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    DIURETICSCarbonic Anhydrase Inhibitors= @proximal tubule CA = luminalmembrane & cytoplasm; critical for HCO3

    - reabsorption

    DRUG EFFECTS USES ADVERSE EFFECTS

    Acetazolamid

    e

    Hyperchloremic metabolic acidosis

    (HC!"reab#or$tion%; milddiuresis

    FE of Na+('% & +()'%

    HCO3-#ecretiona*+eo+#

    ,+mor & CSF $ro-+ction (al#oCSF $H%

    !rinary al"alinization(+ric aci- & c.#tinee/cretion%;#laucoma(I0%$etabolic al"alosis1to excess diuretics+#e(H2lo## in CD% or acute resp% acidosisAcute mountain sic"ness(C3S%

    Hyperchloremic metabolic acidosis

    &enal stones($,o#$,at+ria4 ,.$ercalci+ria%

    + 'astin(,.$o5alemia (correct 67 Cl

    replacementor combo t/%; Aller(icr/n#

    C)I= cirrhosis (3H82e/cretionC3S #/%

    *oop iuretics= ,- Na+ )+). Cl- symport@thic" asc% *OH (l+minal% General = ra$i-l. ab#orbe-4 bo+n-$la#ma $rotein#4 #ecrete- b. OA/sin 0CT

    DRUG EFFECTS USES ADVERSE EFFECTS

    Furosemide(Lasix%/orsemide

    0umetanide

    Ethacrynicacid

    NaCl4 $(.+4 +4&H+excretion

    Ca.+ excretion(miti9ate- in DCT%

    isruptcritical #te$ in $ro-+cin9hypertonic medullary interstitium

    S.#temic :eno+# ca$acitanceFurosemide=

    &0F& redistributesRFmi-corte/

    $O1/ e22icaciousa9ent#; 1eere edema(pulm% edema4 CHF4 cirr,o#i# 67 a#cite#%Acute hypercalcemia (m+#t 9i:e #alinetoo% or hyper"alemia; hyponatremia

    A&F= urine 2lo'; im$ro:e ob#tr+ction#

    Anion oerdose(m+#t 9i:e #aline too%

    Hypo"alemic metabolic al"alosis; ECF4depletion; hypoma(nesemiaOtotoxicity= dose"relate-; +#+all.reersible

    Hyperuricemia= ,.$o:olemic"a##oc< +ric

    aci- reab#or$tion in 0CT

    9o+t attac5#Aller(icr/n# = mo#t are #+lfonami-e#)I= N1AIsbluntloo$ -i+retic effect#

    /hiazides& /hiazide-li"e iuretics= ("% Na+ )Cl - symport@C/(l+minal% Ca12acti:e reab#or$tion controlle- b. 5/H(in#ert# a$ical Ca12c,912excretion+'astin(67 H2e/cretionCa.+ reabsorption(lo6er ?3a2i

    3a27Ca12ba#olateral e/c,an9e%

    54&:ia action# on :a#c+lar S>

    $ild edemaa##oc< 67 CHF4 li:er & 5i-ne.-i#ea#e4 & corticosteroidt,era$.; H/N

    Nephro(enic I ($la#ma :ol+meGFRfiltere- loa- to -i#tal t+b+le#+rine

    :ol+me%I-io$at,ic ,.$ercalci+ria6 Ca .+ nephrolithiasis

    Hypo"alemic metabolic al"alosis

    Hyperuricemia4 hyper(lycemia4hypercalcemia4 ,.$oma9ne#emia

    **; im$otence; hyponatremia;

    ECF4 depletion7 Aller(icr/n# = are#+lfa

    +-1parin( iuretics = @collectin(& late distal tubules; TH t.$e# +#e- to preent hypo"alemia& enhance natriuresis67 loop &thiazides

    DRUG T0E EFFECTS USES ADVERSE EFFECTS

    1pironolacton

    e

    Eplerenone

    Aldosterone

    Ranta(onists

    1mall(1'% excretionof filtere-

    loa- (limite- ca$acit. of late DCT& CD to reab#orb #ol+te#%

    Excretionof + 6 H+6 Ca.+ 6 $(.+

    (-+e to l+men"ne9ati:e

    tran#e$it,elial $otential%

    5ost-$I; t/ H/N; T/mineralocorticoid excessB

    8= Conn# #.n-< or ecto$ic

    ACTH; 1= CHF4 cirrhosis

    Hyper"alemia metabolic acidosis(ri#5 67 renal-i#ea#e or -r+9#renin relea#e%S.nt,etic #teroi-#(ynecomastia4 impotence4

    men#tr+alirre(ularities

    /riamterene

    Amiloride

    Na+ channel

    inhibitors

    T/*ithium-induceddiabetes insipidus

    Triamterene"idney stones;A&Fif combo 67

    indomethacin; Amilori-enausea4 diarrhea

    1

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    Al-o#terone net effect# = l+minal Na+conductance& basolateral3a2"2A/5ase; Na+delieryto C, potential+ )H+ secretiono Relea#e =

    ratio +)Na+#en#e- b. a-renal corte/ cell#; 1N1or renal a22erentart stretchreninATIIal-o#terone3a24 2

    2

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    Osmotic iuretics= action# @proximal tubule4 descendin( *OH4 & C $!1/be 2reely 2iltered4 NO/ reabsorbed4 & metabolicall. inert

    DRUG EFFECTS USES ADVERSE EFFECTS

    $annito

    l

    $!1/9i:e b. I4; medullary tonicity= e/tract 6ater from

    ICFe/$an- ECF com$artment("% renin relea#eRF (e#$ar5e-

    urine

    olume; excretionnearl. all e"l.te# (3a24 24 Ca124 >9124 Cl"4 HC!"%

    Natriuresis lesst,an 'ater diuresis,.$ernatremia (initial ,.$onatremia%

    T/ A&For renal insu22iciency .

    to nephrotoxins

    U#e- toIC5& IO5(9la+coma%

    T/ dialysis dise9uilibrium synd%

    (ra$i- #ol+te remo:al#mEC%

    ECF olume expansion

    (in CHF can2ran"

    pulmonary edema%;37V; H7A; ehydration: hypernatremia

    AH anta(onists = anta9oni#t# of 4.AHR# @collectin( ducts Dr+9# t,at can ca+#e SIADH = $#.c,otro$ic me-#4 #+lfon.l+rea#4 al5aloi-#DRUG EFFECTS USES ADVERSE EFFECTS

    Coniapta

    n

    /olaptan

    cA$5; Coni:a$tan4

    (anta9oni#t @48aR#%

    T/ 1IAH(,.$onatremia; 1to $+lm< -i#ea#e4 C3S in+r.4 $o#t"o$4 -r+9#%T/ CHF6,en olume replacement not desired(ADH 1to V%

    Nephro(enic I

    ARF; ,.$ernatremia

    Chan(esin !rinaryElectrol.te 0attern# & o-. $H Im$ortant Dr+9 Interaction#

    Gro+$ NaCl NaHCO

    3

    +

    o-.$H

    Im$ortantDr+

    3SAID#4 #alt & -econ9e#tant#diminished diureticre#$on#e

    CAinhibitors + +++

    +

    toto/ic -r+9#enhance ototoxicityof loop-i+retic#

    *oopa9ent# ++++ ;

    +

    A

    DISEASE 0RE> TREAT>E3T

    ES

    CHF

    Refle/ control #ee# ,.$o:olemia3a7H1retention$reloa-; E/ce## 3a7H1retentione-ema in $eri$,er. & l+n9#

    *oop -i+retic# or comboloop + thiazide -i+retic#

    Com$lication# = e/ce## +#e can2illin( 5; metabolic al"alosis

    can com$romi#e car-iac f/n; hypo"alemiaarr,.t,mia#

    &enal disease

    Glomer+lar -i#ea#e (D>4 SE%3a7H1 retention

    Diabetic ne$,ro$at,.,.$er5alemia

    3e$,rotic #.n-

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    of intra:a#c+lar :ol+me4 hypo"alemia& metabolic al"alosis

    3

    Essential H/N Hi9, #.#temic 0 &estrict dietary Na+inta5e4 thiazide-i+retic or combo t,era$.

