ses4ses Motion %ic(nessMotion %ic(ness
1 &hese dr"s are sed to treat or prevent motion&hese dr"s are sed to treat or prevent motion
sic(ness becase of their central nervos systemsic(ness becase of their central nervos systemdepressant action.depressant action.
!entistry!entistry
1 &hese dr"s are sed to create a dry, oral field.&hese dr"s are sed to create a dry, oral field.
?>
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Adrener"ic !r"sAdrener"ic !r"s
Adrener"ic dr"s can be classified as havin" directAdrener"ic dr"s can be classified as havin" directaction, indirect action, or mi3ed action.action, indirect action, or mi3ed action.
&hese dr"s stimlate&hese dr"s stimlate --andand receptors thro"hotreceptors thro"hotthe body.the body.
!r"s 'ith direct action Bepinephrine, norepinephrine,!r"s 'ith direct action Bepinephrine, norepinephrine,isoproterenol prodce their effect by directlyisoproterenol prodce their effect by directlystimlatin" the receptor site.stimlatin" the receptor site.
!r"s 'ith indirect action Bamphetamine release!r"s 'ith indirect action Bamphetamine releaseendo"enos norepinephrine 'hich then stimlatesendo"enos norepinephrine 'hich then stimlates
the receptor.the receptor. !r"s 'ith mi3ed action Bephedrine either directly!r"s 'ith mi3ed action Bephedrine either directly
stimlate the receptor or release endo"enosstimlate the receptor or release endo"enosnorepinephrine.norepinephrine.
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Adrener"ic !r"sAdrener"ic !r"s
#harmacolo"y#harmacolo"y Central $ervos %ystem BC$%Central $ervos %ystem BC$%
1 &hese dr"s prodce C$% e3citation or alertness.&hese dr"s prodce C$% e3citation or alertness.
1 =i"her doses prodce an3iety, apprehension,=i"her doses prodce an3iety, apprehension,restlessness, and tremors.restlessness, and tremors.
Cardiovasclar %ystemCardiovasclar %ystem
1 &hese dr"s increase the force and rate of&hese dr"s increase the force and rate ofcontraction of the heart.contraction of the heart.
1
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Adrener"ic !r"sAdrener"ic !r"s
#harmacolo"y#harmacolo"y EyeEye
1 &hese dr"s lo'er intraoclar pressre and can case&hese dr"s lo'er intraoclar pressre and can casemydriasis.mydriasis.
espiratory %ystemespiratory %ystem1 &hese dr"s case a rela3ation of bronchiole smooth&hese dr"s case a rela3ation of bronchiole smooth
mscles.mscles.
Metabolic EffectsMetabolic Effects1 Increased "lyco"enolysis fromIncreased "lyco"enolysis from )receptor stimlation)receptor stimlation
cases hyper"lycemia.cases hyper"lycemia. %alivary 6lands%alivary 6lands
1 &hese dr"s prodce vasoconstriction of the salivary&hese dr"s prodce vasoconstriction of the salivary"lands 'hich leads to decreased salivary flo' 'hich"lands 'hich leads to decreased salivary flo' 'hichreslts in 3erostomia.reslts in 3erostomia.
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Adrener"ic !r"sAdrener"ic !r"s
Adverse eactionsAdverse eactions &he adverse reactions associated 'ith these&he adverse reactions associated 'ith these
dr"s are an e3tension of the dr"sdr"s are an e3tension of the dr"s
pharmacolo"ic effects.pharmacolo"ic effects. &hey inclde8&hey inclde81 An3ietyAn3iety1 &remors&remors1 &achycardia&achycardia
1 Increased blood pressreIncreased blood pressre1 ArrhythmiasArrhythmias
2*
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Adrener"ic !r"sAdrener"ic !r"s
4ses4ses DasoconstrictionDasoconstriction
1 &hese dr"s are sed in dentistry becase of their&hese dr"s are sed in dentistry becase of theirvasoconstrictive actions on blood vessels. &hey arevasoconstrictive actions on blood vessels. &hey areadded to local anesthetics becase they prolon" theadded to local anesthetics becase they prolon" theaction of the local anesthetic, redce the ris( foraction of the local anesthetic, redce the ris( forsystemic to3icity, and help to create a dry field.systemic to3icity, and help to create a dry field.
Cardiac EffectsCardiac Effects1 &hese dr"s are sed to raise blood pressre and to&hese dr"s are sed to raise blood pressre and to
treat cardiac arrest.treat cardiac arrest.
2/
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Adrener"ic !r"sAdrener"ic !r"s
4ses4ses
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Adrener"ic
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Antiadrener"ic !r"sAntiadrener"ic !r"s
#harmacolo"y#harmacolo"y &hese dr"s redce sympathetic tone in the&hese dr"s redce sympathetic tone in the
blood vessels and decrease total peripheralblood vessels and decrease total peripheral
resistance.resistance. &his reslts in a redction in blood pressre.&his reslts in a redction in blood pressre.
4ses4ses &hese dr"s are sed to treat hypertension,&hese dr"s are sed to treat hypertension,
peripheral vasclar disease Bi.e., aynadperipheral vasclar disease Bi.e., aynad
syndrome and beni"n prostatic hypertrophy.syndrome and beni"n prostatic hypertrophy.
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