Vinblastine is an antitumor drug of plant origin, in the chemical formula of which the vinca alkaloid rose pink.
The active substance of this drug is sulphate vinblastine - a powdery fine-grained substance of white( sometimes with a light cream shade) color.
Vinblastine is used to treat patients with malignant neoplasms of various origins and localizations( including chronic leukemia, Hodgkin's disease, non-Hodgkin's lymphomas and testicular cancer).
Composition, form and packaging
Vinblastine is available as a lyophilizate - a lyophilized( obtained by soft drying) powder intended for the preparation of an injection solution. The lyophilizate is packaged in glass bottles( the color of the glass can be orange or neutral), containing 5 or 10 g of the preparation.
One ampoule contains five or ten milliliters of 0.9% isotonic sodium chloride solution( it should not contain any mechanical inclusions).
Packaging is different:
- One bottle( with instruction) can be placed in an individual cardboard box.
- A cardboard bundle, equipped with special plastic pallets or cardboard partitions, can hold five or ten bottles and one instruction on the use of the preparation.
- There are 5 or 10 vials with lyophilizate and 5 or 10 vials with a so-called "solvent" - physiological solution( 0.9% aqueous solution of sodium chloride) inside the cardboard bundle with septums. It is also necessary to put instructions for use, a scarifier( a special plate for opening ampoules) or an ampoule knife. If the ampoules are provided with a fault ring or special incisions, neither the scarifier nor the ampoule knife inside the package is embedded.
- Packaging( box of cardboard), intended for use in hospitals, can accommodate 25, 50, 85 and even 100 bottles. Ampoules with an isotonic solution are not placed in it. Instructions for use are put in the box at a rate of one piece for five bottles.
Vinblastine is produced by specialized companies:
- of the Hungarian pharmaceutical company JSC Gedeon Richter, which has patented the rights to the drug of the Vinblastine-Richter trademark;
- of the Russian production pharmaceutical company LLC "Lance-Farm", which produces the drug "Vinblastine-Lance";
- of the Israeli company Teva Pharmaceutical Industries Ltd., which owns the rights to manufacture the drug Vinblastine-Teva.
Indications for use
Vinblastine is used to treat:
- cancers of the bladder;
- of histiocytosis X( occurring in the form of the Letterter-Sieve disease);
- Malignant neoplasm of the breast;
- kidney cancer;
- with neuroblast;
- of nasopharyngeal tumors;
- of lymphogranulomatosis;
- malignant neoplasms localized in the neck and head;
- generalized stages of mushroom mycosis;
- chorion carcinoma( resistant to other chemotherapeutic agents);
- germinogenic tumors of the ovaries and testes;
- Malignant lung tumors;
- of myeloma;
- of histiocytic lymphoma;
- of Kaposi's sarcoma;
- non-Hodgkin's lymphomas;
- of chronic leukemia.
Vinblastine is contraindicated:
- to patients with pronounced oppression of bone marrow activity;
- for future mothers at any time of pregnancy( exception is made only for patients whose treatment presages a good positive effect exceeding its possible negative effect on the fetus status);
- during the entire lactation period( treatment of a nursing mother with the drug is possible only if the woman refuses to breastfeed during the entire period of therapy);
- for patients with severe hypersensitivity to the active substance;
- in the presence of diseases of infectious and viral etiology.
Particular caution in prescribing vinblastine is required in relation to patients:
- of advanced age;
- with severe liver diseases;
- analyzes of which indicate the presence of thrombocytopenia and leukopenia;
- undergoing a comprehensive treatment, providing simultaneous reception of chemotherapy and radiotherapy sessions. The mechanism of pharmacological action of vinblastine consists in the blockade of tubulin( a protein consisting of microtubules - protein structures that are an integral part of the cell skeleton) and stopping mitosis( the process of cell division) that reached the third stage - metaphase.
Binding to microtubules, the active ingredient of the preparation significantly slows down the formation of dynamic structures called mitotic spindles.
Once inside the patient( through intravenous injection), vinblastine very quickly penetrates into its various tissues, without affecting the structures of the blood-brain barrier( a physiological mechanism regulating the metabolism between the central nervous system, blood and cerebrospinal fluid).
The active active substance of the drug is immediately associated with all the blood elements and blood plasma proteins. Biotransformation of vinblastine in the liver leads to the formation of active metabolites - intermediate products of metabolism in the tissues of cellular structures.
The excretion of vinblastine( mostly along with bile) from the human body occurs in three stages. The mean values of the half-lives are:
- five minutes;
- two hours;
- thirty hours.