    Nephrolithiasi

    s

    &enal stones(calci+m $,o#$,ate or o/alate% /hiazide-i+retic#urinary Ca.+concentration#

    I3ot re#$on#i:e to ADH; t/ = a-e*+ate H1 inta5e /hiazide-i+retic#2luid deliery todilutin( se(ments:ia

    $la#ma :ol+me#F&ma/ :ol+me of -il+te +rineHypercalcemi

    a

    E/ce##i:e Ca12 *oop-i+retic# 67 conc+rrent #aline inf+#ion to $re:ent :ol+mecontraction; ma. nee- to a-- 2a# 6ell

    4

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    A3TIARRHTH>ICSClass I 9eneral c,ar< = Na + channelbloc5er#4 act on 2ast responsecell#4 threshold for firin9 in abnormal $acema5er4 slo' A5 upstro"e

    Class IA= slo's phase ;-e$olariation in :entric+lar m+#cle fiber#4 A5 duration& C46 E&5 H.$er5alemiato/icit. for A cla## I -r+9#DRUG EFFECTS USES ADVERSE EFFECTS

    5rocainamid

    e

    loc5# INa(%4 Ir(1% (intermediate5inetic#%

    Directl. pacema"er rate(SA7AV no-e#%

    5artial (an(lionic bloc"ade0VR05*iermetaboli#mNA5A; renal elimination

    Effecti:e for most atrial& entriculararr,.t,mia# e#$< #.m$tomatic 0VC#4 V"tac,.ndor 3rdDC (after lidocaine4 amiodarone%sustained entriculararr,.t,mia#" acute $I

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    ;B eliminatedb. "idney unchan(ed Effecti:e conertin( AFsinus r,.t,m If com$romi#e- renalf/ntoxic leels

    1otalol

    -bloc"in(effect# (Cla## II%; A5

    duration:ia bloc5in9 +ch%(Cla## III%

    /hresholdof car-iac -efibrillation

    T/ life"t,reatenin9entriculararr,.t,mia#>aintain# sinus r,.t,m in $t# 67 AF5eds= t/ 14 &entriculararr,.t,mia#

    ose"relate- inci-ence of torsade de pointes

    *4 2xnin $t# 67 o:ert CHF

    6

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    Class I4= *-type Ca.+ channelbloc5er#; ,- A5in 1A& A4 nodes; C4& E&5; 5& interal; bloc5# 0O/Hacti:ate- & inacti:ate- Ca12c,AInteract# 67 Na+)+-A/5ase4 +: Ca.+c,annel#

    /orsade de pointes

    i(italis toxicity

    $uscle 'ea"nessin o:er-o#e

    5acema"er cell# A0 (slo' response%B 0,a#e ;= upstro"e; o$enin9 of 4-(ated Ca.+c,annel#; #ome contrib+tion :ia 3a2f+nn. c,aor c+rrent# = non-selectie I2(pacema"er4 Na

    +

    %& I8(in'ardrectifier4 out'ard

    +

    %o Factor# t,at rate= slope-ia#tolic -e$olariation & max-ia#tolic potential (51N14 AC,%; shi2tin t,re#,ol- a'ay from Em

    Non-pacema"ercell# A0 (2ast response%B 0,a#e ;= rapidupstro"e; V"9ate- Na+c, slope:iaBo 0loc"Na+or Ca.+c,annel#ratio of 3a2(or Ca12% to +$ermeabilit. R indirectlyb. bloc"in( +chronotropiceffect# of NE

    7

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    Dr+9 tar9et# for abnormal conduction= slo'con-+ction; induce bidirectionalbloc5 in ob#tacle; dispersionin re2ractory$erio-# Hyper"alemia= A5-+ration4 C44 pacema"er rate& arr,.t,mo9ene#i#4 ectopic pacema"er#ite# are more sensitieto +

    8

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    A3TIH0ERTE3SIVES/hiazide iuretics= ("% Na+ )Cl - symport@C/Na)H.Oexcretion 0lac"$t# 9enerall. respond bettert,an 6,ite $t#

    DRUG EFFECTS USES ADVERSE EFFECTS

    Hydrochlorothiazide(HCT%

    Chlorothalidone

    (moreeffecti:e%

    54

    preload

    CO

    05

    O7 contin+e- t/54& :ia

    direct actionson :a#c+lar S>;Kresettin(ofbaroreceptorsL

    8st line R 67 certain otherantihypertensies to control2luidretention : edema#ome of t,e#ea9ent# ca+#e

    Hypo"alemia = sensitizes myocardiumto arrhythmiasHyper(lycemia; hyperuricemia

    Hyperlipidemia(c,ole#terol4 VD4 & D%>etabolic al5alo#i#4 ,.$onatremia4 ,.$o:olemia

    CC0s(*-type

    Ca

    .+

    Channelloc5er#%B

    Non"-i,.-ro$.ri-ine# =

    4erapamil&

    iltiazem(DH0#%

    ihydropyridines=

    Ni2edipine&

    AmlodipineDRUG EFFECTS USES ADVERSE EFFECTS

    Ni2edipine

    Amlodipin

    e

    C,< bloc5a-e on :a#c+lar S>asodilation; dihydropyridines,a:e e22ect

    on 04s4 6,ile non-dihydropyridines,a:e e22ecton heart; 0O/H

    cla##e#05(preload:a2terload%

    8st lineR incombo67 t,iai-eor RAAS mo-ifier

    An"le edema; an(ina pectoris67

    short actin($re$ of ni2edipine

    Fl+#,in94 tran#ient H7A4 #li9,t HR

    ACE Inhibitors Enala$ril & i#ino$ril = ONCE daily Ca$to$ril = /I 0t# 67 lo' plasma renin(mo#t blac"$t#% ma. NO/ respond as 'ell

    DRUG EFFECTS USES ADVERSE EFFECTS

    Enalapril

    *isinopri

    lCa$to$ril

    ,- ACE

    brady"inin &

    A/II;

    05b7c

    A/II& aldosterone(NO edema%

    5reload& a2terloadNOeffect on contractilit. or HR

    E22ectiein most pts6,en +#e- aloneR in combo67

    thiazide6 CC04 or -bloc"er

    U#e- after ac+te >I4 for CHF & renal

    im$airmentris"of $I6 stro"e4 & diabetic

    nephropathy

    Hyper"alemia4 dry cou(h4dys(eusia; ,.$oten#ion (#t-o#e%C)I= $t# 67 0* renal a%stenosis& pre(nant F

    DRUG T0E EFFECTS USES ADVERSE EFFECTS

    *osartan; /elmisartanOlmesartan

    A&0sCompetitie inhibitorsA/II bindin(A/8&s; preload& a2terload

    Do NO/effect car-iac f/n; -o NO/bra-5ininNOco+9,1imilar to

    ACE

    inhibitors

    Hyper"alemia4 dizzinessC)I= samea# ACE"I#

    Alis"iren&enin

    Inhibitor

    In contrastto ACE"I# & AR#4 does NO/ plasma renin actiity

    *i"eACE"I# & AR#4 preload& a2terload?)Oaffectin9 car-iac f/n

    Hyper"alemia4 diarrheaC)I= samea# ACE"I#

    JIntrinsic 1ympath% Act (ISA% = partial a(onist@R#lessHR & m.ocar-ial -e$re##ion & NO0VR :#< "onl. bloc5er#T,e samei# al#o tr+e 67 mixed : bloc5er#

    ?hite& youn($t# respondbettert,an blac5 & el-erl. $t#

    EFFECTS USES ADVERSE EFFECTS C7I & CAUTI3S

    H&& FCCO05 $ore seere H/N= +#e- in

    combo67 thiazides4 &AA1

    Fati(ue4(eneral tiredness4& exercise C)I=Asthma)CO5; sinus bradycardia

    Cautions= $; 54; ariant an(ina9

    Non-selectie

    -bloc"ers

    8-selectiebloc5er# $ixed

    :

    LipidSoluble WaterSoluble Lipid Soluble Water Soluble LipidSoluble

    5ropranolol4 TimololJ5indolol

    3a-olol >eto$rolol Atenolol J*abetalolCaredilol

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    Re#+lt# in re2lex 1N1

    acti:it. & 54&

    &eninrelease

    modi2iers4 or H5CC0sIHD; arrhythmias; CHF

    tolerance; 54&; bradycardia4 myocardial

    depression; ** & H*

    *ipid #ol+bledepression& other CN1#/

    pectoris; -o NO/ stopchronica-mine/ico e/ce$t 6,en +#e- for an(ina pectoris6 CHF6 arrhythmias6 : post-$I

