1. Human Nervous system
The nervoussystemcontrolsall the majorfunctionsof the body.Itis dividedintocentral andperipheral
nervoussystems.The peripheral nervoussystemincludesthe somaticand
autonomicnervoussystemswhichcontrol voluntaryand involuntaryfunctionsrespectively.
The ANS controlsthe vegetativefunctionsof the body.These include functionslike circulation,
respiration,digestionandthe maintenanceof bodytemperature
2. Peripheral NervousSystem
Cranial Nerves
12 pairs
Originate inbrainand leave the skull throughforamina.
Spinal Nerves
31 pairs
Originate inspinal cordand leave itthroughintervertebral foramina.
Spinal Cord
Cervical segment8pairs(C1-C8)
Thoracic segment12 pairs(T1-T12)
Lumbersegment5 pairs(L1-L5)
Sacral segment5pairs(S1-S5)
Coccygeal segment1pair
ANS AutonomicNervousSystem
The ANS issubdividedintotwomajorsub-divisions;thisclassificationisbasedonboth anatomicand
physiologicgrounds;the two subdivisionsare sympathetic(thoracolumbarT1-L2/L3)) and
parasympathetic(craniosacral S2-S4,Cranial Nerves3,7,9,10).
Autonomicnervesare actuallycomposedof twoneuronsystems,termedpreganglionicand
postganglionic,basedonanatomical locationrelative tothe ganglia.A preganglionicneuronhasitscell
bodyin the spinal cordor brain.
The sympatheticnervoussystemarisesfromthe thoracicandlumbarareas of the spinal cord
and the preganglionicfibersforthe parasympatheticnervoussystemarise fromthe cranial andsacral
nerves.The postganglionicneuronssendtheiraxonsdirectlytothe effectororgans(peripheral
involuntaryvisceral organs).
AutonomicNervous System
ANS acts on smooth muscles & glands
- Controls& regulationof the heart,respiratory.system, GItract,bladder,eyes&glands
- Involuntary - personhaslittle ornocontrol
Somatic- voluntary - personhascontrol (skeletal muscle)
AutonomicNervous System
Central NervousSystem(CNS) - Brainandspinal cord
Peripheral NervousSystem(PNS)- Locatedoutside the brain&spinal cord
* AutonomicNervousSystem(ANS) &the somatic
The PNS receivesstimulifromthe CNS& initiatesresponsestothe stimuli afterit’sinterpretedbythe
brain
ANS
2. ANShas 2 setsof neurons:
1. Afferent(sensory) - sendsimpulsestothe CNSforinterpretation
2. Efferent- receivesimpulses(info.) fromthe brain&transmitsfromthe spinal cordto the effector
organ cells
- 2 branches - sympathetic& parasympatheticnervoussystem
Figure 20-2.
SympatheticandParasympatheticEffectsonBodyTissues
In termsof function,the parasympatheticnervoussystemisconcernedprimarilywith
conservationandrestorationof function.
In contrast,the sympatheticnervoussystemisconcernedwiththe expenditure of energy,i.e
ANS- Sympatheticnervous system(Adrenergic)
SympatheticNervousSystem(adrenergic) Norepinephrine =neurotransmitter
- Drugs that mimic= adrenergicdrugs,sympathomimetic,oradrenomemetics
* Adrenergicagonists- Drugsinitiatea response
- Drugs that block= adrenergicblockers,sympatholyticoradrenolytics
* Adrenergicantagonists - preventaresponse
Receptorsthatrespondto adrenergicnerve transmitterare termedadrenergicreceptors.These
receptorsare subdividedintoalphaandbetaadrenoreceptortypesonthe basisof bothagonist
and antagonistselectivity.The receptorshave subclassesdependingondrugselectivity.These
are alpha1 and2 and beta1, 2 and 3.
