Fljukostat (Solution for infusion)
Active material: Fluconazole
When ATH: J02AC01
CCF: Antifungal agent
ICD-10 codes (testimony): B20, B37.0, B37.1, B37.2, B37.3, B37.4, B37.6, B37.7, B37.8, B45, H19.2, Z29.8
When CSF: 08.01.01
Manufacturer: Dalkhimpharm of (Russia)
Pharmaceutical form, composition and packaging
Solution for infusion clear, colorless.
| 1 ml | 1 fl. | |
| fluconazole | 2 mg | 100 mg |
Excipients: sodium chloride, water d / and.
50 ml – colorless glass vials (1) and holder – packs cardboard.
Pharmacological action
Antifungal agent. Fluconazole - representative of the class of triazole antifungal agents, It is a potent selective inhibitor of sterol synthesis in the fungal cells.
It is active against pathogens fungal infections, caused by Candida spp., Cryptococcus neoformans, Microsporum spp., Trichophyton spp., Blastomyces dermatitidis, Merciless coccidioides, Histoplasma capsulatum.
Pharmacokinetics
Distribution
After the on / in the fluconazole penetrates well into tissues and body fluids. Fluconazole concentration in plasma is directly proportional to the dose administered drug; the concentration in saliva and sputum corresponds plasma concentration. Patients with fungal meningitis etiology fluconazole content in cerebrospinal fluid reaches 80% concentration in blood plasma.
90% Css It is achieved by 4-5 day after multiple injections at the same dose per day. Application of the first day of dose, in 2 times the usual daily, It allows to achieve such levels of drug in plasma, that approach 90% the value of Css, second day.
In Кажущийсяd approaches to total body fluid.
Plasma protein binding is 11-12%.
Metabolism and excretion
Fluconazole metabolites in peripheral blood has been detected. Fluconazole is derived mainly kidneys; with approximately 80% – in unchanged form. The clearance of fluconazole is determined creatinine clearance.
T1/2 – 30 no.
Testimony
- Kryptokokkoz: cryptococcal meningitis, cryptococcal infection lungs and skin; prevention of relapse of cryptococcosis in AIDS patients, in organ transplantation or in other instances immunodeficiency;
- Generalized candidiasis: kandidemija, disseminated candidiasis and other forms of invasive Candida infections (infection of the abdominal cavity, endokarda, eye, respiratory and urinary tract infections);
- Mucosal candidiasis: oral, throat, esophageal and non-invasive bronchopulmonary infections; kandidurija;
- Vaginal candidiasis: acute or chronic relapsing;
- Prevention of fungal infections in patients with malignant tumors, predisposed to such infections as a result of chemotherapy cytostatics or radiation therapy.
Dosage regimen
Adults at cryptococcal infections the average dose fljukostat® is 400 mg 1 time / day on the first day of treatment, then - on 200-400 mg 1 time / day. The duration of treatment for infections kriptokokovyh determined clinical effectiveness, confirmed by mycological examination, and averages 6-8 weeks.
To prevention of relapse of cryptococcal meningitis AIDS patients after completion of a full course of primary therapy, the drug is prescribed to the patient at a dose of at least 200 mg / day for a long period.
At kandidemii, disseminated candidiasis and other invasive Candida infections the drug is prescribed in a dose 400 mg on the first day and 200 mg on subsequent days. If necessary, may increase the dose fljukostat® to 400 mg / day. The duration of therapy is determined by the clinical efficacy.
At orofaringealьnom kandidoze (incl. in patients with impaired immunity) the average dose is 50-100 mg 1 times / day for 7-14 days. If necessary, (especially in patients with severe impaired immunity) Therapy may be continued.
At other Candida infections (when esophagitis, non-invasive bronchopulmonary infections, kandidurii, candidiasis of the skin and mucous membranes) the average daily dose is 50-100 mg for 14-30 days.
To prevention of fungal infections in patients with malignant tumors dose is 50 mg 1 times / day until, while the patient refers to the increased risk of carrying cytostatic or radiation therapy.
Babies the drug should not be administered in a daily dose, greater than that of adults. The drug is used 1 time / day. As with adults, the duration of therapy is determined by the clinical and laboratory efficiency.
At mucosal candidiasis The recommended dose of fluconazole 3 mg / kg / day. The 1-day to achieve constant equilibrium concentrations can be assigned to the loading dose 6 mg / kg.
At generalized candidiasis and cryptococcal infection The recommended dose is 6-12 mg / kg / day, depending on the severity of the disease.
To prevention of fungal infections in children with reduced immunity the drug is prescribed for 3-12 mg / kg / day ( depending on the severity and duration of neutropenia induced by conservation).
In Newborn removing fljukostat® zamedleno, Therefore, in the first 2 weeks of life, the drug is prescribed in the same dose, and that older children, but the intervals 72 no. For children 3 and 4 weeks drug is administered at the same dose intervals 48 no.
Elderly patients with normal renal function, the drug is prescribed in high doses. At impaired renal function (CC<50 ml / min) dosing regimen should be adjusted.
In patients with impaired renal function a single application of the drug dosage adjustment is required.