    10

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    DRUG T0E EFFECTS USES ADVERSE EFFECTS

    5razosin

    8

    selectiebloc"ers

    05b. preload& a2terload

    (arterial) enous asodilator%;

    H*)**

    T/ H/N(NO/8stline%; t/ 05H 5ostural hypotension (8st-o#e%&e2lextachycardia4 H7A4 incontinence4im$otence4 na#al con9e#tion

    Clonidine

    $ethyldop

    a

    Central

    .

    a(onists

    In C3S1N1& 51N1acti:it.;

    NE release@peripheral 1N1 n%

    U#e- to 0 in $t# 6,o ,a:e notrespondedto ot,er combo#CANK/+#e a# monotherapy

    $ental depression; sedation4 drymouth4 & constipation; Abrupt )Cafter $rotracte- +#ehypertensie crisis

    &eserpine

    5ost

    1N1bloc"er

    ,- 4$A/.on :e#icle# in 3E ner:e#

    NE depletion in $eri$,er. & C3S

    Combined67 -i+retic for mil- to

    mo-< H/N(not 6i-el. +#e- b7c C3SA7E%

    CN1(#e-ation4 psychic depression%; CV

    (04 HR%; -iarr,ea4 aci-4 na#al con9+#cle%; selectielydilate arteriesNO/ einspreloadC'or"& O.demandDRUG EFFECTS USES ADVERSE EFFECTS

    Hydralazin

    e

    Ca.+ aailabilitya2terload Orallyeffecti:e VD# +#e- in adanced sta(e of H/Nto 0in $t# 6,o ,a:e not re#$on-e- a-e*+atel. to ot,er combo#;

    $!1/be (ien67 loop diuretic :

    -bloc"er; C)I= $t# 67

    IH; refle/1N1& &AA1ma.an9ina & i#c,emic

    arr.,t,mia#

    >a.1*E-li"e syndrome

    (art,ral9ia4 #5in ra#,e#4fe:er%

    $inoxidil

    Opens +

    channels,.$er$olariation & S>

    relaxation

    a2terload

    Hypertrichosis(,air%

    Dr+9# U#e- to /x Hypertensie Crises= acute

    0567 05 88;or 105 8;; emer(ency= acutetar9et or9an dama(e; ur(ency= NO/$re#ent

    DRUG 0R0ERTIES EFFECTS ADVERSE EFFECTS

    Nitroprussid

    e

    I4; effect# -i#a$$ear 67inmin+te# of D7C inf+#ion

    ilates 0O/Harteries& einsAct# on E&F-&(#C%releases NO

    Cyanide toxicity67 $rolon9e- (P8Q,% or too ra$i- inf+#ionC)I= -+rin9 pre(nancy

    HydralazineU#e- forhypertensie emer(enciesinpre(nancy relate- toeclampsia See abo:e

    *abetalol &apidon#et4 la#t# 3- hrs loc5# :

    8st line dru(sfor t/ H/N= thiazide-i+retic#4 &AA1mo-ifier# (ACE"I#4 AR#4 Renin In,ibitor#%4 & CC0s

    Dr+9 interaction = A/ modi2iers& N1AIsimpaired renal 2unctione#$< in elderly & olume depleted$t#

    +sparin(-i+retic# (1pironolactone& /riamterene% = NO/+#e- a# solea9ent; +#e- in combo67 thiazide& loop-i+retic#+loss *oop-i+retic# (Furosemide% = +#e- 67 antihypertensie a(entst,at cause pronounced 2luid retention; mo#t effecti:e -i+retic b+t mo#t to/ic N)' lifetime $robabilit. of -e:elo$in9 HT3 5rehypertension = S0 8.;"!N or D0 ;"QN 1ta(e 8HT3 = S0 8>;"N or D0 ;"NN If NO/controlle-$I4 an(ina$ectori#4 arrhythmias4 #+--en death4 renal 2ailure4 stro"e4 & isual disturbances

    11

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    A3TIA3GI3A DRUGSOr(anic Nitrate 4asodilators = NO(2% #Cc#$5dephosphorylation of myosin li(ht chainsascular 1$ relaxation

    DRUG 0R0ERTIES EFFECTS USES ADVERSE EFFECTS

    Nitro(lycerin

    Isosorbide

    dinitrate

    Isosorbide-G-mononitrate

    *ipid-soluble; rapidlyab#orbe- & de(radedin lier/olerance deelops rapidly67 lon("actin9 a9ent#4nee- daily hr dru(-2ree periods1ublin(ual(3G% = route o2 choicefor acuteattac5#;ma/ effect# !") min; -+ration DL hr

    Oral(all% = prophylaxis; -+ration 8"1 ,r#/ransdermal(3G% = prophylaxis; Q"8 ,r#I4(3G% = 8st.> hrsin $t# 67 UA73STE>I (AC1%

    5reload4 a2terload4 & 'all

    tensionO.demand

    8 capacitanceV#; -ilate

    resistanceV# hi(herDo#e# titrated#o no more

    t,an 8; mmH9

    05(P -ro$refle/ S3S%

    Coronar. a< asospasm

    1tablean9ina4ariantan9ina (al#o+#+all. re*+ire CC0s%!nstablean9ina (UA%& N1/E$I(can co"

    a-min 67

    -bloc"ersmortality%

    H)A; orthostatic

    05

    H&& syncope(D%

    )I= 5EG inhibitorse/treme ,.$oten#ion

    -0loc"ers ')o I1A= 5ropranolol6 $etoprolol6 Atenolol = FC*4E4& m.ocar-ial 'or"(correct 67 N#%; abrupt 'ithdra'alsxrea$$earEFFECTS USES ADVERSE EFFECTS

    FC & 0O.demandHRdiastolic per2usiontime

    1table an9ina= cornerstoneof t/ (can co"a-min nitratesor CC0s%;

    1ilenti#c,emia (')o$ain%; !A& N1/E$I(co"a-min 67 oral nitrates%

    NO/:ariant an9ina; mortalityin #ettin9 of acute $I

    Se-ation4 2ati(ue4 impotence4 A4 bloc"C)I=Asthma)CO5; $; decomp%HF)I= additie67 ot,er cardio-depressants

    CC0s = bloc5 *-typeCa.+

    ch%

    tran#membrane Ca12

    in2luxB In ,eart =

    FC4

    1A rate& AV con-+ction &elax ascularS> (arterioles:en+le#%DRUG T0E EFFECTS USES ADVERSE EFFECTS

    4erapami

    l

    iltiazem

    NH

    50O/Ht.$e# = asodilationa2terload(ma@or% &

    enodilationpreload(minor%O.demand

    DH0# =FC& H&diastolic per2usion; bl+nt refle/

    HR

    5rophylactic t/ stable&ariantan9ina (acutely

    asospasm%

    H5s= $t# 67 hx 14/4 A-2iborA-2lutter

    Constipation7acute HF;A4 bloc"; )I= additie67 ot,er car-io"-e$re##ant#

    Ni2edipine H5 $ore selectieon 04s0 Hypotension; re2lex H&

    t,er A9ent# = li$i- lo6erin9 a9ent# (mo#t fre*+entl. 1tatins%#er+m **ris" ischemicCV e:ent# Diet & life#t.le mo-ification# in-icate-

    DRUG >A EFFECTS & USES ADVERSE EFFECTS

    &anolazin

    e

    ,- *ate INain ,eart>o-ifie# FAO

    O.demand; FA mo-ification ma. im$ro:e 1+tiliation; +#e- for prophylaxis

    in chronican9ina (NO/ac+te attac5%; )I= CM53A inhibitorsto/icit.I; improes mortality rates in @ri#5 $o$+lation#;

    : durationof i#c,emic attac5# in $t# 67 CA

    !A(no#i9n#% & N1/E$I(eleatedbiomar5er# of -ama9e% = $t# 67 UA ,a:e 8G-.;B ris"of acute $I67in 8" 65#; a99re##i:e txris"b. G;Bo T/ = N#(8st.>h%lon(-actin(oral nitrate& co"a-min

