Test 3 antineoplastics

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dmatta
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38417
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Test 3 antineoplastics
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2010-10-02 20:38:21
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antineoplastics
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test 3 antineoplastics
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  1. Alkylating Agents:
    • Cyclophosphamide (nitrogen mustards)
    • Carmustine (nitrosureas)
    • Procarbazine (methylhydrazine)
    • Temozolomide (triazine)
    • Cisplatin (Pt coordination complex)
  2. Antimetabolites
    • Methotrexate (folate antagonist)
    • 5- fluorouracil (pyrimidine analogs (U,C))
    • 6-Mercaptopurine
  3. Natural products
    • Vincristine
    • Paclitaxel
    • Doxorubicin
  4. Hormones
    Flutamide (antiandrogen)
  5. Immunomodulator
    Aldesleukin
  6. Monoclonal antibodies
    rituximab
  7. protein tyrosine kinase inhibitors
    imatinib
  8. Cyclophosphamide (nitrogen mustards)
    - alkylating agent
    MOA: DNA alkylation: mispairing, scission, inter/intrastrand x-linking (two war heads)

    Uses: NHL, CLL, AML, Breast, Ovarian

    S/E: myelosuppression, hepatic venooclusive disease (inc fibrin); N/V; hemorrhagic cysitis; neurotoxicity; alopecia; pulmonary fibrosis

    PK: Requires activation via CYP286
  9. Carmustine (nitrosureas)
    - alkylating agent
    MOA: DNA alkylation: mispairing, scission

    Uses: Brain, HD, NHL, melanoma

    S/E: myelosuppression, hepatic venooclusive disease, pulmonary fibrosis, leukemogenic, renal failure, N/V

    PK: Breaks into two pieces, one alkylates DNA, other carbamoylated protein/inactivates AGT (MOR)

    MOR: Alkyl guanine transferase (removes alkylat'n>> healthy DNA)
  10. Procarbazine (methylhydrazine)
    - alkylating agent
    MOA: methylates DNA; free radical prod>> chromosome damage inhibition of DNA, RNA, and protein synthesis

    Uses: HD, NSCLC, Brain (astrocytoma)

    S/E: BMS (leukemia, thrombocytopenia), weak MAOI, 2ary leukemia, teratogen, disulfirum effect (octoberfest w/anabuse, tyramine>> N/V HTN, tachycardia, etc
  11. Temozolomide (triazine)
    -alkylating agent
    MOA: bioactivated into diazomethane (methilates DNA, guanine)

    Uses: brain (astrocytoma), melanoma

    • S/E:
    • BMS (thrombocytopenia, neutropenia) HA, fatigue

    • PK:
    • 98% bioavailability, penetrates BBB
  12. Cisplatin (Pt coordination complex)
    - alkylating agent
    • MOA:
    • DNA adduct formation >> inhibit replication/transcription >> breaks, miscoding (G)

    • Uses:
    • Testicular, ovarian, cervix, bladder, N/SCLC

    • S/E:
    • BMS, peripheral neuropathy, ototoxicity, hypersensitivity rxn, nephrotoxicity (dec. w/NS hydration, diuresis, amifostine (protective)

    • MOR:
    • Loss of mismatch repair (apoptosis trigger)
  13. Methotrexate (folate antagonist)
    - S phase specific
    - Antimetabolite
    • MOA:
    • DHF inhibition (decreases DNA/RNA synthesis)

    • Uses:
    • ALL, CNS leukemia (IT), GTN--> chorion that surrounds baby, breast, NHL

    • S/E:
    • Myelosuppression, pneumonitis, mucositis (whole GI), hepatotoxicity, teratogenesis, meningismus (IT-->intrathecally, right into CSF), nephrotoxicity

    • PK:
    • Dose should be adjusted in those with decreased renal faiulre

    • MOR:
    • Polyglutanated and stays inside cell, DHFR gene amplification is clinically significant in patients with lung cancer, MRP
  14. 5- Fluorouracil (pyrimidine analogs (U,C))
    - S phase specific
    - Antimetabolite
    • MOA:
    • Converted into 5- FDUMP (5-F-deoxyuridine monophosphate) (inhibitor of thymidylate synthase (U>>T); Decreased DNA synthesis

    Uses: Colorectal, breast, gastric, pancreatic, esophageal

    • S/E:
    • N/V/D alopecia, myelosuppression, hand and foot syndrome (selective extravasation on palms/soles, they are RED!!)

