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4 Types of DNA Binding Agents |
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Definition
1) Topoisomerase I inhibitor 2) Topoisomerase II inhibitor 3) DNA intercalation 4) DNA cleavage |
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Definition
nuclear enzyme that reduce DNA torsional stress |
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Definition
Bind to DNA through reversible trans-esterification reaction, creating a cleavable complex which relaxes torsional strain
Topoisomerase I inhibitors bind to cleavable complex to stabilize it |
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Definition
Topoisomerase I inhibitor but exhibited severe toxicity |
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Definition
Topoisomerase I inhibitor (Camptothecin derrivative)
Approved for use in colorectal cancer in combination with 5-FU and leucovorin |
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Topoisomerase I inhibitor
Used for ovarian cancer, cervical cancer, and small-cell lung cancer |
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Irinotecan metabolite, its effect and treatment |
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Definition
SN-38
SN-38 reformation in GI= severe diarrhea
St. John's wort reduces SN-38 by induction of cytochrome P450 and P-glycoprotein |
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Definition
Topoisomerase II
Doxorubicin Daunorubicin Idarubicin Valrubicin Epirubicin |
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Definition
Anthracycline (Topo II inhibitor) with broad activity againist a variety of neoplasma |
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Term
Daunorubicin (Daunomycin) |
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Definition
Anthracycline (Topo II inhibitor) used primarily in acute leukemia |
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Definition
Treats urinary bladder cancer |
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Definition
Anthracycline used as adjuvant therapy following primary breast resection |
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Liposomal form of Doxorubicin (Doxil) |
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Definition
For kaposi's sarcoma
Leads to hand-foot syndrome |
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Definition
Dismutation of superoxide produces highly reactive hydroxyl radicals and hydrogen peroxide leading to antitumor action and cardiotoxicity |
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Definition
Unique characteristic of anthracyclines
Chronic form is cumulative dose-related (mortality rate of chronic form is in excess of 50%)
Treat by giving Vitamin E and iron chelator Dexrazoxane (Zinecard) |
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Definition
Approved for treatment of cardiotoxicity and extravasation from anthracyclines |
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Mitoxantrone (Novantrone) |
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Definition
Deep blue anthracenedione derivative
Treats non-lymphocytic leukemias and prostate cancer
Also used in multiple sclerosis |
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Definition
Complex with DNA and topoisomerase II
Etoposide (Vepesid) Teniposide (Vumon) |
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Definition
Podophyllotoxin approved for refractory testicular tumor and small cell lung cancer |
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Definition
Approved fr refractory acute lymhocytic leukemia |
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Definition
Intercalate into DNA between adjacent G-C base pairs of DNA and block transcription of DNA
Dactinomycin (actinomycin) |
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Term
Dactinomycin (Actinomycin-D, Cosmegen) |
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Definition
DNA intercalator used to treat: 1) Rhabdomyosarcoma 2) Wilms' tumor |
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Term
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Definition
DNA cleaver causing DNA scission by interacting with O2 and Fe to generate free radicles
Combination with other drugs in Squamous cell carcinoma
Degraded by belomycin hydrolase: toxicity is often seen if activity is low in skin and lung |
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Definition
1)Pulmonary toxicity (life-threatening) 2) Cutaneous toxicity |
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Definition
1)Pulmonary toxicity (life-threatening) 2) Cutaneous toxicity |
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