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Molecular Formula: C20H21CaN7O7.xH2O
Молекулярный вес: 511.5
Номер CAS: 1492-18-8
Имена и идентификаторы
| Имя | Кальций фолинатк |
| Синонимы | фолинат кальция Кальций фолинатк LeucovorinCalcium L-Calcium Folinate Кальций лейковорин Calcium L-Folinate Лейковорин Кальций Гидрат фолината кальция Folinic acid calcium salt Folinic acid Calcium salt Folinic acid calcium salt USP28 calcium5-formyltetrahydrofolate FOLINIC ACID, CALCIUM SALT UPS28 CALCIUM FOLINATE(FOLINIC ACID)(RG) Calcium folinate, Leucovorine calcium calcium2-[4-[(2-amino-5-formyl-4-oxo-1,6,7,8-tetrahydropteridin-6-yl)methylamino]benzoyl] aminopentanedioate calcium (2S)-2-[(4-{[(2-amino-5-formyl-4-oxo-1,4,5,6,7,8-hexahydropteridin-6-yl)methyl]amino}benzoyl)amino]pentanedioate calcium (2S)-2-({[4-({[(6S)-2-amino-5-formyl-4-oxo-1,4,5,6,7,8-hexahydropteridin-6-yl]methyl}amino)phenyl]carbonyl}amino)pentanedioate 5-Formyl-5,6,7,8-tetrahydrofolic acid calcium salt, 5-HCO-H4PteGlu, Calcium folinate, Citrovorum factor calcium salt, Leucovorin calcium salt, 5-Formyl-5,6,7,8-tetrahydropteroyl-L-glutamic acid calcium salt |
| CAS | 1492-18-8 |
| EINECS | 216-082-8 |
| InChI | InChI=1/C20H23N7O7.Ca/c21-20-25-16-15(18(32)26-20)27(9-28)12(8-23-16)7-22-11-3-1-10(2-4-11)17(31)24-13(19(33)34)5-6-14(29)30;/h1-4,9,12-13,22H,5-8H2,(H,24,31)(H,29,30)(H,33,34)(H4,21,23,25,26,32);/q;+2/p-2/t12-,13-;/m0./s1 |
1492-18-8 – Физико-химические свойства
| Молекулярная формула | C20H25CaN7O7 |
| Молярная масса | 515.54 |
| Температура плавления | > 300 ° С |
| Растворимость | Sparingly soluble in water, practically insoluble in acetone and in ethanol (96 per cent). |
| Внешний вид | Желтый кристаллический порошок |
| Цвет | Pale Yellow to Light Yellow |
| BRN | 5723924 |
| Условия хранения | Хранить в темном месте, инертная атмосфера, комнатная температура. |
| Стабильность | гигроскопический |
| MDL | MFCD00006704 |
| Используйте | It is mainly used as an antidote for folic acid antagonists such as methotrexate, pyrimethamine or trimethoprim. 2. For the Prevention of methotrexate overdose or high-dose treatment caused by serious toxic effects. 3. Megaloblastic anemia caused by folic acid deficiency. 4. When combined with fluorouracil, it is used for the treatment of advanced colon cancer and rectal cancer. |
1492-18-8 – Риск и безопасность
| Символы опасности | Xn – Вредный |
| Коды рисков | R36/37/38 – Раздражает глаза, дыхательную систему и кожу. R42/43 – Может вызвать сенсибилизацию при вдыхании и контакте с кожей. |
| Описание безопасности | S26 – При попадании в глаза немедленно промыть большим количеством воды и обратиться к врачу. S36 – Носите подходящую защитную одежду. S36/37 – Надевайте подходящую защитную одежду и перчатки. S22 – Не вдыхайте пыль. S45 – В случае несчастного случая или плохого самочувствия немедленно обратитесь к врачу (по возможности покажите этикетку). |
| WGK Германия | 3 |
| RTECS | MA0600500 |
| F-КОДЫ МАРКИ FLUKA | 3-8-10-23 |
| Код ТН ВЭД | 29362900 |
Справочная информация
| введение | calcium folinate is an antidote for folic acid antagonistic drugs, also known as calcium folate, calcium folate, calcium aldehyde hydrofolate, ferrous acetic acid, calcium aluronate, calcium formyltetrahydrofolate, yellowish white to yellow crystal or amorphous powder at room temperature, odorless. Easily soluble in water, almost insoluble in ethanol or ether, easily soluble in sodium hydroxide solution. Calcium folinate is a reduced formylated derivative of folic acid. Its effect is similar to that of folic acid. It is an activated form of folic acid in the body. After entering the human body, it is converted into tetrahydrofolate by tetrahydrofolate reductase, which can effectively resist the toxic reaction caused by methotrexate. Calcium folinate has the toxic reaction of “rescuing” excessive folic acid antagonists in the body, which is beneficial to the synthesis of thymine nucleotides, DNA, RNA and even protein, and can stimulate the growth and maturation of white blood cells. This product can limit the damage degree of methotrexate to normal cells, through mutual competition, and can reverse the