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Pharma- AntiCancer Flashcards

1
Q

Rescue drug for:

Methotrexate

A

Leucovorin

readily absorbed, TH4 analog

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2
Q

Rescue drug for:

Cyclophosphamide

A

MESNA (mercaptoethanesulfonate)
- traps ACROLEIN released by Cyclophosphamide
prevents hemorrhagic cystitis

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3
Q

Rescue drug for:
Anthracyclins
eg Doxorubicin

A

Dexrazoxane

inhibits free radical formation
protects agains Cardiotoxicity

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4
Q

4 requirements in choosing combination of anticancer drugs

A
  1. Each drug should be effective against cancer when used alone
  2. Different mechanism of action
  3. Minimal Cross reaction
  4. Different toxicity
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5
Q

5 types of anticancer drugs

A 
Alkylating agent
Antimetabolite
Natural products
Antitumor Antibiotics
Miscellaneous
Hormonal
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6
Q

Alkylating agents: CCNS drugs

  1. Nitrogen mustards
  2. Nitrosureas
  3. Alkyl sulfonates
  4. Others
A

Mechlorethamine
Cyclophosphamide
Chlorambucil

Carmustine
Lomustine

Busulfan

Cisplatin
Dacarbazine
Procarbazine

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7
Q

MoA of Alkylating agents

A

they form reactive species that ALKYLATE NUCLEOPHILIC GROUPS ON DNA BASES
esp N-7 postition of guanine

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8
Q

Tumor cell resistance to Alkylating agents

A

Increased DNA repair
Formation of trapping agents like thiol
Decreased Drug permeability

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9
Q

This SPONTANEOUSLY forms a reactive cytotoxic product

Marked vesicant (Blister-forming) actions

A

Mechlorethamine

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10
Q

Platinum analogs
used IV
Cleared renaly

A

cisplatin, carboplatin, Oxaliplatin

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11
Q

Platinum analog that causes GI distress, mild hematotoxicity, AND NEUROTOXIC ( periph neuropathy and acoustic nerve damage)
Nephrotoxic

A

Cisplatin

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12
Q

Platinum analog that causes dose-limiting Neurotoxicity

A

Oxaliplatin

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13
Q

Alkylating agent that causes

  • adrenal insufficiency, pulmonary fibrosis and skin pigmentation
A

Busulfan

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14
Q

Antimetabolite agents: CCS drugs
- S phase

  • Anti Folic Acid
  • Purine
  • Pyrimidine
A

Methotrexate

mercaptoPURINE, Thioguanine

Fluorouracil, Cytarabine, Gemcitabine

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15
Q

Inhibitor of Dihydrofolate Reductase
Formation of polyglutamate derivatives

Clearance is dependent on renal function

A

Methotrexate

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16
Q

Methotrexate also useful for

A

Rheumatoid Arthritis Psoriasis

Ectopic Pregnancy

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17
Q

Mercaptopurine and Thioguanine activated by

A

HGPRTase

Used for Acute Leukemia
Chronic Myelocytic leukemia

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18
Q

Dose limiting for Mercaptopurine and Thioguanine

A

Bone marrow suppresion

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19
Q

Converted to FdUMP

A

5-FU

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20
Q

Topical 5-FU used for

A

Keratoses and Superficial basal cell carcionma

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21
Q

Pyrimidine antimetabolite activated to AraCTP-> inhibits DNA polymerase

A

Cytarabine

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22
Q

Antimetabolite most specific for S phase

A

Cytarabine

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23
Q

Natural Product Anticancer: CCS

Vinca Alkaloids
Podophyllytoxin
Camptothecan
Taxanes

A

Vinblastine, Vincristine, Vinorelbine

eTOPOside, teniPOside

IrinoTECAN, topoTECAN

pacliTAXEL, doceTAXEL

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24
Q

MoA block the formation of mitotic spindle by preventing assembly of tubulin dimers into microtubules

Specific to M phase

A

Vinka alkaloids

Given IV
Good penetration except CNS

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25
Q

Resistance to Vinka Alkaloids due to

A

Increased efflux of the drugs from tumor cells

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26
Q

used for Non Small Cell Lung Cancer and Breast Cancer

Wilm’s tumor

Kaposi’s sarcom

A

Vinorelbine

Vincristine

Vinblastine

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27
Q

Vinka alkaloids that does NOT cause MYELOSUPPRESSION but has NEUROTOXIC ACTIONS

A

Vincristine

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28
Q

Semisynthetic derivative of podophyllotoxin, DNA breakage via inhibition of TOPO II

active against Late S and early G2 phase

A

Etoposide

renal excretion
Germ cell , gastric cancer

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29
Q

Produce DNA damage by inhibiting TOPO I

A

Camptothecins

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30
Q

Prodrug converted in the LIVER to SN-38

A

Irinotecan

exreted in bile and feces
Markedly affected by Genetic variation

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31
Q

Causes excessive toxicity in Irinotecan

A

variant of UGT1A that result to low GLUCURONIDATION activity

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32
Q

2nd line therapy for Advanced ovarian ca and Small cell lung ca

Metastatic colorectal Ca

A

Topotecan

Irinotecan

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33
Q

2 most common AE of Camptothecan

A

Myelosuppresion

Diarrhea

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34
Q

Interferes with mitotic spindle by preventing microtubule disassembly into tubulin monomers

