How to relieve pain after vincristine. Use of the drug vincristine in the treatment of transmissible venereal sarcoma in dogs. Use during pregnancy


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Vincristine is an alkaloid cytotoxic drug that is obtained from periwinkle Vinca rosea L. It is included in the list of vital and essential medicines. It is used for treatment various types leukemia and solid tumors. Vincristine can also be used for non-oncological diseases.

  • Active substance: vincristine sulfate.
  • Pharmacotherapeutic group: Antineoplastic agent. Alkaloid plant origin.
  • ATS code: L01C A02.
  • Release form: lyophilisate for solution for injection.
  • Storage conditions: Store vials at 2-8 °C.
  • Terms of sale: on prescription.

Indications for use

Vincristine is prescribed for:

  • (for example, in combination therapy of acute lymphoblastic leukemia in children);

According to the instructions, Vincristine may be used in chemotherapy to treat:

  • , ureter, ;
  • Williams tumors;
  • neuroblastoma;
  • ependymomas;
  • malignant tumors on the genitals in girls;
  • idiopathic thrombocytopenic purpura, resistant to glucocorticosteroids, as well as in cases where splenectomy had no effect.

Contraindications

Vincristine is not prescribed to patients with:

  • high sensitivity to vinca alkaloids;
  • acute infectious diseases of fungal, viral or bacterial origin;
  • severe bone marrow suppression;
  • neurodystrophic pathologies.

Also, the drug should not be prescribed to patients who receive radiation to the liver area.

Vincristine is used with extreme caution if the patient has obstructive jaundice, hyperbilirubinemia, or suppression of bone marrow hematopoiesis after radiation therapy, against the background of hyperuricemia and liver failure.

Taking Vincristine during pregnancy and lactation

The drug can penetrate into breast milk. Do not breastfeed while undergoing therapy!

There is positive evidence that vincristine has teratogenic properties, so it should only be used during pregnancy. emergency situations, when there is a danger to the mother’s life and there is no safer drug.

pharmachologic effect

After entering the bloodstream, Vincristine binds to the protein tubulin, affecting the synthesis of DNA and RNA of tumor cells. The drug disrupts the formation of mitotic spindles, which stop the replication of cells during metaphase, a special phase in the life of cells.

Vincristine also interferes with nucleic acid and protein synthesis.

Pharmacokinetics

After intravenous administration Vincristine is rapidly distributed throughout body tissues. Up to 90% of the drug binds to blood proteins. His active substance has the ability to accumulate in the tissues of the liver, lungs, spleen, pancreas, and kidneys. Vincristine does not penetrate the meninges.

The elimination half-life of Vincristine is three-phase and is 5 minutes, 2.3 hours and 85 hours, respectively. Metabolism is hepatic. Clearance is 146 ml/min. Excretion occurs mainly in feces (80%) and 20% in urine.

Instructions for use of Vincristine

The vincristine solution must be prepared immediately before administration. The dry contents of the bottle are dissolved using a solvent, which is often included in the kit. This may be sodium chloride solution or water for injection. Typically, Vincristine is administered once a week as intravenous injection or a short infusion lasting 15 minutes. The treatment regimen is prescribed strictly individually.

The average weekly dose of vincristine according to the instructions is 0.4-1.4 mg/m2 (for adults). Children are prescribed 1.5-2 mg/m2 of body. On average, the duration of therapy is at least 1-1.5 months, after which a break is taken. If the concentration of bilirubin in the blood changes, the dose of vincristine should be reduced by 50%.

In some cases, the drug is injected into the cavity between the membranes of the lungs - 1 mg of the drug dissolved in 10 ml of physiological solution. Intrathecal administration of vincristine is not carried out, as there is a possibility of death.

Important: Leakage of vincristine from a vein into the surrounding area can cause severe skin and tissue damage. Tell your nurse right away if you have pain or redness at the injection site.

