Active substanceHydroxycarbamideHydroxycarbamide
Similar drugsTo uncover
  • Hydrea®
    capsules inwards 
  • Hydroxycarbamide medec
    capsules inwards 
    medac GmbH     Germany
  • Hydroxycarbamide-LENS
    capsules inwards 
    VEROPHARM SA     Russia
  • Hydroxycarbamide-native
    capsules inwards 
    NATIVA, LLC     Russia
  • Hydroxyurea
    capsules inwards 
  • Dosage form: & nbspcapsules
    Composition:

    Each capsule contains:

    active substance: hydroxycarbamide 500 mg;

    Excipients: lactose monohydrate 25 mg, calcium citrate 25 mg, disodium citrate 50 mg, magnesium stearate 6 mg;

    capsule shell: gelatin 98 mg, titanium dioxide (E 171) 2 mg.

    Description:

    Hard gelatin capsules No. 0, with a white opaque body and lid, filled with a powder of almost white color.

    Pharmacotherapeutic group:antitumour agent - antimetabolite
    ATX: & nbsp

    L.01.X.X.05   Hydroxycarbamide

    Pharmacodynamics:

    Hydroxycarbamide is a phase-specific cytostatic drug (antimetabolite, according to some data - the alkylating action), acting in phase S cell cycle. Blocks cell growth in interphase Gl-S, which is essential for simultaneous radiotherapy, since synergistic sensitivity of tumor cells appears in the phase G1 for irradiation.Strengthening the action of the RNA reductase inhibitor, ribonucleoside diphosphate reductase, causes suppression of DNA synthesis. The drug does not affect the synthesis of RNA and protein.

    Pharmacokinetics:

    After oral administration, it is rapidly absorbed from the gastrointestinal tract. The maximum concentration of the drug in the blood plasma is reached within 2 hours after ingestion. Data on the effect of food intake on the absorption of the drug there. Quickly distributed to the tissues of the body, it penetrates the blood-brain barrier. In the cerebrospinal fluid is determined 10-20%, in the ascitic fluid - 15-50% of the concentration in the blood plasma. Hydroxycarbamide accumulates in leukocytes and erythrocytes. The half-life is -3-4 hours. Partially metabolized in the liver and kidneys. 80% hydroxyurea for 12 hours is excreted in the urine, with 50% unchanged and in small amounts in the form of urea. The drug is also excreted through the respiratory tract as carbon dioxide. After 24 hours in the plasma is not determined.

    Indications:

    - Chronic myelogenous leukemia;

    - true polycythemia (erythremia);

    - essential thrombocythemia;

    - osteomyelophybrosis;

    - melanoma;

    - Malignant tumors of the head and neck, with the exception of lip cancer (in combination with radiotherapy);

    - cervical cancer (in combination with radiotherapy).

    Contraindications:

    - Hypersensitivity to hydroxycarbamide or other components of the drug;

    - pregnancy and the period of breastfeeding;

    - leukopenia below 2.5x109/ l, thrombocytopenia below 100x109/ l;

    - age to 18 years.

    Carefully:

    Prior radio or chemotherapy, hepatic and / or renal failure, anemia (should be corrected before treatment), lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

    Pregnancy and lactation:

    Pregnancy

    The use of hydroxycarbamide during pregnancy is contraindicated. Women of childbearing age should start using contraceptives before starting treatment with hydroxycarbamide and continue throughout the treatment period. When pregnancy occurs against the background of treatment with hydroxycarbamide, you need to consult a genetic consultation. Hydroxycarbamide penetrates the placental barrier.

    Breastfeeding period

    As hydroxycarbamide penetrates into breast milk, then if you need the drug, breastfeeding should be discontinued before the treatment with hydroxycarbamide.

    Dosing and Administration:

    Treatment with the drug should be carried out only under the supervision of a doctor who has experience of antitumor therapy. Doses are set based on the real or ideal body weight of the patient, depending on which one is smaller.

    The drug is used inside, without chewing, with a glass of water. If swallowing is difficult, the capsule can be opened, dissolved in a glass of water and drunk entirely. In this case, some water-insoluble auxiliary substances can float on the surface of the solution.

    During treatment with the drug should take a fairly large amount of fluid.

    Solid tumors, melanoma

    Intermittent therapy: 80 mg / kg once a day every three days (6-7 doses).

    Continuous therapy: 20-30 mg / kg daily for 3 weeks.

    Carcinoma of the head and neck, cervical carcinoma

    80 mg / kg once a day, every third day in combination with radiotherapy.

    Treatment with the drug begins at least 7 days before the start of radiotherapy and continues during radiotherapy.After radiotherapy, the drug continues to be taken for an unlimited time, with strict observation of the patient and in the absence of unusual or severe toxicity reactions.

