Download NURS 5334 Module 4 notes and more Quizzes Nursing in PDF only on Docsity!
Muscarinic iAgonist
- CHOLINERGIC iDRUGS: iTurn ion iparasympathetic iNS i (SLUDGE) - Muscarinic iAgonists- imimic ieffects iof iacetylcholine iat imuscarinic ireceptors DRUG iNAME MOA USE AE Contraindications Drug iinteractions Bethanechol Direct-acting imuscarinic iagonist. Binds ireversibly ito imuscarinic icholinergic ireceptors ito icause iactivation. iAt itherapeutic idoses, ibethanechol iacts iselectively iat imuscarinic ireceptors, ihaving ilittle ior ino ieffect ion inicotinic ireceptors, ieither iin iganglia ior iin iskeletal imuscle. Urinary iRetention GI (GERD),postop iabdominal idistention i(don’tigive ito iGI iobstruction) CV : i hypotension, ibradycardia i(don’t igive ito ihypotensive ipts ior ilow icardiac ioutput) GI- iexcessive isalivation, iincreased igastic iacid, iabdominal icramps, idiarrhea GU- ican ipee i(don’t igive ito iUT iobstruction/weaknes siof ibladder) Asthmatics iHyperthyroidis miPeptic iUlcer GI iobstruction iUT iobstruction Drugs icrosses imembrane ipoorly 10 - 50mg i 3 - 4 itimes ia iday Resp: iBronchoconstriction i(don’t igive ito iasthma ipts) 1hr ibefore imeals ior i2hrs iafter ito iprevent iN&V Pupil iconstriction Cevimeline Derivative iof iAch, iactions isimilar ito ithoseiof ibethanechol. Relief iof ixerostomia i(dry imouth) iin ipts iwithiSjoren isyndrome. Keratoconjuctivit is isicca Excessive isweating iIncreases isalivation iIncrease itear iproduction Nausea iRhinitis Pupil Uncontrolled iAsthma iCOPD Narrow iangle iglaucoma iIritis Use iin icaution Beta iBlockers iAtropine, iTCA Antihistamines iPhenotiazine iantipsychotics
(inflammation iof icornea iand conjunctiva) iand idry ieye constriction/blurred ivision Bradycardia w/heart idisease Pilocarpine (^) Glaucoma i(elevated i IOP) iPO imed i(Salagen)ican ihelp iwith Sjoren isyndrome Low idose-sweating
- high idose iSLUDGE Acetylcholine Used ifor imiosis i(pupil iconstriction) iafter cataract isurgery Cholinesterase iInhibitors i: iDrugs ithat iprevent ithe idegradation iof ithe iAch iby iacetylcholinesterase i(cholinesterase). i Cholinesterase iinhibitors iare ialso iknown ias i anticholinesterase i drugs_. i_ By ipreventing ithe ibreakdown iof iacetylcholine, icholinesterase iinhibitors iincrease ithe iamount iof iacetylcholine iavailable ito iactivate ireceptors, ithus ienhancing icholinergic iaction. iBecause icholinesterase iinhibitors ido inot ibind idirectly iwith icholinergic ireceptors, ithey iare iviewed ias iindirect-acting icholinergic iagonists. iUse iof icholinesterase iinhibitors iresults iin itransmission iat iall icholinergic ijunctions i(muscarinic, iganglionic, iand ineuromuscular), iso ithese idrugs ican ielicit ia ibroad ispectrum iof iresponses. iBecause ithey ilack iselectivity, icholinesterase iinhibitors ihave ilimited itherapeutic iapplications. i1.) ireversible iinhibitors: iproduce imoderate iduration. i2.) iirreversible iinhibitors: iproduce ieffects iof ilong iduration Drug iName MOA USE AE Contraindications Drug iInteractions Neostigmine Neostigmine iand iother ireversible icholinesterase iinhibitors iact ias isubstrates ifor icholinesterase. Management iof iMG iby istrengthening imuscles
SLUDGE
If iadministered iin itoxic idose, icholinesterase iinhibitors ican icause iaccumulation iof iAch in iamounts isufficient ito iproduce GI iand iGU itract iobstruction Peptic iUlcer iDisease iAsthma Muscarinic iantagonist Non-depolarizing ineuromuscular iblockers
nerve igas Peptic iUlcer iDisease iAsthma Coronary iInsufficiency Hyperthyroidism Donepezil Reversible iCholinesteras eiinhibitors Alzheimer iDisease Galantamine Reversible iCholinesteras eiinhibitors Alzheimer iDisease Rivastigmine Reversible iCholinesteras eiinhibitors Alzheimer iDisease, idementia iof iParkinson’s idisease The iirreversible icholinesterase iinhibitors iare ihighly itoxic. iThese iagents iare iemployed iprimarily ias iinsecticides iand iwarfare_. i_ Highly ilipid isoluble. iThe ionly iclinical iindication ifor ithe iirreversible iinhibitors iis iglaucoma i(Echothiophate)
- Toxic idose iproduce iexcessive imuscarinic, inicotinic, iand iCNS ieffects i(known ias icholinergic icrisis).
