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156 Cards in this Set

  • Front
  • Back
Ampho B MOA
binds to ergosterol and creates pores

relative selectivity ergosterol> our cholesterol
DOC for life-threatening systemic fungal infections
Ampho B
whats first line for invasive Aspergillis
Ampho B

but Voriconazole used more
what is Ampho B used for?
acute cryptococcus neoformins meningitis
Ampho ADRs
rev Nephrotoxic
no more than 4g/tx episode

causes hypoK
anemia
how to Tx infusion related ADR's of Ampho?
tx thrombophlebitis
meperidine, cortisol, Ibuprofen

-inject heparin along with ampho
is Ampho cidial or static?
cidal in vitro
how is Ampho eliminated/metab
Unkown
t1/2=15 days
Nystatin MOA
like Ampho-pokes holes
fungicial
uses of nystatin
candidiasis(thrush)
fungal diarrhea
nystatin toxic when given...?
systemically
oral is ok
which drugs are polyene antifungals?
ampho B
nystatin
Anti-metab antifungal drug?
flucytosine
Flucytosine MOA

static or cidal?
converted to 5-FU only in fungal cells-inhibits thymidylate synthetase

static
Flucocytosine slectivity, how?
only fungal cells have a cytosine permease-brings drug into cell
-cytosine deaminase converts drug to 5-FU(only in fungus)
Flucytosine suse?
tx's cryptococcal meningitis
used with amphoB
flucytosine resistance
develops rapidly-never use as the singular agent
Flucytosine ADR's
bacteria convert it to 5-FU in the intestine-abs in body and inhibits OUR thymidylate synthetase
Flucytosine result of ADR's
teratogenic
bone marrow depression
hair loss
azole has most CYP inhib
least?
most-ketoconazole
least-fluconazole
azole MOA
blocks the synthesis of ergosterol-inhibits enzyme sterol 14-alpha-demethylase
what should not be used with azole?
ampho B NOT to be used concomitantly
azole cidal or static?
static, but at hight dosescan be cidal
fluconazole DOC for?
oropharynheal/systemic candida
which azoles have broadest antifungal spectrums
voriconazole
posaconazole
which drugs is 2nd line for aspergillus
itraconazole
what is DOC for invasive aspergillus
voriconazole
posaconazole covers?
good-candida + aspergillus

only agent for-zygomycetes
DOC for treating cushings disease?
ketoconazole
posaconazole should be taken how?
with fatty meal
tx for chronic suppression cryptococcal neoformans meningitis
fluconazole
which azole is only excreted thry kidney
fluconazole
what inhibits P-glycoprotein
keto and fluconazole
ketoconazole
absorption?
CNS penet?
ab-requires acidic environment
tk with coke
decrease abs with food
No CNS penetration
Fluconzole
abs?
CNS?
abs-unaffected by food
CNS-yes
Itraconazole
abs
CNS
requires acidic environ.
abs incr. with food in caps
abs dec with food in oral soln
which 2 antifungals can cross BBB
FF
Fluconazole + flucytosine
Vori inhibits
2C19
2C9
3A4
Cyp inhib by potentcy
keto>itra=vori>>flu
ketoconazole SE
inhib formation of testosterone- no hardons, big tities, N/V
monitor what in all AZOLES?
LFTs-for hepatotoxicity
HTN + fluid retention in all Azoles
Fluconazole SE
rash in immunosupp. pt's
Vori SE
visual disturbances
itraconazole SE
may exacerbate or cause HF
which azoles are teratogenic
ALL
Griseofulvin is an inhib of what?
NOTHING
ITS A INDUCER!!!!
uses for griseofulvin
onychomycosis-tx for 6 months
griseofulvin
abs
SE
abs-increased with fatty meals + microcrystallne formulation

SE-photosens. HA/insomnia memory impairment
terbinafine MOA
cidal or static?
inhibits squalene oxidase-results in decreased synthesis of ergosterol

cidal
terbinafine uses
onychomycosis-3months
terbinafine AE
taste disturbances
hemotopoetic effects-pancytopenia, neutropenia
changes in ocular lens + retina
Bufenatine, Naftifine
MOA?
like terbinafine
ciclopirox MOA
chelates AL + Fe-inhibits metal dep. enzymes necessary for degradtion of toxic peroxides
capsofungin
MOA
echinocandins
blocks synthesis of B(1.3) cell wall
capsofungin biggest use
fluconazole resistant candida
capsofungin elimination?
absorb?
primarily feces

