Vinblastine-Richter is an alkaloid isolated from a plant of the genus Vinca (periwinkle).
Pharmacological properties
Vinblastine blocks mitotic cell division in the metaphase of the cell cycle. It acts by binding to microtubules by inhibiting the formation of mitotic spindles. In tumor cells, it selectively inhibits the synthesis of DNA and RNA by inhibiting DNA-dependent RNA polymerase.
Pharmacokinetics
After intravenous administration, it is rapidly distributed in tissues. Does not penetrate the blood-brain barrier. The connection with proteins is 80%. Metabolized in the liver. It is excreted from the body in three phases T1 / 2 with a duration (average values) of 3.7 min, 1.6 h and 24.8 h, respectively, mainly with bile. A small amount of unchanged vinblastine and in the form of metabolites is determined in the urine.
Indications for use
Indications for the use of the drug Vinblastine-Richter are: Hodgkin's disease; non-Hodgkin lymphomas; chronic lymphocytic leukemia; germ cell tumors of the testicle and ovaries; bladder cancer; Kaposi's sarcoma; Letterer-Siwe disease (histiocytosis X); fungal mycosis (generalized stages).
Mode of application
A drug Vinblastine-Richter intended exclusively for intravenous administration (extravasation should be avoided).
Do not administer intrathecally!
The dose is selected taking into account the individual characteristics of the patient and the chemotherapy regimen used, guided by the data of special literature.
The usual dose is: adults 5.5-7.4 mg / m2 body surface, children 3.75-5 mg / m2 body surface.
The drug is administered 1 time / week or 1 time / 2 weeks.
They can also use the modes of gradually increasing weekly doses:
Adults: 1st dose - 3.7 mg / m2, each subsequent weekly dose with a leukocyte count of at least 4000 cells / μL of blood increases by 1.8-1.9 mg / m2 until a maximum single dose of 18.5 mg / m2 is reached.
Children: a weekly dose increase of 1.25 mg / m2 is carried out according to the same principle as in adults, starting with an initial dose of 2.5 mg / m2 and up to a maximum dose of 12.5 mg / m2.
Doses are increased until the leukocyte count drops to 3,000 cells / μL, or the tumor size decreases, or the maximum single dose is reached, after which they switch to maintenance doses that are 1.8- less than the final value of the last dose for adults. 1.9 mg / m2 and for children at 1.25 mg / m2. Maintenance doses are administered once every 7-14 days.
When the level of bilirubin in the blood serum is above 3 mg / 100 ml (50 μmol / L), a dose reduction of 50% is recommended.
A freshly prepared solution is used, for which the contents of the vial with the lyophilized powder are dissolved in the supplied solvent.
Immediately before administration, the drug, if necessary, can be diluted with 0.9% sodium chloride solution (other solutions are not recommended) to a concentration of 1 mg / 1 ml.
Side effects
On the part of the hematopoietic system: most often leukopenia, granulocytopenia (the lowest level of granulocytes is observed 5-10 days after the last injection, complete recovery usually occurs within the next 7-14 days); less often thrombocytopenia, anemia.
From the digestive system: stomatitis, pharyngitis, decreased appetite, nausea, vomiting, constipation, diarrhea, abdominal pain, paralytic intestinal obstruction, hemorrhagic enterocolitis, bleeding from previously diagnosed ulcers of the gastrointestinal tract.
From the side of the central nervous system and peripheral nervous system: paresthesias, decrease or loss of deep tendon reflexes, peripheral neuritis, depression, headache, convulsions, dizziness, diplopia, weakness, pain in the jaw, neuritis of the VIII pair of cranial nerves (partial or complete deafness , dizziness, nystagmus).
From the side of the cardiovascular system: increased blood pressure, myocardial ischemia, incl. angina pectoris or myocardial infarction (usually with simultaneous use with bleomycin and cisplatin), microangiopathy (Raynaud's syndrome with simultaneous use of bleomycin).
From the respiratory system: bronchospasm (usually when used simultaneously with mitomycin) with acute respiratory failure, cyanosis, shortness of breath and often with the formation of pulmonary infiltrates and pneumonitis.
Dermatological reactions: alopecia, urticaria.
