Autonomic Nervous System Veterinary Pharmacology Flashcards

Neurotransmitter
Terms Definitions
Parasympathetic EffectsHR:BP:GI:blood volume:
Parasympathetic EffectsHR: slow and regularBP: normalGI: high motor/secretory, extracting nutrientsblood volume: most in dilated visceral vascular bed
Sympathetic effectsHR:BP:GI:blood volume:
Sympathetic effectsHR: increasedBP:GI: decreased digestion, motility, and secretionblood volume: vascular vasoconstriction
Parasympatheticanatomical
craniosacral
Sympatheticanatomical
thoracolumbar
Parasympatheticneurotransmitters
Ach
Sympathetic neurotransmitters
AchNorepi
ParasympatheticPreganglionic fiber:Postganglionic fiber:Effector organ receptor:
ParasympatheticPreganglionic fiber: cholinergicPostganglionic fiber: cholinergicEffector organ receptor: muscarinic
SympatheticPreganglionic fiber:Postganglionic fiber:Effector organ receptor:
SympatheticPreganglionic fiber: cholinergicPostganglionic fiber: adrenergicEffector organ receptor: adrenergic
Somaticneurotransmitter:effector organ receptor:
Somaticneurotransmitter: Acheffector organ receptor: nicotinic muscle
Noradrenergic junctionsynthesis:blocked by:
Noradrenergic junctionsynthesis: tyrosine, dopa, dopamine, norepiblocked by: metyrosine (tyrosine hydrolase inhibitor)
Noradrenergic Junctionstorage blocked by:
Noradrenergic Junctionstorage blocked by: reserpine
Noradrenergic junctionrelease blocked by:
Noradrenergic junctionrelease blocked by: guanethidine
Noradrenergic junctionoutcomes:
Noradrenergic junctionoutcomes:bind adrenergic receptordiffuse to synapsereuptake/recycledegraded by monoamine oxidase
Cholinergic junctionsynthesis:blocked by:
Cholinergic junctionsynthesis: choline, AcCoA, Achblocked by: hemicholiniums
Cholinergic junctionstorage blocked by:
Cholinergic junctionstorage blocked by: vesamicol
Cholinergic junctionrelease:blocked by:
Cholinergic junctionrelease: voltage-dependent changesblocked by: botulism toxin
Cholinergic junctionoutcomes:
Cholinergic junctionoutcomes:bind nicotinic or muscarinic receptordiffuse to synapsereuptake/recycledegraded by acetylcholinesterase
Increase in arterial BPeffect on baroreceptor:efferent sympathetic nerve activity:efferent parasympathetic nerve activity:
Increase in arterial BPeffect on baroreceptor: stretchesefferent sympathetic nerve activity: decreasesefferent parasympathetic nerve activity: increases
Decrease in arterial BPeffect on baroreceptor:efferent sympathetic nerve activity:efferent parasympathetic nerve activity:
Decrease in arterial BPeffect on baroreceptor: unloadsefferent sympathetic nerve activity: increasesefferent parasympathetic nerve activity: decreases
Adrenergic Receptor Agonistsalpha 1 >> alpha 2
phenylephrinemethoxamine
Adrenergic Receptor Agonistsalpha 2 >> alpha 1(alpha)
detomidinemedetomidineclonidinexylazine
Adrenergic Receptor Agonistsalpha 1 = alpha 2B1 >> B2(alpha and beta)
norepinephrine
Adrenergic Receptor Agonistsalpha 1 = alpha 2B1 = B2(alpha and beta)
epinephrine
Adrenergic Receptor AgonistsB1 > B2 >>>> alpha(beta)
dobutamine
Adrenergic Receptor AgonistsB1 = B2 >>>> alpha(beta)
isoproterenol
Adrenergic Receptor AgonistsB2 >> B1 >>>> alpha(beta)
terbutalinealbuterol
Adrenergic Receptor AgonistsD1 = D2 >> B >> alpha
dopamine
Adrenergic Receptor Antagonistsalpha 1 >>>> alpha 2(alpha)
prazosin
Adrenergic Receptor Antagonistsalpha 1 > alpha 2(alpha)
phenoxybenzamine
Adrenergic Receptor Antagonistsalpha 1 = alpha 2(alpha)
phentolamine
Adrenergic Receptor Antagonistsalpha 2 >> alpha 1(alpha)
yohimbinetolazolineatipamezole
Adrenergic Receptor AntagonistsB1 = B2 >_ alpha 1 > alpha 2(mixed)
labetalolcarvedilol
Adrenergic Receptor AntagonistsB1 >> B2(beta)
metoprololatenolol
Adrenergic Receptor AntagonistsB1 = B2(beta)
propranolol