ANS
4 typesof adrenergicreceptororgancells:
1. Alpha-1= vasoconstrictionof bloodvessels
inc.bloodreturnto heart,inc.circulation,inc.BP
2. Alpha-2= inhibitsreleaseof norepinephrine
dec. invasoconstriction,dec.BP
3. Beta-1 = inc.inheart rate & force of contraction
4. Beta-2 = relaxationof smoothmuscle inbronchi,uterus,peripheral bloodvessels
3. ANS - ParasympatheticNervous System(Cholinergic)
ParasympatheticorCholinergicNervousSystem
Acetylcholine =neurotransmitter
- Drugs that mimic= cholinergicdrugs,parasympathomimetics
Cholinergicagonists - initiatesaresponse
- Drugs that block= anticholinergic,parasympatholytics
Cholinergicantagonists - preventsaresponse
Sympathomimetic
pathway
Norepinephrine
From adrenergicneuron
Inc. heartrate
Pupil dilation
Adrenergic(sympathomimetic) agents
Fightor Flight
Parasymathomimetic
pathway
Acetylcholine
From cholinergicneuron
Dec. heartrate
pupil constriction
Cholinergic(parasympathomimeticagents)
AdrenergicsandAdrenergicBlockers
Drugs that Stimulate the sympatheticNervousSystem(adrenergics,adrenergicagonists,
sypathomimetics,oradrenomimetics)
Mimic the sympatheticneruotransmittersnorepinephrine andepinephrine
Act on one or more adrenergicreceptorsiteslocatedonthe cellsof smoothmuscles - heart,
bronchioles,GItract,bladder,eye.
4 mainreceptors(alpha-1,alpha-2,beta-1,beta-2)
SYMPATHETIC RESPONSES
4. Sympathomimetics/Adrenomimetics
Stimulate adrenergicreceptors:3categories
1. Direct-acting= directlystimulatesreceptors
(epinephrineornorepinephrine)
2. Indirect-acting=stimulatesrelease of norep.fromvesiclesof adrenergicneuron,blockthe reuptake of
noradrenaline (amphetamine)
3. Mixed-acting(indirect&direct) =stimulatesreceptorsites&releaseof norep.fromadrenergic
neuron(Ephedrine)
SympathomimeticAgents/ Adrenergics
Action- Many of the adrenergicdrugsstimulate more thanone of the adrenergicreceptorsites(alpha&
Beta)
Response =Inc. BP,pupil dilation,inc.HR,&bronchodilation
Use = Cardiac stimulation,bronchodilator,decongestant
Side effects=State of hyperactivityinbody
Sympathomimetics/Adrenergics
Albuterol - Beta-2agonist(bronchodilation)(Increasesairflow tolungs)
5. Use - bronchospasm,asthma,bronchitis
SE – headache,dizziness,NVD,Sleepproblems
Epinephrine - stimulatesalpha&betareceptors(ActsquicklytoconstrictBloodvessels,broncodilation
, helpstostop swellingonface)
Use -Severe allergicreaction(Anaphylaxis),cardiac arrest
SE - nervousness,agitation(anxietyornervousexcitement)
AdrenergicAgents
Dopamine - alpha-1& beta-1stimulation(Increase contractilityandCardiacoutput,Vasoconstriction
alpha1 effect,Increase bloodflow tokidneys)
Use – Hypotensionthatoccur wheninshockwhichmaybe causedbyheart attack , trauma andother
seriousconditions.Itincreasescardiacoutput,improve perfusiontovital organs
ADRENERGIC DRUGS
Review of functions of sympathetic nervous system receptors
Alpha 1—vasoconstriction, increase BP
Alpha 2-negative feedback causes less norepinephrine to be released so BP is reduced
Beta 1—increased heart rate
Beta 2—bronchodilation, Relaxation of smooth muscles of bronchi, uterus
Beta 3—actual site for lipolysis
What is AdergenicDrug?
As their name suggests, these drugs resemble sympathetic nerve stimulation in their effects;
They may be divided into two groups on the basics of their chemical structure.
1. CATECHOLAMINES:-these are compounds which have the catechol nucleus.
Catecholamines have a direct action on sympathetic effectors cells through interactions with
receptor sites on the cell membrane.
The group includes adrenaline, noradrenaline, dopamine, isoprenaline, and dobutamine
2. NONCATECHOLMINES:- lack the catechol nucleus.
They may directly act on the receptors or may indirectly release the physiologic
catecholaminese.{ephedrine, phenylephrine, amphetamine}
Adrenergic drugs, like cholinergic drugs, can be grouped by mode of action and by the
spectrum of receptors that they affect.
Oral Usability:-Catecholamines are ineffective orally because they are quickly metabolized by
COMT and MAO whereas noncatecholamines are effective orally because they are metabolized
slowly.
Durationofaction: Catecholamines have shorter duration of action whereas
noncatecholamines have longer duration.
