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Medical school antihypertensive drug chart. Lists different drug classes and the most important drugs for each class.
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Normalcontrol
PosturalBaroreflex
RenalresponsetoBP
DrugClass DrugExamples MOA ClinicalIndications AdverseEffects Contraindications DrugInteractions/Comorbidities
Cardioselectiveagents1selective:Atenolol,Metoprolol
block1A.R.onheart,kidneyHR(negavechronotrope)contraclity(negaveinotrope)COrenalreninsecreon
treatsHTNcthefollowingcomorbidities:Ischemicheartdisease,nondecomensatedheartfailure,dissectingthoracicaneurysm(notaseffectiveforelderlyorAA)insevereHTN,usefultopreventreflextachythatresultsfromdirectvasodilators
Vasodilatingagents:Carvedilol,Labetalol,Nebivolol
carevilolandlabetalolblockand;nebivololcoupledcNO(release)andonly
htncarvedilolandlabetalol:pheochromocytoma,HTNemergencies,andclonidinewithdrawalsyndrome
AgentscISA:Pindolol,Acebutolol,penbutolol
arepartialagonists(blockcsomeintrinsicsympathomimeticactivity):BPbyPVR
note:HRandCOlessthanotherbetablockers(greateragonsitthanantagonistactivityat2)preferredforpaentscbradyarrhythmiasorPVD
EsmololBeta1selectiveblockerthatisrapidlymetabolizedviahydrolysisbyRBC
shorthalflifemakesitpreferredforintraoperativeandpostoperativeHTN,andHTNemergenicesassociatedctachycardia
1and2blockers(phenoxybenzamine,phentolamine)
relaxvascularsmoothmusclesbypreventingNEfrominteractingc1receptorsandblocks2onpresynapticsympatheticautrecptors
Phenoxybenazomine/phentolamine:dxandtxpheochromocytomaPhentolamine:addpropranololtotxclonidinewithdrawalsyndrome
reflextachycardia(blocks,1stdosehypotension,posturalhypotension,urinaryincontinence
note:ex:doxazosinhaslong1/2life(1012hrs)
1selectiveblocker(prazosin,doxazosin,terazosin)
relaxvascularsmoothmusclesbypreventingNEfrominteractingc1receptors
Prazosin:uselimitedbysevereposturalhypotension,usefulonlyasaddontotreatresistanthypertensionDoxazosin:sxofbladderoulowtractobstructionandBPH
1stdosehypotension,posturalhypotension,urinaryincontinence
Methyldopa
takenupintoadrenergicnerveconvertedtomethylNEinCNSwhere2receptorsarestimulatedtosympathecoulowtoperiphery
DOCduringpregnancyusefulinpatientswhocan'ttolerateotherdrugsPVR(variableinHRandCO)
note:advantageiscausesreduconinrenalvascularresistance
Clonidine(partialagonist)
BPbyCO2*HRandrelaxaonofcapacitancevessels,TPR;alsorenalvascularresistanceandmaintenanceofrenalbloodflowbindstoimidazolinereceptorNEreleasecentrally
HRandCOmorethanmethyldopa
drymouthandsedationDONOTstopsuddenlywillcauselifethreateningHTNcrisis2*symphactivity
ptsatriskfordepression,concomitantcTCAs
causesshortBP(directsmofperipheralreceptors)prolongedhypotension(adrenoceptorsinmedulla)
IndirectlydrugmetabolismbyCOhepacbloodflow(egdrugschighhepaticextractionratio:lidocaine,morphine,sodiumpentothal,ASA,propranolol)Additiveeffectscverapamil,lidocaine,&othernegativeinotropes(ifverapamilandBblockergiventogether:canbefatal)
decompensatedheartfailureasthma
adrenergicblockers(systemic)
PharmacologyAntiHypertensives
Sympatholytics
kidneysresponsibleforlongtermBPcontrol,renalperfusionpressurecausesintrarenalredistribuonofbloodflowandreabsorponofsaltandwaterreninproduconangiotensinIIproducon;angiotensinIIcauses1)directconstrictionsofresistancevessels,2)stimulationofaldosteronesynthesisinadrenalcortex(renalNaabsorponandintravascularbloodvolume);vasopressinreleasedfromposteriorpituitaryregulateswaterreabsorptionbykidneys
NormalregulationofBP
