Ifosfamide
【Drug Name】 General name: Ifosfamide for injection English name:Ifosfamide for Injection Pinyin: Zhusheyong Yihuanlinxian'an 【Ingredients】 The main ingredient of this product is ifosfamide.
Keywords：
Ifosfamide
Categories：
Anti-neoplastic Drug Series
Hotline：
Ifosfamide
【Drug Name】
General name: Ifosfamide for injection
English name:Ifosfamide for Injection
Pinyin: Zhusheyong Yihuanlinxian'an
【Ingredients】
The main ingredient of this product is ifosfamide.
Chemical name: 3-(α-chloroethyl)-2-[(2-chloroethyl)amino]-tetrahydro-2H-1,3,2-oxaphosphor 2-oxide.
Molecular formula:C7H15Cl2N2O2P
Molecular weight: 261.09
Used accessories: glycine, mannitol.
【Properties】 This product is a white or almost white loose block or powder.
【Adaptiveness】 Suitable for testicular cancer, ovarian cancer, breast cancer, sarcoma, malignant lymphoma, and lung cancer.
【Specifications】 1.0g
【Dosage】
This product was dissolved and diluted with 0.9% sodium chloride solution and slowly instilled for at least 30 minutes.
Single-agent treatment Intravenous injection of 1.2~2.5g/m2 daily for body surface area is a course of treatment for 5 consecutive days.
Combination of drugs intravenous injection of body surface area daily 1.2 ~ 2.0g/m2, a course of treatment for 5 consecutive days.
At the same time as the administration and at 4 hours and 8 hours after the administration, Mesona sodium 0.4 g was intravenously injected into physiological saline.
The dose administered to patients with impaired liver and kidney function has not been determined.
【Adverse reactions】
In patients who used only monophosphamide alone, the limiting dose toxicity was myelosuppression and uremic toxicity. The use of doses in divided doses, large intakes of water, and the use of protective agents such as Mesna, can significantly reduce hemorrhagic cystitis with hematuria, particularly the incidence of hematuria seen with the naked eye. The daily dose of 1.2g/m2, once every 5 days, is usually mild to moderate if leukopenia occurs. Other significant side effects are hair loss, nausea, vomiting, and central nervous system toxicity.
1. Hematological Toxicity: Myelosuppression is dose-related and limit-dose toxicity. Mainly leukopenia, followed by thrombocytopenia. Daily use of ifosfamide 1.2g/m2 alone, 50% of patients who have used 5 days on the 5th day may have a white blood cell count of less than 3000/μl. Thrombocytopenia (< 100000/μl) occurs in approximately 20% of patients at this dose. At higher doses, there is almost a decrease in leukopenia. In the total dose of 10 ~ 12g/m2 course of treatment, half of the patients had white blood cells below 1000/μl, and 8% had platelets below 50,000/μl. Myelosuppression is usually reversible and can be given every 3 to 4 weeks. When ifosfamide is used in combination with other myelosuppressants, the dose must be adjusted. Patients with severe bone marrow suppression may increase the risk of infection.
2. Digestive System: Nausea and vomiting occur in 58% of patients treated with this drug and can usually be controlled with standard antiemetic therapy. Other gastrointestinal side effects are anorexia, diarrhea, and constipation in some cases.
3. Urinary System: Urinary tract toxicity is hemorrhagic cystitis, dysuria, urinary frequency and other bladder irritation. Hematuria occurs in 6% to 92% of patients treated with this drug. By ingesting a large amount of water, the use of a protective agent such as Mesna sodium in divided doses can significantly reduce the incidence and severity of hematuria. At a daily dose of 1.2 g/m2, on 5 consecutive days, about half of the patients who did not use protective agents had microscopic hematuria, and about 8% of patients had macroscopic hematuria.
Kidney toxicity occurred in only 6% of patients treated with ifosfamide alone. Clinical indications of elevated blood urea nitrogen (BUN) or serum creatinine, or reduced creatinine clearance, are usually temporary. These may be related to the damage of the renal tubules. One case of occasional renal tubular acidosis has been reported to progress to chronic renal failure, with proteinuria and acidosis occurring in rare cases. In one study, the dose of this drug was 2 to 2.5 g/m 2 daily, and on 4 days, metabolic acidosis occurred in 31% of patients. Renal tubular acidosis, Fanconi syndrome, and nephrotic rickets have also been reported. It is therefore advisable to closely monitor serum and urine chemistry, including phosphorus, potassium, alkaline phosphatase and other appropriate laboratory tests. Appropriate replacement therapy should be used.
4. Central nervous system: 12% of patients receiving this drug have central nervous system side effects. The most common are drowsiness, confusion, depressive psychosis and hallucinations. Other rare symptoms are dizziness, loss of orientation, and cerebral nerve dysfunction. Occasionally reported seizures and fatal coma. Patients with altered renal function have a higher incidence of central nervous system toxicity.
5. Other: About 83% of patients treated with ifosfamide monotherapy developed hair loss. The incidence of combined medication can be as high as 100%, depending on other drugs in the chemotherapy regimen. An increase in liver enzymes and/or bilirubin occurred in 3% of patients. Other rare side effects are: phlebitis, pulmonary symptoms, unexplained fever, allergic reactions, stomatitis, cardiotoxicity, and polyneuropathy.
Long-term medication can produce immunosuppression, hypopituitarism, infertility and secondary tumors.
Taboo is not clear.
【Precautions】
1. Urinary system: The use of ifosfamide is often associated with the toxic side effects of the urinary system, especially hemorrhagic cystitis, so it is recommended to give routine analysis of urine before each dose of the drug. If the microscopic examination has hematuria (more than 10 red blood cells per high power field), it should be disabled until complete elimination of hematuria. After the application of this drug, it is necessary to drink plenty of water or inject large amounts of aqueous solution.
2. Hematopoietic system: Ifosfamide is used in conjunction with other chemotherapeutic agents and often presents with severe bone marrow suppression. Therefore, it is recommended to closely monitor hematological parameters. Leukocytes, platelet counts, and hemoglobin measurements were taken before each dose and at appropriate intervals. Diaphosphamide should not be given unless clinically necessary, for patients with less than 2000/μl white blood cells and/or platelets less than 50,000/μl.
3. Central nervous system: Neurological symptoms reported after ifosfamide treatment are: lethargy, confusion, hallucinations, and coma in some cases. Stop taking this medicine when these symptoms occur. These symptoms are usually reversible and can take symptomatic supportive therapy until it completely disappears.
4. Ifosfamide should be used with caution in patients with impaired liver and kidney function, impaired bone marrow function, such as leukopenia, neutropenia, extensive bone marrow metastases, first radiotherapy, or previous use of other cells. Poison drug therapy; hypoalbuminemia; women of childbearing age.
5. Laboratory tests: During the treatment, the patient's blood (especially neutrophils and platelets) should be tested regularly to understand the degree of hematopoietic suppression. Red blood cells in the urine should also be checked regularly, which can occur before hemorrhagic cystitis.
6. This product is unstable in aqueous solution and needs to be used immediately. Wear gloves while dispensing. If you accidentally touch this product, skin reactions may occur. Wash immediately with soap and water.
Pregnancy and lactation women medication
Animal studies have shown that this product has mutagenic, teratogenic effects, can cause fetal death or congenital malformations, pregnant women disabled. This product can be excreted in breast milk, and you must stop breastfeeding when you start using it.
Pediatric Use is not clear.
Elderly medication is not yet clear.
【medicine interactions】
1. Previous use of cisplatin patients can aggravate the bone marrow suppression, neurotoxicity, and nephrotoxicity of ifosfamide.
2. Using anticoagulant drugs at the same time may lead to bleeding.
3. Using hypoglycemic drugs at the same time can enhance hypoglycemic effect.
4. When combined with other cytotoxic drugs, they should be reduced as appropriate.
5. At the same time, radiotherapy can increase the skin reaction caused by radiotherapy.
[overdosage] There is no special antidote for ifosfamide poisoning. Supportive care is generally used to maintain the patient's life.
Pharmacology and Toxicology
Pharmacological effects
This product has no anticancer activity in vitro and enters the body and is hydrolyzed by the phosphoramidase or phosphatase present in the liver or tumor, and becomes active phosphamide mustard. Its mechanism of action may be cross-linking with DNA, inhibiting DNA synthesis, and may also interfere with the function of RNA. It is a cell cycle non-specific drug. This product has a broad spectrum of anti-tumor, inhibiting a variety of tumors.
Toxicological research
Genotoxicity: In vitro bacterial mutation tests and tests conducted in mammalian cells have shown that this product has a mutagenic effect. Mutations in mice and Drosophila melanogaster blasts can be induced in vivo and cause dominant lethal mutations in male mice and recessive linked lethal mutations in Drosophila.
Reproductive toxicity: Pregnancy mice were given ifosfamide 30 mg/m2 on the 11th day of pregnancy. On the 19th day, the increase in embryonic uptake was observed. After the use of ifosfamide 54 mg/m2 from the sixth to the 15th day of pregnancy, the embryonic lethal effect was observed. Rabbits were given ifosfamide 88 mg/m2 from the 6th to the 18th day after mating, and embryotoxicity was observed. Abnormal embryos increased significantly compared with the control group.
Carcinogenicity: This product was found to be carcinogenic in rat studies. Female rats developed leiomyosarcoma and mammary fibroids.
【Pharmacokinetics】
After entering the body, it is extensively metabolized and different individual metabolites may be different. Metabolic saturation occurs at high doses. According to the body surface area of a single intravenous injection of 3.8 ~ 5.0g/m2, blood concentration was biphasic attenuation, terminal elimination half-life of about 15 hours; according to the body surface area of a single intravenous injection of 1.6 ~ 2.4g/m2, plasma concentration was single-phase attenuation The elimination half-life of the terminal is about 7 hours; 70%-80% is excreted by the kidneys; when the body surface area is intravenously 5.0g/m2, 61% is discharged by the prototype; when the body surface area is once intravenously 1.2-2.4g/m2 Only 12% to 18% are discharged as prototypes.
【Storage】 Shade, save in cold place.
【Packing】 Regulated glass bottles, 1 pc/box.
【Valid period】 36 months.
[Executive standard] National Drug Standard YBH11862005
【Approval number】 National Drug Qualification H20055196
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