Active substanceZidovudineZidovudine
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  • Dosage form: & nbspcapsules
    Composition:

    Composition per one capsule:

    Active substance

    Zidovudine 100 mg

    Excipients

    Corn starch 82.8 mg

    Microcrystalline cellulose 34.5 mg

    Sodium carboxymethyl starch 11.5 mg

    Magnesium stearate 1.2 mg

    Capsule shell

    Hard gelatin capsule number 1 [body: titanium dioxide - 1%, iron dye 80.0 mg, oxide yellow - 0.192%, gelatin - up to 100%; lid: ferric oxide black oxide - 0.53%, iron dye oxide red 0.93%, iron dye oxide yellow 0.2%, titanium dioxide 0.3333%, gelatin 100%]

    Description:

    Hard gelatin capsules No. 1 with a yellow body and a brown lid. The contents of the capsules are a white or almost white powder.

    Pharmacotherapeutic group:Antiviral [HIV] agent
    ATX: & nbsp

    J.05.A.F.01   Zidovudine

    Pharmacodynamics:

    Mechanism of action. Zidovudine is an antiviral drug, highly active in vitro in relation to retroviruses, including the human immunodeficiency virus (HIV).

    Both in infected and uninfected cells zidovudine is phosphorylated to form a monophosphate derivative. This reaction is catalyzed by cellular thymidine kinase. After this, zidovudine monophosphate is phosphorylated to diphosphate, then to triphosphate (the reactions are catalyzed by cellular thymidine kinase and nonspecific kinases, respectively). Zidovudine-triphosphate acts as an inhibitor and substrate for reverse transcriptase of the virus.Synthesis of viral DNA is blocked by the inclusion of zidovudine monophosphate in its chain, the chain is broken. The affinity of zidovudine-triphosphate for reverse transcriptase of HIV is 100 times higher than that of cellular DNA polymerase alpha.

    Clinical virology. HIV Sensitivity Assessment in vitro is not a standardized method, and the results may vary due to the nature of the technique. There are reports of a decrease in the sensitivity of HIV to zidovudine in vitro in patients with long-term zidovudine. In addition, in the early stages of HIV infection, the frequency and degree of decrease in the sensitivity of the virus in vitro significantly lower than in the late stages of the disease.

    Reducing the sensitivity of viruses and the emergence of resistant to zidovudine strains limits the use of monotherapy with zidovudine. Zidovudine, especially in combination with lamivudine, as well as didanosine or zalcitabine, significantly reduces the risk of progression of the disease and reduces lethality. The use of protease inhibitors together with zidovudine and lamivudine provides additional benefits, slowing the progression of the disease and improving survival rates, as compared to a combination of the two drugs.

    It was shown that the combination of zidovudine and lamivudine, as well as studies in vitro demonstrated that isolates of zidovudine-resistant viruses can become zidovudine-sensitive when they acquire resistance to lamivudine. Moreover, there is evidence that the combination of zidovudine and lamivudine slows the development of resistance to zidovudine in patients who have not previously received antiretroviral therapy.

    Zidovudine may act additively or synergistically with other drugs used to treat HIV (lamivudine, didanosine and interferon-alpha), inhibiting viral replication in cell culture. However, combinations of three nucleoside analogues or two nucleoside analogues and a protease inhibitor more effectively suppress the cytopathic effects of HIV-1, compared to monotherapy or a combination of the two drugs.

    Resistance to thymidine analogs (which include zidovudine) is characterized in detail and is associated with incremental accumulation of specific mutations (in 6 codons) in the HIV reverse transcriptase gene (codons 41, 67, 70, 210, 215 and 219). The viruses acquire phenotypic resistance to thymidine analogues when the mutations are combined in codons 41 and 215 or when 4 to 6 mutations are accumulated.These mutations do not cause cross-resistance to other nucleoside analogs, which allows the use of other drugs of reverse transcriptase inhibitors for further treatment of HIV infection.

