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118 Cards in this Set

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DOC for invasive aspergillosis
voriconazole
DOC for cryptococcus
amphotericin b + flucytosine
MOA of ampho b
INTERACTION (not inhibition) w/ ergosterol → large transmembrane ion channels → depolarize cell
major toxicity of ampho b
nephrotoxic !!!
elevated liver enzymes
antifungal that causes disulfiram-like effects
griseofulvin
MOA of flucytosine
converted to 5-FU which interferes w/ fungal DNA synthesis
ketoconazole & fluconazole effects on P450?
ketoconazole → inhibits CYP3A4

fluconazole → NO inhibition of P450
2 major things about fluconazole
excellent CNS penetration
no inhibition of P450
how do azoles act?
inhibit ergosterol synthesis
MOA of griseofulvin?
binds microtubules
MOA of nystatin?
similar to ampho B - interact w/ ergosterol
how is griseofulvin used?
ORAL to tx topical infection

binds specifically to keratin
doesn't reach high enough [ ] in blood for systemic effects
builds up in keratin-containing tissues
DOC for thrush
nystatin
MOA & toxicity of terbinafine
inhibits ergosterol synthesis

may cause heaptic failure, so oral prep is Rx only (topical OTC)
MOA of acyclovir
phosphorylated by VIRAL thymidine kinase → concentrates the drug w/in infected cells

drug competes w/ dGTP & inhibits viral DNA polymerase
toxicity of acyclovir
virtually non toxic to normal cells b/c it needs to be activated by a viral enzyme
DOC for herpes
acyclovir
MOA of foscarnet?
use?
direct inhibition of viral DNA polymerase

used for acyclovir-resistant herpes
MOA of docosanol?
use?
inhibits fusion of HSV envelope to cell

topical for cold sores
MOA of ganciclovir
phosphorylated by thymidine kinase in herpes infected cells

in CMV infected cells - viral protein kinase phosphotransferase
what are the prodrugs of acyclovir & ganciclovir?
valacyclovir
valganciclovir
toxicity of ganciclovir
neutropenia, esp. when combined w/ zidovudine
MOA of oseltamivir
influenza drug

neuraminidase inhibitor - inhibits release of virus from infected cells
class of zamamivir?
how is it applied?
side effect?
neuraminidase inhbitor (for influenza)

intranasal or oral inhaler

bronchospasm
side effects of oseltamivir?
N/V
what are amantadine & rimantadine used for?
which drug is more commonly used?
influenza

usually use oseltamivir
ribavirin MOA
inhibits viral mRNA synthesis
uses of ribavirin
RSV - aerosol
combo w/ interferon for hep C
antivirals & pregnancy:
- acyclovir
- ribavirin
- efavirenz
- acyclovir = safe
- ribavirn = category X ***
- efavirenz = teratogenic *** (cat D)
side effects of ribavirin
dyspnea, anemia

pregnancy category X!!
don't even let pregnant women administer it. it is seriously that bad.
use of interferon-alfa2b
pegylated alfa-2b combo w/ ribavrin for hep C
side effects of interferon-alfa2b
depression & suicide !!

anemia, flu-like sx
DOC for hepatitis B
lamivudine
side effects of lamivudine
trick question.
it is well tolerated & has very few side effects.
that's why it is DOC for hep B
side effects of boceprevir & teleprevir
strong inhibitors of CYP3A4
anemia
first choice RTI combo for HIV

second choice
1st = tenofovir/emtricitabine

2nd = zidovudine/lamivudine
major issue w/ all reverse transcriptase inhibitors
must d/c drug if signs of metabolic acidosis or ↑ aminotransferase levels are detected !!!!
zidovudine MOA
becomes incorporated into DNA
inhibits viral RT
side effects of zidovudine
anemia, neutropenia
CNS, GI
what happens if you combine zidovudine w/ acetaminophen or ganciclovir?
↑ risk for neutropenia
what is the DOC NNRTI?
efavrienz

unless she is pregnant!
which 3 RTIs → peripheral neuropathy
didanosine *** (this is the bold one)
stavudine
zalcitabine
MOA & SE of enfuvirtide
binds gp41 (fusion inhibitor)