    Resistant chronic myelogenous leukemia

    Continuous therapy. The initial daily dose is 40 mg / kg. The dose reduction depends on the number of leukocytes in the blood plasma. The dose is reduced by 50%, if the number of white blood cells is less than 20x109/ l. In the case of leukopenia, the dose should be adjusted so as to maintain the number of leukocytes at the level 5-10x109/ l. With a decrease in the number of white blood cells less 5x109/ l, the dose should be reduced. Increase the dose can only after reaching the number of leukocytes no less than 10x109/ l. Treatment is suspended if the number of white blood cells is less than 2,5x109/ l or platelets less than 100x109/ l. Renewal of treatment is possible after recovery of the number of leukocytes and platelets. The evaluation period for the antitumor activity of the drug is 6 weeks. If there is a significant deterioration in the course of the disease, treatment should be discontinued. With clinically meaningful improvement, treatment is extended indefinitely.

    True polycythemia

    Treatment begins with a daily dose of 15-20 mg / kg. The dose is set individually, seeking to maintain a hematocrit below 45%, and the platelet count is lower 400x109/ l. In most patients, it is possible to achieve these parameters by constantly applying hydroxycarbamide in a daily dose of 500 to 1000 mg. If the hematocrit and platelet counts can be successfully controlled, treatment should continue for an unlimited time.

    Essential thrombocythemia

    Usually, the drug is prescribed in the initial daily dose of 15 mg / kg; then select a dose that maintains the number of platelets at a level below 600x109/ l, without leading to a decrease in the number of white blood cells below 4 x 109/ l.

    Osteomyelophybrosis

    The initial daily dose is from 5 to 20 mg / kg. The maintenance daily dose is 10 mg / kg.

    Patients with impaired hepatic function

    There are no instructions for correcting doses in this group of patients. It should be carefully monitored blood levels in patients with impaired liver function.

    Patients with impaired renal function

    Because the hydroxycarbamide is excreted mainly by the kidneys, in such patients it is necessary to reduce the dose of the drug. Patients with a creatinine clearance less than 60 ml / min are usually given a dose of 15 mg / kg.Patients in the terminal stage of renal failure receive the drug at a dose of 15 mg / kg twice, with an interval of 7 days between doses: the first time - at the end of the 4-hour hemodialysis session, the second time before the hemodialysis session.

    Elderly patients

    Since elderly patients are more likely to develop side effects when using hydroxycarbamide than younger patients, the recommended dose for patients in this group should not exceed 60 mg / kg per day.

    Side effects:

    Adverse reactions occurring more often than in single cases are listed according to the following gradation: very often (> 1/10) often (> 1/100, <1/10) infrequently (> 1/1000, <1/100), rarely (> 1/10000, <1/1000), very rarely (< 1/10000, including individual messages), the frequency can not be estimated (the frequency can not be determined from the available data).

    Infections: the frequency can not be evaluated - gangrene.

    From the hematopoiesis: often - leukopenia, bone marrow depression, megaloblastosis; infrequently - anemia, thrombocytopenia.

    From the nervous system: rarely - headache, dizziness, fatigue, drowsiness, disorientation,hallucinations and convulsions; the frequency can not be assessed - peripheral neuropathy (in HIV-infected patients who simultaneously receive antiretroviral therapy, in particular didanosine and stavudine).

    On the part of the digestive system: often diarrhea or constipation; infrequently - stomatitis, anorexia, nausea, vomiting, mucosal ulceration of the gastrointestinal tract, the increase in liver enzymes and bilirubin concentration in the blood plasma; frequency can not be estimated - hepatotoxicity and pancreatitis, sometimes fatal (in HIV-infected patients concomitantly receiving antiretroviral therapy, particularly didanosine and stavudine).

    From the skin and subcutaneous tissues: infrequently - face erythema, palmar-plantar syndrome, maculopapular rashes; rarely - alopecia; very rarely - similar to dermatomyositis, skin changes, hyperpigmentation or atrophy of skin and nails, skin ulcers (especially leg ulcers), pruritus, radiation keratosis, skin cancer (cheshuychatokletochny, basal cell carcinoma), violet papules, scaling of the skin; frequency can not be estimated - cutaneous vasculitis, cutaneous vasculitis toxic (including vasculitis ulceration and gangrene), peripheral erythema.

    From the urinary system: infrequently - transient disorders of renal tubular function with an increase in the concentration of uric acid, urea and creatinine in the blood plasma; rarely - dysuria; very rarely - renal failure, interstitial nephritis.

    From the respiratory system, chest and mediastinum: rare - acute reactions (diffuse infiltrates in the lungs, fever, dyspnea), allergic alveolitis, the frequency can not be assessed - pulmonary fibrosis.

    From the immune system: rarely - hypersensitivity reactions.

    Other: infrequently - chills, malaise, general weakness, drug fever; rarely - tumor disintegration syndrome, impaired fertility (amenorrhea, azoospermia); very rarely - an increase in the rate of erythrocyte sedimentation; the frequency can not be evaluated - hyperkalemia. hyponatremia.

    Overdose:

    In patients receiving hydroxycarbamide in doses several times higher than recommended, severe reactions from the skin and mucous membranes can develop.

