Alkylating Agents

mogonube's version from 2016-10-06 13:47


Question Answer
most reactive alkylating agentMechlorethamine
Therapeutic use of MechlorethamineHodgkins
Adverse effects of MechlorethamineBM suppression, and intestinal mucosa
List 4 Nitrogen MustardsMechlorethamine, cyclosphosphamide, ifosfamide, melphalan, chlorambucil
Adverse Effect of cyclophosphamideMetabolism can produce acrolein (toxic) treat with MESNA, immunosuppression and alopecia
Therapeutic use for ifosfamidetesticular cancer
Adverse effects of ifosfamideUrinary tract and CNS toxicity - MESNA, immunosuppression
Therapeutic use for Melphalanmultiple myeloma
List 3 NitrosureasCarmustine, Lomustine , Streptozocin
Therapeutic use of Carmustinebrain tumors
Adverse effects of Carmustine and LomustineBM supp. long term- renal failure
Name of the drug thats a TriazeneDacarbazine
what drug inhibits DNA/RNA synthesis by forming toxic methyl carbonium ionsDacarbazine
Therapeutic use of Dacarbazinemelanoma, and Hodgkins
Adverse effects of Dacarbazineflu like syndrome
Tx for multiple myeloma?Melphalan
Tx for melanoma?Dacarbazine
What is the drug thats a MethylhydrazineProcarbazine
What is the MOA of ProcarbazineMethylates DNA , produces free radicals that lyse DNA strands and inhibits RNA synthesis
Therapeutic use of ProcarbazineHodgkins, Non- Hodgkins, brain tumors
significant reactions of procarbazineDisulfiram- like reaction with alcohol
adverse effects of procarbazineBM supp, neurotoxicity
Platinum complexesCisplatin, carboplatin, oxaliplatin
Therapeutic use of Cisplatintesticular, ovarian, bladder and lung cancers
MOA of Platinum Complexesattaches to nucleophilic sites on DNA and form interstrand and intrastrand crosslinks which inhibits replication & transcription
use of Oxaliplatinadvanced colorectal cancer (part of FOLFOX)
adverse effects of cisplatinnephrotoxicity, ototoxicity, periph neuropathy
adverse effects of oxaliplatinperiph neuropathy
List 3 purine analogs6- mercaptopurine (6-MP), 6-thioguanine (6-TG), Fludarabine-5-phosphate
Use for 6-MPmaintenance of remission of acute lymphoblastic leukemia
use for 6-TGacute granulocytic leukemia
what is an important adverse effect of 6-MPpts with allopurinol must be given a reduced dose of 6-MP bc allopurinol inhibits xanthine oxidase which metabolizes 6-MP
MOA of Fludarabine-5-phosphateadenosine analog; inhibits DNA polymerase, primase and ligase
use for Fludarabine-5-phosphatelow grade lymphoma, chronic lymphocytic leukemia (CLL)
what are the classes of drugs that fall under the category of antimetabolites?purine analogs, folic acid analogs, folate antagonist rescue agent, pyrimidine analogs
what is the drug that is a folic acid analog?methotrexate
MOA of methotrexateinhibits dihydrofolate reductase
therpeutic use for methotrexateALL, burkitts, non-hodgkins, head & neck cancers (high doses- osteogenic cancer, choriocarcinomas)
how is toxicity from methotrexate prevented or reversed ?from admin of leucovorin
MOA of 5-Fluorouracil (5-FU)inhibits thymidylate synthase which inhibits DNA synthesis and RNA synth
use of 5-FUcolorectal cancer, breast cancer, basal cell carcinomas
adverse effects of 5-FUBM supp, GI tract toxicity
list 3 pyrimidine analogs5- fluorouracil, cytarabine, gemcitabine
MOA of cytarabineconverted to a triphosphate form (ARA-CTP) that inhibits polymerase and prevents DNA synthesis
Use of cytarabineacute myelogenous leukemia (AML)
Use for gemcitabinemetatstatic pancreatic cancer and non-small cell lung cancer and bladder cancer

Antineoplastics 2

Question Answer
what are the classes of plant alkaloidsvinca alkaloids, taxanes, camptothecins, epipodophyllotoxins
2 vinca alkaloidsvinblastine, vincristine
MOA of vinca alkaloidsantimitotic, m-phase specific, bind tubulin and prevent microtubule assembly
use for vincristinetx of choice with glucorticoids for childhood acute lymphoblastic leukemia
use for vinblastinefor metatstatic testicular tumors in combo with bleomycin and cisplatin
adverse effects for the vinca alkaloidsBM supp for vinblastine, periph neuropathy for vincristine
list the 2 taxanespaclitaxel, abraxane
how do the taxanes work?promote mircotubule assembly and stabilization created malformed ones, that block mitosis
what is special about abraxane ?bound to albumin
use of taxanesovarian , breast, lung, head and neck cancers
adverse effects of taxanesneutropenia and hypersensitivity reactions
what drug is a camptothecintopotecan
MOA of topotecans-phase specific, binds to and stabilizes topoisomerase I-DNA complex (cleaves but no resealing)
adverse effects of topotecanmyelosuppression, nausea, vomiting, bronzing of skin
what class does etoposide belong to?epipodophyllotoxin (plant alkaloid)
MOA of etoposidecomplexes with topoisomerase II- prevents resealing of breaks, blocks replication
MOA of actinomycin Dbinds to DNA by intercalating btw GC base pairs
one of the most antitumor agents knownactinomycin D (Dactinomycin)
list an important anthracyclineDoxorubicin (Adriamycin)
MOA of anthracyclinesbind to DNA backbone blocking synthesis
adverse effects of anthracyclinesBM supp, alopecia, cardiotoxicity-from free radicals and lack of SOD in cardiac tissue
use of leuprolide acetatemetastatic gonadal sterioid dependant prostate cancer
list a drug thats an antiestrogenfulvestrant
use of Fulvestrantbreast cancer in postmenopausal women
antiandrogen drugFlutamide
use of Flutamideprostate cancer
list 2 selective estrogen receptor modulatorsTamoxifen, Raloxifene
MOA of tamoxifenanti-estrogen on breast
adverse effects of Tamoxifenacts as estrogen on endometrium-- inc risk of cancer
use of raloxifenereduction of risk of breast cancer and osteoporosis in postmenopausal women who are at high risk
what is the beneficial side effect of Raloxifeneneutral effect on endometrium
MOA of Anastrozoleinhibits estrogen synthesis

miscellaneous antineoplastic agents

Question Answer
MOA of Tretinoininduces differentiation
Use for Tretinoinacute promyelocytic leukemia (APL)
adverse effects of Tretinoinretinoic acid syndrome, vit A toxicity
2 protein tyrosine kinase inhibitorsImatinib mesylate, Gefitinib
MOA of Imatinibinhibits Bcr-Able tyrosine kinase and c- kit receptor protein kinase
use of ImatinibCML and gastric stromal tumors
MOA of Gefitinibinhibits epidermal growth factor receptor tyrosine kinase, blocks signal transduction pathways
use of Gefitinibnon-small cell lung cancer
what is an important proteasome inhibitorBortezomib
MOA of Bortezomibacts as a reversible inhibitor of the 26S proteasome
Use for Bortezomibrefractory multiple myeloma
MOA of Trastuzumabblocks the HER2/neu receptor for breast cancer
MOA of Rituximabbinds to CD20 ag on B lymphocytes causes cell lysis- for low grade lymphoma
MOA of Cetuximabbinds EGFR and blocks activation of receptor-assoc kinases inhibiting cell growth
use of Cetuximabcolon cancer
MOA of Bevacizumabbinds to VEGF and inhibits formation of new bld vessels
Use of Bevacizumabmetastatic colorectal cancer
what an adverse effect of Bevacizumabhypertension
what biologic response modifier induces a t- cell response that is cytolytic for tumors ?interleukin-2