Pharmacology Atb Antifungal And Antiprotozoal Drugs Spring 2011

Front 1

Description of a fungal cell

Back 1

eukaryotic cells with a rigid cell wall with chitin, and a cell membrane composed of ergosterol

have different ribosomes and distinct nuclei

Front 2

Predisposing factors to a fungal infection (5)

Back 2

1. Loss of barriers (burns, surgery)
2. Immuno-deficiency (HIV, cancer, transplants)
3. Metabolic abnormalities (DM)
4. Suppression of competing organisms
5. Warm moist environment (diaper rash, athlete's foot)

Front 3

Fungi that can affect organs (systemic infections)

Back 3

Aspergillis
Blastomyces
Candidia
Coccidiodes
Crytococcus
Histoplasma
Zygomycetes

Front 4

Fungi that affect skin layers (Subcutaneous)

Back 4

Chromocycosis
Pseydaliescheriasis
Sporotrichosis

Front 5

Fungi that affect hair, nails, mucous membranes

Back 5

Epidermophyton
Microporum
Trichophyton

Front 6

Name the antifungal drug groups (7)

Back 6

- Polyenes
- Flucytosine
- Imidazoles
- Triazoles
- Echinocadins
- Griseofulvin
- Allylamines

Front 7

Which drugs work on the fungi cell membrane?

Back 7

- Polyenes
- Azoles
- Allylamines

Front 8

Which drugs work on the fungi cell wall?

Back 8

- Echinocandins

Front 9

Which drugs work on the fungi cell division?

Back 9

- Griseofulvin

Front 10

Which drugs work on the fungal nucleic acid synthesis?

Back 10

- Flucytosine

Front 11

Amphotericin B MOA? Drug class?

Back 11

Polyene fungal atb

MOA: forms channels in ergosterol membranes to allow K and Mg to leak out, causes oxidative damage to cells

Front 12

Ampho B dosage forms?

Back 12

IV infusions, lipid formlations also available to decrease tox (but $$)

infuse over 4 hours

Front 13

Ampho B Indications?

Back 13

Crytococcus, Blatomyces, Histoplasma, candida, coccidioides, aepergillus

Front 14

Ampho B A/E

Back 14

- Fever/chills (due to IL-1 and TNF, so pretreat with APAP, antihista, steroids)
- Electrolyte abnormalities
- Hypotension
- Uremia
- Monitor Life-Dose **3-5 grams**
- Renal tubule damage

Front 15

Nystatin class?

Back 15

polyenes, related to Ampho B

used topically for oral or vaginal candidiasis
nephrotoxic

Front 16

5-Flurocytosine class? MOA? Indications?

Back 16

it's own class or antifungal

converted to 5-flurouridine by cytosine deaminase to inhibit thymidylate sythase which inhibits DNA and RNA synthesis

Indications are with AmphoB in crytococcal meningitis; used with itraconazole in chromoblastomycosis

Front 17

5-Flurocytosine A/E

Back 17

- Bone marrow suppression
- Hepatotox
- GI
- Rash

Front 18

Major Imidazoles and Triazoles (5)

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- Ketoconazole
- Itraconazole
- Posaconazole
- Fluconazole
- Voriconazole

Front 19

Imidazoles and Triazoles MOA

Back 19

Inhibits 14-alpha-demethylase involved in conversion of lanosterol to ergosterol

No ergosterol! so cell membrane inhibited

Front 20

Imidazoles and Triazoles indications

Back 20

dandida, cryptococcus, blastomyces, histoplasma, coccidioides, aspergillis

Tinea pedis, tinea coporis, tinea cururis, tinea unguium

Front 21

Ketoconazole class? kinetics? A/E?

Back 21

Imidazole

Oral, take with meals

A/E: N/V/anorexia, ***Inhibits 3A4 so MANY drug interactions (not used much), can prolong QT intervals

Front 22

Itraconazole class? activity? A/E?

Back 22

Triazole

wider spectrum; usefull in blastomycosis, histoplasmosis, onchyomycosis, febrile neutropenic pts not responding to ATB

3A4 interactions! teratogenic

Front 23

Posaconazole class? kinetics? effective for? A/E?

Back 23

Triazole, related to itraconazole

oral suspension, excreted unchanged in feces, high protein binding, W/F

**Effective against aspergillis and candida and is the ONLY AZOLE against Zytomycetes

A/E:QT, fever, diarrhea, hypokalemia, thrombocytopenia

Front 24

Fluconazole class? for? S/E?

Back 24

Triazole

used for crytococcal meningitis (xBBB), oral and vaginal candidiasis

A/E: N/V, teratogenic, **3A4 interactions

Front 25

Voriconazole effective for? A/E?

Back 25

effective for systemic aspergillis and candida

Interacts with 2C19, 2C9, 3A4

A/E: lots of vision problems, liver and renal changes

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S/E common of all azoles

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teratogenic

Front 27

Name the three Echinocandins? general MOA?

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1. Caspofungin
2. Micafungin
3. Anidulafungin

MOA: Inhibit synthesis of 1,3,beta-D-glucan in cell wall

Front 28

Caspofungin via? for? A/E?

