Gemzar
Gemzar: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Gemzar
ATX code: L01BC05
Active ingredient: gemcitabine (gemcitabinum)
Producer: Eli Lilly Vostok SA, Switzerland
Description and photo update: 2019-13-08
Prices in pharmacies: from 740 rubles.
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Gemzar is an antimetabolite from the group of pyrimidine analogs, an antineoplastic drug.
Release form and composition
The dosage form of Gemzar is a lyophilisate for the preparation of a solution for infusion (in glass bottles, 1 bottle in a cardboard box).
Active ingredient: gemcitabine (in the form of hydrochloride), in 1 bottle - 200 or 1000 mg.
Additional components: mannitol, sodium acetate.
Pharmacological properties
According to the instructions, Gemzar has a cytostatic and antitumor effect.
Pharmacodynamics
Gemcitabine is an antimetabolite belonging to the group of pyrimidine analogs. The substance is characterized by cyclo-specificity, affecting cells in the S phases (replication stage) and Gi / S (the interval between the initial growth stage and the replication stage).
Gemcitabine is involved in intracellular metabolic processes, undergoing transformation under the action of nucleoside kinases and forming triphosphate and diphosphate nucleosides with pharmacological activity. Diphosphate nucleosides inhibit the activity of ribonucleotide reductase, which is the only catalyst for the reactions resulting in the formation of deoxynucleoside triphosphates. The latter are required for the production of deoxyribonucleic acid (DNA).
Triphosphate nucleosides are active competitors of deoxycytidine triphosphate in the processes of incorporation into RNA and DNA. When the intracellular metabolites of gemcitabine are inserted into the DNA chain, its growing strands are replenished with one more additional nucleotide. This leads to the complete inhibition of further DNA production and apoptosis - programmed cell death.
Pharmacokinetics
Gemcitabine is excreted from the body quickly enough through the kidneys, mainly in the form of a metabolite of 2'-deoxy-2 ', 2'-difluoruridine, which does not exhibit pharmacological activity. When Gemzar is administered intravenously, less than 10% of the dose that has entered the body is excreted in the urine unchanged. Gemcitabine binds to plasma proteins to a small extent.
The results of pharmacokinetic studies, in which doses were administered both once and repeatedly, demonstrate that the volume of distribution is significantly dependent on gender. Systemic clearance, which ranges from 30–90 l / h / m 2, also depends on gender and age. The half-life is 32 to 94 minutes.
Indications for use
Locally advanced and metastatic cancer of the following organs:
- Bladder;
- Ureter;
- Pelvis;
- Urethra;
- Pancreas;
- Cervix;
- Ovaries (as a monopreparation or in combination with carboplatin in patients with progressive disease after the end of the first line of therapy with platinum derivatives);
- Non-small cell lung cancer (first-line therapy in combination with carboplatin or cisplatin, as well as as a monopreparation in elderly patients with functional status 2).
Gemzar is also effective for the following diseases:
- Biliary tract cancer;
- Advanced small cell lung cancer;
- Advanced refractory testicular cancer;
- Metastatic, locally recurrent and unresectable breast cancer (in combination with paclitaxel after adjuvant and / or neoadjuvant therapy with anthracyclines, if there were no contraindications to them).
Contraindications
Absolute:
- Pregnancy;
- Lactation;
- Age under 18;
- Hypersensitivity to the drug.
Relative (due to the risk of complications, special care should be taken):
- Acute infectious diseases of fungal, bacterial and viral origin;
- Impaired renal / liver function;
- Inhibition of bone marrow hematopoiesis, including as a result of concomitant chemotherapy or radiation therapy.
Instructions for the use of Gemzar: method and dosage
The solution prepared from the lyophilisate is injected intravenously over 30 minutes. Only 0.9% sodium chloride solution (without preservatives) is used as a solvent: the contents of the 200 mg bottle are dissolved in at least 5 ml, and the 1000 mg bottle is dissolved in 25 ml of solution, after which the bottle is gently shaken until the powder is completely dissolved (the solution should be transparent, do not have mechanical impurities).
