Drugs and reproductive system neoplasms Flashcards
What is the MOA of Methotrexate?
Competitive and reversible DHRF inhibitor
What is the antidotes for methotrexate?
Leucovorin/ folinic acid- the rescue agent
What are the uses of methotrexate?
solid tumors / immunosuppression in graft rejection
What are the toxicities of methotrexate?
NEPHROTOXIC, myelosuppressive, pulmonary and hepatotoxic
What are the uses of cyclophosphamide?
leukemia, solid tumor, non hodgkins lymphoma, ovarian ca, neuroblastoma, immunosuppressive to prevent graft rejection
What is the MOA of cyclophosphamide?
become strong electrophiles thru formation of carbonic ion, converted to active nitrogen mustard which ends products of metabolism so ultimately affects DNA and RNA synthesis
What are the antidotes for cyclophosphamide?
Mesna and acrolein
What is the toxicity of cyclophosphamide?
bone marrow suppression, cystitis, darkening of nails and hair loss
What are the uses of cisplatin?
urinogenital cancers (testicular, ovarian and bladder) alone is effective in colorectal cancer
What is the MOA of cisplatin?
reacts with DNA forming strand links leading to breaks and miscoding, causing inhibition of replication and transcription
What are the toxicities for cisplatin?
nephrotoxicity, electrolyte disturbance, and ototoxicity
What are the uses for doxorubicin?
solid tumors of breast, endometrium, testes and lung. used for Hodgkins and non hodgkins lymphoma, sarcomas and metastatic carcinoma of the thyroid
What is the MOA for doxorubicin?
prevents TOPII resealing helical breaks. a TOPII poison. Drug induced single and double strand breaks causes free radical formation
What would cause resistance to doxorubicin?
- development of abnormal transport proteins
2. MDR gene over expresses the glycoprotein regulating efflux
What are the toxicities for doxorubicin?
serious cardiomyopathy. with repeated doses supraventricular arrhythmia may occur
What is the antidote for doxorubicin
Dexrazoxane, an iron chelators, reduces the cardiomyopathy damage induced
What are the uses for bleomycin?
testicular cancers, squamouse ca of the head neck and lungs, and lymphomas
What is the MOA of bleomycin?
fragmentation of DNA; RS formation cause chromosomal fragmentation, cells accumulate in G2 phase of cell cycle
What are the toxicities associated with bleomycin?
pulmonary toxicity (dry cough) and pulmonary fibrosis
What is the MOA of etoposide?
stabilizes the topoisomerase II DNA complex causing double strand DNA breaks during DNA replication.
What are the uses for etoposide?
treats first time and metastatic testicular cancer
What are the uses for paclitaxel?
Ovarian and breast, lung esophageal, bladder, head and neck cancer
What is the MOA of paclitaxel?
Inhibits microtubule disassembly and microtubular plates accumulate in cells causing abnormal and dysfunctional spindles
What are the toxicities assoc with paclitaxel?
Hypersensitivity reactions, neutropenia, cardiac conduction defects
What are the uses for tamoxifen?
Breast ca, infertility and gynecomastia
What is the MOA of tamoxifen?
blocks binding of estrogen to its receptor in breast ca
What are the toxicities for tamoxifen?
N/V, hot flashes, vaginal bleeding, disease flare, hypercalemia, ocular dysfunction and peripheral edema
What is the use for anastrozole?
breast cancer
What is the MOA of anastrozole?
aromatase inhibitor prevents estrogen synthesis, so decrease production of testosterone and estrone
What is the use of Fulvestrant?
Antiestrogen for hormone sensitive tumors
What is the MOA of flutamide?
Nonsteroidal androgen antagonis (NSAA) which inhibits the translocation of steroid receptors to the nucleus
What is the MOA finasteride?
5 alpha reductase inhibitor-inhibits synthesis of dihydrotestosterone.
What is the use of finaseride?
prostate cancer
What is the MOA of leuprolide?
GnRH analogue which acts as a partial agonist at GnRH receptors.
What is leuprolide used for?
treatment of prostate cancer
What is the MOA of trastuzumab?
recombinant DNA derived humanized monoclonal antibody (G1 kappa)
What is the use for trastuzumab?
specific HER2 breast cancer
what are the adverse effects of trastuzumab?
cardiotoxicity (uncommon)
What is the use of Pamidronate?
bisphosphonate that treats osteoporosis used in disease of bone mineral homeostasis
What is the MOA of pamidronate?
suppresses the activity of osteoclasts via inhibition of farnesyl pyrophosphate synthesis
What are the toxicities for pamidronate?
adynamic bone, possible renal failure, osteonecrosis
What are the uses for Raloxifene?
prevention and treatment of osteoporosis in postmenopausal women
What is the MOA of raloxifene?
SERM - selective estrogen receptor modulator
what is the adverse effect of raloxifene?
possible venous thromboembolism
What is the use of zoledronic acid ?
used in the treatment of skeletal metastases and hypercalcemia in patients with breast cancer or osteolytic lesions of myeloma
What is the MOA of oxandrolone?
a synthetic anabolic steroid derivative of dihydrotestosterone
What are the uses of oxandrolene?
promotes skeletal muscle protein synthesis through direct action on testosterone or dihydrotesterone receptors. **it will not aromatize
-maybe used to treat wasting disease in AIDS