IV no oral
capsofungin ADR
releases histamine-warmth/vasodil.
micafungin and anidulofungin
same as capsofungin

use micafungin-candidia prophylaxis in HSCT(stem cell transplant)
prevention of viral pen or uncoating
amantadine, rimantadine
inhib of viral specific enzymes
all nucleoside analogs
steps of viral infection
absorption
penetration
uncoating
translation
replication
release
drugs interfering with uncoating
amantadine
rimantadine
Amantadine/rimantadine
MOA
inhibit viral M2 protein->prevents dissociation (uncoating)
amanaadines/riman uses
prophylaxis and tx of influenza A with 24-48H
Amantadine/Rim SE
anticholinergic effects(rim has less)
N/V
encephalopathy with amantadine(renal failue)
when should we use amantadine?
when not?
use in liver failure
not in renal failue
when should we use rimantadine
when not?
use in kideny failure
not in liver
tadines are C/I when?
pregnancy
Neuraminidase inhib.
zanamivir
oseltamivir
zanamivir/oseltamivir
MOA
dec. release of infected cell particles, increases form of viral aggregates
uses of amivir's
for influenza A + B
amivirs used how?
zanamvir is inhaled

oseltamivir is ORAL prodrug
what is oseltamivir DOC for
avian "bird" flu
IFN-alpha MOA
induces synthesis of TIPS, slectively inhibits translation of viral mRNA

activates macros and natural killer lymphocytes
INF-alpha uses
Hep B+HepC, haircell leukemia, Karposi
INF-alpha SE
flu, fatigue, depression
guanosine analogs
acyclovir, valacyclovir, ganciclovir, pencyclovir, ribavirin
thymidine analogs
idoxuridine, trifluridine, cidofovir
adenosine analog
vidarabine
cytosine analogs
cytarabine
acyclovir uses
slective toxicity->only herpes infected cells

IV-DOC for serious infections
Acyclovir SE
crystalline nephropathy-must hydrate

burning sensation when topical
Valacyclovir
prodrug of acyclovir(prodrug)

esterified with valine
famciclovir
penciclovir
fam-prodrug of pen
pen is active form
hydrolysis to active form in liver + small intestine

pen is NOT a side chain terminator-its a DNA poly inhib.
fam
pen
uses
localized herpes zoster-give within 72H
recurrent genital herpes in immunoCOMPETENT pts
Ganciclovir
MOA
admined IV
comp inhib of DNA poly. and a chain term.
-undergoes slow catabolism
whats prob with ganciclovir
incorporated into human DNA also
valganciclovir
oral prodrug of ganciclovir
ganciclovir uses
CMV retinitis
DOC for any CMV virus
ganciclovir SE
myelosuppresion
seizures--gancic is worst
retinal detachment
mutagenic and carcinogenic
Foscarnet MOA
not a nucleoside analogue
NO activation req. by viral or host kinases
foscarnet uses
how is it taken?
Epstein-Barr
ganciclovir-resistant CMV

IV-poor oral bioavail.
Foscarnet SE
electrolyte disturbances
nephrotoxic
N/V(47%)-WORST antiviral
cidofovir MOA
inhib and substrate for DNA poly.
does not need activation by viral Thymidalye kinase
cidofovir admin?
SE
IV

nephrotoxic(give with probenacid)
ocular problems
idoxuridine MOA
NOT a side termin
puts kinks into DNA-susceptible for breaking
idoxuridine uses
topically only
herpes of eye
idoxuridine SE
corneal + conjuctival ulceration and change
trifluridine MOA
mech unkown
rev. inhibits thymidylate synthetase
trifluridine use
SE
topically only-herpes keratitis
DOC cuz its LEAST toxic

palpebral edema
Ribavirin MOA
interferes with IMP dehydrogenase-required for synthesis of guanosine
ribavirin is DOC for?
how do you give ribavirin
respiratory syncytial virus

aerosol-requires special nebulizing dose

also used with INF-Hep C
Adefovir MOA
nucleoTIDE analog-active form is diphosphate
serves as chain termin.
tri-P like
Adefovir uses
SE
Chronic active Hep B

severe hepatitis exacerbation when discontinued
Nephrotoxic
Nucleoside Reverse Transcriptase Inhib.(NRTIs) gen info
all are prodrugs->must be converted to triphosphates
3P's are added by host kinases
-chain terminators
NRTI's never give as?
monotherapy
Zidovudine(AZT)
moa
triphos-incorp in to viral DNA

monophos-comp inhib of host TK
Zidovudine ADR
HEMATOLOGICAL toxicites-myelosuppresion
panctyopenia-after 14 weeks of tx
asethnia-muscle weakness
Zidovudine interactions
antagonizes actions of stavudine, ribavirin

with ganciclovir-may cause additive myelosupp but NOT a C/I
Didanosine(DDI) MOA
incorp into DNA-chain terminator
highly selective
DDI kinetics
degrades in acid
caution with quinolones/tetracyclines
MUST take on EMPTY stomach
DDI adr's
pancreatitis-WORST among NRTI
peripheral neuropathy-all NRTI with d in it do this
caution if pentamadine also given
Zalcitabine(ddC) MOA
least potent NRTI
no longer marketed

