Diflucan solution for infusion 2mg ml 200ml
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Active ingredients
Fluconazole
Release form
Solution
Composition
In 1 ml. ratsvora: fluconazole 2 mg. Excipients: sodium chloride - 9 mg, water d / and - up to 1 ml.
Pharmacological effect
Antifungal drug triazole series, is a powerful selective inhibitor of sterol synthesis in the cell of fungi. Fluconazole activity has been shown in vitro and in clinical infections for most of the following microorganisms: Candida alhicans, Candida glabrata (many strains are moderately sensitive), Candida parapsilosis, Candida tropicalis, Cryptococcus neoformans. In vitro fluconazole activity was shown against the following microorganisms, however, its clinical significance is unknown: Candida dubliniensis, Candida guilliermondii, Candida kefyr, Candida lusitaniae. When administered and with a / in the introduction of fluconazole was active in various models of fungal infections in animals. The activity of the drug was demonstrated in opportunistic mycoses, incl. caused by candida spp. (including generalized candidiasis in immunocompromised animals), Cryptococcus neoformans (including intracranial infections), Microsporum spp. and Trychoptyton spp. Fluconazole activity has also been established in models of endemic mycoses in animals, including infections caused by Blastomyces dermatitidis, Coccidioides immitis (including intracranial infections) and Histoplasma capsulatum in animals with normal and reduced immunity. Fluconazole has a high specificity for fungal enzymes dependent on cytochrome P450. Fluconazole therapy at 50 mg / day for up to 28 days does not affect the plasma testosterone concentration in men or the concentration of steroids in women of childbearing age. Fluconazole at a dose of 200-400 mg / day did not have a clinically significant effect on the levels of endogenous steroids and their response to stimulation of ACTH in healthy male volunteers. Mechanisms of Fluconazole Resistance Development Fluconazole resistance may develop in the following cases: a qualitative or quantitative change in the enzyme that targets fluconazole (lanosteril 14 -? - demethylase), a decrease in access to the fluconazole target, or a combination of these mechanisms. Point mutations in the ERG11 gene, which encodes a target enzyme, result in a modification of the target and a decrease in affinity for the azoles. Increasing the expression of the ERG11 gene leads to the production of high concentrations of the target enzyme, which creates the need to increase the concentration of fluconazole in the intracellular fluid to suppress all enzyme molecules in the cell.The second significant mechanism of resistance lies in the active elimination of fluconazole from the intracellular space by activating two types of transporters involved in the active elimination (efflux) of drugs from the fungal cell. Such transporters include the main mediator encoded by MDR genes (multidrug resistance) and the ATP-binding transporter cassette superfamily encoded by CDR genes (genes of resistance of Candida spp. To azole antimycotics). Overexpression of the MDR gene leads to resistance to fluconazole, while overexpression of CDR genes can lead to resistance to various azoles. Resistance to Candida glabrata is usually mediated by overexpression of the CDR gene, which leads to resistance to many azoles. For those strains in which the MIC is defined as an intermediate (16-32 mcg / ml) it is recommended to use the maximum dose of fluconazole. Candida krusei should be considered as a pathogen resistant to fluconazole. The mechanism of resistance is associated with a reduced sensitivity of the target enzyme to the inhibitory effects of fluconazole.
Indications
Kiptokokkoz, including cryptococcal meningitis and infections of other localization (for example, lungs, skin), including in patients with a normal immune response and in patients with AIDS, recipients of transplanted organs and patients with other forms of immunodeficiency. supportive therapy to prevent the recurrence of cryptococcosis in AIDS patients. generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidal infection, such as infections of the peritoneum, endocardium, eyes, respiratory and urinary tract, including in patients with malignant tumors who are in the ICU and receive cytotoxic or immunosuppressive agents, as well as in patients with other factors predisposing to the development of candidiasis. candidiasis of the mucous membranes, including the mucous membranes of the oral cavity and pharynx, esophagus, non-invasive bronchopulmonary infections, candiduria, mucocutaneous and chronic atrophic candidiasis of the oral cavity (associated with the wearing of dental prostheses), including in patients with normal and suppressed immune function. prevention of recurrent oropharyngeal candidiasis in AIDS patients. genital candidiasis. acute or recurrent vaginal candidiasis. prevention in order to reduce the frequency of recurrences of vaginal candidiasis (3 or more episodes per year). candidal balanitis. prevention of fungal infections in patients with malignant tumors,predisposed to the development of such infections as a result of cytotoxic chemotherapy or radiation therapy. mycoses of the skin, including mycoses of the feet, body, inguinal region, pityriasis versicolor, onychomycosis, and skin candidal infections. deep endemic mycoses in patients with normal immunity, coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis.