    -bloc"ers; A1A4 heparin4 ot,er anti$latelet# (G0IIb"IIIa & AD0"R anta9oni#t#%

    1/E$I= pla9ue ruptureoccludesa

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    !nstable (!A% or KAcceleratin(L An9ina = occ+r# @rest; $ain e/,ibit# in character4 & duration; tonein epicardialaaI 1table(classic4 exertional% an9ina = atherosclerotic pla9ue limitsflo6 +#+all. in lar(e conduitaaaor -eterminant# of m.ocar-ial O.-eman- = 'all stress (preload4 a2terload4 & :entric+lar 'all tension%4H&4 &contractility

    13

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    TREAT>E3T F HEART FAIURE AGE3TS ?I/HO!/0SITIVE I3TR0iuretics= essential for symptomatic HF67 2luid retention; preent$ro9re##ion from hypertrophyHF; spironolactoneimproes surial

    Aldosterone= 3a27H1 retentionedema; + 'astin($otential for arr,.t,mia#; mo-+late# colla9en -e$o#ition (2ibrosisin heart& 04s%o Effect# of al-o#terone 2 3a2oxidatie stress:a#c+lar in2lammation4 dama(e4 & fibro#i# 04s= endothelial dys2xn& remodelin(

    o >anife#tation#B V# = H/N4 atherosclerosis4 i#c,emia rain (baroreceptor dys2xn% = stro"e &enal 2ailure

    Heart (:entric+lar hypertrophy& remodelin(4 +1N1% = heart 2ailure4 SCD4 $I

    DRUG >A EFFECTS & USES ADVERSE EFFECTS

    Furosemide

    0umetanide

    ,- Na+)+). Cl-

    @thic" asc% *OH

    3aCl7H1 excretion; preload& a2terload; edemaNO eidencefor mortality bene2it/hiazides similareffect# to loop4 b+t lessefficacio+#

    *oop & /hiazides= +6 Na+6 metabolic

    al"alosis4 hyperuricemia6 0+1N1)&AA1*ooponl. = $(.+4 ototoxicityHC/ ,-Na

    +)Cl-@C/

    1pironolacton

    e

    Eplerenone

    Aldosterone

    anta(onists @Cs4

    heart4 & arterial 'all

    Natriuresis; $reloa-; aderse remodelin(in ,eart& V#;

    mortality; T/ 1ta(e III-I4 CHF; recentor

    currentCHF #/; t/ hyperaldosteronism& H/N; +

    Hyper"alemia;endocrine abnormalities(9.necoma#tia4 im$otence4 men#tr+al irre9+laritie#4-ee$ene- :oice%

    Coniaptan

    /olaptan

    4.& anta(onists

    solute-2ree+rineSer+m Na+in CHF $t#; +#e- in hospitalfor acute decompensated HF(,a:e AHDle:el of CHF%; for

    euolemic ,.$oten#ion; NOeidencefor mortality

    ACE-Is = ,- ACE

    A/II; ("% 5inina#e II

    brady"ininasodilation& 5# release ATII =

    4C4 +1N14

    aldosterone& AHrelea#e

    A&0s = competitie inhibitorsATII bin-in9 +#+all. @A/8&s A/8R# = 4C& proli2eratieaction# A/.R# = 4& anti$roliferati:e action#DRUG EFFECTS USES ADVERSE EFFECTS

    Enalapril

    Captopri

    l

    5reload& a2terload05

    &CO; aldosteroneV

    Aderse cardiac remodelin(

    1lo's :entric+lar -ilation

    0ene2its in A**cla##e# of CHF(asymptomaticto

    seere%; H/N; diabetic renal disease; improessx;

    mortality

    ACE-Is =05(#t-o#e%4 renal 2xn4 +4

    cou(h4 an(ioedema; C)I= intolerance4 0*renal a% stenosis4 pre(nancy4 ARF

    A&0s = +4 an(ioneurotic edema*osartan

    Efficac. NO/ e9ualACE-Is(for $t# intolerantto ACE"I#%

    $ortalitye#$< in $t# 67 seere systolic HF(EF 8)'%

    -0loc"ers = ,- cardiotoxicityof catecholamines; +1N1)&AA1; H&4 preload4 & a2terload; anti"i#c,emic4 anti",.$erten#i:e4 & anti"arr.,t,mic

    DRUG EFFECTS USES ADVERSE EFFECTS

    $etoprolo

    l

    Caredilol

    $ortality; improessx & surial;aderse remodelin(of ,eart; sudden

    cardiac death; ,o#$italiation#

    1ymptomaticHF; asymptomaticV-.#f/n (EF !"8)'%; a2teracute$I

    Can co"a-min 67 ACE-Is

    054 2ati(ue4 2luidretention4 HR4 heartbloc"C)I=asthma; A4 bloc"(+nle## $ace-%; ac+te

    car-iac decompensation; #e:ere 0

    4asodilators)4enodilators

    DRUG >A & EFFECTS USES ADVERSE EFFECTS

    Isosorbide

    dinitrate

    4enodilator= NO release(2% GCpreload&

    $4O.; $+lm< e-ema; coronar. VDmyocardialper2usion; arterial VDa2terload05

    Acute& chronicHF 67 myocardialischemia; orthopnea& 5N; nitrate#2 ,.-ralaine in ACE"I intolerant $t#

    H)A; orthostatic 05; H&

    )I= #.ner9i#tic 67 5EG-Is; a--iti:e67 ot,er :a#o-ilator#

    14

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    Hydralazine Arterial asodilator = NO synthesisa2terload Hydralazine2 nitrates= mortality 1*E-li"e synd%; fl+i- retention4 HRNitroprusside $ixedasodilator= preload& a2terload Acute cardiac decompression; hypertensieemer(encies; A)E= E/ce## 0

    15

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    TREAT>E3T F HEART FAIURE 5O1I/I4E INO/&O5ICAGE3TS +Inotropict,era$. = maymortality(except for di(oxin%; #ome +#e in re2ractoryCHF; NO/for +#e a# chronict,era$.

    o >.oc.te cA>0 = o$en# slo'in6ar- Ca.+c,annel+inotropy; Ca12stora(eb. SR+lusitropy(m.ocar-ial relaxation%i(italis #lycosides= ,- Na+)+-A/5asePNa+Qi& Na

    +)Ca .+e/c,an9e Net e22ect= more Ca.+aailable for lon9er -+rin9 A0contractility

    DRUG EFFECTS USES C3TRAI3DICATI3S

    i(oxi

    n

    Natriuresis; 1N1& &AA1;

    a(altone (atrial rate & A4C4%Normalizesarterial barore2lex

    Chronic symptomaticHF (if noade9uate responseto ACE-Is2

    diuretics2 -bloc"ers; combo 67 ACE"I# 2 -i+retic# if #/

    $er#i#t%; t/ A-2ib(for rate control%; -oe# NO/improesurial

    in CHF

    A-:ance-A4 bloc"4 H&or sic"

    sinus (67o $acin9%; 54Cs& 4-

    tach; +; ?5?#.n-< 67 A-2ib

    -a(onists= ,+ AC

    cA$5(2% 0phosphorylates Ca.+ch%

    Ca.+ in2lux

    FCC Gi:en I4only /oxicity = arrhythmiasDRUG EFFECTS USES

    obutamine 8-selectie (minor.&8%; 8H&4 FC0 & C T/ acute decompensated HF; intermittentt,era$. in chronicHFto sxopamine(A%

    *o'-o#e = 84in :i#cera4 heart; hi(h-o#e = 8FC

    4ery hi(h-o#e = 8VC05

    T/ acute decompensatedHF& shoc"

    0ipyridines =0DE"I# (5hosphodiesterase In,ibitor#%

    DRUG >A EFFECTS USES TICIT

    $ilrinone;Inamrinone ,- 5E-3

    brea"do'nof cA$5

    Contractility& asodilation T/ acute decompensated HF Arrhythmias

    >ana9ementof acute HFB Acute $I(27" $re"e/i#tin9 CHF% = t/ 67emer(ency reascularization(e:en if #+cce##f+l4 ac+te HF ma. -e:elo$

    o T,era$. (8I4ro+te% = -i+retic (2urosemide= >C%; A ordobutamine($t# 67 seere 05%; :a#o-ilator# (nitroprusside6 N#%

    Nesiritide(0N5 a(onist%VD; Coniaptanfor e+:olemic ,.$oten#ion ($t# 67

    AH% CC0s= C)Ifor acute HF

    1C (S+--en Car-iac Deat,% 5reentionB 8= G;-R;B$t# 67 lo' EF& symptomaticHF ,a:e e$i#o-e# of nonsustained 4-tacho $ost antiarrhythmic-r+9# ,a:e ,- inotropiceffect# & can ris"of #erio+# arr,.t,mia; e#$< ,i9, for 9ro+$# IA4 I04 & #ome III(#otalol%

