CHEMOTHERAPY OF NEOPLASTIC DISEASES 3 Flashcards
Who are the vinca alkaloids and what do they do
Vincristine
Vinblastine
- Destabilizing agents.
- 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.
Adverse effects of vincristine
- Peripheral neuropathy.*****
- Bone marrow depression is mild.
- Alopecia.
Adverse effects of vinblastine
• Myelosuppression is the dose-limiting
adverse effect.*****
• Peripheral neuropathy
• Alopecia
Example of a taxane and its MOA
Paclitaxel
- Stabilizing agent.
- 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.
TAXANES: ADVERSE EFFECTS
• Hypersensitivity, myelosuppression, peripheral neuropathy, alopecia.
How to reduce hypersensitivity from taxane
by premedication with dexamethasone, diphenhydramine and an H2 blocker
EPIPODOPHYLLOTOXINS:
ETOPOSIDE MOA
Inhibits topoisomerase II, resulting in DNA damage through strand breakage.
Blocks cell in late S-G2 phase
What are the adverse effects of etoposide
- Nausea, vomiting, alopecia.
* Myelosuppression.
Which drugs are camptothecins and what is their MOA
TOPOTECAN
IRINOTECAN
Inhibit topoisomerase I. Inhibition results in DNA damage.
Adverse effects of camptothecins
Myelosuppression and diarrhea
Which glucocorticoid is used and what is it used for
PREDNISONE
• Glucocorticoids are lympholytic and suppress mitosis in lymphocytes.
• They are used for acute leukemia and malignant lymphomas.
Who are the estrogen inhibitors
- SELECTIVE ESTROGEN-RECEPTOR MODULATORS (SERMs)
- ESTROGEN-RECEPTOR ANTAGONISTS
- AROMATASE INHIBITORS (AIs)
Who are your SERMS AND what do they do
TAMOXIFEN
RALOXIFENE
• SERMs bind to estrogen receptors and act as agonists or antagonists depending on the tissue.
What is tamoxifen used for
- Metastatic breast cancer in women and men.
* Preventive agent in women at risk for breast cancer.
- Tamoxifen is an ____________ on breast tissue.
* Tamoxifen is an ____________ in nonbreast tissues.
- Tamoxifen is an antagonist on breast tissue.
* Tamoxifen is an agonist in nonbreast tissues.
ADVERSE EFFECTS of tamoxifen
- Hot flashes. Nausea. Vomiting. Fluid retention.
- Vaginal bleeding.
- Venous thromboembolism.
- Increases incidence of endometrial cancer**
Tamoxifen is metabolized by CYP2D6 so it needs to stay away from Strong inhibitors of CYP2D6. Or else there would be accumulation . Who are Strong Inhibitors of CYP2D6?
Bupropion Fluoxetine Paroxetine
What is raloxifene used for ?
- Prophylaxis of breast cancer in high-risk postmenopausal women. (Anti estrogen effect)
- Treatment and prevention of osteoporosis in postmenopausal women. (Estrogenic effect)
Adverse effects of raloxefine
- Hot flashes.
- Leg cramps.
- Venous thromboembolism.
Who is the estrogen antagonist
FULVESTRANT
• Fulvestrant is devoid of estrogen agonist activity.
• Fulvestrant binds to the estrogen receptor (ER) inhibits its dimerization and increases its degradation.
• ER-mediated transcription is abolished.
Which drug is the Treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following antiestrogen therapy.
FULVESTRANT
• Aromatase converts ______ to estrone.
• Aromatase converts androstenedione to estrone.
Uses of aromatase inhibitors
the standard of care for adjuvant treatment of postmenopausal women with hormone receptor–positive breast cancer.
Who are the non steroidal aromatase inhibitors
ANASTROZOLE & LETROZOLE
• Nonsteroidal.
• Reversible competitive inhibitors of aromatase.
