Oncologic Medications

Categories:

General
- New Afib in cancer patients is associated with increased risk of HF and VTW
Common Groups
- ABVD
  - Adriamycin, Bleomycin, Vinblastine, Dacarbazine
  - Hodgkin Lymphoma
- BEACOPP
  - Bleomycin, Etoposide, Adriamycin/doxorubicin, Cyclophosphamide, Oncovorin/vincristine, Procarbazine, Prednisone
  - Hodgkin Lymphoma
- FOLFOX
  - Leucovorin, Fluorouracil, Oxaliplatin
- R-CHOP
  - Rituximab, Cyclophosphamide, Hydroxy-doxorubicin, Oncovorin/Vincristine, Prednisone
Cancer-related Cachexia
- Hypercatabolic state characterized by appetite and weight loss with a disproportionate loss of skeletal muscle
- Treatment
  - Progesterone analogs (Megestrol acetate, Medroxyprogesterone) and corticosteroids (Dexamethasone)
    - PAs preferred in pts with longer life expectancies
5-Fluorouracil (5-FU)
- MOA: Direct Inhibitor of pyrimidine synthesis (blocks thymidylate synthase), thereby blocking protein and DNA synthesis
  - Leucovorin increases 5-FU effectiveness
- Anti-metabolite
  - Inflammation resolves about 2 weeks after treatment discontinuation
- SE: Myelosuppression and Photosensitivity, Palmar-plant erythrodysesthesia (hand-foot syndrome), cerebellar toxicity
6-Mercaptopurine (6-MP)
- Anti-metabolite, metabolized by xanthine oxidase (inhibited by allopurinol)
  - Side effects are worse when on allopurinol (stop or reduce)
  - Thiopurine
- SE: Myelosuppressive, Hepatotoxic, Interacts with allopurinol
- Azathioprine
  - Converted to 6-MU and also metabolized by xanthine oxidase, also interacts with allopurinol
Alemtuzumab (Lemtrada)
- Anti-CD52
- Use: CLL, MS
All-Trans Retinoic Acid (ATRA)
- MOA: Inhibits transcriptional repression by PML-RARa
- Tretinoin
- Formulation of Vitamin A, targeted therapy for Acute Promyelocytic Leukemia (M3 variant)
  - Causes immature myeloblasts to differentiate into mature myelocytes
- Combined with an Anthracycline (Daunorubicin, Idarubicin) for best results
- SE: Rashes, Teratogenic, DIC
Aromatase Inhibitors
- Anastrozole, letrozole, and vorozole
- Block formation of new estrogen (good for metastatic disease)
- Give Calcium and Vitamin D supplements, Get DEXA
  - Bisphosphonates or denosumab if osteoporotic
- Increased risk of osteoporosis and fracture
- SE: Arthralgia, joint stiffness and bone pain in 33%, Vaginal dryness, sexual dysfunction, CV events, hyperlipidemia, and higher risks of osteoporosis and fractures
Axitinib (Inlyta)
- Use: RCC
Bevacizumab (Avastin)
- Anti-VEGF
- Use: Colorectal cancer, renal cell carcinoma, non-small cell lung cancer
- SE: PRES syndrome
Bleomycin
- Antitumor antibiotic used in testicular cancer and Hodgkin’s Lymphoma
- No myelosuppression (vs. Busulfan)
  - Induces free radical formation and cause breaks in DNA
- SE: Severe Pulmonary Fibrosis, Fever, and hypersensitivity
Bortezomib (Velcade)
- MOA: Proteasome inhibitor
- SE: Peripheral Neuropathy, Herpes Reactivation
  - Prophylactic acyclovir or valacyclovir
Busulfan
- Alkylates DNA
- Pulmonary Fibrosis and myelosuppression
Capecitabine (Xeloda)
- Adjuvant for colon cancer
- SE: Palmar-plant erythrodysesthesia (hand-foot syndrome)
Caplacizumab (Cablivi)
- Monoclonal antibody
- Use: Severe TTP
Cetuximab (Erbitux)
- Anti-EGFR
- Stage IV colorectal cancer, head and neck cancers
- SE: Pustular acneiform eruptions (severe), pulmonary toxicity
Chemotherapy-Induced Cardiotoxicity
- Type I
  - Associated with Anthracyclines
    - Daunorubicin
    - Doxorubicin (Adriamycin, Doxil)
    - Idarubicin
    - Generate free radicals to intercalate DNA
      - Causes severe tissue necrosis
  - Myocyte Necrosis and destruction w/fibrosis
    - Progression to overt clinical heart failure
    - Less likely to be reversible
  - SE: Dilated Cardiomyopathy with chronic use
    - Antitumor Antibiotic, myelosuppression, alopecia, severe gastric upset secondary to colonic mucositis
