Gemzar

Gemzar has cytostatic and antitumor properties.

Indications of the gemzar

It is used to eliminate such diseases:

• treatment of cholangiocarcinoma and urea cancer (together with cisplatin);
• a locally advanced form of pancreatic cancer or with the formation of metastases;
• breast cancer metastatic, inoperable, and with local recurrences (along with paclitaxel);
• carcinoma in the ovary (epithelial), simultaneously with carboplatin;
• bronchogenic carcinoma of non-small cell type (in combination with cisplatinum).

[1], [2], [3]

Release form

The release is made in the form of lyophilizate, in glass bottles in a dose of 0.2 g or 1 g inside the box.

[4], [5],

Pharmacodynamics

Gemcitabine kills cells passing through the DNA binding stage, and in some circumstances can block the process of cellular passage through the boundary of the G1 / S stage.

The metabolic processes of the drug pass inside the cells under the influence of the enzyme nucleoside kinase, transforming into active 3-phosphate or 2-phosphate nucleotides. The slowing down of DNA binding processes develops under the influence of 2 major metabolic products - 3-phosphate, and 2-phosphate nucleosides. At the initial stage, the 2-phosphate nucleoside inhibits the binding of the ribonucleotide reductase enzyme, resulting in the binding of the deoxynucleoside triphosphate required for DNA replication processes.

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

[6], [7],

Pharmacokinetics

After entering the circulatory system, the active element is rapidly 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.

The data from the clinical tests demonstrated that the sex of the patient has a significant effect on the distribution volume of the medicine within the body. The level of overall clearance in women is lower than that of men by 30%.

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

[8], [9], [10], [11], [12], [13]

Dosing and administration

The medicine is injected / in the method, slowly (for 30 minutes), through a dropper. Injection should be performed by an experienced specialist who previously treated oncological patients.

Before each treatment session, it is required to take from the patient tests that control the work of the bone marrow. At the same time, if the results of the tests turned out to be bad, Gemzar should be refused treatment.

The dosing schedule, as well as the duration of therapy, is selected by the treating doctor, taking into account the type of pathology and its stage.

When performing the infusion, you need to closely monitor the patient's condition.

It is extremely cautious to treat people who suffer from renal or hepatic pathologies in severe degree.

The scheme of manufacturing a medicamental solution.

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

The solution is manufactured aseptically. Inside the vial, add at least 5 ml of sodium chloride (0.2 g of lyophilizate) or a minimum of 25 ml (per 1 g of powder). After the addition of the solvent, the container is shaken to mix the mixture. The finished solution can be slightly yellowish.

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

The drug is forbidden to apply if foreign substances are noticed in the solution or the hue of the liquid has changed.

Breast cancer.

The drug is combined with paclitaxel. Gemzar is required to enter after an infusion of additional drugs (this procedure lasts 3 hours) - for half an hour on the 1st, and also the 8th days of the treatment cycle (lasting 21 days).

Cancer of the pancreas.

It is necessary to prescribe 1 g / m ^{2 of the} drug, with a one-time application for 7 days. This course lasts 7 weeks, after which a 7-day interval is required. After this, the patient is transferred to a treatment regimen with 3-week cycles, followed by 7 days of interruption.

Cholangiocarcinoma.

With monotherapy, a single dose regimen of 1 g / m ^{2 of} medication is used for 1 week . This therapy lasts 21 days, after which they take a break, which is 1 week, and then continue a few more of the same cycles. Taking into account the clinical picture, the portion size can be reduced and the number of cycles can vary.

When the drug is combined with cisplatin on the first day of the course, 70 mg / m ^{2 of the} drug is administered to the patient , and then Gemzar, at a dosage of 1250 mg / m ², on the first and also the 8th day of each 3-week cycle cycles are required to be repeated). Correct the size of portions is allowed.

Cancer of the gallbladder.

In the course of therapy, 1 g / m ^{2 of the} solution is injected iv by the method - on the 1st, 8th, and also the 15th day of each 28-day treatment cycle (when combined with cisplatin - for every 2 nd day of such a cycle ). Further, such 4-week treatment cycles must be repeated.

Bronchogenic carcinoma of non-small cell type.

When performing monotherapy, it is necessary to administer 1 g / m ^{2 of} LS, once per 7 days for 3 weeks, after which it is necessary to take a 7-day break. Then this course should be repeated. When the drug is combined with other drugs, the portion size is 1250 mg / m ². It is introduced on the 1st, 8th, and 21st days of the ongoing cycle.

Carcinoma of the ovaries.

Gemzar is administered in combination with carboplatin. Gemcitabine is administered at a dosage of 1 g / m ², on the 1st, and also on the 8th day of the treatment cycle lasting 21 days.

To determine the hematological toxicity of the medication, hepatic and renal activity is checked. Given these indicators, a gradual decrease in the size of a portion of medicament is allowed with an increase in the burden on the patient's body.

