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Advanced Pharmacology > Antineoplastic Drugs > Flashcards

Antineoplastic Drugs Flashcards

(49 cards)

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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

Study These Flashcards
A
  1. Tamoxifen

2. Flutamide

21
Q

Tamoxifen

Study These Flashcards
A

an estrogen receptor antagonist in mammary tissue

22
Q

Flutamide

Study These Flashcards
A

an androgen receptor antagonist (testosterone)

23
Q

Hormone Receptor Agonist

24
Q

Prednisone

Study These Flashcards
A

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

25
Inhibition of DNA Replication
1. Cyclophosamide 2. Cisplatin Both bind to DNA and inhibit replication. Both are Cytotoxic
26
Cyclophosamide
Bind to DNA and inhibit replication. | Cytotoxic
27
Cisplatin
Bind to DNA and inhibit replication. Cytotoxic; Renal toxic.
28
Inhibition of RNA and Protein Synthesis
``` Actinomycin D (an antibiotic) binds to DNA and inhibits the catalytic activity of RNA polymerase. Cytotoxic ```
29
Actinomycin D
An antibiotic that binds to DNA and inhibits the catalytic activity of RNA polymerase. Cytotoxic
30
Asparaginase
catalyzes conversion of asparagine to aspartate; reduces blood levels of AA asparagine, essential for some leukemias. Not Cytotoxic.
31
Antimetabolites
``` Inhibit enzymes that produce intermediates needed for CA cell division Cytotoxic. 1. Methotrexate 2. Mercaptopurine 3. 5-flurouracil (5-FU) ```
32
Methotrexate
an antimetabolite. | inhibits the enzyme that catalyzes production of folic acid
33
Mercaptopurine
An antimetabolite. | Inhibits enzymes used in the production of purines
34
5-flurouracil (5-FU)
An antimetabolite. | Inhibits enzymes used in production of pyrimidines
35
Inhibitors of spindle fiber formation
Cytotoxic Blocks mitosis 1. Vincristine/vinblastine 2. Taxol
36
Vincristine/Vinblastine
Inhibitors of Spindle fiber formation. Cytotoxic They inhibit microtubule polymerization
37
Taxol
Inhibitor of spindle fiber formation. Cytotoxic Stimulates uncontrolled polymerization of microtubules
38
Oncogenes
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
Herceptin
Interferes with production of local Growth factors. | Treats breast CA
40
TK inhibitors
blocks signal transduction | Treats some myelogenous leukemia
41
VEGF (Vascular endothelial GF) inhibitors
Monoclonal antibody inhibiting angiogenesis | Treats colorectal CA
42
PARP (Poly ADP-ribose polymerase) Inhibitors
Prevent repair of DNA repair mechanisms. | Treats Non-small cell lung carcinoma
43
Combination chemotherapy
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
Pharmacotoxicology
Nonselective on cell division | Therapeutic index is near 1
45
Toxic effects of chemotherapeutic agents
Bone marrow suppression causes: 1. anemia. Treated with EPO. 2. Leukopenia (low WBCs). Treated with a growth hormone, GMCSF.
46
2nd Toxic effect of Chemotherapeutic agents
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
3rd Toxic effect of Chemotherapeutic agents
alopecia (temporary)
48
4th Toxic effect of Chemotherapeutic agents
Sterility; | Reduces sperm counts and can induce premature menopause
49
How do CA cells develop drug resistance?
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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