BPmaintainedbyregofCOandPVR(atarterioles,postcapillaryvenules(capacitancevessels),andheart),kidneyregulatesintravascularfluidvolume,localreleaseofvasoactivesubstancesfromvascularendothelium(i.e.endothelin1constricts,NOdilates);baroreceptors(controlledbyautonomicsandreninsystem)coordinateoverallfunctiontomaintainnmlBP;cHTNthesystemis"set"forahigherpressure
baroreceptorsresponsibleforrapidadjustmentsinBP,sympatheticneuronsinmedullaaretonicallyactive,carotidbaroreceptorsarestimulatedbystretchofthevesselwall2*to BP,baroreceptorsmulaoninhibitscentralsympatheticdischarge(oppositeisalsotrue);whensomeonestands,baroreceptorssensethereductioninBPfrompoolingofbloodintheveins>sympatheticdischargeisdisinhibited sympatheticoutflowtoPVR(constrictsarterioles)andCO(directsmofheartandconstriconofcapacitancevessels)
Blockers
TGsandHDLbronchospasm:useccautioninCOPDfatigue,coldextremities,canworsenRaynaud's,vividdreams,impotence,hyperglycemiapropranolol(nonselective):willmaskhypoglycemiainDM
Centrallyacting2adrenergicagonist
MCsedation(atonsetoftx)depression,hepatitis,immunehemolyticanemia(positiveCoomb'stest),fever,nightmares,lactation;longtermtx:persistentmentallassitudeandimpairedconcentration
ACEinhibitors(angiotensin
convertingenzyme)
longactingdrugs:trandolapril,ramipril=qddosing"pril"
competitiveinhibitorofACEinhibitsynthesisofangiotensinIIandaccumulationofbradykinincirculanglevelsofaldosterone
preferredfor:whiteyoungorAsianhypertensivepatient,plasmareninmortalityin:acuteMI,CHF,riskofCVdiseaserenalprotectiveinchronickidneydiseaseandchypertensiveptscdiabeticneuropathy
1stdosehypotension,drycough&angioedema(bradykinin),dysgeusia,anemia(EPO),serumK+,hypoglycemia,fxnalrenalfailurechxofrenalstenosis
pregnancy(devdefectsifgivenin2nd,3rd)b/lrenalarterystenosis,renalfailure,angioedema
beneficialdruginteractions:K+wastingdiuretic(loopdiuretic,thiazidediuretics)badinteractions:K+supplements,allK+sparingdiuretics,NSAIDs,ARBs
AngiotensinReceptorBlockers(ARBs)
allendin"sartan"losartan,candesartan,eprosartan,irbesartan,olmesartan,telmisartan,valsartan
inhibitsangiotensin2receptors(AT1,AT2)aldosteronelevelsplasmavolumeandTPRnoeffectonbradykinin
riskofcough/angioedemaofACEsameasabove,effectiveafteracuteMI,heartfailure
1stdosehypotension(lisinopril)givenighttimedoseserumK+(M)
Hydralazineunclear,directvasodilatoractiononvascularsmoothmuscle;usuallycombinedwithotherdrugs
severehypertensionduringpregnancy(nifedipineispreferredbysome)
HA,flushing,tachycardia,fluidretentionlongtermtherapycdosesmycauseSLElikesxinsomepts
Fenoldopam
AlcoholCigaretteSmoking
WeightRegularExerciseDietarychoicesRelaxation
Diuretics(thiazides) betablockers
Thiazides
ACEinhibitors ARBs CCBs(nondihydropyridine) thiazide ACEinhibitorsdiuretics ACEI CCBs
aerobicexerciseuseful,HRandconcentraoncirculangcatecholamine's,HDL,ANPreleasecaloricrestrictionandfruitsandvegetablesuseful
LifestyleChronicalcoholintakecorrelatescHTN,consumptionresistancetoanhypertensivemedssecondarytobioavailabilityofanhypertensivedrugstransientinBP2*toeectofniconeonautonomicganglia,riskfordevelopingsustainedhypertension,atherogenic
CalciumChannelBlockers(CCB)
briefhere,morelater
effectiveinelderlypts,AA,CaribbeanriskofMIandstrokeinptscHTNatrialflutter(combinedcquinine)angina
generallywelltoleratedshortacting(nifedipinecapsules):flushing,HA,anginapedaledemaverapamil:exacerbateheartfailure,constipation
IVverapamil:cancausecirculatorycollapsecconcurrentblockers
VisceralobesitycorrelatescHTN,if10%idealweightthen10kgweightloss520mmHgdropinsystolicBP,waisttohipraoimportantindex
1stlineforuncomplicatedHTN
Diabetes
Elderly
BestUse(inorderLefttoRight)
Reninangiotensinaldosteronesystemantagonists
PeripheralvasodilatorsworkbestincombowithdrugthatwillopposecompensatoryCVresponsecautionwithischemicheartdisease2*toreflextachycardia
Oralvasodilators
parenteralvasodilators
