Sebivo pills 600 mg 28 pcs
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Active ingredients
Telbivudin
Release form
Pills
Composition
1 ml ranibizumab * 10 mg. 1 fl. ranibizumab * 3 mg.
Pharmacological effect
Telbivudine (INN - telbivudine - telbivudin) is a synthetic analogue of thymidine nucleoside, which has activity against the DNA polymerase of hepatitis B virus. Telbivudin is actively phosphorylated by cellular kinases to an active triphosphate form with an intracellular half-life of 14 h. Hepatitis B virus DNA (reverse transcriptase), competing with natural thymidine-5? -Triphosphate. The inclusion of telbivudin-5? -Triphosphate in viral DNA causes a break in the DNA chain, and this inhibits the replication of the hepatitis B virus. Telbivudin is an inhibitor of the synthesis of both the first strand of the hepatitis B virus (50% effective concentration of 0.4–1.3 μmol) and another line (50% effective concentration of 0.12–0.24 μmol). Telbivudin-5? -Phosphate at a concentration of up to 100 mcmol did not inhibit cellular DNA polymerase (?,? And?) Of human cells. The drug in concentrations up to 10 mcmol did not have a significant toxic effect on the structure of mitochondria, as well as on the content and function of DNA and did not increase the formation of lactic acid in vitro.
Pharmacokinetics
The pharmacokinetics of single and multiple doses of telbivudine were evaluated among healthy volunteers and among patients with chronic hepatitis B. The pharmacokinetics of telbivudine were similar in both groups. In healthy volunteers after taking the drug orally in a single dose of 600 mg, the maximum concentration of telbivudine in the blood plasma was 3.69 ± 1.25 mcg / ml (mean ± standard deviation) and was achieved on average 2 h after administration. AUC was 26.1 ± 7.2 h / ml (mean ± standard deviation). Individual variability of systemic indicators (maximum concentration, AUC) is? 30%. Constant serum concentration was reached after approximately 5–7 days of using telbivudine multiplicity 1 time per day.
Indications
Treatment of chronic hepatitis B in patients with obvious signs of viral replication and active liver inflammation. Indications are determined on the basis of virological, serological, biochemical and histological reactions, which were observed in patients with chronic hepatitis B, with a positive and negative reaction to the antigen of the hepatitis B virus (HBeAg).
Contraindications
Hypersensitivity to the active substance or one of the ingredients of the drug.
Precautionary measures
Noted increased levels of CK in the serum. However, the average level of CPK reached a maximum at the 52nd week with the use of telbivudine and did not increase further. In most cases, an increase in the level of CPK was asymptomatic, usually against the background of continuous therapy, there was a further decrease in the concentration of CPK. Possible fluctuation in the level of AlAT during treatment.
Use during pregnancy and lactation
Clinical data on the effect of telbivudine on pregnancy are not available. During pregnancy, Sebivo should be used only when the expected benefit to the mother outweighs the potential hazard to the fetus.
Dosage and administration
The recommended dose of Sebivo for adults is 600 mg (1 tablet) 1 time per day. The pill is taken orally with meals or alone. The optimal duration of treatment has not been established. Sebivo can be used to treat chronic hepatitis B in patients with renal failure. For patients with creatinine clearance of 50 ml / min, there is no need to correct the recommended dose of telbivudine. If patients have creatinine clearance of 50 ml / min, including end-stage renal failure with hemodialysis. Terminal stage of renal failure 600 mg 1 time every 96 hours. If necessary, use of the drug Sebivo in patients with liver damage dose adjustment is not required.
Side effects
In clinical trials lasting 104 weeks, the adverse reactions reported were usually mild to moderate. Frequent undesirable reactions with a possible connection with taking telbivudine were a 3/4 degree increase in blood CK (6.8%), fatigue (4.4%), headache (3%) and nausea (2.6%).
Overdose
no cases of overdose have been reported. The studied doses up to 1800 mg / kg (3 times higher than the recommended daily dose) were well tolerated. The maximum tolerated dose of telbivudine has not been determined. Treatment: in case of overdose, Telbivudine should be discontinued and, if necessary, appropriate general supportive and symptomatic therapy should be prescribed.
