8.7.2013(pharm-anticancer Drugs) 60 Flashcards
Most susceptible atom to Alkylating agents
N7 of guanine
Gompertzian model
Growth fraction peaks when tumor is approx 37% of its maximum size
Mesna
Mercaptoethane sulfonic acid
Mechlorethamine is used in
Hodgkin lymphoma
Adverse effects of cyclophosphamide
Cardiac dysfunction
Pulmonary toxicity
SIADH
Anticancer drugs that cause delayed neutropenia
Nitrsoureas
Adverse effects of busulfan
Adrenal insufficiency
Pulmonary fibrosis
Skin hyperpigmentation
Hyperuricemia
CNS side effects of procarbazine
Hypnosis
Vivid dreams
Drug used for CLL
Chlorambucil
As it spares myelocytes
Cisplatin nephrotoxicity can be prevented by
Chloride diuresis
Doesnot help against ototoxicity
Cisplatin is inactivated by
Aluminium
Drug that can be given to prevent cisplatin induced nephrotoxicity
Amifostine
Electrolyte abnormalities associated with cisplatin
Reduces all ions Hypomagnesimia Hypokalemia Hypophosphatemia Hypocalcemia
Anticancer drugs with strong vesicant properties
Nitrosoureas
Mechlorethamine
Alkylating agent with less chance of secondary leukemia
Cyclophosphamide
Anticancer drugs causing veno occlusive disease
All Alkylating agents in high doses
Alkylating agents causing pulmonary fibrosis
All Alkylating agents
Mechanisms of MTX resistance
Decreased MTX transporter Decreased formation of MTX polyglutamate Increased levels of DHFR due to GENE AMPLIFICATION altered DHFR Increased drug efflux transporter
Enzyme required for activation of MTX and pemetrexed
Folylpolyglutamate synthase
MTX is DOC for
Choriocarcinoma
Pemetrexed is approved for treatment of
Mesothelioma
Citrovorum factor
N10 formyl THF
Rx of MTX toxicity
Citrovorum factor
Alkalinisation of urine
Dialysis
Glucarpidase
Glucarpidase
MTX cleaving enzyme
Pralatrexate is used for Rx of
Peripheral T cell lymphoma
Adverse effects of MTX
Hepatotoxicity
Pulmonary infiltrates and fibrosis
Bone marrow supression
Mucositis
DOC for CLL
Fludarabine
Purine analogs
6MP
6TG
Cladribine
Fludarabine
DOC for Hairy cell leukemia
Cladribine(resistant to degradation by ADA)
Drug that must be given to longterm purine analog users
Cotrimoxazole for PCP prophylaxis as long term purine analog use leads to Immunosuppression
Dose of which anti metabolites should be reduced when given along with allopurinol
6-MP
azathioprine
Pyramidine analogs
5FU cytarabine Capecitabine Gemcitabine 5-azacytidine Decitabine
Single most effective agent for induction of remission in AML
Cytarabine
Anticancer drug eliminated by lungs
5FU
converted to CO2
Adverse effect of capecitabine
Hyperbilirubinemia
Metabolism of thiopurines
TPMT
thiopurine methyl transferase
5FU is catabolised by
Dihydropyramidine dehydrogenase
5FU action is augmented by
Leukovorin
DOC for pancreatic cancer
Gemcitabine
Adverse effect of thiopurines
Hepatotoxicity
Adverse effects of 5FU
Neurotoxicity
Hand foot syndrome
Side effect of fludarabine
Arthralgia
Side effect of gemcitabine
Diarrhoea
Marrow sparing cytotoxic drugs
Vincristine
Bleomycin
L-asparaginase
Diff btw vincristine and vinblastine
Vinblastine causes bone marrow supression
Vincristine has bone marrow sparing effect but dose limiting neurotoxicity
Use of vinblastine
Metastatic testicular tumors
Use of vincristine
Induction of remission in childhood leukemias
Pediatric solid tumors-Wilms,neuroblastoma,rhabdomyosarcoma
Taxanes that causes hypersensitivity reactions
Paclitaxel
Taxanes that don’t cause hypersensitivity reactions
Docetaxel
Nabpaclitaxel(protein bound paclitaxel)
Adverse effect of Taxanes
Bone marrow suppression
Neurotoxicity
Taxanes drug interactions
Cisplatin decreases paclitaxel clearance
Paclitaxel decreases doxorubicin clearance
Use of Cabazitaxel
Rx of refractory metastatic prostate cancer in combination with prednisone
MOA of action of Ixabepilone
Microtubule stabilisation
Estramustine is combination of
Estrogen and Mechlorethamine
Use of estramustine
Prostatic Ca
Side effects of estramustine
Gynacomastia
Impotence
MOA of camptothecins
Inhibits topoisomerase 1
Elimination of camptothecins
Irinotecan eliminated in bile
Topotecan eliminated by renal route
Rx of choice for advanced colorectal carcinoma
Irinotecan+5FU
Dose limiting toxicities of camptothecins
Irinotecan-diarrhoea
Topotecan- neutropenia
Adverse effects of irinotecan
Diarrhoea
Myelosuppression
Cholinergic syndrome(inhibits acetyl choline esterase)
MOA of etoposide and teniposide
Inhibit topoisomerase 2
Use of etoposide
Testicular Ca
Prostate Ca
Small cell Ca of lung
Etoposide induced secondary leukemia
Develops at short interval
Not preceded by myelodysplasia
It’s acute non lymphocytic type
Toxicity of etoposide
Hepatotoxicity
All anti tumor antibiotics are obtained from
Streptomyces
Cardiotoxicity of anthracyclins can be reduced by
Alpha tocopherol
Dexrazoxane
MOA of anthracyclins
Inhibits topoisomerase 2
Less cardiotoxic anthracyclin
Mitoxantrone
Radiation recall reaction is seen with
Anthracyclins
Use of Mitoxantrone
Hormone resistant prostate cancer
AML
SPMS(secondary progressive MS)
Leukemia caused by Mitoxantrone
Acute promyelocytic leukemia
Use of valrubicin
BCG refractory urinary bladder Ca insitu
Radiosensitizers
Hydroxy urea Gemcitabine Metronidazole 5FU dactinomycin