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Hematology & Oncology > Basic Pharmacology of Cancer Chemotherapies > Flashcards

Basic Pharmacology of Cancer Chemotherapies Flashcards

1
Q

Are alkylating agents cell cycle dependent? How do they work?

A

NO- they are NOT CELL CYCLE DEPENDENT

they form electrophilic bonds in Guanine of DNA which HALTS CELL REPRODUCTION

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2
Q

What are the Nitrogen Mustards? What drugs are included in this category?

A

Nitrogen Mustards are ALKYLATING AGENTS

CYCLOPHOSPHAMIDE

Melphalan

Chlorambucil

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3
Q

Hemorrhagic cystitis is a toxicity associated with Cyclophosphamide. What causes the bladder toxicity, and how can it be prevented?

A

Acrolein is a toxic metabolite of cyclophosphomide that causes hemorrhagic cystitis.

Hemorrhagic cystitis can be partially prevented by the use of MESNA- the thiol group of mesna binds the toxic metabolite

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4
Q

What are the Nitrosureas? What category of anti-cancer drugs do they belong to?

A

“-MUSTINE” + STREPTOZOCIN

CarMUSTINE

LoMUSTINE

SeMUSTINE

Nitrosureas= ALKYLATING AGENTS

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5
Q

What category of drugs can cross the BBB and are therefore useful for the treatment of brain tumors?

A

NITROSOUREAS (“-mustine +Streptozocin)

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6
Q

What drug destroys pancreatic beta cells & is used to treat insulinomas?

A

Streptozocin (Nitrosurea Alkylating Agent)

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7
Q

What category of anti-cancer drugs is Busulfan?

A

Alkylating Agent (Alkyl Sulfonate)

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8
Q

What is Busulfan primarily used to treat?

A

CML

Ablation of pt’s bone marrow before BM transplantation

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9
Q

What phase of the cell cycle do Antimetabolites target?

A

S-PHASE

Highly toxic to rapidly proliferating cells (including normal tissue- hair & GI tract)

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10
Q

What drugs are in the antimetabolite category?

A

Methotrexate (MTX)

5-Fluorouracil (5-FU)

Cytarabine (ara-C)

Azathioprine

6-Mercaptopurine (6-MP)

6-Thioguanine (6-TG)

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11
Q

What is the mechanism of MTX? Can myelosuppression be reversed?

A

Folic Acid analog inhibits DHFR–>Decreases THF available for conversion of dUMP–>dTMP–>

Decreased dTMP, DNA & protein synthesis

Myelosuppression IS reversible with LEUCOVORIN (folinic acid rescue)

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12
Q

What is the mechanism of 5-FU? Can myelosuppression be reversed?

A

PYRIMIDINE analog bioactivated to 5F-dUMP–> covalently complexes to folic acid–>

INHIBITS THYMIDYLATE SYNTHASE–> decrease in dTMP

Myelosuppression is NOT REVERIBLE w Leucovorin

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13
Q

What is the mechanism of Cytarabine (Ara-C)?

A

Pyrimidine Analog (Cytidine) INHIBITS DNA POLYMERASE

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14
Q

What are the toxicities associated w Ara-C?

A

Leukopenia

Thrombocytopenia

Megaloblastic Anemia

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15
Q

Azathioprine, 6-MP, & 6-TG all share the SAME mechanism of action. What is the mechanism?

What enzyme are these drugs metabolized by? (What drug increases their toxicity?)

A

PURINE ANALOGS activated by HGPRT & decrease De Novo Purine Synthesis

Metabolized by XANTHINE OXIDASE (Allopurinol increases their toxicity EXCEPT for 6-Thioguanine- 6-TG)

Use 6-TG in pts taking Allopurinol

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16
Q

What is the mechanism of Antitumor Antibiotics? Give examples of antitumor antibiotics

A

Intercalate DNA strands–> free radical formation

Dactinomycin

Anthracyclines (Doxorubicin, Daunorubicin & Idarubicin)

Bleomycin

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17
Q

What phase of the cell cycle does Bleomycin affect? Mechanism?

