Gemzar

Gemzar has cytostatic and antitumor properties.

Indications Gemzara

It is used to eliminate the following diseases:

• treatment of cholangiocarcinoma and bladder cancer (together with cisplatin);
• locally advanced pancreatic cancer or with the formation of metastases;
• metastatic, inoperable breast cancer, as well as with local recurrences (together with paclitaxel);
• carcinoma in the ovarian region (epithelial nature), simultaneously with the use of carboplatin;
• non-small cell bronchogenic carcinoma (in combination with cisplatin).

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Release form

It is produced in the form of a lyophilisate, in glass vials in a dose of 0.2 g or 1 g inside a box.

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Pharmacodynamics

Gemcitabine kills cells that are undergoing DNA binding and, under some conditions, may block the process of cellular passage through the G1/S phase boundary.

The metabolic processes of the drug occur inside the cells under the influence of the enzyme nucleoside kinase, transforming into active 3-phosphate or 2-phosphate nucleotides. Slowing down of DNA binding processes develops under the influence of 2 main metabolic products – 3-phosphate and 2-phosphate nucleosides. At the initial stage, 2-phosphate nucleoside inhibits the binding of the enzyme ribonucleotide reductase, as a result of which the binding of deoxynucleoside triphosphate required for DNA replication processes does not occur.

After this, the process of competition with the development of self-potentiation between the elements dFdCTP and dCTP begins, which ultimately leads to a decrease in dCTP values. As a result, during the processes of DNA binding, an extra nucleotide is added to its chain, which prevents the possibility of further binding, and the cell is programmed for death (cellular apoptosis).

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Pharmacokinetics

After entering the bloodstream, the active element is quickly excreted from the blood plasma by metabolic processes. Less than 10% of the drug is excreted unchanged through the kidneys. The level of synthesis of metabolic products, as well as gemcitabine with plasma protein, is quite low.

Clinical test data have shown that the patient's gender has a significant impact on the distribution volume of the drug within the body. The level of total clearance in women is 30% lower than in men.

The half-life after prolonged treatment is 30-95 minutes.

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Dosing and administration

The medicine is administered intravenously, slowly (over 30 minutes), through a drip. The injection should be performed by an experienced specialist who has previously treated cancer patients.

Before each treatment session, it is necessary to take tests from the patient to monitor the functioning of the bone marrow. However, if the test results are bad, treatment with Gemzar should be abandoned.

The dosage regimen, as well as the duration of therapy, is selected by the attending physician, taking into account the type of pathology and its stage.

When performing an infusion, the patient's condition must be closely monitored.

People who suffer from severe kidney or liver pathologies should be treated with extreme caution.

Scheme for the preparation of a medicinal solution.

The powder should be dissolved with 0.9% sodium chloride injection solution. The most suitable concentration is 40 mg/1 ml of the drug.

The solution is prepared using an aseptic method. At least 5 ml of sodium chloride (per 0.2 g of lyophilisate) or at least 25 ml (per 1 g of powder) are added to the vial. After adding the solvent, the container is shaken to mix the mixture. The finished solution may be slightly yellowish.

The injection can be started immediately after the preparation of the medicinal solution.

The drug must not be used if foreign elements are noticed in the solution or the color of the liquid has changed.

Breast cancer.

The drug is combined with paclitaxel. Gemzar must be administered after the infusion of additional drugs (this procedure lasts 3 hours) - half an hour on the 1st and 8th days of the treatment cycle (lasts 21 days).

Pancreatic cancer.

The required dose is 1 g/m2 ^of the drug, administered once 7 days before. This course lasts 7 weeks, after which a 7-day interval is required. The patient is then transferred to a treatment regimen with 3-week cycles, followed by a 7-day break.

Cholangiocarcinoma.

^{In monotherapy, a regimen with a single administration of 1 g/ m2} of the drug per week is used. This therapy lasts 21 days, after which a break of 1 week is taken, and then several more such cycles are carried out. Taking into account the clinical picture, the portion size can be reduced and the number of cycles can be changed.

^{When combining the drug with cisplatin, the patient is administered 70 mg/ m2} of the drug on the first day of the course, and then Gemzar at a dosage of 1250 mg/m2 ^on the first and 8th day of each 3-week cycle (these cycles must be repeated). Adjusting the portion sizes is permitted.

Gallbladder cancer.

During therapy, 1 g/m2 ^of solution is administered intravenously on the 1st, 8th, and 15th days of each 28-day treatment cycle (in combination with cisplatin - on every 2nd day of such a cycle). Then such 4-week treatment cycles must be repeated.

Non-small cell bronchogenic carcinoma.

When performing monotherapy, it is necessary to administer 1 g/m2 ^of the drug, once every 7 days for 3 weeks, after which it is necessary to take a 7-day break. Then this course should be repeated. When combining the drug with other drugs, the dose size is 1250 mg/m2 ^. It is administered on the 1st, 8th, and 21st days of the ongoing cycle.

Ovarian carcinoma.

Gemzar is administered in combination with the substance carboplatin. Gemcitabine is administered at a dosage of 1 g/m2 ^, on the 1st and 8th day of a treatment cycle lasting 21 days.