    Two kinds of mutations lead to the development of multiple drug resistance. In the first case, these are mutations in codons 62, 75, 77, 116 and 151 of HIV reverse transcriptase, in the second - a mutation of T69S in combination with insertion into the position of the 6th pair of nitrogenous bases corresponding to this position. These changes lead to the development of phenotypic resistance to zidovudine, as well as to other nucleoside reverse transcriptase inhibitors. Both types of mutations leading to multiple drug resistance significantly limit the therapeutic possibilities for HIV infection.

    Pharmacokinetics:

    Adults

    Absorption. Zidovudine well absorbed in the intestine. For all studied dosages, the bioavailability of the drug is 60-70%. When taking zidovudine at a dose of 300 mg twice a day, the average values ​​of concentrations in the equilibrium state are: maximum (Css max) 8.57 (54%) μmol / L (2.29 μg / ml), the minimum (Css min) 0.08 (96%) μmol / L (0.02 μg / ml) and the area under the concentration-time curve (AUCSS) - 8.39 (40%) h * μg / ml (2.24 h * μg / ml).

    Distribution. The apparent volume of zidovudine distribution is 1.6 l / kg. Binding to plasma proteins from 34% to 38%.

    Metabolism. Elimination of zidovudine is carried out mainly in the liver due to its transformation into an inactive metabolite (conjugation into glucuronide). 5'-glucuronide of zidovudine is the main metabolite of the drug, which is determined in blood plasma and urine. In the form of 5'-glucuronide, 50-80% of the dose is excreted in the urine.

    Excretion. The renal clearance of zidovudine significantly exceeds the creatinine clearance, which indicates the significant role of tubular secretion.

    Special patient groups

    Children

    Absorption. In children older than 5-6 months, the pharmacokinetic profile of zidovudine does not differ from the pharmacokinetic profile of adults. Zidovudine is well absorbed in the intestine. For all studied dosages, the bioavailability of the drug was 60-74% (mean - 65%).

    Distribution. In children, the average ratio of zidovudine concentrations in plasma and cerebrospinal fluid 0.5-4 hours after oral administration of the drug is 0.52-0.85.

    Metabolism. The main metabolite of zidovudine - 5'-glucuronide in plasma and urine is about 50-80% of the administered dose. Eliminated by renal excretion.

    Excretion. The renal clearance of zidovudine significantly exceeds the creatinine clearance, which indicates the significant role of tubular secretion.

    Data on the pharmacokinetics of the drug in newborns and infants indicate that in neonates the decrease in zidovudine glucuronization, accompanied by increased bioavailability, decreased clearance and a longer half-life of the drug, is less pronounced than in children aged 14 days. At an older age, the pharmacokinetics of zidovudine in children does not differ from the pharmacokinetics in adults.

    Pregnancy

    In pregnant women, the accumulation of the drug is not observed, and the pharmacokinetics of zidovudine does not differ from pharmacokinetics in non-pregnant. In accordance with the passive mechanism of passing the drug through the placenta, plasma concentrations of zidovudine in newborns were equal to the concentration of the drug in the blood of mothers during labor.

    Elderly patients

    Special data on the pharmacokinetics of zidovudine in elderly patients are lacking.

    Renal insufficiency

    In severe renal failure, zidovudine clearance after oral administration is 50% of clearance in individuals with normal renal function. The effectiveness of hemodialysis and peritoneal dialysis for the elimination of zidovudine is limited, but they are able to accelerate the excretion of glucuronide (zidovudine metabolite).

    Liver failure

    In patients with hepatic insufficiency, zidovudine accumulation associated with glucuronidation suppression may be observed, which may require correction of the dose of the drug.

    Indications:

    Treatment of HIV-1 infection in combination antiretroviral therapy.

    Treatment of HIV-1 infection in pregnant women to reduce the incidence of transplacental HIV transmission from mother to fetus.

