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Heme-Onc First Aid > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

what antineoplastics act on the mitosis stage of cell cycle? what exactly do they do?

A
  • vinca alkaloids inhibit microtubule formation

- paclitaxel (trade name Taxol) inhibits microtubule disassembly

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2
Q

what antineoplastics prevent nucleotide synthesis?

A

methotrexate and 5-FU inhibit thymidine synthesis

6-mercaptopurine (6-MP) inhibits purine synthesis

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3
Q

what antineoplastics ruin existing DNA?

A
  • alkylating agents and cisplatin cross-link DNA
  • doxorubicin and dactinomycin intercalate DNA
  • etoposide inhibits topoisomerase II (which normally relieves supercoils in the DNA)
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4
Q

what exactly is methotrexate (molecule-wise) and what is it used to treat (cancer and non-cancer uses)?

A

folic acid analogue that inhibits DHF reductase; cancer uses: leukemia, lymphoma, choriocarcinoma
non-cancer uses: abortion, ectopic pregnancy, rheumatoid arthritis, psoriasis

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5
Q

what toxicities does methotrexate use cause?

A

myelosuppresion (reversed by lucovorin aka folinic acid rescue); macrovesicular fatty change in the liver; mucositis; teratogen

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6
Q

what exactly is 5-FU and what does it inhibit?

A

5F-dUMP (deoxyuridine monophosphate) analog that inhibits thymidylate synthase which normally converts dUMP to dTMP

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7
Q

what is 5-FU used to treat?

A

colon cancer, basal cell carcinoma (topical Tx)

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8
Q

what toxicities are associated with 5-FU

A

myelosuppression (not rescueable with leucovorin, must use thymidine);

photosensitivity

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9
Q

what is cytarabine and what does it treat?

A

pyrimidine analog that inhibits DNA polymerase; it is used to treat leukemias and lymphomas

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10
Q

what are the toxicities associated with cytarabine?

A

leukopenia, thrombocytopenia, megaloblastic anemia

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11
Q

name three purine analogs that are used to treat leukemias

A

6-mercaptopurine, azathioprine, 6-thioguanine

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12
Q

what toxicities are associated with 6-MP, azathioprine and 6-TG?

A

bone marrow, GI and liver toxicities; 6-MP toxicity exacerbated by allopurinol since it is metabolized by xanthine oxidase (which causes AMP and GMP accumulation by blocking their breakdown to uric acid and negatively feeding back on purine synthesis)

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13
Q

what does dactinomycin treat and what are its associated toxicities?

A

Wilm’s tumor (childhood kidney cancer), Ewing’s sarcoma (malignant bone tumor that affects children), rhabdomyosarcoma (skeletal muscle cancer that occurs in children)
toxicity=myelosuppresion

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14
Q

what do doxorubicin and daunorubicin treat and what are their associated toxicities?

A

leukemias, lymphomas and solid tumors
toxicities=dilated cardiomyopathy (Tx with dexrazoxane to prevent cardiotoxicity), myelosuppression, alopecia, toxic to tissues following extravasation

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15
Q

what is bleomycin used to treat and how does it work

A

testicular cancer, Hodgkin’s lymphoma; it introduces free radicals which cause breaks in DNA strands

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16
Q

what toxicities are associated with bleomycin?

A

pulmonary fibrosis, skin changes (minimal myelosuppression)

17
Q

name some alkylating agents used to treat cancers?

A

cyclophosphamide, ifosfamide, nitrosureas (carmustine, lomustine, semustine, streptozocin), busulfan

18
Q

what are cyclophoshamide and ifosfamide (cross-link DNA at guanine) used to treat? what are their toxicities?

A

solid tumors, leukemia, lymphomas and some brain cancers

toxicities=myelosuppression, hemorrhagic cystitis (can partially be prevented by mesna)

19
Q

what are nitrosureas (carmustine, lomustine, semustine and streptozocin) used to treat? what are their toxicities?

A

brain tumors;

CNS toxicities like dizziness and ataxia

20
Q

what is busulfan used to treat and what are its associated toxicities?

A

CML and bone marrow ablation before transplant

toxicities=pulmonary fibrosis and hyperpigmentation

21
Q

vincristine and vinblastine are vinca alkaloids that treat what cancers? what are their respective toxicities?

A

solid tumors, leukemias and lymphomas (by inhibiting microtubule formation)

vincristine causes neurotoxicity and paralytic ileus
vinblastine causes bone marrow suppression

22
Q

what does paclitaxel treat and what are its toxicities?

A

ovarian and breast carcinomas

toxicities are myelosuppression and hypersensitivity (allergy)

23
Q

what are cisplatin and carboplatin used to treat? what are their toxicities?

A

testicular, bladder, ovary and lung carcinomas

toxicities=nephrotoxicities (prevent with amifostine and chloride diuresis) and acoustic nerve damage

24
Q

what are etoposide and teniposide used to treat?

what are their toxicities?

A

solid tumors, leukemias and lymphomas

toxicities=myelosuppresion, GI irritation, alopecia

25
Q

what is hydroxyurea used to treat?

what are its toxicities?

A

melanoma, CML, sickle cell

toxicities=bone marrow suppression, GI upset

26
Q

what are prednisone and prednisolone used to treat?

what are their associated toxicities?

A

CLL, non-Hodgkin’s lymphoma, autoimmune diseases
toxicities=Cushing’s-like symptoms, immunesuppression, catarats, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis

27
Q

what is the mechanism of action of tamoxifen and raloxifene?

what are their associated toxicities?

A

selective estrogen receptor modulators: they block estrogen to estrogen receptor binding

toxicities=tamoxifen increases risk of endometrial cancer, it also causes hot flashes

28
Q

what does trastuzumab (herceptin) do?

what are its toxicities?

A

monoclonal antibody against HER-2, a tyrosine kinase involved in breast cancer

toxicities=cardiotoxicity

29
Q

how does imatinib (Gleevec) work?
what is it used to treat?
what are its associated toxicities?

A

inhibits brc-abl tyrosine kinase
used to treat CML and GI stromal tumors
toxicity=fluid retention

30
Q

how does rituximab work and what does it treat?

A

rituximab is a monoclonal antibody against CD20 (found on B cell neoplasms)
it treats non-Hodgkin’s lymphoma and rheumatoid arthritis

31
Q

what does vemurafenib treat and how does it work

A

treats metastatic melanoma;

vemurafenib is a small molecule inhibitor of B-raf kinase with V600E mutation

32
Q

how does bevacizumab work and what does it treat?

A

bevacizumab is a monoclonal antibody againt VEGF that inhibits angiogenesis;
it treats solid tumors

33
Q

which chemo drugs commonly cause nephrotoxicity and acoustic nerve damage?

A

carboplatin and cisplatin

34
Q

which chemo drugs commonly cause cardiotoxicity?

A

trastuzumab and doxorubicin

35
Q

which chemo drugs commonly cause myelosuppresion?

A

5-FU, methotrexate, 6-MP

36
Q

which chemo drug commonly causes hemorrhagic cystitis?

A

cyclophosphamide

37
Q

which chemo drugs commonly cause pulmonary fibrosis?

A

bleomycin and busulfan

38
Q

which chemo drug commonly causes peripheral neuropathy?

A

vincristine

Heme-Onc First Aid (2 decks)

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