introduction to autonomic pharmacology

AUTONOMIC PHARMACOLOGYAUTONOMIC PHARMACOLOGY

A. Q. SangalangA. Q. Sangalang, , MD, FPOGSMD, FPOGS FACULTY OF PHARMACYFACULTY OF PHARMACY

UNIVERSITY OF SANTO TOMASUNIVERSITY OF SANTO TOMAS


NERVOUS SYSTEMNERVOUS SYSTEM

SSympatheticympathetic (Thoracolumbar) (Thoracolumbar) SomaticSomatic AutonomicAutonomic T1-T12 (voluntary) T1-T12 (voluntary)

(involuntary)(involuntary) L1-L5 L1-L5

ParasympatheticParasympathetic (Craniosacral)(Craniosacral) CN 3,7,9,10CN 3,7,9,10 S2-S4S2-S4


SPINAL ROOTS OF ORIGINSPINAL ROOTS OF ORIGINSYMPATHETIC (SANS)SYMPATHETIC (SANS)

Preganglionic fibers originate fromPreganglionic fibers originate fromThoracic (T1-T12) segments of the cordThoracic (T1-T12) segments of the cordLumbar (L1-L5) segments of the cordLumbar (L1-L5) segments of the cord


SPINAL ROOTS OF ORIGINSPINAL ROOTS OF ORIGINPARASYMPATHETIC (PANS)PARASYMPATHETIC (PANS)

Preganglionic motor fibers originate fromPreganglionic motor fibers originate fromCranial nerve nuclei III, VII, IX and X Cranial nerve nuclei III, VII, IX and X Sacral segments (S2-S4)Sacral segments (S2-S4)


LOCATION OF GANGLIALOCATION OF GANGLIASYMPATHETICSYMPATHETIC

Most of the ganglia are located in 2 paravertebralMost of the ganglia are located in 2 paravertebralchains that lie along the spinal cordchains that lie along the spinal cordFew (prevertebral) on the anterior aspect of theFew (prevertebral) on the anterior aspect of theaortaaortaPreganglionic fibers are short and the Preganglionic fibers are short and the postganglionic fibers are longpostganglionic fibers are long


LOCATION OF GANGLIALOCATION OF GANGLIAPARASYMPATHETICPARASYMPATHETIC

Most of the ganglia are located in the organsMost of the ganglia are located in the organsinnervated, most distant from the spinal cordinnervated, most distant from the spinal cordPreganglionic fibers are long and the Preganglionic fibers are long and the postganglionic fibers are shortpostganglionic fibers are short


NEUROTRANSMITTERS (NTAs)NEUROTRANSMITTERS (NTAs)4 FEATURES4 FEATURES1.1. SynthesisSynthesis2.2. StorageStorage3.3. ReleaseRelease4.4. Termination of actionTermination of action


NEUROTRANSMITTERSNEUROTRANSMITTERSA.A.CHOLINERGIC TRANSMISSION CHOLINERGIC TRANSMISSION

Acetylcholine (ACh) Acetylcholine (ACh) Primary transmitter in all autonomic ganglion Primary transmitter in all autonomic ganglion and parasympathetic postganglionic synapses and parasympathetic postganglionic synapses


NEUROTRANSMITTERSNEUROTRANSMITTERSA.A. CHOLINERGIC TRANSMISSION CHOLINERGIC TRANSMISSION 1.1. Synthesis and storageSynthesis and storage

ACh is ACh is synthesizesynthesize from acetyl-CoA and choline from acetyl-CoA and cholineby choline acetyltransferaseby choline acetyltransferase

Inhibited by Inhibited by HEMICHOLINIUMHEMICHOLINIUMActively transported into the vesicle for Actively transported into the vesicle for storagestorage

Inhibited by Inhibited by VESAMICOL VESAMICOL


NEUROTRANSMITTERSNEUROTRANSMITTERSA.A. CHOLINERGIC TRANSMISSION CHOLINERGIC TRANSMISSION 2.2. Release of AChRelease of ACh