    Contraindications:

    Hypersensitivity to the zidovudine itself or any other components of the drug; severe neutropenia / leukopenia (neutrophil count below 0.75 x 109/ l) or anemia (hemoglobin below 75 g / l or below 4.65 mmol / l); Children under 3 years old (for this dosage form).

    Carefully:

    Inhibition of bone marrow hematopoiesis, a deficiency of cyanocobalamin or folic acid,old age (over 65 years), hepatic insufficiency, obesity, hepatomegaly, hepatitis, or any risk factors for liver disease, neutropenia / leukopenia (neutrophil count 0.75-1.0 x 109/ l), anemia (hemoglobin 75-90 g / l).

    Pregnancy and lactation:

    Pregnancy

    Zidovudine penetrates the placenta. The drug can be used during pregnancy before 14 weeks, only if the potential benefit to the mother exceeds the possible risk to the fetus. The use of zidovudine after 14 weeks of pregnancy and its subsequent use in neonates leads to a decrease in the frequency of HIV transmission from mother to the fetus. The long-term effects of zidovudine in children who received it in the prenatal or neonatal periods are unknown.

    It is impossible to completely exclude the possibility of carcinogenic effects. There have been reports of a slight transient increase in serum lactate concentration, which may be due to mitochondrial dysfunction in newborns and infants exposed to nucleoside reverse transcriptase inhibitors (NRTIs) during the intrauterine or perinatal period.The clinical significance of the transient increase in serum lactate concentration is unknown. There are very rare reports of cases of developmental delay, convulsive seizures and other neurological disorders (eg, muscle tone increase). Nevertheless, a causal relationship between these phenomena and intrauterine or perinatal exposure of NRTIs has not been established. These data do not affect the current recommendations on the use of antiretroviral therapy in pregnancy to prevent the vertical pathway of HIV transmission.

    Lactation

    HIV-infected women are advised not to breast-feed to avoid HIV transmission to the child. After taking a single dose of zidovudine (200 mg), the average concentrations of zidovudine in breast milk and serum of HIV-infected women are the same, therefore, HIV-infected women should stop breastfeeding.

    Dosing and Administration:

    Inside.

    Adults and children over 12 years of age with a body weight of 30 kg and more

    The recommended dose of zidovudine in combination therapy is 600 mg per day in several doses.

    Children from 3 years to 12 years:

    Children weighing more than 21 kg, but less than 30 kg

    The recommended dose of zidovudine in combination therapy is 200 mg (two 100 mg capsules) in the morning and 200 mg (two 100 mg capsules) in the evening.

    Children with a body weight of at least 14 kg and up to 21 kg

    The recommended dose of zidovudine in combination therapy is 100 mg (one 100 mg capsule) in the morning and 200 mg (two 100 mg capsules) in the evening.

    Children with a body weight of at least 8 kg and up to 14 kg

    The recommended dose of zidovudine is 100 mg (one 100 mg capsule) in the morning and 100 mg (one 100 mg capsule) in the evening.

    Weight bodies (kg)

    Morning

    Evening

    Daily dose (mg)

    8-13

    one capsule for 100 mg

    one capsule for 100 mg

    200

    14-21

    one capsule for 100 mg

    two capsules of 100 mg each

    300

    22-30

    two capsules of 100 mg each

    two capsules of 100 mg each

    400


    Children with a body weight of less than 8 kg, as well as children unable to swallow capsules (regardless of body weight), it is recommended to use other dosage forms of zidovudine for oral use.

    Prevention of mother-to-child transmission of HIV

    Zidovudine is given to pregnant women after 14 weeks of gestation at a dose of 500 mg / day (100 mg five times a day). The drug is taken before the onset of labor. During childbirth, with caesarean section, as well as newborns,To prevent the vertical transmission of HIV, other dosage forms of zidovudine should be used in accordance with the recommended administration regimens.

    Correction of the dose for undesirable reactions from the blood and lymphatic system

    At a marked decrease in hemoglobin (up to 75-90 g / l (4.65-5.59 mmol / l)) or the number of neutrophils (up to 0.75-1.0x109/ l) it may be necessary to correct the dosage regimen - dose reduction or drug cancellation.