Back 28

IV infusion

for esophageal candidiasis, systemic aspergillis not responding to azole/ampho B

S/E: fever, HA, N/D. myalgia, hypersensitivity

Front 29

Micafungin via? for? A/E?

Back 29

IV infusion

for esophageal candidiasis, candida peritonitis and abscesses, prophylaxis for candida

A/E: D, rash, hives, hematological changes, hypokalemia,

Front 30

Anidulafungin via? For? A/E?

Back 30

IV injection

for esophageal candidiasis, candidemia

A/E: **monitor liver function! D, rash, hives, hypokalemia

Front 31

Griseofulvin MOA? useful in?

Back 31

MOA: interrupts mitotic spindles, stops cell division

deposited in keratin precursor cells so good for scalp, nail infections

**NOT effective against candida

Front 32

Length of tx in Griseofulvin?

Back 32

Scalp = 1 month
Fingernails = 6-9 months
Toenails = up to 12 months

Front 33

Griseofulvin kinetics, a/e?

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lipid soluble, increased absorption with meals

A/E: HA, mental confusion, blurred vision, 3A4 inducer

Front 34

Allylamines (2) MOA?

Back 34

Naftifine
Terbinafine

MOA: inhibit ergosterol synthesis

Front 35

Naftifine is used ____ and Terbinafine is used______

Back 35

Naft is topically, Terbinafine is used orally

Front 36

Tolnafate mainly used for?

Back 36

Athletes foot

ineffective against candida

Front 37

Difference between tx for fungi and protozoa?

Back 37

Best to try to prevent protozoals - tx is very difficult

Front 38

Strategies for antiprotozoal prevention?

Back 38

- control parasite
- hygiene/sanitation
- vaccination
- prophylaxis

Front 39

Common protozoal infections (6)?

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1. Leishmaniasis
2. Trypanosomiasis
3. Amoebiasis
4. Giardiasis
5. Trichomonaisis
6. Malaria

Front 40

Metronidazole used for?

Back 40

fungal AND protozoal infections (amoebiasis, giardiasis, trichomonaisis)

Front 41

Metronidazole MOA?

Back 41

production of nitroradicals which attack DNA of protozoa

Front 42

Metronidazole A/E?

Back 42

GI, ***Disulfuram reactions with alcohol, metallic taste, avoid in 1st trimester

Front 43

Tinidazole is related to? tx for?

Back 43

second generation agent related to metronidazole for metronidazole-resistant organisms

Front 44

Malaria life cycle

Back 44

Mosquito => blood => sporocyte to liver => matures to merozoites => cell bursts => to plasma => to RBC => becomes schizonts => rupture RBC (produces Sx) => passed to another person

Front 45

Malaria drugs (5)

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1. Pyrimethamine
2. Chloroquine
3. Primaquine
4. Quinine
5. Atovaquone

Front 46

Malaria drugs against which step in cycle?

Back 46

Pyrimethamine prevents growth in RBC
Chloroquine clears protozoa from blood
Primaquine effective in late hepatic phase
Quinine effective in RBC stage
Atovaquone used in prophylaxis and mild attacks

Front 47

Pyrimethamine MOA? used in?

Back 47

Malaria!

Inhibits protozoal dihydrofolate reductase (like sulfa drugs for protozoas)

prevents formation of schizonts in RBCs

Front 48

Pyrimethamine S/E?

Back 48

folic acid def, leucopenia, thrombocytopenia, SJS

Front 49

Chloroquine MOA? for?

Back 49

Tx and prophylaxis of malaria

MOA: kills blood borne protozoa (use mult doses to kill all)

Front 50

Chloroquine S/E

Back 50

Itching
V
HA
retinopathy
cardiac depression
ototoxicity

Front 51

Mefloquine for?

Back 51

Chloroquine resistant malaria

but resistance is building

Front 52

Mefloquine s/e?

Back 52

neuropsychiartric syndrome

Front 53

Primaquine in what stage?

Back 53

used WITH chloroquine, treats the late hepatic stage of malaria

Front 54

Primaquine most common A/E

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GI problems

Front 55

Quinine for what stage? can be replaced by?

Back 55

For the ethrocrytic state of malaria

Can use quinidine instead (antiarrhythmic)

Front 56

Quinine A/E

Back 56

cardiac depression, hypotension, visual/auditory disturbances, blood dyscriasis

Front 57

Atovaquone MOA? what stage?

Back 57

works by inhibiting mitochondrial function during the liver stages of malaria

used in combination with proguanil to prevent resistance

Front 58

Atovaquone used with?

Back 58

Proguanil to prevent resistance

Front 59

Atovaquone S/E

Back 59

GI related

Front 60

Most common prophylactic for malaria?

Back 60

Doxycycline

Front 61

Doxycycline is used how long for malaria?

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1-2 days before, during trip, 4 weeks after

Front 62

Doxycycline used in combo with___ to tx ____

Back 62

In combo with quinine to treat chloroquine resistant plasmodium falciparum

Front 63

Pneymocystis jirovicii etiology?

Back 63

85% of children have the fungi; many asymptomatic

Can cause pneumonia in malnourished/premature infants or immunocomp pts

Front 64

Pneumocystis jirovicii Tx?

Back 64

Prophylactic in AIDS: TMP/SMX

Tx: Timetrexate, atovaquone, dapsone