B9 W6 drugs Flashcards
Alkylating agents drugs
Cisplatin
Dacarbazine
Cyclophosphamide
G1 phase inhibitors
Anti-metabolites drugs
5-fluourouracil
Methotrexate
S phase inhibitors
Anti-microtubule drugs
Paclitaxel
Vinblastine
These are M phase inhibitors which can lead to neuropathy.
Topoisomerase inhibitors drugs
Doxorubicin
Etoposide
Ciprofloxacin
These are G2 phase inhibitors.
Which drugs are G1 inhibitors?
Cisplatin
Cyclophosphamide
Dacarbazine
Which drugs are M phase inhibitors?
Paclitaxel
Vinblastine
Which drugs are S phase inhibitors?
Azathriopine
Methotrexate
5-fluorouracil
Which drugs are the G2 phase inhibitors?
Etoposide
Doxorubicin
Ciprofloxacin
Dacarbazine
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
Cyclophosphamide
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.
Cyclophosphamide - considerations
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
Rituximab
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
Doxorubicin
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.
Doxorubicin- considerations
Anthracycline which prevents DNA replication. Causes cardio suppression so cannot be given for myocardial insufficiency or severe infection.
Tretinoin
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.
Tretinoin- considerations
Tretinoin increases cell development but may lead to GI problems due to higher Ca2+, anxiety and increased infection risk.
Paclitaxel
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.
Paclitaxel-considerations
Inhibits mitotic spindle which causes peripheral neuropathy and bone marrow disorders.
Cannot be given for acute porphyria due to already low Hb levels.
Tamoxifen
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.
Tamoxifen- considerations
Competitively inhibits oestrogen in hypothalamus, drop in oestrogen results in:
hair loss, i
increased risk of embolism and thromboembolism and cerebral ischaemia
5-fluorouracil
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.
5-fluorouracil considerations
Inhibits DNA and RNA synthesis that leads to bone marrow disorders. Cannot be given for deficiency in dihydropyramidine dehydrogenase for pyramidine breakdown.
Etoposide
Topoisomerase inhibitor alpha-isoform for S-G2 phase given for organ cancers such as prostate, testicular, breast.
It is a G2 phase inhibitor.
Etoposide considerations
Topoisomerase inhibitor which causes bone marrow disorders and cannot be given for low blood count
Vinblastine
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.
Vinblastine- considerations
Alkaloid anti-microtubule which can cause nerve damage and not provided intrathecal or destruction of the spinal cord can occur.
Imatinib
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
Imatinib- considerations
Inhibits tyrosine kinase downstream signalling and cannot be taken with grapefruit juice or it will increase conc of drug.
Cisplatin
Alkylating agent which causes DNA crosslinking and nucleotide mispairing.
Given for testicular cancer, squamous cell carcinoma of head and neck.
Cisplatin considerations-
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.
Methotrexate
Anti-metabolite which inhibits DHF reductase for DNA and RNA synthesis, given for rheumatoid arthritis, Crohn’s disease and neoplastic disorders.
Methotrexate- considerations
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