    Elderly patients

    In patients older than 65 years, the pharmacokinetics of zidovudine has not been studied, there is no relevant data. However, taking into account age-related features - a decrease in renal function, a change in blood counts - elderly patients need special control. Before starting zidovudine and during therapy, you should carefully monitor the condition of these patients.

    Renal insufficiency

    The recommended dose of zidovudine in severe renal failure (creatinine clearance <10 ml / min) and the terminal stage of renal failure (patients on hemodialysis or peritoneal dialysis) is 100 mg every 6-8 hours (300-400 mg / day). The change in blood counts and some clinical reactions may require correction of the dose of the drug.

    Liver failure

    The data obtained in patients with cirrhosis of the liver suggest that, with hepatic insufficiency, zidovudine accumulation associated with suppression of glucuronization can be observed. It may be necessary to adjust the dose of the drug, however, the exposure of zidovudine in liver failure of varying degrees (from mild to severe) varies considerably, and therefore it is difficult to provide specific recommendations for dose changes. If it is not possible to control the concentration of zidovudine in plasma, clinical signs of drug intolerance should be followed (for example, severe adverse reactions from the blood system: anemia, leukopenia, neutropenia). If necessary, reduce the dose of zidovudine and / or increase the interval between doses of the drug.

    Side effects:

    Undesirable reactions that occur in the treatment of zidovudine in children and adults coincide.

    To estimate the incidence of undesirable reactions, the following grades were used: very often (more than 10%), often (1-10%), infrequently (0.1-1%), rarely (0.01-0.1%) and very rare (less than 0.01%).

    Violations from the blood and lymphatic system: often anemia (which may require blood transfusion), neutropenia and leukopenia (the incidence of neutropenia increases in patients with which showed a decrease in the number of neutrophils, content hemoglobin and vitamin B12 in the serum at the beginning of the treatment); infrequently - pancytopenia with bone marrow hypoplasia, thrombocytopenia; rarely - true erythrocyte aplasia; very rarely - aplastic anemia.

    Disorders from the metabolism and nutrition: often - hyperlactatemia; rarely - lactic acidosis in the absence of hypoxemia, anorexia.

    Disorders of the psyche: rarely - anxiety and depression.

    Impaired nervous system: very often - headache; often - dizziness; rarely - cramps, decreased cognitive function, insomnia, paresthesia, drowsiness.

    Heart Disease: rarely - cardiomyopathy.

    Disturbances from the respiratory system, chest and mediastinal organs: infrequently - shortness of breath; rarely - a cough.

    Disorders from the gastrointestinal tract: very often - nausea; often - vomiting, diarrhea, abdominal pain; infrequently - flatulence; rarely - pancreatitis, pigmentation of the oral mucosa, taste disorders, dyspepsia.

    Disorders from the liver and bile ducts: often - an increase in hepatic enzyme activity and concentration bilirubin; rarely - liver disease, such as severe hepatomegaly in combination with steatosis.

    Disturbances from the skin and subcutaneous tissues: infrequent - rash and itching; rarely - hives, pigmentation of skin and nails, sweating.

    Disturbances from the musculoskeletal and connective tissue: often - myalgia; infrequently - myopathy.

    Disorders from the kidneys and urinary tract: rarely - frequent urination.

    Violations of the genitals and breast: rarely - gynecomastia.

    Other: often - a feeling of indisposition; infrequently - asthenia, fever, generalized pain syndrome; rarely - pain in the chest, flu-like syndrome, chills. The common unwanted reactions consistently decrease during the first few weeks of zidovudine therapy.

    Undesirable reactions that occur when zidovudine is used to prevent the transmission of HIV from mother to fetus.

    Pregnant women are well tolerated zidovudine in recommended doses. Children have a decrease in hemoglobin, which, however, does not require blood transfusions. Anemia disappears 6 weeks after the end of zidovudine therapy.

