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First Aid Pharmacology > Oncology Drugs > Flashcards

Oncology Drugs Flashcards

1
Q

Cancer Drugs Targeting Nucleotide Synthesis

A

MTX, 5-FU (thymidine synthesis)
6-MP (de novo purine synthesis)
Hydroxyurea (inhibits ribonucleotide reductase)

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2
Q

Cancer Drugs Targeting DNA

A

Crosslink DNA: alkylating agents, cisplatin
DNA strand breaks: Bleomycin
Intercalate DNA: Dactinomycin, doxorubicin
Topo II inhibitor: Etoposide
Topo I inhibitor: Irinotecan

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3
Q

Cancer Drugs Targeting Cell Division

A

Vinca alkaloids: inhibit microtubule formation

Paclitaxel; inhibits microtubule disassembly

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4
Q

Cell Cycle Independent Drugs

A 
Platinum agents (cisplatin)
Alkylating agents (busulfan, cyclophosphamide, ifosfamide, nitrosoureas (carmustine))
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5
Q

Antimetabolites (S phase specific - DNA synthesis)

A

Azathioprine, cladribine, cytarabine, 5-FU, hydroxyurea, methotrexate, 6-MP

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6
Q

Topoisomerase Inhibitors (inhibits S -DNA synthesis & G2 - repair checkpoint)

A

Etoposide, Teniposide, Irinotecan, Topotecan

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7
Q

G2 phase specific - repair checkpoint

A

Bleomycin

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8
Q

Microtubule Inhibitors (M phase specific)

A

Paclitaxel, Vinblastine, Vincristine

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9
Q

Azathioprine, 6-mercaptopurine

A

Purine (thiol) analogs (inhibit de novo synthesis)
Activated by HGPRT; Azathioprine is metabolized into 6-MP
CU: prevent organ rejection, RA, IBD, SLE, weaning off steroids in chronic dz, Tx steroid-refractory chronic dz
AE: myelosuppression, GI, liver
Metabolized by xanthine oxidase = increased toxicity with allopurinol or febuxostat

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10
Q

Cladribine

A

Purine analog w/multiple mechanisms:
inhibits DNA pol & DNA strand breaks
CU: Hairy cell leukemia
AE: Myelosuppression, nephrotoxic & neurotoxic

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11
Q

Cytarabine (arabinofuranosyl cytidine)

A

Pyrimidine analog - inhibits DNA pol
CU: Leukemias (AML), lymphomas
AE: Myelosuppression w/megaloblastic anemia
CYTarabine causes panCYTopenia

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12
Q

5-fluorouracil

A

Pyrimidine analog bioactivated to 5-FdUMP - covalently complexes folic acid and then inhibits thymidylate synthase (decreases dTMP / DNA synthesis)
EFFECTS ENHANCED w/LEUCOVORIN (folinic acid)
CU: colon & pancreatic cancer, topical for basal cell carcinoma
AE: myelosuppression - worse w/leucovorin

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13
Q

Methotrexate

A

Folic acid analog - competitively inhibits dihydrofolate reductase (decreases dTMP / DNA synthesis)
CU: Cancers: leukemias (ALL), lymphomas, chorioca, sarcoma. Non-neoplastic: ectopic pregnancy, abortion (w/misoprostol), RA, psoriasis, IBD, vasculitis
AE: Myelosuppression; reversible w/leucovorin “rescue”
Hepatotoxic, mucositis (mouth ulcers), pulmonary fibrosis

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14
Q

Anti-tumor Antibiotics

A

Bleomycin, Dactinomycin (actinomycin D), Doxorubicin, Daunorubicin

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15
Q

Alkylating Agents

A

Busulfan, Cyclophosphamide/ifosfamide, Nitrosureas (carmustine, lomustine, semustine, streptozocin)

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16
Q

Microtubule Inhibitors

A

Paclitaxel (other taxols), Vincristine, Vinblastine

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17
Q

Bleomycin

A

Induces free radical formation - breaks in DNA strands
CU: testicular cancer, Hodgkin lymphoma
AE: pulmonary fibrosis, skin hyperpigmentation, minimal myelosuppression

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18
Q

Dactinomycin

A

Intercalates DNA
CU: Wilms tumor, Ewing sarcoma, rhabdomyosarcoma - used for childhood tumors (kids ACT out dACTinomycin)
AE: myelosuppresion

19
Q

Doxorubicin, Daunorubucin

A

Generate free radicals - intercalate DNA - breaks
CU: solid tumors, leukemias, lymphomas
AE: Cardiotoxicity (dilated CM), myelosuppression, alopecia
Dexrazoxane (iron chelating agent) used to prevent cardiotoxicity

20
Q

Busulfan

A

Cross-links DNA
CU: CML, ablate pt’s bone marrow before BM transplant
AE: severe myelosuppression (always), pulmonary fibrosis, hyperpigmentation

21
Q

Cyclophosphamide, Ifosfamide

A

Crosslink DNA at guanine N-7
Require bioactivation by liver
CU: solid tumors, leukemias, lymphomas
AE: Myelosuppression, hemorrhagic cystitis (prevent w/mesna which binds toxic metabolites or N-acetylcysteine)

