Chemo Drugs Flashcards
Cisplatin
Platinum complexes
MOA: antineoplasm: Crosslink between and within DNA –> Apoptosis
AE: highly emetogenic, n/v, nephrotoxicity: tubular, electrolytes: hypocalcium/magnesium/potassium, peripheral neuropathy, ototoxicity
Etoposide
Topo II Inh.
MOA: Forms a complex with DNA and Topo II–> prevents religation of DNA breaks which occur when coils unwind–> apoptosis
AE: n/v, myelosuppression, alopecia
Bleomycin
Abx antineoplastic
MOA: Induction of DNA breaks
AE: pulmonary fibrosis, may cause oxygen toxicity, be careful with people going to get general anesthesia b/c it may cause acute pulmonary toxicity
Cyclophosphamide
Alkylating agent: cross-links DNA and prevents uncoiling or prevents gene transcription.
AE: n/v, alopecia, myelosuppression, hemorrhagic cystitis (exretion of acrolein through bladder)
Anti- metabolites
Mtx, cytosine arabinoside, 5-FU, fludarrabine, gemcitabine
MOA: interferes with nucleic acid synthesis by incorporating into RNA or DNA or by interefering with enzymes required for synthesis
5-FU (5-Fluorouracil)
Antimet.
MOA: prevents uracil turning into thymine and inhibits DNA syn., also inhibits RNA synthesis
AE: stomatitis, sometimes with ulceration, n/v, diarrhea, myelosuppression
MTX
Antimet.
MOA: MTX binds to DHFR and inhibits dihydrofolate from becoming tetrahydrofolate; thereby inhibiting thymidine which is essential for DNA synthesis
AE: stomatitis, sometimes with ulceration, n/v, diarrhea, myelosuppression
Gemcitabine
Antimet.
MOA: The diphosphate molecule blocks DNA synthesis by inhibiting
ribonucleotide reductase and the triphosphate form is incorporated into DNA and inhibits DNA
polymerase.
AE: stomatitis, sometimes with ulceration, n/v, diarrhea, myelosuppression
Vincristine
Vinca alkaloids
MOA: antimicrotubules, bind to tubulin dimers and prevent their incorporation into MT. Cannot synthesize MT
AE: Peripheral neuropathy- paresthesias–> myasthenia
ANS-impaired gut motility w/ constipation and/or paralytic ileus, orthopnea, bladder atony
Doxorubicin
Anthracycline
MOA: 1- Intercalation into DNA, 2- Topo II inhib., 3- Generation of free radicals
AE: dose-related CM w/ decreased EF, n/v, stomatitis, diarrhea, myelosuppression, alopecia
Paclitaxel
Taxane
MOA: bind to tubulin and inhibit MT disassembly
AE: peripheral neuropathy, n/v, oral mucositis, diarrhea, alopecia, myelosuppression
Irinotecan
Topo I inhib.
MOA: converted to active metabolite (SN-38) in the liver, binds to topo I-DNA cmoplex and prevents religating the DNA strand breaks–> apoptosis
AE: myelosupression, diarrhea-very serious and potentially life-threatening
Monoclonal antibodies
Rituximab
Trastuzumab
Bevacizumab
Cetuximab
Rituximab
Monoclonal antibody
MOA: CD20 Ab, ADCC, complement activation, apoptosis
AE: Infusion: hypotension, broncho-spasm, urticarial and cardiac arrhythmia; HBV: reactivation of the infection
Trastuzumab
Monoclonal Ab
MOA: Extracellular binding of HER2 & ADCC
AE: CM w/ reduced LVEF (esp. in pts. with anthracycline regimen); infusion rxns: fever, chills, n/v, HA
Bevacizumab
Monoclonal Ab
MOA: Ab to VEGF and inhibits downstream signaling, which is necessary for angiogensis
AE: cause or worsen HTN, hemorrhage, infusion rxns, wound healing-withhold 28 days prior/after to surgery
Cetuximab
Monoclonal Ab
MOA: Binds to EGFR
AE: Acneiform rash-correlated with disease response and prolonged survival; infusion rxn: bronchospasm and hypotension
Imatinib
Small molecule inhibitors
MOA: TKI, notably bcr-abl & c-kit, sits at the site where ATP binds.
AE: myelosuppression, n/v, diarrhea
Sorafenib
Small molecule inhibitors
MOA: TKI, VEGFR and Raf kinase
AE: Derm: palmar-plantar erythrodysesthesia, alopecia and rashes; diarrhea, abd. pain and anorexia
Erlotinib
Small molecule inhibitors
MOA: reversible TKI, EGFR
AE: Derm: acneiform rash affecting face and neck, anorexia and diarrhea
Vemurafenib
Small molecule inhibitors
MOA: Inhibits the BRAF kinase enzyme in activating mutation V600E
AE: Derm: cutaneous sq. cell carcinomas, keratoacanthomas, and melanoma
Prostate cancer treatment
Leuprolide- GnRH agonist
Bicalutamide- Androgen receptor inhibitor
Abiraterone- CYPc17 blockade
Leuprolide
Prostate CA tx
MOA: binds irreversibly to pituitary GnRH receptors and acts as an agonist
AE: decreased libido and ED; loss of bone density; initial surge in LH/FSH cause bone pain, bladder outlet obs. vertebral body mets, spinal cord compression
Abiraterone
Prostate CA tx
MOA: Irreversibly inhibits the enzyme 17 alpha-hydroxylase/c17, 20-lyase-necessary for the precusor molecules to test., DHEA and androstenedione
AE: decreased libido and impotence
Breast Cancer treatment
Tamoxifen
Anastrozole
Tamoxifen
Breast Cancer treatment
MOA: SERM, acts on estrogen receptors in breast cancer cells as an antagonist. Recruits other co-repressors and then binds to DNA to modulate gene expression
AE: females: vasomotors side effects (eg hot flashes and night sweats), DVT/PE, slight risk of uterine cancer
Anastrozole
Breast cancer treatment
MOA: aromatase inhibitor-ncessary to convert androstenedione to estrone and test to estradiol
AE: Females: risk of developing reduced bone mineral density and may have an increased risk of bone fractures
All trans retinoic acid (tretinoin)
Acute promyelocytic leukemia (APL: t(15;17) treatment
MOA: Dissociate co-repressors from the PML-RAR complexes and the inhibition of maturation is then removed
AE: 25%- APL differentiation syndrome: fever, dyspnea–> ARDS- initiate steroids with consideration of starting anthracycline chemo; 40% rapid leukocytosis; 50% elevated LFTs
AML tx
7d (cytosine arabinose) + 3d (doxorubicin)
DLBCL tx
R (rituximab), C (cyclophosphamide),
H (Doxorubicin), O (Vincristine), P (Prednisone)
HL tx
A (adriamycin), B (bleomycin), V (Vincristine), D (Decarbazine)
Decarbazine
Alkylating agent
MOA: Adds akyl group to DNA and causes apoptosis
AE: No special associated side effects
Antimetabolite Drugs: Classes
Folic Acid Analogs
Pyrimidine Analogs
Purine Analogs
