How Effective Is Gemcitabine for Lung Cancer?

Gemcitabine hydrochloride for injection, indications for this product can be used to treat the following diseases:-locally advanced or metastatic non-small cell lung cancer;-locally advanced or metastatic pancreatic cancer;-combination of gemcitabine and paclitaxel, suitable for treatment Recurrence after adjuvant / neo-adjuvant chemotherapy, unresectable, locally recurrent, or metastatic breast cancer. Unless clinically contraindicated, anthracyclines should be used in previous chemotherapy.

Gemcitabine hydrochloride for injection, indications for this product can be used to treat the following diseases:-locally advanced or metastatic non-small cell lung cancer;-locally advanced or metastatic pancreatic cancer;-combination of gemcitabine and paclitaxel, suitable for treatment Recurrence after adjuvant / neo-adjuvant chemotherapy, unresectable, locally recurrent, or metastatic breast cancer. Unless clinically contraindicated, anthracyclines should be used in previous chemotherapy.

Drug Name

Gemcitabine hydrochloride for injection

Drug type

Prescription drugs, medicines for medical workers' injuries

Use classification

Cytotoxic drugs

Gemcitabine Hydrochloride Ingredients for Injection

The main ingredient of this product is gemcitabine hydrochloride.
Chemical name: (+) 2'-deoxy-2'2'-difluorocytosine hydrochloride.
Chemical Structure:

Molecular formula: C ₉ H ₁₁ F ₂ N ₃ O ₄ · HCl
Molecular weight: 299.70
Excipients: mannitol, sodium acetate.

Characteristics of gemcitabine hydrochloride for injection

This product is a white loose block.

Indications for gemcitabine hydrochloride for injection

This product can be used to treat the following diseases:
-Locally advanced or metastatic non-small cell lung cancer;
-Locally advanced or metastatic pancreatic cancer;
Gemcitabine combined with paclitaxel is suitable for the treatment of relapsed, unresectable, locally recurrent or metastatic breast cancer after adjuvant / neo-adjuvant chemotherapy. Unless clinically contraindicated, anthracyclines should be used in previous chemotherapy.

Gemcitabine Hydrochloride for Injection Specifications

0.2g; 1.0g (calculated as gemcitabine).

Gemcitabine Hydrochloride for Injection

This product should be used under the guidance of an experienced oncologist. It is recommended to refer to the existing clinical trial data to adjust the dosage according to the individual clinical situation.
Dosage < br Adult:
Non-small cell lung cancer < br Monotherapy:
The recommended dose of gemcitabine is 1000 mg / m ² , which is administered intravenously for 30 minutes. The drug was administered once a week, and the patient was rested for 1 week after 3 weeks of treatment, and the above 4-week treatment cycle was repeated. Depending on the patient's tolerance to gemcitabine, dose reduction may be considered in each treatment cycle or within a treatment cycle.
Combination therapy:
There are two treatment options for gemcitabine combined with cisplatin: 3-week therapy and 4-week therapy.
3-week therapy: The recommended dose of gemcitabine is 1250 mg / m ² , which is administered intravenously for 30 minutes. Administration was performed every 28 days on the 1st, 8th, and 15th days of the treatment cycle. Depending on the patient's tolerance to gemcitabine, dose reduction may be considered in each treatment cycle or within a treatment cycle.
Pancreatic cancer < br The recommended dose of gemcitabine is 1000 mg / m ² , which is administered intravenously for 30 minutes. Once a week for 7 consecutive weeks, followed by a week off. The subsequent treatment cycle was changed to 4-week therapy: once a week, 3 consecutive weeks of treatment, followed by a rest of 1 week. Depending on the patient's tolerance to gemcitabine, dose reduction may be considered in each treatment cycle or within a treatment cycle.
Breast Cancer < br Gemcitabine is recommended in combination with paclitaxel. Paclitaxel (175 mg / m ² ) was given intravenously on the first day of every 21-day treatment cycle for about 3 hours, followed by gemcitabine (1250 mg / m ² ) on the 1st and 8th days for 30 minutes. Depending on the patient's tolerance to gemcitabine, dose reduction may be considered in each treatment cycle or within a treatment cycle. Before receiving gemcitabine + paclitaxel combined chemotherapy, the patient's absolute granulocyte count should be at least 1,500 (× 10 ⁶ / L).
Toxicity monitoring and dose adjustment based on toxicity < br Dose adjustment due to non-hematological toxicity < br Patients who use gemcitabine should undergo regular routine clinical examinations of liver and kidney function to detect non-hematological toxicity. Depending on the patient's tolerance to gemcitabine, dose reduction may be considered in each treatment cycle or within a treatment cycle. In general, for severe (grade 3 or 4) non-hematological toxicity other than nausea / vomiting, gemcitabine treatment should be discontinued or reduced by a doctor's judgment. Based on the opinion of the clinician, consider stopping treatment until the toxic response disappears.
For dose adjustment of cisplatin, carboplatin, and paclitaxel when combined, please refer to the relevant product manual.
Dose adjustments due to hematological toxicity <br Beginning of the treatment cycle<br /> For all indications, patients must undergo platelet and granulocyte count examinations each time gemcitabine is used. Before the beginning of each treatment cycle, the patient's absolute granulocyte count should be not less than 1,500 (× 10 ⁶ / L), and the platelet count must reach 100,000 (× 10 ⁶ / L).
During the treatment cycle < br Dose adjustment of gemcitabine during the treatment cycle should be performed according to the following table:

For all indications, the dose adjustment for the next treatment cycle according to hematological toxicity <br /> When the following hematological toxicity occurs, the dose of gemcitabine should be reduced to 75% of the dose used in the initial treatment cycle.
· Absolute granulocyte count <500 × 10 ⁶ / L for more than 5 days · Absolute granulocyte count <100 × 10 ⁶ / L for more than 3 days · Fever neutropenia · Platelets <25,000 × 10 ⁶ / L
Delayed treatment cycle due to toxicity for more than one week.
Gemcitabine is well tolerated during infusion and is easy to administer. If extravasation occurs, the infusion should be stopped immediately, and the blood vessel should be replaced to restart the infusion. Patients should be closely observed after administration. If a non-intravenous route of administration occurs, it must be stopped immediately.
Special precautions for preparation, handling, and other handling When preparing and handling infusions, you must read the general handling safety precautions for cytostatics. Handle infusions in a safety box, wear protective clothing and protective gloves. If you do not have a safety box, you should also wear a protective face shield and protective glasses.
If the prepared solution comes in contact with the glasses, it may cause severe irritation, and the glasses should be thoroughly rinsed with water immediately. If irritation persists, consult a doctor. If solution spills on skin, rinse thoroughly with water.
Re-dissolution (and further dilution, if applicable) Operating Instructions Sodium Chloride Injection (without preservatives) at a concentration of 9 mg / ml (0.9%) is the only solution allowed to redissolve sterile gemcitabine powder. According to the solubility of the drug, the concentration of gemcitabine should not exceed 40 mg / ml after re-dissolution. If the reconstitution solution concentration is greater than 40mg / ml, it may cause incomplete dissolution of the drug and should be avoided.
1. Redissolve and further dilute the intravenous infusion with gemcitabine should be handled aseptically.
2. When re-dissolving, add 5ml of sterile preservative-free sodium chloride injection at a concentration of 9mg / ml (0.9%) to a 200mg vial or 25ml of 9mg / ml (0.9%) without Preservative-free sodium chloride injection was added to a 1000 mg vial. The total volume of the solution after re-dissolution is 5.26ml (200mg specification) or 26.3ml (1000mg specification). The concentration of gemcitabine obtained after dissolution was 38 mg / ml, and the drainage volume of the lyophilized powder was included in the calculation. Shake until dissolved. It can be further diluted with 9 mg / ml (0.9%) sterile preservative-free sodium chloride injection. Redissolution is a clear, colorless to pale yellow liquid.
3. Injectable drug solution should be checked for insoluble particulate matter and discoloration before use. Do not use if particulate matter is found.
Any used product or waste should be disposed of in accordance with local requirements.
Special populations <br Patients with kidney or liver damage < br For patients with liver or renal insufficiency, gemcitabine should be used with caution, because the clinical research data on patients here are not sufficient, and clear recommendations cannot be drawn based on this Dose (see [Precautions] and [Pharmacokinetics]).

