2. Chemo Pharmacology 1 Flashcards

1
Q

What are the chemotherapy categories?

A
  • Alkylating agents
  • Antimetabolites
  • Microtubule Targeting Agents
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2
Q

What are the alkylating agents?

A
  • nitrogen mustards
  • nitrosureas
  • heavy metals
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3
Q

What are the antimetabolite agents?

A
  • fluorinated pyrimidines
  • cytidine analogs
  • purine and purine metabolites
  • antifolates
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4
Q

What are the microtubule targeting agents?

A
  • vinca alkyloids
  • taxanes
  • topoisomerase targeting drugs
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5
Q

What are the topoisomerase targeting drugs?

A
  • Topo I - camptothecins

- Topo II - etoposide/anthracene

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6
Q

To what class does cyclophosphamide belong?

A

traditional alkylating agent

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7
Q

What conditions does cyclophosphamide have activity against?

A
  • leukemias
  • Hodgkin’s disease
  • Non-Hodgkin’s lymphoma
  • breast cancer
  • endometrial cancer
  • sarcomas
  • other less common tumors
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8
Q

What is the dose of cyclophosphamide?

A

1-5 mg/kg/day daily PO
10-50 mg/kg weekly IV
3-4 gm/m² IV x 1

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9
Q

What are the toxicities of cyclophosphamide?

A
  • hemorrhagic cysitis
  • NV
  • myelosuppression
  • neutropenia
  • SIADH
  • alopecia
  • sterility
  • secondary malignancies
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10
Q

How are cyclophosphamide toxicities prevented?

A
  • antiemetics
  • hydration +/- Mesna (high dose - transplant)
  • take oral tablets in the morning
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11
Q

Cyclophosphamide is a prodrug. (T/F)

A

True

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12
Q

Cyclophosphamide is activated by what hepatic enzyme?

A

cytochrome P450

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13
Q

What is cyclophosphamide metabolized into?

A

4-hydroxycyclophosphamide

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14
Q

With cyclophosphamide administration, the WBC nadir occurs when?

A

at 10-14 days

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15
Q

What is the WBC nadir?

A

the lowest point of a patients WBC - highest risk of infection

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16
Q

With cyclophosphamide administration, how long does it take for WBC to recover?

A

22-39 days

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17
Q

What causes hemorrhagic cystitis?

A

metabolite acrolein

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18
Q

When cyclophosphamide is given in clinic, patients must be advised of what?

A

maintain good fluid intake and empty bladder often

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19
Q

To what class does cisplatin belong?

A

non-traditional alkylating agent

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20
Q

What conditions does cisplatin have activity against?

A
  • lung cancer
  • testicular cancer
  • ovarian cancer
  • head and neck cancer
  • endometrial cancer
  • bladder cancer
  • other less common tumors
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21
Q

What are the toxicities of cisplatin?

A
  • severe NV
  • renal failure
  • hypomagnesemia
  • hypokalemia
  • ototoxicity
  • neurotoxicity (peripheral neuropathy)
  • anemia (chronic dosing)
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22
Q

Cisplatin is highly myelosuppressive. (T/F)

A

False, it is generally not highly myelosuppressive.

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23
Q

How can toxicity with cisplatin be prevented?

A
  • pre and post hydration with NaCl containing fluid +/- magnesium and mannitol
  • antiemetics
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24
Q

What does cisplatin precipitate with?

A

aluminium

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25
Q

What other drugs should be avoided with cisplatin use?

A

other nephrotoxic or ototoxic medication

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26
Q

At what SCr should you hold cisplatin dose?

A

> 1.5 mg/dL

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27
Q

At what CrCl should you hold cisplatin dose?

A

< 60 mL/min

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28
Q

At what platelet count should you hold cisplatin dose?

A

< 100,000

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29
Q

At what WBC should you hold cisplatin dose?

A

< 4000 cells

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30
Q

At what ANC should you hold cisplatin dose?

A

< 1000 cells

31
Q

To what class does carboplatin belong?

A

non-traditional alkylating agent

32
Q

What conditions does carboplatin have activity against?

A
  • lung cancer
  • testicular cancer
  • ovarian cancer
  • head and neck cancer
  • endometrial cancer
  • other less common tumors
33
Q

What is the one cancer that cisplatin has activity against that carboplatin doesn’t?

A

bladder cancer

34
Q

What formula is used to calculate the carboplatin dose?

A

Calvert formula

35
Q

What is the Calvert formula?

A

Dose (mg) = (target AUC) x (GFR + 25)

36
Q

What is the target AUC for a patient who has had prior treatment with carboplatin or is using multiple agents?

A

AUC 4-6

37
Q

What is the target AUC for a patient who has not been previously treated and is using carboplatin as a single agent?

