Active substanceTenofovirTenofovir
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  • Dosage form: & nbspfilm-coated tablets
    Composition:

    Active Ingredient:

    Tenofovir disoproxil fumarate 300.0 mg Excipients:

    Croscarmellose sodium 40.0 mg Lactose monohydrate 153.66 mg Microcrystalline cellulose 133.34 mg Pregelatinized starch 33.33 mg Magnesium stearate 6.67 mg

    Opaprai II light blue (Dioxide of titanium - dye; FD&C blue № 2, aluminum varnish certified in accordance with the law FD&C (FD&C Blue # 2 Aluminum Lake) - dye; Hypromellose; Lactose Monohydrate (Lactose Monohydrate) - filler; Triacetin (Triacetin)) 32.0 mg

    Description:The tablets covered with a film shell of light blue color, biconcave, triangular with rounded ends, with engraving "H" on one side and "123" on the other side.
    Pharmacotherapeutic group:An antiviral agent.
    ATX: & nbsp

    J.05.A.F.07   Tenofovir

    Pharmacodynamics:

    Tenofovir disoproxil fumarate in vivo turns into tenofovir, an analogue of the nucleoside monophosphate (nucleotide) of adenosine monophosphate. Tenofovir in the subsequent turns into an active metabolite - tenofovir diphosphate. Tenofovir - nucleotide reverse transcriptase inhibitor, has specific activity against the human immunodeficiency virus (HIV-1 and HIV-2).

    Pharmacokinetics:

    When administered orally on an empty stomach, the bioavailability of tenofovir is approximately 25% and up to 40% (during meals); improves when taken with food, especially with a high fat content. Clinically significant effect on the effectiveness of tenofovir does not have food. After a single oral fasting dose of 300 mg, the maximum concentration in blood serum is achieved after 1 ± 0.4 h. The pharmacokinetics of tenofovir are dose-dependent.

    The half-life (T1 / 2) of the cell is> 60 h;

    After a single oral administration of tenofovir, T1 / 2 tenofovir is approximately 17 hours. After repeated oral administration at a dose of 300 mg once a day (under fasting conditions), 32 + 10% of the accepted dose is determined in the urine for more than 24 hours.

    Tenofovir is excreted by the kidneys, by glomerular filtration and active tubular secretion.

    Indications:

    - Treatment of HIV-1 infection in combination antiretroviral therapy in adults.

    Contraindications:

    Hypersensitivity to any component of the drug.

    Children under 18 years.

    Patients from renal insufficiency with creatinine clearance less than 30 ml / min, as well as patients who need hemodialysis.

    Lactation period.

    Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.

    Simultaneous application of together with other drugs containing tenofovir, didanosine, adefovir.

    Carefully:

    Renal failure with creatinine clearance less than 50 ml / min, including patients on hemodialysis. When creatinine clearance is less than 30 ml / min, use of the drug should be avoided; in the event that other treatment is not available, the kidney function should be carefully monitored and the interval between administration of the drug should be adjusted.

    Pregnancy and lactation:

    When deciding on the use of the drug in pregnancy, it is necessary to correlate the expected therapeutic effect for the mother with the possible risk of using the drug for the fetus. In connection with the revealed changes in bone tissue on the background of taking the drug,and limited experience of use, it is recommended that the drug be used with caution during pregnancy. Women of childbearing age during treatment should use reliable methods of contraception.

    Nursing mothers: HIV-infected women should be were instructed to exclude breastfeeding.

    Dosing and Administration:

    Inside, regardless of food intake.

    The recommended dose for the treatment of HIV-1 infection is 300 mg once a day. Antiretroviral therapy is shown, as a rule, throughout life.

    In the treatment of chronic hepatitis EP 300 mg once a day.

    - Have HBeAg - positive patients without cirrhosis liver treatment should be continued for at least 6-12 months after confirmation of seroconversion by HBe (disappearance HBeAg or the disappearance of the DNA of the hepatitis B virus, with the detection of anti-EPBe), or before seroconversion to HBs, and until the loss of effectiveness. To detect any delayed virological relapse after the end of treatment, it is necessary to regularly check the levels of ALT and DNA of the hepatitis B virus, in the blood serum.

    - Have HBeAg - negative patients without cirrhosis liver treatment should be continued at least until seroconversion HBs or before the moment loss effectiveness.