ReleaseRelease of transmitter stores from vesicles of transmitter stores from vesicles in the nerve endings requires the entry of in the nerve endings requires the entry of calcium and interaction between several calcium and interaction between several proteins in the vesicleproteins in the vesicle

BOTULINUM TOXINBOTULINUM TOXIN prevents the release prevents the release processprocess


NEUROTRANSMITTERSNEUROTRANSMITTERSA.A. CHOLINERGIC TRANSMISSION CHOLINERGIC TRANSMISSION 3.3. Termination of action of AChTermination of action of ACh

Metabolized to acetate and choline by Metabolized to acetate and choline by acetylcholinesteraseacetylcholinesteraseNot excreted but recycled in the bodyNot excreted but recycled in the bodyDrugs can inhibit acetylcholinesteraseDrugs can inhibit acetylcholinesterase


NEUROTRANSMITTERSNEUROTRANSMITTERSTERMINATION OF ACTIONTERMINATION OF ACTION

By metabolismBy metabolism Monoamine oxidase (MAO)Monoamine oxidase (MAO) Cathecol-o-methly transferase (COMT)Cathecol-o-methly transferase (COMT)

Diffuse away from the synaptic cleft and Diffuse away from the synaptic cleft and get metabolized elsewhereget metabolized elsewhere


NEUROTRANSMITTERSNEUROTRANSMITTERSTERMINATION OF ACTIONTERMINATION OF ACTION

Taken up to presynaptic cell Taken up to presynaptic cell UPTAKE 1UPTAKE 1

Taken up to postsynaptic cellTaken up to postsynaptic cell UPTAKE 2UPTAKE 2

AUTONOMIC PHARMACOLOGYAUTONOMIC PHARMACOLOGYDRUG EFFECTS ON THE SYNTHESIS, STORAGE,DRUG EFFECTS ON THE SYNTHESIS, STORAGE,RELEASE AND TERMINATION OF ACTION OF AChRELEASE AND TERMINATION OF ACTION OF ACh

HEMICHOLINIUMHEMICHOLINIUMInhibits synthesis of ACh into the cellInhibits synthesis of ACh into the cell

VESAMICOLVESAMICOLInhibits storage of ACh into the vesicleInhibits storage of ACh into the vesicle

BOTULINUM TOXINBOTULINUM TOXINInhibits the release of AChInhibits the release of ACh

These drugs are not very useful for systemic therapy These drugs are not very useful for systemic therapy because their effects are not sufficiently selectivebecause their effects are not sufficiently selective


NEUROTRANSMITTERSNEUROTRANSMITTERSB.B. ADRENERGIC TRANSMISSION ADRENERGIC TRANSMISSION

Norepinephrine (NE)Norepinephrine (NE)Primary transmitter at the sympathetic Primary transmitter at the sympathetic postganglionic synapsespostganglionic synapses


NEUROTRANSMITTERSNEUROTRANSMITTERSB.B. ADRENERGIC TRANSMISSION ADRENERGIC TRANSMISSION 1.1. Synthesis and storageSynthesis and storage

tyrosine hydroxylasetyrosine hydroxylase

Tyrosine –--------------------DOPA Tyrosine –--------------------DOPA Decarboxylated to dopamineDecarboxylated to dopamineHydroxylated to norepinephrineHydroxylated to norepinephrineTyrosine hydroxylase is inhibited by Tyrosine hydroxylase is inhibited by METYROSINEMETYROSINE


NEUROTRANSMITTERSNEUROTRANSMITTERSB.B. ADRENERGIC TRANSMISSION ADRENERGIC TRANSMISSION 1.1. Synthesis and storageSynthesis and storage

NE and dopamine are transported into NE and dopamine are transported into vesicles and storedvesicles and storedMAO inactivates portions of the NTA in MAO inactivates portions of the NTA in the cytoplasmthe cytoplasmMAO INHIBITORSMAO INHIBITORS may increase stores may increase storesRESERPINERESERPINE inhibits the transport inhibits the transport


