Velbin concentrate for infusion solution 10mg/ml 5ml vial, 1pc

Composition

Active ingredients:

1 ml of vinorelbine ditartrate is 13.85 mg, which corresponds to the content of vinorelbine 10 mg.

Auxiliary substances:

d/i water-up to 1 ml

Pharmacological action

Pharmacodynamics

Antitumor drug, from the group of vincaalkaloids, is an alkaloid of pink Periwinkle. Interferes with tubulin polymerization during cellular mitosis. Blocks mitosis in the G2+M phase and causes cell destruction in interphase or in subsequent mitosis. It acts mainly on mitotic microtubules; when used in high doses, it also affects axonal microtubules. The effect of tubulin spiralization caused by vinorelbine is less pronounced than that of vincristine.

Pharmacokinetics

After intravenous use of the drug, three-phase kinetics is observed.

Distribution

Binding to plasma proteins is 13.5%. Intensely binds to blood cells and especially platelets (78%). It penetrates well into the tissues and stays in them for a long time. It is detected in large amounts in the spleen, liver, kidneys, lungs and thymus gland, moderate-in the heart and muscles; in minimal amounts-in adipose tissue and bone marrow. It does not penetrate the BBB. The concentration in the lungs is 300 times higher than the concentration in the plasma.

Metabolism

It is metabolized in the liver, mainly under the action of the SURZA 4 isoenzyme. It forms a number of metabolites, one of which, diacetylvinorelbine, retains antitumor activity.

Deduction

The average T1 / 2 in the final phase is 40 (27.7-43.6) hours. It is mainly excreted in bile.

Pharmacokinetics in special clinical cases

, the pharmacokinetics of vinorelbine administered at a dose of 20 mg/m2 weekly in patients with moderate or severe hepatic insufficiency do not change.

The pharmacokinetics of vinorelbine do not depend on the age of patients.

Indications

• Non-small cell lung cancer;
• breast cancer;
• prostate cancer resistant to hormone therapy (in combination with low doses of oral corticosteroids).

Use during pregnancy and lactation

Contraindicated use during pregnancy and lactation (breastfeeding).

Reliable methods of contraception should be used during and for at least 3 months after discontinuation of therapy.

Contraindications

• The initial number of neutrophils in the blood < 1500/µl, the platelet count < 75 000 /µl;
• serious infectious diseases during the initiation of therapy or transferred within the last 2 weeks;
• severe hepatic impairment is not associated with the tumor process;
• the need for continuous oxygen therapy in patients with lung tumor;
• pregnancy;
• lactation (breastfeeding);
• hypersensitivity to the components of the drug;
• increased sensitivity to vinylchloride.

With caution: the drug should be used in case of respiratory failure, suppression of bone marrow hematopoiesis (including after previous chemotherapy or radiation treatment), constipation or a history of intestinal obstruction, neuropathy in the anamnesis.

Side effects

From the hematopoietic organs: neutropenia, anemia, thrombocytopenia; against the background of inhibition 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 lowest number of neutrophils is observed on 7-10 days from the start of therapy, recovery occurs in the next 5-7 days.

No accumulation of hematotoxicity was observed.

Allergic reactions: rarely-anaphylactic shock or angioedema.

Nervous system disorders: paresthesia, hyperesthesia, decreased or lost deep tendon reflexes, weakness in the legs, pain in the jaw area, rarely severe paresthesia with sensory and motor symptoms, usually reversible.

From the cardiovascular system: increased or decreased blood pressure, hot flashes and cold extremities, IHD (angina pectoris, myocardial infarction), severe hypotension, collapse; extremely rare-tachycardia, palpitations and cardiac arrhythmia.

Respiratory system disorders: dyspnea, bronchospasm, interstitial pneumonia (in combination therapy with mitomycin C), acute respiratory distress syndrome.

From the digestive system: nausea, vomiting, anorexia, stomatitis, constipation, diarrhea, pancreatitis, intestinal paresis, transient increase in bilirubin levels 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 the vein, phlebitis; with extravasation-inflammation of subcutaneous fat, necrosis of surrounding tissues.

Others: weakness, myalgia, arthralgia, fever, pain of various localization, including pain in the chest and in the area of tumor formations, hyponatremia, hemorrhagic cystitis and syndrome of inadequate ADH secretion.

Interaction

When combined with other cytostatics, side effects may be mutually aggravated, primarily myelosuppression.

When combined with mitomycin C, acute respiratory failure may develop.

When used together with paclitaxel, the risk of neurotoxicity increases.

Use during radiation therapy leads to radiosensitization. When using vinorelbine after radiation therapy, it can lead to repeated occurrence of radiation reactions.

Concomitant use of the drug with cytochrome P450 inducers and inhibitors may lead to changes in the pharmacokinetics of vinorelbine.

How to take, course of use and dosage

Velbin is used both as monotherapy and in combination with other antitumor drugs. When choosing the dose and mode of use in each individual case, you should refer to the special literature.

Velbin is administered strictly intravenously 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 area 1 time/week.

The drug is diluted in 0.9% sodium chloride solution or 5% dextrose solution to a concentration of 1.0-2.0 mg / ml. After use of the drug, the vein should be flushed, adding at least 250 ml of 0.9% sodium chloride solution or 5% dextrose solution.

For patients with a body surface area of >2 m2, a single dose of Velbin with intravenous use should not exceed 60 mg. >

In polychemotherapy, the dose and frequency of use of Velbin depend on the specific antitumor therapy program.

With reduced neutrophil count < 1500 / µl or thrombocytopenia If due to hematological toxicity, it was necessary to refrain from 3 weekly injections of the drug, the use of Velbin is recommended to stop.

In patients with severe hepatic insufficiency, Velbin should be administered with caution at a dose not exceeding 20 mg / m2.

Overdose

Symptoms: possible suppression of bone marrow function and manifestations of neurotoxicity.

Treatment: No specific antidote is known. In case of overdose, the patient should be hospitalized and carefully monitor the functions of vital organs. Conducting symptomatic therapy.

Special instructions

Treatment with Velbin should be carried out under the supervision of a doctor who has experience with antitumor drugs.

Treatment is carried out under strict hematological control, determining the number of white blood cells, neutrophils, platelets and hemoglobin levels before each regular injection or oral use. If the neutrophil count is below 1,500 cells/µl and/or the platelet count is below 75,000 cells/µl, the next dose should be delayed until normal levels are restored.

In patients with severe hepatic impairment, the dose of Velbin should be reduced by 33%.

If renal function is impaired, the patient should be closely monitored.

If signs of neurotoxicity of 2 or more degrees appear, the use of Velbin should be discontinued.

If dyspnea, cough or hypoxia of unknown etiology occur, the patient should be examined to exclude pulmonary toxicity.

In case of extravasation, the infusion of the drug should be stopped immediately, the remaining dose is injected into another vein.

If Welbin gets into the eyes, they should be thoroughly and thoroughly rinsed with water.

There are no specific instructions for the use of Velbin in elderly patients.

Use with Pediatrics

The safety and efficacy of Velbin in children has not been studied.

Form of production

Concentrate for preparation of solution for infusions.

Storage conditions

Store at a temperature of 2 to 8°C.

Shelf

life is 18 months.

Active ingredient

Vinorelbin

Conditions of release from pharmacies

By prescription

Dosage form

solution for infusions

Purpose

For adults as directed by your doctor

Indications

Breast Cancer, Cancer