CNS penetration:Catecholamines have poor penetration into CNS whereas non catecholamines
are less polar so more penetration in CNS.
6. Sympathomimetics/Adrenomimetics
Stimulate adrenergicreceptors:3categories
1. Direct-acting= directlystimulatesreceptors(epinephrine ornorepinephrine,Phenylephrine)
2. Indirect-acting=stimulatesrelease of norep.fromvesiclesof adrenergicneuron,blockthe reuptake
of noradrenaline (amphetamine,cocaine)
3. Mixed-acting(indirect&direct) =stimulatesreceptorsites&releaseof norepinephrinefrom
adrenergicneuron(Ephedrine,Psedoephederine)
Organ-systemEffectsof Activationofthe AdrenergicSystem
1. CVS:
a. Heart: increasedrate andforce of contraction,increasedcardiacoutput,myocardial demand,andAV
conduction
b. BloodVesselsandBloodpressure:constrictionof bloodvessels,increase inBP
2. SmoothMuscle:
a. Bronchi:relaxation.
b. Uterus:relaxationof the pregnantuterus
c. GIT: relaxationof wall musclesanddecrease motility
d. Bladder:relaxationof detrusormuscle;urinaryretention
7. 3. Eye: mydriasis;reductionof intraocularpressure innormal andglacucomatouseyes
4. Respiration:Bronchodilatation;reliefof congestion;mildstimulationof respiration
5. Metabolic:Increasedhepaticglycogenolysis;increasedfree fattyacidsinthe blood(lipolysis)
6. CNS: excitement,vomiting,restlessness
ADRENALINE
Pharmacokinetics
Adrenalineisrapidlydestroyedinthe gastrointestinaltract,conjugated,andoxidizedinthe liver.
It istherefore ineffective whengivenorallyandshouldbe givenintramuscularlyorsubcutaneous.
Intravenousinjectionishighlydangerousandislikelytoprecipitate ventricularfibrillation
Individualadrenergicdrugs
Epinephrine—prototype
Effectsinclude:increasedBP,increasedheartrate,relaxationof bronchial smoothmuscle,
vasoconstrictioninperipheral bloodvessels
Pharmacodynamics
Adrenalinedirectlystimulatesall the adrenergic receptorsbothandbringsabouteffectsof sympathetic
nerve stimulation.Itsactionmaybe dividedintotwo,dependingonthe type of receptorstimulated.
The α effectsconsistof vasoconstrictioninskinandviscera,mydriasis,plateletaggregationand some
increase inbloodglucose.
The ß effectsconsistsof increasedcontractilityandrate of heart,bronchial relaxation(ß2) uterine
relaxation(ß2),hyperglycemiaandincreasedcirculatingfree fattyacids.
Indications
1. Anaphylaxis
2. Acute bronchial asthma
3. Cardiac arrest
Contraindication
1. Coronarydiseases
2. Hyperthyroidism
3. Hypertension
4. Digitalistherapy
5. Injectionaroundendarteries
NOR ADRENALINE
Nor adrenaline isthe mediatorreleasedbynerve impulsesandvariousdrugsfromthe postganglionic
adrenergicnerves.
It alsoconstitutes20%of the adrenal medullacatecholamineoutput.
Pharmacokinetics
Like adrenaline,noradrenaline isineffective orallysoithas tobe givenintravenouslywithcaution.
It isnot givensubcutaneous orintramuscularlybecauseof itsstrongvasoconstrictoreffect.
The metabolismissimilartoadrenaline;onlyalittle is
excretedunchangedinurine.
Pharmacodynamics
Nor adrenaline isapredominantlyα receptoragonistwithrelativelylessβagonist actionwhen
comparedto adrenaline.
Indication
Nor adrenalinesisusedashypertensiveagentinhypotensive states
8. Adverseeffectsinclude:
- Anxiety,headache,bradycardiaare commonside effects
- Severe Hypertensioninsensitive individuals
ISOPRENALINE DOPAMINE, DOBUTAMINE.
These are the othercatecholamineswhichhave similarpropertiestoadrenalineandnoradrenaline.
Dopamine isnaturallyoccurringandisa precursor of noradrenaline.The othertwo-isoprenalineand
dobutamine- are synthetic.
These drugshave advantage overthe othersbecause theyare more selective intheiractionsothat
theyhave fewerside effectsthanadrenaline andnoradrenaline.
