Velbine concentrate for solution for infusion 10 mg ml 5 ml N1
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Active ingredients
Vinorelbine
Composition
1 ml of 1 fl. Vinorelbine tartrate 13.85 mg 69.25 mg, which corresponds to the content of vinorelbine base 10 mg 50 mg. Excipients: water d / and - up to 5 ml.
Pharmacological effect
The antitumor drug, from the group of vincaalkaloids, is a Vinca roseal alkaloid. Violates tubulin polymerization during cell mitosis. It blocks mitosis in the G2 + M phase and causes cell destruction in the interphase or during subsequent mitosis. Affects mainly mitotic microtubules; when used in high doses, has an effect on axonal microtubules. The effect of tubulin spiraling caused by vinorelbine is less pronounced than that of vincristine.
Pharmacokinetics
After the on / in the introduction of the drug can be traced three-phase kinetics. Distribution Plasma protein binding is 13.5%. Intensively binds to blood cells and especially platelets (78%). It penetrates well into tissues and lingers in them for a long time. In large quantities is determined in the spleen, liver, kidneys, lungs and thymus, moderate - in the heart and muscles; in minimal quantities in adipose tissue and bone marrow. Does not penetrate the BBB. Concentration in the lungs is 300 times the plasma concentration. Metabolism Metabolized in the liver, mainly by the action of the CYPZA4 isoenzyme. Forms a number of metabolites, one of which, diacetylquinorelbine, retains antitumor activity. Withdrawal The average T1 / 2 in the final phase is 40 (27.7-43.6) hours. It is derived mainly from the bile. Pharmacokinetics in special clinical situations The pharmacokinetics of vinorelbine, administered at a dose of 20 mg / m2 weekly in patients with moderate or severe liver failure, does not change. The pharmacokinetics of vinorelbine does not depend on the age of the patients.
Indications
- non-small cell lung cancer - breast cancer - prostate cancer resistant to hormone therapy (in combination with small doses of oral corticosteroids).
Contraindications
- the initial number of neutrophils in the blood is less than 1500 / μl, the platelet count is less than 75 000 / μl - severe infectious diseases during the start of therapy or transferred during the last 2 weeks - severe liver failure,unrelated to the tumor process - the need for constant oxygen therapy - in patients with a lung tumor - pregnancy - lactation period (breastfeeding) - hypersensitivity to the components of the drug - hypersensitivity to vinca alkaloids. The drug should be used with caution in case of respiratory failure, inhibition of bone marrow hematopoiesis (including after previous chemotherapy or radiation treatment), constipation or symptoms of intestinal obstruction in history, neuropathy in history.
Use during pregnancy and lactation
Contraindicated use during pregnancy and lactation (breastfeeding). During and for at least 3 months after cessation of therapy, it is necessary to use reliable methods of contraception.
Dosage and administration
Velbin is used both as monotherapy, and in combination with other anticancer drugs. When choosing a dose and mode of administration in each individual case, refer to the special literature. Velbin is administered strictly in / in the form of a 6-10 minute infusion. With monotherapy, the usual dose of the drug is 25-30 mg / m2 of body surface 1 time / week. The drug is diluted in a 0.9% solution of sodium chloride or 5% dextrose solution to a concentration of 1.0-2.0 mg / ml. After the introduction of the drug, the vein should be washed, adding an additional at least 250 ml of 0.9% sodium chloride solution or 5% dextrose solution. For patients with a surface area of> 2 m 2, a single dose of Velbine with IV should not exceed 60 mg. In polychemotherapy, the dose and frequency of Velbin administration depends on the specific program of antitumor therapy. With a decrease in the neutrophil content of less than 1500 / μl or thrombocytopenia less than 75 000 / μl, the regular administration of Velbine is postponed for 1 week. If, due to hematological toxicity, it was necessary to refrain from 3 weekly injections of the drug, it is recommended to discontinue the use of Velbin. In patients with severe liver failure, Velbine should be administered with caution at a dose not exceeding 20 mg / m2.
Side effects
Co side of the blood-forming organs: neutropenia, anemia, thrombocytopenia; against the background of oppression of bone marrow hematopoiesis - the addition of secondary infections, fever (> 38 ° C), sepsis, septicemia, very rarely - complicated septicemia, in some cases leading to death. The smallest number of neutrophils is observed on days 7-10 from the start of therapy, recovery occurs in the next 5-7 days. Cumulative hematotoxicity is not observed.Allergic reactions: rarely - anaphylactic shock or angioedema. On the part of the nervous system: paresthesia, hyperesthesia, decrease or loss of deep tendon reflexes, weakness in the legs, pain in the jaw area, rarely severe paresthesias with sensory and motor symptoms, as a rule, are reversible. On the part of the cardiovascular system: an increase or decrease in blood pressure, hot flashes and cooling of the extremities, coronary heart disease (angina pectoris, myocardial infarction), severe hypotension, collapse; extremely rarely - tachycardia, palpitations and heart rhythm disturbances. On the part of the respiratory system: shortness of breath, bronchospasm, interstitial pneumonia (with combination therapy with mitomycin C), acute respiratory distress syndrome. On the part of the digestive system: nausea, vomiting, anorexia, stomatitis, constipation, diarrhea, pancreatitis, intestinal paresis, transient increase in bilirubin level and increased activity of hepatic transaminases. From the skin and skin appendages: alopecia, skin rashes. Local reactions: pain / burning or redness at the injection site, discoloration of veins, phlebitis; with extravasation - inflammation of the subcutaneous fatty tissue, necrosis of the surrounding tissues. Others: weakness, myalgia, arthralgia, fever, pain of various localization, including pain in the chest and in the area of tumor formation, hyponatremia, hemorrhagic cystitis and syndrome of inadequate secretion of ADH.
Overdose
Symptoms: possible suppression of bone marrow function and manifestations of neurotoxicity. Treatment: The specific antidote is not known. In case of overdose, the patient should be hospitalized and the functions of vital organs should be carefully monitored. Symptomatic therapy.
Interaction with other drugs
When used together with other cytostatics, mutual aggravation of side effects is possible, first of all, myelosuppression. When combined with mitomycin C, the development of acute respiratory failure is possible. When used in conjunction with paclitaxel, the risk of neurotoxicity increases. Application on the background of radiation therapy leads to radiosensitization. When using vinorelbine after radiation therapy can lead to the reappearance of radiation reactions.The simultaneous use of the drug with inducers and inhibitors of cytochrome P450 may lead to changes in the pharmacokinetics of vinorelbine.
special instructions
Treatment with Velbin should be carried out under the supervision of a physician with experience in working with anticancer drugs. The treatment is carried out under strict hematological control, determining the number of leukocytes, neutrophils, platelets and hemoglobin level before each regular injection or ingestion. When the neutrophil content is below 1500 cells / mcl and / or platelets below 75,000 cells / mcl, the introduction of the next dose should be postponed until the normal level is restored. In case of markedly impaired liver function, the dose of Velbina should be reduced by 33%. In case of impaired renal function, enhanced monitoring of the patient is necessary. With the appearance of signs of neurotoxicity of 2 or more degrees, Velbin should be discontinued. If dyspnea, cough or hypoxia of unknown etiology occurs, the patient should be examined to exclude pulmonary toxicity. With extravasation, the infusion of the drug should be immediately stopped, the remaining dose is injected into another vein. If Velbin gets into the eyes, they should be washed thoroughly with water. Any special instructions for use of the drug Velbin in elderly patients are not available. Use with Pediatrics The safety and effectiveness of Velbin in children has not been studied.