Shared Flashcard Set

Details

Pharm Antifungals Antihelminths
KYCOM Block 10
108
Pharmacology
Graduate
09/28/2013

Additional Pharmacology Flashcards

 


 

Cards

Term
what are the systemic antifungal agents (9)
Definition
amphotericin B
amphotericin B lipid complex
flucytosine 5-FC
ketoconazole
flyconazole
itraconazole
capofungin
vircanazole
posaconazole
Term
what are the superificial antifungal agents (7)
Definition
frisofulvin
tervinafine
nystatin
ketocanazole
microanazole
clotrimazole
terconazole
Term
what fungal agents are clearly fungistatic (2)
Definition
griseofulvin
ketoconazole depending on dose
Term
what fungal agents are celarly fungicdic (1)
Definition
ketoconazole depending on dose
Term
4 ways to get a fungal infection and some examples for each
Definition
1. loss of mechanical barrier: burn, surgery, catheter
2. organ transplant and anti-rejection therapy
3. Immunodeficiency: AIDs, diabetes
4. supression of competing organisms: antibiotics
Term
MOA amphotericin b (2)
Definition
binds to sterols (ergesterol) allows K followed by Mg out, deranges cell metabolism causing cell death

sometimes binds sterols in humans because isnt specific
Term
MOA ABLC (2)
Definition
binds to sterols (ergesterol) allows K followed by Mg out, deranges cell metabolism causing cell death

complexes two phospholipids so it can go into ergosterol fungal membranes without interfering with human cholesterol
Term
MOA flucotysine (3)
Definition
needs amphotericin B synergy to allow it to penetrate wall

enters cell via cytosine-specific permease, converted to…
A. 5-FdUMP which inhibits thymudylate synthease lowering thymidylic acid (needed for DNA)
B. 5-FUMP which is put in fungal RNA disrupting protein synthesis
Term
MOA ketoconazole
Definition
interacts with P450 enzyme C14-a-demythylase and blocks demythelation of lanosterol to ergosterol disrupting membrane function and increasing permeability
Term
MOA fluconazole
Definition
nteracts with P450 enzyme C14-a-demythylase and blocks demythelation of lanosterol to ergosterol disrupting membrane function and increasing permeability
Term
MOA itraconazole
Definition
interacts with P450 enzyme C14-a-demythylase and blocks demythelation of lanosterol to ergosterol disrupting membrane function and increasing permeability
Term
MOA capofungin
Definition
inhibits formation of B(1,3)-D-glucans in fungal cell wal
Term
resistance to amphotericin B can happen by
Definition
fungi without or with decreased ergosterol
Term
resistance to ABLC can heppen by
Definition
fungi without or with decreased ergosterol
Term
resistance to flucotysine can happen by
Definition
develops fast when used as monotherapy (without amphotericin B)
Term
resistance to fluconazole can happen by
Definition
seen in HIV infected patients with more serious infections
Term
side effects of amphotericin B (7)
Definition
fever, chills
renal failure
hypotension (shock)
thrombophlebitis
neuro when administered intrathecal
normocytic norochromic anemia deu to RBC production supression
Term
side effect for ABLC, why
Definition
less toxic than ampotericin B because it is more selective and does not bind human sterols as often
Term
side effects flucytosine (4)
Definition
hematological toxicity: neutropenia, thrombocytopenia

hepatic dysfunction: elevation of serum transaminase and alkaline phosphatase
Term
side effects of ketoconazole (4)
Definition
nausea, vomting

hepatic: rare but serious

endocrine: antiandrogen (stops C17-lyase which decreases testosterone causing impotence)
Term
side effects fluconazole (2)
Definition
P450 inhibitor
teratogen
Term
side effects of itraconazole (3)
Definition
hypokalemia, hypertension, edema
Term
side effects of capofungin (2)
Definition
histamine release, liver function issues sometimes
Term
side effect viraconazole
Definition
occasional drug interactions
Term
side effect posaconazole
Definition
occasional drug interactions
Term
amphotericin B: administration, administration instructions
Definition
IV
intrathecal for meningitis
Term
ABLC: administration, administration instructions
Definition
IV
intrathecal for meningitis
Term
flucytosine: administration, administration instructions
Definition
oral
Term
ketoconazole: administration, administration instructions (4)
Definition
oral

absorption impaired by food, antacids, cimetadine, rifampin

acid improves absorption (pop)
Term
fluconazole: administration, administration instructions
Definition
IV or oral
Term
itaconazole: administration, administration instructions
Definition
oral- well absorbed

