harm 1.

2 - ANS
D|rect-Acnng Cho||nerg|c Agon|sts
-AceLylchollne - muscarlnlc and nlcounlc recepLors
-8eLhanechol - muscarlnlc and nlcounlc recepLors, sumulaLe perlsLalsls and urlnauon
-llocarplne - #1 Lx glaucoma, sweaL and sallvaLe excesslvely
-Cevlmellne - selecuve for M3 recepLors, lncrease sallvauon w/o sweaung
-nlcoune - nlcounlc recepLors, Lx polsonlng wlLh aLroplne, anuconvulsanLs, resplrauon
-varenlcllne - parual agonlsL on nlcounlc alpha,beLa, recepLors, Lx nlcoune cravlng
Cho||nesterase Inh|b|tors
-Ldrophonlum - blnds reverslbly, lv, dlagnosls of myasLhenla gravls, shorL acuon
-neosugmlne - does noL peneLraLe 888, Lx myasLhenla gravls
-hysosugmlne - lnsull dlrecLly lnLo eye, Lx glaucoma
-LchoLhlophaLe - lnsull dlrecLly lnLo eye, Lx glaucoma ln emergency, long acuon
-ralldoxlme - early Lx organophosphaLe
(CarbamaLes)
Cho||nerg|c (Muscar|n|c) Antagon|sts
-ALroplne - early Ml Lo decrease bradycardla or Av block
-Scopolamlne - paLch Lx mouon slckness
-1olLerodlne - selecuve M3 recepLor anLagonlsL, Lx overacuve bladder ln elderly
-CxybuLynln - prevenL bladder spasm aer prosLaLe surgery
-ClycopyrrolaLe - used ln sx Lo decrease vagal Lone, decrease slde eecLs ln Lx of MC
-Sollfenaclne - M3 recepLor anLagonlsL, Lx overacuve bladder w/ llule eecL on sallvauon
-lpraLroplum - lnhalauon for Lx CCu
-1roplcamlde - shorL-acung mydrlasls and cycloplegla for eye examlnauons
-PomaLroplne - shorLer durauon Lhan aLroplne, dllaLes Lhe eye
-ulphenoxylaLe-aLroplne - Lx dlarrhea
-8enzLroplne - decrease exLrapyramldal sympLoms of anupsychoucs, arklnson's
Non-Depo|ar|z|ng Neuromuscu|ar 8|ockers
-d-1ubocurarlne - 4-6 onseL, 2-3 hr durauon, hlsLamlne release
-ancuronlum - 4-6 onseL, 2-3 hr durauon, vagal blockade and Lachycardla
-vecuronlum - 2-4 onseL, 20-40 durauon
-ClsaLracurlum - 2-4 onseL, 20-40 durauon
-8ocuronlum - 1-2 onseL, 20-33 durauon, lnLubauon
Depo|ar|z|ng Neuromuscu|ar 8|ocker
-Succlnylchollne - lnlual sumulauon and conLracuon-blockade, rapld procedures
Gang||on 8|ockers
-Mecamylamlne - crosses 888, blocks nlcounlc recepLors, causes sedauon, Lremor
-PexameLhonlum - eecLs llke blocklng boLh sympaLheuc and parasympaLheuc lnpuL,
cycloplegla, mydrlasls, orLhosLauc hypoLenslon, Lachycardla, urlnary reLenuon
Adrenerg|c Snmu|ants
Catecho|am|nes
-Lplnephrlne - low dose/hlgh dose, Lx anaphylacuc shock, cardlac arresL, glaucoma
-noreplnephrlne - sumulaLe o=,>>,, severe vasoconsLrlcuon aL lnfuslon slLe-necrosls
-lsoproLerenol - , and , agonlsL, emergency Lx of cardlac arresL
A|pha Agon|sts
-henylephrlne - o, selecuve agonlsL, use ln hypoLenslve emergency, produces mydrlasls
-seudoephedrlne - decongesLanL
A|pha-2 Agon|sts
-Clonldlne - selecuve o, agonlsL, Lransdermal paLch, Lx for P1n, reduce cravlng
-Apraclonldlne - used ln eye Lo Lx lnLraocular pressure
8eta-1 Agon|sts
-uobuLamlne - selecuve , agonlsL, cardlac sLress LesL
8eta-2 Agon|sts
-AlbuLerol - selecuve , agonlsL, Lx asLhma
-8lLrodlne - relax Lhe uLerus
Cthers
-Lphedrlne - bronchodllauon, deaLh due Lo P1n
-AmpheLamlne - CnS sumulanL, Lachycardla, P1n, psychosls
-MeLhylphenldaLe - used ln chlldren wlLh auenuon declL
-Cocalne - lnhlblLs re-upLake of uA and nL, addlcung, causes P1n, sLroke ln younglns
-1yramlne - depresslon pLs Lx wlLh MAC lnhlblLors: may cause severe hyperLenslon crlsls
Dopam|ne Agon|sts
-uopamlne - low dose acuvaLe u1, hlgh dose , on hearL, Lx cardlac shock w/o vC
-lenoldopam - selecuve u1 agonlsL, rapld decrease 8 ln severe P1n
Adrenerg|c 8|ock|ng Agents
A|pha-keceptor 8|ockers
-henLolamlne - compeuuve anLagonlsL aL o, and o,, Lx pheochromocLoma
-henoxybenzamlne - lrreverslble anLagonlsL
A|pha-1 8|ockers
-razosln - very selecuve for o,, lack of o, block reduces llkellhood of reex Lachycardla
-1erazosln - Lx 8P ooJ P1n, 1
1/2
12 hours-glve once a day
-uoxazosln - Lx 8P ooJ P1n, 1
1/2
20 hours-glve once a day
-1amsulosln - selecuve for o
1A
, Lx 8P w/ llule eecL on blood pressure
-Alfuzosln - slmllar Lo 1amsulosln buL causes dlzzlness
A|pha-2 8|ockers
-?ohlmblne - o, selecuve anLagonlsL, lncreases nL release, acLs opposlLe Clonldlne
8eta-keceptor 8|ockers
-ropranolol - non-selecuve compeuuve anLagonlsL, Lx hyperLhyroldlsm, mlgralne, frlghL
-1lmolol - Lx glaucoma, may be absorbed so should noL be used ln asLhmaucs
Card|ospec|hc or 8eta-1 8|ockers
-MeLoprolol - lnc. llfe posL-Ml, decrease renln, beuer exerclse Lolerance, rlsky ln asLhma
-ALenolol - same as meLoprolol
-Lsmolol - very shorL durauon of acuon, glve lv, Lx lf unsure pL can handle beLa blockers
-8eLaxolol - Lx glaucoma
8eta-8|ockers w|th (ISA) Intr|ns|c Sympathenc Acnv|ty
-lndolol - nonselecuve wlLh some lSA
-AcebuLolol - selecuve , anLagonlsL w/ lnLrlnslc acuvlLy, rlsk of bradycardla decreased
Comb|ned A|pha- & 8eta-8|ockers
-LabeLalol - blocks , , and o,, lv Lx hyperLenslve emergency, assoclaLed w/ llver ln[ury
-Carvedllol (Coreg) - -blocker and o, blocker, decreases free radlcals, Lx P1n/CPl
Synthes|s Inh|b|tor
-MeLyroslne - blocks Lyroslne hydroxylase, pre-surglcal Lx of pheochromocyLoma
harm 1.3 - Card|ovascu|ar Drugs
D|urenc Agents (|oop>>th|az|des>>CA |nh.>k spar|ng)
Carbon|c Anhydrase Inh|b|tors
lnh CA (proxlmal Lubule) - j blcarb reabsorpuon, ^ na excreuon (jP lC), so ^ k exc.
Alkallnlzes urlne, hyper-Cl, hypo-k, meLabollc acldosls, j aqueous humor
1x: meL alkalosls, acuLe mLn slckness, glaucoma, alkallnlze urlne
Cl: clrrhosls
Lecuve for only a few days
-AceLazolamlde - oral
-8rlnzolamlde - Loplcal
-uorzolamlde - Loplcal
Loop D|urencs (2S of Na) - oral
8lock nak2Cl coLransporL (Lhlck asc. loop) - ^na, k, Mg, Ca, P excreuon
Pypo-k, hypo-Cl, meLabollc alkalosls, oLoLoxlc, heavy dluresls
1x: CPl, pulm edema, acuLe renal fallure, hyper-k, hyper-Ca
Cl: avold nSAlus,
-lurosemlde (Laslx)
-1orsemlde - lower dose
-8umeLanlde - lower dose
-LLhacrynlc Acld - mosL oLoLoxlc, non-sulfa
1h|az|de D|urencs and re|ated (S of Na) - oral
lnh na reabsorpuon (dlsLal dlluung slLe) - ^na, k, Cl excreuon, Ca sparlng
Pypo-k, meL alkalosls, Ca sparlng (j sLones), hyperglycemla, hyperllpldemla, hyperurlcemla, llver
meLabollsm
1x: P1n, CPl, nephrogenlc u. lnslpldus
Cl: avold nSAlus
-PydrochloroLhlazlde - uCC: P1n
-ChlorLhalldone - slower absorpuon, longer durauon
-MeLolazone - dluresls ln pauenLs w/ reduced Cl8
-lndapamlde - less meLabollc compllcauons, CC8 llke eecLs
otass|um Spar|ng D|urencs - oral
lnh na/k exchange (collecung ducLs) - ^na excreuon, k sparlng
Pyper-k, acuLe renal fallure
1x: CPl, comblned wlLh k loslng drugs, clrrhosls
Cl: Pyper-k
-1rlamLerene
-Amllorlde
AlJostetooe Aotoqoolsts - lnh. AldosLerone recepLors ln dlsLal/collecung ducL
-SplronolacLone - ^ survlval ln CPl, gynecomasua
-Lplerenone - ^ survlval ln CPl, j endocrlne SL's, C?3A4 meL
Csmonc D|urencs - lv
lncreased osmouc acuvlLy, waLer reLenuon (prox, loop, Cu) (freely lLerable agenLs)
uehydrauon, hyper-na
Cl: severe CPl (early over-expanslon of lnLravascular space)
-MannlLol - j lnLracranlal pressure, neuro-sx prophylaxls
-lsosorblde
-Clycerln
-urea
ADn Antagon|sts
^ permeablllLy ln Cu
-uemeclocycllne
-LlLhlum
CnI Drugs
Inotrop|c Agents
D|g|ta||s (foxglove, ulqltolls potpoteo, dra evaders, arrow polson) oral
lnh na/k-A1ase - ^ lC na (j lC k) - j Ca expulslon so ^ lC Ca - ^ conLracullLy
^ conLracullLy, j P8, ^ CC & vaso-u ln falllng hearLs only, j Av conducuon
1x: CPl, A-b, A-uuer
SL: Cl upseL - lower dose, cardlac (brady, Av block, blgemlny) - cease Lherapy, CnS
1oxlclLy: ^ by Ca, j by k, 1x LoxlclLy w/ k or ulgl8lnd for Cu
Cl(relauve): qulnldlne (^ serum drug), k loslng drugs, -blockers, cardloverslon (excepL v-b)
-ulgoxln - 1 week Lo sLeady sLaLe
-ulglLoxln - noL ln uS, unfavorable Pk
-Cuabaln - experlmenLal
hosphod|esterase Inh|b|tors (lnodllaLors) lv
lnh uL 3 - ^cAM - ^conLracullLy, vasodllauon, ^ CC
^ MorLallLy
-lnamrlnone
-Mllrlnone
Sympathom|mencs
-uobuLamlne - -1 agonlsL, ^ conLracullLy, mlld ^ P8, lv
-uopamlne - low dose - ^renal 8l (^ urlne producuon), ^CC, 1x: severe refracLory CPl,
med dose - 1 agonlsL, llule Lo no change ln 8, hlgh dose - o agonlsL, vaso-c, ^8
Ca|c|um Sens|nzers
-Levoslmendan, plmobendan - experlmenLal
Drugs w]out os|nve Inotrop|c Lects
Loop agents
lnLenslve dluresls
-lurosemlde, Lorsemlde, bumeLanlde, eLhacrynlc acld
1h|az|des and ke|ated Compounds
MalnLenance Lherapy
-PydrochloroLhlazlde, eLc.
-MeLolazone, lndapamlde, eLc
k Spar|ng (lncludlng AldosLerone AnLagonlsLs)
-1rlamLerene, amllorlde
-SplronolacLone, Lplerenone - jmorLallLy
8 1ype Natr|urenc epnde
-neslrlude (naLrecor) - 1x: acuLe decompensaLed CPl, wlll jCW
ACL Inh|b|tors - oral or lv
jpreload (j dlrecL vaso-C), jaerload (j aldosLerone), jussue remodellng
SL: dry cough (^bradyklnln), hyper-k
Cl: bllaLeral renal arLery sLenosls, pregnancy
jmorLallLy, no reex Lachy
-CapLoprll, Lnalaprll, eLc.
Ang|otens|n II keceptor 8|ockers (Ak8's) - oral
Same eecLs as ACL lnh. w/ ouL ^bradyklnln and cough
-LosarLan, valsarLan, candesarLan
8eta-8|ockers -Carvedllol (Coreg, o-1 & ), 8lsoprolol, MeLoprolol (Lopressor, -1), eLc ,
jmorLallLy, jremodellng, jrenln Cl: severe CPl
Vasod||ators
SL: reex Lachycardla, uld reLenuon - glve concomlLanLly w/ -blocker and dlureuc
-Sodlum nlLroprusslde - lv, dllaLes arLerles and velns, Lx: acuLe decomp. CPl
-Pydralazlne - oral, dllaLes arLerles, ^CC, SL: SLL
-lsosorblde dlnlLraLe, nlLroglycerln - subllngual (sklp 1' pass), dllaLes velns -jpreload, develop
Lolerance so noL for long Lerm use
Ca|c|um Channe| 8|ockers
Cenerally Cl ln CPl
-Amlodlplne - sllghLesL negauve lnoLroplc eecL, belng sLudled for use ln CPl
Cthers
-Amlodarone - class lll anuarrhyLhmlc, may ^ e[ecuon fracuon ln CPl
Drugs Used |n Card|ac Arrhythm|as
C|ass I (Sod|um channe| b|ockers)
[l-A] - blnd open & lnacuvaLed na channels -^L8, ^A durauon,
^ C8S,C1 durauons -Lorsades,
- Culnldlne - oral, SL: Cl upseL(dlarrhea), paradoxlcal Lachy-C, Lorsades & syncope, ^axn of
warfarln, dlgoxln, & nM! blockers axn, clnchonlsm, 1x: broad specLrum, supravenL. & venL.
arrhyLhmlas , Cl: Av block
-rocalnamlde - lv, SL: SLL
-ulsopyramlde - oral , 1x: venLrlcular Lachycardla, SL: (-)lnoLroplc
[l-8] - jL8, no A C8S,C1
-Lldocalne - lv, 1x: venLrlcular arr, convulslon, bradycardla
-henyLoln - oral/lv, 1x: dlg. lnduced venL. arr, lnLeraxn: proLeln blndlng, -430
-1ocalnlde - oral, use: pLs w/ lldo allergy, venL. arr.