    • PK:
    • people with low levels of dihydropyrimidine dehydrogenase can have very severe toxicity with 5-FU
  15. 6-Mercaptopurine
    - Antimetabolite
    • MOA:
    • converted to 6-thioguanine nucleotides (inc. into DNA/RNA >> cytotoxicity)

    • Uses:
    • ALL

    • S/E:
    • myelosuppression, N/V/D, hepatotoxic
  16. Vincristine
    • MOA:
    • bind tubulin and block ability to polymerize into microtubules

    • Uses:
    • HD, NHL, Brain, ALL

    • S/E:
    • fatal (IT, seizures, coma); alopecia, myelosuppression, neurotoxicity, constipation (damage ANS, peristalsis)

    • PK:
    • CYP3A4; dec dose 75% for hepatic dysfxn
  17. Paclitaxel
    • MOA:
    • Bind microtubules and antagonize disassembly >> arrest in mitosis

    • Uses:
    • Ovarian, N/SCLC, breast, H/N, KS (kaposi)

    • S/E:
    • myelosuppression, peripheral neuropathy, mucositis (ulcers), hypersensitivity (50/50 EtOH:Castor oil vehicle)

    • PK:
    • CYP3A4, hep dysfxn dec. dose 50-75%
  18. Doxorubicin
    • MOA:
    • DNA intercalation (>> single/dbl strand breaks); bind topo-II complx (dbl strand breaks); free radical production (esp. in presence of Fe)

    • Uses:
    • AML; ALL; HD; KS; Breast; Neuroblastoma

    • S/E:
    • BMS (dose lt'ing); extravasation (tissue necrosis), stomatitis, alopecia, 2ary AML, cardiotoxicity (arrhythmia, CHF, tx = Dexrazoxane (cardioprotect Fe chelator)

    • PK:
    • CYP3A4; hep dysfxn dec. dose 50%
  19. Flutamide (antiandrogen)
    - Hormone
    • MOA:
    • Androgen receptor antagonist

    Use: Prostate (usually w GnRH analog)

    • S/E:
    • Nausea (mild); gynecomastia; hot flash; decreased libido, hepatotoxicity

    PK: CYP3A4
  20. Aldesleukin
    -immunomodulator
    • MOA:
    • human recombinant IL-2; $ immune sys (inc. TNF, IL-1, IFNy for inhibiting tumor growth)

    • Uses:
    • RCC, melanom

    • S/E:
    • capillary leak syn (hypotension, dec. organ perfusion, edema); infections; BMS (RBC, platelets); mental status changes (irritability, confusion, depression); thyroid fxn impairment, arrhythmias

    • PK:
    • CYP3A4
  21. Rituximab
    - monoclonal antibody
    • MOA:
    • Fab binds CD20 on B cells, Fc stimulates the immune system for their lysis

    • Uses:
    • NHL, CLL, RA (b/c of B cells)

    • S/E:
    • arrhythmias, hypersensitivity rxns (hypotension, bronchospasm, angioedema), HepB infections, tumor lysis syn

    • PK:
    • CYP3A4
  22. Imatinib
    Protein tyrosine kinase inhibitors
    • MOA:
    • Inhibit TK association w/Bcr-Abl (decreases proliferation, stimulates apoptosis)
    • inhibit tyrosine kinase associated w/ EGFR (epidermal growth factor), ∴ ↓ proliferation & stimulates apoptosis


    • Uses:
    • CML, GIST, ALL

    • S/E:
    • Edema (periorbital, pulmonary) BMS, hepatotoxicity

    • PK:
    • CYP3A4

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