A

AUC 6-8

38
Q

What are the toxicities of carboplatin?

A
  • myelosuppression
  • thrombocytopenia
  • neutropenia
  • anemia
  • NV (moderate - some delayed)
  • hypersensitivity reaction
39
Q

How are carboplatin toxicities prevented?

A

antiemetics

40
Q

At what CrCl should the carboplatin dose be reduced?

A

< 60 mL/min if using mg/m² dosing

41
Q

To what category does Gemcitabine belong?

A

S phase antimetabolite

42
Q

What is the MOA of Gemcitabine?

A
  • incorporated into DNA
  • inhibits DNA synthesis
  • ribonucleotide reductase inhibitor
  • prevents DNA chain elongation
43
Q

What cancers does Gemcitabine have activity against?

A
  • pancreatic
  • lung
  • breast
  • head and neck
  • bladder
  • testicular
  • ovarian
44
Q

What are the toxicities associated with Gemcitabine?

A
  • melosuppression: neutropenia
  • thrombocytopenia
  • flu-like syndrome
  • ↑ LFTs
  • NV
45
Q

What toxicities of Gemcitabine can be prevented?

A
  • NV: antiemetics
46
Q

With Gemcitabine administration, the WBC nadir occurs when?

A

10-14 days

47
Q

Neutrophil nadir is severe with Gemcitabine administration when what occurs?

A

infusions > 1 hour

48
Q

Gemcitabine associated rash can be treated with what?

A

topical steroids

49
Q

Gemcitabine associated fever can be treated with what?

A

acetaminophen

50
Q

To what class does 5-FU/Capecitabine belong?

A

S phase antimetabolite

51
Q

What is the MOA of 5-FU/Capecitabine?

A
  • FU to F-dUMP inhibits T.S.
  • incorporated into RNA
  • terminates elongation
52
Q

What cancers does 5-FU/Capecitabine have activity against?

A
  • breast
  • colon and rectal
  • GI
  • head and neck
  • esophageal
  • pancreatic
  • cervical
53
Q

What toxicities are associated with 5-FU/Capecitabine?

A
  • mucositis
  • NVD
  • myelosuppression
  • neurotoxicity
  • dermatologic (rash)
  • photosensitivity
  • hand-foot syndrome
  • ocular
  • cardiac
54
Q

What toxicities of 5-FU/Capecitabine can be prevented?

A

NV: antiemetics

55
Q

5-FU is the prodrug formulation. (T/F)

A

False: Capecitabine is the oral prodrug formulation

56
Q

With 5-FU/Capecitabine administration, the WBC nadir occurs when?

A

10 - 14 days

57
Q

What is the topical 5-FU formula and when is it used?

A

Effudex → skin cancers

58
Q

What counseling points should be stressed with Effudex?

A

patient must wash hands after application

59
Q

To what category does Vincristine belong?

A

Natural product: microtubule targeting

60
Q

What cancers does Vincristine have activity against?

A
  • leukemias
  • lymphomas
  • sarcomas
  • lung
  • uncommon tumors
61
Q

What are the toxicities associated with Vincristine?

A
  • peripheral neuropathy: motor sensory
  • autonomic (paresthesias, paralytic iliac, urinary retention, facial palsies)
  • SIADH
  • NV
  • vesicant
62
Q

How can toxicities associated with Vincristine be prevented?

A

monitoring

63
Q

Through which route can Vincristine NOT be given?

A

intrathecal

64
Q

Why could the maximum dose of Vincristine be reduced and what would it be reduced to?

A
  • high bilirubin

- 2 mg

65
Q

To what class does Vinorelbine belong?

A

Natural product: microtubule targeting

66
Q

What cancers does Vinorelbine have activity against?

A
  • lung
  • breast
  • prostate
  • Hodgkin’s lymphoma
  • ovarian
  • less common tumors
67
Q

What are the toxicities associated with Vinorelbine?

A
  • myelosuppression: neutropenia
  • NV
  • peripheral neuropathy
  • constipation
  • low back pain
  • vesicant
  • phlebitis
  • alopecia uncommon
68
Q

How can toxicities associated with Vinorelbine be prevented?

A

NV: antiemetics

69
Q

Dose of Vinorelbine should be reduced due to what lab value?

A

elevated bilirubin

70
Q

Through which route can Vinorelbine NOT be given?

A

intrathecal

71
Q

With Vinorelbine administration, the WBC nadir occurs when?

A

7-10 days

72
Q

How long does it take for WBCs to recover after Vinorelbine administration?

A

7-14 days

73
Q

What are the drug interactions with Vinorelbine?

A
  • phenytoin (↓ levels)

- erythromycin (↑ Vinorelbine levels)