-
What are the names of the two ANTITUMOR ANTIBIOTICS?
-
What is the brand name for Doxorubicin?
Adriamycin
-
Doxorubicin - MOA
An anthracycline which can intercalate between base pairs, inhibit topoisomerase II, and generate free radicals, binding to cellular membranes to alter fluidity and ion transport
- • Blocks the synthesis of RNA and DNA
- and causes DNA strand scission.
-
Doxorubicin - CCNS or CCS?
CCNS
-
Doxorubicin – Pharmacokinetics
•Must be given IV.
- •Metabolized in the liver and excreted in
- the urine, imparting to it a red color.
-
Doxorubicin - Clinical use
- Lymphoma,
- sarcoma,
- acute leukemia,
- breast,
- lung,
- testes,
- thyroid,
- and ovary
-
Doxorubicin – Toxicity
- Myelosuppression,
- GI distress,
- and alopecia.
- Unique side effect is cardiotoxicity.
-
Bleomycin - MOA
- acts by binding to DNA, which results in
- single-strand and double-strand breaks following free radical formation, and inhibition of DNA biosynthesis
- Cell cycle-specific drug that causes
- accumulation of cells in the G2 phase of the cell cycle.
-
Bleomycin - Clinical treatment of
- Hodgkin's and non-Hodgkin's lymphomas,
- germ cell tumor,
- head and neck cancer,
- and squamous cell cancer of the skin, cervix, and vulva.
-
Bleomycin - Pharmokinetics
May be given IV, IM, or SQ
-
Bleomycin - Toxicity
pneumonitis
-
Plant Alkaloids are CCS drugs which include?
- vinca alkaloids,
- the podophyllotoxins,
- and the taxenes.
-
Brand name for Vincristine?
Oncovin
-
Vincristine - MOA
A spindle poison derived from the periwinkle plant. Prevents the assembly of tubulin dimers into microtubules, and blocks the formation of the mitotic spindle.
Acts on the M phase of the cell cycle
-
Vincristine – Resistance
occurs as a result of increased efflux from the cell by a transporter molecule.
-
Vincristine – Pharmacokinetics
- Given IV.
- Good tissue penetration except into the CSF.
- Cleared mainly by biliary excretion
-
Vincristine - Clinical use
- Lymphoma,
- Hodgkin’s disease,
- Wilm’s tumor,
- childhood acute leukemia
-
Vincristine – Toxicity
- GI distress,
- alopecia,
- myelosuppression,
- Peripheral neuropathy.
-
What type of plant alkaloid is Etoposide?
- a podophyllotoxin
- derived from the May apple plant
-
Etoposide - MOA
- Interacts with Topoisomerase II to increase the degradation of DNA.
- - Most active in the late S and early G2 phases.
-
Etoposide – Pharmacokinetics
- Good oral absorption,
- eliminated via the kidney
-
Etoposide – Toxicity
- GI,
- alopecia,
- myelosuppression
-
Etoposide - Clinical use
- treat germ cell cancers,
- small cell and non-small cell lung cancers,
- Hodgkin’s and non-Hodgkin’s lymphomas,
- and gastric cancer.
-
Brand name for Paclitaxel?
Taxol
-
Paclitaxel - What type of plant alkaloid is it?
- A taxane derived from the Pacific yew tree.
-
Paclitaxel - MOA
- Mitotic spindle poison,
- M phase specific
•given IV
-
Paclitaxel - Clinical use
Breast and ovarian cancer
-
Paclitaxel – Toxicity
- Myelosuppression,
- neuropathy,
- and hypersensitivity reactions
-
What are SERM’s?
SERM’s are mixed estrogen agonists that act as antagonists in certain tissues
-
Name two hormones used in the treatment of cancer.
- Prednisone,
- Tamoxifen (Nolvadex)
-
Prednisone is used to treat?
- acute leukemia,
- Hodgkin’s disease,
- and lymphoma
-
Brand name for Tamoxifen?
Nolvadex
-
Tamoxifen - MOA
- Selective Estrogen Receptor Modifier
- (SERM) which blocks the binding of estrogen to receptors of estrogen-sensitive cancer cells in breast tissue.
- acts as an antagonist in hormone-responsive breast cancers where it prevents receptor activation by endogenous estrogen.
-
Tamoxifen - Clinical use
- Used in the treatment of receptor-positive breast cancers and may help prevent cancer in high risk women.
- has more agonist than antagonist action on bone and thus helps to prevent osteoporosis.
-
Tamoxifen - Toxicity
- nausea,
- vomiting,
- hot flushes,
- vaginal bleeding,
- hypercalcemia,
- and peripheral edema.
-
Interferon alfa-2 - MOA
- Made by lymphocytes,
- inhibits cell proliferation,
-
Interferon alfa-2 - Clinical use
- hairy cell leukemia,
- Kaposi’s sarcoma,
- and hepatitis.
-
Interferon alfa-2 - Side effects
- –Causes flu-like symptoms,
- fatigue,
- depression,
- NVD
-
Imatinib - MOA
- the first member of a new class of drugs that act by specifically inhibiting an enzyme that is characteristic of a cancer cell rather than non-specifically killing all rapidly dividing cells.
- inhibitor of the tyrosine kinase domain of the Bcr-Abl oncoprotein
-
Imatinib - Clinical use
Indication - chronic myelogenous leukemia (CML),
- - Given orally,
- - Metabolized by CYP3A4
-
What does EGFR stand for?
Epidermal growth factor receptor
-
What is the anticancer drug classified as an
Epidermal growth factor receptor inhibitor?
Cetuximab
-
Cetuximab - Clinical use
metastatic colon cancer
-
Cetuximab - Toxicity
- Acneiform skin rash,
- hypersensitivity,
- and hypomagnesemia
-
What does VEGF stand for?
vascular endothelial growth factor
- - (VEGF) is one of the most important angiogenic growth factors. The growth of both primary and metastatic tumors requires an
- intact vasculature. As a result, the VEGF-signaling pathway represents an
- attractive target for chemotherapy.
-
Bevacizumab - MOA
- Bevacizumab is a recombinant humanized monoclonal antibody that targets all forms of VEGF-A.
- This antibody binds to and prevents VEGF-A from interacting with the target VEGF receptors.
-
Bevacizumab - Clinical use
- can be safely and effectively combined with 5-FU-, irinotecan-, and oxaliplatin-based chemotherapy
- - in the treatment of
- metastatic colorectal cancer.
-
Name 3 drugs used to treat renal cell cancer.
- Sorafenib,
- Sunitinib,
- Pazopanib
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