    With the use of nucleoside analogs, cases of lactic acidosis, sometimes with a lethal outcome, often accompanied by severe hepatomegaly and steatosis of the liver, have been reported.

    Highly active antiretroviral therapy (HAART) in HIV-infected patients is often accompanied by a redistribution of adipose tissue (lipodystrophy). The manifestations of lipodystrophy include a decrease in the amount of peripheral subcutaneous fat and fat in the facial area, visceral obesity, mammary gland hypertrophy and accumulation of adipose tissue in the back (in the cervical and thoracic spine, "bovine hump").

    HAART is associated with metabolic disorders such as hypertriglyceridemia, hypercholesterolemia, insulin resistance, hyperglycemia and hyperlactatemia.

    In HIV-infected patients with severe immunodeficiency, the onset of HAART can be accompanied by an inflammatory response to asymptomatic or residual opportunistic pathogens.

    There are reports of cases of osteonecrosis, especially with known risk factors (late stages of HIV infection and / or prolonged use of HAART). The frequency of this reaction is unknown.

    Overdose:

    Symptoms

    Specific symptoms and signs of acute overdose of zidovudine are absent. There are known reactions listed as side effects: fatigue, headache, vomiting, in a number of cases, violations on the part of the blood system. There is one report of an overdose of an unknown amount of zidovudine; according to serum concentrations, the dose of the drug was more than 17 g. No clinical, biochemical or hematological short-term effects were observed.

    Treatment

    Patients should be carefully monitored for signs of toxicity. If necessary, appropriate supportive therapy is prescribed.

    The effectiveness of hemodialysis and peritoneal dialysis for the elimination of zidovudine is limited, but they are able to accelerate the excretion of glucuronide (zidovudine metabolite).

    Interaction:

    The available data suggest that the joint administration of zidovudine and rifampicin leads to a decrease in AUC zidovudine (area under the pharmacokinetic curve) by 48% ± 34%. This can lead to partial or complete loss of the effectiveness of the drug. Joint use of zidovudine and rifampicin should be avoided.

    FROM ribavirin, stavudine, doxorubicin antagonism in the antiviral action of zidovudine has been established. Joint use of zidovudine and stavudine, ribavirin or doxorubicin should be avoided.

    Probenecid increases zidovudine AUC by 106% (100-170%). Patients receiving both drugs need careful monitoring of blood counts.

    The combined use of zidovudine and lamivudine results in an insignificant increase in Cmax (28%), but the total exposure (AUC) changes insignificantly. Zidovudine does not affect the pharmacokinetics of lamivudine.

    In a number of patients who took zidovudine, there was a decrease in concentration phenytoin in blood, whereas in one patient, on the contrary, there was an increase in the concentration of phenytoin. With the joint intake of these drugs should monitor the concentration of phenytoin in the blood.

    Atovahon: zidovudine does not affect the pharmacokinetics of atovahona. However, pharmacokinetic data demonstrate that atovahon reduces the rate of transformation of zidovudine to glucuronide (the zidovudine AUC in the equilibrium state is increased by 33%, the peak plasma concentration of glucuronide decreases by 19%). It is unlikely that a three-week intake of atovahona, together with zidovudine (500-600 mg / day), can increase the frequency of unwanted reactions associated with an increase in plasma concentrations of the latter. Nevertheless, it is necessary to monitor the status of patients receiving atovahona together with zidovudine.

    Simultaneous reception with other drugs containing zidovudine. Zidovudine should not be prescribed with other medications containing zidovudine.

    Joint use of zidovudine and valproic acid, fluconazole or methadone leads to an increase in zidovudine AUC and a corresponding decrease in its clearance. When co-administration of zidovudine and valproic acid, fluconazole or methadone, patients should be carefully monitored to avoid toxic effects associated with zidovudine.

