Anticancer 3 Flashcards
MICROTUBULE INHIBITORS groups and two drugs in each?
VINCA ALKALOIDS
VINCRISTINE
VINBLASTINE
TAXANES
PACLITAXEL
DOCETAXEL
Vinca alkaloids MOA?
Vinca alkaloids bind to β-tubulin and inhibit its
ability to polymerize into microtubules.
• This results in mitotic arrest in metaphase.
• Cell division stops. Cells die by apoptosis.
AE of Vincristine?
Vincristine: Peripheral neuropathy. Bone
marrow depression is mild. Alopecia.
Ae of vinblastine?
Vinblastine: Myelosuppression is the doselimiting
adverse effect. Other adverse effects
include alopecia and peripheral neuropathy
Taxanes MOA?
Taxanes bind to the β-tubulin subunit of
microtubules and promote microtubule
polymerization.
• Stabilization of the microtubules in a polymerized
state arrests cells in mitosis and leads to apoptosis.
AE of Paclitaxel?
Hypersensitivity, myelosuppression, peripheral
neuropathy, alopecia.
• Hypersensitivity is reduced by premedication with
dexamethasone, diphenhydramine and an H2
blocker
Ae of Docetaxel?
Myelosuppression, peripheral neuropathy, fluid
retention, alopecia, mucositis.
• Pretreatment with dexamethasone is required to
prevent fluid retention.
• Docetaxel does not cause neuropathy as
frequently as paclitaxel.
• Myelosuppression is dose-limiting.
EPIPODOPHYLLOTOXINS? MOA?
ETOPOSIDE Inhibits topoisomerase II, resulting in DNA damage through strand breakage. • Blocks cell in late S-G2 phase.
What are the two Captothecans? MOA?
TOPOTECAN IRINOTECAN Inhibit topoisomerase I. Inhibition results in DNA damage.
Prednisone use?
Glucocorticoids are lympholytic and suppress
mitosis in lymphocytes.
• They are used for acute leukemia and malignant
lymphomas.
Three types of estrogen inhibitors?
SELECTIVE ESTROGEN-RECEPTOR MODULATORS (SERMs) SELECTIVE ESTROGEN-RECEPTOR DOWNREGULATORS (SERDs) AROMATASE INHIBITORS (AIs)
Which two are SELECTIVE ESTROGEN-RECEPTOR
MODULATORS(SERMs)?
RALOXIFENE
Tamoxifen
Describe Raloxifene and its uses?
Raloxifene is an antiestrogen in the uterus and
the breast, while promoting estrogenic effects in
the bone to inhibit resorption.
• Used for prevention of postmenopausal
osteoporosis and prophylaxis of breast cancer in
high risk postmenopausal women.
Describe Tamoxifen?
TAMOXIFEN
• SERMs bind to estrogen receptors and act as
agonists or antagonist depending on the tissue.
• Tamoxifen is an antagonist on breast cancer.
• Tamoxifen is an agonist in nonbreast tissues.
• Used for receptor-positive breast cancer.
• Chemopreventive agent in women at risk for
breast cancer.
Describe Fulvestrant?
SERDs are devoid of estrogen agonist activity.
• Fulvestrant binds to the estrogen receptor (ER)
inhibits its dimerization and increases its
degradation.
• ER-mediated transcription is abolished.