NEUROTRANSMITTERSNEUROTRANSMITTERSB.B. ADRENERGIC TRANSMISSION ADRENERGIC TRANSMISSION 2.2. Release and termination of actionRelease and termination of action

Release mechanism is the same as AChRelease mechanism is the same as AChMetabolism is not responsible for termination Metabolism is not responsible for termination of actionof actionDiffusion and reuptake I reduce the Diffusion and reuptake I reduce the concentration and stop the actionconcentration and stop the action


NEUROTRANSMITTERSNEUROTRANSMITTERSB.B. ADRENERGIC TRANSMISSION ADRENERGIC TRANSMISSION 2.2. Release and termination of actionRelease and termination of action

Outside the cleft, it can be metabolized by Outside the cleft, it can be metabolized by MAO and COMT and are excretedMAO and COMT and are excretedGUANETHIDINE inhibits the releaseGUANETHIDINE inhibits the releaseMAO INHIBITORS inhibit the metabolismMAO INHIBITORS inhibit the metabolism


DRUG EFFECTS ON ADRENERGIC TRANSMISSIONDRUG EFFECTS ON ADRENERGIC TRANSMISSION

METYROSINEMETYROSINEInhibits the synthesis of NEInhibits the synthesis of NE

RESERPINERESERPINEInhibits the storage of NEInhibits the storage of NE

These drugs have been used in several diseases because These drugs have been used in several diseases because they block sympathetic but not parasympathetic functionsthey block sympathetic but not parasympathetic functions


DRUG EFFECTS ON ADRENERGIC TRANSMISSIONDRUG EFFECTS ON ADRENERGIC TRANSMISSION

GUANETHEDINEGUANETHEDINEInhibits release of NEInhibits release of NE

MAO INHIBITORSMAO INHIBITORSInhibits metabolism of NEInhibits metabolism of NE

These drugs have been used in several diseases because These drugs have been used in several diseases because they block sympathetic but not parasympathetic functionsthey block sympathetic but not parasympathetic functions


NEUROTRANSMITTERS NEUROTRANSMITTERS Acetylcholine [ACh (cholinergic)]Acetylcholine [ACh (cholinergic)]Norepinephrine [NE (adrenergic)]Norepinephrine [NE (adrenergic)]


CHOLINERGICCHOLINERGICA nerve ending that releases A nerve ending that releases acetylcholineacetylcholine as as

the primary transmitterthe primary transmitterAlso a synapse in which Also a synapse in which acetylcholineacetylcholine is the is theprimary transmitterprimary transmitter


ADRENERGICADRENERGICA nerve ending that releases A nerve ending that releases norepinephrinenorepinephrine as asthe primary transmitterthe primary transmitterAlso a synapse in which Also a synapse in which norepinephrinenorepinephrine is the is theprimary transmitter primary transmitter


All preganglionicAll preganglionic fibers are fibers are cholinergiccholinergic

heart (parasympathetic)heart (parasympathetic)

heart (sympathetic)heart (sympathetic)

md

sp

ACh

ACh


All postganglionic parasympatheticAll postganglionic parasympathetic fibers are fibers arecholinergiccholinergicA A few few postganglionic sympatheticpostganglionic sympathetic fibers are fibers arecholinergiccholinergic

Sweating Sweating SympatheticSympatheticACh ACh


Most Most postganglionic sympatheticpostganglionic sympathetic fibers are fibers areadrenergicadrenergicException: Exception: Postganglionic sympatheticPostganglionic sympathetic fibers fibers are are cholinergiccholinergic

Thermoregulatory Thermoregulatory (eccrine) (eccrine) sweat glandssweat glands Vasodilator sympathetic fibers in the skeletalVasodilator sympathetic fibers in the skeletalmusclesmuscles


ADRENAL GLANDADRENAL GLANDAdrenal cortex and medullaAdrenal cortex and medullaDuctless gland that functions as a ganglionDuctless gland that functions as a ganglionPostganglionicPostganglionic fibers are fibers are cholinergiccholinergic


