Zeffix coated pills 100mg N28
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Active ingredients
Lamivudin
Release form
Pills
Composition
1 tablet contains: Active substance: lamivudine 100 mg. Auxiliary substances: microcrystalline cellulose, sodium starch glycolate, magnesium stearate. Composition of the shell: yellowish brown material for applying the shell YS-1-17307-A (hypromellose, titanium dioxide, iron red oxide (E172), iron oxide yellow (E172), macrogol 400, polysorbate 80).
Pharmacological effect
Antiviral drug - nucleoside analogue. Highly active against the hepatitis B virus. In both infected and non-infected cells, lamivudine is metabolized to lamivudine triphosphate, which is the active form of the drug and serves as a substrate for the hepatitis B virus polymerase. The inclusion of lamivudine triphosphate in the chain of viral DNA and the subsequent breakage of the chain block further the formation of viral DNA. Lamivudina triphosphate does not disrupt the normal cellular metabolism of DNA. It is also a weak inhibitor of mammalian α- and β-DNA polymerases. Lamivudina triphosphate does not have a significant effect on the DNA content in the cells. Lamivudine did not show any significant toxic effects on the structure of mitochondria, as well as on the content and function of DNA. Lamivudin has a very weak ability to reduce the content of mitochondrial DNA, is not included in its chain and does not inhibit γ-polymerase.
Pharmacokinetics
AbsorptionAfter ingestion, lamivudine is well absorbed from the gastrointestinal tract. Bioavailability in adults after oral administration is usually 80-85%. Cmax in serum is reached on average in approximately 1 hour. When prescribing the drug in therapeutic doses (100 mg 1 time / day) Cmax is 1.1-1.5 mcg / ml, Cmin - 0.015-0.2 mcg / ml. Reception of Zeffix with food leads to increase the time to reach Cmax and reduce its value (up to 47%). At the same time, food intake did not affect the overall degree of absorption of lamivudine (calculated on the basis of the concentration-time curve). Distribution When administered intravenously, lamivudine Vd averaged 1.3 l / kg. In the therapeutic dose range, lamivudine has linear pharmacokinetics and is slightly associated with plasma proteins. Lamivudine penetrates into the central nervous system and into the cerebrospinal fluid. After 2-4 hours after ingestion, the ratio of lamivudine concentrations in the cerebrospinal fluid and serum was approximately 0.12. Metabolism Mildly (5-10%) is metabolized in the liver. Introduction The systemic clearance of lamivudine is, on average, about 0.3 l / h / kg. T1 / 2 - approximately 5-7 h.Most of lamivudine is excreted unchanged by the kidneys through glomerular filtration and active secretion (the system of transport of organic cations). The proportion of renal clearance accounts for about 70% of lamivudine elimination. Pharmacokinetics in special clinical situations In patients with renal failure, the elimination of lamivudine from the body slows down. Patients with creatinine clearance less than 50 ml / min need to reduce the dose of Zeffix. Patients with hepatic insufficiency (not infected with HIV and hepatitis B virus) are well tolerated by lamivudine. Impaired liver function does not affect the pharmacokinetics of lamivudine, unless combined with renal insufficiency. In elderly patients, age-related decline in renal function does not significantly affect the elimination of lamivudine in CC over 50 ml / min. In women in late pregnancy, lamivudine pharmacokinetics after administration inside was similar to that of non-pregnant women. The pharmacokinetics of lamivudine in children do not differ from the pharmacokinetics in adults. However, in children, lamivudine clearance, adjusted for body weight, is higher than in adults, resulting in a decrease in AUC. The highest clearance of lamivudine is observed in children aged 2 years and decreases by the age of 12, when its values become similar to those in adults. The recommended dose for children from 2 to 11 years is 3 mg / kg 1 time / day (up to 100 mg / day ) able to provide a comparable dose to an adult dose (100 mg / day) of lamivudine. There are few data on the pharmacokinetics of lamivudine in children under 2 years of age.
