5 Chemotherapeutic Agents



10.1055/b-0038-160296

5 Chemotherapeutic Agents

Douglas M. Coldwell

Abraxane, see Paclitaxel Adriamycin, see Doxorubicin Allopurinol


Type: Antihyperuricemic agent.


Method of action: Xanthine oxidase inhibitor.


Half-life: 2 hours.


Metabolized: Liver.


Excretion: Feces.


Indications: Originally gout but hyperuricemia as part of tumor lysis syndrome, which occurs when large volumes of tumors become necrotic and can obstruct the renal tubules. When large tumors are embolized, oral allopurinol therapy can be started several days in advance at 300 mg every 12 hours.


Side effects:




  • Unusual: Skin rash, fever, eosinophilia, hepatitis, decreased renal function, Stevens–Johnson syndrome.



Amifostine


Type: Organic hypophosphate prodrug that is hydrolyzed to the active cytoprotective drug.


Method of action: Free radical scavenger within cells.


Half-life: 8 minutes.


Metabolized: Liver.


Excretion: Feces.


Indications: Cytoprotective agent to reduce renal toxicity from cisplatin and neutropenia-induced fever.


Side effects:




  • Common: diarrhea, hypocalcemia, nausea, vomiting.



  • Serious: Hypotension (in over 60%), cutaneous rash, Stevens–Johnson syndrome, toxic epidermal necrolysis, rash.




BCNU (Carmustine)


Type: Nitrogen mustard alkylating agent.


Method of action: Forms links between deoxyribonucleic acid (DNA)


strands preventing replication and transcription.


Half-life: 1.4 minutes.


Metabolized: Liver.


Excretion: Urine.


Indications: Brain tumors as it will cross the blood–brain barrier, multiple myeloma, Hodgkin’s disease, Non-Hodgkin’s lymphoma.


Side effects: Seizures, hemiplegia, headache, metabolic disorder, somnolence, fever.



Bevacizumab (Avastin)


Type: Angiogenesis inhibitor.


Method of action: Monoclonal antibody binding to vascular endothelial


growth factor-A inhibiting the formation of tumor neovascularity.


Half-life: 20 days.


Excretion: Systemic.


Indications: Colon, lung, renal, ovarian cancers, glioblastoma multiforme.


Side effects: Inhibition of wound healing, arterial dissection, bleeding, bowel perforation, fatigue, infection, thrombotic microangiopathy, necrotizing fasciitis.



Bleomycin


Type: Byproduct of bacterium Streptomyces verticillus.


Method of action: Induces DNA strand breaks and may inhibit the incorporation of thymidine into DNA.


Half-life: 2 hours.


Metabolized: Liver.


Excretion: Urine.


Indications: Hodgkin’s/non-Hodgkin’s disease, testicular, ovarian cervical cancers.


Side effects: Pulmonary fibrosis with oxygen sensitivity, fever, alopecia, Raynaud’s phenomenon (secondary Raynaud’s).




Capecitabine (Xeloda)


Type: Oral prodrug that forms 5-fluorouracil (5FU) by thymidine phosphorylase in tumor tissue.


Method of action: Inhibits DNA synthesis during S phase by thymidylate synthetase inhibition.


Half-life: 0.75 hours.


Metabolized: Liver.


Excretion: Urine.


Indications: Colon cancer, breast cancer.


Side effects: Increases effects of warfarin and increases INR (international normalized ratio). Nausea, diarrhea, cardiotoxicity, hand–foot syndrome, severe mucocutaneous reactions such as Stevens–Johnson syndrome and toxic epidermal necrolysis.



Carmustine, see BCNU Cetuximab (Erbitux)


Type: Monoclonal antibody to human epidermal growth factor receptor (EGFR).


Method of action: Prevents uncontrolled growth via the EGF pathway but must have KRAS (V-Ki-ras2 Kirsten rat sarcoma viral oncogene homolog) wild-type receptor.


Half-life: 114 hours.


Excretion: Systemic.


Indications: KRAS wild-type colorectal carcinoma, head and neck cancer, non–small cell lung cancer.


