Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmacology > GI: Cancer Therapy Drugs > Flashcards

GI: Cancer Therapy Drugs Flashcards

1
Q

Alkylating Agents?

A
  • Melphalan
  • Chlorambucil
  • Cyclophosphamide
  • Lomustine
  • Carmustine
  • Cisplatin
  • Oxaliplatin
  • Carboplatin
  • Procarbazine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Nitrogen Mustard Alkylators?

A

Nitrogen Mustard Alkylators?

  • Melphalan
  • Chlorambucil
  • Cyclophosphamide
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Melphalan

Chlorambucil

Cyclophosphamide

A

Nitrogen Mustard Alkylators

  • Cause Alkylation of DNA at the N-7 position of **Guanine
  • -> Misreadingof DNA duringReplication
  • -> Lethal errors** (depurination and strand breaks)
  • Hepatotoxicity
  • Immunosuppression
  • Alopecia
  • Carcinogenesis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is special about

Cyclophosphamide?

A

Nitrogen Mustard Aklylator - Cyclophosphamide

  • Consolidation Therapy (Step 2)
    • Active Form + –> Guanine N7
    • Acrolein (toxic) form –> **‘Hemorrhagic Cystitis’
  • -> Mensa** (Traps Acrolein)
  • No Hepatotoxicity
  • Requires activation by CYP450 w/in Liver
  • Tx: Non-Hodgkin, Ovarian, Breast cancer, Neuroblastoma, Solid tumors, Leukemia, Lymphomas
  • Side effects: Hemorrhagic cystitis (Mesna - protects Bladder, traps Acrolein and is protective)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Nitrosourea Alkylators?

A

Nitrosourea Alkylators?

“-mustine”

  • Lomustine
  • Carmustine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Lomustine

Carmustine

A

Nitrosourea Alkylators

  • Carmustine –> CNS
  • Lipid Soluble –> able to cross the BBB
  • Alkylation of DNA
  • DNA crosslinking and Carbomoylation of Proteins
  • Tx: Brain tumors
  • Toxic: CNS toxicity (Dizziness, Ataxia)
  • Delayed Severe Immunosuppression
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Platinum Alkylators?

A

Platinum Alkylators?

“-platin”

  • Cisplatin
  • Oxaliplatin
  • Carboplatin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Cisplatin

Oxaliplatin

Carboplatin

A

Platinum Alkylators

  • Causes DNA crosslinks
  • Testicular, Ovary, Bladder, and Lung Cancer
  • Cisplatin causes Nausea and Vomiting (use Ondansetron)
  • Toxic:
    • Nephrotoxicity -
      • ​Heavy metals are bad for Kidneys
      • Use Amifostine (protects Kidneys)
    • Ototoxicity (Deafness)
      • ​Listening to too many Platinum records will lead to Hearing Loss
      • Ears shaped like “C”s
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

“Natural” Microtubule Inhibitors?

A

“Natural” Microtubule Inhibitors

“Vin-“

  • Vincristine
  • Vinblastine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Vincristine

Vinblastine

A

“Natural” Microtubule Inhibitors

  • Microtubles are the Vines of the cells
  • Plant-derived; Bindds Beta-tubulin in Microtubles
  • -> Inhibits polymerization
  • -> Inhibition of Mitosis (M-phase) and Cytoskeletal movements (CNS)
  • Similar to Cochicine (used for Tx of Gout)
  • Induction Chemotherapy Agent for Solid tumors, Leukemias, Lymphomas
  • Side effects:
    • VinCriStiNe - CNS - (neurotoxicity), Wilms, Hodgkin
    • VinBlastine - Destruction of Blasts = Myelosuppression, Hodgkin, Testes, Kaposi
  • MDR - Mechanism of Resistance
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

“Natural” Microtubules Stabilizers?

A

“Natural” Microtubules Stabilizers

“Its TAXing to stay polymerized”

  • Paclitaxel
  • Docetaxel
  • Ixabepilone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Paclitaxel

Docetaxel

Ixabepilone

A

“Natural” Microtubules Stabilizers

  • Stabilize Polymerized Microtubules by Inhibiting Depolarization in Anaphase –> M phase Interruption
  • Side effects: Myelosuppression, Cardiotoxicity, Peripheral neuropathy (Ixabepilone only)
  • Ovarian and Breast Cancer
  • MDR - Mechanism of Resistance
  • Dont use Paclitaxel and Vincristine together.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

“Natural” Chemotherapies?

