Cancer Chemotherapeutic Agents

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
Adverse effects:

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With cancer chemotherapeutics, adverse effects are often an extension of the therapeutic action of the drug.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
Minimizing adverse effects:

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-Central line ifusion produces the same therapeutic effects as continuous infusion, but produces less adverse effects.
-drugs that are synergistic in therapeutic mechanism (but have different adverse effects) may be used in combination therapy. Lower doses of each drug may be used to decrease the probability of adverse effects.
_Radiation sensitizeers- Some drugs sensitize tumor tissue to the effects of radiation, which increases the effects of radiation therapy. Since low doses of drug are often all that is necessary for maximum efficacy, adverse effects are dramtically decreased.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
List all subclasses

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alkylating agents
nitrogen containing drugs
Unclassified Agents
Platinum containing compounds

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
Mech of action:

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act by chemically reacting with DNA- adding a chemical group called an alkyl group to certain parts of DNA. (RNA may also be affected at high doses.) These drugs may have active sites at one or both ends of the molecule. Depending on where the active sites are, the drugs may crosslink DNA strands (leading to lack of DNA replication), or simply cause errors in DNA replication and gragmentation of DNA strands. The ultimate result in either case is an inability of the tumor cells to replicate.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
Therapeutic effects

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Most alkylating agents are non cell specific and will affect cells at any stage of division. Thus, cell division, particularly in a tumor with rapidly dividing cells is halted in a manner that is dose dependant. Those cells that divide less rapidly (e.g. normal tissue) have the opportunity to repair the damaged DNA and are less affected by the drug.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
Uses:

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Due to their ability to obstuct cell division, alkylating agents are most useful in the treatment of smaller tumors, which have more dividing cells, but they may also be useful in some slower growing rumors, as well.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
nitrogen containing drug
Mech of action:

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Nitrogen mustards cause a decrease in the rate of growth of lymphoid tissue and are thus useful in the treatment of lymphomas. Mechlorethamine is the only pure nitrogen mustard still in use, but its use is restricted to the treatment of Hodgkin’s disease.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
nitrogen containing drug
Nitrogen Mustards and their Derivatives
List all drugs:

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1. Cyclophosphamide (cytoxan)
2. Ifosphamide (ifex)

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
nitrogen containing drug
Nitrogen Mustards and their Derivatives
Cyclophosphamide (cytoxan)
Uses:

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therapy of multiple myeloma, lymphomas, and lymphoid leukemias; useful in the treatment of lymphomas. It is also useful in treatment of autoimmune disease and in transplantation, due to its immunosuppressant effect.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
nitrogen containing drug
Nitrogen Mustards and their Derivatives
Cyclophosphamide (cytoxan)
Adverse effects:

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inflammation of bladder with bleeding; hemorrhagic cysitis

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
nitrogen containing drug
Nitrogen Mustards and their Derivatives
Ifosphamide (ifex)
Adverse effects:

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inflammation of bladder with bleeding; severe bone marrow toxicity;hemorrhagic cystitis

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
nitrogen containing drug
Nitrogen Mustards and their Derivatives
Ifosphamide (ifex)
Uses:

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third-line chemotherapy in germ cell testicular cancer.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
nitrogen containing drug
Nitrogen Mustards and their Derivatives
Ifosphamide (ifex)
Form:

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Only available in combination packages with Mesnex, a protective agent ofr the renal system

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
nitrogen containing drug
Nitrogen Mustards and their Derivatives
Nitrosoureas (derived from nitrogen mustards)
List all drugs:

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1.Carmustine( BICNU)
2. Lomustine (CEENU)

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
nitrogen containing drug
Nitrogen Mustards and their Derivatives
Nitrosoureas (derived from nitrogen mustards)
Carmustine( BICNU)
Uses:

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Carmustine may be used as adjunct therapy for brain tumors, as it crosses the blood-brain barrier

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
nitrogen containing drug
Nitrogen Mustards and their Derivatives
Nitrosoureas (derived from nitrogen mustards)
Lomustine (CEENU)
USES:

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may be used as a last resort therapy in lung cancer

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
alkylating agents
nitrogen containing drug
Nitrogen Mustards and their Derivatives
Nitrosoureas (derived from nitrogen mustards)
Streptozocin
Uses:

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Directly toxic to pancreatic Beta-cells and thus is used strictly as an agent to combat islet cell carcinoma.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
Unclassified Agents
List all drugs:

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1. Thiotepa (Thioplex)
2. Busufan (busulfex)

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
Unclassified Agents
Thiotepa (Thioplex)
Uses:

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may be used in the thearpy of breast and bladder cancer; however, it is rarely used as a cancer chemotherapeutic agent at the present time. The major use of this durg is as a preparative agent in bone marrow transplantation in the therapy of breast cancer… Used (rarely) in the therapy of adenocarcinoma of the breast and ovary

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
Unclassified Agents
Thiotepa (Thioplex)
Form:

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must be filtered through a .22 micron sterile filter before administraiton.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
Unclassified Agents
Busufan (busulfex)
Uses:

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prepartation of bone marrow/stem cell transplants… used to destroy the myeloid cell line prior to an allergenic bone marrow transplant for leukemia

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
Platinum containing compounds
Mech of action:

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these drugs are DNA crosslinking agents-they form crosslinks between DNA strands, effectively binding the strands together so that they cannot separate and be copied. Thus, cellular replication is halted.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
Platinum containing compounds
List all drugs:

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1. Cispatin (platinol, platinol AQ (aqueous formulation)
2. Carboplatin (Paraplatin)

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
Platinum containing compounds
Cispatin (platinol, platinol AQ (aqueous formulation)
Mech of action:

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unique in that it must first enter the cell before it is activated. Once inside the cell, the ring structure of the drug reacts with water to form the active form of the drug, which effectively crosslinks the strands of DNA and RNA. Because the drug is activated inside of the tumor cell, adverse effects are reduced.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
Platinum containing compounds
Cispatin (platinol, platinol AQ (aqueous formulation)
Adverse effects:

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hypersensitivity reaction (allergic reacions); bone marrow suppression, alopecia, and nausea are likely to occur… Toxic to the kidney, ear, and bone marrow;neprhrotoxicity, ototoxicity, peripheral neuropathy

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
Platinum containing compounds
Cispatin (platinol, platinol AQ (aqueous formulation)
Contraindications:

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pregnancy; chemically reacts with aluminum-any portion of the intravenous infusion set containing aluminum may cause a black precipitate to be formed.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
Platinum containing compounds
Cispatin (platinol, platinol AQ (aqueous formulation)
Carboplatin (Paraplatin)
Mech of action:

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radiation sensitizer(potientiates the effects of radiation); unique in that it must first enter the cell before it is activated. Once inside the cell, the ring structure of the drug reacts with water to form the active form of the drug, which effectively crosslinks the strands of DNA And RNA. Because the drug is activated inside of the tumor cell, adverse effects are reduced.

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CANCER CHEMOTHERAPEUTIC AGENTS
Major Chemotherapeutic Drugs By Class
Platinum containing compounds
Cispatin (platinol, platinol AQ (aqueous formulation)
Carboplatin (Paraplatin)
Uses:

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therapy of advanced ovarian carcinoma (second line therapy); radiation sensitizer- concurrent use with radiation therapy potentiates the effects of radiation.

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CANCER CHEMOTHERAPEUTIC AGENTS
Anti-Tumor Antibiotics
Alkylating agents that are antibiotics
List drug:

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Mitomycin (mutamycin)

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CANCER CHEMOTHERAPEUTIC AGENTS
Anti-Tumor Antibiotics
Alkylating agents that are antibiotics
Mitomycin (mutamycin)
Mech of action:

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Activated inside the cell and is concentrated in tumor tissue. The active metabolite binds to guanine residues and may form crosslinks with DNA, resulting in inhibition of DNA synthesis.

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CANCER CHEMOTHERAPEUTIC AGENTS
Anti-Tumor Antibiotics
Alkylating agents that are antibiotics
Mitomycin (mutamycin)
Uses:

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combo therapy, acts as a radiation senstizer. It is thus used in combo with radiation therapy.

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CANCER CHEMOTHERAPEUTIC AGENTS
Anti-Tumor Antibiotics
Alkylating agents that are antibiotics
Mitomycin (mutamycin)
Adverse effects:

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severe bone marrow toxicity; carcinogenic agent-may promote tumor formation; potent teratogen-may cause sever birth defects

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CANCER CHEMOTHERAPEUTIC AGENTS
Antimetabolite Antineoplastic Drugs
Mech of action:

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These drugs interfere with the utilzation of folic acid, which is normally sused to make thymidine, a component of DNA.