Dopamine anddobutamine are veryusefuldrugsforthe treatmentof shock.Isoprenaline isused for
bradycardia.
Anti-adrenergics
Sympatholytic
Blockor decrease the effectsof sympatheticnerve stimulation,endogenouscatecholaminesand
adrenergicdrugs
Antiadrenergics—mechanisms ofactionand effects
Can occur by blockingalpha1 receptorspostsynaptically,Orbystimulationpresynapticalpha2
receptors.
Resultsinreturnof norepineprhinetopresynapticsite.Activatesalpha2resultinginnegative feedback.
Decreasesrelease of additionalnorepinephrine.
Alpha-Adrenergic Agonists and blockingagents
Alpha2 agonistsinhibitrelease of norepinephrineinbrain;thus,decrease effectsonentire body
Resultsindecrease of BP
Alsoaffectspancreaticisletcells,thussome suppressionof insulinsecretion
Alpha1 adrenergicblockingagents
Act on bloodvessels,eye andGItract
Effects:
Dilationof arteriolesandveins
Decreasedbloodpressure,
Pupillaryconstriction,
Increasedmotilityof GItract
Alpha 1 antagonists:
Minipress(prazosin)—prototype.
TerazosinandDoxasocin—bothare longeractingthanMinipress.
All of these drugsdecreasesbloodpressureandare usedintreatinghypertension
Beta adrenergicblockingmedications
Preventreceptorsfromrespondingtosympatheticnerve impulses,catecholaminesandbetaadrenergic
drugs.
Effectsofbeta blockingdrugs
Decreasedheartrate
Decreasedforce of contraction
DecreasedCO
Slowcardiac conduction
Decreasedreninsecretionfromkidneys
DecreasedBP
Bronchoconstriction
9. Lesseffective metabolismof glucose.Mayresultinmore pronouncedhypoglycemiaandearlys/sof
hypoglycemiamaybe blocker(tachycardia)
Regitine (phentolamine)
Usedfor extravasationof potentvasoconstrictors(dopamine,norepinephrine) intosubcutaneous
tissues
Beta blockingmedications
Mainlyfor cardiovasculardisorders(angina,dysrhythmias,hypertension,MI)
In angina,betablockersdecrease myocardial oxygenconsumptionbydecreasingrate,BPand
contractility.SlowconductionbothinSA node andAV node.
Beta blockers
Possiblyworkbyinhibitionof renin,decreasingcardiacoutputandbydecreasingsympathetic
stimulation
May worsenconditionof heartfailure May reduce riskof “suddendeath”
Beta blockers
Inderal (propranolol) isprototype
Useful intreatmentof hypertension,dysrhythmias,anginapectoris,MI
Receptor selectivity
Acetutolol,atenolol,betaxolol,esmolol,andmetoprolol are relativelycardioselective
These agentslose cardioselectionathigherdosesasmostorganshave both beta1 andbeta 2 receptors
Non-Receptorselectivity
Carteolol,levobunolol,metipranolol,nadolol,propranolol,sotalol andtimololare all non-selective
Can cause bronchoconstriction,peripheral vasoconstrictionandinterference withglycogenolysis
Combinationselectivity
Labetalol andcarvedilol (Coreg) blockalpha1receptorstocause vasodilation,reducingBPandbeta1
and beta2 receptorswhichaffectheartandlungs.
Both alphaand betapropertiescontributetoantihypertensive effect
Q.Whichof the followingdrugisusedfornasal congestion
A. Atenolol
B. Pseudoephederine
C. Prazocin
D. Inderal
Q. Whichof the followingistreatmentof shock?
A. Prazocin
B. Dopamine
C. Isoproterenol
D. Pseudoephedrine
Q. Phenylephrine is
A. Pure alphablocker B. Pure alphaagonist C. Pure betablocker D. Pure beta agonist
Q. Whichof the followingispropertyof catecholamines?
A. Itis orallyeffective because itisnotmetabolizedbyMAOand COMT
B. It hasshorterdurationofactionbecauseit is metabolizedbyMAOand COMT
C. It crossesbloodbrainbarrier D. None of the above
CHOLINERGIC DRUG
10. CHOLINERGIC ALKALOIDS.
1. Those withchieflynicotinicactionsincludenicotine,lobeline etc.
2. Those withchieflymuscarinicactionsinclude muscarine,pilocarpine,etc.
PILOCARPINE:
Pharmacokinetics
Thisdrug isreadilyabsorbedfromthe gastrointestinaltractand itis nothydrolyzedbycholinesterase
enzyme.Itisexcretedpartlydestroyedandpartlyunchangedinthe urine.
