Antineoplastic Agents

Antineoplastic Agents

Antineoplastic Agents

Antineoplastic Agents are drugs used to combat cancer or the growth of neoplasms.

Antineoplastic agents comprise one aspect of chemotherapy.

The term used to describe the use of anti-cancer drugs in the treatment of cancer is chemotherapy

These drugs act on and kill altered human cells. While their action is intended to target abnormal cells, normal cells are also affected.

These drugs can work by affecting cell survival or by boosting the immune system in its efforts to combat the abnormal cells.

Common Terms

  • Alopecia: hair loss; a common adverse effect of many antineoplastic drugs, which are more effective against rapidly multiplying cells such as those of hair follicles.
  • Anaplasia: loss of organization and structure; property of cancer cells.
  • Angiogenesis: the generation of new blood vessels; cancer cells release an enzyme that will cause angiogenesis or the growth of new blood vessels to feed the cancer cells.
  • Antineoplastic agent: drug used to combat cancer or the growth of neoplasms.
  • Carcinoma: tumor that originates in epithelial cells.
  • Metastasis: ability to enter the circulatory or lymphatic system and travel to other areas of the body that are conducive to growth and survival; property of cancer cells.
  • Neoplasm: new or cancerous growth; occurs when abnormal cells have the opportunity to multiply and grow.
  • Sarcoma: tumor that originates in the mesenchyme and is made up of embryonic connective tissue cells.
  • Autonomy is the ability to grow without usual homeostatic restrictions that regulate cell growth and control.
  • Cancer: refers to a malignant neoplasm or new growth

Cancers can be divided into two groups:

  1. Solid tumors
  2. Hematological

Solid tumors can further be differentiated into carcinomas, or tumors that originate in epithelial cells, and sarcomas, or tumors that originate in the mesenchyme and are made up of embryonic connective tissue cells.

Hematological malignancies involve blood forming organs of the body, the bone marrow, the lymphatic system. These malignancies alter the body’s ability to produce and regulate the cells found in the blood.

Types of anti-neoplastic drugs

  1. Alkylating Agents
  2. Antimetabolites
  3. Antineoplastic Antibiotics
  4. Mitotic Inhibitors
  5. Hormone and Hormone Modulators
  6. Cancer cell-specific Agents
  7. Miscellaneous Antineoplastics.

Alkylating agents/DNA replication inhibitors

They bind to the DNA of cancer cells and prevent it from replicating.

These are the agents of choice for slow-growing cancers.

Indications

  1. Treatment of slow-growing cancers, like lymphomas, leukemias, myelomas, some ovarian, testicular, and breast cancers, and pancreatic cancers.
  2. Pulmonary carcinoma/Lung cancer
  3. Leukemia
  4. Neuroblastoma
  5. Lymphomas
  6. Rheumatoid arthritis
  7. Retinoblastoma

Contraindications

  1. Pregnancy and Lactation: Severe effects to fetus and neonate.

 Caution is exercised in;

  1. Known allergy to prevent hypersensitivity reactions.
  2. Bone marrow suppression
  3. Anemia
  4. Thrombocytopenia
  5. Leukopenia
  6. Suppressed renal or hepatic function. Interfere with drug metabolism and excretion.

Adverse Effects

Use of alkylating agents may result to these adverse effects:

  1. GI: nausea, vomiting, anorexia, diarrhea, and mucous membrane deterioration, hepatic toxicity
  2. GU: renal toxicity, potentially toxic increase in uric acid levels
  3. Hematological: bone marrow suppression
  4. Alopecia or hair loss

Examples of drugs

Cyclophosphamide (Cytoxan, Neosar)

Dose;

  • Induction: 40–50 mg/kg per day IV over 2–5 days, or 1–5 mg/kg per day Orally
  • Maintenance: 1–5 mg/kg per day Orally, or 10–15 mg/kg IV for 7–10 days

Busulfan (Busulfex, Myleran)

Dose;

  • Induction: 4–8 mg/d Orally
  • Maintenance: 1–3 mg/d Orally
  • Injection: 0.8 mg/kg as a 2-hrly IV infusion for 4 days via a central venous catheter

Chlorambucil (Leukeran)

Dose;

  • 0.1–0.2 mg/kg per day Orally for 3–6 weeks; or
  • 0.4 mg/kg Orally every 2 weeks with maintenance dose of 0.03–0.1 mg/kg per day Orally.