COTRANSMITTERSCOTRANSMITTERSOther transmitter molecules in addition to the Other transmitter molecules in addition to the primary agents (ACh or NE) primary agents (ACh or NE) Contained in many autonomic nervesContained in many autonomic nervesLocalized in the same vesicle as the primaryLocalized in the same vesicle as the primarytransmitter or in a separate population of vesiclestransmitter or in a separate population of vesicles


COTRANSMITTERSCOTRANSMITTERSATP, enkephalins, VIP, neuropeptide Y,ATP, enkephalins, VIP, neuropeptide Y,substance P, somatostatinsubstance P, somatostatinInvolved in the modulation of synaptic Involved in the modulation of synaptic transmissiontransmission


RECEPTOR CHARACTERISTICSRECEPTOR CHARACTERISTICSA.A. CHOLINOCEPTORSCHOLINOCEPTORS

Also referred as cholinergic receptorsAlso referred as cholinergic receptorsRespond to ACh and its analogsRespond to ACh and its analogs


RECEPTOR CHARACTERISTICSRECEPTOR CHARACTERISTICSA.A. CHOLINOCEPTORSCHOLINOCEPTORS

Subdivided intoSubdivided into1.1. MUSCARINICMUSCARINIC receptors receptors2.2. NICOTINICNICOTINIC receptors receptors


RECEPTOR CHARACTERISTICSRECEPTOR CHARACTERISTICSA.A. CHOLINOCEPTORSCHOLINOCEPTORS1.1. MUSCARINICMUSCARINIC receptors receptors

Respond to muscarine (an alkaloid)Respond to muscarine (an alkaloid)Respond to AChRespond to AChMimics the effects of parasympatheticMimics the effects of parasympatheticG-protein coupledG-protein coupled



Located primarily on autonomic effector cellsLocated primarily on autonomic effector cellsHeartHeartBlood vesselsBlood vesselsSmooth muscles Smooth muscles Presynaptic nerve terminals Presynaptic nerve terminals Exocrine glandsExocrine glands



5 subtypes5 subtypes3 are important in peripheral autonomic transmission3 are important in peripheral autonomic transmission

MM11-nerve endings-nerve endings

MM22-heart, some nerve endings-heart, some nerve endings

MM33-effector cells, smooth muscle, exocrine-effector cells, smooth muscle, exocrine

glands, endotheliumglands, endothelium


RECEPTOR CHARACTERISTICSRECEPTOR CHARACTERISTICSA.A. CHOLINOCEPTORSCHOLINOCEPTORS2.2. NICOTINICNICOTINIC receptors receptors

Respond to ACh Respond to ACh Respond to nicotine (another ACh mimic) Respond to nicotine (another ACh mimic) Do not respond to muscarineDo not respond to muscarineLigand-gatedLigand-gated


RECEPTOR CHARACTERISTICSRECEPTOR CHARACTERISTICSA.A. CHOLINOCEPTORSCHOLINOCEPTORS2.2. NICOTINICNICOTINIC receptors receptors

2 major subtypes2 major subtypesNNnn-neuronal (ANS ganglia)-neuronal (ANS ganglia)

NNmm-neuromuscular endplate (skeletal muscle)-neuromuscular endplate (skeletal muscle)


RECEPTOR CHARACTERISTICSRECEPTOR CHARACTERISTICS CHOLINOCEPTORSCHOLINOCEPTORS

MUSCARINICMUSCARINIC NICOTINICNICOTINIC(G-protein coupled)(G-protein coupled) (ion channel)(ion channel)MM11, M, M22, M, M33 NNnn, N, Nmm


CHOLINOCEPTORSCHOLINOCEPTORSMM11 Nerve endingsNerve endings G-coupledG-coupled Increase IPIncrease IP3 3

MM22 Heart, some nerve endingsHeart, some nerve endings G-coupledG-coupled Decrease cAMP, Decrease cAMP, activates K+ channelactivates K+ channel

