Thiotepa is a polyfunctional, organophosphorus alkylating agent and a stable derivative of N,N',N''-triethylenephosphoramide (TEPA), with antineoplastic activity. Thiotepa may cause fetal harm when administered to a pregnant woman, based on its mechanism of action and animal studies. In vivo and vitro studies show alkylation of DNA by Thiotepa and Tepa can follow two pathways, but it remains unclear which pathway represents the precise mechanism of action. Author information: (1)Faculty of Life Science, Kunming University of Science and Technology, Kunming, Yunnan, 650093, China. Although its mechanism of action is not fully understood, busulfan appears to act through the alkylation of DNA. 2. Following systemic absorption of busulfan, carbonium ions are formed, resulting in DNA alkylation and DNA breaks and inhibition of DNA replication and RNA transcription. Thiotepa for Injection, USP DESCRIPTION Thiotepa for injection is an ethylenimine-type compound. Therefore, thiotepa combined with other alkylating agents such as The radiomimetic action of thiotepa is believed to occur through the release of ethylenimine radicals which, like irradiation, disrupt the bonds of DNA. Ethylenimine groups attaches with N7 position of guanine base pair of DNA This will induce the cross linkages between the ds-DNA. MECHANISM OF ACTION: Thiotepa, a derivative of nitrogen mustard, acts as a polyfunctional alkylating agent. The Scottish Medicines Consortium has advised (June 2012) that thiotepa (Tepadina ®) is not recommended for use within NHS Scotland in combination with other chemotherapy as conditioning treatment in adults or children with haematological diseases, or solid tumours prior to haematopoietic stem cell transplantation. It is supplied as a non-pyrogenic, sterile lyophilized powder for intravenous, intracavitary or intravesical ... mechanism of action. Chemistry, pharmacology and pharmacokinetics of N,N′,N ... but it remains unclear which pathway represents the precise mechanism of action. In vivo and vitro studies show alkylation of DNA by Thiotepa and Tepa can follow two pathways, but it remains unclear which pathway represents the precise mechanism of action. Alkylating agent that produces crosslinking of DNA strands by reacting with phosphate groups to inhibit protein synthesis, DNA, and RNA. Most people develop side effects. This will further interferes with the … It may control malignant effusion by a direct antineoplastic effect after intracavitary admin. Alkylating agents produce their anti-cancer effects by causing a chemical reaction that damages the DNA in a cell. The DNA damage caused by thiotepa results in cell death. ♦Thiotepa (thy-oh-tep'-ah) Triethylene, Thio-Tepa, TESPA, TSPA Pregnancy Category D Mechanism of Action An alkylating agent that alters DNA replication, RNA transcription, and nucleic acid formation, resulting in cell death. The currently available sensitive analytical methods for thioTEPA and its metabolites can be used to elucidate the many questions that still exist even so many years after its introduction. What is the mechanism of action? One of the principal bond disruptions is initiated by alkylation of guanine at the N-7 position, which severs the linkage between the purine base and the sugar and liberates alkylated guanines. Pharmacokinetics. Indications Carcinoma of the bladder, ovaries, and breast; brain tumors; Hodgkin's disease; non-Hodgkin's lymphoma; lymphosarcoma; malignant effusions. Advise females of reproductive potential to avoid pregnancy while taking thiotepa. One of the principal bond disruptions is initiated by alkylation of guanine at the N-7 position, which severs the linkage between the purine base and the sugar and liberates alkylated guanines. It is also immunosupressive. Indications Carcinoma of the bladder, ovaries, and breast; brain tumors; Hodgkin's disease; non-Hodgkin's lymphoma; lymphosarcoma; malignant effusions. Mechanism Of Action. ... What are the possible late side effects of treatment with thiotepa? Alkylation takes place through the formation of a highly reactive ethylenimine radical. The aziridine ring opens after protonation of the ring nitrogen. Thiotepa belongs to a class of drugs called alkylating agents. How is thiotepa … ♦Thiotepa (thy-oh-tep'-ah) Triethylene, Thio-Tepa, TESPA, TSPA Pregnancy Category D Mechanism of Action An alkylating agent that alters DNA replication, RNA transcription, and nucleic acid formation, resulting in cell death.
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