Gemcitover 1 g

The antitumor agent. It has a cytostatic effect, which is associated with the inhibition of DNA synthesis. In the cell, it is metabolized to active diphosphate and triphosphate nucleosides. Diphosphate nucleosides inhibit the action of ribonucleotide reductase, with the participation of which in a cell formed deoxynucleoside triphosphates required to synthesize DNA, which leads to a decrease in their concentration in the cell. Triphosphate nucleosides actively compete for incorporation into the DNA chain, and may also be incorporated into RNA. After insertion of the intracellular metabolites gemcitabine in a DNA strand to its growing chains added one additional nucleotide that results in complete inhibition of further DNA synthesis and programmed cell death.

Active substance:
Gemcitabine

Manufacturer

Lance-Pharm, Russia

Composition

Active ingredient: gemcitabine hydrochloride in terms of gemcitabine – 1000 mg
Excipients: mannitol, sodium acetate, sodium hydroxide (sodium hydroxide) or hydrochloric acid 1 M

Indications

Non-small cell lung cancer (IIIa-IV stage); late pancreatic carcinoma.

Contraindications

Hypersensitivity to gemcitabine.

Side effects

From the side of hematopoiesis: often – leukopenia, neutropenia, thrombocytopenia, and anemia; very rarely – thrombocytosis. On the part of the digestive system: very often – nausea, vomiting, increase in liver transaminases, alkaline phosphatase; often – anorexia, diarrhea, constipation, stomatitis, hyperbilirubinemia. From the urinary system: very often – proteinuria and hematuria; -gemolitiko rare-uremic syndrome and / or renal failure. Of the skin and skin appendages: common – skin rash, pruritus, alopecia. The respiratory system: very often – shortness of breath; often – cough, rhinitis; sometimes -bronhospazm, interstitial pneumonia, pulmonary edema; rarely – acute respiratory distress syndrome (treatment should be discontinued when a data symptoms). Cardio-vascular system: seldom – a decrease in blood pressure, myocardial infarction, heart failure, arrhythmia. From the nervous system: often – headache, drowsiness, insomnia, paresthesia. Allergic reactions: very rare – anaphylactic reactions. Other: very often – flu-like symptoms, peripheral edema; often – fever, chills, asthenia, back pain, myalgia; sometimes – swelling of the face

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How to accept, acceptance rate and dosage

Gemtsitover injected intravenously over 30 minutes.
Non-small cell lung cancer (locally advanced or disseminated) monotherapy.
The recommended dose is 1000 mg / m2 1 time per week for 3 weeks followed by one week apart, every 28 days. The combination therapy.
The recommended dose – 1250 mg / m2 day 1 and 8 of each 21-day cycle, or 1000 mg / m2 of 1, 8 and 15 days of each 28-day cycle. Cisplatin was administered at a dose of 70 mg / m2 on day 1 of the cycle after the infusion of gemcitabine on the background overhydration.
Breast Cancer (locally advanced or disseminated)
monotherapy.
With the progression of the disease after the first line therapy including anthracyclines or without (with contraindications application anthracyclines) recommended dose – 1000-1200 mg / m2 of 1, 8 and 15 days every 28 days
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The combination therapy.
As first line therapy at progression neoadyovantnoy therapy with inclusion of anthracyclines. The recommended dose – 1250 mg / m2 day 1 and 8 in combination with paclitaxel 175 mg / m2 after about 3 hours after the administration of gemcitabine on day 1 of each 21 day cycle
.
Bladder Cancer (locally advanced, disseminated or surface)
monotherapy.
The recommended dose – 1250 mg / m2 of 1, 8 and 15 days every 28 days
.
The combination therapy.
The recommended dose – 1000 mg / m2- 1, 8 and 15 days in combination with cisplatin, which is administered in a dose of 70 mg / m2 immediately after the infusion of gemcitabine of 1 or 2 day during each 28-day cycle
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Intravesical chemotherapy The recommended dose -. 2000 mg. For solution preparation installations are dissolved in 100 ml of 50 or 0.9% sodium chloride solution to a concentration of 20 to 40 mg / ml. Exposure of the drug is 60 minutes. Is administered once a week for 6 weeks. The concentration of the solution should not exceed 40 mg / ml.
Epithelial ovarian cancer (locally advanced or disseminated).
monotherapy.
The recommended dose – 800-1250 mg / m2 to 1, 8 and 15 days every 28 days
.
The combination therapy.
The recommended dose – 1000 mg / m2 day 1 and 8 in combination with carboplatin, which is administered immediately after the infusion of gemcitabine on day 1 of each 21-day cycle
.
Pancreatic Cancer (locally advanced or disseminated).
monotherapy.
The recommended dose – 1000 mg / m2 once weekly for seven weeks followed by one week apart. Subsequent cycles should consist of infusions, held once a week for 3 weeks followed by one week apart.
Cervical Cancer (locally advanced or disseminated).
The combination therapy.
When the sequential mestnorasprostranonnom cancer chemoradiotherapy (neoadjuvant) and metastatic cancer, gemcitabine is administered at a dose of 1250 mg / m2 day 1 and 8 of a 21 day cycle. Cisplatin is administered after the administration of gemcitabine at a dose of 70 mg / m2 day 1 cycle every 21 days on a background overhydration.
When mestnorasprostranonnom cancer with simultaneous chemoradiotherapy 1 time per week for 1-2 hours before the radiation therapy is administered in a dose of gemcitabine is 125 mg / m2, followed by (directly after gemcitabine administration) administration of cisplatin at a dose of 40 mg / m2.
In the case of hematological toxicity of gemcitabine dose can be reduced or its administration delayed in accordance with the following scheme:

The absolute granulocyte count (in 1 ul) No. of platelets (in 1 l)% of the previous dose > 1000i > 100000100500-1000ili50000-10000075 < 500ili < 50000Otlozhit introduction

To identify hematological toxicity necessary to carry out regular inspection of the patient and monitoring of liver and kidney function. Depending on the degree of toxicity of the dose can be reduced in the course of each cycle or the beginning of a new cycle of steps.
The decision to postpone the next administration should be based on clinical assessment of physician speakers toxicity.
Special patient groups
Elderly patients: evidence to suggest that elderly patients need to adjust the dose, is not available, although gemcitabine clearance and half-life vary with age
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Patients with impaired liver and kidney function: to use gemcitabine in patients with hepatic insufficiency or with impaired renal function, care should be taken as sufficient data on the use of the drug in this category of patients there. Mild to moderate renal impairment (creatinine clearance of 30 ml / min to 80 mL / minute) has no marked effect on the pharmacokinetics of Gemcitabine.
Children: the use of gemcitabine in children has not been studied

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Storage conditions

In a dry place, protected from light, at a temperature of 15-30 ° C

Active substance

Gemcitabine

Interaction

Gemtsitover has a radiosensitizing effect, so when using the drug on a background radiation therapy can be expected to enhance radiation reactions. Reduces the production of antibodies and increases the side effects associated with simultaneous use of inactivated or live virus vaccines (the interval between the application of medicaments to be from 3 to 12 months.). Immunosuppressants (azathioprine, chlorambucil, corticosteroids, cyclophosphamide, cyclosporine, mercaptopurine) increase the risk of infections.

Special conditions

Gemtsitoverom treatment can be carried out only under the supervision of a physician who is experienced in the use of anticancer chemotherapy. Before each administration of the drug is necessary to control the number of platelets, leukocytes and neutrophils in the blood. When signs of bone marrow suppression necessary to stop treatment or adjust the dose. Periodically assess kidney and liver function. Increasing the duration and frequency of infusion infusion leads to an increase in toxicity. Gemcitabine with metastases in the liver, hepatitis and alcoholism in history, as well as in liver cirrhosis increases the risk of liver failure. If you experience the first signs of hemolytic-uremic syndrome treated with gemcitabine should be stopped. In patients with lung cancer or lung metastases increased risk of side effects from the respiratory system. At the first signs of pneumonitis or appearance of infiltrates in the lung gemcitabine treatment should cease. Gemcitabine can be administered after starting the permission of acute radiation reactions or not earlier than 7 days after the radiotherapy. Women and men during treatment with gemcitabine and for at least 6 months should use reliable methods of contraception. The treatment should be careful when driving and other lesson potentially dangerous activities which require high concentration and psychomotor speed reactions.

Overdose

Symptoms: Myelosuppression, paresthesias, severe skin rash. Treatment: No specific antidote. In case of suspected overdose patient must be under constant medical supervision, including the blood count of the formula; if necessary, symptomatic treatment.