Carustine

Carustine Uses, Dosage, Side Effects, Food Interaction and all others data.

A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed)

Carustine is one of the nitrosoureas indicated as palliative therapy as a single agent or in established combination therapy with other approved chemotherapeutic agents in treatment of brain tumors, multiple myeloma, Hodgkin's disease, and non-Hodgkin's lymphomas. Although it is generally agreed that carmustine alkylates DNA and RNA, it is not cross resistant with other alkylators. As with other nitrosoureas, it may also inhibit several key enzymatic processes by carbamoylation of amino acids in proteins.

Trade Name Carustine
Availability Prescription only
Generic Carmustine
Carmustine Other Names BCNU, bis-chloroethylnitrosourea, Bischloroethyl nitrosourea, Carmustina, Carmustine, Carmustinum
Related Drugs methotrexate, Keytruda, rituximab, pembrolizumab, Rituxan, doxorubicin, cisplatin, cyclophosphamide, Revlimid, Avastin
Type
Formula C5H9Cl2N3O2
Weight Average: 214.05
Monoisotopic: 213.007181961
Protein binding

80%

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Carustine
Carustine

Uses

Carustine is an alkylating agent used in the treatment of various malignancies, including brain tumours and multiple myeloma, among others.

For the treatment of brain tumors, multiple myeloma, Hodgkin's disease and Non-Hodgkin's lymphomas.

Carustine is also used to associated treatment for these conditions: Astrocytomas, Brain Stem Gliomas, Ependymomas, Glioblastomas, Medulloblastomas, Mycosis Fungoides (MF), Recurrent Glioblastoma Multiforme, Refractory Hodgkin Lymphoma, Refractory Multiple Myeloma, Tumors Metastatic to Brain, High grade newly diagnosed Glioma, Refractory Non-Hodgkin's lymphoma

How Carustine works

Carustine causes cross-links in DNA and RNA, leading to the inhibition of DNA synthesis, RNA production and RNA translation (protein synthesis). Carustine also binds to and modifies (carbamoylates) glutathione reductase. This leads to cell death.

Toxicity

The oral LD50s in rat and mouse are 20 mg/kg and 45 mg/kg, respectively. Side effects include leukopenia, thrombocytopenia, nausea. Toxic effects include pulmonary fibrosis (20-0%) and bone marrow toxicity.

Food Interaction

  • Avoid echinacea.

Elimination Route

5 to 28% bioavailability

Half Life

15-30 minutes

Elimination Route

Approximately 60% to 70% of a total dose is excreted in the urine in 96 hours and about 10% as respiratory CO2.

Innovators Monograph

You find simplified version here Carustine

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http://classyfire.wishartlab.com/tax_nodes/C0001516
http://classyfire.wishartlab.com/tax_nodes/C0003940
http://classyfire.wishartlab.com/tax_nodes/C0004150
http://classyfire.wishartlab.com/tax_nodes/C0001831
http://classyfire.wishartlab.com/tax_nodes/C0001026
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:3423
http://www.hmdb.ca/metabolites/HMDB0014407
http://www.genome.jp/dbget-bin/www_bget?drug:D00254
http://www.genome.jp/dbget-bin/www_bget?cpd:C06873
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2578
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506980
https://www.chemspider.com/Chemical-Structure.2480.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50015950
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=2105
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=3423
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL513
https://zinc.docking.org/substances/ZINC000003830387
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000041
http://www.pharmgkb.org/drug/PA448810
http://www.rxlist.com/cgi/generic3/carmustine.htm
https://www.drugs.com/cdi/carmustine.html
https://en.wikipedia.org/wiki/Carmustine
*** Taking medicines without doctor's advice can cause long-term problems.
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