Anti-metabolites

Antimetabolites are drugs that have chemical structures similar to those of various natural metabolites that are necessary for growth and division of rapidly growing neoplastic cells and normal cells.

Indications

  1. Treatment of various leukemias and some GI and basal cell cancers
  2. Leukemia
  3. Lymphomas
  4. Psoriasis
  5. Cancer of the breasts, stomach, pancreas and colon
  6. Use has been somewhat limited because neoplastic cells rapidly develop resistance to these Therefore, they are commonly administered as part of combination therapy.

Contraindications and Cautions

The following are contraindications and cautions for the use of antimetabolites:

  1. Known allergy to drug: Prevent hypersensitivity reactions
  2. Pregnancy and lactation: Severe effects on the fetus and neonate
  3. Bone marrow suppression:
  4. Renal and hepatic dysfunction: Interfere with drug metabolism and excretion
  5. Known GI ulceration or ulcerative diseases: Can be exacerbated by the effects of the drug

Adverse Effects

Use of antimetabolites may result to these adverse effects:

  1. CNS: headache, drowsiness, aphasia, fatigue, malaise, dizziness
  2. Respiratory: pulmonary toxicity, interstitial pneumonitis
  3. Hematological: bone marrow suppression
  4. GI: nausea, vomiting, anorexia, diarrhea, mucous membrane deterioration, hepatic toxicity
  5. GU: renal toxicity
  6. Leucovorin is an active form of folic acid that is used to rescue normal cells from the adverse effects of methotrexate therapy in the treatment of osteosarcoma.

Examples of anti-metabolite drugs

Methotrexate (Rheumatrex, Trexall)

Dose;

  • Dose varies with route and disease being treated; 15–30 mg Orally or IM is common

Fluorouracil (Adrucil, Carac, Efudex, Fluoroplex)

Dose;

  • 12 mg/kg per day IV on days 1–4, then 6 mg/kg IV on days 6, 8, 10, and 12 

Anti neoplastic antibiotics

This group of drugs is selective for bacterial cells. However, they are also toxic to human cells. They are aimed towards rapidly-multiplying cells.

NB: These drugs have potentially adverse effects which limit their usefulness in patients with pre-existing disease and those who are debilitated.

Indications

  1. Treatment of various types of cancer, particularly those with rapidly-dividing nature.
  2. Choriocarcinoma/hydatidform mole disease
  3. Testicular cancer
  4. Lymphoma
  5. Lymphosarcoma
  6. Squamous cell carcinoma

Contraindications and Cautions

The following are contraindications and cautions for the use of antineoplastic antibiotics:

  1. Known allergy to drug: Prevent hypersensitivity reactions
  2. Pregnancy and lactation: Severe effects on the fetus and neonate
  3. Bone marrow suppression: Index of re-dosing and dosing levels
  4. Renal and hepatic dysfunction: Interfere with drug metabolism and excretion
  5. Known GI ulceration or ulcerative diseases: Can be exacerbated by the effects of the drug
  6. Pulmonary problems: Exacerbated by bleomycin or mitomycin
  7. Cardiac problems: Exacerbated by idarubicin or mitoxantrone

Adverse Effects

  1. CNS: headache, drowsiness, aphasia, fatigue, malaise, dizziness
  2. Respiratory: pulmonary toxicity, interstitial pneumonitis
  3. Hematological: bone marrow suppression
  4. GI: nausea, vomiting, anorexia, diarrhea, mucous membrane deterioration, hepatic toxicity
  5. GU: renal toxicity
  6. Alopecia

Examples of antineoplastic antibiotic drugs

Bleomycin (Blenoxane);

Dose;

  • A test dose of 1-2units given 2-4hours prior to therapy is recommend; 0.25–0.5 units/kg IM, IV, or SC once or twice weekly 

Dactinomycin (Cosmegen)

Dose;

  • Adult: 0.5 mg/d IV for up to 5 days
  • Pediatric : 0.015 mg/kg/d IV for up to 5 days

Doxorubicin (Adriamycin, Doxil)

Dose;

  • 60–75 mg/m2 as a single IV dose; repeat every 21 days.

Mitomycin (Mutamycin)

Dose;

  • Mutamycin 20 mg/m2 IV as a single dose at 6–8-weeks intervals

Valrubicin (Valstar)

Dose;

Mitotic inhibitors/Vinca alkaloids

Drugs that kill cells as the process of mitosis begins. Mitotic inhibitors are cell cycle-specific agents that inhibit DNA synthesis.