Adverse reactions of gemcitabine hydrochloride for injection

Clinical research data blood and lymphatic system:
Because gemcitabine is a bone marrow inhibitor, anemia, leukocytopenia, and thrombocytopenia are all likely to occur after treatment with gemcitabine. Fever neutropenia is also frequently reported.
Gastrointestinal system:
Hepatic dysfunction is very common, but often only mild and non-progressive, and treatment termination due to abnormal liver function is rare.
Nausea and nausea with vomiting are very common, medication doses are rarely required to be reduced, and they are easily controlled with anti-vomiting drugs.
Diarrhea and stomatitis are also frequently reported.
Reproductive-urinary system:
Mild proteinuria and hematuria are very common.
Skin and accessory organs:
Rash is very common and is often associated with itching. The rash is usually mild. Hair loss (usually mild hair loss) is also often reported.
Respiratory system:
Dyspnea is often reported. There are few reports of bronchospasm after intravenous infusion of gemcitabine. This drug should not be given again if the patient is known to be highly allergic to gemcitabine.
There are currently few reports of interstitial pneumonia.
whole body:
Flu-like symptoms are very common. Fever, headache, chills, myalgia, fatigue and anorexia are the most common symptoms. Cough, rhinitis, malaise and sweating are also frequently reported. Fever and fatigue are also often separate symptoms.
Hypersensitivity: Reports of severe allergic reactions are very rare.
Radiotoxicity has been reported (see [Drug Interactions]).
Adverse reactions to drowsiness are also commonly reported.
Cardiovascular System:
Reports of edema / peripheral edema are very common. A few cases have reported hypotension. Some studies have reported myocardial infarction.
Post-marketing information respiratory system:
Pulmonary symptoms or severe pulmonary symptoms (such as pulmonary edema, interstitial pneumonia, or adult respiratory distress syndrome (ARDS)) associated with gemcitabine treatment are rarely reported. The cause of these pulmonary symptoms is unknown. Once this occurs, consideration should be given to discontinuing gemcitabine. Early use of supportive care may help alleviate the condition.
Reproductive-urinary system:
In patients receiving gemcitabine, clinical manifestations similar to hemolytic uremic syndrome (HUS) rarely occur. If there is a manifestation of microvascular hemolytic anemia, such as rapid decline in hemoglobin with thrombocytopenia, elevated serum bilirubin, creatinine, urea nitrogen or lactate dehydrogenase levels, the drug should be discontinued immediately. Even if the drug is discontinued, the patient's kidney damage may be irreversible, so dialysis treatment should be given.
Cardiovascular System:
Reports of heart failure are very rare. Arrhythmias have been reported, especially supraventricular arrhythmias.
Blood vessels:
Reports of clinical manifestations associated with peripheral vasculitis and gangrene are rare.
Skin and accessory organs:
Reports of severe skin reactions, including exfoliative dermatitis and bullous rash, are rare.
After continuous radiation therapy and gemcitabine treatment, severe skin and dermatomyositis-type muscle disorders have been reported in areas previously treated with radiation.
Hepatobiliary system:
Increased liver function indicators, including increased levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), -glutamyl transpeptidase (GGT), alkaline phosphatase, and bilirubin High reports are rare.
Injuries, poisoning and complications during the course of the disease:
There have been reports of radiological memory reactions.

Gemcitabine hydrochloride for contraindications

-Patients who are highly allergic to gemcitabine or any excipient-Gemcitabine is used in combination with radiation therapy (due to radiation sensitization and the risk of severe pulmonary and esophageal fibrosis).
-Combination of gemcitabine and cisplatin in patients with severe renal insufficiency.

