NR566 Final Exam Weeks 5 & 7.
i i i i i i
NR 566 Final Exam Review
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Week 5 Review i i
Chapter i18: iDrugs iAffecting ithe iHematopoietic iSystem
1. Anticoagulants (oral & parenteral)
i i i i
Oral Anticoagulants
i
▪ Warfarin i(Coumadin): iInhibits isynthesis iof ivitamin iK-dependent iclotting ifactors iX, iIX, iVII, iand iII
i(prothrombin)
▪ Pharmacokinetics
▪ Well-absorbed iwhen itaken iorally
▪ Metabolized iby iCYP i1A2 iand i2C9
▪ Half-life iof i3 ito i4 idays
▪ Precautions iand icontraindications
▪ Pregnancy icategory iX
▪ Use icautiously iin ipatients iwith ifall irisk, idementia, ior iuncontrolled ihypertension.
▪ Avoid iin ihypermetabolic istate.
▪ The imajor iadverse idrug ireaction iis ibleeding i(Antidote iis ivitamin iK)
▪ Many idrug iinteractions, iincluding i(but inot ilimited ito):
▪ Antiplatelet idrugs
▪ Thrombolytic idrugs
▪ Oral icontraceptives, icarbamazepine, iVitamin iK-containing ifoods, ietc.
▪ Clinical iuse iand idosing
▪ Drug iof ichoice ifor ideep ivein ithrombosis i(DVT) iand ipulmonary iembolism i(PE)
▪ Start iat i5 img iper iday i(7.5 img/d iif iweight igreater ithan i80 ikg).
▪ Consider ilower idose iin ithe ifollowing isituations:
▪ Older ithan i75 iyears
▪ Multiple icomorbid iconditions
▪ Elevated iliver ienzymes
▪ Changing ithyroid istatus
▪ Dose ito imaintain iinternational inormalized iratio i(INR) ibetween i2 iand i3.
▪ Monitoring
▪ INR idaily iuntil iin itherapeutic irange ifor i2 iconsecutive idays
▪ Then itwo ior ithree itimes iweekly ifor i1 ito i2 iweeks
▪ Then iless ifrequently ibut iat ileast ievery i6 iweeks
▪ Rivaroxaban i(Xarelto): iFactor iXa iinhibitor
▪ Apixaban i(Eliquis): iFactor iXa iinhibitor
▪ Reduction iof irisk iof istroke iand isystemic iembolism iin inonvalvular iatrial ifibrillation
▪ Prophylaxis iof iDVT ifollowing iknee ireplacement isurgery
▪ Treatment iof iDVT iand iPE
,Parenteral Anticoagulants
i
▪ Heparin
▪ Binds iwith ithe iantithrombin iIII
▪ Inactivates ifactors iIXa, iXa, iXIIa, iXIII
▪ Pharmacokinetics
▪ Given iIV ior isubcutaneously i(SC)
▪ Extensively iprotein-bound
▪ Metabolized iby iliver iand irenally ieliminated
▪ Precautions iand icontraindications
▪ Pregnancy icategory iC
▪ Avoid iin iadvanced ihepatic ior irenal idisease.
▪ Avoid iin ibleeding idisorders ior iactive ibleeding.
