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ANTINEOPLASTIC

Drug Class and Examples                        Mechanism of Action         Cell Cycle Specificity          Common Side Effects
Alkylting Agents

 Busulfan (Busulfex.Myleran), carboplatin      Alter DNA structure by      Cell cycle-nonspecific          Bone marrow
(Paraplatin), chlorambucil (Leukeran)          misreading DNA code,                                        suppression, nausea,
,cisplatin (Platinol,AQ), cylophos- phamide    intiating breaks in the                                     vomiting, cystitis
(Cytoxan),dacarbazine        (DTIC,            DNA molecule,cross-                                         (cyclophosphamide;
Dome),hexamethylene amine          or          linkin DNA strands                                          ifosfamide), stomatitics,
altertamine (Hexalen)                                                                                      alopecia, gonabal
,ifosfamide(Ifex),melphalan (Alkeran),                                                                     suppression, renal
nitrogen mustard (Mustargen),                                                                              toxicity (cisplatin)
oxaliplation(Eloxatin), thiotepa (Thioplex)

Nitrosoureas                                   Similar to the alkylating   Cell cycle-nonspecific          Delayed and cumulative
Carmustine(BCNU[BiCNU,Gliadel]),               agents; cross the blood-                                    myelosuppression,
lomustine or CCNU (CeeNU), semustine           brain barrier                                               especially
(methyl CCNU[ MeCCNU]),streptozocin                                                                        thrombocytopenia;nausea
(Zanosar)                                                                                                  vomiting

Topoisomerase I Inhibitors Irinotecan          Induce breaks in the        Cell cycle-specific (S phase)   Bone marrow
(Camprosar) Topotecan (Hycamtin)               DNA strand by binding                                       suppression, diarrhea,
                                               to enzyme                                                   nausea,vomiting ,
                                               topoisomerase I,                                            hepatotoxicity
                                               preventing cells from
                                               dividing
Antimetabolites
5-Azacytadine, capecitabine (Xeloda),          Interferes with the     Cell Cycle–specific (Sparse)        Nausea, vomiting,
cytarabine (DepoCyt, Tarabine),edatrexate      biosynthesis of                                             diarrhea, bone marrow
fludarabine (flurada), 5-fluorouracil (5-      metabolites or nucleic                                      suppression, proctitics,
FU),gemcitabine (Gemzar), hydroxyurea          acids necessary for RNA                                     stomatitis, renal toxicity
(Droxia, Hydrea),cladribine (Leustatin), 6-    and DNA synthesis                                           (methotrexate),
mercaptopurine (Purinethol), mercaptopurine                                                                hepatotoxicity
(Trexall, Rheumarrex), pentostatin (Nipent),
6-thioguanine (Tabloid)

Antitumor Antibiotics                          Interfere with DNA          Cell cycle-nonspecific          Bone marrow
Bleomycin (BLM, Blenoxane), dactinomycin       synthesis by biding                                         suppression nausea,
(Cosmegen), daunorubicin(DaunoXome),           DNA; prevent RNA                                            vomiting alopecia,
doxorubicin (Adriamycin),                      synthesis                                                   anorexia, cardiac toxicity
idarubicin(Idamycin), mitomycin                                                                            (daumorubicin,
(Mutamycin), mitoxantrone (Novantrone),                                                                    doxorubicin)
plicamyin (Mithracin)
                                                                                                           Bone marrow
Mitotic Spindle Poisons                        Arrest metaphase by        Cell cycle-specific (M phase)    suppression (mild with
Plant Alkaloids: etoposide (Toposar),          inhibiting mitotic tubular                                  VCR), neuropathies
teniposide (Vumon)vinblastine (Velban),        formation (spindle);                                        (VCR), stomatitis
vincristine (VCR[Oncovin]), vindesine          inhibit DNA and protein
(Eldisine),vinorelbine (Navelbine)             synthesis                                                   Bradcardia,
Taxanes: paclitaxel (Taxol), docetaxel         Arrest metaphase by        Cell cycle-specific (M phase)    hypersensitivity
(Taxotere)                                     inhibiting tubulin                                          reactions, bone marrow
                                               depolymerization                                            suppression, alopecia
                                                                                                           neuropathics

Hormonal Agents                                Bind to hormone            Cell cycle-nonspecific           Hypercalcemia, jaundice,
Androgens and antiandrogens, estrogens and     receptors sites that alter                                  increased appetite,
antiestrogens, progestins and antiprogestin,   cellular growth; block                                      masculinization,
aromatase inhibitors, luteinizing hormone-     binding of estrogens to                                     feminization, sodium and
releasing hormone analogues, steroids          receptors sites                                             fluid rerention, nausea,
                                               (antiestrogen); inhibit                                     vomiting hot
                                               RNA synthesis; suppress                                     flashes,vaginal estrogen
                                               aromarase of P450                                           dryness
                                               system, which decreases
                                               level

