Pharmacology Study GuideTest 2.docx
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Pharmacology Study GuideTest 2.docx
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PharmacologyStudyGuideTest2
PharmacologyStudyGuide–Test2
AnalgesicAgentsCh.10
☐Analgesic:
relivespainw/ocausingunconsciousness
☐Pain:
mostcommonlydescribedasunpleasantsensory&emotionalexperienceassociatedw/eitheractualorpotentialtissuedamage.
☐Painthreshold:
levelofstimulustoproduceperceptionofpain
☐Paintolerance:
amountofpainaPTcanendurew/oitinterferingw/normalfx.
☐Acutepain:
suddeninonset;subsidesw/tx
☐Chronicpain:
persistent&recurring
☐Somaticpain:
originatesfromskeletalmuscles,ligaments&joints
☐Visceralpain:
originatesfromorgans/smoothmuscles(superficial)skin,mucousmembranes
oVisc/superficialtx=opiods
oSomaticpaintx=nonopiods
☐Vascularpain:
originatesfromsomepathologyofthevascularorperipheraltissues
☐Referredpain:
visceralneverfiberssynapsingatalevelinthespinalcordclosetofibersthatsupplyspecificsubQtissuesinthebody
☐Neuropathicpain:
injury/damagetoperinervefibersordamagetoCNS
☐Phantompain:
removedbodypart(burning,itching,tingling)
☐Cancerpain:
manycauses,i.e.pressureontissues,organsornerves,hypoxia,blockagetoanorgan,matastisis,pathologicfractures,musclespasms,sideefxofradiation,surg&chemo
☐Phsychogenicpain:
psychologicalfactorsthatactuallystimulatesnervepainimpulses
☐Centralpain:
tumors,trauma,inflammationofbrainandmayoccurwithanyconditionthatinducesCNSdamage
TypeofFiber
Myelinsheath
Fibersize
Conductionspeed
Typeofpain
A
Yes
Large
Fast
Sharp/local
C
No
Small
Slow
Dull/nonlocalized
Neuronregulation:
1.Conductinganactionpotential
2.releasingneurotransmitter
3.bindingtransmittermoleculestoreceptors
PainGateTheory
Massagetoarearelievespain…largesensoryfibersfromperireceptorscarryimpulsestospinalcord…thiscausesimpulsetransmissiontobeinhibited&gateclosed,whichreducestherecogofpainimpulsesarrivingbymeansofthesmallfibers.Opiodsworkinthisway.p.149
StepsinJunctionalTransmission
Synthesis:
atransmittersubstanceisneeded
Storage:
thistransmittermustbestoreduntilreleased
Release:
triggeredbyanactionpotentialattheaxonterminal
Receptorbinding:
afterrelease,transmitterundergoesreversiblebindingtoreceptorsite
Termination:
removaloftransmitteroccurs
PNSRX
▪Cholinergics:
eitherblockorstimulateactionsofAch
▪Blockers:
muscarinics,ganglionics,neuromuscularblockers,cholinesteraseinhibitors
▪Adrenergicagonists(epi)vs.antagonistsblockorstimulateSNS
▪Indirectactingantiadrenergics
▪NeurologicRx:
pathoofdisorderisdepletionofdopamine(inhibtransmitter)i.e.Levodopa;carbidopalevodopa
▪EpilepsyTX:
reducerateofd/cofneurons;preventspreadofseizurestorestofbraini.e.phenytoin;Phenobarbital;tegretol;diazapam
▪Musclespasm/spasticityRXi.e.analgesics(ASA),centrallyactingrelaxants(Diazapam)
OpioidAnalgesics(only3clinicallyuseful,morphine,codeine,papaverine)
Mechanismofaction&DE
¦Agonistbindstoopioidpainreceptorinbrain&causesananalgesicresponse
¦Partialagonist:
bindstopainreceptorandcausesonlylimitedactions
¦Antagonist:
reversestheefxoftheseonpainreceptors
¦Primarilybindtomu,kappa&deltareceptors
¦ManyopiodshaveaffinityforCNS…suppressmedullarycoughcenter
¦Strongopiodsforsurgery:
fentanyl,sufentanil,alfentanil(balancedanesthesia)
¦Post-oppainTX:
Morphine,meperidine,oxycodone,MSContin…longacting
¦Analgesia:
codeine(alsoantitussive)
NSAIDS
¦Lodine:
dental
¦Ibuprofen:
onlyOTCNSAID
¦Indocin:
ifASAorTylenoldoesn’twork
¦Naprosyn:
fortxofO/A(monitoreffectiveness)
MixedNarcotics&Non-narcotics:
¦Percoset:
mixedwithTylenol
¦Perdocan:
mixedwithASA
¦Darvon&DarvonN:
weakerinaction,analgesic,sedative?
