Вориконазол
- английское имяVoriconazole
- CAS №137234-62-9
- CBNumberCB1160110
- ФормулаC16H14F3N5O
- мольный вес349.31
- EINECS629-701-5
- номер MDLMFCD00905717
- файл Mol137234-62-9.mol
химическое свойство
| Температура плавления | 127-130°C |
| альфа | D25 -62° (c = 1 in methanol) |
| Температура кипения | 508.6±60.0 °C(Predicted) |
| плотность | 1.42±0.1 g/cm3(Predicted) |
| Fp | 9℃ |
| температура хранения | 2-8°C |
| растворимость | DMSO: >20mg/mL |
| пка | 11.54±0.29(Predicted) |
| форма | white powder |
| цвет | White to Almost white |
| Мерк | 14,10033 |
| InChI | InChI=1/C16H14F3N5O/c1-10(15-14(19)5-20-7-22-15)16(25,6-24-9-21-8-23-24)12-3-2-11(17)4-13(12)18/h2-5,7-10,25H,6H2,1H3/t10-,16+/s3 |
| ИнЧИКей | BCEHBSKCWLPMDN-MGPLVRAMSA-N |
| SMILES | [C@@](C1C=CC(F)=CC=1F)(O)(CN1N=CN=C1)[C@H](C1=NC=NC=C1F)C |&1:0,16,r| |
| Справочник по базе данных CAS | 137234-62-9(CAS DataBase Reference) |
| FDA UNII | JFU09I87TR |
| Словарь онкологических терминов NCI | voriconazole |
| Словарь наркотиков NCI | voriconazole |
| Код УВД | J02AC03 |
больше
| Коды опасности | Xn,T,F | |||||||||
| Заявления о рисках | 22-36/38-52/53-48/22-40-25-61-39/23/24/25-23/24/25-11 | |||||||||
| Заявления о безопасности | 26-36-45-36/37-22-53-16 | |||||||||
| РИДАДР | UN1230 - class 3 - PG 2 - Methanol, solution | |||||||||
| WGK Германия | 3 | |||||||||
| RTECS | UV9145000 | |||||||||
| Класс опасности | 6.1 | |||||||||
| Группа упаковки | III | |||||||||
| кода HS | 29335990 | |||||||||
| NFPA 704: |
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рисовальное письмо(GHS)
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рисовальное письмо(GHS)
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сигнальный язык
опасность
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вредная бумага
H301：Токсично при проглатывании.
H341：Предполагается, что данное вещество вызывает генетические дефекты.
H372：Поражает органы в результате многократного или продолжительного воздействия.
H351：Предполагается, что данное вещество вызывает раковые заболевания.
H373：Может поражать органы (Нервная система) в результате многократного или продолжительного воздействия при вдыхании.
H361：Предполагается, что данное вещество может отрицательно повлиять на способность к деторождению или на неродившегося ребенка.
H371：Может поражать органы (Глаза) в результате однократного воздействия.
H412：Вредно для водных организмов с долгосрочными последствиями.
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оператор предупредительных мер
P201：Беречь от тепла, горячих поверхностей, искр, открытого огня и других источников воспламенения. Не курить.
P202：Перед использованием ознакомиться с инструкциями по технике безопасности.
P260：Не вдыхать газ/ пары/ пыль/ аэрозоли/ дым/ туман.
P264：После работы тщательно вымыть кожу.
P273：Избегать попадания в окружающую среду.
P301+P310：ПРИ ПРОГЛАТЫВАНИИ: Немедленно обратиться за медицинской помощью. Прополоскать рот.