A

G2 & M phase

Complexes with iron & reacts with oxygen–>Induces free radical formation which causes BREAKS in DNA strands

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18
Q

What drugs are Microtubule Inhibitors aka ANTIMITOTICS?

A

Vinca Alkaloids (Vincristine & Vinblastine)

Paclitaxel & Taxols

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19
Q

What phase of the cell cycle do Vinca Alkaloids (Vincristine & Vinblastine) affect? Mechanism?

A

M-phase

Bind to TUBULIN & block polymerization of microtubules so that mitotic spindle cannot form.

(Think of Microtubles= M-phase as the VINes of your cells)

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20
Q

What are the toxicities associated with Vincristine & Vinblastine?

A

Vincristine= NEUROTOXIC (areflexia, peripheral neuritis, paralytic ileus)

VinBLASTine BLASTS Bone marrow (suppression)

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21
Q

What phase of the cell cycle do the Taxenes (Paclitaxel & Docetaxel) act on? Mechanism?

A

G2 & M-Phase

Bind TUBULIN–> hyperstabilizes polymerized microtubules so the mitotic spindle cannot break down & anaphase can not procede

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22
Q

Does the action of anticancer drugs follow first-order or second- order kinetics?

A

First Order- rate of elimination is directly proportional to the drug concentration (constant FRACTION of drug is eliminated per unit time)

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23
Q

What is responsible for multidrug resistance of chemotherapeutic agents (ie pumping drugs out of cells)?

A

P-glycoprotein is an ATP-dependent membrane efflux transporter responsible for pumping drugs out of cells

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24
Q

Cancer Chemotherapy agents commonly associated with stomatitis & esophagitis?

A

MTX

5-FU

Dactinomycin

25
Q

Hepatotoxic Chemo agents?

A

Etoposide

L-Asparaginase

26
Q

Pancreatitis associated chemo agents?

A

6-MP

Busulfan

Cyclophosphamide

27
Q

Cutaneous Toxicity (Hand-Foot Syndrome)

A

L-Asparaginase

5-FU

28
Q

Dilsufiram-Type Rxn

A

Procabazine

29
Q

What is the antidote that binds to and inactivates the toxic metabolites responsible for cisplatin induced nephrotoxicity?

A

AMIFOSTINE

30
Q

Which agent is used to decrease the incidence & severity of doxorubicin-induced cardiomyopathy in pts w metastatic BC who have received a lifetime cumulative Doxo dose >300mg?

A

DEXRAZOXANE- iron chelating agent

31
Q

What RXN does DHFR catalyze?

A

Conversion of folic acid to tetrahydrofolic acid (active form)

32
Q

What drug is used as a “rescue medication” in pts taking MTX?

A

Leucovorin

acts as an active form of folic acid (replenishing the folate pool) that has bypassed the inhibited DHFR & is more readily taken up by normal cells than by malignant cells

33
Q

What are the adverse effects of MTX?

A

Stomatitis

BMS

Urticaria

Alopecia

NVD

Nephrotoxicity

Hepatotoxicity

Pulmonary Toxicity

Neurotoxicity

34
Q

What immunosuppressive drug becomes active only after being converted to 6-MP?

A

Azathioprine

35
Q

What enzyme activates 6-MP to its corresponding nucleotide form by adding a ribose phosphate to its structure?

A

Hypoxanthine-Guanine Phosphoribosyl Transferase (HGPRT)

36
Q

What are the major s/e of 6MP?

A

NVD

Hepatotoxicity

BMS

37
Q

Are the antitumor antibiotics CCS (Cell Cycle Specific)?

A

Yes- S Phase

38
Q

What is the MOA of Anthracycline Antibiotics?