-Mexlleune - 1x: palnful dlabeuc neuropaLhy, venL. arr. ln lldo reslsLanL pLs
[l-C] - poLenL, 1x: llfe LhreaLenlng venLrlcular arrhyLhmlas
-llecalnlde - oral, lnh. fasL na channels, jA durauon, ^C8S, 1x: Sv1, A-b, A-uuer,
Cl: Av block, CPl
-ropafenone - oral
-Morlclzlne - oral, lA, l8, lC llke eecLs
C|ass II (8eta-b|ockers)
-ropranolol - 1x: A-b, A-uuer, Sv1, WW, selecLed venL. arr, SL: anglna lf w/drawn qulckly, Cl:
8aynaud's
-Lsmolol (8revlbloc) - lv, -l block, rapld & shorL axn, 1x: acuLe Sv1 (2 Lo adenoslne)
C|ass III (pro|ong repo|ar|zanon, k channe| b|ockers)
-Amlodarone - oral/lv, class l-lv eecLs & some o, blocklng, jP8, jconducuon, ^C8S,C1,
SL: Llvlra(brown eyes, gray skln), brady, pulm. brosls, less proarrhyLhmlc, 1x: broad arr, ACLS v-Lach,
v-b
-SoLalol (8eLapace)- oral, class ll & lll eecLs, 1x: venL. & supravenL. arr, SL: Lorsades, -block
-8reLyllum - lv, 1x: v-b, v-Lach
-lbuullde, uofeullde - 1x: converL A-b & A-uuer Lo normal slnus, SL: Lorsades
C|ass IV (Ca|c|um channe| b|ockers)
lnh L-Lype Ca channels, ^L8, jP8, (-)lnoLrope
-verapamll-1x: reenLranL supravenL. Lachy-C, CI: vent. Arr, CPl, Av block, -blockers
-ulluazem (Cardlzem) - oral/lv more perlpheral eecLs Lhan verapamll- ^CC,
1x: rlnzmeLal's varlanL anglna, sLable anglna
-8eprldll
M|sce||aneous
-Adenoslne - lv, ^k conducLance, jcAM-Ca, 1x: uCC acuLe Sv1, WW, reenLry
-ulgoxln - 1x: pre-Lx for A-b before class lA ls glven
-Magneslum - 1x: Lorsades de polnLes, eclampsla
-oLasslum - Lx dlgoxln LoxlclLy
Annhypertens|ve Agents
D|urencs (1h|az|des, Loops, k Spar|ng)
-PydrochloroLhlazlde - rsL drug, Afrlcan Amerlcans, SL: hyperurlcemla, Lu
-ChlorLhalldone, MeLolazone
-lndapamlde - dlrecL vasodllaLor
-lurosemlde (Loop) - severe cases, pLs w/ renal lnsumclency, CPl
-1rlamLerene (k sparlng) - combo w/ PC1Z and loops
-SplronolacLone, Lplerenone - aldosLerone anLag. & k sparlng
Sympatho|yncs
AcuvaLe baroreexes and reLaln na - comblne w/ dlureuc
Centra||y Acnng Drugs
o-2 agonlsL - jsymp. Lone, jrenln, SL: sedauon, urug lnLraxn: yohlmblne
-Clonldlne - sudden wlLhdrawal - P1n crlsls
-MeLhyldopa - SL: hemolyuc anemla w/ (+)Coombs LesL
Gang||on 8|ock|ng Agents
-Mecamylamlne - many SL's
Adrenerg|c Neuron-b|ock|ng Agents
jnL release -jsympaLheuc Lone
-CuaneLhldlne - 8eplaces nL ln veslcles -jnL release, vaso-u, causes hyperLenslve crlsls ln
pheochromocyLoma (lnlual large nL bolus release)
-8eserplne - lnh nL LransporL lnLo veslcles
MAC Inh|b|tors
-henelzlne
A|pha-1 Adrenerg|c 8|ockers
o-1 block - vaso-u, less reex Lachy, SL: 1' dose phenomenon -hypoLenslon
-razosln, uoxazosln, 1erazosln
8eta-receptor 8|ockers
Works well for caucaslans & young, Avold ln pLs w/ uM, hyperllpld, severe CPl
jCC, lnlual jrenln, SL: reex ^renln and Lachy-C, and Lhe usual
-ropranolol, nadolol, 1lmolol - nonselecuve
-MeLoprolol (Lopressor), ALenolol, 8lsoprolol - -1 block
-lndolol - -block w/ lSA
-AcebuLolol - -1 block w/ lSA
-LabeLalol, Carvedllol (Coreg) - o-1 & blocker
D|rect Acnng Vasod||ators
SL: reex ^renln & Lachy-C, uld reLenuon - glve w/ -blocker and dlureuc
-Sodlum nlLroprusslde- lv, dllaLes arLerles & velns, 1x: severe P1n, acuLe decomp. CPl
-Pydralazlne - oral, dllaLes arLerles, ^CC, SL: SLL, anglna
-lsosorblde dlnlLraLe, nlLroglycerln - subllngual (sklp 1' pass), dllaLes velns -jpreload, develop
Lolerance so noL for long Lerm use
-Mlnoxldll - oral, arLerles, opens k channels, hyperLrlchosls (Loplcal: 8ogalne)
-ulazoxlde - lv, arLerles, +A1-k channels, jlnsulln secreuon (Lx: lnsullnoma)
-lenoldopam - lv, arLerles, u1 agonlsL -vaso-u
Ca|c|um Channe| 8|ockers
-verapamll-sLrongesL cardlac eecLs, jP8, (-)lnoLrope, depress SA/Av, SL:consupauon
-ulluazem (Cardlzem) - ln-beLween verapamll and nlfedlplne, depress SA and Av node dlrecLly
-nlfedlplne (rocardla), Amlodlplne (norvasc) - sLrongesL vasodllaLors, reex Lachycardla
ACL Inh|b|tors - oral or lv
jpreload (j dlrecL vaso-C), jaerload (j aldosLerone), jussue remodellng
1x: rsL cholce for uM, chronlc renal dlsease, LvP
SL: dry cough (^bradyklnln), hyper-k, angloedema
Cl: bllaLeral renal arLery sLenosls, pregnancy
-CapLoprll, Lnalaprll, eLc.
Ang|otens|n II keceptor 8|ockers (Ak8's) - oral
Same eecLs as ACL lnh. w/ ouL ^bradyklnln, cough, or anglo(neurouc)edema
-LosarLan, valsarLan, candesarLan
ken|n Antagon|st
-Allsklren (1ekLurna) - llke A88's
!"#$%&'"($)#*"+%*(,-*./*$0*1+2&+"*3-4($)&#
N|trates and N|tr|tes - subllngual
MosL eecL on ve|ns, nlLrlLe lon -nC -^cCM -vaso-u, 1x: anglna, Cn polsonlng
1olerance develops qulckly, Monday dlsease ln exploslve manufacLurers
-nlLroglycerln, lsosorblde dlnlLraLe, Amyl nlLrlLe (lnhaled, euphorla)
Ca|c|um Channe| 8|ockers - oral
-verapamll-sLrongesL card|ac eecLs, jP8, (-)lnoLrope, depress SA/Av, SL:consupauon
-ulluazem (Cardlzem) - ln beLween verapamll and nlfedlplne, depress SA/Av node dlrecLly
ulbyJtopytlJloes
SLrongesL vasodllaLors, reex Lachycardla
-nlfedlplne (rocardla) - oral/Loplcal, Amlodlplne (norvasc), lsradlplne
8eta 8|ockers
jcardlac workload -jC2 demand, jP8 -^perfuslon ume, jvaso-C
-ropranolol (), MeLoprolol(-1), ALenolol(-1)
hosphod|esterase-S Inh|b|tors - oral
lnh uL3(& some uL6) -^cCM, 1x: erecule dysfuncuon, SL: headache, ushlng
-Slldenal (vlagra) - ~60 mln Lo axn, C?3A4, Cl: nlLraLes, o blockers, SL: vlsual
-vardenal (LevlLra) - more selecuve for uL3-jvlsual SL, fasLer onseL of axn
-1adalal (Clalls) - longesL durauon of axn, allows for crazy weekends ln vegas
Cthers
-8anolazlne - oral, lnh. lox, lnh. LaLe na currenL, jLv wall suness, 1x: chronlc sLable anglna (noL
1' llne), SL: C?3A4, LeraLogenlc
-8osenLan - oral, endothe||n recepLor anLagonlsL, only use ln severe pulmonary P1n
Agents Used |n nyper||p|dem|a
8||e Ac|d 8|nd|ng kes|ns
-CholesLyramlne, colesupol, colesevelam - blnds blle aclds Lo prevenL lnLesunal absorpuon, ^LuL
recepLors (llver)- jserum LuL, SL: consupauon, bloaung, lmpalr drug absorpuon, noL eecuve ln
homozygous famlllal hyperchol. (no LuL recepLors)
Drugs that Impa|r Synthes|s of L|poprote|ns
-nlcounlc Acld - lnh. vLuL secreuon, ^PuL, SL: skln ushes, hyperurlcemla
nMC-coA teJoctose loblbltots - jLuL synLhesls, ^LuL recepLors, Cl: pregnancy
Also jC8, ^nC, ^plaque sLablllLy, joxldauon, jplL. agg, SL: llver, rhabdomyolysls
-LovasLaun (Mevacor), SlmvasLaun (Zocor), ALorvasLaun (LlplLor), 8osuvasLaun (CresLor), eLc
I|br|c Ac|d Der|vanves - oral
A8-o llgand -^llpoproLeln llpase acuvlLy - vLuL caLabollsm, j1C's,
SL: llver, choleLhlasls, lneecuve ln famlllal hypercholesLerolemla
-Cembrozll, ClobraLe, lenobraLe (1rlcor)
Cther
-Lzeumlbe (Zeua) - blocks lnLesunal absorpuon of cholesLerol, comblne w/ sLaun
-robucol - lnh. cholesLerol LransporL from lnLesune & ^chol. Lxcreuon, j plaque progresslon,
SL: jPuL
-d-1hyroxlne - obsoleLe
-vyLorln - Lzeumlbe/SlmvasLaun
harm 2.1 - CNS harmaco|ogy
Neurotransm|uers |n the CNS
- AceLylchollne - acLs on M and n recepLors, memory, cogn|non, auenuon, Ach neurons degeneraLe
ln Alzhelmer's, balances ouL uA
- noreplnephrlne - j = depress|on, pa|n regulauon
- uopamlne - add|cnon, emouons, movement, nlgro-sLrlaLal uA neuron degenerauon ln
arklnson's, excess = psychosls, schlzophrenla
- SeroLonln (3-P1) - decrease=depress|on, anx|ety, excess = sleep, raphe nuc Lo llmblc
- CA8A - ma[or lnhlblLory, lnLerneurons, ^=anx|ety rellef, j = se|zures (^nMuA acuvlLy)
CA8A
A
- ^Cl conducLance
CA8A
8
- ^k, jCa conducLance
- CluLamaLe - ma[or exclLaLory, lnoLroplc, meLaboLroplc, eLoh blocks [ nMuA,
NMDA recepLor - learnlng, memory, long Lerm poLenuauon, ^ = se|zures
- Clyclne - lnhlblLory, braln sLem & splnal cord lnLerneurons, blocked by sLrychnlne
- neuropepudes - endogenous oplaLes, endorphlns, enkephalln, subsLance
- Cannablnolds - 1PC, memory, cognluon, paln
Sedanve-nypnonc & Ann-Anx|ety Drugs
8arb|turates
8lnd CA8A
A
, enhance axn &+%-5-+%-+( of GA8A, hypnosls, Low safeLy margln, llfe LhreaLenlng
wlLhdrawal, schedule ll of lll, synergy w/ eLoh, Cyp430 lnducer
SL: CnS depresslon, mood dlsLoruon, jresplraLory drlve, j8, j8LM sleep
Cl: porphyrla, 1x of Cu: dluresls/alkallnlzauon of urlne, don'L glve sumulanL
- henobarblLal - anuconvulsanL
- 1hlopenLal - ulLra shorL acung, anesLhesla lnducuon
8enzod|azep|nes
8lnd CA8A
A
complex, enhance axn only when CA8A ls pteseot - celllng eecL, relauvely safe, llver
meL (no Cyp), synergy w/ eLoh, schedule lv
L: ann-anx|ety, sedanon, muscle relax, anuconvulsanL
SL: CnS depresslon, drowslness, memory loss, esp. ln elderly
1olerance: when used chronlcally, dlsconunuauon - lnsomnla, anxleLy, selzures
Cl: pregnancy, chlldren, sleep apnea
1x: anxleLy excepL CCu, 1Su, agoraphobla, chlldren
- ulazepam (vallum) - long 1
1/2
, Lx: status ep||epncus, eLoh/barb w/drawl, D1's, muscle spasm
- Chlordlazepoxlde (Llbrlum) - long 1
1/2
, Lx: eLoh w/drawl, D1's
- llurazepam (ualmane) - long 1
1/2
, hypnouc
- Lorazepam (Auvan) - lnL 1
1/2
, Lx: status ep||epncus
- Alprazolam (xanax) - shorL 1
1/2
, anxleLy + depresslon
- Mldazolam (versed) - very shorL 1
1/2
, sedauon, calmlng, amnesla ln surgery
- 1emazepam (8esLorll), 1rlazolam (Palclon) - hypnouc
- Clonazepam (klonopln) - Lx: selzures
8enzo Antagon|st
- llumazenll - compeuuve anLagonlsL, Lx: reverse CnS depresslon ln anesLhesla or Cu
SL: Lrlgger w/drawl & se|zures ln dependenL pLs
Cthers (Ann-anx|ety & Sedanves)
8lnd 8Z recepLor wlLh some CA8A enhanclng eecLs, sLrong sedauves, mlnor eecL on 8LM sleep,
llver meL & kldney excreuon, low dependence
SL: drowslness, blackouLs - sleepwalklng
- Zolpldem (Amblen) - 8Z, recepLor, 2 hour 1
1/2
- Zaleplon (SonaLa) - 8Z, recepLor, 1 hour 1
1/2
- Lszoplclone (LunesLa) - 6 hour 1
1/2
, Lx: long Lerm lnsomnla
- 8amelLeon (8ozerem) - me|aton|n agonlsL, sleep ald, Cl: sever llver dlsease
- 8usplrone (8uSpar) - Sn1
1A
parna| agon|st, tx: anx|ety w]out caus|ng sedanon, 2 weeks for
eecL, very low addlcuon poLenual, llule Lo no sedauon, SL: resLlessness, lnLraxn: ^8 wlLh MACl's
- kava - herbal anu-anxleLy, noL luA approved, SL: llver LoxlclLy, Cl: pregnancy
A|coho||sm & W|thdrawa|
Alcohol - (+) on CA8A, (-) on nMuA, Chronlc - jCA8A, ^ nMuA recepLors, lnduces Cyp2L1 (^
1ylenol meL & LoxlclLy), vasodllaLor, dlureuc, cardloLoxlc, alcohol (alcohol dehydrogenase) -
aceLaldehyde (aldehyde dehydrogenase) - aceLaLe, 1oxlclLy: emesls, coma, jresplrauon, deaLh, also
elecLrolyLe dlsLurbances, cuLaneous vaso-u
WlLhdrawal: can lasL up Lo 3 days, anxleLy, nlghLmares, Lachy, halluclnauons, u1's, selzures,
arrhyLhmlas, ^8
- ulazepam, Chlordlazepoxlde - long acung benzo's, Lx: Laper wlLhdrawal
- Paloperldol - anu-psychouc, u2 block, Lx: halluclnauons, aggresslon
- nalLrexone - oplold rec anLagonlsL, jreward & cravlng, SL: nausea, ||ver damage
- AcamprosaLe - GA8A ana|ogue, resLores balance of CA8A-CluLamaLe (nMuA), kldney
excreuon, no ||ver tox|c|ty
- ulsulram (AnLabuse) - blocks aldehyde dehydrogenase- ^ushlng, headache, nausea,
confuslon, long durauon (3-4 days), dangerous, n8
MeLhanol & LLhylene Clycol olsonlng
MeLhanol (alcohol dehydrogenase) - formaldehyde -formlc acld - Lhls ls bad
- vlsual dlsLurbances, bradycardla, coma
LLhylene glycol - anufreeze (alc dh) - aldehydes & oxalaLes - also negauve
- meLabollc acldosls
- LLhanol - beuer subsLraLe for alcohol dehydrogenase, j formauon of Loxlc meLabollLes
- lomeplzole - alcohol dehydrogenase lnhlblLor, j formauon of Loxlc meLabollLes
Anndepressants
All buL one acL on 3P1 & nL
AnudepressanL eecL Lakes 2-3 weeks Lo develop
1r|cyc||c Anndepressants
lnh reupLake of 3P1 & nL, also block M, o, and P recepLors, no euphorla, llver meL
SL: sedauon (P block), memory loss (Ach block), analgesla (^nL), card|ac |rr|tab|||ty (Lorsades), o,
block - posLural hypoLenslon, reex Lachy, dry mouLh, welghL galn, se|zure thresho|d, SIADn,
sexua| dysfuncnon, sulcldal Lendencles
urug lnLraxn: MACl's - seroLonln syndrome - hyperpyrexla, selzures, coma, walL 2-3 weeks aer
MACl, SS8l's - ^1CA levels, LoxlclLy, AmpheLamlne - hyperLenslon, Cocalne - arrhyLhmlas
1x: depresslon, panlc auacks, chronlc paln, bromyalgla, neuropaLhlc paln, enuresls
- AmlLrlpLyllne, lmlpramlne - Leruary amlne, more sedaung, - acuve meLabollLe (nor, ues)
- norLrlpLyllne, ueslpramlne - secondary amlne, less sedaung, acuve form
MAC Inh|b|tors
MAC-A breaks down 3P1 & nL and Lyramlne, MAC-8 - breaks down dopamlne, MACl's lrreverslbly
lnhlblL MAC-A & 8, long 1
1/2
, llver meL, 1x: depresslon
SL: orLhosLauc hypoLenslon, welghL galn, o block-dry mouLh, headache, blurred vlslon, sexual
dysfuncuon
Drug Intraxn: 1yramlne ln food (red wlne, beer, cheese) - hyperLenslve crlsls, Sudafed/ AmpheLamlne
- hyperLenslon, SS8l's/ 1CA's/Meperldlne - seroLonln syndrome
- henelzlne (nardll) - MACl
SSkI's
lnh 3P1 reupLake, Lake 2-3 weeks for eecL, mlld SL's
SL: Cl upseL, welghL loss, CnS sumulauon - anxleLy, |nsomn|a, sexual dysfuncuon
urug lnLraxn: MACl's/SL !ohn's WarL - seroLonln syndrome, 1CA's - ^1CA levels, LoxlclLy, Cplolds
(w/ uoxeune) - j oplold eecL
1x: depresslon uCC, panlc uCC, CCu uCC, agoraphobla, bullmla, alcohollsm, klds
- lluoxeune (rozac) - very long 1
1/2
, 3 weeks Lo clear, |nh Cyp2D6
- aroxeune (axll) - lnh Cyp2u6, Lx: CCD, agoraphobla, elderly, SL: sedanon, anorexla
- SerLrallne (Zolo) - more selecuve, shorLer 1
1/2

- ClLalopram (Celexa), LsclLalopram (Lexapro) - faster onset (1-2 weeks), fewer lnLraxns
Cthers
- venlafaxlne (Lexor) - lnh 3P1 & nL reupLake, Lx: depresslon more SL's, ^8
- uuloxeune (CymbalLa) - lnh 3P1 & nL reupLake, Lx: depresslon, neuropath|c pa|n, hepatotox|c
- 8uproplon (WellbuLrln) - lnh uopamlne reupLake, Lx: depresslon, ADnD, smoklng cessauon,
|ess sexua| dysfuncnon, Cl: pLs w/ se|zures or head Lrauma
