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What is the indication for Bisulfan (important to know)?
- Used in combo w/ cyclophosphamide
- For allogenic bone marrow transfers in chronic myelogenous leukemia
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What is the MOA of Bisulfan?
- Cross links DNA
- Like an alkylating agent
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What are the SEs for Bisulfan?
- Bone marrow suppression
- Pulmonary toxicity = fibrosis
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What is the MOA of carmustine (BiCNU)?
- Alyklyates DNA
- Carbamoylates proteins
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What are the side effects of Carmustine (BiCNU)?
- N/V
- Pulmonary fibrosis
- BONE MARROW TOXICITY (thrombocytopenia, leukocytopenia)
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Why can Carmustine be used for Brain Cancer?
- Highly lipophilic
- Crosses the BBB
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What is the route of administration for Carmustine?
IV
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What are the Nitrosureas?
Camustine and Lomustine
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Can Bisulfan penetrate the BBB?
Yes, but Brain cancer is not a normal indication
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What are the side effects of Bidulfan and the Nitrosureas?
- Acute: N/V
- Delayed: Myelosuppression, teratogenic, reproductive organ inhibition, high dose pulmonary toxicity (fibrosis)
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What treatment regimens is Dacarbazine (DTIC-Dome) used in?
CHOP (C) and ABCD (D)
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What is the MOA for Dacarbazine (DTIC-Dome)?
Metabolite is a Non-cell cycle specific alkylating agent
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By what route is Dacarbazine (DTIC-Dome) given?
IV
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How is Dacarbazine (DTIC-Dome) activated?
By liver microsomal enzymes
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What is Dacarbazine (DTIC-Dome) mainly used for?
Melanoma, especially in combo with newer drugs
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What is the MOA for Temozolomide (Temodar)?
- Metabolite acts as a non-cell cycle specific alkylating agent
- (same as Dacarbazine)
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How is Temozolomide (Temodar) administered?
Orally
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What physiological functions need to be competent for Temozolomide (Temodar) to be activated?
Liver microsomal enzymes
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What is the indication for Temozolomide (Temodar) and why?
Lipophilic = brain tumors/cancer
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What is Bendamustine (Treanda) a derivative of?
Mechlorethamine
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What is the MOA of Bendamustine (Treanda)?
Alkylating agent that inhibits mitotic check points ( stops cell from entering mitosis)
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How is Bendamustine (Treanda) administered?
IV
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What are the general indications for Bendamustine (Treanda)?
Lymphoma and Leukemia
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Is Bendamustine (Treanda) a prodrug or active as is?
Prodrug
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Of Decarbazine, bendamustine and temozolamide, which has the longest half life?
Temozolamide
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What are the Platinum coordination complexes (Alkylating-like agents)?
- cisplatin (Platinol)
- oxaliplatin (Eloxatin)
- carboplatin (Paraplatin)
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How are the Platinum coordination complexes (Alkylating-like agents) administered?
IV
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What is the MOA of the platinum coordination complexes?
- Pt- guanine DNA crosslinking
- Inhibit DNA and RNA polymerase
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What is the main indication or Oxaliplatin?
Colorectal cancer
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What two platinum coordination complexes have essentially the same indications?
Carboplatin and Cisplatin
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What general type of cancers are platinum coordination complexes intended for?
Solid tumors
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What is common drug combination with platinum coordination complexes?
- Cisplatin and 5-FU
- Together they penetrate the BB well
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Dose Cisplatin penetrate the BBB well?
No, needs 5-FU to open the membranes for it.
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