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CANCER CHEMOTHERAPEUTIC AGENTS
Antimetabolite Antineoplastic Drugs
Inhibitors of Folic Acid Utilization
List drug:

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Methotrexate ( Trexall, methotrex, rheumatrex DP)

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CANCER CHEMOTHERAPEUTIC AGENTS
Antimetabolite Antineoplastic Drugs
Inhibitors of Folic Acid Utilization
Methotrexate ( Trexall, methotrex, rheumatrex DP)
Mech of action:

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inhibitor of the enzyme dihydrofloate reductase (DHFR), which is involved in the cellular cascade that results in the production of thymidine, a building bolck for the synthesis of DNA. The lack of thymidine results in DNA strand breakage and decreased cellular reproduction. TNA is not affected, as thymidine is not used in RNA.

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CANCER CHEMOTHERAPEUTIC AGENTS
Antimetabolite Antineoplastic Drugs
Inhibitors of Folic Acid Utilization
Methotrexate ( Trexall, methotrex, rheumatrex DP)
Uses:

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choriocarcinoma, acute lymphocytic leukemia, breast cancer, and other cancer types; used in the therapy of rheumation arthritis(due to it’s immunosuppressant properties) exhibits cell selectivity- the drug is selectively concentrated in lymph tissue making it useful in the therapy of acute lymphoblasic leukemia, as well as treatment of choriocarcinoma and moderated grade lymphomas ( grades 3 and 4). Methotrexate is also useful in treatment of cancers of the breast and bladder, and is used intrathecally to treat malignant disease that has spread to the meninges.

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CANCER CHEMOTHERAPEUTIC AGENTS
Antimetabolite Antineoplastic Drugs
Inhibitors of Folic Acid Utilization
Methotrexate ( Trexall, methotrex, rheumatrex DP)
Methotrexate resistance:

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Tumor cell resistance to this drug in sno uncommon. Cells may produce altere DHFR or increased levels of DHFR. Entrance of the drug into the tumor cell may also be inhibited.

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CANCER CHEMOTHERAPEUTIC AGENTS
Antimetabolite Antineoplastic Drugs
Inhibitors of Folic Acid Utilization
Methotrexate ( Trexall, methotrex, rheumatrex DP)
adverse effects:

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rash, immunosuppresio, bone marrow suppresion, and liver fibrosis (rare)

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CANCER CHEMOTHERAPEUTIC AGENTS
Antimetabolite Antineoplastic Drugs
leukovorin rescue
List drug:

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leukovorin calcium (leukovorin CA, Wellcovorin)

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CANCER CHEMOTHERAPEUTIC AGENTS
Antimetabolite Antineoplastic Drugs
leukovorin rescue
leukovorin calcium (leukovorin CA, Wellcovorin)
Mech of action:

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Normal cells exposed to methotrexate can be “rescued” from the effects of the drug by the administation of leukovorin (reduced folic acid). The leukovorin allows for normal activity of DHFR, and allows production of thymidine. High doses of methotrexate can therefore be administered therapeutically, and the normal cells “rescued” with leukovorin. This provides for a significant effect on the rapidly dividing tumor cells, while minimizing effects on normal tissue.

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CANCER CHEMOTHERAPEUTIC AGENTS
Pyrimidine Antagonists
Mech:

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This class of drug inhibit’s the synthesis of DNA by inhibiting the synthesis of nucleotides.

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CANCER CHEMOTHERAPEUTIC AGENTS
Pyrimidine Antagonists
Form:

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orally but preffered administration is central line

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CANCER CHEMOTHERAPEUTIC AGENTS
Pyrimidine Antagonists
List all subclasses

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6-Mercaptopurine and thioguanine
Taxanes
Topoisomerase inhibitors
Camptothectins
Antibiotic Chemotherapeutic Agents
Anthracycline antibiotics

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CANCER CHEMOTHERAPEUTIC AGENTS
Pyrimidine Antagonists
Adverse effects:

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bone marrow suppresion, thrombocytopenia, and hand and foot syndrome (in hand and foot syndrome, the patient experiences reddening of the palms and the soles of the feet- this is thought to be due to blood vessel damage caused by the drug.

