Fluorouracil Sodium Chloride Injection
Function and Efficacy
Pharmacological action Fluorouracil is converted into 5-fluorouracil deoxynucleoside by enzymes in the body, and forms a covalent bond with the active center of thymidine synthetase, which inhibits the activity of the enzyme, reduces the production of thymidine nucleoside, and leads to the obstruction of DNA biosynthesis; in addition, it can also be converted into fluorouracil triphosphate and incorporated into RNA in the form of pseudo-metabolites, thereby interfering with the normal physiological function of RNA and affecting protein biosynthesis. In recent years, studies have found that the active metabolites of this product, 5-fluorouracil deoxynucleoside and methylenetetrahydrofolate, can form a triple complex with thymidine synthetase, preventing the activity of thymidine synthetase, thereby inhibiting DNA synthesis. Fluorouracil has a significant killing effect on proliferating cells, especially on S phase cells, but it can also delay the migration of G1 phase cells to S phase, thus resulting in a self-limiting phenomenon. Toxicological studies Genetic toxicity: Fluorouracil can induce cancerous changes in mouse embryonic fibroblasts in vitro, but the relationship between carcinogenicity and mutagenicity is not clear. Although fluorouracil has no mutagenic effect on TA92, TA98 and TA100 Salmonella typhimurium, it has mutagenic effects on TA1535, TA1537, TA1538 Salmonella typhimurium and Saccharomyces cerevisiae. In addition, the results of the fluorouracil mouse bone marrow micronucleus test were positive. In vitro experiments, high concentrations of fluorouracil can cause chromosome breaks in hamster fibroblasts. Reproductive toxicity: Intraperitoneal injection of 125 or 250 mg/kg of fluorouracil in rats can cause chromosomal aberrations and changes in the chromosome structure of spermatogonia, and can also inhibit the differentiation of spermatogonia, leading to infertility. Female rats were intraperitoneally injected with 25 or 50 mg/kg of fluorouracil every week for 3 consecutive weeks before ovulation, which can significantly reduce the occurrence of mating, delay the development of embryos before and after implantation, increase pre-implantation mortality, and cause embryonic chromosomal abnormalities. Animal experiments show that fluorouracil is teratogenic. Mice showed the most obvious teratogenic effect when given a single intraperitoneal injection of 10-40 mg/kg of fluorouracil on the 10th or 12th day of pregnancy. Rats were given intramuscular injections of 12-37 mg/kg of fluorouracil on days 9-12 of pregnancy and 3-9 mg of fluorouracil on days 8-11 of pregnancy, and teratogenic effects were observed, including cleft palate, skeletal abnormalities, and deformities of appendages, claws, and tails. The above doses for teratogenic effects are 1-3 times the maximum recommended clinical therapeutic dose. Monkeys were given a total of 40 mg/kg of fluorouracil on days 20-24 of pregnancy without teratogenic effects. Although there is no direct evidence of human malformations caused by fluorouracil, it should be noted that other DNA synthesis inhibitors have been reported to cause human malformations. Therefore, women of childbearing potential should avoid pregnancy. If patients use fluorouracil during pregnancy or become pregnant during medication, they should be informed of the potential harm of fluorouracil to the fetus. Fluorouracil can only be used during pregnancy if its potential benefits outweigh its potential harm to the fetus. There is no data on the perinatal toxicity of fluorouracil, but fluorouracil can enter the blood circulation of rat fetuses through the placenta, leading to absorption and death of the embryo. When pregnant monkeys were given fluorouracil at a dose of more than 40 mg/kg, all embryos exposed to the drug had miscarriages. It is not clear whether fluorouracil is excreted in human milk. Given that fluorouracil can inhibit the synthesis of DNA, RNA and protein, mothers should stop breastfeeding when using fluorouracil. Carcinogenicity: There is no experimental data on long-term administration of fluorouracil to fully evaluate the carcinogenicity of fluorouracil. Rats were given 0.3, 1, and 3 mg/rat orally for 5 days a week for 52 consecutive weeks, and then observed for 6 months, and no carcinogenic effect was observed. Male rats were intravenously injected with 33 mg/kg of fluorouracil once a week for 52 consecutive weeks, and their life course was subsequently observed, and no carcinogenic effect was observed. Female mice were intravenously injected with 1 mg of fluorouracil once a week for 16 weeks, which had no effect on the incidence of lung adenocarcinoma. However, based on the existing data, it is not possible to evaluate the carcinogenicity of fluorouracil in humans.
