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Pharm 4 > Cancer Chemo > Flashcards

Cancer Chemo Flashcards

1
Q

Neoplasm

A

Uncontrolled growth of cells

May or may not form tumors. Usually don’t.

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2
Q

Invasiveness

A

Movement of neoplastic cells to adj. tissues

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3
Q

Metastasis

A

Movement of neoplastic cells to distant tissues

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4
Q

Tx of neoplasia

A

Surgery (solid tumor)

Radiation therapy (disrupt DNA of abnormal cells)

Pharmacologic agents (usually adjunct but sometimes primary modality)

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5
Q

Non-specific vs cell cycle specific agents

What about newer agents?

A

Non-specific

Act on cell in all phases of replication and resting-all cells

Form covalent bonds w/ all cell DNA

Prevent DNA cell fxn

Cell cycle specific

Act on cells replicating rapidly

Act on more defined sites

Anti-metabolites, enzyme inh, mitotic spindle inh.

Newer agents

Very specific

Kinase inh-“nibs”

Monoclonal antibodies-“nabs”

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6
Q

Alkylating agents

Names and mech.

A

Cyclophosphamide

Lomustine

Cisplatin

Mech

  • Add alkyl group to DNA
  • Causes DNA cross linking, inhibits cell replication, and RNA synth
  • Non specific
  • Inhibit non-replicating tumor cells
  • Worry about extravasation-leakage into surrounding tissue
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7
Q

Cyclophosphamide

A

Tx: Cancer

Mech: Alkylating agent

  • Add alkyl group to DNA
  • Causes DNA cross linking, inhibits cell replication, and RNA synth

Nitrogen mustard

Developed from mustard gas-destroys everything it touches

Prodrug given orally or IV

Stops cell from replicating once it hits DNA

Lots of collateral damage

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8
Q

Lomustine

A

Tx: Cancer

Mech: Alkylating agent

  • Add alkyl group to DNA
  • Causes DNA cross linking, inhibits cell replication, and RNA synth

Prodrug given IV

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9
Q

Cisplatin

A

Tx: Cancer

Mech: Alkylating agent

  • Add alkyl group to DNA
  • Causes DNA cross linking, inhibits cell replication, and RNA synth

Contains platinum (expensive)

Associated w/ renal damage and ototoxicity

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10
Q

Doxorubicin

And other rubicins

A

Tx: Cancer

Mech: Intercalates w/ DNA→blocks DNA and RNA synth

Produces free radicals→break down DNA strands

Class: Antibiotic (produced by microorganisms)

SE:

  • Can cause heart m. degeneration
    • Irr. due to free radicals
  • Fall in love w/ Ruby but she’s a free radical and breaks your heart.*
  • Rubicin. Causes free radicals–> heart damage. Breaks DNA*
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11
Q

Dactinomycin

A

Tx: Cancer

Mech: Intercalates w/ DNA and interferes w/ mRNA synth

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12
Q

Bleomycin

A

Tx: Cancer

Mech: Intercalates w/ DNA-causes DNA strand breakage

SE: pulmonary fibrosis

_Bl_eo_my_cin _bl_ows my DNA apart

_Bleo_mycin affects your ability to blow (Pulmonary fibrosis)

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13
Q

Methotrexate

A

Tx: Cancer (and RA and psoriasis)

Mech:

  • Analog of Folic Acid
  • Inh. enzyme: Dihydrofolate reductase
  • PABA→Folic acid⇒Dihydrofolic acid⇒tetrahydrofolic acid
    • ⇒ indicate where DHFR works

SE:

  • Myelosuppression-inh. of blood cells
    • Can be dealt w/ by giving leucovorin-THFA analog
      • Does not require DHFR
    • Will rescue “normal” cells, but not malignant cells
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14
Q

5-fluorouracil

A

Tx: Cancer

Mech: Inh. thymidylate synthatase→inh. thymidine synth

Prodrug–Pyrimidine analog

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15
Q

cytarabine

A

Tx: Cancer

Mech: Inh. DNA polymerase

Prodrug–Pyrimidine analog

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16
Q

6-mercaptopurine

A

Tx: Cancer

Mech: Converted in cell to an analog that inhibits several enzymes needed for purine synth

Prodrug–purine analog

  • Azathioprine=immunosuppressant prodrug. *
  • Gets converted into 6-mercaptopurine.*
  • Used for Chron’s, RA, and transplants*
17
Q

Vincristine and vinblastine

A

Tx: Cancer

Mech: Bind to microtubules and block cell mitosis

Route: IV

Natural product

18
Q

Paclitaxel

and other “-taxel”s

A

Tx: Cancer

Mech: Forms abnormal microtubules

Natural-from western yew tree. But now purely synthetic

”-_t_axels” make _t_errible _t_ubules

19
Q

Eribulin

A

Tx: Cancer

Mech: inh. microtubules-prevents mitosis, causes apoptosis

Fully synthetic

20
Q

Ixabepilone

A

Tx: Cancer

Mech: Binds to microtubules

Natural product

  • Ixabepilone *
  • Pixabepilone*
  • Pixy sticks=tube=microtubules*
  • Yeah this one is a stretch…*
21
Q