Side effects

The most common side effects of Vincristine are listed below. They may be temporary, and some may be permanent. This:

  • insomnia;
  • headache;
  • dizziness;
  • muscle weakness;
  • hair loss;
  • numbness in the limbs;
  • motor dysfunction;
  • constipation;
  • fever;
  • weight loss;
  • decrease in the number of leukocytes in the blood.

In addition, the drug is neurotoxic, that is, it has bad influence nervous central system. This should be taken into account when treating older people and those who have previously suffered neurological diseases.

Tell your doctor right away if you have any serious side effects, including: vision/hearing changes, mental/mood changes (eg, depression, hallucinations, confusion), extreme fatigue, cramps, chest pain.

Rarely, taking Vincristine can provoke:

  • excessive urination;
  • inflammation of the oral mucosa;
  • dysuria;
  • loss of appetite;
  • vomiting, nausea;
  • hypotension;
  • bronchospasm.

Dark colored urine constant nausea, vomiting, abdominal pain, yellowing of the eyes and skin may be signs of liver dysfunction!

Vincristine may cause pulmonary toxicity in some patients. This is most often observed with combination chemotherapy with Mitomycin-C. Contact us immediately medical care if you experience shortness of breath or cough.

Serious allergic reaction This drug is rare. However, be sure to contact your doctor if you notice one of these the following symptoms: rash, itching, swelling (especially of the face, tongue, throat).

Frequency and severity side effects are largely related to the duration of treatment and the dose of the drug received.

Overdose

In case of overdose, the above-mentioned side effects are aggravated. In severe cases, liver failure, cirrhosis and coma may develop. Treatment of overdose with Vincristine is symptomatic. Hemodialysis is ineffective in such cases.

special instructions

The drug should be administered under the supervision of an experienced physician in a facility equipped to diagnose and treat possible complications.

The product is highly irritant, so avoid contact with skin and eyes.

Unless your doctor tells you otherwise, drink plenty of fluids while using Vincristine. This helps reduce some side effects on the kidneys. Since patients often develop constipation during treatment, it is advisable to take laxatives or perform cleansing enemas.

This medicine may make you more susceptible to getting an infection, so wash your hands well to prevent the spread of bacteria and avoid contact with people who are sick.

Do not drive or do anything that requires alertness as vincristine causes dizziness. Limit your consumption of alcoholic beverages.

Women and men who have been treated with Vincristine should use reliable contraception for 3-6 months after the last dose.

Interaction

Taking certain drugs at the same time may affect pharmachologic effect Vincristine or increase the risk of serious side effects. Do not start taking any medication without your doctor's approval.

Here are some drugs that may interact with Vincristine:

  • Digoxin;
  • Phenytoin;
  • platinum compounds;
  • drugs that may cause difficulty urinating (for example, belladonna alkaloids);
  • Atropine and other anticholinergic drugs;
  • Dicyclomine;
  • Oxybutynin.

There are also medications that can affect the removal of vincristine from the body, such as azole antifungals (such as Itraconazole), macrolide antibiotics (Erythromycin), rifamycins (Rifabutin), anticonvulsants (Carbamazepine), and others.

Vincristine sulfate is not used simultaneously with Furosemide solution, Cefepime, sodium bicarbonate.

Vincristine is compatible with the following drugs: , .

Instructions for medical use drug

Description of pharmacological action

Binds to tubulin, inhibits the formation of the mitotic spindle and stops mitotic cell division at the metaphase stage. IN high doses also inhibits the synthesis of nucleic acids and proteins.

Indications for use

Acute leukemia, lymphogranulomatosis, non-Hodgkin's lymphoma, rhabdomyosarcoma, neuroblastoma, Wilms tumor, osteogenic sarcoma, Ewing's sarcoma, bone and soft tissue sarcoma, breast and uterine cancer, small cell carcinoma lungs, gynecological tumors in children.