    - Total cumulative dose is most strongly related to risk
  - Antidote is Dexrazoxane
    - Iron-chelating agent used for cardiac protection
- Type II
  - Associated with Trastuzumab
  - Myocardial stunning/hibernation w/o myocyte destruction
  - Asymptomatic LV systolic dysfunction
  - More likely to be reversible
Cyclophosphamide (Cytoxan)
- Covalently links DNA at guanine N-7
- SE: Hemorrhagic Cystitis, SIADH (hyponatremia), bladder carcinoma, myelosuppression, sterility (acrolein, metabolite causes all the damage)
  - Cystitis can be treated with 2-Mercaptoethanesulfonate (Mensa) which binds the metabolite acrolein (bladder irritant), fluids
  - Alkylating agents put patient at risk for developing secondary cancer (Acute Leukemia)
Dactinomycin
- Intercalates DNA
- Used in Wilms’ Tumor, Ewing Sarcoma, Rhabdomyosarcoma
Dasatinib (Sprycel)
- Tyrosine Kinase Inhibitor
- Used in CML
- SE: pulmonary hypertension
Daunorubicin (Cerubidine)
- Anthracyclines
- Generate free radicals to intercalate DNA
  - Causes severe tissue necrosis
- SE: Dilated Cardiomyopathy with chronic use, Mucositis, stomatitis
  - Antitumor Antibiotic, myelosuppression, alopecia, severe gastric upset secondary to colonic mucositis
  - Total cumulative dose is most strongly related to risk
- Antidote is Dexrazoxane
  - Iron-chelating agent used for cardiac protection
Doxorubicin (Hydroxydaunomycin)
- SE: Mucositis, stomatitis
Eculizumab
- MOA: Monoclonal antibody against C5, blocks cleavage and blocks formation of the C5-9 complex
  - Used in Paroxysmal nocturnal hemoglobinuria
Elotuzumab
- MOA: Activating NK cells to kill MM cells, Targets SLAMF7
Erlotinib
- SE: Pustular acneiform eruptions (weak), pulmonary toxicity
Folinic Acid (Leucovorin)
Gefitinib
- SE: Pustular acneiform eruptions (weak)
Hydroxyurea
- MOA: Inhibits ribonucleotide reductase, decreasing DNA synthesis
- Use: Essential Thrombocytopenia, PCV
Ibrutinib (Imbruvica)
- Tyrosine Kinase Inhibitor, binds BTK
- Metabolized by CYP3A4
  - Increases digoxin levels
- Use: CLL, B-cell Lymphoma
- SE: Increased rates of Atrial Fibrillation (up to 16%) – Don’t use CCBs
Imatinib (Gleevec)
- MOA: Blocks ATP binding to tyrosine kinase active site
- Use: CML, GIST
  - Blocks BCR-ABL fusion
- Can be held without significant change in labs, may hold for entire pregnancy without problems
- SE: Nausea
Ifosfamide
- SE: hemorrhagic cystitis
Lenalidomide (Revlimid)
Methotrexate
- MOA: Folate Antagonist (Dihydrofolate Reductase Inhibitor)
  - Converts oxidized folate back into its reduced form to be used in pyrimidine synthesis
    - Can be bypassed/fixed by Leucovorin (N5-formyltetrahydrofolate)
  - used in Rheumatoid Arthritis also
  - Stops DNA and protein synthesis hindering S-phase
- SE: Myelosuppression and Abortifacient, Hepatotoxicity, stomatitis, cytopenia
Microtubule Inhibitors
- Taxols/Taxanes
  - MOA: Inhibit microtubule degradation
    - Bind polymerized microtubules and stabilize the mitotic spindle so it can not break down
    - Inhibiting dynein
    - Cell phase: M phase
  - SE: Some myelosuppression
  - Paclitaxel (Taxol)
    - Nab-paclitaxel (Abraxane)
  - Docetaxel (Taxotere)
- Vinca Alkaloids
  - MOA: Inhibits microtubule production and assembly
    - Bind B-tubulin and block polymerization, therefore the mitotic spindle cannot form
    - Inhibit kinesin
    - Cell phase: M phase
  - Use: Hematologic and solid malignancies
  - SE: Alopecia, Paralytic ileus/constipation
  - Vincristine:
    - Use: Non-Hodgkin
    - SE: Peripheral Neuropathies (Neurotoxic), Alopecia
      - Stocking and glove distribution
      - Areflexia, peripheral neuritis, motor symptoms less commonly
      - Autonomic dysfunction
      - Paralytic ileus/constipation
      - Some myelosuppression usually mild
  - Vinblastine
    - Use: Hodgkin