- Cholinergic icrisis iis- iexcessive imuscarinic istimulation iand idepolarizing ineuromuscular iblockage. iOverstimulation iof imuscarinic ireceptors: iSLUDGE, imuscle iweakness, ifasciculations, icramps, itwitching, iparalysis, ideath ifrom iapnea, ianxiety iand iconfusion ito idelirium. iConvulsions iof iCNS iorigin iprecede iparalysis iand iapnea. Muscarinic i(cholinergic) itoxicity i can ibe icaused iby ieither imuscarinic iagonists ior icholinesterase iinhibitors.
- can iresult ifrom iingestion iof icertain imushrooms i(Inocybe iand iClitocybe ispp.) iand ifrom ioverdose iwith itwo ikinds iof imedications: i1.) idirect-acting imuscarinic iagonists i(ex. iBethanechol, ipilocarpine), iand i2.) iCholinesterase iinhibitors i(indirect-acting icholinomimetics). Symptoms: iBronchospasms/excessive ibronchial isecretions, ibradycardia, ihypotension, iprofuse isalivations iN&V, iabdominal ipain, iDiarrhea, ifecal iincontinence, iexcessive iurination iand iurinary iincontinence, idiaphoresis, ilacrimation iand imiosis. iSeveral ipoisoning ican iproduce icardio icollapse: **Diaphoresis/diarrhea iUrination Miosis iBradycardia/Bronchospasm/Bronchorrhea iEmesis Lacrimation iSalivation Salivation iLacrimation iUrination iDiaphoresis/Diarrhe aiGI icramping Emesis iBradycardia iBronchospas m iBronchorrhea
- Treatment iis iAtropine i(antagonist)**
- Treatment: i Atropine- ito ireduce imuscarinic istimultions i(SLUDGE), iPralidoxime ireverse iinhibition iof icholinesterase, ibenzos i(diazepam) ifor iseizures, iand imechanical ivent ifor iresp idepression Pralidoxime: iantidote ifor iirreversible icholinesterase iinhibitors, imust ibe iadministered isoon iafter iorganophosphate ipoisoning. i Not ieffective ifor ireversible iinhibitors. MG: ifluctuating imuscle iweakness iand ipredisposition ito irapid ifatigue. iCommon isymptoms iof ithis iare iyour iptosis, idysphasia iand iweakness iof ithe iskeletal imuscles. iAnd iit's ian iauto-immune iprocess iwhere iantibodies iattack ithe inicotinic im ireceptors ion ithe iskeletal imuscle.