injection site reaction
interactions of PIs
metabolized by CYP3A4
millions of drug interactions

st john's wort will induce metabolism of PIs
SEs of PIs
altered body fat distribution - like corticosteroids, but facial ATROPHY
hyperglycemia
↑ serum cholesterol
use of ritonavir
inhibits metabolism of other PIs
used to increase their bioavailability

it is a toxic drug, but can give it at sub-therapeutic doses to help out the other PIs
which PI is DOC?
why?
atazanavir

fewer side effects
less lipoprotein effects
what drug can kill tissue schizonts?
primaquine
SEs of primaquine
hemolytic anemia (G6PD)
teratogenic
how is mefloqine given?
who can't have it?
oral

don't give to pts w/ hx of metal illness or epilepsy
gimme question:
DOC for chloroquine sensitive malaria prophylaxis

PHK & SEs
very long 1/2 life - can give 1x/wk for prophylaxis

SEs - dizziness, ringing in the ears
DOC for chloroquine resistant malaria prophylaxis
mofloquine

atovaquone + proguanil
DOC for MDR malaria prophylaxis
doxycycline

atovaquone + proguanil
DOC for chloroquine resistant P. falciparum infection
atovaquone + proguanil
DOC for chloroquine resistant P. vivax infection
quinine sulfate + doxycycline, clindamycin, or tetracycline
DOC for complicated/severe malaria infection
quinidine gluconate + doxycycline, clindamycin, or tetracycline

need to use combo
inject drugs slowly
SEs of quinine sulfate or quinidine gluconate
HA, tinnitus, N/V
class I antiarrhythmic - may cause arrhythmia
DOC for entamoeba histolytica
metronidazole + luminal amoebicide
DOC for giardia
metronidazole
DOC for trihomonas vaginalis
metronidazole
DOC for toxoplasma gondii
pyrimethamine + sulfadiazine + folinic acid
DOC for pneumocystic jiroveci
TMP-SMX + folinic acid
DOC for nemotodes (ascaris, enterobius, necator)
mebendazole
or pyrantel pamoate
DOC for trichonella spiralis
mebendazole
DOC for tapeworms (cestodes)
niclosamide
DOC for cysticercosis
praziquantel
DOC for schistosoma (flukes)
praziquantel
what is the use of pyrimethamine + sulfadoxine
carry it w/ you, and if you get sx of malaria, start taking it until you can get to medical help
what is artemisinin
new drug for severe malaria
don't know much about its SEs yet
what is the effect/use of prednisone as immune therapy
broad effect in suppressing immune response; also lyses lymphocytes

used post-transplant or after acute rejection episode
MOA of cyclosporine
SEs
calcineurin inhibitor - cell can't make IL-2

does NOT suppress BM
HTN, renal tox, hyperglycemia
**gingival hyperplasia
MOA of tacrolimus
SEs
inhibits calcineurin

does NOT suppress BM
HTN, renal tox, hyperglycemia
**insomnia
MOA of sirolimus
SEs
mTOR inhibitor
blocks response of T cells to IL-2

profound myelosuppression
use of sirolimus
kidney transplants
good b/c it doesn't cause renal damage
MOA of mycophenolate mofetil
SEs
inhibits inosine monophosphate dehydrogenase
needed for de novo purine synth in T & B cells, so fairly selective

skin rash is major SE
why is cyclophosphamide a bad-ass?
it can inhibit an ESTABLISHED immune response! most drugs can only prevent one from occuring

great for organ transplant RESCUE
what are the uses of thalidomide?
multiple myeloma
prevent GVH
AML
leprosy
RA
MOA of muromonab-CD3
SEs
mouse mab to CD3

cytokine release syndrome b/c it is not humanized
use of daclizumab & basiliximab
reduce rejection after renal transplant
long 1/2 life

humanized & chimeric so no cytokine release w/ these guys
where does lymphocyte Ig come from?
use?
SE?
from horse or rabbit

used for acute rejection episodes, but you better pre-tx w/ corticosteroids

possible anaphylaxis
what cancers is IL-2 used for?
metastatic RCC
malignant melanoma
use of G-CSF
SE
given SQ for severe neutropenia (DOC)

causes bone pain
use of epoetin
SE
recombinant human EPO
treat anemia!

