B9 W6 drugs

Question 1

Alkylating agents drugs

Answer 1

Cisplatin
Dacarbazine
Cyclophosphamide

G1 phase inhibitors

Question 2

Anti-metabolites drugs

Answer 2

5-fluourouracil
Methotrexate

S phase inhibitors

Question 3

Anti-microtubule drugs

Answer 3

Paclitaxel
Vinblastine

These are M phase inhibitors which can lead to neuropathy.

Question 4

Topoisomerase inhibitors drugs

Answer 4

Doxorubicin
Etoposide
Ciprofloxacin

These are G2 phase inhibitors.

Question 5

Which drugs are G1 inhibitors?

Answer 5

Cisplatin
Cyclophosphamide
Dacarbazine

Question 6

Which drugs are M phase inhibitors?

Answer 6

Paclitaxel
Vinblastine

Question 7

Which drugs are S phase inhibitors?

Answer 7

Azathriopine
Methotrexate
5-fluorouracil

Question 8

Which drugs are the G2 phase inhibitors?

Answer 8

Etoposide
Doxorubicin
Ciprofloxacin

Question 9

Dacarbazine

Answer 9

Purine analogue which is a G1 phase inhibitor that forms covalent bond for alkylation of DNA to cause crosslinking. Treatment for melanoma, sarcoma and Hodgkin’s lymphoma

Question 10

Cyclophosphamide

Answer 10

Alkylating agent which is a G1 phase inhibitor requires bio activation in the liver to be converted to -> hydroxyphosphamide -> active aldophosphamide.

It acts on the guanine portion to cause cross linking.

Used to treat rheumatoid arthritis and malignant tumours.

Question 11

Cyclophosphamide - considerations

Answer 11

Alkyating agent which causes DNA mutations at guanine region and causes immunosuppression and blood disorders. Cannot be given for:

—>Haemorrhagic cystitis (bleeding of urinary bladder)
—>Breastfeeding
—>Diabetes mellitus (type 1)
—>Acute porphyria: biosynthesis of enzymes in the haem pathway

Question 12

Rituximab

Answer 12

Monoclonal B antibody inhibitor which binds to CD20 receptor of B cells to induce apoptosis. Given for rheumatoid arthritis , Non-Hodgkin’s lymphoma and Granulomatosis

Question 13

Doxorubicin

Answer 13

Anthracycline which acts as a Topoisomerase inhibitor by intercalating into the DNA and forming H bonds to prevent replication. It is a g2 phase inhibitor.

Given for acute leukaemia, bladder cancer, sarcoma and lymphoma.

Question 14

Doxorubicin- considerations

Answer 14

Anthracycline which prevents DNA replication. Causes cardio suppression so cannot be given for myocardial insufficiency or severe infection.

Question 15

Tretinoin

Answer 15

Vitamin A which binds to retinoid X receptors for the transcription of genes for cell development and regulation and increases Ca2+ levels. It has an anti-neoplastic effect and is given in acute promyelocytic leukaemia for the development of mature functioning RBC.

Question 16

Tretinoin- considerations

Answer 16

Tretinoin increases cell development but may lead to GI problems due to higher Ca2+, anxiety and increased infection risk.

Question 17

Paclitaxel

Answer 17

Anti-microtubule is an M phase inhibitor that binds to the beta tubulin subunit and prevents polymerisation and stabilisation of mitotic spindle.

Given for ovarian cancer, breast cancer, pancreatic and Kapsoi’s sarcoma.

Question 18

Paclitaxel-considerations

Answer 18

Inhibits mitotic spindle which causes peripheral neuropathy and bone marrow disorders.

Cannot be given for acute porphyria due to already low Hb levels.

Question 19

Tamoxifen

Answer 19

Competitive selective oestrogen modulator of hypothalamus receptors to increase FSH and LH release for ovarian follicle maturation. It is given for breast cancer and anovulatory infertility risk.

Question 20

Tamoxifen- considerations

Answer 20

Competitively inhibits oestrogen in hypothalamus, drop in oestrogen results in:
hair loss, i
increased risk of embolism and thromboembolism and cerebral ischaemia

Question 21

5-fluorouracil

Answer 21

Anti-metabolite converted to F-dUMP by thymidine kinase to inhibits thymidylate synthase for DNA and RNA synthesis. Given for solid tumours and skin lesions.

It is a S phase inhibitor.

Question 22

5-fluorouracil considerations

Answer 22

Inhibits DNA and RNA synthesis that leads to bone marrow disorders. Cannot be given for deficiency in dihydropyramidine dehydrogenase for pyramidine breakdown.

Question 23

Etoposide

Answer 23

Topoisomerase inhibitor alpha-isoform for S-G2 phase given for organ cancers such as prostate, testicular, breast.

It is a G2 phase inhibitor.

Question 24

Etoposide considerations

Answer 24

Topoisomerase inhibitor which causes bone marrow disorders and cannot be given for low blood count

Question 25

Vinblastine

Answer 25

Anti-microtubule which is an M phase inhibitor that binds to tubulin to cause hyperstabilisation of the microtubule.

Given for Lymphoma, Leukemia and solid tumours.

Question 26

Vinblastine- considerations

Answer 26

Alkaloid anti-microtubule which can cause nerve damage and not provided intrathecal or destruction of the spinal cord can occur.

Question 27

Imatinib

Answer 27

Binds to ATP active site to prevent binding of tyrosine kinase. Also inhibits the C-kit oncogene for tyrosine kinase activation as a treatment for GIST. Treatment for philadelphia chromosome in CML and ALL and myeloproliferative disorders

Question 28

Imatinib- considerations

Answer 28

Inhibits tyrosine kinase downstream signalling and cannot be taken with grapefruit juice or it will increase conc of drug.

Question 29

Cisplatin

Answer 29

Alkylating agent which causes DNA crosslinking and nucleotide mispairing.

Given for testicular cancer, squamous cell carcinoma of head and neck.

Question 30

Cisplatin considerations-

Answer 30

Alkylating agent which causes electrolyte imbalance due to loss of K+ and Mg2+ with anaemia and bone marrow disorder.

It causes ototoxicity (hearing loss) and nephrotoxicity.

Question 31

Methotrexate

Answer 31

Anti-metabolite which inhibits DHF reductase for DNA and RNA synthesis, given for rheumatoid arthritis, Crohn’s disease and neoplastic disorders.

Question 32

Methotrexate- considerations

Answer 32

Anti-metabolite which can cause **liver cirrhosis and failure. **

Cannot be given for ascites due to liver damage and anaemia due to bone marrow suppression