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Oncology > Alkylating Agents and Cisplatin > Flashcards

Alkylating Agents and Cisplatin Flashcards

1
Q

Alkylating drugs: Nitrogen Mustards

A

Mechlorethamine, cyclophosphamide, ifosfamide, melphalan, chlorambucil, bendamustine

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2
Q

Alkylating drugs: Ethyleneiminies and Methylmelamines

A

Altretamine, Thiotepa

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3
Q

Alkylating drugs: Alkyl Sulfonates

A

Busulfan

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4
Q

Alkylating drugs: Nitrosoureas

A

Carmustine (BCNU), streptozocin

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5
Q

Alkylating drugs: Triazenes

A

Dacarbazine (DTIC), Temozolomide

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6
Q

Alkylating drugs: Methylhydrazines

A

Procarbazine

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7
Q

Cytotoxic drugs

A

kills cells that are growing rapidly. stops cancer from dividing and growing and may cause tumors to shrink in size.

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8
Q

Cytotoxic drugs primary curative for which diseases?

A

Leukemias, lymphomas, choriocarcinomas, testicular cancer

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9
Q

cytotoxic drug usage?

A

for palliative purposes-to reduce tumor size/growth and untoward symptoms

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10
Q

What are categories of cytotoxic drugs?

A

Alkylating agents, platinum coordination complexes, antimetabolites, natural products

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11
Q

Alkylating agents MOA:

A

alkylates DNA, RNA, and proteins

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12
Q

Platinum Coordination Complexes

A

Do not alkylate DNA but forms covalent metal adducts with DNA

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13
Q

Antimetabolties MOA

A

Affects DNA or RNA synthesis

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14
Q

Natural Products MOA:

A

Affects DNA, RNA, and protein involving cell growth and division

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15
Q

Alkylating drugs AE?

A

Marrow, mucosa, hair follicles, nervous system, leukemogenesis

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15
Q

Alkylating drugs AE?

A

Marrow, mucosa, hair follicles, nervous system, leukemogenesis

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16
Q

Mono-functional alkylating agents?

A

react with only one strand of DNA (simple methylation)
greater capacity for mutagenesis and carcinogenesis

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17
Q

Bi-functional alkylating agent?

A

react with an atom on both strands of DNA-produces cross-link that covalently links two strands of DNA double helix
Cytotoxic effects predominate

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18
Q

Mono-functional methylating agents:

A

procarbazine, dacarbazine, temozolomide

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19
Q

which mono-functional methylating agent is highly carcinogenic?

A

Procarbazine

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20
Q

alkylating agents form?

A

highly reactive carbonium ion intermediates

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21
Q

alkylating drugs link ?

A

covalently to sites of high electron density-phosphates, amines, sulfhydryl, hydroxyl groups

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22
Q

alkylating cytotoxic effects related to alkylation of?

A

reactive amines, oxygens, or phosphates

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23
Q

N7 atom of guanine susceptible to

A

formation of covalent bond with bifunctional alkylating agents

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24
Q

which alkylating agents are prodrugs?

A

Cyclophosphamide and ifosfamide

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25
Q

cyclophosphamide and ifosfamide undergo what metabolism?

A

hepatic

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26
Q

what factors affect alkylating agents activities in vivo?

A

lipophilicity, sites of macomolecular attack, mechanism of DNA repair, active transport

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27
Q

Nitrogen mustards are what type of alkylating agents?

A

bi-functional

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28
Q

what is the treatment regimen for hodgkin lymphoma?

A

MOPP
Mustargen (Mechlorethamine)
Oncovin (Vincristine)
Procarbazine (Matulane)
Prednisone (Deltasone)

29
Q

Cyclophosphamide showed complete remissions and cures in which cancer?

A

Burkitt Lymphoma

30
Q

which alkylating agent is good in pediatrics?

A

Chlorambucil (really no toxicity)

31
Q

Nitrogen Mustard: Cyclophsophamide generates?

A

Phosphoramide mustard and Acrolein

32
Q

What is phosphoramide mustard responsible for?

A

antitumor effects

33
Q

What does acrolein cause?

A

hemorrhagic cystitis

34
Q

what is the intermediate of cyclophosphamide?

A

4-hydroxy intermediate

35
Q

Altretamine can be palliative treatment in persistent or recurrent ____?

A

ovarian cancer following cisplatin based combo therapy

36
Q

Busulfan is a ?

