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

    Active substance:

    Tenofovir disoproxil fumarate 150 mg, 300 mg Excipients:

    Each film-coated tablet contains:

    Core: carboxymethyl starch sodium (primogel) - 16.5 mg / 33.0 mg, silicon dioxide colloid (aerosil grade A-300) - 1.5 mg / 3.0 mg, croscarmellose sodium -21,0 mg / 42.0 mg, lactose monohydrate 72.0 mg / 144.0 mg, magnesium stearate 3.0 mg / 6.0 mg, microcrystalline cellulose 36.0 mg / 72.0 mg.

    Finished water-soluble film shell- 9.0 mg / 18.0 mg.

    (Sheath composition: hydroxypropylmethylcellulose (hypromellose) - 74,2 %, polyethylene glycol 6000 (Macrogol 6000) - 14.3%, titanium dioxide 3.5%, talc-2.3%, iron dye red oxide-1.4%, iron-oxide oxide yellow-4.3%).

    Description:

    For a dosage of 150 mg:

    Round biconvex tablets covered with a film coat from light brown to brown.

    For a dosage of 300 mg:

    Oval biconvex tablets covered with a film coat from light brown to brown.

    On the cross-section the nucleus is white or white with a yellowish tint of color.
    Pharmacotherapeutic group:An antiviral agent.
    ATX: & nbsp

    J.05.A.F.07   Tenofovir

    Pharmacodynamics:

    Mechanism of action

    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) and hepatitis B virus.

    Tenofovir diphosphate inhibits HIV-1 reverse transcriptase by a competitive mechanism, resulting in the termination of DNA chain synthesis.

    Tenofovir diphosphate is a mild inhibitor of mammalian DNA polymerases. In the tests in vitro tenofovir at concentrations of 300 μmol / l had no effect on the synthesis of mitochondrial DNA and the formation of lactic acid.

    Antiviral activity

    The antiviral activity of tenofovir against laboratory and clinical strains of HIV-1 was evaluated on the lines of lymphoblastoid cells, primary monocytes / macrophages and peripheral blood lymphocytes. The indicator of the effective concentration of tenofovir was in the range from 0.04 to 8.5 μmol.

    In cell culture tenofovir showed showed antiviral action against HIV-1 subtypes A, B, C, D, E, F, G, O (the effective concentration was in the range from 0.5 to 2.2 μmol), as well as the inhibitory effect on some strains of HIV-2 (the effective concentration was in the range from 1.6 to 5.5 μmol).

    In studies of combined use of the drug with HIV protease inhibitors and with nucleoside and non-nucleoside reverse transcriptase inhibitors HIV-1, additive or synergistic effects were noted.

    Resistance

    In studies in vitro and in some patients infected with HIV-1, strains with tenofovir resistance due to mutation K65R in reverse transcriptase.

    The use of tenofovir by the disoproxil fumarate should be avoided in the presence of mutations K65R in patients who had previously received antiretroviral therapy.

    Pharmacokinetics:

    Suction

    After oral administration, in HIV-infected patients, tenofovir disoproxil fumarate is rapidly absorbed and converted into tenofovir. Maximum Concentrations Tenofovir in the blood serum was observed an hour after taking an empty stomach and two hours after ingestion with food. With oral administration of tenofovir, the disoproxil fumarate on an empty stomach was bioavailable at approximately 25%.

    When TDF was administered with disoproxil fumarate with food, bioavailability increased, while the area under the concentration-time curve and the average maximum tenofovir concentration increased approximately 40% and 14%, respectively. After a single dose of tenofovir, dizoproxil fumarate with food, the maximum serum concentration is from 213 to 375 μg / ml.

    Distribution

    The distribution volume in the equilibrium state after intravenous administration of tenofovir was approximately 800 ml / kg. At concentrations of tenofovir from 0.01 to 25 μg / ml, the binding of tenofovir to plasma and serum proteins in vitro is less than 0.7% and 7.2%, respectively.

    Metabolism

    In studies in vitro studies have shown that neither tenofovir disoproxil fumarate nor tenofovir are not substrates of human cytochrome P450 isoenzymes. Moreover, at concentrations significantly (approximately 300 times) higher than the concentrations observed in vivo, tenofovir in conditions in vitro did not inhibit the metabolic processes taking place with participation of the main isoenzymes of human cytochrome P450 (CYP3A4, CYP2D6, CYP2C9, CYP2E1 and etc.). Tenofovir disoproxil fumarate did not affect any cytochrome P450 isoenzymes except for CYP1A1/2 (there was a small (6%), but a statistically significant decrease in substrate metabolism CYP1A1/2).