Release form

injection solution 1 mg/ml; bottle (bottle) 1 ml, cardboard packaging 10;

Solution for injection 1 mg/ml; bottle (bottle) 2 ml, cardboard packaging 10;

Solution for injection 1 mg/ml; bottle (bottle) 3 ml, cardboard packaging 10;

Solution for injection 1 mg/ml; bottle (bottle) 5 ml, cardboard packaging 10;

Pharmacokinetics

After intravenous administration, more than 90% binds to tissues. Penetrates poorly cerebrospinal fluid. Metabolized in the liver.

Excreted in feces (80%) and urine. Elimination kinetics is three-phase, T1/2 - 19–155 hours.

Use during pregnancy

Contraindications for use

Diseases nervous system; pregnancy, breastfeeding.

Side effects

Convulsions with increased blood pressure, paresthesia, intestinal paresis, vomiting, weight loss, polyuria, dysuria, impaired ADH secretion, shortness of breath, bronchospasm, fever, headache, damage to cranial nerves, ataxia, alopecia, amenorrhea, azoospermia.

Directions for use and doses

IV, with an interval between two injections of at least 1 week. The average dose for a child is 2 mg/m2, for an adult - 1.4 mg/m2 (but not more than 2 mg/m2 per injection).

For liver failure, the dose should not exceed 1 mg/m2.

The solution can be injected directly into a vein or into a rubber tube during another perfusion already in progress. The injection duration should be approximately 1 minute.

Overdose

Symptoms: increased severity of side effects.

Treatment: prevention of the syndrome of impaired ADH secretion (limiting fluid intake, prescribing a diuretic), administration of phenobarbital (to prevent seizures) and other means of symptomatic therapy, intestinal lavage (prevention of obstruction), if necessary, administration of calcium folinate (iv at a dose of 100 mg every 3 hours for 24 hours, then every 6 hours for at least 2 days), monitor function of cardio-vascular system, hematological control. A specific antidote is unknown. Hemodialysis is ineffective.

Interactions with other drugs

Vincristine may reduce the anticonvulsant activity of phenytoin (reduces its content in the blood). Vincristine may increase concentrations uric acid in the blood (in the treatment of hyperuricemia and gout, dose adjustment of anti-gout medications may be necessary).

At simultaneous administration with uricosuric drugs, the risk of developing nephropathy associated with increased formation of uric acid increases. The most preferred drug for preventing or eliminating hyperuricemia associated with vincristine therapy is allopurinol.

When taken concomitantly with other drugs that have a neurotoxic effect (for example, isoniazid, itraconazole) or irradiation spinal cord neurotoxicity increases.

Incompatible with L-asparaginase (the latter can only be administered at intervals of 12–24 hours) - additive neurotoxic effects are possible.

Against the background of mitomycin, the likelihood of developing respiratory depression and bronchospasm increases (especially in predisposed patients).

Pharmaceutically incompatible with furosemide solution (precipitate may form). Glucocorticoids, androgens, estrogens and progestins potentiate the effect of vincristine.

Precautions for use

To prevent acute urate nephropathy, it is necessary to regularly monitor plasma uric acid levels and ensure adequate diuresis.

It is not recommended to prescribe against the background of radiation therapy or the use of drugs that affect the hematopoietic organs (due to a possible mutual increase in myelotoxic effect), with the exception of special chemotherapy programs with individual dose selection.

During treatment, the composition of peripheral blood should be monitored (with leukopenia, caution is necessary; it is advisable to take a break and prescribe antibiotics), bilirubin content and the concentration of sodium ions in the serum (the introduction of appropriate solutions is recommended to correct hyponatremia).

Any complaints of eye pain or decreased vision require a thorough ophthalmological examination. Neurotoxicity of vincristine may adversely affect psychomotor speed and control ability. vehicles. Elderly people and patients with a history of neurological diseases are more susceptible to neurotoxic effects.

IM administration is unacceptable due to possible necrosis fabrics.

Special instructions for use

Avoid contact of vincristine solution with the eyes.

Storage conditions

List A.: In a dark place, at a temperature of 4 °C.

