urugs for Perpes

urug MCA Cllnlcal uses SL noLes

Acyclovlr rodrug LhaL ls monophosphorylaLed by vlral Lhymldlne klnase(1k) Lhen
furLher blacLlvaLed by hosLcell klnases Lo AcyclovlrLrl ls boLh a
subsLraLe for for vlral unA olymerase when lncorporaLed lnLo ! unA
molecule lL acLs as a chaln LermlnaLor bec lL lacks ! rlbosyl 3' CP grp
PSv1 PSv2
vZv
nC1 # CMv bec lL lacks a speclflc vlral 1k
skln lrrlLaLlon (C)
CrysLalllne nephropaLhy rapld lnfuslon
Cl1 upseL nC1 hemaLoLoxlc
neuroLoxlclLy (C) (Lremor selzures)
ool oral l use valacyclovlr (valyl esLer)
8enally excreLed d ln renal fallure
lamclclovlr(C) meL by aceLylaLlonenclclovlr(1)
enclclovlr unA polymerase nC1 chaln LermlnaLor
Canclclovlr rodrug ln lnlLlal sLep ls vlralspeclflc lnvolves 1k ln PSv
a phosphoLransferase(uL97) ln CMv 1rl form vlral unA polymerase
buL does nC1 cause chaln LermlnaLlon
CMv lnduced reLlnlLls pneumonla (uCC)
Plv lnfecLed paLlenL CMvreLlnlLls
lmmunosuppresed Lherapy (LranspalanL)
PSvvZv
8MS(anemla AgranulocyLosls
LhrombocyLopenla)
CrysLallurla
Selzures ln (C)
Cl Zldovudlne granulocyLopenla
mipenem-cilastatin ( Selzures)
8enally excreLed d ln renal fallure
valganclclovlr oral l
Cldofovlr CyLoslne analogue acLlvaLed by hosL enzymes( does nC1 requlre v1k) Lo
1rl vlral unA synLhesls
# Acyclovlr Canclclovlr reslsLanL sLralns nephroLoxlclLy
neuLropenla
MeLabollc acldosls
Ccular hypoLony lnLravlLreal
rlsk by hydration & Probenecid adm.
loscarneL Syn nonnucleoslde analogue of pyrophosphaLe LhaL blnds dlrecLly Lo !
pyrophosphaLe blndlng slLe vlral unA or 8nA polymerase

Also Plv 81
2
nd
llne ln CMv reLlnlLls ln
lmmunocompromlsed paLlenLs
AcyclovlrreslsLanL PSv
# 1k deflclenL sLralns(dL nC1 requlre )
8enal LoxlclLy by hydraLlon
Anemla fever n u
PypocalcemlaMg k manlfesLed by
Selzures parasLhesla arryLhmlas
SynerglsLlc Canclclovlr

dL dlvalenL caLlon celaLlon
deposlLed ln bone LeeLh
lomlvlrsen ls an anLlsense ollgonucleoLlde dlrecLed # CMv m8nA (adm lnLravlLreally) CMv reLlnlLls lrlLls vlrlLls vlslon change lC
8lbavlrln noL clear buL
Mono lM dehydrogenase
Tri- viral RNA polymerase & end-capping of viral RNA.
8esplraLory syncyLlal vlrus (aerosol)
lnfluenza A 8
Lassa fever PanLa fever
PepaLlLs 8 C ( lnld )
PaemolyLlc anemla
Cl1 upseL
8esplraLory lrrlLaLlon
Con[uncLlvlLls

ldoxurldlne hosphorylaLed meL lncorporaLes lnLo unA causlng sLrand breaks PS heraLlLls (1) Ldema around Lhe eye wlLh paln
rurlLls
lnflammaLlon
used Loplcally dL sever sysLemlc LoxlclLy
vldarablne Perpes keraLlLls Cl1 lrrlLaLlon
arasLheslas
1remors convulslons
PepaLlc dysfuncLlon
used Loplcally dL rapld lnacLlvaLlon marked Loxlc
poLenLlal

