Zefei

Zefei

gemcitabine

Manufacturer:

Jiangsu Hansoh

Distributor:

Goodfellow
Full Prescribing Info
Contents
Gemcitabine HCl.
Description
Gemcitabine HCl is a nucleoside analogue that exhibits antitumor activity. Gemcitabine HCl is 2'-deoxy-2',2'-difluorocytidine monohydrochloride (b-isomer). The empirical formula is C9H11F2N3O4·HCl. It has a molecular weight of 299.66. Gemcitabine HCl is a white to off-white solid. It is soluble in water, slightly soluble in methanol and practically insoluble in ethanol and polar organic solvents.
Action
Pharmacology: Gemcitabine exhibits cell phase specificity, primarily killing cells undergoing DNA synthesis (S-phase) and also blocking the progression of cells through the G1/S phase boundary. Gemcitabine is metabolized intracellularly by nucleoside kinases to the active diphosphate (dFdCDP) and triphosphate (dFdCTP) nucleosides. The cytotoxic effect of gemcitabine is attributed to a combination of 2 actions of the diphosphate and the triphosphate nucleosides, which leads to the inhibition of DNA synthesis. First, gemcitabine diphosphate inhibits ribonucleotide reductase, which is responsible for catalyzing the reactions that generate the deoxynucleoside triphosphates for DNA synthesis. Inhibition of this enzyme by the diphosphate nucleoside causes a reduction in the concentrations of deoxynucleotides, including dCTP. Second, gemcitabine triphosphate competes with dCTP for incorporation into DNA. The reduction in the intracellular concentration of dCTP (by the action of the diphosphate) enhances the incorporation of gemcitabine triphosphate into DNA (self-potentiation).
Indications/Uses
Non-Small Cell Lung Cancer: Zefei is indicated in combination with cisplatin for the first-line treatment of patients with inoperable, locally advanced (stage IIIA or IIIB) or metastatic (stage IV) non-small cell lung cancer.
Pancreatic Cancer: Zefei is indicated as first-line treatment for patients with locally advanced (nonresectable stage II or stage III) or metastatic (stage IV) adenocarcinoma of the pancreas. It is also indicated for patients previously treated with 5-FU.
Dosage/Direction for Use
Zefei is for IV use only.
Adults: Single-agent for Pancreatic Cancer: Administered by IV infusion at a dose of 1000 mg/m2 over 30 min once weekly for up to 7 weeks (or until toxicity necessitates reducing or holding a dose), followed by a week of rest from treatment. Subsequent cycles should consist of infusions once weekly for 3 consecutive weeks out of every 4 weeks.
Combination Use for Non-Small Cell Lung Cancer: With the 4-week schedule, gemcitabine HCl should be administered IV at 1000 mg/m2 over 30 min on days 1, 8 and 15 of each 28-day cycle. Cisplatin should be administered IV at 100 mg/m2 on day 1 after the infusion of gemcitabine HCl. With the 3-week schedule, gemcitabine HCl should be administered IV at 1250 mg/m2 over 30 min on days 1 and 8 of each 21-day cycle. Cisplatin at a dose of 100 mg/m2 should be administered IV after the infusion of gemcitabine HCl on day 1.
Dosage Modification: Dosage adjustment for hematologic toxicity maybe required for gemcitabine HCl and cisplatin.
Reconstitution: To reconstitute, add 5 mL of 0.9% sodium chloride injection to the 200 mg vial or 25 mL of sodium chloride injection to the 1 g vial.
When prepared as directed, solutions are stable for 24 hrs at 25°C. Discard the unused portion.
Warnings
Prolongation of the infusion beyond 60 min and more frequent than weekly dosing have been shown to increase toxicity.
Special Precautions
Patients receiving Zefei should be monitored prior to each dose with complete blood count (CBC) including differential and platelet, leukocyte and granulocyte count. Suspension or modification of therapy should be considered when marrow suppression is detected.
Laboratory evaluation of renal and hepatic function should be performed prior to initiation of therapy and periodically thereafter.
Use in pregnancy: Gemcitabine HCl can cause fetal harm when administered to a pregnant woman. If gemcitabine HCl is used during pregnancy, or if the patient becomes pregnant while taking gemcitabine HCl, the patient should be apprised of the potential hazard to the fetus.
Use In Pregnancy & Lactation
Use in pregnancy: Gemcitabine HCl can cause fetal harm when administered to a pregnant woman. If gemcitabine HCl is used during pregnancy, or if the patient becomes pregnant while taking gemcitabine HCl, the patient should be apprised of the potential hazard to the fetus.
Adverse Reactions
Anemia, leukocytopenia, thrombocytopenia, elavation of liver transaminase enzymes, or alkaline phosphatase, nausea and vomiting, diarrhea or mild constipation, moderate proteinuria and hematuria, dyspnea, allergic skin reactions, anaphylactoid reaction, somnolence, flu-like symptoms, edema, alopecia, oral soreness and erythema.
Storage
Store at temperature not exceeding 25°C.
ATC Classification
L01BC05 - gemcitabine ; Belongs to the class of antimetabolites, pyrimidine analogues. Used in the treatment of cancer.
Presentation/Packing
Powd for inj (vial, lyophilized powder) 200 mg x 1's. 1 g x 1's.
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