    When prolonged treatment for more than 2 years, it is recommended that the patient be examined regularly to confirm that the treatment chosen for a particular patient remains adequate.

    Recommended mode dosing Tenofovir at renal failure:

    Creatinine clearance 50-80 ml / min: there is no need to adjust the dose. It is necessary to carry out constant monitoring of creatinine clearance and concentrations phosphates in serum.

    Creatinine clearance 30-49 ml / min: 300 mg every 48 hours.

    Creatinine clearance less than 30 ml / min (including patients, which requires hemodialysis): the drug use Not recommended. Patients with a dysfunction of the liver do not need a dose adjustment.

    The duration of treatment with the drug Tenofovir is determined individually by the attending physician.

    Side effects:

    Below are the undesirable reactions with the alleged (possible) connection with the drug, listed by system-organ classes in order of decreasing their severity, with the following frequency: very often (> 1/10) and often (> 1/100, <1/10 ), rarely (> 1/10000, <1/1000), very rarely (<1/10000), including individual cases.

    Disruption of metabolism and nutrition: very often - hypophosphatemia.

    From the nervous system: very often - dizziness.

    From the gastrointestinal tract: very often - diarrhea, vomiting, nausea; often - flatulence.

    Combined retroviral therapy was associated with metabolic disorders such as hypertriglyceridemia, hypercholesterolemia, insulin resistance, hyperglycemia and hyperlactatemia; redistribution of subcutaneous tissue (lipodystrophy).

    Osteonecrosis cases have been reported, especially in patients with risk factors or with long-term combined antiviral therapy. The frequency is unknown.

    Post-marketing experience

    Disturbance of metabolism and nutrition: rarely - lactic acidosis, frequency is unknown - hypokalemia

    Respiratory, thoracic and mediastinal disorders: very rarely - dyspnoea.

    From the gastrointestinal tract: rarely - pancreatitis.

    From the hepatobiliary system: rarely - increased activity of transaminases; very rarely - hepatitis, the frequency is unknown - steatosis of the liver.

    From the skin and subcutaneous tissues: rarely - a rash.

    From the musculoskeletal system: frequency unknown -bradomyolysis, osteomalacia, muscle weakness, myopathy.

    From the urinary system: rarely acute renal failure, proximal renal tubulopathy (including Fanconi syndrome), hypercreatininaemia; very rarely - acute tubular necrosis; frequency unknown - nephritis (including acute interstitial), nephrogenic diabetes insipidus.

    General disorders and changes in the place of administration: very rarely - asthenia.
    Overdose:

    In case of an overdose, the patient should be examined to identify possible signs of intoxication. If necessary, standard maintenance therapy is used.

    Tenofovir is effectively removed by hemodialysis with an extraction ratio of approximately 54%. After taking 300 mg of tenofovir, a 4-hour hemodialysis procedure results in the removal of approximately 10% of the accepted dose of tenofovir.

    Interaction:

    Didanosine: increase in the concentration of didanosine in a joint

    application; it is necessary to use them with caution and to monitor the manifestations of toxicity of didanosine (eg, pancreatitis, neuropathy).The combination of tenofovir with didanosine is not recommended; if warranted, consideration should be given to reducing the dose or discontinuation of didanosine therapy. Tenofovir is combined with reduced doses of didanosine (for example, patients with a body weight> 60 kg are prescribed didanosine 250 mg once a day; <60 kg - 200 mg once a day). On the other hand, this low-dose combination may be characterized by low antiviral activity and an insufficient increase in the number of C04 lymphocytes, as indicated by the high incidence of treatment failure with this combination with the addition of efavirenz or nevirapine.

    Atazanavir: a decrease in the concentration of atazanavir in joint use and an increase in tenofovir concentrations. It should be applied tenofovir with atazanavir only with an additional increase in the action of the latter with ritonavir.

    Lopinavir / ritonavir: increased concentrations of tenofovir joint application.

    Darunavir: increases the concentration of tenofovir by 20-25%. The drugs should be used in standard doses, while carefully monitoring the nephrotoxic effect of tenofovir.

    Tenofovir is mainly excreted through the kidneys, the joint use of tenofovir with drugs that reduce renal function or shorten / stop active tubular secretion, may increase the serum concentration of tenofovir and / or increase the concentrations of other drugs that are excreted through the kidneys.