    Excretion

    Deprivation of tenofovir mainly occurs through the kidneys through glomerular filtration and active tubular secretion.

    Linearity / nonlinearity

    The pharmacokinetics of tenofovir does not depend on the dose of tenofovir disoproxil fumarate (when taken in doses of 75 to 600 mg). Multiple administration of the drug at any dose also does not affect the pharmacokinetics of tenofovir.

    Pharmacokinetics in special populations

    The pharmacokinetics in men and women do not differ significantly.

    No pharmacokinetic studies have been conducted with the participation of children, adolescents under 18, and elderly people over 65 years of age.

    Special studies of pharmacokinetics in different ethnic groups were not conducted.

    Indications:Treatment of HIV-1 infection in combination antiretroviral therapy.
    Contraindications:

    Hypersensitivity to any of the components of the drug.

    Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption syndrome, since the preparation contains lactose.

    Simultaneous reception with didanosine.

    Simultaneous reception with other drugs containing tenofovir; simultaneous administration with adefovir.

    Children under 18 years.

    Renal failure with creatinine clearance less than 30 ml / min, including patients who need hemodialysis.

    Lactation period.

    Carefully:

    Age over 65 years.

    Renal failure with a creatinine clearance greater than 30 ml / min and less than 50 ml / min.
    Pregnancy and lactation:

    Tenofovir should be prescribed during pregnancy only in those cases where the expected benefit to the mother exceeds the possible risk to the fetus.

    In animal studies, it was shown that tenofovir excreted in breast milk. It is not known whether tenofovir with human breast milk.

    It is not recommended to breast-feed HIV-infected mothers receiving therapy with tenofovir, in order to prevent the risk of postnatal HIV transmission.

    Dosing and Administration:

    Inside, during meals or on an empty stomach. Adults drug prescribed in a dose of 300 mg 1 time per day.

    Patients with impaired renal function

    For patients with mild renal impairment (when creatinine clearance is 50-80 ml / min), tenofovir 1 time per day is safe and effective, so there is no need to adjust the dose, these patients need to conduct a constant monitoring of creatinine clearance and serum phosphate concentrations .

    In patients with creatinine clearance from 30 to 49 ml / min, the interval between doses should be adjusted in accordance with the recommendations in Table 1.

    Table 1. Correction of dose in patients with altered creatinine clearance

    Creatinine clearance (ml / min)1

    >50

    30-49

    < 30 (including patients who need hemodialysis)

    Recommended interval between meals

    Every 24 hours

    Every 48 hours

    Tenofovir is not recommended

    1 the ideal body weight was used in the calculations

    Patients with impaired hepatic function no dose adjustment is required. Antiretroviral therapy is shown, as a rule, throughout life. The duration of therapy with tenofovir is determined individually by the attending physician.
    Side effects:

    From the gastrointestinal tract: diarrhea, vomiting, nausea, flatulence, increased activity of amylase, pancreatitis, abdominal pain, bloating.

    From the nervous system: dizziness, headache, depression.

    On the part of the immune system, allergic reactions, including angioedema.

    From the side of metabolism: hypophosphatemia, lactate-acidosis, hypokalemia.

    From the respiratory system: shortness of breath.

    From the liver and biliary tract: fatty liver dystrophy, increased activity of liver enzymes (most often - aspartate aminotransferase, alanine aminotransferase, gamma-glutamyltranspeptidase), hepatitis.

    From the skin and subcutaneous fat: rash.

    From the musculoskeletal system: rhabdomyolysis, osteomalacia (more often manifested by pain in the bones, occasionally leads to fractures), muscle weakness, myopathy.

    From the urinary system: renal failure, acute renal tubular necrosis, Fanconi syndrome, proximal proximal tubulopathy, interstitial nephritis (including cases of acute nephritis), nephrogenic diabetes insipidus, increased creatinine concentration, proteinuria, polyuria.

    Other: asthenia, fatigue.

    Overdose:

    There is limited clinical experience with the use of tenofovir in doses exceeding the therapeutic dose of 300 mg. Eight patients received 600 mg of tenofovir dizoproxil fumarate for 28 days, with no serious adverse reactions observed. Symptoms of overdose when taking higher doses are not known.

