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GI: Cancer Therapy Drugs Flashcards

1
Q

Alkylating Agents?

A
  • Melphalan
  • Chlorambucil
  • Cyclophosphamide
  • Lomustine
  • Carmustine
  • Cisplatin
  • Oxaliplatin
  • Carboplatin
  • Procarbazine
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2
Q

Nitrogen Mustard Alkylators?

A

Nitrogen Mustard Alkylators?

  • Melphalan
  • Chlorambucil
  • Cyclophosphamide
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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
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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)
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5
Q

Nitrosourea Alkylators?

A

Nitrosourea Alkylators?

“-mustine”

  • Lomustine
  • Carmustine
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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
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7
Q

Platinum Alkylators?

A

Platinum Alkylators?

“-platin”

  • Cisplatin
  • Oxaliplatin
  • Carboplatin
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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
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9
Q

“Natural” Microtubule Inhibitors?

A

“Natural” Microtubule Inhibitors

“Vin-“

  • Vincristine
  • Vinblastine
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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
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11
Q

“Natural” Microtubules Stabilizers?

A

“Natural” Microtubules Stabilizers

“Its TAXing to stay polymerized”

  • Paclitaxel
  • Docetaxel
  • Ixabepilone
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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.
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13
Q

“Natural” Chemotherapies?

A

“Natural” Chemotherapies

“-poside”

  • Etoposide
  • Teniposide

“-tecan”

  • Irinotecan
  • Topotecan
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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
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15
Q

“Natural” Anthracyclines?

A

“Natural” Anthracyclines

“-rubicin”

  • Doxorubicin
  • Daunorubicin
  • Dexrazoxane (iron Chelator)
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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
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17
Q

“Natural” Antibiotic Chemotherapy?

A

“Natural” AntiBiotic Chemotherapie

  • Bleomycin
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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
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19
Q

Antimetabolites?

A

Antimetabolites

  • Methotrexate (MTX)
  • 5-Fluorouracil (5-FU)
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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
6-mercaptopurine 6-thioguanine
Purine Analogue Antimetabolites * Converted to nucleoside monophosphates via * *HGPRT --\>** Inhibit **de novo Purine synthesis - -\> Incorporated**into**DNA**and**RNA - -\> 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
Kinase Inhibitors?
Kinase Inhibitors **"-nib"** * Imati**nib** * Erloti**nib** * Gefiti**nib** * Vemurafe**nib**
27
Imatinib Erlotinib Gefitinib Vemurafenib
Kinase Inhibitors * Imati**nib** Mesylate - **c-abl** TK blocker * **Philidelphia +** Chrom. **t(9;22)** * **CML (always).** **ALL (sometimes), AML (rarely)** * Erloti**nib**, Gefiti**nib** - EGF TK, nsc Lung Cancer * Vemurafe**nib - BRAF** Serine/Threonine Kinase w/ **V600E** mutation; **Melanoma** * **Better side effect profile than other Chemotherapy drugs, except** * **​****Congestive Heart Failure**- all except**Vemurafenib**
28
Antibody Chemotherapies?
Antibody Chemotherapies **"-mab"** * Rituxi**mab** * Bevacizu**mab** * Trastuzu**mab**
29
Rituximab Bevacizumab Trastuzumab
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
Biological Agents?
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
L-asparaginase
L-asparaginase * Depletes **Asparagine** from Cancer cells - -\> **Protein synthesis inhibition** * **Induction** chemotherapy agent * **Hypersisitivity** Risk, **Hepatotoxicity** * A/w increase risk of **Pancreatitis!**
32
Prednisone
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
Procarbazine
Alkalating Agent * Hodgkin * Side Effect: Bone marrow suppression, Leukemogenic (**promotes Leukemia**)
34
Renal Toxicity Drugs?
Renal Toxicity Drugs * Cisplatin (Less Bone marrow suppression) * Use **Amifostine** to save the Kidneys! * Methotrexate (MTX) * Use **Leucovorin** for **Rescue**
35
Pulmonary Toxicity Drugs?
Pulmonary Toxicity Drugs * Bleomycin (Less Bone marrow suppression) * Busulfan * Procarazine
36
Cardiac Toxicity Drugs?
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
Neurologic Toxicity Drugs?
Neurologic Toxicity Drugs * Vin**C**ri**S**ti**N**e (CNS) (Less Bone marrow suppression) * Cisplatin * Use **Amifostine** to save the Kidneys!
38
Immunosuppressive Toxicity Drugs?
Immunosuppressive Toxicity Drugs * Cyclophosphamide (& **Hemorrhagic Cystitis**) * Use **Mesna** to save the Bladder * Methotrexate * Use **Leucovorin** for **Rescue Bone marrow**
39
Aldesleukin (IL-2) use?
Aldesleukin (IL-2) * *Increases* **Lymphocyte** differentiation * *Increases* Natural Killer cells (**NK cells**) * Use in **Renal cell carcinoma** and **Metastatic Melanoma**
40
Interleukin-11 use?
Interleukin-11 * *Increase* Platelet formation * Used in **Thrombocytopenia**
41
Filgrastrim (G-CSF) use?
Filgrastrim (G-CSF) * *Increase* **Granulocytes** * Used in Bone marrow recovery
42
Sargramostim (GM-CSF) use?
Sargramostim (GM-CSF) * *Increase* **Granulocytes** and **Macrophages** * Use for Bone marrow recovery
43
Erythropoietin (EPO) use?
Erythropoietin (EPO) * Anemias, especially a/w Renal failure
44
Thrombopoietin use?
Thrombopoietin * Thrombocytopenia
45
S phase Drugs? Anti-metabolite drugs --\> interfere w/ DNA synthesis
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
G2 phase drugs?
G2 phase drugs * **Bleomycin** (Complexes w/ Fe2+ and O2 --\> DNA strand 'scission' or cuts)
47
M phase drugs?
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
Non-cell Cycle specific phase?
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
Drugs that **DO NOT** suppress the Bone Marrow?
Drugs that DO NOT suppress the Bone Marrow? * **Cisplatin** (Renal toxicity) * **Bleomycin** (Pulmonary toxicity) * **VinCriStiNe** (Neurologic toxicity)

Pharmacology (29 decks)

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