causes HTN & increased risk for blood clots
use of oprelvekin
SE
tx thrombocytopenia

fluid retention
category A
controlled human studies demonstrated NO risk, even in 1st trimester

possibility of fetal harm is remote
category B
animal studies indicate no fetal risk, but no human studies conducted
OR
adverse effects in animals, but not in well-controlled human studies
category C
no adequate human or animal studies
OR
adverse effects in animals, but no available human data

may be used, but only if benefits outweigh risks
category D
evidence of fetal risk has been demonstrated

used only if there is life-threatening disease or where other drugs carry a greater risk
category X
absolutely contraindicated

evidence of fetal damage, risk outweighs any benefits
list some category X drugs
** ribavirin
** thalidomide
statins
warfarin
misoprostol
isoretinoin
which drugs are used for brain tumors
nitrosoureas (carmustine)
they are lipophilic, so they can cross BBB
general toxicities of alkylating agents
bone marrow suppression
severe N/V - CTZ & GI cells
hair follicles
gonads - sterility
teratogenic
use of mechlorethamine
SE
hodgkin's

causes hyperuricemia - tx w/ hydration & allopurinol
drug that causes hemorrhagic cystitis

due to what accumulating?
treatment?
cyclophosphamide

due to accumulation of acrolein
tx w/ mesna

another SE of this drug is SIADH
drug for bladder cancer
thiotepa
use of busulfan
CML
use of streptozocin
pancreatic cancer
cisplatin
MOA
use
SE
acts like alkylating agent - crosslins DNA

breast, testicular, lung cancers

NO myelosuppression
*** acoustic nerve damage!!
renal toxicity, anaphylaxis
MTX
MOA
toxicity & how to tx
DHF reductase inhibitor

use leucovorin to rescue for toxicity
ppts in kidneys
hepatotoxic
pulmonary fibrosis
major drug for pulmonary fibrosis
*** bleomycin
mercaptopurine
MOA
interaction
SE
antimetabolite that is activated by HGPRT in the tumor cells (resistance possible!)

metabolized by xanthine oxidase, so interacts w/ allopurinol

cholestatic jaundice
5-FU
MOA
use
SE
inhibits thymidilate synthase
augmented by leucovorin

colorectal cancer, topically for BCC

bone marrow suppression
use of cytarabine
AML ****
daunorubicin & doxorubicin
MOA
use
resistance
SE
intercalate into DNA → damage

breast & ovarian

substrate for P glycoprotein, so can get pumped out by the cancer cell

*** cardiotoxic
how to tx cardiotoxicity d/t daunorubicin & doxorubicin
dexrazoxane
iron chelator
bleomycin
MOA
use
SE
chops up DNA

testicular cancer

*** pulmonary fibrosis
dactnomycin
MOA
SE
suppresses RNA synthesis & inhibits proliferation

radiation recall
vincristine & vinblastine MOA & SEs
act on microtubules

vincristine - crisps the nerves
vinblastine - blasts the BM
paclitaxel
MOA
use
SE
binds microtubules

advanced cancers - breast, ovarian, lung

very toxic - a whole bunch of shit
use of etoposide
testicular cancer
use of topotecan
colorectal & breast cancers
use of aspariginase
leukemias

unique b/c it hydrolyzes asparigine (as its name suggests)
cancer uses o INF alfa-2a
hairy cell leukemia
kaposi sarcoma
cancer use of IL-2
advanced malignant melanoma
tamoxifen
SERM
estrogen + tumors
trastuzumab

MOA & tox
antibody to Her2

↑ cardiotoxicity w/ doxorubicin
flutamide
testosterone R antagonist

suppress flare of prostate cancer growth when starting leuprolide
imatinib
CML- 90% have philly chromosome

protein kinase inhibitor - BCR-ABL fusion kinase (philly chromosome)