Chemo Rx 2 Flashcards
List the sub-classes of the mitotic inhibitor class of chemo rx.
- vinka alkaloids
- -“taxanes”
Mitotic inhibitors are _____ (CCS/CCNS).
CCS → halt the M phase
Vinblastine is the most _______ (AE); Vincristine is the most ______(AE)
- myelosuppressive
- neurotoxic
(mn: Vinblastine BLASTS the bones; Vincristine CRISps the nerves”)
Mechanism of resistance to the mitotic inhibitors is via P-glycoprotein. Which mechanisms are specific to vinka alkaloids? “-taxanes”?
vinka: increase Rx efflux
“-taxanes”: mutate B-tubulin
The mitotic inhibitors halt M phase by targeting microtubules, how are the vinka alkaloids and the taxanes different in their MOA?
- vinka: inhibits tubulin polymerization
- taxanes: promote b-tubulin formation
(mn: “No Assemblies allowed in the vineyard; Taxes are Stable.”)
Which Taxane targets solid tumors? Which target non-small cell, head, neck, ovarian, bladder and breast?
- paclitaxel
- docetaxel
_______ (vinka alkaloid) targets lymphoma (hodgkins & NHL), breast and testicular cancer.
vinblastine
(most myelosuppressive)
_______ (vinka alkaloid) targets ALL, Hodgkin, leukemia & Wilms tumor?
Vincristine
(most neurotoxic)
Vinorelbine targets ______ (cancer)
solid tumors
(non-small cell lung, breast)
AE of the Taxanes (2)
- Myelosuppression
- hypersensitivity reaction (pre-treat w/corticosteroids & antihistamines)
(Docetaxel → neurotoxicity)
List the 2 sub-classes of the Topoisomerase Inhibitors (reduce supercoiling of DNA)
- Camptothecins
- Podophyllotoxins
(inhibiting the S phase)
What is the difference in the MOA between the Camptothecins and the Podophyllotoxins?
- camptothecin inhibits topoisomerase I
- podophyllotoxin inhibits topoisomerase II
(both cause strand to break from ⇣ supercoiling)
Which camptothecin treats metastatic colorectal cancer? Which treats ovarian?
- Irinotecan: colorectal
- Topotecan: ovarian
Which camptothecin has severe diarrhea as an adverse effect in addition to N/V & alopecia?
Irinotecan
(tx: metastatic colorectal CA)
Which of the topoisomerase inhibitors needs a dosage adjustment for renal dysfunction?
Etoposide (podophyllotoxin sub-class)
(tx: Lung CA & Lymphomas)
Which podophyllotoxin (sub-class of topoisomerase inhibitors) treats Lung CA & lymphoma? Which treats Acute Leukemia?
- Etoposide: Lung & Lymphoma
- Teniposide: Acute Leukemia
Which of the Antitumor ABX is CCS?
Bleomycin
(the other antitumor ABX are CCNS)
List the 3 anthracyclines (sub-class of antitumor ABX)
- Doxorubicin
- Daunorubicin
- Mitoxantrone
Doxorubicin & Mitoxantrone target solid tumors, specifically _____.
breast cancer
Which anthracyclines both treat AML?
- Daunorubicin
- Mitoxantrone
Doxorubicin treats breast cancer and _____.
(mitoxantrone tx breast CA also)
leukemia/lymphoma
Mitoxantrone treats breast CA, and ______(4).
- prostate
- AML
- NHL
- GE
Which antitumor ABX treats HL, testicular, head, neck and skin CA?
Bleomycin
(AE: pulmonary fibrosis & mucocutaneous rxn)
Which 3 Antitumor ABX impair topoisomerase II & generate free radicals to inhibit RNA & DNA synthesis?