    Amiodarone= noeffect on #+r:i:al in $t# 67 lo' EF& HF; +#e- to preent recurrent AFor #.m$tomatic :entric+lar arr,.t,mia#

    o IC= for . preentionof 1C from4-tach in $t# 67 ot,er6i#e (ood clinical 2xn &pro(nosis

    *o' outputHF = diastolic-.#f/n (hypertrophy& sti22ness; C4 EF o"% & systolic-.#f/n (e#$< post-$I4 C & EF8'%

    Com$en#ator. mec,ani#m# = Fran"-1tarlin( (intrin#ic%; neurohormonalre#$on#e (

    1N14 &AA14 & AH; reset barore2lex%; hypertrophy Sta9e A= @ris"for HF4 NO-i#ea#e or #/; 9oal# = t/H/N4 lipids&metabolic#.n-

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    orca#erinSelecti:e a9oni#t of "HT 1C"R;

    a$$etite6ei9,tA-+nct for o:er6ei9,t or obe#e $t# 67 2comorbi-itie#

    H7A4 URTI4 -iine##4 na+#eaC7I = $re9nanc.; D7I = SSRI#

    17

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    A3TIH0ERI0IDE>IC AGE3TSNiacin= .x**4 >xH*4 3x/#s(4**%4 & cholesterol (in VD & D% )I= hypotensionin $t# t/ 67 asodilators

    DRUG

    >A USES ADVERSE EFFECTS

    Niaci

    n

    in-# #5C&on a-i$oc.te#H1*li$ol.#i#FFA&

    /#s; ,- hepatic 4** production;

    tLof apoAIHD$O1/ e22ectiefor

    H*; t/ FH&

    FCH

    Cutaneous 2lushin((67 E"R; ta"e A1A priorto%;na+#ea4 predisposition to (out4 G4 hepatoxicity

    Fibrates= **4 3xH*4 >x/#s NO/for 2amilial,.$erchylomicronemia C)I= seerehepatic& renal-.#f/n R (allbladder-i#ea#e $t#

    DRUG >A USES ADVERSE EFFECTS

    #em2ibrozi

    l

    Feno2ibrate

    *i(andsfor nuclear-& 55A&-

    *5* transcriptionhydrolysisof

    /#sin C$s& 4**

    T/ disorders 6784** &

    dysbetalipoproteinemia;preentin( pancreatitisin $t# 67

    seere /#s

    S5in ra#,e#4 mil- GI -i#tre##; (allstone 2ormation&habdomyolysisin $t# ta5in9 bot, 2ibrates& statins)I= com$ete 67 coumarinfor

    00

    anticoa(ulation

    0ile Acid 1e9uestrants = 3x**4 H* NOe22ecton $t# 67 homozy(ous FH(NOf+nctional **-&s% Cholestyraminefor C. difficilem9mt

    DRUG >A USES ADVERSE EFFECTS

    Cholestyramine

    Colestipol

    in- bile aci-#7#alt#excretedin

    2eces

    bile acidconcx**4 .xH*4 .x/#s .benefit# = $t#hospitalizedfor in2luenzat,at 'ere on statins,a- >;B mortality:#A USES ADVERSE EFFECTS

    Atorastatin

    1imastatin

    5raastatin

    &osuastatin

    ,- H$#-CoA reductase=committe- #te$de noo

    cholesterol synthesis; 1=

    IC c,ole#terol

    **-&s

    T/ disorders67 **& cholesterol

    in A**,.$erli$o$roteinemia t.$e#

    ON*Mcla## of -r+9# to mortalityin

    8

    : .

    preention o2 C4

    &habdomyolysis= +ncommon; most o2tenin elderly F67 hi(h-o#e# or 6,en statins+#e- in combo67 ot,er# (e

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    19/31

    In $t# 67 $ree/i#tin9 ,.$ertri9l.ceri-emia4 ma. #er+m TG le:el#

    19

  • 7/25/2019 Test2 Chart

    20/31

    DRUGS AFFECTI3G D CTTI3GAnticoa(ulantsB Eno/a$arin=LMWH4Lovenox t,er direct thrombin-Is9i:en I4; t/ HIT; elimination = e$ir+-in (renal%; Ar9atroban (,e$atic%

    DRUG T0E & >A 0HAR>ACI3ETICS ADVERSE EFFECTS

    Heparin

    (UFH%

    Indirect thrombin inhibitors

    Allosteric enhancersof antithrombin=de(rades clottin( 2actor proteases4 e#$& ot,er#4 dietary 4it Antidote= 4it 8(phytonadione% 2 FF0

    &iaroxiban

    irect 2actor a inhibitor; U#e# =preents4/(after oint replacement%

    & embolismin $t# 67 non-alularA-2ib

    8x daily 5O;NOmonitorin9 nee-e-&enal& hepaticelimination

    /x&

    recurrenceof 4/& 5E

    0leedin((NOanti-ote%)I= CM53A>& 5-(pin,ibitor#

    abi(atran

    irect thrombin competitie inhibitor

    $O&E e22ectiet,an 'ar2arinfor stro"epreentionin $t# 67 non-alularA-2ib

    0I5O; NOmonitorin9 nee-e-

    0ro-r+9; 8renalelimination

    0leedin((NO antidote%

    C)I = $t# 67 mechanical,eart ales)I= 5-(ptran#$orter in,ibitor#

    Antiplatelet A(ents A5= ca+#e# platelet a((re(ation TT0 = T,rombotic T,romboc.to$enic 0+r$+ra IRR = Irre:er#ible

    DRUG >A USES ADVERSE EFFECTS

    Aspirin I&& acetylation of CO,- /A.synthesis 8prophylaxisof $I; .preentionin $t# 67 hxascular eents; 0CI

    Clopido(rel

    (Plavix%

    I&& bloc"adeof A5 &s(5.M8.%,-a((re(ation

    5rodru(,+b. CM5.C8()I& (enetic ariation%

    Recent$Ior stro"e; e#tabli#,e- 5A;AC1; 0CI; often +#e- 67 ASA & 00I

    0leedin(; //5; D7I = me$raole &ot,er 00I# ($anto$raole be#t c,oice%

    5rasu(rel 3e6 a9ent in samec,emical class as aboe; NO/affecte- b. 5>G; (enotype#tat+# lee-in9 ri#5/ica(relor &eersible bloc"adeof A5 &s; already actie U#e- for ACS; A1A-o#e $!1/8;; m()day; blee-in94 HR4 -.#$neaAbciximab I&& bloc"s#5 IIb)IIIa &("% fibrino9en cro##"lin5in9 Gi:en I4for 5CI(0erc+taneo+# coronar. inter:ention%

    Fibrinolytic ru(s= catalyzecon:er#ion of plasmino(enplasmin= #erine $rotea#e de(rades 2ibrin; A 9i:en I4

    DRUG >A USES & ADVERSE EFFECTS

    1trepto"inase Combines67 endo(enous actiator 0E4 #e:ere DVT4 ac+te >I; a#cen-in9 t,rombo$,lebiti#A7E = bleedin(; imm+ne re#$on#e to #tre$to5ina#e; antidote= aminocaproic acidAlteplase(tPA%4 Uro5ina#e Act# directly

    /A.& "HT = ca+#e# platelet a((re(ation &asoconstriction; Ca.+= lin5# clottin( 2actors(-carboxy(lutamate residues%actiatedcell# Coa(ulationca#ca-e = #tart# 67 interaction of /F(/issue Factor% & Factor 4II(TF0I in,ibit# t,i# interaction%; en- $ro-+ct = thrombin(IIa%

    20

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    o 5roteins C& 1= ,-cofactor#4a& 4IIIa HI/ tx= )C,e$arin4 startdirect thrombin inhibitor(-abi9atran% or 2ondaparinux

    Fibrinolysis= tissue plasmino(en actiatorcon:ert# plasmino(enplasmin 5AI; .Antiplasmin= ("% $la#min not a##oc< 67 clot#

    21

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    Antidotes & ru(s !sed in 0leedin( isorders 4it 8= NO/ e22ectiefor ,emorr,a9ic -iat,e#i# from li:er fail+re

    DRUG >A USES ADVERSE EFFECTS

    5rotamine sul2ate a#ic $rotamine 2 aci-ic ,e$arin#table #alt Antidote for heparin; 9i:en IV 37V4 04 ana$,.la/i#; bleedin(4it 8

    (phytonadione%Co-2actor-carboxylation#lu residueson

    2actorsII64II6 I6 4C4 1; la( timefor onset

    Antidotefor 'ar2arin; 9i:en to A**ne'bornsto $re:ent 4it de2%

    If I4 9i:en too2astdyspnea4

    chest& bac" pain4 death

    Aminocaproic acid in-# $la#mino9en & ,- conersionplasmin Antidotefor 2ibrinolytics; ,emo$,iliac#&is"for thrombosis; C7I = DIC

    esmopressin Factor 4IIIactiity; AHact%(analo9+e% Hemo#ta#i# in $t# 67 ,emo$,ilia A4 :OD *ess 1$ contractiont,an ADH

    Factor 4IIa(recomb% in-# 67 tissue 2actor,+ extrinsicpath Hemo#ta#i# in $t# 67 ,emo$,ilia4 VII -ef /hrombosis; ,.$er#en#iti:it.

