Anticancer Drugs

Question 1

Methotrexate— MOA, Uses, S/E

Answer 1

MOA:

1) Inhibits DHFRase and prevents synthesis of THFA from DHFA. THFA is essential for synthesis of DTMP from dUMP for DNA synthesis
2) It also inhibits Thymidilate synthase and blocks RNA and protein synthesis

Uses:

Neoplastic uses:

a) DoC for Choriocarcinoma
b) DoC for Carcinomatous meningitis
c) ovarian, breast cancers
d) Osteosarcoma
e) Leukemia

Non-neoplastic uses:

a) DoC for Rheumatoid arthritis
b) Doc for Psoriasis
c) Wegners granulomatosis

S/E:
1. Severe bone marrow suppression (blocking purine synthesis) causing Megaloblastic anemia and pancytopenia—> Folinic acid is given (Folic acid won’t be useful as it cannot be activated without THFA)

2. Mucositis, diarrhea
3. Nephrotoxicity
4. Hepatotoxicity
5. By intrathecal route it can causes seizures, meningismus, arachnoiditis

Question 2

DOC for early onset chemo induced nausea and vomiting

Answer 2

5HT3 blockers:
Ondansetron, Palonosetron

Question 3

DOC for late onset chemo induced nausea and vomiting

Answer 3

NK1 blocker- Aprepitant