MM33 Effector cells, smooth Effector cells, smooth muscle, glands, endothelium muscle, glands, endothelium

G-coupledG-coupled Increase IPIncrease IP33

NNnn ANS gangliaANS ganglia Ion channelIon channel Depolarizes, evokes Depolarizes, evokes action potentialaction potential

NNmm Neuromuscular end platesNeuromuscular end plates Ion channelIon channel Depolarizes, evokes Depolarizes, evokes action potentialaction potential


RECEPTOR CHARACTERISTICSRECEPTOR CHARACTERISTICSB.B. ADRENOCEPTORSADRENOCEPTORS

Also referred as adrenergic receptorsAlso referred as adrenergic receptorsRespond to NERespond to NEG-protein coupledG-protein coupled


RECEPTOR CHARACTERISTICSRECEPTOR CHARACTERISTICSB.B. ADRENOCEPTORSADRENOCEPTORS

Subdivided intoSubdivided into1.1. ALPHAALPHA receptors receptors2.2. BETA BETA receptorsreceptors


RECEPTOR CHARACTERISTICSRECEPTOR CHARACTERISTICSB.B. ADRENOCEPTORSADRENOCEPTORS1.1. ALPHAALPHA receptors receptors

Located inLocated inBlood vesselsBlood vesselsPresynaptic nerve terminalsPresynaptic nerve terminalsBlood platelets Blood platelets Fat cells (lipocytes) Fat cells (lipocytes) Neurons in the brainNeurons in the brain


RECEPTOR CHARACTERISTICSRECEPTOR CHARACTERISTICSB.B. ADRENOCEPTORSADRENOCEPTORS1.1. ALPHAALPHA receptors receptors

2 subtypes2 subtypesALPHAALPHA11-effector tissues, smooth muscles, -effector tissues, smooth muscles, glandsglandsALPHAALPHA22-nerve endings, some smooth -nerve endings, some smooth musclesmuscles


RECEPTOR CHARACTERISTICSRECEPTOR CHARACTERISTICSB.B. ADRENOCEPTORSADRENOCEPTORS2.2. BETABETA receptors receptors

Located on Located on Most types of smooth muscleMost types of smooth muscleCardiac muscleCardiac muscleSome presynaptic nerve terminalSome presynaptic nerve terminalLipocytesLipocytesBrainBrain


RECEPTOR CHARACTERISTICSRECEPTOR CHARACTERISTICSB.B. ADRENOCEPTORSADRENOCEPTORS2.2. BETABETA receptors receptors

3 major subtypes3 major subtypesBETABETA11-heart and kidney-heart and kidney

BETABETA22-lungs, uterus, liver, heart-lungs, uterus, liver, heart

BETABETA33-fat or adipose tissue-fat or adipose tissue


RECEPTOR CHARACTERISTICSRECEPTOR CHARACTERISTICS ADRENOCEPTORSADRENOCEPTORS

ALPHAALPHA BETA BETA(G-protein coupled)(G-protein coupled) (G-protein coupled)(G-protein coupled)ALPHAALPHA11 BETABETA11

ALPHAALPHA22 BETABETA22

BETABETA33


ADRENOCEPTORSADRENOCEPTORSAlphaAlpha11 Effector tissues, Effector tissues,

smooth muscle, smooth muscle, glandsglands

G-G- Increase Increase IPIP33

Increase CaIncrease Ca2+2+ ,causes ,causes

contraction, secretioncontraction, secretion

AlphaAlpha22 Nerve endings, some Nerve endings, some smooth musclesmooth muscle

G-G- Decrease Decrease cAMPcAMP

Decrease transmitter Decrease transmitter release, causes release, causes contractioncontraction

BetaBeta11 Cardiac muscle, Cardiac muscle, kidneykidney

G-G- Increase Increase cAMPcAMP

Increase heart rate, force, Increase heart rate, force, increase renin release increase renin release

BetaBeta22 Lungs, uterus, heartLungs, uterus, heart G-G- Increase Increase cAMPcAMP