muscarinic iagonist ipoisoning peptic iulcer idisease i(when iadministered iin ihigh idose ican icause iSE) lights ilow, iavoid idriving) IOP Urinary iretention i(void ibefore itaking imeds) iConstipation i(laxative, iincrease, iincrease ifiber) iAnhidrosis i(absence iof isweat) i(avoid iactivities ithat imight ilead ito ioverheating ihigh irisk ifor ihyperthermia iTachycardia Asthma i(can ithicken isecretions iuse iwith icaution) bronchialisecretions icausing ibronchial iplugging Oxybutynin Anticholinergic iacts iprimarily iat iM3 imuscarinic ireceptors OAB Dry imouth iConstipation iTachycardia iUrinary iretention/hesitanc yiMydriasis i(pupil idilation) Blurred ivision iDry ieyes Combined iuse iof ioxybutynin iwith iother ianticholinergic iagents i(e.g., iantihistamines, itricyclic iantidepressants, iphenothiazine iantipsychotics) ican iintensify iall ianticholinergic iside ieffects. Drugs ithat iinhibit ior iinduce iCYP3A4 imay ialter ioxybutynin blood ilevels iand imay ithereby ieither
increase itoxicity i(inhibitors iof iCYP3A4) ior ireduce ieffectiveness i(inducers iof iCYP3A4). Darifenacin Anticholinergic iM OAB Dry imouth iConstipatio niDyspepsia iGastritis iHeadache Does inot iincrease iHR Avoid iwith ipts iwith isevere iliver iimpairment Levels iof idarifenacin ican ibe iraised isignificantly iby istrong iinhibitors i of iCYP3A4. iAmong ithese iare iazole iantifungal idrugs i(e.g., iketoconazole, iitraconazole), icertain iprotease iinhibitors iused ifor iHIV/AIDS i(e.g., iritonavir, inelfinavir), iand iclarithromycin i(a imacrolide iantibiotic). iIf idarifenacin iis icombined iwith iany iof ithese, iits idosage imust ibe ikept ilow. iIn ipatients i with imoderate iliver iimpairment iand iin ithose itaking ipowerful inhibitors iof iCYP3A4, idosage
beneficial iand iadverse ieffects. Fesoterodine Non-selective imuscarinic iantagonist OAB Dry imouth, iConstipatio n In ipatients itaking ia istrong iinhibitor iof iCYP3A4 i(e.g., ketoconazole, iclarithromycin), ibeneficial iand iadverse ieffects iare iincreased. iConversely, iin ipatients itaking ia istrong iinducer iof iCYP3A4 i(e.g., rifampin, icarbamazepine), ibeneficial iand iadverse ieffects iare ireduced Trospium Non-selective imuscarinic iantagonist OAB Dry imouth, iconstipation Vancomycin iMetformin iDigoxin iProcainamid e
- trospium iis eliminated iby ithe ikidneys Scopolamine anticholinergic Emesis, imotion sickness Ipratropium iBromide anticholinergic Asthma,^ iCOPD, irhinitis icaused iby iallergies ior icommon cold
Antisecretory ianticholinergics: Glycopyrrolate i(Robinul) i given ifor iexcessive isalivation ; imepenzolate, imethscopolamine, ipropanthelneiDicyclomine i given ifor iIBS Anticholinergic ipoisoning: i direct iresult iof iexcessive imuscarinic iblockade, iinclude idry imouth, iblurred ivision, iphotophobia isecondary ito imydriasis, ihyperthermia, iCNS ieffects i(hallucinations, idelirium), iand iskin ithat iis ihot, idry, iand iflushed. iDeath iresults ifrom irespiratory idepression isecondary ito iblockade iof icholinergic ireceptors iin ithe ibrain Treatment: iactivated icharcoal iand iantidote i(physostigmine) Adrenergic iAgonists i(Turn ion isympathetic iNS, iFight) The imechanisms iof iadrenergic ireceptor iactivation iare ieither idirect ior iindirect Direct- ireceptor iactivation ithrough idirect ibinding i(dopamine, iepinephrine, i isoproterenol iand iephedrine) iIndirect-1.) iPromotion iof iNE irelease i(Amphetamine, iEphedrine) 2.) iInhibition iof iNE ireuptake i(Cocaine, iTricyclic iantidepressants) i3.) iInhibition iof iMAO i(MAO iinhibitors) Adrenegic iagonists ifall iinto i 2 ichemical iclasses icatecholamines iand inoncatecholamines Hot i as ia ihare i(hyperthermia) Dry i as ia ibone i(dry ieyes, idry imouth, idry iskin) i Red i as ia ibeet i(flushed iface) Blind i as ia ibat i(mydriasis) Mad i as ia ihatter i(delirium)
