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97 Cards in this Set

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This drug inhibits the microtubules of fungal cells, inhibiting mitosis:
Griseofulvin
This drug class inhibits B-(1,3)-D-glucan on fungal cells:
Echinocondins
_____ inhibit lanosterols while ____ inhibit squalenes in the synthesis of ____ in fungal cells.
Azoles inhibit lanosterols and terbinafines inhibit squalenes, which are enzymes involved in the synth of ergosterol in fungal cells.
Of all the antifungals, this one actually inhibits DNA synthesis:

It is often combined with ____ for the tx of cryptococci:
Flucytosine

Amphotericin B
This drug causes the formation of ion pores in the PM of fungal cells:

Major toxicity?
Amphotericin B

Nephrotoxic so don't use with aminoglycosides
Besides forming ion pores, what is another mech for amphotericin B?

How is it administered and why do we care?
(-) AA uptake

IV mostly. Usually hospitalized.
What is a topical "version" of amphotericin B?

What is it used for?
Nystatin

Candida mostly
Your pt has histo, crypto, blasto, glabrata, and braziliensis. Luckily, you can give them what to tx all that?
Amphotericin B
How does the concentration of Amphotericin in the CSF and eye compare to serum?

What if you get an OD of amphotericin B?
lower.

Tough cookies. It cannot be removed via hemodialysis.
This antifungal can cause eye discoloration if injected in the subconjunctiva:
Amphotericin B.
This drug is used for crypto, candida, aspergillus and sporo. It inhibits thymidylate synthase in fungi:

Route?
Flucytosine

Oral
Your pt has paracocci infection and mucocutaneous candida. They are also experiencing gynecomastia as a result of their drug tx. How does this drug work?
This drug is ketoconazole and is an inhibitor of fungal CYP3A (aka lanosine 14a demetheylase)
How is ketoconazole normally administered?

What are it's major SEs (3)?
Orally.

CYP3A inhibitor and gynecomastia/testicular atrophy
Which azole is used topically for M. furfur?

How do you NOT administer it?
Chlortrimazole

NO subQ admin.
How does fluconazole differ from ketoconazole in terms of coverage?

Why is it good for the first listed?
Good for crypto meningitis and HIV/transplant candidiasis.

90% avail in CSF vs 10% ketoconazole
What are the two routes of admin for fluconazole?

It is okay in pts taking drugs that inhibit CYP3A?
oral and IV

nope. less worrisome than ketoconazole but still dangerous.
How do ketoconazole and fluconazole differ in terms of SEs?

Can fluconazole be used in onchomycosis?
No gynecomastia/testicular atrophy with fluconazole.

yes.
This triazole is great for Aspergillus:

What is the DOC for Aspergillus?
Itraconazole

DOC is Voriconazole
How is the administration of Itraconazole different from ketoconazole?
Oral dosing can be in capsules or solution. Capsules are best with meal; solution is best without a meal. Do not mix these routes.
This drug has a PPB rate of 99%, is metabolized to 30 metabolites but only one is active, and often causes a rash:

What is the active metabolite?
Itraconazole

Hydroxy-itraconazole
Voriconazole is most like what other azole?

What is different in it's metabolism?
Fluconazole.

Metabolizes many more P450 enzymes: 2C19, 2C9, 3A4.
Your pt has been diagnosed with an Aspergillus infection and you rx them the DOC. A few weeks later they come back freaking out because they are losing their sight. What is the appropriate course of action?
Leave them on it. It usually resolves. You may also take them off. Either way, it's reversible.
You tx a pt for Aspergillus and a few days later they are seen in the ER for severe hepatotoxicity sxs. What happened?
The pt may have had a genetic polymorphism that left them 4x more susceptible to the P450 inhibition that occurs with use of Voriconazole.
What are two lesser SE of voriconazole?
CP, edema.
How do echinocandins work against fungi?

How is resistance developed?

What are the main CIs and SEs?
Inhibit the B-(1,3)-D-glucans in the fungal PM.

It isn't.

There aren't.
How are the enchinocandins administered?

This one comes with inc LFTs:
IV.