Precautions for gemcitabine hydrochloride for injection

Prolonged infusion time and increased dosing frequency may increase toxicity.
[u] Hematological toxicity [/ u]
Gemcitabine may cause bone marrow function inhibition, and leukopenia, thrombocytopenia, and anemia may occur after application.
Patients must monitor platelet, leukocyte, and granulocyte counts before each treatment with gemcitabine. When it is confirmed that the drug has caused bone marrow suppression, chemotherapy should be suspended or the treatment plan should be modified (see [Dosage and Administration]). However, the duration of bone marrow suppression is short, doses are usually not reduced, and treatment discontinuation is rare.
After stopping gemcitabine, peripheral blood cell counts may continue to decline. Patients with impaired bone marrow function should be treated with caution. When combined with other antitumor drugs for combined or sequential chemotherapy, accumulation of bone marrow suppressive effects should be considered.
[u] Hepatic insufficiency [/ u]
The use of gemcitabine in patients with liver metastases or patients with a previous history of hepatitis, alcoholism, or cirrhosis may lead to worsening of underlying liver dysfunction.
Laboratory evaluations of renal and liver function, including virological tests, should be performed on a regular basis.
Because sufficient information on clear dose recommendations for these patient groups has not been obtained from clinical studies, gemcitabine should be used with caution in patients with liver insufficiency or renal impairment, as clinical research data on such patients are not sufficient, No clear recommended dose has yet been derived from this. (See [Usage and dosage]).
[u] Synchronous chemoradiotherapy [/ u]
Simultaneous chemoradiotherapy (radiochemotherapy applied together or interval between different treatments 7 days); toxic reactions have been reported (see [Drug Interactions] for detailed information and recommended doses).
Gemcitabine administered at 1000 mg / m ² concurrently with radiation therapy can cause severe lung or esophageal lesions.
If gemcitabine is given continuously with radiation therapy, gemcitabine should be separated from radiation therapy by at least 4 weeks due to the possibility of severe radiation sensitization. Shorten the interval if patient circumstances permit.
[u] Live vaccine [/ u]
Yellow fever vaccine and other live attenuated vaccines are not recommended for patients receiving gemcitabine (see [Drug Interactions]).
[u] Cardiovascular system [/ u]
Because gemcitabine can cause heart and / or cardiovascular conditions, patients with a history of cardiovascular disease should be especially careful when using gemcitabine.
[u] lung [/ u]
Pulmonary symptoms related to gemcitabine treatment, sometimes severe pulmonary symptoms such as pulmonary edema, interstitial pneumonia, or adult respiratory distress syndrome (ARDS) have been reported. The cause of these symptoms is unknown. Once this occurs, consideration should be given to discontinuing gemcitabine. Early use of supportive care may help alleviate the condition.
[u] kidney [/ u]
Clinical manifestations similar to hemolytic uremic syndrome (HUS) are rare in patients taking gemcitabine (see [Adverse Reactions]). If there is a manifestation of hemolytic anemia of microangiopathies, such as a rapid decrease in hemoglobin with thrombocytopenia, an increase in serum bilirubin, creatinine, urea nitrogen, and lactate dehydrogenase, the drug should be stopped immediately. After stopping the drug, the patient's renal function damage may be irreversible, and dialysis treatment should be given.
[u] Fertility [/ u]
In fertility studies, gemcitabine was found to cause too little sperm production in male mice (see Preclinical Safety Data). Therefore, men receiving gemcitabine treatment should be advised not to have children during treatment and 6 months after treatment, and because gemcitabine may cause infertility, men should be told to save sperm before treatment.
[u] Sodium [/ u]
Gemcitabine in a 200 mg / bottle format contains 3.5 mg (<1 mmol) of sodium, and patients should consider controlling sodium intake.
1000 mg / bottle of gemcitabine contains 17.5 mg of sodium (<1 mmol), and patients should consider controlling sodium intake.
[u] Effects on driving and manipulating machinery [/ u]
Studies on the effects of gemcitabine on driving and handling machinery have not been conducted. However, it has been reported that gemcitabine can cause mild to moderate drowsiness, especially when drinking alcoholic beverages during medication. The patient must therefore be prohibited from driving and operating the machine during this period until the identification is no longer exhausted.
[u] Incompatibility [/ u]
Except for the drugs specified in [Special Precautions for Preparation and Disposal Operations], this product must not be mixed with other drugs.