reaction of methotrexate to bone marrow and gastrointestinal mucosa, but has no effect on the existing neurotoxicity of methotrexate. Mainly used as an antidote for folic acid antagonists (such as methotrexate, methotrexate, phenytoin, phenobarbital, pyrimethamine or trimethoprim, etc.). When oral folic acid is not effective, it is used for stomatitis diarrhea, malnutrition, megaloblastic anemia caused by pregnancy or infancy, and leukopenia. However, it is not applicable to vitamin B12 deficiency anemia. In recent years, calcium folinate has been used as an adjuvant treatment for colon and rectal cancer. Combined with fluorouracil, it can prolong survival. |
| Фармакологические эффекты | Calcium folinate (CF) is a calcium salt of calcium formyl tetrahydrofolate derivative, which is an activated form of folic acid in the body. It is mainly used as an antidote for folic acid antagonistic drugs, such as aminopterin, methotrexate, pyrimethamine and trimethoprim, which can competitively inhibit dihydrofolate reductase and prevent folic acid from becoming tetrahydrofolic acid, leading to DNA synthesis disorders, and supplementing calcium formyltetrahydrofolate can detoxify. It can also treat megaloblastic anemia caused by folic acid deficiency, and promote the differentiation, maturation and release of bone marrow hematopoietic cells. In recent years, a large number of experiments and clinical studies at home and abroad have fully proved that calcium folinate can be used as an efficient biochemical regulator, which can significantly enhance the anti-tumor activity of fluorouracil (5-FU) drugs. Fluorouracil is a pyrimidine antagonist, which is the main drug for the treatment of gastrointestinal tumors, breast cancer, head and neck cancer and trophoblastic tumors. Calcium folinate is easy to be absorbed orally, and the serum folate reduction can reach the peak value at (1.72±0.80) hours; It is (0.71±0.09) hours when injected intramuscularly. The half-life of serum folate reduction after intramuscular injection is 3.5 hours. The drug effect was maintained for 3 to 6 hours. The metabolite is 5-methyltetrahydrofolate, which is excreted through the kidney 80% ~ 90%. |
| пользования | is used to treat megaloblastic anemia, 15mg orally every day; Or intramuscular injection of 1~5mg per day, and oral administration of 5mg/d after 10~15 days until blood picture is normal and symptoms disappear. If the deficiency of cobalamin cannot be ruled out, it should be combined with cobalamin adenosine. It is used for rescue of methotrexate, 3-4 times a day, 5-15mg orally for 2 days; Or 3-6mg intramuscular injection; Methotrexate is ineffective after taking this drug for more than 4 hours. Used for detoxification of pyrimethamine or trimethoprim, 5~15mg orally daily. Calcium folinate is used in combination with fluorouracil, 20~30mg/m2, and is taken orally half an hour after fluorouracil administration. |
| drug and application | calcium folinate (CF) has no anti-tumor effect by itself, and is mainly used for high-dose rescue and simultaneous application with fluorouracil to strengthen the therapeutic effect of the latter. The so-called high-dose methotrexate-calcium folinate (HD MTX-CF) rescue therapy is the application of MTX intravenous drip more than 100 times higher than the conventional dose, generally 2~5mg/m2, intravenous drip for 4~6h, so that the blood concentration reaches a fairly high level, so that the intracellular MTX reaches an effective concentration above 10-5mol/L. In this way, it can be spread to solid tumors with poor blood supply and cross the physiological barriers such as blood-cerebrospinal fluid and testis. However, high-dose MTX can have fatal toxic reactions, so detoxification measures must be taken within a certain time after MTX drip. CF rescue usually starts 2~18 hours after MTX drip ends. Intramuscular injection or intravenous injection at a dose of 6~15 μg/m2, once/6h, for a total of 12 times for 3 days. CF dose and injection time are related to the application of MTX, that is, the blood drug concentration of MTX can be stopped when the safety threshold is below 10-7mol/L. In addition, auxiliary