Best before date

ATX classification:

** The Drug Directory is intended for informational purposes only. To get more complete information Please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use Vincristine, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee positive effect medicine.

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Gross formula

C 46 H 56 N 4 O 10

Pharmacological group of the substance Vincristine

Nosological classification (ICD-10)

CAS Code

57-22-7

Characteristics of the substance Vincristine

Antitumor agent of plant origin. An alkaloid found in the rose periwinkle plant. (Vinca rosea L.).

Vincristine lyophilized - white or slightly yellowish color. Vincristine sulfate is easily soluble in water (1:2), soluble in methanol, chloroform (1:30), slightly soluble in ethanol, practically insoluble in ether.

Pharmacology

pharmachologic effect- antitumor, cytostatic.

Binds to tubulin, inhibits the formation of the mitotic spindle and stops mitotic cell division at the metaphase stage. In high doses, it also inhibits the synthesis of nucleic acids and proteins.

After intravenous administration, it is quickly distributed into tissues (90% of the substance within 15-30 minutes after administration). Does not pass through the BBB. Plasma protein binding – 75-90%. Metabolized in the liver. The metabolism of vincristine is mediated by hepatic isoenzymes of the CYP3A subfamily of cytochrome P450. The kinetics of elimination is three-phase. T1/2alpha is 5 minutes, T1/2beta is 2.3 hours, T1/2gamma is on average 85 hours (range 19-155 hours). Excreted in bile (80%) and urine (10-20%).

Application of the substance Vincristine

Acute leukemia, acute lymphoblastic leukemia in children (for combination therapy), lymphogranulomatosis (Hodgkin's disease), non-Hodgkin's malignant lymphomas, myeloma, rhabdomyosarcoma, bone and soft tissue sarcomas, Ewing's sarcoma, granuloma fungoides, breast cancer, small cell lung cancer, melanoma , mycosis fungoides, Kaposi's sarcoma, renal pelvis and ureter cancer, cancer Bladder, neuroblastoma, Wilms tumor, cervical cancer, uterine sarcoma, germ cell tumor of the testicle and ovaries, uterine chorionepithelioma, ependymoma, meningioma, pleurisy of tumor etiology, malignant tumors genital organs in girls, idiopathic thrombocytopenic purpura (in the absence of effect from splenectomy and glucocorticoid therapy).

Contraindications

Hypersensitivity, infectious diseases, neurodystrophic diseases (in particular the demyelinating form of Charcot-Marie-Tooth syndrome), intrathecal administration (possible death), pregnancy, breastfeeding.

Restrictions on use

Hyperbilirubinemia, obstructive jaundice, bone marrow hypoplasia, previous radiation therapy of the hepatobiliary region and the spinal cord region, elderly age.

Use during pregnancy and breastfeeding

Side effects of Vincristine

From the nervous system and sensory organs: convulsions with increased blood pressure, paresthesia, headache, loss of sensitivity, neuralgia, neuropathy, disorder motor function, decreased muscle strength, ataxia, decreased deep tendon reflexes, isolated paresis, muscle paralysis, dysfunction of the cranial nerves (especially the VIII pair), depression, hallucinations, sleep disturbance, diplopia, ptosis, transient blindness and atrophy optic nerve.

From the cardiovascular system and blood (hematopoiesis, hemostasis): lability of blood pressure; in patients with previously irradiated mediastinum, when using polychemotherapy with the inclusion of vincristine, angina pectoris and myocardial infarction, moderate leukopenia, thrombocytopenia and anemia may occur.

From the respiratory system: acute respiratory failure, shortness of breath, bronchospasm (especially when combined with mitomycin).

From the gastrointestinal tract: nausea, vomiting, anorexia, stomatitis, spasm of smooth muscles of the gastrointestinal tract, abdominal pain, constipation or diarrhea, paralytic ileus (especially in children), necrosis or perforation of the wall small intestine.