- MlrLazaplne (8emeron) - blocks o,-^3P1 & nL buL blocks 3P1
2A, 3
recepLors- fewer SS8l
SL's (|ess sexua| dysfuncnon), Lx: depresslon SL: sedanon
- 1razodone - parual agonlsL aL 3P1
1A
& blocks 3P1,, Lx: sleep ald, paln, SL: sedanon, prlaplsm
- SL !ohn's WarL - may block 3P1 & nL reupLake, SL: sun sensluvlLy, 430 lnducer, lnLraxn:
MACl's, SS8l's, 1CA's, l-dopa, ^general anesLheuc eecL
Ann-sychonc Drugs & Mood Stab|||zers
Schlzophrenla - halluclnauons, lack of aecL, apaLhy, deluslons, ^dopamlnerglc acuvlLy
uopamlnerglc sysLem - Nlqtosttlotol - Sn Lo caudaLe/puLamen (parL of sLrlaLum), posLure &
movemenL, j ln acuvlLy - exLrapyramldal sympLoms (arklnson's)
Mesollmblc-Mesocotucol - venLral LegmenLal area (mldbraln) Lo llmblc-nucleus accumbens
(sLrlaLum)/fronLal corLex, reward, emouons, cognluon, ^ acuvlLy - psychosls
lltoltoty - ArcuaLe nuc (hypoLhalamus) Lo anL plLulLary, lnh prolacun secreuon
u2 block for Lx of posluve" sympLoms - deluslons
u4 & 3P1
2A
block for Lx of negauve" sympLoms - apaLhy
LxLrapyramldal sympLoms (L's) - akaLhlsla, dysLonla, Lremor, Lardlve dysklnesla: Lx by brlnglng
dopamlne and Ach acuvlLy lnLo balance, so drugs wlLh more anu-Ach have jL sympLoms
henoth|az|nes
8lock u2, o, P, and anu-Ach eecL
LecL: j fear, jhalluclnauons, janxleLy, anuemeuc
SL: welghL galn, ^prolacun, dry mouLh, orLhosLauc hypoLenslon, sexual dysfuncuon, sedauon,
se|zure thresho|d, neuro|epnc ma||gnant syndrome, L's
- Chlorpromazlne - Lx: schlzo, nausea, manla, halluclnauons, SL: m||d [aund|ce
- 1hlorldazlne - more anu-Ach - L's, ^sedauon, hypoLenslon
- rochlorperazlne (Compazlne) - anuemeuc
- Paloperldol (Paldol) - more selecuve block of u2 w/ some eecL on o and 3P1,, Lx: acuLe
psychosls, SL: many L sympLoms
New Generanon]Atyp|ca| Annpsychoncs
SL: welghL galn, sedauon
- Clozaplne - u2, D4, & Sn1
2A
block, blocks o,, P, and anu-Ach eecL, j L sympLoms, few
prolacun eecLs, SL: agranu|ocytos|s - frequenL blood LesLs requlred
- Cueuaplne - llke Clozaplne buL no agranulocyLosls, jL's, pro|acnn eects
- Clanzaplne - u2, D4, & Sn1
2A
block, anu-Ach eecL, j L sympLoms, 1x: b|po|ar, negauve
sympLoms, SL: 1ype II D|abetes]hyperg|ycem|a
- 8lsperldone - Sn1
2A
, u2, & o block, enhances uA ln basal ganglla j L sympLoms, SL: posLural
hypoLenslon, |ong 1, ^prolacun
- Zlprasldone - llke 8lsperldone, some anndepressant eecL
- Arlplprazole (Ablllfy) -blocks Sn1
2A
, parna| agon|st at D2 & Sn1
1A
, dopamlne sLablllzer",
jL's, jprolacun eecLs, SL: orLhosLauc hypoLenslon, hyperglycemla, esophagea| mon||ty,
sedauon, selzures
Mood Stab|||zers
1x: blpolar dlsorder
- LlLhlum - kldney excreuon, compeLes w/ na for resorpuon, 1hlazldes, nSAlu's, & jna-^
[Ll], SL: nausea, headache, Lremor, jLhyrold funcuon, edema, welghL galn, dlabeLes lnslpldus (Lx
w/ amllorlde), narrow Lherapeuuc range, 1oxlclLy: nausea, Lremor, fasclculauons -confuslon,
aLaxla, selzures, arrhyLhmlas, coma
- valprolc Acld, ulvalproex - anuconvulsanL and mood sLablllzer, rapld onseL, SL: Cl upseL,
welghL galn, ||ver damage
- Carbamazeplne - anuconvulsanL and mood sLablllzer, Lx: neuropaLhlc paln, Cl: pregnancy
- 1oplramaLe - anuconvulsanL, Lx: neuropaLhlc paln
ark|nson's and A|zhe|mer's Drugs
ark|nson's d|sease
nlgrosLrlaLal dopamlnerglc neurons - Sn Lo caudaLe/puLamen (parL of sLrlaLum), degenerauon -
juA (& relauve ^Ach acuvlLy) - arklnson's
uA meLabollsm - Lyroslne - l-dopa (dopa decarboxylase) - dopamlne (MAC-8 & CCM1) -
PvA, uA doesn'L cross 888, l-dopa does cross 888
- L-uopa (Levodopa) - sympLomauc rellef only, greaLly meLabollzed ln Cl and perlphery -
nausea
- Carbldopa/Levodopa (SlnemeL) - carbldopa: lnh dopa decarboxylase, carbldopa does noL cross
888, ^ l-dopa enLry lnLo braln-j dose requlred, jperlpheral eecLs, jeecuveness w/ ume
(3-4 years) due Lo conunued loss of uA neurons, SL: nausea, posLural hypoLenslon, psychosls,
lnsomnla, dysklnesla, on-o", lnLraxn: MACl's - hyperLenslve crlsls, Cl: psychosls, mallgnanL
melanoma
- Seleglllne - lnh MAC-8, j8CS, may s|ow d|sease progress|on,
used w/ l-dopa/carbldopa
- 8romocrlpune - dlrecL uA recepLor agonlsL- eecnveness does not w|th nme, SL: anorexla,
nausea, erythrome|a|g|a - red, Lender, swollen feeL, posLural hypoLenslon, arrhyLhmlas,
dysklnesla, deluslons,
- ramlpexole, 8oplnlrole - uA agonlsL, well LoleraLed, |n|na| tx, j on-o", SL: sudden sleep
- AmanLadlne - anuvlral, may ^ uA release, SL: psychosls, selzures, spomng of skln
- 8enzLroplne (Cogenun) - anu-Ach, resLores uA-Ach balance, j Lremor, j rlgldlLy, llule
eecL on bradyklnesla
CCM1 lnhlblLors - 1olcapone, LnLacapone - ad[uncL Lo levo/carbl
A|zhe|mer's Drugs
Confuslon, memory loss, personallLy changes - anxleLy, dlmculLy recognlzlng famlly/frlends -
loss of speech, appeuLe, bladder conLrol
uegenerauon of chollnerglc neurons - nuc basalls of MeynerL Lo cerebral corLex &
hlppocampus, jAch levels, evenLual j ln nL & 3P1
- Memanune - NMDA antagon|st - prevenLs gluLamaLe neuroLoxlclLy- may slow dlsease
progresslon, SL: aglLauon, lnconunence, lnsomnla, lnLraxn - enhances l-dopa adverse eecLs
cbolloestetose loblbltots
rolong Ach eecL, lmprove sympLoms unul dlsease progresses
- uonepezll (& 1acrlne, 8lvasugmlne, CalanLamlne)
Centra||y Acnng Musc|e ke|axants (Spasmo|yncs)
- 8aclofen - GA8A
8
agonlsL- pre-syn lnhlbluon of exclLaLory n1 release ln braln/splnal cord,
|ntratheca|, jspasuclLy, jpaln, Lx: chronlc spasuclLy, SL: muscle weakness
- ulazepam - enhances CA8A
A
ln splnal cord, relaxes muscle/mlnd, Lx: local muscle Lrauma SL:
sedauon
CNS Depressants
- Cyclobenzaprlne (llexerll) - CnS depressanL, anu-Ach acuvlLy, 1CA llke, Lx: acute spasm, SL:
sedauon, confuslon, halluclnauons, drug of abuse
- Carlsoprodol (Soma) - CnS depressanL, meLabollzed Lo meprobamate (barb. llke), drug of
abuse (soma-coma), Lx: spasuclLy, paln, SL: sedauon
Cthers
- 1lzanldlne - o-2 agonlsL, Lx: chronlc spasuclLy, acuLe spasm, SL: sedanon, hypotens|on
- uanLrolene - jCa release ln muscle (sarc reuculum), Lx: mallgnanL hypoLhermla, neurolepuc
mallgnanL syndrome (anupsychoucs)
- 8oLullnum 1oxln (8oLox) - blocks Ach release, Lx: conLrol local spasm, remove wrlnkles
CNS Snmu|ants
^uA (& nL) levels
LecLs - Low dose: ^8, ^alerLness, jappeuLe, euphorla
Med dose: Lremor, resLlessness, ^resplrauon
Plgh dose: behavloral repeuuon, psychosls
hyslcal dependence, abuse poLenual
- AmpheLamlne (Adderall) - Lx: AuPu, narcolepsy
- MeLhylphenldaLe (8lLalln, ConcerLa) - Lx: AuPu, narcolepsy
- ALomoxeune (SLrauera) - Sn8l, (-)nL reupLake, Lx: AuPu
- Caelne - blocks adenoslne recepLors, (-)uL- ^cAM, L: ^alerLness, ^ gasLrlc acld,
dluresls vaso-C cerebral 8v's- headache rellef, Plgh dose: Lachy, hyperLenslon, lnsomnla
uepresslon AnxleLy Selzures Memory/Learnlng aln
3P1 CA8A nMuA Ach nL
nL 3P1 CA8A nMuA
(uA)
Schlzo arual AgonlsLs - 3P1
1A
uA 8usplrone
Mesocorucal Arlplprazole & u2 (& blocks 3P1,)
1razodone (& blocks 3P1,)
harm 2.2 - Smorgasbord
Genera| Anesthencs
Inha|ed Agents
Mech: nebulous, llkely ^CA8A
A
acuvlLy
SL: resplraLory depresslon, j8, hypoLhermla, nausea, ^lC, Lmergence: ^8, Lachy
-PaloLhane - MAC 0.73, 8lood/Cas 2.34, slow lnducuon/awakenlng, SL: ^caLecholamlne
sensluvlLy, myocardlal depresslon, hepanc necros|s, mallgnanL hyperLhermla
-lsourane - MAC 1.17, 8/C 1.46, common, $$, fasLer, useful ln neurosurgery (j cerebral C,
consumpuon), low LoxlclLy, pungenL odor (no lnducuon), SL: ^nk
-Sevourane - MAC 1.80, 8/C 0.69, rapld lnducuon/awakenlng, leasL lrrlLaung, safest for CV
d|sease (leasL j8)
-uesurane - MAC 6.60, 8/C 0.42, most rap|d, low LoxlclLy, lrrlLaung (no lnducuon), SL: ^nk
-nlLrous Cxlde - MAC 103, 8/C 0.46, rapld, ad[uvanL Lo lncrease raLe of lnducuon w/ oLher
agenLs, ana|ges|a, dluslon hypoxla, auenuates hypotens|on, SL: nausea, 1oxlclLy:
megaloblasuc anemla, perlpheral neuropaLhy, abuse
IV Agents
Mech: ^CA8A
A
acuvlLy
-1blopeotol - barblLuraLe, noL really used anymore, Cl: porphyrla
-Mldazolam (versed) - ulLrashorL acung, sedauon, janxleLy, amnesla, lv, reversed w/ llumazenll
-ropofol - uCC anesLheuc, rapld on/o, jcerebral blood ow- IC SL: resplraLory depresslon,
8 w/ no ^P8, anaphylacuc rxn (eggs, albumln)
-tomlJote - no 8 eecL, SL: nausea
-keLamlne - nMuA anLagonlsL, dlssoclauve eecL, ana|ges|a, llule resp. dep. or nausea, daLe rape
drug, SL: emergence dellrlum ln adulLs
Cp|o|d Ana|ges|cs
-lenLanyl - lv oplold for analgesla, rapld, lolllpops, reversed w/ naloxone (narcan)
Loca| Anesthencs
Mech: block na channels, hlgher amnlLy acuvaLed channels, base form crosses membrane,
lnammauon- jbody pP -^lonlzed drug- jeecL
[8P] / [8] = 10
(pka - pP)
Carbonauon - j lnLracellular pP- ^ lnLracellular drug[ ], vasoconsLrlcLors (Lpl) jdrug dluslon
away from slLe
1oxlclLy: CnS - Longue numb/meLalllc LasLe, aud/vls dlsLurbance, LwlLchlng, convulslons,
Cv - arrhyLhmlas, A8A (esLers) allergy
stets - one l", meLabollzed ln blood by pseudocho||nesterase
-rocalne (novocaln) - shorL axn, A8A lnhlblLs sulfonamldes
-1eLracalne (onLocalne) - slower, longer, sp|na| anesLhesla, w/ 10 dexLrose Lo ^speclc
gravlLy ln CSl
-8enzocalne - top|ca| for sunburn (LooLh - Anbesol), C1C
-Cocalne - shorL axn, Loplcal, blocks nL reupLake, vaso-c, Lachy
AmlJes - Lwo l's", meLabollzed ln ||ver
-Lldocalne (xylocalne) - rapld onseL, lnLermedlaLe durauon, lnlLrauon & epldural,
-8uplvacalne (Marcalne) - |ong durauon, lnlLrauon & epldural, SL: card|otox|c|ty
-8oplvacalne (naropln) - long durauon, S-lsomer (8up ls racemlc), jllpld soluble,
jcardloLoxlc
-Meplvocoloe (Carbocalne) - lnL durauon
-rllocalne (ClLanesL) - SL: methemog|ob|nem|a, Cl: Cv or resplraLory dlsease
Annconvu|sants
Selzures - arual: Slmple - [erklng, ~20 sec, preservauon of consclousness
Complex - lmpalred consclousness <2 mln
Cenerallzed: 1onlc-Clonlc (Crand Mal) - loss of consclousness, muscle conLracuons
Absence (euL Mal) - sLarlng, ~30 sec
Myoclonlc - brlef muscle conLracuon
osslble due Lo jCA8A or ^CluLamaLe (nMuA) acuvlLy
Cl: pregnancy
-henyLoln (ullanun) - prolongs na channel lnacuvauon, 1x: parual & Lonlc-clonlc selzures,
lnduces 4S0, ^ [warfarln], ^oral conLracepuve meLabollsm, dose dependenL ellmlnauon, SL:
g|ng|va| hyperp|as|a, h|rsunsm
-Carbamazeplne - blocks na channels, 1x: parna|(uCC) & Lonlc-clonlc selzures, tr|gem|na|
neura|g|a, blpolar dlsorder, urug lnLraxns, lnduces 430, SL: blood dyscraslas, Cl upseL,
-henobarblLal - prolongs Cl
-
openlng aL CA8A, 8arb|turate, 1x: parual & Lonlc-clonlc
-Cabapenun (neuronun) - CA8A analog buL nebulous mech, 1x: ad[unct for parual & Lonlc-
clonlc selzures, neuropath|c pa|n, blpolar dlsorder, k|dney excreuon
-lteqobollo (lytlco) - Lx: neuropaLhlc paln, bromyalgla
-1opltomote - blocks na, ^CA8A, jgluLamaLe
-LLhosuxlmlde - jCa currenL ln Lhalamus, 1x: absence se|zures(uCC), SL: Cl paln
-valprolc Acld - jrepeuuve rlng, 1x: absence + ton|c-c|on|c(uCC), myoclonlc, blpolar, mlgralne,
SL: hepaLoLoxlclLy, Many drug lnLraxns
-Clonazepam (klonopln) - 1x: absence selzures
-ulazepam (vallum) - 1x: sLaLus epllepucus(uCC)
Stevens-Iohnson Syndrome
PypersensluvlLy auLolmmune (lmmune complex) reacuon, can happen w/ anuconvulsanLs,
Lpldermls separaLes from dermls, 1x: dlsconunue drug
LryLhema muluforme, arLhrlus, nephrlus, CnS abnormallues, myocardlus
Cp|o|d Ana|ges|cs (Narconcs)
CplaLe recepLors - G
|
, close presynapuc Ca channels- jLransmluer release (sub , Ach, nL,
3P1, gluLamaLe), open posLsynapuc k channels ()- hyperpolarlze
Mu () - euphorla, analgesla, sedauon, mlosls, jCl moullLy
kappa (x) - dysphorla, analgesla, mlosls
uelLa () - dysphorla, halluclnauons, mydrlasls
Also lnhlblL CA8A -jlnhlbluon of lnhlblLory paln bers (3 lnhlbluons) -jpaln
Cplold LecLs - analgesla (sensory & aecuve), sedauon, euphorla/dysphorla, anuLusslve,
resplraLory depresslon, ^lC, mlosls, consupauon, anudluresls
1olerance - Plgh: analgesla, euphorla, sedauon, Mlnlmal: mlosls, consupauon
lnLraxns - MACl's: hyperpyrexlc coma, 1x: paln, cough, dlarrhea, anesLhesla, pulmonary edema
Cl: head ln[urles (^lC), pregnancy, pLs w/ lmpalred pulmonary, renal, or hepauc funcuon
Cu: CnS depresslon, j resplrauon, mlosls -mydrlasls (hypoxlc, near deaLh)
WlLhdrawal: dysphorla, dlarrhea, rhlnorrhea, lnsomnla, anxleLy, vomlung, hosullLy, more
prone Lo cerLaln lnfecuons
Strong Agon|sts
-Morphlne - blnds ,k,, exL 1' pass (oral), L
1/2
= 2hrs, Llver meLabollsm 1, Con[ugaLed Lo 3-
glucuronlde -anLagonlzes morphlne & 6- whlch ls more poLenL analgeslc, Schedule ll, Causes
hlsLamlne release- perlpheral vaso-u, j8
-nyJtomotpbooe (ullooJlJ) - morphlne derlvauve, sLronger, fasLer
-Pydrocodone - oral, MeLabollsm: Cyp2D6, lnhlblLors wlll janalgesla (qulnldlne, SS8l's)
-vlcoJlo, lottob, lotcet - hydrocodone/aceLamlnophen
-Cxycodone (CxyConun) - oral, 1x: paln, resLless leg, 1oureue's, Llver meL - Cyp2u6
-letcocet - oxycodone/aceLamlnophen
-Meperldlne (uemerol) - oral/parenLeral, shorL acung, D||ates pup||s, No anntuss|ve,
anumuscarlnlc, blocks 3P1 reupLake, addlcuve, meLabollLe: normeperldlne -anxleLy, selzures,
kldney exc, noL reversed by naloxone, M1 -parklnson's
-MeLhadone - oral/recLal, longer axn, mllder wlLhdrawal, 1x: paln, hero|n addlcLs, w/drawal
-lenLanyl - 100x morphlne, shorLer axn, MeL: Cyp3A4 (lnd/lnh wlll cause lnLraxns),
1x: chronlc paln, lnducuon, anesLhesla (malnLalns cardlac sLablllLy ln surgery, auenuaLes
hemodynamlc response- less j8)
-AlfenLanll - 10x morphlne, shorLer axn Lhan fenLanyl, $$, MeL: Cyp3A4
-5ofeotooll - 1000x morphlne
-Peroln - passes 888, 10x morphlne, meLabollzed Lo morphlne
Moderate Agon|sts
-Codelne - musL be meLabollzed by Cyp2D6 -morphlne (lnh by qulnldlne, SS8l's), 1x: mlld paln,
anuLusslve, low addlcuon poLenual
