Cisplatin - instructions for use, reviews, analogues and forms of release (injection solution) of the drug for the treatment of tumors

In this article, you can read the instructions for using the drug Cisplatinum. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Cisplatin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Cisplatin in the presence of existing structural analogues. Use for the treatment of tumors and malignant neoplasms.

Cisplatinum (cis-diamine-dichloroplatin) - is an antitumor drug containing a heavy metal platinum.

Cisplatin has properties,similar to the properties of bifunctional alkylating agents, forming interstitial and interstitial crosslinks in DNA, thereby violating its functions, which leads to cell death; the preparation does not have cyclic and phase specificity. Has immunosuppressive and radiosensitizing properties.

Pharmacokinetics

After rapid intravenous infusion, the appearance of cisplatin in the blood plasma and the peak of its concentration is determined immediately after administration. With IV infusion for 6-24 hours the concentration of the drug in the plasma increases gradually during the infusion, reaching a maximum at the end of the injection.

Cisplatin is characterized by extensive distribution in body fluids and in tissues; with the highest concentrations being achieved in the kidneys, liver and prostate gland. Platinum, released from cisplatin, quickly binds to tissue and plasma proteins. Two hours after the end of the three-hour infusion, 90% of the platinum in the plasma is in the protein-bound state. Cisplatin has the ability to accumulate in the body and is found in some tissues for another six months after the administration of the last dose of the drug.Biotransformation of cisplatin is carried out by rapid non-enzymatic transformation with formation of inactive metabolites. Cytotoxic action is exerted only by cisplatin, not bound to proteins, or its platinum-containing metabolites.

The half-life of total platinum has a very wide individual variability and ranges between 2-72 hours in healthy people, and 1-240 hours with severe renal failure. Cisplatin is excreted mainly with urine. Cisplatin can be excreted from the systemic blood flow by dialysis, but only within the first 3 hours after the administration of the drug.

Indications

Cisplatin, usually as part of combined chemotherapy regimens, is widely used in the treatment of the following solid tumors:

• germinogenous tumors of women and men;
• ovarian and testicular cancer;
• lung cancer;
• head and neck tumors

In addition, cisplatin has antitumor activity in the following types of tumors:

• cervical cancer;
• cancer of the bladder;
• osteosarcoma;
• melanoma;
• neuroblastoma;
• esophageal carcinoma.

Forms of release

Solution or concentrate for the preparation of injections 10 mg, 25 mg, 50 mg.

Instructions for use

Cisplatin can be used as a monotherapy or in combination with other cytostatics in different doses depending on the therapy scheme. For individual dose selection, reference should be made to the literature.

Cisplatin is administered intravenously or with indications (intraperitoneal tumors) into the abdominal cavity.

Cisplatin in monotherapy or in combination with other chemotherapy drugs is administered at a dose of 50-100 mg / m2 as an IV infusion every 3-4 weeks or 15-20 mg / m2 IV drip daily for 5 days every 3-4 weeks .

To stimulate diuresis (up to 100 ml / h) and to minimize the nephrotoxic effect of the drug, hydration is performed. Before the introduction of Cisplatin IV / in, drip up to 2 liters of fluid (0.9% solution of sodium chloride or 5% solution of dextrose). After the infusion is completed, 400 ml of a 0.9% solution of sodium chloride or a 5% solution of Dextrose are additionally added. Fluid intake and diuresis should be maintained for 24 hours. If intensive hydration is insufficient to maintain adequate diuresis, an osmotic diuretic (eg mannitol) can be administered.

Cisplastin is administered intravenously at the rate of not more than 1 mg / min. Prolonged infusions are carried out within 6-8-24 hours provided sufficient diuresis before and during administration of the drug.

Cisplatin is diluted in 0.9% sodium chloride solution to a concentration of 1 mg / ml. Lysophilate Cisplastin must first be dissolved in 10-25 ml of water for injection.

Do not use dextrose (glucose) solutions to dilute cisplatin.

Note: because aluminum reacts with cisplatin and inactivates it, and also causes the formation of sludge, it is very important for the preparation and administration of cisplatin does not use needles and other equipment containing aluminum.

