Composition, form of production and packaging
Concentrate for the preparation of a solution for infusions is transparent, slightly colored.
1 ml
vinorelbine ditartrate 13.85 mg,
in t.ch. vinorelbine 10 mg
Auxiliary substances: water d / and.
1 ml - bottles (1) - packs of cardboard.
Concentrate for the preparation of a solution for infusions is transparent, slightly colored.
1 ml of 1 fl.
vinorelbine ditartrate 13.85 mg 69.25 mg,
in t.ch. vinorelbine 10 mg 50 mg
Auxiliary substances: water d / and.
5 ml - bottles (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
An antitumor drug from the group of vincaalkaloids (vinorelbine is an alkaloid of the vinca rosea, obtained semi-synthetically).
Violates the polymerization of tubulin in the process of cellular mitosis. It blocks mitosis in the G 2 + M phase and causes cell destruction in the interphase or subsequent mitosis. Acts mainly on mitotic microtubules; when high doses are applied, it also affects axonal microtubules. The effect of spiral tubulin, caused by vinorelbine, is less pronounced than that of vincristine.
PHARMACOKINETICS
Suction
After iv introduction of the preparation, three-phase kinetics can be traced.
Distribution
The binding with plasma proteins is 79.6-91.2%. Intensively binds to platelets, lymphocytes, alpha 1- acid glycoprotein, albumin and lipoproteins. It penetrates well into tissues and lingers in them for a long time. Large quantities are found in the spleen, liver, kidneys, lungs and thymus, moderate in the heart and muscles, minimal in fat tissue, head and bone marrow. Concentration in the lungs is 300 times higher than the concentration in the plasma.
Metabolism
Forms a number of metabolites; one of the metabolites, diacetylvinorelbine, retains antitumor activity. Metabolised in the liver.
Excretion
The mean T 1/2 in the final phase is 40 h (27.7-43.6). It is excreted mainly with bile.
INDICATIONS
- non-small cell lung cancer;
- mammary cancer.
DOSING MODE
Vinorelbine is used both in the form of monotherapy, and in combination with other antitumor drugs. When choosing a dose and mode of administration in each individual case, you should refer to the special literature.
Vinorelbine is administered strictly IV in the form of a 15-20 minute infusion. In the monotherapy regime, the usual dose of the drug is 25-30 mg / m body surface once a week.
The drug is diluted in 0.9% solution of sodium chloride or 5% solution of dextrose to a concentration of 1.5-3.0 mg / ml. After the administration of the drug, the vein should be washed, adding an additional 50-100 ml of a 0.9% solution of sodium chloride.
Correction of dosing regimen of vinorelbine depending on hematological parameters:
Number of granulocytes on the day of drug administration (cells / Ојl) Percentage of starting dose of vinorelbine
? 1500 100%
1499-1000 50%
<1000 The drug is not given. The number of granulocytes is repeated after 1 week. If due to granulocytopenia had to refrain from 3 weekly injections of the drug, the use of vinorelbine is recommended to be discontinued.
In patients with hyperthermia and / or sepsis on the background of granulocytopenia during treatment or when two weekly injections of the drug are missed due to the low number of granulocytes, the doses for subsequent administrations should be as a percentage of the previous doses:
? 1500 75%
1499-1000 37.5%
<1000 The drug is not given.
Correction of dosing regimen of vinorelbine in liver failure: patients with hepatic insufficiency vinorelbine should be administered with caution, with the appearance of hyperbilirubinemia in the background of vinorelbine treatment, subsequent doses should be reduced according to the following recommendations:
Concentration of total bilirubin (Ојmol / L) Percentage of starting dose of vinorelbine
? 34.2 100%
35.9-51.3 50%
> 51.3 25%
For patients with a body surface area> 2 m 2, a single dose of vinorelbine should not exceed 60 mg.
Special instructions for the use of vinorelbine in elderly patients are lacking.
