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Who published the first edition of the Pharmacological Basis of Therapeutics in 1940? |
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Definition
Louis Goodman and Alfred Gilman |
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When cancer cells fail to respond to molecular signals (either from within or without) that control the rate of cell growth. Therefore due to genetic mutations, the cell undergoes uncontrolled growth. |
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Many types of mutations in a cell will cause the cell to undergo programmed cell death know as ____________ |
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Cancer cells learn how to evade the normal cell's mechanisms of apoptosis and therefore become ________ |
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Definition
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As cancer cells grow they continue to ____________ |
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Definition
Proliferate without limit |
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Cancer cells have the capacity to cause formation of new blood vessels. What is this process called? |
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Cancer cells have the ability to avoid detection by the ____________ |
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The most feared characteristics of cancer cells is their ability to break loose from their site of origin and become implanted in other tissues. |
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What is the major target for alkylating agents? |
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What was the first chemical agent used to treat cancer. (hint: used in combat during WWI) |
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In WW2, a US ship carrying over 2000 mustard gas bombs exploded in a harbour in what location? |
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Definition
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Term
What is the name and year of the first drug used for chemotherapy of cancer? |
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Definition
Mechlorethamine (Mustargen) |
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Term
What does mustard gas look like? |
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Definition
Two chloroethyl groups each attached to a central sulfur atom |
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Term
_____________ acts as an alkylating agent through the intermediacy of the highly reactive three-membered aziridinium ion |
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Definition
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Term
Most alkylating agents are chemically reactive and do not tend to target any one phase of the cell cycle; therefore often described as ____________ |
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Definition
Cell cycle non-specific drugs |
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Term
Because they react with and damage DNA, nitrogen mustards are ______________ |
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Definition
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Term
Mechlorethamine is very reactive and toxic. This drug must be administered carefully because it can cause _____________ |
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Definition
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Term
______________ is the recommended antidote for treating mechlorethamine extravasation |
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Definition
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Term
The addition of a benzene ring acts as an ___________________ to reduce the nucleophilicty of the nitrogen atom |
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Definition
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Term
What are the names of the less reactive mustards that can be used orally? |
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Definition
Chlorambucil and Melphalan (phenylalanine mustard) |
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Term
What is the most useful mustard? |
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Definition
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Term
The six-membered ring of cyclophosphamide is oxidized by __________________ |
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Definition
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Term
________ is a metabolite from cyclophosphamide and is responsible for potentially fatal adverse reaction known as _____________ |
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Definition
Acrolein
Hemorrhagic cystitis |
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Term
What is the name of cyclophosphamide's isomer? |
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Definition
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Term
Hemorrhagic cystitis can be treated or prevented by adequate hydration of the patient and by administration of ________________ or _________________ |
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Definition
Mesna (sodium 2-mercaptoethane sulfonate)
N-acetylcysteine |
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Term
What are the two members of the "nitrosourea" class? |
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Definition
Carmustine (BCNU, Gliadel) Lomustine (CCNU) |
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Term
Because the nitrosourea compounds are highly _________________ they are able to easily cross the ____________ and are important agents for the treatment of _______ tumors |
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Definition
Lipophilic Blood brain barrier Brain |
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Term
Which drug is an impregnated biodegradable wafer for direct application to residual tumor tissue following surgery to remove a brain tumor? |
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Definition
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Term
Which drug is closely related to carmustine and lomustine and is a naturally occuring antibiotic indicated for the treatment of islet cell carcinoma (insulinoma)? |
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Definition
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Term
The nitrosoureas undergo spontaneous degradation, and cause interstrand and/or intrastrand _______________ |
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Definition
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Term
Which DNA repair enzyme can remove the adduct formed from nitrosoureas before DNA replication occurs? |
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Definition
Guanine O6-alkyl transferase |
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Term
The triazenes are characterized by having 3 contiguous nitrogen atoms; which two drugs belong in this group? |
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Definition
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Term
Dacarbazine MOA is to act by conversion to ____________ with release of the powerful methylating agent ________________ |
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Definition
AIC (purine precursor) Diazomethane (CH2N2) |
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Term
What drug is rapidly absorbed when given orally and readily crosses the blood brain barrier and is the standard drug in the treatment of gliomas in combination with radiation. |
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The discovery of anticancer activity of platinum coordination complexes is attributed to what university? |
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What is the first platinum coordination complex anticancer drug? |
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Definition
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Term
What is the process called where chlorine atoms of cisplatin are displaced by water? |
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Definition
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Reaction of cisplatin with DNA produces both _____ and ______ strand crosslinks |
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Definition
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Term
This platinum anticancer drug is only approved in advanced ovarian cancer |
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Definition
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Cisplatin causes severe __________; which can be diminished by ____________ pretreatment. |
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This drug is used in combo with fluorouracil and leucovorin for the treatment of colorectal cancer. |
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Definition
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Term
Which drug produces unique cold induced neuropathies? |
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Definition
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This drug is a cytoprotective drug that is used to reduce renal toxicity associated with cisplatin use. |
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Definition
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Term
This drug was first discovered as an antibiotic and contains an aziridine ring and a quinone group |
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Definition
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Term
This drug was a hydrazine derivative that was first used as a monoamine oxidase inhibitor |
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