Ingredients
The main ingredients of this product are fluorouracil and sodium chloride. The chemical name of fluorouracil: 5-fluoro-2,4 (1H, 3H)-pyrimidinedione. Chemical structure: Molecular formula: C4H3FN2O2 Molecular weight: 130.08
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| 5-FluorouracilIngredients |
It is converted into 5-fluorouracil deoxynucleoside by enzymes in the body, forming a covalent bond with the active center of thymidine synthetase, inhibiting the activity of the enzyme and hindering the biosynthesis of DNA; it can also be converted into fluorouracil triphosphate and incorporated into RNA in the form of pseudometabolites, interfering with the normal physiological function of RNA and affecting the biosynthesis of proteins. The active metabolites 5-fluorouracil deoxynucleoside and methylenetetrahydrofolate can form a triple complex with thymidine synthetase, preventing the activity of thymidine synthetase and thus inhibiting DNA synthesis. It has a significant killing effect on proliferating cells, especially on S phase cells, and can also delay the migration of G1 phase cells to S phase. More |
51-21-8 | 21 | |
| Sodium chlorideExcipients |
Pharmacological action Fluorouracil is converted into 5-fluorouracil deoxynucleoside by enzymes in the body, and forms a covalent bond with the active center of thymidine synthetase, which inhibits the activity of the enzyme, reduces the production of thymidine nucleoside, and leads to the obstruction of DNA biosynthesis; in addition, it can also be converted into fluorouracil triphosphate and incorporated into RNA in the form of pseudo-metabolites, thereby interfering with the normal physiological function of RNA and affecting protein biosynthesis. In recent years, studies have found that the active metabolites of this product, 5-fluorouracil deoxynucleoside and methylenetetrahydrofolate, can form a triple complex with thymidine synthetase, preventing the activity of thymidine synthetase, thereby inhibiting DNA synthesis. Fluorouracil has a significant killing effect on proliferating cells, especially on S phase cells, but it can also delay the migration of G1 phase cells to S phase, thus resulting in a self-limiting phenomenon. Toxicological studies Genetic toxicity: Fluorouracil can induce cancerous changes in mouse embryonic fibroblasts in vitro, but the relationship between carcinogenicity and mutagenicity is not clear. Although fluorouracil has no mutagenic effect on TA92, TA98 and TA100 Salmonella typhimurium, it has mutagenic effects on TA1535, TA1537, TA1538 Salmonella typhimurium and Saccharomyces cerevisiae. In addition, the results of the fluorouracil mouse bone marrow micronucleus test were positive. In vitro experiments, high concentrations of fluorouracil can cause chromosome breaks in hamster fibroblasts. Reproductive toxicity: Intraperitoneal injection of 125 or 250 mg/kg of fluorouracil in rats can cause chromosomal aberrations and changes in the chromosome structure of spermatogonia, and can also inhibit the differentiation of spermatogonia, leading to infertility. Female rats were intraperitoneally injected with 25 or 50 mg/kg of fluorouracil every week for 3 consecutive weeks before ovulation, which can significantly reduce the occurrence of mating, delay the development of embryos before and after implantation, increase pre-implantation mortality, and cause embryonic chromosomal abnormalities. Animal experiments show that fluorouracil is teratogenic. Mice showed the most obvious teratogenic effect when given a single intraperitoneal injection of 10-40 mg/kg of fluorouracil on the 10th or 12th day of pregnancy. Rats were given intramuscular injections of 12-37 mg/kg of fluorouracil on days 9-12 of pregnancy and 3-9 mg of fluorouracil on days 8-11 of pregnancy, and teratogenic effects were observed, including cleft palate, skeletal abnormalities, and deformities of appendages, claws, and tails. The above doses for teratogenic effects are 1-3 times the maximum recommended clinical therapeutic dose. Monkeys were given a total of 40 mg/kg of fluorouracil on days 20-24 of pregnancy without teratogenic effects. Although there is no direct evidence of human malformations caused by fluorouracil, it should be noted that other DNA synthesis inhibitors have been reported to cause human malformations. Therefore, women of childbearing potential should avoid pregnancy. If patients use fluorouracil during pregnancy or become pregnant during medication, they should be informed of the potential harm of fluorouracil to the fetus. Fluorouracil can only be used during pregnancy if its potential benefits outweigh its potential harm to the fetus. There is no data on the perinatal toxicity of fluorouracil, but fluorouracil can enter the blood circulation of rat fetuses through the placenta, leading to absorption and death of the embryo. When pregnant monkeys were given fluorouracil at a dose of more than 40 mg/kg, all embryos exposed to the drug had miscarriages. It is not clear whether fluorouracil is excreted in human milk. Given that fluorouracil can inhibit the synthesis of DNA, RNA and protein, mothers should stop breastfeeding when using fluorouracil. Carcinogenicity: There is no experimental data on long-term administration of fluorouracil to fully evaluate the carcinogenicity of fluorouracil. Rats were given 0.3, 1, and 3 mg/rat orally for 5 days a week for 52 consecutive weeks, and then observed for 6 months, and no carcinogenic effect was observed. Male rats were intravenously injected with 33 mg/kg of fluorouracil once a week for 52 consecutive weeks, and their life course was subsequently observed, and no carcinogenic effect was observed. Female mice were intravenously injected with 1 mg of fluorouracil once a week for 16 weeks, which had no effect on the incidence of lung adenocarcinoma. However, based on the existing data, it is not possible to evaluate the carcinogenicity of fluorouracil in humans. More |
7647-14-5 | 43 |
Appearance
This product is a colorless or almost colorless clear liquid.