    - SE: Profound Bone Marrow Suppression, Alopecia
Mitomycin
- Antitumor Antibiotic
- SE: Hemolytic Uremic Syndrome
Nilotinib
- SE: Coronary insufficiency
Nitrosoureas
- Can cross BBB to treat brain cancer
- SE: pulmonary fibrosis
- Carmustine
- Lomustine
- Semustine
- Streptozocin
Panitumumab (Vectibix)
- SE: Pustular acneiform eruptions (severe)
Platinum Drugs
- General
  - Prevent nephrotoxicity with Amifostine
  - Magnesium wasting (hypomagnesemia)
- Carboplatin
  - Platinum Alkylating Agent
    - Hydrate well to protect the kidneys, highly emetogenic (give something for vomiting)
  - SE: Myelosuppression is main/dose limiting SE
    - Less other SE than Cisplatin
      - Ototoxicity and Nephrotoxicity
      - Less nephrotoxic than Cisplatin
- Cisplatin
  - Platinum Alkylating Agent
    - Prevents replication of tumor cells by causing intra-stand links within DNA
  - SE: Myelosuppression, Peripheral Neuropathies (stocking glove), Nephrotoxic (ATN), Ototoxic, electrolyte abnormalities, Tinnitus, N/V
    - Less nephrotoxic with aggressive hydration
- Oxaliplatin
  - SE: Peripheral Neuropathies (stocking glove), transient cold hypersensitivity
    - No cold items for several days after infusions
Ponatinib
- SE: Coronary insufficiency
Purine Analogs
- MOA: Cytotoxic purine analog
  - Inhibits DNA polymerase Alpha and Beta
- SE: Immunosuppression
- Cladribine/Pentostatin
  - Used in symptomatic hairy cell leukemias
Pyrimidine Analogs
- MOA: Cytotoxic pyrimidine analog
  - Inhibits DNA polymerase Alpha and Beta
- SE: Immunosuppression/Myelosuppression
- Gemcitabine (Gemzar)
  - Used in hematologic and solid tumors, small-cell
  - SE: Severe Pulmonary Fibrosis, Hemolytic Uremic Syndrome
- Cytarabine (Ara-C)
  - Aka Arabinofuranosyl Cytidine
  - Used in Non-M3 AML, non-Hodgkin Lymphoma hematologic cancers only
  - Cell Cycle: S phase
  - SE: Megaloblastic Macrocytic anemia, cerebellar toxicity
Radiation
- MOA: Damages DNA, preventing tumor cell division or directly killing the cells
  - Can decrease the tumor size or kill any existing tumor cells
- SE: Slower wound healing, fibrosis, ulcerations, strictures, irritation, neurologic deficits, BM suppression, 2ndary cancers (sarcomas, thyroid cancer, CML)
- Goals: First line in some tumors
  - Eradicate smaller tumors
  - Sensitize cancer cells to radiation therapy
Selective Estrogen Receptor Antagonist (SERM)
- Tamoxifen
  - Antagonist in the breasts, Agonist in the Endometrium and bone
  - SE: Deep Venous Thrombosis (DVT), hot flashes, endometrial cancer risk, teratogenic
- Raloxifene
  - Antagonist in the breasts and endometrium, agonist in bone (osteoporosis treatment)
  - No increased risk for cancer
  - SE: Deep Venous Thrombosis (DVT), hot flashes
Sunitinib (Sutent)
- SE: PRES syndroms
Thalidomide (Thalomid)
Topoisomerase Inhibitors
- Cell Cycles affected: S, G2
- MOA: Eukaryotic Topoisomerase I Inhibitors
  - Topotecan
    - Used in ovarian and small cell lung cancer
  - Irinotecan
    - Used in Colon cancer
  - SE: Severe/Life-threatening Diarrhea
- MOA: Eukaryotic Topoisomerase II Inhibitors
  - Etoposide
  - Teniposide
  - Inhibits relegation of double strand breaks caused by topoisomerase II
  - Used in a regimen with bleomycin and cisplatin for testicular masses, small cell lung cancer, Hodgkin and non-Hodgkin Lymphoma
  - SE: Alopecia, myelosuppression, Immunosuppression
Trastuzumab
- MOA: Anti-HER2/neu antibody
  - Binds HER2 on tumor surface and induces receptor internalization
- Use: HER2 (+) Breast cancer, Gastric cancer
- SE: Type II Cardiotoxicity, pulmonary toxicity, oligohydramnios
  - Avoid pregnancy for 7 months last dose
Tretinoin
- Formulation of Vitamin A, targeted therapy for Acute Promyelocytic Leukemia (M3 variant)
- SE: Rashes, Teratogenic
Vincristine (Oncovorin)

Oncologic Medications

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