    Symptoms: pain, purple erythema, edema of the palms and feet, hyperkeratosis of the hands and feet, intense hyperpigmentation of the skin, stomatitis.

    Treatment: gastric lavage, symptomatic therapy, monitoring of hematopoiesis. Hemodialysis is possible.

    Interaction:

    With the simultaneous use of the drug with other myelosuppressive drugs or radiation therapy, the degree of suppression of bone marrow function or the development of other side effects may increase.

    The drug can increase the content of uric acid in the blood, so the simultaneous use of drugs that increase the excretion of uric acid, increases the risk of urate nephropathy. If a simultaneous application is necessary, adjust the dose of such drugs, or designate allopurinol.

    Hydroxycarbamide may enhance the antiretroviral activity of nucleoside reverse transcriptase inhibitors (NRTIs), such as didanosine and stavudine. Hydroxycarbamide inhibits the synthesis of DNA and the replication of the human immunodeficiency virus by reducing the intracellular deoxynucleotide. Hydroxycarbamide may also increase the side effects of this group of drugs, such as hepatotoxicity, pancreatitis and peripheral neuropathy.

    There have been cases of false positive results in the determination of urea, uric acid and lactic acid as a result of the interaction of hydroxycarbamide and enzymes (urease, uricase, lactate dehydrogenase).

    Special instructions:

    Treatment with the drug should be carried out only under the supervision of a doctor who has experience of antitumor therapy. Before each course and periodically during treatment with the drug, it is necessary to check the function of the bone marrow, kidneys and liver. A clinical blood test, including determining the level of hemoglobin, the expanded leukocyte formula and the number of platelets, should be performed regularly at least once a week throughout the period of treatment with the drug. When the number of leukocytes in the blood is less than 2,5x109/ l or platelets less than 100x109/ l treatment should be suspended until the normalization of hematological indicators. The drug has a cytotoxic effect, so you should use caution when opening the capsules and avoid getting capsule powder on the skin, mucous membranes or inhaling the drug.

    Anemia is not a contraindication for drug treatment.Severe form of anemia should be compensated before treatment with the drug.

    During treatment with the drug, myelosuppression may develop, mainly leukopenia. Thrombocytopenia and anemia develop less frequently and very rarely without previous leukopenia. Anemia, even in severe form, is stopped without interruption of treatment. Myelosuppression is most likely in patients after recently preceding intensive radiation therapy or chemotherapy with other drugs. After recent intensive radiation therapy, the drug should be used with caution because of possible exacerbation of post-radiation erythema and increased severity of side effects (bone marrow aplasia, dyspepsia and ulcerative lesions of the gastrointestinal tract).

    In the early stages of drug treatment, a moderate megaloblastic erythropoiesis is often observed. Morphological changes resemble malignant anemia, but they are not associated with vitamin deficiency AT12 or folic acid.

    The use of the drug can cause a decrease in iron clearance from the blood plasma and the efficiency of iron utilization by erythrocytes, however it does not affect the life span of erythrocytes.

    Cases of pancreatitis and hepatotoxicity (with possible fatal outcome) have been observed with simultaneous use of hydroxycarbamide and antiretroviral drugs in HIV-infected patients. It is necessary to regularly monitor the concentration of uric acid, creatinine, transaminase activity in blood plasma.

    During treatment, patients should consume a sufficient amount of fluid.

    During the treatment with hydroxycarbamide it is recommended to monitor the skin condition, since individual cases of development of squamous cell carcinoma of the skin are described.

    During drug treatment in patients with myeloproliferative diseases toxic toxic vasculitis, including vasculitic ulceration and gangrene.

    Hydroxycarbamide can cause painful ulceration of the skin of the lower extremities, which are difficult to treat and require discontinuation of therapy. The withdrawal of the drug leads to the healing of ulcers within two weeks.

    With prolonged use of hydroxycarbamide in patients with myeloproliferative diseases, such as true polycythemia and thrombocythemia, cases of secondary leukemia are noted.

    Men and women of childbearing age should use effective methods of contraception before starting therapy with hydroxyurea, during and within 3 months after the end. Because the hydroxycarbamide may have genotoxic effect, it is recommended that patients planning a pregnancy after the completion of therapy have a genetic consultation.

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

    During treatment it is recommended to refrain from driving vehicles and controlling mechanisms due to the fact that against the background of taking hydroxycarbamide, side reactions may develop: dizziness, disorientation, clouding of consciousness, affecting the ability to concentrate attention and the speed of psychomotor reactions.

    Form release / dosage:

    Capsules, 500 mg.

    Packaging:

    10 capsules per blister.

    For 5 or 10 blisters together with the instructions for use are placed in a 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:

    4 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N016025 / 01
    Date of registration:03.12.2009 / 02.10.2014
    The owner of the registration certificate:medac GmbHmedac GmbH Germany
    Manufacturer: & nbsp
    Representation: & nbspTIRUFARM, LLCTIRUFARM, LLCRussia
    Information update date: & nbsp17.01.2016
    Illustrated instructions
      Instructions
      Up