A small amount of the drug in the form of metabolites, as well as unchanged, is found in the urine.
Instructions for use Vinblastine: dosage of
Injections of vinblastine are performed exclusively intravenously( jet injection of the drug is carried out for one to two minutes).The introduction of vinblastine in the tissues of the spinal cord( the so-called intrathecal application) is strictly prohibited.
The solution of vinblastine should be freshly prepared: it is prepared only before the introduction into the patient's body. To do this, the contents of one bottle are diluted in five milliliters of isotonic 0.9% sodium chloride solution( the use of any other solutions is prohibited).
The dosage of vinblastine is determined based on the clinical course of the disease, the general condition of the patient, the chemotherapy regimen used, and the number of leukocytes in his blood.
Generally, the adult dosage of the drug is 5 to 7.5 milligrams per square meter of body surface area.
For children, the amount of the drug administered should not exceed five milligrams per m2 of body surface area. The administration of vinblastine is carried out once every seven or fourteen days.
In some cases, the tactic of a gradual and continuous increase in the weekly dosage is applied:
- For adults, the first dose is 3.7 mg / m2.If the white blood cell count is at least 4,000 per unit volume, the weekly dosage is increased by 1.8 mg / m2 until the amount of the drug administered reaches the maximum single dose of 18.5 mg / m2.
- For small patients, the weekly increment of a single dose of 1.25 mg / m2 is carried out in the same way as in adults, with the difference that the initial dose is 2.5 mg / m2 and the maximum single dose is 12,5 mg / m2.
From this point on, they are proceeding with the administration of maintenance doses of vinblastine( once every one or two weeks), the values of which are less than the last initial dosage:
- for adults of - by 1.8 mg / m2;
- for small patients - by 1.25 mg / m2.
If the level of bilirubin in the blood serum exceeds 51 μmol / l, single dose is reduced by 50%.
Side effect of
- Side effect of vinblastine on the hematopoiesis system can often manifest itself in the development of granulocytopenia( the lowest content of granulocytes is observed 6-10 days after the most recent injection, and the restoration of the previous level occurs in the next one or two weeks) and leukopenia;the development of anemia and thrombocytopenia is much less common.
- The negative effect of vinblastine on the organs of the gastrointestinal tract consists in the appearance of nausea, vomiting, abdominal pain, severe diarrhea or persistent constipation( up to paralytic intestinal obstruction), the development of pharyngitis, stomatitis, hemorrhagic enterocolitis, and bleeding in the backgroundalready existing ulcer.
- Side effect of vinblastine on the functioning of the nervous system leads to a significant( until complete loss) reduction of deep tendon reflexes, severe headaches and dizziness, paresthesia, seizures, double vision( diplopia), pain in the jaw zone, general weakness.
- Allergic reactions , provoked by the introduction of vinblastine, are manifested in the development of urticaria and bronchospasm.
- After the injection of vinblastine, a local reaction may occur, manifested in pain and redness of the skin; getting the drug under the skin can become the culprit of inflammation of the subcutaneous fat or venous walls( phlebitis) with possible development of necrosis of the affected tissues. In addition to the aforementioned complications, vinblastine can provoke the development of urinary acid nephropathy, hyperuricemia ( increased uric acid in the blood), alopecia, bone pains, amenorrhea( absence of menstruation for six months) and azoospermia( lack of sperm in the ejaculate).In addition, the patient may have increased blood pressure, and in patients with Raynaud's disease, there is often increased clinical symptoms.
- The administration of increased doses of vinblastine is fraught with the development of the syndrome of inappropriate production of vasopressin ( antidiuretic hormone).
In case of an unexpected overdose, side effects increase. There is no specific antidote.
Symptomatic therapy consists in performing the following actions:
- Patients with developed syndrome of inadequate production of antidiuretic hormone are prescribed diuretics and recommend limiting the use of fluid.
- The functioning of the cardiovascular system is under strict control.
- Blood is also subjected to the same careful monitoring. If necessary, blood transfusion is performed.
- Patients are prescribed anticonvulsants.
- To prevent intestinal obstruction, patients are given laxatives and enemas.
In case of an overdose of vinblastine, hemodialysis( the technique of adrenal cleansing of the blood) is not prescribed, since in this case it is completely ineffective.
- With great care, vinblastine should be used for nephrolithiasis, gout, chicken pox, herpes zoster and other acute infectious diseases.
- Treatment with vinblastine requires strict control of the leukocyte count in the patient's blood. Reducing their number to 3000 / μl is an indication for stopping the use of vinblastine.