Miscellaneous Agents                           Unknown or too              Varies                          Anorexia, nausea
Asparaginase (Elspar), procarbazine            complex to categorize                                       vomiting bone marrow
(Matulane)                                                                                                 suppression
                                                                                                           hepatotoxicity,
                                                                                                           anaphylaxis,
                                                                                                           hypotension, altered
                                                                                                           glucose metabolism
Antineoplastic

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Antineoplastic

  • 1. ANTINEOPLASTIC Drug Class and Examples Mechanism of Action Cell Cycle Specificity Common Side Effects Alkylting Agents Busulfan (Busulfex.Myleran), carboplatin Alter DNA structure by Cell cycle-nonspecific Bone marrow (Paraplatin), chlorambucil (Leukeran) misreading DNA code, suppression, nausea, ,cisplatin (Platinol,AQ), cylophos- phamide intiating breaks in the vomiting, cystitis (Cytoxan),dacarbazine (DTIC, DNA molecule,cross- (cyclophosphamide; Dome),hexamethylene amine or linkin DNA strands ifosfamide), stomatitics, altertamine (Hexalen) alopecia, gonabal ,ifosfamide(Ifex),melphalan (Alkeran), suppression, renal nitrogen mustard (Mustargen), toxicity (cisplatin) oxaliplation(Eloxatin), thiotepa (Thioplex) Nitrosoureas Similar to the alkylating Cell cycle-nonspecific Delayed and cumulative Carmustine(BCNU[BiCNU,Gliadel]), agents; cross the blood- myelosuppression, lomustine or CCNU (CeeNU), semustine brain barrier especially (methyl CCNU[ MeCCNU]),streptozocin thrombocytopenia;nausea (Zanosar) vomiting Topoisomerase I Inhibitors Irinotecan Induce breaks in the Cell cycle-specific (S phase) Bone marrow (Camprosar) Topotecan (Hycamtin) DNA strand by binding suppression, diarrhea, to enzyme nausea,vomiting , topoisomerase I, hepatotoxicity preventing cells from dividing Antimetabolites 5-Azacytadine, capecitabine (Xeloda), Interferes with the Cell Cycle–specific (Sparse) Nausea, vomiting, cytarabine (DepoCyt, Tarabine),edatrexate biosynthesis of diarrhea, bone marrow fludarabine (flurada), 5-fluorouracil (5- metabolites or nucleic suppression, proctitics, FU),gemcitabine (Gemzar), hydroxyurea acids necessary for RNA stomatitis, renal toxicity (Droxia, Hydrea),cladribine (Leustatin), 6- and DNA synthesis (methotrexate), mercaptopurine (Purinethol), mercaptopurine hepatotoxicity (Trexall, Rheumarrex), pentostatin (Nipent), 6-thioguanine (Tabloid) Antitumor Antibiotics Interfere with DNA Cell cycle-nonspecific Bone marrow Bleomycin (BLM, Blenoxane), dactinomycin synthesis by biding suppression nausea, (Cosmegen), daunorubicin(DaunoXome), DNA; prevent RNA vomiting alopecia, doxorubicin (Adriamycin), synthesis anorexia, cardiac toxicity idarubicin(Idamycin), mitomycin (daumorubicin, (Mutamycin), mitoxantrone (Novantrone), doxorubicin) plicamyin (Mithracin) Bone marrow Mitotic Spindle Poisons Arrest metaphase by Cell cycle-specific (M phase) suppression (mild with Plant Alkaloids: etoposide (Toposar), inhibiting mitotic tubular VCR), neuropathies teniposide (Vumon)vinblastine (Velban), formation (spindle); (VCR), stomatitis vincristine (VCR[Oncovin]), vindesine inhibit DNA and protein (Eldisine),vinorelbine (Navelbine) synthesis Bradcardia, Taxanes: paclitaxel (Taxol), docetaxel Arrest metaphase by Cell cycle-specific (M phase) hypersensitivity (Taxotere) inhibiting tubulin reactions, bone marrow depolymerization suppression, alopecia neuropathics Hormonal Agents Bind to hormone Cell cycle-nonspecific Hypercalcemia, jaundice, Androgens and antiandrogens, estrogens and receptors sites that alter increased appetite, antiestrogens, progestins and antiprogestin, cellular growth; block masculinization, aromatase inhibitors, luteinizing hormone- binding of estrogens to feminization, sodium and releasing hormone analogues, steroids receptors sites fluid rerention, nausea, (antiestrogen); inhibit vomiting hot RNA synthesis; suppress flashes,vaginal estrogen aromarase of P450 dryness system, which decreases level Miscellaneous Agents Unknown or too Varies Anorexia, nausea Asparaginase (Elspar), procarbazine complex to categorize vomiting bone marrow (Matulane) suppression hepatotoxicity, anaphylaxis, hypotension, altered glucose metabolism