Active substanceStavudineStavudine
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  • Dosage form: & nbspcapsules
    Composition:

    Capsules 30 mg
    Each capsule contains:
    Active substance: Stavudine 30 mg. Auxiliary components: cellulose microcrystalline 56.4 mg, lactose monohydrate 178.68 mg, sodium carboxymethyl starch 14.1 mg, magnesium stearate 2.82 mg.
    Capsule shell: gelatin to 100%, titanium dioxide 1.9829%, sodium lauryl ether sulfate 0.08%.
    Ink for printing blue TEK 6018 (Shellac NF 22-27%, alcohol anhydrous * USP 33-38%, isopropanol * USP 0.5-4%, butanol * No. 4-8, propylene glycol USP 3- 6%, strong ammonia solution NF 1-2% lacquer aluminum blue 24-28%) - qs Inks for printing black TEK 9008 (shellac NF 24-27%, alcohol anhydrous * USP 23-26%, isopropanol * USP 1-3%, butanol * NF 1-3%, propylene glycol USP 3-7%, strong solution of ammonia NF 1-2%, color iron oxide black NF 24-28%, potassium hydroxide NF 0.05-0.1%, purified water * USP 15-18%) - qs
    * Removed during production.

    Capsules 40 mg

    Each capsule contains:
    Active substance: Stavudine 40 mg.
    Auxiliary components:
    cellulose microcrystalline 75.2 mg, lactose monohydrate 238,24 mg, sodium carboxymethyl starch 18.8 mg, magnesium stearate 3.76 mg.
    Capsule shell: gelatin to 100%, titanium dioxide 1.9829%, sodium lauryl sulfate 0.08%.
    Inks for printing red TEK SB1018 (shellac NF 22-27%, alcohol anhydrous * USP 13-17%, isopropanol * USP 18-24%, butanol * NF 6-11%, propylene glycol USP 2-5%, sodium hydroxide NF 0.05-0.1 %, titanium dioxide USP 2-5%, povidone USP 8-12%, lacquer aluminum red 19-24%) - qs
    Inks for printing black TEK 9008 (shellac NF 24-27%, alcohol anhydrous * USP 23-26%, isopropanol * USP 1-3%, butanol * NF 1-3%, propylene glycol USP 3-7%, strong solution of ammonia NF 1-2%, color iron oxide black NF 24-28%, potassium hydroxide NF 0.05-0.1%, purified water * USP 15-18%) - qs
    * Removed during production.

    Description:
    Capsules 30 mg
    Hard gelatin capsules in size "2", from white to pale pink, opaque, with body and lid, printed with blue ink "RA" on the lid and black ink "22" on the case, the contents of the capsules - white or almost white powder.
    Capsules 40 mg
    Hard gelatin capsules the size of "1", from white to pale pink, opaque, with a body and lid,with a red "RA" ink stamp on the lid and black ink "23" on the case, the contents of the capsules are white or almost white powder.
    Pharmacotherapeutic group:Antiviral [HIV] agent
    ATX: & nbsp

    J.05.A.F   Nucleosides - reverse transcriptase inhibitors

    J.05.A.F.04   Stavudine

    Pharmacodynamics:

    Stavudine is a synthetic analogue of thymidine nucleoside, suppresses replication of HIV in cultured human cells and in cell lines in vitro. After entering the cage stavudine under the action of cellular enzymes is converted into an active metabolite of stavudine triphosphate, which suppresses the activity of HIV reverse transcriptase due to competition with the natural substrate of dioxytimidine triphosphate and disrupts the replication of HIV. Stavudine triphosphate also enhances the termination of viral DIC chains due to the absence of 3'-hydroxyl groups in the molecule, necessary for the construction of DNA. Besides. Stavudine triphosphate inhibits cellular DNA polymerases β and γ and markedly reduces the synthesis of mitochondrial DNA.

    A study of the inhibitory activity of stavudine in combination with zidovudine in vitro showed that both drugs are phosphorylated by cellular thymidine kinase. Moreover, the conversion of zidovudia into an active form occurs faster, slowing the activity of stavudine.Considering this. combined treatment with these drugs is not recommended. According to research in vitro, phosphorylation of stavudine also slows down in the presence of doxorubicin and ribavirin. The sensitivity to stavudine was observed in the culture of cells isolated from patients who received stavudine. A decrease in sensitivity to stavudine after a prolonged course of treatment has been identified; several cases of multiple resistance to nucleoside analogues have been found. There have also been cases of cross-resistance to reverse transcriptase inhibitors. So, long-term treatment with stavudine can induce or maintain resistance to zidovudine. In the presence of mutations of the HIV-1 gene (especially M41L and T215Y) as a result of the treatment with nucleoside analogs, stavudine is not recommended.