    The use of zidovudine in combination HIV therapy can exacerbate anemia associated with admission ribavirin, but the mechanisms of this phenomenon are not clear. Due to the increased risk of anemia, the concomitant use of ribavirin and zidovudine is not recommended. If the patient is already receiving zidovudine in the HAART, should consider the possibility of replacing it with another drug. This is especially important if there is an anemia in the history of an anemia caused by taking zidovudine.

    Concomitant therapy (especially urgent) with potentially nephrotoxic or myelosuppressive drugs (eg, systemic pentamidine, dapsone, pyrimethamine, colomoxazole, amphotericin B, flucytosine, ganciclovir, interferon alfa, vincristine, vinblastine and doxorubicin) may increase the risk of adverse reactions associated with zidovudine. If concomitant therapy with any of these drugs is necessary, the patient's condition (especially kidney function and blood counts) should be carefully monitored and, if necessary, the dosage of one or more drugs should be reduced.

    There is no significant increase in the risk of adverse reactions associated with zidovudine if co-trimoxazole, pentamidine (in the form of an aerosol), pyrimethamine and acyclovir used in preventive dosages.

    Clarithromycin (tablet form) reduces the absorption of zidovudine. A two-hour or longer interval between doses of zidovudine and clarithromycin avoids this reaction.

    Other: acetylsalicylic acid, codeine, methadone, morphine, indomethacin, ketoprofen, naproxen, oxazepam, lorazepam, cimetidine, clofibrate, dapsone, inosine pranobex can disrupt zidovudine metabolism by competitive inhibition of glucuronization or direct suppression of microsomal metabolism in the liver. The possibility of using these drugs in combination with zidovudine, especially with prolonged therapy, should be approached with caution.

    Special instructions:

    Patients should be informed that zidovudine does not prevent the transmission of HIV to other people during sexual intercourse or blood transfusion. Therefore, patients should take appropriate precautions.

    Zidovudine can not completely cure HIV infection or acquired immunodeficiency syndrome (AIDS). In patients receiving zidovudine or other antiretroviral drugs, opportunistic infections or other complications of HIV infection can continue to develop.

    Pregnant women considering the possibility of using zidovudine during pregnancy to prevent the transmission of HIV to their children should be informed that in some cases transmission can occur even despite treatment.

    FROM ribavirin, stavudine, doxorubicin antagonism in the antiviral action of zidovudine has been established. Joint use of zidovudine and stavudine, ribavirin or doxorubicin should be avoided.

    Joint use of zidovudine should be avoided. rifampicin.

    Violations of the blood and lymphatic system. In patients receiving zidovudine, it is possible to expect the development of anemia (most often 6 weeks after the start of zidovudine therapy, exceptions are possible), neutropenia (most often 4 weeks after the start of zidovudine therapy, exceptions are possible) and leukopenia (usually secondary, associated with neutropenia).These unwanted reactions often develop at high doses (1200-1500 mg / day) and in patients with decreased bone marrow function prior to initiation of therapy (usually in later stages of HIV infection).

    It is necessary to carefully monitor blood counts. In the late stages of HIV infection, in the presence of symptoms, during the first 3 months of therapy it is recommended that the blood test be performed at least once every 2 weeks, then every month. Depending on the general condition of the patient, blood counts can be controlled less often (for example, every 1-3 months).

    When the hemoglobin content is reduced to 75-90 g / l (4.65-5.59 mmol / l) and the neutrophil count to 0.75 x 109/ l and 1.0 x 109/ l daily dose of zidovudine can be reduced, taking a reduced dose can continue until the recovery of blood values. An alternative option to restore blood counts is a short-term withdrawal of the drug (for 2-4 weeks). Recovery of blood counts usually occurs after 2 weeks, after which the therapy with zidovudine (in a smaller dose) can be resumed. With severe anemia, dose adjustment does not always avoid blood transfusion.

    Lactic acidosis. Lactic acidosis, observed with the use of nucleoside analogs, is usually associated with hepatomegaly and hepatic steatosis. Early symptoms of lactic acidosis include dyspeptic manifestations (nausea, vomiting and abdominal pain), a feeling of malaise, decreased appetite, weight loss, respiratory symptoms (rapid and / or deep breathing) or neurological symptoms (including muscle weakness). Lactic acidosis is a condition with high mortality and can be associated with pancreatitis, hepatic or renal insufficiency. Lactic acidosis is usually observed after several months of taking the drug.