Relax smooth muscle, Relax smooth muscle, increase glycogenolysis, increase glycogenolysis, increase HR, forceincrease HR, force

BetaBeta33 Adipose cellsAdipose cells G-G- Increase Increase cAMPcAMP

Increase lipolysisIncrease lipolysis


CENTRAL INTEGRATIONCENTRAL INTEGRATIONPredominant state in any situationPredominant state in any situation

SYMPATHETICSYMPATHETICErgotrophic (energy expenditure)Ergotrophic (energy expenditure)””Fight or flightFight or flight” response” response


CENTRAL INTEGRATIONCENTRAL INTEGRATIONPARASYMPATHETICPARASYMPATHETIC

Tropotrophic (energy saving)Tropotrophic (energy saving)Leading to growthLeading to growth””Rest and digestRest and digest””

RESPONSES OF MAJOR ORGANS TO AUTONOMIC NERVE IMPULSES

OrganOrgan Sympathetic StimulationSympathetic Stimulation Parasympathetic Parasympathetic StimulationStimulation

HeartHeart

Increased heart rate betaIncreased heart rate beta11 (& beta (& beta22)) Decreased heart rateDecreased heart rate

Increased force of contraction betaIncreased force of contraction beta11 (& beta (& beta22)) Decreased force of contractionDecreased force of contraction

Increased conduction velocityIncreased conduction velocity Decreased conduction velocityDecreased conduction velocity

ArteriesArteriesConstriction (alphaConstriction (alpha11))

DilationDilationDilation (betaDilation (beta22))

VeinsVeinsConstriction (alphaConstriction (alpha11))

Dilation (betaDilation (beta22))

LungsLungs Bronchial muscle relaxation (betaBronchial muscle relaxation (beta22))Bronchial muscle contractionBronchial muscle contraction

Increased bronchial gland Increased bronchial gland secretionssecretions

Gastro-Gastro-intestinal tractintestinal tract

Decreased motility (betaDecreased motility (beta22)) Increased motilityIncreased motility

Contraction of sphincters (alpha)Contraction of sphincters (alpha) Relaxation of sphinctersRelaxation of sphincters

RESPONSES OF MAJOR ORGANS TO AUTONOMIC NERVE IMPULSES

OrganOrgan Sympathetic StimulationSympathetic Stimulation Parasympathetic Parasympathetic StimulationStimulation

LiverLiver

Glycogenolysis (betaGlycogenolysis (beta22 & alpha) & alpha)

Glycogen synthesisGlycogen synthesisGluconeogenesis (betaGluconeogenesis (beta22 & alpha) & alpha)

Lipolysis (betaLipolysis (beta22 & alpha) & alpha)

KidneyKidney Renin secretion (betaRenin secretion (beta22))

BladderBladderDetrussor relaxation (betaDetrussor relaxation (beta22)) Detrussor contractionDetrussor contraction

Contraction of sphincter (alpha)Contraction of sphincter (alpha) Relaxation of sphincterRelaxation of sphincter

UterusUterus

Contraction of pregnant uterus (alpha)Contraction of pregnant uterus (alpha)

Relaxation of pregnant and non-pregnant Relaxation of pregnant and non-pregnant uterus (betauterus (beta22))

EyeEye Dilates pupil (alpha)Dilates pupil (alpha)

Constricts pupilConstricts pupil

Increased lacrimal gland Increased lacrimal gland secretionssecretions

Submandibular & parotid Submandibular & parotid glandsglands Viscous salivary secretions (alpha)Viscous salivary secretions (alpha) Watery salivary secretions Watery salivary secretions


PRESYNAPTIC REGULATIONPRESYNAPTIC REGULATIONPrinciple of negative feedback control Principle of negative feedback control Eg, alpha receptors located on noradrenergicEg, alpha receptors located on noradrenergic

terminals which are activated by NE and otherterminals which are activated by NE and othersimilar moleculessimilar moleculesActivation diminishes further the release of NEActivation diminishes further the release of NEfrom these nerve endingsfrom these nerve endings