Adrenergic Receptor AntagonistsB2 >>> B1(beta)
butoxamine
Cardiovascular responsesmean arterial pressureNE:Epi:Iso:
Cardiovascular responsesmean arterial pressureNE: incEpi: incIso: dec
Cardiovascular responsesfemoral blood flowNE: Epi: Iso:
Cardiovascular responsesfemoral blood flowNE: decEpi: incIso: inc
Cardiovascular responsesrenal blood flowNE:Epi:Iso:
Cardiovascular responsesrenal blood flowNE: decEpi: dec Iso: inc
Cardiovascular responsesperipheral resistanceNE:Epi:Iso:
Cardiovascular responsesperipheral resistanceNE: incEpi: incIso: dec
Cardiovascular responsesmyocardial contractile forceNE:Epi:Iso:
Cardiovascular responsesmyocardial contractile forceNE: incEpi: incIso: inc
Cardiovascular responsesheart rateNE:Epi:Iso:
Cardiovascular responsesheart rateNE: decEpi: incIso: inc
Cardiovascular responsescardiac outputNE:Epi:Iso:
Cardiovascular responsescardiac outputNE: NA (inc)Epi: incIso: inc
receptordef
component of cell that interacts with a drug (neurotransmitter) and initiates a chain of biochemical events (pharm effects)
PNS responses are primarily subserved by ________ receptors
PNS responses are primarily subserved by MUSCARINIC receptors
ganglionic transmission is mediated by _________ receptors
ganglionic transmission is mediated by NICOTINIC receptors
cholinergic fibersdef.nervous system location
nerve fibers that synthesize and release acetylcholineparasympathetic, sympathetic, and somatic3 types: pregang, postgang, somatic
adrenergic fibersdef.nervous system location
nerve fibers that synthesize and release norepinephrinesympathetic
3 endogenous catecholamines
dopaminenorepinephrineepinephrine
only NANC postganglionic neurotransmitter:
nitric oxide NO
arterial smooth muscle is generally not innervated by the ___
arterial smooth muscle is generally not innervated by the PNS
cholinergic receptors in most arterial beds are not associated with ___________ nerves
cholinergic receptors in most arterial beds are not associated with PARASYMPATHETIC nerves
in skeletal muscle arteries, _____ receptors are more sensitive than _____ receptors
in skeletal muscle arteries, BETA receptors are MORE sensitive than ALPHA receptors
in visceral blood vessels, ____ receptors are more important than ____ receptors
in visceral blood vessels, ALPHA receptors are more important than BETA receptors
agonist
bind to and activate the receptor
antagonist
by binding to a receptor, prevent binding by other molecules
alpha 1 receptoragonist
Epi = NE >> Iso
alpha 1 receptorantagonist
Prazosin
alpha 1 receptortissue:response:
tissue: vascular smooth musclelivergenitourinary smooth muscleresponse: contract, glycogenolysis, gluconeogenesis
glycogenolysis
breakdown glycogen
alpha 1subtypes
1A1B1D
alpha 2 receptoragonist
Epi = NE >> Iso
alpha 2 receptorantagonist
yohimbine
alpha 2 receptortissue:response:
tissue: presynaptic nerve terminalsvascular smooth musclepancreatic isletsresponse: decreased release NEcontractdecreased insulin release
alpha 2 receptorsubtypes
2A2B2C
beta 1 receptoragonist
Iso > Epi = NE
beta 1 receptorantagonist
metropolol
beta 1 receptortissue:response:
tissue: heartjuxtaglomerular cellsresponse: increased contractility, HR, conduction velocityincreased renin secretion
beta 2 receptoragonist
Iso > Epi >> NE
beta 2 receptor antagonist
no specific drugICI 118551 in industry
beta 2 receptortissue:response:
tissue: smooth muscleliverresponse: relax/ dilate skeletal arteriolesglycogenolysis
beta 3 receptoragonist
Iso = NE > Epi
beta 3 receptorantagonist
ICI 118551
beta 3 receptortissue:response:
tissue: adiposeresponse: lipolysis
cholinergic receptors
nicotinic musclenicotinic neuralmuscarinic
nicotinic muscle receptoragonist
Ach
nicotinic muscle receptorantagonist
tubocurarine
nicotinic muscle receptortissue:response:
tissue: neuromuscular junctionresponse: endplate depolarizationskeletal muscle contraction
nicotinic neural receptoragonist
Ach
nicotinic neural receptorantagonist
trimethaphan
nicotinic neural receptortissue:response:
tissue: autonomic gangliaadrenal medullaCNSresponse: depolarizationsecretion catecholaminesfiring postganglionic neurons
muscarinic 1 receptoragonist
Ach
muscarinic 1 receptorantagonist
atropine
muscarinic 1 receptortissue:response:
tissue: autonomic gangliaCNSresponse: depolarizationundefined
muscarinic 2 receptoragonist
Ach
muscarinic 2 receptorantagonist
atropine
muscarinic 2 receptortissue:response:
tissue: heartmyocardiumresponse: decrease HR (dec contractile force, not as prominent)hyperpolarization (SA node)
M1 primarily __________
M1 primarily PARASYMPATHETIC
muscarinic 3 receptoragonist
Ach
muscarinic 3 receptorantagonist
atropine
muscarinic 3 receptortissue:response:
tissue: smooth musclesecretory glands(vascular endothelium)response: dilate BVincreased secretion
smooth muscle receptors
alpha 1alpha 2beta 2M3
pressure = _____ x _______
pressure = cardiac output x resistance
cardiac output = ____ x _____
cardiac output = heart rate x stroke volume
cardiac sympathetic-mediated responses are _______
cardiac sympathetic-mediated responses are EXCITATORYincrease HR
cardiac parasympathetic-mediated responses are ______
cardiac parasympathetic-mediated responses are INHIBITORYdecrease HR
change in bladder tensionmuscarinic agonist
contract body
change in bladder tensionalpha agonist
contract neck and base
change in bladder tensionB agonist
relax body
bladderB:alpha:
B: dilationalpha: contraction
Bladder Fillingexternal sphincter ______ by ______ nervesinternal sphincter _______ by _______ nerves, _______ receptorsbladder body ______ by ________ nerves, _____ receptors________ receptors inhibiting _________________ P
Bladder Fillingexternal sphincter CONTRACTION by SOMATIC nervesinternal sphincter CONTRACTION by SYMPATHETIC nerves, ALPHA 1 receptorsbladder body RELAXATION by SYMPATHETIC nerves, B2 receptorsADRENERGIC (ALPHA 2)receptors inhibiting PARASYMPATHETIC GANGLIA SACRAL PNS outflow inactive
Bladder Filling - Adrenergic inhibiting parasympathetic____ from postganglioc sympathetic activates presynaptic ______activated ______ inhibits ____ release from preganglionic parasympathetic_____ muscle contraction
NOREPINEPHRINE from postganglioc sympathetic activates presynaptic ALPHA 2 RECEPTORSactivated ALPHA 2 inhibit ACH release from preganglionic parasympatheticDECREASED muscle contractionbladder fills
Bladder emptyinginhibition of ____ ____ activity and _____ ____ outflowactivation of _____ _____ outflow by ________ receptorsM3 stimulation by ____ leads to _______ contractionB stimulation by ______ leads to ______ relaxat
inhibition of EXTERNAL SPHINCTER activity and SYMPATHETIC NERVE outflowactivation of PARASYMPATHETIC NERVE outflow by MUSCARINIC receptorsM3 stimulation by ACH leads to ACTIVE contractionB stimulation by NOREPI leads to ACTIVE relaxationM2 stimulation by ACH leads to INDIRECT contraction by inhibiting RELAXATION
Bladder EmptyingM3 stimulation causes contraction by _____ _______ and accumulation of _____
M3 stimulation causes contraction by PHOSPHOINOSITOL HYDROLYSIS and accumulation of CALCIUM
Bladder EmptyingM2 activation indirectly leads to contraction by inhibiting _________ ________ and _____ receptors
M2 activation indirectly leads to contraction by inhibiting ADENYLATE CYCLASE and B2 receptors
NANC transmitters and Bladder Function______ is a NANC transmitter
ATP
NANC transmitters and bladder function_____ _______ _______ is localized in nerve fibers of trigonal and urethral tissue
Nitric Oxide Synthase NOS
NO may influence bladder tone by modulation of ____ release
ACH