Before administration, the prepared gemcitabine solution containing the required dose is diluted with 0.9% sodium chloride solution in an amount sufficient for a 30-minute intravenous infusion.
Recommended doses of Gemzar, depending on indications and treatment regimens:
Locally advanced or metastatic non-small cell lung cancer, first line of therapy:
- Monotherapy: 1000 mg / m 2 on the 1st, 8th and 15th days of each 28-day cycle;
- Combination therapy with cisplatin: 1250 mg / m 2 in the 1st and 8th days of each 21-day cycle, or 1000 mg / m 2 in 1st, 8th and 15th days of each 28-day cycle … Cisplatin is administered on the 1st day of the cycle against the background of overhydration after Gemzar infusion at a dose of 70 mg / m 2;
- Combined therapy with carboplatin: 1000 or 1200 mg / m 2 on the 1st and 8th days of each 21-day cycle. Carboplatin is administered on the 1st day of the cycle after Gemzar infusion at a dose based on AUC 5 mg / ml / minute.
Locally advanced, metastatic or platinum-resistant epithelial ovarian cancer:
- Monotherapy: 800-1250 mg / m 2 on the 1st, 8th and 15th days of each 28-day cycle;
- Combined therapy with carboplatin: 1000 mg / m 2 on the 1st and 8th days of each 21-day cycle. Carboplatin is administered on the 1st day of each cycle immediately after the Gemzar infusion at a dose of 4 mg / ml / min AUC.
Urothelial cancer (superficial, locally advanced and metastatic bladder cancer, cancer of the urethra, ureter, renal pelvis):
- Monotherapy: 1250 mg / m 2 on the 1st, 8th and 15th days of each 28-day cycle;
- Combination therapy with cisplatin: Gemzar is administered at 1000 mg / m 2 on the 1st, 8th and 15th days of each 28-day cycle, cisplatin - on the 1st or 2nd day of the cycle immediately after the infusion of Gemzar in a dose 70 mg / m 2.
For locally recurrent, metastatic, unresectable breast cancer, combination therapy with paclitaxel is performed (with the progression of the disease after neoadjuvant and / or adjuvant therapy with anthracyclines (provided that there are no contraindications to them) as first-line therapy): paclitaxel is slowly injected intravenously within 3 hours) at a dose of 175 mg / m 2 on the 1st day of the 21-day cycle before gemcitabine, Gemzar is administered at 1250 mg / m 2 on the 1st and 8th days of each 21-day cycle. Before starting such therapy, check the absolute number of granulocytes in the blood - it must be at least 1500 / μl.
For locally advanced, metastatic (including those resistant to 5-fluorouracil therapy) pancreatic cancer, monotherapy is carried out with the drug: for 7 weeks - 1000 mg / m 2 once a week, followed by a 7-day break, then in this the same dose on the 1st, 8th and 15th days of each 28-day cycle.
In cancer of the biliary tract, a combination therapy with cisplatin is performed. Cisplatin are administered on a background of overhydration at one-day cycle at a dose of 70 mg / m 2 before the administration of gemcitabine. Gemzar is administered at 1250 mg / m 2 on the 1st and 8th days of each 21-day cycle.
For locally advanced or metastatic cervical cancer, combined therapy with cisplatin is performed. With locally advanced cancer and sequential chemoradiation therapy (neoadjuvant), as well as with metastatic cancer, cisplatin is administered against the background of overhydration on the 1st day of the cycle before gemcitabine at a dose of 70 mg / m 2. Gemzar is administered at 1250 mg / m 2 on the 1st and 8th days of each 21-day cycle.
For locally advanced cancer and simultaneous chemoradiation therapy, cisplatin is administered at a dose of 40 mg / m 2. Gemzar is administered 1 time in 7 days at a dose of 125 mg / m 2 immediately after the administration of cisplatin, 1-2 hours before the start of radiation therapy.