Side effects: Dermatologic reaction, erythema, acneiform dermatitis, pruritus, hypomagnesemia, fatigue, abdominal pain, nausea, diarrhea/constipation, vomiting.


Rare: pulmonary or cardiac toxicity.



Cyclophosphamide (Cytoxan)


Type: Alkylating antineoplastic.


Method of Action: Cross-linking with tumor DNA, not cell cycle stage specific, immunosuppressive.


Half-life: 3 to 12 hours.


Metabolized: Liver.


Excretion: Feces.


Indications: Non-Hodgkin’s lymphoma (NHL), breast cancer.


Side Effects: Immunosuppression, hemorrhagic cystitis, radiation recall effect.




Dacarbazine (DTIC)


Type: Alkylating agent for both DNA and ribonucleic acid (RNA). Method of Action: Causes DNA double-strand breaks and apoptosis.


Half-life: 5 hours.


Metabolized: Liver.


Excretion: Urine.


Indications: Hodgkin’s disease, metastatic melanoma.


Side effects: Nausea, vomiting, leukopenia, thrombocytopenia, hypersensitivity.



Daunorubicin


Type: Anthracycline antitumor antibiotic.


Method of Action: Intercalates between DNA base pairs and inhibits topoisomerase II.


Half-life: 18.5 to 26 hours.


Metabolized: Liver.


Excretion: Feces.


Indications: Acute nonlymphocytic leukemia, acute lymphocytic leukemia.


Side Effects: Nausea, vomiting, cardiac arrhythmias.



Docetaxel (Taxotere)


Type: Semisynthetic taxane.


Method of Action: Prevents depolymerization of cellular microtubules resulting in DNA, RNA, and protein synthesis inhibition.


Half-life: 11 hours.


Metabolized: Liver.


Excretion: Urine.


Indications: Breast cancer, non-small cell lung cancer, gastric cancer, head and neck cancer, prostate cancer (with prednisone).


Side effects: Peripheral neuropathy, stomatitis, renal or hepatic impairment, neutropenia, diarrhea, thrombocytopenia, alopecia.




Doxorubicin (Adriamycin)


Type: Anthracycline antitumor antibiotic.


Method of action: Intercalates with tumor DNA preventing the action of the enzyme topoisomerase II cleaving the DNA and results in apoptosis.


Half-life: 1 to 3 hours.


Metabolized: Liver.


Excretion: Urine, feces.


Indications: Bladder, breast, stomach, lung, ovaries, thyroid, soft-tissue sarcoma, multiple myeloma.


Side Effects: Cardiac toxicity, myelosuppression, alopecia.



Epirubicin


Type: Anthracycline antitumor antibiotic.


Method of action: Intercalates with tumor DNA preventing the action of the enzyme topoisomerase II cleaving the DNA and results in apoptosis.


Half-life: 31 to 35 hours.


Metabolized: Liver.


Excretion: Feces.


Indications: Breast cancer.


Side effects: Hepatic and renal dysfunction, bone marrow dysfunction, neutropenia, alopecia, nausea, vomiting, leukopenia, thrombocytopenia, amenorrhea, anemia, mucositis.



Epoetin Alfa (EPO, Procrit, Epogen)


Type: Hematopoietic growth factor.


Method of action: Stimulates erythropoiesis via division and differentiation in bone marrow.


Half-life: 16 to 67 hours.


Metabolized: Liver.


Excretion: Feces.


Indications: Anemia due to chemotherapy or kidney disease, preparation for surgery with high risk of blood loss.


Side Effects: Fever, nausea, hypertension, cough, vomiting, pruritus, rash, headache, arthralgias.




Erbitux, see Cetuximab Erlotinib (Tarceva)


Type: Small molecule tyrosine kinase inhibitor.


Method of action: Binds to EGFR and inhibits the production of tyrosine kinase.


Half-life: 36.2 hours.


Metabolized: Liver.


Excretion: Feces.


Indications: Non–small cell lung cancer, locally advanced pancreatic cancer.


Side effects: Acneiform rash (which is thought to be a marker of clinical benefit), erythema, pruritus, fatigue, diarrhea.

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May 21, 2020 | Posted by in ONCOLOGY | Comments Off on 5 Chemotherapeutic Agents
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