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Advanced Pharmacology > Antineoplastic Drugs > Flashcards

Antineoplastic Drugs Flashcards

1
Q

What are 3 Characteristics of cancer cells?

A
  1. persistent proliferation
  2. Grow invasively; beyond typical borders
  3. cells form metastases; they spread to remote sites through lymph or blood vessels.
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2
Q

Strategy 1 for antineoplastic drug treatment

A

Treatment of choice for disseminated, metastatic cancer

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3
Q

Strategy 2 for antineoplastic drug treatment

A

Adjuvant to surgery or radiation for solid tumors

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4
Q

Strategy 3 for antineoplastic drug treatment

A

Smart drugs are chemically linked to antibodies that target only cells with specific tumor antigen.
Problem is cancer cells mutate and antigen changes.

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5
Q

Strategy 4 for antineoplastic drug treatment

A

Rounds of treatment:
therapy_recovery_therapy…
often 8 rounds.

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6
Q

Cancer Immunotherapy

A

Highly selective, perhaps permanent, less toxic.
Only a fraction of patients respond on a subset of cancers.
Much research ongoing.

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7
Q

Monoclonal antibodies

A

Synthetic immune proteins that can be designed to attack a specific component of a cancer cell

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8
Q

Cancer vaccines

A

substances designed to trigger an immune response against a disease.
“Dream” for fighting cancer

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9
Q

Non-specific immunotherapy

A

General immune system stimulation to increase anti cancer activity.
Cytokines like interleukins and interferons

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10
Q

Categories of antineoplastic drugs

A
  1. Cytotoxic

2. Non-cytotoxic

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11
Q

Cytotoxic Drugs

A

Cause cellular injury.
Often called chemotherapy.
Administered in cycles.

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12
Q

Non-cytotoxic Drugs

A

Drugs that don’t cause cellular injury.

Immunotherapy, hormone therapy…

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13
Q

How does endocrine manipulation help to fight cancer?

A

20% male cancer and 40% female cancers grow in response to sex steroids.
One strategy is to interfere with hormones that control cell growth.

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14
Q

Leuprolide

A

A long-acting gonadotropin releasing hormone (GnRH) receptor agonist.
Suppresses release of LH and FSH, reducing production of estrogens and androgens.
Treats hormone-dependent prostate and breast CA

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15
Q

Anastrozole

A

aromatase inhibitor;
used to treat estrogen-positive breast CA in post menopausal patients;
Blocks synthesis of estradiol

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16
Q

Estradiol

A

Active sex steroid produced by ovaries (small amount by testes)

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17
Q

Exemestane (Aromasin)

A 
aromatase inhibitor (new);
Prevents development of breast CA in select risk groups;
Prophylactic
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18
Q

Cholesterol

A

Precursor for all steroid hormones

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19
Q

Aromatase Inhibitor

A

Blocks production of estradiol in ovaries, controlling hormone dependent CA growth.

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20
Q

Hormone Receptor Antagonists

A
  1. Tamoxifen

2. Flutamide

21
Q

Tamoxifen

A

an estrogen receptor antagonist in mammary tissue

22
Q

Flutamide

A

an androgen receptor antagonist (testosterone)

23
Q

Hormone Receptor Agonist

A

Prednisone

24
Q

Prednisone

A

A cortisol receptor agonist that induces leukocyte apoptosis; activates an inhibitory pathway that prevents DNA replication

25
Q

Inhibition of DNA Replication

A
  1. Cyclophosamide
  2. Cisplatin
    Both bind to DNA and inhibit replication.
    Both are Cytotoxic
26
Q

Cyclophosamide

A

Bind to DNA and inhibit replication.

Cytotoxic

27
Q

Cisplatin

A

Bind to DNA and inhibit replication.
Cytotoxic;
Renal toxic.

28
Q

Inhibition of RNA and Protein Synthesis

A 
Actinomycin D (an antibiotic)  binds to DNA and inhibits the catalytic activity of RNA polymerase.
Cytotoxic
29
Q

Actinomycin D

A

An antibiotic that binds to DNA and inhibits the catalytic activity of RNA polymerase.
Cytotoxic

30
Q

Asparaginase

A

catalyzes conversion of asparagine to aspartate; reduces blood levels of AA asparagine, essential for some leukemias.
Not Cytotoxic.

31
Q

Antimetabolites

A 
Inhibit enzymes that produce intermediates needed for CA cell division
Cytotoxic.
1. Methotrexate
2. Mercaptopurine
3. 5-flurouracil (5-FU)
32
Q

Methotrexate

A

an antimetabolite.

inhibits the enzyme that catalyzes production of folic acid

33
Q

Mercaptopurine

A

An antimetabolite.

Inhibits enzymes used in the production of purines

34
Q

5-flurouracil (5-FU)

A

An antimetabolite.

Inhibits enzymes used in production of pyrimidines

35
Q

Inhibitors of spindle fiber formation

A

Cytotoxic
Blocks mitosis
1. Vincristine/vinblastine
2. Taxol

36
Q

Vincristine/Vinblastine

A

Inhibitors of Spindle fiber formation.
Cytotoxic
They inhibit microtubule polymerization

37
Q

Taxol

A

Inhibitor of spindle fiber formation.
Cytotoxic
Stimulates uncontrolled polymerization of microtubules

38
Q

Oncogenes

A

Control CA cell growth;

  1. Control localized production of growth factors (GF) and cytokines; EGF, IGF
  2. Signal transduction events triggered by GF receptors; Tyrosine Kinase (TK)
  3. angiogenesis
  4. DNA Repair
39
Q

Herceptin

A

Interferes with production of local Growth factors.

Treats breast CA

40
Q

TK inhibitors

A

blocks signal transduction

Treats some myelogenous leukemia

41
Q

VEGF (Vascular endothelial GF) inhibitors

A

Monoclonal antibody inhibiting angiogenesis

Treats colorectal CA

42
Q

PARP (Poly ADP-ribose polymerase) Inhibitors

A

Prevent repair of DNA repair mechanisms.

Treats Non-small cell lung carcinoma

43
Q

Combination chemotherapy

A

CMF: cyclophosamide, methotrexate, and fluorouracil.
Advantages:
1. Each drug’s dose is reduced, thus reducing organ-specific toxicity
2. Inhibits cell division at more than one site making them more effective.
3. Helps prevents resistance.

44
Q

Pharmacotoxicology

A

Nonselective on cell division

Therapeutic index is near 1

45
Q

Toxic effects of chemotherapeutic agents

A

Bone marrow suppression causes:

  1. anemia. Treated with EPO.
  2. Leukopenia (low WBCs). Treated with a growth hormone, GMCSF.
46
Q

2nd Toxic effect of Chemotherapeutic agents

A

Suppression of GI tract cell division; walls become thin, causing ulcers, N/V.
Treated with Ondansetron, a serotonin receptor antagonist and Cimetidine, a H2 receptor antagonist.

47
Q

3rd Toxic effect of Chemotherapeutic agents

A

alopecia (temporary)

48
Q

4th Toxic effect of Chemotherapeutic agents

A

Sterility;

Reduces sperm counts and can induce premature menopause

49
Q

How do CA cells develop drug resistance?

A
  1. Increased production of conjugation enzymes, increasing metabolism and elimination
  2. Increased production of p-glycoproteins to transport drugs out of cells. (Vincristine)
  3. Gene amplification: Increase the production of the inhibited enzyme. Increase folic acid production in response to methotrexate.

Advanced Pharmacology (7 decks)

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