    Mutations of resistance to thymidine analogs in antiviral therapy are observed equally often with stavudine and zidovudia. The activity of stavudine decreases with a mutation that causes multiple drug resistance - Q151M.

    A mutation of resistance K65R in patients receiving stavudine / didanosine or stavudine / lamivudine, but not in patients receiving stavudine in the form of monotherapy.

    Pharmacokinetics:
    Adults.
    Stavudine is rapidly absorbed when taken orally. Absolute bioavailability is about 86.4%. After a single dose, the maximum concentration of the drug (Cmax) in the blood plasma is observed in less than 1 hour. The values ​​(Cmax) increase in proportion to the increase in the doses of the drug. Cumulation of stavudine in its application every 6, 8 or 12 hours was not observed.
    The pharmacokinetics of stavudine in patients with HIV without clinical manifestations taking the drug after or during a meal with a high fat content or fasting did not change noticeably.
    Apparent volume of distribution after a single dose of the drug is an average of 66 liters and does not depend on the dose. The drug is equally distributed between red and white blood cells. Binding to blood proteins is negligible. After a single oral dose of 40 mg, the concentration in the cerebrospinal fluid (CSF) of healthy volunteers was 63 ng / ml (average 44-71ng / ml) for 4-5 hours. The ratio of CSF to plasma concentration was about 40% (mean 31-45%).
    Metabolism of stavudine in the human body remains unexplored.
    After oral administration, the half-life of the drug is 1.44 hours and is dose independent.
    Renal clearance was 40% of the total clearance, and almost twice the endogenous creatinine clearance, which indicates the active tubular secretion in deriving stavudine through the kidneys along with glomerular filtration. Children. Absolute bioavailability of the drug in children is an average of 76.9%. The pharmacokinetics after a single dose of the drug is similar to the pharmacokinetics of adults and is independent of dose. Drug concentration in CSF after single and repeated oral administration comprise from 16 to 125% relative to concentration in plasma. Cumulation of stavudine with a dose of 0.125-2 mg / kg every 12 hours is not observed. Half-life is an average of 1 hour. About 34.5% of the drug is excreted through the kidneys unchanged.
    Elderly patients.
    Pharmacokinetics in patients older than 65 years has not been studied.
    Impaired renal function.
    With dysfunction of the kidneys, the clearance of stavudine is reduced.
    A dose adjustment is recommended (see Dosage and Administration).
    Violation of the function of the liver.
    Pharmacokinetics of the drug has a similarity in patients with impaired and normal liver function.Patients with impaired liver function in a stable state are not required to adjust the initial dose of the drug.
    Indications:
    Treatment of HIV infection (in combination with other nucleoside and non-nucleoside reverse transcriptase inhibitors and protease inhibitors).
    Contraindications:
    Hypersensitivity to stavudine and / or any of the excipients of the drug, children with a body weight of less than 30 kg, chronic renal failure (CRF) with creatinine clearance less than 50 ml / min. Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.
    Carefully:Alcoholism, chronic renal failure, hepatic insufficiency, peripheral neuropathy, application in combination with didanosine, pancreatitis.
    Pregnancy and lactation:
    To apply Woodistry during pregnancy should only be in the presence of strict indications and only in those cases when the potential benefit of treatment for the mother outweighs the possible risk to the fetus. Studies in animals have shown that stavudine and / or its metabolites pass through the placenta. It is not known whether the drug passes into breast milk.During treatment with the drug, breast-feeding should not be.
    Dosing and Administration:
    Inside. The time of taking the drug does not depend on the time of eating. The dose of the drug depends on the body weight.
    Adults and children with a body weight of at least 30 kg

    Body mass

    Doses

    ≥60 kg

    40 mg every 12 hours

    ≥30 kg <60 kg

    30 mg every 12 hours

    If swallowing capsules is difficult, you should gently open the capsule and take the contents with a small amount of food.
    Adults with impaired renal function are recommended to reduce the dose depending on the creatinine clearance:

    Creatinine clearance (ml / min)

    Dosage according to body weight


    ≥60 kg

    <60 kg

    >50*

    40 mg every 12 hours

    30 mg every 12 hours

    * Usual dose, dose adjustment is not required.

