Drugs for fungal infections, head lice, hyperhidrosis, hair growth and pigmentation - Sweatman Flashcards
what is the unique, significnat adverse effect of ketoconazole use that were the subject of a recent FDA article?
Adrenal insufficiency - ketoconazoles ability to disrupt steroid synthesis
what are 2 common adverse effects shared by all azoles
Hepatotoxicity
Drug-drug interactions via CYP interactions
what are 3 BBW associated with Itraconazole use? Why does it carry these?
Heart Failure
Ventricular dysfunction
Co-administration with drugs (CYP)
Itraconazole produces negative inotropic effects on the heart
Are azoles safe in pregnancy?
no
Are azoles safe in breast feeding?
no - potential of the drug to pass to infant
which azoles produce QT prolongation?
Fluconazole, Psoaconazole, Voriconazole
Which azole are you worried about visual disturbances due to optic neuritis?
Voriconazole
Which azole are you worried about photosensitization of skin?
Voriconazole
which azole must be administered with a full meal for adequate bioavailability?
Posaconazole
This is a potential test question
You have a pt that has a fungal infection and renal failure - what azole can you not give, or at least need to dose adjust?
Fluconazole
most azoles are extensively hepatically metabolized, but fluconazole is metabolized and eliinated renally
which azoles have access to CSF?
Fluconazole and Voriconazole
What is the MOA of Griseofulvin?
binds microtubules, disrupts the mitotic spindle - thus inhibits fungal growth
what is the effect of Griseofulvin on CYP?
it is a CYP3A4 inducer (azoles are inhibitors)
is Griseofulvin safe in pregnancy?
no
What drug allergy in a pt would make you not want to give Griseofulvin?
Penicillin allergy
commonality in structure with Beta lactams
What is the MOA of Terbinafine and Naftifine (allylamines)?
inhibit squalene epoxidase, a step in ergosterol synthesis
is terbinafine safe in pregnancy?
yes
what precautions do you need to take with Terbinafine?
CBCs and LFTs
what is an important point about the allylamines and azoles in combination therapy?
both classes work to block ergosterol incorporation into fungal cell walls - there is no gain in combining the two classes
what is the route of delivery for Ciclopirox and Amorolfine?
TOPICAL ONLY
for review only, what is the MOA of azoles? what enzyme do they inhibit?
inhibit the cytochrome P450 enzyme sterol 14 demethylase
blocks production of ergosterol
for review only, what is the MOA of capsofungin (and Echinocandin)
inhibits 1,3-B-glucan synthase
results in disruption of cell wall integrity
for review only, what is the MOA of amphotericin B?
binds ergosterol and creates pores in the fungal cell membrane
what is the general mechanism used to treat hyperhidrosis?
anti-cholinergics
from the CNS, what causes activation of Eccrine (thermoregulatory) sweat glands?
sympathetic innervation with Ach as neurotransmitter, rather than customary NE
(the nerves innervating eccrine, or thermoregulatory, sweat glands are sympathetic cholinergic nerves, this is unique)