Anti-Neoplastic Drugs (Pb&t)

Front 1

Drug Name: Taxanes (Paclitaxel and docetaxel)
Where applicable list:

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Back 1

USES: Anticancer (esp solid tumors)
MECHANISM: Inhibits microtubule Depolymerization. Binds to inside of microtubules. M-phase specific
SIDE EFFECTS: Periph neuropathy. Hypersensitivity
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OTHER: Originally isolated from Yew tree

Front 2

Drug Name: Thioguanine
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Back 2

USES: Acute myelocytic leukemia
MECHANISM: Antimetabolite similar to 6-mercaptopurine. Inhibits purine synthesis via HGPRT.
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OTHER:

Front 3

Drug Name: Pentostatin
Where applicable list:

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Back 3

USES: Anticancer
MECHANISM: Antimetabolite. Inhibits ADA (required for purine synthesis) Leads to feedback inhibition
SIDE EFFECTS:
TOXICITY: Lethal to lymphocytes
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OTHER:

Front 4

Drug Name: Hydroxyurea
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Back 4

USES: Myelogenous leukemia
MECHANISM: Inhibits ribonucleotide reductase.
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OTHER: Used for sickle cell disease. No longer a first line drug for cancer

Front 5

Drug Name: Cladribine
Where applicable list:

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Back 5

USES: Anticancer, hairy cell leukemia
MECHANISM: Analogue incorporated into DNA. Chlorinated purine
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OTHER:

Front 6

Drug Name: Fludarabine
Where applicable list:

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Back 6

USES: Anticancer - lympho-proliferative disorders
MECHANISM: Analogue incorporated into DNA. Fluorinated purine analogue
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OTHER:

Front 7

Drug Name: 5-Azacytidine
Where applicable list:

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Back 7

USES: Investigational for leukemias, lymphoma
MECHANISM: Analogue incorporated into DNA. Cytidine analogue.
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OTHER:

Front 8

Drug Name: Cytosine Arabinoside (ARA C)
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Back 8

USES: Acute myelogenous Leukemia
MECHANISM: Analogue incorporated into DNA. Cytidine analogue competes for CTP incorporation and causes chain termination.
SIDE EFFECTS:
TOXICITY: VERY myelotoxic. (Limits its use)
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OTHER: Also potent inhibitor of DNA polymerase

Front 9

Drug Name: Alkylating agents (Cyclophasphamide)
Where applicable list:

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Back 9

USES: Anticancer, immunosuppressive
MECHANISM: Polyfunctional Alkylating agent leads to DNA damage, blockage of replication fork.
SIDE EFFECTS:
TOXICITY: Can cause tissue damage if given orally. Bladder damage. Secondary neoplasms.
ANTIDOTES: Mesna to stop bladder damage
CONTRAINDICATIONS: Teratogenic
INTERACTIONS:
OTHER: Cyclophosphamide is a pro-drug oxidized by P450 to become active. Also used as immunosuppressive

Front 10

Drug Name: Platinum agents (Cisplatin)
Where applicable list:

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Back 10

USES: Anticancer (esp testicular cancer)
MECHANISM: Act similar to bis-alkylating agents by binding multiple sites. (Cross-link DNA)
SIDE EFFECTS:
TOXICITY: Nephrotoxic (renal failure)
ANTIDOTES: Co-administer with Diuretic to dilute drug in nephron
CONTRAINDICATIONS:
INTERACTIONS: Synergy w/ Vinblastine/Bleomycin. Cisplatin can draw non-dividing cells into cell cycle, where they can then be killed by the other agents
OTHER:

Front 11

Drug Name: Bleomycin
Where applicable list:

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Back 11

USES: Myelotoxicity (in combo with other agents)
MECHANISM: Binds to DNA and iron causing dysfunction
SIDE EFFECTS:
TOXICITY: Moderate myelotoxicity. Pulmonary fibrosis (porportional to total dose)
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OTHER: Antibiotic from streptomyces

Front 12

Drug Name: Anthracyclines (Doxorbucin & Daunorbucin)
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Back 12

USES: Anticancer
MECHANISM: Interferes with topo II leading to free radical reaction. Causes DNA strand breaks
SIDE EFFECTS: Toxicity at injection site
TOXICITY: CHF (damage is electrically silent)
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CONTRAINDICATIONS: CHF patients
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OTHER:

Front 13

Drug Name: Epipopdophyllotoxins and Amascrine
Where applicable list:

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Back 13

USES: Drug resistant metastic ovarian and small cell lung cancer
MECHANISM: Inhibit topo II religation step, causing double strand breaks. DNA dysfunction during Mitosis.
SIDE EFFECTS:
TOXICITY: Very toxic! GI toxicity (incl lethal diarrhea); marrow toxicity.
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INTERACTIONS: Synergy when used with Cisplatin, bleomycin and etopside for testicular cancer
OTHER: Amsacrine intercalates DNA.

Front 14

Drug Name: Colchicine
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Back 14

USES: Anticancer
MECHANISM: Inhibits microtubule polymerization. Binds to interface btw alpha and beta tubulin leading to microtubule assemply. M phase specific
SIDE EFFECTS: Peripheral neuropathy due to anti-tubule action. Tremors, ataxia, parasthesias
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OTHER:

Front 15

Drug Name: Vinca alkaloids (vincristine, vinblastine)
Where applicable list:

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Back 15

USES: Anticancer
MECHANISM: Inhibits microtubule polymerization. Bind to plus ends of microtubule. M phase specific
SIDE EFFECTS: Peripheral neuropathy due to anti-tubule action. Tremors, ataxia, parasthesias
TOXICITY:
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CONTRAINDICATIONS:
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OTHER: Vincristine much less myelo-suppressive than vinblastine

Front 16

Drug Name: Methotrexate
Where applicable list:

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Back 16

USES: Antimetabolite
MECHANISM: Antagonist to DHFR (enz reduces DHF to THF). THF needed for dUMP->dTMP and purine synthesis.
SIDE EFFECTS:
TOXICITY: Dividing stem cell tox, hepatic fibrosis, cirrhosis
ANTIDOTES: Folinic acid ("Leukovorin)
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Also an immunosuppressive

Front 17

Drug Name: 5-Fluorouracil
Where applicable list:

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Back 17

USES: Breast, colon, skin cancer
MECHANISM: Antimetabolite. Inhibits Thymidylate synthase (dUMP->dTMP)
SIDE EFFECTS:
TOXICITY: Very toxic against normal stem cells
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OTHER: Also an immunosuppressive

Front 18

Drug Name: 6-Mercaptopurine
Where applicable list:

Therapeutic Uses:
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Back 18

USES: Anticancer
MECHANISM: Antimetabolite. Inhibits purine synthesis. Antagonist to HGPRT (salvage pathway)
SIDE EFFECTS:
TOXICITY: May lead to increase in purines (gout)
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS: Allopurinol. Both drugs degraded by xanthine oxidase. Thus coadmin can lead to toxic amts of 6-MP
OTHER: Also an immunosuppressive via Azathioprine