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Pharm SJSM > Block 3 materials (Anticancers) > Flashcards

Block 3 materials (Anticancers) Flashcards

1
Q

Bleomycin

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Forms free radicals to cause DNA strand breaks in G2 & Mitosis

Clinical uses:
Testicular cancer
Hodgkin Lymphoma

Adverse effects:
1) Pulmonary fibrosis
2) Skin hyperpigmentation

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2
Q

MOA:
Forms free radicals to cause DNA strand breaks in G2 & Mitosis

Clinical uses:
Testicular cancer
Hodgkin Lymphoma

Adverse effects:
1) Pulmonary fibrosis
2) Skin hyperpigmentation

A

Bleomycin

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3
Q

What drugs are used to treat Hodgkin Lymphoma?

A

Adriamycin
Bleomycin
Vinblastine
Dacarbazine

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4
Q

Dactinomycin (Actinomycin D)

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Intercalates into DNA to prevent RNA synthesis (blocks RNA polymerase) in G2 & Mitosis

Clinical uses:
Childhood tumors
- Wilms
- Ewing sarcoma
- Rhabdomyosarcoma

Adverse effects:
Myelosuppression

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5
Q

MOA:
Intercalates into DNA to prevent RNA synthesis (blocks RNA polymerase) in G2 & Mitosis

Clinical uses:
Childhood tumors
- Wilms
- Ewing sarcoma
- Rhabdomyosarcoma

Adverse effects:
Myelosuppression

A

Dactinomycin (Actinomycin D)

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6
Q

Anthracyclines

MOA:

Clinical uses:

Adverse effects:

A

Doxorubicin & Daunorubicin

MOA:
Makes free radicals that intercalate into DNA & cause strand breaks to reduce replication & inhibit topoisomerase II (DNA gyrase)

Clinical uses:
Solid tumors
Leukemia
Lymphoma

Adverse effects:
1) Dilated cardiomyopathy (avoid with dexrazoxane)
2) Alopecia
3) Myelosuppression

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7
Q

Doxorubicin & Daunorubicin

MOA:
Makes free radicals that intercalate into DNA & cause strand breaks to reduce replication & inhibit topoisomerase II (DNA gyrase)

Clinical uses:
Solid tumors
Leukemia
Lymphoma

Adverse effects:
1) Dilated cardiomyopathy (avoid with dexrazoxane)
2) Alopecia
3) Myelosuppression

A

Anthracyclines

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8
Q

Thiopurines

MOA

Clinical uses

Adverse effects

A

Azathioprine & 6-Mercaptopurine

MOA: Antimetabolites
Purine (thiol) analogs that reduce de novo purine synthesis.
AZA is converted to 6-MP & then activated by HGPRT to form purine analogs that insert into DNA/RNA to halt synthesis

Clinical uses:
Prevent organ transplant rejection
Weaning off steroids
Rheumatoid arthritis
IBD
SLE
ALL
Steroid factory disease

Adverse effects:
1) 6-MP toxicity when given with Allopurinol or Febuxostat (antigout)
2) Pancreatitis
3) Myelosuppression
4) Liver & Gi toxicity

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9
Q

Azathioprine & 6-Mercaptopurine

MOA: Antimetabolites
Purine (thiol) analogs that reduce de novo purine synthesis.
AZA is converted to 6-MP & then activated by HGPRT to form purine analogs that insert into DNA/RNA to halt synthesis

Clinical uses:
Prevent organ transplant rejection
Weaning off steroids
Rheumatoid arthritis
IBD
SLE
ALL
Steroid factory disease

Adverse effects:
1) 6-MP toxicity when given with Allopurinol or Febuxostat (antigout)
2) Pancreatitis
3) Myelosuppression
4) Liver & Gi toxicity

A

Thiopurines

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10
Q

Cladribine & Pentostatin

MOA:

Clinical uses:

Adverse effects:

A

MOA: Antimetabolites
Purine analogs that cause premature DNA breaks

Clinical uses Antimetabolites:
Hairy cell leukemia

Adverse effects:
1) Nephrotoxicity
2) Neurotoxicity
3) Myelosuppression

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11
Q

MOA: Antimetabolites
Purine analogs that cause premature DNA breaks

Clinical uses:
Hairy cell leukemia

Adverse effects:
1) Nephrotoxicity
2) Neurotoxicity
3) Myelosuppression

“Purine analogs break hairy Cell leukemia”

A

Cladribine & Pentostatin

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12
Q

Cytarabine (arabinofuranosylcytosine)

MOA:

Clinical uses:

Adverse effects:

A

MOA: Antimetabolites
Pyrimidine analog that causes DNA chain termination & DNA polymerase inhibition during S phase

Clinical uses:
Leukemias (ALL & AML)
Lymphomas

Adverse effects:
1) Myelosuppression
2) Megaloblastic anemia

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13
Q

MOA: Antimetabolites
Pyrimidine analog that causes DNA chain termination & DNA polymerase inhibition during S phase

Clinical uses:
Leukemias (ALL & AML)
Lymphomas

Adverse effects:
1) Myelosuppression
2) Megaloblastic anemia

A

Cytarabine (arabinofuranosylcytosine)

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14
Q

5-Fluorouracil

MOA:

Clinical uses:

Adverse effects:

A

MOA: Antimetabolites
Pyrimidine analog that is bioactivated by 5-FdUMP to inhibit thymidylate synthase to reduce DNA synthesis

Clinical uses:
Colon & Pancreatic cancers
Actinic keratosis
Basal cell carcinoma

Adverse effects:
1) Myelosuppression
2) Palmar-Plantar erythrodysesthesia (hand/foots syndrome)

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15
Q

MOA: Antimetabolites
Pyrimidine analog that is bioactivated by 5-FdUMP to inhibit thymidylate synthase to reduce DNA synthesis

Clinical uses:
Colon & Pancreatic cancers
Actinic keratosis
Basal cell carcinoma

Adverse effects:
1) Myelosuppression
2) Palmar-Plantar erythrodysesthesia (hand/foots syndrome)

A

5-Fluorouracil

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16
Q

Hydroxyurea

MOA:

Clinical uses:

Adverse effects:

A

MOA: Antimetabolites
Inhibits RNR (ribonucleotide reductase) to reduce DNA synthesis in S phase

Clinicals:
1) Myeloproliferative disorders (CML, & Polycythemia vera)
2) Megaloblastic anemia

Adverse effects:
1) Severe myelosuppression
2) Megaloblastic anemia

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17
Q

MOA: Antimetabolites
Inhibits RNR (ribonucleotide reductase) to reduce DNA synthesis in S phase

Clinicals:
1) Myeloproliferative disorders (CML, & Polycythemia vera)
2) Megaloblastic anemia

Adverse effects:
1) Severe myelosuppression
2) Megaloblastic anemia

A

Hydroxyurea

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18
Q

Methotrexate

MOA:

Clinical uses:

Adverse effects:

A

MOA: Antimetabolites
Folic acid analog that competitively inhibits dihydrofolate reductase to reduce DNA synthesis

Clinicals:
- Cancers
(leukemias (ALL), lymphomas, choriocarcinoma, & sarcomas)
- Ectopic pregnancy
- Medical abortion (with misoprostol)
- Rheumatoid arthritis
- Psoriasis
- IBD
- Vasculitis

Adverse:
1) Myelosuppression (give leucovorin)
2) Hepatotoxicity
3) Mucositis (Mouth ulcers)
4) Pulmonary fibrosis
5) Folate deficiency
6) Nephrotoxicity

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19
Q

MOA: Antimetabolites
Folic acid analog that competitively inhibits dihydrofolate reductase to reduce DNA synthesis