    Ganciclovir, valganciclovir and cidofovir compete with tenofovir for active tubular secretion by the kidneys, resulting in increased levels of tenofovir or a concomitant medication; caution is required regarding possible side effects. Nephrotoxic drugs may also increase the concentration of tenofovir in serum.

    Special instructions:

    Patients receiving tenofovir, should be informed that treatment with antiretroviral drugs does not prevent the risk of transmission of HIV and hepatitis B to other people. During sexual intercourse, appropriate precautions should be taken.

    Simultaneous use with other medicinal products.

    Tenofovir is contraindicated in conjunction with other drugs containing tenofovir, didanosine, adefovir.

    Triple therapy with nucleoside / nucleotide, and inhibin and tori and reverse transcriptase of HIV. A possible rapid development of virological failure and the emergence of resistance in the early stages of HIV-infected patients receiving tenofovir dizoproxil fumarate in combination with lamivudine and abacavir, as well as lamivudine and didanosine, taken once a day, has been reported.

    Lactate acidosis and severe hepatomegaly with steatosis.

    When used in HIV-infected patients individuals

    nucleoside analogs, including tenofovir, dizoproxil fumarate, in combination with other antiretroviral drugs, lactate acidosis and a pronounced increase in liver size with its fatty dystrophy, sometimes fatal, have been reported. As a rule, lactic acidosis develops after several months from the beginning of treatment.

    If the patient develops clinical (on the part of the digestive system - nausea, vomiting, abdominal pain, general malaise, loss of appetite, weight loss; violation of breathing;

    neurologic symptoms - impaired motor functions, muscular weakness) or laboratory signs (the content of lactic acid in the serum above 5 mmol / l), indicating lactate acidosis or pronounced hepatotoxicity, tenofovir therapy must be suspended.

    Caution should be exercised when prescribing nucleoside analogues following patients: women with increased mass body, patients with hepatomegaly, hepatitis or other known risk factors for liver disease (including medicines and alcohol).

    Special risk present are patients with a co-infection of HIV and hepatitis C taking alpha interferon and ribavirin.

    Patients with impaired renal function.

    Deprivation of tenofovir mainly occurs through the kidneys. When tenofovir was used in clinical practice, cases of detection of renal failure were reported, increasing concentration creatinine, hypophosphatemia, and Fanconi syndrome. Have all patients before the start of therapy, and if there is a clinical indication, during therapy with tenofovir, it is recommended to calculate the clearance of creatinine. Interval correction between doses of the drug should be in accordance with the recommendations (see."Method of administration and dose"). Have patients with a risk of developing a disorder kidney function, including patients who have previously been found to have impaired kidney function when treated with adefovir, should be given a regular monitoring the calculated clearance of creatinine and the concentration of phosphorus in the blood serum. The drug can not be used concomitantly with nephrotoxic drugs or in the case of recent use of drugs of this kind.

    Use tenofovir in patients with creatinine clearance from 30 to 49 ml / min should be used with caution, at this adjust intervals between doses (cm. "Method of administration and dose"). Have of such patients should be conduct a thorough observation behind the kidney function.

    Undesirable reactions may result from renal tubulopathy of the proximal type: rhabdomyolysis, osteomalacia (manifested by pain in the bones, can lead to fractures), hypokalemia, muscle weakness, myopathy, hypophosphatemia.

    Patients infected with HIV, hepatitis B and C virus.

    Patients with chronic hepatitis B or C and taking antiretroviral therapy, are at increased risk of severe and potentially fatal adverse reactions from the liver.

    In the case of combined antiviral therapy for hepatitis B or C, contained in the instructions on the use of these drugs.

    In patients infected with HIV and hepatitis B virus, severe withdrawal may occur after withdrawal of tenofovir therapy hepatitis A. For patients infected with HIV and hepatitis B virus who stopped using tenofovir, A close monitoring, both clinical and laboratory, should be carried out at least 6 months after discontinuation of therapy. In some cases, it may be necessary resumption of hepatitis B therapy. In patients with severe liver disease (cirrhosis), it is not recommended to discontinue treatment, because after exacerbation of therapy, exacerbation of hepatitis can lead to decompensation of liver function.

    Testing for antibodies to HIV should be available to all patients, infected with hepatitis B virus before the initiation of therapy with tenofovir.