    In case of an overdose, it is necessary to monitor the patient's condition to detect signs of toxicity. If necessary, standard maintenance therapy is used. Tenofovir is removed from the body by hemodialysis; The median clearance of tenofovir is 134 ml / min. It is not known whether tenofovir from the body with peritoneal dialysis.

    Interaction:

    With the simultaneous administration of tenofovir with didanosine, the systemic exposure of didanosine increases by 40-60%, which increases the risk of side effects of didanosine (such as pancreatitis, lactic acidosis, including fatal). The simultaneous administration of tenofovir and didanosine at a dose of 400 mg / day resulted in a decrease in the number Cd4+ lymphocytes (probably due to intracellular interaction, the phosphorylation of didanosine increases). The combined use of tenofovir and didanosine is not recommended.

    With simultaneous application darunavir increases plasma concentrations of tenofovir by 20-25%. When assigning this combination darunavir and tenofovir should be used in standard doses, and careful monitoring is required to detect tenofovir nephrotoxicity.

    Tenofovir changes the pharmacokinetics of atazanavir. When co-prescribing these drugs, it is recommended that atazanavir only in combination with ritonavir (atazanavir 300 mg / ritonavir 100 mg).

    In studies conducted on healthy volunteers,Clinically significant drug interactions were not observed with simultaneous use of tenofovir with abacavir, efavirenz, emtricitabine, lamivudine, indinavir, lopinavir / ritonavir, nelfinavir, oral contraceptives, ribavirin, saquinavir / ritonavir.

    Tenofovir is mainly excreted from the body through the kidneys, the joint use of tenofovir with drugs that affect kidney function or reduce / stop active tubular secretion can increase the concentration of tenofovir in the blood serum and / or increase the concentration of co-administered drugs that are excreted through the kidneys:

    Ganciclovir competes with tenofovir for active tubular secretion by the kidneys, resulting in increased concentrations of tenofovir in blood plasma. When this combination is prescribed, careful clinical monitoring is required to identify possible side effects of tenofovir.

    With the simultaneous use of tenofovir with aminoglycosides or amphotericin B, the risk of developing nephrotoxicity increases, possibly a rise in serum creatinine levels.Joint use of tenofovir with aminoglycoside or amphotericin B should be avoided. In cases where joint use can not be avoided, careful monitoring of renal function should be performed during treatment, by conducting the necessary laboratory tests.

    Simultaneous use of tenofovir with tacrolimus increases the risk of developing nephrotoxicity. When this combination is prescribed, careful monitoring of renal function is required.

    Special instructions:

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

    Simultaneous use with other medicinal products

    Tenofovir should not be used concurrently with drugs that contain

    tenofovir or adefovir. It is not recommended simultaneous use of tenofovir and didanosine.

    Osteonecrosis

    Although the etiology of osteonecrosis is considered multifactorial (for example, taking glucocorticosteroids, drinking alcohol, acute immunosuppression, increased body mass index play an important role in the development of this complication),there are reports of such cases, particularly in patients with advanced HIV infection / or duration of antiretroviral therapy. Patients should seek medical advice from a physician if symptoms such as lethargy, stiffness, joint pain or difficulty with movement occur. Mitochondrial dysfunction

    In conditions in vitro and in vivo the ability of nucleotide and nucleoside analogs to cause damage to mitochondria of different degrees was revealed. There have been cases mitochondrial dysfunction in HIV-negative children exposed to nucleoside analogues in utero or immediately after birth. The main manifestations of mitochondrial dysfunction, often transient, were anemia, neutropenia, hyperlactatemia and increased lipase activity in blood plasma. Lactic acidosis, vyraeyuenaya hepatomegaly with steatosis When used in HIV-infected patients, the nucleotide and nucleoside analogs, including tenofovir disoproxil fumarate in combination with other antiretroviral drugs, reported cases of lactic acidosis and a marked increase in size of the liver and its steatosis, including fatal cases.Due to the high risk of developing lactic acidosis, special care should be taken when administering tenofovir to patients (especially women with excessive body weight) with hepatomegaly and fatty liver disease, with hepatitis, and in the presence of risk factors for liver damage. Clinical or laboratory signs of lactic acidosis can be detected several months after the start of treatment, but the development of this complication is possible in a shorter time. If the patient develops clinical (from the digestive system - nausea, vomiting, abdominal pain, general malaise, loss of appetite, weight loss, respiratory failure, neurologic symptoms - impaired motor function, muscle weakness) or laboratory (lactic acid in serum blood levels above 5 mmol / l) signs of lactic acidosis, or severe hepatotoxicity, therapy with tenofovir should be suspended.

