Steroids Raw Powder Lomustine CAS 13010-47-4

Steroids Raw Powder Lomustine is an alkylated drug, belonging to chloroethylamine nitrosourea anticancer drugs. It acts on the G1 phase, G1 ~ s boundary, and M phase, and also acts on the G2 phase. It is a cell cycle nonspecific drug. This product is characterized by high-fat solubility, can pass through the blood-brain barrier, and has fast use absorption.Lomustine powder is used for primary and secondary tumors, such as glioma, malignant lymphoma, lung cancer, breast cancer, gastrointestinal cancer, and so on. And primary and metastatic brain tumors after appropriate surgical and radiotherapy procedures. At the same time, in the second-line treatment of Hodgkin's lymphoma, combined with other chemotherapy drugs, this product can be used to treat patients with lymphoma recurrence or ineffective primary treatment.

What is the drug toxicology of lomustine?

1. The Steroids Raw Powder Lomustineis a cell cycle nonspecific drug. It is most sensitive to cells at the g2-s boundary or early S phase, and also has an inhibitory effect on the G2 phase.

2. Animal experiments show that its mechanism is similar to that of BCNU. After entering the human body, the molecule breaks from the carbamide bond into two parts:

(1) One is the chloroethylamine part, which dissociates chlorine to form ethylene carbon positive ion and plays the role of alkylation, resulting in DNA strand breakage and alkylation of RNA and protein, which are mainly related to the anti-tumor effect.

(2) The other is that the carbamoyl part is changed into isocyanate or converted into carbamic acid to play the role of carbamoylation. It mainly reacts with proteins, especially the terminal amino group of lysine. It is believed that this is mainly related to bone marrow toxicity. Carbamoylation can also destroy some enzyme proteins, making it difficult to repair DNA after alkylation, which is conducive to the anticancer effect.

3. Although the CCNU has the function of alkylating agent. However, it has no cross-resistance to general alkylating agents, vincristine, methyl benzyl hydrazine, and antimetabolic drugs. Experiments on mice and rabbits showed that the drug was carcinogenic.

What is the pharmacokinetics of this product?

1. It is easily absorbed by use administration and quickly becomes metabolites in the body. The organs are mainly distributed in the liver (bile), kidney, and spleen, followed by the lung, heart, muscle, small intestine, large intestine, etc. It can pass through the blood-brain barrier. After a few minutes, the drug concentration in cerebrospinal fluid is 15 ~ 30% of that in plasma. It can be discharged into the intestine through bile to form Hepatointestinal circulation, so the efficacy is long-lasting.

2. The plasma protein binding rate is 50% (metabolite), and T1 / 2 is 16 ~ 18 hours. Its persistence may cause delayed bone marrow suppression.

3. It is metabolized completely in the liver, excreted in bile, and has intestinal liver circulation, so it has a long-lasting effect.

4. There is no prototype drug in urine, plasma, and cerebrospinal fluid.

5. Within 24 hours after use administration, 50% of the steroids Raw Powder Lomustine is excreted from urine in the form of metabolites, but the excretion in 4 days is less than 75%, less than 5% from feces, and about 10% from the respiratory tract.

6. Because of its strong fat solubility, it can effectively penetrate the blood-brain barrier.

7. the drug concentration in cerebrospinal fluid is 50% or higher than that in plasma.

What should we pay attention to when using lomustine?

The advantages of this product are very obvious. For example, this product has strong fat solubility and can enter cerebrospinal fluid through the blood-brain barrier. It is often used in primary brain tumors (such as glioblastoma) and secondary tumors. The combination of drugs has outstanding effects in the treatment of gastric cancer, rectal cancer, bronchial lung cancer, and malignant lymphoma.

However, in the following cases, users should pay attention, consult doctors and use with caution.

1. Nausea and vomiting can occur within 6 hours after use administration, which can last for 2 ~ 3 days. It can be alleviated by taking sedatives or metoclopramide in advance and taking drugs on an empty stomach.

2. A few patients have gastrointestinal bleeding and liver function damage. Bone marrow suppression and thrombocytopenia can be seen 3 ~ 5 weeks after taking the medicine, and leukopenia can occur twice in the first and fourth weeks after taking the medicine, and recover only in the sixth to eighth weeks; However, bone marrow suppression is cumulative.

3. Occasional systemic rash may cause teratogenesis, inhibit testicular or ovarian function, and cause amenorrhea or sperm deficiency. It should be prohibited for pregnant and lactating women.

4. Liver function damage and white blood cell lower than 4 × 109 / L, platelet less than 80 × 109 / L is forbidden. In case of combined infection, the infection should be treated first.

If everything is normal after using this product, pay attention to follow-up and check blood routine and platelet, blood urea nitrogen, blood uric acid, creatinine clearance, blood bilirubin, alanine aminotransferase, lung function, etc.

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