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CANCER CHEMOTHERAPEUTIC AGENTS
Pyrimidine Antagonists
List all drugs:

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A.5-Fluorouracil [5-fu] (Aducil, efudex, fluoroplex)
B. Use of leukovorin with F-5u
When used in conjunction with 5-fu, leukovorin produces the oppoiste effect of its usse with methotrexate. Instead of rescuing cells, it potentiates the actions of the drug, by allowing more cofactor to be made and thus increasing the number of stabilized enzyme -cofactor complexes. This reduces the amount of enzyme available, and decreases the synthesis of thymidine. Thus, the use of leukoorin allows lower doses of 5-fu to be administered, decreasing the severity of adverse effects.
B. Capecitabine (xeloda)
C. Cytarabine (cytosar U, DepoCyt (liposomal formulation)

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CANCER CHEMOTHERAPEUTIC AGENTS
Pyrimidine Antagonists
5-Fluorouracil [5-fu] (Aducil, efudex, fluoroplex)
Mech of action:

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pro-drug that is converted to an altered building block of DNA. Fluorouracil interferes in nucleic acid function, by inactivating a key enzyme required for the synthesis of DNA.

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CANCER CHEMOTHERAPEUTIC AGENTS
Pyrimidine Antagonists
Capecitabine (xeloda)
Uses:

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therapy of breast cancer, which is resistant to anthracycline antibiotics and paclitaxel.

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CANCER CHEMOTHERAPEUTIC AGENTS
Pyrimidine Antagonists
Cytarabine (cytosar U, DepoCyt (liposomal formulation)
Mech of action:

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Pro-drug. It is metabolized intracellularly to an agent that competitively inhibits DNA polymerase, resulting in decreased DNA synthesis. This drug is also directly incorporated into both RNA and DNA, resulting in altered DNA and RNA synthesis.

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CANCER CHEMOTHERAPEUTIC AGENTS
Pyrimidine Antagonists
Cytarabine (cytosar U, DepoCyt (liposomal formulation)
Uses:

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thearpy of acute myeloid and lymphoid leukemias. Also used in combination with anthracyclines (eg. Idarubicin) for induction therapy of acute myelogenous leukemia (AML.) Used intrathecally to treat malignant disease that has spread to the meninges

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CANCER CHEMOTHERAPEUTIC AGENTS
6-Mercaptopurine and thioguanine
Mech of action:

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These drugs are metabolized to the nucleotide form of the nucleic acid via hypoxanthine-guanine phosphoribosyl transferase (HGPRT). The nucleotide form is recognized by synthetic enzymes, and acts as a false substrate in the pruine synthesis pathway.

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CANCER CHEMOTHERAPEUTIC AGENTS
6-Mercaptopurine and thioguanine
List drugs in class:

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A. 6-mercaptopurine (purinethol)
B. 6- thioguanine (tabloid)
C. Fludarabine
D. Fludarabind Phosphate (fludara)
E. Pentostatin (nipent)

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CANCER CHEMOTHERAPEUTIC AGENTS
6- thioguanine (tabloid)
Uses:

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therapy of acute, non lymphocyctic leukemia only

Front 53

CANCER CHEMOTHERAPEUTIC AGENTS
6- thioguanine (tabloid)
Adverse effects:

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these durgs cause rapid tumor cell lysis, which may precipitate gout.

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CANCER CHEMOTHERAPEUTIC AGENTS
Fludarabine
Mech of action:

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cell specific agent. It acts to inhibit DNA polymerase and interfere with cellular replication

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CANCER CHEMOTHERAPEUTIC AGENTS
Fludarabind Phosphate (fludara)
Mech:

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fludarabind is a cell cycle specific agent. itacts to inhibit DNA polymerase and interfere with cellular repliaction.

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CANCER CHEMOTHERAPEUTIC AGENTS
Fludarabind Phosphate (fludara)
Uses:

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therapy of B-cell chronic lymphocytic leukemia (CLL)

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CANCER CHEMOTHERAPEUTIC AGENTS
Fludarabind Phosphate (fludara)
Adverse effects:

Back 57

myelosuppresion

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CANCER CHEMOTHERAPEUTIC AGENTS
Pentostatin (nipent)
Mech of action:

Back 58

Pentostatin is stucturally similar to a component of DNA that is necessary for DNA synthesis. Thus, it interferes with DNA synthesis. It is cell specific… antimetabolite drug.

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CANCER CHEMOTHERAPEUTIC AGENTS
Pentostatin (nipent)
Therapeutic:

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treatment of patients with active hairy cell leukemia who have not received previous treatment or who have not responded to treatment with alpha interferons.

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CANCER CHEMOTHERAPEUTIC AGENTS
Pentostatin (nipent)
Contraindiaction

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Not recommended for combination therapy with other drugs

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CANCER CHEMOTHERAPEUTIC AGENTS
Pentostatin (nipent)
Adverse Effects:

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may worsen gout; myelosuppression. May also cause severe allergic reaciont rash or hives to anaphylaxis… may cause secondary malignancies.. Infertility

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CANCER CHEMOTHERAPEUTIC AGENTS
Pentostatin (nipent)
Contrindications:

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should not be used in combination with fludarabine, as extedme pulmonary toxicity may occur… concurrent administtarion of allopurinal, colchicine, or probenecid for pre-existing gout; pentostatin may increase serum uric acid, due to rapid cell lysis.; Concurrent administraion of agents that suppress bone marrow (e.g carabamazepine, felbamate, alkylating chemotherapy agents) Concurrent radiation therapy-bone marrow suppression may occur.; Pentostatin is cleared by the kidney, so dosage should be reduced in patients without adeuate renal function.

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CANCER CHEMOTHERAPEUTIC AGENTS
Taxanes
List all drugs:

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A. Docetaxel (taxotere)
B. paclitaxel (taxol, paxtene, onxol)

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CANCER CHEMOTHERAPEUTIC AGENTS
Taxanes
Docetaxel (taxotere)
Mech of action:

Back 64

Docetaxel affects the formation of the cellular spindle “anchors” (centrosomes) in S phase, resulting in lack of mitotic spindle integrity The drug also has limited effects on cells in the M phase (metaphase)

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CANCER CHEMOTHERAPEUTIC AGENTS
Taxanes
Docetaxel (taxotere)
Uses:

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therapy of breast and lung cancers

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CANCER CHEMOTHERAPEUTIC AGENTS
Taxanes
Docetaxel (taxotere)
Contraindications:

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should not be administered to patients with insufficient lever funcion

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CANCER CHEMOTHERAPEUTIC AGENTS
Taxanes
paclitaxel (taxol, paxtene, onxol)
Mechanism of action:

Back 67

affects the formation of mitotic spindles, resulting in inhibition of mitosis. It stabilizes micrtubules, so that the normal assembly/dissassembly procedure required for cellular transportation and mitosis cannot take place. In addition, it promotes aggregation of microtubules into bundles, rendering them nonfunctional.

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CANCER CHEMOTHERAPEUTIC AGENTS
Taxanes
Uses:
paclitaxel (taxol, paxtene, onxol)

Back 68

Breast cancer; may also be used for no-small cell lung cancer; second line agent for the treatment of AIDS-related Karposi’s sarcoma.

Front 69

CANCER CHEMOTHERAPEUTIC AGENTS
Taxanes
paclitaxel (taxol, paxtene, onxol)
Caution:

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Premedication with desamethazone is required to prevent possible hypersensitivity reacions; Cytotoxicity of the drug correlates with total dosage, rather than prolonged exposure, making the drug virtually schedule independent.

Front 70

CANCER CHEMOTHERAPEUTIC AGENTS
Taxanes
paclitaxel (taxol, paxtene, onxol)
Adverse effects:

Back 70

Hematologic toxicity- bone marrow suppresion, thrombocytopenia; increased susceptibility to infection,fever; edema; skin toxicity- rash /hies on feet and hands; change in pigmentation of nails; Inflammation of the mouth; cardiovascular effects, particularly hypotenson; febrile neutropenia; confusion, seizures; pulmonary edema, repiratory distress, interstitial pneumonina

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CANCER CHEMOTHERAPEUTIC AGENTS
Taxanes
Drug interaction:
paclitaxel (taxol, paxtene, onxol)

Back 71

Drug interactions may occur with medications metabolized by the cytochrome P450 system- specifically cytochrome P450. These include major macrolide antibiotics, cerain antifungal drugs, and others

Front 72

CANCER CHEMOTHERAPEUTIC AGENTS
Taxanes
paclitaxel (taxol, paxtene, onxol)
Contraindiaction:

Back 72

Severe hypersensitivity reactions occure in about 2% of patients and may be fatal. Patients who experience hypersensitivity reaciont should be taken off of the drug and not be reinstuited. Patients with neutrophil counts < 1,500 celll/mm3 should not have taxane therapy, due to myelosuppressant effects. For patients with AIDS, this limitation drops to 1000/mm#

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CANCER CHEMOTHERAPEUTIC AGENTS
Taxanes
paclitaxel (taxol, paxtene, onxol)
Resistance:

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“multidrug resistance” due to alterations in cellular drug efflux pump.; Alterations in the alpha and the beta-tubulin subunits which decrease the rate of polymerization int omicrotubules.