    Patients with impaired renal function

    The excretion of tenofovir mainly occurs through the kidneys. With the use of tenofovir in clinical practice, there have been cases of renal failure, increasing the concentration of creatinine, hypophosphatemia, as well as Fanconi syndrome.

    All patients before the start of therapy and, if there is a clinical indication, during therapy with tenofovir is recommended to determine the clearance of creatinine. Correction of intervals between doses of the drug should be carried out in accordance with the recommendations presented in the section "Method of administration and dose" (subsection "Patients with impaired renal function").

    In patients at risk of developing renal dysfunction, including patients who previously had renal dysfunction with adefovir, regular monitoring of creatinine clearance and serum phosphorus concentrations should be performed.

    Tenofovir is not recommended to be used concomitantly with nephrotoxic drugs or after the recent use of such drugs.

    The safety and effectiveness of the use of tenofovir in patients with creatinine clearance from 30 to 49 ml / min are not determined, therefore, the ratio of the potential benefit of taking the drug and the possible risk of toxic effects on the kidneys should be evaluated. If nevertheless there is a necessity of appointment of tenofovir,then correction of the intervals between doses is required. Such patients should be closely monitored for the function of the kidneys.

    Undesirable reactions listed in the section "Side effect", presented above, can arise from renal tubulopathy of the proximal type: rhabdomyolysis, osteomalacia (manifested by bone pain, occasionally leads to fractures), hypokalemia, muscle weakness, myopathy, hypophosphatemia. It is believed that the cause of the development of these phenomena is not associated with therapy with tenofovir in the absence of renal tubulopathy of the proximal type.

    Patients infected with both HIV and hepatitis B virus g and C The risk of hepatotoxic effect of antiretroviral drugs in patients with co-infected HIV infection and the hepatitis B or C virus is higher than in the presence of only HIV infection. Therefore, patients with chronic hepatitis B or C who simultaneously take antiretroviral drugs are at increased risk of adverse effects on the liver with possible fatal outcome. These patients should be carefully monitored, both clinically and laboratory.

    In patients infected with both HIV and hepatitis B virus, severe exacerbations of hepatitis may occur after discontinuation of therapy with tenofovir. In some cases, it may be necessary to resume therapy for viral hepatitis. In patients with severe liver disease (cirrhosis), it is not recommended to discontinue treatment, since the aggravation of hepatitis that occurs after the abolition of therapy can lead to decompensation of liver function. Patients infected with HIV and hepatitis B virus should be closely monitored, both clinically and laboratory, for at least 6 months after stopping therapy with tenofovir. It is recommended that all HIV-infected patients be tested for the presence of viral hepatitis B before initiating antiretroviral therapy.

    Caution should be exercised when assigning nucleotide and nucleoside analogues to patients with concomitant hepatitis C who receive interferon alfa and ribavirin in connection with the high risk of lactate-acidosis. Such patients should undergo thorough clinical and laboratory monitoring.

    Diseases of the liver

    Hepatotoxic reactions occur at different times against combined antiretroviral therapy. The risk of developing hepatotoxicity with combined antiretroviral therapy is higher in patients with underlying liver function impairment. For patients with liver disease receiving tenofovir in combination antiretroviral therapy, careful monitoring should be conducted; if signs of impaired liver function appear, consideration should be given to the possibility of interrupting or canceling therapy.

    Triple therapy with nucleosides

    A decrease in the frequency of the virologic response in the administration of triple therapy with nucleosides was reportedtenofovir in combination with abacavir and lamivudine), as well as the development of resistance at an early stage of using this combination when taking medications once a day.

    Lipodystrophy

    In patients receiving antiretroviral therapy, there was a redistribution / accumulation of fatty tissue, including obesity of the central type, an increase in adipose tissue in the dorso-cervical region ("buffalo buffalo"), a reduction in the volume of peripheral adipose tissue, a reduction in subcutaneous fat in the face, mammary hypertrophy and "Cushingoid appearance."The mechanism of development and the long-term effects of these effects are currently unknown, their cause-and-effect relationship with the use of certain drugs has not been established. Effect on the bone system

    In animals, after administration of tenofovir, toxic effects on bone tissue were observed, including a reduction in bone mineral density. However, in the clinical study of long-term use of the drug (more than 3 years), there were no clinically significant pathological changes in bone tissue. Nevertheless, pathological changes in bone tissue (occasionally leading to fractures) can be observed with renal tubulopathy of the proximal type (see section "Side effect"). If there is a suspicion of disturbances from the bone system, an appropriate examination should be carried out.