Dose adjustment
If hematological toxicity develops during the period of therapy, the administration of Gemzar should be postponed or the dose of gemcitabine should be reduced in accordance with the following regimens.
In-cycle dose adjustments (as monotherapy or in combination with cisplatin) for pancreatic cancer, non-small cell lung cancer and urothelial cancer:
- The absolute number of granulocytes in 1 μl> 1000 and the number of platelets in 1 μl> 100,000: the dose is not changed;
- The absolute number of granulocytes in 1 μl 500-1000 or the number of platelets in 1 μl 50,000-100,000: 75% of the previous dose;
- Absolute granulocyte count in 1 μl <500 or platelet count in 1 μl <50,000: administration should be delayed.
Cycle dose adjustment (in combination with paclitaxel) for breast cancer:
- Absolute granulocyte count in 1 μl ≥1200 and platelet count in 1 μl> 75,000: dose does not change;
- The absolute number of granulocytes in 1 μl 1000 - <1200 or the number of platelets in 1 μl 50,000-75,000: 75% of the previous dose;
- The absolute number of granulocytes in 1 μl 700 - <1000 and the number of platelets in 1 μl ≥50,000: 50% of the previous dose;
- Absolute granulocyte count in 1 μl <700 or platelet count in 1 μl <50,000: administration should be delayed.
Dose adjustments within the cycle (in combination with carboplatin) for ovarian cancer:
- Absolute granulocyte count in 1 μl> 1500 and platelet count in 1 μl ≥100,000: dose does not change;
- The absolute number of granulocytes in 1 μl 1000-1500 or the number of platelets in 1 μl 75 000-100 000: 50% of the previous dose;
- Absolute granulocyte count in 1 μl <1000 or platelet count in 1 μl <75,000: administration should be delayed.
In cases where it is necessary to postpone the introduction of Gemzar, the duration of the break is determined by the doctor.
In order to timely identify non-hematological toxicity, the patient should be regularly examined, the functions of his kidneys and liver should be monitored. Depending on the identified degree of toxicity, the dose can be reduced stepwise at the beginning of a new cycle or during each cycle.
Side effects
- Hematopoietic system: very often (≥10%) - thrombocytopenia, leukopenia and anemia; often (≥1%, <10%) - febrile neutropenia; very rarely (<0.01%) - thrombocytosis;
- Respiratory system: very often - shortness of breath; often - rhinitis and cough; infrequently (≥0.1%, <1%) - bronchospasm;
- Cardiovascular system: very often - edema (including peripheral); infrequently - arrhythmia (more often supraventricular); rarely (≥0.01%, <0.1%) - decrease in blood pressure, myocardial infarction;
- Nervous system: often - drowsiness, sleep disturbances, headache;
- Digestive system: very often - nausea and vomiting, functional impairment of the liver (usually mild, so discontinuation of treatment is rarely required); often - stomatitis, diarrhea and constipation;
- Urinary system: very often - hematuria, mild proteinuria;
- Musculoskeletal system: often - back pain, myalgia;
- Skin and subcutaneous tissue: very often - mild skin rash with itching, alopecia (usually minor); often - sweating, itching; rarely - vesicles, ulcers;
- Allergic reactions: very rarely - anaphylactic and anaphylactoid reactions;
- Others: very often - flu-like syndrome (headache, malaise, asthenia, chills, fever); rarely - reactions at the injection site.
In the post-marketing period, the following side effects were also noted:
- Cardiovascular system: infrequently - heart failure; rarely - peripheral vasculitis, gangrene; very rarely - syndrome of increased capillary permeability;
- Respiratory system: infrequently - interstitial pneumonitis; rarely - pulmonary edema, respiratory distress syndrome;
- Digestive system: very rarely - ischemic colitis;
- Urinary system: infrequently - hemolytic uremic syndrome;
- Biliary tract and liver: very often - increased alkaline phosphatase, aspartate aminotransferase, alanine aminotransferase; often - an increase in the concentration of bilirubin; infrequently - severe hepatotoxicity, incl. liver failure; rarely - increased activity of gamma glutamyl transferase;
- Skin and subcutaneous tissues: rarely - severe skin reactions, incl. bullous skin lesions and desquamation;
- Others: very rarely - Stevens-Johnson and Lyell syndromes, radiation reactions.