Caspofungin
This enchinocandin may be used for pts with invasive Aspergillus or refractory esoph candida:
Caspofungin but is not DOC
Which enchinocandin was listed specifically as fungicidal vs fungistatic?
Anidulafungin
This drug is mostly used for systemic tx of dermatophytoses (like 'ringworm'):
Griseofulvin
This antifungal is poorly orally absorbed, which is made worse by barbituates and better with fatty foods or it's microcrystalline form:
Grisofulvin
Your pt has dermatophytosis and you need a drug that binds keratin. What are the main CIs of the drug you would choose (4)?
Do not use in:
* Acute intermittent porphyria
* Hepatocellular failure
* Rx of warfarin (dec warfarin)
* Barbiturate use (dec Gris)
This antifungal may cause GI sxs, hemo sxs, estrogen-like effects in kids, disulfiram like effects, and photosensitivity:
Griseofulvin
This drug sucks for candida but is great for onchomycosis:

Describe it's mech:
Terbinafine

Inhibs squalene monoxygenase and interferes with ergosterol synth
These two antifungals interfere with amphotericin B via their mech:
Azoles and terbinafine
Terbinafine is usually administered _____ for tx of onchomycosis:
Orally. 99% PPB and great oral abs. Sits around in CNS and nail beds.
What is a very rare complication of terbinafine tx?

But considered ok in?
Hepatic failure in pts with preexisting liver dz

Notes say hepato-renal dz.
Which broad spectrum antifungal tinea tx would you avoid using in your eyes?

What is an alternate tx for tinea?
Naftifine

Tolnaftate
You want to tx tinea pedis with a cream. What is it and for how long do you tx?

How about for vag candidiasis?
Miconazole nitrate

4 wks for tinea pedis.

2 wk cream or 7 day tabs for vag.
Which is better for vaginal yeast infections - miconazole or nystatin?
Miconazole
Terbinafine >> _____ and _____ for onchomycosis.
Griseofulvin and itraconazole
Name the 4 flu drugs:
Oseltamivir, Zanamivir, Amantadine, Rimantadine
How do neurominidase inhibiting antivirals impact the virus?

What are they used for?
Prevents release of virus

Flu drugs
This antiviral blocks the uncoating of influenza and has a very long t1/2:

What are the two main side effects (related)?
Amantadine

Crosses BBB and is a DA agonist, so may make people go nuts.
This drug has GI issues, blocks uncoating of the virus once inside the host, does not cross the BBB, and is used in flu tx:
Rimantadine

Amantadine also has GI issues. Both are oral admin.
Your neonatal pt has RSV. You are pregnant. What do you have to ask someone else to administer?

Mech?
Ribavarin

Gets phosphorylated and inhibs viral mRNA synth.
This drug is used to treat active RSV or HCV:

For HCV it is combined with:
Ribavarin

IFN
Your pt has Lassa fever. What drug might save her life?

What side effects might she experience (5)?
IV Ribavarin.

Dyspnea, cardiac arrest, hypotension, anemia, depression.
Ribavarin is an analog of what nucleic acid?
Purine, specifically Guanosine
You decide your high risk RSV pt needs prophylactic treatment. What do you prescribe?
Palivizumab
Your pt has HSV & VZV, what do you prescribe?

Your other one has HSV and CMV, what do you prescribe?
Acyclovir

Ganciclovir
This drug gets phosphorylated by viral thymidine kinase and ultimately becomes up to 300x concentrated in infected cells. It is used for (4):
Acyclovir.

Used for HSV, VZV, Hairy leukoplakia in AIDS, prophylaxis in transplants.
Why might you choose famciclovir over acyclovir (2)?
Pt also has EBV or HBV, OR because it's only taken 2x/day.
This drug is converted into panciclovir in vivo:
Famciclovir
How does ganciclovir work in HSV?

In CMV?
Gets phosphorylated by thymidine kinase

Gets phosphorylated by viral protein kinase phosphotransferase
This drug, often combined with foscarnet, may be used IV in serious CMV cases, or as a retinal implant for eye CMV:
Ganciclovir
What happens if you combine AZT with acyclovir?

With ganciclovir?
Somnolence

Hematological issues!
What three antivirals are indicated for CMV retinitis?

Which one is an antisense mech?
Ganciclovir (implant), cidofovir (renal tub necrosis), and fomivirsen (injection.)

Fomivirsen
This drug inhibits viral DNA polymerase, RNA polymerase, and reverse transcriptase:

What is it?
Foscarnet

Inorganic analog of pyrophosphate
This drug is IV only and administered for resistant HSV and CMV infections in AIDS pts:

Name the major SEs (5):
Foscarnet
Your AIDS pt receives an IV only drug for tx of his resistant CMV & HSV. He comes in complaining of CVA pain and genital ulcers. What drug was he on?
Foscarnet
Your AIDS pt has P. jirovecii and CMV. She is on two drug regiments. She tells you she keeps tetanic contractions. What are the drugs, and what do they cause when combined?
Foscarnet and pentimadine.

Together cause hypocalcemia.
What is the goal in tx of chronic HBV?

