B.32 Flashcards
Drugs in cancer treatment IV (Hormonal agents)
SERM: Tamoxifen
Aromatase inhibitor: Anastrozole
GnRH analogs: Goserelin, Degarelix
Antiandrogens: Bicalutamide
Glucocorticoids: Prednisolone
Somatostatin analogs: Octreotide
Cardiotoxic effects of the oncopharmacons
->Heart failure:
Anthracyclins (Doxorubicin, Epirubicin)
HER2 Inhibitors (Trastuzumab)
Other targeted therapy (Imatinib, Sunitinib)
->Other cardiotoxicity:
Immune checkpoint inhibitors(ICI)
VEGF-inhibitors (Bevacizumab)
Antimetabolites (5-FU)
Alkylating agents (Cyclophosphamide)
Tamoxifen
MOA: SERM (acts as antagnist on estrogen receptors in the breast);
IND: Breast cc (in pre- and postmenopausal women); SEs: heat waves (in 20-80%), thromboembolism (1-3%), increased risk for endometrial cc, nausea, headaches, edema
Anastrozole
MOA: Aromatase inhibitor (inhibits estrogen synthesis); IND: Advanced Breast cc (in postmenopausal women with Tamoxifen resistance);
SEs: Headache, hair loss, arthralgia, fatigue, bone ache, heat waves (in 15%), diarrhea (rare), nausea, vomiting, thrombophlebitis
Goserelin
MOA: GnRH agonist;
IND: Prostate cc, advanced breast cc, (other non-neoplastic cases such as- endometriosis, assisted fertilization, preterm puberty);
SEs: Heat waves, ↓libido, headache, diarrhea, the tumor may be temporarily activated, might be increase in serum Testosterone level, redness, gynecomastia, impotence;
Important: continuous administration for cancer therapy, pulsatile administration for ovulation stimulation
Degarelix
MOA: GnRH antagonist;
IND: Advanced, hormone-dependent prostate cc;
SEs: impotence, weight gain, ↓glucose tolerance, osteoporosis, QT-prolongation, ↑cardiovascular risk
Bicalutamide
MOA: Androgen receptor antagonist;
IND: In prostate cc. (in combination with GnRH analog); SEs: QT prolongation, vomiting, diarrhea, pressure sensitivity of the nipples, androgen hormone deprivation→ osteoporosis
Prednisolone
MOA: Glucocorticoid analog. Inhibits all phases of inflammation (vascular, cellular, and repain), Immunosuppressive effects, Induces apoptosis in lymphomas, Appetite enhancer, Decreased ICP, Decreased nausea;
IND: Myeloma multiplex, ALL, CLL, NHL, Brain and spinal tumors (reduced ICP), Chemo- or radiotherapy induced vomiting (adjuvant to decrease nausea), Reduced weight loss, Reduction of bone metastasis pain (adjuvant);
SEs: Tumorlysis syndrome (when treating lymphoma), HTN, hyperglycemia, Osteoporosis, peptic ulcers, striae and more GCs side effects
Octreotide
MOA: Somatostatin analog (inhibits GH release and inhibits pancreatic insulin and glucagon release);
IND: Acromegaly, Gastro-pancreatic neuroendocrine tumors (GEP-NET), Neuroendocrine tumors (NET), TSH-secreting adenomas, Varicose bleeding, endoscopic sclerosis;
SEs: Mild transient GI symptoms, During long term treatment (→ bile thickening and gallstones due to CKK inhibition, rarely deterioration of glucose tolerance due to ↓insulin)
Tumor lysis syndrome
occurs when tumor cells release their inner content to the bloodstream, either in response to therapy or spontaneously, leading to hyperuricemia, hyperkalemia, hypophosphatemia, and hypocalcemia
Effects of the oncopharmacons
- Oncology medications often have cardiotoxic effects, which can be acute, life-threatening events, or long-term heart disease
- In addition to therapy, the cardiovascular outcome is determined by cancer and the patient’s cardiovascular risk factors
- Not only classical chemotherapeutic drugs (e.g. Doxorubicin) have cardiotoxic effects, but also newer, targeted or immunotherapies
Hormone and hormone analog cytostatic agents
-Anti-estrogens (inhibition of estrogen receptors)
-Aromatase inhibitors (inhibition of estrogen synthesis)
-GnRH analogs
-Antiandrogens (androgen receptor antagonists)
-Glucocorticoids and somatostatin analogs
-Progesterone derivatives
Anti-estrogens (inhibition of estrogen receptors)
Tamoxifen, Toremifen, Fulvestrant
Aromatase inhibitors (inhibition of estrogen synthesis)
Anastrosole, Letrosol, Exemestan
GnRH analogs
Goserelin, Buserelin, Leuprorelin, Triptorelin, Degarelix