hydration and alkalization treatment should be given to support it. The preparation of CF is generally 6mg water injection. Another therapy is calcium folinate and fluorouracil to improve the efficacy of the latter, which is generally called CF-FU combination therapy. The principle is: in the process of DNA synthesis, deoxyuridonic acid (dUMP) needs to accept the methyl group converted from tetrahydrofolate (THF) under the catalysis of adenylate synthase (TMPS) to form deoxyadenylate (d TMP). At this time, dihydrofolate reductase converts dihydrofolate into tetrahydrofolate. The main mechanism of action of fluorouracil is to become fluorouracil deoxynucleotide after entering the human body, inhibiting TMPS. During the reaction, TMPS, THF, and dUMP 3 form a transitional complex. After the general reaction is over, this complex decomposes and releases dihydrofolate, TMPS and dTMP. However, after FU is given, this complex cannot be decomposed, the function of the enzyme is inhibited, and dTMP cannot be generated. The binding force of the fluorouracil deoxynucleotide to the enzyme is proportional to the concentration of THF. Increasing the supply of THF can enhance the effect of FU in inhibiting TMPS. The specific clinical application is generally: intravenous drip of 200~500mg/m2CF for 2 hours first, intravenous injection of FU370mg/m2 after drip, and continuous use for 5 days as a course of treatment; This treatment can be repeated for 21~28 days. This CF-FU combination therapy has a better effect on the treatment of colorectal cancer, which is better than FU alone, and the adverse reactions have not increased much. |
| adverse reactions, contraindications and drug effects | occasional rash, urticaria or asthma, etc. Malignant anemia or megaloblastic anemia caused by vitamin B12 deficiency is contraindicated. It is not suitable to be used at the same time as folic acid antagonists such as methotrexate, and this drug should be applied 24~48h after using large doses of methotrexate; be careful to combine acidic urine, ascites, water loss, gastrointestinal obstruction, pleural effusion or The detoxification treatment of methotrexate for renal dysfunction; for those in urgent need of the disease, the dosage of this drug should be increased; creatinine clearance rate should be measured before treatment, and plasma or serum methotrexate concentration should be measured every 12~24 hours after the application; serum creatinine was measured before and every 24 h after treatment with methotrexate, and the 50% after treatment was greater than that before treatment, indicating severe nephrotoxicity. Urine acidity was monitored every 6h before and after methotrexate, urine pH value was kept above 7, and sodium bicarbonate and hydration were used if necessary. A larger dose is used together with barbiturate, promione or phenytoin sodium, which can affect the antiepileptic effect. |
| использование | 1. Mainly used as an antidote for folic acid antagonists (such as methotrexate, pyrimethamine or trimethoprim, etc.). 2. It is used to prevent severe toxic effects caused by excessive or high-dose methotrexate treatment. 3. Megaloblastic anemia caused by folic acid deficiency. 4. When combined with fluorouracil, it is used to treat advanced colon cancer and rectal cancer. It can be used to relieve the toxic reaction caused by the overdose of aminotrexate and methotrexate, and it can also be used to treat giant red blood cell anemia. Calcium folinate counteracts the effect of folic acid antagonists, which bind folic acid dehydroreductase (dihydrofolate reductase) to prevent the conversion of folic acid into tetrahydrofolic acid. Medically, after methotrexate chemotherapy, calcium folinate is used to reduce the toxicity of methotrexate. Calcium folinate also enhances the cytotoxic effect of 5-fluorouracil in anti-cancer. Calcium folinate can counteract the effect of folic acid antagonists. Folic acid works by binding dihydrofolate reductase and blocking the conversion of folic acid into tetrahydrofolate. In medicine, calcium folinate is used to reduce the toxicity of methotrexate after methotrexate treatment. |
Фабрика и отгрузка