SIDE EFFECT
From the hemopoietic system: granulocytopenia, anemia; rarely - thrombocytopenia. The smallest number of granulocytes is observed on the 7-10th day from the beginning of therapy, recovery occurs in the next 7-14 days.
From the side of the central nervous system and peripheral nervous system: decrease or loss of deep tendon reflexes, paresthesia, hyperesthesia, weakness in the legs, pain in the jaw area, headache, intestinal paresis; rarely - paralytic ileus.
On the part of the digestive system: nausea, vomiting, anorexia, constipation, diarrhea, dysphagia, mucositis, pancreatitis, increased bilirubin levels and increased activity of hepatic transaminases.
On the part of the respiratory system: difficulty breathing, dyspnea, bronchospasm, interstitial pneumonia, acute respiratory distress syndrome.
From the cardiovascular system: pain in the chest, increase or decrease in blood pressure, tachycardia; rarely - myocardial infarction, pulmonary edema.
Local reactions: pain or redness at the injection site; with extravasation - cellulite, phlebitis and, possibly, necrosis of surrounding tissues.
Other: weakness, alopecia, myalgia, arthralgia, skin rashes, allergic reactions, hot flushes to the face, increased level of creatinine, hyponatremia, hemorrhagic cystitis, ADH inadequate secretion syndrome.
CONTRAINDICATIONS
- pronounced violations of the liver function;
- initial number of neutrophils <1000 cells / Ојl;
- Radiation therapy of the hepatobiliary region;
- Pregnancy;
- the period of breastfeeding;
- hypersensitivity to vinaalkaloids.
With caution , use the drug with respiratory failure, oppression of bone marrow hematopoiesis (including after previous chemotherapy, radiation treatment), constipation, intestinal obstruction in history, neuropathy in history.
PREGNANCY AND LACTATION
The use of the drug during pregnancy and during breastfeeding is contraindicated.
During and for at least 3 months after cessation of therapy, reliable methods of contraception should be used.
APPLICATION FOR FUNCTIONS OF THE LIVER
If the kidney function is impaired, intensive monitoring of the patient is necessary.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
If the liver function is impaired, vinorelbine should be reduced. Contraindicated use of the drug in severe violations of liver function.
SPECIAL INSTRUCTIONS
Treatment vinorelbine should be conducted under the supervision of a doctor who has experience with antitumor drugs.
Treatment vinorelbine should be carried out under strict hematological control, determining the number of leukocytes, granulocytes and hemoglobin level before each next injection.
If the liver function is impaired, vinorelbine should be reduced.
If the kidney function is impaired, intensive monitoring of the patient is necessary.
When there are signs of neurotoxicity, treatment with the drug should be discarded.
If dyspnoea, cough or hypoxia of unexplained etiology appears, the patient should be examined to exclude pulmonary toxicity.
When extravasation, the infusion of the drug should be stopped immediately, the remaining dose is injected into another vein.
If vinorelbine comes into the eye, rinse thoroughly and thoroughly with water.
Use in Pediatrics
The safety and efficacy of vinorelbine in children have not been studied.
OVERDOSE
Symptoms: suppression of bone marrow function, peripheral neuropathy.
Treatment: In case of an overdose, the patient should be hospitalized and closely monitor the functions of vital organs. Treatment is symptomatic. The specific antidote is not known.
DRUG INTERACTION
With the simultaneous application of MAVEREX with mitomycin C, acute respiratory failure may develop.
With the simultaneous application of MAVEREX with paclitaxel, the risk of neurotoxicity increases.
With the simultaneous application of MAVEREX with cisplatin, granulocytopenia is enhanced.
The use of Mawerex on the background of radiotherapy leads to radiosensitization.
The drug should be used with caution with CYPZA isoenzyme inhibitors.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children, protected from light at a temperature of 2 В° to 8 В° C. After additional dilution, the shelf life is 24 hours at room temperature. Shelf life - 3 years.