arteriolesonly,notveins
Generalorderofuse
Peripheralneuropathynoalphaorbetablockers
stresshormones(cortisol,NE,epi)arereleaseandcouldBP,relaxaonstateusefultoBP
diuretics CCBbetablockers ACEIbetablockers orCCB(notboth!)CCBMethyldopa NifedipineorHydralazine ifpreeclampsia:labetalolalphablockers ACEI(ARBs) CCBs IndapamideACEI(unlessb/lstenosis)betablockers nondihydropyridineCCBsalpha1selectiveblockersbetablockers ACEIACEI(ARB) diuretics aldosterone betablockersGout:thiazides Asthma:betablockers
DrugClass DrugExamples MOA ClinicalIndications AdverseEffects Contraindications DrugInteractions
GeneraleecveinAAandelderly(saltsensitive)
LoopDiuretics(Highceiling)
Furosemide(lasix),Ethacynicacid,Toresmide,Bumetanide
inhibitsNa/K/2Cltransporter(TALthickascendinglimb)reabsorponofdivalentcaons(Mg,Ca)SignificantKwasting
Acutepulmonaryedema,edemaofnephroticsyndrome,HTN(2*tothiazidesinsufficiency),CHF,severehypercalcemia(combinecisotonicsaline),urineflowindrugoverdose
hypokalemia,hypomagnesaemia(riskforarrhythmias);hypochloremicmetabolicalkalosis(H+,K+depletion)hyperuricemiagoutaacksototoxicity(highdosesalterendolymph)
postmenopausalosteopenicwomen
note:generallytoopotentandshortlivedforuseasantihypertensiveagents;butusefulinptscrenalinsufficiencywhodonotrespondtootherdiuretics
ThiazidesHydrochlorothiazide(HCTZ),chlorothiazide,chlorthlidone,indapmide
inhibitsNaClsymportintheDCTonlythiazideshavesignificanteffectonthissymport
bestinitialtherapyforuncomplicatedHTN,heartfailure,hepaticcirrhosis,nephroticsyndrome,chronicliverfailure,acuteglomerulonephritis,nephrogenicdiabetesinsipidus,calciumnephrolithiasisandosteoporosis
hypokalemicmetabolicalkalosisandhyperuricemia,hyperlipidemia(totalcholesterolandLDL),impairedcarbohydratetolerance,quinidineinducestorsadesdepointes
mostcommonlyuseddiureticinHTN
amiloridetriameterene
lumennegavetransepithelialvoltageexcreonrateofK+,H+,Ca,MgantikaliureticactiontooffsettheexcretionofK+andH+byK+wastingdiureticslowimpactonNa+excretion
UsedincombinationwithotherdiureticstocurtailK+lossduringtreatmentofedemaassociatedwithCHFand/orhypertensionAmilorideblocksLi+transportinthecollectingtubulesandisthereforeusedtotreatlithiuminducednephrogenicdiabetes
commonforboth:N/Vamiloride:diarrhea,HAtriameterne:legcrampsanddizzinessriskoflifethreatening:contraindicatedinptscrenalfailureortakingACEI,otherK+sparingdiuretic,K+supplement,pentamidine,trimethoprimTriamtereneisaweakfolicacidantagonistandcanexacerbatemegaloblastosis
AmilorideisexcretedintactintheurineTriamtereneundergoesextensivehepatictransformationcautioninbothhepaticandrenalinsufficiency
Aldosteroneantagonists:Eplerenone(Inspra)andSpironolactone(Aldactone)
Inhibitsmineralocorticoidreceptor(MR)inepithelialcellsoftheDCTandCTConservepotassiumattheexpenseofsodium
Spironolactone:diureticofchoiceinptschepaticcirrhosis,PrimaryAldosteronism,Refractoryedemaassociatedwithsecondaryhyperaldosteronism
Hyperkalemia,Impotence,decreaselibido,hirsutism,gynecomastia,deepeningofthevoiceandmenstrualirregularities;diarrhea,gastritis,gastricbleedingandpepticulcers;SpironolactonemaycauseskinrashanditsCNSeffectsmayincludedrowsiness,ataxia,lethargy,confusionandHA
patientswithgastriculcers
Osmoticdiuretic Mannitolwaterexcreoninpreferencetosodiumexcretion;majoreffectinPCTanddescendinglimbofHenle
intracranialhypertension
Diuretics(Naexcreon,rateofurineflow)
youngwhiteexertionalangina
Pregnancy
priorMI
AfricanAmerican
heartfailure
prinzmetal'svariant
dyslipidemiachronickidney
BPHMigrainecephalgia
Avoids Depression:Centralalphaagonists,betablockers
circulatoryvolume,CO,andmeanarterialpressure;mosteecveinpaentscmildtomoderateHTNwhohavenormalrenalfxn,1015mmHg
K+sparingdiuretics