Interaction with other drugs
Telbivudin is mainly excreted by the kidneys, therefore, when prescribing Sebivo with drugs that affect kidney function, it is possible to increase the plasma concentration of Telbivudine and / or simultaneously used drugs.In vitro telbivudine in concentrations 12 times higher than therapeutic, did not inhibit the metabolic processes occurring with the participation of microsomal isoenzymes 1A2, 2C9, 2C19, 2D26, 2E1 and 3A4 of cytochrome P450 of the liver. In animals, telbivudine does not induce cytochrome P450 isoenzymes. Given the above results and the known pathways for elimination of telbivudine, there is a low potential for interactions of Sebivo with other drugs at the level of cytochrome P450. The pharmacokinetic parameters of Telbivudine in the equilibrium state did not change after repeated use in combination with lamivudine, adefovir, dipivoxil, cyclosporine and interferon? -2a.
special instructions
after discontinuation of hepatitis B therapy, telbivudine was reported to have severe exacerbations of the disease in patients. It is necessary to carefully monitor liver function by clinical and laboratory parameters in patients who for one reason or another suspended treatment with telbivudine. If necessary, you should immediately resume therapy with drugs for the treatment of hepatitis B. When using nucleotide / nucleoside analogues as monotherapy or in combination with antiretroviral drugs, lactic acidosis and severe hepatomegaly, sometimes fatal, have been reported. When using telbivudine and other drugs of this class, cases of myopathy have been reported, recorded during the use of the drug for a period of several weeks to months from the start of therapy. Factors contributing to the development of myopathy among patients taking telbivudine are not known. Patients should immediately report any persistent pain of unknown etiology or muscle weakness. Telbivudine therapy should be discontinued if myopathy is diagnosed. The physician should regularly monitor patients at risk of myopathy. Patients with impaired renal function Telbivudin is mainly excreted through the kidneys, so patients with creatinine clearance of 50 ml / min, including patients on hemodialysis, should choose the interval between doses in accordance with the recommendations given. In addition, taking Sebivo simultaneously with drugs that can affect kidney function may cause changes in the concentrations of telbivudine or the corresponding drugs in the blood plasma.Patients infected with hepatitis B with resistance to antiviral drugs Adequate and properly controlled studies of treatment with telbivudine in patients infected with hepatitis B with established resistance to lamivudine were not conducted. In vitro, telbivudine demonstrated efficacy against single mutations of the M204V hepatitis B virus strain with no activity for M204V / L180M double mutations and single mutations of M204I virus strains. Also, adequate and well-controlled studies of the treatment of telbivudine infected with hepatitis B patients with established resistance to adefovir were not conducted. In vitro, Telbivudine was active against mutant strains of the N236T virus. Patients after liver transplantation Safety and efficacy of telbivudine in patients with transplanted liver are not known. The pharmacokinetics of the achieved telbivudine level did not change when continuously taken in combination with cyclosporine. If there is a need for telbivudine therapy in patients with a transplanted liver who have taken or are receiving immunosuppressants with a known effect on liver function (in particular, cyclosporine or tacrolimus), it is necessary to monitor liver function before and during Sebivo treatment. Separate groups of patients The use of the drug Sebivo was not investigated among patients with hepatitis B who had co-infections (for example, they were simultaneously infected with HIV, hepatitis C or D). Elderly patients Clinical studies of Telbivudine were not performed in patients over the age of 65 in an amount sufficient to determine the difference in their responses compared with young patients. In general, it is necessary to take elderly patients with Sebivo with caution, given the abnormal liver function that is common in this age group due to concomitant diseases and due to the concurrent use of other medications. Information for patients Patients should be informed that treatment with Sebivo does not reduce the risk of transmission of hepatitis B virus through sex or with blood. Clinical data on the effects of telbivudine on female and male reproductive function are absent. Children.Studies on the use of this drug in children under the age of 18 years have not been conducted. Therefore, to obtain a more complete amount of information Sebivo is not recommended for use in the treatment of children. The ability to influence the reaction rate when driving vehicles or other mechanisms. Data on the effect of the drug and recommendations are not available.