    Hyperlactatemia is accompanied by symptoms: metabolic lactic acidosis, progressive hepatomegaly, rapid increase in transaminase activity. Hyperlactatemia is an indication for the cancellation of nucleoside analogues.

    Caution should be exercised when assigning nucleoside analogs to patients with hepatomegaly (especially women who are obese), hepatitis or other known risk factors for liver disease and steatosis of the liver (including a number of medications and alcohol abuse).Patients infected with the hepatitis C virus and taking interferon-alpha and ribavirin, have a particularly high risk.

    Patients with a high risk of lactic acidosis should be monitored more carefully.

    Mitochondrial toxicity. Analogues of nucleosides and nucleotides can cause mitochondrial toxicity of varying severity. Mitochondrial dysfunction is observed in HIV-negative neonates exposed to nucleoside analogs in the prenatal and / or postnatal period. The main undesirable phenomena include hematologic (anemia, neutropenia) and metabolic disorders (hyperlactatemia, hyperlipazemia); they are often transient. There are also reports of delayed reactions from the nervous system (hypertonic muscle, seizures, pathological behavior), the degree of reversibility of which is unknown. Every child who has been exposed to nucleoside analogues in the prenatal period needs to monitor clinical and laboratory indicators regardless of HIV status.When the corresponding symptoms appear, a complete examination is shown to exclude possible mitochondrial dysfunction. Data on mitochondrial dysfunction do not affect current recommendations on the use of antiretroviral therapy in pregnant women (prevention of the vertical pathway of HIV transmission).

    Lipodystrophy. Combined antiretroviral therapy in HIV-infected patients is often accompanied by a redistribution of adipose tissue (lipodystrophy). The long-term consequences of this phenomenon are currently unclear, the data on the mechanism of its occurrence are limited. It is assumed that the reception of protease inhibitors is associated with visceral lipomatosis, and the reception of nucleoside reverse transcriptase inhibitors with lipoatrophy. The factors that increase the risk of lipoatrophy are elderly age (individual factor), as well as long-term antiretroviral therapy and associated metabolic changes (drug factors). At physical examination it is necessary to pay attention to signs of redistribution of adipose tissue. It is also necessary to monitor the concentration of lipids and glucose in the blood (fasting).Therapy of lipid metabolism disorders is carried out in accordance with the clinical picture.

    Myopathy. Myopathy and myositis with pathological changes characteristic of the course of HIV infection were associated with prolonged use of zidovudine.

    Diseases of the liverneither. The data obtained in patients with cirrhosis of the liver suggest that, with hepatic insufficiency, zidovudine accumulation associated with suppression of glucuronization can be observed. It may be necessary to adjust the dose of the drug, however, the exposure of zidovudine in liver failure of varying degrees (from mild to severe) varies considerably, and therefore it is difficult to provide specific recommendations for dose changes. If it is not possible to control the concentration of zidovudine in plasma, clinical signs of drug intolerance should be followed (for example, severe adverse reactions from the blood system: anemia, leukopenia, neutropenia). If necessary, reduce the dose of zidovudine and / or increase the interval between doses of the drug.

    Patients,suffering from chronic hepatitis B or C and receiving combination antiretroviral therapy, have an increased risk of severe unwanted liver reactions, which can also lead to death. When appointing patients with hepatitis B or C, combined antiretroviral therapy, you should carefully read information about all the medications that the patient will receive.

    Presence of previous liver diseases (including chronic active hepatitis) increases the risk of liver dysfunction during combined antiretroviral therapy, the condition of such patients should be monitored in accordance with clinical practice standards. In case of aggravation of liver disease, it is necessary to reduce the dose of the drug or interrupt its reception.