Pharmacodynamics
The drug directlystimulatesthe muscarinicreceptorstobringaboutall the muscariniceffectsof
acetylcholine.
Indications
• Glaucoma
ANTICHOLINESTERASE DRUGS
The commonlyusedcholinesteraseinhibitorsfall intothree chemical groups:
1. Simple alcoholsbearingquaternaryamines,e.g.,edrophonium
2. Carbamate and relatedquaternaryortertiaryamines,e.g.,neostigmine,physostigmine
3. Organic derivativesof phosphates,e.g.,isofluorophate,echothiophate
PHYSOSTIGMINE
Pharmacokinetics
Thisdrug iscompletelyabsorbedfromthe gastrointestinaland ishighlydistributedthroughout
the body;it can pass the bloodbrainbarrier.
Pharmacodynamics:
Inhibitsthe enzyme cholinesterase;therefore,itincreasesandprolongsthe effectof
endogenousacetylcholine atthe differentsites.Ithasnodirecteffectoncholinergicreceptors.
Indications
• Glaucoma
• Atropine overdosage
NEOSTIGMINE
Pharmacokinetics
Thisdrug ispoorlyabsorbedfromthe gastro intestinal tractandispoorlydistributedthroughout
the body;it cannot passthe bloodbrainbarrier.
Pharmacodynamics
Justlike physostigmine,itinhibitscholinesterase enzyme;butunlikephysostigmine,ithasa
directnicotinicactiononskeletal muscles.
INDICATIONS
• Myastheniagravis
• ParalyticIleus
• Reversal of effectof muscle relaxants,e.g.tubocurarine
• Postoperative urine retention
Organophosphates such as echothiophate, isofluorophate, etc. combine with
cholinesterase
Irreversiblyandthushydrolysisisveryslow.Theymaybe usedinglaucoma.Otherorganophosphates
like parathionandmalathionare usedasinsecticides.Poisoningwithorganophosphatesisanimportant
cause of morbidityandmortalityall overthe world.Itusuallyresultsfrom:
11. • Occupational exposure asinpersonsengagedinsprayinginsecticides,
• Accidental exposure,and Ingestionof anyof these compoundswithsuicidalintent
CholinergicOpSideEffectsDUMBBELS
I. Darrhea
II. Utination
III. M/muscle weaknes
IV. Bronchorrea
V. B radycardia
VI. E mos's
MG crisisvsCholinergiccrisis
Myastheniccrisis
Respiratorydistress
Increasedpulse and
bloodpressure
Poorcough
Secretionaspiration
Weakness –
Worse withedrophonium
• Cholinergiccrisis
Abdominal cramps
<-Diarrhes
Nausesandvomiting
-Excessive secretions
Miosis
Fasciculations
Dysphagia,Welnes
CholinergicDrugs-1(Summary)
▪ Twotypesof cholinergicreceptors(muscarinic&nicotinic)
▪ Muscarinicreceptors-smoothmuscles/cardiacmuscle/glands/CNS
Nicotinicreceptors-skeletalmuscles/ganglia/CNS
CholinergicDrugs(Direct& Indirect-acting)
AChactionson variousorgan systems
Choline esters&cholinomimeticalkaloids
What are the twotypesof cholinergicreceptors?
A. NicotinicandMuscarinic
B. NicotinicandAdrenergic
C. Alpha1 and Alpha2
D. None of the above
Which of the followingisnotthe side effectof ODof cholinergic effects?
A. Diarrhea
B. Urination
C. Miosis
D. Mydriasis
M2 receptorsact on
A. GI tract
B. Heart
C. Eye
D. Urinary tract
Betanechol isbetterthanCarbachol because?