Clinicals:
- Cancers
(leukemias (ALL), lymphomas, choriocarcinoma, & sarcomas)
- Ectopic pregnancy
- Medical abortion (with misoprostol)
- Rheumatoid arthritis
- Psoriasis
- IBD
- Vasculitis

Adverse:
1) Myelosuppression (give leucovorin)
2) Hepatotoxicity
3) Mucositis (Mouth ulcers)
4) Pulmonary fibrosis
5) Folate deficiency
6) Nephrotoxicity

A

Methotrexate

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20
Q

Busulfan

MOA:

Clinical uses:

Adverse effects:

A

MOA: Alkylating agent
Cross-links DNA via guanosine (N7) that affects a cell’s ability to multiply

Clinicals:
Ablate bone marrow (transplant)

Adverse effects:
1) Severe myelosuppression
2) Pulmonary fibrosis
3) Hyperpigmentation

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21
Q

MOA: Alkylating agent
Cross-links DNA via guanosine (N7) that affects a cell’s ability to multiply

Clinicals:
Ablate bone marrow (transplant)

Adverse effects:
1) Severe myelosuppression
2) Pulmonary fibrosis
3) Hyperpigmentation

A

Busulfan

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22
Q

Nitrogen Mustards

MOA:

Clinical uses:

Adverse effects:

A

MOA: Alkylating agents
Cross-links DNA via guanosine (N7) that is bioactivated by the liver & interferes with replication & transcription

Clinical uses:
1) Solid tumors (breast & ovary)
2) Leukemia
3) Non-Hodgkin lymphoma
4) Rheumatic disease (SLE & Wegners)

Adverse effects:
1) Hemorrhagic cystitis (avoid with MESNA)
2) Myelosuppression
3) Fanconi syndrome (Ifosfamide)

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23
Q

Cyclophosphamide,
ifosfamide

MOA: Alkylating agents
Cross-links DNA via guanosine (N7) that is bioactivated by the liver & interferes with replication & transcription

Clinical uses:
1) Solid tumors (breast & ovary)
2) Leukemia
3) Non-Hodgkin lymphoma
4) Rheumatic disease (SLE & Wegners)

Adverse effects:
1) Hemorrhagic cystitis (avoid with MESNA)
2) Myelosuppression
3) Fanconi syndrome (Ifosfamide)

A

Nitrogen Mustards

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24
Q

Nitrogen Mustards

MOA:

Clinical uses:

Adverse effects:

A

Cyclophosphamide & Ifosfamide

MOA:
Cross-links DNA via guanosine (N7) that is bioactivated by the liver & interferes with replication & transcription

Clinicals:
Solid tumors (breast & ovary)
Leukemia
Non-Hodgkin lymphoma
Rheumatic disease (SLE & Wegners)

Adverse effects:
1) Hemorrhagic cystitis (avoid with MESNA)
2) Myelosuppression
3) Fanconi syndrome (Ifosfamide)

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25
Q

Cyclophosphamide & Ifosfamide

MOA:
Cross-links DNA via guanosine (N7) that is bioactivated by the liver & interferes with replication & transcription

Clinicals:
Solid tumors (breast & ovary)
Leukemia
Non-Hodgkin lymphoma
Rheumatic disease (SLE & Wegners)

Adverse effects:
1) Hemorrhagic cystitis (avoid with MESNA)
2) Myelosuppression
3) Fanconi syndrome (Ifosfamide)

A

Nitrogen Mustards

26
Q

Procarbazine

MOA:

Clinical uses:

Adverse effects:

A

MOA: Alkylating agent
Weak MAO inhibitor

Clinicals:
Hodgkin lymphoma
Brain tumors
- Primary CNS lymphoma
- Glioblastoma multiforme
- Anaplastic oligodendroglioma

Adverse effects:
1) Bone marrow suppression
2) Pulmonary toxicity (pneumocystis)
3) Leukemia
4) Disulfiram-like reaction