-1yleool J - codelne/aceLamlnophen
-ropoxyphene - llke codelne, more Loxlc, hlgh dose -se|zure, psychosls
-uotvocet - propoxyphene/aceLamlnophen
M|xed Agon|sts]Antagon|sts
-enLazoclne - agonlsL on x, parna| agon|st on , less eecuve Lhan morphlne, more
halluclnauons
-8uprenorphlne - parna| agon|st on &x, 1x: heroln addlcuon, lv, subllngual, lnLranasal,
subllngual comblned w/ naloxone (noL absorbed sub-L) Lo prevenL lv abuse
-1ramadol - weak agonlsL, lnh reupLake of Sn1 & NL, mlld SL's, 1x: moderaLe paln
Anntuss|ves
-uexLromeLhorphan (8oblLussln) - no analgeslc or addlcuve properues, Cl: MACl's
-Codelne
Antagon|sts
-naloxone (narcan) - lv, shorL axn, can preclplLaLe wlLhdrawal sympLoms
-nalLrexone (8evla) - Cral, long axn, used Lo prevenL Lhe oplaLe hlgh
-Nolmefeoe (kevex) - llke naloxone buL longer axn
Autoco|ds
hosphollpase A, - Lakes membrane phosphollplds - Arachldonlc Acld
CCx-1 - C's, 1x's, consuLuluve, proLecLs gasLrlc mucosa, +plaLeleL aggregauon, vaso-C
CCx-2 - C's, 1x's, lnduclble, +lnammauon, lnh plaLeleL agg, vaso-u
Llpoxygenase - LeukoLrlenes
Cl - vaso-u, broncho-u, ^Cl8, 1x: pulm P1n
CL - vaso-u, broncho-u, ^Cl8, uLerlne conLracuon, 1x: aboruon, lnduce labor, penlle ln[ecuon for
Lu, malnLaln paLenL uA, Cl proLecuon (M|soprosto|)
Cl - broncho-C, uLerlne conLracuon, 1x: glaucoma [LaLanoprosL - (xalaLan)]
1xA - vaso-C, broncho-C
NSAID's
-AceLylsallcyllc Acld (Asplrln) - lrreverslbly lnh CCx-1 & 2, anu-lnammaLory, analgeslc, anupyreuc,
lnh plaLeleLs, kldney exc, lnlual ^resplrauon, Lhen j, low dose -jurlc acld excreuon, hlgh dose
-^urlc acld exc, lnduces asLhma, ^Cl acld, jC's -ulcers, Long Lerm- kldney damage,
8eye's Syndrome - cerebral edema ln klds w/ vlral lnf
Sa||cy|ates
-ulunlsal, 5olsolote - 1x: 8A, CA, paln
CCk-2 Inh|b|tors
-Celecoxlb (Celebrex) - CCx-2 lnh (cox-2:1 lnh 7:1), fewer Cl SL's
-kofecoxlb (vloxx) - CCx-2 lnh (cox-2:1 lnh 70:1), 8lood clomng Cv evenLs, w/drawn
Nonspec|hc CCk Inh|b|tors
-lndomeLhacln - |nh hospho||pase A,, lnh Mn mlgrauon, potent, mosL SL's, 1x: close uA
-ulclofenac - lnh CCx
-ArLhroLec - dlclofenac/mlsoprosLol
-keLorolac - lnh CCx, potent, oral/IV/lM 1x: posL-op paln, use max 3 days (SL's)
-lbuprofen - lnh CCx, analgesla, anupyreuc, anu-lnf, low SL's, ASA eect, 1x: CA, 8A
-naproxen (naprosyn, Aleve) - llke lbuprofen, |ong t
1]2
, Cl: pregnancy
-lroxlcam - j8CS, lnh Mn mlgrauon, long L
1/2
, many SL's
-nabumeLone - long L
1/2
, few SL's
-toJoloc
-xceJtlo - aceLamlnophen/asplrln/caelne
Cther
-AceLamlnophen/araceLamol (1ylenol) - nebulous mech, anupyreuc, analgeslc, no anu-lnf, safe
aL Lherapeuuc doses, 1oxlclLy: hepaLoLoxlclLy (10-13g), hepauc necrosls (23g), Loxlc meLabollLe
exceeds CSP levels, 1oxlclLy 1x: n-aceLylcysLelne (MucomysL)
DMAkD's
uMA8u's Lake weeks Lo monLhs for full eecL
-Metbottexote - lnh dlhydrofolaLe reducLase (uPl8)- junA synLhesls & maybe j1-cell
acuvauon, Cl: pregnancy, llver dlsease
-AuroLhloglucose - oral/parenLeral, gold salLs, lnh phagocyLosls, jC's, jproLeolyuc enzymes
-enlclllamlne - oral, chelaung agenL, 1-ce|| acnv|ty, jlgM 8heumaLold lacLor, lnh collagen
synLhesls, adverse rxns
-Pydroxychloroqulne (laquenll) - oral, anuhlsLamlne, anu-Ach, anuproLease, jC's,
jchemoLaxls, SL: hemolysls ln C6u def
-Sulfasalazlne - oral, maybe lnh CCx & LC, well LoleraLed, 1x: 8A, l8u, SL: Cl upseL
-lnlxlmab (8emlcade) - lv, ch|mer|c lgC agalnsL 1NI-o, 1x 8A w/ meLhoLrexaLe
-8lLuxlmab -lv, chlmerlc lgC agalnsL CD20 (8-ce||), 1x: 8A, non-Podgkln Lymphoma
-Adallmumab (Pumlra) - SC, human lgC agalnsL 1NI-o, MonoLherapy for 8A, SL: rash, u- llke
sympLoms
-LLanercepL (Lnbrel) - lv/SC, 1NI-o receptor fus|on prote|n, blnds and lnacuvaLes 1nl
-AbaLacepL - lv, human recomblnanL fuslon proLeln, b|ocks 1-ce|| acnvanon
-Leunomlde - oral, |nh DnCDn- jpyrlmldlne synLhesls, lnh CCx-2
-MycophenolaLe Mofeul (MMl) - oral/lv, prodrug, |nh IMDn- jlymph purlne synLhesls
-Anaklnra - SC, lL-1 8ecepLor anLagonlsL (IL-1ka), monoLherapy or w/ oLher uMA8u
Drugs for 1he Gout
urugs Cl ln 1he CouL: 1hlazlde & Loop dlureucs, 1rlamLerene, Asplrln, LLoh, more
Drugs for Acute Auacks
-Colchlclne - oral, blnds Lubulln- |nh m|crotubu|es- lnh Mn acuvlLy, jlnf, no analgesla, SL:
d|arrhea, used prophylacucally w/ urlcosurlc agenLs
nSAlu's
-lndomeLhacln, naproxen, Celecoxlb
Cl: asplrln b/c j urlc acld excreuon
Drugs for nyperur|cem|a
6)&4$#7)&4*12-+(#
8lock acuve reabsorpuon of urlc acld ln proxlmal Lubule
SL: kldney sLones (drlnk loLs of waLer), jexcreuon of oLher acldlc compounds
May tr|gger gouty auack (prophylax w/ colchlclne), noL used ln acuLe auacks
-robenecld
-Sulnpyrazone - lnh plaLeleL agg, lnh warfarln meLabollsm
kanth|ne Cx|dase Inh|b|tors
-Allopurlnol - |nh kC: blocks purlnes-hypoxanLhlne-xanLhlne-urlc acld, may Lrlgger gouLy
auack, lnh meLabollsm of warfarln & probenecld
Cther
-8asburlcase - recomb|nant urate ox|dase (noL endogenous ln humans) from Aspetqlllos, urlc
acld- a||anto|n (readlly excreLed), Anaphylaxls on 2 admln posslble
M|gra|ne Drugs
Mlgralne - Lhrobblng, 2-72 hrs, vlsual auras, phoLosensluvlLy, nausea
llrsL phase - lnLracranlal vaso-C, lschemlc changes, prodromlc vlsual aura
Second phase - exLracranlal vaso-u, vasoacuve maLerlal release- paln, lnf
ClusLer - excruclaung paln, around eyes, durlng sleep 13-90 mln
1enslon - sLress onseL, dull, perslsLenL, ughLenlng, 30 mln - 7 days
Symptomanc 1reatment
89.*12$+&#(#
-SumaLrlpLan (lmlLrex) - Sn1
1D&18
agon|st -vaso-C lnLracranlal, oral/SC, SL: vasospasm, sLroke,
lnLracranlal bleedlng, perlpheral lschemla, Cl: Au, CAu, cerebrovascular dlsease, 1x: acute mlgralne
-Notottlptoo, klzottlptoo, lettlptoo, etc.
1+"'2-#&4#
-Asplrln, AceLamlnophen, Codelne, eLc.
:;1<=>#
-naproxen, lbuprofen, eLc.
rophy|ax|s
tqot AlkololJ - ergoL ls a fungus, grows on rye , weL season- Lrgousm (SL. AnLhony's llre): vaso-
C (burnlng), gangrene, halluclnauons
-tqotomloe - parual agonlsL 3P1 & o recepLors, 1x: mlgralne durlng prodrome SL: ergousm
-MeLhyserglde (SanserL) - parual agonlsL on Sn1, weak vaso-C, 1x: mlgralne prophy|ax|s, SL:
reLroperlLoneal brosls
-8lockets - ropanolol
colclom cboooel 8lockets - verapamll
AouJeptessoots - AmlLrlpLyllne, LlLhlum CarbonaLe, valprolc Acld, 1oplramaLe
lemole notmooes - LsLradlol
Drugs of Abuse
-Cocalne
-MeLhampheLamlne
-nlcoune
-Caelne
-Alcohol
-8enzodlazeplnes
-Cplolds
-Marl[uana
-LSu
-Mescallne
-MuMA (LcsLasy)
-hencyclldlne (C, Angel uusL)
-keLamlne (Speclal k)
-lnhaled
Drugs Aecnng Coagu|anon
lnLrlnslc - xll, xl, lx, vlll, 11 ume
LxLrlnslc - 1l, vll, 1 ume, ln8
Common - x, v, ll, l
Collagen - vWl - C1b
Cllb/llla - llbrlnogen
laLeleL acuvauon - Au, 1xA,, 3P1
Anucoagulauon - 1ll, 1hrombomodulln, A1lll
llbrlnolysls - lasmlnogen- lasmln, roLeln C, L-A, uroklnase, sLrepLoklnase
Anncoagu|ants
-Peparln sodlum - lv, acceleraLes A1III axn, ^11 ume, axn prolonged ln renal/hepauc dys
-Lnoxaparln (Lovenox) - LMWP, SC, SL: Pl1, Cl: lnLracranlal hemorrhage, renal/hepauc dlsease,
useful ln pregnancy, doesn'L cross placenLa
-lepltoJlo - dlrecL lnh Lhrombln, leeches, 8enal exc, dlmculL Lo reverse, 1x: Pl1
-Atqottoboo - dlrecL lnh Lhrombln, Llver meL, dlmculL Lo reverse, 1x: Pl1
-Warfarln (Coumadln) - vlL k analog, jll, vll, lx, x, sweeL clover, raL polson, monlLor w/ 1]
INk, lnlual ^c|omng (rapld jproLeln C), LecL Lakes 12-16 hrs Lo develop, 98 plasma proLeln
bound, oral conLracepuves jeecL, Clmeudlne ^eecL
8eversal - vlL k, ll, lacLor lx
Anncoagu|ant keversa| Agents
-roLamlne sulfaLe - heparln anLagonlsL, ln absence of heparln, anucoagulanL eecL
-vlLamln k, - warfarln reversal
I|br|no|ync Agents
-1lssue plasmlnogen acuvaLor (L-A) - acuvaLes plasmlnogen- plasmln, $$
-SLrepLoklnase - brlnolyuc, may cause A8 formauon- a||erg|c response, jemcacy
-utokloose - acuvaLes plasmlnogen- plasmln
-AnlsLreplase - plasmlnogen/sLrepLoklnase
Annhbr|no|ync Agents
-Amlnocaprolc acld - lnh plasmlnogen acuvauon, 1x: bleedlng dlsorders, reverse brlnolyuc
agenLs
Annp|ate|et Agents (Annthromboncs)
-Asplrln - jplaLeleL agg, lrreverslble for llfe of plaLeleL (7-10 days)
-Clopldogrel (lavlx) - oral, lnh AD ln plaLeleL, less Cl SL's Lhan asplrln
-Abclxlmab (8eoro) - lv, |nh GIIb]IIIa, $$
-pufbouJe (lnLegrllln) - lv, lnh Cllb/llla, raule snake venom derlved
-1ltofboo (AggrasLaL) - lv, lnh Cllb/llla
harm 2.3 - GI]Lndocr|ne]D|abetes
Annh|stam|nes
PlsLamlne - lgL lnLraxn, drugs LhaL cause release of P - morphlne, succlnylchollne,
radloconLrasL dyes, venom
P1 - Cq, l,, uAC, vaso-u, broncho-C ^wakefulness & appeuLe, smooLh muscle, endoLhellum, braln
P2 - Cs, ^cAM, ^gasLrlc acld, hearL, braln
Anaphylaxls Lx: eplnephrlne, dlphenhydramlne (ln[ecLed preferably), corucosLerolds
I|rst Generanon n1 Antagon|sts
Sedaung (poLenuaLed by L1CP), anuchollnerglc eecLs (jsecreuons), LoxlclLy: aLroplne llke
polsonlng
- ulphenhydramlne (8enadryl) - hlghly sedaung, Lx: allerglc rhlnlus, mouon slckness,
anuchollnerglc
- romeLhazlne (henergan) - very sedaung, anu-emeuc
- Pydroxyzlne - anuemeuc
- ulmeobyJtloote (utomomloe) - Lx: mouon slckness
- cblotpbeoltomloe - Lx: allerglc rhlnlus
- uoxylomloe (uolsom) - sleep ald
Moderate|y-sedanng Annh|stam|nes
- 8romphenlramlne maleaLe, Chlorphenlramlne maleaLe, clemosuoe, cycllzloe, Mecllzloe
Second Generanon n1 Antagon|sts
non-sedaung - don'L cross 888, no anu-Ach, LoxlclLy: cardlac arrhyLhmlas
- LoraLadlne (Clarlun) - Lx allerglc rhlnlus
- Ceurlzlne (ZyrLec) - Lx allerglc rhlnlus, urucarla, ellmlnaLed by kldney
- lexofenadlne (Allegra) - Lx allerglc rhlnlus
- Actlvosuoe/lseoJoepbeJtloe (5emptex)
Nasa| n1 Antagon|sts
- Azelosuoe - nasal P1 blocker
- levocobosuoe
1reatment of Asthma and CCD
8-Adrenerg|c Agon|sts
- lsoproLerenol - , & , agonlsL, posluve lnoLroplc & chronoLroplc eecLs, vasodllauon, rarely used
-2 Agon|sts - frequenL use -jregulauon of recepLors & jeecuveness, comblnauon w/
corucosLerold can prevenL Lhls
- AlbuLerol - L
1/2
= 4-8 hrs, lnhaled and oral, Lx: acuLe auack
- LevalbuLerol - more bronchodllauon, Lx: acuLe auack
- lrbuLerol (Maxalr) - LoleraLed beuer, can'L be used w/ spacer- dlmculL Lo use ln acuLe auack
- SalmeLerol (SerevenL) - L
1/2
= 12 hrs & slower onseL, 1x: prophylaxls for nocLurnal asLhma,
ALWA?S use w/ corucosLerold
- 5olmetetol/lloucosooe (AJvolt), lotmotetol
Cther 8ronchod||ators
- lpraLroplum (ALrovenL) - muscarlnlc anLagonlsL, quaLernary, uCC CCu, use w/ 82 agonlsL
- 1loLroplum (Splrlva) - llke lpraLroplum, longer axn, once-a-day admlnlsLrauon
- 1heophylllne - blocks adenoslne recepLors, lnh uL, low Lherapeuuc lndex, long-lasung
broncho-u, Smoklng, oral conLracepuves, phenyLoln ^clearance of, Clmeudlne &
eryLhromycln jclearance of, may cause arrhyLhmlas (llke looklng aL a beauuful woman)
Inha|ed Corncostero|ds - decrease alrway lnammauon, SL: Lhrush, hoarseness, jbone
denslLy, jSL w/ use of spacer
- 8eclomeLhasone (8eclovenL)
- llunlsollde (Aero8ld)
- lloucosooe (lloveot), 5olmetetol/lloucosooe (AJvolt), 8oJesoolJe, 1tlomcloolooe (Azmocott)
Leukotr|ene Inh|b|tors - jasLhmauc response Lo exerclse/cold alr, blocks L1 recepLor, musL be Laken
chronlcally, lneecuve for acuLe auack
- MonLelukasL (Slngulalr)
- ZarlukasL - same
- ranlulkasL - same
- ZlleuLon - blocks 3-llpoxygenase -jsynLhesls of L1s, jasLhmauc reacuon Lo asplrln & nSAlus,
Cther
- Cromolyn sodlum - lnhlblLs release of hlsLamlne, chronlc prophylaxls, anu-lnammaLory uCC ln
chlldren
- Cmallzumab - monoclonal anubody LargeLed Lo lgL, subC ln[ecuon every 2-4 weeks
Gastro|ntesnna| Drugs
Ac|d-Neutra||z|ng Agents (Antac|ds)
urug lnLraxn: jbloavallablllLy of phenyLoln, dlglLalls, ^levels of sulfonamldes, L-dopa, valprolc acld,
^ ellmlnauon of sallcylaLes, phenobarblLal
Magneslum - ^gasLrlc moullLy, dlarrhea
Alumlnlum - j gasLrlc moullLy, consupauon
- Calclum carbonaLe (1ums) - can cause Mllk Alkall", noL for pepuc ulcer
- Magneslum/Alumlnum Pydroxlde (Maalox, Cavlscon) - sympLomauc rellef of hearLburn and
gasLrlus
- 5oJlom 8lcotbooote (Alko 5eltzet) - rapld, Lx: hearLburn, noL CL8u or ulcer
n2 Antagon|sts - 1x: uCC pepuc ulcer, CL8u, Z-L syndrome, pre-op
CasLrln, Ach, hlsLamlne (P2) -^gasLrlc acld (parleLal cells)
- Clmeudlne (1agameL) - hlgh doses anu-androgenlc eecL, lnh Cyp3A (jmeL of warfarln,
dlgoxln, phenyLoln, eLc)
- 8anludlne (ZanLac)
- nlzaudlne (Axld)
- lomouJloe (lepclJ)
roton ump Inh|b|tors - lrreverslbly lnhlblL Lhe P/k-A1ase, Lx: uCC CL8u, ulcers, ZLS, Lake
on empLy sLomach, may lncrease rlsk for osLeoporosls (jCa absorpuon)
- Cmeprazole (rllosec) - admlnlsLered lnacuve form, mlnlmal SL
- Lsomeprazole (nexlum)
- 8abeprazole (Aclphex) - llule eecL on hepauc enzymes
- loosoptozole (ltevoclJ), lootoptozole (ltotoolx)
Cytoprotecnve Agents
- SucralfaLe - forms proLecuve barrler ln ulcer craLer, SL: consupauon
- MlsoprosLol - CL1 analog, proLecuve agalnsL nSAlu-lnduced ulcers, Cl: pregnancy
- 8lsmuLh subsallcylaLe - coaLs sLomach, anubacLerlal agalnsL P. pylorl, Cl: ASA allergy
rok|nenc Agents
- 8eLhanechol - muscarlnlc agonlsL, lncrease LLS Lone, does noL geL lnLo CnS
- MeLoclopramlde (8eglan) - u2 recepLor anLagonlsL, ^Ach, ^moullLy & Lone of smooLh muscle, Lx:
gasLroparesls, CL8u anu-emeuc, Cl: pregnancy
Annspasmod|cs - 1reaLmenL of l8S
- ClycopyrrolaLe, ulcyclomlne - anumuscarlnlc, reduce release of gasLrlc acld
- 1egaserod - 3P1, parual agonlsL, Lx: women w/ consupauon, SL: dlarrhea
- AloseLron - blocks 3P1, recepLors, Lx: women w/ severe dlarrhea, SL: consupauon
Laxanves
- llber - bulk, besL way Lo prevenL consupauon and dlverucullus, SL: bloaung and farLs LhaL'll make
you have Lo check your panLs, drlnk plenLy of waLer
- sylllum (MeLamucll) - brous maLerlal from lanLago seeds - hlgh ber!
