Description
Release form
Lyophilisate for solution for infusion
Packaging
1 fl.
Pharmacological action
Gemcitover – an antitumor agent, antimetabolite.
Gemcitabine is an antimetabolite group of pyrimidine analogues. Suppresses synthesis of deoxyribonucleic acid (DNA). It shows cyclospecificity, acting on cells in phases S and G1 / S. It is metabolized inside the cell under the action of nucleoside kinases with the formation of active diphosphate and triphosphate nucleosides. Diphosphate nucleosides inhibit ribonucleotide reductase, which is the only enzyme that catalyzes the formation of deoxynucleoside triphosphates necessary for DNA synthesis. Triphosphate nucleosides actively compete with deoxycytidine triphosphate for incorporation into DNA and RNA molecules. After embedding intracellular gemcitabine metabolites in the DNA chain, another additional nucleotide is added to its growing strands, which leads to complete inhibition of further DNA synthesis and programmed cell lysis, known as apoptosis.
Indications
Non-small cell lung cancer
Breast cancer
Bladder cancer
Ovarian cancer
Pancreatic cancer
Cervical cancer also has been shown to be and biliary tract cancer.
Contraindications
hypersensitivity to gemcitabine or other components of the drug Gemcitover,
pregnancy and lactation.
With caution: in case of impaired liver and / or kidney function, inhibition of bone marrow hematopoiesis (including the background of concomitant radiation or chemotherapy), with simultaneous radiation therapy, acute infectious diseases of a viral, fungal or bacterial nature (including chickenpox, shingles).
Special instructions
Gemcitover treatment can only be carried out under the supervision of a doctor with experience in the use of antitumor chemotherapy.
Before each administration of the drug, it is necessary to control the number of platelets, white blood cells and neutrophils in the blood. With signs of inhibition of bone marrow function, it is necessary to suspend treatment or adjust the dose.
Periodically, an assessment of kidney and liver function is necessary.
An increase in infusion duration and infusion rate leads to increased toxicity.
Introduction of gemcitabine for liver metastases, with a history of hepatitis and alcoholism, as well as with cirrhosis of the liver, the risk of developing liver failure increases. If the first signs of hemolytic uremic syndrome occur, treatment with gemcitabine should be discontinued.
Patients with lung cancer or lung metastases have an increased risk of side effects from the respiratory system.
When the first signs of pneumonitis or the appearance of infiltrates in the lungs appear, treatment with gemcitabine should be discontinued.
Gemcitabine can be started after the resolution of acute radiation reactions or not earlier than 7 days after the end of radiation therapy.
Women and men should use reliable methods of contraception during treatment with gemcitabine and for at least 6 months after.
During the treatment period, caution should be exercised when driving vehicles and engaging in potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.
Composition
1 bottle contains: active substance: gemcitabine hydrochloride in terms of gemcitabine – 1000 mg
excipients: mannitol, sodium acetate, sodium hydroxide (sodium hydroxide) or hydrochloric acid 1 M
Dosage and administration
Gemcitover is administered intravenously dropwise for 30 minutes.
Non-small cell lung cancer (locally or disseminated) Monotherapy.
The recommended dose of the drug is 1000 mg / m2 once a week for 3 weeks, followed by a weekly break, every 28 days. Combination therapy
The recommended dose is 1250 mg / m2 on days 1 and 8 of each 21-day cycle or 1000 mg / m2 on days 1, 8 and 15 of each 28-day cycle. Cisplatin is administered at a dose of 70 mg / m2 on the 1st day of the cycle after gemcitabine infusion with hyperhydration.
Breast cancer (locally or disseminated)
Monotherapy.
When the disease progresses after the first line of therapy, including or without anthracyclines (with contraindications for the use of anthracyclines), the recommended dose is 1000-1200 mg / m2 on days 1, 8 and 15 every 28 days.
Combination therapy.
As a first-line therapy, with the progression of neoadjuvant therapy, with the inclusion of anthracyclines. The recommended dose of the drug is 1250 mg / m2 on days 1 and 8 in combination with paclitaxel at a dose of 175 mg / m2 about 3 hours after the administration of gemcitabine on day 1 of every 21 day cycle.
Bladder cancer (locally, disseminated, or superficial)
Monotherapy.
The recommended dose is 1250 mg / m2 on days 1, 8 and 15 every 28 days.
Combination therapy.
The recommended dose of the drug is 1000 mg / m2 – on days 1, 8 and 15 in combination with cisplatin, which is administered at a dose of 70 mg / m2 immediately after gemcitabine infusion on 1 or 2 days of each 28-day cycle.
Intravesical chemotherapy. The recommended dose of the drug is 2000 mg. To obtain a solution for installations, the drug is dissolved in 100 or 50 ml 0, 9% sodium chloride solution to a concentration of 20 to 40 mg / ml. The exposure of the drug is 60 minutes. It is administered once a week for 6 weeks. The concentration of the solution should not exceed 40 mg / ml.
