Voriconazole tablets

1. The mechanism of action of voriconazole is to inhibit the demethylation of 14α-sterol mediated by cytochrome P450 in fungi, thereby inhibiting the biosynthesis of ergosterol. In vitro tests have shown that voriconazole has a broad-spectrum antifungal effect. This product has antibacterial effects on Candida species (including fluconazole-resistant Candida krusei, Candida glabrata and Candida albicans resistant strains) and has a bactericidal effect on all Aspergillus fungi tested. In addition, voriconazole also has a bactericidal effect on other pathogenic fungi in vitro, including species with low sensitivity to existing antifungal drugs, such as Actinomyces and Fusarium. Animal experiments have found that the minimum inhibitory concentration value of voriconazole is related to its efficacy. However, in clinical studies, there is no correlation between the minimum inhibitory concentration and clinical efficacy, and there seems to be no correlation between the blood concentration of the drug and the clinical efficacy. This is a characteristic of azole antifungal drugs. 2. Microbiology: Clinical trials have shown that voriconazole has clinical efficacy (improvement or cure, see the clinical experience section below) against Aspergillus, including Aspergillus flavus, Aspergillus fumigatus, Aspergillus terreus, Aspergillus niger, and Aspergillus nidulans; Candida, including Candida albicans, and some Candida dubliniensis, Candida glabrata, C. incopicua, Candida krusei, Candida parapsilosis, Candida tropicalis, and Candida guillimonda; Actinomyces, including Mycoplasma apiaceum and Mycoplasma prolificum, and Fusarium. 3. Other fungal infections that are effective (usually cured or improved) with voriconazole include Alternaria, Blastomyces dermatitidis, Blastomyces head division, Cladosporium, Coccidioides immitis, Coronary Ear Mold, Cryptococcus neoformans, Beak-shaped Aureobasidium, Ectoplasma spinulosa, Peyer's Chromosomes, Madura mycetoma, Paecilomyces, Penicillium, including Penicillium manifestosus, Wood Bottle, Scopulariopsis and Trichosporon, including white Trichosporon infection. 4. In vitro tests have observed that voriconazole has antibacterial effects on the following clinically isolated fungi, including Acremonium, Alternaria, Dipolaris, Cladosporium, Cladophialophoraspp., and Capsular Histoplasma. 0.05-2μg/ml of voriconazole can inhibit most strains. In vitro tests have shown that voriconazole has antibacterial effects on Curvularia and Sporothrix, but its clinical significance is still unclear. Before treatment, specimens should be collected for fungal culture, and other relevant laboratory tests (serological tests and histopathological tests) should be performed to isolate and identify pathogens. Anti-infection treatment must be carried out before obtaining the results of culture and other laboratory tests, but once the results are obtained, the medication regimen should be adjusted accordingly. Clinical strains with reduced sensitivity to voriconazole have been found. However, an increase in the minimum inhibitory concentration value does not necessarily lead to clinical treatment failure. There are also patients with clinically effective treatments for infections caused by other azole-resistant strains. Due to the complexity of the patients enrolled in clinical trials, it is difficult to determine the relationship between in vitro antibacterial activity and clinical treatment outcomes. The critical concentration of voriconazole in drug sensitivity tests has not yet been established. Resistance: There is no sufficient research on the in vitro resistance of Candida, Aspergillus, Actinomycetes, and Fusarium to voriconazole. 5. The development of resistance to various fungi in the antibacterial spectrum of voriconazole is currently unknown. Fungi with reduced susceptibility to fluconazole and itraconazole may also have reduced susceptibility to voriconazole, suggesting that cross-resistance may exist among these azole drugs. The relationship between cross-resistance and clinical efficacy has not been fully established. If the isolates of clinical cases show cross-resistance, other antifungal drugs may be needed for treatment.

Voriconazole. Chemical name: (2R, 3S)-2-(2,4-difluorophenyl)-3-(5-fluoro-4-pyrimidine)-1-(1H-1,2,4-triazol-1-yl)-2-butanol

This product is a film-coated tablet, which appears white to off-white after removing the coating.

This product is used to treat invasive aspergillosis, severe invasive candidiasis infections resistant to fluconazole (including Candida krusei), and severe fungal infections caused by Actinomyces and Fusarium. It is mainly used for patients with progressive, life-threatening immune damage.

Voriconazole film-coated tablets should be taken at least 1 hour before or 1 hour after a meal.

The most common adverse events in the treatment trials were visual disturbances, fever, rash, nausea, vomiting, diarrhea, headache, sepsis, peripheral edema, abdominal pain, and respiratory dysfunction. The most common adverse events related to treatment that led to discontinuation included increased liver function test values, rash, and visual disturbances.

This product is contraindicated in patients with a known history of hypersensitivity to voriconazole or any of the excipients. This product is contraindicated for use with CYP3A4 substrates, terfenadine, astemizole, cisapride, pimozide or quinidine, because this product can increase the blood concentration of the above drugs, resulting in Q-T interval prolongation and occasional torsade de pointes ventricular tachycardia (see [Drug Interactions]). This product is contraindicated for use with rifampicin, carbamazepine and phenobarbital, the latter of which can significantly reduce the blood concentration of this product. This product should not be used in combination with ergot alkaloids (ergotamine, dihydroergotamine). Ergot alkaloids are substrates of CYP3A4. After the two are used together, the increased blood concentration of ergot drugs can lead to ergot poisoning. When sirolimus is used in combination with voriconazole, the blood concentration of the former may increase significantly.

Precautions for children: The safety and efficacy of voriconazole in children under 12 years old have not been established. In the therapeutic study, 22 patients with invasive aspergillosis aged 12-18 years were enrolled and given a maintenance dose of voriconazole, i.e. 4 mg/kg once every 12 hours. Twelve patients (55%) were effectively treated. Precautions for pregnancy and lactation: Pregnant women: There is currently insufficient data on the use of voriconazole in pregnant women. Animal experiments have shown that this product has reproductive toxicity (see preclinical safety data), but the potential risk to humans has not yet been determined. Voriconazole should not be used in pregnant women unless the benefits to the mother significantly outweigh the potential toxicity to the fetus. Precautions for the elderly: After intravenous or oral administration of voriconazole, the blood concentration of elderly patients is about 80%-90% higher than that of younger patients. However, the overall safety of the elderly is similar to that of young people, so there is no need to adjust the dose.

1. Voriconazole is prohibited from being dripped in the same intravenous route with other drugs, including parenteral nutrition agents (such as Aminofusin 10% Plus). Voriconazole is physically incompatible with Aminofusin 10% Plus, and the two can produce insoluble particles after being stored at 4°C for 24 hours. Voriconazole should not be dripped simultaneously with blood products or any electrolyte supplements. Voriconazole injection can be dripped intravenously at the same time as total parenteral nutrition solution in a different intravenous route. There is a contraindication for the use of 4.2% sodium bicarbonate intravenous injection with voriconazole. The weak alkalinity of this diluent can cause voriconazole to slightly degrade after being stored at room temperature for 24 hours. Although refrigeration is recommended for the diluted voriconazole solution, it is still not recommended to use 4.2% sodium bicarbonate injection as a diluent.

seal.

200 mg

36 months