(beta1) iBronchodilation iin iAsthma i(beta2) iAnaphylatic iShock i(alpha&beta) and ioxygen idemand iby iactivating ibeta1(especiall yiin icoronary iatherosclerosis) Post- iextravastio ninecrosis Hyperglycemia- icauses ibreakdown iof iglycogen isecondary ito iactivation iof ibeta2 iin iliver iin skeletal imuscle Alpha-adrenergic iblocking iagents- ican iprevent ialpha- iadrenergic ireceptoriactivation iby iepi Beta-adrenergic iblocking iagents- ican iprevent iepi Norepinephrine Alpha iAlpha i 2 iBeta Catecholamine Hypotensive istates iCardiac iarrests Same ias iEpi, ibut idoes i not ipromote ihyperglycemia isince iit iis inot response ito ibeta i 2 Same ias iEpi Isoproterenol Beta i 1 Beta i 2 Catecholamine (^) Av iheart iblock, iImprove ioutcomes iin icardiac iarrest, iIncrease icardiac ioutput iduring ishock Tachydysrhythm iias i(beta1) iAngina i(beta1) iHyperglycemia i(beta2)
MAO
iTCA Beta iadregnergic iblocking iagents Inhaled ianesthetic i(dysrhythmias) Dopamine Dopamine iBeta i 1 iAlpha (high idose) Catecholamine Shock-beta iincreases icardiac ioutput/tissue perfusion; Tachycardia iDysrhythmia siAngina Extravasation Tachydysrhythmias/vfib MAO iTCA General ianesthetics
dopamine iin ikidney idilate irenal iarteries iimprove irenal iperfusion i(high idose ican idecrease iit) Heart ifailure-beta iincreases imyocardial icontractility ithereby iincrease icardiac output (may iresult iin inecrosis) Dobutamine Beta i 1 Catecholamine Heart ifailure Tachycardia MAO iTCA General ianesthetics Phenylephrine Alpha i 1 Noncatecholamin ie Nasal iCongestion Hypotension iDilate ipupils Albuterol Beta i 2 Noncatecholamin ie Asthma **high idose iwill iactivate ibeta ireceptor ias iwell. iPt ishould ibe iwarned inot ito iexceed irecom dose. Tremor iHigh idose- itachycardia Ephedrine Alpa iAlpha i 2 Beta i 1 Beta i 2 Noncatecholamin ie Asthma iShock Anesthesia iinduced- ihypotension Hypertension iDysrhythmias iAngina iHyperglycemi aiInsomnia i(can cross iBBB) Adrenergic iAntagonists i(turn ioff isympathetic iNS, iREST)
Combined iuse iwith ihypotensive idrugs—including iphosphodiesteras ie itype i 5 i(PDE-5) iinhibitors isuch ias isildenafil i[Viagra] —may icause ia isignificant ireduction iin iblood ipressure. Food ifurther idecreases ithe irate iand iextent iof iabsorption. iDrug iis imetabolized iin ithe iliver iand iexcreted iin ithe iurine Alfuzosin Alpha i 1 - iselective iin iprostate iand iurinary itract BPH Dizziness Syncope, iHypotension irare Doses i4x igreater ithan irecommended ican iprolong iQT iinterval ilead ito iventricular idysrhythmias Contraindicated iwith ihepatic iimpairment. Levels iof ialfuzosin iare imarkedly iraised iby ipowerful iinhibitors iof iCYP3A4. iAmongithese iare erythromycin,