Local reactions: pain or redness at the injection site, phlebitis, if the drug gets under the skin - inflammation of the subcutaneous fat and, possibly, necrosis.
Others: hyperuricemia, uric acid nephropathy, weakness, fatigue, myalgia, ossalgia, pain in the area of tumor nodes, azoospermia and amenorrhea (sometimes irreversible).
Contraindications
Contraindications to the use of the drug Vinblastine-Richter are: pronounced inhibition of bone marrow function; bacterial and viral infections; pregnancy and lactation; hypersensitivity to vinca alkaloids and to the components of the drug.
With caution: recent or concurrent myelosuppressive chemotherapy or radiotherapy, leukopenia, thrombocytopenia, liver dysfunction, hyperuricemia, old age.
Pregnancy
A drug Vinblastine-Richter contraindicated for use during pregnancy and during breastfeeding.
Interaction with other medicinal products
The simultaneous use of neurotoxic drugs (isoniazid, L-asparaginase) is prohibited.
Caution should be exercised with the simultaneous use of ototoxic drugs.
With simultaneous use with mitomycin, caution should be exercised due to the possible development of acute bronchospasm.
When taken simultaneously with vinblastine, the plasma concentration of phenytoin decreases, which can lead to a decrease in its anticonvulsant activity.
With simultaneous use with bleomycin, Raynaud's syndrome may develop.
When using vinblastine in combination with bleomycin and cisplatin, there have been cases of myocardial infarction, cerebrovascular accident.
When used in combination with drugs containing platinum, the risk of damage to the VIII pair of cranial nerves increases.
Anti-gout medicines (allopurinol, colchicine, probenicid, sulfinpyrazone) can cause an increase in the level of uric acid in the blood; it may be necessary to adjust their doses in order to prevent the development of hyperuricemia; for the prevention and treatment of hyperuricemia caused by vinblastine, it is preferable to use allopurinol in order to avoid the development of acute uric acid nephropathy as a result of the use of uricosuric anti-gout drugs.
The thrombocytopenic and leukopenic effects of vinblastine are enhanced by drugs, which, in turn, are also capable of exerting similar effects if their use is carried out simultaneously with vinblastine or precedes it; the dose of vinblastine may need to be adjusted according to the blood picture.
The interval between stopping treatment with vinblastine and vaccination with an attenuated or live viral vaccine depends on the type and degree of drug immunosuppression, the underlying disease and other factors and lasts 3-12 months.
Overdose
Overdose symptoms Vinblastine-Richter: development of side effects in a more pronounced form.
Treatment: there is no specific antidote, symptomatic and supportive therapy is performed.
The following measures are recommended: with the development of a syndrome of inadequate secretion of antidiuretic hormone - limited fluid intake and the appointment of diuretics; the appointment of anticonvulsants; control over the function of the cardiovascular system; careful monitoring of the blood picture, if necessary - blood transfusion; the use of enemas and laxatives (prevention of intestinal obstruction).
Hemodialysis is ineffective with Vinblastine overdose.
Storage conditions
A drug Vinblastine-Richter should be stored at a temperature of 2-8 ° C in a dark place out of the reach of children.
Release form
Vinblastine-Richter - lyophilisate for preparing a solution for intravenous administration. In dark glass vials, complete with solvent in 5 ml ampoules; 10 sets in a box.
Composition
1 bottle Vinblastine-Richter contains: vinblastine sulfate 5 mg.
Solvent: 0.9% sodium chloride solution - 5 ml.
Additionally
Treatment can only be carried out under the supervision of a physician experienced in the use of anticancer chemotherapy.
Make sure the needle is in the vein before starting the injection. In case of extravasation of the drug, its administration should be stopped immediately; the remaining solution with the drug must be injected into another vein. It is recommended to inject hyaluronidase into the affected area.
During treatment, regular monitoring of the number of leukocytes, platelets and hemoglobin levels is necessary.
With a decrease in the number of leukocytes to 3000 cells / μl, treatment should be discontinued.
In the course of treatment, it is also necessary to control the activity of liver enzymes and the content of bilirubin in the blood serum.
If signs of neurotoxicity appear, treatment with the drug should be discontinued.