Overactive bladderM3 receptorsstimulation by:leads to:receptors also located:
M3 receptorsstimulation by: Achleads to: smooth muscle contraction, bladder emptyingreceptors also located: salivary glands
Overactive bladderTolterodineeffect:type of drug:
Tolterodineeffect: greater bladder than salivation inhibition, no dry mouthtype of drug: competitive muscarinic receptor antagonist, bladder selectivity
Overactive bladderOxybutynineffect:type of drug:
Oxybutynineffect: greater effect on salivation, dry mouthtype of drug: selective muscarinic receptor antagonist
Overactive bladderAtropineeffect:
Atropineeffect: same effects on bladder and salivation
Overactive bladder selectivity for ___ receptors over other muscarinic subtypes is not necessary for effective inhibition of bladder ______, may result in more pronounced effects on _______
selectivity for M3 receptors over other muscarinic subtypes is not necessary for effective inhibition of bladder CONTRACTION, may result in more pronounced effects on SALIVATION
Stressed urinary incontinenceOnuf's nucleuslocation/pathway
Onuf's nucleus in sacral spinal cordalpha motor neurons/somatic motor neurons out to external urethral sphincter
Onuf's nucleusglutamate
excitatory amino acidpower ON button, raises synaptic cleft levels of NE and serotonin
Onuf's nucleusDuloxetine
NE and serotonin/5-HT reuptake inhibitorincreases receptor activation
Food safety regulatory agenciespharmaceuticals:biologics/vaccines:pesticides:nutritional supplements:
pharmaceuticals: FDAbiologics/vaccines: USDApesticides: EPAnutritional supplements: none
Food safetyFARAD
Food Animal Residue Avoidance Databankestablish appropriate withdrawal times in cases of extralabel drug use
Drug residuesTolerance TOL
maximum level of drug residue allowed in edible tissue
Drug residuesWithdrawal time WDT
length of time from the last treatment for drug residues to deplete to or below TOLminimum length of time that must be waited prior to slaughtering
Drug residuesExtralabel drug use ELDU
administering drug in manner different than label directions
AMDUCA
Animal Medicinal Drug Use Clarification Act
ELDU allowed under certain conditions:
valid DVM-client-patient relationshipnot permitted by lay personadequate info available to establish WDTELDU of feed additives strictly prohibitedELDU due to cost not allowedall approved drugs are ineffectivecareful diagnosis"substantially extended" WDT is establishedensure ID of treated animalsassure WDT is followed
drugs prohibited from ELDU under AMDUCA
diethylstibestrol (DES)chloramphenicolnitroimidazoles (metronidazole)sulfonamides in dairy >- 20moclenbuteroldipyronefluoroquinolonesglycopeptidesnitrofuransphenylbutazone in dairy >- 20mo
ELDUGrade A Pasteurized Milk Ordinance PMO
FDA regulatory ordinanceprohibits use of:dimethyl sulfoxide DMSOcolloidal silver
_______ should be contacted for appropriate _____ in cases of ELDU
FARAD should be contacted for appropriate WDT in cases of ELDU
Thalidomideprohibited b/c:
concern of human exposure and birth defects
Causes of illegal residues
failure to follow WDTfailure to identify treated animalsfailure to follow label directions
route of administration effects
IM and SC not always identicalpoor technique - inject into fascial plane instead of IM, poor vascular supply, delayed/incomplete absorptionimproper location - SC in ear b/c discarded at slaughter
aminoglycosidesgentamicinpro:con:
pro: effective against some resistant gram negative bac, inexpensivecon: renal tubular reabsorption means in the kidneys for prolonged time (18mo)
Food animal drug approvals require:
extensive safety evaluationresidue depletion studiesregulated by FDA
Extralabel Drug use
allowed under AMDUCArequires specific conditionscertain drugs prohibited
illegal residues
from failure to follow directionsoccur infrequently
