• 注射用盐酸吉西他滨
ENGLISH NAME: Gemcitabine Hydrochloride for Injection 
SPECIFICATIONS: 0.2 g (according Carboplatin) 
LICENSE NUMBER: 0.2 g  H20113371
PRODUCT PACKAGING: Penicillin Bottle 
FORMULATION: Lyophilized Powder 
STORAGE CONDITION: Shading, Closed, Preservation of the Shade
SHELF LIFE: 24 Months
Description: Gemcitabine Hydrochloride 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. Gemcitabine Hydrochloride for Injection is a nucleoside analogue that exhibits antitumor activity. It is used to treat certain types of lung cancer, bladder cancer, breast cancer, and cancer of the pancreas. It is 2′-deoxy-2′,2′-difluorocytidine monohydrochloride (β–isomer). The clinical formulation is supplied in a sterile form for intravenous use only. 
Pharmacological effects: 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 two actions of the diphosphate and the triphosphate nucleosides, which leads to 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). After the gemcitabine nucleotide is incorporated into DNA, only one additional nucleotide is added to the growing DNA strands. After this addition, there is inhibition of further DNA synthesis. DNA polymerase epsilon is unable to remove the gemcitabine nucleotide and repair the growing DNA strands (masked chain termination). In CEM T lymphoblastoid cells, gemcitabine induces internucleosomal DNA fragmentation, one of the characteristics of programmed cell death. Gemcitabine demonstrated dose–dependent synergistic activity with cisplatin in vitro. No effect of cisplatin on gemcitabine triphosphate accumulation or DNA double–strand breaks was observed. In vivo, gemcitabine showed activity in combination with cisplatin against the LX–1 and CALU–6 human lung xenografts, but minimal activity was seen with the NCI–H460 or NCI–H520 xenografts. Gemcitabine was synergistic with cisplatin in the Lewis lung murine xenograft. Sequential exposure to gemcitabine 4 hours before cisplatin produced the greatest interaction.

Pharmacokinetics: Gemcitabine disposition was studied within one week, 92% to 98% of the dose was recovered, almost entirely in the urine. Gemcitabine (<10%) and the inactive uracil metabolite, 2’-deoxy-2’,2’-difluorouridine (dFdU), accounted for 99% of the excreted dose. The metabolite dFdU is also found in plasma. Gemcitabine plasma protein binding is negligible. Population pharmacokinetic analyses of combined single and multiple dose studies showed that the volume of distribution of gemcitabine was significantly influenced by duration of infusion and gender. Clearance was affected by age and gender. Differences in either clearance or volume of distribution based on patient characteristics or the duration of infusion result in changes in half–life and plasma concentrations. The maximum plasma concentrations of dFdU (inactive metabolite) were achieved up to 30 minutes after discontinuation of the infusions and the metabolite is excreted in urine without undergoing further biotransformation. The metabolite did not accumulate with weekly dosing, but its elimination is dependent on renal excretion, and could accumulate with decreased renal function.

Indications: It is used to treat certain types of lung cancer, bladder cancer, breast cancer, and cancer of the pancreas.

Precautions: Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. This medication can reduce the number of platelet cells in the blood. Your doctor will monitor the number of platelets in your blood with regular blood tests while you are using this medication. Platelets help the blood to clot, and a shortage could make you bleed more easily. Tell your doctor of any signs that your blood is not clotting as quickly. Such symptoms may include black and tarry stools, nosebleeds, bleeding gums, blood in the urine, easy bruising, or cuts that won't stop bleeding.Gemcitabine can cause a fever and flu-like symptoms (chills, feeling unwell) that are not associated with an infection. Your doctor may prescribed acetaminophen to help treat this reaction. As well as killing cancer cells, this medication can reduce the number of cells that fight infection in the body (white blood cells). Avoid contact with people who have contagious infections and tell your doctor if you begin to notice signs of an infection, such as fever or chills. Your doctor will monitor the number of white blood cells in your blood with regular blood tests while you are using this medication. Gemcitabine should not be used during pregnancy. Effective birth control should be used while receiving this medication. Gemcitabine may harm the baby if used during pregnancy. Women receiving gemcitabine should not breast-feed.

Adverse reaction: chills, cough, difficulty sleeping, feeling of illness, fever (not associated with infection), headache, musclepain, runnynose, sweating, weakness, nausea and vomiting, numbness or tingling of hands or feet, severe drowsiness, temporary hair loss. Check with your doctor as soon as possible if any of the following side effects occur: high blood pressure, pain at site of injection, pinpoint-sized red spots on skin, skin rash, sores on mouth or lips, swelling of fingers, feet, or lower legs, unusual tiredness or weakness, vomiting lasting more than 24 hours after treatment.
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