Chemo Drugs Part II Flashcards
What do Topoisomerase Inhibitors correct?
Topoisomerases are enzymes which correct alterations in DNA that occur during replication & transcription
What are the characteristics of Topoisomerase Inhibitors?
Certain chemotherapeutic drugs inhibit either topoisomerase I or topoisomerase II
What does toxicity of Topoisomerase Inhibitors reflect?
Toxicity reflects effects of inhibition of topoisomerase enzymes on normal proliferating tissues (myelosuppression and mucositis)
What are examples of Topoisomerase II inhibitors?
include doxorubicin, daunorubicin, etoposide, and teniposide
What are examples of Topoisomerase I inhibitors?
topotecan and irinotecan
What anthracycline antibiotics used as chemotherapy agents?
Doxorubicin and Daunorubicin
What is the use of Daunorubicin?
To treat acute lymphocytic and myelocytic leukemia (Epocrates app says daunorubicin as solo tx is discontinued but can still be used in combination w/another drug)
What is the clinical use of Doxorubicin (Adriamycin)?
one of the most active single drugs for treating many cancers including metastatic adenocarcinoma of the breast, bronchogenic carcinoma, metastatic thyroid carcinoma, oat cell carcinoma, and osteogenic carcinoma
What are side effects of Doxorubicin and Daunorubicin?
cardiomyopathy, myelosuppression (leukopenia, thrombocytopenia, anemia), stomatitis, GI disturbances, alopecia
How is cardiomyopathy produced from Doxorubicin and Daunorubicin?
drug-induced injury to myocardial cells is dose-related & often irreversible side
What are the first types of cardiomyopathy that occur when Doxorubicin and Daunorubicin is administered?
acute form in 10% of patients; characterized by nonspecific ST-T changes and decreased QRS voltage, PVCs, SVT, cardiac conduction abnormalities & left axis deviation
What are the second types of cardiomyopathy that occur when Doxorubicin and Daunorubicin is administered?
slow onset of symptoms followed by rapidly progressing heart failure unresponsive to inotropic drugs & mechanical ventricular assistance
What is the occurance of 2nd form of cardiomyopathy?
•Occurs in 2% of treated patients and is fatal approximately 3 weeks after the onset of symptoms in nearly 60% of affected patients
What can increase the risk of cardiomyopathy?
Incidence of cardiomyopathy rises significantly when given with HER2+ breast CA treated with Herceptin (Antibody class of chemotherapy)
What is the properties of Dactinomycin?
Antibiotic with chemotherapeutic activity resulting from its ability to bind to DNA esp. in rapidly proliferating cells
What is the use of Dactinomycin?
Used in the treatment of Wilms tumor in children and rhabdomyosarcoma
What are the toxic effects of Dactinomycin?
early onset N&V, followed by myelosuppression (pancytopenia), glossitis, ulcerations of the oral mucosa, diarrhea, and alopecia
What is an example of Antitumor Antibiotics?
Bleomycin
What is the use of Bleomycin?
Effective in the treatment of testicular carcinoma and palliative treatment of squamous cell carcinomas of the head, neck, esophagus, skin, and GU tract
What is the most common side effect of Bleomycin?
include mucocutaneous reactions (stomatitis), alopecia, only causes minimal myelosuppression
What can patients with lymphonas develop when given Bleomycin?
Patients with lymphomas may develop an acute reaction characterized by hyperthermia, hypotension, and hypoventilation
What is the most serious side effect of Bleomycin?
dose-related pulmonary toxicity (most often pulmonary fibrosis) in 4% of patients
What is the concetration of Bleomycin?
is preferentially concentrated in the lungs and is inactivated by a hydrolase enzyme, which is relatively deficient in lung tissue
What is the MOA of Bleomycin: Pulmonary Toxicity?
Bleomycin produces pulmonary capillary endothelial damage, progressing to alveolar epithelial injury with necrosis of type I and proliferation of type II alveolar cells – interstitial fibrosis develops and may progress to involve the entire lung
What are inital signs of Bleomycin: Pulmonary Toxicity?
are cough, dyspnea, and basilar rales, which lead to either a mild form of toxicity (exertional dyspnea and a normal resting Pao2)
What is the CXR results of Bleomycin?
or a more severe form of arterial hypoxemia at rest with CXR indicative of interstitial pneumonitis and fibrosis
What are risk factors for Bleomycin: Pulmonary Toxicity?
Risk factors for developing chemotherapy-induced pulmonary toxicity are total drug dose, patient age, chest radiation, oxygen therapy, combination chemotherapy, preexisting pulmonary disease, genetic predisposition, tobacco abuse