To avoid acute uric acid nephropathy, serum uric acid levels should be monitored regularly and adequate fluid intake should be ensured. It is recommended to prescribe allopurinol if necessary.
Women of childbearing age need to use non-hormonal reliable methods of contraception during treatment with vinblastine.
It is forbidden to vaccinate with a live viral vaccine of patients undergoing treatment with Vinblastine-Richter.
In case of accidental eye contact, immediately rinse thoroughly with water to prevent severe irritation or possible ulceration of the cornea.
Some side effects of the drug (neurotoxicity) can adversely affect the ability to drive and perform potentially hazardous activities that require increased concentration and psychomotor speed. In this regard, care should be taken when driving vehicles and mechanisms.
main parameters
| Name: | VINBLASTIN RICHTER |
| ATX code: | L01CA01 - |
Vinblastine (Vinblastin) - an effective antineoplastic agent of plant origin. The active substance of the drug is an alkaloid obtained by extract from pink periwinkle.
It is able to inhibit the division of a cancer cell in the metaphase, and thereby stop the progression of the disease. The medication is used to treat cancer of various localization.
About manufacturers
Medicines based on Vinblastine are produced by pharmaceutical companies in different countries:
- Hungary - the company Gedeon Richter, produced under the trade name "Vinblastine-Richter";
- Israel - corporation Teva Pharmaceutical Industries LTD, TM Vinblastin-Teva;
- Russia - Lens-Pharm company, TM Vinblastin-Lance.
Instructions for use
You should carefully study the instructions before starting the treatment recommended by the doctor, because it contains important information about the peculiarities of taking the medicine.
Release form
Lyophilized powder for the preparation of a medicinal solution.
Description and composition
Vinblastine is a dry powder of white or light cream color. The active substance is prepared by lyophilization, a soft drying method. The powder is packed in glass bottles of 5 or 10 mg. The active ingredient is not supplemented with any other ingredients.
Immediately before injection, the powder is diluted with saline.
Depending on the manufacturer, the number of vials and the complete set of the medication differ. Vials are placed in a cardboard box of 1, 5, 10 pieces. Possible complete set with solvent (ampoules with saline solution) and ampoule knife.
Pharmacological classification
Refers to herbal anticancer medicines, cytostatic agents (cytostatics).
Pharmacodynamics
The active substance binds to tubulin, a protein from which microtubules are built. When interacting, it inhibits the formation of dynamic structures - mitotic spindles, thereby blocking the process of mitosis (indirect cell division) in the metaphase stage.
Pharmacokinetics
After entering the bloodstream, it binds to proteins. Bioavailability is 75%. In the liver, it turns into metabolites, which are then excreted along with bile.
The half-life is divided into 3 phases, the duration of which is:
- 3.7 minutes;
- 1.6 h;
- 24.8 hrs
Information on the main active ingredient
The plant alkaloid in the form of sulfate is obtained from periwinkle pink, belonging to the genus of creeping dwarf shrubs of the Kutrov family. Vinblastine can also be isolated from pink catharanthus. Preparations based on this substance, along with vincristine and vinorelbine, are classified as vital medicines.
Indications for use
They are used to treat various types of oncology:
- cancer of the breast, ovary, cervix, bladder, placenta, testicle, nasopharynx, lungs, kidneys;
- lymphogranulomatosis;
- chorionic carcinoma;
- Kaposi's sarcomas;
- neuroblastoma;
- histiocytosis X;
- myeloid leukemia;
- follicular non-Hodgins lymphoma;
- generalized fungal mycosis;
- cancer localized in the neck and head.
Contraindications
The medicine is not prescribed to the following patients:
- having severe disorders of the spinal function;
- with hypersensitivity to the active substance;
- throughout pregnancy and lactation;
- in the presence of acute infections.
Patients who suffer from:
- severe liver pathologies;
- thrombocytopenia;
- leukopenia;
- age-related changes in health (advanced age).
Application and dosage
Injections are given once a week. The medicine is prepared just before the procedure. The powder is diluted exclusively with saline. Before preparing the product, it is necessary to check the purity of the saline solution - it should not contain any inclusions.
An anticancer drug is injected into a vein by a jet method, within one to two minutes. No other application is allowed.