A. It has fewersideeffects becauseofless nicotinicreceptors
B. It has fewerside effectsbecauseof lessmuscarinicreceptors
C. It has fewerside effectsbecause of more nicotinicreceptors
D. It has fewerside effectsbecauseof more muscarinicreceptors
12. Anticholinergic Drugs
Action
Usedto blockthe effectsof acetylcholine
Lyse,or blockeffectsof the PNS;alsocalledparasympatholyticagents
Uses (betterdrugsare available now)
Decrease GI activityandsecretions(treatulcers)
Decrease parasympatheticactivitiestoallow the sympatheticsystemtobecome more dominant
Anticholinergics/Parasympatholytics
Derivedfromthe plantBelladonna
Blockonlythe muscariniceffectorsinthe PNSandcholinergicreceptorsinthe SNS
Act by competingwithacetylcholineforthe muscarinicacetylcholine receptorsites
Do not blockthe nicotinicreceptors
Have little orno effectatthe neuromuscularjunction
EffectsofBlockingtheParasympatheticSystem
• Increase inheartrate
• Decrease inGI activity
Decrease inurinarybladdertone and function
Pupil dilation
Cycloplegia
ANTICHOLINERGIC DRUGS
Are those whichantagonise the effectof neurotransmitter
Acetylcholine (ACh) onautonomiceffectors&inthe CNSexertedthrough"Muscarinicreceptors".
Thoughnicotinicantagonistsalsoblockcertainactionsof Ach,theyare referredtoas "Ganglion
blockers"&"Neuromuscularblockers"
Muscarinicreceptorsite
Heart
Salivaryglands
Smoothmusclesof GIT
Genitourinarytract
Urinary bladder
Whichblockthe actionsof Ach on autonomiceffectorsandin the CNS;exertedthroughmuscarinic
receptors.• Nicotinicantagonistsare referredtoasganglionblockersandneuromuscularblockers.•
Prototype isATROPINE• Highlyselectiveformuscarinicreceptors.•Syntheticsubstitutespossess
nicotinicblockingproperties also.
Classification
Natural alkaloid - Atropine,Scopolamine(hyoscine)
Semi-syntheticderivative- Homatropine,
Atropine mithonitrate,Ipratropiumbromide.
Syntheticcompound -
a) Mydriatics:Cyclopentolate,tropicamide
b)Anti-seceretory –
13. Quarternary:Glycopyrolate,Propantheline,Isopropamide.
Tertiaryamines:Pirenzepine,Dicyclomine
c) Vasicoselective:Oxybutynin,flavoxate.
d)Anti-parkinsonian:Benzhexol,biperiden.
Actions
Blocksthe acetylcholinereceptorsatthe muscariccholinergic receptorsite
Indications
Decrease secretions
Restore cardiacrate and bloodpressure
Pylorospasmandhyperactivebowel.
Relax uterine hypertonicity
• Pharmacokinetics
Well absorbed
Widelydistributedthroughoutthe body
Crossthe bloodbrainbarrier
T ½ variesbasedonroute and drug
Excretedinthe urine
Anticholinergic Agents and Their Indications
Atropine
- Blocksparasympatheticeffectsinmanysituations
• Dicyclomine(Antispas,Dibent,andothers)
RelaxesGItract; treatshyperactive orirritable bowel
Glycopyrrolate(Robinul):Adjunctinthe treatmentof ulcers
Propantheline(Pro-Banthine):Adjunctinthe treatmentof ulcers
ATROPINE
Atropine isfoundinthe plantAtropabelladonnaanditis the prototype of muscarinicantagonists.
Pharmacokinetics
Atropine isabsorbedcompletelyfromall sitesof administrationexceptfromthe skinwall,where
absorptionisforlimitedextent;ithasgooddistribution.About60% of the drug is excretedunchangedin
urine.
Pharmacodynamics
Atropine antagonizesthe effectof acetylcholinebycompetingforthe muscarinicreceptors
peripherallyandinthe CNS;therefore the effectsof atropine are opposite tothe acetylcholine
effects.
Administrationof atropine cause fever?????????
Organ-system Effects:
Eyes: - Dilationof pupil(relaxationof constrictorpupillae)(mydriasis)
relaxationorweakeningof ciliarymuscle (cycloplegia-lossof the abilitytoaccommodate
Body Temperature:Increasedbodytemperaturedue tolossof sweatingand stimulationof temp
centersinhypothalamus
CVS:- Small doses:Decreaseheartrate
Large doses:Increasedheartrate,FacilitatesAV conduction
Respiratory:- bronchodilatationandreductionof secretion
14. GIT: - decreasedmotilityandsecretions
GUS:- Relaxessmoothmuscle of ureterandbladderwall;voidingisslowed.