A

“Natural” Chemotherapies

“-poside”

  • Etoposide
  • Teniposide

“-tecan”

  • Irinotecan
  • Topotecan
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Etoposide

Teniposide

Irinotecan

Topotecan

A

“Natural” Chemotherapies

  • Podophyllotoxin derived - VP 16 and VP 25
  • Two Sides to every story = Topoisomerase II inhibitor
  • Leukopenia, Thrombocytopenia

Block S-phase supercoil uncoiling

  • Camptothecin derived
  • One tea can = Topoisomerase I inhibitor
  • Neutropenia
  • MDR is Mechanism of Resistance
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

“Natural” Anthracyclines?

A

“Natural” Anthracyclines

“-rubicin”

  • Doxorubicin
  • Daunorubicin
  • Dexrazoxane (iron Chelator)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Doxorubicin

Daunorubicin

A

“Natural” Anthracyclines

  • cin = antibiotic, rubbing alcolhol = Free Radicals
  • Anthraquionone ring –> DNA intercalator and Forms Free Radicals, Introduction of Single Strand Breaks and
    inhibits Topoisomerase II (S-phase halt)
  • Induce double stranded breaks –> cell death pathway
  • Induction Chemotherapy agent
  • Side effects:
    • Free radical disposition –> attacks cardiac cells
    • Rubbing alcohol = Dilated cardiomyopathy
    • Bone marrow suppression
    • Myelosuppression, Alopecia, Extravasation toxicity
  • MDR is Mechanism of Resistance
  • Antidote is Dexrazoxane - Iron chelator used to prevent Free Radical formation and Cardiotoxicity
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

“Natural” Antibiotic Chemotherapy?

A

“Natural” AntiBiotic Chemotherapie

  • Bleomycin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Bleomycin

A

“Natural” AntiBiotic Chemotherapy

  • Binds DNA and Iron (Fe2+ and O2)
  • -> Uses Iron to Depurinate and Depyrimidate DNA
  • -> Single and Double DNA Strand Breaks (‘scission’)
  • *–>** Problem in G2 phase of cell cycle
  • Testicular, Hodgkin’s Lymphoma, Head, Skin cancer
  • Side effects: Pulmonary fibrosis (lungs look like large B’s, Skin changes, Minimal myelosuppression
  • NOT MDR - Mechanism of Resistance
    • Increased DNA repair enzymes, decreased cellular uptake, Inactivation by Bleomycin hydrolase overexpression
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Antimetabolites?

A

Antimetabolites

  • Methotrexate (MTX)
  • 5-Fluorouracil (5-FU)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Methotrexate (MTX)

A

Methotrexate (MTX)

  • Folic acid analogue
  • Competitive inhibitor of DHFR (Dihydrofolate reductase)
  • -> Cannot perform single carbon transfers
  • -> Cannot synthesize DNA
  • Consolidation Therapy - for Leukemias, Lymphomas, Sarcomas, RA, Psoriasis, Abortion, Ectopic pregnancy
  • Side effects: Severe myelosuppression (requires Leucovorin rescue Bone marrow), Renal and Hepatotoxicity, Neurotoxicity, Teratogenicity, Mucositis
  • Mechanism of Resistance: Increased DHFR activity
21
Q

5-Fluorouracil (5-FU)

A

5-Fluorouracil (5-FU)

  • Suicide inhibitor of TS (Thymidylate synthase)
  • -> no dTMP produced –> 5-FUTP incorporated into RNA
  • -> Defective transcripts
  • Pyrimidine antimetabolite (S phase)
  • Bioactivated Inhibit TS
  • CRC, Basal cell Carcinoma (Topical) and Keratoses
  • Bone marrow Myelosuppression (not reversible w/ Leucovorin), Photosensitivity
  • Mechanism of Resistance: Overexpression of TS or TS mutations
22
Q

Pyrimidine Analogue Antimetabolites?

