Term
| What are the major classes of chemotherapeutic drugs? |
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Definition
1) DNA reactive drugs
2) Topoisomerase I/II inhibitors
3) Antimetabolites
4) Tubulin binders |
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Term
| How do DNA reactive drugs work? |
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Definition
| They are bifunctional alkylating agents. They possess reactive chloride ions which act to cross-link the DNA and prevent proliferation. |
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Term
| Name 5 common bifunctional alkylating agents. |
|
Definition
1) Bischloroethylamine
2) Chlorambucil
3) Melphalan (oral or iv)
4) Cyclophosphamide (requires metabolic activation)
5) Busulphan (strongly myelosuppressive). |
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Term
| What are bifunctional alkylating agents used for? |
|
Definition
| Treatment of lymphomas, breast cancer, ovarian cancer and sarcomas. |
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Term
|
Definition
| Forms DNA cross links intra and inter strand. |
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Term
| What are the side effects of cisplatin? |
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Definition
1) Nausea and vomiting for several days
2) Impairment of renal function
3) Peripheral neuropathy
4) High tone deafness
5) Urinary magnesium loss leading to convulsions. |
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Term
|
Definition
| An analogue of cisplatin but with less toxicity. |
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Term
| What is the difference between topoisomerase I and II? |
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Definition
| Topoisomerase II causes double strand breaks and acts to relieve supercoiling. Topoisomerase I causes single strand breaks to relieve torsion. |
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Term
| What is the major side effect of anthracyclines? |
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Definition
|
|
Term
| How does doxorubicin (adriamycin) work? |
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Definition
| Intercalates DNA and causes fragmentation due to topoisomerase inhibition. |
|
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Term
| How do topotecan and irinotecan work? |
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Definition
| They inhibit topoisomerase I. |
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Term
| How does methotrexate work? |
|
Definition
| Inhibits dihydrofolate reductase (DHFR) which prevents thymidine and purine synthesis which prevents DNA and RNA formation. |
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Term
| How does 5-fluoracil work? |
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Definition
| Inhibits thymidilate synthase. |
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Term
| How do taxanes and vincristine work? |
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Definition
| Stabilise tubulin in the cellular matrix: antimitotic. |
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Term
| Which protein is involved with multidrug resistance? |
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Definition
| p-glycoprotein. It pumps out a lot of chemotherapy agents from the cell. |
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