Anti-fungal Medications

Question 1

Nystatin MOA

Answer 1

Binds to ergosterol in fungal cell membrane&raquo_space; altered membrane permeability&raquo_space; releasing of intracellular K+, sugars, and metabolites&raquo_space; disruption of membrane&raquo_space; fungal cell death

Question 2

Nystatin Pharmacodynamics

Answer 2

Concentration dependent, fungicidal, post-antifungal effect

Question 3

Nystatin indication

Answer 3

Oral candidiasis, mucocutaneous infections, gut decontamination

Question 4

Nystatin Adverse Effects

Answer 4

N/V/D, GI discomfort

Question 5

Amphotericin B MOA

Answer 5

Binding to ergosterol&raquo_space; leakage of intracellular cations and proteins

Question 6

Amphotericin B absorption

Answer 6

No GI absorption
Highly protein bounds - absorbs into most tissues
Poor CSF penetration

Question 7

Amphotericin Elimination

Answer 7

Biphasic elimination in urine and bile» initial elimination 24-48 hrs, long terminal elimination several days

Question 8

Amphotericin Pharmacodynamics

Answer 8

concentration dependent, fungicidal, post-antifungal effect

Question 9

Amphotericin Adverse Effects

Answer 9

Nephrotoxicity&raquo_space; giving NS bolus prior to infusion may help

Acute infusion reactions&raquo_space; fever, chills, hypotension, tachypnea, malaise, rigors

Hypokalmia, electrolyte disturbances

Anemia

Hepatic dysfunction

Question 10

Amphotericin Indications

Answer 10

Most broad spectrum of any anti-fungal&raquo_space; tx of choice for most invasive or life-threatening fungal infections

Use for febrile neutropenic patients unresponsive to antibacterial therapy

Question 11

Benefits of lipid-ampho B

Answer 11

high tissue concentration, decreased infusion reactions, marked decrease in nephrotoxicity but very expensive

Question 12

Azole MOA

Answer 12

inhibits 14-alpha-demethylase enzyme&raquo_space; inhibits conversions of lanosterol to ergosterol&raquo_space; causes accumulation of 14-aplha methyl sterols (toxic sterol) and depletion of ergosterol

Question 13

fluconazole and voriconazole have _________ oral absorption

Answer 13

Good

Question 14

__________ & _________ are CSF distributed

Answer 14

fluconazole, voriconazole

Question 15

Fluconazole elimination

Answer 15

Renal

Question 16

General Azole Adverse Effects

Answer 16

N/V, GI distress, rash, hepatic dysfunction, QT prolongation (except Isavuconazole – shorter QTc)

Question 17

Voriconazole specific adverse effects

Answer 17

hepatitis, altered light perception, blurring, photophobia, skin cancer

Question 18

Drug of choice for noninvasive candida and cryptococcal infections?

Answer 18

Fluconazole

Question 19

Drug of choice for noninvasive histoplasmosis, blastomycosis, and coccidioidomycosis?

also covers Aspergillus

Answer 19

Itraconazole

Question 20

Drug of choice for invasive Aspergillus infections?

Answer 20

Voriconazole

Question 21

Safety monitoring for azole therapy?

Answer 21

EKG, plasma levels, liver enzymes

Renal function with IV azole use

Question 22

Terbinafine MOA

Answer 22

Inhibits ergosterol synthesis by inhibiting squalene epoxidase

Question 23

Flucytosine distributes into what tissue?

Answer 23

All tissues

major organs, bone, CSF

Question 24

Terbinafine has high _________ & __________ properties

Answer 24

lipophilic and keratinophilic

Question 25

Terbinafine indications

Answer 25

Dermatophytosis | Onychomycosis

Question 26

Flucytosine MOA

Answer 26

Inhibits fungal DNA synthesis and protein synthesis

Question 27

Flucytosine elimination

Answer 27

Renal

Question 28

Flucytosine adverse effects

Answer 28

``` Bone marrow toxicity Hematologic GI Distress  N/V Hepatic toxicity Photosensitivity ```

Question 29

Echinocandin MOA

Answer 29

Inhibits cell wall glucan synthesis