    Children with impaired renal function. Precise recommendations for adjusting the dose of the drug in children are absent. It is possible to reduce the dose and / or increase the interval between doses of the drug.

    Side effects:

    The frequency of adverse reactions was determined in accordance with the WHO classification (World Health Organization): very often (1/10), often (≥1 / 100 and <1/10), infrequently (≥1 / 1000 and <1/100), rarely (≥1 / 10000 and <1/1000), very rarely (<1/10000), the frequency is unknown (the frequency can not be estimated from available data, including individual messages).

    Violations of the side of the blood and lymphatic system: rarely - anemia, very rarely - neutropenia, thrombocytopenia.

    Endocrine disorders: infrequently - gynecomastia.

    Metabolic and nutritional disorders: often - lipoatrophy, lipodystrophy, asymptomatic hyperlactatemia, infrequently - lactic acidosis, anorexia, rarely - hyperglycemia, very rarely - diabetes mellitus.

    Mental disorders: often - depression, infrequently - anxiety, emotional lability.

    Impaired nervous system: often - peripheral neuropathy, paresthesia, peripheral neuritis, dizziness, abnormal dreams, headache, insomnia, drowsiness, frequency is unknown - pathological thinking.

    Disorders from the gastrointestinal tract: often - diarrhea, abdominal pain, nausea, dyspepsia, infrequently - pancreatitis, vomiting, frequency unknown - dry mouth.

    Disorders from the hepatobiliary system: infrequently - hepatitis, jaundice,

    a violation of liver function, rarely - steatosis of the liver, very rarely - liver failure, the frequency is unknown increase in the activity of "liver" transaminases, hyperbilirubinemia.

    Disturbances from the skin and subcutaneous tissues: often - a rash, itching, infrequently -hives.

    Disturbances from the musculoskeletal system and connective tissue: infrequently - arthralgia, myalgiaI.

    General disorders: often - fatigue, infrequently - asthenia, frequency unknown - chills, fever, increased lipase activity.

    When used in combination with other drugs with similar toxicity, the risk of side effects increases.

    Combined antiretroviral therapy has been associated with metabolic disorders, such as hypertriglyceridemia, hypercholesterolemia, insulin resistance. hyperglycemia and hyperlactatemia.

    Peripheral Neuropathy is an severe and dose-dependent side effect of the drug. The risk of developing this effect increases with osimultaneous application with didanosine. Peripheral neuropathy is usually accompanied by a bilateral symmetrical sense of numbness in the limbs: tingling and pain in the soles of the feet and less in the hands. In clinical trials, the frequency of these reactions depended on the dose and / or stage of the disease. In the early stages of the disease, these phenomena are less frequent. Pancreatitis varying degrees of severity, including death, can develop in the patient at different stages of treatment and does not depend on whether the drug is administered as monotherapy or in combination with other drugs, or on the degree of immunosuppression. When using the drug in combination with didanosine or other drugs that have a toxic effect on the pancreas, the risk of developing pancreatitis increases.

    Steatosis. Severe forms of steatosis with hepatomegaly, including death, are noted when nucleoside analogues are used in monotherapy or in combination with other antiviral drugs, including stavudine. With the use of stavudine in combination with didanosine, the risk of liver dysfunction significantly increases. Nausea, vomiting, pain in the abdominal region, rapid breathing or shortness of breath, or muscle weakness may indicate the development of lactic acidosis.

    Redistribution of fatty tissue. In patients receiving antiretroviral therapy, there were cases of redistribution / accumulation of fatty tissue (lipodystrophy / lipoatrophy), which manifested itself as obese by the central type,an increase in the amount of fat in the dorsocervical zone, a decrease in the amount of fatty tissue in the limbs and face, an increase in the breast, and a "cushingoid face." In randomized comparative clinical trials, it was found that in patients who had not previouslyrimretroviral therapy, lipodystrophy / lipoatrophy are more common in stavudine than with other nucleoside analogues (tenofovir or abacavir).

    Muscle weakness. In rare cases, the treatment with stavudine develops muscle weakness. Its symptoms may be similar to the clinical signs of Guillain-Barre syndrome (including respiratory failure). Symptoms may persist or worsen after discontinuation of therapy.