From the outside genitourinary system: dysuria, urinary retention due to bladder atony, acute uric acid nephropathy, azospermia, amenorrhea.

Allergic reactions: anaphylaxis, rash, Quincke's edema.

Others: alopecia, feeling of heat, syndrome of inappropriate secretion of antidiuretic hormone, hyponatremia, polyuria, weight loss; local reactions if it gets under the skin - cellulite, phlebitis, necrosis.

Interaction

Vincristine may reduce the anticonvulsant activity of phenytoin (reduces its content in the blood). Vincristine may increase the concentration of uric acid in the blood (dose adjustments of antigout medications may be necessary when treating hyperuricemia and gout). When taken simultaneously with uricosuric drugs, the risk of developing nephropathy associated with increased formation of uric acid increases. The most preferred drug for preventing or eliminating hyperuricemia associated with vincristine therapy is allopurinol. When taken simultaneously with other drugs that have a neurotoxic effect (for example, isoniazid, itraconazole) or irradiation of the spinal cord, neurotoxicity increases. Incompatible with L-asparaginase (the latter can only be administered at intervals of 12-24 hours) - additive neurotoxic effects are possible. Against the background of mitomycin, the likelihood of developing respiratory depression and bronchospasm increases (especially in predisposed patients). Pharmaceutically incompatible with furosemide solution (precipitate may form). Glucocorticoids, androgens, estrogens and progestins potentiate the effect of vincristine.

Overdose

Symptoms: increased severity of side effects.

Treatment: prevention of the syndrome of impaired ADH secretion (limiting fluid intake, prescribing a diuretic), administration of phenobarbital (to prevent seizures) and other means of symptomatic therapy, intestinal lavage (prevention of obstruction), if necessary, administration of calcium folinate (iv at a dose of 100 mg every 3 hours for 24 hours, then every 6 hours for at least 2 days), monitoring of cardiovascular function, hematological control. A specific antidote is unknown. Hemodialysis is ineffective.

Active substance

Vincristine sulfate (vincristine)

Release form, composition and packaging

Lyophilized powder for solution for injection white or yellowish-white.

Excipients: lactose.

Solvent: benzyl alcohol, water (10 ml).

Dark glass bottles (1) complete with solvent (1 bottle) - cardboard packs.
Dark glass bottles (10) complete with solvent (10 bottles) - cardboard packs.

Injection

Excipients: methylhydroxybenzoate, propylhydroxybenzoate, sodium hydroxide, sulfuric acid, water for injection.

1 ml - dark glass bottles (1) - cardboard packs.

Injection transparent, colorless or slightly yellow, free from mechanical inclusions.

2 ml - dark glass bottles (1) - cardboard packs.

Injection transparent, colorless or slightly yellow, free from mechanical inclusions.

Excipients: mannitol, methylhydroxybenzoate, propylhydroxybenzoate, sodium hydroxide, sulfuric acid, water for injection.

5 ml - dark glass bottles (1) - cardboard packs.

pharmachologic effect

Antitumor agent of plant origin.

Vincristine is a rose vinca alkaloid and is a cytostatic chemotherapeutic agent. Vincristine binds to the tubulin protein and leads to disruption of the microtubular apparatus of cells and to rupture of the mitotic spindle. Suppresses mitosis in metaphase. It also interferes with glutamate metabolism and possible nucleic acid synthesis and has an immunosuppressive effect.

Pharmacokinetics

After intravenous administration, vincristine is rapidly cleared from the blood. About 90% of the drug is protein bound. Vincristine is metabolized in the liver and excreted mainly in bile; 70-80% of the drug is found in feces unchanged and in the form of metabolites, 10-20% of the drug is detected in urine. The initial, average and final T1/2 are 5 minutes, 2.3 hours and 85 hours, respectively. Terminal T1/2 can range from 19 to 155 hours. Vincristine penetrates the BBB poorly.