- To ensure that the patient receiving vinblastine does not develop urine acid diathesis, it is necessary to regularly monitor the level of uric acid in the blood serum, prescribe the intake of allopurinol and monitor the volume of fluid entering the body.
- During the entire therapeutic course, it is required to monitor the level of hepatic transaminase activity( special enzymes that provide the metabolism inside the cellular structures), the level of bilirubin and lactate dehydrogenase( an enzyme involved in the synthesis of lactic acid and glucose oxidation).
- Symptomatic of neurointoxication indicates the need for discontinuation of treatment.
- It is not recommended to appoint vinblastine to patients suffering from ulcerative skin lesions and cachexia because of the high risk of developing leukopenia.
- The use of even moderate doses of vinblastine against patients with metastases to the bone marrow can cause a sharp decrease in the number of platelets and white blood cells. If this occurs, the drug should be discontinued immediately.
- In case of accidental ingestion of vinblastine into subcutaneous tissues( extravasation), an extremely painful local reaction and tissue necrosis may develop. If this happens, the remedy is injected into another vein;In the tissue of the affected area, it is necessary to introduce hyaluronidase.
- Vinblastine, accidentally caught in the eyes, can cause significant irritation or ulceration of the cornea, so they must be rinsed immediately with plenty of running water.
- It is pointless to vaccinate patients and their family members during treatment with vinblastine.
- When taking vinblastine treatment, you will have to refrain from engaging in certain activities that could be potentially dangerous, for which the speed of psychomotor reactions is required and the high concentration of attention, as well as the driving of any vehicles.
- It is undesirable to administer vinblastine to the vein of the limb, the circulation of which was disturbed.
- Intrathecal( intrathecal) administration of the drug is fraught with a lethal outcome.
It is forbidden to co-administer vinblastine with neurotoxic drugs( typical representatives of this drug group are L-asparaginase and isoniazid).
Special caution requires the joint use of vinblastine and:
- Phenytoin is an antiepileptic drug that exerts an anticonvulsant action and is used as a muscle relaxant and antiarrhythmic agent. The effect of vinblastine, which reduces the presence of phenytoin in the blood, can negate the anticonvulsant activity of this drug.
- Antifungal drugs. Under the influence of vinblastine, the toxicity of these medications can be significantly increased.
- Combinations of two drugs: cisplatin and bleomycin. The combined effect of these three potent agents can trigger circulatory disorders in the brain tissues and myocardial infarction.
- Medicines containing platinum. In combination with vinblastine, these drugs pose a threat to the eighth pair of CHMN( cranial nerves).
With great difficulty - through intermediaries - got the drug Vinblastine Richter, paying for it a very decent amount. The result was not only disappointing, but also cast down discouragement. Instead of the expected improvement, blood tests have sharply deteriorated - they show a significant reduction in the number of leukocytes.
The attending physician, trying to calm, says that this is a common phenomenon, indicating the need for temporary replacement of the drug. Personally, I was just unsettled by such news. Spent so much money, and the result was zero.
After the application of vinblastine, there was a sharp decrease in white blood cells in my blood. I read the annotation to the drug and made sure that this is a typical picture. My attending physician also took it calmly and temporarily canceled the introduction of this medicine. Now I am concerned with finding medicines and ways to help restore the level of leukocytes.
Price Vinblastine in Moscow
The cost of the drug in pharmacies in Moscow is listed below:
- Packing with one bottle of antitumor preparation Vinblastine-Teva, containing 10 mg of lyophilized powder for the preparation of an injection solution - 1450 rubles.
- Cardboard pack with one bottle( 5 mg) of Vinblastine-Lance preparation - 196 rubles.
- Packing of Vinblastine-Richter preparation containing ten bottles( 5 mg each) with lyophilizate and ten ampoules with 0.9% sodium chloride solution - 9980 rubles.
Similar drugs have medicines:
Vinblastine has several synonymous names: "Vinblastine sulfate", "Vinblastine-Lance", "Vinblastine-Richter" and "Vinblastine-Teva".
To store vinblastine, a darkened cool place( with a temperature of 2 to 8 degrees), which excludes light and is completely inaccessible to small children, is necessary.
Shelf life of the lyophilized powder is 24 months, the ampoule solvent is five years.
On the lid of a cardboard pack containing a vial of lyophilizate and ampoules with a solvent, always indicate the shelf life of sulphate of vinblastine. Admission of an overdue product poses a risk to the patient's health.