Fitz DRUG LIST Flashcards
Methotrexate, pemetrexed, pralatrexate
Mech Resistance Pharmacokinetics Interactions Uses Toxicity Synergy Class/general type
Mech - DHFR competative inhibition (of purine synthesis)
Resistance- Increased DHFR, decreased afinity, decreased polygultamation
Pharmacokinetics - oral for low dose, IV for high
Interactions - Don’t take w/ NSAIDS, Cisplatin, Aspitin
Uses - broad spectrum, solid tumors (choriocarcinoma, breast cancer)
Toxicity - Bone marrow suppresion, Gi epithelium tox, **mucositis and myelosuppression peak at 5-10 days, pneumonitis, hepatic fibrosis, alopecia/dermatitis, abortifacient (MTX)
Synergy - leucovorin. a reduced form of folate that allows normal tissue to bypass inhibition of DHFR (can increas dose of MTX)
Class/general type - folic acid annalogue (nucleotide synthesis inhibitor)
5-FU, capecitabine, cytarabine, gecitabine
Mech
Resistance
Pharmacokinetics
Interactions
Uses
Toxicity
Synergy
Class/general type
Mech - capecitabine converted into 5-FU in cancer cells. 5-FU cannot be methylated by thymidylate synthase, decrease in dTMP production.
Resistance - Changes to thymidylate synthase, decrease in activation of prodrug (Pyrimidine monophosphate kinase)
Pharmacokinetics - 5-FU given IV - gut has high dihydropyrimidine dehydrogenase. Capecitabine given orally
Interactions - none listed
Uses - colorectal cancer, ovarian and breast cancer
Toxicity - low therapeutic index, myelosuppression, GI upset, acute cerebellar syndrome, alopecia, dermatitis
Synergy - MTX, Leucorvin - increased 5-FU binding to thymidylate synthase –> increased half life
Class/general type - pyrimidine analogues, inhibits nucleotide synth
Doxorubicin
Intercalating - cytotoxic
Natural product
brest cancer
Reduce Tox with Methylene blue
Bleomycin
Topo II - G2 specific - cytotoxic
natural product - antibiotic
lack of bone marrow suppression
Etoposide
topo II - G2/S phase - cytotoxic
natural plant alkyloid
p-glycoprotien pumps it out
Irinotecan, topotecan
topo I - G2/S
natural - plant alkyloid
Diarrhea - if actue treat with atropine
Vinblastine (vinorelbine)
Halts spindle assembly - M phase
Natural - plant alkyloid (vinca)
neurotoxic
only difference from vincristine is “*N/V”
Vincristine
Halts spindle assembly - M phase
Natural - plant alkyloid (vinca)
neurotoxic
Paclitazel (docataxel, cabazitaxel)
Enhances spindle assembly - m phase
Natural - plant alkyloid
can cause hypersensitivity reactions
Ixabepilone
Enhances spindle assembly - m phase
Natural - antibiotic
Leucovorin
folate that normal cells can use
give with MTX
intrathecal -> fatal
6-MP (mercaptopurine) and 6-TG (thioguanine)
Inhibitions of purine nucleotide interconversion, decrease in guanine
must be activated by HGPRT (hypoxanthine guanine phosphoribosyl transferase)
Can cause tumor lysis Syndrome - give allopurinol
Cladarabine
Inhibits DNA synthesis by inhibiting DNA polymerase
s phase
Fludarabine
acts on DNA pol and Ribonucleotide resuctase - inhibits synth
Cytarabine (ARA-C)
Antimetabolite
stops DNA pol, Ribonucleotide reductase - inhibits synth
