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
Gemcytabine
Antimetabolite
stops DNA pol, Ribonucleotide reductase - inhibits synth
Hydroxyurea
Antimetabolite
stops ribonucleotide reductase, syncs cells in G0
Carmustine (BCNU)
Lomustine (CCNU)
Nitrosourea
cross links
not asn subject to cross resistance
Brain tumors
TMZ (temozolomide)
crosslinks (alkylating)
small lipophilic
brain tumors
cisplatin (carboplatin, oxaloplatin)
crosslinks
*N/V
slow excretion - hydration is crutial
newer ones - less GI and renal toxicity
Mechlorethamine
nitrogen mustard
crosslinks DNA
- vcesicant
- *N/V
- *bone marrow suppresion
Cyclophosphamide (ifosfamide)
nitrogen mustard
crosslinks DNA
Hemorrhagic cyctitis - treat with MENSA and hydration
Busulfan
cross links
busulfan tan - hyperpigmentation
Chlorambucil
nitrogen mustard
cross links
Dacarabazine
Cross links
melphalan
nitrogen mustard
cross links
procarbazine
cross links, causes strand breaks
causes increased risk of leukemia
Mitomycin
Antibiotic
Cross links
*lung and kidney tox