Indications

  • acute leukemia;
  • Hodgkin and non-Hodgkin lymphomas;
  • Wilms tumor;
  • rhabdomyosarcoma;
  • neuroblastoma;
  • myeloma;
  • Kaposi's sarcoma;
  • sarcomas of bones and soft tissues;
  • small cell lung cancer;
  • choriocarcinoma of the uterus;
  • brain tumors.

Vincristine is also used for idiopathic thrombocytopenic purpura (with resistance to corticosteroid drugs and failure of splenectomy).

Contraindications

  • neurodystrophic diseases (for example, demyelinated form of Charcot-Marie-Tooth syndrome);
  • pregnancy;
  • lactation period;
  • hypersensitivity to vincoalkaloids.

Dosage

Intrathecal administration of vincristine is prohibited.

Vincristine is administered strictly intravenously at intervals of 1 week. The injection duration should be approximately 1 minute.

Before administration, the contents of the bottle are diluted in the supplied solvent with the addition of the required amount of 0.9% sodium chloride solution to obtain a concentration of 0.1 mg/ml.

When administering, care must be taken to avoid extravasation.

The dose is selected individually. On average the dose is for adults: 1.4 mg/m2 body surface, a single dose should not exceed 2 mg; For children - 1.5-2 mg/m2 body surface. For children weighing up to 10 kg the initial dose should be 0.05 mg/kg per week.

U patients with impaired liver function and plasma bilirubin concentrations above 51.3 µmol/l

Side effects

From the central nervous system and peripheral nervous system: seizures with increased blood pressure, paresthesia, neuralgia, neuropathy, jaw pain, decreased muscle strength, loss of tendon reflexes, ataxia, headache, depression, hallucinations, sleep disturbances, diplopia, ptosis, transient blindness and optic atrophy. Neurotoxicity is the dose-limiting factor.

From the outside digestive system: nausea, vomiting, stomatitis, constipation, paralytic intestinal obstruction(especially often in children), pain in abdominal cavity, necrosis of the small intestine and/or perforation, diarrhea.

From the urinary system: polyuria, dysuria, urinary retention due to bladder atony, edema.

From the cardiovascular system: increase or decrease in blood pressure. In patients with previously irradiated mediastinum, when using polychemotherapy with the inclusion of vincristine, angina pectoris and myocardial infarction may occur.

From the respiratory system: Acute dyspnea and severe bronchospasm have been observed with the use of vincristine with mitomycin C.

From the endocrine system: A syndrome caused by impaired secretion of antidiuretic hormone, which is characterized by a large excretion of sodium in the urine and causes hyponatremia, is rarely observed. There are no signs of damage to the kidneys and adrenal glands, arterial hypotension, dehydration, azotemia and edema.

From the hematopoietic system: does not have a significant effect on hematopoiesis. However, mild leukopenia, thrombocytopenia and anemia may occur.

Local reactions: if the drug gets under the skin, cellulite, phlebitis, and even necrosis can develop.

Others: alopecia, rash, amenorrhea, azoospermia.

Overdose

In case of accidental overdose, increased side effects of Vincristine should be expected. A specific antidote is not known.

Treatment is symptomatic in nature and should include limiting fluid intake, prescribing diuretics (to prevent complications associated with the development of antidiuretic hormone hypersecretion syndrome), use (to prevent seizures), and the use of laxatives (to prevent intestinal obstruction). It is also necessary to monitor the activity of the cardiovascular system and carry out hematological control. Hemodialysis is not effective.

In addition to the above, leucovorin 100 mg IV every 3 hours for 24 hours and then every 6 hours for at least 48 hours may be prescribed.

Drug interactions

Vincristine may reduce the anticonvulsant effect of phenytoin.

At simultaneous use with neurotoxic drugs (, itraconazole, nifedipine) there is an increase in side effects from the nervous system.

When used simultaneously, vincristine weakens the effect of anti-gout drugs. When used simultaneously with medicines, increasing the level of uric acid in the blood serum, increases the risk of nephropathy.

