Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
46 Cards in this Set
- Front
- Back
|
Allylamines |
Terbinafine |
|
|
Terbinafine MOA |
Inhibit Squalene Epoxidase - preventthe formation of lanosterol,which is a precursor for ergosterol. - These drugs also promote accumulation ofthe toxic metabolite in the fungal cell, making them fungicidal undermost circumstances |
|
|
Terbinafine USE |
-DOC for dermatophytosis (Tinea infection) : tineacorporis, tinea cruris, tinea pedis, & tinea capitis -up to 90% cure rate for onychomycosis (Disease of nails of fingers and toes)- more effective than griseofulvinor itraconazole |
|
|
Terbinafine ADVERSE EFFECTS |
- GIT disturbance, rash, headaches - Hepatotoxicity! |
|
|
Terbinafine CONTRAINDICATIONS |
renalor hepatic failure and pregnancy |
|
|
Benzylamine |
Butenafine |
|
|
Butenafine MOA |
Inhibit Squalene Epoxidase- prevent the formation of lanosterol, which is a precursor for ergosterol. - These drugs also promote accumulation of the toxic metabolite in the fungal cell, making them fungicidal under most circumstances |
|
|
Butenafine USE |
-moreeffective thantopical azole agents against commondermatophytes,especially those causing Tinea pedis. -less effective for Candida skin infections |
|
|
Imidazoles |
Ketoconazole Clotrimazole Miconazole |
|
|
Ketoconazole MOA |
-targets14α-sterol demethylase inthe ergosterolsynthesis pathway, which is a microsomal cytochrome P450 enzyme thatconverts lanosterol to ergosterol. -inhibit human p450 enzymes |
|
|
Ketoconazole USE |
•Paracoccidioides, Blastomycoses , Histoplasmosis |
|
|
Ketoconazole ADVERSE EFFECTS |
-Endocrinedisturbances(gynecomastia, infertility, menstrual iregularities)-hepatotoxic, increased plasma level of liver transaminases-Contraindication:Pregnancy |
|
|
Clotrimazole and Miconazole MOA |
-targets 14α-sterol demethylase in the ergosterol synthesis pathway, which is a microsomal cytochrome P450 enzyme that converts lanosterol to ergosterol. -inhibit human p450 enzymes |
|
|
Clotrimazole and Miconazole USE |
Candida, Dermatophytes |
|
|
Triazoles |
Itraconazole Voriconcazole Fluconazole |
|
|
Itraconazole MOA |
targets 14α-steroldemethylase inthe ergosterolsynthesis pathway, which is a microsomal cytochrome P450 enzyme thatconverts lanosterol to ergosterol some interaction with hepatic microsomal p450 enzyme poor penetration in CSF |
|
|
Itraconazole USE |
DOC for Aspergillosis, Blastomycoses, Sporotrichosis |
|
|
Itraconazole ADVERSE EFFECTS |
most common side effects are: Nausea,vomitingGITdisturbance Lesscommon:Hepatotoxicity than ketoconazole but more safe and efficient |
|
|
Voriconazole MOA |
targets 14α-sterol demethylase in the ergosterol synthesis pathway, which is a microsomal cytochrome P450 enzyme that converts lanosterol to ergosterol inhibits hepatic p450 enzymes |
|
|
Voriconazole USE |
DOC for Invasive Aspergillosis and includes Candida species |
|
|
Voriconazole ADVERSE EFFECTS |
-increasedhepatic transaminases. -visualdisturbances whichare common including blurring and changes in the color vision or brightness. |
|
|
Fluconazole MOA |
targets 14α-sterol demethylase in the ergosterol synthesis pathway, which is a microsomal cytochrome P450 enzyme that converts lanosterol to ergosterol |
|
|
Fluconazole ADVANTAGES |
- limited drug-drug interactions - least effect on cytochromeP450 hepatic microsomalenzyme system -Widetherapeutic window ! - Cross BBB |
|
|
