Test Two: Antifungals Flashcards
Why does amphoterecin B need to be prepared carefully?
Highly polar-cannot be taken orally, and easily photo-oxidized
Basic mechanism of action for antifungals
Disruption of cell membrane
Denature proteins
Interfere with metabolic processes
Mechanism of action for amphoterecin B?
Fungistatic/cidal depending on dose. Binds to ergosterol to alter cell membrane permeability
How is nystatin/mycostatin diff from amphoterecin b?
Same method of action on ergosterol, but narrower spectrum and does not absorb into skin so it acts locally
Nystatin dosage forms
Lozenges, suspensions for oral thrush, and topical creams in conjunction with steroids like triamcinolone for anti-inflammatory properties
What is the action of griseofulvin?
Fungistatic–affects fungal replication, absorbed well with fatty meals bc of increased bile secretion, can reach hair, skin, and nails
Important facts about azoles
Used for systemic mycoses
Inhibit ergosterol synthesis by blocking an enzyme
Can interfere with steroid hormone formation–don’t take during puberty (esp ketoconazole)
Why shouldn’t ketoconazole be taken with antacids?
They are absorbed readily in acidic environments
How is fluconazole/diflucan diff from ketoconazole?
Well absorbed from GIT with less sensitivity to high pH, less potent inhibitor of steroid hormones, good for systemic use like yeast infxn-only one dose necessary
What is the use of clotrimazole?
Good for topical use (ringworm or athletes foot) , can cause GI upset, available for intraoral use as 10 mg troche
What is used to treat influenza?
Amantadine inhibits viral replication
Osteltamivir (tamiflu) inhibits neuraminidase, should be taken within first days of being infected (like a prophy)
Acyclovir use
Effective against HSV, VZ, CMV (esp immune compromised) as a nucleoside analog–inhibits DNA polymerase and viral synthesis
Acyclovir side effects
Not very prominent bc not taken for a long time, ointment can cause pain/pruritis and tablet can cause nephrotoxicity
Valcyclocir/valtrex
Prodrug of acyclovir, similar to acyclovir except rapid oral absorption and tx acyclovir-resistant HSV (same as Foscarnet-causes electrolyte imbalance) 500-1000mg daily
Nucleoside reverse transcriptase inhibitors (NRTIs)
NRTIs are faulty versions of building blocks that HIV needs to make copies of itself. Ie: zidovudine (AZT)