A

inhibition of DNA topoisomerase 2

formation of free radicals–> DNA strand breaks DNA intercalation Inhibition of DNA & RNA synthesis

39
Q

Give example of anticancer alkylating agents:

A

Cyclophosphamide

Isofosfamide

Mechlorethamine

Nitrosoureas (-mustine + Streptozotocin)

Cisplatin & Carboplatin

40
Q

What plant are the vinca alkaloids derived from?

A

Periwinkle plant

41
Q

Which plant is paclitaxel a derivative of?

A

Needles of the Western or Pacific Yew Tree

42
Q

What are the adverse effects of Paclitaxel?

A

Neutropenia

Alopecia

Hypersensitivity RXNs

43
Q

What adverse s/e doe vincristine & vinblastine have in common? Are they vesicants?

A

NVD

Alopecia

Phlebitis

Cellulites

They are STRONG Vesicants

44
Q

How are hypersensitivity rxns prevented in pts receiving paclitaxel cancer chemotherapy?

A

Pretreatment w DIPHENHYDRAMINE & DEXAMETHASONE

45
Q

Give 2 examples of epipodophylotoxin cancer chemotherapeutic agents

A
  1. Etoposide
  2. Teniposide
46
Q

What is the MOA of the epipodophyllotoxin cancer chemotherapeutic agents?

A

Inhibition of DNA topoisomerase 2–> increase DNA degradation

47
Q

Give 2 examples of chemotherapeutic agents that inhibits DNA topoisomerase 1

A
  1. Topotecan
  2. Irinotecan
48
Q

What is the MOA of L-asparaginase?

A

Hydrolyzes asparagine to aspartic acid & ammonia, thereby depriving tumor cells of asparagine required for protein synthesis

49
Q

Give a brief summary of what happens during each of the following phases of the cell cycle.

What cancer drugs act at each phase?

A

G0- Cells are not actively dividing (resting state)

G1- Enzymes & proteins required for DNA replication are synthesized

S- Replication of DNA (ANTIMETABOLITES & ETOPOSIDE)

G2- Enzymes & proteins required for mitosis are synthesized (BLEOMYCIN & ETOPOSIDE)

M- Mitosis Occurs (VINCA ALKALOIDS & TAXOLS)

50
Q

What is the MOA of Bavacizumab? What is its clinical use?

A

Monoclonal antibody against VEGF- inhibits angiogenesis

used for solid tumors

51
Q

What is the MOA of VEMURAFENIB?

A

small molecule inhibitor of forms of the B-Raf kinase with the V600E mutation

used for METASTATIC MELANOMA

52
Q

MOA of RITUXIMAB?

Clinical Use?

A

Monoclonal antibody against CD20 (found on most B-cell neoplasms)

Used for Non-Hodgkin’s Lymphoma & RA (w MTX)

53
Q

MOA of IMATINIB?

Clinical Use?

S/E?

A

Philadelphia chromosome bcr-abl TYROSINE KINASE inhibitor

Use for CML, & GI stromal tumors

Toxicity= Fluid Retention

54
Q

What is the major toxicity associated with TRASTUZUMAB (Herceptin)?

A

CARDIOTOXICITY

55
Q

What is the MOA of Trastuzumab? What type of cancer is it useful for?

A

Monoclonal antibody against HER2 (Human Epidermal growth factor Receptor 2) (c-erbB2) a TYROSINE KINASE

Usesful to kill HER-2 positive breast cancer cells that overexpress HER-2, possibly through antibody-dependent cytotoxicity

56
Q

What is the MOA of Tamoxifen & Raloxifene?

A

SERMs- receptor blockers in breast & agonists in bone (promote bone growth)

Block the binding of estrogen to estrogen receptor-positive cells

57
Q

Which SERM increases the risk of endometrial cancer?

A

TAMOXIFEN due to its partial agonist activity in endometrium

(Raloxifene has no increased risk of endometrial carcinoma because it is an endometrial antagonist)

58
Q

MOA of Hydroxyurea?

A

inhibits RIBONUCLEOTIDE REDUCTASE

decreases DNA Synthesis

S-Phase Specific

Hematology & Oncology (3 decks)

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