    Osteonecrosis. Cases of osteonecrosis were noted in patients taking stavudine, especially with prolonged treatment with antiretroviral drugs. An important role in the etiology of osteonecrosis is played by such factors as treatment with glucocorticosteroids, alcohol abuse, severe immunosuppression, obesity.

    Children. In clinical trials, the side effects of the drug in children and adults patients did not differ. The development of peripheral neuropathy in children was less common than in adults. However, the symptoms of peripheral neuropathy in children were more difficult to identify.

    In conditions in vitro and in vivo the ability of nucleotide and nucleoside analogues to cause damage to mitochondria is revealed. Mitochondrial dysfunction was reported in HIV-negative children exposed to nucleoside analogues during the antenatal period or immediately after birth. The main manifestations of mitochondrial dysfunction, often transient, were anemia, neutropenia, hyperlactatemia and hyperlipazemia.

    There were also later manifestations of this disorder: hypertonus of the muscles, convulsions, anomalies of behavior.

    Immunodeficiency Syndrome

    In HIV-infected patients with severe immunodeficiency after onset combination antiretroviral therapy may occur asymptomatic opportunistic infections or their residual manifestations. Also reported were autoimmune disorders, such as Graves' disease, polymyositis, and Guillain-Barre syndrome. The time of occurrence is very variable and may be several months fromtreatment.

    Overdose:
    Peripheral neuropathy and impaired liver function. Treatment: symptomatic. Stavudine is removed during hemodialysis (the rate of excretion is 120 ± 18 ml / min). Peritoneal dialysis is not effective.
    Interaction:
    Woodustasis is not recommended to be applied simultaneously with the drug zidovudine. The conversion of stavudine into an active metabolite decreases in the presence of zidovudine. Simultaneously accepted didanosine, lamivudine or nelfinavir Woodstar does not affect the effectiveness of the drug. The risk of developing side effects of the drug Woodistas increases with simultaneous with didanosine.
    Stavudine almost does not bind to blood proteins, which indicates a low probability of drug interactions involving the mechanism of displacement from the binding sites. It is not recommended concomitant use of drugs that cause peripheral neurological disorders (chloramphenicol, cisplatin, dapsone, ethambutol, ethionamide, hydralazine, isoniazid, lithium, metronidazole, nitrofurantoin, phenytoin, vincristine, zalcitabine).
    Special instructions:

    Despite the effectiveness antiretroviral therapy, it is impossible to exclude the risk of transmission of the virus during sexual intercourse to the end. Standard precautions against transmission of infection should be observed.

    Peripheral neuropathy. The drug should be used with caution in patients with an increased risk of peripheral neuropathy, with progressive HIV infection, with a history of peripheral neuropathy, and when used in combination with didanosine. Feeling numbness, tingling, or pain in the extremities can indicate the development of peripheral neuropathy, which can disappear immediately after discontinuation of the drug. If these symptoms occur, you should temporarily stop treatment with the drug. Resumption of treatment with the drug can only be after complete disappearance of symptoms. Can It is necessary to reduce the dose to half the recommended dose.

    Pancreatitis. The drug should be used with caution in patients with an increased risk of developing pancreatitis with progressive HIV infection simultaneous application with didanosine. When symptoms of pancreatitis appear, treatment with the drug should be stopped, with repeated treatment with the drug, the simultaneous use of didanosine and hydroxycarbamide should be avoided.For the purpose of early detection of the development of pancreatitis, it is often necessary to check the function of the pancreas glands.

    Lipodystrophy. During the therapy, a permanent medical check of the liver and kidney function is performed. The severity of lipodystrophy in patients taking stavudine, decreases when transferring them to treatment with tenofovir or abacavir; but the clinical manifestations of lipoatrophy do not decrease. In each case, the risk ratio lipodystrophy / lipoatrophy and the benefits of stavudine-containing regimens; At a high risk level, consideration should be given to the use of alternative treatment regimens. A thorough monitoring of the symptoms of lipodystrophy / lipoatrophy in all patients taking stavudine.

    Syndrome of restoration of immunity. In HIV-infected patients with severe immunodeficiency at the time of combined antiretroviral therapy, asymptomatic opportunistic infections or their residual manifestations, leading to worsening of the condition or exacerbation of symptoms. Typically, such reactions were observed during the first few weeks or months after the onset of combined antiretroviral therapy.Cytomegalovirus retinitis, generalized and / or focal mycobacterial infections and pneumocystis pneumonia are described. Any inflammatory symptoms should be evaluated and, if necessary, appropriate treatment should be applied.

