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What is Carmustin?

Nov. 2021/6/21 15:18:01 By LEAP Chem


This is part of our ongoing series helping consumers better understand pharmaceutical ingredients. We translate the pharmaceutical science, explain the drug natures, and give you an honest advice, so you can choose the right drugs for your family!

Molecular formula of carmustin: C5H9Cl2N3O2

Chemical IUPAC Name: 1,3-bis(2-chloroethyl)-1-nitroso-urea

Molecular weight: 214.049 g/mol

CAS No.: 154-93-8

Structural Formula:

 154-93-8.png

Carmustin

Carmustin (bis-chloroethylnitrosourea, BCNU, BiCNU), an alkylating agent, is an anti-cancer medication used to treat various types of cancers. It is a medication introduced in the United Kingdom and distributed by Bristol-Myers Squibb. Carmustin is a chemotherapy medication given to patients with cancers like lymphomas, brain tumors and myeloma. As a dialkylating agent, BCNU is able to form interstrand crosslinks in DNA, which prevents DNA replication and DNA transcription. It has the appearance of an orange-yellow solid.

 

Uses of Carmustin

It is used in the treatment of several types of brain cancer (including glioma, glioblastoma multiforme, medulloblastoma and astrocytoma), multiple myeloma and lymphoma (Hodgkin's and non-Hodgkin). BCNU is sometimes used in conjunction with alkyl guanine transferase (AGT) inhibitors, such as O6-benzylguanine. The AGT-inhibitors increase the efficacy of BCNU by inhibiting the direct reversal pathway of DNA repair, which will prevent formation of the interstrand crosslink between the N1 of guanine and the N3 of cytosine.

 

It is also used as part of a chemotherapeutic protocol in preparation for hematological stem cell transplantation, a type of bone marrow transplant, in order to reduce the white blood cell count in the recipient (patient). Use under this protocol, usually with Fludarabine and Melphalan, was coined by oncologists at the University of Texas MD Anderson Cancer Center.

 

Side Effects of Carmustin

The dosage for Carmustin is determined by the doctor and based on the patient's condition and the cancer. It is usually given with other chemotherapy medicaments to complete a treatment session. This also determines how long the treatment will last. Since Carmustin is in a liquid form, it is given through intrusion method.

 

Some side effects may occur with Carmustin, the degree of which may vary depending on the dosage being taken and the condition of the patient. Some patients experience wamble or feel sick just a few hours after the medication is given. In this case, doctors often prescribe anti-sickness medicaments.

 

Delayed haematological toxicity

The main danger of this haematological toxicity lies in its delayed occurrence. Severe thrombocytopaenia may be observed 4 to 5 weeks after treatment, and severe leucopaenia at 5 to 6 weeks.

This toxicity is dose-dependent and may become cumulative. Precise adaptation measures should therefore be instituted.

 

Pulmonary toxicity

This toxicity is characterised by infiltrates and/or fibrosis. It can be either acute (a few days after treatment) of most often delayed (3 to 4 years after treatment).

For patients with pulmonary toxicity, the cumulative dose was generally higher than 1,400 mg/m2 (prolonged efficient treatments).

Long term studies on patients treated for a brain tumour during childhood have revealed extremely delayed pulmonary toxicity occuring up to 15 years after treatment. In such cases, the cumulative doses proved to be of great importance.

 

Secondary cancer risk

Acute secondary leukaemia and medullar dysplasia have been observed after prolonged treatment.

 

References

https://en.wikipedia.org/wiki/Carmustine

https://www.ncbi.nlm.nih.gov/pubmed/383437

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