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Chemotherapeutic Agents


Risk

  • Cancer is the second most common cause of death in USA. In 2016, about 1,685,210 pts will be diagnosed with cancer and 595,690 will die of it.

  • More than two-thirds of all cancers are diagnosed in people 50 y of age or older. Prostate cancer is the most common among men, while breast cancer is the most frequent in women. In both genders, lung cancer is the leading cause of death due to cancer.

Uses

  • Drugs or biological agents (interleukins and interferon) are commonly used to (1) stop cancer cells from proliferating, migrating, and invading and/or (2) facilitate their recognition by the immune system.

  • Traditional chemotherapy agents, targeted chemotherapies, and immunotherapies are still front-line drugs for the treatment of solid and hematologic malignancies.

  • Neoadjuvant (before surgery) chemotherapy (and possibly radiation) remains the treatment of choice for many solid cancers.

Perioperative Risks

  • Intraop bleeding due to thrombocytopenia, postop infection, complications (leukopenias), blood transfusions (anemia).

  • Cardiac insufficiency and fluid overload (due to cardiotoxic agents such as the anthracyclines). Pulm toxicities can lead to periop pulm edema.

  • Acute kidney injury (nephrotoxic agents).

  • Mononeuropathy (neurotoxic drugs). Bone demineralization (osteopenia) is a risk for fracture after inadequate pt positioning.

Classification According to Mechanism of Action

Class Activity Agents
Alkylating agents Covalent binding to nucleic acids or proteins Nitrogen mustards (cyclophosphamide, melphalan, chlorambucil)
Aziridines (thiotepa and mitomycin C)
Procarbazine, oxazaphosphorines (cyclophosphamide, ifosfamide)
Alkyl alkane sulfonates (busulphan)
Nitrosoureas (carmustine, bendamustine, lomustine)
Tetrazines (dacarbazine, mitozolomide, temozolomide)
Antimetabolites Competition with natural substrates for the active site Pyrimidine analogues (fluorouracil, cytarabine, sapacitabine, gemcitabine)
Purine analogues (6-mercaptopurine, thioguanine)
Folic acid antagonists (methotrexate)
Spindle agents
  • (1)

    Vinca alkaloids: Binding to microtubules (assembly inhibition)

  • (2)

    Taxanes: Binding to microtubules (assembly facilitation)

Vincristine, vinblastine
Paclitaxel, docetaxel, abraxane
Epothilones, discodermolide
Antibiotics Alteration of function and synthesis of nucleic acids Anthracyclines (derived from Streptomyces ), most commonly doxorubicin, daunorubicin, and epirubicin (most generic names except mitoxantrone end with -rubicin), actinomycin D, bleomycin, mitomycin C, vosaroxin
Heavy metals Platinum agents: Crosslink with DNA strands—inhibition of protein synthesis Cisplatin, carboplatin, oxaliplatin
Topoisomerase inhibitors Inhibition of DNA replication Topoisomerase I inhibitors: Camptothecin, irinotecan, topotecan
Topoisomerase II inhibitors: Epipodophyllotoxin derivatives, vosaroxin
Hormone receptors, antagonists, and hormonal agents
  • (1)

    Estrogen receptor antagonists

  • (2)

    Aromatase inhibitors (block conversion of androgens to estrogens)

  • (3)

    Androgen receptor antagonists

  • (4)

    Gn-RH antagonist

  • (5)

    LHRH agonists

  • (1)

    Tamoxifen

  • (2)

    Anastrozole, letrozole, exemestane

  • (3)

    Enzalutamide

  • (4)

    Degarelix

Proteasome inhibitors Bortezomib
Monoclonal antibodies and small-molecule inhibitors Direct effects against receptors or signaling molecules Anti-HER-2 antibody (trastuzumab), antiangiogenesis (bevacizumab, ramucirumab), anti-EFGR antibody (cetuximab), anti-bcr-abl antibody, anti-CD20 antibody (rituximab), anti-CD30 antibody (brentuximab), and anti-CD33 antibody (SGN-33, AMG-330)
Tyrosine kinase inhibitors (gefitinib, erlotinib), PIK-1 inhibitors (volasertib), FLT3 inhibitor (sorafenib, midostaurin, quizartinib), JAK inhibitors (pacritinib), mTOR inhibitors (everolimus), aurora A kinase inhibitor (alisertib)
Histone deacetylase inhibitors
CDK4-CDK6 inhibitors
  • (1)

    Selective of paninhibition of HDAC

  • (2)

    Inhibition of DNA synthetic phase

Vorinostat, romidepsin, belinostat, mocetinostat, panobinostat
Palbociclib, ribociclib, abemaciclib
Biological response modifiers Interferon, interleukin 2
Anti-PD-1 antibodies (nivolumab, atezolizumab, pembrolizumab, pembrolizumab)
CTLA-4 blocker (ipilimumab)
Thalidomide, lenalidomide
Key References: Ai D, Banchs J, Owusu-Agyemang P, et al.: Chemotherapy-induced cardiovascular toxicity: beyond anthracyclines, Minerva Anestesiol 80(5):586–594, 2014; Sahai SK: Perioperative assessment of the cancer patient, Best Pract Res Clin Anaesthesiol 27(4):465–480, 2013.

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