Hem & Onc - Pharm (Individual Cancer Drugs & Common Chemotoxicities) Flashcards
Pg. 405-407 in First Aid 2014 or Pg. 373-375 in First Aid 2013 Sections include: -Cisplastin, carboplatin -Etoposide, teniposide -Irinotecan, topotecan -Hydroxyurea -Prednisone, prednisolone -Tamoxifen, raloxifene -Trastuzumab (Herceptin) -Imatinib (Gleevec) -Rituximab -Vemurafenib -Bevacizumab -Common chemotoxicities
What drug has the same mechanism of Cisplatin? What is their mechanism?
Carboplatin; Cross-link DNA
For what cancers are cisplatin and/or carboplatin used clinically?
(1) Testicular (2) Bladder (3) Ovary (4) Lung (carcinomas)
What are the toxicities associated with Cisplatin/carboplatin?
(1) Nephrotoxicity (2) Acoustic nerve damage
What prevents the nephrotoxicity effect of cisplatin/carboplatin?
Amifostine (free radical scavenger) & chloride diuresis
What drug has the same mechanism as Etoposide? What is their mechanism?
Teniposide; Inhibit topoisomerase II –> decreased DNA degradation; Think: “ eTOPOside inhibits TOPOisomerase II”
For what 3 major cancers are etoposide and/or teniposide used clinically?
(1) Solid tumors (particularly testicular and small cell lung cancer) (2) Leukemias (3) Lymphomas
What are the toxicities associated with etoposide/teniposide?
(1) Myelosuppression (2) GI irritation (3) Alopecia
What is the mechanism of hydroxyurea?
Inhibits nucleotide reductase –> decreased DNA synthesis (S-phase specific)
For what is hydroxyurea used clinically?
(1) Melanoma (2) CML (3) Sickle cell disease (increase HbF)
What are the toxicities associated with hydroxyurea?
(1) Bone marrow suppression (2) GI upset
What is the name of another drug that functions similarly to Prednisone? What is their proposed mechanism?
Prednisolone; May trigger apoptosis, may even work on nondividing cells
For what are prednisone and/or prednisolone used clinically?
(1) Most commonly used glucocorticoid in cancer chemotherapy - Used in CLL, non-Hodgkin’s lymphomas (part of combination chemotherapy regimen) (2) Immunosuppressant (e.g., autoimmune diseases)
What are the toxicities associated with prednisolone and/or prednisone?
Cushing-like symtoms: weight gain, central obesity, muscle breakdown, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis
What is a drug that shares the same mechanism as Tamoxifen? What is their mechanism?
Raloxifene; SERMs - receptor antagonists in breast and agonists in bone. Block binding of estrogen to estrogen receptor-positive cells
For what are Tamoxifen and/or Raloxifene used clinically?
(1) Breast cancer treatment (tamoxifen only) and prevention (2) Raloxifene also useful to prevent osteoporosis
What are the toxicities associated with Tamoxifen versus Raloxifene?
TAMOXIFEN - partial agonist in endometrium, which increases risk of endometrial cancer; “hot flashes”; RALOXIFENE - no increase in endometrial carcinoma because it is an endometrial antagonist
What is the brand name of Trastuzumab? What is its mechanism?
Herceptin; Monoclonal antibody against HER-2 (c-erbB2), a tyrosine kinase. Helps kill breast cancer cells that overexpress HER-2, through inhibition of HER2-initiated cellular signaling and antibody-dependent cytotoxicity
For what is Trastuzumab (Herceptin) used clinically?
HER 2-positive breast cancer and gastric cancer; Think: “her-2 tras2zumab”
What is the toxicity associated with Trastuzumab (Herceptin)?
Cardiotoxicity; Think: “HEARTceptin damages the HEART”