In patients (including children) with impaired renal function if necessary, reusable first drug is administered in a dose of shock (50-400 mg). Then the dose is adjusted to the index QC.
| CC (ml / min) | % the recommended dose |
| >50 | 100% |
| <50 (without dialysis) | 50% |
| Patients, residing on dialysis | 100% after each dialysis |
When translating from / in the introduction of the drug in the oral and vice versa is not necessary to change the daily dose.
Terms of preparation and administration of infusion solution
The drug is introduced into / in the drip at a rate of not more than 20 mg (10 ml) min.
Flucostat® for / in the introduction is compatible with the following solutions: 20% glucose, Ringer, Hartmann's solution, solution of potassium chloride in glucose, 4.2% solution of sodium bicarbonate, aminofuzin, isotonic sodium chloride solution.
Infusions fljukostat® It can be carried out using conventional kits for transfusion.
Side effect
From the digestive system: change in taste, nausea, flatulence, vomiting, stomach ache, diarrhea; rarely – abnormal liver function (jaundice, hepatitis, gepatonekroz, giperʙiliruʙinemija, increased ALT, IS, Alkaline phosphatase), incl. fatal.
CNS: headache, dizziness; rarely – convulsions.
From the hematopoietic system: rarely – leukopenia, thrombocytopenia, neutropenia, agranulocytosis.
Cardio-vascular system: prolongation of the QT interval, flicker, ventricular flutter.
Allergic reactions: skin rash; rarely - exudative erythema multiforme (T. C in Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions (incl. angioedema, swelling of the face, hives, itching).
Metabolism: rarely – hypercholesterolemia, hypertriglyceridemia, kaliopenia.
Other: rarely – renal dysfunction, alopecia.
Contraindications
- Concurrent use of terfenadine, astemizole, or cisapride;
- Lactation (breast-feeding);
- Hypersensitivity to the drug or similar in structure azole compounds.
FROM caution use in patients with hepatic insufficiency, with the appearance of rash during treatment with fluconazole in patients with superficial fungal infection and invasive / systemic fungal infections, if proaritmogennoe states in patients with multiple risk factors (organic heart disease, electrolyte imbalance, concomitant use of drugs, arhythmogenic), Pregnancy.
Pregnancy and lactation
Use of the drug during pregnancy is contraindicated, except severe generalized and potentially life-threatening fungal infections.
If necessary, use during lactation should stop breastfeeding.
Cautions
In applying the drug in rare cases it noted hepatotoxic effects (incl. fatal), primarily in patients with serious underlying medical conditions.
In patients receiving the drug should be monitored laboratory parameters of liver function. If signs of liver dysfunction, which can be associated with taking fljukostat®, the drug should be discontinued.
If a rash in patients with reduced immunity should be carefully monitored, the progression of skin reactions should be discontinued fluconazole (the risk of developing Stevens-Johnson syndrome and Lyell's syndrome).
Care must be taken while the application of fluconazole with cisapride, astemizolom, rifaʙutinom, tacrolimus or other drugs, metabolized by cytochrome P450 isoenzymes.
Overdose
Symptoms: hallucinations, paranoidalynoe behavior.
Treatment: symptomatic therapy. As fluconazole is excreted in the urine, forced diuresis enhances its excretion. Hemodialysis for 3 h decreases the plasma concentration of fluconazole approximately 50%.
Drug Interactions
With simultaneous use of fluconazole with indirect anticoagulants may increase the prothrombin time (this figure should be carefully monitored).
With simultaneous use of fluconazole increases T1/2 oral hypoglycemic drugs – sulfonylureas. Therefore, with a joint appointment of fluconazole and oral hypoglycemic agents should consider the possibility of hypoglycemia.
Concomitant use of fluconazole and phenytoin may cause a higher concentration of phenytoin to a clinically significant degree, which requires a reduction of the dose.
Simultaneous administration of fluconazole and rifampicin reduces the Cmax and shortening T1/2 flukonazola. Therefore, in patients receiving concomitant rifampicin, dose of fluconazole is recommended to increase.
The combined use of fluconazole and rifabutin is accompanied by increased serum levels of the last. With simultaneous use of fluconazole and rifabutin described cases of uveitis.
While the use of fluconazole may increase the concentration of cyclosporine in the blood plasma (requires monitoring).
With simultaneous use of fluconazole with astemizole and terfenadine may develop severe, life-threatening arrhythmias. So combination contraindicated.
When combined fluconazole and cisapride described cases of adverse reactions from the heart, including paroxysms of ventricular tachycardia. The combined use is contraindicated.
In a joint application of fluconazole with zidovudine may increase the concentration of the latter in the blood plasma (In such cases, monitoring of the patient for early detection of adverse effects of zidovudine).
Fluconazole results in reduced clearance of theophylline medium from plasma, Consequently, It increases the risk of toxic action, and an overdose of theophylline.
Pharmaceutical interaction
Manifestations of pharmaceutical incompatibility is not described. However, mixing the solution fljukostat® with solutions of other drugs, other than used for the preparation of infusion solution, not recommended.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored in the dark, away from children at a temperature of 5 ° to 30 ° C. Shelf life – 3 year.