Gemcitabine hydrochloride for injections for pregnant and lactating women

[u] pregnancy [/ u]
There are not enough data to establish the safety of gemcitabine in pregnant women. Animal experiments have shown reproductive toxicity (see Preclinical Safety Data). Based on the results of animal experiments and the mechanism of gemcitabine action, pregnant women should avoid the use of gemcitabine unless there is a clear need for it. Women should be advised to avoid pregnancy during gemcitabine treatment, and their pregnant doctor should be notified immediately if they become pregnant.
[u] lactation [/ u]
It is unclear whether gemcitabine can be secreted from milk and its adverse effects on lactating young children cannot be ruled out. Breastfeeding must be stopped while receiving gemcitabine.
[u] Fertility [/ u]
In fertility studies, gemcitabine was found to cause too little sperm production in male mice (see Preclinical Safety Data). Therefore, men receiving gemcitabine should be advised not to give birth during treatment and 6 months after treatment, and because gemcitabine may cause infertility, men should be advised to save sperm before treatment.

Gemcitabine hydrochloride for children

Due to insufficient data to support the effectiveness and safety of children's medication, gemcitabine is not recommended for children under 18 years of age.

Gemcitabine Hydrochloride for Injection

Patients over 65 years of age are well tolerated by gemcitabine, and with the exception of the recommended dose adjustments for all patients, there is no evidence that a special dose adjustment is necessary for elderly patients.

Gemcitabine hydrochloride for drug interactions

No special interaction studies were performed. (See [Pharmacokinetics])
Radiotherapy concurrent chemoradiotherapy (simultaneous chemoradiotherapy or interval between different treatments 7 days)-The toxicity associated with this multidisciplinary comprehensive treatment depends on many different factors, including the dose of gemcitabine, the frequency of gemcitabine administration, The dose of radiotherapy, the technology used in radiotherapy, the target tissue and target volume, etc. Preclinical and clinical studies have shown that gemcitabine has a radiosensitizing effect. In a single study, patients with non-small cell lung cancer received both gemcitabine and chest therapeutic radiation at a dose of 1,000 mg / m ² for 6 consecutive weeks. Patients with severe, potentially fatal mucositis were observed. It is esophagitis and pneumonia, especially for patients who are receiving high-dose radiation therapy [mdeian treatment volumes 4,795 cm ³ . Studies since then have shown that given the predictable toxicity, it is feasible to administer radiation therapy with relatively low doses of gemcitabine. For example, in a phase II clinical study of non-small cell carcinoma, 66 Gy of chest radiotherapy, gemcitabine (600 mg / m ² , 4 times), and cisplatin (80 mg / m ² , 2 were given concurrently over a 6-week period. Times) combined treatment. At present, the best safe treatment plan for concurrent use of gemcitabine and radiotherapy has not been determined in all tumor types.
Non-synchronized chemoradiotherapy (interval> 7 days)-Data analysis shows that applying gemcitabine for more than 7 days before and after radiotherapy will not increase toxicity, but may have a radio memory response. Research data show that gemcitabine treatment should not be performed until the response to the radiation therapy has improved or at least 1 week after the end of radiotherapy.
There have been reports of radiation damage to target tissues (such as esophagitis, colitis, and pneumonia), which are related to gemcitabine applied to patients at the same time or at different times during radiotherapy.
Because of the risk of causing systemic and potentially fatal diseases, yellow fever vaccines and other live-attenuated vaccines are not recommended, especially for immunosuppressed patients.