Indication
1. Used as adjuvant chemotherapy and palliative treatment for breast cancer, digestive tract cancer (including primary and metastatic liver cancer, biliary system cancer and pancreatic cancer), ovarian cancer and primary bronchopulmonary adenocarcinoma. 2. Main chemotherapy drug for the treatment of malignant hydatidiform mole and choriocarcinoma. 3. Head and neck malignancies and liver cancer.
Usage and Dosage
Intravenous drip, the usual dose for adults is 0.5-1.0g of fluorouracil per day, used for 5 consecutive days every 3-4 weeks; it can also be used once a week, 0.5-0.75g of fluorouracil each time, used for 2-4 weeks and then rested for 2 weeks as a course of treatment. Please follow the doctor's advice on the drip rate. Combination chemotherapy, commonly used are: ① Mitomycin, fluorouracil and vincristine (MF0), used for gastrointestinal adenocarcinoma; ② Cyclophosphamide, methotrexate and fluorouracil (CMF), used for breast cancer; ③ Fluorouracil, doxorubicin, mitomycin (FAM) or fluorouracil, doxorubicin and nitrosoureas (CCNU or methyl CCNU) for gastric cancer or biliary system and pancreatic cancer. The specific combination chemotherapy regimen should be formulated and recommended by the clinician, please follow the doctor's advice.
Adverse Reactions
(1) Nausea, loss of appetite or vomiting. Most of the symptoms are not serious at normal doses. Occasionally, oral mucosal inflammation or ulcers, abdominal discomfort or diarrhea may occur. Peripheral leukopenia is common (mostly reaching the lowest point 2 to 3 weeks after the start of the treatment and returning to normal within about 3 to 4 weeks). Thrombocytopenia is rare. Coughing, shortness of breath or cerebellar ataxia are extremely rare. Hair loss or pigmentation of the injected vein is quite common. (2) Drug overflow at the intravenous drip site may cause local pain, necrosis or cellulitis. (3) Long-term use may lead to nervous system toxicity. (4) Occasionally, myocardial ischemia may occur after medication, and angina pectoris and electrocardiogram changes may occur.
Precautions
(1) Pregnant and lactating women are prohibited from using this product. (2) This product is prohibited when accompanied by chickenpox or herpes zoster. (3) This product is prohibited for patients with severe malnutrition, low bone marrow hematopoietic function, severe infection or allergy to fluorouracil.
Special Population Medication
Precautions for children: intravenous drip, 10-12 mg/kg per body weight, once a day or every other day. Or follow the doctor's advice. Precautions for pregnancy and lactation: (1) There have been very few cases of congenital malformations caused by the use of this product during the first three months of pregnancy, and it may have long-term effects on the fetus. Therefore, it should be prohibited for women during pregnancy. (2) Due to the potential mutagenicity, teratogenicity and carcinogenicity of this product and the possible toxic and side effects in infants, breastfeeding is not allowed during the use of this product. Precautions for the elderly: The dose should be reduced for the elderly.
Drug Interactions
(1) When used in combination with methotrexate, the latter should be given first, and fluorouracil should be given 4 to 6 hours later, otherwise the effect will be reduced. (2) When using this product, it is not advisable to drink alcohol or use aspirin at the same time to reduce the possibility of gastrointestinal bleeding.
Storage
Keep away from light and store in a sealed container.
Packaging Specification
250ml: 0.5g fluorouracil and 2.25g sodium chloride
Validity Period
18 months
Manufacturer
Harbin Medisan Pharmaceutical Co., Ltd.
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Founded in:
1996-06-21 -
Address:
Beijing Road, Limin Development Zone, Harbin -
Tax NO.:
91230100607168790X -
Registered Funds:
316.35755 million yuan -
Website:
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Email: