Pharm Antifungals

Question 1

*Polyenes (amphotericin, nystatin, natamycin)MOA

Answer 1

• BIND TO ERGOSTEROL (create HYDROPHILIC pores/leaks)

- IMPAIR MEMBRANE MEMBRANE

Question 2

*Allylamines (terbinafine, naftitine) MOA

Answer 2

• Inhibit SQUALENE-2,3-EPOXIDASE (lanosterol synthesis?) synthesis (squalene surplus) (inhibit squalene 2,3 epoxidase)–create deficit of ergosterol
• Impair membrane integrity

Question 3

*Azoles (ketoconazole, clotrimazole, miconazole, tioconazole, fluoconazole) MOA

Answer 3

Inhibit ergosterol synthesis (lanosterol surplus) (inhibit lanosterol 12-alpha-demethylase)–create deficit of ergosterol

Question 4

*Griseofulvin MOA

Answer 4

• BIND TO MICROTUBLES (tubulin, microtubule proteins)

- Impair Mitosis

Question 5

How does a fungus evade polyene MOA?

Answer 5

Ergosterol deficit–so drug can not work

Question 6

*Natamycin used where?

Answer 6

OPTHALAMIC, -CIDAL

Question 7

*Nystatin used where and when?

Answer 7

• MOUTH/ESOPHAGUS. AGAINST CANDIDA
• TOPICAL FORM (too toxic for systemic)
• DIAPER RASH, VAGINAL CANDIDA
• NOT DERMATOPHYTES
• Tablet poorly absorbed, so can reach Candida in intestine

Question 8

*Allylamines used to treat what?

Answer 8

• TINEA ANYTHING, both dugs can treat topical/local problems

- TERMINAFINE (SCALP, FINGER OR TOE NAIL FUNGAL INFECTIONS)

Question 9

*Terbinafine (an allylamine) specifically used when? Contraindication?

Answer 9

• CONTRA IN PREGNANCY
• Systemic and local delivery
• Used to treat Tinea capitis or systemic problems

Question 10

Clotrimazole (an azole) used to treat what?

Answer 10

Oropharyngeal Candidiasis. Use intraconazole for immunocompromised (low yield)

Question 11

*Azoles used to treat what?

Answer 11

• VAGINAL/BLADDER CANDIDA
• OROPHARYNGEAL CANDIDA (THRUSH)
• DERMATOPHYTES AND CANDIDA

Question 12

*Fluconazole (an azole) used to treat what?

Answer 12

• BLADDER INFECTION

- 75% renal excretion

Question 13

*Griseofulvin used when? And eliminated how?

Answer 13

• static
• -DERMATOPHYTES, NOT CANDIDA
• TINEA CAPITIS or widespread tinea
• CYP450 INDUCTION, AVOID ALCOHOL

Question 14

Don’t use cortical steroids along side treatment

Answer 14

factual info (low yield?)

Question 15

*TERBINAFINE uses

Answer 15

-DERMATOPHYTES, WEAK AGAINST CANDIDA