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118 Cards in this Set
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DOC for invasive aspergillosis
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voriconazole
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DOC for cryptococcus
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amphotericin b + flucytosine
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MOA of ampho b
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INTERACTION (not inhibition) w/ ergosterol → large transmembrane ion channels → depolarize cell
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major toxicity of ampho b
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nephrotoxic !!!
elevated liver enzymes |
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antifungal that causes disulfiram-like effects
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griseofulvin
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MOA of flucytosine
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converted to 5-FU which interferes w/ fungal DNA synthesis
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ketoconazole & fluconazole effects on P450?
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ketoconazole → inhibits CYP3A4
fluconazole → NO inhibition of P450 |
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2 major things about fluconazole
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excellent CNS penetration
no inhibition of P450 |
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how do azoles act?
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inhibit ergosterol synthesis
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MOA of griseofulvin?
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binds microtubules
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MOA of nystatin?
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similar to ampho B - interact w/ ergosterol
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how is griseofulvin used?
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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 |
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DOC for thrush
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nystatin
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MOA & toxicity of terbinafine
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inhibits ergosterol synthesis
may cause heaptic failure, so oral prep is Rx only (topical OTC) |
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MOA of acyclovir
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phosphorylated by VIRAL thymidine kinase → concentrates the drug w/in infected cells
drug competes w/ dGTP & inhibits viral DNA polymerase |
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toxicity of acyclovir
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virtually non toxic to normal cells b/c it needs to be activated by a viral enzyme
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DOC for herpes
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acyclovir
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MOA of foscarnet?
use? |
direct inhibition of viral DNA polymerase
used for acyclovir-resistant herpes |
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MOA of docosanol?
use? |
inhibits fusion of HSV envelope to cell
topical for cold sores |
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MOA of ganciclovir
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phosphorylated by thymidine kinase in herpes infected cells
in CMV infected cells - viral protein kinase phosphotransferase |
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what are the prodrugs of acyclovir & ganciclovir?
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valacyclovir
valganciclovir |
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toxicity of ganciclovir
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neutropenia, esp. when combined w/ zidovudine
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MOA of oseltamivir
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influenza drug
neuraminidase inhibitor - inhibits release of virus from infected cells |
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class of zamamivir?
how is it applied? side effect? |
neuraminidase inhbitor (for influenza)
intranasal or oral inhaler bronchospasm |
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side effects of oseltamivir?
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N/V
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what are amantadine & rimantadine used for?
which drug is more commonly used? |
influenza
usually use oseltamivir |
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ribavirin MOA
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inhibits viral mRNA synthesis
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uses of ribavirin
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RSV - aerosol
combo w/ interferon for hep C |
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antivirals & pregnancy:
- acyclovir - ribavirin - efavirenz |
- acyclovir = safe
- ribavirn = category X *** - efavirenz = teratogenic *** (cat D) |
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side effects of ribavirin
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dyspnea, anemia
pregnancy category X!! don't even let pregnant women administer it. it is seriously that bad. |
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use of interferon-alfa2b
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pegylated alfa-2b combo w/ ribavrin for hep C
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side effects of interferon-alfa2b
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depression & suicide !!
anemia, flu-like sx |
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DOC for hepatitis B
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lamivudine
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side effects of lamivudine
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trick question.
it is well tolerated & has very few side effects. that's why it is DOC for hep B |
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side effects of boceprevir & teleprevir
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strong inhibitors of CYP3A4
anemia |
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first choice RTI combo for HIV
second choice |
1st = tenofovir/emtricitabine
2nd = zidovudine/lamivudine |
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major issue w/ all reverse transcriptase inhibitors
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must d/c drug if signs of metabolic acidosis or ↑ aminotransferase levels are detected !!!!
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zidovudine MOA
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becomes incorporated into DNA
inhibits viral RT |
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side effects of zidovudine
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anemia, neutropenia
CNS, GI |
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what happens if you combine zidovudine w/ acetaminophen or ganciclovir?
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↑ risk for neutropenia
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what is the DOC NNRTI?
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efavrienz
unless she is pregnant! |
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which 3 RTIs → peripheral neuropathy
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didanosine *** (this is the bold one)
stavudine zalcitabine |
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MOA & SE of enfuvirtide
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binds gp41 (fusion inhibitor)
injection site reaction |
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interactions of PIs
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metabolized by CYP3A4
millions of drug interactions st john's wort will induce metabolism of PIs |
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SEs of PIs
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altered body fat distribution - like corticosteroids, but facial ATROPHY
hyperglycemia ↑ serum cholesterol |
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use of ritonavir
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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 |
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which PI is DOC?
why? |
atazanavir
fewer side effects less lipoprotein effects |
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what drug can kill tissue schizonts?
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primaquine
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SEs of primaquine
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hemolytic anemia (G6PD)
teratogenic |
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how is mefloqine given?