Gemcitabine hydrochloride for injection overdose

There are no known antidotes against gemcitabine overdose. In the Phase I study, several patients received a single intravenous injection of 5700 mg / m ^{2 of} gemcitabine every 2 weeks for more than 30 minutes. The main toxicity observed included bone marrow suppression, paresthesia, and severe rash. Once the clinical situation is suspected of overdose, hematological indicators should be properly monitored, and supportive treatment should be provided to patients if necessary.

Pharmacology and Toxicology of Gemcitabine Hydrochloride for Injection

[u] Pharmacological action [/ u]
Mechanism:
Cell metabolism and mechanism of action: Gemcitabine (dFdC) is a pyrimidine antimetabolite, which is metabolized into dFdCDP and dFdCTP by nucleoside kinases in cells. dFdCDP and dFdCTP inhibit DNA synthesis through two mechanisms of action, thereby achieving the cytotoxic effect of gemcitabine. First, dFdCDP inhibits the activity of nucleotide reductase, resulting in the inhibition of the production of deoxynucleoside triphosphate (dCTP) necessary for the synthesis of DNA. Second, dFdCTP competes with dCTP for incorporation into the DNA strand (self-enhancing effect). Similarly, a small amount of gemcitabine can also be incorporated into RNA molecules. Therefore, the decrease of intracellular dCTP concentration is more favorable for the incorporation of dFdCTP into the DNA strand. DNA polymerase cannot remove the incorporated gemcitabine and repair the formed DNA strand. When gemcitabine was incorporated into the DNA strand, a nucleotide was added to the extended DNA strand. This added nucleotide can completely inhibit further synthesis of the DNA strand (hidden strand termination). Gemcitabine caused apoptosis in the DNA strand.
Cytotoxic activity on cultured cells:
Gemcitabine has obvious cytotoxic activity on various cultured human and mouse tumor cells. Its effect is cell cycle specific, that is, gemcitabine mainly acts on the cells of DNA synthesis (S-phase), and under certain conditions, it can prevent the progress of cells at the G1 / S phase junction. In vitro, the cytotoxic effect of gemcitabine depends on concentration and time.
Study of antitumor activity in animal models:
In the study of tumor animal models, the antitumor activity of gemcitabine was found to be related to the mode of administration. The daily administration method results in high animal mortality and low antitumor activity. When administered every 3-4 days, gemcitabine has good antitumor activity against a variety of tumors in mice at non-lethal doses.
[u] Toxic effect [/ u]
In a 6-month repeated dose study of rats and dogs, a reversible dose-dependent inhibition of hematopoietic function was found.
Genotoxicity < br Gemcitabine can cause mutations in in vitro mutation experiments and in vivo bone marrow micronucleus tests. Long-term animal studies evaluating the carcinogenic potential have not been performed.
In fertility studies, gemcitabine was found to cause reversible spermatogenesis in male mice. No effect on the fertility of females has been found.
Animal tests show that gemcitabine has reproductive toxicity, such as causing physiological defects in newborn animals or other effects on embryo or fetal development, pregnancy or perinatal and postpartum periods.
Animal tests show that gemcitabine has reproductive toxicity, such as causing physiological defects in newborn animals or other effects on embryo or fetal development, pregnancy or perinatal and postpartum periods.