Etoposide

A

Tx: Cancer

Mech: Inhibits topoisomerase II→unrepairable DNA breaks

Natural product

  • You know its a topoisomerase inhibitor but which one?*
  • Add the first letter of one vs two to the front. If it makes sense it’s correct*
  • Tetoposide vs oetoposide*
  • **T-etoposide so topoisomerase Two***
22
Q

Topotecan

and irinotecan

A

Tx: Cancer

Mech: inhibits topoisomerase 1

  • You know its a topoisomerase inhibitor but which one?*
  • Add the first letter of one vs two to the front. If it makes sense it’s correct*
  • ttopotecan vs otopotecan*
  • **O-topotecan so topoisomerase One***
23
Q

Flutamide

and other “lutamides”

A

Tx: Cancer (prostate)

Mech: Blocks androgen receptor

Androgen receptor inside cell

Some tumors are hormone dependent

  • Careful:*
  • Flunomides-inh dihydroorate DH*
  • Flutamides-block androgen receptor*
24
Q

Abiraterone

A

Tx: Cancer (prostate)

Mech: Inhibits 17-hydroxylase lyase (CYP 17)

Inhibits androgen synthesis

Inhibits P450

  • Get this man a beer, at least 17 sips, he can’t make any androgens.*
  • Get this men abir-aterone, 17 CYP, can’t make any androgens*
  • P450 inhibitors from this unit: Abiraterone and -flunomides*
25
Q

Leuprolide

A

Tx: Cancer (prostate)

Mech: Activates GnRH receptor

Initially increases test synth, but eventually down regulates it

Used in comb. w/ other drugs

Lou Ferrigno was a pro bodybuilder w/ _AR_nold–initially boosted test. synth but eventually downregulated it

Leu-pro-lide _A_ctivates GnRH _R_eceptor–initially boosted test. synth but eventually downregulated it

26
Q

Tamoxifen

A

Tx: Cancer

Mech: Blocks estrogen receptor

SE:

  • Cataracts
  • Retinal changes

Tammy is as big as an ox because her estrogen receptor is blocked. She’s obsessed w/ Ron Swanson and has CRazy eyes

Tamoxifen blocks estrogen receptor. Side effects associated w/ eyes: Cataracts and Retinal damage

27
Q

Fulvestrant

A

Same as Tamoxifen

Tx: Cancer

Mech: Blocks estrogen receptor

SE:

  • Cataracts
  • Retinal changes
28
Q

Anastrazole

A

Tx: Cancer

Mech: Inh. aromatase

Aromatase converts test→estr.

  • Ana is strong b/c aromatase inh. so test can’t be converted to est. *
  • Ana-stro-zole. Aromatase Inh so no conversion to est.*
  • *Both of the estrogen blockers have a woman’s name and a reference to strength**

Tam-ox-ifen

Ana-stro-zole

29
Q

Prednisone

A

Tx: Cancer-leukemias and lymphomas

Mech: Inh. immune system fxns (refer to other lecture)

SE: lots of them

30
Q

Imitinib

A

Tx: Chronic myelogenous leukemia (CML)

Mech: Kinase inh.

In CML a gene codes for a kinase that shuts off apoptosis

So cells keep multiplying and don’t die=cancer

Imitinib inhibits the kinase so that apoptosis occurs again

Orally

SE: Edema (only a few SE)

31
Q

-nib

A

Nib=inhibitor, usually of a kinase

Newer “nibs” inhibit specific pathways in cancer cells

32
Q

Bortezomib

and carfilzomib

A

Tx: Multiply myeloma

Mech: Proteasome/protease inh.

Enzyme inhibitors

Allows excess proteins to accumulate and kill myeloma

“Zomibs” inh. proteaZomes

33
Q

Trastuzumab

A

Tx: Cancer

Mech: vs HER2

Human epidermal growth factor receptor

  • Don’t hook up w/ her too, that’s trashy*
  • Don’t hook up w/ HER2, thats tras-tuzumab*
34
Q

Bevacizumab

A

Tx: Cancer

Mech: blocks VEGF

Prevents Vascular epi. growth factor from binding to receptor

Tumor can only grow w/ blood supply-this blocks it

_Beave_rs are _veg_etarians

Beva-cizumab–VEGF

35
Q

Rituximab

A

Tx: Chronic lymphocytic leukemia and RA

Mech: vs CD20

36
Q

Ibritumomab

A

Tx: Cancer

Mouse MAB

Severe infusion rxn

37
Q

Difficulties in treating neoplasia

A
  1. Not all cancer cells divide rapidly
  2. Normall cells are affected
  • Hair
  • Bone marrow
  • GI
  • Skin
  • Oral mucosa
  • Reproductive

Increase in renal and bladder tox.

Chemobrain

  1. Not all cancer cells killed by drug–may regrow
  2. Cancer cells can become resistant
  3. Drugs may not enter CNS–problem for brain cancer
  4. Alkylating agents may cause neoplasia
38
Q

Successes w/ cancer

A

Curable (>5yr survival rate)

  • Choriocarcinoma
  • ALL
  • Hodgkin’s lymphoma
  • Testicular cancer
  • Osteosarcoma

Greater success:

  • Breast
  • Ovarian
  • Colon
  • Multiple myeloma

Give larger doses early on

Better combinations

Prevent side effects (EPO w/ bone marrow loss)

Pharm 4 (9 decks)

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