Contraindications
The simultaneous use of terfenadine during repeated use of fluconazole at a dose of 400 mg / day or more. simultaneous use with drugs that increase the QT interval and are metabolized by the isoenzyme CYP3A4, such as cisapride, astemizole, erythromycin, pimozide, and quinidine. deficiency of sucrase / isomaltase, fructose intolerance, glucose-galactose malabsorption (for powder for suspension) .— galactose intolerance, lactase deficiency and glucose / galactose absorption (for capsules). children's age up to 3 years (for capsules). hypersensitivity to fluconazole, other components of the drug or azole substances with a structure similar to fluconazole.
Use during pregnancy and lactation
Adequate and controlled studies of the safety of the drug in pregnant women have not been conducted. Cases of multiple congenital malformations in newborns whose mothers for 3 or more months received therapy with fluconazole in a high dose (400-800 mg / day) for coccidioidomycosis have been described. The following developmental disorders were noted: brachycephaly, impaired development of the facial part of the skull, impaired formation of the cranial vault, cleft palate, curvature of the femur bones, thinning and elongation of the ribs, arthrogryposis and congenital heart defects. Currently, there is no evidence of the connection of these congenital disorders with the use of fluconazole in low doses (150 mg once for the treatment of vulvovaginal candidiasis) in the first trimester of pregnancy. The use of fluconazole during pregnancy should be avoided, except in cases of severe and potentially life-threatening fungal infections, when the expected benefit of treatment outweighs the possible risk to the fetus. Therefore, women of childbearing age should use reliable contraception.Fluconazole is found in breast milk in concentrations close to the plasma, so use Diflucan. during lactation (breastfeeding) is not recommended.
Side effects
The most common side effects were reported in clinical and post-marketing (*) studies of the drug Diflucan .. From the nervous system: headache, dizziness *, seizures *, taste change *, paresthesia, insomnia, drowsiness, tremor. On the part of the digestive system: abdominal pain, diarrhea, flatulence, nausea, dyspepsia *, vomiting *, dryness of the oral mucosa, constipation, hepatotoxicity (in some cases fatal), increased concentrations of bilirubin, serum ALT and AST, alkaline phosphorus , abnormal liver function *, hepatitis *, hepatocellular necrosis *, jaundice *, cholestasis, hepatocellular damage. Since the cardiovascular system *: an increase in the QT interval on the ECG, arrhythmia, including ventricular tachysystolic type "pirouette". On the part of the skin: rash, alopecia *, exfoliative skin diseases *, including Stevens-Johnson syndrome and toxic epidermal necrolysis, acute generalized exantmatous pustules, increased sweating, drug rash. On the part of the hemopoietic system *: leukopenia, including neutropenia and agranulocytosis, thrombocytopenia, anemia. Metabolism *: increased cholesterol and triglycerides in plasma, hypokalemia. From the musculoskeletal system: myalgia. Allergic reactions *: anaphylactic reactions (including angioedema, swelling of the face, urticaria, pruritus). Others: weakness, asthenia, fatigue, fever, vertigo. In some patients, especially with serious diseases (AIDS, malignant neoplasms), when treated with the drug Diflucan. and similar drugs were observed changes in blood parameters, kidney and liver function, however, the clinical significance of these changes and their relationship to treatment has not been established. Tolerability is usually very good.
special instructions
The most common side effects were reported in clinical and post-marketing (*) studies of the drug Diflucan ..On the part of the nervous system: headache, dizziness *, cramps *, change in taste *, paresthesia, insomnia, drowsiness, tremor. On the part of the digestive system: abdominal pain, diarrhea, flatulence, nausea, dyspepsia *, vomiting *, dryness of the oral mucosa, constipation, hepatotoxicity (in some cases fatal), increased concentrations of bilirubin, serum ALT and AST, alkaline phosphorus , abnormal liver function *, hepatitis *, hepatocellular necrosis *, jaundice *, cholestasis, hepatocellular damage. Since the cardiovascular system *: an increase in the QT interval on the ECG, arrhythmia, including ventricular tachysystolic type "pirouette". On the part of the skin: rash, alopecia *, exfoliative skin diseases *, including Stevens-Johnson syndrome and toxic epidermal necrolysis, acute generalized exantmatous pustules, increased sweating, drug rash. On the part of the hemopoietic system *: leukopenia, including neutropenia and agranulocytosis, thrombocytopenia, anemia. Metabolism *: increased cholesterol and triglycerides in plasma, hypokalemia. From the musculoskeletal system: myalgia. Allergic reactions *: anaphylactic reactions (including angioedema, swelling of the face, urticaria, pruritus). Others: weakness, asthenia, fatigue, fever, vertigo. In some patients, especially with serious diseases (AIDS, malignant neoplasms), when treated with the drug Diflucan. and similar drugs were observed changes in blood parameters, kidney and liver function, however, the clinical significance of these changes and their relationship to treatment has not been established. Tolerability is usually very good.