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CANCER CHEMOTHERAPEUTIC AGENTS
Topoisomerase inhibitors
Mech of action:

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etoposide and teniposide are inhibitors of topoisomeraseII. Unlike the anthracyclines, these drugs do not bind directly to the enzyme, but stabilze the compex formed by the enzyme and DNA. When DNA and topoisomerase II are bound together, and can no longer dissociate, both are inactivated and further progression in the cell cycle is halted. DNA strand breaks develop, and the cell dies. These drugs are cell cycle specific.

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CANCER CHEMOTHERAPEUTIC AGENTS
Topoisomerase inhibitors
List all drugs:

Back 75

A.etoposide (vepacid, toposar, etopophos (etoposide phosphate)
B. teniposide (vumon)

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CANCER CHEMOTHERAPEUTIC AGENTS
Topoisomerase inhibitors
Topoisoetoposide (vepacid, toposar, etopophos (etoposide phosphate)merase inhibitors
Uses:

Back 76

refractory testicular tumors and small cell lung cancer.

Front 77

CANCER CHEMOTHERAPEUTIC AGENTS
Topoisomerase inhibitors
etoposide (vepacid, toposar, etopophos (etoposide phosphate)
Adverse effects:

Back 77

Bone marrow suppression. White cell count is lowest around two weeks into therapy. Recovery form suppression may occur as early as three weeks post therapy.; Nausea and vomiting; Changes in blood pressure (hypertensive of hypotensive episodes).; Allergic reaction, including anaphylaxis, particularly during initial infusion. Alopecia….. Infrequent andverse effects, such as GI distress, abdominal pain, stevens Johnson syndrome, cortical blindness, and hepatotoxicity.

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CANCER CHEMOTHERAPEUTIC AGENTS
Topoisomerase inhibitors
etoposide (vepacid, toposar, etopophos (etoposide phosphate)
Contraindications:

Back 78

concurrent use of Levimasole, cyclsporin

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CANCER CHEMOTHERAPEUTIC AGENTS
Topoisomerase inhibitors
Mech of action:
teniposide (vumon)

Back 79

Teniposide is a phase specific cytotoxic drug, acting in the late S or early G2 phase of the cell cycle. It causes dose-dependant single and double stranded breaks in DNA and RNA; protein crosslinking of DNA strands also occurs

Front 80

CANCER CHEMOTHERAPEUTIC AGENTS
Topoisomerase inhibitors
teniposide (vumon)
Dosage:

Back 80

250 mg/m2 weekly ofr four to eight weeks, in combo with vincristine and prednisone. Teniposide is administered intravenously, and should be dipensed from a nonreacive glass IV bottle or polyolefin bag to prevent extraction of plastic components.

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CANCER CHEMOTHERAPEUTIC AGENTS
Topoisomerase inhibitors
teniposide (vumon)
Uses:

Back 81

Used as initaial (inductions) thearpy of acute lymphoblastic leukemia in children

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CANCER CHEMOTHERAPEUTIC AGENTS
Topoisomerase inhibitors
teniposide (vumon)
Adverse effects:

Back 82

Severe myelosuppresion with delayed recovery; nausea and vomiting; alopecia; hypersensitivity reacions; CNS depesion, particularly with prior administarion of phenothiazine type antiemetics ( e.g. compazine); hypotension

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CANCER CHEMOTHERAPEUTIC AGENTS
Topoisomerase inhibitors
teniposide (vumon)
Contraindications:

Back 83

hepatic insufficiency… concurrent therapy with drugs that depress the central nervous system ( e.g antihistamines, sedative-hypnotic drugs, anti convulant drugs, narcotics); concurrent therapy with drugs that are highly plasma protein bound (e.g warfarin, carbeamezepine, benzodiazepines)

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CANCER CHEMOTHERAPEUTIC AGENTS
Camptothectins
Mech of action:

Back 84

The camptothectins, topotecan and irinotecan, are inhibitors of the enzyme topoisomerase I which regulates the uncoiling of DNA prior to replication. They are highly cell-cycle specific, and cause defects in DNA repair, resulting in strand breakage. RNA is also affected.