    H0THAA>US & 0ITUITAR HR>3ES (HT"0 AIS%HT"0"GH A/i#B #H= polypeptide4 pulsatilerelea#e in sleep #hrelin= al#o #H#ecretion *aron d'ar2ism= #H-&mutationNOIGF"

    DRUG >A USES & 0HAR>ACI3ETICS ADVERSE EFFECTS

    1ermorelin #H&H ia(nostic(etiolo(yof short stature% = if $t 67 !-eficienc.4 a-minGH Sale a# Kanti-a(in(L

    1omatotropi

    n

    Recomb #HI#F-8

    #ecretion b. li:er

    T/ #H-dependent(ro'th retardation= bone (ro'th& cartila(e synthesis;t/ #H de2icientadults= lean m% mass4 6a#tin9 in HIV $t#; 9i:en 1C-ail.

    Children= scoliosisAdults= e-ema4 m.al9ia

    5e(isomant

    Selecti:e #H-&

    anta(onistI#F-8

    .nd -line; t/ acrome(aly(somatotropha-enoma in adults; in "ids(i(antism%

    in $t# 6,o ONK/respond7tolerateot,er t/; 9i:en 1C-ail.

    (5E#.late-

    tL%

    *ieren.me#; size

    of tumor(yearly $&I%

    1omatostatin ,- &elease#H4 insulin *imitedt,era$e+tic useb7c many e22ects& rapidly cleared; al#o ,- 5&*4 /1H Hyper(lycemia

    Octreotide

    1omatostatin analo(=potency6 #H"selectie

    T/ acrome(aly4 #I bleedin((#$lanc,nic bloo- flo6%4 secretory diarrhea4carcinoid syndrome4 & 4I5omas; 9i:en a# depot1Cinection monthly

    Nausea4 #I motility4

    #in+# bra-.car-ia

    HT"0"0rolactin A/i#B actotro$,# = tonic ,-b. A$ortal #.#tem disruption5&*= ,- #n&H release:(onadtrophsensitiityin2ertility

    DRUG >A USES & 0HAR>ACI3ETICS ADVERSE EFFECTS

    0romocriptin

    e

    Caber(oline

    A a(onists=er(ot-eri:< bind.-&s

    T/ hyperprolactinemia4 in2ertility4 & acrome(aly(

    t+mor size%; romocri$tine

    daily4 neuroleptic mali(nant #.n- (off"label%; Caber9oline.x)'ee"4

    nausea

    Nausea4 H7A4 ort,o#tatic

    0; psychmani2estations

    HT"0"T,.roi- A/i#B T,.roi- hormone replacement= e22ectiet,era$. for ,.$ot,.roi-i#m If 8

    = $t ,a#

    /1H leels

    DRUG

    T0E USES & 0HAR>ACI3ETICS ADVERSE EFFECTS

    /&H

    /1H

    TRH = synthetictripeptide; 9i:e I4

    ia(nosis hypothyroidismetiolo(y; if .= a-min /1Hthyroid

    ,ormone#; if 3= a-min /&H/1H; TRH tW = 8 min; /&H= al#o 5&*

    relea#e

    Nausea4 +r9e to urinate4 metallicta#te4 li9,t",ea-e-ne##4 tran#ient HT3

    HT"0"Re$ro-+cti:e A/i#B A** 3,ormone# ,a:e same & di22 "#+b+nit#; *H& hC#are nearlyidentical A**$re$# 9i:en 1Cor I$

    DRU T0E EFFECTS USES ADVERSE EFFECTS

    22

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    G

    F1H!ro2ollitropin= $+rifie-urineextract

    Follicle deelopment4 #teroi-o9ene#i#;(ameto(enesis

    Induce oulationin F 67 anoulation

    1to ,.$o9ona-otro$i#m4 0CS4obe#it. (& no re#$on#e to ot,er t/%;

    controlledo:ar. #tim+lation in A&/;t/ in2ertility

    Oarian hyperstimulation4

    ri#5 multiple$re9nancie#;H7A4 -e$re##ion4 e-ema;

    (ynecomastiain >*H

    *utropin al2a= recomb< Oulation tri((er; steroido(enesis(>7F%

    hC# 0+rifie-urine extract Action# :ia *H &s; +#e- insteadof *H

    23

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    SE HR>3ESGona-al Hormone S.nt,e#i# In,ibitor# Te#to#terone & e#tro9en (usually% = ,- #n&H4 *H4 & F1H In,ibin#("% FSH; acti:in(2% FSH

    DRUG T0E & EFFECTS USES ADVERSE EFFECTS

    *euprolide

    #oserelin

    #n&H a(onists= CON/IN!O!1-o#einitial,+;

    t,endesensitization,- *H : F1H release

    5remeno$a+#al F 67 adanced breast CA;le+$roli-e for prostate CA(effecti:e ascastration%4en-ometrio#i#4 precocious puberty& IVF

    Hot fla#,e#4 impotence4

    (ynecomastia4 libi-o;ri#5 of $& C4

    Finasterid

    e

    /ype II G-reductase competitieinhibitors,-

    local H/$ro-+ctionslo's$ro#tate(ro'th

    T/ 05H4 male pattern baldness*ibido & E; ,- $

    2etal#e/ -e:elo$ment

    *etrozoleAna#troole

    Aromatase competitieinhibitors

    estro(en;induce oulationb.

    ,- 2eedbac"T/ estro(en-drien metastatic breast CA(moree22ectiet,an 1E&$s%; I4F($t# t,at failclomi$,ene%

    3a+#ea4 fati9+e4 ,otfla#,e#; osteoporosis

    #anirelix#n&H anta(onist=preent *H sur(e;immediate

    Controlled oarian hyperstimulationin I4F

    1E&$s(Selecti:e Estro(enRece$tor >o-+lator#% = mixed a(onists)anta(onists; ER"& = tissue& li(anddependente#tro9en tar(et speci2icityDRUG EFFECTS USES ADVERSE EFFECTS

    /amoxi2en )/lo'er affinit. t,an e#tro9en; a(onistin endometrium4 bone Estro(en-drienbreast CA Hot fla#,e#; endometrial CA

    &aloxi2ene

    A(onist in boneON*M(NOeffect on endometriumNO

    $re-i#$o#ition to CA%;

    bone resorption;

    **le:el#

    Osteoporosisin postmeno$a+#al

    F; preentbreast CAin hi(h ris"$t#

    Hot fla#,e#4 37V;

    thromboembolic eents

    Clomiphen

    e

    Anta(onistin H/& ant% pituitaryrelie2of ,- 2eedbac"b.

    estro(en#n&H; partial a(onistin oaries2ollicle

    (ro'th

    F1H& *HInduces oulation

    (/I$IN#i# 5e.% in anoulatoryF

    $ultiple 2ollicles;

    oary

    size; #el-omHS (:#< F1H%

    Andro(en &eceptor Competitie Anta(onistsB 1pironolactone= al#o can in-+ce normal menstrual periods67 anoulatory hyperandro(enism

    DRUG EFFECTS USES ADVERSE EFFECTS

    Flutamide;ical+tami-eNonsteroidal; #ince ("% AR#GnRH4 +#e- '7 leuprolide $etastatic prostate CA; 0H #ynecomastia4 N)44

    hepatitis

    1pironolactone ,-Andro(en synthesis; mild anti-andro(en$ro$< T/ hirsutism4 perimeno$a+#al acne

