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AN OVERVIEW OF AZOLE ANTIFUNGALS

Ketoconazole can interfere with synthesis of certain Steroid Hormones especially adrenocortical hormones (i.e.

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TABLE 2: AZOLES AS ANTIFUNGAL AGENTS

Drug Interactions – Posaconazole is primarily metabolized through UDP glucuronidation and is also a substrate of P-gp.1 Any drug that inhibits or induces these clearance pathways may alter serum concentrations of posaconazole. Drugs that increase gastric pH, such as proton pump inhibitors, H2-receptor blockers or antacids, may decrease the absorption of posaconazole. Posaconazole is a strong inhibitor of CYP3A4 and may increase serum concentrations of drugs that are metabolized by this enzyme. Posaconazole is contraindicated for use with sirolimus, ergot alkaloids, and CYP3A4 substrates that also prolong the QT interval. It should be used with caution with other drugs known to prolong the QT interval.

The triazoles also secondarily target other steps in the ergosterol biosynthesis pathway.

Itraconazole is a strong inhibitor of CYP3A4 and may significantly increase serum concentrations of drugs metabolized by this enzyme. It is contraindicated for use with some drugs that are metabolized by CYP3A4, particularly those known to prolong the QT interval. Itraconazole may increase the serum concentrations and negative inotropic effects of calcium channel blockers. It is also a P-gp inhibitor and can increase serum concentrations of P-gp substrates.

TABLE 3: SPECTRUM OF ACTIVITY OF AZOLES

VORICONAZOLE — Voriconazole (Vfend) has a spectrum of activity similar to that of itraconazole but appears to be more active against Aspergillus spp. and most species of Candida, including C. glabrata and C. krusei. Unlike itraconazole, voriconazole is active against Fusarium spp. and Scedosporium spp. It is not active against Sporothrix spp. or Zygomycetes; infection with these organisms has developed during treatment with voriconazole. In a randomized trial of initial treatment of invasive aspergillosis, voriconazole improved survival compared to amphotericin B and caused fewer severe adverse effects.

Patients with mild to moderate hepatic insufficiency should receive a normal loading dose of voriconazole, but half the maintenance dose. Serum concentrations of voriconazole may need monitoring; they vary from patient to patient and with the formulation used (lower with capsules and higher with the solution). Children need a higher per-kg dose than adults because they clear the drug more rapidly.

TABLE 5: ADVERSE EFFECTS OF AZOLES

Adverse Effects – Transient visual disturbances including blurred vision, photophobia and altered perception of color or image have occurred in about 20% of patients treated with voriconazole. Rash (including Stevens-Johnson syndrome), photosensitivity, increased transaminase levels, confusion and hallucinations have also occurred. In patients with creatinine clearance

Itraconazole is a substrate of CYP3A4 and P-glycoprotein (P-gp); its metabolism may be affected by both inducers and inhibitors of these pathways.

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  • Ketoconazole Cream Drug Information

    AZOLES

  • Oral Azole Drugs as Systemic Antifungal Therapy — …

    Azole antifungal agents inhibit synthesis of ergosterol, an essential component of the fungal cell membrane.

  • Azole Antifungals | Pathway Medicine

    Como JA, and Dismukes WE: Oral azole drugs as systemicantifungal therapy. New Engl J Med 330:263-272, 1994

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Resistance of yeasts to azole derivative antifungals.

Drug Interactions – Voriconazole is a substrate of CYP2C19, 2C9, 3A4 and P-gp. Drugs that inhibit or induce one or more of these clearance pathways may significantly alter serum concentrations of voriconazole. Patients deficient in CYP2C19 (about 3-5% of Caucasians and African-Americans and about 15% of Asians do not express it) may have 2- to 4-fold higher serum concentrations of voriconazole.

Antifungal Drugs, Azole Antifungal Drugs, Allylamine …

Voriconazole is an inhibitor (in vitro) of CYP2C9, 3A4 and, to a lesser extent, 2C19; it may significantly increase serum concentrations of drugs metabolized by these enzymes. Concurrent use of voriconazole with other drugs that prolong the QT interval, particularly those metabolized by CYP2C9, 2C19 or 3A4, may increase the risk of QT prolongation and torsades de pointes.

Synthesis and antifungal activity investigation of a …

Two other classes of antifungal agents represent new additionsto topical treatment of the dermatomycoses in Europe. The twoallylamines (naftifine and terbinafine) inhibit ergosterolsynthesis at the level of squalene epoxidase; one morpholenederivative (amorolfine) inhibits at a subsequent step in theergosterol pathway.

Synthesis and antifungal activity investigation of a ..

POSACONAZOLE — Posaconazole (Noxafil), the newest triazole, has an antifungal spectrum similar to that of itraconazole, but its in vitro activity is about twice as great; it can be used to treat Fusarium spp. and Scedosporium spp. and has up to 4-fold greater activity against many species of Mucor, such as Absidia spp. Posaconazole is only available for oral use and must be taken with meals for optimal absorption.

Structures of synthesised azole agents have ..

With the advent of the polyenes, azoles, and fluorocytosine,previously fatal infections can now be treated. However, asmodern medicine continues to extend life through aggressivetherapy of other life-threatening diseases such as cancer, thereis an increasing population at risk for opportunistic fungalinfections. Such patients represent a special challenge becausethey often are left with little host immune function. Therefore,chemotherapeutic agents should be fungicidal and not justfungistatic. The search continues for fungicidal agents that arenontoxic to the host. Research is also directed towardimmunomodulating agents that can reverse the defects of nativehost immunity.

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