27
Q

MOA: Alkylating agent
Weak MAO inhibitor

Clinicals:
Hodgkin lymphoma
Brain tumors
- Primary CNS lymphoma
- Glioblastoma multiforme
- Anaplastic oligodendroglioma

Adverse effects:
1) Bone marrow suppression
2) Pulmonary toxicity (pneumocystis)
3) Leukemia
4) Disulfiram-like reaction

A

Procarbazine

28
Q

Platinum-containing drugs

MOA:

Clinical uses:

Adverse effects:

A

Cisplatin, Carboplatin, & Oxaliplatin

MOA:
Platinum ions cross-links DNA

Clinical uses:
1) Solid tumors (Testicular, Bladder, Ovarian, Gi, & Lungs)
2) Lymphoma

Adverse effects:
1) Nephrotoxicity (ATN & Fanconi syndrome avoid with Amifostine & Chloride diuresis)
2) Peripheral neuropathy
3) Ototoxicity (hearing loss)

29
Q

Cisplatin, Carboplatin, & Oxaliplatin

MOA:
Platinum ions cross-links DNA

Clinical uses:
1) Solid tumors (Testicular, Bladder, Ovarian, Gi, & Lungs)
2) Lymphoma

Adverse effects:
1) Nephrotoxicity (ATN & Fanconi syndrome avoid with Amifostine & Chloride diuresis)
2) Peripheral neuropathy
3) Ototoxicity (hearing loss)

A

Platinum-containing drugs

30
Q

Taxanes

MOA:

Clinical uses:

Adverse effects:

A

Paclitaxel & Docetaxel

MOA: Microtubule inhibitors
Inhibits microtubule formation & prevents mitotic spindle breakdown (hyper stabilize) in M phase

Clinicals:
Ovarian & Breast cancers

Adverse effects:
1) Myelosuppression
2) Neuropathy
3) Hypersensitivity

31
Q

Paclitaxel & Docetaxel

MOA: Microtubule inhibitors
Inhibits microtubule formation & prevents mitotic spindle breakdown (hyper stabilize) in M phase

Clinicals:
Ovarian & Breast cancers

Adverse effects:
1) Myelosuppression
2) Neuropathy
3) Hypersensitivity

A

Taxanes

32
Q

Vinca alkaloids

MOA:

Clinical uses:

Adverse effects:

A

Vincristine & Vinblastine

MOA: Microtubule inhibitors
Binds B-tubulin & inhibits it’s polymerization to prevent mitotic spindle formation in M phase

Clinical uses:
Solid tumors
Leukemia
Hodgkin/Non-Hodgkin lymphoma

Adverse effects:
1) Neurotoxicity (Vincristine)
- peripheral neurotoxicity
- areflexia
- Paralytic ileus
2) Bone marrow suppression (Vinblastine)

33
Q

Vincristine & Vinblastine

MOA: Microtubule inhibitors
Binds B-tubulin & inhibits it’s polymerization to prevent mitotic spindle formation in M phase

Clinical uses:
Solid tumors
Leukemia
Hodgkin/Non-Hodgkin lymphoma

Adverse effects:
1) Neurotoxicity (Vincristine)
- peripheral neurotoxicity
- areflexia
- Paralytic ileus
2) Bone marrow suppression (Vinblastine)

A

Vinca alkaloids

34
Q

Etoposide & Teniposide

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Topoisomerase II inhibitors (DNA gyrase) in S & G2 phase, causing double strand breaks

Clinicals:
Testicular & SCLC
Leukemia
Lymphoma
ALL cancer

Adverse effects:
1) Myelosuppression
2) Alopecia
3) Gi upset

35
Q

MOA:
Topoisomerase II inhibitors (DNA gyrase) in S & G2 phase, causing double strand breaks

Clinicals:
Testicular & SCLC
Leukemia
Lymphoma
ALL cancer

Adverse effects:
1) Myelosuppression
2) Alopecia
3) Gi upset

A

Etoposide & Teniposide

36
Q

Irinotecan & Topotecan

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Topoisomerase I inhibitor that causes single stranded breaks in G2 & S phases

