Pharmacology of Voriconazole Mechanism of action Pharmacokinetics Uses Effects
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Voriconazole is a broad-spectrum triazole antifungal medication used to treat serious fungal infections. Here's an overview of its pharmacology: • Mechanism of Action • Voriconazole works by inhibiting the enzyme lanosterol 14α-demethylase, which is essential for the synthesis of ergosterol, a key component of fungal cell membranes. This disruption in ergosterol synthesis leads to increased membrane permeability and ultimately fungal cell death1. • Pharmacokinetics • Absorption: Voriconazole has high oral bioavailability (approximately 96%) and can be administered both orally and intravenously. • Distribution: It is widely distributed throughout the body, with a volume of distribution of approximately 4.2 L/kg. It is highly protein-bound (58-98%)2. • Metabolism: Voriconazole is extensively metabolized in the liver by cytochrome P450 enzymes, primarily CYP2C19 and CYP3A4. • Elimination: The elimination half-life is approximately 6 hours, but this can vary significantly between individuals due to genetic polymorphisms in CYP2C19. • Excretion: Voriconazole is excreted primarily in the urine (approximately 80%) and to a lesser extent in the feces. • Uses • Voriconazole is used to treat a variety of serious fungal infections, including: • Invasive Aspergillosis: A severe infection caused by Aspergillus species. • Invasive Candidiasis: Infections caused by Candida species. • Scedosporium and Fusarium Infections: Emerging fungal infections that are often resistant to other antifungal agents. • Effects • Efficacy: Voriconazole has shown high efficacy in treating invasive fungal infections, particularly those resistant to other antifungal drugs. • Side Effects: Common side effects include visual disturbances, liver enzyme abnormalities, skin rash, and gastrointestinal symptoms3. • Drug Interactions: Voriconazole can interact with many other medications, including those metabolized by CYP2C19 and CYP3A4, which can lead to increased toxicity or reduced efficacy • #Voriconazole
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