¦Vicodin:
Tylenol&narcotic
¦Stadol:
usedinMCH,pre-op,watchforOD,changeinalertness,hallucinations
NARCOTICANTAGONIST:
NARCAN:
usedIVforimmediateaction,blocksmu&kappareceptors;reversesopiodworksinmins,usedwhenresparebelow10/Rperminute,minimaltoxicity
CONTRAINDICATIONS:
allergy,asthma,RTinsufficiency,elevatedICP,pregnancy
SE/AE:
euphoria,dependence,tachycardia,BP,mentalagitation,nausea,vomitingconstipation,urinaryretention,pruritis(duetohisrelease),flushing,orthostatichypotension…serioussideefx=CNSdepressionwhichleadstoR.dep
Non-OpioidAnalgesics(primary:
Acetominophen(alldrugsinNSAIDclass)
Mechanismofaction&DE
¦SimilartoSalicylates…blockedpainimpulsesperipherallviaresponsetoprostaglandininhibition
¦Acetaminophen:
↓feverbyactingonthehypothalamus;vasodilation&heatloss
Noeffectonplatelets,cardiovascularorrespiratorysystem,oracid-basechanges
¦Fever,moderatepainTX
NOTSUREIFTHISDRUGWILLBEONTEST
CNSDepressents&MuscleRelaxantsCh.12
Sedatives:
reducenervousness,excitability&irritabilityw/ocausingsleep
Hypnotics:
morepotentthansedatives;causessleep
Sedative-hypnotics:
barbiturates;benzodiazepines,etc.
Barbituates
¦Firstusedfortxofinsomnia&producingsedation;narrowtherapeuticindex
Mechanismofaction&DE
¦CNSdepressantworksinthereticularformation
¦InhibitsnerveimpulsetransmissiontravelingtoareasofbrainduetoabilitytopotentiateaninhibitoryaminoacidGABA
¦Lowdosesactassedatives
¦Highdosesactashypnotics
¦Causeenzymesinlivertometabolizedrugsmorequickly,whichshortenstheiractions.
