Sweatman antifungals from chapter 48

Question 1

T/F with advances in medicine, fungal infections are decreasing

Answer 1

False

Question 2

T/F Amphotericin B is completely ineffective if given orally

Answer 2

False, oral Amphotericin B can treat GI fungus

Question 3

T/F Amphotericin B is highly bound to serum proteins

Answer 3

True

Question 4

Half life of Amphotericin B?

Answer 4

15 days

Question 5

Where is Amphotericin B distributed? What tissues?

Answer 5

All tissues except CNS

Question 6

Whats the benefit of Liposomal Amphotericin B?

Answer 6

Lipid transporter of Amphotericin allows for higher doses and less toxicity without losing effects

Question 7

Amphotericin B’s mechanism of action please?

Answer 7

Binds to ergosterol on fungus membranes and causes pore formation

Question 8

How can a fungus become resistant to Amphotericin B?

Answer 8

If ergosterol binding is impaired, of course!

Question 9

How can this happen?

Answer 9

Reducing or modifying ergosterol on fungal membranes

Question 10

Antifungal agent with broadest spectrum of action?

Answer 10

Amphotericin B

Question 11

For treatment of systemic fungal disease, how is amphotericin B administered?

Answer 11

Slow IV infusion

Question 12

Most common toxic reaction for Amphotericin?

Answer 12

Renal damage

Question 13

Name of the fungal enzyme that metabolizes flucytosine leading to the drug’s selective toxicity in fungi

Answer 13

Cytosine permease

Question 14

Mechanism of action of azoles please?

Answer 14

Inhibit fungal CYP450’s thus reducing ergosterol production

Question 15

T/F Azoles are usually highly toxic

Answer 15

False, they are relatively nontoxic. Most common adverse reaction is a minor upset stomach

Question 16

Why are azoles so ready to have adverse reactions?

Answer 16

Because they act on CYP450s. They inhibit fungal cyp450, but we have them too! Lots of adverse interactions

Question 17

Intraconazole has reduced bioavailability when taken in conduction with what drug?

Answer 17

Rifamycins

Question 18

Treating HBS (histoplasma, blastomyces, sporothrix). what azole to use?

Answer 18

Itraconazole

Question 19

Widest theraputic index of the azoles?

Answer 19

Fluconazole

Question 20

Fluconazole has a low or high penetration of CSF?

Answer 20

HIgh, it gets in that CSF like a sum bitch

Question 21

Azole with most inhibition of CYP3A4?

Answer 21

Vericonazole

Question 22

Vericonazole has what common side effect?

Answer 22

Vision disturbances

Question 23

Treatment of choice (TOC) for invasive aspergillosis?

Answer 23

Vericonazole

Question 24

This azole is particularly high distributing in tissues

Answer 24

Posaconazole

Question 25

Broadest spectrum anti fungal of the azole family

Answer 25

Posaconazole (has activity against most sp. of Candida and Aspergillus)

Question 26

Caspofungin, micafungin, anidulafungin all belong to a group of anti-fungals called?

Answer 26

Echinocandins

Question 27

Mechanism of action of echinocandins please?

Answer 27

Inhibit beta-glucan in fungal cell walls

Question 28

What treats systemic dermatophytosis?

Answer 28

Griseofulvin

Question 29

Mechanism of action of Terbinafine please?

Answer 29

Inhibits squalene epoxidase