    Syndrome of restoration of immunity. In HIV-infected patients with severe immunodeficiency, the onset of HAART can be accompanied by an inflammatory response to asymptomatic or residual opportunistic pathogens. This reaction can lead to the development of severe clinical manifestations or aggravate existing symptoms.Usually, similar reactions are observed during the first weeks or months after the onset of HAART. Examples include cytomegalovirus retinitis, generalized and / or local mycobacterial infections and pneumocystis pneumonia. It is necessary to control the symptoms of inflammation and, if necessary, prescribe appropriate therapy. There may be autoimmune diseases (such as Graves' disease, polymyositis and Guillain-Barre syndrome) on the background of restoration of immunity, but the time of primary manifestations varies, and the disease can occur many months after the initiation of therapy and have an atypical course.

    Osteonecrosis. Although the etiology of bone necrosis is considered multifactorial (including the use of corticosteroids, alcohol abuse, severe immunosuppression, high body mass index), cases of osteonecrosis are mainly observed in the late stages of HIV infection and / or with prolonged use of HAART. Patients should be warned that discomfort and pain in the joints, a feeling of stiffness and difficulty of movement require a doctor's advice.

    Co-infection with the hepatitis C virus. Joint reception of ribavirin and zidovudine is not recommended in connection with an increased risk of anemia. Patients should be warned that taking any other medications without prescribing a doctor is undesirable.

    In patients infected with HIV and hepatitis C virus and receiving combined antiretroviral therapy for HIV and interferon alfa in combination with ribavirin or without it, hepatic insufficiency (sometimes with lethal outcome) was observed. It is necessary to ensure that patients receiving interferon alfa with or without ribavirin, and zidovudine, in order to identify the toxic effects associated with treatment, especially the development of hepatic insufficiency, neutropenia and anemia. In such cases, discontinuation of zidovudine should be considered. It should also consider a dose reduction or discontinuation of interferon alpha, ribavirin, or both drugs in the event the clinical signs of toxicity, including hepatic failure (e.g., more than 6 points according to Child-Pugh classification) (see.instructions for the use of interferon alfa and ribavirin).

    It is necessary to change the regimen of antiretroviral therapy, using a scheme that does not contain zidovudine, especially in patients with a history of zidovudine-induced anemia.

    Simultaneous reception with other drugs containing zidovudine. Zidovudine should not be prescribed with other medications containing zidovudine.

    In patients receiving zidovudine as part of combined antiviral therapy, there may be a syndrome of immune reconstitution, which may require medical intervention.

    Estimating the tolerability of the drug, it should be borne in mind that skin rash, dizziness, weakness, headache, anorexia, diarrhea, myalgia, anemia, thrombocytopenia can be a manifestation of HIV infection itself and secondary diseases associated with it, rather than the toxic effect of zidovudine.

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

    Studies to study the effect of zidovudine on the ability to drive a car or work with mechanisms have not been conducted. Pharmacodynamic properties of the drug do not allow to assume the presence of a similar effect.Nevertheless, when assessing a patient's ability to drive or work with machinery, the general condition of the patient and the nature of the adverse reactions should be considered.

    Form release / dosage:Capsules 100 mg.
    Packaging:

    10 capsules per contour cell packaging made of polyvinylchloride film and aluminum foil printed lacquered.

    By 10, 20 or 100 capsules in a jar (bottle) polymer for medicines or in a jar (bottle) for medicines made of plastic. Free space in the jar (vial) is filled with cotton wool with medical hygroscopic or sterile cotton ball medical.

    Each jar (bottle), 1, 2 or 10 contour mesh packages together with the instruction for use is placed in a pack of cardboard box.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002398
    Date of registration:13.03.2014
    Expiration Date:13.03.2019
    The owner of the registration certificate:TECHNOLOGY OF DRUGS, LTD. TECHNOLOGY OF DRUGS, LTD. Russia
    Manufacturer: & nbsp
    Information update date: & nbsp13.10.2017
    Illustrated instructions
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