Hemite vial, 200 mg (gemcitabine)

Latin name

GEMITA

Release form

Lyophilisate for solution for infusion.

Packing

In a bottle of 200 mg. In a cardboard box 1 bottle.

Pharmacological action

Pharmacodynamics

Antitumor drug, antimetabolite group of pyrimidine analogues, inhibits DNA synthesis. It shows cyclospecificity, acting on cells in phase S and at the boundary of phases G1 and S. It is metabolized in the cell under the action of nucleoside kinases to active diphosphate and triphosphate nucleosides. Diphosphate nucleosides inhibit the action of ribonucleotide reductase (the only enzyme that catalyzes the formation of deoxynucleoside triphosphates necessary for DNA synthesis). Triphosphate nucleosides are able to integrate into the DNA chain (to a lesser extent RNA), which leads to the cessation of further DNA synthesis and programmed cell lysis (apoptosis).

Gemcitabine is also a powerful radiosensitizing agent, even at concentrations lower than cytotoxic.

Pharmacokinetics of

Cmax gemcitabine (3.2 μg / ml to 45.5 μg / ml) is achieved 5 minutes after the end of the infusion. A pharmacokinetic analysis of single and multiple dose studies indicates that Vd is highly gender dependent. The binding of gemcitabine to plasma proteins is negligible.

In the body, gemcitabine is rapidly metabolized by the action of cytidine deaminase in the liver, kidneys, blood and other tissues, resulting in the formation of gemcitabine mono-, di- and triphosphates, of which gemcitabine di- and triphosphates are considered active.

Gemcitabine is rapidly excreted by the kidneys mainly in the form of an inactive metabolite of 2'-deoxy-2 ', 2'-difluoruridine. Less than 10% of the iv dose is found in the urine in the form of unchanged gemcitabine. Systemic clearance, which ranges from about 30 l / h / m2 to 90 l / h / m2, depends on age and gender.

T1 / 2 ranges from 42 minutes to 94 minutes. Subject to the recommended dosage regimen, complete elimination of gemcitabine occurs within 5-11 hours from the start of the infusion. When administered once a week, gemcitabine does not accumulate in the body.

Combination therapy with gemcitabine and paclitaxel. With the joint administration of gemcitabine and paclitaxel, the pharmacokinetics of the drugs does not change.

Combination therapy with gemcitabine and carboplatin. With the joint administration of gemcitabine and carboplatin, the pharmacokinetics of gemcitabine does not change.

Impaired renal function. Mild to moderate renal failure (creatinine clearance 30-80 ml / min) does not significantly affect the pharmacokinetics of gemcitabine.

Indications

Locally advanced or metastatic non-small cell lung cancer as first-line therapy in combination with cisplatin and monotherapy in elderly patients with a functional status of 2 (ECOG-BOP)

inoperable, locally relapsing cancer or locally relapsing cancer glands after neoadjuvant and / or adjuvant therapy with the inclusion of anthracyclines in the absence of contraindications to their appointment as part of combination therapy with locally distributed paclitaxel

n or metastatic urothelial cancer (cancer of the bladder, renal pelvis, ureter, urethra)

locally advanced or metastatic ovarian cancer as monotherapy or in combination with carboplatin in patients with disease progression after the first line of therapy with platinum-containing

preparations locally advanced or metastatic pancreatic cancer

locally advanced or metastatic cancer cervix.

Contraindications

Pregnancy

lactation

children under 18 years of age (lack of sufficient data on efficacy and safety)

hypersensitivity to the active substance or to any of the excipients.

With caution: the drug should be prescribed in case of impaired liver and / or kidney function, inhibition of bone marrow hematopoiesis (including against the background of concomitant radiation or chemotherapy), cardiovascular diseases, with metastatic liver damage, hepatitis, alcoholism, with simultaneous radiation therapy acute infectious diseases of a viral, fungal or bacterial nature (including chickenpox, shingles).

Use during pregnancy and lactation

The use of the drug during pregnancy and the period of lactation (breastfeeding) are contraindicated.

Composition

1 vial contains:

Active substances: gemcitabine hydrochloride 227.72 mg, which corresponds to a gemcitabine content of 200 mg.

Excipients: mannitol - 200 mg, sodium acetate trihydrate - 12.5 mg, hydrochloric acid - qs to adjust the pH, sodium hydroxide - qs to adjust the pH.

