Anti-Neoplastics N/c

Front 1

What happens in tumor lysis syndrome?

Back 1

↑ uric acid (gout), ↑ phosphate (hypocalcemia), hyperkalemia

Front 2

What are the 2 branches of anti-neoplastics?

Back 2

1. Cell cycle specific
2. Cell-cycle non-specific

Front 3

What classes are cell-cycle specific? What phase of cell cycle for each?

Back 3

M-phase= Anti-microtubule (Vinca, taxanes)
S = Antimetabolites, Daunorubicin, topotecan
G2 = Bleomycin

Front 4

MoA of alkylating agents?

Back 4

add alkyl group → damage DNA

Front 5

What are the common SE of alkylating agents?

Back 5

myelosuppression, mouth sore, hair loss, 2o AML

Front 6

Bendamustine

MoA?

Back 6

alkylating agent

Front 7

Cyclophosphamide

How is it activated?
MoA?
Toxicity? How do you prevent?

Back 7

need hepatic +

Alkylating agent

Hemorrhagic cystitis (Mesna prevents by binding toxic metabolites)

Front 8

Busulfan

MoA?
Toxicity?

Back 8

alkylating agent

Pulmonary fibrosis
Hyperpigmentation

Front 9

Nitrosoureas: Carmustine & Lomustine

MoA?
Use?
Toxicity?

Back 9

Alkylating agents (cross BBB)

Brain tumors (glioblastoma)

Pulmonary fibrosis, CNS toxicity

Front 10

General MoA of antimetabolites?

Back 10

compete w/ or ↓ synthesis of DNA nucelotides (purine or pyramidine) → S PHASE SPECIFIC

Front 11

Common SE of Antimetabolites?

Back 11

myelosuppression, mouth sore

Front 12

Methotrexate

MoA?
Toxicity?
How to rescue?

Back 12

Antimetabolite: (-)DHFR (folate to THF) → ↓ THF → ↓ thymine (pyramidine)

Liver irritation

Leucovorin (gives a substrate after DHFR block to restore THF)

Front 13

5-fluoruracil (5-FU)

MoA?
What ↑ toxicity?

Back 13

Antimetabolite: (-) thymidylate synthase → ↓ thymine (pyramidine)

DPD deficiency (DPD normally metabolizes 5-FU)

Front 14

Cytarabine (Ara-C)

MoA?
Use?
Toxicity?

Back 14

Pyrimidine analog (cystosine)

7 in 7+3 tx of AML

CNS toxicity (Cerebellar)

Front 15

Cladribine

MoA?
Use?
Toxicity?

Back 15

Antimetabolite: Purine analog (Adenine)

CLL

Immunosuppression (fungal, reactivate VZV)

Front 16

6-Mercaptopurine (6-MP)

MoA?
Use?
Toxicity?

Back 16

Antimetabolite: Purine analog (Guanine)

ALL

Hepatic Venoocclusive Disease, tumor lysis

Front 17

Azacitidine & Decitabine

MoA?
Use?

Back 17

Antimetabolite: (-)methyltransferase → demethylates tumor suppressor genes → ↑ tumor suppression

MDS

Front 18

Hydroxyurea

MoA? (2)
Use?
Toxicity?

Back 18

Antimetabolite: (-)Ribonucleotide reductase → ↓ deoxyribonucleotides ----- MPD
↑ HbF ------Sickle cell anemia

Infertility, skin ulcers

Front 19

Thalidomide, Lenalidomide (-omide)

Use?
Toxicity?

Back 19

5q MDS

Peripheral neuropathy, blood clot, teratogen

Front 20

Glucocorticoid

MoA?
toxicity?

Back 20

lysis of lymphoid cells

Weight gain, ulcers, immunosuppression

Front 21

Cisplatin

MoA?
Toxicity?

Back 21

Platinum Analogue: crosslinks DNA → prevent separation for transcription

Renal& hearing loss

Front 22

Daunorubicin

MoA?
Use?
Toxicity?

