Voriconazole

Products

Voriconazole is commercially available as film-coated tablets, powder for the preparation of an infusion solution, and powder for the preparation of a suspension (Vfend, generics). It has been approved in many countries since 2002.

Structure and properties

Voriconazole (C16H14F3N5O, Mr = 349.3 g/mol) exists as a white powder that is very sparingly soluble in water. It is a fluorinated pyrimidine derivative and a triazole antifungal agent. Voriconazole is derived from fluconazole.

Effects

Voriconazole (ATC J02AC03) has antifungal properties with a broad spectrum of activity against , , and . Effects are based on inhibition of lanosterol 14α-demethylase, ergosterol biosynthesis, and consequent disruption of cell wall assembly.

Indications

For the treatment of severe fungal infections with susceptible pathogens.

Dosage

According to the SmPC. The infusion is administered intravenously. Oral drugs must be taken fasting, at least one hour before or two hours after a meal.

Contraindications

For complete precautions, see the drug label.

Interactions

Voriconazole has a high potential for drug-drug interactions. It is metabolized by CYP2C19, CYP2C9, and CYP3A4 and is a CYP inhibitor. Combination with carbamazepine, CYP3A4 substrates that prolong the QT interval, efavirenz, ergot alkaloids that are CYP3A4 substrates, St. John’s wort preparations, phenobarbital, rifampicin, high-dose ritonavir, and sirolimus is contraindicated.

Adverse effects

The most common potential adverse effects include vomiting, nausea, diarrhea, abdominal pain, fever, peripheral edema, rash, headache, and visual disturbances. Voriconazole may prolong the QT interval.