Вориконазол химические свойства, назначение, производство
Описание
Voriconazole is a broad-spectrum triazole antifungal ,it is primarily used for the treatment of progressive, possibly life-threatening infections in immune deficiency patients. Indications include: immunosuppressed patients with severe fungal infections, acute invasive aspergillosis (the most common pathogen is Aspergillus fumigatus, followed by A. flavus, Aspergillus niger and Aspergillus soil), severe invasive infections caused by fluconazole-resistant Candida (including C. krusei) severe infection caused by Foot actinomycetes bacteria genus and Fusarium bacteria genus . Moderate to severe renal insufficiency is administered intravenously paying caution.Химические свойства
Cyrstalline SolidИспользование
Voriconazole is an antifungal (systemic) that belong to an ergosterol biosynthesis inhibitor. It is used to treat serious fungal or yeast infections, such as aspergillosis (fungal infection in the lungs), candidemia (fungal infection in the blood), esophageal candidiasis (candida esophagitis), or other fungal infections (infections in the skin, stomach, kidney, bladder, or wounds).Определение
ChEBI: Voriconazole is a triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4. It has a role as a P450 inhibitor. It is a member of pyrimidines, a difluorobenzene, a tertiary alcohol, a triazole antifungal drug and a conazole antifungal drug.Показания
Voriconazole (Vfend), a derivative of fluconazole, is a second-generation triazole that has improved antifungal activity against Aspergillus and Fusarium spp., P. boydii, Penicillium marneffei, and fluconazole-resistant Candida spp. Like fluconazole, voriconazole has high oral bioavailability and good cerebrospinal fluid penetration, but unlike fluconazole, it undergoes extensive hepatic metabolism and is highly protein bound. No significant amount of bioactive drug is excreted into the urine. Dosage reduction is necessary with severe hepatic insufficiency but not with renal insufficiency.Антимикробная активность
The spectrum includes most fungi that cause human disease: dimorphic fungi (Blast. dermatitidis, Coccidioides spp., Hist. capsulatum, Paracocc. brasiliensis, Pen. marneffei and Spor. schenckii), molds (Aspergillus spp., Fusarium spp. and Scedosporium spp.), dematiaceous fungi and yeasts (Candida spp., Cryptococcus spp. and Trichosporon spp.).Приобретенная устойчивость
Some fluconazole- and itraconazole-resistant strains of Candida and Aspergillus spp. show reduced susceptibility to voriconazole.Общее описание
Voriconazole is a synthetically prepared, broad-spectrum triazole derivative of fluconazole, which shows in vitro activity against many yeasts and a broad-spectrum of mold and dermatophyte isolates. Its mode of action involves the inhibition of cytochrome P450 (CYP)-dependent enzyme, 14-α-sterol demethylase, and hence it is involved in disrupting the cell membrane and terminate the fungal growth.Фармацевтические приложения
Voriconazole is a triazole, antifungal agent that inhibits a broad range of pathogenic yeasts, including Candida (MIC = 0.03-8 μg/ml), and filamentous fungi such as Aspergillus, Scedosporium, and Fusarium. Its inhibitory action results from its ability to inhibit the synthesis of ergosterol, the major sterol of the fungal cell membrane.Биологическая активность
Voriconazole is an triazole antifungal agent used to treat serious fungal infections. It inhibits ergosterol synthesis by inhibiting CYP450-dependent 14-α sterol demethylase resulting in a depletion of ergosterol in fungal cell membranes. Displays potent activity against Candida , Cryptococcus and Aspergillus species.Фармакокине?тика
Oral absorption: 96%Cmax 400 mg oral: c. 2 mg/L after 2 h
Plasma half-life: c. 6 h
Volume of distribution: 4.6 L/kg
Plasma protein binding: 58%
Absorption
Oral absorption is rapid and almost complete, and is unaffected by intragastric pH. In adults, there is a disproportionate increase in blood concentrations with increasing oral and parenteral dosage, due to partial saturation of first-pass metabolism. In children given low dosages of the drug, proportional changes in drug levels are seen.
Distribution
It is widely distributed into body tissues and fluids, including brain and CSF.
Metabolism and excretion
It is extensively metabolized by the liver. More than 80% of a dose appears in the urine, but less than 2% is excreted in unchanged form. It is metabolized by several different hepatic cytochrome P450 enzymes. Some people with point mutations in the genes encoding these enzymes are poor metabolizers while others are extensive metabolizers. Drug levels are as much as four-fold lower in individuals who metabolize the drug more extensively.
Клиническое использование
Acute and chronic invasive aspergillosisSerious invasive Candida infections
Serious infections caused by Scedosporium and Fusarium spp.
Побочные эффекты
Unwanted effects include mild to moderate visual disturbance, rashes, and transient abnormalities of liver enzymes. Rare side effects include life-threatening hepatitis.Способ действия
Voriconazole is structurally related to fluconazole (Pfizer, diflucan) and acts by inhibiting the cytochrome P450- dependant enzyme 14a-sterol demethylase of ergosterol synthesis (thereby resulting in the formation of a cell membrane with abnormal characteristics and accumulation of toxic sterol intermediates). Voriconazole was more active than itraconazole and fluconazole against Cryptococcus neoformans and a variety of Candidas species such as C. albicans, C. glabrata C. krusei. It also exhibits similar or superior activity compared to amphotericin B and itraconazole against filamentous fungi such as Aspergillus, an important pathogen which is not susceptible to fluconazole.Меры предосторожности
Significant drug interactions include cyclosporins(increased cyclosporine levels), phenytoin, rifampin,and rifabutin (decreased voriconazole levels). Becauseof its low toxicity profile, this drug may gain importancein the chronic treatment of infections with invasive dimorphicfungi and resistant Candida spp.Вориконазол запасные части и сырье
сырьё
- ВОДОРОД
- Гидроксид палладия
- Bicyclo[2.2.1]heptane-1-methanesulfonic acid, 7,7-dimethyl-2-oxo-, (1S,4R)-, compd. with (αR,βS)-α-(2,4-difluorophenyl)-5-fluoro-β-methyl-α-(1H-1,2,4-triazol-1-ylmethyl)-4-pyrimidineethanol (1:1)
- Pyrimidine, 4-ethenyl-5-fluoro-
- 2,4-дифтор-альфа- (1H-1,2,4-триазолил) ацетофенон
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Вориконазол поставщик
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