When administered in combination with mitomycin C, vincristine may cause severe bronchospasm.

If it is necessary to use the drug in combination with L-asparaginase, vincristine should be administered 12-24 hours before using L-asparaginase. Prescribing vincristine before administration may interfere with its elimination from the liver.

Concomitant use of vincristine with other myelosuppressive drugs and prednisolone may increase the suppression of bone marrow hematopoiesis.

special instructions

Intrathecal administration of vincristine can cause death.

During treatment, regular hematological monitoring should be carried out. In case of development of leukopenia, special precautions should be taken when administering repeated doses.

If liver function tests increase, the dose of vincristine should be reduced.

The concentration of sodium ions in the blood serum should be determined periodically. To correct hyponatremia, it is recommended to administer appropriate solutions.

Patients with a history of neuropathy are subject to special monitoring.

Vincristine should be prescribed with caution to elderly patients, because their neurotoxicity may be more pronounced.

Any complaints of eye pain or decreased vision require a thorough ophthalmological examination.

Avoid getting vincristine solution into your eyes. If this happens, you should immediately rinse your eyes generously and thoroughly with plenty of liquid.

For liver dysfunction

U patients with plasma bilirubin concentrations above 51.3 µmol/l A dose reduction of 50% is recommended.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

Store the solution at a temperature of 2-8 ° C out of the reach of children. Shelf life - 2 years.

Store the lyophilized powder at a temperature of 2-8 ° C out of the reach of children. Shelf life - 3 years.

Photo of the drug

Latin name: Vincristine sulfate

ATX code: L01CA02

Active substance: Vincristine

Analogs: Vero-Vincristine

Manufacturer: Pharmachemie B.V. (Netherlands)

Updating instructions: 19.09.17

Vincristine – antitumor agent plant origin, which has antitumor properties.

Active substance

Release form and composition

Available in the form of a lyophilisate for the preparation of a solution for intravenous administration and a solution for injection in bottles of 1, 2, 3 and 5 ml.

Indications for use

Used as an immunosuppressive and cytostatic agent.

As an immunosuppressant, it is prescribed only for idiopathic thrombocytopenic purpura if splenectomy is ineffective and the patient is resistant to glucocorticoids.

As a cytostatic (antitumor) drug, it is prescribed for the treatment of the following diseases:

  • acute leukemia;
  • non-Hodgkin's lymphomas;
  • gynecological tumors of the genital organs in children;
  • rhabdomyosarcoma;
  • sarcoma of bones and soft tissues;
  • osteogenic sarcoma;
  • uterine sarcoma;
  • Kaposi's sarcoma;
  • Ewing's sarcoma;
  • lymphogranulomatosis;
  • multiple myeloma;
  • melanoma, meningioma, neuroblastoma;
  • breast cancer, cervical cancer, uterine choriocarcinoma;
  • bladder cancer;
  • cancer of the renal pelvis and ureters;
  • small cell lung cancer;
  • germ cell tumor of the testicle and ovaries;
  • epithelioma, ependymoma, pleurisy of tumor origin.

Contraindications

Diseases of the nervous system and severe leukopenia.

Take with caution in the following cases:

  • decreased liver function;
  • inhibition of bone marrow hematopoiesis;
  • presence of constipation;
  • history of neuropathy;
  • previous radiotherapy or chemotherapy;
  • acute infections;
  • elderly age.

Instructions for use Vincristine (method and dosage)

Intended exclusively for intravenous administration.

  • The injection solution must be injected directly into the vein or rubber tube while perfusion is already in progress. The time during which the injection is given should be about one minute, and the duration of the interval between two injections of the drug should be at least a week.
  • The dosage regimen is set individually and depends on the phase of the disease, the state of the hematopoietic system, as well as on the planned antitumor therapy regimen. For adults, the average dose is 1.4 mg/m2, but not more than 2 mg/m2 per injection; for children, the average dose should also not exceed 2 mg/m2 per injection.
  • Due to the fact that the use of the drug can cause kidney damage, it is recommended to monitor the uric acid content and alkalinization of urine during the treatment period. Not used during radiation therapy and not used simultaneously with other medicines having a neurotoxic effect.