    Lactic acidosis. When using reverse transcriptase inhibitors, the development of lactic acidosis accompanied by genomegaly and steatosis of the liver was reported. Early symptoms include nausea, vomiting, abdominal pain, general malaise, loss of appetite, weight loss, frequent and / or deep breathing, and neurologic symptoms (motor weakness). Lactic acidosis is often combined with pancreatitis, liver failure, renal disease insufficiency or paralysis and is life threatening condition. Lactic acidosis often develops several months after the start of treatment. When hyperlactatemia occurs. metabolic (lactate) acidosis, progressive hepatomegaly or a rapid increase in the activity of aminotripsferase treatment Woodstar should be discontinued. You must observe caution when using Woodistav in patients (especially women with obesity) with hepatomegaly.hepatitis or other risk factors for the development of steatosis of the liver (certain medications and alcohol). A special risk group is patients with hepatitis C, treated with alpha interferon and ribavirin. Patients with an increased risk of steatosis during treatment should be carefully observed.

    Patients with co-infection with hepatitis C, host α-interferon and ribavirin, can be a particular danger. Patients in the high-risk group should be closely monitored.

    Diseases of the liver. In patients receiving stavudia, as well as in patients taking antiretroviral drugs in combination with hydroxycarbamide. hepatitis and hepatic insufficiency, sometimes with a lethal outcome, were observed. When using a combination of antiretroviral drugs, as well as with the administration of stavudine, patients with liver disease should be carefully monitored by patients; If signs of worsening liver function appear, consider reversing treatment.

    Patients with chronic hepatitis B and C when treated with Woodustav, there is an increased risk of developing severe and potentially fatal adverse reactions from the liver.In such patients, careful monitoring of liver function should be performed and, if liver function worsens, interrupt or cancel treatment. In the case of a rapid increase in the activity of transaminases (a 5-fold increase in activity ACT and ALT), treatment with Woodustaw must be discontinued.

    Osteonecrosis. With prolonged use of a combination of antiretroviral drugs, patients with progressive immunodeficiency reported cases of osteonecrosis. The use of glucocorticosteroids, alcohol abuse, severe immunosuppression, obesity are factors, predisposing to the development of osteonecrosis. When there are such signs of osteonecrosis as aches and pains in joints, joint stiffness, restriction of the volume of movements in the joints, it is recommended to consult a doctor.

    Mitochondrial dysfunction. AT research in vitro and in vivo the ability of nucleotide and nucleoside analogs to cause damage to mitochondria is revealed. Mitochondrial dysfunction was reported in HIV-negative children exposed to nucleoside analogues during the antenatal period or immediately after birth.The main manifestations of mitochondrial dysfunction, often transient, were anemia, neutropenia, hyperlactatemia and hyperlipazemia. There were also later manifestations of this disorder: hypertonus of the muscles, convulsions, anomalies of behavior. It is not known whether neurological disorders are transient. After using nucleotide and nucleoside analogues in the antenatal period, the child is subject to careful clinical and laboratory monitoring to identify possible mitochondrial dysfunction, even in the absence of HIV.

    Autoimmune diseases. In rare cases, the treatment with stavudine develops muscle weakness. Its symptoms may be similar to the clinical signs of Guillain-Barre syndrome (including respiratory insufficiency). Symptoms may persist or worsen after discontinuation of therapy.

    Effect on the ability to drive transp. cf. and fur:Not studied.
    Form release / dosage:
    Capsules 30 mg, 40 mg.
    Packaging:
    60 capsules in a bottle of high-density white polyethylene with a screw cap that has a protective device against opening by children.2 sachets with a moisture absorber and absorbent material (cotton wool) are placed in the bottle; 1 bottle with instructions for use in a cardboard pack.
    10 capsules in a blister of aluminum foil, laminated PVC; 3, 6 or 9 blisters with instructions for use in a cardboard bundle.
    Storage conditions:
    Store in a dry 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 the date shown on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-001195
    Date of registration:11.11.2011 / 07.05.2015
    Expiration Date:11.11.2016
    Date of cancellation:2016-12-21
    The owner of the registration certificate:Ranbaxy Laboratories LimitedRanbaxy Laboratories Limited India
    Manufacturer: & nbsp
    Representation: & nbspRABBAYS LABORATORY LIMITEDRABBAYS LABORATORY LIMITED
    Information update date: & nbsp10.03.2017
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