▪ Adverse idrug ireactions i(ADRs)
▪ May icause ithrombocytopenia
▪ Life-threatening ibleeding
▪ Pain iat iinjection isite i(SC)
▪ Antidote iis iprotamine isulfate
▪ Drug iinteractions
▪ Cephalosporins iand ipenicillins; iWarfarin, iantiplatelets iand ithrombolytics;
iValproic iacid
▪ Clinical iuse iand idosing
▪ Given i2 ihours ipre-operatively
▪ Maintenance ievery i8 ito i12 ihours ifor i7 idays iafter isurgery
▪ Heparin iis iprocessed iinto ismaller imolecules i low molecular-weight heparins
i i i
(LMWH)
i
▪ Inactivates ifactor iXa
▪ Enoxaparin
▪ DVT ior iPE
▪ Given i2 ihours ibefore isurgery
▪ Fondaparinux i- iSelective iinhibitor iof iantithrombin iIII iand ifactor iXa iinhibitor
▪ DVT
▪ Hip ifracture isurgery ior iknee ireplacement
▪ Dalteparin
▪ Prevention iof iDVT iafter iabdominal isurgery ior ihip ireplacement
▪ Monitoring ifor iAnticoagulants
▪ Activated ipartial ithromboplastin itime
▪ Platelet iand ihematocrit i(Hct) ievery i2 ito i3 idays iinitially
▪ Patient iEducation ifor iAnticoagulants
▪ Administration
▪ Warfarin idosing imay ivary iday ito iday.
▪ SC iadministration iinstruction ifor iLMWH iat ihome
▪ ADRs ifor iAnticoagulants
▪ Risk ifor ibleeding
, ▪ Vitamin iK-containing ifoods
I. Antiplatelet Drugsi
▪ Aspirin: iInhibits icyclooxygenase i& iinterferes iwith iplatelet iaggregation
▪ Well-absorbed iwhen itaken iorally
▪ Metabolized iin iliver
▪ Renally iexcreted i (pH iaffects iexcretion)
▪ Aspirin iHypersensitivity i-- iCross-sensitivity iwith iNSAIDs
▪ Pregnancy icategory iC i(D iin ithird itrimester)
▪ Can icause iReye isyndrome iin ichildren
▪ ADR: iBleeding; iMay icause igastrointestinal i(GI) ibleeding; iSalicylism i(tinnitus)
▪ Drug iinteractions: iConcurrent iuse iof iother iantiplatelet, ianticoagulant, ior ifibrinolytic
idrugs
▪ Aspirin: iHerbals i(ginko, igarlic, iginseng), iNSAIDs
▪ Clinical iuse iand idosing ifor iaspirin:
▪ Myocardial iinfarction i(MI) iprevention: i75 ito i162 img idaily
▪ Persistent iatrial ifibrillation: i75 ito i325 img idaily
▪ Stroke ior itransient iischemic iattacks: i50 ito i100 img idaily
▪ Patient iEducation ifor iadministration:
▪ Take iaspirin iwith ia ifull iglass iof iwater.
▪ Aspirin imust ibe istopped i7 idays ibefore isurgery.
▪ Ticlodipine i& iclopidrogrel: ireduce iplatelet iaggregation iby iinhibiting iadenosine idiphosphate
ipathway
▪ Ticlopidine: iRapidly iabsorbed iafter ioral iadministration; iMetabolized iin iliver; iHalf-life
ilengthens iwith irepeated idosing; iDecreased irenal iclearance iwith iage
▪ Clopidogrel: iProdrug: imetabolized iinto iactive imetabolite; iExcreted iin iurine iand ifeces
▪ Ticlopidine iADR: ineutropenia; iAvoid iin ipatients iwith iliver idysfunction
▪ Clopidogrel iADR: ibleeding; iAvoid iin ipatients iwith iliver idysfunction
▪ Drug iinteractions: iConcurrent iuse iof iother iantiplatelet, ianticoagulant, ior ifibrinolytic
idrugs
▪ Clopidogrel-specific: iProton ipump iinhibitors i(PPIs); iCYP i2C19 iinhibitors
▪ Ticlopidine-specific: iAntacids; iDigoxin; iCimetadine
▪ Clinical iuse iand idosing ifor iclopidogrel:
▪ MI iprevention: i75 img idaily
▪ ST-elevation iacute icoronary isyndrome: i300 img idaily iif iless ithan i75 iyears iof iage
iand i75 img idaily iif imore ithan i75 iyears iof iage
▪ Clinical iuse iand idosing ifor iticlopidine:
▪ Prevent istones iin ipatients iintolerant iof iacetylsalicylic iacid: i250 img itwice idaily
i i i i i i
NR 566 Final Exam Review
i i i i
Week 5 Review i i
Chapter i18: iDrugs iAffecting ithe iHematopoietic iSystem
1. Anticoagulants (oral & parenteral)
i i i i
Oral Anticoagulants
i
▪ Warfarin i(Coumadin): iInhibits isynthesis iof ivitamin iK-dependent iclotting ifactors iX, iIX, iVII, iand iII
i(prothrombin)
▪ Pharmacokinetics
▪ Well-absorbed iwhen itaken iorally
▪ Metabolized iby iCYP i1A2 iand i2C9
▪ Half-life iof i3 ito i4 idays
▪ Precautions iand icontraindications
▪ Pregnancy icategory iX
▪ Use icautiously iin ipatients iwith ifall irisk, idementia, ior iuncontrolled ihypertension.