Overdose
To date, the specific antidote for gemcitabine remains unknown. With intravenous administration of single doses of Gemzar, not exceeding 5.7 g / m 2, clinically acceptable toxicity was observed for 30 minutes every 2 weeks.
If a specialist suspects an overdose, the patient should undergo regular medical monitoring, including counting the blood count. If necessary, the patient is prescribed a course of symptomatic treatment.
special instructions
Treatment with Gemzar should be carried out only under the supervision of a medical specialist with experience in anticancer therapy.
Before each administration of the drug, the number of leukocytes, granulocytes and platelets in the blood should be monitored. If signs of bone marrow function suppression appear, it is necessary to adjust the dose or suspend the use of Gemzar.
It is also necessary to regularly examine the patient and assess the functions of his liver and kidneys. The introduction of gemcitabine in liver cirrhosis, as well as in alcoholism, hepatitis and liver metastases in the anamnesis increases the risk of developing liver failure.
With an increase in the duration and frequency of Gemzar infusion, toxicity increases.
Studies on the influence of Gemzar on the speed of reactions and the ability to concentrate have not been conducted. However, the drug may cause drowsiness, especially if you drink alcohol together. Patients who experience drowsiness during treatment should refrain from driving vehicles and working with complex mechanisms.
Application during pregnancy and lactation
The safety of using Gemzar in pregnant women has not been studied. Experimental studies have shown that fetotoxic and embryotoxic effects are characteristic of gemcitabine. Also, the substance negatively affects the course of pregnancy and the further postnatal development of the child. For this reason, it is not recommended to prescribe Gemzar to pregnant women. During treatment, women of reproductive age should use reliable contraception. If it is necessary to use the drug during lactation, you should refuse breastfeeding.
Drug interactions
When using Gemzar during the period of radiation therapy or with an interval of less than 7 days, toxicity is noted.
During the course of treatment with gemcitabine, live yellow fever vaccines or other live vaccines should not be administered, as the risk of developing a systemic disease leading to death, especially in immunosuppressed patients, increases.
Analogs
The analogues of Gemzar are: Xeloda, Oncoril, Hertsizar, Cytogem, Vizgem, Viztar, Laracite, Cytin, Cytarabin, Ental, Hematix, Gemcitabine, Gemcitera, Hemite, Gemcitar, Gemcybin, Oncohem, Ongetsin, Tolgecitrig, Dertsin.
Terms and conditions of storage
Store at a temperature of 15-30 ºС. Keep out of the reach of children.
The shelf life of the lyophilisate is 3 years. The solution prepared from it can be stored for no more than 24 hours at a temperature of 15-30 ºС.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Gemzar
According to reviews, Gemzar is liked by most of the patients who took him, who speak positively about him and are very satisfied with the result of the treatment. As with other chemotherapy drugs, side effects are present when using the drug, but they appear less frequently and are weaker compared to similar drugs. Gemzar has proven itself especially well in the treatment of pancreatic cancer. However, when using the drug, it is imperative to follow the treatment regimen and the doctor's recommendations.
Price for Gemzar in pharmacies
The approximate price for Gemzar with a dosage of 200 mg is about 1118-1210 rubles. The drug with a dosage of 1000 mg can be purchased for approximately 4780–5600 rubles.
Gemzar: prices in online pharmacies
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Drug name Price Pharmacy |
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Gemzar 200 mg lyophilisate for preparation of solution for infusion 10 ml 1 pc. 740 RUB Buy |
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Gemzar lyof. for prigot. solution for inf. 200mg 1149 RUB Buy |
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Gemzar 1 g lyophilisate for preparation of solution for infusion 50 ml 1 pc. 4499 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