Cholinergic receptorstypes
nicotnicmuscarinic
Nicotinic receptorssubtypes
NmNn
Nicotinicagonists
Achnicotine
Nicotinicresponse
NMJautonomic gangliaadrenal medulla
Nicotinicantagonists
TubocurarineTrimethaphan
Muscarinicsubtypes
M1M2M3
Muscarinicagonists
Achcholine esters
Muscarinicresponse
myenteric plexusheartbladdereyesmooth muscleurinary bladderGI sphincters
Muscarinicantagonists
Atropine
Cholinergic stimulants2 broad categories
direct-actingindirect-acting
cholinergic stimulants activate cholinergic receptors2 types
muscarinicnicotinic
muscarinic targets
nerveheartglands
nicotinic targets
neuromuscular ganglionic
cholinergic stimulantsdirect acting
similar to achactivate cholinergic receptors located on the effector cells
cholinergic stimulantsindirect acting
(cholinesterase inhibitors)allow endogenous Ach to accumulate and thereby prolong/augment its actionraises Ach levels
2 types of direct acting receptor agonists
choline estersalkaloids
choline esters
achmethacholinecarbacholbethanecol
alkaloids
muscarinepilocarpine
nonuniform susceptibility to _________nonuniform affinities for _______nonuniform ____ ______ effects
nonuniform susceptibility to CHOLINESTERASEnonuniform affinities for MUS AND NIC RECEPTORSnonuniform TARGET ORGAN effects
remove Ach with ______
ACETYLCHOLINESTERASE
Acetylcholinesterase inhibitors
neostigminephysostigmineedrophonium
Acetylcholinesterase inhibitorsmech action
inhibit acetylcholinesterase leading to increase in conc endogenous Ach
Acetylcholinesterase inhibitorstarget organ effects
similar to effects of direct-acting cholinergic agonists
Neostigmine lacks ___________ whereas __________ produces them
Neostigmine lacks CNS EFFECTS whereas PHYSOSTIGMINE produces them
Neostigmine affects _____ more than the _______
Neostigmine affects NMJ more than the ANS
Physostigmine affects ____ more than the ______
Physostigmine affects ANS more than the NMJ
Muscarinic receptor antagonists
atropineglycopyrrolatescopolamine
Muscarinic receptor antagonistsmech action
cause reversible blockade (comp ant) of actions of cholinomimetics at muscarinic receptors
muscarinic receptors are generally ________
NONSELECTIVE (receptor subtypes)can be regionally selective
Muscarinic receptor antagoniststarget organ effectseye:CV:GI:bronchioles:bladder:sweat glands:CNS:
eye: pupillary dilation, loss of accomodationCV: increase HR, may increase CO due to tachycardicGI: relax smooth muscle, decreased secretionsbronchioles: decrease secretions, increase luminal diameterbladder: urine retention due to inhibition smooth musclesweat glands: decrease sweating in humansCNS: excessive doses cause hallucinations/disorientation in humans, mania/excitement in domestics
Biosynthetic pathway for Nitric oxidelocation:substrates:enzyme:product:inhibitor:
location: endotheliumsubstrates: O2, L-arginineenzyme: NO synthaseproduct: NOinhibitor: L-name (competitively inhibits NOS)
Equine sweatingsympathetic nerves activate _________ in skin to evoke _________
sympathetic nerves activate BETA-ADRENERGIC MECHANISMS in skin to evoke THERMOREGULATORY SWEATING
L-name inhibits __________ and decreases __________
L-name inhibits NITRIC OXIDE SYNTHASE (NOS)and decreases SWEAT RATE
in humans, sweat glands are innervated by ____________
SYMPATHETIC CHOLINERGIC FIBERS
equine sweatingatropineblocked:no sig effect on:suggests:
blocked: sweatingno sig effect on: blood flowsuggests: independent mech
equine sweatingbotulism toxinmech:prevents:which suggests:
mech: presynaptically inhibits Ach release prevents: sweating and rise in skin blood flowsuggests: substance (NO?) cotransmitted with Ach to evoke rise in skin blood flow
neuromuscular blocking drugs
specifically block neuromuscular transmissionused with general anesthesia