severe peripheral neuropathy
oral/esophageal ulcers
STAVUDINE(D4T) ADR
highest incidence of lactic acidosis + hepatic steatosis
highest lipotrophy among NRTI

hyperlipidemia
stavudine interctions
interacts with zidovudine, zid inhibits hosts TK, which Stav needs to become activated
Lamivudine(3TC) adr
NO major toxicites-1st breakthru drug

never use alone(only a single point mutation=resistance)
Lamivudine interactions
synergistic with zidovudine
AZT+Lami=combivir
AZT +Lami+Abacavir=Trizivir
Abacavir+Lami=epzicom
Abacavir ADR
hypersent. reaction

if hypersent..dont ever go back->hypotension, resp distress
Emtricitabine MOA
a QD fluorinated lamivudine

emtric + tenofovir=truvada
truvada+efavirenz=atripla
NucleoTIDE reverse transcriptase inhib.
tenofovir
tenofovir MOA
doesnt need to add 1st P
chain termin
dosed QD
tenofovir ADR
well tolerated
renal insuff/fanconi syndrome
decreae in mineral density/osteomalacia
Non-nucleoside rev. transc. inhib.(NNRTI's)
MOA
inhib thru allosteric inhib following binding to enzyme at regions REMOTE fromactive site
NNRTI class toxicites
Rash-nevirapine most likely
LFT elevations
resistance for NNRTIs
a single mutation causes resistance to 3 of the NNRTI's
Nevirapine
inhib or induces?
se
induces CYP3A4

most likely to cause rash, elevated LFTs
Niviraprine-more severe hepatotoxic
may cause withdrawls if pt on methadone
Delaviradine
rasies levels of protease inhib
least potent NNRTI
TID dosing
Efavirenz
MOST potent of NNRTIs
QD dosing
inducer and inhib of CYP450
Efavirenz ADR
pen CNS-nightmares, vivid dreams, dizziness, conf, hallucinations

do not use in 1st trimester of preg
Etravirine abs
inducer or inhib?
admin with meal to enhance absorpt. (fasting reduces abs by 50%)

induces 3A4 + INHIB 2C9, 2C19
Etravirine uses
treatment-resistent patients
BID dosing
Protease inhib class MOA
protease diffs from human protease-ours has aspartate

bind non-cov-thus are reversible inhib

NEVER mono therapy
PI class toxicities
dislipemias + changes in fat distrub.->protease paunch
hyperchloesterolemia insulin resist.
GI interolance
PIs are inducers or inhib?
inhibitors
Saquinavir
LEAST potent PI
ALWAYS comboed with ritonavir(cuz ritonavir inhib metabolism of saq)
ritonavir
potent inhibtor of 3A4
caps must be refrigerated
ritonavir ADRs
circumoral parasthesias
taste perversion with liquid formulation
SEVERE nausea
Indinavir
ADR's
Q 8 H, NOT TID(???) wtf?
nephrolithiasis-avoid by hydration
hyperbilirubinemia
Nelfinavir ADR
diarrhea + loose stools-use loperamide
Never finish going to the bathroom
fosamprenavir
abs?
allergy?
high fat meals decrease abs
watch in sulfa allergy
atazanavir
is prefereed PI
needs acid for dissolution
atazanavir ADR
indirect hyperbilrubinemia
prolong PR interval
lowest incidence of hyperlipidemia-advantage
lopinavir/ritonavir
recc. PI in preg.
tipranavir and darunavir
newest PI
must be comboed with ritonovir
which drugs watch out for if sulfa allergy?
fosamprenavir
tipranavir
darunavir
tipranavir toxicities
severe hepatotoxic including fatalities or cerebreal hemorrhage
NOT preferred agent
darunavir
better tolerated
new onset of diabetes, hyperglycemia NOT seen with darunavir like most PI's
viral infusion inhibitor
enfuviritide
enfuviritide MOA
fusion inhibtor
very expensive(last line)
maraviroc
CCR5 antagonist
not all HIV strands need ccr5 to bind-so test pt first
maraviroc uses
taken how?
last line
for tx experienced pts

PO
maraviroc interaction with?
Saint johns wart
decreases maraviroc serum conc.
raltegravir
integrase inhib
slows adv of HIV by blocking integrase enzyme
raltegravir SE
associated with increase in CPK, myopathy
hydroxyurea MOA
no direct anti-viral activity
inhib cellular ribonucleotide reducatase
-arrests cell in GI prior to DNA synthesis-depletes dNTP pool
agents dosed qd
LATEE
Lamivudine
Atazanavir
Tenofovir
Emtricitabine
Efavirenz