Antifungals and antiprotozoals Flashcards Preview

STEP 1 Pharm > Antifungals and antiprotozoals > Flashcards

Flashcards in Antifungals and antiprotozoals Deck (31):
1

Azoles (ketokonazole, fluconazole, clotrimazole, itraconazole, voriconazole). Mechanism and usage

Inhibits the synthesis of fungal ergosterol from lanosterol by blocking the cyp450 enzyme (14 alpha demethylase). Used for local systemic mycoses (Histoplasmosis, blastomycosis, coccidiomycosis).

2

What is fluconazole used for?

Chronic suppression of cryptococcal meningitis in AIDS patients and candidal infections of all types.

3

Azoles Toxicity

Blocks testosterone synthesis (gynecomastia, especially with ketoconazole).

Liver dysfunction (because inhibits cytochrome P450)

4

Amphotericin B Mechanism and Usage

Binds to ergosterol and forms a pore in the fungal membrane. This causes leakage of electrolytes. Used for serious systemic mycoses (Histo, blasto, coccidiomycosis,).

5

How to administer Amphotericin B

With K+ and Mg2+ because of altered renal tubule permeability.

6

Amphotericin B toxicity

This is a shitty drug (amphoterrible) Fever/chills (shake and bake), hypotension, nephrotoxicity, arrhytmias, anemia, IV phlebitis.

7

How to reduce amphotericin toxicity

Concurrent hydration to decrease nephrotoxicity.

Liposomal amphotericin is better.

Also make sure to give K and Mg due to altered renal tubule permeability.

8

Nystatin mechanism and usage

Binds to ergosterol and makes a hole in the membrane for electrolyte leakage. Used as a swish and swallow for oral candidiasis. Topicall for diaper rash or vaginal candidiasis.

9

Nystatin administration

Topical form because too toxic for systemic use

10

Flucytosine mechanism and useage

Used in the treatment of cryptococcus in combination with amphotericin B.

Inhibits DNA and RNA biosynthesis by conversion to 5FU by cytosine deaminase.

11

Flucytosine Toxicity

Bone marrow suppression

12

Echinocandins (caspofungin, micafungin, andiulafungin) mechanism and usage

Inhibits cell wall synthesis by inhibiting synthesis of B-glucan.

Used for invasive aspergillosis, candida

13

Echinocandins toxicity

GI upset, flushing (histamine release)

14

Terbinafine mechanism and usage

Used for onchomycosis (and dermatophytoses)

Inhibits squalene epoxidase, which prevents squalene epoxide, which prevents synthesis of lanoesterol and finally ergosterol.

15

Terbinafine toxicity

Gi upset, headaches, hepatotoxicity, taste disTURBANce.

16

Griseofulvin

Used to treat dermatophytes or oral treatment of superficial infections.

Works by inhibiting microtubule function, distrupts mitosis. Deposits in keratin containing tissues like nails.

17

Griseofulvin toxicity

Teratogenic, carcinogenic, confusion, headaches, induces cyp450.

18

Griseofulvin toxicity

Teratogenic, carcinogenic, confusion, headaches, induces cyp450.

19

How to treat toxoplasmosis

Pyrimethamine

20

How to treat trypanosoma brucei

Suramin and melarsoprol

21

how to treat trypanozoma cruzi

Nifurtimox

22

how to treat leismaniasis?

Sodium stibogluconate.

23

how to treat leishmaniasis?

Sodium stibogluconate.

24

how to treat leishmaniasis?

Sodium stibogluconate.

25

Chloroquine mechanism and use

Blocks detoxification of heme to hematozoin. Heme accumulates and is toxic to plasmodia.

Used to treat plasmodium EXCEPT falciparum (resistance too high).

26

How to treat plasmodium falciparum?

Use arthemeter/lumefantrine or atovaquone/proguanil.

27

How to treat life-threatening malaria?

Quinidine.

28

Toxicity of chloroquine

Pruritus (especially in dark skinned) and retinopathy.

29

How to treat helminths

Albendazole, mebendazole, ivermectin, praziquantel. They immobalize the helminths

30

How to treat flukes (trematodes)?

Praziquantel

31

How to treat flukes (trematodes)?

Praziquantel (in trematodes like schistosoma).