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Pharmacology > Antifungals and Antiparasitcs > Flashcards

Antifungals and Antiparasitcs Flashcards

1
Q

Amphotericin B is a fungi_____ agent given for ____ fungal infections.

A

cidal

systemic

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2
Q

Which types of fungus does Amphotericin treat?

A

Aspergillus
Cryptococcus
Histoplasma

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3
Q

AE of Amphotericin include:

A

Infusion reaction (decr. rate, premed)
Nephrotoxicity
Electrolyte abnormalities- hypokalemia, hypomagnesemia

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4
Q

Liposomal formulation of Amphotericin and adequate hydration help to prevent what AE?

A

Nephrotoxicity

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5
Q

DI associated with amphotericin are relative to ______ toxicity with other ______ agents

A

cumulative

nephrotoxic

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6
Q

Fluconazole is mainly used for what organisms?

A

Yeast (Candida, Cryptococcus)

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7
Q

Itraconazole is mainly used for what organisms?

A

Endemic fungi (Histoplasma) and yeasts

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8
Q

Voriconazole and Posconazole arre mainly used for what organisms:

A

Expanded yeasts, molds (Asperigillus)
Serious systemic infections
Tx and prophylaxis in immunocompromised patients

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9
Q

How do Triazoles work?

A

Inhibition of CYP450-dependent enzyme that converts lanosterol to ergosterol (an important component in funal cellular membranes). This causes cell membrane permeability, lysis, and death
(some are fungistatic)

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10
Q

Triazoles AE:

A

Generally well tolerated
GI upset- N/V/D
Hepatotoxicity

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11
Q

PK of Fluconazole (PO, IV)

A

Well absorbed, no food or pH effect
CNS penetration
Long half-life (1x/day)
Renal excretion

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12
Q

What is different between the capsules and the oral solution of Itraconazole?

A

Not interchangeable
Capsules: Food and acidic pH requirement, lower bioavailability
Oral solution: Empty stomach increases absorption, no pH effect, more GI upset

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13
Q

Itraconazole is highly ______ with a high Vd, and extensive _______ metabolism.

A

lipophillic

hepatic

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14
Q

Therapeutic drug monitoring for itraconazole includes which to values?

A

Itraconazole level

OH-itraconazole level (active metabolite)

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15
Q

AE of Itraconazole:

A

HTN
Hypokalemia
Peripheral edema

(avoid in patients with congestive HF)

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16
Q

PK of Voriconazole (PO, IV):

A

Empty stomach increases absorption
High Vd, CSF penetration, extensive hepatic metabolism
Little none is renally excreted unchanged

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17
Q

What is true of the IV formulation of voriconazole and what should patients be monitored for?

A

Cyclodextrin vehicle used. This can accumulate with renal impairment.
Use only in patients that have CrCl >50ml/min

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18
Q

AE of Voriconazole include:

A

Transient vision changes (flashes, color changes)
Visual hallucinations
Photosensitivity, rash

19
Q

PK of Posaconazole (oral suspension):

A

Optimal absorption with high-fat meal or liquid nutritional supplement
Long half life but multiple dose/day increase absorption
Hepatically metabolized

20
Q

DI of Fluconazole:

A

CYP2C19 (Plavix) and 2C9 (warfarin) inhibitor

21
Q

DI of Ketoconazole/itraconazole:

A

CYP450 3A4 substrate and inhibitor
(ex of how this can be used to the drugs advantage-if itraconazole used with PI to treat histoplasmosis it can be dose daily)

22
Q

DI of Voriconazole:

A

CYP 450 2C19, 2C9, 3A4 inhibitor

CYP 2C19 and 3A4 substrate

23
Q

DI of Posconazole:

A

CYP 3A4 inhibitor

Metabolized by glucuronidation = not usually affected by other drugs but can affect other drugs

24
Q

Terbinafine (Lamisil) is fungi_____

A

cidal

25
Q

Terbinafine (Lamisil) PO treatment for onchomycosis length of treatment:

A

6 wks for fingernails

12wks for toenails

26
Q

AE and DI of Terbinafine (Lamisil):

A

Less toxic and DI than -azoles
AE: GI upset, HA, taste disturbances, hepatotoxicity esp in patients with pre-existing liver disease
DI: CYP450 2D6 inhibitor (ritonavir may be affected but not enough to dose adjust)

27
Q

Efficonazole (Jublia) for onchomycosis: Adminstration, pros/cons

A

Topical
Cons: 48wks of treatment (and may not be better than typical tx: terbinafine or oral azoles)
Pros: may be safer than oral meds, less toxicity risk

28
Q

Common AE of the fungistatic Griseofulvin (Grifulvin):

A

Common: HA, fatigue, confusion, syncope, lethargy
Rare: hepatotoxicity, neutropenia, angioedema, urticaria

29
Q

MOA of Flucytosine:

A

Prodrug converted to 5-FU by fungal enzymes

Causes formation of faulty fungal proteins and enzymes

30
Q

What drug is flucytosine use in combination with for the treatment of cryptococcal meningitis?

A

Amphotericin B

31
Q

Echinocandins: Caspofungin, micafungin, anidulafungin are all given:

A

IV (low bioavailability)

32
Q

MOA of echinocandins:

A

Inhibits fungal synthesis of Beta (1, 3) D-glucan

33
Q

What is the spectrum of action of echinocandins?

A
  • *Candida (fungicidal)

* *Aspergillus (fungistatic)

34
Q

AE of echinocandins:

A

N/V, flushing, injection site reaction

35
Q

Which echinocandin can be induced by rifampin?

A

Caspofungin

36
Q

Do echinocandins have CYP reactions?

A

No

37
Q

Metronidazole (Flagyl), Tinidazole (Tindamax, Fasigyn) are used for the treatment of what type of organisms?

A

Anaerobic bacteria, amebiasis, giardiasis, trichomoniasis

C.diff colitis

38
Q

What should patients taking Metronidazole (Flagyl) avoid doing?

A

Drinking alcohol during and for 48hrs after stopping the drug- it can produce a disulfiram effect and causes the build up of alcohol in the system making people feel sick

39
Q

The antiprotozoal agent Nitazoxanide (Alinia) is used to treat:

A

Giardiasis, Crytosporidosis

40
Q

The antiprotozoal agent Pentamidine (Nebupent, Pentam) is used to treat:

A

PCP- inhaled or IV

41
Q

The antiprotozoal agent Atovaquone is used to treat:

A

PCP, toxoplasmosis- oral liquid (give with food)

Malaria

42
Q

What is the MOA of the antihelminthic, Ivermectin?

A

Binds selectively to glutamate-gated Cl channels
Paralyzes worms by causing hyperpolarization of nerve and muscle cells

Low affinity for human ligand-gated Cl channels
Poor CNS penetration

43
Q

What is the MOA of the antihelminthics, Albendazole and Mebendazole?

A

Inhibits formation of worm microtubules

AE: bone marrow suppression, hepatotoxicity, acute renal failure

44
Q

What is the usual length of a course of antihelminthics?

A

Very short, sometimes even just one dose

Pharmacology (48 decks)

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