    5ro(esterone(0G% &eceptor Competitie Anta(onist 5#& A&s= $O1/closely related 5#= s endometrium$roliferati:esecretory

    DRUG EFFECTS USES A7E

    $i2epriston

    e (&!->%

    eathof deciduablastocyst dies& detaches

    ,CGcor$+# l+te+m in:ol+te#5##.nt,e#i#8st trimester abortions(+#e- 67 misoprostolcontraction#%;

    t/ en-ometrio#i# & 0G"-e$en-ent CA; #Canta9oni#tExcess a(inal

    bleedin(

    H&/= +#e lo'estdosesfor shortesttime & #tart sooner(@onset% Estradiol= patch4 to$ical; $remarin = 0 Te#to#terone c.$ionate = I$

    DRUG EFFECTS USES ADVERSE EFFECTS

    5remarinCon@u(ated estro(ens= A*?AM167pro(estinin F 67 intact uterus

    &elieemenopausesx(hot 2lashes4UG atrophy4 & preent osteoporosis%

    N)44 $o#tmeno$a+#al blee-in94 edema6 breast2ullness4 mi(raines

    24

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    Fluoxymesteron

    e

    /estosterone deriatie9i:en 5O(normal te#to#terone CANK/b7c hi(h 8st

    passmetaboli#m%; muscle mass;

    bioa:ailabilit. transdermal(best%

    T/ hypo(onadism; libido4 #enile

    o#teo$oro#i#4 hereditary an(ioedema4

    breast CA

    F= masculinization 4 men#tr+al irre9+laritie#;C)I= pre(nancy; $= (ynecomastia4

    $ria$i#m4 impotence4 #$ermato9ene#i#4@aundice4 HCCids= premature epiphyseal closure

    25

    C i E $O1/ di l (E % (E % i l (E % 5 i d 2i i l b " h h bl di

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    ContraceptionB E#tro9en#B $O1/$otent = estradiol(E1% P e#trone (E% P estriol(E!% 5ro(estinde2iciency= latebrea"throu(h bleedin(

    DRUG EFFECTS USES ADVERSE EFFECTS

    Combination

    ,- #n&H4 *H4 & F1H#ecretion,- oulation; cerical

    mucous& endometrial s; PNN' effecti:e ta"en as directed

    (N1'%; mono" = constantamt; bi" & tri$,a#ic $re$# amt

    $ro9e#tin

    total amounta-min; *o'"-o#e estro(en(ethinyl

    estradiolor mestranol% = blee-in94 $otentiate# $ro9e#tin(A*?AM19i:en ') pro(estin%

    5ro(estin(norethindrone4 nor(estrel% = ("% o:+lation )"Q)'& $re9nanc. MN'; ne'er67 anti- (a% or andro(enicactCC infant -eat, 0reterm = ! 65#; $remat+re = lb# 3ormal = 8) 65# 0o#t"term = 81 65#; Xri#5 of meconi+m

    /.tocic# = for labor inductionor au(mentation abor = contraction# optional; Sta9e#B 8= cer:ical -ilation; -eli:er. of infant (.% & $lacenta (3%

    DRUG EFFECTS USES ADVERSE EFFECTS

    Oxytocin

    0oth&2orceof contractions;

    ON*Meffecti:e @endof $re9nanc.

    (dependent on oxytocin &s%

    *abor induction& au(mentation(:ia

    constant in2usion%; mil" Tlet-do'nU(:ia

    na#al #$ra.%; 8postpartum hemorrha(e

    HT3 cri#i#4Na+4 arr,.t,mia4 +terine

    r+$t+re4 fetal -eat,; C)I= fetal distress4abn%fetal $re#entation4 prior maor #+r9er.

    $isoprostol (5#E8% 5rosta(landinscan initiate laborANMtimein $re9nanc. (:#< o/.tocin%

    In-+ce labor4 ripen cerix(:a9inal in#ert% 37V4 -iarr,ea4 abnormal contraction#

    Carboprost (5#F.

    % ON*Mto #to$ postpartum bleedin( N)44diarrhea4 fe:er; C7I = a#t,ma

    $ethyler(onoineEr(ot al"aloid,+

    &sintense4

    prolon(edcontraction; NO/b.I4

    ON*Mfor control or preentionofpostpartum hemorrha(e

    Ac+te >I4 CVA4 an9ina4 HT34 bra-.car-ia;C7I = HT3 or Ra.na+-# #.n-rome

    /ocolytics= +#e- to delay preterm delieryhrs-days#o GC# can fetal l+n9 mat+rit.; al#o +#e- #o infant# in breec, $o#ition can be t+rne-DRUG EFFECTS USES ADVERSE EFFECTS

    Indomethacin(3SAID#% 0ro#ta9lan-in #.nt,e#i# = $O1/e22icacious@delayin( pretermbirt, 67 leastA7E OCfor 0T be2ore 3. '"s; m+#tmonitor 0DA to en#+re flo6 P #afe le:el $ayinci-ence of necrotiin9 enterocoliti#& neonatal renal in#+fficienc.Ni2edipine H5 CC0= S>"#electi:e; ("% SR Ca12relea#e T/ 0T 3.-3> '"s9e#tation Fl+#,in94 -iine##4 H7A

    /erbutaline.-a(onist= cA>0(2% 0A>C$,o#$,or.lationS> rela/ation

    Dela. labor for 8Q ,r# (limite- b.

    desensitization%Tremor4 $al$itation#4 04 $+lm< e-ema4HR; can cross$lacenta

    $( sul2ateUn5no6n >A; com$ete# 67 Ca12& #tabilie#

    cell membrane; inci-ence of cerebral $al#.OCfor preention o2 eclampsia; t/

    unpleasantfor $t#I distress4 sensation o2 oerheatin(4

    s'eatin(4 37V4 H7A4 HR; C7I = >GNitro(lycerin Ra$i-l. rela/ :eno+# & +terine S> 3ot eno+9, e:i-ence for 0T Diine##4 H7A

    8R -hydroxypro(esterone caproate= 9i:en I> 6ee5l. T/ in .ndtrimester,el$# ris"of preterm birthin hi(h ris" pts

    26

    I3SUI3

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    I3SUI3= all subcutaneous(1C% inection# T.$e 8(I$% = seere insulinopenia-+e to loss o2 cells; dependenton exo(enousin#+lin to $re:ent DA & -eat, T.$e .(NI$% = $C; insulin resistance& secretory de2ect; NO/dependenton e/o9eno+#4 ma. re*+ire in $erio-# of stressor if re2ractoryDRUG 0R0ERTIES 0 D EFFECTS F I3SUI3 THER

    *ispro(Humalog%

    &apid-actin(= mo-ification# preent

    2ormationof hexamers

    absorption

    ratefrom 1Cinection #ite

    ;%.

    G

    )4 b+tform# microprecipitatea2ter 1Cinection

    etemir*on(-actin(= fa#ter ab#or$tion4 b+t slo'releasefrom bindin(to albumin "1

    #luca(on=

    secretionin $t# 67 insulin de2iciency; ener(y mobilization4 rapid

    (lyco(enolysis& (luconeo(enesis; emer(encytx hypo(lycemia

    DRUGS FR T0E 1 D> = all orala9ent# exceptincretin mimetic# & am.lin analo9.nd#eneration1ul2onylureas(SU#% = in#+linsecreta(o(ue; 1n-9eneration -r+9# D8;; times more potentt,an 8st9eneration (ionic bindin()I%

    DRUG >A4 EFFECTS4 & 0HAR>ACI3ETICS ADVERSE EFFECTS

    #lipizide

    #lyburide

    #limepirid

    e

    ,- A/5-dependent + ch%on -cellsdepolarizationPCa .+ Qi

    insulin release; can insulin resistance; HbA8c; NO/e22ectie

    in t/ /ype 8 $(NO2xn"cell#%; hi(hly boundto albumin(non-ionicbin-in9%; 0O/Hhepatic& renalelimination

    Hypo(lycemia4 'ei(ht (ain4 GI r/n#4 #5in ra#,e#; C7I =

    pre(nancy

    Hypo(lycemia= sul2onamides(displace1!sfrom albumin%;

    H1bloc5er# (metaboli#m%; "bloc5er#?orsenin( (lycemic control= rifam$in; t,iai-e#; GC#