Fluconazole USE |
-drugof choice of systemic candidiasis,Cryptococcal meningitis &coccidiodalmeningitis alternative to intrathecal aphotericin B |
|
|
Fluconazole ADVERSE EFFECTS |
-nausea, abdominal distress - alopecia - hepatotoxic (rare) |
|
|
Polyenes |
Amphotericin B Nystatin |
|
|
Amphotericin B MOA |
- actby binding to ergosteroland disruptingfungal membrane stability - Fungicidalagainst mostmycoticinfections |
|
|
Amphotericin B RESISTANCE |
Due to impairment of ergosterolbinding:•decreasingthe membrane concentration of ergosterol •modificationof the sterol target molecule toreduce affinity for the drug |
|
|
Amphotericin B USE |
-Drug of choice for nearly alllife-threatening fungalinfections. (Candida albicans& Cryptococcus neoformans,Histoplasma capsulatum, Blastomyces dermatidis& Coccidioides immitis,Aspergillus,Mucor,Sporothrix) -* It is used with flucytosine to work synergistically in candidiasis and cryptococcus |
|
|
Amphotericin B USE IN IMMUNOSUPPRESSED |
severe fungal pneumonia cryptococcalmeningitis used in neutropenic and cancer patients |
|
|
Amphotericin B ADVERSE EFFECTS (immediate) |
-fever, chills, vomiting andhypotension withinthe first several hours after drug isgiven |
|
|
Amphotericin B ADVERSE EFFECTS (Delayed) |
Renal toxicity (mediatedvasoconstriction of afferent arterioles) Hematologictoxicity- anemia |
|
|
Nystatin MOA |
Increasesthe permeability of the cell membrane of sensitive fungi by binding to sterols |
|
|
Nystatin USE |
DOC for topical treatment of candidiasis such as oropharyngealthrush and vaginal candidiasis |
|
|
Nystatin ADVERSE EFFECTS |
Nausea and vomiting are the main side effects.Too toxic for systemic use. |
|
|
Griseofulvin MOA |
Fungiostatic(derivedfrom Penicillium griseofulvum) Inhibit fungal mitosis Disrupt microtubule mitotic spindle formation Cause mitotic arrest at metaphase Accumulates in keratin precursor cells bind tightly to keratin (allow new growth of skin, hair or nail free of infection) |
|
|
Griseofulvin USE |
Dermatophytosis, Trichophyton,Epidermophyton, Onychomycosis -Mycotic diseases ofskin, hair (particularly for scalp) and nail.It is also highly effective in athlete'sfoot. |
|
|
Griseofulvin ADVERSE EFFECTS |
Allergy.HepatotoxicityDisulfiram-likeeffect |
|
|
Flucytosine MOA |
Inhibit fungal nucleic acid synthesis Enters the fungal cell via a transmembrane cytosine permease. Converted to 5-fluorouracil to 5-FdUMP Potent inhibitor of Thymidylate Synthase Block conversion of dUMP to dTMP Inhibit DNA synthesis |
|
|
Flucytosine USE |
synergistickilling of candidiasis, cryptococcus (neoformans & meningitis) by combinationwith amphotericin B |
|
|
Flucytosine ADVERSE EFFECTS |
Blood: bonemarrow suppression leadingto leukopenia and thrombocytopenia GIT: nausea, vomiting, diarrhea, and reversible hepatic dysfunction. Narrow therapeutic window (toxicityof higher levels; rapid development of resistance at lower,sub-therapeutic levels) |
|
|
Echinocandins |
Caspofungin |
|
|
Caspofungin MOA |
Inhibit fungal wall synthesis Non-competitively inhibit the synthesis of B-(1,3)-D-glucans |
|
|
Caspofungin USE |
fungicidalagainst esophageal candidiasis, candidemia and Aspergillus species |
|
|
Caspofungin DRUG INTERACTION |
cyclosporine significantlyincreases theplasma concentration of caspofungin andelevates liver function enzymes |
|
|
Caspofungin ADVERSE EFFECTS |
headache, fever , abnormal liver functiontests, and GITdistress. |
