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Neuro week 3- antifungals/antiparasitics
Pharmacology
52
Medical
Graduate
10/18/2018

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Cards

Term
Amphotericin B MOA?
Definition
Replaces ergosterol in fungal cytoplasmic membrane --> forms pores --> ions enter and depolarize the cell and it dies
Term
What is a major side effect of amphotericin?
Definition
Nephrotoxicity- Cr rise of 2-3
Due to vasoconstriction in afferent arterioles
Renal tubular acidosis- wasting of K+, Mg++, HCO3-
Term
What medications exacerbate amphotericin nephrotoxicity?
Definition
Solid organ transplant drugs (cyclosporine, tacrolimus)
Aminoglycosides
Term
How can we ameliorate the nephrotoxic effects of amphotericin?
Definition
Saline loading before/after
Increase infusion time (24hrs rather than 6)
Term
How is amphotericin tolerated?
Definition
Can cause fever/rigors (premedicate w/ acetaminophen/diphenhydramine, tx rigors w/ meperidine)
N/V
Anemia (long-term administration)
Term
Alternative to conventional ampho B?
Definition
Liposomal amphotericin (less nephrotoxic)
Term
Which causes less rigors: Ambisome or ABLC?
Definition
Ambisome (better tolerated)
Term
What formulation of ampho is best for brain infections?
Definition
Liposomal ampho B
Term
How well does ampho penetrate CSF?
Definition
Very poorly
Term
MOA of triazoles?
Definition
Inhibit enzyme that does C14 alpha demethylation of lanosterol to form ergosterol
Term
What candida species are resistant to fluconazole?
Definition
Glabrata & krusei
Term
Can we use fluconazole against aspergillus spp.?
Definition
No
Term
Effects on metabolism of fluconazole?
Definition
Moderate inhibitor of 3A4
Term
How does fluconazole affect warfarin dose?
Definition
Increases INR- need to reduce warfarin levels
Term
What is the drug of choice for c. krusei infections?
Definition
Voriconazole
Term
What trough level is the goal in Therapeutic Drug Monitoring (TDM) for voriconazole?
Definition
1 to 5 mcg/mL
Term
Voriconazole side fx?
Definition
Transient vision changes
Rash
Periostosis due to fluoride toxicity
Term
Voriconazole's "claim to fame"?
Definition
Aspergillus tx
Term
Drug of choice for histoplasmosis?
Definition
Itraconazole
Term
Which formulation of itraconazole is preferred: oral cyclodextrin or capsules?
Definition
Oral cyclodextrin- not pH dependent, more bioavailable
Term
How should posaconazole be taken?
Definition
W/ a high fat meal to enhance absorption
Term
Which meds may tx some mucorales spp?
Definition
Posaconazole, isavuconazole
Term
Echinocandins MOA?
Definition
Inhibit beta (1,3) D-glucan synthase --> inhibit fungal cell wall formation
Term
Where don't echinocandins penetrate?
Definition
CNS and urine
Term
Which echinocandins are hepatically metabolized?
Definition
Caspofungin & micafungin
Term
Which echinocandin is metabolized by serum esterases?
Definition
anidulafungin
Term
Indications for echinocandins?
Definition
C. glabrata candidemia
Azole-resistant C. esophagatii
Term
Echinocandin sfx?
Definition
Infusion-related histamin rxn- tx w/ diphenhydramine
Term
Which echinocandin interacts w/ cyclosporine, tacrolimus, rifampin?
Definition
Caspofungin
Term
What is the vector for malaria?
Definition
Female anopheles mosquito
Term
What malaria species have a dormant liver stage called the hypnozoite?
Definition
P. vivax & P. ovale
Term
Chloroquine MOA?
Definition
Antierythrocytic
Inhibits heme polymerase (which protects parasite from iron) --> cell membrane damage
Term
What part of the world has not developed chloroquine resistance?
Definition
Caribbean/central america
Term
Chloroquine half-life?
Definition
4 days
Term
Quinine half-life?
Definition
5-15hrs
Term
What's the IV formulation of quinine?
Definition
Quinidine (D-isomer)
Term
Quinine toxicity?
Definition
Cinchonism (Headache, N/V, tinnitus)- reversible
Rare- rash, blackwater fever (hemolysis)
Term
Indication for mefloquine?
Definition
Anti-malarial prophylaxis, chloroquine-resistant P. falciparum
Term
Mefloquine half-life?
Definition
6-23 days (mean 14 days)
Term
Mefloquine toxicity?
Definition
Neuropsychiatric effects, N/V, vivid dreams, cardiac conduction disturbances
Term
How to give doxycycline?
Definition
In combo w/ quinine
Term
Drawback of doxy?
Definition
Phototoxicity
Term
Proguanil MOA?
Definition
Inhibits dihydrofolate reductase
Term
Atovaquone MOA?
Definition
Hydroxynaphthoquinone- uncouples oxidative metabolism
Term
First line tx for intestinal nematodes?
Definition
Albendazole (broad spectrum of activity)
Term
Other indications for albendazole?
Definition
echinococcis (liver hydatid cysts)
Neurocysticercosis
Term
Organism that causes Neurocysticercosis?
Definition
T. solium (pork tapeworm)- causes seizures
Term
MOA of albendazole?
Definition
Inhibits microtubule synthesis in nematodes
Term
Indications for ivermectin?
Definition
Drug of choice for human onchocerciasis (causes river blindness)
DOC for strongyloidiasis
Ectoparasites (scabies)
Term
Metronidazole MOA?
Definition
acts as an electron sink and causes free radical formation which damages the DNA of the organism directly.
Term
Ivermectin MOA?
Definition
potentiates the opening of glutamate channels in the organism, such as nematodes and arthropods
Term
Metronidazole coverage?
Definition
Protozoans:
Entamoeba histolytica
Trichomonas vaginalis
Giardia lamblia
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