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LHT1 > Cancer chemotherapy and Anti-neoplastics--Antimitotic and G/M phase drugs > Flashcards

Cancer chemotherapy and Anti-neoplastics--Antimitotic and G/M phase drugs Flashcards

1
Q

Antimitotic drugs- classes, distinction

A
  • Vinca alkaloids- inhibit tubulin polymerization (block assembly of MTs)
  • Taxanes- enhance tubulin polymerization (stabilize MTs)
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2
Q

Vinca alkaloids- drugs

A
  • VINblastine
  • VINcristine
  • VINorelbine
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3
Q

Taxanes- drugs

A
  • TAXol

- TAXotere

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4
Q

Vinblastine- therapeutic uses

A

-testicular cancer (with bleomycin and cisplatin), lymphomas, neuroblastoma

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5
Q

Vincristine- therapeutic uses

A

-ALL (pediatric), lymphoma, neuroblastoma, Wilms tumor, Ewings sarcoma

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6
Q

Vinorelbine- therapeutic uses

A

-advanced non small cell lung cancer

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7
Q

Paclitaxel- therapeutic uses

A

-breast and ovarian (with cisplatin)

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8
Q

Docetaxel- therapeutic uses

A

-breast, ovarian

also solid tumors

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9
Q

Vincristine- dose limiting toxicity

A

-neurotoxicity, peripheral neuropathy

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10
Q

Vinca alkaloids- moa

A
  • inhibit tubulin polymerization!
  • bind to B tubulin on forming end of MTs (positive end)
  • fraying (neg end) continues- shortening MTs!!
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11
Q

Taxanes- moa

A
  • stabilize MTs!!
  • bind to B tubulin at forming end of MTs
  • taxanes reach the negative end and inhibit fraying- enhance tubulin polymerization and stabilize MTs!!!
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12
Q

Vinca alkaloids and Taxanes- what cell cycle?

A

-M phase (mitosis)

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13
Q

Antimitotic drugs- adverse effects

A
  • peripheral neuropathy- esp Vincristine!!

- Vinblastine substitutes for vincristine when neuropathy is severe

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14
Q

Antimitotic drugs- resistance

A

MDR due to inc expression of P-glycoprotein and its enhanced extrusion of drugs from tumor cell
-assoc with treatment failure!!
(cancer drugs with mechs that involve the exterior cell surface are not prone to P-glycoprotein MDR!- monoclonal ab’s)

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15
Q

opoisomerase inhibitors (cause DNA strand breaks)- classes, distinction

A
  • Epipodophyllotoxins- Topoisomerase II inhibition- DNA dbl strand breaks
  • Camptothecins- Topoisomerase I inhibition- DNA single strand breaks
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16
Q

EpipodophylloToxins- drugs

A

-Etoposide
-Teniposide
(ET)

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17
Q

Camptothecins- drugs

A
  • Irinotecan

- Topotecan

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18
Q

Etoposide- therapeutic uses

A

-oat cell carcinoma of lung, testicular cancer (with cisplatin and bleomycin)

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19
Q

Teniposide- therapeutic uses

A

-glioma and neuroblastoma

20
Q

Irinotecan- therapeutic uses

A

-metastatic colorectal cancer

21
Q

Topotecan- therapeutic uses

A

-2nd line various- failed prior first line

22
Q

Irinotecan- dose limiting toxicity

A

-severe diarrhea (can be life threatening!)

23
Q

Topoisomerase inhibitors- moa

A
  • bind to DNA-enzyme complex and create a persistently cleavable complex
  • Topoisomerase I inhibitors- S phase
  • Topoisomerase II inhibitors- Mixed
24
Q

DNA intercalation and oxidative scission drugs- class, distinction

A
  • Antibiotics- free radical generation- DNA strand breaks

- Anthracyclines- DNA intercalating agents, free radical generation

25
Q

Antibiotics- drugs

A

-Bleomycin

26
Q

Anthracyclines- drugs

A

-Doxorubicin
-Daunorubicin
-Epirubicin
-Idarubicin
-Mitoxantrone
(DDEIM)

27
Q

Bleomycin- therapeutic uses

A

-testicular cancer (with vinblastine, cisplatin or etoposide)

28
Q

Doxorubicin, Epirubicin- therapeutic uses

A

breast, ovarian

29
Q

Daunorubicin- therapeutic uses

A

leukemia (AML, ALL)

30
Q

Idarubicin- therapeutic uses

A

leukemia (aML, ALL, CML and blast crisis)

31
Q

Mitoxantrone- therapeutic uses

32
Q

Bleomycin- dose limiting toxicity

A

-pulm fibrosis- “bleomycin lung”!!!!!

33
Q

Anthracyclines- dose limiting toxicity

A

cardiotoxicity, dilated cardiomyopathy, CHF!!!!!- occurs over time

34
Q

Doxorubicin (anthracyclines)- moa, toxicity

A
  • intercalate b/w DNA dbl helix- disrupt DNA integrity
  • via Cyp450 reductase–> superoxide H2O2
  • dilated cardiomyopathy, HF!!!!
35
Q

risk factors for Anthracycline cardiotoxicity

A

Bleomycin- toxicity-cumulative dose

  • age
  • preexisting CV dz
  • longer duration of survival- pediatric pts!!
36
Q

Bleomycin- toxicity

A
  • skin and lung damage- don’t have the enzyme required to metabolize the drug!!!
  • superoxide hydroxy radicals–> fibrosis in lungs!!!
37
Q

Causes dilated cardiomyopathy, HF?

A

-Doxorubicin (anthracyclines)

38
Q

causes pulm fibrosis?

39
Q

ABVD regimen for hodgkin lymphoma

A
  • Adriamycin (doxorubicin)- cardiotoxicity)
  • Bleomycin- pulm fibrosis
  • Vinblastine- peripheral neuropathy
  • Dacarbazine- N/V, myelosuppression
40
Q

CHOP regimen for non-hodgkin lymphoma

A
  • Cyclophosphamide- hemorrhagic cystitis
  • Hydroxydaunorubicin (doxorubicin)- cardiotoxicity!!!
  • Oncovin (Vincristine)- peripheral neuropathy
  • Prednisone- hyperglycemia, osteopenia
41
Q

Tumor lysis syndrome- manage by?

A

allopurinol (xanthine oxidase inhibitor)

42
Q

Tumor lysis syndrome

A
  • Hyperkalemia
  • Hyperphosphatemia
  • Hyperuricemia
43
Q

allopurinol simultaneous admin with what can cause problems?

A

6-mercaptopurine (metabolized by xanthine oxidase)

-dose must be reduced

44
Q

Tumor lysis syndrome- management with uricase

A

(pegloticase- uric acid oxidase)

45
Q

chemotherapy induced N/V by?

A

-direct activation of medullary CTZ
-cell damage of GI tract- 5HT release
(serotonin R antagonists should be used!)

LHT1 (6 decks)

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