The dosage is determined on an individual basis. The doctor focuses on the type of oncology, features of the clinical course of the disease, age, general well-being of the patient, blood tests, concomitant treatment.
The dose is calculated from the ratio of the amount of active substance per area of the human body. The standard adult dosage is 5 - 7.5 mg / m2, for children - from 4 to 5 mg / m2.
Therapy regimen with a gradual dose increase:
- For adults, the initial dosage is 3.7 mg / m2, with a subsequent increase of 1.8 mg / m2 with each injection. During therapy, blood is taken from the patient and the effectiveness of the therapeutic dose is determined. The maximum value should not exceed 18.5 mg / m2. Supportive therapy is carried out at a dosage lower than the most effective by 1.8 mg / m2.
- For children, the initial dose is 2.5 mg / m2, followed by an increase of 1.25 mg / m2 and a maximum concentration of 12.5 mg / m2.
With an increase in the concentration of bilirubin in the blood, the dosage is adjusted downward.
Side effects
During therapy, disturbances may occur from the work of the gastrointestinal tract, nervous system, heart, blood vessels, blood system.
The most common negative reactions are:
- nausea, upset stool, abdominal pain, stomatitis;
- increased blood pressure, problems with cerebral circulation;
- migraine, dizziness, convulsions, depression;
- bronchospasm, urticaria;
- general weakness, loss of appetite, nosebleeds, photophobia, tissue inflammation at the injection site.
There are more severe manifestations in the form of the development of peripheral neuritis, hemorrhagic enterocolitis, jaundice, myocardial infarction, blood diseases, cranial nerve damage, bleeding from the gastrointestinal tract.
Interaction with other medicinal products
- Mitomycin combined with Vinblastine increases the risk of severe bronchospasm.
- With the use of myelodepressants or with the simultaneous passage of radiation therapy, unwanted reactions from the circulatory system increase.
- The combined course with bleomycin and cisplatin can lead to myocardial infarction.
- Vinblastine reduces the effect of anticonvulsants.
Alcohol compatibility
In order to reduce the risk of side effects, it is not recommended to consume alcohol during therapy.
special instructions
The medication should be carefully used to treat elderly patients.
During therapy, it is necessary to constantly examine blood counts.
It is highly undesirable to prescribe an anticancer drug in combination with radiation therapy.
Before directly administering the medication, you must make sure that the needle is in the vein. In case of extravasation, the needle must be removed and the remaining medication injected into another vein. It is recommended to inject hyaluronidase into the affected area.
Overdose
Injections should be done under the supervision of an experienced oncologist. When the dose is exceeded in humans, peripheral nerves are affected, serious blood disorders occur, and a coma may occur. Treatment should be carried out in a hospital. In some cases, a blood transfusion may be required.
Storage conditions
Anticancer medication must be stored at a temperature in the range from 2 to 8 ° C. It is necessary to exclude access to medicine for small children.
Shelf life
2 years from the date of production if stored properly.
Termination of therapy
Treatment is completed when a stable therapeutic effect is achieved, or with the development of severe health complications.
Analogs
Structural analogues of Vinblastine are:
- Vinblastine sulfate;
- Vinblastine-LENS;
- Welbe;
- Vero-Vinblastine aqueous;
- Vinblastine-Richter.
Medicines differ by brand name, manufacturer and country in which they are manufactured. European drugs are of a higher quality due to the system for purifying drugs from harmful impurities. This guarantees a lower likelihood of side effects and high treatment success.
Price and where to buy
Vinblastine is produced in Russia. The drug can be bought in large pharmacies in Moscow and St. Petersburg. You can also use the services of intermediaries and purchase a quality anticancer agent in Europe - Hungary, Germany and other countries.
One bottle of the drug containing 10 ml costs about 185 euros. When buying several bottles, a system of discounts applies.
Vinblastine is an anticancer drug of plant origin, the chemical formula of which includes the alkaloid of pink vinca.
The active ingredient of this drug is vinblastine sulfate - a powdery fine-crystalline substance of white (sometimes with a light cream shade) color.
Vinblastine is used to treat patients with malignant neoplasms of various origins and localization (including chronic leukemia, Hodgkin's disease, non-Hodgkin's lymphomas and testicular cancer).
