Karmustin is a cytostatic antitumor chemotherapeutic drug with an alkylating type of action from the group of nitrosourea derivatives .
| Karmustin | |
|---|---|
| Chemical compound | |
| Gross formula | C 5 H 9 Cl 2 N 3 O 2 |
| Cas | |
| PubChem | |
| Drugbank | |
| ATX | |
Content
- 1 Pharmacological action
- 2 Pharmacokinetics
- 3 Indications
- 4 dosage
- 5 Side effects
- 6 Contraindications
- 7 Pregnancy and lactation
- 8 Special instructions
- 9 Drug Interactions
- 10 notes
Pharmacological action
Antitumor agent of alkylating action from the group of nitrosourea derivatives. It acts on the bases and phosphate groups of DNA, which leads to breaks and cross-linking of its molecule. It is a cyclone-specific compound. The action of karmustin can also be associated with the modification of proteins.
Pharmacokinetics
It is rapidly metabolized in the liver with the formation of active metabolites. Metabolites can persist in blood plasma for several days. Penetrates through the BBB. It is excreted mainly by the kidneys in the form of metabolites - 60-70%, with feces - 1%, through the respiratory tract - 10%.
Indications
Brain tumors (glioblastoma, brain stem glioma, medulloblastoma, astrocytoma, ependymoma), metastatic brain tumors; multiple myeloma (in combination with prednisone); lymphogranulomatosis (in combination with other drugs); non-Hodgkin lymphomas.
Dosage
Installed individually, depending on the indications and stage of the disease, the state of the hematopoietic system, anti-tumor therapy regimen.
Side effect
From the hemopoietic system: often - myelodepression; anemia is possible. From the digestive system: often - nausea, vomiting; manifestations of hepatotoxicity are possible - an increase in the activity of transaminases, alkaline phosphatase, and bilirubin level. From the respiratory system: the occurrence of infiltrates and / or foci of fibrosis in the lungs is possible. From the urinary system: after prolonged use in high cumulative doses - progressive azotemia, a decrease in kidney size. With rapid iv administration: a burning sensation at the injection site is possible, as well as severe reddening of the skin and swelling of the conjunctiva within 2-4 hours. Other: neuroretinitis, chest pain, headache, allergic reactions, arterial hypotension, tachycardia are possible.
Contraindications
Hypersensitivity to carmustine or other nitrosourea derivatives.
Pregnancy and lactation
Adequate and strictly controlled safety studies of the use of karmustin during pregnancy in humans have not been conducted. There is evidence of the embryotoxic effect of carmustine during pregnancy in humans. In experimental studies, it was shown that carmustine has an embryotoxic effect in pregnancy in rats and rabbits and a teratogenic effect in rats in doses equivalent to the doses used in humans. Women of childbearing age are recommended to use reliable methods of contraception during the treatment period. It is not known whether carmustine with breast milk is excreted. If necessary, use during lactation should stop breastfeeding.
Special instructions
In the process of treatment, it is necessary to control the picture of peripheral blood, liver, kidney and X-ray examination of the lungs. Since the distinctive feature of karmustin is the delayed manifestation of a depressing effect on hematopoiesis, the monitoring of the picture of peripheral blood should be carried out weekly for 6 weeks after the end of use.
Drug Interactions
With simultaneous use with other drugs that cause myelodepression, additive inhibition of bone marrow function is possible; with drugs that have a hepato- or nephrotoxic effect - an increase in the manifestations of hepato- or nephrotoxicity.