Clinical uses:
Colon cancer (Irinotecan)
Ovarian & SCLC (Topotecan)

Adverse effects:
1) Severe myelosuppression
2) Diarrhea

37
Q

MOA:
Topoisomerase I inhibitor that causes single stranded breaks in G2 & S phases

Clinical uses:
Colon cancer (Irinotecan)
Ovarian & SCLC (Topotecan)

Adverse effects:
1) Severe myelosuppression
2) Diarrhea

A

Irinotecan & Topotecan

38
Q

Tamoxifen & Raloxifene

MOA:

Clinical uses:

Adverse effects:

A

MOA: SERM
Antagonists in breast tissue & partial agonist in endometrial & bone tissue

Clinical uses:
ER/PR +ve breast cancers

Adverse effects:
1) Higher risk of endometrial cancer (Tamoxifen)

2) Higher risk of thromboembolic events (DVT & PE)

3) Hot flashes

39
Q

MOA: SERM
Antagonists in breast tissue & partial agonist in endometrial & bone tissue

Clinical uses:
ER/PR +ve breast cancers

Adverse effects:
1) Higher risk of endometrial cancer (Tamoxifen)

2) Higher risk of thromboembolic events (DVT & PE)

3) Hot flashes

A

Tamoxifen & Raloxifene

40
Q

Alemtuzumab

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Anticancer monoclonal antibodies against CD52

Clinical uses:
1) Chronic lymphocytic leukemia (CLL)
2) Multiple sclerosis

Adverse effects:
1) Higher risk of infections & autoimmunity (ITP)

41
Q

MOA:
Anticancer monoclonal antibodies against CD52

Clinical uses:
1) Chronic lymphocytic leukemia (CLL)
2) Multiple sclerosis

Adverse effects:
1) Higher risk of infections & autoimmunity (ITP)

A

Alemtuzumab

42
Q

Bevacizumab

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Anticancer monoclonal antibodies against VEGF to inhibit blood vessel formation

Clinical uses:
1) Solid tumors (Colorectal cancer, Renal cell carcinoma & Non-small cell carcinoma

2) Angio-proliferative retinopathy (wet-age related macular degeneration)

Adverse effects:
1) Hemorrhaging
2) Blood clots
3) Impaired wound healing

43
Q

MOA:
Anticancer monoclonal antibodies against VEGF to inhibit blood vessel formation

Clinical uses:
1) Solid tumors (Colorectal cancer, Renal cell carcinoma & Non-small cell carcinoma

2) Angio-proliferative retinopathy (wet-age related macular degeneration)

Adverse effects:
1) Hemorrhaging
2) Blood clots
3) Impaired wound healing

A

Bevacizumab

44
Q

Cetuximab & Panitumumab

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Anticancer monoclonal antibodies targeted against EGFR

Clinical uses:
Metastatic (stage IV) Colorectal cancer
Head & Neck cancers

Adverse effects:
1) Elevated LFT’s
2) Rash
3) Diarrhea

45
Q

MOA:
Anticancer monoclonal antibodies targeted against EGFR

Clinical uses:
Metastatic (stage IV) Colorectal cancer
Head & Neck cancers

Adverse effects:
1) Elevated LFT’s
2) Rash
3) Diarrhea

A

Cetuximab & Panitumumab

46
Q

Rituximab

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Anticancer monoclonal antibodies against CD20 on the surface of B cells

Clinical uses:
1) Non-Hodgkin lymphoma
2) CLL
3) Immune Thrombocytopenic Purpura
4) Rheumatoid arthritis

Adverse effects:
1) increased risk of subsequent progressive multifocal leukoencephalopathy caused by JC virus reactivation

47
Q

MOA:
Anticancer monoclonal antibodies against CD20 on the surface of B cells

Clinical uses:
1) Non-Hodgkin lymphoma
2) CLL
3) Immune Thrombocytopenic Purpura
4) Rheumatoid arthritis

