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Pharm Block 10 DeAtley
KYCOM Block 10
190
Pharmacology
Graduate
10/03/2013

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
Term
why do antiprotozoal drugs cause more side effects, where are they usualy at? (4)
Definition
Protozoa are eukaryotes and have metabolic processes closer to humans so drugs have more toxic effects

Increased in cells with high metabolic activity like kidney, neurons, intestinal, and stem cells
Term
what is the most common ameoba pathogen and the disease it causes
Definition
E. histolitica
amebiasis (amebic dysentery)
Term
what are the three categories of amebocides, what distinguishes them
Definition
mixed: effective in lumen and systemic, concentration too low for single drug treatment

luminal: act on parasite in lumen of bowel

systemic: act on parasite in intestine wall and liver
Term
what are the three antiameoba drugs and their category
Definition
mixed: metronidazole
luminal: diloxanide furolate
systemic: chloroquine
Term
what transmits malaria
Definition
female anopheles mosquito
Term
what are the 4 types of malaria, what is the their severity and prevelence
Definition
plasmodium falciparum: severe, common
P. vivax: mild, common
P. malariae: mild very common
P. ovale: mild, rare
Term
what categories of drugs are used to treat malaria (2)
Definition
tissue schizoniticides
blood schizoniticides
Term
what are the tissue schizoniticides
Definition
primaquine
Term
what are the blood schizoniticides (3)
Definition
chloroquine
quinine
mefloquine
Term
what two diseases do trypanosomiasis cause
Definition
african sleeping sickness
american sleeping sickness (Chagas')
Term
what microbes cause african sleeping sickness (2)
Definition
T. bruceo gambiense
T. bruci rhodinese
Term
what microbe causes american sleeping sickness
Definition
T. cruzi
Term
what is the treatment for trypanosomiasis (3)
Definition
melarsoprol
pentamidine
isethionate
nifurtimox
Term
how is leshmianisis transmitted
Definition
animal to human by bite of sand flies
Term
what are the three types of leshimaniasis
Definition
cutaneous
mucocutaneous
visceral
Term
what is the treatment for leshimaniasis
Definition
sodium sitbogluconate
Term
what is the cause of toxoplasmosis
Definition
Toxoplasma gondii
Term
what is the transmission of toxoplasmosis gondii (2)
Definition
raw meat or oocytes shed from cats
Term
what is the treatment of toxoplasmosis gondii
Definition
pyrimethamine
Term
what is the most commonly diagnosed intestinal parasite in the US
Definition
giardia lamblia
Term
how is giardia transmitted
Definition
contaminated water
Term
how is giardia treated
Definition
metronidazole
Term
what are the two forms of E. histolytica, where are they located
Definition
Cysts: survive outside the body

Labile: invasive trophozoites that cannot live outside the body
Term
how is E. histolica transferred, where does it grow, how does it cause infection
Definition
Cysts ingested through feces contamination and pass to intestines

Trophozoites are born and invade and ulcerate the mucosa and feed on intestinal bacteria

As they increase in numbers they are able to invade systemically

As they migrate to the rectum they return to cyst form and are excreted in feces
Term
how is E. histolitca diagnosed
Definition
E. histolytica in fresh feces
Term
what are the signs of P. falciparum (5)
Definition
persistent high fever
orthostatic hypotension
erythrocytosis (swollen limbs)
capillary obstructiondeath
Term
why is P. falciprum dangerous (3)
Definition
it can infect RBC of any age
increased drug resistance
increased insectacide resistance
Term
what is the main clinical concern for P. vivax
Definition
may remain in the liver after the blood part of the disease is elminated
Term
what is the main clinical concern for P. ovale
Definition
may remain in the liver after the blood part of the disease is elminated
Term
how is trypanosomiasis acquired, where does it go in the body, how does it cause pathoology, what are the signs
Definition
Initially live and grow in the blood

Invade CNS and cause inflammation of the brain and spinal cord

Produces lethargy and continuous sleep
Term
metronidazole: MOA
Definition
ferredoxin like, low redox, e- transport chains occur in anaerobic abeobe making ROS.

nitro group of drug accepts e- and forms reduced cytotoxic compounds that bind to proteins and DNA causing cell death
Term
diloxanide furolate: MOA
Definition
abebicidal, unknown
Term
chloroquine: MOA (4 parts)
Definition
1. decreases DNA synthesis but disrupting tertiary structure of DNA

2. alkalinization of food vacoule: tops Hb digestion of the parasite by going into food vacoule and picking up a protein and making the food basic

3. interferes with heme polymerase: parasites eat Hb to get AA and Fe but this makes soluble Hb which is toxic so it uses heme polymerase and turns the Hb into hemozoin and puts it away in its food vacoule.

4. binds ferriprotoprophyrin iX damaging membrane causing lysis of the parasite and RBC
Term
primaquine: MOA
Definition
intermediates act as oxidants which cause hemolysis and methemoglobenmia toxicities
Term
quinine: MOA (3 parts)
Definition
inhibit heme polymerase

affect DNA synthesis

damage the membrane
Term
mefloquine: MOA
Definition
damage parasite membrane
Term
melarsprol: MOA
Definition
reacts with sulfhydryl inducing enzymes in organism and host
Term
pentamide isethionate: MOA
Definition
binds to parasite DnA and stops RNA/DNA/phospholipid/protein synthesis in parasite
Term
nufutrimox: MOA
Definition
undergoes reduction so it has a free e- to attack O2 forming superoxide, hydeoxyl, and H2O2 raicals. Organism dosent have catalase so it kills it
Term
sodium sitbogluconate: MOA
Definition
reduced to trivalent antiomy for activity

inhibits phosphofructokinase stopping glycolysis
Term
pyrimethamine: MOA
Definition
stops diydrofolate reductase at a low enough concentration to not inhibit it in the host

this deprives it of tetrahydrofolate so it cant make purines and pyrimidines
Term
chloroquine resistance
Definition
some P. falciprum has become resistant
Term
metronidazole resistance
Definition
some trichomonas have become resistant
Term
metronidazole: side effects (7)
Definition
GI: nausea, vomiting, cramp

metalic taste
oral moniliasis

disulfiram like effect

rare CNS: numbness upon drug discontinuation
Term
diloxanide fulorate: side effects (3)
Definition
mild flatulence

dryness of the mouth

puritus
Term
chloroquine: side effects (3)
Definition
ECG changes - quinidine effect

chronic Tx: discoloration of nail beds, visual disturbances
Term
primaquine: side effects (3)
Definition
GI

drug induced hemolytic anemia in people with low G6PDH

rare blood dyscrasia in patients with lupus
Term
quinine: side effects (7)
Definition
cinchonism: nausea, vomiting, tinnitus, vertigo

discontiune for positive coombs test for hemolytic anemia

potentiation of neuromuscular blocking agents (surgery)

elevation of digoxin levels
Term
mefloquine: side effects (3)
Definition
dizzy, disorientation, hallucinations (caution to SCUBA divers), neurotic and psychotic stuff
Term
melarsoprol: side effects (1)
Definition
CNS: encephalopathy may appear soon after therapy. Usually subsides, can be fatal
Term
pentamide isethionate: side effects (3)
Definition
renal dysfunction

hypotension

toxic to B cells of pancreas
Term
nifurtimox: side effects (3)
Definition
anaphylaxis

delayed hypersensitivity

peripherial neuropathy
Term
sodium sitbogluconate: side effects (1)
Definition
cardiac arrhythmia
Term
pyrimethamine: side effects (2)
Definition
megaloblastic anemia: reversable with leuconvorin

hypersensitivity (can be severe)
Term
metronidazole: administration, absorption
Definition
oral
rapid and complete
Term
diloxanide furolate: administration, absorption (and its significance)
Definition
90% absorbed, but the unabsorbed part is the amebocide
Term
chloroquine: administration
Definition
oral
Term
primaquine: administration
Definition
oral
Term
melarsoprol: administration
Definition
IV
Term
pentamide isethionate: administration methods, why not the others
Definition
IM or aerosol

Avoid IV: tachycardia, decrease in BP
Term
sodium sitboqluconate: asministration
Definition
paraentral
Term
metronidazole: how is it metabolized (2), what can enhance this (1), what can increase the half life (1)
Definition
hepatic oxidation of the side chain by oxidase and glucuronidation (accumulates in hepatic disease)

enhanced by phenobarbital

cimetidine increases half life (heart burn)
Term
chloroquine: metabolism
Definition
some metabolic products retain antimalarial activity
Term
primaquine: metabolism
Definition
rapidly oxidized to many other compounds
Term
primaquine: distribution and its significance
Definition
can get to the liver to get P. vivax and P. ovale but does not concentrate anywhere in particular
Term
quinine: distribution
Definition
widly distributed
Term
quinine: excretion
Definition
excretion decreased due to alkalinization of the urine
Term
what antiprotozoa has the longest half life how long is it, who is the runner up
Definition
mefloquine
long half life (17d)

pentamide isethionate
Term
what antiprotozoa enters the CNS
Definition
melarsoprol
Term
melarsoprol: metabolism
Definition
host oxidizes non-toxic pentavalent arsenic compoind
Term
what is pyrmithamine used to
Definition
T. gondii
Term
what is sodium sitboglyconate used for
Definition
leishmaniasis
Term
what is nifurtumox used for
Definition
acute T. cruzi infection, chronic stage treatment results are variable (drug is supressive not curative)
Term
what is pentamide isethionate used for (2)
Definition
T. brucei gambinese in hematological stage

Pneymocystis carinii
Term
what is melarsoprol used for
Definition
drug of choice: late stages with CNS involvement for gambinense and rhodesiense
Term
what is mefloquine used for (2)
Definition
prophylaxis for chloroquine resistant malaria (also doxycycline)

treatment for chloroquine resistant malaria
Term
what is quinine used for (2)
Definition
reserved for resistant strains

treatment for chloroquine resistant malaria
Term
what is primaquine used for (5)
Definition
kills…
*primary exoerythrocytic P. falciparum and P. vivax
*secondary exoerythrocytic forms of P. vivax and P. ovale (in liver)
*sexual forms of all plasmodia are destoried in blood or prevented from maturing
*little activity on erythrocytic schizonts so often used in combo with blood schizoniticide
Term
what is metronidazole used for (3), how is it used
Definition
E. histolitica
Giardia lamblia
Trichomonas vaginalis

usually combined with a luminal ameboside because it is rapidly absorbed
Term
what is diloxanide furolate used for (2)
Definition
asymptomatic passers of cysts

intestinal amebiasis
Term
what is chloroquine used for (4)
Definition
use with metronidazole and diloaxnide to treat and preent liver abscesses

drug of choice forerythrocytic P. falciparum

prophylaxis for chloroquine sensitive malaria

treatment for chloroquine sensitive acute malaria
Term
what drug has to be gotten from the CDC
Definition
diloxanide furolate
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