21854326
Description
Flashcards by Sam Adeyiga, updated more than 1 year ago
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Created by Sam Adeyiga
over 4 years ago
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| Question | Answer |
| Anthracyclines drugs are | 1. doxorubicin*** 2. daunorubicin 3. epirubicin (epidoxorubicin) *** *** are the commonly mentioned. |
| Describe "steal liposomal" | 1. Use in doxorubicin (Doxil) drug delivery 2. synthetically prepared vesicle consisting of a lipid bilayer which encapsulates a drug. 3.Has lipid bilayer consisting of fully hydrogenated soy phosphatidylcholine (HSPC), encapsulates doxorubucin. 4. MPEG-DSPE, a pegylated diacylglycerol derivative, coats the bilayer, decreasing uptake by phagocytes and increasing the circulatory half-life of Doxil. |
| merit of "steal liposomal" | 1. Decreases AEs like cardiotoxicity compare to traditional doxorubicin solution. 2. Anthracyclines are well known for causing cardiotoxicity. |
| Anthracyclines SEs + solutions (1) | 1. arrhythmias and ST- and T-wave alterations. 2. permanent cardiac damage presenting as heart failure that does not respond to HF therapy. 3. Solutions: stick w/ lifetime doses of Anthracyclines. |
| Lifetime doses of Anthracyclines. 1. Doxorubicin: -----? 2. Daunorubicin: -----? 3. Epirubicin: -------? | Doxorubicin: 550 mg/m2 Daunorubicin: 1000 mg/m2 Epirubicin: 900 mg/m2 |
| Anthracyclines SEs + solutions (2) | 1. myelosuppression = is the dose-limiting toxicity 2. mucositis 3. emesis 4. diarrhea 5. alopecia |
| Treatment for anthracycline IV extravasates are ..... | 1. Dimethyl sulfoxide (DMSO) 99% 2. Dexrazoxane (Totect®) |
| What is the difference btw 1. Dexrazoxane (Zinecard®) 2. Dexrazoxane (Totect®) | 1. Dexrazoxane (Zinecard®) = provides protection against cardiotoxicity 2. Dexrazoxane (Totect®) = for the treatment of extravasation of IV anthracycline therapy. |
| Alkylating Agent is | Cyclophosphamide (a nitrogen mustard alkylating agent) |
| Cyclophosphamide is closely related to ----? | ifosfamide |
| cyclophosphamide requires activation by CYP450 to have an anticancer effect, the primary isoforms are -----? | 1. CYP2B6 2. some CYP3A4 |
| What is the name of the metabolite formed by cyclophosphamide wh/ causes hemorrhagic cystitis? | Acrolein |
| The therapeutic, DNA reactive metabolite is of cyclophosphamide is ----? | a nitrogen mustard |
| acrolein is a ------? | bladder-toxic metabolite formed as a result of this activation |
| 1. Due to bladder toxicity, -------- is necessary with either IV or PO administration of cyclophosphamide. 2. During high-dose treatment, patients should receive vigorous IV -------? | 1. hydration 2. hydration |
| AEs of cyclophosphamides | 1. Alopecia 2. Emesis (dose-dependent) 3. Hemorrhagic cystitis *** 4. Infertility issues 5. Leukopenia (dose-limiting)*** 6. Secondary malignancy 7. SIADH *** |
| Taxanes drugs are ---- | 1. Paclitaxel +/- Bevacizumab 2. Docetaxel |
| Taxanes MOA | 1. Inhibits microtubules disassemblage |
| Why do patients receive dexamethasone with docetaxel? | . |
| What are the major toxicities associated with paclitaxel and docetaxel? | . |
| Why do patients receive premedication with dexamethasone, diphenhydramine and an H2 antagonist prior to paclitaxel? | . |
| Microtubule inhibitors are | 1. Vinorelbine 2. Eribulin 3. Ixabepilone (taxane & anthracycline failures)*** |
| Microtubule inhibitors MOA | 1. binds to tubulin and inhibits microtubulin formation. 2. Inhibits the formation of mitotic spindle. 3. M phase specific microtubule stabilizing agents. |
| Ixabepilone (epithilone) is associated with -----? | 1. myelosuppression (neutropenia) 2. peripheral neuropathy 3. cognitive impairment. |
| Ixabepilone BBW includes ------? | 1. a black box warning against its use in patients with impaired liver function, as this increases the risk of life threatening neutropenia. |
| Cremophor (also used as an excipient in taxane formulations) is known to be a --------- and may lead to ----------- which can be life threatening if not treated appropriately | 1. sensitizing agent 2. hypersensitivity reactions |
| Cremophol EL requires ---------- as premeds | H1 & H2 antagonists |
| What is the purpose of Cremophor® EL in taxane and microtubulin inhibitors formulations? | to improve solubility |
| vinorelbine (Navelbine®) is used for ---? | metastatic breast cancer |
| Antimetabolites | 1. Gemcitabine 2. Capecitabine *** |
| Capecitabine is available in tablets form as ------------- prodrug? | 5-Fluorouracil prodrug |
| Capecitabine is an elegant drug in that it allows for -------- concentrations of --------- (the active product provided by 5-FU) in cancerous cells than in normal cells. | 1. higher 2. 5-F-dUMP |
| Activation of 5-FU through several steps to yield a metabolite which targets thymidylate synthase and acts as a suicide inhibitor is an MOA of -------------- drugs? | Antimetabolite = Capecitabine |
| Capecitabine SEs are ----- ? | 1. bone marrow suppression 2. N / V/ D 3. “hand-and-foot syndrome” |
| How do you identify drug leakage caused by “hand-and-foot syndrome”? | 1. redness 2. tenderness 3. numbness/tingling 4. peeling of the palms and sole that looks like sunburn. |
| capecitabine carries a black box warning of a -------? | potential to increase the anticoagulating effects of warfarin |
| Antibodies (moAb) that TARGETS HER2/neu and HER2(+) | 1. Trastuzumab 2. Pertuzumab 3. Trastuzumab Hyaluronidase (Herceptin Hylecta®) 4. Ado-trastuzumab emtansine (Kadcyla™) *** They both target different epitopes. Hence, can be used in combination for greater effects. |
| Trastuzumab (Herceptin®) and pertuzumab (Perjeta®) MOA ---? | 1. inhibit HER2 homo- or heterodimerization ==> block tyrosine kinase activity which normally leads to cell growth due to downstream signaling, 2. mark the breast cancer cell for attack via activation of antibody-dependent cellular cytotoxicity 3. inhibit HER2 stimulated blood vessel growth (angiogenesis) in the tumor. |
| Trastuzumab (Herceptin®) and pertuzumab (Perjeta®) SEs are -----? | 1. Hypersensitivity 2. cardiotoxicity |
| Trastuzumab (Herceptin®) and pertuzumab (Perjeta®) BBW is ----? | 1. Infusion-related toxicity (hypersensitivity) 2. Cardiotoxicity 3. pulmonary toxicity |
| What are pretreatment drug recommendations for Trastuzumab (Herceptin®) and pertuzumab (Perjeta®) in other to avoid infusion related toxicitity? | 1. APAP 2. Benadryl (diphenhydramine) |
| What is the difference btw Trastuzumab (Herceptin®) and Ado-trastuzumab emtansine (Kadcyla™) | 1. Ado-trastu is a HER2-antibody drug conjugate which incorporates the HER2 targeted actions of trastuzumab with the microtubule inhibitor DM1 (aka. Mertansine) 2. The conjugate allows for selective delivery of the cytotoxic agent (DM1) into HER2 overexpressing cells, resulting in cell cycle arrest and apoptosis via a mechanism similar to that of the vinca alkaloids. |
| Ado-trastuzumab emtansine (Kadcyla™) BBW includes ----? | 1. Cardiotoxicity (evaluate pt Q3mo) 2. Hepatotoxicity (Monitor transaminases & bilirubin at baseline and b4 each dose) |
| DM1 is associated with | 1. peripheral neuropathy 2. bone marrow suppression 3. extravasation reactions |
| Fam-trastuzumab deruxtecan-nxki (Enhertu®) indication is -----? | approved for unresectable or metastatic HER2(+) breast cancer in patients who have received two or more prior anti HER2-based regimens in the metastatic setting. |
| Fam-trastuzumab deruxtecan-nxki (Enhertu®) MOA? | 1. targets HER-2 with a small molecule, DXd (a topoisomerase I inhibitor) which attached to the antibody by a cleavable linker. 2. membrane permeable DXd causes DNA damage and apoptotic cell death. |
| Fam-trastuzumab deruxtecan-nxki (Enhertu®) AES | 1. Cardotoxicity 2. fatigue 3. Nausea and vomiting 4. alopecia 5. constipation 6. decrease appetite 7. anemia 8. neutropenia 9. diarrhea 10. leukopenia 11. cough 12. thrombocytopenia. Warnings and precautions include interstitial lung disease and pneumonitis which have resulted in death. |
| Kinase Inhibitors are | 1. Lapatinib (TKI [tyrosine kinase inhibitor]) 2. Neratinib (“pan- EGFR TKI inhibitor) |
| Lapatinib and Neratinib MOA? | bind to the kinase domains of activated EGFR (ErbB1) and other HER (ErbB) receptors, preventing their ability to phosphorylate downstream signalling proteins, thereby preventing transmission of growth signals |
| Lapatinib and Neratinib AEs ---? | Hepatotoxicity *** BBW for Lapatinib but not for Neratinib rash nausea fatigue Severe diarrhea (aggressively managed with loperamide prophylaxis) |
| Lapatinib (Only) SEs ---? | 1. risk of cardiotoxicity - decreases in left ventricular ejection fraction (LVEF) and heart failure (less severe than trastuzumab) 2. pulmonary toxicity (interstitial lung disease (ILD) and pneumonitis), and 3. QTC elongation |
| Lapatinib BBW | “Hepatotoxicity" |
| Lapatinib indication ---? | 1. approved for use in HER2(+) patients with brain metasteses, 2. in those who have prior exposure to trastuzumab, anthracyclines, or taxanes, or 3. in those with an indication of hormone therapy. |
| Neratinib (Nerlynx®) indication ----? | approved for use in combination with capecitabine in patients with advanced or metastatic HER2(+) breast cancer who have received 2 or more prior anti-HER-2 based regimens. |
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