Composition, release form and packaging
Vinblastine is produced in the form of a lyophilisate - a lyophilized (obtained by soft drying) powder intended for obtaining an injection solution. The lyophilisate is packaged in glass vials (glass color can be orange or neutral), containing 5 or 10 g of the drug.
One vial of the drug contains five or ten milligrams of vinblastine (without any excipients).
One ampoule contains five or ten milliliters of 0.9% isotonic sodium chloride solution (it should not contain any mechanical impurities).
The package contents are different:
- One bottle (with instructions) can be placed in an individual cardboard box.
- A cardboard box equipped with special plastic pallets or cardboard partitions can hold five or ten bottles and one instruction for use of the drug.
- Inside a cardboard box with partitions, there can be 5 or 10 vials with lyophilisate and 5 or 10 ampoules with the so-called "solvent" - saline (0.9% aqueous sodium chloride solution). Instructions for use, a scarifier (a special plate for opening ampoules) or an ampoule knife must be included here. If the ampoules are equipped with a break ring or special notches, neither the scarifier nor the ampoule knife is inserted into the package.
- Packaging (box made of thick cardboard) intended for use in hospitals can hold 25, 50, 85 and even 100 vials. Ampoules with isotonic solution are not placed in it. Instructions for use are included in the box at the rate of one per five vials.
Manufacturers
Vinblastine is produced by specialized enterprises:
- the Hungarian pharmaceutical company Gedeon Richter OJSC, which has patented the rights to the Vinblastine-Richter drug;
- the Russian manufacturing pharmaceutical company LLC Lance-Pharm, which produces the drug Vinblastine-Lance;
- 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:
- histiocytosis X (occurring in the form of Letterera-Siwe disease);
- malignant neoplasms localized in the neck and head;
- generalized stages of fungal mycosis;
- (immune to the effects of other chemotherapeutic agents);
- germ cells and;
- malignant;
Contraindications
Taking vinblastine is contraindicated:
- patients with pronounced bone marrow suppression;
- expectant mothers at any stage of pregnancy (an exception is made only for patients whose treatment portends a good positive effect that exceeds its possible negative effect on the condition of the fetus);
- during the entire period of lactation (treatment of a nursing mother with a drug is possible only if the woman refuses to breastfeed the baby throughout the entire period of therapy);
- 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:
- old age;
- with severe liver pathologies;
- analyzes of which indicate the presence of thrombocytopenia and leukopenia;
- undergoing complex treatment, including the simultaneous administration of chemotherapy and radiation therapy sessions.
pharmachologic effect
The mechanism of the pharmacological action of vinblastine consists in blocking tubulin (the protein that makes up microtubules - protein structures that are an integral part of the cell skeleton) and stopping mitosis (the process of cell division), which has reached the third stage - metaphase.
By binding to microtubules, the active ingredient of the drug significantly slows down the formation of dynamic structures called mitotic spindles.
In cancer cells, under the influence of vinblastine, the production of RNA and DNA is suspended by inhibition of the RNA-dependent enzyme, polymerase.
Once in the patient's body (through intravenous injection), vinblastine very quickly penetrates into his various tissues without affecting the structures of the blood-brain barrier (the physiological mechanism that regulates the metabolism between the central nervous system, blood and cerebrospinal fluid).
The active active ingredient of the drug immediately binds to all blood cells and blood plasma proteins. Biotransformation of vinblastine in the liver leads to the formation of active metabolites - intermediate metabolic products in the tissues of cellular structures.
The elimination of vinblastine (mostly together with bile) from the human body occurs in three stages. The average 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 the use of Vinblastine: dosage
Vinblastine injections are performed exclusively intravenously (jet injection of the drug is carried out for one to two minutes). The introduction of vinblastine into the tissue of the spinal cord (the so-called intrathecal application) is strictly prohibited.
The vinblastine solution must be freshly prepared: it is prepared only before being introduced 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 characteristics of the clinical course of the disease, the general condition of the patient, the chemotherapy regimen used and the number of leukocytes in his blood.
Typically, the adult dosage is 5 to 7.5 milligrams per square meter of body surface.