22
Q

Nitrosureas (Carmustine, Lomustine, Semustine, Streptozocin)

A

Bioactivated; Cross BBB - crosslink DNA
CU: Brain tumors (including glioblastoma multiforme)
AE: CNS toxicity (convulsions, dizziness, ataxia)

23
Q

Paclitaxel, other taxols

A

Hyperstabilizes microtubules in M phase - mitotic spindle cannot break down for anaphase
CU: ovarian & breast carcinomas
AE: myelosuppression, neuropathy, hypersensitivity

24
Q

Vincristine, Vinblastine

A

Vinca alkaloids - bind B-tubulin to inhibit polymerization into microtubules - prevents mitotic spindle formation (M phase arrest)
CU: solid tumors, leukemias,
Hodgkin (blastine) & non-Hodgkin (cristine) lymphomas
AE: Vincristine: neurotoxicity (areflexia, peripheral neuritis), constipation (paralytic ileus)

25
Q

Cisplatin, Carboplatin

A

Crosslink DNA
CU: testicular, bladder, ovary & lung ca.
AE: nephro/ototoxicity
Prevent nephrotoxicity w/AMIFOSTINE (free radical scavenger) & chloride (saline) diuresis

26
Q

Etoposide, Teniposide

A

Topo II inhibitors = DNA degradation
CU: solid tumors (testicular & small cell lung ca), leukemias, lymphomas
AE: myelosuppression, alopecia

27
Q

Irinotecan, Topotecan

A

Topo I inhibitors = prevent DNA unwinding/replication
CU: colon cancer (irinotecan), ovarian & small cell lung ca (topotecans)
AE: severe myelosuppression, diarrhea

28
Q

Hydroxyurea

A

Inhibits ribonucleotide reductase - decrease DNA synthesis (S phase specific)
CU: melanoma, CML, sickle cell dz (increases HbF)
AE: severe myelosuppresion

29
Q

Prednisone, Prednisolone

A

Bind intracytoplasmic steroid R - alter gene txn
CU: most commonly used GC in chemo. CLL, non-Hodgkin lymphoma. Also used in AI dz.
AE: Cushing-like Sx’s: wt gain, central obesity, muscle breakdown, cataracts, acne, osteoporosis, HTN, peptic ulcers, hyperglycemia, psychosis

30
Q

Bevacizumab

A

Monoclonal Ab against VEGF - inhibits angiogenesis
CU: solid tumors (CRC, RCC)
AE: hemorrhage, blood clots, impaired wound healing

31
Q

Erlotinib

A

EGFR tyrosine kinase inhibitor
CU: non-small cell lung cancer
AE: rash

32
Q

Cetuximab

A

Monoclonal Ab against EGFR
CU: Stage IV CRC (wild-type KRAS), head/neck cancer
AE: rash, elevated LFTs, diarrhea

33
Q

Imatinib

A

TK inhibitor of BCR-ABL (Philadelphia chrom in CML) and c-kit (GI stromal tumors)
CU: CML, GI stromal tumors
AE: fluid retention

34
Q

Rituximab

A

Monoclonal Ab against CD20 (B-cell cancers)
CU: Non-Hodgkin lymphoma, CLL, ITP, RA
AE: progressive multifocal leukoencephalopathy

35
Q

Tamoxifen, Raloxifene

A

Selective estrogen R modulators (SERMs)
R antagonist in breast; agonist in bone
Block estrogen binding in ER+ cells
CU: Breast cancer (tamoxifen only); Osteoporosis (raloxifene)
AE: Tamo- partial agonist endometrium (endometrial cancer, “hot flashes”); Ralo- (antagonist in endometrium, no increase in cancer risk)
Both increase thromboembolism (DVT, PE)

36
Q

Trastuzumab

A

“Herceptin” Ab against HER-2 (c-erbB2) TK receptor.
Inhibits HER2 signaling in tumor cells overexpressing it.
Also induces Ab-dependent cytotoxicity of tumor cells
CU: Breast & gastric cancer (tras2zumab)
AE: Cardiotoxicity (Heart-ceptin damages the heart)

37
Q

Vemurafenib

A

Small molecule inhibitor of BRAF oncogene + melanoma
VEmuRAF-enib = V600E-mutated BRAF inhibition
CU: metastatic melanoma

38
Q

Ototoxicity & nephrotoxicity

A

Cisplatin/Carboplatin

- acoustic nerve damage

39
Q

Peripheral neuropathy

A

Vincristine

40
Q

Pulmonary Fibrosis

A

Busulfan, Bleomycin, MTX

41
Q

Cardiotoxicity

A

Doxorubicin (Dexrazoxane (iron chelating agent)), Trastuzumab

42
Q

Hemorrhagic cystitis

A

Cyclophosphamide (prevent w/mesna which binds toxic metabolites or N-acetylcysteine)

43
Q

Myelosuppression

A

5-FU, 6-MP, MTX

First Aid Pharmacology (6 decks)

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