A

Pyrimidine Analogue Antimetabolites

“Cyt-“

  • Cytarabine
  • Gemcitabine
  • Azacitidine
  • Capecitabine
23
Q

Cytarabine

Gemcitabine

Azacitidine

Capecitabine

A

Pyrimidine Analogue Antimetabolites

  • Cytidine analogues
    • Cytarabine - inhibition of DNA polymerase, defective ligation and Premature Chain termination
    • Azacitidine - inhibits **DNA methyltransferase
  • -> Hypomethylation**
  • Consolidation therapy for Leukemias, Lymphomas, Myelodysplastic syndrome (Azacitidine)
  • Megaloblastic anemia, Leukopenia, Thrombocytopenia
  • Mechanism of Resistance: Decreased Cytosine Kinase activity, Increased Cytosine Deaminase activity
24
Q

Purine Analogue Antimetabolites?

A

Purine Analogue Antimetabolites

“Pure As Gold” - “Purine Adenine Guanine”

  • 6-mercaptopurine
  • 6-thioguanine
25
Q

6-mercaptopurine

6-thioguanine

A

Purine Analogue Antimetabolites

  • Converted to nucleoside monophosphates via
  • *HGPRT –>** Inhibit **de novo Purine synthesis
  • -> IncorporatedintoDNAandRNA
  • -> S phase inhibition**
  • HGPRT def. –> Lesch-Nyhan syndrome (Purine recovery)
    • Hypoxanthine and Guanine –> IMP and GMP
  • Bioactivated by HGPR transferase
  • Consolidation CT treatment of ALL, Immunosuppression,
  • Side effects: Myelosuppression, Hepatotoxicity
  • Allopurionol - Increased toxicity when used w/ 6-mercaptopurine (6-MP), Oxidation by Xanthine Oxidase
  • Mechanism of Resistance: HPRT mutations
26
Q

Kinase Inhibitors?

A

Kinase Inhibitors

“-nib”

  • Imatinib
  • Erlotinib
  • Gefitinib
  • Vemurafenib
27
Q

Imatinib

Erlotinib

Gefitinib

Vemurafenib

A

Kinase Inhibitors

  • Imatinib Mesylate - c-abl TK blocker
    • Philidelphia + Chrom. t(9;22)
    • CML (always). ALL (sometimes), AML (rarely)
  • Erlotinib, Gefitinib - EGF TK, nsc Lung Cancer
  • Vemurafenib - BRAF Serine/Threonine Kinase w/ V600E mutation; Melanoma
  • Better side effect profile than other Chemotherapy drugs, except
    • ​Congestive Heart Failure- all exceptVemurafenib
28
Q

Antibody Chemotherapies?

A

Antibody Chemotherapies

“-mab”

  • Rituximab
  • Bevacizumab
  • Trastuzumab
29
Q

Rituximab

Bevacizumab

Trastuzumab

A

Antibody Chemotherapies

  • Rituximab - anti-CD20 Ab - Non-Hodgkin’s Lymphoma
  • Bevacizumab - anti-VEGF Ab, Solid tumors, Increased clotting risk
  • Trastuzumab - aka Herceptin, anti-HER2 Ab (TK), HER2 positive Breast cancer; Cardiotoxicity
30
Q

Biological Agents?

A

Biological Agents

  • All-trans-retinoic acid (Vitamin A)
    • Treatment for Promeyelocytic Leukemia
    • Differentiating agent, Promotes differentiation of Promyelocytes
    • t(15;17) - Auer rods - Acute myelogenous leukemia M3 type of AML
    • “Differentiation syndrome” w/ respiratory distress, Pleural and pericardial effusions, CNS symptoms
  • Vorinostat
    • ​Histone Deacetylase Inhibitor
  • Bortezomib
    • Proteasome inhibitor
31
Q

L-asparaginase

A

L-asparaginase

  • Depletes Asparagine from Cancer cells
  • -> Protein synthesis inhibition
  • Induction chemotherapy agent
  • Hypersisitivity Risk, Hepatotoxicity
  • A/w increase risk of Pancreatitis!
32
Q

Prednisone

A

Prednisone

  • Induction of Apoptosis of T cells, may also work on Non-dividing cells
  • Induction chemotherapy agent
  • Cushing’s like syndrome (Weight gain, Hyperglycemia), Avascular necrosis, Immunosuppression
33
Q

Procarbazine

A

Alkalating Agent

  • Hodgkin
  • Side Effect: Bone marrow suppression, Leukemogenic (promotes Leukemia)
34
Q

Renal Toxicity Drugs?