PRESYNAPTIC REGULATIONPRESYNAPTIC REGULATIONAUTORECEPTORSAUTORECEPTORS

Presynaptic receptors that respond toPresynaptic receptors that respond totransmitter substances released by the transmitter substances released by the nerve endingsnerve endings


POSTSYNAPTIC REGULATIONPOSTSYNAPTIC REGULATIONUp- and down-regulation are known to Up- and down-regulation are known to occur in response to decreased or occur in response to decreased or increased activation of the receptorsincreased activation of the receptorsUp regulation (agonist)Up regulation (agonist)Down regulation (antagonist)Down regulation (antagonist)


PHARMACOLOGIC MODIFICATION OF PHARMACOLOGIC MODIFICATION OF AUTONOMIC FUNCTIONAUTONOMIC FUNCTION

Transmission involves different mechanisms Transmission involves different mechanisms in different segments of the ANSin different segments of the ANSSome drugs produce highly specific effects Some drugs produce highly specific effects Others drugs are much less selective in their Others drugs are much less selective in their actionsactions


PHARMACOLOGIC MODIFICATION OF PHARMACOLOGIC MODIFICATION OF AUTONOMIC FUNCTIONAUTONOMIC FUNCTIONLOCAL ANESTHETICSLOCAL ANESTHETICS

Drug that block action potentialDrug that block action potentialVery nonselective Very nonselective Act on the process that is common to all Act on the process that is common to all neuronsneurons



Drugs that act on the biochemical processes Drugs that act on the biochemical processes involved in transmitter synthesis and storage involved in transmitter synthesis and storage are more selective are more selective



Biochemistry of adrenergic transmission is Biochemistry of adrenergic transmission is very different from cholinergic transmissionvery different from cholinergic transmission

(Table 6-5 Katzung)(Table 6-5 Katzung)



TYRAMINE TYRAMINE ANDAND AMPHETAMINE AMPHETAMINEPromote the release of NEPromote the release of NEEffect is sympatheticEffect is sympathetic

HEMICHOLINIUMHEMICHOLINIUMBlocks uptake of ACh Blocks uptake of ACh Slows synthesis of AChSlows synthesis of ACh



VESAMICOLVESAMICOLPrevents storage of AChPrevents storage of ACh

BOTULINUM TOXINBOTULINUM TOXINPrevents release AChPrevents release ACh



NOREPHINEPHRINENOREPHINEPHRINEBinds alpha receptorsBinds alpha receptorsCauses activation (agonist)Causes activation (agonist)

PHENTOLAMINEPHENTOLAMINEBinds alpha receptorsBinds alpha receptorsPrevents activation (antagonist)Prevents activation (antagonist)



ISOPROTERENOLISOPROTERENOLBinds beta receptorsBinds beta receptorsActivates adenyl cyclase (agonist)Activates adenyl cyclase (agonist)

PROPRANOLOLPROPRANOLOLBinds to beta receptorsBinds to beta receptorsPrevents activation (antagonist)Prevents activation (antagonist)



NICOTINENICOTINECauses skeletal muscle contraction Causes skeletal muscle contraction (agonist)(agonist)

TUBOCURARINETUBOCURARINEPrevents skeletal muscle contraction Prevents skeletal muscle contraction (antagonist)(antagonist)



BETANECHOLBETANECHOLBinds muscarinic receptorsBinds muscarinic receptorsActivates (agonist)Activates (agonist)

ATROPINEATROPINEBinds muscarinic receptorsBinds muscarinic receptorsPrevents activationPrevents activation



NEOSTIGMINENEOSTIGMINEInhibits enzyme acetylcholinesteraseInhibits enzyme acetylcholinesteraseProlongs and intensifies transmitter action Prolongs and intensifies transmitter action

TRANYLCYPROMINETRANYLCYPROMINEInhibits MAOInhibits MAOIncreases stored transmitter pool Increases stored transmitter pool

introduction to autonomic pharmacology

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