Slide 1NeuropharmacologyTerms to knowPNSSympatheticReceptorsMuscarinic (acetylcholine)Muscarinic (acetylcholine)OABMyasthenia GravisNicotinic CholinergicBe AwareAdrenergic AgonistsAlpha1Alpha2Beta1Beta2Slide 18MedicationsNorepinephrine (Levophed)IsoproterenolDopaminePhenylephrineDobutamineAlbuterolAdrenergic AntagonistAlpha BlockadesTerazosin (Hytrin)Beta blockersBeta blockers are used to treat:MedicationsOther anti-adrenergicBreak: 10 minutes Do you know where this is?Neurological pharmacologyParkinson's diseaseNormal vs. Parkinson’s NeurotransmissionParkinson’s treatmentLevodopaLevodopa (cont)Combination of Levodopa + Carbidopa (Sinemet®)Slide 41PharmacologyNSG 325Module 2September 9, 20131Nervous system controls EVERYTHING!PNS: peripheral nervous systemCNS: central nervous systemDrugs work by increasing or decreasing receptor activationNeuropharmacology2Agonist-increase receptor activationAntagonist-decrease receptor activationAdrenergic- receptors that mediate response to epinephrine (and norepinephrine)Cholinergic- receptors that mediate response to acetylcholineTerms to know3Autonomic system divided into parasympathetic and sympathetic.Parasympathetic: (“read and feed” or “rest and digest”) Slows heart Increases gastric secretionEmpty bladderEmpty bowelFocusing the eye for near visionConstricting the pupilContraction bronchial smooth musclesPNS4Flight or fight responseIncrease HR, B/PShunts blood away from skin to skeletal musclesDilates bronchus Dilates pupilsSympathetic 5Cholinergic (acetylcholine)NicotinicNitotinicMuscarinicAdrenergic (epinephrine)Alpha1Alpha2Beta1Beta2Receptors6Related to parasympathetic system-similar effectsBethanechol-agonist used to treat urinary retention (increase tone of muscles and relaxing sphincters). Possible side effects, hypotension, bradycardia, excessive salivation, abd cramps, exacerbation of asthma (broncho-constriction).Muscarinic (acetylcholine)7Atropine- antagonist or anticholinergicEffects primarily heart, exocrine glands, smooth muscles and eyeIncreases heart rate (ACLS drug for bradycardia)Decreases secretion from salivary, bronchial and sweat glands along with decreased acid-secreting cells in stomach. Used pre-operatively to decrease secretionsMuscarinic (acetylcholine)8Oxybutynin (Ditropan)-Use for overactive bladder Best treatment?SE: dry mouth constipation, confusion, tachycardia, insomnia, nervousnessScopolamine- anticholinergic, also decreases emesis and motion sickness (transdermal patch)OAB9Autoimmune diseaseAntibody-mediated loss of acetylcholine receptorsDiagnosis made through history, test dose of Edrophonium (Tensilon) an acetylcholinersterase inhibitorTreatment: Pyridostigmine and neostigmineMyasthenia Gravis10Neuromuscular blocking agents- prevent acetylcholine from activating nicotinic resulting in muscle relaxationVecuronium (Norcuron): Neuromuscular agent used for intubation, general anesthesia and management of ventilated patient. Does not release histamine which means more stable CV status. Eliminated bile/liver. Onset 3-5 min last 30 minutesSuccinylcholine (Anectine): Ultra-short-acting neuromuscular. Used for intubation, ECT, bronchoscopy. Onset 1 minute, last 10 minNicotinic Cholinergic11Neuromuscular blocking agents: cause relaxation of ALL muscles including respiratory!! Do not decrease LOC…patient can’t moveGive sedative with med for LOCMUST have emergency equipment available at the bedsideBe Aware12Work with sympathetic nervous systemAlso called sympathomimeticCatecholamineShort durationDon’t cross blood brain barrierCan not be taken orallyNon-catecholamineLonger durationCan cross blood brain barrierCan be taken orallyAdrenergic Agonists13Epinephrine, norepinephrine, dopamine, phenylephrineActivation of Alpha1 cause:VasoconstrictionMydriasis (pupil dilatation)Used to treat: hemostasis, nasal decongestion, elevation of blood pressure, adjunct to anesthesia (SQ), dilate pupil for eye exam Adverse reactions: hypertension, necrosis, bradycardiaAlpha114Peripheral: no clinical applicationCentral: anti-hypertensive Clonidine (Catapress)Selective activation of alpha2 in brain stem receptors reduces sympathetic outflow to blood vessels and to the heartPO or transdermalAdverse reaction: drowsiness, rebound HTNAlpha215Main effect is on the heartIncreases inotropic effectIncreases HREnhance conductivity through AV nodeBeta116Lungs and uterusBronchodilitationDelay preterm laborAdverse:HyperglycemiatremorBeta21718Epinephrine- α1,α2,β1,β2 VasoconstrictorControl bleedingIncrease B/PIncreased HR/conductivityBronchodilitationTreatment for anaphylactic shockRoutes: IV, IM, IT IC, SQAdverse effects: HTN crisis, Dysrhythmias, Angina Pectoris, Necrosis with extravasation, HyperglycemiaMedications19α1,α2,β1Similar to epinephrine in actionOnly approved for hypotension and cardiac arrestRoute- IVNorepinephrine (Levophed)20β1,β2“Chemical pacemaker”Increases conductivity through AV nodeRoute IVAdverse effects: tachy-dysrhythmia, angina, hyperglycemiaIsoproterenol21Dose dependent Moderate dose Beta1High dose alpha 1 with Beta 1Used to treat shock, heart failure, acute renal failure (ARF)Adverse effects: tachycardia, dysrhythmiaDopamine22Alpha1Used to treat hypotension via IV route (especially in septic shock)Used to treat nasal congestion (nasal spray)Dilate pupil (eye drop)Adverse effects depend on routePhenylephrine23Beta 1Increased contractility in heartIndicated in heart failureAdverse effects: tachycardiaDobutamine24Beta2Dilates bronchusUsed to treat asthmaIf used in large dose will become Beta1 and Beta 2Adverse effects tremor, tachycardiaAlbuterol25Blocks the response to α1,α2,β1,β2 receptorsCan be selective or nonselectiveAdrenergic Antagonist26Blood vessels- dilatesBladder-relaxes/tones Used to treat: HTNBPHExtravasation of IV with vasoconstrictor (phentolomine) RegitineAdverse Effects: postural hypotension, reflex tachycardiaAlpha Blockades27Treat BPHTreat HTNTake at bedtime to minimize effects of hypotensionAdverse effects: hypotension, nasal congestionDose differs if treating BPH vs. HTNTerazosin