Vinelbin, 10 mg/ml 1 ml

Vinorelbine is an antitumor agent from the group of cytostatics, it is a semi-synthetic derivative of one of the alkaloids of pink periwinkle – vinblastine. Like vinblastine, vinorelbine blocks cell mitosis at the metaphase stage due to binding to tubulin protein.

Pharmacokinetics

After intravenous administration, vinorelbine is widely distributed in tissues, V_d is over 40 l/kg. Binding to plasma proteins is moderate – 13.5%, with platelets – high – 78%.

The kinetics of vinorelbine in plasma is three-phase. The average T_1/2 of the active substance in the final phase is 40 hours. Systemic clearance is 1.3 L/h/kg. It is excreted mainly with bile.

Indications

Breast cancer, lung cancer (except small cell).

Active ingredient

Composition

1 ml of concentrate for preparation of solution for infusion contains:

the active ingredient:

Vinorelbine (in the form of vinorelbine ditartrate) 10 mg

excipients:

water for injection – q.s. up to 1 ml

How to take, the dosage

Vinelbine is used both as monotherapy and in combination with other anticancer drugs. When choosing the dose and mode of administration in each individual case the special literature should be consulted.

Vinelbin is administered strictly intravenously as a 6-10 minute infusion. In the monotherapy regimen, the usual dose of the drug is 25-30 mg/m2 body surface once a 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 the drug is injected, the vein should be flushed with at least 250 ml of additional 0.9% sodium chloride solution or 5% dextrose solution.

For patients with a body surface area ≥ 2 m2 a single dose of Vinelbin administered by IV should not exceed 60 mg.

In polychemotherapy, the dose and frequency of Vinelbine administration depend on the specific antitumor therapy program.

If neutrophil count < 1500 cells/µl of blood or thrombocytopenia <75 000 cells/µl of blood decrease, the next injection of Vinelbin should be postponed for 1 week. If due to hematologic toxicity 3 weekly injections of the drug had to be withheld, Vinelbin should be discontinued.

Vinelbine dosing regimen correction in patients with hepatic impairment: in patients with significant hepatic impairment, Vinelbine should be administered with caution, in a dose not exceeding 20 mg/m2.

Children: The safety and effectiveness of Vinelbine in children has not been studied.

Elderly people: there are no specific instructions for the use of Vinelbine in the elderly.

Interaction

Concomitant use with mitomycin C increases the risk of respiratory depression, bronchospasm, especially in predisposed patients; with cisplatin – increased incidence of toxic reactions.

Special Instructions

Treatment with vinorelbine should be carried out only in a specialized hospital by personnel experienced in the treatment with chemotherapeutic agents. Peripheral blood counts must be monitored prior to treatment, and also prior to each subsequent administration of vinorelbine. If the granulocyte count is less than 2000/μL, the next injection should not be given, postponing it until a safe granulocyte level is reached.

Vinorelbine is used with caution in patients with impaired liver function, in which case the dose is reduced.

At the time of vinorelbine use X-ray therapy on the liver area is not prescribed.

In intravenous infusion avoid extravasation. Ingestion of vinorelbine into the surrounding vein leads to pain, inflammation, and in severe cases, necrosis.

Vinorelbine solution should be avoided in the eyes.

Contraindications

Side effects

Blood system disorders: granulocytopenia, anemia.

Peripheral nervous system disorders: decrease (up to complete extinction) of osteotendinous reflexes is possible; paresthesias is rare; with long-term use – increased fatigue of the muscles of the lower extremities.

Digestive system disorders: nausea, rarely – vomiting; due to the effect of the drug on vegetative innervation of the intestine – constipation; in some cases – intestinal paresis; rarely – paralytic bowel obstruction.

Allergic reactions: difficulty in breathing, bronchospasm; in isolated cases – skin reactions.

Others: alopecia, pain in the jaw.

Local reactions: phlebitis.

Pregnancy use

It is contraindicated in pregnancy.

If it is necessary to use during lactation, discontinue breastfeeding should be considered.