Asparaginase. Give MoA, side effects, and if relevant cell cycle specificity.
MoA: Depletes circulating L-asparaginase reducing protein production.
SE: hypersensitivity, hepatotoxicity, pancreatitis, thrombosis & bleeding.
G1 specific.
Cyclophosphamide.
Platinum based cross-linking agents which cause DNA intrastrand and interstrand breaks.
Cisplatium analogs: Cisplatin, Carboplatin, Oxaliplatin.
BMS, Mucositis, hepatotoxicity, nephrotoxicity (metabolite crystals).
Leucovorin rescue for the mucositis.
Methotrexate.
Can treat the nephrotoxic crystals with urinary alkalinization and fluids.
Pneumonitis, pulmonary fibrosis, dematologic toxicity
Bleomycin
Doxirubicin or Daunorubicin. Give MoA, side effects, and if relevant cell cycle specificity.
1. Intercalates with DNA -> DNA strand breaks
2. Binds to topoisomerase II -> DNA breaks, decreased DNA synthesis and DNA repair.
3. Increased free radicals -> DNA strand breaks, cellular macromolecule damage
Inhibits thymidylate synthetase by incorporating metabolite into DNA. Using Leucovorin enhances the effect.
5-fluorouracil (5-FU):
Pyrimidine antimetabolite bioactivated to inhibit thymidylate synthetase => ↓ dMTP; misincorporation of the metabolite of 5-FU => dysfunction of DNA &RNA
Forms complex with topoisomerase I and DNA causing strand breaks.
Irinotecan. I = 1.
Nephrotoxicity, Ototoxicity.
Cisplatin.
BMS, neuropathy.
Taxanes: Paclitaxel and Docetaxel.
5-FU. Give MoA, side effects, and if relevant cell cycle specificity.
Pyrimidine antimetabolite bioactivated to inhibit thymidylate synthetase. Misincorporates metabolite into DNA, stopping DNA synthesis. Leucovorin is added to enhance the formation of the ternary complex which enhances the inhibition of thymidylate synthetase.
Side effects: BMS, cardiotoxicity, severe vomiting and diarrhea.
S-phase specific.
S-phase specific. Purine antimetabolite bioactivated by HGPR transferase. Inhibits interconversion of purine nucleotide (Guanine).
6-MercaptoPURINE.
M-phase specific. Inhibits microtubule depolymerization.
Taxanes: Paclitaxel or Docetaxel.
BMS, Cardiotoxicity, ruby pee from meds.
Daunorubicin, doxirubicin
BMS, Hemorrhagic cystitis, hepatotoxicity.
Cyclophosphamide
Bleomycin. Give MoA, side effects, and if relevant cell cycle specificity.
MoA: Causes DNA damage by complexing with Fe and O2 to generate free radicals.
SE: Pneumonitis, pulmonary fibrosis, and dermatologic toxicity.
G2 specific.
MoA: Depletes circulating L-asparaginase reducing protein production.
Asparaginase.
M-phase specific. Inhibits microtuble polymerization.
Vinca alkaloids: Vincristine and Vinblastine.
BMS, cardiotoxicity, severe vomiting and diarrhea.
5-FU
Intrathecal injection leads to higher chances of neurotoxicity.
Conjunctivitis, Ara-C syndrome
Cytarabine (SIGHT-arabine)
Cytosine analog that inhibits DNA polymerase
Methotrexate. Give MoA, side effects, and if relevant cell cycle specificity.
MoA: Inhibits dihydrofolate (DHF) reductase which directly inhibits thymidylate synthetase in the folate cycle, stopping DNA synthesis.
SE: BMS, Mucositis, nephrotoxicity, hepatotoxicity. Leucovorin rescue helps with mucositis.
S-phase specific.
Inhibits dihydrofolate (DHF) reductase directly inhibiting thymidylate synthetase and stopping DNA synthesis.
Methotrexate.
Three mechanisms:
1. Intercalates with DNA causing strand breaks.
2. Binds to topoisomerase II causing DNA breaks and reduced repair.
3. Increases the amount of free radicals released causing DNA damage.
Doxorubicin, daunorubicin.
BMS, neurotoxicity. One of these drugs causes worse BMS than the other.
NEVER give this drug intrathecally.
Vinca alkaloids: Vincristine and Vinblastine.
Vinblasting BLASTS your bone marrow.
Hypersensitivity, Hepatotoxicity, Pancreatitis, Thrombosis & Bleeding (less than thrombosis).
Used for Acute Lymphoblastic Lymphoma (ALL).
Asparaginase.