Side effects

The use of Vincristine may cause the following side effects:

  • peripheral nerve neuritis, optic nerve atrophy, neuropathy, seizures, headache, hallucinations, impaired motor function, ataxia (disorder of motor coordination), depression, ptosis (drooping upper eyelid), diplopia (“double vision”), sleep disturbances, decreased deep tendon reflexes;
  • thrombocytopenia, anemia, leukopenia, myocardial infarction;
  • constipation, diarrhea, nausea, vomiting, stomatitis, anorexia, paralytic ileus (intestinal obstruction);
  • dysuria, bladder atony, polyuria, acute uric acid nephropathy, edema;
  • arterial hypotension (decreased blood pressure), alopecia (hair loss that goes away after treatment is stopped).
  • alopecia, feeling of heat, syndrome of inappropriate secretion of antidiuretic hormone, hyponatremia, polyuria, weight loss; local reactions upon contact with the skin - cellulite, phlebitis, necrosis.

Overdose

An overdose of Vincristine can cause ADH secretion syndrome. To prevent this phenomenon, fluid intake is limited and a diuretic is prescribed that acts at the level of the loop of Henle and distal tubules. To prevent seizures, phenobarbital and other symptomatic drugs are indicated. Colon lavage is recommended.

Analogs

Vero-Vincristine, Vinblastine, Welbine, Vincatera.

pharmachologic effect

  • Vincristine has a cytostatic (antitumor) pharmacological effect. It has the ability to prevent the formation of the mitotic spindle by blocking tubulin (a protein that is the “building material” of the cell cytoskeleton) and thereby stopping mitotic cell division at the metaphase stage.
  • In idiopathic thrombocytopenic purpura, it exhibits a specific immunosuppressive effect, reducing penetration into Bone marrow lymphocytes, reducing the cytotoxic activity of lymphocytes against platelets and lowering the level of antiplatelet antibodies.
  • The drug is included in the list of Essential and Essential Medicines.

special instructions

  • When administering repeated doses of drugs, special care must be taken and regular hematological monitoring must be carried out.
  • An increase in uric acid levels is an indication for urine alkalization and the use of uricosynthesis inhibitors. As liver test levels increase, the dosage is reduced.
  • Patients are advised to monitor the concentration of sodium ions in the blood serum and, if the indicator decreases, administer appropriate solutions.
  • Patients with a history of neuropathy and elderly patients should be monitored with particular caution.
  • For complaints of decreased vision and pain in the eyes, it is necessary to ophthalmological examination. If the drug gets into your eyes, you should immediately rinse your eyelids with plenty of water.
  • Negatively affects the ability to operate machinery and vehicles due to its neurotoxic effect.
  • Intrathecal administration may cause death.

Pregnancy and lactation

Contraindicated during pregnancy and lactation.

In childhood

Information is absent.

In old age

It is prescribed with caution, since in old age the neurotoxicity of the drug is more pronounced.

For impaired renal function

For liver dysfunction

When the plasma bilirubin concentration is above 51.3 µmol/l, the dosage should be reduced by 50%.

Drug interactions

  • Concomitant use with phenytoin reduces the anticonvulsant effect of the latter.
  • Use with neurotoxic drugs increases side symptoms from the nervous system. In combination with anti-gout drugs, it reduces the effect of the latter. In combination with drugs that increase serum uric acid levels, the risk of nephropathy increases.
  • In combination with mitomycin C, it causes severe bronchospasm.
  • When taken with L-asparaginase, the interval between drug administrations should be 12-24 hours. If asparaginase is administered before vincristine, this may interfere with its elimination from the liver.
  • Use in combination with prednisolone and myelosuppressive drugs can increase the inhibition of hematopoietic processes in the bone marrow.