Indications
Comprehensive treatment of acute and chronic inflammatory diseases of the nasal cavity, paranasal sinuses and nasopharynx: acute and chronic rhinitis; acute and chronic sinusitis; acute and chronic adenoiditis; allergic rhinitis; atrophic rhinitis. Complex treatment of SARS and influenza. Prevention of ARVI and influenza during an epidemic. Care of the nasal cavity: after surgery, cleansing from bacteria, viruses, dust, pollen, smoke, preparation of the mucosa for the use of drugs, long-term therapy with topical corticosteroids.
Contraindications
Hypersensitivity to lamivudine or to any other component of the drug. Pregnancy I trimester. With caution should be used for renal failure, pancreatitis (including history), peripheral neuropathy, pregnancy (II-III trimester), during lactation, in children aged up to 2 years.
Use during pregnancy and lactation
There are not enough data on the safety of lamivudine during pregnancy. Lamivudine crosses the placenta. The concentration of lamivudine in the serum of newborns at the time of birth is the same as in mother’s serum and in the blood from the umbilical cord. The drug is contraindicated for use in the first trimester of pregnancy. if the pregnancy occurred during treatment with Zeffix, it should be borne in mind that after discontinuation of the drug may develop an exacerbation of hepatitis B. After ingestion, the concentration of lamivudine in the chest Om milk is not significantly different from its concentration in serum (1 μg / ml). Studies on animals suggest that the concentration of lamivudine in the human breast milk does not have a toxic effect on children during breastfeeding. Information about the transplacental transmission of the hepatitis B virus in pregnant women receiving Zeffix is absent. It is recommended to conduct a standard procedure for immunization of newborns against hepatitis B. In experimental animal studies, lamivudine showed no signs of teratogenicity or an effect on fertility. Data from studies in rabbits indicate a possible risk of spontaneous abortion in early pregnancy.
Dosage and administration
Zeffix can be taken regardless of the meal. Adults and children aged 12 years and over 100 mg once a day. Children from 2 to 11 years old 3 mg / kg once a day, but not more than 100 mg per day. Children under 2 years old There are insufficient data to recommend dosages in this age group. Renal failure In patients with creatinine clearance less than 50 ml / min, the dose should be reduced. If you need a dose of less than 100 mg per day, you should use Zeffix solution for oral administration. The degree of dose reduction in children with renal insufficiency is the same as in adults. Data on patients on hemodialysis (dialysis sessions 2-3 times a week for 4 hours or less) show that after the initial dose reduction of Zeffix in accordance with creatinine clearance, there is no further dose adjustment during the whole period of hemodialysis.Hepatic impairment In hepatic impairment, if it is not accompanied by renal failure, no dose adjustment of lamivudine is required.
Side effects
Zeffix is well tolerated by patients with chronic hepatitis B. The most common side effects are general malaise and fatigue, respiratory infections, headache, discomfort and abdominal pain, nausea, vomiting and diarrhea. The following are side effects from various systems. The category of frequency is indicated only for those side effects, the connection of which with the treatment with Zeffix is considered at least possible. In terms of frequency, side effects were divided into the following categories: very frequent (more than 1:10), frequent (more than 1: 100 and less than 1:10), infrequent (21: 1000 and less than 1: 100), rare (more than 1: 10 000 and less than 1: 1000 ), very rare (less than 1/10 000). The categories of frequency of side effects given below are estimates, since for most of the side effects there are no data on the basis of which their frequency could be calculated. The categories very frequent and frequent were determined based on the results of clinical trials, and the background frequency in the placebo groups was not taken into account . Side effects identified during post-marketing use of Zeffix are considered rare or very rare.
Overdose
No specific symptoms of lamivudine overdose have been identified. There are limited data on the effects of high doses of lamivudine in humans. Lethal outcomes were not observed, the condition of all patients returned to normal. In experimental studies, the administration of very high doses of lamivudine did not have a toxic effect on the organs. Treatment: gastric lavage, administration of activated carbon, monitoring of the patient’s condition, and standard maintenance therapy are recommended. Continuous hemodialysis may be used to remove lamivudine, but no special studies have been conducted.
