Nikavir® (Nikavir)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substancePhosphazidePhosphazide
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  • Nikavir®
    pills inwards 
    AZT PHARMA KB, LLC     Russia
  • Nikavir®
    pills inwards 
    AZT PHARMA KB, LLC     Russia
    • Dosage form: & nbsppills
    Composition:

    Active substance: Phosphazide - 200 mg.

    Excipients: calcium carbonate (precipitated) - 120.6 mg; microcrystalline cellulose - 37.5 mg; silicon dioxide colloid (aerosil) - 13.2 mg; calcium stearate - 3.7 mg

    Description:

    Tablets are white or white with a yellowish-grayish hue, with yellowish-gray splotches, flat-cylindrical shape with a facet and a risk, with a characteristic odor.

    Pharmacotherapeutic group:An antiviral [HIV] agent.
    ATX: & nbsp

    J.05.A.X   Other antiviral drugs

    Pharmacodynamics:

    Active substance phosphazide belongs to the class of inhibitors of reverse transcriptase (revertase) of retroviruses, being a modified analogue of the natural thymidine nucleoside. Phosphazide, having penetrated into the infected cell, is twice phosphorylated to the active metabolite - azidothymidine triphosphate, which is inserted in place of thymidine triphosphate in the reverse-side chain of proviral DNA, which leads to inhibition of the revertase, breakage of the DNA chain, and stopping the reproduction of viral particles. This mechanism is based therapeutic effect of the drug to reduce the concentration of HIV in the patient's blood.Also, the preparation inhibits the replication of some other mammalian retroviruses, for example, the hepatitis B virus.

    Pharmacokinetics:

    Phosphazide well absorbed from the gastrointestinal tract. The time of full absorption is 3-3.5 h; half-life from the body - 3-4 hours; the maximum concentration of phosphazide in the blood plasma - 19-22 μg / ml is reached after 4-5 hours.

    Bioavailability of tablets is about 20% of intravenous administration. The relative bioavailability of phosphazide is 83.7% of zidovudine. Phosphazide penetrates the blood-brain barrier and is found in cerebrospinal fluid at a concentration of 15-64% of the initial dose. The active substance penetrates well through the placenta, so that its concentration in the blood of the umbilical cord is comparable to that in the mother's blood. Metabolism of phosphazide occurs in the liver with the formation of glucuronide, which is excreted from the body by the kidneys with urine.

    Indications:

    HIV Infection. The drug is used in monotherapy or in combination with other antiretroviral drugs in HIV-infected patients in the stage of secondary diseases (STA, ST, PO phases according to Pokrovsky VI classification, 1989),in the stage of acute infection (2A) and at primary manifestations (2B, 2B) with a decrease in the level of CD4T-lymphocytes less than 400-500 in 1 mm3 and an increase in the level of HIV RNA more than 20 thousand copies per 1 ml RT PCR), as well as in the stage of incubation (stage 1).

    The drug can be used for emergency prevention of HIV infection in the case of occupational risk of contamination with contaminated HIV-infected biological material in cases of injections, cuts, and contact with mucous membranes.

    Acute hepatitis B. The drug is prescribed to patients in mild and moderate form (icteric period).

    Contraindications:

    Hypersensitivity to phosphazide or to any of the excipients of the drug. Before taking the drug, consult a doctor.

    When hepatitis B in children is not applied.

    Carefully:

    A relative contraindication to the prescription of the drug is severe nausea, vomiting, a decrease in hemoglobin below 50 g / l, an increase in the activity of aminotransferases and creatinine in the blood serum more than 5 times the upper limit of the norm, a decrease in the number of neutrophils to 500 in μL, a decrease in the number of platelets less than 25 thousand in μl.

    Pregnancy and lactation:

    HIV-infected women are not recommended to take the drug before 14 weeks of pregnancy; women who use the drug are not recommended to breast-feed

    Dosing and Administration:

    HIV Infection. Take inside tablets of 200 mg.

    Daily doses for HIV infection:

    • adults: 600-1200 mg per day in 2 divided doses;

    • children under 13 years: 10 mg per 1 kg of body weight in 2-3 divided doses;

    • adolescents over 13 years: 200 mg 3 times a day.

    Recommended doses in terms of body weight.