- Senna (SenokoL) - acLs on colon, eecuve aer abouL 8-10 hours, very mlld
- uocusaLe sodlum - emulslfylng agenL, soens poo
- costot Oll - lnLense laxauve, requlres blle, Cl: pregnancy
- 8lsocoJyl - lnh waLer absorpuon
- Clycetlo - lubrlcaung laxauve
Csmonc Laxanves
- Magneslum hydroxlde (Mllk of Magnesla) - poorly absorbed, pLs w/ poor renal funcuon -Mg
accumulauon
- Sodlum phosphaLe & blsphosphaLe - oral, enema, drlnk loLs of waLer Cl: CPl
- LacLulose - noL absorbed, Lx: jammonla bulldup ln pLs w/ clrrhosls
- olyeLhylene glycol - nasogasLrlc Lube, oral
- 5otbltol & Moooltol - sweeLeners, osmoucally acuve -dlarrhea
Ann-Consnpanon
- LublprosLone - CL1 derlvauve, ^lnLesunal secreuons, soens & ^moullLy, Lake chronlcally
Ann-Gas
- SlmeLhlcone (Cas-x) - coaLs and dlsslpaLes gas from Lhe ass
Annd|arrhea|s
- llbet - absorbs waLer
- Loperamlde (lmodlum) - oplold -jperlsLalsls, no CnS eecLs, Cl: lnfecuous dlarrhea, pLs w/ uC
may -Lo Loxlc megacolon
-ulphenoxylaLe/ALroplne (Lomoul) - oplold w/ CnS eecLs, aLroplne jabuse poLenual, same Cl as
above
-8lsmuLh subsallcylaLe (epLo-8lsmol) - Lx: Lraveler's dlarrhea, Cl: ASA allergy- use blsmuLh clLraLe
lnsLead, also Cl ln klds -8eye's syndrome
- Sulfasalazlne - mlld anu-lnammaLory, Lx: uC, also a uMA8u, Cl: klds (8eye's), sulfa allergy
Introducnon to Lndocr|ne harmaco|ogy
Cyp11A1 - raLe llmlung enzyme for sLerold producuon (cholesLerol -pregnenolone)
rolacun - mllk producuon, lnhlblLed by dopamlne
- 8romocrlpune - dopamlne agonlsL -jprolacun release, Lx: prolacunomas, Cl: pregnancy
- cobetqolloe
Growth normone ke|ated
- SomaLoLropln - SC or lM, SL: hyperglycemla, jlnsulln eecL, Lx: growLh fallure (CP declency,
1urner syndrome), cachexla, Cl: dlabeLes, hypoLhyroldlsm
- SomaLrem
- 5emotello - CP8P agonlsL
- Mecasermln rlnfabaLe - SC Lwlce/day, lCl-1 agonlsL, Lx: pLs unresponslve Lo CP Lherapy
(normally noL as eecuve as CP Lherapy)
- CcLreoude - somaLosLaun analog, $, Lx: CP excess (acromegaly), vloma, carclnold, excesslve
dlarrhea, SL: Cl, gallsLones
- looteouJe
- egvlsomanL - CP recepLor anLagonlsL, Lx: CP excess, Cl: hepauc dlsease
Drugs that Aect 1hyro|d Iuncnon
1hyro|d normone kep|acement
13 - synLheslzed ln Lhyrold, llver converLs 14-13, more acuve, recepLors: unA blndlng
14 - derlved from Lhyrold only, ma[orlLy of Lhyrold secreuon, longer L
1/2

lodlde - conLrols Lhyrold hormone synLhesls
PypoLhyroldlsm - 1: ^1SP(PashlmoLo), 2: 1SP declency- j1SP, 3: 18P declency- j1SP
1x conslderauons: PearL dlsease - ^dose gradually, Adrenal lnsu: corucosLerold replacemenL rsL,
ulabeLes - may ^need for lnsulln
urug lnLraxns - LsLrogen: jLhyrold hormone eecL, Warfarln eecL^ by 1P, eecL w/ CC's?
- LevoLhyroxlne sodlum (SynLhrold) - 14, uCC hypoLhyroldlsm, Lx: PashlmoLo's, golLer, Lhyrold
carclnoma
- LloLhyronlne sodlum - na salL of 13, lnlual Lherapy of myxedema, noL for malnLenance
- llottlx (otbtolJ), 1bytolJ u5l
Inh|b|tors of 1hyro|d normone Synthes|s
PyperLhyroldlsm 1x conslderauons: 8adloacuve lodlne - rlsk of Lhyrold sLorm, surgery, -
blockers, synLhesls lnhlblung drugs
- ropylLhlouracll (1u) - lnhlblL synLhesls of Lhyrold hormone, j14 -13, Lx: uCC Crave's, uCC
ln pregnancy, SL: lLchlng, granulocyLopenla/agranulocyLosls heralded by a sore LhroaL
- MeLhylLhlouracll, MeLhlmazole - more poLenL and longer-acung, does noL j14 -13
- lodldes - j ln release of Lhyrold hormone, used prlor Lo Lhyrold sx, Lx: prevenL radloacuve lodlne
upLake ln evenL of an accldenL
- 8adloacuve lodlne (l'') - low dose- dlagnosuc, hlgh dose- Lhyrold ablauon, Lx:
hyperLhyroldlsm ln elderly and pLs w/ hearL dlsease
- ropranolol - j slgns/sympLoms of hyperLhyroldlsm, Cl: asLhma, dlabeLes, use CC8 when Cl
Csteoporos|s Drugs
- CalclLonln - lnLranasal or ln[ecLed, salmon calclLonln, jback paln, SL: anaphylaxls
- 1erlparaude - r1P, SC admln, Lx: osLeoporosls, hypoparaLhyroldlsm, SL: hypercalcemla/urla
- AlendronaLe (losamax) - blsphosphonaLe, josLeoclasuc acuvlLy, Lx: osLeoporosls, Lake w/ouL food,
Ca, or Mg, Laken orally buL absorpuon ls poor, once/week, sLand/slL uprlghL for aL leasL 30 mln
aer Laklng, SL: esophaglus
- uJtooote, lomlJtooote - ooo-otol, klseJtooote (Actooel), 1lloJtooote
Sex normones and Gonadotrop|ns
SLerold recepLor - ln nucleus, alLer gene Lranscrlpuon, slow process
Gonadotrop|n ke|ated
- Conadorelln - shorL acung Cn8P agonlsL, pulsed lv, ^lSP & LP producuon, Lx: lnferullLy,
dlagnosuc for hypogonadoLroplc hypogonadlsm
- Leuprollde - long acung Cn8P agonlsL, conunuous admlnlsLrauon- jregulauon recepLors-
jgonadoLropln release, Lx: prosLaLe CA (w/ lluLamlde), endomeLrlosls, precoclous puberLy, SL:
menopausal sympLoms, Lesucular aLrophy, Cl: pregnancy, breasL-feedlng
- Coserelln, Nofotello - same-lsh
- CeLrorellx, Cooltellx - Cn8P anLagonlsL, ln[ecLed SC by pL, jLP & lSP for lvl
Gonadotrop|n M|xtures (lSP & LP) - Lx: lnferullLy ln women w/ funcuonal ovarles
SL: ovarlan enlargemenL, ovarlan hypersumulauon syndrome, muluple blrLhs, gynecomasua
lemale lnferullLy - hMC (lSP) unul esLradlol levels are normal, Lhen hCC
Male lnferullLy - hCC Lo ^LesLosLerone, Lhen hMC for several monLhs
- hMC, MenoLroplns (Puman menopausal gonadoLropln) - lSP & LP, prepares folllcle for
ovulauon
- hCC - LP agonlsL, lnduces ovulauon
- lolllttoplo olfo, beto - tl5n, cbotloqoooJottoplo olfo - tbcC, lottoplo - tln
Lstrogens
- LLhlnyl esLradlol - synLheuc esLrogen, used ln oral conLracepuve
- MesLranol - same
- LsLradlol
- Con[ugaLed esLrogens - used for P81
- LsLerled esLrogens - same
- uleLhylsulbesLrol - non-sLerold w/ esLrogenlc acuvlLy, Lx: prlmary hypogonadlsm, P81, SL:
mlgralnes, P1n, Lhromboembollsm, Cl: esLrogen dependenL breasL CA
Annestrogens
- 1amoxlfen - SL8M (selecuve esLrogen recepLor modulaLor), agonlsL ln uLerus & bone, anLagonlsL ln
breasL, Lx: esLrogen-dependenL breasL CA (for 3 yrs), SL: ^rlsk uLerlne CA
- 8aloxlfene - SL8M, agonlsL ln bone, anLagonlsL ln breasL & uLerus and llver, Lx: osLeoporosls
- Clomlphene - SL8M, anLagonlsL ln hypoLhalamus, agonlsL elsewhere, Lx: lnferullLy- sumulaLes
secreuon of LP & lSP, SL: muluple pregnancles
- lolvesttoot - pure esLrogen recepLor anLagonlsL, Lx: 1amoxlfen-reslsLanL Lumors
- AnasLrozole, lettozole - nonsLeroldal aromaLase lnhlblLor, Lx: advanced breasL CA ln
posLmenopausal women unresponslve Lo 1amoxlfen
- xemestooe - same buL sLerold
rogesnns - Lx: oral conLracepuves, prevenuon of endomeLrlal hyperplasla
- rogesLerone - pregnane, androgenlc acuvlLy, lnh mlneralocorucold recepLor
- MedroxyprogesLerone (uepo-rovera) - same, slow absorblng depoL ln[ecuon, progesun only
conLracepuon
- noreLhlndrone - esLrane, progesun & androgenlc acuvlLy
- norgesLrel - gonanes, no androgenlc acuvlLy
- levoootqesttel (lloo 8) - mornlng aer plll, no 8
x
requlred for pLs over 18
Annprogesnns
- MlfeprlsLone (8u 486) - blocks progesLerone & glucocorucold recepLor, pregnancy Lermlnauon
- uanazol - suppresses ovarlan funcuon, Lx: endomeLrlosls
Contracepnon - progesun/esLrogen
SL: welghL galn, edema, depresslon, mld-cycle bleedlng (low dose or progesun only pllls),
^coagulablllLy, jeecL of anucoagulanLs, LeraLogenlc
Cl: Lhromboembollc phenomena, esLrogen dependenL CA, adolescenLs (esLrogen closes eplphyseal
plaLe- sLunLed growLh, may use progesun only preparauons)
8eneLs: no bables, jrlsk ovarlan/endomeLrlal cancer, jacne
- urosplrenone/eLhlnyl esLradlol (?az) - no LP surge- lnh ovulauon, j lmplanLauon, j waLer
reLenuon, only plll approved for reduclng Muu sympLoms
- MedroxyprogesLerone (uepo-rovera) - progesun only, see above
- toooqesttel/etbloyl esttoJlol (Novokloq) - vaglnal rlng, 3 weeks supply
- toooqesttel (lmploooo) - progesun only, lmplanLed ln arm every 3 monLhs
- Mlteoo - levonorgesLrel luC (lnLra-uLerlne) for 3 years
Pormone 8eplacemenL 1herapy (P81)
osL-hysLerecLomy - esLrogen only
8eneLs - josLeoporosls, breasL CA regresslon, endomeLrlal CA reg., prosLaLe CA reg.
Concerns - ^Ml, ^breasL CA, ^uLerlne CA, ^gallbladder dlsease
Androgens
1x: Lesucular declency, female hypoplLulLarlsm ad[uncL, hypoproLelnemla of nephrosls, negauve
nlLrogen balance
SL: jLesLosLerone producuon, mascullnlzauon, olly skln, decreased PuL, 8Clu 8ACL!!!
