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Antineoplastic (Anticancer) Drugs
PHAR450
25
Pharmacology
Undergraduate 4
04/01/2014

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Cards

Term
Ondansteron
Definition
5-HT3 receptor antagonist
Emesis control to reduce host toxicity in chemotherapy
Term
Methotrexate
Definition
Antimetabolite
Folic acid analog, may be poly(glutamylated)
Inhibitor of dihydrofolate reductase (FH4 & purine) & thymidylate synthase (FH2 & thymidine)
Term
Uracil/5-Fluorouracil
Definition
Antimetabolite
Pyrimidine analogue
Used to treat colon cancer & solid tumours of the stomach, breast, liver esophagus, head, neck & anus
Requires bioactivation in the cell
Incorporated into RNA/DNA and interferes with RNA & DNA synthesis & function
Inhibits thymidylate synthase
Term
Cytidine/Deoxycytidine
Definition
Antimetabolite
Pyrimidine analogue
Term
Cytosine arabinoside (AraC)
Definition
Antimetabolite
Pyrimidine analog, S-phase-specific
Inhibits RNA and DNA synthesis after conversion to active drug
Used to treat haematologic malignancies (acute myelogenous leukemia, Non-Hodgkin's lymphoma)
Term
6-Mercaptopurine
Definition
Antimetabolite
Purine analogue
Pro-drug converted to drug forms via HGPRT
Administered with allopurinol to inhibit metabolism
Term
Allopurinol
Definition
Xanthine oxidase inhibitor
Blocks conversion of 6-mercaptopurine (purine analogue) to inactive 6-thiouric acid
Prevents gout & nephrotoxicity caused by excessive uric acid
Term
Cladribine (Leustatin)
Definition
Aantimetabolite
Purine analogue
Specific to lymphoid cells
Term
Fludarabine (Fludara)
Definition
Antimetabolite
Purine analogue
Used to treat low grade Non-Hodgkin's lymphoma & chronic lymphocytic leukemia (CLL)
Term
Vincristine
Definition
Antimicrotubule agent
Inhibits polymerization
Mitotic arrest at M-phase leading to cell death
Used to treat Hodgkins & Non-Hodgkins lymphoma, multiple myeloma, paediactric tumours
Toxicity: syndrome of inappropriate ADH secretion
Term
Vinblastine
Definition
Antimicrotubule agent
Inhibits polymerization
Mitotic arrest at M-phase leading to cell death
Used to treat Hodgkins & Non-Hodgkins lymphoma, breast & germ cell cancer
Toxicity: vesicant (blistering), nausea, vomiting
Term
Paclitaxel (Taxol)
Definition
Antimicrotubule agent
Prevents depolymerization
Mitotic spindle poison via enhanced polymerisation without MAP & GTP
Used to treat ovarian cancer, breast cancer, small cell and non-small cell cancer etc.
Administered with dexamethasone and diphenylhydramine to reduce hypersensitivity reactions
Term
Docetaxel
Definition
Antimicrotubule agent
Prevents depolymerization
Term
Dexamethasone
Definition
Administered with paclitaxil to reduce the incidence of hypersensitivity reactions
Term
Diphenylhydramine
Definition
Administered with paclitaxil to reduce the incidence of hypersensitivity reactions
Term
Cyclophosphamide
Definition
Alkylating agent
Cross-linking DNA, depurination, cleavage of ringed bases, abnormal base pairing
P450 activation is required
Used by Lance Armstrong to treat testicular cancer
Term
Cisplantin
Definition
Alkylating agent
Cures testicular cancer but renal toxicity is a major limitation
Used to treat solid tumours
Term
Carboplantin
Definition
Alkylating agent
Cures testicular cancer but renal toxicity is a major limitation
Used to treat solid tumours
Term
Camptothecin
Definition
Topoisomerase I inhibitor
Stabilizes DNA/Topo I complexes
DNA breaks accumulates & replication is impaired
Term
Doxorubicin (Doxil)
Definition
Topoisomerase II inhibitor
Anthracycline
Cardiotoxicity, myocardial damage may lead to CHF
Term
Etoposide (VP-16)
Definition
Topoisomerase II inhibitor
Causes DNA damage that increases risk of secondary malignancies later in adulthood
Term
Daunorubicin
Definition
Topoisomerase II inhibitor
Anthracycline
Term
Gefitinib
Definition
Targeted non-cytotoxic agent
Inhibits EGF receptor
Used to treat lung cancer
Term
Sorafenib
Definition
Targeted non-cytotoxic agent
Inhibits Ras/Raf kinases & other Tyr kinases
Used to treat renal cell cancer, melanoma
Term
Trastuzumab (Herceptin)
Definition
Targeted non-cytotoxic agent
Inhibits human epidermal growth factor receptor (HER2)
Used to treat breast, gastric, & esophageal cancer
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