They work by Interfering with the ability of the cell to divide by blocking or altering the M phase of the cell cycle.

Indications

  1. Treatment of a variety of tumors and leukemias.
    • Leukemia
    • Lymphomas g. Hodgkin’s lymphoma, histiocystic lymphoma
    • Karposis sarcoma
    • Testicular cancer
    • Breast cancer
  2. They inhibit mitosis thereby preventing the replication of cancer cells.

Contraindications and Cautions

The following are contraindications and cautions for the use of mitotic inhibitors:

  1. Known allergy to drug: Prevent hypersensitivity reactions
  2. Pregnancy and lactation: Severe effects on the fetus and neonate
  3. Bone marrow suppression: Index of re-dosing and dosing levels
  4. Renal and hepatic dysfunction: Interfere with drug metabolism and excretion
  5. Known GI ulceration or ulcerative diseases: Can be exacerbated by the effects of the drug
  6. Anemia
  7. Leukopenia
  8. Thrombocytopenia

Adverse Effects

Use of mitotic inhibitors may result to these adverse effects:

  1. CNS: headache, drowsiness, aphasia, fatigue, malaise, dizziness
  2. Respiratory: pulmonary toxicity, interstitial pneumonitis
  3. Hematological: bone marrow suppression
  4. GI: nausea, vomiting, anorexia, diarrhea, mucous membrane deterioration, hepatic toxicity
  5. GU: renal toxicity
  6. Alopecia
  7. Parathesia
  8. Stomatitis
  9. Nausea and vomiting
  10. Diarrhea
  11. Constipation
  12. Can cause necrosis and cellulitis if extravasation occurs

Examples of Mitotic inhibitors

Vincristine(Oncovin, Vincasar)

Dose;

  • Adult: 1.4 mg/m2 IV at weekly intervals
  • Pediatric: 1.5–2 mg/m2 IV once weekly

Vinblastine (Velban)

Dose:

  • Adult: 3.7 mg/m2 IV once weekly
  • Pediatric: 2.5 mg/m2 IV once weekly.

 

Hormones and Hormone Modulators

Introduction

Some cancers, particularly those involving the breast tissue, ovaries, uterus, prostate, and testes, are sensitive to estrogen stimulation. Estrogen-receptor sites on the tumor react with circulating estrogen, and this reaction stimulates the tumor cells to grow and divide

Hormones and hormone modulators block or interfere with these receptor sites to prevent growth of the cancer and cause cell death.

Some hormones are used to block the release of gonadotropic hormones in breast or prostate cancer if the tumors are responsive to gonadotropic hormones. Others may block androgen-receptor sites directly.

Indications

  1. Treatment of breast cancer in postmenopausal women or in other women without ovarian
  2. Treatment of prostatic cancers that are sensitive to hormone

Contraindications and Cautions

  1. Known allergy to drug: Prevent hypersensitivity reactions
  2. Hypercalcemia: Contraindication to the use of toremifene because the drug can increase serum calcium
  3. Pregnancy and lactation: Severe effects on the fetus and neonate
  4. Bone marrow suppression: Index of re-dosing and dosing levels
  5. Renal and hepatic dysfunction: Interfere with drug metabolism and excretion
  6. Known GI ulceration or ulcerative diseases: Can be exacerbated by the effects of the drug

Adverse Effects

  1. Menopause-associated effects: hot flashes, vaginal spotting, vaginal dryness, moodiness, and depression
  2. Hematological: bone marrow suppression
  3. GI: hepatic toxicity
  4. GU: renal toxicity
  5. Hypercalcemia is encountered as the calcium is pulled out of the bones without estrogen activity to promote calcium

Examples of Hormones and Hormone Modulators

Tamoxifen (Nolvadex, Soltamox)

Dose;

  • 20–40 mg/d Orally

Others;

  • Androgen testolactone
  • Conjugate estrogens
  • Progestin megestrol

Cancer Cell-Specific Agents

These drugs would not have the devastating effects on healthy cells in the body and would be more effective against particular cancer cells. Three groups of drugs are available for cancer cell–specific actions: protein tyrosine kinase inhibitors, an epidermal growth factor inhibitor, and a proteasome inhibitor.

