Ankotil

Roman name

Ancotil

Characteristics

Flucytosine (5-FT) is a fluorinated pirimidin.

Pharmacokinetics

Ankotil well distributed in the tissues and liquid environments organism, including diffuses into spinnomozgovu liquid. The distribution of the / in the amount of 0.8 l / mm Linking plasma protein to a minimum (2-4%). The concentration of the drug in likwore and peritonealna fluid is about 75% of the level of concentration in сыворотке.Концентрац��я in the vaccine must be at least 20 to 25 mg / l (except for the treatment of candidiasis urinary tract, see "Dosing and Administration"). Avoid prolonged maintenance concentrations above 100 mg / l due to an increase in the risk of adverse reackzi.90% dose 5-FT displayed kidneys unchanged to (clubockova filtering). A few flucytosine dezaminiruetsa in 5-ftorurazil (5-FU). The AUC and 5-FU 5-FT is about 4%. In adults with normal kidney function T_1/2 is 3-6 h, the premature babies at 6-7 In normal kidney functions of the concentration of a substance in the urine is always much higher than in Savorotke.poskolku Ankotil extracted through kidney virtually unaltered, the renal function increases T_ | 1 / 2 |. That should be necessarily taken into account when determining the dosage.

Farmakodinamika

Ankotil has fungistaticski and antifungal effects in vitro and in vivo against yeasts (candida), as well as agents of cryptococcosis (Cryptococcus neoformans) and hromoblastomikoza. In aspergilleze Ankotil is fungistaticescuu activity; The course of combination therapy in combination with Amfoteritinom In the clinical Effect.v most strains isolated from patients from the European countries who have not previously received therapy were sensitive to 5-FT (93% diagnosed with candidiasis, 96% криптококкоз).Минимал ьная concentration to suppress these microorganisms is usually at a level between 0.03 and 12.5 mg / O When treating the Ankotilom originally sensitive to the strains gradually may develop a resistance. Therefore, the sensitivity is recommended that before and during treatment using tests developed Shadomy and Speller and growth media free of antagonists. The use of disk tests 5-FC.V studies in vitro and in vivo showed that the combined use of Ankotila and Amfoteritina Their activity mutually reinforced by the many strains of pathogens. This effect was particularly pronounced in the case of pathogens, little sensitive Ankotilu.

Clinical pharmacology

Based on the experimental data, combined with Ankotila Amfoteritinom B, in many cases, a degree or at least additivoe Actie.klinicescie studies have shown that the combination of these two drugs is a better therapeutic effect than each of them as a stand alone treatment. Furthermore, the use of combination therapy reduces therapeutic dose Amfoteritina B, and thus its toxic side effects. At the same time, decreasing the duration of treatment. Finally, the use of combination therapy to prevent or delay the development of resistance secondary pathogens that can be observed in alone Ankotilom.primenenie this combination very effective in the treatment of cryptococcosis, and the subacute and chronic fungal infections (meningitis, endocardit, kandidozny uveit, etc.).

Indications

Systemic infection caused by yeast and other fungal diseases, sensitive to the effects of drugs : generalizovanny candidiasis; Kriptokokkoz; Hromoblastomikoz; Aspergillez (only in combination with Amfoteritinom B); Infection caused by microorganisms Torulopsis glabrata and Hansenula.

Pregnancy and lactation

Controlled studies involving pregnant women has been carried out. The product can be granted only in cases where the expected therapeutic effect outweighs the potential risk for the development of Ploda.ne found inside the active substance in mother's milk. Given the importance of treating the drug to the mother, a doctor must decide whether to suspend breastfeeding at the time of therapy.

Contraindications

Hypersensitivity to flucitosinu or other components of the preparation.

Specific guidance

The regular monitoring concentrations 5-FT in vaccine and, if necessary, corresponding adjustments to the Dozirovania.pri measurement of 5-FT concentration in the serum, it should be borne in mind that 5-FT concentration in blood samples obtained at the time of or immediately after the drug nepokazationa for subsequent sea level 5-FT concentration in the serum. In order to monitor the level of concentration savorotocna 5-FT recommended blood shortly before the next Procedura.vo treatment Ankotilom in combination with Amfoteritinom B should periodically monitor detailed formula blood; To monitor kidney function should be regularly to determine serum creatinine and creatinine Cl. It should also be subject to the normal precautions and recommendations on the application to Amfoteritino B. In determining the level of creatinine in a two-enzyme analysis does not rule out the distortion of the analysis (lozhnopolojitelnaya azotemia) as a result of flucytosine. There is a need to use other methods to determine Kreatinina.pri calculations of the electrolyte solutions for patients suffering from kidney and / or heart failure and also, in violation of elektrolitnogo balance, it is necessary to take into account the input infuzing Ankotila solution and sodium content (138 mmol / l).

Patient interaction

As for the treatment of Ankotilom there is a risk of radiation (especially neutropenia, often accompanied by trombozitopenia), while treatment zitostatikami a daily monitoring peripheral Krovi.v because 5-FT withdrawal has come almost exclusively through the kidneys, all drugs that reduce clubockovu filtering increase T_1/2 active substance Ankotila. In such cases, regular monitoring of Cl creatinine, as well as to adapt solutions Dozy.infuzie Ankotila and Amfoteritina In should be Razdelno.ankotil can be used in conjunction with the parenteral solutions of sodium chloride 0.9% or 0.18%, and glucose 5% and 4% respectively. No other property should not be added to infuzionnomu Ankotila solution.

Precautions

Before and during the treatment, it was necessary to monitor kidney function in patients, preferably by identifying Cl creatinine. If it necessary, the correction of Dozirovania.u patients with renal insufficiency, should monitor kidney function at least once in Nedelj.ankotil should not be applied to patients suffering from renal failure, in the absence of equipment to be monitored concentrations 5-FT in whey Krovi.sleduet caution in the application of the drug in patients with depressed function of bone marrow or blood diseases. The picture control peripheral blood and the liver-daily at the beginning of treatment, then once or twice a week.

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