A

alkyl sulfonate

37
Q

Busulfan may induce?

A

cross-linkage of DNA to nuclear proteins

38
Q

Busulfan metabolized by?

A

Glutathione (GSH) conjugation by GSTA1A in the liver and further by CYP dependent pathways to inactivate metabolites

39
Q

What is the major action of Carmustine (BCNU)?

A

bi-functional alkylation-of DNA at the O6-guanine position—-repair by MGMT

40
Q

Carmustine and lomustine are highly?

A

Lipophillic (crosses BBB)

41
Q

Carmustine (BCNU) is used in treatment of?

A

Malignant gliomas (brain tumors)
-enters CSF
-Use IV

42
Q

What is the major action of streptozocin?

A

methylnitrosourea moitey to the 2-carbon of glucose of DNA

43
Q

Triazenes are prodrugs:

A

Dacarbazine and Temozolomide

44
Q

Triazenes function?

A

kill cells in all phases of the cell cycle

45
Q

Triazenes especially Dacarbazine causes?

A

removal of methyl group from O6 guanine bases in DNA by MGMT—-causing drug resistance

46
Q

Dacarbazine administration? and excretion?

A

IV
50% excreted intact in urine by tubular secretion

47
Q

Alkylating agents used as a single agent has _____ resistance? Due to?

A

High
Decreased permeation of actively transported drugs
Increased intracellular concentrations of nucleophilic substances such as elevated glutathione levels and increased activity of glutathione transferases (detoxification)

48
Q

resistance is also due to?

A

increased activity of DNA repair pathways (MGMT, mutations of p53)
increased rates of metabolic degradation of the activated forms of cyclophosphamide and ifosfamide to their inactive keto and carboxy metabolites by aldehyde dehydrogenase
loss of ability to recognize adducts formed by nitrosoureas and methylating agents (defective mismatch repair and checkpoint function)
impaired apoptotic pathways (overexpression of Bcl-2: apoptosis inhibitor)

49
Q

which drugs have high expression of MGMT?

A

BCNU, Dacrabazine, temozolomide, and procarbazine

50
Q

Alkylating agents at high doses ________ ________

A

kills more slow proliferating cells

51
Q

alkylating agents suppress?

A

cellular and humoral immunity-chance for opportunisitc infections

52
Q

alkylating agents may cause:

A

Myelosuppression (bone marrow activity decreased)
loss of hair follicles, mucosal damage
nausea and vomitting
can induce leukemia (melphalan and procarbazine)

53
Q

Which alkylating agent is the most neurotoxic?

A

Ifosfamide-alters mental status and coma, seizures

54
Q

Busulfan or BCNU high doses can cause vascular endothelial damage which can be reversed by?

A

Defibrotide

55
Q

Acrolein metabolite may cause hemorrhagic cystitis what should you coadminister with Cyclophosphamide and ifosfamide to prevent?

56
Q

What is the major organ toxicity of alkylating agents?

A

Hepatic VOD (vein occlusive disease)

57
Q

What drugs are platinum complexes?

A

cisplatin, carboplatin, oxaliplatin

58
Q

Platinum complexes DO NOT?

A

form carbonium ion intermediates or alkylate DNA (no alkyl group)

59
Q

Platinum coordination complexes have a broad antineoplastic activity.

60
Q

DNA Platinum adducts inhibit?

A

replication and transcription-leading to breaks and miscoding

61
Q

Overexpression of nucleotide excision repair (NER) causes

A

poor response to cisplatin/oxaliplatin therapies

62
Q

What do you give prior to treatment of Cisplatin?

A

Normal saline to establish chloride diuresis (prevention of renal toxicitiy)

63
Q

Carboplatin is eliminated by?

A

renal excretion

64
Q

Carboplatin is ____ _____ reactive than cisplatin

A

much less (drug in plasma remains in parent form and unbound to proteins)
less side effects too

65
Q

Cisplatin can cure when used in combo with alkylating agents ?

A

testicular cancer

66
Q

to prevent renal toxicity with use of Cisplatin give?

A

Amifostine

67
Q

Cisplatin adverse effect?

A

development of AML (4 years of treatment)

68
Q

Oxaliplatin can cause what after months to years of treatment?

69
Q

Oxiplatin is used in which cancers?

A

colorectal and gastric

Oncology (10 decks)

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