To determine the hematological toxicity of the drug, liver and kidney function is tested. Taking these indicators into account, a gradual reduction in the size of the drug portion is allowed with an increase in the load on the patient's body.

When checking the granulocyte count before performing a new infusion, the value should be at least 1500 (x106/L) and the platelet values should be equal to 100,000 (x106/L).

If the following signs of toxicity develop, reduce the dose by 25% of the initial dosage:

• neutropenic fever;
• for 3 days the granulocyte count is less than 100x106/l;
• over the course of 5 days the number of granulocytes is less than 500x106/l;
• platelet count is less than 25,000/106/L;
• in cases where, due to the development of toxicity symptoms, treatment was discontinued for more than 1 week.

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Use Gemzara during pregnancy

It is prohibited to prescribe Gemzar to breastfeeding mothers and pregnant women.

Contraindications

It is prohibited to use the medication if you have an intolerance to any of its components.

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Side effects Gemzara

Vomiting, increased phosphatase and liver enzyme levels, and nausea are common in patients taking Gemzar. Hematuria or proteinuria are also common.

There are also cases of development of skin rash of an allergic nature (sometimes with itching), as well as dyspnea.

It has been shown that the nature and frequency of adverse effects are determined by the dose size, the rate of administration of the drug, and in addition, the dosing schedule. A decrease in the leukocyte count with platelets and granulocytes is a dose-dependent symptom.

Clinical test data show that patients may experience the following side effects:

• insomnia with headaches, as well as a feeling of drowsiness. Rarely, a stroke is noted;
• development of thrombocytopenia or leukopenia, thrombocytosis, anemia, and neuropenic fever;
• increased bilirubin or liver enzyme levels. Occasionally, GGT and ALP levels increase;
• the occurrence of mouth ulcers, vomiting, constipation, nausea, diarrhea, the development of stomatitis or ischemic colitis;
• back pain, as well as myalgia;
• itching and skin rash, development of cough or allergic rhinitis, hair loss, hyperhidrosis. Rarely, tumors or ulcers, bullous rash, skin peeling and Stevens-Johnson syndrome appear;
• loss of appetite, development of anorexia;
• development of renal failure, hematuria or proteinuria;
• anaphylactoid symptoms are observed occasionally;
• development of dyspnea (mainly with bronchogenic carcinoma), rhinitis and cough. Occasionally, pulmonary edema, bronchospasm and fibrosing alveolitis are observed;
• radiotoxicity occasionally occurs;
• flu-like symptoms (asthenia with myalgia, chills, and loss of appetite), facial swelling and skin manifestations at the injection site;
• the appearance of heart failure or arrhythmia. Rarely, vasculitis, myocardial infarction or a decrease in blood pressure occur.

The combination of the drug with paclitaxel (during the treatment of breast cancer) increases the incidence of neutropenia, neutropenic fever, a feeling of weakness, and also anemia.

Sensory polyneuropathy is more frequently observed with concomitant use of Gemzar than with monotherapy with this agent.

Post-marketing surveillance data have shown that patients may develop the following symptoms:

• pulmonary edema, hyaline membrane disease (rarely);
• severe degree of hepatotoxicity, sometimes reaching complete liver failure;
• cerebrovascular disorders;
• gangrene, TEN and vasculitis occur sporadically;
• rapid decrease in hemoglobin levels, development of MHA, increase in creatinine with bilirubin and urea values (occurs rarely; if these signs appear, treatment should be stopped; in some cases, hemodialysis may be required);
• ischemic colitis;
• supraventricular anemia;
• photosensitivity.

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Overdose

When using the drug in doses of up to 5.7 g/ ^m2 every 14 days, no development of intoxication was observed.

If poisoning is suspected, blood should be taken for analysis and symptomatic procedures should be performed. The drug has no antidote.

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Interactions with other drugs

It has not yet been possible to select an acceptable radiation dose that would allow it to be combined with the use of Gemzar.

In cases where radiotherapy lasts less than 1 week, no increase in drug toxicity is observed. The use of the drug is permitted only after the acute symptoms caused by radiation have disappeared, or after at least 1 week has passed.

In addition, after radiotherapy procedures and the use of drugs, the incidence of pneumonitis with esophagitis, as well as other tissue damage, increases.

It is prohibited to combine the drug with attenuated live vaccines.

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Storage conditions

Gemzar in powder form can be stored at a temperature of 15-30°C, out of the reach of small children. The prepared infusion solution can be stored for a maximum of 24 hours. It is prohibited to freeze the drug.

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Shelf life

Gemzar can be used for 3 years from the date of manufacture of the drug.

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Application for children

No studies have been conducted on the use of the drug in children.

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Analogues

The following medications are analogs of the drug: Oncoril with Viztar, Xeloda and Cytogem with Hercizar, Cytin, Vizgem, Ental with Cytarabine and Laracit.

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Reviews

Gemzar receives mostly positive reviews. People who have used this medicine were generally satisfied with the results they received. Negative reactions always occur, as happens with any chemotherapy procedures, but their frequency and severity are lower compared to other similar drugs.

The drug achieved particularly good results in the treatment of cancer in the pancreas.

It is necessary to especially emphasize that the medication must be used in strict accordance with the treatment regimen and following all recommendations of the attending physician.