food increases bioavability
Term
capofungin: administration, administration instructions
Definition
IV over one hour
Term
which systemic antifungals enter the CNS (4)
Definition
amphotericin B and ABLC if administered intrathecal
flucytosine
fluconazole
Term
which systemic antifungals bind to plasma proteins (4)
Definition
amphotericin B
ABLC
ketoconazole
fluconazole - minimal
Term
which systemic antifungals cross the plcaenta, which are teratogenic (3)
Definition
amphotericin B
ABLC
fluconazole - teratogen
Term
what tissues does ketoconazole reach (4)
Definition
lung, bone, skin, soft tissue
Term
what tissues does itraconazole reach (4)
Definition
bone, sputum, adipose, most tissues
Term
which systemic antifungals are metabolized by the liver, how well or to what extent (3)
Definition
fluconazole - poorly
ketoconazole - extensive
itraconazole - extensive
Term
which systemic antifungal are excreted by the kidney (2)
Definition
flucytosine
fluconazole
Term
what is the most broad spectrum azole of them all
Definition
poscanoazole
Term
what is viraconazole used for (3)
Definition
candidia
DOC
invasive aspergillosis
Term
what is capofungin used for (4)
Definition
azole resistat isolates of C. albicans

aspergillus fumigantus
P. carinii
H. capsulatum
Term
what is itraconazole the drug of choice for (1), what else does it di (5)
Definition
Broad
drug of choice: blastomycosis

AIDS associated histoplasmosis

aspergillosis, candidemia, coccidioidomycosis, cryptococcosis
Term
what is fluconazole the drug of choice for (4), what else does it do (2)
Definition
Drug of choice: cryptococcus neoformans, candidemia, coccidiodomycosis

chronic ambulitory treatment, reduce fungal infection in marrow transplant
Term
what is ketoconazole good at killing (4), what combination should it be in and why, what combination shouldnt it be in and why
Definition
same as amphotericin B but together antagonizes its activity, narrow

good at histoplasmosis andnonmeningeal coccidioidomycosis and blastomycosis

add to flucytosine for candida
Term
what does flucytosine kill (2)
Definition
systemic mycosis and meningitis caused by…

cryptococcus neoformans

candidia
Term
what does amphotericin B and ABLC (6)
Definition
broad
candidia albicans
histoplasma capsulatum
cryptococcus neoformans
coccidioides immitis
aspergillus
blastomyces dermatitidis
Term
MOA griseofulvin (2)
Definition
energy dependent enterance within microtubules
disrupts mitotic spindles
inhibits mitosis
Term
MOA terbinafine
Definition
inhibits fungal enzyme squaline epoxidase causing accumulation of sterol swualine which is toxic
Term
MOA mystatin
Definition
polyene antibiotic resemboles amphotericin B in MOA
Term
MOA superificial ketonconazole
Definition
interacts with P450 enzyme C14-a-demythylase and blocks demythelation of lanosterol to ergosterol disrupting membrane function and increasing permeability
Term
MOA miconazole
Definition
interacts with P450 enzyme C14-a-demythylase and blocks demythelation of lanosterol to ergosterol disrupting membrane function and increasing permeability
Term
MOA clotrimazole
Definition
interacts with P450 enzyme C14-a-demythylase and blocks demythelation of lanosterol to ergosterol disrupting membrane function and increasing permeability
Term
MOA terconazole
Definition
interacts with P450 enzyme C14-a-demythylase and blocks demythelation of lanosterol to ergosterol disrupting membrane function and increasing permeability
Term
how do you get resisance or stop the drug griseofulvin from working
Definition
phenobarbital: epilepsy drug stops drug absorption
Term
what are the side effects of griseofulvin (4)
Definition
induces P450 for many drugs

teratogenic

hepatotoxicity in patients with prophyria

disufram reaction
Term
what are the side effects of terbinafine
Definition
no P450 effects
Term
how is terconazole aministered
Definition
vaginal
Term
how is miconazole administered
Definition
topical and vaginal
Term
how is clotrimazole administered
Definition
topical and vaginal
Term
how is superificial ketoconazole administered
Definition
topical
Term
how is nystatin administered, why
Definition
topical and oral swish and swallow

not absorbed in the GI tract
Term
how is terbinafine administered
Definition
oral or topical gel
Term
how is griseofulvin administered, any instructions
Definition
oral - not absorbed well so take with fats
Term
what antifungal do you have to take for a long time, why
Definition
griseofulvin
ust continue therapy until normal tissue replaces infected tissue
weeks to months
Term
where does griseofulvin distribute to (2)
Definition
keritin tissues
placenta
Term
how is griseofulvin metabolized
Definition
metabolized in the liver via P450
Term
what is nystatin used for
Definition
candidia
Term
what is superificial ketoconazole used for
Definition
tinea corporis, T. pedis, T. curis, T. versicolor, candidasis
Term
what is micronazole used for (5)
Definition
tinea corporis, T. pedis, T. curis, T. versicolor, candidasis
Term
what is clotrimazole used for (5)
Definition
tinea corporis, T. pedis, T. curis, T. versicolor, candidasis
Term
what is terconazole used for (5)
Definition
tinea corporis, T. pedis, T. curis, T. versicolor, candidasis
Term
what is terbinafine used for
Definition
same as grisofulvin but more effective
Term
what is griseofulvin used for (5)
Definition
dermatophytes: trichophyton, microsporum, epidermophyton,