Pharmacokinetics of gemcitabine hydrochloride for injection

Pharmacokinetic characteristics < br The pharmacokinetic characteristics of gemcitabine were evaluated in 7 studies with a total of 353 patients. There were 121 female patients and 232 male patients, aged 29-79. Of these patients, approximately 45% are patients with non-small cell lung cancer and 35% are patients with pancreatic cancer. The following pharmacokinetic parameters were obtained: the dosage range was 500-2,592 mg / m ² , and the infusion time range was 0.4-1.2 hours.
The peak plasma concentration (obtained within 5 minutes after the end of the infusion) was 3.2-45.5 g / ml. According to the dose of 1000 mg / m ² / 30min, the plasma concentration of the parent compound can be continuously higher than 5 g / ml within 30 minutes of the end of the infusion, and its plasma concentration is also higher than 0.4 g / ml within 1 hour after the end of the infusion.
Distribution < br The volume of distribution in the central compartment is 12.4 L / m ² for women and 17.5 L / m ^{2 for} men (individual difference is 91.9%). The distributed volume of the peripheral compartment is 47.4 L / m ² . The volume of peripheral compartments is not related to gender.
Plasma protein binding is negligible.
Half-life: The half-life is 42-94 minutes and is related to age and gender. For the recommended dosing regimen, gemcitabine is completely cleared within 5-11 hours after the start of the infusion. When given once a week, gemcitabine does not accumulate.
Metabolism < br Gemcitabine is rapidly metabolized by cytidine deaminase in liver, kidney, blood and other tissues. In the cell, gemcitabine is metabolized in the cell to produce gemcitabine monophosphate, diphosphate, and nucleoside triphosphate (dFdCMP, dFdCDP, and dFdCTP), of which dFdCDP and dFdCTP are active. Metabolites formed in these cells have not been detected in plasma or urine.
The main metabolite 2'-deoxy-2 ', 2'-difluorouridine (dFdU) is inactive and can be detected in both plasma and urine.
Excretion < br The systemic clearance rate is 29.2L / hr / m ² -92.2L / hr / m ² , which is related to gender and age (individual difference is 52.2%). Clearance is about 25% lower for women than for men. Although the clearance rate is fast, both the male and female clearance rates decrease with age. The recommended dose of gemcitabine is 1000 mg / m ² for intravenous infusion for 30 minutes. It is not necessary to reduce the dose of gemcitabine due to the reduced clearance of men and women.
Urinary excretion: less than 10% is excreted in the form of the original drug.
Renal clearance: 2-7L / hr / m ² .
Within one week after administration, 92% -98% of the dose of gemcitabine administered was detected, of which 99% was excreted mainly in the form of dFdU through urine and 1% was excreted in feces.
Kinetics of dFdCTP <br /> This metabolite is found in peripheral blood mononuclear cells. The following information refers to the situation in such cells. When administered at 35-350mg / m ² / 30min, the increase in the concentration of dFdCTP in the cell is proportional to the increase in dose. The steady state concentration of the drug is 0.4-5 g / ml. When the plasma concentration of gemcitabine exceeded 5 g / ml, the dFdCTP concentration no longer increased, indicating that it was saturated in the cells.
Terminal elimination half-life: 0.7-12 hours.
Kinetic characteristics of dFdU <br /> Peak plasma concentration (1000 mg / m ² , intravenous drip for 30 minutes, 3-15 minutes after the end): 28-52 g / ml.
The trough concentration after administration every Monday: 0.07-1.12 g / ml, no obvious accumulation.
The average half-life of the terminal phase of the three-phase drug curve is -65 hours (range 33-84 hours).
The proportion of dFdU formed from the parent drug: 91% -98%.
Central chamber average distribution volume: 18L / m ² (range 11-22L / m ² ).
Organizational distribution: Extensive.
Average apparent clearance: 2.5L / hr / m ² (range 1-4L / hr / m ² ).
Urinary excretion: all.
Gemcitabine combined with paclitaxel combined treatment <br /> Combined treatment of gemcitabine and paclitaxel did not change the pharmacokinetic characteristics of gemcitabine or paclitaxel.
Renal function impairment < br Mild to moderate renal insufficiency (GFR from 30ml / min-80ml / min) does not have a consistent significant effect on the pharmacokinetic characteristics of gemcitabine.

Gemcitabine Hydrochloride for Injection Storage

Keep tightly closed in a dry place.

Gemcitabine hydrochloride for injection

(1) 0.2g: bottle of glass control injection, 8 bottles / box.
(2) 1.0g: bottle of glass control injection, 3 bottles / box.

Gemcitabine Hydrochloride for Injection

36 months

Gemcitabine hydrochloride for injection

YBH00982011 ^[1]