Principles and definitions + alkylating agents

Question 0

What is growth fraction?

Answer 0

cytotoxic drugs are more effective against tumors that have high growth fraction(high turn over rate). Normal cells with high growth fraction, e.g. bone marrow, will show more side effects from chemo therapy.

Question 1

What is the Log-kill hypothesis?

Answer 1

A fixed percentage of tumor cells that are killed from a certain anticancer drug.

Question 2

Where do we use drugs with cell-sycle specificity?

Answer 2

In cancers with high growth fraction, e.g lymphomas and leukemias

Question 3

S phase specific drugs general picture?

Answer 3

This class of drugs is called antimetabolites, as they “mimick” certain metabolites of the S phase

Question 4

G2 specific anticancer drug?

Answer 4

bleomycin

Question 5

M phase anticancer drugs work by …….

Answer 5

inhibiting microtubules

Question 6

Vinblastine and Vincristine moa?

Answer 6

inhibit polymerasation of microtubules

Question 7

Paclitaxel moa?

Answer 7

inhibits depolymerization of microtubules - therby creating an overly stable and rigid microtubule which prevents cell division

Question 8

Which drugs work in G0 phase?

Answer 8

drugs that can work on cells that are in rest - slow growing tumors.

• Alkylating agents
• Antitumor antibiotics
• Nitrosoureas
• Cisplatin

Question 9

Cyclophosphamide moa?

Answer 9

attack guanine N7 rendering DNA dysfunctional

Question 10

What i acrolein?

Answer 10

toxic metabolite of cyclophosphamide. May result in hemorrhagic cystitis

Question 11

Cisplatin moa?

Answer 11

alkylating agent that cross-links DNA strands

Question 12

Cisplatin side effects?

Answer 12

One of the worst to cause nausea and vomiting

Question 13

ondansetron area of use?

Answer 13

antiemetic to cure side effects of chemo therapy

Question 14

Ondansetron moa?

Answer 14

binds to 5H-T3 serotonin receptor

Question 15

Procarbazine moa and area of use?

Answer 15

alkylating agent used to treat Hodgkin

Question 16

procarbazine side effect?

Answer 16

bone marrow suppression and leukemogenic

Question 17

Doxorubicin moa?

Answer 17

• interaclator
• forms free radicals
• inhibits topoisomerase

Question 18

Doxorubicin side effects?

Answer 18

delayed congestive hert failure due to damage to myocardium from free radicals(heart can not metabolize these very well)

Question 19

Dexrazoxane area of use?

Answer 19

prevent myocardial free radical damage from doxorubicin

Question 20

General moa of alkylating agents?

Answer 20

They target nitrogens( esp. N-7 of guanine) and oxygens and purines and pyrimidines

Question 21

Busulfan moa and area of use?

Answer 21

Busulfan inhibits granulocytopoiesis. It is used in CML

Question 22

Name 3x Nitrosoureas and a handy “special effect” that they have

Answer 22

Carmustine, lomustine, semustine. They are lipophilic and cross the BBB.

Question 23

S phase alkylating agents?

Answer 23

Methotrexate
6-mercaptopurine
Hydroxyurea
Cytarabine

Question 24

Bleomycin and busulfan side effects?

Answer 24

pulmonary fibrosis