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156 Cards in this Set
- Front
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Ampho B MOA
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binds to ergosterol and creates pores
relative selectivity ergosterol> our cholesterol |
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DOC for life-threatening systemic fungal infections
|
Ampho B
|
|
whats first line for invasive Aspergillis
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Ampho B
but Voriconazole used more |
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what is Ampho B used for?
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acute cryptococcus neoformins meningitis
|
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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 |
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is Ampho cidial or static?
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cidal in vitro
|
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how is Ampho eliminated/metab
|
Unkown
t1/2=15 days |
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Nystatin MOA
|
like Ampho-pokes holes
fungicial |
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uses of nystatin
|
candidiasis(thrush)
fungal diarrhea |
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nystatin toxic when given...?
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systemically
oral is ok |
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which drugs are polyene antifungals?
|
ampho B
nystatin |
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Anti-metab antifungal drug?
|
flucytosine
|
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Flucytosine MOA
static or cidal? |
converted to 5-FU only in fungal cells-inhibits thymidylate synthetase
static |
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Flucocytosine slectivity, how?
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only fungal cells have a cytosine permease-brings drug into cell
-cytosine deaminase converts drug to 5-FU(only in fungus) |
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Flucytosine suse?
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tx's cryptococcal meningitis
used with amphoB |
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flucytosine resistance
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develops rapidly-never use as the singular agent
|
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Flucytosine ADR's
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bacteria convert it to 5-FU in the intestine-abs in body and inhibits OUR thymidylate synthetase
|
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Flucytosine result of ADR's
|
teratogenic
bone marrow depression hair loss |
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azole has most CYP inhib
least? |
most-ketoconazole
least-fluconazole |
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azole MOA
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blocks the synthesis of ergosterol-inhibits enzyme sterol 14-alpha-demethylase
|
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what should not be used with azole?
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ampho B NOT to be used concomitantly
|
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azole cidal or static?
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static, but at hight dosescan be cidal
|
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fluconazole DOC for?
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oropharynheal/systemic candida
|
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which azoles have broadest antifungal spectrums
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voriconazole
posaconazole |
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which drugs is 2nd line for aspergillus
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itraconazole
|
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what is DOC for invasive aspergillus
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voriconazole
|
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posaconazole covers?
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good-candida + aspergillus
only agent for-zygomycetes |
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DOC for treating cushings disease?
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ketoconazole
|
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posaconazole should be taken how?
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with fatty meal
|
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tx for chronic suppression cryptococcal neoformans meningitis
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fluconazole
|
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which azole is only excreted thry kidney
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fluconazole
|
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what inhibits P-glycoprotein
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keto and fluconazole
|
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ketoconazole
absorption? CNS penet? |
ab-requires acidic environment
tk with coke decrease abs with food No CNS penetration |
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Fluconzole
abs? CNS? |
abs-unaffected by food
CNS-yes |
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Itraconazole
abs CNS |
requires acidic environ.
abs incr. with food in caps abs dec with food in oral soln |
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which 2 antifungals can cross BBB
|
FF
Fluconazole + flucytosine |
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Vori inhibits
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2C19
2C9 3A4 |
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Cyp inhib by potentcy
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keto>itra=vori>>flu
|
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ketoconazole SE
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inhib formation of testosterone- no hardons, big tities, N/V
|
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monitor what in all AZOLES?
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LFTs-for hepatotoxicity
HTN + fluid retention in all Azoles |
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Fluconazole SE
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rash in immunosupp. pt's
|
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Vori SE
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visual disturbances
|
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itraconazole SE
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may exacerbate or cause HF
|
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which azoles are teratogenic
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ALL
|
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Griseofulvin is an inhib of what?
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NOTHING
ITS A INDUCER!!!! |
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uses for griseofulvin
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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 |
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terbinafine uses
|
onychomycosis-3months
|
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terbinafine AE
|
taste disturbances
hemotopoetic effects-pancytopenia, neutropenia changes in ocular lens + retina |
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Bufenatine, Naftifine
MOA? |
like terbinafine
|
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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
|
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capsofungin elimination?
absorb? |
primarily feces
IV no oral |
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capsofungin ADR
|
releases histamine-warmth/vasodil.
|
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micafungin and anidulofungin
|
same as capsofungin
use micafungin-candidia prophylaxis in HSCT(stem cell transplant) |
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prevention of viral pen or uncoating
|
amantadine, rimantadine
|
|
inhib of viral specific enzymes
|
all nucleoside analogs
|
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steps of viral infection
|
absorption
penetration uncoating translation replication release |
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drugs interfering with uncoating
|
amantadine
rimantadine |
|
Amantadine/rimantadine
MOA |
inhibit viral M2 protein->prevents dissociation (uncoating)
|
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amanaadines/riman uses
|
prophylaxis and tx of influenza A with 24-48H
|
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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 |
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tadines are C/I when?
|
pregnancy
|
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Neuraminidase inhib.
|
zanamivir
oseltamivir |
|
zanamivir/oseltamivir
MOA |
dec. release of infected cell particles, increases form of viral aggregates
|
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uses of amivir's
|
for influenza A + B
|
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amivirs used how?
|
zanamvir is inhaled
oseltamivir is ORAL prodrug |
|
what is oseltamivir DOC for
|
avian "bird" flu
|
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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
|
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INF-alpha SE
|
flu, fatigue, depression
|
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guanosine analogs
|
acyclovir, valacyclovir, ganciclovir, pencyclovir, ribavirin
|
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thymidine analogs
|
idoxuridine, trifluridine, cidofovir
|
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adenosine analog
|
vidarabine
|
|
cytosine analogs
|
cytarabine
|
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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
|
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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 |
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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 |