Epithelial ovarian cancer (locally or disseminated).
Monotherapy.
The recommended dose of the drug is 800-1250 mg / m2 on days 1, 8 and 15 every 28 days.
Combination therapy.
The recommended dose of the drug is 1000 mg / m2 on days 1 and 8 in combination with carboplatin, which is administered immediately after gemcitabine infusion on day 1 of every 21-day cycle.
Pancreatic cancer (locally or disseminated).
Monotherapy.
The recommended dose is 1000 mg / m2 once a week for 7 weeks, followed by a weekly break. Subsequent cycles should consist of infusions carried out once a week for 3 weeks, followed by a weekly break.
Cervical cancer (locally or disseminated).
Combination therapy.
For locally advanced cancer with sequential chemoradiotherapy (neoadjuvant) and for disseminated cancer, gemcitabine is administered at a dose of 1250 mg / m2 on days 1 and 8 of the 21-day cycle. Cisplatin is administered after administration of gemcitabine at a dose of 70 mg / m2 on 1 day of the cycle every 21 days against the background of hyperhydration.
In case of locally advanced cancer with simultaneous chemoradiotherapy 1 time per week 1-2 hours before the start of radiation therapy, gemcitabine is administered at a dose of 125 mg / m2 followed by (immediately after gemcitabine administration) administration of cisplatin at a dose of 40 mg / m2.
If hematologic toxicity develops, the dose of gemcitabine can be reduced, or its administration can be delayed in accordance with the following scheme:
Absolute granulocyte count (in 1 ?l) Platelet count (in 1 ?l)% of the previous dose
> 1000and> 100000100
500- 1000 or 50000-10000075
<500 or <50000 Postpone the administration of To detect non-hematologic toxicity, regular examination of the patient and monitoring of liver and kidney function are necessary. Depending on the degree of toxicity, the dose can be reduced stepwise during each cycle or with the start of a new cycle. The decision to postpone the next administration of the drug should be based on the doctor s clinical assessment of the dynamics of toxicity. Special patient groups Elderly patients: evidence to suggest that in elderly patients it is necessary to adjust the dose, it is not available, although the clearance of gemcitabine and the elimination half-life change with age. Patients with impaired liver and kidney function: gemcitabine should be used with caution in patients with hepatic impairment or impaired renal function, since there are no sufficient data on the use of the drug in this category of patients. Mild or moderate severity of renal failure (creatinine clearance from 30 ml / min to 80 ml / min) does not significantly affect the pharmacokinetics of gemcitabine. Children: The use of gemcitabine in children has not been studied. Side effects Adverse reactions that occurred more often than in single cases are listed according to the following gradation: very often (> 10%) often (> 1%, <10%) sometimes (> 0.1%, <1 %) rarely (> 0.01%, <0.1%) extremely rarely (<0.01%). From the hemopoietic organs: often – leukopenia, neutropenia, thrombocytopenia, anemia is very rare – thrombocytosis. From the digestive system: very often – nausea, vomiting, increased activity of hepatic transaminases, alkaline phosphatase often – anorexia, diarrhea, constipation, stomatitis, hyperbilirubinemia. From the urinary system: very often – proteinuria and hematuria rarely hemolytic-uremic syndrome and / or renal failure. From the skin and skin appendages: often – skin rashes, pruritus, alopecia. From the respiratory system: very often – shortness of breath often – coughing, rhinitis sometimes – bronchospasm, interstitial pneumonia, pulmonary edema rarely – acute respiratory distress syndrome (if these symptoms occur, treatment should be discontinued). From the cardiovascular system: rarely – lowering blood pressure, myocardial infarction, heart failure, arrhythmia. From the nervous system: often – headache, drowsiness, insomnia, paresthesia. Allergic reactions: very rarely – anaphylactic reactions. Other: very often – flu-like syndrome, peripheral edema often – fever, chills, asthenia, back pain, myalgia sometimes – swelling of the face. Drug interaction Gemcitover has a radiosensitizing effect, therefore, when using the drug against the background of radiation therapy, an increase in radiation reactions can be expected. Reduces the production of antibodies and enhances side effects with the simultaneous use of inactivated or live viral vaccines (the interval between the use of drugs should be from 3 to 12 months). Immunosuppressants (azathioprine, chlorambucil, glucocorticosteroids, cyclophosphamide, cyclosporine, mercaptopurine) increase the risk of infections. Overdose of Symptoms: myelosuppression, paresthesia, severe skin rash. Treatment: there is no specific antidote. If an overdose is suspected, the patient should be under constant medical supervision, including a blood count, if necessary, symptomatic treatment is carried out. Storage conditions In a dry, protected from light at a temperature of 15 to 30 ° C. Keep out of reach of children. Deystvuyuschee substances gemcitabine Pharmacy terms Prescription Form of Treatment simply entails dlya infusing Lance-Farm, Russia