Adverse effects:
1) increased risk of subsequent progressive multifocal leukoencephalopathy caused by JC virus reactivation

A

Rituximab

48
Q

Trastuzumab

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Anticancer monoclonal antibodies against HER2/neu tyrosine kinase receptor

Clinicals:
1) HER2/neu +ve Breast cancer
2) Gastric cancer

Adverse effects:
Dilated cardiomyopathy

49
Q

MOA:
Anticancer monoclonal antibodies against HER2/neu tyrosine kinase receptor

Clinicals:
1) HER2/neu +ve Breast cancer
2) Gastric cancer

Adverse effects:
Dilated cardiomyopathy

A

Trastuzumab

50
Q

Alectinib

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Targets ALK genes

Clinical uses:
Non-Small cell carcinoma

Adverse effects:
1) Edema
2) Rash
3) Diarrhea

51
Q

MOA:
Targets ALK genes

Clinical uses:
Non-Small cell carcinoma

Adverse effects:
1) Edema
2) Rash
3) Diarrhea

A

Alectinib

52
Q

Erlotinib, Gefitinib, & Afatinib

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Targets EGFR tyrosine kinase inhibitor

Clinical uses:
Non-small cell carcinoma

Adverse effects:
Rash (face/back)

53
Q

MOA:
Targets EGFR tyrosine kinase inhibitor

Clinical uses:
Non-small cell carcinoma

Adverse effects:
Rash (face/back)

A

Erlotinib, Gefitinib, & Afatinib

54
Q

Imatinib, Dasatinib, & Nilotinib

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Targets BCR-ABL (cKIT)

Clinical uses:
CML, ALL, GIST

Adverse effects:
1) Myelosuppression
2) Elevated LFT’s
3) Edema
4) Myalgias

55
Q

MOA:
Targets BCR-ABL (cKIT)

Clinical uses:
CML, ALL, GIST

Adverse effects:
1) Myelosuppression
2) Elevated LFT’s
3) Edema
4) Myalgias

A

Imatinib, Dasatinib, & Nilotinib

56
Q

Ruxolitinib

MOA

Clinical uses:

Adverse effects:

A

MOA:
Targets jak 1/2

Clinical uses:
Polycythemia vera

Adverse effects:
1) Bruises
2) LFT’s

57
Q

MOA:
Targets jak 1/2

Clinical uses:
Polycythemia vera

Adverse effects:
1) Bruises
2) LFT’s

A

Ruxolitinib

58
Q

Bortezomib, Carfizomib, & Ixazomib

MOA

Clinical uses:

Adverse effects:

A

MOA:
Targets proteasomes to induce cell cycle arrest at G2 & M phase to cause apoptosis

Clinicals:
Multiple myeloma
Mantle cell lympoma

Adverse effects:
1) Rash/fatigue/diarrhea

59
Q

MOA:
Targets proteasomes to induce cell cycle arrest at G2 & M phase to cause apoptosis

Clinicals:
Multiple myeloma
Mantle cell lympoma

Adverse effects:
1) Rash/fatigue/diarrhea

A

Bortezomib, Carfizomib, & Ixazomib

60
Q

Vemurafenib, Dabrafenib, & Encorafenib

MOA

Clinical uses:

Adverse effects:

A

MOA:
BRAK Kinase mutase inhibitor used for BRAF mutations like V600E

Clinical uses:
Metastatic melanoma

Adverse effects:
1) Peripheral neuropathy (HSV reactivation)

61
Q

MOA:
BRAK Kinase mutase inhibitor used for BRAF mutations like V600E

Clinical uses:
Metastatic melanoma

Adverse effects:
1) Peripheral neuropathy (HSV reactivation)

A

Vemurafenib, Dabrafenib, & Encorafenib

62
Q
A

Pharm SJSM (23 decks)

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