Tinea that didn’t respond to other treatment
Term
what anti-helminth drugs are used to treat nematodes (5)
Definition
albendazole
pyrantel
thiabendazole
ivermectin
diethylbarbamazin
Term
what anti-helminth drugs are used to treat cestodes and termatodes
Definition
praziquantel
Term
cestode: aka, 4 features of its body, location in host, how to acquire (3)
Definition
tapeworm
flat, segmented, attach to intestines, no mouth, no digestive tract
found in beef, pork, fish
Term
termatode: aka, shape, 4 places in host its found
Definition
flukes
leaf shape
liver, lungs, intestine, blood
Term
MOA abbendazole (3)
Definition
binds to microtubules, stops their synthesis

decreases glycose uptake

parasite is expelled in feces
Term
MOA pyrantel
Definition
depolarizing neuromuscular blocking agent. Activates nicotinic receptors and paralizes worm which is then expelled
Term
MOA thiabendazole (3)
Definition
binds to microtubules, stops their synthesis

decreases glycose uptake

parasite is expelled in feces
Term
MOA ivermectin
Definition
targets gamma-aminobutyric acid (GABA-A) letting Cl out hyperpolarizing the cells, causing worm paralysis and expulsion
Term
MOA diethylcarbamazine
Definition
decrease muscle activity of parasites
Term
MOA praziquantel (2)
Definition
permeability of cell membrane to Ca increases causing contracture and paralysis

inhibit mitochondrial anaerobic phosphorlyation (uncomple reaction from ADP to ATP)
Term
how can the effectiveness of thiabenzadiole be drecreased
Definition
taking carbamazepines
Term
side effects pyrantel(6)
Definition
dizzy
headache
abdominal cramps
vomiting
elevated liver enzymes
hepatic disease
Term
side effects thiabendazole (11)
Definition
behavorial changes, dizzy, fever, seizures, bradycardia, hypotension, hepatic disease, renal disease, jaundic, abormal smelling urine, Steven's Johnson syndrome
Term
side effects ivermectin (3)
Definition
dizzy
diarrhea
leukopenia
Mazzotti reaction: rapid killing of microfilaria induces ocular inflammatory response
Term
side effects diethylcarbamazine (2)
Definition
nausea, vomiting
Term
side effects praziquantel (5)
Definition
nausea
vomiting
fever
rash
alcohol within 24h increases CNS issues
Term
how can the plasma level of praziquantel be
Definition
cimetidine is a P450 inhibitor for it
Term
what is the dosing redigimes for albendazole (2)
Definition
1 tablet, repeat 3 weeks later for pinworms (treat everyone in home)

1 tablet twice a day for 3 days for other
Term
howis pyrantel administered, what administration instructions
Definition
oral or suspension
if it is a pinworm infection treat everyone in the home
Term
how is thiabendazole administered
Definition
oral suspension or tablet
Term
how is ivermectin administered
Definition
oral
Term
what interactions are there with ivermectin, why
Definition
benzodiasapines and barbitols act like the drug and may cayse OD
Term
how is praziquantel administered, administration instructions, why
Definition
oral

take laxative before med to purge of death segments and allow for good ova liberation and avoid cysticerosis
Term
which antihelminth pass into the placenta, which a teratogenic (4)
Definition
praziquantel - teratogenic
ivermectin - teratogenic
thiabendazole - teratogenic
pyrantel - teratogenic maybe
Term
which antihelminth passes into the CNS
Definition
all but ivermectin
Term
which antihelminths are metabolized in the liver (3)
Definition
praziquantel
ivermectin
albendazole
Term
which antihelminths are excreted in the liver (2)
Definition
albendazole
iveromectin (then feces)
Term
which antihelminths are excreted in the kidney (2)
Definition
thiabendazole
praziquantel
Term
what is praziquantel drug of choice for, what else is it used for (3)
Definition
all cestode infections, cysticerosis + termatodes

drug of choice for most tapeworm infections
Term
what is diethylcarbamazine used for (1)
Definition
Filariasis caused by Wuchereria bancrofti
Term
what is ivermectin used for (2)
Definition
River Blindness: onchocerca volvus (where the worm was in the eye)
Scabes
Term
what is thiabendazole used for (3)
Definition
Thread worm: strongyloides stercoralis
cutaneous larval margins
trichinella spiralis (trichinosis)
Term
what is pyrantel used for (3), when do you use it
Definition
round worms
pin worms
hookworms

not as good as albendazole
Term
what is albendazole used for (5)
Definition
Broad spectrum

Whip worm: trichuris trchiura
Pinworm: enterobius vermicularis
hookworm: necator americanus
round worm: ascariasis lumbricoides
Supporting users have an ad free experience!