Anticancer 3 Flashcards

1
Q

MICROTUBULE INHIBITORS groups and two drugs in each?

A

VINCA ALKALOIDS
VINCRISTINE
VINBLASTINE

TAXANES
PACLITAXEL
DOCETAXEL

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2
Q

Vinca alkaloids MOA?

A

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.

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3
Q

AE of Vincristine?

A

Vincristine: Peripheral neuropathy. Bone

marrow depression is mild. Alopecia.

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4
Q

Ae of vinblastine?

A

Vinblastine: Myelosuppression is the doselimiting
adverse effect. Other adverse effects
include alopecia and peripheral neuropathy

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5
Q

Taxanes MOA?

A

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.

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6
Q

AE of Paclitaxel?

A

Hypersensitivity, myelosuppression, peripheral
neuropathy, alopecia.
• Hypersensitivity is reduced by premedication with
dexamethasone, diphenhydramine and an H2
blocker

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7
Q

Ae of Docetaxel?

A

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.

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8
Q

EPIPODOPHYLLOTOXINS? MOA?

A
ETOPOSIDE
Inhibits topoisomerase II,
resulting in DNA damage
through strand breakage.
• Blocks cell in late S-G2 phase.
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9
Q

What are the two Captothecans? MOA?

A
TOPOTECAN
IRINOTECAN
Inhibit topoisomerase I.
Inhibition results in DNA
damage.
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10
Q

Prednisone use?

A

Glucocorticoids are lympholytic and suppress
mitosis in lymphocytes.
• They are used for acute leukemia and malignant
lymphomas.

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11
Q

Three types of estrogen inhibitors?

A
SELECTIVE ESTROGEN-RECEPTOR
MODULATORS (SERMs)
SELECTIVE ESTROGEN-RECEPTOR
DOWNREGULATORS (SERDs)
AROMATASE INHIBITORS (AIs)
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12
Q

Which two are SELECTIVE ESTROGEN-RECEPTOR

MODULATORS(SERMs)?

A

RALOXIFENE

Tamoxifen

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13
Q

Describe Raloxifene and its uses?

A

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.

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14
Q

Describe Tamoxifen?

A

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.

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15
Q

Describe Fulvestrant?

A

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.

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16
Q

Describe aromatase inhibitors?

A

Aromatase converts androstenedione to estrone.
• In postmenopausal women, this conversion is
the primary source of circulating estrogens.
• Aromatase inhibitors are the standard of care for
adjuvant treatment of postmenopausal women
with hormone receptor–positive breast cancer.

17
Q

Nonsteroidal and Reversible competitive inhibitors of aromatase?

A

ANASTROZOLE & LETROZOLE

18
Q

Steroidal and Irreversible inhibitor of aromatase?

A

EXEMESTANE

19
Q

ANDROGEN INHIBITORS subgroups?

A

GONADOTROPIN-RELEASING
HORMONE AGONISTS
ANDROGEN RECEPTOR BLOCKERS

20
Q

Preferred approach to prostate cancer?

A

use of GnRH agonists,
alone or in combination with an androgen
receptor blocker.

21
Q

Which two are gonadotropin releasing hormone agonists?

A

GOSERELIN

LEUPROLIDE

22
Q

Describe gonadotropin releasing hormone agonists?

A

When given continuously or as a depot, GnRH
agonists cause an initial surge in LH and FSH
levels, followed by inhibition of gonadotropin
release.
• Testosterone levels fall to 10% of their initial
values after a month.
• The initial surge can be counteracted by
concurrent administration of flutamide for 2-4
weeks.

23
Q

Describe Flutamide?

A

Synthetic, nonsteroidal antiandrogen.
• Metabolized to an active metabolite that acts as a
competitive antagonist at the androgen receptor,
preventing its translocation to the nucleus.

24
Q

Inhibitor of EDFR tyrosine kinase solely?

A

Gefitnib and Erlotinib

25
Q

Inhibitor of trysosine kinase BCr-abl

A

Imatinib

26
Q

Lapatinib inhibits?

A

Inhibitor of EGFR and ErbB2 tyrosine kinases.

27
Q

Trastuzumab acts against?

A

Monoclonal antibody against ErbB2.

28
Q

Asparginase MOA?

A
Most normal tissues synthesize
L-asparagine in amounts
sufficient for protein synthesis.
• Certain neoplastic tissues,
however, require exogenous
source.
• Asparaginase hydrolyzes serum
asparagine, depriving these cells
of the asparagine necessary for
protein synthesis, leading to cell
death.
29
Q

Ae of Asparaginase?

A
• Hypersensitivity.
• Decrease in clotting factors.
• Liver abnormalities.
• Pancreatitis, seizures, coma due to ammonia
toxicity.
30
Q

Describe Hydroxyurea?

A
Inhibits ribonucleotide reductase.
• This leads to depletion of deoxynucleoside
trisphosphate pools.
• DNA synthesis is thereby inhibited.
• Kills cells in S phase.
• Given orally.
31
Q

What is interferon gamma used for?

A

Approved for hairy cell leukemia, chronic
myelogenous leukemia (CML), malignant
melanoma and Kaposi’s sarcoma.

32
Q

AE of Interferon Gamma?

A

Depression.
• Fever with chills.
• Leukopenia, thrombocytopenia. Fatigue, malaise, anorexia, weight loss, alopecia,
transient elevation of liver enzymes.

33
Q

Uses for Hydroxyurea?

A

Used for melanoma, chronic myelocytic leukemia, and carcinoma of the ovary.
• Hydroxyurea used concomitantly with irradiation therapy is used for carcinomas of the
head and neck.
• Hydroxyurea is also approved for use in the treatment of adult sickle cell disease.