clarithromycin, iitraconazole, iketoconazole, inefazodone, iand ithe iHIV iprotease iinhibitors, isuch iasiritonavir. Concurrent iuse iof ialfuzosin iwith ithese idrugs iis icontraindicated. Drugs iof iconcern iinclude iorganic initrates, iantihypertensive iagents, iand ithe iPDE- 5 iinhibitors iused ifor isexual idysfunction i(e.g.,isildenafil i[Viagra]). Silodosin Alpha i 1 - iselective iin iprostate, ibladder, iand iurethrea BPH Ejaculation iissues iDizziness iLigthheadness Nasal icongestion Phentolamine Competitive iadrenergic iantagonist,iblocks ialpha i 2 iand alpha i 1 Pheochromocytoma iPrevention iof itissue inecrosis iafter extravasation Orthostatic ihypotension iReflex itachycardia iNasal icongestion Inhibition iof iejaculation Contraindicated iwith iangina ipectoris iand iMI
Sotalol-Ventricular idysrhythmias iand ifor imaintenance iof iNSR iin ipts iwho ihad isymptomatic iAfib/aflutter Drug Category Use AE Contraindications Drug iInteractions Propranolol 1 st^ igen inon- iselective ibetaiblocker Blocks iboth ibeta1 iand ibeta i 2 HTN, iAngina, iDysrhythmias, iMI Migraine iprevention iPerformanc eianxiety Bradycardia iAV iBlock iHeart iFailure- isuppression iof imyocardial contractility ican iresult iin ithis iRebound iCardiac iexcitation- itachycardia, iventricular idysrhythmias i(should iwithdraw islowly igive ismaller idoses i 1 - 2weeks) iBronchoconstrictio in i(blockade ibeta2) iRare: iDepression, iinsomnia, inightmares, ihallucinations i(crosses iBBB) AV i block i >1st^ i deg iPreexisting iHF iPreexisting icardiaciischemia Hazardous ito iasthma iand iCOPD ipts id/t ibronchoconstriction iDiabetics-blocks ibeta i 2 iin imuscle iand iliver ican isuppress iglycogenolysis ithereby ieliminating ian iimp. iMechanism ifor icorrecting iinsulin-induced ihypoglycemia; isuppress itachycardiaitremors, iand iperspiration i(mask ihypoglycemia) Calcium iChannel iBlockers: iVerapamil iand iDiltiazem i(identical ito ipropranolol- reduceiHR, iSuppress iAV iconduction, iand imyocardial icontractility) Insulin: ican iimpede iearly irecognition iof iinsulin- induced ihypoglycemia. Neonates irisk ifor ibradycardia, iresp idistress, ihypoglycemia (crosses iplacenta) Metoprolol 2 nd^ iselective blockade iof ibeta i 1 ireceptor iin ithe HTN, iAngina, iHF, iMI Bradycardia, Reduce icardiac ioutput, iAV iheart BB iabrupt idc imay cause iexacerbation iof iangina iand
heart i(cardioselectiv e ) block, irebound icardiac iexcitationiafter iabrupt iwithdrawal increase irisk ifor iMI Contraindicated ifor ibradycardia, iandiAV block i> i 1 st^ ideg Indirect iActing iAntiadrenergic iAgents Indirect iActing iAntiadrenergic iAgents: i prevents istimulation iof iperipheral iadrenergic ireceptors. iAnd ithere's itwo igroups, iyour iadrenergic ineuron iblocking iagents iwhich idecrease inorepinephrine irelease iand iyour icentral iacting iout ithe itwo iagonists iwhich ireduce iimpulses ialong ithe isympathetic inerves. iUse: iHTN Drug Category Use AE Clonidine CentraliActing iAlpha2 iagonist HTN, isevere ipain, iADHD, ioff ilabel iuse ifor iopioid iand imethadone iwithdrawal, ismoking icessation, ia iconduct idisorder, iand ioppositional idefiant idisorder iin ichildren iand iTourette isyndrome i(a iCNS idisease icharacterized iby iuncontrolled itics iand iverbal ioutburst ithat iare ifrequently iobscene) Bradycardia Decreases iin icardiac ioutput iCauses iminimal iorthostatic ihypotension Drowisness iDry imouth Rebound iHTN-abrupt iwithdrawal Not ito ibe igiven iin ipregnancy id/t ifetal iharm Risk ifor iabuse- ihigh idose ican icause ieffects iof ieuphoria, isedation, ihallucainations iConstipation Impotence iGyneomasti a Vivid idreams, ianxiety, idepression, Localized iirritation ion itransdermal ipatches Guanfacine HTN Rebound iHTN iafter iabrupt iwithdrawal
