抗肿瘤药(英文版课件

Click to edit Master title style,Click to edit Master text styles,Second level,Third level,Fourth level,Fifth level,*,单击此处编辑母版标题样式,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,*,单击此处编辑母版标题样式,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,*,抗肿瘤药(英文版）,抗肿瘤药(英文版）,1,“CANCER”,Refers to a Malignant neoplasm (New growth),Cancer cells can manifest:,Uncontrolled Proliferation.,Loss of function due to lack of ability to differentiate.,Invasiveness.,The ability to metastasize.,Cancer arises as a result of a series of genetic changes,in the cell, the main genetic lesions being:,Inactivation of tumor suppressor genes.,The activation of oncogenes.,“CANCER”,2,抗肿瘤药(英文版课件,3,抗肿瘤药(英文版课件,4,抗肿瘤药(英文版课件,5,抗肿瘤药(英文版课件,6,抗肿瘤药(英文版课件,7,抗肿瘤药(英文版课件,8,ANTINEOPLASTIC AGENTS,DEFINITIONS:,ALKYLATION,- chemical reaction that cleaves DNA and,interferes with mitosis,BIFUNCTIONAL ALKYLATING AGENTS,- have 2 alkyl groups,and alkalate 2 DNA strands,DOSE-LIMITED SIDE EFFECTS,- adverse effects that prevent an agent from being given in higher doses,EMETIC POTENTIAL,- potential of an agent to cause N & V,ANTINEOPLASTIC AGENTS,9,ANTINEOPLASTIC AGENTS,ADVERSE EFFECTS:,Kills all fast growing cells,Hair follicles,GI tract mucosa,Bone marrow suppression (BMS) causing anemiaand leukopenia,All are pregnancy category D !,Most are nephro- hepato- and ototoxic,Extravasation of IV can result in loss of limb,ANTINEOPLASTIC AGENTS,10,Antineoplastic Agents,ADVERSE EFFECTS: (Contd),All have a BMS and emetic index,All have wide interaction with other drugs.,Special training required for nursing,Most agents can be harmful to nurse administering them,Antineoplastic Agents,11,DEFINITIONS:,GROWTH FRACTION,% of cells in mitosis at any given time,LEUCOVORIN RESCUE,-,use of leucovorin to reverse methotrexate-induced toxicity,MITOTIC INDEX,number of cells per unit undergoing mitosis during a given time,NADIR,lowest point (as in blood count) after being depressed by chemotherapy,PARANEOPLASTIC SYNDROME (PNS),S/S of cancer located distant from tumor or its metastatic sites,DEFINITIONS:,12,ANTINEOPLASTIC AGENTS,2 MAIN GROUPS OF AGENTS:,CELL CYCLE - NONSPECIFIC (CCNS,),ALKYLATING AGENTS,cytotoxic in any phase of cell cycle,effective against slowly growing tumors,CELL CYCLE - SPECIFIC (CCS),3 TYPES,ANTIMETABOLITES,- cytotoxic is S phase,MITOTIC INHIBITORS,- cytotoxic in M phase,CYTOTOXIC ANTIBIOTICS,(some are CCNS),effective against rapidly growing tumors,ANTINEOPLASTIC AGENTS,13,ALKYLATING AGENTS,NITROGEN MUSTARDS,first developed in 1940s,CCNS killing ability,mechlorethamine,is the prototypical agent,USES: Hodgkins disease & lymphomas.,leukemias,CANCERS OF,lung,breast,ovary,testes,brain,bladder,Most widely used agent, often in combination with other agents.,ALKYLATING AGENTS,14,ALKYLATING AGENTS,SELECTED AGENTS:,Mechlorethamine,(Mustine, Mustargen),IV only (adult use only),Cyclophosphamide,(Cytoxan, Neosar),IV and PO, adults and pediatric use,Carmustine,(BiCNU),IV, adult only, can cross blood-brain barrier,therefore used to tread brain lesions,OTHER AGENTS: Chlorambucil, Streptozotocin,ALKYLATING AGENTS,15,Hepatic cytochrome,P,450,0xidase,4-Hydroxycyclophosphamide Aldophosphamide,Enzymatic,Non enzymatic,Hepatic aldehyde oxidase,4-Ketocyclophosphamide,(Inactive).,Acrolein Cytotoxic Phosphamide Mustard,Cytotoxic.,Carboxyphosphamide (Inactive).,Responsible for unwanted effects,Cyclophosphamide (Inactive),16,Cyclophosphamide (Inactive,),Hepatic cytochrome,P,450,0xidase,4-Hydroxycyclophosphamide,Aldophosphamide,Enzymatic,Non enzymatic,Hepatic aldehyde oxidase,4-Ketocyclophosphamide,(Inactive).,Acrolein Cytotoxic Phosphamide Mustard,Cytotoxic,Carboxyphosphamide (Inactive).,Responsible for unwanted effects,17,ANTIMETABOLITES,ACTIONS:,Antagonism of folate,purines, and pyrimidines needed for synthesis of nucleic acids -,stops cell replication,USES:,Solid tumors,(breast, lung, liver, brain, colon. Stomach, pancreas),Lymphomas, leukemias.,Some agents also immunosuppressive,Useful in treating immune-mediated diseases,ANTIMETABOLITES,18,ANTIMETABOLITES,SELECTED AGENTS:,(FOLIC ACID ANALOG),METHOTREXATE,(Folex, Rheumatrex, MTx),Folic acid antagonist,PO & IM, adult and pediatric use,Also used to treat immune-mediated diseases,Used incombination with misoprostol for therapeutic abortion,Causes profound anemia (folate depletion),Therefore leucovorin “rescue” often used to counteract,ANTIMETABOLITES,19,ANTIMETABOLITES,SELECTED AGENTS:,PURINE ANALOG,- MERCAPTOPURINE,(6-MP, Purinethol),- Purine antagonist,- PO only, adult and pediatric use,PYRIMIDINE ANALOG,-,CYTARABINE,(Ara-C, Cytosar-U),-Pyrimidine antagonist,-IV and intrathecal (within spinal canal),ANTIMETABOLITES,20,MITOTIC INHIBITORS,ACTIONS:,Plant alkaloids (periwinkle, yew tree, mandrake plant, etc.),Bind to and disrupt mitotic spindles,USES:,Lymphomas (Hodgkins and non-Hodgkins),Neuroblastoma,Kaposis sarcoma,Solid tumors (breast, testicular, etc.),MITOTIC INHIBITORS,21,MITOTIC INHIBITORS,SELECTED AGENTS:,ETOPOSIDE,(VP-16, VePesid),IV and PO, adult use only,PACLITAZEL,(Taxol),IV only, adult use only,drug of choice for ovary and breast ca,VINCRISTINE,(LCR, VCR,Oncovin),IV only, adult and pediatric use,drug of choice for acute leukemia,MITOTIC INHIBITORS,22,CYTOTOXIC ANTIBIOTICS,ACTIONS:,Source: Streptomyces mold - work by intercalation (insertion of drug molecule between the 2 DNA strands causing it to (“unwind”),Kill some bacteria and viruses but are too toxic to use for,infections,IV extravasation constant danger !,USES:,wide variety of solid tumors, always used in combination with other agents,CYTOTOXIC ANTIBIOTICS,23,CYTOTOXIC ANTIBIOTICS,SELECTED AGENTS:,DOXORUBICIN,(ADR, Rubex, Doxil),IV only, adult use only,BLEOMYCIN,(BLM, Blenoxane),IM, IV, SQ, adult use only,very toxic agents !,CYTOTOXIC ANTIBIOTICS,24,MISCELLANEOUS ANTINEOPLASTICS,Various actions,Both CCNS and CCS,Used in combinations with other agents,SELECTED AGENTS:,Cisplatin,(Platinol),IV, adult and pediatric use,ALTRETAMINE,(Hexalen),PO only, adult use only, primarily used to treat ovarian cancer,ASPARAGINASE,(Elspar),IV only, adult and pediatric use,HYDROXYUREA,(Hydrea),PO only, adult use only,MISCELLANEOUS ANTINEOPLASTICS,25,MISCELLANEOUS ANTINEOPLASTICS,HORMONES AND ANTAGONISTS.,1. Adrenocortical Suppressant:,Mitotane, Aminoglutethimide.,(Adrenal Cortex),2.Adrenocortical Steroids.,Prednisone.,(Lukemias, Lymphomas, Breast),3.Progestins,.,Hydroxyprogestrone.(Endometrium,(Breast),Medroprogestrone, Megesterol acetate.,4.Estrogens,.,DES, Ethinylesterdiol,.(Breast, Prostate),5.Antiestrogens,.,Tamoxifen,.(Breast),6.Androgens,.,Testosterone,(Breast),7,.,Antiandrogens.,Flutamide,(Prostate).,8.Gonadotropin Releasing Hormone Analog.,Leuprolide.,(Prostate),MISCELLANEOUS ANTINEOPLASTICS,26,结束语,谢谢大家聆听！,27,结束语谢谢大家聆听！27,