    Body weight, kg

    Daily dose in milligrams

    The daily dose of 200 mg tablets

    up to 7,5

    50

    1/4 tablets

    7,5-12,5

    100

    1/2 tablet

    12,5-17,5

    150

    3/4 tablets

    17,5-22,5

    200

    1 tablet

    22,5-27,5

    250

    1 tablet + 1/4 tablet

    27,5-32,5

    300

    1 tablet + 1 tablet

    32,5-37,5

    350

    1 tablet + 3/4 tablets

    37,5-42,5

    400

    2 tablets

    42,5-47,5

    450

    2 tablets +1/4 tablets

    It is recommended to take the drug before eating and drink with a glass of water. When the central nervous system affects the retrovirus, the drug is prescribed in a daily dose of 1200 mg for adults and 20 mg per 1 kg of body weight - for children. If the drug is poorly tolerated, the daily dose can be reduced to 400 mg per day in adults and up to 5 mg per kg of body weight in children.

    A course of treatment. The drug is prescribed for a long, almost unlimited period, if necessary, the course can be interrupted, but the duration should be at least 12 weeks with a break between courses - no more than 12 weeks.

    Treatment with the drug (monotherapy) is carried out in a continuous scheme in patients with acute HIV infection (stage 2A) for the period of clinical manifestations (plus 1 month after, but not less than three months); in the stage of CV - permanently, in the stages of ZA and ST - in clinical manifestations. In the stages of ZA and ST in the phase of the absence of clinical manifestations, as well as in the stages of primary manifestations (2B and 2B), the drug is prescribed with the number of CD4T-lymphocytes 200 <CD4 <500 courses for 12 weeks with a break of 12 weeks.

    For the prevention of occupational HIV infection, it is recommended to start taking the drug 600 mg twice a day for 4 weeks as soon as possible, but no later than 72 hours after the eventual infection.

    Acute hepatitis B. The drug is prescribed to adults 400 mg twice a day for 20 days. It is recommended to start taking the drug no later than 7 days after the onset of jaundice. Data on the use of the drug in children are absent.


    Side effects:In rare cases, at the beginning of the course of treatment - nausea, headache7 heaviness in epigastrium, diarrhea, disappearing during the next few days of treatment. In isolated cases, granulocytopenia and anemia, however, their association with therapy with the drug Nikavir® has not been proven.If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor about it
    Overdose:In case of intoxication with the drug (until now it has not been noted) hemodialysis and peritoneal dialysis significantly increase the excretion of the glucuronic metabolite of phosphazide.
    Interaction:
    The drug can be used in combination with other antiretroviral drugs in combined treatment regimens, but the joint use of the drug Nikavir® with zidovudine, stavudine leads to a mutual decrease in activity against HIV.
    Co-administration with alpha-interferon, didanosine, lamivudine, foscarnet results in a mutual increase in activity against HIV.
    Co-administration with doxorubicin, alpha-interferon, amphotericin-B, co-trimoxazole, vinblastine, vincristine, ganciclovir, dapsone, sulfadiazine and other sulfanilamides may lead to mutual enhancement of myelotoxicity, therefore additional control over the concentration of hemoglobin and granulocytes is required.

    Special instructions:
    Usually the drug is well tolerated by both adults and children. Phosphazide - low-toxic substance. Its toxicity is 5-6 times lower than zidovudine. Assessing the tolerability of the drug, it should be borne in mind that these side effects and other symptoms and syndromes can be manifestations of not only therapy, but also of HIV infection and concomitant diseases.
    If some unwanted phenomena appear in the early stages of taking the drug, you should not abolish it, it is recommended to continue therapy.
    Irregularity of taking the drug to patients (violation of the treatment regimen) can lead to the development of resistance (stability) of the retrovirus to it, which will result in a decrease in the effectiveness of the therapy and the need to replace the drug.
    To avoid complications, the drug is used under the supervision of a doctor.
    Therapy with the drug does not reduce the risk of transmission of HIV to other people during sexual intercourse or during blood transfusion.
    Effect on the ability to drive transp. cf. and fur:

    Studies have not been carried out, however, when deciding whether to control a car, mechanisms, one should keep in mind the patient's condition and the possibility of developing adverse reactions to Nikavir®, such as nausea, headache, diarrhea.

    Form release / dosage:

    tablets of 200 mg

    Packaging:10 tablets of 200 mg in contour acrylic packaging (blister) of film-PVC and foil; 2 blisters (20 tablets 200 mg each) with instructions for use in a pack of cardboard. For 20, 30, 60 tablets in cans of polymeric, ukuporennyh cover. Bank with instructions for use in a pack of cardboard
    Storage conditions:

    In dry, dark place at a temperature of no higher than 20 ° C. Keep away from children.

    Shelf life:

    2 years. Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:P N003864 / 01
    Date of registration:05.02.2010
    The owner of the registration certificate:AZT PHARMA KB, LLC AZT PHARMA KB, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp28.10.2015
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