Gemcitabine

Gemcitabine is an antimetabolite and has an antitumor effect.

[1], [2], [3], [4], [5], [6], [7], [8],

Indications Gemcitabine

It is used for the therapy of such diseases:

• cancer affecting the pancreas;
• carcinoma in the region of the urethra, prostate or kidney;
• breast or ovarian cancer;
• pulmonary carcinoma.

[9], [10], [11]

Release form

Release of the medication is carried out in the form of lyophilizate, in flakonchikah capacity of 0.2 or 1 g.

[12], [13], [14], [15], [16], [17]

Pharmacodynamics

Gemcitabine has a depressing effect on the process of DNA binding. The medication affects cells in stages S, as well as G1 / S. Metabolism of the substance occurs before the formation of 2-phosphate and 3-phosphate nucleosides. In this case, the former slow down the activity of RNA, while the latter - are built in the chains of RNA and DNA. As a result, DNA binding is blocked, and pathogenic cells die.

It is noted the drug effectiveness of drugs in pancreatic carcinoma. At monotherapy in 25-40% of patients clinical improvement of a condition is observed. Combination of the drug with cisplatin increases the therapeutic effect. At the same time, at lower concentrations, the preparation has radiosensitizing properties.

[18], [19], [20], [21], [22],

Pharmacokinetics

When infusion of a portion of 1 g / m ², the plasma Cmax values are noted after 3-15 minutes; while the medicinal properties of the drug are preserved for another 90 minutes.

The drug has a weak synthesis with protein. Exchange processes occur inside the kidneys with the liver, as a result of which the active element of the drug is converted into an inactive metabolic product.

Excretion is carried out through the kidneys (89%), and with the weakening of their work, the inactive decay product begins to accumulate.

[23], [24], [25], [26]

Dosing and administration

The medication is administered intravenously, through a dropper. As a solvent, only 0.9% NaCl solution can be used. First, 25 ml of solvent are poured into the container with 1 g of the drug, and then shaken and diluted with the required amount of solution. The resulting mixture should not contain undissolved particles. It is allowed to be stored at room temperature for 24 hours.

Chemotherapy with Gemcitabine is performed in the form of monotherapy or in combination with platinum drugs (among them oxaliplatin and cisplatin with carboplatin). Below are exemplary therapy regimens.

In carcinoma in the urea area, 1.25 g / m ^{2 of} substance is used, on the 1st, 8th and 15th days of the cycle, with intervals of 28 days.

With pulmonary carcinoma, 1 g / m ^{2 of} medication is administered, once a week for a period of 3 consecutive weeks. Next, you need to take a break, which is 7 days, and repeat the above cycle.

During carcinoma in the pancreatic region, 1 g / m ^{2 of the} drug is administered once a week , for a period of 7 weeks in a row. Next, you should take a break for 7 days, and continue the therapy at the above dosage, with a single injection for a week, for the 21st day in a row. When the frequency of injections is increased, the toxic properties of the drug are potentiated.

During the treatment cycle, it is necessary to monitor the white blood cells and platelets. If the patient develops hematoxicity, the portion is reduced or the injection is postponed. In addition, you must constantly monitor the work of the kidneys and liver.

[32], [33], [34], [35]

Use Gemcitabine during pregnancy

Gemcitabine is not allowed for pregnant women.

Contraindications

The main contraindications are the patient's intolerance to the medication, as well as the period of breastfeeding.

Caution is necessary when used in people with kidney failure or liver, suppression of bone marrow function, as well as with diseases that have a bacterial or viral etiology.

[27], [28]

Side effects Gemcitabine

The use of medication can lead to the appearance of some side-effects:

• insomnia and headaches;
• bronchial spasms, dyspnoea, pulmonary edema and cough;
• arrhythmias and lowering blood pressure;
• anemia, leukocyte or thrombocytopenia;
• stomatitis, diarrhea, nausea, as well as an increase in liver transaminase;
• hematuria or proteinuria;
• hair loss or rash;
• pain in the back;
• facial puffiness;
• myalgia.

[29], [30], [31]

Overdose

When intoxication occurs, myelodepression, chills, fatigue and cough. In addition, bleeding, pain in the lower back, paresthesia, blood in the urine and feces, as well as eruptions on the epidermis.

Gemcitabine does not have an antidote. The patient should be under medical supervision; In addition, he undergoes symptomatic procedures and follows the blood composition in dynamics.

[36], [37], [38], [39]

Interactions with other drugs

The combination with immunosuppressants (among them mercaptopurine, cyclophosphamide, chlorambucil, and in addition, cyclosporine and azathioprine with GCS) increases the likelihood of infection.

When performing radiotherapy simultaneously with the use of Gemcitabine, suppression of bone marrow function is enhanced. With pulmonary carcinoma, radiation therapy led to the appearance of toxic reactions (pneumonia and esophagitis), which carried the danger of the patient's life.

Combination with vaccines of a viral nature led to the fact that the drug weakened the production of antibodies.

[40], [41],

Storage conditions

Gemcitabine should be kept at a temperature not exceeding 25 ° C.

[42], [43]

Shelf life

Gemcitabine is allowed to be used within 36 months of the manufacture of the therapeutic agent.

[44], [45], [46]

Application for children

Gemcitabine was studied during limited clinical trials of stage 1 and 2 in children - as a means of therapy for different types of neoplasms. The information obtained in these tests does not allow to determine the degree of safety and therapeutic effectiveness of the drug for the child, because of what it is not used in pediatrics.

[47], [48],

Analogues

Analogues of the drug are Gemcitera, Tolgetzit, Hematics with Gemtaz, and in addition Citogem, Dercin, Gemtsibin with Oncohem, and also Gemcitera and Strigem.

[49], [50], [51], [52], [53], [54], [55],

Reviews

Gemcitabine shows high efficacy in monotherapy during urea cancer. However, in the case of malignant tumors in the field of other organs, the drug should be used in combination. During pulmonary carcinoma, the substance is combined with cisplatin; with tarce - with pancreatic carcinoma (locally distributed form). Such a scheme shows that when it is used, the survival of patients is increased.

Since the drug was usually used in conjunction with other drugs, it is difficult to evaluate its own therapeutic effectiveness. It is possible to rely exclusively on the data of randomized tests. Based on these, it can be concluded that there were no significant differences between combinations of cisplatin with gemcitabine, as well as paclitaxel with carboplatin or cisplatin with paclitaxel.

Of the minuses in the reviews most often mention the negative effects of the drug.