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Fluorouracil (5-FU, 5-fluorouracil), sold under the brand name Adrucil among others, is a cytotoxic chemotherapy medication used to treat cancer. [3] By intravenous injection it is used for treatment of colorectal cancer , oesophageal cancer , stomach cancer , pancreatic cancer , breast cancer , and cervical cancer . [ 3 ]
Two major mechanisms of action have been elucidated: Flucytosine is intrafungally converted into the cytostatic fluorouracil [9] which undergoes further steps of activation and finally interacts as 5-fluorouridinetriphosphate with RNA biosynthesis thus disturbing the building of certain essential proteins.
The transporter recognizes 5-FU as an endogenous molecule. Subsequently, the uracil and 5-FU compete to enter the cellular interior and it is the molecule with the highest concentration that will enter in greater abundance. For 5-FU to inhibit TS by its mechanism of action, it must first be bioactivated through a series of reactions:
The cytotoxic antibiotics are a varied group of drugs that have various mechanisms of action. The common theme that they share in their chemotherapy indication is that they interrupt cell division . The most important subgroup is the anthracyclines and the bleomycins ; other prominent examples include mitomycin C and actinomycin .
Tegafur is a chemotherapeutic prodrug of 5-fluorouracil (5-FU) used in the treatment of cancers. It is a component of the combination drug tegafur/uracil. When metabolised, it becomes 5-FU. [1] It was patented in 1967 and approved for medical use in 1972. [2]
Floxuridine is rapidly catabolized to 5-fluorouracil, which is the active form of the drug. The primary effect is interference with DNA synthesis and to a lesser extent, inhibition of RNA formation through the drug's incorporation into RNA , thus leading to the production of fraudulent RNA.
Examples: 5-Fluorouracil, Gemcitabine, and Cytarabine; nucleoside analogues – nucleoside alternatives that consist of a nucleic acid analogue and a sugar. This means these are the same bases as above, but with an added sugar group. For the nucleoside analogues either the base or the sugar component can be altered.
The mechanism of action of carmofur prodrug is traditionally thought to be the generation of 5–FU. [2] However, carmofur is a highly potent acid ceramidase (AC) inhibitor. [2] Ceramide influences cancer cell survival, growth and death. [2] Inhibition of AC activity sensitizes tumor cells to the effects of antineoplastic agents and radiation. [2]
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