What is the only acceptable monotherapy?
Seroconversion

Lamivudine
Lamivudine is cross reactive with ____ but not with ____.
entecavir but not adefovir.
Adefovir is used in ____ and has these two toxicities:
HBV

Renal tox and lactic acidosis
This drug is a major tx of HCV and pretty much does everything but blocks microtubules:

Route?
IFN.

SubQ 1x/week
Major side effects of IFN tx:
Flu-like, depression, myalgia, hemo sxs, edema, hypotension, inc ALT
How long do you tx a pt with IFN for HCV genotype I?

What other drugs might you add to this?
At least 1 year.

Boceprivir and/or telaprevir AND ribavarin
How long do you tx a pt with IFN for HCV genotypes 2 or 3?

What else can it be used to tx (2)?
24 weeks

warts, HSV keratitis
These two drugs inhibit viral replication and are often adjunct txs in pts with HCV genotype I:

Their mech?

Major SEs (2)?
Bocepriver and teleprevir

Protease inhibitors

(-) CYP3A4, hemo sxs
What is the 1st choice drug combo for HIV?

2nd choice?
Tenofovir and emtricitabine

AZT & Lamivudine
Your prego HIV pt is on a drug that has a high first pass metab, good oral abs, and decreases the disease progression but does not eradicate it?
AZT.
You can use this drug in AIDS pts with Kaposi's sarcoma, pregnancy to prevent tranission, and in AIDS dementia?
AZT
This HIV drug is neurotoxic, nephrotoxic, has GI sxs, myelotoxic, and can also be used in psoriasis and Adult T cell leukemia:
AZT
AZT + acyclovir =

AZT + cimetidine/benzos =

AZT + probenicid =

AZT + tylenol or ganciclovir =
somnolence

inhib liver metab of AZT

Probenecid impairs elim of AZT

Neutropenia
Major SE of tenofovir?

Type of molecule?
Flatulence

Adenosine analog
This HIV drug is a deoxythymidine analog:

Route?
AZT/zidovudine

Oral 5x/day
Name the main NRTIs (4):

Name the special ones (3):
AZT, tenofovir, lamivudine, emtricabine

didanosine, zalcitabine, stavidine
These NRTIs cause peripheral neuropathy:

These NRTIs cause Lactic acidosis:
Didanosine, stavudine, zalcitabine

AZT, didanosine, stavudine, zalcitabine
These NRTIs cause anemia and granulocytopenia:

This NRTI causes major HS reactions and NVD:
AZT, didanosine

Abacavir
This NRTI is often combined with AZT and is an inhibitor of mito DNA synthesis:

This mechanism contributes to what major side effect?
Didanosine

periph neuropathy
This mito DNA synth inhibitor is used in HIV tx, may cause pancreatitis that is worse with ETOH and pentimadine, may also cause hyperuricema and lactic acidosis:

What would have been a dead giveaway?
didanosine

Combo with AZT and causes periph neuropathy
This dideoxythymidine analog NRTI should never be used with AZT:
Stavidine
What is so special about NNRTIs in AIDS tx?

What are they CI in (2)?
They do not require phosphorylation

Protease inhibs and other strong CYP3A4 inhibs
Besides being CI in pregnancy, what NNRTI crosses the BBB and should be eaten with fatty foods?
Efavirenz
Ketoconazole, cimetidine, and macrolides will increase the effect of what NNRTI?

What needs to be monitored?

What is another risk if combined with corticosteroids?
Nevirapine

LFTs

SJS
These drugs end in '-navir':

What is their major OTC CI?
Protease inhibs used in HIV

St John's Wort!!! Increases their metab.
This -navir causes increased bilirubin via inhib of UGT1A1:

May also cause (2):
Atazenavir

NV, rash
This -navir contains propylene glycol:

Should never be used with (2):

Notable risk:
Amprenavir

Metro or disulfiram

SJS
This -navir is used with ritonavir and causes diarrhea:
lopinavir
This drug is frequently used to increase the effects of -navirs. What is it and why?
Ritonavir. Inhibs CYP3A4
List the CIs for ritonavir (10 - FML):
Metro, propofol, buproprion, quinidine, ergot/zolpidem, clozapine, pimozide, benzos, amiodarone, -cainides.
What is an interesting SE of ritonavir use?

What does it contain?
Mouth tingling.

ETOH!
This -navir might be used with grapefruit juice or ritonavir to increase it's effects, but it also causes rhinitis:
Saquinavir
This navir is great for CSF penetration but might cause nephrolithiasis:
Indinavir
What is the only non-peptide PI for HIV tx?
Tipranivir
Name the two fusion inhibitors that are used in HIV:

What do they bind?
Enfuviritide and Marviroc

gp41 and CCr5 respectively
This HIV fusion inhibitor may increase risk of pneumonia and is administered subQ:
Enfurvirtide