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Drugs > Oncology > Flashcards

Oncology Flashcards

1
Q

Azathioprine

6-mercaptopurine

A

Inhibit S phase in cell cycle

MOA:
Purine analogs —> dec. de novo purine synthesis
Activated by HGPRT
Azathioprine is metabolized into 6-MP

Use:
Preventing organ rejection
Rheumatoid arthritis
IBD
SLE
Used to wean ptns off steroids in chronic disease and to treat steroid refractory chronic disease.
Adv. effects:
Myelosuppression
GI
Liver
Increased toxicity with allopurinol or febuxostat
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2
Q

Cladribine

A

Inhibit S phase in cell cycle

MOA:
Purine analong —> mult. mechanisms (inhibitin of DNA pol., DNA strand breaks)

Use: Hairy cell leukemia

Adv. effects:
Myelosuppression
Nephrotoxicity
Neurotoxicity

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3
Q

Cytarabine

A

Inhibit S phase in cell cycle

MOA: Pyrimidine analog —> inhibition of DNA polymerase

Use:
Leukemias (AML)
Lymphomas

Adv. effects:
Myelosuppression w/ megaloblastic anemia

“CYTarabine causes panCYTopenia”

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4
Q

5-fluorouracil

A

Inhibit S phase in cell cycle

MOA:
Pyrimidine analog bioactivated to 5-FdUMP
5-FdUMP covalently complexes folic acid
Complex inhibits thymidylate synthase —> dec. dTMP —> dec. DNA synthesis

Use:
Colon cancer
Pancreatic cancer
Basal cell carcinoma (topical)

Effects enhanced with the addition of leucovorin

Adv. effects:
Myelosuppresion - worsened with add. of leucovorin (folinic acid)

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5
Q

Methotrexate

A

Inhibit S phase in cell cycle

MOA:
Folic acid analog that competitively inhibits diydrofolate reductase –> dec. dTMP —> dec. DNA synthesis

Use:
Cancers - leukemias (ALL), lymphomas, choriocarcinoma, sarcomas
Non neoplastic - ectopic pregnancy, medical abortion (w/misoprostol), rheumatoid arthritis, psoriasis, IBD, vasculitis

Adv. effects:
Myelosuppression - reversible with leucovorin "rescue"
Hepatotoxicity
Mucositis (mouth ulcers)
Pulmonary fibrosis
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6
Q

Bleomycin

A

Inhibits G2 phase of cell cycle

MOA:
Induces free radical formation –> breaks in DNA strands

Use:
Testicular cancer
Hodgkin lymphoma

Adv. effects:
Pulmonary fibrosis
Skin hyperpigmentation
Minimal myelosuppression

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7
Q

Dactinomycin

A

MOA: Intercalates in DNA

Use:
Wilms tumor
Ewing sarcoma
Rhabdomyosarcoma
Used for childhood tumors ("children ACT out")

Adv. effects:
Myelosuppression

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8
Q

Doxorubicin, Daunorubicin

A

MOA:
Generate free radicals
Intercalate in DNA –> breaks in DNA –> dec. replication

Use:
Solid tumors
Leukemias
Lymphomas

Adv. effects:
Cardiotoxicity* (dilated cardiomyopathy)
Myelosuppression
Alopecia

Dexrazoxane - iron chelating agent; used to prevent cardiotoxicity

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9
Q

Busulfan

A

MOA: Cross links DNA

Use:
CML
Used to ablate patient’s bone marrow before bone marrow transplantation

Adverse effects:
Severe myelosuppression
Pulmonary fibrosis
Hyperpigmentation

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10
Q

Cyclophosphamide, Ifosfamide

A

MOA:
Cross-link DNA at guanine N-7
Require bioactivation by liver

Use:
Solid tumors
Leukemia
Lymphomas

Adv. effects:
Myelosuppression
Hemorrhagic cystitis (prevented w/ mesna or N-acetylcysteine)

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11
Q

Nitrosoureas

Carmustine, Lomustine, Semustine, Streptozocin

A

MOA:
Require bioactivation
Cross blood-brain barrier —> CNS
Cross link DNA

Use:
Brain tumors (including glioblastoma multiforme)
Adv. effects:
CNS toxicity (convulsions, dizziness, ataxia)
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12
Q

Paclitaxel

A

MOA:
Hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur)

Use:
Ovarian & breast carcinomas

Adv. effects:
Myelosuppression
Neuropathy
Hypersensitivity

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13
Q

Vincristine

Vinblastine

A

MOA:
Vinca alkaloids that bind B-tubulin and inhibit its polymerization into microtubules –> prevent mitotic spindle formation (M-phase arrest)

Use:
Solid tumors
Leukemias
Hodgkin lymphoma (vinblastine)
Non-Hodgkin lymphoma (vincristine)

Adv. effects:
Vincristine - neurotoxicity, constipation

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14
Q

Cisplatin

Carboplatin

A

MOA: Cross-link DNA

Use:
Testicular, bladder, ovary and lung carcinomas

Adv. effects:
Nephrotoxicity, peripheral neuropathy, ototoxicity

Prevent nephrotoxicity w/ amifostine (free radical scavenger) and chloride (saline) diuresis

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15
Q

Etoposide, Teniposide

A

MOA:
ETOPOside inhibits TOPOisomerase II –> Increases DNA degradation

Use:
Solid tumors (testicular & small cell lung cancer)
Leukemias
Lymphomas

Adv. effects:
Myelosuppression
Alopecia

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16
Q

Irinotecan, Topotecan

A

MOA:
Inhibit topoisomerase I and prevent DNA unwinding and replication.

Use:
Colon cancer (irinotecan)
Ovarian and small cell lung cancers (topotecan)

Adv. effects:
Severe myelosuppression
Diarrhea

17
Q

Hydroxyurea

A

MOA:
Inhibits ribonucleotide reductase –> dec. DNA synthesis (S-phase specific)

Use:
Melanoma
CML
Sickle cell disease (increase HbF)

Adv. effects:
Severe myelosuppression

18
Q

Prednisone, Prednisolone

A

MOA:
Bind intracytoplasmic steroid receptor
Alter gene transcription

Use:
CLL
non-Hodgkin lymphoma (part of combo regimen)
used as immunosuppressants (in autoimmmune diseases)

Adv. effects:
Cushing-like symptoms
Weight gain
Central obesity
Muscle breakdown
Cataracts
Acne
Osteoporosis
Hypertension
Peptic ulcers
Hyperglycemia
Psychosis
19
Q

Bevacizumab

A

MOA:
Monoclonal antibody against VEGF; inhibits angiogenesis

Use: 
Solid tumors (colorectal cancer, renal cell carcinoma)

Adv. effects:
Hemorrhage, blood clots, & impaired wound healing

20
Q

Erlotinib

A

MOA: EGFR tyrosine kinase inhibitor

Use: Non-small cell lung carcinoma

Adv. effects: Rash

21
Q

Cetuximab

A

MOA: Monoclonal antibody against EGFR

Use:
Stage IV colorectal cancer (wild type KRAS)
Head and neck cancer

Adv. effects:
Rash, elevated LFTs, diarrhea

22
Q

Imatinib

A

MOA:
Tyrosine kinase inhibitor of BCR-ABL (in CML) and c-kit (in GI stromal tumors)

Use:
CML
GI stromal tumors

Adv. effects:
Fluid retention

23
Q

Rituximab

A

MOA:
Monoclonal antibody against CD20 (found on most B-cell neoplasms)

Use: 
Non-Hodgkin lymphoma
CLL
ITP
Rheumatoid arthritis
24
Q

Tamoxifen, Raloxifene

A

MOA:
Selective estrogen receptor modulators - receptor antagonists in breast and agonists in bone
Block binding of estrogen to ER + cells

Use:
Breast cancer treatment (tamoxifen) & prevention
Prevent osteoporosis (Raloxifene)

Adv. effects:
Tamoxifen - partial agonist in endometrium (increases risk of endometrial cancer); hot flashes
Raloxifene - no increase in endometrial carcinoma bc it is an estrogen receptor antagonist in endometrial tissue.
Both increase risk of thromboembolic events (DVT, PE)

25
Q

Trastuzumab (Herceptin)

A

MOA:
Monoclonal antibody against HER-2 (tyrosine kinase receptor)
Helps kill cancer cells that overexpress HER-2 through inhibition of HER2-initiated cellular signaling and antibody-dependent cytotoxicity

Use:
HER-2 + breast cancer & gastric cancer

Adv. effects:
Cardiotoxicity

“Heartceptin” damages the heart

26
Q

Vemurafenib

A

MOA:
small molecule inhibitor of BRAF oncogene + melanoma
V600E-mutated BRAF inhibition

Use: Metastatic melanoma

27
Q

Cisplatin/Carboplatin toxicity?

A

Ototoxicity (acoustic nerve damage)

Nephrotoxicity

28
Q

Vincristine toxicity?

A

Peripheral neuropathy

29
Q

Bleomycin, Busulfatan toxicity?

A

Pulmonary fibrosis

30
Q

Doxorubicin toxicity?

A

Cardiotoxicity

31
Q

Trastuzumab toxicity?

A

Cardiotoxicity

32
Q

Cyclophosphamide toxicity?

A

Hemorrhagic cystitis

33
Q

5-FU toxicity?

A

Myelosuppression

34
Q

6-MP toxicity?

A

Myelosuppression

35
Q

Methotrexate toxicity?

A

Myelosuppression

Drugs (15 decks)

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