Side effect

From the urinary system:

• nephrotoxicity (is cumulative and is the main toxic factor limiting the dose of Cisplatinum).

On the part of the digestive system:

• nausea and vomiting, which usually begin within the first hour of therapy and last for 24 hours or more, occur in 65% of patients;
• pain in the abdomen;
• diarrhea and constipation.

On the part of the hematopoiesis system:

• myelosuppression, (in most cases, it is slightly or moderately expressed and is reversible in normal doses);
• anemia.

From the side of the hearing system:

• unilateral or bilateral tinnitus, with or without loss of hearing, occurs in approximately 10% of patients; usually this side effect is reversible.

From the side of the central nervous system and the peripheral nervous system:

• peripheral neuropathies;
• autonomic neuropathy;
• convulsions;
• slurred speech;
• loss of taste;
• memory loss;
• Lermitt syndrome (myelopathy of the spine and autonomic neuropathy).

From the immune system:

• allergic reactions, manifested as reddening and swelling of the face, whistling rales in the lungs, a tachycardia and decrease of blood pressure;
• hives;
• patchy-papular skin rash.

From the side of the vision system:

• optic neuritis;
• edema of the optic disc;
• Cortical blindness;
• changes in the perception of colors, especially in the yellow-blue part of the spectrum.

Violations from electrolyte balance:

• hypomagnesemia;
• hypocalcemia;
• hypokalemia;
• hyponatremia.

Contraindications

• individual intolerance to cisplatin or other compounds containing platinum;
• impaired renal function (serum creatinine level more than 115 μmol / liter);
• oppression of bone marrow hematopoiesis;
• heart failure;
• pregnancy and lactation;
• generalized infections.

Application in pregnancy and lactation

Contraindicated take the drug during pregnancy and lactation.

special instructions

Introduction Cisplatin should be administered under the supervision of a physician with experience in the use of antitumor drugs.

Men and women of childbearing age during treatment with Cisplatin should use reliable methods of contraception.

Patients on the background of cisplatin treatment should periodically be examined by a neurologist. With obvious symptoms of toxic effects on the central nervous system, cisplatin should be discontinued.

Before the start of therapy, audiometry should be performed, and in cases where there are symptoms of hearing damage or clinical hearing impairments, repeated audiometry is indicated. In clinically significant hearing disorders, dosage adjustment or cancellation of therapy may be required.

In the process of treatment with Cisplatinum requires periodic blood analysis, determination of the content of leukocytes, platelets, hemoglobin, blood elements, renal and hepatic functional tests, as well as the level of electrolytes in blood serum.

When using Cisplatin, all the usual instructions for the use of cytotoxic drugs should be observed.

If the product gets into the eyes, they must be washed immediately with a large amount of water or with 0.9% sodium chloride solution. In case of contact with the skin, immediately contact the product with plenty of water. If the product is inhaled or if it gets into the mouth, immediately consult a doctor.

Drug Interactions

Simultaneous or sequential use of cisplatin with aminoglycoside antibiotics (gentamicin, kanamycin, streptomycin) or other potentially nephrotoxic drugs (eg, amphotericin B) can potentiate its nephrotoxic and ototoxic effects.

"Loop" diuretics (furosemide, clopamid, ethacrynic acid) can enhance the ototoxicity of cisplatin.

It is known that cisplatin can disrupt the excretion via the kidneys of bleomycin and Methotrexate (possibly due to cisplatin-induced nephrotoxic action) and increase the toxicity of these drugs.

In patients receiving cisplatin and anticonvulsants, the serum concentration of the latter may decrease to subtherapeutic values.

Cisplatin may cause an increase in the concentration of uric acid in the blood. Therefore, patients who simultaneously take medicines for the treatment of gout, such as allopurinol, colchicine, probenecid or sulfinpyrazone, it may be necessary to adjust the dosage of these drugs to control hyperuricemia and gout attacks.

Analogues of the drug Cisplatinum

Structural analogs for the active substance:

• Blastol;
• Displanor;
• Кемоплат;
• Oncoplatinum;
• Platidiam;
• Platimit;
• Platinum;
• Cisanplat;
• Cisplatin-LENS;
• Cisplatin-Teva;
• Cisplatin-Ebewe;
• Cytoplatinum.

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