normal neuromuscular transmissiondepolarization ofrelease ofbinds toopensinflux ofmetabolized by
depolarization of motor nerverelease of AchAch binds to nicotinic receptors on motor end plateopens membrane channelinflux of Na and KAch metabolized by acetylcholinesterase
Nicotinic receptordef:what binds:result:
transmembrane protein with ion channel pore that is usually closedAch binds to alpha subunitsconformation change in protein, ion channel opens, ions flow, membrane depolarizes
Nondepolarizing NMB
competitive antagonists to Ach at nicotinic receptorsprevent binding of Achreversible
cholinesterase inhibitor
biases competition in favor of Ach by allowing build-up Ach and displacing NMB
Nondepolarizing NMBhighly ______poorly _________do not cross _________act _________
highly polarpoorly lipid solubledo not cross blood brain barrieract peripherally
Nondepolarizing NMBside effects
ganglionic blockade at higher dosageshistamine releasereversal agents have muscarinic side effectspretreat with atropine
Nondepolarizing NMBdrug interactionsaugmented by:potentiated by:
augmented by: inhalation anestheticspotentiated by: aminoglycosdie antibiotics
Common nondepolarizing NMB
gallaminepancuroniumd-tubocurarineatracurium
reversal agents for nondepolarizing NMB
neostigminephysostigmineedrophonium
Effects of NMB
muscle paralysisprogression: eye, facial, pharyngeal, limb, torso, diaphragm
CNS transmitters
GABAglycineglutamate and aspartatenorepidopamine5-hydroxytryptamine (serotonin)
GABA
main inhibitory transmitter in brain
Gaba-a receptors:Gaba-b receptors:
Gaba-a receptors: postsynapticGaba-b receptors: presynaptic inhibition
agonistsGaba-a:Gaba-b:
Gaba-a: muscimolGaba-b: baclofen
antagonistsGaba-a:
Gaba-a: bicucullin, picrotoxin
GABAreceptor mech
increases chloride conductance, hyperpolarizes
Glycine
inhibitory transmitter in spinal cord
Glycineagonist
taurine
Glycineantagonist
strychnine
Glycinereceptor mech
increases chloride conductance, hyperpolarizes
Glutamate and aspartateclassified as:mediate:anatomy:
excitatory amino acids EAAmediate fast excitatory responses in CNSinterneurons at all levels: spinal and supraspinal
Glutamate and aspartate3 main EAA receptor subtypes
NMDAAMPAkainate
Glutamate and aspartatereceptor mechNMDA:AMPA:metobotropic:
NMDA: slow EPSPAMPA: fast EPSPmetobotropic: neural modulation by many mech
Norepianatomy
all levelslong axons from pons and brainstem
Norepiagonists
alpha 2: xylazine, medetomidine, clonidine
Norepiantagonist
yohimbine
Norepireceptor mech
G protein mediated effects on generation of second messengers and on activity of ion channels
Dopamineanatomy
all levelsshort, medium, and long connections
Dopamineagonist
apomorphine
Dopamineantagonist
phenothiazines and butyrophenones (preanesthetics)
Dopaminereceptor mech2 types receptors:CNS effects:
2 types receptors: D1 and D2CNS effects: mainly inhibition, pre and post synaptic
5-hydroxytryptamineanatomy
5-HT neurons concentrated in midline raphe nuclei in pons and medulla project diffusely to cortex, limbic system, hypothalamus, spinal cord
5-HTantagonist
ketanserin
5-HTreceptor mecheffects:functions associated with pathways:
effects: inhibitory or excitatory, pre or post synapticfunctions: feeding beh, control of mood, emotion, sleep/wake, sensory pathways, nociception, body temp, vomiting
paindef.
coupling of an unpleasant stimulus with conscious perception and an emotional response
nociceptiondef.
sensation of an unpleasant stimulus
nociceptorsdef.
free nerve endings distributed thruout the body which detect nociceptive stimuli
Why feel pain? (3)
warning of actual tissue injurywarning of impending tissue injurywarning of danger to a social group
sensitization
stimulus which is normally innocuous becomes a nociceptive stimulus
Sensitization1.2.