- 1esLosLerone - 1:1 androgenlc:anabollc acuvlLy
- MeLhylLesLosLerone - 1:1
- llooxymestetooe - 1.2, NooJtolooe, 5tooozolol - 1.J to 1.6
Ann-Androgens
- lluLamlde - androgen recepLor anLagonlsL, Lx: prosLaLe CA (co-admlnlsLer w/ Leuprollde), Loplcally
for hlrsuusm & male pauern baldness, SL: jllbldo, reverslble hepaLoLoxlclLy
- 8lcolotomlJe, NllotomlJe - same
- llnasLerlde (ropecla) - 3o-reducLase lnhlblLor- juP1, ^LesLosLerone, no eecL on llbldo, Lx:
8P, male pauern baldness, SL: LeraLogenlc
- uuLasLerlde - same
- 5pltoooloctooe - k sparlng dlureuc w/ anu-androgen eecLs (used ln sex changes for male Lo female
Lransformauon, llke kevln's mom)
AC1n and Adrena| Stero|ds
SLerold recepLor - ln nucleus, alLer gene Lranscrlpuon, slow process
kep|acement - admlnlsLer AC1P Lo deLermlne of lnsumclency ls prlmary or secondary, ln pLs w/
adrenal lnsumclency glve large amounLs of glucocorucolds ln umes of surgery/lnfecuon Cl (relauve):
sysLemlc bacLerlal lnf, dlabeLes, osLeoporosls, hearL dlsease, Lhere are no Cl's for CC Lherapy ln pLs w/
adrenocorucal lnsumclency
SL: long Lerm dally CC Lherapy- jPA axls, adrenal aLrophy, adrenal lnsu w/ abrupL sLop of Lx,
cenLral obeslLy, hyperglycemla, osLeoporosls, caLaracLs, edema, muscle wasung, lnsomnla, Lhlnnlng of
skln, pepuc ulcer
- Pydrocorusone - aka Corusol, MC = CC properues, uCC for replacemenL Lherapy ln pLs w/ adrenal
lnsumclency, shorL acung
- Corusone - MC = CC, 80 sLrengLh of hydrocorusone, shorL acung
- lludrocorusone - MC > CC properues, Lx: 81 ln adrenocorucal lnsumclency
Ann-|nammatory - Lx: 8A sympLoms, asLhma, rhlnlus, allergles
- rednlsone - CC > MC, converLed Lo prednlsolone ln Lhe llver- acuve, lnLermedlaLe durauon of
axn, oral for sever asLhma
- rednlsolone - same buL acuve
- MeLhylprednlsolone, 1tlomcloolooe (keooloq) - CC acuvlLy only, no salL reLenuon, hlgher anu-
lnammaLory eecL, lnLermedlaLe durauon
- uexameLhasone - preferred CC for cerebral edema, measure endogenous corusol levels, very hlgh
anu-lnammaLory, no salL reLenuon, long axn, Lx: 8A
- 8eclomeLhasone (8eclovenL), lluucasone (llovenL) - CC for lnhaled or lnLranasal use, Lx: asLhma,
rhlnlus
Corncostero|d Antagon|sts or Synthes|s Inh|b|tors
- AmlnogluLeLhlmlde - lnh cholesLerol- pregnenolone- jadrenal sLerold synLhesls, Lx: Cushlng's
syndrome, meLasLauc breasL and prosLaLe CA, ALWA?S Lx w/ concomlLanL corucosLerold Lo jAC1P
release, SL: skln rash, agranulocyLosls
- keLoconazole - orally anufungal, lnhlblLs sLerold synLhesls, very hlgh doses used ln pauenLs w/
Cushlng's prlor Lo sx or radlauon, mosL eecuve lnhlblLor
- MeLyrapone - lnh Cyp1181, Lx: shorL Lerm managemenL of Cushlng's & for LesLs of adrenal funcuon,
only drug LhaL can be glven ln pregnancy
- MlLoLane - adrenocorucolyuc, selecuve aLrophy of zona fasclculaLa & reucularls, Lx: prlmary adrenal
carclnoma, SL: severe Cl dlsLress
- MlfeprlsLone - aL hlgh dose anLagonlzes glucocorucold recepLors, Lx: lnoperable pauenLs w/ ecLoplc
AC1P secreuon or adrenal carclnoma
- SplronolacLone - k sparlng dlureuc, aldosLerone anLagonlsL, Lx: prlmary hyperaldosLeronlsm,
hlrsuusm, asclLes
Annd|abenc Drugs & Insu||ns
U|tra-short-acnng |nsu||ns
- lnsulln llspro (Pumalog)
- lnsulln asparL
- lnsulln glullslne
Short-acnng |nsu||ns
- 8egular novolln 8
- 8egular Pumulln
- velosulln 88
Intermed|ate-acnng |nsu||ns
- LenLe Pumulln
- LenLe
- nP Pumulln
- nP
rem|xed |nsu||ns
- novolln 70/30
- Pumulln 70/30 and 30/30
- 30/30 nL, Llspro
- 70/23 nL, Llspro
- 70/30 nP, AsparL
Long-acnng |nsu||ns - provlde basal level of lnsulln LhroughouL Lhe day
- ulLralenLe Pumulln u
- lnsulln glarglne
- lnsulln deLemlr
ukA 1x: regular lnsulln, dexLrose, ulds
SL of lnsulln Lherapy: hypoglycemla (mosL common), local rxn, llpodysLrophy
lnLraxns: excess CP & corucosLerold anLagonlze lnsulln
Su|fony|ureas - sumulaLe lnsulln release, SL: hyperlnsullnemla, hypoglycemla, welghL galn,
Cl: sulfa allergy
- 1olbuLamlde - rapld absorpuon, 1
1/2
=4-3 hours, safesL ln elderly
- Chlorpropamlde (ulablnese) - 1
1/2
= 32 hours, dlsulram-llke eecL (lnhlblL aceLaldehyde
dehydrogenase)
- 1olozomlJe, AcetobexomlJe
- Clyburlde - eecL lasLs 24 hours
- Cllplzlde - 1
1/2
= 2-4 hours
- Cllmeplrlde - once a day admlnlsLrauon, llule hypoglycemlc eecL
Meg||nn|des - ^lnsulln release, SL: hyperlnsullnemla, hypoglycemla, more rapld & shorL acung
Lhan sulfonylureas, may be used ln sulfa allergy class C pregnancy
- 8epagllnlde
- naLegllnlde
8|guan|des
- Meuormln - uCC 1ype ll uM, slows glucose absorpuon, jgluconeogenesls, beneclal llpld prole,
jmacrovascular evenLs, no welghL galn, safe for use ln klds > 10, renal ellmlnauon, SL: lacuc acldosls
(rare), dlarrhea, Cl: pregnancy, ussue hypoxlc sLaLes (eg. CPl, CCu)
1h|azo||d|ned|ones - lnsulln sensluzers, A8 recepLor llgands, no Cl sympLoms, ^PuL, j1C,
jdevelopmenL of 1ype ll uM, SL: welghL galn, edema, cauuon ln pLs w/ CPl, hepauc dlsease,
pregnancy
- 8oslgllLazone (Avandla) - black label warnlng - 2x lncrease of Ml and anglna
- logllLazone (AcLos)
A|pha-g|ucos|dase Inh|b|tors - lnh carb dlgesuon/absorpuon, j1C, SL: Cl
- Acarbose
- MlgllLol
GL-1 Ana|ogue
- Lxenaude - SC admlnlsLrauon, u-lv reslsLanL, promoLes glycemlc conLrol, slows gasLrlc empLylng,
welghL loss, renal ellmlnauon
D-IV Inh|b|tors
- SlLagllpun - poLenuaLes eecL of lncreuns, no Cl sympLoms, renal ellmlnauon,
Amy||n-||ke pepnde
- ramllnude (Symlln) - SC admlnlsLrauon, analog of amylln, regulaLes posLprandlal glucose, delays
gasLrlc empLylng, decrease glucagon secreuon, welghL loss, used ln 1ype 1 & 2, renal ellmlnauon,
pregnancy class C
nyperg|ycem|c Agents
- Clucagon - parenLeral admlnlsLrauon, moblllzes hepauc glycogen, poLenL lnoLroplc & chronoLroplc
eecLs, Lherefore used ln -blocker Cu
- ulazoxlde - oral admlnlsLrauon, lnhlblLs lnsulln secreuon, Lx lnsullnoma, (vasodllaLor)
Cxytoc|cs (uLerlne sumulanLs)
- CxyLocln - lv, lM, nasal admlnlsLrauon, clrculaLes as free pepude, Lx: lnduce labor, prevenL
hemorrhage, mllk leL-down, SL: waLer lnLoxlcauon, uLerlne rupLure, allergy, anaphylaxls, feLal
bradycardla
Lrgot A|ka|o|d
- Lrgonovlne MaleaLe - +conLracuon of uLerlne muscle- jbleedlng, uC nC1 use Lo lnduce labor,
Cl: hepauc, renal, and obllLerauve vascular dlsease
- Metbyletqooovloe Moleote
rostag|and|ns
- ulnoprosLone - CL2 analog, vaglnal supposlLory, Lx: aboruon, posL-aboruon expulslon, SL: Cl w/
vomlung & dlarrhea
- cotboptost 1tometbomloe - lCl-2, loJoce obotuoo
- ulooptost 1tometbomloe - lojecteJ loto omolouc soc, loJoce obotuoo
1oco|yncs (uLerlne relaxanLs)
-2 Agon|sts
- 8lLodrlne - lnhlblLs uLerlne conLracuons, delay premaLure labor
- 1erbuLallne - same
Cther Agents
- Alcohol - lv, lnhlblLs uLerlne conLracuon
- Magneslum sulfaLe - lv, lnhlblLs uLerlne conLracuon, use ln pre-eclampuc pLs
- lndomeLhacln - causes parual closure of uA ln uLero, lnvesugauve Lo delay preLerm labor
- ALoslban - oxyLocln anLagonlsL, sull lnvesugauonal
- PydroxyprogesLerone CaproaLe - prophylacuc Lx of premaLure dellvery (16-37' week)
- Calclum channel blockers - second-llne Lx of premaLure dellvery
- nlLroglycerln - lv, emergency use only, very shorL acung
harm 3.1 - 1he Cancer, Worms, and V|r||
Annneop|asnc Agents
A|ky|anng Agents - alkylaLe unA- lneecuve unA, mosL Loxlc Lo rapldly dlvldlng cells, SL:
veslcanL, nausea, myelosuppresslon, sLerlllLy, LeraLogenlc
- MechloreLhamlne - Lx: Podgkln's MC (mechloreLhamlne, oncovln, procarbazlne, prednlsone),
SL: hyperurlcemla (Lx w/ allopurlnol)
- Cyclophosphamlde - Lx broad specLrum, lncludlng non-Podgkln's and 8urklu's, mosL carclnomas,
SL: hemorrhaglc cysuus (acroleln ln bladder, Lx w/ MLSnA), SlAuP
- lfosfomlJe - llke cyclopbospbomlJe
- cblotombocll - slowest ocuoq, tx cll
- 1blotepo - tx bloJJet cA
- 8usulfan - Lx CML, SL: hyperurlcemla
- Carmusune - hlghly llpld soluble, Lx braln CA
- lomosuoe - JeloyeJ myelosopptessloo, slmllot to cotmosuoe
- 5tteptozoclo - selecuve fot poocteouc cA (lottlck 5woyze)
- uocotbozloe - uNA ctossllokloq, tx noJqklos
- Clsplaun - Lx advanced Lesucular CA & many solld Lumors, oen comblned w/ oLher drugs, SL:
nephroLoxlclLy, unnlLus (acousuc nerve damage), anaphylaxls
Annmetabo||tes
- MeLhoLrexaLe - lnh dlhydrofolaLe reducLase, Lx ALL, chorlocarclnoma, SL: renal preclplLauon (ppL),
hepaLoLoxlclLy, pulmonary lnlLraLes, LeraLogenlc
- leocovotlo (follolc oclJ) - teJoces toxlclty/tevetses metbottexote, eobooces tespoose of footootocll
ur|ne Ana|ogs - lnh unA/8nA synLhesls, converslon by PC81 requlred, SL: myelosuppresslon
- MercapLopurlne -xC meL, blocked by allopurlnol, Lx: leukemlas, SL: hyperurlcemla
- 6-1bloqoooloe - some bot oot metobollzeJ by \O, so oo ollopotlool e[ect, tx. AMl
- cloJtlbloe
- lloJotobloe
- leotostouo
yr|m|d|ne Ana|ogs
- lluorouracll (3-lu) - blnds LhymldylaLe synLhase, lnh 8LS of unA synLhesls, leucovorln ^ eecL, Lx:
colorecLal CA, Loplcal admlnlsLrauon for basal cell CA
- copecltobloe - oral prodrug - 3-lu ln Lumor cells, Lx meLasLauc breasL CA, colorecLal, no alopecla
and myelosuppresslon uncommon
- cytotobloe - tx AMl, 5. sevete leokopeolo
- nyJtoxyoteo - tx cbtoolc qtooolocyuc leokemlo (ooJ slckle cell), 5. bypetplqmeotouoo (toJlouoo
tecoll)
Annb|oncs
Anthracyc||nes - lnh unA/8nA, generaLes 8CS (^ 8CS w/ le), SL: cardloLoxlclLy (decreased w/
le chelaLors), reslsLance due Lo -glycoproLeln
- uaunorublcln PCl - Lx non-lymphoblasuc leukemla, SL: red urlne (fun aL parues)
- uoxorublcln PCl - Lx lymphoma, breasL & Lhyrold CAs & sarcomas
- lJotoblclo - less cotJlotoxlc
- Mltoxoottooe
- voltoblclo - losulleJ loto bloJJet (oll otbets ote lv)
Cthers
- 8leomycln SulfaLe - unA fragmenLauon, Lx Lesucular and ovarlan CA, llule myelosuppresslon, SL:
pulmonary brosls, anaphylaxls
- uacunomycln - blnds dsunA, Lx: Wllm's Lumor, rhabdomyosarcoma, chorlocarclnoma (w/
meLhoLrexaLe), SL: radlauon recall
|ant A|ka|o|ds
- vlncrlsune (Cncovln) - blnds Lubulln, Lx: MC reglmen for Podgkln's, acuLe leukemla ln chlldren,
llule myelosuppresslon, SL: neuroLoxlclLy, perlpheral neuropaLhy
- vlnblasune - blnds Lubulln, Lx: Lesucular CA, SL: hlgh myelosuppresslon
- vlootelbloe
- acllLaxel - blnds (mlcro-)Lubulln- arresL mlLosls, Lx: breasL & ovarlan CA, hlghly Loxlc so lasL-dlLch
eorL, SL: myelosuppresslon, perlpheral neuropaLhy, myalgla and arLhralgla
- toposlJe - Jooble sttooJ bteokoqe of uNA, tx tesucolot cA
- 1opotecoo
ozymes
- Aspotoqloose
8|o|og|ca| kesponse Mod|hers
- lnLerferon-alfa - Lx halry cell leukemla, kaposl's sarcoma, and condylomaLa acumlnaLa, SL: u-llke
syndrome, depresslon (sulcldal), alopecla
- lnLerleukln 2 - Lx advanced mallgnanL melanoma & renal cell carclnoma
normones and Antagon|sts
- rednlsone - suppress mlLosls ln lymphocyLes, Lx leukemla & lymphoma ln adulLs
- 1amoxlfen - esLrogen anLagonlsL ln breasL, prevenuon of breasL CA ln women w/ prevlous hx, ^rlsk
uLerlne CA
- 1rasLuzumab - ab agalnsL PL82 proLeln, Lx meLasLauc breasL CA, SL: cardlomyopaLhy (don'L use w/
daunorublcln or doxorublcln)
- lluLamlde - blocks androgen recepLors, Lx meLasLauc prosLaLe CA
- Cosetello, leoptollJe - Jecteose teleose of ln, l5n, tx ptostote cA w/ fotomlJe
Immunosuppress|ves and Immunomodu|ators
Corncostero|ds
- rednlsone
1-ce|| Suppressants
- Cyclosporlne - lnh. 1-cell acuvauon w/ouL causlng myelosuppresslon, meLabollzed by C?3A, used
Lo prevenL re[ecuon ln organ LransplanL pauenLs, preparauons Sandlmmune and neoral dler & are
noL lnLerchangeable, SL: P1n, renal LoxlclLy
- 1acrollmus - lnh. funcuon of calclneurln and 1-cell acuvauon, uCC LransplanL re[ecuon, rescue"
durlng re[ecuon eplsode, C?3A meL, SL: P1n, nephroLoxlclLy, hyperglycemla, neuroLoxlclLy, ^rlsk of
skln cancer - all less poLenL Lhan w/ cyclosporlne, grapefrulL [ulce musL noL be consumed!!
- 5ltollmos - me too!
- llmectollmos - me too!