SweatGlands,Salivary glands andLacrimation: - suppressessweating,salivationandlacrimation
Atropine
Depressessalivationandbronchial secretions
. Dilatesthe bronchi
• Inhibitsvagal responsesinthe heart
• Relaxesthe GIandgenitourinarytracts
InhibitsGIsecretions
Causesmydriasis
• Causescycloplegia
Clinical Indications
Pre anestheticmedication:Reducesexcessivesalivationandrespiratorysecretions
Ophthalmic:MydriaticandCycloplegiceffect
Anti spasmodic:Itisusedas an anti-spasmodictorelax GItract
CVS:It is usedto treatbradycardia
Anti-secretory agent: Blocksecretionsof upperandlowerrespiratorytractpriorto surgery
Anti-dotefor cholinergicagonist:Atropineisusedforthe treatmentof organophospate and
overdose of physostigmine.
Sideeffects
• Belladonapoisoningdue todrugoverdose.
• Dry mouth,difficutlyinswallowingandtalking.
Dry,flushedandhotskin.
Feverdifficultyinmicturition,decreasedbowel sounds.
Dilatedpupil,photophobia,blurringof nearvision.
Excitement,ataxia,delirium,hallucination.
Convulsionandcomamayoccur insevere poisoning
Drynessof the mouth
Tachycardia
Blurredvision
• Retentionof urine
CNS:confusionhallucinations,restlessnessmayprogresstodepression
Treatment: Physostigmine
Contraindications:Glaucoma&Bladderoutletobstruction
Anticholinergics
Anticholinergicseffectthe CNS&benefitpeople prone tomotionsickness
Scopolamine Patch- Classifiedasanantimuscarinicformotionsickness
- Topical skinpatchbehindthe earfor 3 days
Use = Preventionof motionsickness,cruisingonwater,flying,carsickness
Postoperative nauseaandvomiting
SE = Dry mouth,visual disturbances,pupil dilation,same asatropine
HYOSCINE (SCOPOLAMINE)
Thisdrug has the same effectasatropine exceptforsome differenceswhichincludes:-
- It has LONGER durationof action
- GreaterActionon CNS
15. 3. Betterforpreanestheticmedicationbecause of strongantisecretoryandantiemeticactionandalso
bringsaboutamnesia.
4. Can be usedforshort- travel motionsickness
SYNTHETIC ATROPINE DERIVATIVES
There are a numberof syntheticatropine derivatives,whichare usedinthe treatmentof various
conditions,theiractionsare similartothat of atropine buthave fewerside effects.Thesegroupsof
drugsinclude
In ophthalmology to producemydriasisand cycloplegia priortorefraction:Tropicamide and
Cyclopentolate
Anti parkinsonianatropinesubstitute: Benztropine,biperidine
Treatment of COPD and BronchialAsthma:IpratropiumandTiotropium
Atropinesubstitutes which decreaseurinary bladderactivity:Oxybutynin
Contraindications
Allergy
Anyconditionthatcouldbe exacerbatedbyblocking of the parasympatheticnervoussystem
• Glaucoma
• Pepticulcerdisease
Prostatichypertrophy
Bladderobstruction
AdverseReactions
Blurredvision
Mydriasis
Cycloplegia
Photophobia
Palpitations,bradycardia
Dry mouth,alteredtaste perception
Urinary hesitancyandretention
Decreasedsweating;predispositiontoheatprostration.
Quiz1: What isthe effectof atropine onheart?
A. It decreases heartrate insmalldoses and increases heartrateinlarge doses
B. It increasesheartrate in small dosesanddecreasesheartrate inlarge doses
C. Increasedcardiacactivityinbothsmall and large doses
D. Decreasedcardiacactivityinbothsmall and large doses
Quiz2: Whichof the followinganti cholinergicdrugisusedinmotionsickness?
A. Oxybutynin
B. Ipratropium
C. Scopolamine
D. Benztropine
Quiz3: Whichof the followinganti cholinergicdrugisusedinbronchial asthmaand COPD?
A. Oxybutynin
B. Ipratropium
C. Scopolamine
D. Benztropine
Quiz4:Which of the followinganti cholinergicdrugisAnti parkinsonian?
A. Oxybutynin
B. Ipratropium
C. Scopolamine
D. Benztropine
Quiz5
Atropine substituteswhichdecreasesurinarybladderactivity?
A.Oxybutynin
B. Ipratropium
C. Scopolamine
D. Benztropine