-
S Phase specific drugs:
- Hydroxyurea
- Methotrexate (self-limiting)
-
M phase specific drug:
Vincristine
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Cell cycle non-specific drugs:
Alkylating drugs
-
-
Tyrosine Kinase inhibitors:
Imatinib and Dasatinib
-
Alkylating agent:
Cychlophosphamide
-
Mechanism of action for Cyclophosphamide
Alkylation of N7 guanine
-
Therapeutic indication for cyclophosphamide:
Solid tumors leukemia, lymphomas
-
Which drug has High oral bioavailability and Bioactivation by the liver?
Cyclophosphamide
-
Which drug produces cytotoxic metabolite that leads to hemorrhagic cystitis?
Cyclophosphamide
-
-
What is Mesna?
A chemoprotectant given with cyclophosphamide to protect bladder by binding toxic metabolites
-
What are the two drugs that need to be used together to prevent hemorrhagic cystitis due to formation of cytotoxic metabolite Acrolein?
Cyclophosphamide and IV Mesna
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_______ produces a cytotoxic metabolite called ______ and so the use of _______ in combination with said drug is recommended
- Cyclophosphamide
- Acrolein
- IV Mesna
-
ADR of Mesna?
- GI complaints
- Abd pain, diarrhea
- Lack of strength
-
Bleomycin targets _____ phase, and its MOA is:
- G2
- MOA: induce free radicals via iron interacting with O2 causing DNA damage
-
Therapeutic indications for bleomycin:
Hodgkin/ Non-Hodgkin lymphoma
-
Bleomycin can be given in _____ form(s)
IM, IV
-
ADR of bleomycin:
- Allergic reaction
- PULMONARY FIBROSIS (dose-limiting ADR)
-
Which drug can cause pulmonary fibrosis and thus need to be dose limited?
Bleomycin (G2 phase specific)
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T/F: Methotrexate is an antimetabolite/ anti-folate, that is S phase specific
True; interfere with DNA synthesis
-
MOA of methotrexate:
Competitively inhibits dihydrofolate reductase
-
Therapeutic indications for methotrexate?
- acute lymphoblastic leukemia (ALL)
- Lymphoma
-
ROA for methotrexate:
Oral, IV, intrathecal
-
ADR for methotrexate:
- Myelosuppression
- Mucositis
-
Which drug can cause myelosuppression:
- Methotrexate
- Hydroxyurea
- Vincristine
- etoposide
-
Hydroxyurea is an _____
Antimetabolite
-
MOA of hydroxyurea
Inhibit ribonucleotide reductase (convert nucleotides to deoxynucleotide)
-
Which drug’s MOA is to inhibit ribonucleotide reductase?
Hydroxyurea
-
Therapeutic indications for hydroxyurea:
- Polycythemia vera
- Leukemia
- Sickle cell anemia
-
Which drug can also be used to treat sickle cell anemia in addition to leukemia?
Hydroxyurea
-
Which drug can also be used to treat polycythemia vera in addition to leukemia?
Hydroxyurea
-
Hydroxyurea is given _______
Orally
-
ADR for hydroxyurea:
- Myelosuppression
- Malignancy
-
Which drug can have a side effect of malignancy?
Hydroxyurea
-
What is the therapeutic indications for leucovorin?
“rescue” methotrexate toxicity
-
What is a reduced form of folic acid:
Leucovorin (calcium folinate)
-
In case of methotrexate toxicity, what is the rescue drug used?
Leucovorin
-
Leucovorin ROA:
Oral, IV, IM
-
ADR for leucovorin (Rescue methotrexate):
- Allergic reaction
- Urticaria
- Anaphylactoid reactions
-
MOA of vincristine:
Inhibit tubulin polymerization
-
Which type of drug prohibits the formation of microtubules and mitotic spindles formation?
Vinca alkaloids (agent: vincristine)
-
Therapeutic indication for vincristine?
- solid tumor
- Leukemia
- HL and NHL
-
T/: Vincristine is given IV only
True
-
ADR of vincristine:
- Peripheral neuropathy
- Myelosuppression
-
Which drug can cause peripheral neuropathy:
Vincristine
-
MOA of tyrosine kinase inhibitors:
Inhibit tyrosine kinase activity of BCR-ABL oncoprotein
-
Therapeutic indications for tyrosine kinase inhibitor (imatinib) :
- CML
- Philadelphia chromosome positive ALL
-
ADR for imatinib:
- GI
- Fluid retention
- CHF
- Myalgia
-
Which drug is indicated for CML and Ph+ ALL
Imatinib
-
Which leukemia drug can cause CHF and Fluid retention as a side effect:
Imatinib
-
MOA of etoposide:
Inhibit topoisomerase which inhibits DNA synthesis and function
-
Which type of drug inhibits topoisomerase?
Etoposide
-
Therapeutic uses for etoposide:
- HL and NHL
- Gastric cancer
- Lung cancer
-
T/F: etoposide oral form is twice as potent as its IV form, which only has 50% bioavailbility
False; oral only 50% bioavailable while IV is twice as strong
-
ADR of etoposide?
- N/V
- Myelosuppression and alopecia
-
Which drug can lead to alopecia?
Etoposide
-
For HL or NHL, use:
- Bleomycin
- Vincristine
- Etoposide
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