Cytotox|c Agents
- AzaLhloprlne - converLed lo vlvo Lo 6-mercapLopurlne, prevenLs re[ecuon and Lx severe 8A, SL:
myelosuppresslon, LeraLogenlc, meLabollzed by xC - ln pauenLs LreaLed w/ allopurlnol, Lhe dose musL
be reduced slgnlcanLly
- lefooomlJe
- Cyclophosphamlde - organ LransplanL rescue" and bone marrow LransplanL, SL: hemorrhaglc
cysuus, myelosuppresslon, bladder brosls and CA
- Metbottexote - lob. JlbyJtofolote teJoctose, otqoo ttoosploots ooJ tx psotlosls ooJ kA, 5.
myelosopptessloo, tetotoqeolc
- 1bollJomlJe - sopptesses 1Nl-o, pteveouoo of Cvsn lo 8M ttoosploot, pteqooocy ?1.@ABCD*E
Drugs 1argenng keceptors
- MycophenolaLe Mofeul - lnh. lnoslne monophosphaLe dehydrogenase (Je oovo purlne synLhesls ln
1&8 cells), comblned w/ cyclosporlne or Lacrollmus and glucocorucolds Lo prevenL re[ecuon, SL:
^lnfecuons, skln rash
Annbody Suppressants
- Muromonab-Cu3 - mousey ab Lo Lhe 13 (Cu3) slLe on 1-lymphs, Cu3+ cells ln clrculauon removed
mlnuLes aer lv admlnlsLrauon, musL be glven parenLerally, ln[ecLed 10-14 days, acuLe LransplanL
re[ecuon, SL: cyLoklne release syndrome (u-llke response, shock)
- uacllzumab - humanlzed monoclonal ab LhaL block lL-2 recepLor, lnducuon agenL for LransplanLs,
does noL cause cyLoklne release syndrome, few SL
- 8aslllxlmab - very slmllar buL lL's spelled dlerenLly
- LymphocyLe lmmune Clobulln - lgC fracuons Lo 1-cells prepared from horsles or bunnles,
admlnlsLered w/ corucosLerolds, Lx: acuLe re[ecuon eplsodes, lnducuon for renal LransplanL (lnsLead
of nephroLoxlc cyclosporlne/Lacrollmus), SL: allerglc response (responds Lo corucosLerold Lx),
anaphylaxls - skln LesL for sensluvlLy
Immunomodu|ators and Immunosnmu|ants
lnLerferons: SL: depresslon (sulclde), u-llke sympLoms, ^1C's, ^AL1
- lmmune Clobulln -
- lnLerferon alfa-2b - Lx chronlc Pep 8 and C, comblne w/ oral rlbavlrln
- lnLerferon alfa-2a - Lx Pep C, halry cell CA, kaposl's sarcoma, condylomaLa acumlnaLa
- lotetfetoo olfo-oJ - tx cooJylomoto ocomlooto
- lotetfetoo beto-1b - sometbloq oboot moluple scletosls
- lotetfetoo qommo-1b - mote poteot lmmooosumoloot tbot olfo ooJ beto lotetfetoos
- lnLerleukln-2 - Lx meLasLauc renal cell CA, mallgnanL melanoma, musL be admlnlsLered ln hosplLal,
SL: severe hypoLenslon, pulmonary edema and dyspnea
- C-CSl - Lx neuLropenla due Lo CA chemoLherapy, SL: bone paln - use 1ylenol Lo Lx Lhls
- Optelveklo (tb ll-11, Neomeqo) - rec lL-11, Lx: prevenL LhrombocyLopenla, SL: uld reLenuon
Annma|ar|a| Chemotherapy
8|ood Sch|zonnc|des
- Chloroqulne - acLs on eryLhrocyuc forms, no eecL on secondary ussue forms, prophylaxls for all
sensluve forms, long half llfe, long durauon of acuon, less Loxlc Lhan qulnlne, SL: dlzzlness, headache,
unnlLus, reunal and corneal LoxlclLy, Cl: porphyrla & psorlasls
- Culnlne/Culnldlne - class l anuarrhyLhmlc, uCC unconsclous pauenL lnfecLed w/ chloroqulne-
reslsLanL l. vlvox and l. folclpotom, comblned w/ doxycycllne, SL: clnchonlsm
- uoxycycllne - ad[uncL Lo qulnlne
- Meoqulne - uCC prophylaxls chloroqulne-reslsLanL l. folclpotom, SL: Cl upseL, myocardlal
depresslon, selzures, Cl: hx menLal lllness or epllepsy
- 5olfoJoxloe - lnh A8A lncorporauon lnLo follc acld
- lytlmetbomloe, ltoqoooll, 1tlmetboptlm - lnh dlhydrofolaLe reducLase (dl- - LeLra-hydrofollc acld)
- yrlmeLhamlne + sulfadoxlne - used for presumpuve Lx
- ALovaquone + proguanll (Malarone) - besL Lx for uncompllcaLed lnfecuon w/ chloroqulne-reslsLanL
malarla, also approved Lo Lx l. jltovecl (cotloll) ln pauenLs unable Lo LoleraLe 1MSMx, SL: Cl, may
^llver enzymes
- nolofoottloe
- Attemlslolo, Attesooote, Attemetbet
1|ssue Sch|zonnc|de
- rlmaqulne - acuve agalnsL ussue forms of all specles of plasmodla, Lx: follow up Lherapy Lo klll
secondary forms of l. vlvox ooJ l. ovole, noL used for prophylaxls b/c poLenual LoxlclLy even Lhough lL
can prevenL Lhe lnlual developmenL of paraslLe ln Lhe llver, SL: hemolyuc anemla ln pauenLs w/ C6u
declency, LeraLogenlc - walL unul baby ls born Lo admlnlsLer
Annprotozoa| Drugs
- MeLronldazole - uCC . blstolyuco, C. lombllo, 1. voqloolls, also for Lx 8. ftoqllls, c. Jl[clle, &
CotJoetello, SL: Cl lrrlLauon, meLalllc LasLe, dlsulram-llke lnLeracuon, red urlne
- 1lolJozole
- ulloxoolJe fotoote
- lodoqulnol - Lx . blstolyuco
- aromomycln - Lx . blstolyuco, 1. voqloolls
- meuoe ooJ uebyJtoemeuoe
- cblotopoloe
- Culnacrlne - anumalarlal drug LhaL ls eecuve agalnsL C. lombllo
- lotozollJooe
- 1rlmeLhoprlm/SulfameLhoxazole (+ follnlc acld) - uCC Lx pneumocysLosls, recommended
prophylaxls agalnsL l. jltovecl (cotloll) ln AluS pauenLs
- 1tlmettexote
- leotomlJloe
- ALovaquone - Lx pneumocysLosls ln pauenLs who don'L LoleraLe 1M/SMx
- yrlmeLhamlne plus Sulfadlazlne plus follnlc acld - uCC Loxoplasmosls, comblne w/ leucovorln Lo
reduce LoxlclLy
Annhe|m|nnc Drugs
- Mebendazole - blnds Lubulln, uCC roundworm (A. lombtlcolJes), whlpworm (1. ttlcbloto),
hookworm (N. ometlcooos), and plnworm (. vetmlcolotls), may also be eecuve agalnsL Lapeworms,
Loplcally agalnsL cuLaneous lotvo mlqtoos, SL: Cl, LeraLogenlc
- yranLel pamoaLe - C1C, broad-specLrum agalnsL nemaLodes (roundworm, plnworm, and
hookworm), chollnesLerase lnhlblLor (worm nM! more sensluve Lhan human)
- 1blobeoJozole - totely oseJ except fot tbteoJwotm (sttooqylolJlosls)
- nlclosamlde - uCC agalnsL lnLesunal Lapeworms (1. soqlooto, 1. sollom, u. lotom, n. oooo), lf Lx 1.
sollom, use concomlLanL laxauve Lo reduce rlsk of cysucercosls, noL eecuve Lx of cysucercosls - use
prazlquanLel
- razlquanLel - uCC all specles schlsLosomes, neurocysucercosls
- lvetmecuo - oltets petmeoblllty to cl loos ooJ potolyzes tbe potoslte, uOc flotlo lofestouoo
- llpetozloe - e[ecuve oqolost toooJwotm (A. lumbrlcoldes), systemlc 5 posslble, c/l pteqooocy
- uletbylcotbomozloe
- Oxomolpoloe
- 8ltbloool
Annv|ra| Drugs
Inuenza
- AmanLadlne - blocks uncoaung of vlrus, mlld uA agonlsL, prevenuon & Lx lnuenza A2 ln hlgh rlsk
pauenLs, SL: halluclnauons, confuslon
- 8lmanLadlne - same buL does noL cross 888 - no CnS eecLs
- CselLamlvlr - neuramlnldase lnhlblLor selecuve for lnuenza A & 8, lnh. release of vlrus from
lnfecLed cells, oral, SL: nausea, vomlung
- Zanamlvlr - same mechanlsm, glven lnLranasally or by lnhaler SL: bronchospasm
kSV
- 8lbavlrln - aerosol, oral, lnh. vlral m8nA synLhesls, lnh. 8Sv, PSv, lnuenza, comblned w/ lln for Lx
Pep C, SL: hypoLenslon, anemla, depresslon, pregnancy CA1LGCk k - may be absorbed passlvely
so lL shouldn'L even be admlnlsLered by pregnanL women
- allvlzumab - confers passlve lmmunlLy Lo 8Sv, prophylaxls for hlgh-rlsk neonaLes
nerpes
- Acyclovlr - oral, Loplcal, lv, phosphorylaLed by vlral Lhymldlne klnase (more rapld ln herpes-lnfecLed
cells), lnh. vlral unA polymerase & dC1, kldney excreuon, Lx PSv-1&2, less poLenL vZv, SL:
somnolence & leLhargy when comblned w/ AZ1, safe ln pregnancy
- valacyclovlr (valLrex) - oral pro-drug, hlgher bloavallablllLy
- lamclclovlr - Lx PSv-1, -2, vZv, L8v, P8v, slmllar mechanlsm as acyclovlr
- uocosanol - lnh. fuslon b/w plasma membrane & PSv envelope, C1C Loplcal Lx cold sores
CMV]nerpes
- Canclclovlr - eecuve agalnsL CMv, more Loxlc, phosphorylaLed by Lhymldlne klnase & vlral proLeln
klnase phosphoLransferase, lv, SL: LeraLogenlc, neuLropenla, LhrombocyLopenla - Lx w/ C-CSl
- valganclclovlr - oral, hlgher bloavallablllLy, same SL prole
- clJofovlt - oseJ lv fot cMv teuolus
- loscarneL - dlrecLly lnh. vlral unA polymerase, 8nA polymerase and reverse LranscrlpLase, lv Lx
acyclovlr-reslsLanL PSv lnfecuons & CMv reunlus, SL: nephroLoxlc - monlLor creaunlne clearance &
keep pauenL hydraLed
- lomlvltseo - tx cMv, lottovltteol lojecuoo, 5. ocolot lofommouoo/vlsool lmpoltmeot
nepanns 8 and C
- lnLerferon alfa-2b, lnLerferon alfa-2a, alfacon-1 - comblned w/ rlbavlrln Lo Lx Pep C, musL be
ln[ecLed, SL: depresslon, anemla, ^AL1, hypoLenslon
- lnLerferon alfa-2b - also Lx Pep 8
- Lamlvudlne - lnh. P8v unA polymerase & Plv reverse LranscrlpLase, Lx: uCC chronlc Pep 8, Plv,
good combo wlLh AZ1
- Adefovlr - lnh P8v unA polymerase
- otecovlt - tx n8v, well toletoteJ
nIV: keverse 1ranscr|ptase Inh|b|tors - lnhlblL vlral reverse LranscrlpLase, phosphorylaLed lnLo
acuve sLaLe
- Zldovudlne (A21) - ma[orlLy meLabollzed ln llver, shorL acung, j raLe of dlsease progresslon, ^
survlval and j Lransmlsslon from pregnanL moLher Lo newborn, Lesung posslble Lx psorlasls and
adulL 1-cell leukemla, SL: myelosuppresslon (anemla, neuLropenla), CnS, Cl, lacuc acldosls &
hepaLoLoxlclLy
- uldanoslne - lnh. mlLochondrlal unA synLhesls, used ln comblnauon w/ AZ1 or alone ln pauenLs
lnLoleranL/reslsLanL Lo AZ1, SL: perlpheral neuropaLhy, pancreauus, hyperurlcemla
- Lamlvudlne - lnh. P8v unA polymerase, Lx: Plv & chronlc Pep 8, combo w/ AZ1 Lo Lx Plv, very
well LoleraLed
- SLavudlne - do noL comblne w/ zldovudlne, SL: perlpheral neuropaLhy
- 1enofovlr
nIV: Non-Nuc|eonde keverse 1ranscr|ptase Inh|b|tors - blnd dlrecLly Lo reverse
LranscrlpLase (does noL requlre phosphorylauon), comblne w/ AZ1 Lo avold reslsLance, C?3A4
lnducuon & meLabollsm
- Lfavlrenz - lnduces C?3A4, preferred excepL durlng pregnancy - LeraLogenlc, SL: CnS
- nevlraplne - lnduces C?3A4, should noL be glven w/ keLoconazole, preferred ln pregnancy, SL:
SLevens-!ohnson syndrome, hepauus
nIV: rotease Inh|b|tors - meLabollzed by C?3A4, poor bloavallablllLy, always use w/ reverse
LranscrlpLase lnhlblLors, avold SL. !ohn's WorL, SL: alLered body faL dlsLrlbuuon (corucosLerold-llke buL
w/ faclal aLrophy), lnsulln reslsLance, ^ serum cholesLerol - should noL be comblned w/ sLauns
- Saqulnavlr - lnh. Plv proLease, grapefrulL [ulce lncreases levels (LhaL's CCCu!)
- 8lLonavlr - lnh. Plv-1 and -2 proLeases, sLrong lnhlblLor of C?3A4, comblned w/ many oLher
proLease lnhlblLors due Lo meLabollsm lnhlbluon- ^eecuveness, SL: do noL comblne w/ dlsulram
or meLronldazole (formulauon conLalns alcohol.8l1 Cn!)
- lndlnavlr - lnh. Plv-1 and -2 proLeases, cross-reslsLance w/ rlLonavlr, SL: nephrollLhlasls
- Amprenavlr - slmllar Lo lndlnavlr and rlLonavlr, also does Lhe dlsulram Lhlng
- Loplnavlr/rlLonavlr - more eecuve Lhan rlLonavlr alone - lncreases avallablllLy of loplnavlr
- 1lpranavlr - non-pepude proLease lnhlblLor, glve w/ rlLonavlr and food, do noL comblne w/ benzos,
sLauns, Amlodarone, rlfampln, SL. !ohn's WorL, eLc.
nIV: Ius|on Inh|b|tor
- Lnfuvlrlude (luzeon) - SC ln[ecuon, no cross-reslsLance w/ oLher reLrovlral agenLs, SL: ln[ecuon slLe
reacuons
er|phera| Neuropathy
vlncrlsune, acllLaxel, uldanoslne, SLavudlne
1ubu||n 8|nd|ng
vlncrlsune, vlnblasune, Mebendazole, acllLaxel
No Mye|osuppress|on
SLrepLozocln, 8leomycln, vlncrlsune, Cyclosporlne, CapeclLablne, (Clsplaun)
Card|otox|c|ty
uaunorublcln, uoxorublcln, 1rasLuzumab
kad|anon keca||
Pydroxyurea, uacunomycln
1eratogen|c
Alkylaung agenLs, MeLhoLrexaLe, 1halldomlde, rlmaqulne, Mebendazole, 8lbavlrln, Lfavlrenz,
AzaLhloprlne
harm 3.2 - norsek|cks
Inh|b|tors of Ce|| Wa|| Synthes|s I. en|c||||ns
1. en|c||||ns - ume-dependenL kllllng, kldney excreuon lnhlblLed by probenecld, ln general Lhey
are falrly non-Loxlc and safe
Natura| en|c||||ns
- enlclllln C - lv, sttep, stopb, oelssetlo meoloqluJls, ttepooemo polllJom, closttlJlom
- 8enzaLhlne penlclllln
- rocalne penlclllln - lv
- enlclllln v - oral
en|c||||nase kes|stant en|c||||ns (Ann-Strep en|c||||ns) - requlre double Lhe loadlng dose
due Lo hlgh proLeln blndlng (>90)
- nafclllln - lv
- Cloxaclllln - oral
- Cxaclllln - oral
- ulcloxaclllln - oral
- MeLhlclllln - Lesung only, lf bacLerla are reslsLanL, Lhere ls alLerauon of Lhe 8, SL: lnLersuual nephrlus
Lxtended Spectrum en|c||||ns
- Amplclllln - oral
- Amoxlclllln - oral
- 8acamplclllln - oral
Annpseudomona| en|c||||ns
- Carbenlclllln - lv
- 1lcarclllln - lv
- Mezloclllln - lv
- lperaclllln - lv, mosL acuve, comblne w/ amlnoglycosldes Lo Lx lseoJomooos oetoqlooso
2. Cepha|ospor|ns - ume-dependenL bacLerlcldal acuvlLy
3. Monobactams - ume-dependenL bacLerlcldal acuvlLy
- AzLreonam - gram - rods
4. Carbapenems - ume-dependenL kllllng, (*anaerobes*)
- lmlpenem, CllasLaun - broad specLrum anaerobes, lv, reslsLanL Lo -lacLamase, comblne w/
amlnoglycosldes, SL: selzures
- Meropenem - same buL fewer selzures golng on
- LrLapenem
S. -|actamase Inh|b|tors
- Clavulanlc acld
- SulbacLam
- 1azobacLam
M|sce||aneous Comb|nanon roducts - (*anaerobes*)
- Augmenun (Amoxlclllln + Clavulanlc acld) - Lx anaerobes ln kluy caL blLe
- 1lmenun (1lcarclllln + Clavulanlc acld)
- unasyn (Amplclllln + SulbacLam)
- Zosyn (lperaclllln + 1azobacLam)
6. Cthers
- vancomycln - only gram +, oral Lx pseudomembranous collus/c. Jl[, lv Lx M8SA, comblne w/
amlnoglycosldes, poor CnS peneLrauon, excreLed unchanged by kldney, SL: hlsLamlne release (red
man syndrome), oLoLoxlc, nephroLoxlc
- losfomycln - broad specLrum, oral, Lx uncompllcaLed u1l ln women
- 8aclLracln - [acks up phosphollpld carrler cycle, gram +, Loplcal w/ olymlxln 8 and neomycln, SL:
oral dose-nephroLoxlclLy
- Cycloserlne - second llne broad specLrum 18 and u1l, SL: CnS and perlpheral neuropaLhy so avold
lL llke Lhe plague"
Inh|b|tors of Ce|| Wa|| Synthes|s II. Cepha|ospor|ns
Much llke penlcllllns, probenecld slows excreuon raLe. uncommon and reverslble SL:
pseudomembranous collus, dlsulram-llke reacuon (cefoperazone, cefamandole), dose-dependenL
renal Lubular necrosls, candldlasls
I|rst Generanon Cephs - good gram +, moderaLe gram -, uCC for . coll, klebslello, and ltoteos
lnfecuons
- Cefazolln (Ancef) - lM, lv, uCC surgery prophylaxls (add neomycln for colorecLal sx)
- Cephalexln (keex) - oral
- Cephradlne - oral, lM, lv (all Lhree, wow LhaL's rad!)