▪ Avoid iin ihypermetabolic istate.
▪ The imajor iadverse idrug ireaction iis ibleeding i(Antidote iis ivitamin iK)
▪ Many idrug iinteractions, iincluding i(but inot ilimited ito):
▪ Antiplatelet idrugs
▪ Thrombolytic idrugs
▪ Oral icontraceptives, icarbamazepine, iVitamin iK-containing ifoods, ietc.
▪ Clinical iuse iand idosing
▪ Drug iof ichoice ifor ideep ivein ithrombosis i(DVT) iand ipulmonary iembolism i(PE)
▪ Start iat i5 img iper iday i(7.5 img/d iif iweight igreater ithan i80 ikg).
▪ Consider ilower idose iin ithe ifollowing isituations:
▪ Older ithan i75 iyears
▪ Multiple icomorbid iconditions
▪ Elevated iliver ienzymes
▪ Changing ithyroid istatus
▪ Dose ito imaintain iinternational inormalized iratio i(INR) ibetween i2 iand i3.
▪ Monitoring
▪ INR idaily iuntil iin itherapeutic irange ifor i2 iconsecutive idays
▪ Then itwo ior ithree itimes iweekly ifor i1 ito i2 iweeks
▪ Then iless ifrequently ibut iat ileast ievery i6 iweeks
▪ Rivaroxaban i(Xarelto): iFactor iXa iinhibitor
▪ Apixaban i(Eliquis): iFactor iXa iinhibitor
▪ Reduction iof irisk iof istroke iand isystemic iembolism iin inonvalvular iatrial ifibrillation
▪ Prophylaxis iof iDVT ifollowing iknee ireplacement isurgery
▪ Treatment iof iDVT iand iPE
,Parenteral Anticoagulants
i
▪ Heparin
▪ Binds iwith ithe iantithrombin iIII
▪ Inactivates ifactors iIXa, iXa, iXIIa, iXIII
▪ Pharmacokinetics
▪ Given iIV ior isubcutaneously i(SC)
▪ Extensively iprotein-bound
▪ Metabolized iby iliver iand irenally ieliminated
▪ Precautions iand icontraindications
▪ Pregnancy icategory iC
▪ Avoid iin iadvanced ihepatic ior irenal idisease.
▪ Avoid iin ibleeding idisorders ior iactive ibleeding.