    In connection with the risk of developing resistance tenofovir should use as part of the relevant antiretroviral treatment for those infected with HIV and hepatitis B.

    Liver disease.

    Tenofovir and disoproxil fumarate are metabolized by the liver.

    Patients with existing liver dysfunction, including those with chronic active hepatitis, are more likely to have liver function abnormalities with combined antiretroviral therapy. Such patients should monitor liver function in accordance with standard practice. With the development of symptoms of worsening liver disease in this category of patients, interrupt or stop treatment.

    Lipodystrophy.

    Patients undergoing antiretroviral therapy, redistribution / accumulation of adipose tissue in the body, including obesity of the central type, increased deposition of adipose tissue on the back and neck ("buffalo hump"), a decrease in the volume of peripheral adipose tissue and subcutaneous fat in the face, mammary hypertrophy and the so-called "Cushingoid appearance".

    Mechanisms and long-term consequences of these phenomena are still unknown, there is no causal relationship with the use of certain drugs.

    Osteonecrosis.

    Despite the fact that the etiology of osteonecrosis is considered multifactorial (including the use of corticosteroids, alcohol consumption, etc.), cases of osteonecrosis have been documented, especially in patients with HIV infection and / or at long antiretroviral therapy. Patients should be advised to see a doctor if they experience joint pain and difficulty moving.

    Early virological inefficiency.

    In clinical studies involving HIV-infected patients, it was shown that a number of regimens using nucleoside reverse are generally less effective than triple regimes involving the use of two nucleoside reverse transcriptase inhibitors in combination with non-nucleoside inhibitors reverse transcriptase or HIV-1 protease inhibitors. Early virological inefficiency and high incidence of mutations (by type of substitution), causing the development of resistance. On this basis, regimes involving the use of three nucleoside inhibitors reverse transcriptase, use with caution. For patients whose mode of use of only three nucleoside inhibitors reverse transcriptase should be carefully monitored; in such cases it is also recommended to consider the possibility of changing the scheme of therapy.

    Syndrome restoration of immunity.

    In HIV-infected patients, receiving a combination antiretroviral therapy there was a development of the immune reconstitution syndrome.

    In patients with severe immunodeficiency at the onset of antiretroviral therapy, an inflammatory response may occur in response to asymptomatic or residual opportunistic infections, which can lead to the development of serious clinical states or increase severity of symptoms. Such reactions are observed, as a rule, in the first few weeks or months of antiretroviral

    Examples can cytomegalovirus generalized and / or focal mycobacterial infection and pneumonia, called Pneumocystis jiroveci. Any symptoms of an inflammatory nature requires an appropriate assessment and, if necessary, the beginning of treatment. Patients should be under careful clinical observation specialists with experience in the treatment of patients with HIV diseases.Autoimmune diseases diseases (eg, Graves' disease) were observed on background recovery immunity, however, the time of primary sprains varied and the disease could occur many months after initiation of therapy and have an atypical course.

    Mitochondrial dysfunction. Nucleoside and nucleotide analogs in conditions in vitro and in vivo demonstrated the ability of damage mitochondria.

    The main adverse disorders are hematologic violations (anemia, neutropenia) and metabolic disorders (hyperlactatemia, hyperlipazemia). These events are often temporary. There were are registered later neurological violations (hypertension, convulsions, behavioral disorders).

    Effect on the ability to drive transp. cf. and fur:During the period of application of the drug, patients are recommended with caution drive and engage in other potentially hazardous activities due to possible dizziness. When the described undesirable phenomena should refrain from performing these activities.

    Form release / dosage:

    Film-coated tablets 300 mg.

    Packing: 30, 60, 100, 500 or 1000 tablets in a polymer bottle. The bottle with instructions for medical use is placed in a cardboard box.

    Packaging:film coated tablets, 300 mg (can) 30 x 1 tablets, film-coated, 300 mg (bottle) 30/60/100/500/1000 x 1
    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:2 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-002600/10
    Date of registration:30.03.2010
    The owner of the registration certificate:DIALOGPARMA, LLC DIALOGPARMA, LLC Russia
    Manufacturer: & nbsp
    Representation: & nbspDIALOGPARMA, LLCDIALOGPARMA, LLC
    Information update date: & nbsp17.09.2015
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