【Drug Name】

General name: Formosamide for injection

English name:Fotemustine for Injection

Pinyin: Zhusheyong Fumositing

 

【Ingredients】

The main ingredients of  this product: Formerine.

Chemical name: (±) 1-[3-(2-chloroethyl)-3-nitrosourea]ethyl diethylphosphite.

Molecular formula:C9H19ClN3O5P

Molecular weight: 315.69

 

【Properties】 This product is light yellow lyophilized powder. The injection solvent is a colorless, transparent liquid with an odor of ethanol.

 

Indications Used to treat primary malignant brain tumors and disseminated malignant melanomas (including intracerebral sites).

 

【Specification】 208mg

 

【Dosage】

Prepare the solution immediately before use. Once the solution is formulated, it must be given in dark conditions; intravenous infusion is controlled for more than 1 hour.

The contents of the formalinator bottle were dissolved in 4 ml of sterile ethanol solution in an ampule, and the amount of the drug was calculated. The solution was diluted with 250 ml of 5% isotonic glucose injection and used for intravenous infusion.

1. Single-agent chemotherapy includes:

Induction therapy: After 3 times a week, stop taking medication for 4 to 5 weeks.

Maintenance treatment: treatment every three weeks.

A dose of 100 mg/m2 is usually used.

2. Combination Chemotherapy: Remove the third dose of induction therapy at a dose of 100 mg/m2.

 

【Adverse reactions】

1. The adverse reactions were mainly on hematological effects, manifested as thrombocytopenia (40.3%) and neutropenia (46.3%), occurred later, the lowest levels were 4 to 5 weeks and 5 to 6 after the first dose of induction therapy. Week appears.

If chemotherapy is used prior to the administration of formostatin for injection and/or the product is used in combination with other drugs that can induce hematopoietic toxicity, adverse reactions in the blood system may increase.

2. Common moderate nausea and vomiting (46.7%) mostly occurred within 2 hours after injection. In addition, there was a moderate, temporary, reversible increase (29.5%) in aminotransferase, alkaline phosphatase, and blood bilirubin.

3. Rare adverse reactions included fever (3.3%), injection site phlebitis (2.9%), diarrhea (2.6%), abdominal pain (1.3%), temporary increase in urea (0.8%), pruritus (0.7%), temporary, Reversible neurological dysfunction (impaired consciousness, paresthesia, and deodorization) (0.7%).

4. In combination with dacarbazine (see drug interactions), very little pulmonary toxicity (acute adult respiratory depression syndrome) was observed.

 

Taboo

1. Pregnancy and lactation women;

2. Prohibited from the combined use of yellow fever vaccine and the use of phenytoin as a prophylactic treatment (see drug interactions);

3. This product is generally not recommended for use in conjunction with live attenuated vaccines.

 

【Precautions】

1. This product is not recommended for patients who have received chemotherapy within the past 4 weeks (or who have been treated with nitrosoureas within 6 weeks).

2. Only patients should consider using this product when their platelet and/or granulocyte counts are equal to or greater than 100,000/mm3 and 2,000/mm3, respectively.

3. Prior to each new dose, blood cell counts will be required and the doses will be adjusted based on the hematology. The following table can be used as a guide:

4. It is recommended that from the start of induction therapy to the start of maintenance therapy, the recommended interval is 8 weeks between every two maintenance treatment cycles, with an interval of 3 weeks.

5. Maintenance therapy is only considered when platelet and/or granulocyte counts reach 100,000/mm3 and 2,000/mm3, respectively.

6. Liver function tests are recommended during induction and after treatment.

7. The formulated solution should avoid contact with the skin and mucous membranes, as well as the possibility of absorption of any drug solution. It is advisable to wear masks and protective gloves when preparing the solution. If accidentally splashed out, rinse thoroughly with water.

8. Contaminated items should be discarded under conditions that ensure safety.

 

[pregnant and lactating women medication] This product is banned during pregnancy and lactation.

 

Pediatric Use There is currently no information available on the study of children in this product.

 

[Geriatric Use] This experiment was not conducted and there is no reliable reference.

 

【medicine interactions】

It has the same interaction with all cytotoxic drugs.

1. Because tumors increase the risk of thrombosis, anticoagulation therapy is usually used. There is a large inter-individual variation in blood coagulation in tumor cases, which increases the unanticipated event of interaction between oral anticoagulants and anti-tumor chemotherapy. Therefore, if you decide to take oral anticoagulant therapy, you need to increase the number of INR tests.

2. Combination drug contraindication

1) Phenytoin (in order to prevent the application of certain antitumor drugs induced seizures)

Doxorubicin, daunorubicin, carboplatin, cisplatin, carmustine, vincristine, vinblastine, bleomycin, methotrexate, phenytoin absorption in the digestive tract due to inhibitors of cell proliferation The decrease, thereby triggering the onset of convulsions. Can be used together with anticonvulsant benzodiazepines for a short period of time.

2) Yellow fever vaccine poses a risk of widespread fatal vaccine diseases.

3. Combination medications need to be considered

1) Cyclosporine (doxorubicin, etoposide): There may be excessive immunosuppression, resulting in lymph node hyperplasia.

2) Immunosuppressive agents (derived from cyclosporine extrapolation): Excessive immunosuppression leads to the risk of lymphocyte proliferation.

4. The specific interaction of this product with dacarbazine:

Pneumoconiosis (acute adult respiratory distress syndrome) occasionally occurs when this product is applied on the same day as a large dose of dacarbazine, and care should be taken to avoid such administration.

Combination therapy should be based on the following recommended methods:

1) Induction therapy:

Forstine 100 mg/m2/day on days 1 and 8.

Dacarbazine 250 mg/m2/day on days 15, 16, 17 and 18.

5 weeks treatment rest period.

2) Maintenance treatment:

Formalin 100 mg/m2/day on day 1.

Dacarbazine 250 mg/m2/day on days 2, 3, 4, and 5.

 

【Overdosage】 There is no effective antidote at present, and hematological monitoring must be strengthened.

 

Pharmacology and Toxicology

Formanstine is an antitumor drug that inhibits cell proliferation in nitrosoureas, has alkylation and carbamylation activity, and has experimental broad spectrum antitumor activity. Its chemical structure contains an alanine bio-electronic ligand (amino-1-ethyl-phosphate) that allows it to easily penetrate cells and pass through the blood-brain barrier.

 

【Pharmacokinetics】

After intravenous infusion in humans, the plasma elimination kinetics is eliminated with a single or double index, and the terminal half-life is short. Drug molecules are almost completely metabolized. The plasma protein binding rate is low (25-30%).

Formersin can cross the blood-brain barrier.

 

[Storage] Shading, sealing, storage at 2-8°C, newly prepared solution must be used immediately.

 

【Package】

Medicinal antibiotic glass bottles.

Each kit includes: 1 bottle of powder containing 208 mg of Formalosine; 1 ampoult solvent for dilute powder for parenteral application containing 95% (v/v) ethanol 3.35 ml and water for injection The total amount of 4 ml. The prepared solution was 4.16 ml, that is, 4 ml of the solution contained 200 mg of Formoxerine.

 

【Valid period】 24 months.

 

【Performance】 YBH32102005

 

【Approval number】 State Drug Qualification H20058774