▪ Adverse idrug ireactions i(ADRs)
▪ May icause ithrombocytopenia
▪ Life-threatening ibleeding
▪ Pain iat iinjection isite i(SC)
▪ Antidote iis iprotamine isulfate
▪ Drug iinteractions
▪ Cephalosporins iand ipenicillins; iWarfarin, iantiplatelets iand ithrombolytics;
iValproic iacid
▪ Clinical iuse iand idosing
▪ Given i2 ihours ipre-operatively
▪ Maintenance ievery i8 ito i12 ihours ifor i7 idays iafter isurgery
▪ Heparin iis iprocessed iinto ismaller imolecules i low molecular-weight heparins
i i i
(LMWH)
i
▪ Inactivates ifactor iXa
▪ Enoxaparin
▪ DVT ior iPE
▪ Given i2 ihours ibefore isurgery
▪ Fondaparinux i- iSelective iinhibitor iof iantithrombin iIII iand ifactor iXa iinhibitor
▪ DVT
▪ Hip ifracture isurgery ior iknee ireplacement
▪ Dalteparin
▪ Prevention iof iDVT iafter iabdominal isurgery ior ihip ireplacement
▪ Monitoring ifor iAnticoagulants
▪ Activated ipartial ithromboplastin itime
▪ Platelet iand ihematocrit i(Hct) ievery i2 ito i3 idays iinitially
▪ Patient iEducation ifor iAnticoagulants
▪ Administration
▪ Warfarin idosing imay ivary iday ito iday.
▪ SC iadministration iinstruction ifor iLMWH iat ihome
▪ ADRs ifor iAnticoagulants
▪ Risk ifor ibleeding
, ▪ Vitamin iK-containing ifoods
I. Antiplatelet Drugsi
▪ Aspirin: iInhibits icyclooxygenase i& iinterferes iwith iplatelet iaggregation
▪ Well-absorbed iwhen itaken iorally
▪ Metabolized iin iliver
▪ Renally iexcreted i (pH iaffects iexcretion)
▪ Aspirin iHypersensitivity i-- iCross-sensitivity iwith iNSAIDs
▪ Pregnancy icategory iC i(D iin ithird itrimester)
▪ Can icause iReye isyndrome iin ichildren
▪ ADR: iBleeding; iMay icause igastrointestinal i(GI) ibleeding; iSalicylism i(tinnitus)
▪ Drug iinteractions: iConcurrent iuse iof iother iantiplatelet, ianticoagulant, ior ifibrinolytic
idrugs
▪ Aspirin: iHerbals i(ginko, igarlic, iginseng), iNSAIDs
▪ Clinical iuse iand idosing ifor iaspirin:
▪ Myocardial iinfarction i(MI) iprevention: i75 ito i162 img idaily
▪ Persistent iatrial ifibrillation: i75 ito i325 img idaily
▪ Stroke ior itransient iischemic iattacks: i50 ito i100 img idaily
▪ Patient iEducation ifor iadministration:
▪ Take iaspirin iwith ia ifull iglass iof iwater.
▪ Aspirin imust ibe istopped i7 idays ibefore isurgery.
▪ Ticlodipine i& iclopidrogrel: ireduce iplatelet iaggregation iby iinhibiting iadenosine idiphosphate
ipathway
▪ Ticlopidine: iRapidly iabsorbed iafter ioral iadministration; iMetabolized iin iliver; iHalf-life
ilengthens iwith irepeated idosing; iDecreased irenal iclearance iwith iage
▪ Clopidogrel: iProdrug: imetabolized iinto iactive imetabolite; iExcreted iin iurine iand ifeces
▪ Ticlopidine iADR: ineutropenia; iAvoid iin ipatients iwith iliver idysfunction
▪ Clopidogrel iADR: ibleeding; iAvoid iin ipatients iwith iliver idysfunction
▪ Drug iinteractions: iConcurrent iuse iof iother iantiplatelet, ianticoagulant, ior ifibrinolytic
idrugs
▪ Clopidogrel-specific: iProton ipump iinhibitors i(PPIs); iCYP i2C19 iinhibitors
▪ Ticlopidine-specific: iAntacids; iDigoxin; iCimetadine
▪ Clinical iuse iand idosing ifor iclopidogrel:
▪ MI iprevention: i75 img idaily
▪ ST-elevation iacute icoronary isyndrome: i300 img idaily iif iless ithan i75 iyears iof iage
iand i75 img idaily iif imore ithan i75 iyears iof iage
▪ Clinical iuse iand idosing ifor iticlopidine:
▪ Prevent istones iin ipatients iintolerant iof iacetylsalicylic iacid: i250 img itwice idaily