Chemotherapy II: Alkylating Agents Flashcards Preview

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Flashcards in Chemotherapy II: Alkylating Agents Deck (57):
1

What do the alkylating agents alkylate?

N-7 of guanine

2

Resistance in alkylating agents is due to:

Enhanced DNA repair
Binding to sulfar containing molecules

3

Bis(chloroethyl)aminea (2)

Cyclophosphamide
Ifosfamide

4

Cyclophosphamide MOA

Bifunctional alkylater: intrastrand cross link or interstrand cross link; DNA replication impaired

5

Cyclosphosphamide activation

In the liver (P-450 oxidase)

6

Cyclosphosphamide SE

Nausea, vomiting, hair loss, myelosupression

HEMATURIA (phosphoramide mustard is irritating)

7

How can you decrease hematuria associated with Cyclosphosphamide?

Give drug in morning, frequent urination, maintain hydration

8

Cyclosphosphamide Indication

breast cancer
NON-HODGKIN's LYMPHOMA (diffuse large B cell)

9

Ifosfamide

Bischloroethylamine

1/5 alkylating ability of Cyclosphosphamide

MUCH HIGHER DOSE required

10

Ifosfamide SE

Blood in Urine
*Must give Mesna (uroprotectant)*

Lethargy, confusion

MYELOSUPPRESSION= d-l

11

Mesna

Monomer binds metabolites in urine, eliminates hematuria of Ifosfamide

12

Ifosfamide Indication

Sarcoma
Testicular cancers

13

Temozolomide

Monofunctional alkylating agent

14

Temozolomide MOA

Methylates DNA

15

Temozolomide SE

Myelosuppression, nausea, vomiting, hair loss

16

What must you give to a patient that is on Temozolomide for a prolonged period?

Prophylaxis for PCP (PJP) pneumonia

17

Temozolomide Indication

Primary brain tumors
(glioblastoma)

18

Platinum (Pt) Coordination Compounds MOA

Undergo sequential aquation reactions

aquated species = DNA reactive species

Covalently bind DNA at N7 of adenine and guanine

19

Platinum (Pt) Coordination Compounds

Cisplatin
Carboplatin
Oxaliplatin

20

Cisplatin SE

NEPHROTOXIC = d-l
*give with saline hydration and mannitol diuresis

emetogenic, neuropathy, hypomagnesemia, high frequency hearing loss

21

What should you check in a patient taking Cisplatin?

Mg levels

22

What should you co-administer with Cisplatin?

Saline hydration and mannitol diuresis

23

Cisplatin Indication

Curative in TESTICULAR CANCER

lung, ovary, head, neck, bladder cancer

24

What type of patient should not receive cisplatin?

CHF, renal insufficiency

Must be able to tolerate fluid load

25

Why is Cisplatin difficult to administer

Patient has to be in clinic for a very long time

26

Is Carboplatin nephrotoxic?

NO!

27

Carboplatin dose-limiting SE

MYELOSYPPRESSION

28

If a patient is resistant to cisplatin, can you give carboplatin instead?

NO! Cross resistant

29

Can you give carboplatin to a patient on dialysis?

YES! Easier to give!

30

Carboplatin indications

Same activity as cisplatin

31

Oxiplatin indication

COLORECTAL CANCER

32

Oxiplatin dose-limiting SE

MYELOSUPPRESSION

33

Oxiplatin SE (others)

Vein irritant (portacath)

Acute cold induced neuropathy

Chronic sensory neuropathy

34

Plant Alkaloids

Vincristine, Vinblastine, Taxol, Etoposide

35

Which of the plant alkaloids are cell cycle specific?

Vincristine, Vinblastine, Taxol

36

Which of the plant alkaloids inhibit mitotic spindle formation

Vincristine, Vinblastine

37

Which of the plant alkaloids inhibits the breakdown of the mitotic spindle?

Taxol

38

Which of the plant alkaloids inhibits topoisomerase II?

Etoposide

39

Vincristine MOA

Prevents polymerization of tubulin
Cell cyle specific (M-phase)

40

In which patients should you lower the dose of Vincristine?

Pts with elevated bilirubin (excreted in the bile)

41

Vincristine dose-limiting SE

NEUROPATHY
(loss of ankle jerk reflexes, N/T in fingers)

42

Does vincristine cause myelosuppresion?

NO!

43

Vincristine indications

Lymphoma, Hodgkin's disease, Lymphoblastic leukemia

44

What are the differences between vincristine and vinblastine?

Vinblastin is less neurotoxic but causes more myelosuppression

45

Paclitaxel = Taxol MOA

Cell cycle specific (M-phase)
Prevents tubulin disassembly

46

In which patients should you dose reduce Taxol

Hepatic dysfunction

47

Taxol SE

Myelosuppression, hair loss, nausea, vomiting, stomatitis, peripheral sensory neuropathy, myalgias, arthralgias

*Premedicate to prevent allergic reactions

48

Carbotaxol = Carboplatin + taxol

Use to treat lung cancer, ovarian cancer, GE junction cancer

49

Taxol Indication

OVARIAN, LUNG, GASTROESOPHAGEAL, BREAST cancers

50

Docetaxel indication

prostate cancer

51

Albumin bound paclitaxel benifits

No allergic reactions
Less myelosuppression
Less neuropathy

52

Carbaxitaxel indication

Prostate cancer

53

Etoposide MOA

Cell cycle specific (G1-S phase)
Inhibits topoisomerase II
Double strand DNA breaks

54

Etoposide SE

Nausea, vomiting, hair loss
MYELOSUPPRESSION = d-l

55

What is the total dose you can give of Etoposide

2 gm/M^2
LEUKEMOGENIC

56

Who should you dose reduce etoposide in?

Renal/hepatic dysfunction

57

Etoposide Indication

TESTICULAR, lung cancer (small cell), lymphomas