    $e(litinides = in#+lin secreta(o(ue; postprandial 0# le:el; more YY t,an SU#; alternatieto SU# if $t ,a# im$aire- renal 2xnor eats sporadically

    DRUG >A4 EFFECTS4 & 0HAR>ACI3ETICS ADVERSE EFFECTS

    &epa(linid

    e

    ,- A/5-dependent+channels@#ite di22erentfrom 1!s; ta5en be2ore eachmeal (rapid onset& short duration%; hepaticmetaboli#m b. CM5>G;

    Hypo(lycemia4 'ei(ht (ain; )I= #er+m le:el#

    ma. be

    b. erythromycin& b. ri2ampin

    -#lucosidase Inhibitors = antihyper(lycemiceffect;

    postprandial (lucose; nota# effecti:e# a# ot,er cla##e#

    DRUG >A4 EFFECTS4 & 0HAR>ACI3ETICS ADVERSE EFFECTS

    Acarbos

    e

    Hydrolysis rate of disaccharides& complex carbsdelayin(

    productionof (lucose& ot,er monosaccharides; renalelimination

    #I e22ectsb7c 2ermentationof unabsorbed carbs in colon;hepatotoxicity; C)I= $t# 67 renal impairment

    27

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    28

    0i(uanide in#+lin sensitizer; 8st line a9ent; $O1/ 'idely used -r+9 for type . $; antihyper(lycemic effect re9uires $re#ence of insulin

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    0i(uanide = in#+lin sensitizer; 8st -linea9ent; $O1/ 'idely used-r+9 for type . $; antihyper(lycemiceffect re9uires$re#ence of insulin

    DRUG >A4 EFFECTS4 & 0HAR>ACI3ETICS ADVERSE EFFECTS

    $et2ormin("lucop#age%

    ,+ A$5(cA$5"acti:ate- protein"inase%hepatic (lucose

    output& insulin sensitiity; /#s& **; renalelimination

    Comparable e22icacyto 1!s; ca+#e# 'ei(ht loss:#< (ain#een 67 1!s

    ose-related #I effect# (nausea4 metallic taste%; potentialforlactic acidosis; C)I= pre(nancy4 alcoholism4 -i#ea#e# t,atpredisposeto acidosis(C0D4 CHF%; impairedrenal 2xn

    /hiazolidinediones (TD#% K-(litazonesL= in#+lin sensitizers; ma. ris" o2 $I(FDA restricteduseof rosi(litazone%; #,o+l- monitorlier 2xn

    DRUG >A4 EFFECTS4 & 0HAR>ACI3ETICS ADVERSE EFFECTS

    5io(litazone&osi(litazon

    e

    #ene expressionb. bindin( to 55A&

    cell responsesto insulin

    Insulin resistanceperipheralti##+e#; HbAc5io9litaone ,a# bene2icialeffect# on #er+m lipids(rosi" ,a# A)E%Hepaticmetaboli#m = bothC0.C4 pio9litaone C03A>al#o

    Fluid retention4 edema4 & 'ei(ht (ain; bone losse#$al#o de(rades other$e$ti-e#

    Amylin Analo(= 9i:en 1C67 mealto postprandial (lucose; ad@unctietherapyfor type 8:.$ Amylin= #+b#tance releasedfrom cells

    DRUG EFFECTS ADVERSE EFFECTS

    5ramlintide(S$mlin% ,- #luca(on release; delays(astric emptyin( N)44 H)A4 anorexia;

    ris"of hypo(lycemia6,en +#e- 67 insulin

    THRIDDRUG EFFECTS USES ADVERSE EFFECTS

    *eothyroxine Synthroid= #.nt,etic />; lon(tW; conertedT! OChypothyroidism 3er:o+#ne##4 HR4 'ei(ht loss4 T*iothyronine /3(most$otent%; 2aster actin(4 shorttW; 2eedbac" ,-of /1H $yxedema coma(T8% 0o##ible a-:er#e car-iac effect#

    $ethimazole,- /3)/>synthesisb. competin(67 /#(t,.ro9lob+lin%

    ,- peroxidase; delayedon#et (65#%Hyperthyroidism Ra#,4 na+#ea4 GI -i#tre##4 (oiter4

    cretinismin 2etus(C)I%

    5ropylthiouracil5/!=samea# met,imiaole4 b+t onl. 8)8;tha# potent,- peripheral conersionof T8T!(alsobloc5e- b. #Cs%

    Can +#e in pre(nancy(lo' dose%; al#o thyroid storm

    Iodides(3a4 4 I1% Hi9, -o#e#,-T!7T8secretion; rapid actin(; tolerance -e:elo$# Glan- #ie be2ore sur(ery; thyroid storm

    29

    At l l 5 l l l ti bl " t l i - - b - i t OC th id t

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    Atenolol 5ropranolol= non"#electi:e; -bloc"erscontrol #/ in-+ce- b. a-rener9ic tone; OC thyroid storm838I= permanenthypot,.roi-i#m

    30

    3E >I3ERA H>ESTASIS

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    3E >I3ERA H>ESTASISHormone# T,at Affect Ca12Homeo#ta#i# 3et Ca12ab#or$tion = M"1)'; 3et 08= M)' At #tea-. #tate4 renal e/cretion = ab#or$tion

    HR>3E

    0R0ERTIES ACTI3S 0ATHG

    5/H

    0ol.$e$ti-e #ecrete- from chie2 cell# in

    parathyroidin re#$on#e to lo' Ca.+:erall =

    Ca.+4 5O>$la#ma leels; idneys= Ca12& 08reabsorption; calcitriol(actieVit D% #.nt,e#i# (Ca.+from GI%; 0oneB 5rolon(ed

    0THRA3osteoclasts; brie20THosteoblast-ifferentiationanabolic

    4itamin

    R-dehydroCVit 3(cholecalciferol% in

    s"in

    .G-,OH D!(calci2erol% in lier

    86.G-,OH.3(calcitriol% in "idney

    :erall =Ca.+4 5O>

    #I= Ca12& 08upta"e; GC# anta9onie effect# @GI0one resorption(osteoclastZ & act%

    Deficienc.so2tenin(of bones;

    in "ids= ric"ets;in adults= osteomalacia

    Calcitonin0ol.$e$ti-e #ecrete- from para2ollicular cell# of thyroidin re#$on#e to hi(h Ca.+

    :erall =Ca.+4 5O>

    0one resorptionb. ("% o#teocla#t#

    E/ce## = fl+#,in94 na+#ea

    HypercalcemiaB Ca+#e# = Vit D; o:ertreatment 67 t,iai-e# S/ = K9roan#4 moan#4 bone#4 #tone#4 $#.c,iatric o:ertone#L HypocalcemiaB Ca+#e# = ,.$o$arat,.roi-i#m4 renal i##+e#4 $,enobarbital S/ = m< tetan.4 con:+l#ion#4 abnormal be,a:ior

    T/ Hypercalcemia= if #e:ere eno+9, $t ,a# #/&E

    o Alendronate= slo'sbone turnoer4 ("% formation79ro6t,7-i##ol+tion of cr.#tal#; a$$ro:e- for $re:ention & t/ o#teo$oro#i# 5hosphate salts= bone 2ormation; ta5en 0; 2astest 'ayto Ca124 b+t ,aar-o+#; +#e- ON*Mif ot,er abo:e met,o-# fail

    T/ HypocalcemiaB /hiazides= Ca.+excretion 4it = Ca12+$ta5e @GI; +#e- for ,.$o$arat,.roi-i#m4 Vit D -eficienc.4 malab#or$tion Directl. $la#ma Ca12B Ca (luconate= OCfor seere,.$ocalcemia; 9i:en I4

    o Ca carbonate= con:erte-Ca12#alt# in #tomac, b. HClconstipation; for mild,.$ocalcemia & maintenancet,era$.

    #teo$oro#i# = >C in postmenopausal F t,er ca+#e# = #Cs4 alcohol4 1$OIN# $a@orityof remodelin(in trabecular(NO/cortical% bone

    DRUG EFFECTS & 0R0ERTIES USES ADVERSE EFFECTS

    Alendronate(Fosamax%

    0isphosphonate= concentratein bone matri/

    more resistantto osteoclastre#or$tion; 0$

    more t,an ralo/ifene; orallyacti:e4 *O?bioa:ail