When checking the number of granulocytes before performing a new infusion, this indicator should be at least 1500 (x106 / L), and the platelet count should be equal to 100,000 (x106 / L).

With the development of the following signs of toxicity, you should reduce the dose by 25% of the initial dosage:

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

[19], [20]

Use of the gemzar during pregnancy

It is forbidden to appoint Gemzar to mothers who breastfeed, as well as to pregnant women.

Contraindications

It is forbidden to use a medicine in the presence of intolerance with regard to its elements.

[14], [15]

Side effects of the gemzar

Often, patients taking Gemzar develop vomiting, an increase in phosphatase and liver enzymes, and nausea. Often there is a development of hematuria or proteinuria.

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

It was proved that the nature, as well as the frequency of side effects, is determined by the size of the dose, the speed of administration of the drug, and in addition the dosing regimen. A decrease in white blood cell counts with platelets and granulocytes is a dose-dependent symptom.

Data from clinical trials show that patients may experience such side effects:

• Insomnia with headaches, and a feeling of drowsiness. Occasionally, there is a stroke;
• development of thrombocyto- or leukopenia, thrombocytosis, anemia, as well as neurophenic fever;
• an increase in bilirubin or liver enzymes. The values of GGT and APF are increased occasionally;
• occurrence of ulcers in the mouth, the appearance of vomiting, constipation, nausea, diarrhea, the development of stomatitis or ischemic form of colitis;
• pain in the back, and also myalgia;
• itching and skin rash, the development of cough or allergic rhinitis, hair loss, hyperhidrosis. Occasionally there are tumors or ulcers, bullous rash, skin peeling and Stevens-Johnson syndrome;
• loss of appetite, development of anorexia;
• development of kidney failure, hematuria or proteinuria;
• single-onset anaphylactoid symptoms;
• development of dyspnea (mainly with bronchogenic carcinoma), rhinitis and cough. Occasionally, there is pulmonary edema, bronchospasm and fibrosing alveolitis;
• Occasionally there is radiotoxicity;
• influenza symptoms (asthenia with myalgia, chills, and loss of appetite), facial puffiness and skin manifestations at the site of injection;
• the occurrence of heart failure or arrhythmia. Occasionally there is vasculitis, myocardial infarction or a decrease in blood pressure.

Combination of medicament with paclitaxel (during treatment of breast cancer) increases the incidence of neutropenia, neutropenic fever, sensation of weakness, and in addition anemia.

Sensory polyneuropathy is more often noted with the combined use of Gemzar than in the case of monotherapy with this agent.

The data of postmarketing studies conducted showed that the following manifestations can develop in patients:

• pulmonary edema, hyaline membrane disease (occasionally);
• a severe degree of hepatotoxicity, sometimes reaching a complete liver failure;
• cerebrovascular disorders;
• gangrene, TEN, and vasculitis occur sporadically;
• a rapid decrease in hemoglobin, development of MHA, an increase in creatinine with bilirubin and urea (occurs occasionally, when these signs should stop treatment, in some cases, you may need to perform hemodialysis);
• colitis ischemic;
• anemia of supraventricular nature;
• photosensitivity.

[16], [17], [18]

Overdose

When using drugs in portions up to 5.7 g / m ², every 14 days of intoxication development was not observed.

If there is a suspicion of poisoning, you should donate blood for analysis and conduct symptomatic procedures. The medicine does not have an antidote.

[21],

Interactions with other drugs

To choose the permissible size of the radiation dose, which allows combining it with the use of Gemzar, has not yet been possible.

In cases where radiotherapy lasts less than the first week, no increase in the toxicity of the drug is observed. The use of drugs is allowed only after the disappearance of acute signs caused by irradiation, or after a minimum of 1 week.

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

It is forbidden to combine medicament with weakened live vaccines.

[22]

Storage conditions

Gemzar in the form of a powder can be kept at temperatures within the limits of 15-30 ° C, in a place inaccessible to small children. The ready-made infusion solution can be stored for a maximum of 24 hours. Do not freeze the drug.

[23], [24]

Shelf life

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

[25], [26],

Application for children

There were no studies of the use of the medicinal product for children.

[27], [28], [29], [30], [31],

Analogues

The following medicines are analogous to drugs: Oncoril with Wiztar, Xeloda and Citogem with Herzizar, Citin, Vizgem, Ental with Citarabin and Laracite.

[32], [33], [34], [35], [36], [37]

Reviews

Gemzar mostly receives positive feedback. People who used this medicine were generally satisfied with the result. Negative reactions always occur, as occurs with any chemotherapeutic procedures, but their frequency and strength of expression are lower in comparison with other similar drugs.

In particular, the drug achieved good results in the treatment of cancer in the pancreas.

It should be emphasized that the drug should be used in strict accordance with the regime of therapy and following all the recommendations of the treating doctor.