For children, the amount of the injected drug should not exceed five milligrams per m2 of body surface. The introduction 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 used:
- For adult patients, the first dose is 3.7 mg / m 2. If the content of leukocytes in the blood is at least 4000 per unit volume, the weekly dosage is increased by 1.8 mg / m 2 until the amount of the injected drug reaches the maximum single dose of 18.5 mg / m 2.
- For small patients, a weekly increase in a single dosage by 1.25 mg / m 2 is carried out according to the same scheme as in adult patients, with the only difference that the initial dose is 2.5 mg / m 2, and the maximum single dose is 12 , 5 mg / m 2.
The increase in single doses is carried out until either the content of leukocytes in the blood reaches the level of 3000 / mm 3, or the size of the malignant neoplasm does not begin to decrease, or the maximum single dosage is reached.
From this moment, they switch to the introduction of maintenance doses of vinblastine (once every one or two weeks), the value of which is less than the last initial dosage:
- for adult patients- by 1.8 mg / m 2;
- for small patients- by 1.25 mg / m 2.
If the level of bilirubin in the blood serum exceeds 51 μmol / L, the single dosage is reduced by 50%.
Side effect
- Side effects of vinblastine on the hematopoietic system most often it can 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 to two weeks) and leukopenia; the development of anemia and thrombocytopenia is observed much less frequently.
- The negative effect of the effects 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, as well as bleeding against the background of an existing ulcer.
- Side effects of vinblastine on the functioning of the nervous system leads to a significant (up to complete loss) decrease in deep tendon reflexes, severe headaches and dizziness, paresthesia, seizures, double vision (diplopia), pain in the jaw area, general weakness.
- Allergic reactions, provoked by the introduction of vinblastine, are manifested in the development of urticaria and bronchospasm.
- After an injection of vinblastine, a local reaction may occur, manifested in pain and redness of the skin; if the drug gets under the skin can become the culprit of inflammation of the subcutaneous fat or venous walls (phlebitis) with the possible development of necrosis of the affected tissues.
- In addition to the above complications, vinblastine can provoke the development of uric acid nephropathy, hyperuricemia (increased uric acid in the blood), alopecia, bone pain, amenorrhea (absence of menstruation for six months) and azoospermia (absence of sperm in the ejaculate). In addition, the patient may have an increase in blood pressure, and in patients with Raynaud's disease, an increase in clinical symptoms is often observed.
- Prescribing high doses of vinblastine is fraught with the development of a syndrome of inadequate production of vasopressin.(antidiuretic hormone).
Overdose
In case of an unexpected overdose, side effects increase. There is no specific antidote.
Symptomatic therapy consists in performing the following actions:
- Patients with advanced syndrome of inadequate antidiuretic hormone production are prescribed diuretics and are advised to limit fluid intake.
- The functioning of the cardiovascular system is taken under strict control.
- The characteristics of the blood are subjected to the same careful control. 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 (a method of extrarenal blood purification) is not prescribed, since in this case it is completely ineffective.
special instructions
- Vinblastine should be used with great care in nephrolithiasis, gout, chickenpox, herpes zoster and other acute infectious diseases.
- Vinblastine treatment requires strict control of the patient's leukocyte count. A decrease in their number to 3000 / μl is an indication for stopping the administration of vinblastine.
- To prevent the development of uric acid diathesis in a patient taking vinblastine treatment, it is necessary to regularly monitor the level of uric acid in the blood serum, prescribe allopurinol and control the volume of fluid entering the body.
- During the entire therapeutic course, it is required to control the level of activity of hepatic transaminases (special enzymes that ensure metabolism within cellular structures), the level of bilirubin and lactate dehydrogenase (an enzyme involved in the synthesis of lactic acid and glucose oxidation).
- Symptoms of neurointoxication indicate the need to discontinue treatment.
- It is not recommended to prescribe vinblastine to patients suffering from ulcerative skin lesions and because of the high risk of developing leukopenia.
- The use of even moderate doses of vinblastine in relation to patients with metastases to the bone marrow can cause a sharp decrease in the number of platelets and leukocytes. If this happens, treatment with the drug should be stopped immediately.
