Diflucan capsules 150mg N12
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Description
Geladrink Forte capsules contain in their composition a highly effective complex of chondroprotectors "SYSADOA", which protect and nourish not only the cartilage tissues, but also the entire ligamentous-articular system, help reduce pain and restore mobility of the joints and the human spine.
Active ingredients
Fluconazole
Release form
Capsules
Composition
Content in 12 capsules (daily allowance): peptide collagen hydrolyzate “Gelita” - 3300 mg, glucosamine sulfate - 1500 mg, chondroitin sulfate - 800 mg, MSM natural - 600 mg, Boswellia serrate - 100 mg, vitamin C - 100 mg, vitamin E - 50 mg, selenium - 50 mg, manganese - 2 mg.
Pharmacological effect
Antifungal drug of the triazole series, is a potent selective inhibitor of sterol synthesis in the fungal cell. Fluconazole activity in vitro and in clinical infections has been shown for most of the following microorganisms: Candida alhicans, Candida glabrata (many strains are moderately sensitive), Candida parapsilosis, Candida tropicalis, Cryptococcus neoforhora .In vitro fluconazole activity was shown in relation to the following microorganisms, however, its clinical significance is unknown: Candida dubliniensis, Candida guilliermondii, Candida kefyr, Candida lusitaniae. When taken orally and with a / in the introduction of f lukonazol 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, cell-dependent, cytotoxic, cell-dependent, cytotoxic, cell-dependent, cytotoxic, immune-dependent animals. . 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. Fluconazole resistance development mechanisms Fluconazole resistance may develop in the following cases: a qualitative or quantitative change in an enzyme that is target for fluconazole (lanosteril 14-α-demethylase), reducing access to the target of fluconazole or a combination of these mechanisms. Point mutations in the ERG11 gene encoding a target enzyme result in a target and lower azoles affinity.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 the enzyme molecules in the cell. in the active elimination (efflux) of fungal cell preparations. These transporters include the main mediator encoded by the MDR genes (multidrug resistance) and the ATP-binding transporter cassette superfamily encoded by the CDR genes (Candida spp. Resistance genes to azole antimycotics). At the same time, 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.
Pharmacokinetics
The pharmacokinetics of fluconazole is similar with intravenous administration and oral administration. Absorption After oral administration, fluconazole is well absorbed, its plasma levels (and total bioavailability) exceed 90% of plasma levels of fluconazole when administered intravenously. Simultaneous ingestion does not affect absorption by ingestion. Cmax is achieved within 0.5-1.5 hours after ingestion of fluconazole on an empty stomach. Plasma concentration is proportional to the dose. The distribution of 90% Css is achieved by the 4-5th day after the start of therapy (with repeated use of 1 time / day). The administration of the loading dose (on the 1st day), 2 times the average daily dose, allows you to reach a Css of 90% by the 2nd day. The Vd approaches the total water content in the body. Plasma protein binding is low (11-12%). Fluconazole penetrates well into all body fluids. Fluconazole levels in saliva and sputum are similar to its plasma concentrations. In patients with fungal meningitis, fluconazole levels in the cerebrospinal fluid make up about 80% of its plasma levels. In the stratum corneum, epidermis, dermis and sweat fluid, high concentrations are reached that exceed serum. Fluconazole builds up in the stratum corneum.When taken in a dose of 50 mg 1 time / day, the concentration of fluconazole after 12 days was 73 mcg / g, and 7 days after stopping treatment - only 5.8 mcg / g. When used in a dose of 150 mg 1 time / week. The concentration of fluconazole in the stratum corneum on the 7th day was 23.4 mcg / g, and 7 days after the second dose was taken - 7.1 mcg / g. The concentration of fluconazole in the nails after 4 months of use at a dose of 150 mg 1 time / week. amounted to 4.05 mcg / g in healthy and 1.8 mcg / g in affected nails; 6 months after completion of therapy, fluconazole was still detected in the nails. When comparing concentrations in saliva and blood plasma after a single dose of fluconazole in a dose of 100 mg in the form of a capsule and suspension for ingestion (rinsing and preserving in the mouth for 2 minutes and swallowing ) it was established that Cmax of fluconazole in saliva after taking the suspension was observed after 5 minutes and 182 times higher than Cmax in saliva after taking the capsule (reached after 4 hours). After about 4 hours, the concentrations of fluconazole in saliva were the same. The mean AUC0-96 in saliva was significantly higher when administered as a suspension than capsules. Significant differences in the rate of excretion from saliva or pharmacokinetics in plasma when using fluconazole in the form of two forms of release were not detected. Metabolism and excretion Fluconazole is excreted mainly by the kidneys; approximately 80% of the administered dose is detected in the urine unchanged. Clearance of fluconazole is proportional to QC. Circulating metabolites not found.
Indications
Recommended for use as a source of peptides of collagen, glucosamine and chondroitin sulfates, vitamins C and E, manganese and selenium. Indications for use: sensitivity to cold when the weather changes, morning stiffness, pain when moving, night pain and pain at rest, pain in muscles, pain in the back and spine, excessive load on the joints and spine, damage to the tissues of the joints and spine, sports injuries, family history of osteoarthritis or osteoporosis, congenital deviation in the position of the hip, knee and other joints, rehabilitation after injuries and surgeries, including after joint replacement.
Contraindications
Simultaneous use of terfenadine during repeated use of fluconazole at a dose of 400 mg / day or more; simultaneous use with drugs,increasing the QT interval and metabolizing using CYP3A4 isoenzyme, such as cisapride, astemizole, erythromycin, pimozide and quinidine; violation of glucose / galactose absorption (for capsules); - children up to 3 years (for capsules); - hypersensitivity to fluconazole, other components of the drug or azole substances with similar fluconazolo m structure.
Precautionary measures
Before use, it is recommended to consult a doctor.
Use during pregnancy and lactation
Contraindicated during pregnancy and lactation.
Dosage and administration
Adults take 12 capsules per day with meals for one or two doses. The duration of use is 2-3 months. The frequency of courses - 2-3 times a year.
special instructions
Contraindications: individual intolerance to the components, pregnancy, breast-feeding. Contains a source of phenylalanine. Does not contain sucrose, cholesterol, gluten, lactose.