A

Pacli and docetaxel

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35
Q

Drug group for SOLID tumors

A

Taxanes

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36
Q

AE Paclitaxel

A

neutropenia, Thrombocytopenia, peripheral neuropathy

37
Q

AE Docetaxel

A

Neurotoxicity and BM suppression

38
Q

CCNS drugs

Antitumor Antibiotics

A

Anthracyclin
Bleomycin
Mitomycin

39
Q

Example of Anthracyclin

A

Doxo, Dauno, idaru, epirubicin

Mitoxantrone

40
Q

Anthracyclin given IV

A

Doxo, dauno

41
Q

for Acute Leukemia

A

Daunorubicin

42
Q

For Acute Myelogenous Leukemia

A

Idarubicin

43
Q

Breast Cancer and GEsoph Ca

A

Epirubicin

44
Q

Toxicity of Doxorubicin

A

Cardiotoxic

45
Q

CCS drug active in G2 phase

A

Bleomycin

b- number two in alphabet
given IV, inactivated by tissue aminopeptidases

46
Q

Toxicity of bleomycin

A

Pulmonary dysfunction- fibrosis, pneumonitis

47
Q

Antibiotic CCNS drug metabolized by liver enzymes that form alkylating agents that cross links DNA
Given IV

48
Q

Drug that acts against hypoxic tumor cells

used in combination for ADENOCARCINOMAS

49
Q

Tyrosine kinase inhibitor of the bcr-abl oncogene

50
Q

This oncogene is commonly expressed in CML associated with Philadelphia chromosome

A

bcr-abl oncogene

51
Q

Effective in treatment of GIST with c-kit tyrosine kinase activity

52
Q

Monoclonal antibody that recognizes surface protein in breast ca that overexpress HER2/neu receptor for Epidermal Growth Factor

A

Trastuzumab

AE: Cardiac dysfunction - HF

53
Q

Chimeric MAB directed to extracellular domain of EGFR

Most commonly used with irinotecan and oxaliplatin for METASTATIC COLON CA

54
Q

Used with RADIATION in HEAD and NECK Ca

55
Q

Fully Human MAB directed against EGFR

A

Panitumumab

56
Q

MAB that binds to VEGF

A

Bevacizumab

57
Q

Mab that induces Complement mediated lysis, direct cytotoxicity and induction of apoptosis
Binds to surface protein in Non-Hodgkin’s lymphoma

58
Q

Endogenous glycoproteins used against Hariy cell leukemia, early stage fo CML, T cell Lymphomas

A

alpha- interferon

59
Q

Depletes serum asparaginase

For T cell auxotrophic cancers ( leukemia and lymphoma)

A

Asparaginase

60
Q

Inhibitors of Chymotrypsin-like activity of the 26S proteasome in mammalian cells

used in Multiple Myeloma

A

Bortezomib

61
Q

Most commonly used glucocorticoid in cancer

A

Prednisone

62
Q

SERM used for ESTROGEN SENSITIVE cancer cells in breast tissue

63
Q

AE of tamoxifen

A

increased risk for endometrial hyperplasia and neoplasia

64
Q

Androgen receptor antagonist used in prostatic carcinoma

65
Q

GNRH analogs

for Prostatic Ca

A

Leuprolide, Goserelin, Nafarelin

Inhibits release of LH and FSH

66
Q

AE of Lueprolide

A

Bone pain, gynecomastia, hematuria, impotence and testicular atrophy

67
Q

Aromatase inihibitors

A

Anastrozole and letrozole

both used for Breast Ca

68
Q

Chimeric MAB directed to extracellular domain of EGFR

Most commonly used with irinotecan and oxaliplatin for METASTATIC COLON CA

69
Q

Used with RADIATION in HEAD and NECK Ca

70
Q

Fully Human MAB directed against EGFR

A

Panitumumab

71
Q

MAB that binds to VEGF

A

Bevacizumab

72
Q

Hodgkin lymphomas ABVD regimen

A

Doxorubicin
Bleomycin
Vinblastine
Dacarbazine

73
Q

Endogenous glycoproteins used against Hariy cell leukemia, early stage fo CML, T cell Lymphomas

A

alpha- interferon

74
Q

Depletes serum asparaginase

For T cell auxotrophic cancers ( leukemia and lymphoma)

A

Asparaginase

75
Q

Inhibitors of Chymotrypsin-like activity of the 26S proteasome in mammalian cells

used in Multiple Myeloma

A

Bortezomib

76
Q

Most commonly used glucocorticoid in cancer

A

Prednisone

77
Q

SERM used for ESTROGEN SENSITIVE cancer cells in breast tissue

78
Q

AE of tamoxifen

A

increased risk for endometrial hyperplasia and neoplasia

79
Q

Androgen receptor antagonist used in prostatic carcinoma

80
Q

GNRH analogs

for Prostatic Ca

A

Leuprolide, Goserelin, Nafarelin

Inhibits release of LH and FSH

81
Q

AE of Lueprolide

A

Bone pain, gynecomastia, hematuria, impotence and testicular atrophy

82
Q

Aromatase inihibitors

A

Anastrozole and letrozole

both used for Breast Ca

83
Q

Most common symptom of Autonomic Neuropathy

A

Constipation

84
Q

AE of Vincristine

A

Neuropathy:

Paresthesia-> muscle weakness, initially wiht the quadricep muscles

85
Q

Characteristic toxicity of CISPLATIN

A

Nephrotoxic

used in combination with Etoposide and Bleomycin for Testicular Ca

86
Q

Hodgkin lymphoma’s MOPP regimen

A

Mechlorethamine
Vincristine
Prednisone
Procarbazine

87
Q

Hodgkin lymphomas ABVD regimen

A

Doxorubicin
Bleomycin
Vinblastine
Dacarbazine

88
Q

if used with ALLOPURINOL, xanthine oxidase inhibitor, dosage should be reduced to 25%

A

Mercaptopurine

metabolized by xanthine oxidase

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