- If vinblastine accidentally gets into the subcutaneous tissue (extravasation), an extremely painful local reaction and tissue necrosis can develop. If this happens, the remainder of the drug is injected into another vein; hyaluronidase must be injected into the tissue of the affected area.
- Vinblastine accidentally splashed into the eyes can cause significant irritation or ulceration of the cornea, so they must be rinsed immediately with plenty of running water.
- It makes no sense to vaccinate patients and family members living with them during treatment with vinblastine.
- Taking treatment with vinblastine, you will have to refrain from engaging in certain activities that can be potentially dangerous, which require quick psychomotor reactions and high concentration of attention, as well as from driving any vehicles.
- It is undesirable to inject vinblastine into a vein of a limb, in which blood circulation has been impaired.
- Intrathecal (intrathecal) administration of the drug is fraught with death.
Drug interactions
Co-administration of vinblastine with neurotoxic drugs is prohibited (typical representatives of this drug group are L-asparaginase and isoniazid).
The combined use of vinblastine and:
- Phenytoin is an antiepileptic drug that has an anticonvulsant effect and is used as a muscle relaxant and antiarrhythmic agent. Exposure to vinblastine, which reduces the presence of phenytoin in the blood, may negate the anticonvulsant activity of this drug.
- Anti-gout drugs. Under the influence of vinblastine, the toxicity of these medications can increase significantly.
- Combinations of two drugs: cisplatin and bleomycin. The combined effect of these three potent agents can provoke circulatory disorders in the tissues of the brain and myocardial infarction.
- Medicines containing platinum. In combination with vinblastine, these drugs pose a threat to the eighth pair of cranial nerves (cranial nerves).
Manufacturer: Richter AG (Hungary)
International name:
Vinblastine
Group affiliation:
Antineoplastic agent, alkaloid
Description of the active substance (INN):
Vinblastine
Dosage form:
concentrate for preparation of solution for intravenous administration, lyophilisate for preparation of solution for intravenous administration
Pharmachologic effect:
Antineoplastic agent Vinblastine of plant origin, affecting the metabolism of amino acids. The mechanism of action is associated with the denaturation of tubulin, which leads to the blockade of mitosis. Suppresses cell division at the metaphase stage, leads to atypical mitotic processes.
Indications:
Lymphogranulomatosis, lymphocytic lymphoma, lymphosarcoma, reticulosarcoma, non-Hodgkin's lymphoma, histiocytic lymphoma, chronic leukemia, fungal mycosis, germ cell tumor of testicles, germ cell tumor of the ovary, chorionepithelioma, myeloma-sarcoma, neural cell carcinoma, urinary tract cancer , lung cancer.
Contraindications:
Hypersensitivity to vincoalkaloids, acute infectious diseases of a viral, fungal or bacterial nature (including chickenpox, shingles), severe depression of bone marrow function (leukopenia - the number of leukocytes is below 4 thousand / μl, granulocytopenia - less than 750 / μl, thrombocytopenia - platelet count below 120 thousand / μl, infiltration of bone marrow with tumor cells), pregnancy, lactation. With caution. Hyperbilirubinemia, obstructive jaundice, inhibition of bone marrow hematopoiesis (including against the background of concomitant radiation or chemotherapy), hyperuricemia (especially manifested by gout or urate nephrourolithiasis), hepatic insufficiency (doses are reduced), old age.
Side effects:
From the side of hematopoiesis: leukopenia, granulocytopenia, anemia, thrombocytopenia. From the digestive system: decreased appetite, nausea, vomiting, diarrhea, abdominal pain, paralytic intestinal obstruction, stomatitis, hemorrhagic enterocolitis, gastrointestinal ulcers, bleeding from the gastrointestinal tract. From the nervous system: paresthesia of the fingers, decreased deep tendon reflexes, peripheral neuritis, depression, headache, convulsions, dizziness, neuritis of the VIII pair of cranial nerves (deafness, dizziness, nystagmus). From the CVS: increased blood pressure, myocardial infarction, cerebrovascular accident, Raynaud's disease (increased symptoms). From the respiratory systems: acute respiratory failure, bronchospasm, progressive shortness of breath, pharyngitis. From the endocrine system: impaired secretion of ADH. Others: alopecia, asthenia, ossalgia, jaw pain, skin ulceration, azoospermia, photophobia, nosebleeds. Local reactions: inflammation, phlebitis and necrosis at the injection site. Overdose. Symptoms: leukopenia, peripheral nerve damage, convulsions, coma. Treatment: there is no specific antidote. As symptomatic therapy, the following measures are recommended: reducing the introduction of fluids and prescribing diuretics. Prescribing antiepileptic drugs. The use of enemas and laxatives drugs. Monitoring the activity of the CVS, for the indicators of the picture of peripheral blood, if necessary - blood transfusion. Hemodialysis is ineffective.