    Early virological inefficiency

    In clinical studies involving HIV-infected patients, it has been shown that a number of therapeutic regimens involving only three nucleoside reverse transcriptase inhibitors are generally less effective than triple regimes involving the use of two nucleoside inhibitors reverse transcriptase in combination with either a non-nucleoside reverse-inhibitor transcriptase, or with an HIV-1 protease inhibitor. In particular, it was reported about early virological inefficiency and high incidence of mutations (by type of replacement), causing the development of resistance. On this basis, regimes involving the use of three nucleoside reverse transcriptase inhibitors should be used with caution. For patients whose treatment regimens involve the use of only three nucleoside reverse transcriptase inhibitors, careful monitoring should be conducted; in such cases, it is also recommended to consider the possibility of changing the treatment regimen.

    Immunodeficiency Syndrome

    In HIV-infected patients receiving combined antiretroviral therapy, the immune reconstitution syndrome was observed. In patients with severe immunodeficiency, an inflammatory response may occur in response to asymptomatic or residual opportunistic infections, which can lead to the development of serious clinical conditions or increased symptom severity.Such reactions are usually observed in the first few weeks or months of antiretroviral therapy. Examples are cytomegalovirus retinitis, generalized and / or focal mycobacterial infection and pneumonia caused by Pneumocystis jirovecii. Any symptomatology of an inflammatory nature requires an appropriate evaluation and, if necessary, the initiation of treatment. Patients should be under close clinical supervision of specialists with experience in the treatment of patients with HIV disease. Autoimmune diseases (such as Graves' disease, polymyositis and Guillain-Barre syndrome) were observed against the background of restoration of immunity, but the time of primary manifestations varied, and the disease could occur many months after the initiation of therapy and have an atypical course.

    Effect on the ability to drive transp. cf. and fur:

    No special studies have been conducted to study the effect of tenofovir disoproxil fumarate on the ability to drive and work with machinery. Patients should be informed of the possible dizziness in the treatment of the drug.

    Patients receiving tenofovir, it is necessary to observe precautions, or to avoid driving and other potentially hazardous activities requiring increased attention and speed of psychomotor reactions, taking into account the profile of side effects.

    Form release / dosage:

    Film-coated tablets, 150 mg and 300 mg Primary packaging of medicinal product.

    For 10 tablets, coated with a film sheath, into a contoured cell packaging made of a polyvinylchloride film and aluminum foil printed lacquered.

    For 30, 60, 100, 500 or 1000 tablets, film-coated in a polymer can with a lid pulled with the control of the first opening. Free space is filled with cotton wool. Labels are applied to cans from paper label or writing paper, or from polymer materials, self-adhesive.

    Secondary packaging of medicinal product.

    For 3, 6 or 10 contour mesh packages together with the instructions for use are placed in a pack of cardboard for consumer packaging subgroups chrome or chrome - ersatz or other similar quality. The packets are placed in a shipping container.

    One bank along with instructions for use is placed in a pack of cardboard for consumer packaging subgroups chrome or chrome - ersatz or other similar quality. The packets are placed in a shipping container.

    Packaging:(10) - packings cellular planimetric (10) - packs cardboard
    (10) - packings, cellular, outline (3) - packs, cardboard
    (10) - packings, cell planimetric (6) - packs cardboard
    (100) - polymer cans (1) - packs of cardboard
    (1000) - polymer cans (1) - packs of cardboard
    (30) - polymer cans (1) - packs of cardboard
    (500) - polymer cans (1) - packs of cardboard
    (60) - polymer cans (1) - packs cardboard
    Storage conditions:

    In the original packaging of the manufacturer 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 indicated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-002419
    Date of registration:03.04.2014
    The owner of the registration certificate:FARMASINTEZ, JSC (Irkutsk) FARMASINTEZ, JSC (Irkutsk) Russia
    Manufacturer: & nbsp
    Information update date: & nbsp17.09.2015
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