Chemotherapy drugs.

Question 1

List the toxic effects of chemotherapy

Answer 1

bone marrow suppression
impaired wound healing
loss of hair 
damage to GI epithelium 
growth stunted 
bleeding/bruising 
N&V
Kidney damage

Question 2

What do Alkylating Agents do?

Answer 2

Target cells in the S phase. Form covalent bonds with DNA to prevent uncoiling which inhibits replication.

Question 3

Name the 4 different classes of alkylating agents…

Answer 3

Nitrogen Mustards
Nitrosoureas
Platinum compounds
Others

Question 4

What is Cyclophosphamide?

Answer 4

A nitrogen mustard. Prodrug - can be administered orally. Activated into Acrolein in the liver.

Question 5

Name some other nitrogen mustard drugs…

Answer 5

Melphalan, chlorambucil, bendamustine, estramustine

Question 6

Carmustine (IV) and Lomustine (oral) are examples of what?

Answer 6

Nitrosoureas. They are given for CNS tumours.

Question 7

Cisplatin is a what?

Answer 7

A Platinum Compound.

Question 8

How does Cisplatin work and what type of cancers can it treat?

Answer 8

Binds to RND, DNA and protein. Binds to purine bases. Testicular, Ovarian, Cervical, Lung, Bladder, Head and neck cancers

Question 9

What are the side effects of Cisplatin?

Answer 9

V. nephrotoxic - requires hydration/infusion
Causes severe N&V
Risk of tinnitus, peripheral neuropathy, gout and anaphylaxis.

Question 10

Name the 2 other platinum compounds…

Answer 10

Carboplatin - for advanced ovarian and lung cancer

Oxaliplatin - colorectal cancer

Question 11

What do antimetabolites do?

Answer 11

Act as folate antagonists so DNA synthesis and cell division is inhibited.

Question 12

Give an example of a folate antagonist.

Answer 12

Methotrexate

Question 13

What does methotrexate do?

Answer 13

Given orally, IM or IV. Mostly excreted unchanged in urine. Tumour cells may develop resistance. Also used to suppress immune system (e.g in RA)

Question 14

What are the other two types of antimetabolites?

Answer 14

Pyrimidine analogues - fluorouracil, capecitabine, cytarabine, gemcitabine.

Purine analogues - mercaptopurine

Question 15

What do cytotoxic antibiotics do?

Answer 15

Bind to DNA and inhibits DNA/RNA synthesis or degrade DNA.

Question 16

What are the names of some cytotoxic antibiotics?

Answer 16

Doxorubicin, Bleomycin, Dactinomycin, Mitomycin.

Question 17

What does Bleomycin do?

Answer 17

Degrades pre-formed DNA> Causes little myelosuppression BUT causes pulmonary fibrosis in 10% of patients.

Question 18

What are Vinca Alkaloids?

Answer 18

Plant derivatives. Prevent polymerisation of tubulin - prevents spindle formation.

Question 19

What are the names of some vinca alkaloids?

Answer 19

Vincristine, Vinblastine, Vindesine.

Question 20

What are taxanes?

Answer 20

Plant derivatives. Similar to vinca alkaloids - prevent spindle formation. E.g paclitaxel, docetaxel.

Question 21

What are oestrogen’s used for?

Answer 21

Ethinyloestradiol - used in prostate cancer palliative care treatment.

Question 22

What are the side effects of Ethinyloestradiol?

Answer 22

nausea, fluid retention, thrombosis, impotence

Question 23

What are the drug names for Progestogens?

Answer 23

Megestrol, Medroxyprogesterone, Norethisterone. Used to treat endometrial cancer.

Question 24

What are GnRH analogues?

Answer 24

Hormones used in prostate and breast cancer.

Question 25

Name the GnRH analogues.

Answer 25

Goserelin, Buserelin, Leuprorelim

Question 26

What are hormone antagonists?

Answer 26

E.g Tamoxifen, Letrozole, Flutamide. Inhibit transcription of oestrogen-responsive genes. Androgen antagonists.

Question 27

How do prednisolone and dexamethasone help to treat cancer?

Answer 27

Inhibit lymphocyte proliferation - for treatment of lymphomas and leukaemia’s.

Question 28

What are the actions of monoclonal antibodies?

Answer 28

React with specific target proteins expressed on cancer cells - this activates the immune system and causes lysis of cancer cells.

Question 29

What is RituxiMAB?

Answer 29

A monoclonal antibody. Causes lysis of B-lymphocytes.

Question 30

What is ImatiNIB?

Answer 30

A protein kinase inhibitor. Blocks tyrosine kniases - prevents angiogenesis. Used to treat chronic myeloid leukaemia.