Sensitization1. Central2. Peripheral
SensitizationCentral (3)
NMDA receptor activation increase in magnitude and response of stimulus - pain is worse reduced activation threshold of nociceptors - pain occurs w/ less of stimulusdecreased endogenous opioidsdesensitization of opiate receptors
SensitizationPeripheral (2)
reduced nociceptor activation thresholdsdecreased tissue pH, cytokines, bradykinin, serotonin, histamine, ATP, prostaglandins, leukotrienes
Peripheral nerves3 axon types
sensory afferentmotor efferentautonomic
Sensory afferent peripheral nervesA-fiber:Aalpha, AB:Adelta:C-fiber:
Sensory afferent peripheral nervesA-fiber: large myelinated nerves, rapid conductionAalpha, AB: prorioception, tactileAdelta: nociception; "first" pain, well localizedC-fiber: unmyelinated, slow conducting; "second" pain, dull aching, poorly localized
Dorsal root ganglionreceptor +, propagate transmission of painful stimulus (3)
AMPA (glutamate)NMDA (glutamate) - loses its Mg block after AMPA activatedPGE2 (COX-2)
Dorsal root ganglionreceptor -, inhibit transmission of painful stimulus (4)
opiate (u, k, delta)alpha-2 (norepi)5-HT (serotonin)GABA (y-aminobutyric acid)
pain transmitted primarily byreceptor:neurotransmitter:
pain transmitted primarily byreceptor: AMPAneurotransmitter: glutamate
Second order neuron_____ to ______primary projection
SPINAL CORD to THALAMUSspinothalamic tract
Second order neuronreceptors+:-:
Second order neuronreceptors+: glutamate, AMPA, NMDA-: GABA, alpha-2, 5-HT
Cerebral cortexprimary projections:
thalamocortical
Cerebral cortexreceptors+:-:
Cerebral cortexreceptors+: glutamate, AMPA, NMDA-: opiate, 5-HT, alpha-2, GABACOX-1 and COX-3 (NSAIDS acetaminophen)
opiatedef.
compound derived from opium plant
opioiddef.
endogenous peptide or synthetic compound interacting on opiate receptors
opioidsprimary metabolism:
opioidsprimary metabolism: hepaticphase I and/or II
Opiate receptors(3)
Mu - endorphin, endogenous ligandKappa - dynorphin, endogenous ligandDelta - enkephalin, endogenous ligand
Opioid effectsa lot
analgesiaeuphoriasedationantitussivenausea/vomitingdec stomach, biliary, pancreatic, and intestinal secretionsdec GI motilitydec urine voidinginc tone antrum stomachdiuresismiosis - dogmydriasis - catpantingwith large doses: dec BP and respirationimmunomodulation
antitussive effectdepression of:independent of:
antitussive effectdepression of: cough center in medullaindependent of: respiratory effects
nausea/emesis effectdirect stimulation of:not protected by:
nausea/emesis effectdirect stimulation of: CRTZnot protected by: blood brain barrier
GI tract (antidiarrheal) effectdecrease:decrease:increase:can cause:
GI tract (antidiarrheal) effectdecrease: secretionsdecrease: in propulsive contractionsincrease: in non-propulsive rhythmic contractionscan cause: constipation
opiate receptorsmu
analgesiaresp antitussivedec GIsedationeuphoria
opiate receptorsk
analgesia, antitussive, dec GI, sedation, inc diuresis
opiate receptorsdelta
analgesia
opioid receptor locations(3)
spinal supraspinalperiphery(GI tract)(other - synovium, leukocytes)
opioid receptor locationssynergistic analgesia between ______ and ______ receptors
synergistic analgesia between SPINAL and SUPRASPINAL receptors
opioid receptor locationsspinal
pre and postsynaptic at dorsal root ganglion
opioid receptor locationssupraspinal
medulla, hypothalamus, periaqueductal gray area, amygdala, cerebral cortex
opioid drugs classified by:____ they interact with and the ______ elicited
opioid drugs classified by:RECEPTORS they interact with and the EFFECT elicited
potency
concentration which elicits the effectaffects dose
efficacy
magnitude of the effectaffects analgesic effect
opiate receptor activation_______ inhibition of ________
opiate receptor activationG-PROTEIN inhibition of ADENYLYL CYCLASE
G-protein inhibition of adenylyl cyclasedec:inc:dec:net:
G-protein inhibition of adenylyl cyclasedec: cAMPinc: receptor linked K currents - inc outward flowdec: voltage-gated Ca currents - dec inward flownet: hyperpolarization of membrane potential
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Term:
Definition:
Definition:

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