who can't have it? |
oral
don't give to pts w/ hx of metal illness or epilepsy |
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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 |
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DOC for chloroquine resistant malaria prophylaxis
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mofloquine
atovaquone + proguanil |
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DOC for MDR malaria prophylaxis
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doxycycline
atovaquone + proguanil |
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DOC for chloroquine resistant P. falciparum infection
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atovaquone + proguanil
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DOC for chloroquine resistant P. vivax infection
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quinine sulfate + doxycycline, clindamycin, or tetracycline
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DOC for complicated/severe malaria infection
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quinidine gluconate + doxycycline, clindamycin, or tetracycline
need to use combo inject drugs slowly |
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SEs of quinine sulfate or quinidine gluconate
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HA, tinnitus, N/V
class I antiarrhythmic - may cause arrhythmia |
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DOC for entamoeba histolytica
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metronidazole + luminal amoebicide
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DOC for giardia
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metronidazole
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DOC for trihomonas vaginalis
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metronidazole
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DOC for toxoplasma gondii
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pyrimethamine + sulfadiazine + folinic acid
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DOC for pneumocystic jiroveci
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TMP-SMX + folinic acid
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DOC for nemotodes (ascaris, enterobius, necator)
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mebendazole
or pyrantel pamoate |
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DOC for trichonella spiralis
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mebendazole
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DOC for tapeworms (cestodes)
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niclosamide
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DOC for cysticercosis
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praziquantel
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DOC for schistosoma (flukes)
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praziquantel
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what is the use of pyrimethamine + sulfadoxine
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carry it w/ you, and if you get sx of malaria, start taking it until you can get to medical help
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what is artemisinin
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new drug for severe malaria
don't know much about its SEs yet |
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what is the effect/use of prednisone as immune therapy
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broad effect in suppressing immune response; also lyses lymphocytes
used post-transplant or after acute rejection episode |
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MOA of cyclosporine
SEs |
calcineurin inhibitor - cell can't make IL-2
does NOT suppress BM HTN, renal tox, hyperglycemia **gingival hyperplasia |
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MOA of tacrolimus
SEs |
inhibits calcineurin
does NOT suppress BM HTN, renal tox, hyperglycemia **insomnia |
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MOA of sirolimus
SEs |
mTOR inhibitor
blocks response of T cells to IL-2 profound myelosuppression |
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use of sirolimus
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kidney transplants
good b/c it doesn't cause renal damage |
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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 |
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why is cyclophosphamide a bad-ass?
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it can inhibit an ESTABLISHED immune response! most drugs can only prevent one from occuring
great for organ transplant RESCUE |
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what are the uses of thalidomide?
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multiple myeloma
prevent GVH AML leprosy RA |
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MOA of muromonab-CD3
SEs |
mouse mab to CD3
cytokine release syndrome b/c it is not humanized |
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use of daclizumab & basiliximab
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reduce rejection after renal transplant
long 1/2 life humanized & chimeric so no cytokine release w/ these guys |
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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 |
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what cancers is IL-2 used for?
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metastatic RCC
malignant melanoma |
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use of G-CSF
SE |
given SQ for severe neutropenia (DOC)
causes bone pain |
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use of epoetin
SE |
recombinant human EPO
treat anemia! causes HTN & increased risk for blood clots |
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use of oprelvekin
SE |
tx thrombocytopenia
fluid retention |
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category A
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controlled human studies demonstrated NO risk, even in 1st trimester
possibility of fetal harm is remote |
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category B
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animal studies indicate no fetal risk, but no human studies conducted
OR adverse effects in animals, but not in well-controlled human studies |
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category C
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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 |
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category D
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evidence of fetal risk has been demonstrated
used only if there is life-threatening disease or where other drugs carry a greater risk |
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category X
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absolutely contraindicated
evidence of fetal damage, risk outweighs any benefits |
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list some category X drugs
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** ribavirin
** thalidomide statins warfarin misoprostol isoretinoin |
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which drugs are used for brain tumors
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nitrosoureas (carmustine)
they are lipophilic, so they can cross BBB |
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general toxicities of alkylating agents
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bone marrow suppression
severe N/V - CTZ & GI cells hair follicles gonads - sterility teratogenic |
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use of mechlorethamine
SE |
hodgkin's
causes hyperuricemia - tx w/ hydration & allopurinol |
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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 |
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drug for bladder cancer
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thiotepa
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use of busulfan
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CML
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use of streptozocin
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pancreatic cancer
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cisplatin
MOA use SE |
acts like alkylating agent - crosslins DNA
breast, testicular, lung cancers NO myelosuppression *** acoustic nerve damage!! renal toxicity, anaphylaxis |
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MTX
MOA toxicity & how to tx |
DHF reductase inhibitor
use leucovorin to rescue for toxicity ppts in kidneys hepatotoxic pulmonary fibrosis |
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major drug for pulmonary fibrosis
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*** bleomycin
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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 |
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5-FU
MOA use SE |
inhibits thymidilate synthase
augmented by leucovorin colorectal cancer, topically for BCC bone marrow suppression |
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use of cytarabine
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AML ****
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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 |
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how to tx cardiotoxicity d/t daunorubicin & doxorubicin
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dexrazoxane
iron chelator |
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bleomycin
MOA use SE |
chops up DNA
testicular cancer *** pulmonary fibrosis |
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dactnomycin
MOA SE |
suppresses RNA synthesis & inhibits proliferation
radiation recall |
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vincristine & vinblastine MOA & SEs
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act on microtubules
vincristine - crisps the nerves vinblastine - blasts the BM |
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paclitaxel
MOA use SE |
binds microtubules
advanced cancers - breast, ovarian, lung very toxic - a whole bunch of shit |
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use of etoposide
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testicular cancer
|
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use of topotecan
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colorectal & breast cancers
|
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use of aspariginase
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leukemias
unique b/c it hydrolyzes asparigine (as its name suggests) |
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cancer uses o INF alfa-2a
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hairy cell leukemia
kaposi sarcoma |
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cancer use of IL-2
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advanced malignant melanoma
|
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tamoxifen
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SERM
estrogen + tumors |
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trastuzumab
MOA & tox |
antibody to Her2
↑ cardiotoxicity w/ doxorubicin |
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flutamide
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testosterone R antagonist
suppress flare of prostate cancer growth when starting leuprolide |
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imatinib
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CML- 90% have philly chromosome
protein kinase inhibitor - BCR-ABL fusion kinase (philly chromosome) |