urugs for lnfluenza
class drugs MCA Cllnlcal uses SL noLes
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AmanLadlne
8lmanLadlne
revenL vlral peneLraLlon uncoaLlng
8y blocklng Lhe P2 lon channel (M2)
lnfluenza A vlrus
( sympLoms duraLlon lf glven
ln 48 hrs afLer conLacL)
AnLlparklnsonlan
CnS effecLs (uepresslon nervousness lnsomnla selzures)
ALroplnellke perlpheral effecLs
Llvedo reLlcularls
CPl
CrLhosLaLlc hypoLenslon
urlnary reLenslon
8lmanLadlne
Longer L1/2
lewer CnS effecLs x1 selzures
no need for dose ad[usLmenL ln renal fallure
Cl ln hepaLlc dysfuncLlon

8oLh excreLed vla Lhe kldney 8lmanLadlne only ls
hepaLlcally meLabollsed
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e

CselLamlvlr
Zanamlvlr
lnfluenza vlrus neuramlndase Lhus
prevenL ! release of newely formed
vlrlons

1hey are LranslLlonsLaLe analoges of slallc
acld subsLraLe
lnfluenza A 8 vlruses Cl1 upseL n CselLamlvlr (C)

8esplraLory LracL lrrlLaLlon Zanamavlr (lnhalaLlon)
CselLamlvlr ls a prodrug ls acLlvaLed ln ! llver

Zanamavlr ls nC1 acLlvaLed and adm by lnhalaLlon
or lnLranasally

8oLh excreLed 8eanally



AnLl Plv drugs
Class urugs MCA SL noLes
n81l Zldovudlne(AZ1)
SLavudlne(d41)
uldanoslne(ddl)
Lamlvudlne(31C)
ZalclLablne(ddc)
Abacavlr(A8C)
1enofovlr(1ul)
nucleoslde Plv 81
Prodrugs Tri
8MS ( ln AZ1 31C)
(granulocyLopenla anemla)
erlpheral neuropaLhy ( d41)
LacLlc acldosls
ancreaLlLs ( dd)

u41 lacLlc acldosls hepatic steatosis.
dd Optic neuritis.
3TC hyperpigmentation of soles & palms
ABC Fatal hypersensitivity Rx HALA genetic screaning
(Fever + Rash,GT sym., Malasia & Resp. Distress)
TDF Fanconi's syndrome (Acute kidney failure)

nn81l nevlraplne(nv)
uelavlrldlne(uLv)
Lfavlrenz(Llv)
LnLravlrlne
non nucleaslde 81l


# HV resistant.
8ashfever nausea headach All + C? 3A4 x1 uelavlrldlne C?430
CnS LoxlclLy ( dlzzlnessP vlvld dreams loss of conc) Lfavlrenz
plasma cholesLerol Lfavlrenz
Adv over n81l
no effecL on ! hosLblood formlng elemenLs
uo nC1 requlre for Lhelr acLlvaLlon
nevlLaplne verLlcal Lransmlsslon
roLease lnhlblLors 8lLonavlr(81v)
Saqulnavlr(SCv)
lndlnavlr(luv)
nelflnavlr(nlv)
losamprenavlr(lAv)
Loplnavlr(Lvr)
ALazanavlr(A1Z)
1lpranavlr(1v)
uarunavlr(u8v)
araLheslanvu
MeLabollc dlsorders (Pyper all)
LlpodysLrophy
8reasL enalrgmenL
All Cyp430 x1 1lpranavlr

8lLonavlr LasLe dlsLurbance
Saqulnavlr 8hlnlLls
lndlnavlr nephrollLhlasls
nelflnavlr ularrhea ( conLrolled by Loperamlde)
losamprenavlr Sever rash
ALazanavlr !aundlce hyperblllrublnemla
rolngs ! 8 lnLerval P8
1lpranavlr laLal hepaLlLls
8lLonavlr harmacoklneLlc boosLer or enhancer (poLenL C?3A4
)
lndlnavlr hlghesL lnsulln reslsLance
nelflnavlr favourable safeLy proflle ln pregnancy
ALazanavlr nC lypodlsLrophy nC meLabollc dlsorder
Cl ls anLaclds as oral absorpLlon requlre
acldlc envlronmenL
uarunavlr # ls reslsLanL