¦Capableofraisingtheseizurethreshold
¦Usedashypnotics,sedatives,anticonvulsants&anesthesiaforsurgicalprocedures.Differinpotency,onset,durationofaction
oUltrashort:
anesthetics
oShort:
sedative-hypnotic
oIntermediate:
anticonvulsant&sedative-hypnotic
oLong:
sedative-hypnotic;anticonvulsant
¦Longacting:
Phenobarbital&shortactingPentobarbital(Nembutal)
CONTRAINDICATIONS:
pregnancy,significantrespiratorydifficulties&severeliverdisease
SE/AE:
drowsiness,lethargy,dizziness,hangover,restlessnessorexcitement;affectnormalsleepbydeprivingREM.Adversereaction:
respiratorydepression;CNSdepression
Toxicity:
activatedcharcoal,assistedrespiration,interactionsw/alcohol,antihistamines,benzodiazepines,opioids&tranquilizers…mostaresecondarytoefxonhepaticenzymesystemi.e.MAOIcoadmin…canresultin↓anticoagulationresponseandclotformation
Benzodiazapines(mostcommonlyprescribedsedative-hypnotics)
Mechanismofaction&DE
¦DepressCNS(hypothalamus,thalamus&limbicsystems)byinhibitingstimulationofbrain
¦ReceptorsthoughttobethoseofinhibitorytransmitterGABA
¦TheydoNOTsuppressREMsleeporinducehepaticmicrosomalenzymeactivity,sosafetoadmitoPTtakingmedsmetabolizedbythisenzymesystem
¦Calmingeffect;controlsagitation&anxietybyinhibitionofhyperexcitablenerves
¦Skeletalmusclerelaxation
¦UsedinTxofalcoholwithdrawal,agitation,depressionandepilepsy
¦Txissymptomatic&supportive
CONTRAINDICATIONS:
pregnancy,narrowangleglaucoma&otherCNSdepressants&coadminw/MAOIs
SE/AE:
drowsiness,headache,excitementornervousness;dizzy&lethargyAdverseefx:
canleadtofallsinelderly,alsoeffectnormalsleepcycle“hangovereffect”
Toxicity:
confusion/coma;diminishedreflexes,somnolence,syrupofipecacgenerallyused,gastriclavage
MuscleRelaxants(neededforconditionssuchastrauma,inflammation,anxiety,pain…canbeassocw/acutemusclespasms)
MechanismofactionandDE
¦Workw/CNS&actionscomefromsedativeefxratherthandirectmusclerelaxation…actonnervetransmissioninspinalcord..enhanceGABA’scentralinhibitoryefx@spinalcord
¦OnlyONEworksdirectlyonskeletalmuscle:
dantrolene
¦EffectsarearesultofCNSdepressioninbrainatlevelofbrainstem,thalamus&basalganglia
¦Txofmuscle-skeletalconditions(spasms,chorea…Involuntarydancingorwrithingofthelimbsorfacialmuscles,spasticity),suchasMS,cerebrallesions,cerebralpalsyorrheumaticdisorders.Huntingtonschorea,↓rigidityinparkinsoniansyndromeorpainassocw/trigeminalneuralgia
¦Flexeril,baclofen(akaLioresal,Atrofen)forTXofhiccups
CONTRAINDICATIONS:
severerenalimpairment
SE/AE:
euphoria,lightheadedness,dizzy/drowsiness,fatigue,muscleweakness…shortlived.Dantrolene=hepattox
Toxicity:
NOspecifictx!
!
!
Supportivetherapy
CNSStimulantAgentsCh.16(stimulateaspecificareaofbrainorspinalcord)
☐Amphetamines:
CNSstimulantsthatelevatemoodoreuphoria,mentalalertnessandcapacitytowork,↓fatigue&drowsiness
☐Analeptics:
CNSstimulantsthathavegeneralizedefxonbrainstem&spinalcord(responsetoext.stimuli)
☐Anorexiants:
suppressappetite
☐Cataplexy:
abruptattacksofmuscleweakness&hypotoniatriggeredbyemotionalstimulisuchasanger,fear,surprise…oftenassociatedw/narcolepsy
☐Narcolepsy:
syndromecharxbysuddensleepattacks,cataplexy,sleepparalysis&visual/auditoryhallucination
☐Seratoninagonist:
newclassofCNSstimulantsusedtotxmigraines…stimulate5-HT1receptors
☐Sympiomymeticagents:
anothernameforCNSstimulants(akaamphet.,caff.,cocaine)
¦Oldestknown:
cocaine&hetamine;alsocaffeine
¦Anorexiantsfortxofexogenousobesity;appetitecontrolviasuppressionofappetitectrlcentersinbrain
¦Analeptics:
generalizedefxonbrainstem&spinalcord
¦Amphetaminesfortxofnarcolepsy&ADHDbytheamt&durationofnoreanddopamine
CONTRAINDICATIONS:
markedanxiety/agitation,glaucoma,tourette’sMAOI’sp276
SE/AE:
“speedup”bodysystems;CV,hypertension,restless/nervousness;getVITALSIGNSforbaseline
AssessforOTC!
i/e.ephedra/ginseng
Adrenergi
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