Interaction with other drugs
Should consider the possibility of interaction of lamivudine with other drugs, especially with such, the main mechanism for the elimination of which is the active renal secretion through the system of transport of organic cations (trimethoprim).The simultaneous use of trimethoprim / sulfamethoxazole (160 mg / 800 mg) increases the concentration of lamivudine in the blood plasma by approximately 40%. Lamivudine does not alter the pharmacokinetics of trimethoprim and sulfamethoxazole (in the absence of renal failure there is no need to reduce the dose of lamivudine). Other drugs (for example, ranitidine, cimetidine) are only partially excreted using this mechanism and do not interact with lamivudine. Preparations that are excreted mainly through active transport of organic anions or by glomerular filtration do not appear to enter into clinically significant interactions with lamivudine. With simultaneous use of lamivudine and zidovudine, there is a moderate (28%) increase in Cmax of zidovudine in plasma, while the AUC does not change significantly. There was no pharmacokinetic The interaction of Zeffix with interferon alpha, as well as with immunosuppressants (for example, with cyclosporin A) Dapson, didanosine, isoniazid and stavudine increase the risk of developing peripheral neuropathy.
special instructions
Zeffix in the form of an oral solution is used to treat children and those patients who cannot take the drug in the form of pills. During treatment with Zeffix, the patient should be monitored regularly by a physician experienced in treating chronic hepatitis B. Termination of Zeffix therapy is possible in patients with normal biochemical parameters (ALT, AST), lack of DNA virus of hepatitis B in the blood and seroconversion HBeAg and / or HBsAg (not earlier than 3 months after the onset of seroconversion). Cancellation of Zeffix is also possible with the failure of further treatment (lack of positive dynamics within 6 months of treatment or symptoms of exacerbation of hepatitis). When discontinuing Zeffix, patients should be under the supervision of a physician to detect symptoms of exacerbation of hepatitis. Termination of therapy is not recommended when there are symptoms of hepatic failure.At present, there is insufficient data on maintaining long-term seroconversion after discontinuation of Zeffix. After discontinuation of treatment with Zeffix, it is necessary to periodically monitor the general condition of patients, as well as monitor functional liver function tests (liver transaminase activity and bilirubin content) for 4 months to detect signs of possible exacerbation of hepatitis ; in the future, patients should be monitored as indicated. Currently, there is no convincing evidence of the effectiveness of repeated treatment with the Zeffix drug for those patients who have exacerbated hepatitis after stopping the course of therapy. Patients should be under medical supervision for at least 6 months after stopping treatment for any reason. The condition of patients with symptoms of liver failure should be monitored more closely. There are few data on the use of lamivudine in patients receiving concomitant immunosuppressive therapy. During prolonged therapy with lamivudine, subpopulations of viral hepatitis B (YMDD-strain) with reduced sensitivity to it were identified. Sometimes this type of virus can cause exacerbation of hepatitis. When treating patients with a combination of HIV infection and hepatitis B virus infection who are already receiving or will receive antiretroviral therapy, including lamivudine, it is necessary to maintain the dose of lamivudine, usually prescribed for the treatment of HIV infection. Patients It is necessary to warn that treatment with Zeffix does not reduce the risk of transmission of hepatitis B to other people and therefore it is necessary to observe appropriate precautions. If necessary, use the drug and in patients with diabetes, it should be borne in mind that each dose of oral solution (100 mg / 20 ml) contains 4 g of sucrose. Use in pediatrics The recommendations for determining the effective and safe dose in children under 2 years of age are not enough. Influence on the ability to drive vehicles and control mechanismsSpecial studies have not been conducted. Based on the pharmacological properties of lamivudine, such an effect is unlikely.