Alkylating agent Alkylating agent (alkylatingagents), also known as alkylating agent, is a class of very active chemical properties of compounds. They have active alkylating group, with cell DNA or protein in the amino, neck, hydroxyl and phosphate and other work, often to form cross-links or give rise to apurinic effect to DNA strand breaks, the next time replication when it is right or wrong can sour the nuclear base code, causing damage to DNA structure and function, in serious cases can lead to cell death.|
Nitrogen mustard Nitrogen mustard (chlorethamine, nitrogenmustard, mechlorethamine, HN2) was the first application of the alkylating agent, selective low, local irritation intensity, to intravenous injection. Role of rapid and short-term (minutes), but the consequences of bone marrow suppression is longer. Currently the main use of its available features, as mediastinal compression symptoms of the malignant lymphoma chemotherapy, and regional arterial chemotherapy administration or half (lower body cycle of oppression aorta), such treatment of head and neck cancer to improve local tumor drug concentration and reduce toxicity. May have nausea, vomiting, "] halo, vision loss, hair loss, jaundice, menstrual disorders and skin rashes and other adverse reactions.
Cyclophosphamide Cyclophosphamide (cyclophosphamide, endoxan, cytoxan, CTX) for the amide nitrogen mustard and a combination of phosphorus compounds.
Pharmacological effects of cyclophosphamide without the in vitro activity of the body via the liver cytochrome P-450 oxide, split ring generated intermediate aldehyde phosphoric amide (aldophosphamide), its tumor cells, has a strong decomposition of the effective phosphorus amide nitrogen mustard (phosphamidemustard), alkylation occurred only with DNA to form cross-linking, inhibition of tumor cell growth and reproduction. Cyclophosphamide broader spectrum anti-tumor, significant effect on malignant lymphoma. On multiple myeloma, acute lymphocytic leukemia, ovarian cancer, breast cancer, were also effective.
Process body good oral absorption, 1 hour, blood peak concentration, 17% ~ 31% of the drugs to prototype by the fecal discharge. 30% for activity type from the urine of kidney and bladder irritation. After intravenous injection of 6 ~ 8mg/kg, plasma t1 / 2 approximately 6.5 hours. In the liver and liver tissue distribution of more.
Side effects of cyclophosphamide can be taken orally or injected; vomiting, mild nausea, intravenous injection of large doses is still common; hair loss rate is higher than that of other alkylating agent about 30% to 60%, more than occurred at 3 to 4 weeks after medication; suppression of bone marrow, the granulocyte was more obvious; on the bladder mucosa irritation can cause hematuria, proteinuria; even can affect liver function, causing jaundice; also induced reduction of prothrombin; long use can cause amenorrhea or decreased sperm.
Thiophene for school Thiazolyl for school (thio-tepa, triethylenethiophosphoramide, TSPA) structure with three ethylene imine, the formation of active carbon to plasma and intracellular DNA three bases combined impact of tumor cell division. Higher selectivity, wider antitumor spectrum, is mainly used in breast cancer, ovarian cancer, liver cancer and malignant melanoma, etc., on the bone marrow inhibition induced neutropenia and thrombocytopenia, but lighter than the nitrogen mustard. Rare gastrointestinal reactions, local stimulation is small, can be used for intravenous injection, intramuscular injection and intra-arterial administration and thoracic (abdominal) cavity administration.
Busulfan (busulfan), also known as Maryland (myleran), an acid ester, in the body dissociation effect from rising alkylation. Small doses can inhibit neutrophil production, on chronic myeloid leukemia were significant (response rate 80% ~ 90%). Inhibited the whole blood increased as the dose. Chronic myeloid leukemia and acute leukemia acute lesions invalid. No significant effect on other tumors. Good oral absorption. After intravenous injection of 2 to 3 minutes, 90% of the drugs disappear from the blood. Most of the metabolism of methane in acid from the urine. The drug's gastrointestinal tract less inhibitory effect on the bone marrow. For a long time can lead to amenorrhea with or testicular atrophy, occasionally bleeding, aplastic anemia and pulmonary fibrosis and other serious reactions.
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