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Pharmacologypharmacologypharmacology PharmacologyPharmacologyPharmacology DrugsDrugs ThatThat AffectAffect The:The: NervousNervous SystemSystem TopicsTopicsTopics •• Analgesics Analgesics andand antagonistsantagonists •• Anesthetics Anesthetics •• Anti-anxiety Anti-anxiety andand sedative-hypnoticssedative-hypnotics •• Anti-seizure Anti-seizure // anti-convulsantsanti-convulsants •• CNS CNS stimulatorsstimulators •• Psychotherapeutics Psychotherapeutics •• ANS/PNS/SNS ANS/PNS/SNS agentsagents ButButBut first...first...first... AA colorfulcolorful reviewreview ofof neurophysiology!neurophysiology! NervousNervousNervous SystemSystemSystem CNSCNS PNSPNS AutonomicAutonomic SomaticSomatic SympatheticSympathetic ParasympatheticParasympathetic AnalgesicsAnalgesicsAnalgesics •• Decrease Decrease inin sensationsensation ofof pain.pain. •• Classes: Classes: –– Opioid. Opioid. •• Agonist. Agonist. •• Antagonist. Antagonist. •• Agonist-antagonist. Agonist-antagonist. –– Non-opioids. Non-opioids. •• Salicylates. Salicylates. •NSAIDs.•NSAIDs. •• Adjuncts. Adjuncts. OpioidsOpioidsOpioids •• Generic Generic reference reference to to morphine-likemorphine-like drugs/actionsdrugs/actions –– Opiate: Opiate: derivative derivative of of opium opium •• Prototype: Prototype: morphine morphine –– Morpheus: Morpheus: god god of of dreams dreams •• Act Act onon endorphinendorphin receptors:receptors: –– Mu Mu (most (most important) important) –– Kappa Kappa ActionsActionsActions ofofof OpioidOpioidOpioid ReceptorsReceptorsReceptors Response Mu Kappa Analgesia ;; Respiratory ; Depression Sedation ;; Euphoria ; Physical Dependence ; ⇓ GI motility ;; ActionsActionsActions atatat OpioidOpioidOpioid ReceptorsReceptorsReceptors Drugs Mu Kappa Pure Agonists Agonist Agonist -morphine, codeine, meperidine (Demerol®), fentanyl (Sublimaze®), remifentanil (Ultiva®), propoxyphene (Darvon®), hydrocodone (Vicodin®), oxycodone (Percocet®) Agonist-Antagonist Antagonist Agonist -nalbuphine (Nubaine®), butorphanol (Stadol®) Pure Antagonist Antagonist Antagonist -naloxone (Narcan®) GeneralGeneralGeneral ActionsActionsActions ofofof OpioidsOpioidsOpioids •• Analgesia Analgesia •• Euphoria/Dysphoria Euphoria/Dysphoria •• Respiratory Respiratory depressiondepression •Sedation•Sedation • Constipation • Constipation •• Miosis Miosis • Urinary retention • Urinary retention –– Pupil Pupil constrictionconstriction • Cough suppression • Cough suppression •• ⇓⇓PreloadPreload && afterloadafterload •Emesis •Emesis –– Watch Watch forfor •Increased•Increased ICPICP hypotension!hypotension! – Indirect through CO – Indirect through CO22 retentionretention NonNonNon-opioid--opioidopioid AnalgesicsAnalgesics Analgesics •• Salicylates Salicylates –– Aspirin Aspirin (Bayer(Bayer®®)) ** (prototype(prototype forfor class)class) •• Non-Steroidal Non-Steroidal Anti-InflammatoryAnti-Inflammatory DrugsDrugs •• Ibuprofen Ibuprofen (Motrin®,(Motrin®, AdvilAdvil®®)) –– Propionic Propionic Acid Acid derivative derivative •• Naproxen Naproxen (Naprosyn(Naprosyn®®)) •• Naproxen Naproxen sodiumsodium (Aleve(Aleve®®)) •• All All competecompete withwith aspirinaspirin forfor proteinprotein bindingbinding sitessites –– Ketorolac Ketorolac (Toradol (Toradol®®)) NSAIDNSAIDNSAID PropertiesPropertiesProperties Drug Fever Inflammation Pain Aspirin ;;; Ibuprofen ;;; Acetaminophen ;; AspirinAspirinAspirin MechanismMechanismMechanism ofofof ActionActionAction •• Inhibit Inhibit synthesissynthesis ofof cyclooxygenasecyclooxygenase (COX)(COX) –– Enzyme Enzyme responsibleresponsible forfor synthesissynthesis of:of: Prostaglandins Thromboxane A Prostaglandins Thromboxane A22 –Pain–Pain response response –Involved–Involved in in platelet platelet –Suppression–Suppression of of gastric gastric acid acid secretion secretion –aggregation–aggregation –Promote–Promote secretion secretion of of gastric gastric mucus mucus and and bicarbonate bicarbonate –Mediation–Mediation of of inflammatory inflammatory response response –Production–Production of of fever fever –Promote–Promote renal renal vasodilation vasodilation ( (⇑⇑bloodblood flow) flow) –Promote–Promote uterine uterine contraction contraction AspirinAspirinAspirin EffectsEffectsEffects GoodGood BadBad •• Pain Pain reliefrelief •• GI GI ulceration:ulceration: •• ⇓⇓FeverFever –– ⇑⇑GastricGastric acidity acidity – ⇓ GI protection •• ⇓⇓InflammationInflammation – ⇓ GI protection •• ⇑⇑BleedingBleeding •• ⇓⇓RenalRenal eliminationelimination •• ⇓⇓UterineUterine contractionscontractions duringduring laborlabor AcetaminophenAcetaminophenAcetaminophen (Tylenol(Tylenol(Tylenol®®®))) •• NSAID NSAID similarsimilar toto aspirinaspirin •• Only Only inhibitsinhibits synthesissynthesis ofof CNSCNS prostaglandinsprostaglandins –Does–Does notnothavehave peripheralperipheral sideside effectseffects ofof ASA:ASA: •• Gastric Gastric ulcerationulceration •• ⇓⇓PlateletPlatelet aggregation aggregation •• ⇓⇓RenalRenal flowflow •• ⇓⇓UterineUterine contractions contractions AcetaminophenAcetaminophenAcetaminophen MetabolismMetabolismMetabolism Major Pathway Non-toxic AcetaminophenAcetaminophen Non-toxic metabolitesmetabolites InducedInduced byby Depleted by ETOH & ETOH Depleted by ETOH & ETOH APAPAPAP overdoseoverdose P-450 ToxicToxic Glutathione Non-toxicNon-toxic metabolitesmetabolites metabolitesmetabolites Minor Pathway AnestheticsAnestheticsAnesthetics •• Loss Loss ofof allall sensationsensation –– Usually Usually withwith lossloss ofof consciousnessconsciousness ––⇓⇓propagationpropagation ofof neuralneural impulsesimpulses •• General General anestheticsanesthetics –Gases–Gases •• Nitrous Nitrous oxideoxide (Nitronox(Nitronox®®),), halothane, halothane, ether ether –IV–IV •• Thiopental Thiopental (Pentothal(Pentothal®®),), methohexital methohexital (Brevitol (Brevitol®®),), diazepamdiazepam (valium®),(valium®), remifentanilremifentanil (Ultiva (Ultiva®®)) AnestheticsAnestheticsAnesthetics •Local•Local –– Affect Affect onon areaarea aroundaround injectioninjection –– Usually Usually accompaniedaccompanied byby epinephrineepinephrine •• Lidocaine Lidocaine (Xylocaine(Xylocaine®®),), topical topical cocaine cocaine AntiAntiAnti-anxiety--anxietyanxiety &&& SedativeSedativeSedative--- hypnotichypnotichypnotic DrugsDrugsDrugs •• Sedation: Sedation: ⇓⇓anxietyanxiety && inhibitionsinhibitions •• Hypnosis: Hypnosis: instigationinstigation ofof sleepsleep •• Insomnia Insomnia –– ⇑⇑LatentLatent periodperiod –– ⇑⇑WakeningsWakenings •• Classes: Classes: – Barbiturates – Barbiturates ChemicallyChemically different, different, –– Benzodiazepines Benzodiazepines FunctionallyFunctionally similar similar –– Alcohol Alcohol MechanismMechanismMechanism ofofof actionactionaction •• Both Both promotepromote thethe effectivenesseffectiveness ofof GABAGABA receptorsreceptors inin thethe CNSCNS –– Benzodiazepines Benzodiazepines promotepromote onlyonly –– Barbiturates Barbiturates promotepromote andand (at(at highhigh doses)doses) stimulatestimulate GABAGABA receptorsreceptors •• GABA GABA == chiefchief CNSCNS inhibitoryinhibitory neurotransmitterneurotransmitter –– Promotes Promotes hyperpolarizationhyperpolarization viavia ⇑⇑ClCl--influxinflux BenzodiazepinesBenzodiazepinesBenzodiazepines vs.vs.vs. BarbituratesBarbituratesBarbiturates Criteria BZ Barb. Relative Safety High Low Maximal CNS depression Low High Respiratory Depression Low High Suicide Potential Low High Abuse Potential Low High Antagonist Available? Yes No BenzodiazepinesBenzodiazepinesBenzodiazepines BenzodiazepinesBenzodiazepines “Non-benzo“Non-benzo benzo” benzo” •• diazepam diazepam (Valium(Valium®®)) •• zolpidem zolpidem (Ambien (Ambien®®)) •• midazolam midazolam (Versed (Versed®®)) •• buspirone buspirone (BusPar (BusPar®®)) •• alprazolam alprazolam (Xanax (Xanax®®)) •• lorazepam lorazepam (Atiavan (Atiavan®®)) •• triazolam triazolam (Halcion (Halcion®®)) BarbituratesBarbituratesBarbiturates Subgroup Prototype Typical Indication Ultra-short thiopental Anesthesia acting (Pentothol®) Short acting secobarbital Insomnia (Seconal®) Long acting phenobarbital Seizures (Luminal®) BarbituratesBarbituratesBarbiturates •• amobarbital amobarbital (Amytal (Amytal®®)) •• pentobarbital pentobarbital (Nembutal(Nembutal®®)) •• thiopental thiopental (Pentothal(Pentothal®®)) •• phenobarbital phenobarbital (Luminal (Luminal ®®)) •• secobarbital secobarbital (Seconal (Seconal®®)) AntiAntiAnti-seizure--seizureseizure MedicationsMedicationsMedications •• Seizures Seizures causedcaused byby hyperactivehyperactive brainbrain areasareas •• Multiple Multiple chemicalchemical classesclasses ofof drugsdrugs –– All All havehave samesame approachapproach –– Decrease Decrease propagationpropagation ofof actionaction potentialspotentials •• ⇓⇓NaNa++,, CaCa++++influxinflux (delay(delay depolarization/prolongdepolarization/prolong repolarization)repolarization) •• ⇑⇑ClCl--influxinflux (hyperpolarize (hyperpolarize membrane) membrane) AntiAntiAnti-Seizure--SeizureSeizure MedicationsMedicationsMedications BenzodiazepinesBenzodiazepines IonIon ChannelChannel InhibitorsInhibitors •• diazepam diazepam (Valium®)(Valium®) •• carbamazepine carbamazepine ® •• lorazepam lorazepam (Ativan (Ativan®®)) (Tegretol(Tegretol®)) BarbituratesBarbiturates •• phenytoin phenytoin (Dilantin®) (Dilantin®) •• phenobarbital phenobarbital Misc.Misc. AgentsAgents (Luminal(Luminal®®)) •• valproic valproic acid acid (Depakote®)(Depakote®) IonIonIon DiffusionDiffusionDiffusion •• Key Key toto neurophysiologyneurophysiology •• Dependent Dependent upon:upon: –– Concentration Concentration gradientgradient –– Electrical Electrical gradientgradient
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