Fungal Pharmacology Flashcards
What are the three species of fungi that cause human infection?
Trichophyton, Microsporum, Epidermophyton
What are the topical azole antifungals?
Clotrimazole (Lotrimin) ointment; (Desenex) powder, Miconazole (Micatin, Monostat Derm), Ketoconazole (Nizoral)
What are the indications for topical azole antifungals?
Tinea corporis, tinea cruris, tinea pedis, cutaneous candidiasis.
What are CI of topical azole antifungals?
Pregnancy, lactation. Use with caution in liver failure. Ketoconazole not for use in asthma patients or history of sulfa allergy
What are indications and CI of clotrimazole?
Cutaneous candidiasis (topical), Vulvovaginal candidiasis (topical), Oropharyngeal candidiasis (oral). CI: Hypersensitivity
What are adverse effects of clotrimazole?
Topical: vulvovaginal burning. Oral: Abnormal LFTs, Pruritus, N/V
What are indications/CI of mycostatin?
Cutaneous and mucocutaneous infections caused by Candidia. Oral and intestinal Candidia infections. CI: Hypersensitivity to mycostatin
What are adverse effects of mycostatin?
Contact dermatitis. Stevens-Johnson syndrome. Oral: N/V, diarrhea
What are the systemic azole antifungals?
Ketoconazole (Nizoral), Itraconazole (Sporanox), Fluconazole (Diflucan)
Why is ketoconazole restricted to treatment of life threatening fungal infections?
hepatotoxicity, decreased adrenal corticosteroid secretion, QT prolongation, inhibitor of CYP450 (many drug interactions)
What potential life threatening infections could ketoconazole be used for if all other options failed?
Blastomycosis, coccidiomycosis, histoplasmosis, chromomycosis, paracoccidioiodmycosis. Should NOT be used for candida or dermatophyte infections
What are indications for Itraconazole (Sporanox)?
Aspergillosis, Blastomycosis, Esophageal and oropharyngeal candidiasis (oral soln), Coccidioidomycosis, Histoplasmosis, Onychomycosis
What are CI to itraconazole (Sporanox)?
Hypersensitivity. Use of other drugs that need CYP450 system. Ventricular dysfunction (negative inotrope): will further reduce ejection fraction
CHF. Pregnancy or intend to become pregnant
What are the pharmacodynamics of itraconazole?
Requires gastric acidity. Better absorbed with food (capsule). Solution better absorbed on an empty stomach. 99.8% protein bound. Half life is about 21 hours
What are adverse effects of itraconazole?
Nausea, diarrhea, Edema, Headache, Rash, Abnormal LFTs, Heart failure, Arrhythmia, Hearing loss
What monitoring is needed with itraconazole?
Baseline liver function tests. Monthly LFTs. Serum concentrations to assure therapeutic levels after 2 weeks of therapy
What are indications for Fluconazole (Diflucan)?
Blastomycosis-CNS. Candidiasis-Candidemia, endocarditis, oropharyngeal, prophylaxis, vaginal.
Coccidioidomycosis-Meningitis, pneumonia, prophylaxis. Crypococcosis-Meningitis, pneumonia
What are CI to fluconazole?
Hypersensitivity. Coadministration of CYP3A4 substrates which may lead to QT prolongation (cisapride, primozide or quinidine)
What are the pharmacokinetics/dynamics of fluconazole?
Good penetration into CSF, eye, peritoneal fluid, sputum, skin and urine. Half life is 30 hours
What are some commonly used drugs the fluconazole interacts with?
statins, viagra, warfarin, sulfonylureas, PPIs, antihypertensives, benzos, macrolides, fentanyl
What are adverse effects of fluconazole?
Pregnancy category C/D, Headache, dizziness, N/V, diarrhea, Elevated LFTs, QT prolongation
What monitoring needs to be done with fluconazole?
Baseline liver function tests. Periodic liver function, renal function, and potassium
What are indications for Terbinafine (Lamisil)?
Oral/systemic formulation-Oncychomycosis, Tinea capitis. Topical-Tinea pedis, Tinea cruris, Tinea corporis
What are the pharmacodynamics/kinetics of Terbinafine (Lamisil)?
half life 36 h. Distribution to the sebum and skin. 99% plasma bound. Hepatic metabolizm
What are some significant drug interactions with terbinafine (Lamisil)?
for the oral formulation it interferes with metroprolol and tramadol
What are SE of Terbinafine (Lamisil)?
ORAL-Headache, Diarrhea, Elevated LFTs. TOPICAL-Burning, Contact dermatitis, Dryness, Pruritus, Rash
What are indications of Griseofulvin?
Most commonly used for tinea capitis. Also used for tinea infections of the skin, hair and nails
How should griseofulvin be administered?
Fatty meal (peanut butter or icecream) can increase GI absorption. With food or milk to decrease GI upset
What are CI of Griseofulvin?
Liver failure, Porphyria, Pregnancy (category X). penicillin allergy has potential for cross reactivity.
Breast feeding not recommended
What monitoring needs to be done with Griseofulvin?
Renal fxn, liver fxn, CBC to watch for granulocytopenia
What are potential drug interactions of Griseofulvin?
Warfarin, oral contraceptives, barbiturates, cyclosporine. If taken w/alcohol can cause N/V, dizziness, palpitations
What are the indications for amphotericin B?
severe systemic and CNS infections that are progressive and potentially life threatening
What are SE of amphotericin B?
Anaphylaxis, infusion reaction, leukoencephalopathy (damage to brain white matter), nephrotoxicity
What needs to be monitored with amphotericin B?
renal and liver function, electrolytes, PT/PTT, CBC
What are drug interactions with amphotericin B?
aminoglycosides, antifungal agents, corticosteroids, cyclosporine
