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Boards Halo halo > Pharma- AntiCancer > Flashcards

Pharma- AntiCancer Flashcards

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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
Resistance to Vinka Alkaloids due to
Increased efflux of the drugs from tumor cells
26
used for Non Small Cell Lung Cancer and Breast Cancer Wilm's tumor Kaposi's sarcom
Vinorelbine Vincristine Vinblastine
27
Vinka alkaloids that does NOT cause MYELOSUPPRESSION but has NEUROTOXIC ACTIONS
Vincristine
28
Semisynthetic derivative of podophyllotoxin, DNA breakage via inhibition of TOPO II active against Late S and early G2 phase
Etoposide renal excretion Germ cell , gastric cancer
29
Produce DNA damage by inhibiting TOPO I
Camptothecins
30
Prodrug converted in the LIVER to SN-38
Irinotecan exreted in bile and feces Markedly affected by Genetic variation
31
Causes excessive toxicity in Irinotecan
variant of UGT1A that result to low GLUCURONIDATION activity
32
2nd line therapy for Advanced ovarian ca and Small cell lung ca Metastatic colorectal Ca
Topotecan Irinotecan
33
2 most common AE of Camptothecan
Myelosuppresion | Diarrhea
34
Interferes with mitotic spindle by preventing microtubule disassembly into tubulin monomers
Pacli and docetaxel
35
Drug group for SOLID tumors
Taxanes
36
AE Paclitaxel
neutropenia, Thrombocytopenia, peripheral neuropathy
37
AE Docetaxel
Neurotoxicity and BM suppression
38
CCNS drugs | Antitumor Antibiotics
Anthracyclin Bleomycin Mitomycin
39
Example of Anthracyclin
Doxo, Dauno, idaru, epirubicin | Mitoxantrone
40
Anthracyclin given IV
Doxo, dauno
41
for Acute Leukemia
Daunorubicin
42
For Acute Myelogenous Leukemia
Idarubicin
43
Breast Cancer and GEsoph Ca
Epirubicin
44
Toxicity of Doxorubicin
Cardiotoxic
45
CCS drug active in G2 phase
Bleomycin b- number two in alphabet given IV, inactivated by tissue aminopeptidases
46
Toxicity of bleomycin
Pulmonary dysfunction- fibrosis, pneumonitis
47
Antibiotic CCNS drug metabolized by liver enzymes that form alkylating agents that cross links DNA Given IV
Mitomycin
48
Drug that acts against hypoxic tumor cells | used in combination for ADENOCARCINOMAS
Mitomycin
49
Tyrosine kinase inhibitor of the bcr-abl oncogene
Imatinib
50
This oncogene is commonly expressed in CML associated with Philadelphia chromosome
bcr-abl oncogene
51
Effective in treatment of GIST with c-kit tyrosine kinase activity
Imatinib
52
Monoclonal antibody that recognizes surface protein in breast ca that overexpress HER2/neu receptor for Epidermal Growth Factor
Trastuzumab AE: Cardiac dysfunction - HF
53
Chimeric MAB directed to extracellular domain of EGFR | Most commonly used with irinotecan and oxaliplatin for METASTATIC COLON CA
Cetuximab
54
Used with RADIATION in HEAD and NECK Ca
Cetuximab
55
Fully Human MAB directed against EGFR
Panitumumab
56
MAB that binds to VEGF
Bevacizumab
57
Mab that induces Complement mediated lysis, direct cytotoxicity and induction of apoptosis Binds to surface protein in Non-Hodgkin's lymphoma
Rituximab
58
Endogenous glycoproteins used against Hariy cell leukemia, early stage fo CML, T cell Lymphomas
alpha- interferon
59
Depletes serum asparaginase For T cell auxotrophic cancers ( leukemia and lymphoma)
Asparaginase
60
Inhibitors of Chymotrypsin-like activity of the 26S proteasome in mammalian cells used in Multiple Myeloma
Bortezomib
61
Most commonly used glucocorticoid in cancer
Prednisone
62
SERM used for ESTROGEN SENSITIVE cancer cells in breast tissue
Tamoxifen
63
AE of tamoxifen
increased risk for endometrial hyperplasia and neoplasia
64
Androgen receptor antagonist used in prostatic carcinoma
Flutamide
65
GNRH analogs | for Prostatic Ca
Leuprolide, Goserelin, Nafarelin Inhibits release of LH and FSH
66
AE of Lueprolide
Bone pain, gynecomastia, hematuria, impotence and testicular atrophy
67
Aromatase inihibitors
Anastrozole and letrozole both used for Breast Ca
68
Chimeric MAB directed to extracellular domain of EGFR | Most commonly used with irinotecan and oxaliplatin for METASTATIC COLON CA
Cetuximab
69
Used with RADIATION in HEAD and NECK Ca
Cetuximab
70
Fully Human MAB directed against EGFR
Panitumumab
71
MAB that binds to VEGF
Bevacizumab
72
Hodgkin lymphomas ABVD regimen
Doxorubicin Bleomycin Vinblastine Dacarbazine
73
Endogenous glycoproteins used against Hariy cell leukemia, early stage fo CML, T cell Lymphomas
alpha- interferon
74
Depletes serum asparaginase For T cell auxotrophic cancers ( leukemia and lymphoma)
Asparaginase
75
Inhibitors of Chymotrypsin-like activity of the 26S proteasome in mammalian cells used in Multiple Myeloma
Bortezomib
76
Most commonly used glucocorticoid in cancer
Prednisone
77
SERM used for ESTROGEN SENSITIVE cancer cells in breast tissue
Tamoxifen
78
AE of tamoxifen
increased risk for endometrial hyperplasia and neoplasia
79
Androgen receptor antagonist used in prostatic carcinoma
Flutamide
80
GNRH analogs | for Prostatic Ca
Leuprolide, Goserelin, Nafarelin Inhibits release of LH and FSH
81
AE of Lueprolide
Bone pain, gynecomastia, hematuria, impotence and testicular atrophy
82
Aromatase inihibitors
Anastrozole and letrozole both used for Breast Ca
83
Most common symptom of Autonomic Neuropathy
Constipation
84
AE of Vincristine
Neuropathy: Paresthesia-> muscle weakness, initially wiht the quadricep muscles
85
Characteristic toxicity of CISPLATIN
Nephrotoxic used in combination with Etoposide and Bleomycin for Testicular Ca
86
Hodgkin lymphoma's MOPP regimen
Mechlorethamine Vincristine Prednisone Procarbazine
87
Hodgkin lymphomas ABVD regimen
Doxorubicin Bleomycin Vinblastine Dacarbazine
88
if used with ALLOPURINOL, xanthine oxidase inhibitor, dosage should be reduced to 25%
Mercaptopurine metabolized by xanthine oxidase

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