- Doxorubicin
- Mitoxantrone
- Daunorubicin
(anthracyclines)
_______ MOA = reaction w/O2→ superoxide hydroxyl radical
bleomycin
(tx: HL, testicular, head, neck & skin CA)
Mechanism of resistance to bleomycin
- increase bleomycin hydrolase
- ⇡ DNA repair
Side effect of ______ is red urine
mitoxantrone
(least cardiotoxic)
Mucocutaneous reaction and pulmonary fibrosis are side effects of _______
bleomycin
(similar to Hand-foot syndrome - AE of Capecitabine)
_______ is the MC acute dose-limiting toxicity of the anthracyclines (subclass of topoisomerase inhibitors)
Myelosuppression
Prednisone is converted to prednisolone by _______.
11-B-HSD
Prednisone is used to treat ______(2 types CA)
- Acute leukemia (ALL)
- Lymphoma (HL & NHL)
______ causes lymphocytopenia & decreases lymphoid mass.
Prednisone
Which hormonal agent is a SERM (selective estrogen receptor modulator) which inhibits RNA synthesis
Tamoxifen
Menopausal sx & endometrial cancer are potential AE of _____. Hot flashes & arthralgia are side effects of ______-
- tamoxifen
- aromatase inhibitors (anastrozole, letrozole, exemestane)
(tx: breast CA)
Which 2 hormonal agents subclasses treat breast cancer?
- Estrogen receptor Antagonist (SERM)
- Aromatase
List the 3 Aromatase inhibitors used to treat breast cancer.
(block conversion of testosterone→estrogen)
- Anastrozole
- Letrozole
- Exemestane
List the 3 Androgen receptor antagonists (DHT)
- Flutamide
- Bicalutamide
- Enzalutamide
List the 2 GnRH agonists
Which 2 subclasses of hormonal agents treat prostate cancer?
- GnRH agonists
- Androgen receptor (DHT) antagonists
________ treats resistant prostate cancer (metastatic castration)
Enzalutamide
______ (subclass of hormonal agents) cause a surge in LH & FSH followed by inhibition.
GnRH agonists
Impotence and gynecomastia are side effects of _____ (subclass of hormonal agents)
GnRH agonists
List the 2 protease inhibitors (chemo Rx)
- Bortezomib
- Carfilzomib
(“-zomib”)
Bortezomib & Carfilzomib inhibit _____ → apoptosis
Proteasome
_______ treats Multiple Myeloma
Bortezomib & Carfilzomib
(“Bart proteasomal inhibitor zombie”)
Which 2 classes of chemo Rx causes peripheral neuropathy, thrombocytopenia and heart failure?
- Proteasome inhibitors (bortezomib & carfilzomib)
- Taxanes
(Vincristine (Vinka alkaloid), also)
Which 2 chemo medications are contraindicated which CYP3A4 inhibitors (including grapefruit juice)?
- Nilotinib
- Proteasome inhibitors (Bortezomib, Carfilzomib)
List 4 monoclonal Ab used to treat cancer
- Bevacizumab
- Cetuximab
- Rituximab
- Trastuzumab
_____ (mAb) treats CLL & lymphoma
Rituximab
_______ is an Anti-CD20 mAb and may cause a hypersensitivity reaction.
Rituximab
(causes complement activation)
_______ is a HER2 growth receptor inhibitor → ADCC. Side effect: CHF.
Trastuzumab
______ is mAb that treats metastatic colorectal cancer and is a VEGF inhibitor.
Bevacizumab
Bevacizumab side effects (5)
- delayed wound healing
- thrombosis
- GI perforation
- proteinuria
- HTN
_____ is used to treat metastatic colorectal cancer, and cancers of the head/neck. Acneiform rash is an indication of efficacy.
Cetuximab
(MOA: epidermal growth factor inhibitor)
Cetuximab is a ______ inhibitor
epidermal growth factor
______ is a side effect of the monoclonal Ab class of chemo Rxs.
tumor lysis syndrome → cytokine release causes fever/chills and hypotension
(may be fatal if w/o intervention)
_______ is a tyrosine kinase inhibitor and is a second line therapy for CML.
Nilotinib
_______ is contraindicated in patients who have a long QT, hypomagnesemia, or hypoK+ or who drink grapefruit juice.
Nilotinib
(Grapefruit juice = CYP3A4 inhibitor)
Nilotinib may cause CHF, QT prolongation or ______.
pancreatitis