Voriconazole for injection

The mechanism of action of voriconazole is to inhibit the demethylation of 14alpha-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 clinical efficacy. This is a characteristic of azole antifungal drugs. Microbiology: Clinical trials have shown that voriconazole has clinical efficacy (improvement or cure, see the Clinical Experience section below) against Aspergillus species, including Aspergillus flavus, Aspergillus fumigatus, Aspergillus terreus, Aspergillus niger, and Aspergillus nidulans; Candida species, including Candida albicans, and some Candida dubliniensis, Candida glabrata, C. inconspicua, Candida krusei, Candida parapsilosis, Candida tropicalis, and Candida guillimonda; Actinomyces species, including Mycoplasma apiaceum and Mycoplasma prolificum, and Fusarium species. Other fungal infections that respond to voriconazole (usually cured or improved) include Alternaria, Blastomyces dermatitidis, Blastomyces head, Cladosporium, Coccidioides immitis, Otocorona, Cryptococcus neoformans, Acanthophorum spp., Exophialum spinulosum, Chromosporium persei, Madura mycetoma, Paecilomyces, Penicillium, including Penicillium manifestum, Xylella fastidiosa, Scopulariopsis brevis, and Trichosporon, including Trichosporon albicans. In vitro studies have observed that voriconazole has antibacterial activity against the following clinically isolated fungi, including Acremonium, Alternaria, Diplodia, Cladosporium, Cladophialophora spp., and Histoplasma capsulatum. Voriconazole at 0.05-2 mu; g/ml can inhibit most strains. In vitro studies have shown that voriconazole has antibacterial activity against Curvularia and Sporothrix, but its clinical significance is 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 culture results and other laboratory test results, 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 treatment in infections caused by other azole-resistant strains. Due to the complexity of 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 not enough research on the in vitro resistance of Candida, Aspergillus, Actinomycetes, and Fusarium to voriconazole. It is currently unknown how the resistance of various fungi in the antibacterial spectrum of voriconazole develops. 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.

The main ingredient of this product is voriconazole.

This product is white or off-white loose mass or powder.

This product is a broad-spectrum triazole antifungal drug with the following indications: Treatment of invasive aspergillosis. Treatment of severe invasive infections caused by Candida species resistant to fluconazole (including Candida krusei). Treatment of severe infections caused by Actinomyces and Fusarium species. This product should be used primarily to treat progressive, potentially life-threatening infections in immunocompromised patients.

This product should be dissolved into 10mg/ml before intravenous drip, and then diluted to 2-5mg/ml. This product should not be used for intravenous push injection. It is recommended that the fastest intravenous drip rate of this product should not exceed 3mg/kg per hour, and the drip time for each bottle after dilution should be more than 1 to 2 hours. For adult medication, the interchangeable use of intravenous drip and oral administration, whether it is intravenous drip or oral administration, the first loading dose should be given on the first day of the first administration, so that the blood drug concentration is close to the steady-state concentration on the first day of administration. Since the bioavailability of oral tablets is very high (96%), the two routes of administration of intravenous drip and oral administration can be interchanged when there is a clinical indication. Oral: Patients weighing >40kg, Patients weighing <40kg Loading dose: 400 mg once every 12 hours 200 mg once every 12 hours (applicable to the first 24 hours) Maintenance dose (initial medication, 200 mg twice a day, 100 mg twice a day, 24 hours later)

Overall: 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.

Precautions for children: Please refer to the [Usage and Dosage] for details. 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. Women of childbearing age Women of childbearing age should take effective contraceptive measures during the use of voriconazole. There is no data on the secretion of voriconazole in breast milk in lactating women. Voriconazole should not be used by lactating women unless the benefits clearly outweigh the risks.

Voriconazole is prohibited from being dripped in the same intravenous line 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 storage 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 line. 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 storage 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. The compatibility of this product with other concentrations of sodium bicarbonate solutions is unclear. 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. 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 cannot be used in combination with ergot alkaloids (ergotamine, dihydroergotamine). Ergot alkaloids are substrates of CYP3A4. After the two are used together, the increase in the 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, so these two drugs cannot be used at the same time. This product is contraindicated for use with ritonavir (400 mg each time, once every 12 hours). When healthy subjects were given ritonavir (400 mg each time, once every 12 hours) and voriconazole simultaneously, the blood concentration of voriconazole was significantly reduced. Ritonavir 100 mg each time, once every 12 hours is used to inhibit CYP3A, thereby increasing the concentration of other antiretroviral drugs, but the effect of this dosing regimen on the concentration of voriconazole has not been studied. This product is prohibited from being used simultaneously with efavirenz. When the two are used simultaneously, the blood concentration of voriconazole is significantly reduced, while the blood concentration of efavirenz is significantly increased. This product is prohibited from being used simultaneously with rifabutin. When the two are used together, the blood concentration of voriconazole is significantly reduced, while the blood concentration of rifabutin is significantly increased.

Store tightly closed at room temperature.

0.2g

24 months

Jincheng Haisi Pharmaceutical Co., Ltd.

• Founded in:

  1997-12-30

• Address:

  Wangtai, Jincheng City, Shanxi Province

• Tax NO.:

  91140500111208832X

• Registered Funds:

  148.512131 yuan

• Email:

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