Therapeutic Action

  1. Protein tyrosine kinase inhibitors act on specific enzymes that are needed for protein building by specific tumor Blocking of these enzymes inhibits tumor cell growth and division. They do not
    affect healthy human cells, so the patient does not experience
    the numerous adverse effects associated with antineoplastic
    chemotherapy. The protein tyrosine kinase inhibitors that are available include everolimus (Afinitor), gefitinib (Iressa), imatinib
    (Gleevec), lapatinib (Tykerb), nilotinib (Tasigna), sorafenib
    (Nexavar), sunitinib (Sutent), and temsirolimus (Torisel). 
  2. Epidermal growth factor inhibitors are drugs that act on epidermal growth factor receptors which are found in both normal and cancerous cells but are more abundant on rapidly
    growing cells. Example is erlotinib (Tarceva),
  3. Proteasome inhibitors are drugs indicated for inhibition of proteasome in human cells, a large protein complex that works to maintain cell homeostasis and protein production.
    Without it, the cell loses homeostasis and dies. This drug was
    shown to delay growth in selected tumors. Example is bortezomib (Velcade)

Indications

Cancer cell-specific agents are indicated for the following medical conditions:

  1. Imatinib, the first drug approved protein tyrosine kinase inhibitor, is given orally and is approved to treat chronic myelocytic leukemia (CML). It selectively inhibits the Bcr-Abl tyrosine kinase created by the Philadelphia chromosome abnormality in
  2. Bortezomib is used for the treatment of multiple myeloma in patients whose disease had progressed after two standard

Contraindications and Cautions

  1. Pregnancy: All drugs in this class is pregnancy category D.
  2. Women of childbearing age: Must be advised to use barrier contraceptives while taking these drugs.
  3. Lactation: Can enter breast milk and use is only justified if benefits outweigh the danger.
  4. Hepatic dysfunction: Increased risk of toxicity with imatinib.
  5. Nilotinib is contraindicated with patients who have
    or who are at risk for prolonged QT intervals (hypokalemia,
    hypomagnesia, or taking another drug that prolongs the QT
    interval) because it prolongs the QT interval, and sudden
    deaths could occur.
  6. Known allergy to the drug: Prevent hypersensitivity

Adverse Effects

Use of cancer cell-specific agents may result to these adverse effects:

  1. Imatinib: GI upset, muscle cramps, heart failure, fluid retention, skin Severe adverse effects of traditional antineoplastic therapy (severe bone marrow depression, alopecia, severe GI effects) do not occur.
  2. Gefitinib: potentially severe interstitial lung disease and various eye symptoms
  3. Pazopanib: some bone marrow depression, diarrhea, hypertension, and liver impairment, change in hair color
  4. Lapatinib: diarrhea, liver impairment, altered heart function
  5. Erlotinib and bortezomib: cardiovascular events, pulmonary toxicity
  6. Bortezomib: peripheral neuropathy, liver and kidney impairment

Platinum analogues/ miscellaneous anti-neoplastics

The mechanism of action of this unrelated group of drugs is not entirely clear.

Examples of miscellaneous anti-neoplastics include

  1. Cisplatin: 20—70 mg/m2 IV
  2. Carboplatin: 360 mg/m2 IV
  3. Hydroxyurea: 20—80 mg/kg PO (it belongs to a class known as substituted ureas)

Indications

  1. Testicular cancer
  2. Ovarian cancer
  3. Bladder cancer
  4. Sickle cell crisis prevention for Contra indications, side effects are the same.

Nursing Considerations

Here are important nursing considerations when administering antineoplastic agents:

Nursing Assessment

These are the important things the nurse should include in conducting assessment, history taking, and examination:

  1. Assess for the mentioned cautions and contraindications (e.g. drug allergies, hepatorenal impairment, bone marrow suppression, pregnancy and lactation, etc.) to prevent any complications.
  2. Perform a thorough physical assessment (other medications taken, orientation and reflexes, vital signs, bowel sounds, etc.) to establish baseline data before drug therapy begins, to determine effectiveness of therapy, and to evaluate for occurrence of any adverse effects associated with drug therapy.
  3. Monitor result of laboratory tests such as CBC with differential to identify possible bone marrow suppression and toxic drug effects and establish appropriate dosing for the drug; and liver and renal function tests to determine need for possible dose adjustment and identify toxic drug effects.
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