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CANCER CHEMOTHERAPEUTIC AGENTS
Camptothectins
List drug:

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topotecan( hycamtin)

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CANCER CHEMOTHERAPEUTIC AGENTS
Camptothectins
topotecan( hycamtin)
Used

Back 86

a second line therapy for carcinoma of the ovary and small cell lung cancer

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CANCER CHEMOTHERAPEUTIC AGENTS
Camptothectins
topotecan( hycamtin)
Adverse effects:

Back 87

Nausea and vomiting are most frequent; toal alopecia, including body hair; mild hepatotoxicity; thrombocytopenia (rare) dermatitis (rare)

Front 88

CANCER CHEMOTHERAPEUTIC AGENTS
Camptothectins
topotecan( hycamtin)
Contraindications:

Back 88

Bone marrow depression may be severe, if given in conjunction with cisplatin; Interactions with other medications have not fully been elucidated

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Antibiotic Chemotherapeutic Agents
List drug

Back 89

Bleomycin (bleo, bleocin, blenoxane)

Front 90

Antibiotic Chemotherapeutic Agents
Bleomycin (bleo, bleocin, blenoxane)
Mech of action:

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Bleomycin is an older drug that is relatively cell cycle specific (G2 and M phases). Initially, the DNA forms a complex with iron and oxygen, in the presence of DNA. This stabilizes the molecule by complexing it. This complex then binds to DNA.

The binding of the bleomycin complew to DNA occurs at certain nucleotide sequences via electrostatic interactions and partial intercalation of bleomycin into the DNA molecule. In addition to stabilizing the molecule, the bleomycin complex causes single and double strand breaks.

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Antibiotic Chemotherapeutic Agents
Bleomycin (bleo, bleocin, blenoxane)
Uses:

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Bleomycin is considered palliative treatment for Hodgkin’s and non hodgkin’s lymphoma, testicular carcinoma, and squamous cell carcinomas of the head and neck.; Used in the therapy of squamous cell carcinoma, testicular carcinoma, and lymphomas

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Antibiotic Chemotherapeutic Agents
Bleomycin (bleo, bleocin, blenoxane)
Adverse effects:

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Pulmonary toxicity is seen… This presents initially as pneumontitis, which progresses to pulmonary fibrosis. Post-therapy, bleomycin can make the adverse pulmonary effects due to oxygen administration worse. Rash and occasional vascular toxcities may be seen.

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CANCER CHEMOTHERAPEUTIC AGENTS
Anthracycline antibiotics
Mech of action:

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Anthracyclines intercalate between base pairs in DNA, causing the helix to change shape, which interferes with strand elongation. They are cell cycle non-specific

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CHEMOTHERAPEUTIC AGENTS
Anthracycline antibiotics
List all drugs:

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A. doxorubicin [adriamycin]
B. doxorubicin HCI (liposomal injection)
C. doxorubicin (adriamyicn, adriamycin PF, rubex)
D. Dactinomycin (cosmegen, (actinomycin-d)
E. Daunorubicin HCI (cerubidine, daunoxome (daunorubicin citrate-liposomal formulation)
F. idarubicin (idamycin)

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CHEMOTHERAPEUTIC AGENTS
Anthracycline antibiotics
doxorubicin [adriamycin]
Uses:

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metastatic cancer of the ovary, which has been shouwn to be refractory to therapy with platins or paclitaxel. Also used in refractory cases of AIDS-Related Karposi’s sarcoma.

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CHEMOTHERAPEUTIC AGENTS
Anthracycline antibiotics
doxorubicin [adriamycin]
Form:

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Doxorubicin is best administered as a liposomal formulation in which the drug is encapsulated in lipid particles that are targeted to tumor cell membranes and more easily assimilated by neoplastic cells. Encapsulation also decreases irritation produced by direct contact of the drug with tissues, and isolateds it from water-based compartments and tissues.