Method of administration and dosage:
Vinblastine IV, IV drip, 1 time per week. The dose is selected individually, taking into account the nature of the disease, the sensitivity of the patient (the degree of decrease in the number of leukocytes). The initial dose for adults is 0.025-0.1 mg / kg (3.7 mg / m2). The number of leukocytes is monitored daily: in the absence of a decrease in them below 2-3 thousand / μl in a week, repeat the injection at a dose of 0.15 mg / kg (if the number of leukocytes is at least 4 thousand / μl - on the 7th day after injection). In the future, in the absence of leukopenia, a single dose can be increased to 0.2 mg / kg. It is necessary to observe a 7-day interval between injections and carefully monitor the number of leukocytes. After the therapeutic effect is achieved, a maintenance dose of 0.15 mg / kg is prescribed, which is administered every 7-14 days until the symptoms are completely eliminated. If the number of leukocytes is less than 3 thousand / μl, it is necessary to interrupt treatment and prophylactically prescribe antibiotics. Another scheme of administration is possible: the initial dose is 0.025-0.1 mg / kg. Further, with daily monitoring of the number of leukocytes, they are injected every day at a dose of 2.5 mg, increasing to 5 mg (but not more). In this case, the therapeutic effect is achieved within 2-3 days. After the normalization of the number of leukocytes, treatment can be continued at a lower dose. Children - once a week at 0.075 mg / kg (2.5 mg / m2). The second dose is administered after the normalization of the number of leukocytes (usually 3-10 days). If the first dose did not cause a decrease in the number of leukocytes, the dose is increased to 0.1, 0.15, 0.2 mg / kg. With an increase in the concentration of direct bilirubin above 3 mg%, the dose is reduced by 2 times. A freshly prepared solution is used, for which the contents of the ampoule are diluted immediately before administration in 5 ml of 0.9% NaCl solution.
Special instructions:
Application during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. If necessary, the appointment of the drug during lactation should stop breastfeeding. Vinblastine can only be administered intravenously. Vinblastine should be used with extreme caution in elderly patients due to possible hypersensitivity to the drug. If the drug enters the paravenous soft tissues, the needle must be removed, after which the injection should be carried out into another vein. The symptoms of inflammation that have arisen at the site of the paravenous injected drug disappear within a few days. During treatment, it is necessary to monitor the number of leukocytes in the peripheral blood daily. In the case of severe leukopenia (less than 3 thousand / μl), it is advisable to take a break in the use of vinblastine. It is not recommended to inject into the vessels of the limb with impaired blood circulation. During the treatment period, it is necessary to determine the hematocrit, Hb, platelets, the activity of AST, ALT, LDH, bilirubin, uric acid.
Interaction:
Vinblastine should not be prescribed against the background of radiation therapy or the use of myelotoxic drugs (mutual enhancement of myelotoxic action), with the exception of special chemotherapy programs. With simultaneous use, it reduces the effect of antiepileptic drugs (for example, phenytoin). Caution is required in the case of combined administration with other potentially ototoxic drugs (for example, containing Pt). Allopurinol, colchicine, sulfinpyrazone, tubular secretion blockers increase the risk of uric acid nephropathy (increased formation of uric acid during treatment), which requires correction of doses of anti-gout drugs. The most preferred drug for preventing or eliminating hyperuricemia during vinblastine therapy is allopurinol. Myelodepressants and radiation therapy increase bone marrow suppression. Inactivated and live viral vaccines - the interval between stopping the use of vinblastine and restoring the ability to respond to the vaccine depends on the dose, underlying disease, and other factors and varies from 3 to 12 months.
Analogues for the current in-vu:
Vinblastine
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