Antifungal Drugs

Question 1

What are the antifungals

Answer 1

Amphoteracin B
Flucytosine
Ketoconazole
Miconazole 
Clotrimazole
Fluconazole  
Itraconazole
Voriconazole 
Posaconazole
Caspofungin
Griseofulvin
Terbinafine
Nystatin

Question 2

What is Amphoteracin B

Answer 2

Polyene ABX

Question 3

How does Amphoteracin work

Answer 3

Binds ergosterol

Pores in cell membrane

Question 4

What does Amphoteracin B work on

Answer 4

Yeast and Molds

Question 5

When do you give Amphoteracin B

Answer 5

Life-threatening infections
Initial therapy to reduce viral load
Continue on azole

Question 6

What is the preferred antifungal for deep fungal infection during pregnancy

Answer 6

Amphoteracin B

Question 7

Amphoteracin B administration

Answer 7

IV

Intrathecal if meningeal disease

Question 8

Amphoteracin B AE

Answer 8

Renal toxicity
Anemia - Decreased EPO
Seizures in intrathecal
Fever, chills, muscle spasms, HA, hypotension

Question 9

How do you reduce nehphrotoxicity with Amphoteracin B

Answer 9

Lipid colloid

Question 10

How does Flucytosine work

Answer 10

Enters cell via cytosine permease
Converted to 5-FU then 5-FdUMP/5-FUMP
Inhibits Thymidylate Synthase
Incorporates into protein
DNA and Protein synthesis inhibition

Question 11

What is Flucytosine used for

Answer 11

Candida

Cryptococcal

Question 12

How does Flucytosine cause BM toxicity

Answer 12

Formation of 5-FU from gut flora

Question 13

Synergistic with Flucytosine

Answer 13

Amphoteracin B

Question 14

Imidazoles

Answer 14

Ketoconazole
Miconazole
Clotrimazole

Question 15

How do the azoles work

Answer 15

Inhibit 14-alpha sterol demethylase
Blocking conversion of lanosterol to ergosterol
Membrane disruption

Question 16

What are the triazoles

Answer 16

Fluconazole
Itraconazole
Voriconazole
Posaconazole

Question 17

Which azoles are less specific for fungal CYP

Answer 17

Imidazoles

Question 18

DOC candida and most coccidioides

Answer 18

Fluconazole

Question 19

Inhibitor of 3A4

Answer 19

Azoles
Fluco - moderate but strong 2C9
Voriconazole - also 2C9, 2C19

Question 20

What do imidazoles potentiate the toxicity of

Answer 20

Warfarin

Cyclosporine

Question 21

Since it has a narrow spectrum what should imidazoles be used for

Answer 21

Superficial mycoses

Question 22

Why can PPIs and H2 blockers interfere with Ketoconazole absorption

Answer 22

Best absorbed at low pH

Question 23

Imidazole AE

Answer 23

Gynecomastia
Menstrual irregularities
Decreased plasma cortisol (inhibition of adrenal steroid synthesis)

Question 24

Which imidazoles are available as topical OTC

Answer 24

Clotrimazole

Miconazole

Question 25

Maintenance therapy or prophylaxis for cryptococcal meningitis

Answer 25

Fluconazole (after Amphoteracin B initial)

Question 26

Which azoles can penetrate CSF

Answer 26

Fluconazole

Question 27

What is the only azole that has renal excretion

Answer 27

Fluconazole

Question 28

What can Fluconazole increase the plasma levels of

Answer 28

Phenytoin Zidovudine Warfarin

Question 29

What is Fluconazole not good for

Answer 29

Aspergillus and other filamentous fungi

Question 30

What is the absorption of Itraconazole reduced by

Answer 30

H2 blockers and PPIs

Question 31

What is Itra/Vori/Posaconazole given for

Answer 31

``` Aspergillus Blastomycoses Sporothrix Histoplasma Dermatophytosis Onychomycosis ```

Question 32

When can Itraconazole cause fatal arrhythmias

Answer 32

When given with Cisapride or Quinidine

Question 33

DOC invasive aspergillosis

Answer 33

Voriconazole

Question 34

Voriconazole AE

Answer 34

Transient visual disturbance

Question 35

Good for Mucor

Answer 35

Posaconazole

Question 36

How does Caspofungin act

Answer 36

Inhibits beta (1.3) glucan synthesis in cell wall

Question 37

What does Caspofungin act on

Answer 37

Candida | Aspergillus

Question 38

What is Caspofungin ineffective against

Answer 38

C. neoformans

Question 39

Structure of Caspofungin

Answer 39

Large cyclic peptide linked to long chain FA

Question 40

How does Griseofulvin work

Answer 40

Disrupt mitotic spindle

Question 41

What is Griseofulvin for

Answer 41

Dermatophysis (skin, hair, nails)

Question 42

How do you improve Griseofulvin absorption

Answer 42

Give with fatty food

Question 43

Induces P450

Answer 43

Griseofulvin

Question 44

Action of Terbinafine

Answer 44

Inhibitis Squalene Epoxidase | No ergosterol and toxic levels of squalene

Question 45

Most effective against Onychomycosis

Answer 45

Terbinafine

Question 46

Is an Allylamine

Answer 46

Terbinafine

Question 47

Accumulates in keratin

Answer 47

Terbinafine

Question 48

No effect on P450

Answer 48

Terbinafine

Question 49

Terbinafine AE

Answer 49

GI upset | Rash, HA, taste disturbance

Question 50

Topical cream use of Terbinafine

Answer 50

Tinea cruris, corporis

Question 51

What is Nystatin

Answer 51

Polyene macrolide

Question 52

What is Nystatin similar to

Answer 52

Amphoteracin B (structure and action)

Question 53

What is the only use of Nystatin

Answer 53

Candidiasis | Cutaneous oral/vaginal administration

Question 54

Why isn't Nystatin given IV

Answer 54

Too toxic

Question 55

What else can you give for cutaneous candidiasis

Answer 55

Topical Amphoteracin B