Antifungals

Question 1

Fungicidal

Bind to ergosterol to form holes in the cell membrane leading to cell death (tears fungal cell mem)

Resistance: decreasing the amount if ergosterol

Answer 1

Amp B

Question 2

Treats all life threatening systemic fungal inf, coccidioidomycosis and aspergillosis

Answer 2

Amp B

Question 3

DOC for mucomycosis

Answer 3

Amp B

Question 4

Dose dependent renal impairment

1) reversible damage by decreasing perfusion
2) irreversible damage by tubular injury

Answer 4

Amp B

Question 5

ADR:

1) shake and bake [tx antipyretic, steroids, antihistamine]
2) nephrotoxicity
3) thrombophlebitis
4) seizure and other CNS effects

Answer 5

Amp B

Question 6

Type of admin for amp B to treat fungal CNS Effects

Answer 6

Intrathecal

Question 7

Non colloidal suspension - amp B deoxycholate (C-AMP)

Lipid Amp B (L-AMP) - reduces toxicity

Answer 7

Amp B

Question 8

Converts flucytosine to 5 flourouracil

Answer 8

Cytosine deaminase

Question 9

MOR: decrease activity of deaminase

ADR: BM depression [due to conversion of 5FU by gut flora], alpoecia, liver dysfunction

Answer 9

Flucytosine

Question 10

Never used alone

• used with Amp B tx cryptococcal meningitis
• used with itraconazole tx chromoblastomycosis

Answer 10

Flucytosine

Question 11

Same MOA as amp B 0 binding ergosterol to form holes in the cell membrane

Active against candida - oral rinse - local effect

Topical tx for mucocutaneous candidiasis (vaginal candidiasis)

Answer 11

Nystatin

Question 12

fungistatic
depend on CYP450 and inhibit CYP450 - 3A
inhibit 14 alpha demethylase

Answer 12

Azoles

Question 13

responsible for converting lanosterol to ergosterol

Answer 13

14 alpha demethylase

Question 14

inhibit CYP450

may cause visual disturbances, blurry vision, flashes of light, color vision changes (blue/green)

treats invasive aspergillosis

Answer 14

voriconizole

Question 15

only azole to treat mucormycosis - 2nd line

Answer 15

posaconazole

Question 16

DOC for cryptococcal and coccidioidal meningitis (and prophylaxis) and vaginal candidiasis

Also treats candida stomatitis and esophagitis

Answer 16

fluconazole

Question 17

only azole with high level CNS penetration

Answer 17

fluconazole

Question 18

treats systemic infections with dimorphic fungi - blastomycosis and sporothrix

absorption increased with food

Answer 18

itraconazole

Question 19

treats tinea infections

Answer 19

clotrimazole

miconazole

Question 20

treats dermatomycosis

inhibits 17, 20 desmolase (1st step of steroid synthesis form cholesterol); production of androgens and estrogens; overproduction of adrenal cortisol; CYP450-3A

Answer 20

ketaconazole

Question 21

fungistatic

binds fungal cell microtubules polymerization - halting metaphase

activates CYP450

treats dermatophytosis

Answer 21

griseofulvin

Question 22

1st line therapy for tinea corpis in children, and for nail fungi
needs prolong therapy - 6 months

Answer 22

griseofulvin

Question 23

toxicity: photosensitivity, disulfiram like rxn, contraceptive failure with OCPs, carcinogenic, liver toxicity

Answer 23

griseofulvin

Question 24

fungicidal

inhibits fungal squalene epoxidase causing accumulation of squalene

No P450 inhibition

Answer 24

terbanifine

Question 25

highly lipophilic: [ ] in dermis, epidermis and adipose tissue

Tx: fungal inf of nails 6- 12 weeks

Answer 25

terbanifine

Question 26

fungicidal

inhibits beta 1-3 glucan of cel wall - no cell wall

avoid combo with cyclosporins

no effect on P450

Answer 26

caspofungin (echinocandins)

Question 27

activity against candida and aspergillus

Answer 27

caspofungin

Question 28

treats for aspergillus

Answer 28

1) Amp B
2) voriconazole
3) caspofungin