I'm the azole drug of choice for invasive Aspergillus. I'm also used to treat some other drug-resistant fungal infections.
I'm a major class of antifungals with a name reflecting the presence of a 5 member ring containing a nitrogen, and at least one other non-carbon atom (e.g. nitrogen, sulfur or oxygen). We inhibit a P450 demethylase that is involved in the synthesis of a key component of the fungal cell membrane. We also are notorious for causing drug interactions because we inhibit human CYP3A4.
I don't get absorbed into the systemic circulation if taken orally, but I am used to treat oropharyngeal and vaginal Candidiasis. I bind selectively to ergosterol, and make fungal cells leaky!
I'm perhaps more famous than my other family members, but because I inhibit P450 and lower testosterone levels if given systemically, my use is now limited to being a topical agent for treating dermatophytosis, candidiasis, and seborrheic dermatitis.
I have some toxic side effects, including hypersensitivity infusion reactions (nausea, vomiting, fever) and nephrotoxicity, which can result in mulitple electrolyte disturbances that can affect a patient's ECG. I am usually given in liposome or lipid complex formulations. Despite all these side effects, I'm a drug of choice for severe/systemic mycotic infections, including Candida, Cryptococus & many molds like Aspergillus.
Combined with Amphotericin B for treating systemic Candida or Cryptococcal infections. Not used as monotherapy due to rapid development of resistance. Converted to an active metabolite by an enzyme present only in fungal cells. Which drug am I?
I have a kind of greasy name, and while I'm not used so much any more, I am effective for systemic treatment of dermatophyte infections.
I inhibit squalene expoxidase, ultimately resulting in reduced ergosterol biosynthesis. Highly lipophilic, and accumulates in skin & nails. A go-to antifungal for dermatophyte infections.
Verticales
This group of antifungals contains two commonly used drugs that are amphipathic, and bind to ergosterol to produce a fungicidal effect
I'm only given orally, and don't get into the CSF very well. I'm mainly used to treat endemic mycoses. I'm a potent inhibitor of CYP3A4. When given along with other drugs that prolong the QTc and which are CYP3A4 substrates, I can elevate their plasma levels to cause serious cardiac arrhythmias.
I rhyme with the major component of LDL, but I'm only found in fungal cell membranes. I'm a target for several classes of antifungal drugs.
All the members of this family of antifungals have "fun" in their name, and are used for empiric treatment of invasive Candida infections.
I'm one of the newest, and the most broad spectrum of the azoles.
I'm safer than the first member of my family, with fewer drug interactions. I have good CNS penetration. I am a preferred prophylactic treatment for cryptococcus. Effective against Candida (which can cause thrush or esphagitis). I'm not effective against Aspergillus or molds.
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