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CHEMOTHERAPEUTIC AGENTS
Anthracycline antibiotics
doxorubicin HCI (liposomal injection)
Uses:

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in the therapy of metastatic carcinoma of the ovary and Karposi’s sarcoma

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CHEMOTHERAPEUTIC AGENTS
Anthracycline antibiotics
doxorubicin (adriamyicn, adriamycin PF, rubex)
Adverse:

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the dose limiting adverse effect of doxorubicin is cardiotocictiy, including congestive heart failure. Other adverse effects include; Bone marrow depression; hand and foot syndrome; dry mouth; nausea and vomiting

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CHEMOTHERAPEUTIC AGENTS
Anthracycline antibiotics
doxorubicin (adriamyicn, adriamycin PF, rubex)
Contraindications:

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doxorubicin should be used with caution in the elderly and patients with compromised heart function

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CHEMOTHERAPEUTIC AGENTS
Anthracycline antibiotics
Dactinomycin (cosmegen, (actinomycin-d)
Uses:

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useful as part of a combo drug regimen in the treatment of wilm’s tumor, childhood rhabdomyosarcoma, ewing’s sarcoma, gestational trophoblastic neoplasia, and non seminiferous metastatic testicular cancer (in combo regimen with cyclophosphamide, bleomycin, vinblastine, and cispatin)

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CHEMOTHERAPEUTIC AGENTS
Anthracycline antibiotics
Dactinomycin (cosmegen, (actinomycin-d)
Contraindications:

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Cardiac failure or cardiac dysfunction; concurrent mediacations that may have negative inotropic actions (e.g., phenytoin, carbamazepine, muscarinic agents, beta receptor blockers etc). Previous courses with daunorubicin or doxorubicin may increase cardiotoxicity.

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CHEMOTHERAPEUTIC AGENTS
Anthracycline antibiotics
Dactinomycin (cosmegen, (actinomycin-d)
Adverse effects:

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Bone marrow derpression; liver toxicity (including hepatomegaly, hepatitis, and ascites); cardiotoxicitys; lung toxicity (pneumonitis); corrosion of soft tissue with extravasation at the injection site; GI and mouth ulceration: alopecian, skin rashes, and emesis

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CHEMOTHERAPEUTIC AGENTS
Anthracycline antibiotics
Daunorubicin HCI (cerubidine, daunoxome (daunorubicin citrate-liposomal formulation)
Uses:

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indicated for treatment of remission in leukemic disorders _AML (adults) and ALL (children and adults): used in the therapy on non lymphocytic leukemia, in combo with cytosine arabinoside

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CHEMOTHERAPEUTIC AGENTS
Anthracycline antibiotics
Daunorubicin HCI (cerubidine, daunoxome (daunorubicin citrate-liposomal formulation)
Adverse effects:

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Dose-limiting toxicity includes myelosuppression and cardiotoxicity (the cardiotoxicity of daunorubicin is decreased as compared with doxorubicin). Thrombophlebitis and/or tissue necrosis at the injection site; Alopecia. Nausea and vomiting; hyperuricemia (espectially in patients with leukimia) Fever and Chills and rarely anaphlaxis

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CHEMOTHERAPEUTIC AGENTS
Anthracycline antibiotics
idarubicin (idamycin)
Analougous of

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Daunorubicin HCI

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Drugs used in combo w/ cancer chemotherapy
Drugs used in the therapy of bone marrow suppression
List all drugs:

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Epoetin alfa (epogen, procrit)

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Drugs used in combo w/ cancer chemotherapy
Drugs used in the therapy of bone marrow suppression
Epoetin alfa (epogen, procrit)
Mech of action

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effective against red blood cell loss

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Drugs used in combo w/ cancer chemotherapy
Drugs used in the therapy of bone marrow suppression
Epoetin alfa (epogen, procrit)
Adverse effects:

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Bone marrow suppression and nausea/vomiting.

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Drugs used in combo w/ cancer chemotherapy
Drugs used in the therapy of bone marrow suppression
Epoetin alfa (epogen, procrit)
Uses:

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for patients with bone marrow suppression

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Drugs used in combo w/ cancer chemotherapy
drugs used in the therapy of emesis
List all drugs:

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1. Metoclopramide HCI (reglan)
2. Prochlorperazine maleate (compazine spansules (sustained realease form)
3. Prochlorperazine edisylate (compazine)

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Drugs used in combo w/ cancer chemotherapy
drugs used in the therapy of emesis
Metoclopramide HCI (reglan)
Mech of action:

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antagonizes dopamine

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Drugs used in combo w/ cancer chemotherapy
drugs used in the therapy of emesis
Metoclopramide HCI (reglan)
Uses:

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therapy of nausea and vomiting

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Drugs used in combo w/ cancer chemotherapy
drugs used in the therapy of emesis
Prochlorperazine maleate (compazine spansules (sustained realease form)
Uses:

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nausea and vomiting