A

Renal Toxicity Drugs

  • Cisplatin (Less Bone marrow suppression)
    • Use Amifostine to save the Kidneys!
  • Methotrexate (MTX)
    • Use Leucovorin for Rescue
35
Q

Pulmonary Toxicity Drugs?

A

Pulmonary Toxicity Drugs

  • Bleomycin (Less Bone marrow suppression)
  • Busulfan
  • Procarazine
36
Q

Cardiac Toxicity Drugs?

A

Cardiac Toxicity Drugs

  • Doxorubicin
  • Daunorubicin

Dexrazoxane –> Iron chelating agent that prevents Free radical formation and Saves the Heart

“Natural” Anthracyclines that forms Free Radicals

37
Q

Neurologic Toxicity Drugs?

A

Neurologic Toxicity Drugs

  • VinCriStiNe (CNS) (Less Bone marrow suppression)
  • Cisplatin
    • Use Amifostine to save the Kidneys!
38
Q

Immunosuppressive Toxicity Drugs?

A

Immunosuppressive Toxicity Drugs

  • Cyclophosphamide (& Hemorrhagic Cystitis)
    • Use Mesna to save the Bladder
  • Methotrexate
    • Use Leucovorin for Rescue Bone marrow
39
Q

Aldesleukin (IL-2) use?

A

Aldesleukin (IL-2)

  • Increases Lymphocyte differentiation
  • Increases Natural Killer cells (NK cells)
  • Use in Renal cell carcinoma and Metastatic Melanoma
40
Q

Interleukin-11 use?

A

Interleukin-11

  • Increase Platelet formation
  • Used in Thrombocytopenia
41
Q

Filgrastrim (G-CSF) use?

A

Filgrastrim (G-CSF)

  • Increase Granulocytes
  • Used in Bone marrow recovery
42
Q

Sargramostim (GM-CSF) use?

A

Sargramostim (GM-CSF)

  • Increase Granulocytes and Macrophages
  • Use for Bone marrow recovery
43
Q

Erythropoietin (EPO) use?

A

Erythropoietin (EPO)

  • Anemias, especially a/w Renal failure
44
Q

Thrombopoietin use?

A

Thrombopoietin

  • Thrombocytopenia
45
Q

S phase Drugs?

Anti-metabolite drugs –> interfere w/ DNA synthesis

A

S phase Drugs

  • Cytarabine (inhibits DNA polymerase)
  • 6-mercaptopurine (Purine antimetabolite)
  • 6-thioguanine (Purine antimetabolite)
  • 5-FU (Pyrimidine antimetabolite)
  • MTX (DHFR antimetabolite)
  • Hydroxyurea
  • Etoposide / Teniposide (Topo. II)
  • Irinotecan / Topotecan (Topo. I)
46
Q

G2 phase drugs?

A

G2 phase drugs

  • Bleomycin (Complexes w/ Fe2+ and O2 –> DNA strand ‘scission’ or cuts)
47
Q

M phase drugs?

A

M phase drugs

  • VinCriStiNe (Microtubule Inhibitors - depolymerization)
  • Vinblastine (Microtubule Inhibitors - depolymerization)
  • PacliTAXel (Blocks Depolymeriaztion of Microtubles - stabalizes in Anaphase and can’t let go)
48
Q

Non-cell Cycle specific phase?

A

Non-cell Cycle specific phase

  • Alkylating agents
    • Cyclophosphamide (Mesna saves bladder!)
    • Cisplatin (Amifostine prevents deafness!)
    • Procarbazine (can cause Leukemia!)
  • Antitumor ABX
    • Doxorubicin (Free Radicals fuck up the Heart)
    • Daunorubicin (Free Radicals fuck up the Heart)
  • Nitrosourea Alkylators
    • Lomustine (BBB –> CNS Tumors)
    • Carmustine (BBB –> CNS Tumors)
49
Q

Drugs that DO NOT suppress the Bone Marrow?

A

Drugs that DO NOT suppress the Bone Marrow?

  • Cisplatin (Renal toxicity)
  • Bleomycin (Pulmonary toxicity)
  • VinCriStiNe (Neurologic toxicity)

Pharmacology (29 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions