S phase drug - acute Non lymphocytic leukemia - toxicity of myelosupression anti purine drug

S phase drug - CLL - Tox: given IV to prevent bacteria from produciting fluoroadenine, myleosupression, and opportunistic infection. adenosine analog that gets triphosphate and incorporated and stops replication

S phase drug - Hairy cell leukemia - tox: myelosupression and drug fever adenosine analog that gets triphosphate and incorporated and stops replication

drugs Flashcards by Justin Armstrong

5-FU

anti pyramiding drug that is used for solid tumors
gets converted by thymidylate phosphorylase in tumors
inhibits thymidylate synthase
damages DNA
Damages RNA
toxicities= cerebellar ataxia, neurologic symptoms, hair loss

S phase drug

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Capecitabine

oral form of 5-FU
gets converted into 5-fu by liver carboxyesterase 1a1 and cytidine deaminase
tymadine phospholase is the final conversion to 5-fu which happens in tumor

toxicity = hand foot syndrome

S phase drug

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cytarabine (ara-c)

enter tumor cells via hENT1 transporter
get phosphorated 3 times get incorporated into DNA and cause chain termination

used for acute leukemia

gets deactivated by Cytocine deaminase and pyrimidine nucleotidase

important because the rate Are-c gets converted to its toxic product hex go bd high than the rate it gets converted to inactive metabolite by cytosine deaminase and pyrimidine nucleotidase!!!!

toxicity is myelosupression

S phase drug

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Gemciatibe

enter tumor cells via hENT1 transporter
get phosphorated 3 times get incorporated into DNA and cause chain termination

used for pancreatic treatment and non small cell lung cancer

toxicity is myelosupression

S phase drug

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Methotrexate

S phase drug
Folate antimetabolite
competitively inhibits dihydrofolate reductase
prego catagory d
Used for ped. leukemias, NHL, choriocarcinoma, Primary CNS lymphoma

-enters cell via RFC (reduced folate carrier)

want to alkalize the urine because it can cause crystallura tubular obstruction.

MTX-glutamate accumulates and inhibits DHFR
Glutamate THF accumulates and inhibits thymidylate synthase

Toxicity

bone marrow suppression -> leukovorin rescue
renal toxicity “7-OH-MTX” doing damage

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Pemetrexed

-S phase drug
1000X less potent of DHFR blocker
-Can be used in MTX resistant cancer
-Used for malignant pleural mesothelioma

-Competetive inhibitor of thymalate synthase and GAR transformylase

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6-mercaptopurine

S phase drug

used in maintenance and remission of ALL
toxicity of myleosupression

6-MP gets converted to thiopurine methyl transferase then to active metabolites like TIMP

xanthine oxidase (80% metabolized by) and thiopurine methyltransferase form inactive metabolite.

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6- thioguanine

S phase drug

acute Non lymphocytic leukemia
toxicity of myelosupression

anti purine drug

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fludarabine

S phase drug

CLL
Tox: given IV to prevent bacteria from produciting fluoroadenine, myleosupression, and opportunistic infection.

adenosine analog that gets triphosphate and incorporated and stops replication

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Cladribine

S phase drug

Hairy cell leukemia
tox: myelosupression and drug fever

adenosine analog that gets triphosphate and incorporated and stops replication

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Vinblastine

M phase drug

blocks microtubual assembly

testicular cancer, lymphomas, neuroblastoma

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Vincristine

M phase drug

blocks microtubual assembly

Pediatri ALL, Lymphoma, neuroblastoma, Willms tumors, ewings sarcome

Neurotoxicity and peripheral neuropathy.

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Venorelbine

M phase drug

blocks microtubual assembly

Advanced non-small cell cancer

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Taxol (paclitaxel)

M phase drug
Stabilize microtubules

Advanced breast and ovarian

side effect is Sever HTN during infusion and required corticosteroid pretreatment

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Taxotere (docetaxel)

M phase drug
Stabilize microtubules

advanced breast and ovarian recurrence

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etoposide

topoisomerase II inhibitor -> DS DNA break

causes leukopenia secondary cancer
Mixed phase drug

oat cell carcinoma and testicular cancer

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Trnioside

topoisomerase II inhibitor -> DS DNA break

causes leukopenia
Mixed phase drug

glioma and neuroblastoma

topotecan

Topoisomerase I blocker
Single stranded DNA breaks
S phase drugs

causes neutropenia and mucositis

second line drug

Irinotecan

Topoisomerase I blocker
Single stranded DNA breaks
S phase drugs

causes Severe diarrhea.

metastatic colorectal cancer.

bleomycin

causes DNA strand breaks because of Fe radical production -> superoxide radical production.

testicular cancer

causes pulmonary fibrosis

daztinomycin

DNA intercalating agent

antibiotic

Doxirubicin

Inhibit topoisomerase II, DNA intercrcalting agent, Free radical generation -> DNA strand breaks
Cardiotoxicity
breast and ovarian but wide spectrum

Daunorubicin

Inhibit topoisomerase II, DNA intercrcalting agent, Free radical generation -> DNA strand breaks
Cardiotoxicity
leukemia ALL and ALL

Epirubicin

Inhibit topoisomerase II, DNA intercrcalting agent, Free radical generation -> DNA strand breaks
Cardiotoxicity
wide spectrum breast and ovarian

idarubicin

Inhibit topoisomerase II, DNA intercrcalting agent, Free radical generation -> DNA strand breaks Leukemia (ALL, AML, CML and blast crisis) Cardiotoxicity

Mitoxatrone

Inhibits topoisomerase II Breast, prostate and NHL Cardiotoxicity

Hodgkin lymphoma treatment

ABVD treatment A= drimycin (doxorubicin ) -> topo II, ect. -> dialated cardio B= Bleomycin -> free radical -> pulm fibrosis V= Vinblastine -> microtubual D= dacarbazine -> nausea vomiting

NHL treatment

CHOP C: cyclophosphamide -> hemorrhagic cystitis H: Hydroxydaunorubicin -> cardiotoxicity O: Oncovin (vincristine) -> neuropathy P: prednisone -> hyperglycemia, osteopenia

Imentinib

Tyrosine kinase inhibitor good for CML (9:22) BCL-ALK also good for GIST's resistance is from changeing of the ATP binding pocket

Dasatinib

Tyrosine kinase inhibitor good for CML (9;22) translocation BCR-ABL also good for ALL that has philly chromosome. will bind to modified BCR-ABL that is imatinib resistant.

Rifampin and St. Johns wart

CYP inducers. important because it can cause faster clearance of Imantinib

Gefitinib

block EGFR -> used in Non-small cell lung cancer | Membrane associated RTK drug

Erlotinib

block EGFR -> used in Non-small cell lung cancer | Membrane associated RTK drug

Lapatinib

block EGFR Blocks HER2 used in breast cancer Membrane associated RTK drug

sunitinib

blocks C-Kit, PDGF, VEGFR, Used for GIST and RCC Membrane associated RTK drug

Sorafinib

Blocks PDGFR and VEGFR and RAF used in RCC and HCC Membrane associated RTK drug

Cetuximab

EGFR receptor Ab's that are used for in colon cancer

Panitumumab

EGFR receptor Ab's that are used for in colon cancer

transtuzumab

HER2 receptor Ab that is used in breast cancer and has cardiotoxic effects.

Bezacizumab

VEGF ligand Ab -> used in RCC (because of VHL)

Rituximab

CD 20 AB | used for NHL