Gemcitabine - instructions for use, dose, side effects, contraindications

Structural analogue of pyrimidine. With the participation of nucleoside kinase is metabolized intracellularly to the active diphosphate (dFdCDP) and triphosphate (dFdCTP) nucleosides, which are attached to the synthesized DNA helix. The additional nucleoside in the helix leads to a complete inhibition of the synthesis of deoxyribonucleic acid and the death of the tumor cell.

Pharmacokinetics:

After intravenous administration, the maximum concentration in the blood plasma is reached after 30 minutes. The connection with plasma proteins is less than 10%.

Metabolism in the liver, kidney and blood enzyme cytidine-deaminase to the inactive metabolite of uracil.

The half-life is 32-94 minutes. The half-life of the active metabolite of triphosphate (dFdCTP) nucleoside is 0.7-12 hours. Elimination by the kidneys in the form of uracil metabolite.

Indications:

It is used for the treatment of non-small cell and small cell lung cancer, ovary, prostate. Used in advanced stages of breast, kidney, pancreas and bladder cancer.

ICD-10

II.C15-C26.C24 Malignant neoplasm of other and unspecified parts of bile ducts

II.C15-C26.C25 Malignant neoplasm of pancreas

II.C30-C39.C34 Malignant neoplasm of bronchi and lungs

II.C50 Malignant neoplasm of breast)

II.C51-C58.C53 Malignant neoplasm of cervix

II.C51-C58.C56 Malignant neoplasm of ovary

II.C60-C63.C62 Malignant neoplasm of testis

II.C64-C68.C67 Malignant neoplasm of bladder

Contraindications:

Leukopenia, thrombocytopenia, immunodeficiency, severe impairment of liver and kidney function, individual intolerance, children under 18 years of age.

Carefully:

Dysfunction of the liver, hypersensitivity.

Pregnancy and lactation:

Recommendations for FDA - Category D. Contraindicated in pregnancy and lactation.

Dosing and Administration:

Intravenous drip 1 g / m² body surface for 30 minutes once a week for 3 weeks. The second course is held after 1 week.

Side effects:

Central and peripheral nervous system: weakness, drowsiness, paresthesia.

Respiratory system: dyspnea, transient bronchospasm, rarely pulmonary edema.

Hemopoietic system: anemia, thrombocytopenia, and leukopenia.

The cardiovascular system: arterial hypotension, rarely arrhythmia, myocardial infarction.

Digestive system: nausea, vomiting, diarrhea, rarely constipation.

Dermatological reactions: hyperhidrosis, vesicular rash, stomatitis, eczema, alopecia.

Urinary system: proteinuria, hematuria, peripheral edema, rarely renal failure.

Allergic reactions.

Overdose:

Cases of overdose are not described.

Treatment is symptomatic.

Interaction:

Has a radiosensitizing effect, so the use of the drug against the background of radiation therapy increases the risk of complications. It is allowed to take the drug no earlier than one week after radiation therapy.

Previous therapy with cytostatics increases the risk and severity of leukocytopenia and thrombocytopenia.

Special instructions:

Weekly monitoring of the composition of peripheral blood. With a decrease in the number of leukocytes to 500-1000 in 1 mm³ and platelets to 50-100 thousand in 1 mm³ a dose reduction of up to 70% is recommended. With a decrease in the number of leukocytes less than 500 in 1 mm³and platelets less than 50 thousand in 1 mm³ it is recommended to cancel the drug.

Should be planted gemcitabine only 0,9% solution of sodium chloride without preservatives and only to the maximum solution concentration 40 mg / ml, since in a higher concentration gemcitabine dissolves not completely.

In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

Instructions

Gemcitabine (Gemcitabinum)