Antineoplastic Drugs

Question 1

What cell phase are Alkylators?

Answer 1

Non-cell-cycle-phase specific and most active in resting phase (G0)

Question 2

How do Alkylating agents work?

Answer 2

• Replacement of hydrogen by an alkyl group

- Produce abnormalities and cross-links in DNA, RNA and proteins, preventing normal cell function

Question 3

How do Anti-metabolites work?

Answer 3

• Cell cycle specific (S phase)
• Interfere with DNA/RNA and protein synthesis during S cycle, and therefore are best for rapidly dividing cancers
• By blocking some types of synthesis, apoptosis can occur
• Resembles metabolic material, so it incorporates into DNA strands and breaks it

Question 4

If a drug belongs to an anti-tumor antibodies group, what suffixes are they likely to end in?

Answer 4

• rubicin

- mycin

Question 5

What are anti-tumor antibiotics?

Answer 5

• Work as both antimicrobial and cytotoxic, cell-cycle nonspecific, to produce toxic effects
• Most act as a way to regulate the twisting/winding of DNA

Question 6

What is targeted therapy?

Answer 6

• The ability to deliver drugs directly to tumors

- Interferes with growth factor signaling (which is involved in the initiating and progression of certain cancers)

Question 7

What are monoclonal antibodies?

Answer 7

• Immunoglobulin molecules from cloned cells, as a targeted therapy
• Works by blocking ligand when binding with an antigen

Question 8

What is hormone therapy?

Answer 8

• Tx of cancers of hormone-derived or hormone-sensitive tumors
• Blocks the stimulation of steroid-specific receptors on the surfaces of cells, thereby blocking the cell from receiving normal hormone growth stimulation
• Decreases the tumor growth factor

Question 9

What are antineoplastic drug toxicities often the result of?

Answer 9

Dose dependent and cumulative dose

Question 10

What causes the toxicities of antimetabolite therapy?

Answer 10

• Suppression of cell growth in mitotically active tissues (eg. bone marrow, GI, skin)

Question 11

What is the suffix for anti-androgens?

Answer 11

• lutamide

Question 12

What is the suffix for topoisomerase I inhibitors?

Answer 12

• otecan

Question 13

What class is topotecan?

Answer 13

• Plant alkaloids

- Topoisomerase I inhibitors

Question 14

What class is irinotecan?

Answer 14

• Plant alkaloids

- Topoisomerase I inhibitors

Question 15

Are nitrosureas CCPNS or CCPS?

Answer 15

CCPNS

Question 16

How do nitrosurea’s work?

Answer 16

Damage DNA or interfere with DNA replication

Question 17

Are vinca plant alkaloids CCPS or CCPNS?

Answer 17

CCPS (M-phase)

Question 18

How do vinca plant alkaloids work?

Answer 18

Cell cycle phase arrest

Question 19

How do corticosteroids work?

Answer 19

• Inhibits the stimulation of steroid-specific receptors located on the surface of cells
• Blocks the receptors to prevent cells from receiving normal hormonal growth stimulation = decreases growth fraction of tumor

Question 20

How do miscellanous agents work?

Answer 20

• CCPNS

- Inhibit DNA, RNA or protein synthesis

Question 21

What are the different classes of hormone therapies?

Answer 21

• Corticosteroids
• Androgens
• Estrogens
• Anti-estrogen’s, progestins
• Estrogen-receptor antagonists
• Aromatase inhibitors (aromatase = needed for estrogen synthesis)
• Luteinizing hormone-releasing hormone analogues
• Gonadotropin-releasing hormone antagonist
• Antiandrogens

Question 22

What is tamoxifen?

Answer 22

• Most common hormone modulator for estrogen positive breast Ca
• Selective estrogen receptor modular (SERM)
• Blocks estrogen in the breast tissue by sitting in place of the estrogen receptor - without estrogen attaching, there is no signal to grow and multiply

Question 23

What are the side effects of tamoxifen?

Answer 23

• Think of common birth control side effects, similar *
• Hot flashes may occur once you start taking it and usually improves with use
• Vaginal discharge or dryness
• Nausea
• Headache
• Muscle or joint pain
• Skin rashes
• Fatigue
• Swelling
• HTN
• Blood clots **
• Weight changes
• Hair thinning
• Changes in cholesterol or triglycerides
• Endometrial cancer (rarely occurs with prolonged use)

Question 24

What are management options for hot flashes?

Answer 24

• Take tamoxifen at bedtime
• If night sweats are interrupting sleep, take tamoxifen in the morning
• Avoid alcohol, spicy foods, and caffeine
• Regular exercises
• Cool environment
• Wear layers

Question 25

What is goserelin?

Answer 25

• Gonadotropin-releasing hormone agonist
• GRH stimulates the pituitary to produce more sex hormones (follice and lutenizing) by blocking the GRH receptor site
• Treats prostate and breast cancer
• In men, decreases testosterone
• In women decreases estrogen and progesterone

Question 26

What are the side effects of goserelin?

Answer 26

• Effects are from lowered estrogen and testosterone
• Increased bone pain (if mets to the bones)
• Hot flashes
• Fatigue
• Impotence
• Decreased libido
• HA
• Weight changes
• Sugar fluctuations
• Increase in cholesterol or triglycerides
• Bone loss happens gradually, increased risk of #’s

Question 27

How are chemo agents classified?

Answer 27

• Cell cycle or non cycle specific

- further classified into subgroups based on chemical structure, biological source and the effects on the cell cycle

Question 28

What are the different classifications of chemo agents?

Answer 28

• Alkylating agents
• Antitumor antibiotics
• Antimetabolites
• Nitrosureas
• Plant alkaloids
• Hormonal agents

Question 29

What chemo drug classes are cycle specific?

Answer 29

Plant alkaloids in M phase (stops cell cycle)

Antimetabolites in S phase (stops DNA synthesis, resembles metabolic elements for cell growth)

Question 30

What chemo classes are cycle non-specific?

Answer 30

• AA (break DNA helix, hinders replication)
• Antitumor antibiotics (bind to DNA and interferes with replication)
• Hormones (interfere with protein synthesis and direct lytic action)