Back 22

Anthracycline: Topoisomerase 2 inhibitor (DNA intercalating agent) → S PHASE SPECIFIC

3 in 7+3 for AML

cardiac dysfunction

Front 23

Topotecan (-tecan)

MoA?
Use?

Back 23

Topoisomerase 1 (-) → S PHASE SPECIFIC

Ovarian cancer, small cell lung cancer

Front 24

Bleomycin

MoA?
Toxicity?

Back 24

Free radicals → bind dsDNA → G2 PHASE SPECIFIC

Front 25

Vincristine, Vinblastine (Vin-)

MoA?
Toxicity?

Back 25

Anti-microtubule: Vinca alakloids -- bind microtubules → (-)formation of mitotic spindle → M-PHASE SPECIFIC

Peripheral neuropathy

Front 26

Paclitaxel (-taxel)

MoA?
Toxicity?

Back 26

Anti-microtubule: Taxanes-- block microtubule dissociation → M-PHASE SPECIFIC

Peripheral neuropathy

Front 27

Tamoxifen

MoA?
Use?
Toxicity?

Back 27

Selective estrogen response modulator (SERM) → (-) ER on breast, + (ER) on endometrium

ER+ breast cancer

↑ risk of endometrial cancer, Thrombosis

Front 28

Anastrozole

MoA?
Use?
Toxicity?

Back 28

aromatase inhibitor: Block conversion of adrenal androgen to estradiol (post-menopause)

ER+ breast cancer

↑ risk of osteoporosis

Front 29

Fulverstrant

MoA?
Use?
Toxicity?

Back 29

estrogen receptor downregulator

ER+ breast cancer after tamoxifen and anastrozole stops working

Front 30

Leuprolide

MoA?
Use?
Toxicity?

Back 30

LHRH analog (from hypothalamus) -- long term stim by hypothalamus instead of pulsatile → pituitary

ER+ breast cancer

Prostate cancer (men) by ↓ T → ↓ DHT

Front 31

Flutamide

MoA?
Use?

Back 31

block binding of androgens to tissues

Prostate Cancer

Front 32

Ketoconazole

MoA?
Use?

Back 32

(-) Adrenal glands → androgens (must use corticosteroid replacement)

Prostate cancer

Front 33

What drugs are used for HL?

Back 33

ABVD

Adriamycin (aka doxorubicin)
Bleomycin
Vinbalastine
Dacarbazine

Front 34

What drugs used for NHL?

Back 34

R-CHOP

Rituximab
Cyclophosphamide
Hydro-Doxyrubicin
Oncovin (Vincristine)
Prednisone

Front 35

MoA Monoclonal Ig?

Intra or extracellular?

Back 35

Targeted therapy: Extracellular target (don’t cross membrane)

1.cytotoxicity (+effector cell -- NK or monocyte)
2. + complement

Front 36

Rituximab

MoA?
Use?

Back 36

monoclonal Ig → CD20

NHL

Front 37

Trastuzumab

MoA?
Use?

Back 37

Monoclonal Ig → Her2/NEU (GF-receptor)

Cardiomyopathy, breast, gastric

Front 38

Cetuximab

MoA?
Use?

Back 38

Monoclonal Ig → EGFR (GF-receptor)

Lung, colon, head, neck

Front 39

Bevacizumab

MoA?
Use?

Back 39

Monoclonal Ig → VEGF (angiogenesis)

Colon, lung, brain, renal cell cancer

Front 40

MoA Small molecules?

Intra or extracellular?

Back 40

Targeted therapy: Intracellular target (cross membrane)

Front 41

Imatinab

MoA
Use?
Toxicity?

Back 41

small molecule → (-) Phl chromosome (BCR-ABL) (tyrosine Kinase)

CML

Edema, anemia, hepatotoxicity

Front 42

Bortezamib

MoA
Use?

Back 42

small molecule → (-)26S proteasome (cleaves ubiquited proteins for apoptosis)/