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Pharm > Chemotherapy II: Alkylating Agents > Flashcards

Chemotherapy II: Alkylating Agents Flashcards

1
Q

What do the alkylating agents alkylate?

A

N-7 of guanine

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2
Q

Resistance in alkylating agents is due to:

A

Enhanced DNA repair

Binding to sulfar containing molecules

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3
Q

Bis(chloroethyl)aminea (2)

A

Cyclophosphamide

Ifosfamide

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4
Q

Cyclophosphamide MOA

A

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

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5
Q

Cyclosphosphamide activation

A

In the liver (P-450 oxidase)

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6
Q

Cyclosphosphamide SE

A

Nausea, vomiting, hair loss, myelosupression

HEMATURIA (phosphoramide mustard is irritating)

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7
Q

How can you decrease hematuria associated with Cyclosphosphamide?

A

Give drug in morning, frequent urination, maintain hydration

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8
Q

Cyclosphosphamide Indication

A

breast cancer

NON-HODGKIN’s LYMPHOMA (diffuse large B cell)

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9
Q

Ifosfamide

A

Bischloroethylamine

1/5 alkylating ability of Cyclosphosphamide

MUCH HIGHER DOSE required

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10
Q

Ifosfamide SE

A

Blood in Urine
Must give Mesna (uroprotectant)

Lethargy, confusion

MYELOSUPPRESSION= d-l

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11
Q

Mesna

A

Monomer binds metabolites in urine, eliminates hematuria of Ifosfamide

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12
Q

Ifosfamide Indication

A

Sarcoma

Testicular cancers

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13
Q

Temozolomide

A

Monofunctional alkylating agent

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14
Q

Temozolomide MOA

A

Methylates DNA

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15
Q

Temozolomide SE

A

Myelosuppression, nausea, vomiting, hair loss

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16
Q

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

A

Prophylaxis for PCP (PJP) pneumonia

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17
Q

Temozolomide Indication

A

Primary brain tumors

glioblastoma

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18
Q

Platinum (Pt) Coordination Compounds MOA

A

Undergo sequential aquation reactions

aquated species = DNA reactive species

Covalently bind DNA at N7 of adenine and guanine

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19
Q

Platinum (Pt) Coordination Compounds

A

Cisplatin
Carboplatin
Oxaliplatin

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20
Q

Cisplatin SE

A

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

emetogenic, neuropathy, hypomagnesemia, high frequency hearing loss

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21
Q

What should you check in a patient taking Cisplatin?

A

Mg levels

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22
Q

What should you co-administer with Cisplatin?

A

Saline hydration and mannitol diuresis

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23
Q

Cisplatin Indication

A

Curative in TESTICULAR CANCER

lung, ovary, head, neck, bladder cancer

24
Q

What type of patient should not receive cisplatin?

A

CHF, renal insufficiency

Must be able to tolerate fluid load

25
Q

Why is Cisplatin difficult to administer

A

Patient has to be in clinic for a very long time

26
Q

Is Carboplatin nephrotoxic?

A

NO!

27
Q

Carboplatin dose-limiting SE

A

MYELOSYPPRESSION

28
Q

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

A

NO! Cross resistant

29
Q

Can you give carboplatin to a patient on dialysis?

A

YES! Easier to give!

30
Q

Carboplatin indications

A

Same activity as cisplatin

31
Q

Oxiplatin indication

A

COLORECTAL CANCER

32
Q

Oxiplatin dose-limiting SE

A

MYELOSUPPRESSION

33
Q

Oxiplatin SE (others)

A

Vein irritant (portacath)

Acute cold induced neuropathy

Chronic sensory neuropathy

34
Q

Plant Alkaloids

A

Vincristine, Vinblastine, Taxol, Etoposide

35
Q

Which of the plant alkaloids are cell cycle specific?

A

Vincristine, Vinblastine, Taxol

36
Q

Which of the plant alkaloids inhibit mitotic spindle formation

A

Vincristine, Vinblastine

37
Q

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

A

Taxol

38
Q

Which of the plant alkaloids inhibits topoisomerase II?

A

Etoposide

39
Q

Vincristine MOA

A

Prevents polymerization of tubulin

Cell cyle specific (M-phase)

40
Q

In which patients should you lower the dose of Vincristine?

A

Pts with elevated bilirubin (excreted in the bile)

41
Q

Vincristine dose-limiting SE

A

NEUROPATHY

loss of ankle jerk reflexes, N/T in fingers

42
Q

Does vincristine cause myelosuppresion?

A

NO!

43
Q

Vincristine indications

A

Lymphoma, Hodgkin’s disease, Lymphoblastic leukemia

44
Q

What are the differences between vincristine and vinblastine?

A

Vinblastin is less neurotoxic but causes more myelosuppression

45
Q

Paclitaxel = Taxol MOA

A

Cell cycle specific (M-phase)

Prevents tubulin disassembly

46
Q

In which patients should you dose reduce Taxol

A

Hepatic dysfunction

47
Q

Taxol SE

A

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

*Premedicate to prevent allergic reactions

48
Q

Carbotaxol = Carboplatin + taxol

A

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

49
Q

Taxol Indication

A

OVARIAN, LUNG, GASTROESOPHAGEAL, BREAST cancers

50
Q

Docetaxel indication

A

prostate cancer

51
Q

Albumin bound paclitaxel benifits

A

No allergic reactions
Less myelosuppression
Less neuropathy

52
Q

Carbaxitaxel indication

A

Prostate cancer

53
Q

Etoposide MOA

A

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

54
Q

Etoposide SE

A

Nausea, vomiting, hair loss

MYELOSUPPRESSION = d-l

55
Q

What is the total dose you can give of Etoposide

A

2 gm/M^2

LEUKEMOGENIC

56
Q

Who should you dose reduce etoposide in?

A

Renal/hepatic dysfunction

57
Q

Etoposide Indication

A

TESTICULAR, lung cancer (small cell), lymphomas

Pharm (20 decks)

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