Side effects of

Adverse reactions that occurred more frequently than in single cases are listed according to the following gradation: very often (> 10%)

often (> 1% to <10%)

infrequently (> 0.1% to < 1%)

rarely (> 0.01% to <0.1%)

very rare (<0.01%).

From the hemopoietic organs: very often - leukopenia, neutropenia, thrombocytopenia, anemia often - febrile neutropenia very rarely - thrombocytosis.

From the digestive system: very often - nausea, vomiting, increased activity of hepatic transaminases (AST, ALT), alkaline phosphatase often - anorexia, diarrhea, constipation, stomatitis, increased bilirubin concentration rarely - increased GGT activity.

From the urinary system: very often - mild hematuria and proteinuria rarely - renal failure, clinical signs and symptoms similar to hemolytic uremic syndrome (decreased hemoglobin, thrombocytopenia, increased concentration of bilirubin, creatinine, urea and / or LDH activity in blood serum).

From the skin and subcutaneous tissues: very often - skin rashes accompanied by itching, alopecia often - itching, excessive sweating rarely - ulceration of the skin, blistering very rarely - severe skin reactions, including desquamation and bullous rashes.

From the respiratory system: very often - shortness of breath often - cough, rhinitis infrequently - bronchospasm, interstitial pneumonitis, pulmonary edema rarely - acute respiratory distress syndrome.

From the cardiovascular system: rarely - lowering blood pressure, myocardial infarction, heart failure, arrhythmia.

From the nervous system: often - headache, increased drowsiness, insomnia.

Other: very often - flu-like syndrome, peripheral edema often - fever, chills, asthenia, back pain, myalgia infrequently - facial swelling very rarely - anaphylactic reactions.

Drug Interaction

Radiotherapy

Concomitant radiotherapy (concomitant with the introduction of hematite or at intervals <7 days prior to treatment): in this situation, the toxicity of treatment depends on many factors, including dose, radiation therapy, the nature of the irradiated tissue and its volume. Gemcitabine has been shown to have radiosensitizing activity. In one study where patients with non-small cell lung cancer received gemcitabine at a dose of 1000 mg / m2 for 6 consecutive weeks in combination with therapeutic radiation to the chest area, significant toxicity was observed in the form of severe and potentially life-threatening mucosal inflammation esophagitis and pneumonitis, especially in patients with high tissue irradiation (median irradiated tissue volume 4795 cm3). Subsequent studies have shown that the combination of lower doses of gemcitabine and radiation therapy is better tolerated by patients and is characterized by a predictable toxicity profile. For example, in one phase II study, patients with non-small cell lung cancer were treated with radiation at a dose of 60 Gy together with the administration of gemcitabine (600 mg / m2 4 times) and cisplatin (80 mg / m2 2 times) for 6 weeks.

Sequential therapy (break> 7 days): According to existing data, the introduction of gemcitabine more than 7 days before the start of radiation therapy or more than 7 days after its completion is not accompanied by increased toxicity, except for skin lesions associated with the introduction of chemotherapy after irradiation . Gemcitabine treatment may be initiated 7 days after irradiation or after resolution of all acute radiation reactions.

Concomitant and sequential use of gemcitabine and radiation therapy may cause radiation damage to the irradiated tissues (eg, esophagitis, colitis, and pneumonitis).

Other types of interaction

When used with live attenuated vaccines, intensification of the vaccine replication process, enhancement of its adverse / adverse effects, and / or decreased antibody production in the patient's body in response to the administration of the vaccine.

Immunosuppressants (including azathioprine, chlorambucil, GCS, cyclophosphamide, cyclosporine, mercaptopurine) increase the risk of infection.

No compatibility studies have been performed on hematite. It is not recommended to mix Hemit preparation with other medicines.

Overdose

The antidote for gemcitabine is unknown. With the introduction of the drug Gemit in doses up to 5700 mg / m2 in / in a drop for 30 min every 2 weeks the level of toxicity of treatment remained acceptable. If gemcitabine overdose is suspected, the degree of cytopenia should be monitored and supportive therapy prescribed.

Storage conditions

Keep out of the reach of children at a temperature not exceeding 25 ° C. Do not freeze.

Expiration

2 years.

Deystvuyuschee substances

gemcitabine



pharmacy terms and conditions

prescription

Dosage form

Dosage form

solution for infusions

Fresenius Kabi, Germany



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