Second Generanon Cephs - ^ acuvlLy agalnsL gram -, added Motoxello coverage
- Cefoxlun - lM, lv
- Cefamandole - lM, lv
- Cefaclor - oral, SL, serum slckness
- Cefuroxlme - lM, lv
- Cefprozll - oral
- Loracarbef - oral
1h|rd Generanon Cephs - j acuve Lhan llrsL agalnsL gram +, much more acuve agalnsL
otetoboctetloceoe and qulLe acuve" agalnsL lseoJomooos oetoqlooso, also Lx 5olmooello,
Motoxello
- CefoLaxlme Sodlum - lM, lv
- Cefoperazone - lM, lv, llver meLabollsm, CnS peneLrauon, anupseudomonal
- Ceazldlme - lM, lv, anupseudomonal
- Cerlaxone - lM, lv, CnS peneLrauon, uCC gonorrhea, penlclllln-reslsLanL 5tteptococcos
poeomooloe
- Cexlme - oral, Lx gonorrhea
Iourth Generanon Cephs - more reslsLanL Lo some -lacLamases
- Cefeplme - lv, has a gay name, ^ ablllLy Lo peneLraLe bacLerlal cell's ouLer membrane, 100
bloavallable aer lM admlnlsLrauon, Lx lseoJomooos
Inh|b|tors of rote|n Synthes|s I.
Macro||des
- LryLhromycln - reverslbly blnds 30S, alLernauve for penlclllln allergy, specLrum slmllar Lo en C
(gram +), uCC leqlooello poeomopbllo, Lx eryslpelas due Lo CAS, pneumonla due Lo M. poeomooloe,
chlamydla, and Leglonnalre's dlsease, acld-sensluve, lnh. C?3A4, anLagonlsm w/ chloramphenlcol,
SL: Cl dlsLurbances, elevaLed hepauc enzymes, cholesLauc [aundlce, oLoLoxlclLy, may prolong C1
- ClarlLhromycln - slmllar mechanlsm, peneLraLes lung and macrophages: Lx MAC, n. pylotl-
assoclaLed duodenal ulcers, communlLy-acqulred pneumonla (CA)
- AzlLhromycln - slmllar mechanlsm, dosed once dally eecuve agalnsL chlamydla and gonorrhea,
pedlaLrlc ouus medla, pharynglus, and MAC prophylaxls, less eecL on C?3A4 and fewesL overall
SL/lnLeracuons
keto||des
- 1ellLhromycln - blnds 30S, broad specLrum, Lx resplraLory paLhogens, lnLracellular and aLyplcal
bacLerla, SL serlous hepaLoLoxlclLy
C||ndamyc|n - blnds Lo 30S, eecuve agalnsL gram + anaerobes only, eecuve w/ pyrlmeLhamlne ln
Lx Loxoplasmlc encephallus ln pauenLs w/ AluS, SL well known cause of pseudomembranous collus
Streptogram|ns
- ualfoprlsun, Culnuprlsun - lrreverslbly blocks rlbosome funcuon 30S, lv, Lx vancomycln-reslsLanL
otetococcos foeclom (vk), M8SA, lnh. C?3A4
Cxazo||d|nones
- Llnezolld (Zyvox) - reverslble, non-selecuve lnhlblLor of MAC, blnds 30S, eecuve agalnsL aeroblc
gram +, oral bloavallablllLy 100, meLabollzed vla non-enzymauc oxldauon (no lnLeracuons), Lx v8L,
M8SA, SL superlnfecuon
Inh|b|tors of rote|n Synthes|s II.
Am|nog|ycos|des - concenLrauon dependenL kllllng, horrlble oral absorpuon and CSl peneLrauon,
lnh. gram - (aeroblc coverage only) by blndlng lrreverslbly Lo 30S, eecuve parucularly agalnsL
lseoJomooos oetoqlooso, also lndlcaLed lf susplclon of sepsls, SL oLoLoxlclLy, nephroLoxlclLy
- CenLamycln - Loplcal appllcauon for Lx burns and wounds, bacLerlcldal ln vlLro agalnsL 93 5.
ooteos, uCC Lularemla, w/ penlclllln Lo Lx lseoJomooos
- 1obramycln - Lx of severe lnfecuons
- Amlkacln - genLamycln-reslsLanL lnfecuons may respond Lo Lhls lnsLead
- SLrepLomycln - Lx Lularemla, bubonlc plague (w/ doxycycllne), 8tocello, 18 (second llne),
endocardlus
- Specunomycln - Lx uncompllcaLed gonorrhea ln pauenLs who are allerglc Lo cerlaxone
- neomycln - Loplcal, Lx hepauc encephalopaLhy, prep for colon surgery
- aromomycln - Lx lnLesunal ameblasls, ctyptospotlJlom potvom lnfecuons
Inh|b|tors of rote|n Synthes|s III. - 8road Spectrum
Ch|oramphen|co| - reverslbly blnds 30S (*anaerobes*), bacLerlosLauc, oral, 100 oral absorpuon,
CnS peneLrauon, noL eecuve agalnsL . blstolyuc or pseoJomooos, reslsLance due Lo bacLerlal aceLyl
Lransferase, dlsLrlbuLed wldely (lncludlng CnS y los o[os), second llne Lx Lyphold fever (bacLrlm rsL),
menlnglus, 8lckeusla, Loplcal Lx eye lnfecuons, ^ eecL warfarln, j eecL penlclllln, SL: gray baby
syndrome, deadly aplasuc anemla
1etracyc||nes - Lx P. pylorl w/ meLronldazole + blsmuLh, Lx M. poeomoolo, chlamydla eL al, Llme
ulsease, vlbtlo cboleto, plague (w/ sLrepLomycln), 8tocello (w/ amlnoglycoslde), blnd speclcally Lo
30S, bacLerlosLauc, dlsLrlbuuon wlde excepL CnS and [olnLs, alumlnum and calclum salLs may greaLly
lnhlblL lnLesunal absorpuon, deposlLs ln bone and LeeLh, c/l pregnancy and chlldren<6
- 1eLracycllne - shorL acung
- uemeclocycllne - lnLermedlaLe acung, SL: lnh. AuP
- uoxycycllne - long acung
- Mlnocycllne - long acung, oLoLoxlclLy
G|ycy|cy||nes
- 1lgecycllne - derlvauve of mlnocycllne, blnds 30S, bacLerlosLauc, lv, Lx M8SA, M8SL, 8S, v8L
1reann' 1hem U1I''s
Some Agents
- nlLrofuranLoln - broad specLrum, no ptoteos and pseoJomooos coverage, > eecL ln acldlc urlne,
SL: brown urlne, meLhemogloblnemla, hemolysls, lnLersuual pulmonary brosls, severe
polyneuropaLhles
- MeLhenamlne MandelaLe - decomposes Lo formaldehyde ln Lhe urlne and blnds amlno groups,
bacLerlcldal, mandelaLe acldles urlne, malnly eecuve agalnsL . coll, reslsLance does noL develop,
non-Loxlc
- nalldlxlc Acld - maln eecL on gram -, esp. . coll, ltoteos mltobllls, klebslello, nlLrofuranLoln
anLagonlzes lf used concomlLanLly, no lseoJomooos coverage, SL: llver, carulage, convulslons
- 1MSMx - SL: LhrombocyLopenla due Lo folaLe meLabollsm lnLerference
- Cephalosporlns
- CenLamlcln
- 1obramycln
- Amlkacln
- Amplclllln - uCC llstetlo specles
- Amoxlclllln
- Augmenun, 1rlmenun, eLc.
- losfomycln LromeLhamlne
Some I|uoroqu|no|ones - lnh. unA gyrase!
- Clprooxacln - oral, broad specLrum bacLerlcldal, hlghly acuve ln vlLro, especlally agalnsL
lseoJomooos oetoqlooso and M8SA, less eecuve agalnsL gram +, anaerobes, and horrlble CnS
peneLrauon, poor 5ttep poeomo coverage, uCC prophylaxls of lnhalauonal anLhrax, Lx 5blqello, SL:
LranslenL ^ Ll1s, Lendon rupLure
- noroxacln
- Coxacln
- 1rovaoxacln, AlaLrooxacln - resLrlcLed Lo cerLaln llfe- or llmb-LhreaLenlng lnfecuons, 100 oral
absorpuon, SL: hepauc dlsease
- Moxloxacln, Cemloxacln - oral once-a-day, broad specLrum, beuer acuvlLy agalnsL penlclllln-
suscepuble and -reslsLanL pneumococcl (5ttep poeomo) (beuer gram +), beuer anaeroblc coverage,
beuer CnS peneLrauon, Lx CA, SL: should be avolded ln pauenLs wlLh long C1/pauenLs recelvlng
class lA (qulnldlne, procalnamlde, dlsopyramlde) or lll anuarrhyLhmlcs (amlodarone, soLalol, eLc.)
- Cauoxacln - Loplcal for eye lnfecuons, o Lhe markeL ln 2006 due Lo SL: ve-assed monkey
Su|fonam|des
lnh. growLh of suscepuble bacLerla, bacLerlosLauc ([ ] Lo bacLerlcldal levels ln urlne), A8A anLagonlsL,
broad specLrum, uCC Lx u1ls, Loxoplasmosls, neumocysus carlnll, oral, cross placenLa and 888, SL:
crysLallurla, kernlcLerus ln nurslng lnfanL, blood dyscrasla, kldney and llver damage, neuropaLhy,
!oeylsahomo syndrome, SLevens-!ohnson syndrome
- Sulsoxazole - shorL acung (qld), ^ proLeln blndlng, exLenslvely excreLed unchanged (bad lf
compromlsed renal funcuon), eecuve agalnsL communlLy-acqulred .coll, seems llke lL should be
called Sulsoxazole
- SulfameLhoxazole - lnLermedlaLe acung (bld), lnh dlhydropLeroaLe synLhase (A8A lncorporauon)
- Sulfasalazlne - prodrug-mesalamlne Lo Lx ulcerauve collus
- Mafenlde - bacLerla only, lnh carbonlc anhydrase
- Sllver Sulfadlazlne - Loplcal anu-lnfecuve agenL for Lx burns, eecuve agalnsL bacLerla and yeasL,
uCC NocotJlo, does noL sLaln
- 1MSMx - also avallable lv, uCC uncompllcaLed u1ls, nosocomlal lnfecuons due Lo xanLhomonas,
Motoxello, otetoboctetloceoe, NocotJlo, uCC loeomocysus cotloll, Lx ouus medla, LrlmeLhoprlm
lnh dlhydrofolaLe reducLase, pregnancy caLegory C-kernlcLerus ln lnfanL
- SulfaLhlazole + SulfaceLamlde + Sulfabenzamlde
- Sulfadoxlne + yrlmeLhamlne - Lx malarla, SL: Loxlc epldermal necrolysls
- SulfaceLamlde, Sulfur - Loplcal Lx dry skln
M|sce||aneous Annb|oncs
Aga|nst Gram +
- uapLomycln - bacLerlcldal, lv, blnds Lo membranes-depolarlzauon, no reslsLance
- Muplrocln - bacLerlosLauc aL [j], bacLerlcldal aL [^], lnh proLeln/8nA synLhesls, Loplcal Lx
lmpeugo, lnLranasal Lx M8SA, no cross-reslsLance
Aga|nst Gram -
- olymlxln 8, L - bacLerlcldal, Loplcal, lv, ^ cell membrane permeablllLy, no eecL on ltoteos or
Nelssetlo, Lx reslsLanL lnfecuons
- CollsumeLhaLe Sodlum - lv, converLed Lo collsun, noL safe because lL llkes Lo eaL our kldneys
- Collsun SulfaLe - Loplcal, comblned w/ some oLher sLu Lo Lx ouus exLerna
Annmycobacter|a| Agents
- lsonlcounlc Acld Pydrazlde - #1 sLunna prophylaxls, oral, lnh mycollc acld, always glven ln
comblnauon w/ aL leasL one oLher anu18 drug, rapld vs slow meLabollzers, SL: CnS sumulauon,
perlpheral neuropaLhy, llver damage, hemolysls (C6u declency)
- LLhambuLol - glven w/ aL leasL one oLher anu18 drug, renal excreuon, SL: decrease of vlsual aculLy
and loss of red-green percepuon suggesung reLrobulbar neurlus
- 8lfampln - broad specLrum, lnh. unA-dependenL 8nA polymerase, acuvlLy approaches LhaL of lnP,
eecuve agalnsL leprosy, SL: orange secreuons
- yrazlnamlde - SL: hepauc ln[ury
- SLrepLomycln
- loto-omloosollcycllc oclJ - blqb toxlclty
- tblooomlJe - oeototoxlc
- copteomyclo - oepbtotoxlc
- cyclosetloe - petlpbetol oeotopotby, cN5 slJe e[ects
- klfobouo - tbtombocytopeolo, polymyolqlo
- klfopeouoe
- clofozomloe
- clptofoxoclo
- Amlkoclo
Agents Used |n Leprosy
- uapsone - uCC leprosy, A8A anLagonlsL, oral, SL: meLhemogloblnemla, hemolysls, perlpheral
neuropaLhy
- 8lfampln
- Clofazamlne - blnds preferenually Lo mycobacLerlal unA, SL: crysLalllne deposlLs, hepaLoLoxlc
- 1halldomlde - uCC eryLhema nodosum leprosum, Lx Plv wasung syndrome, reduces levels of 1nl-
o, oral, pregnancy CaLegory x
Annfunga| Agents
System|c Annfunga|s
- AmphoLerlcln 8 - lv, lnLeracLs w/ ergosLerol - large Lransmembrane lon channels, uCC for all
sysLemlc fungal lnfecuons, requlres lnlual hosplLallzauon, SL: nephroLoxlclLy, hepaLoLoxlc
- AmphoLerlcln 8 Llpld lormulauons
- llucyLoslne - oral, converLed Lo 3-lu and lnh LhymldylaLe synLhase, ucyLoslne + amphoLerlcln 8 =
uCC crypLococcal lnfecuons, SL: bone marrow suppresslon
- keLoconazole - oral, Lx sysLemlc lnfecuons, lnh. fungal lanoslne 14o-demeLhylase, SL: lnh. human
C?3A4, lnh. adrenal and Lesucular funcuon, gynecomasua
- lLraconazole - oral, capsule, Lx Aspetqlllos, cooJlJo, onychomycosls, SL: lnh. C?3A4
- lluconazole - oral, lv, less Loxlc Lhan amphoLerlcln 8 or ucyLoslne, beuer LoleraLed Lhan
keLoconazole, besL CSl peneLrauon
- vorlconazole - oral, lv, exhlblLs acuvlLy agalnsL molds, uCC lnvaslve asperglllosls, SL: lnh. C?3A4,
vlsual lmpalrmenL
Lchlnocandlns - lack nephroLoxlclLy, few drug lnLeracuons, lnh. (1,3)-u-glucan, Lx esophageal
candldlasls
- Caspofungln - lv, Lx lnvaslve asperglllosls ln refracLory pauenLs, esophageal candldlasls
- Mlcafungln - lv, prophylaxls for pauenLs undergolng hemaLopoleuc sLem cell LransplanLauon
- Anldulafungln - lv, Lx esophageal candldlasls
1op|ca| Annfunga|s
- Crlseofulvln - oral, desLroys mlLouc splndle, blnds keraun, Lx rlngworm lnfecuons, onychomycosls,
oLher sysLemlc dermaLophyLosls, SL: acuLe lnLermluenL porphyrla
- nysLaun - oral, Loplcal, ^fungal membrane permeablllLy, Lx Candlda lnfecuons of skln, lnLesunal
LracL, mucous membrane (vaglnal LableLs)
- CloLrlmazole - Loplcal C1C Lx vaglnal candldlasls, unea
- Mlconazole - MonlsLaL 7", Loplcal, Lx vulvovaglnal candldlasls, unea
- 1erblnane - oral, Loplcal, lnLerferes w/ fungal sLerol blosynLhesls, hlghly eecuve Lx onychomycosls
(superlor Lo grlseofulvln and lLraconazole), SL: hepaLoLoxlclLy
- 1olnaaLe - Lx unea pedls, unea verslcolor, noL eecuve agalnsL onychomycosls
8enal LoxlclLy
- Vancomycln, Amlnoglycosldes, Cephalosporlns, AmphoLerlcln 8, Sulfonamldes
PepaLoLoxlclLy
- AmphoLerlcln 8, Cllndamycln, LryLhromycln, Sulfonamldes, InP, 1eLracycllnes
CLoLoxlclLy
- Vancomycln, Amlnoglycosldes, Mlnocycllne, LryLhromycln
8acLerlcldal
- Amlnoglycosldes, 8aclLracln, -lacLams, uapLomycln, lnP, keLolldes, MeLronldazole, olymlxlns,
Culnolones, 8lfampln, 1lgecycllne, vancomycln
8acLerlosLauc
- Chloramphenlcol, Cllndamycln, LLhambuLol, Macrolldes, nlLrofuranLoln, Cxazolldlnones,
Sulfonamldes, 1eLracycllnes, 1rlmeLhoprlm
AgalnsL gram +
- l don'L feel llke Lyplng LhaL llsL
AgalnsL gram -
- Amlnoglycosldes, Carbapenems, Chloramphenlcol, Culnolones, 8lfampln, 1eLracycllne, 1lgecycllne