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AnticancerDrugSectionIBasicPharmacologyofAnticancerDrug1.Classification1(1)AccordingtochemicalconstitutionandresourceAlkylatingagentAntimetabolitesAntibioticsPlant-derivedproductsHormonalagent2Alkylatingagent

Cyclophosphamide

MechlorethamineMelphalanChlorambucil

3AntimetabolitesFolicacidanalogue:methotrexatePyrimidines:fluorouracil,cytarabinePurines:thioguanine,mercaptopurine4AntibioticsAnthracyclinesDactinomycinBleomycinMitomycin5Plant-derivedproductsVincaalkaloidsEtoposidesTaxanes

6HormoneantagonistsHormoneagonistsHormonalagent7（2）AccordingtobiochemistrymechanismsofantitumoreffectAgentsaffectingbiosynthesisofnucleicacidAgentsaffectingstructureandfunctionofDNAAgentsaffectingtranscription

processandinterruptingsynthesisofRNAAgentsinterferingwiththeformationandfunctionofproteins.Agentsaffectinghormonehomeostasis82.Mechanismofpharmacologicaction（1）Cellbiologymechanismsofantitumoreffect（2）Biochemistrymechanismsofantitumoreffect9（1）CellbiologymechanismofantitumoreffectCellCycle-Nonspecific(CCNS)Agents:

Alkylatingagent,Antibiotics,

PlatinumantitumorcompoundCellCycle-Specific(CCS)Agents:

Methotrexate:Sphase

Vincaalkaloid:Mphase10（2）BiochemistrymechanismsofantitumoreffectAffectingbiosynthesisofnucleicacidDihydrofolate

ReductaseInhibitor：Methotrexatesynthesisoftetrahydrofolate

synthesisofthymidylate,purinenucleotidesformationofDNA,RNA11b)PyrimidineAntagonists：Fluorouracildeoxythymidylate

synthetase

deoxyuridylicaciddeoxythymidylicacidDNAsynthesis12C)PurineAntagonists：6-thioinosinicacidHGPRTMercaptopurinepurinenucleotideinterconversion13d)Ribonucleotide

ReductaseInhibitor:Hydroxyurea

cytidylicaciddeoxycytidylicacidDNAsynthesis14e)DNAPolymeraseInhibitor：Cytarabine(ara-C)5'-mononucleotide(AraCMP)triphosphate(AraCTP)

DNApolymeraseDNAsynthesis15DNACross-linkageagent:alkylatingagentsPlatinumantitumorcompound:Cisplatin

Antibiotics:Bleomycin

Topoismeraseinhibitor:camptothecins

AffectingstructureandfunctionofDNA16Affectingtranscription

processandinterruptingsynthesisofRNAAnthracyclinDactinomycin17d.InterferingwiththeformationandfunctionofproteinsMicrotubuleinhibitors:Vincaalkaloidtubulinpolymerizationextensionofmicrotubules

terminationofmitoticdivision18b)AgentinfluenceaminoacidsupplyAsparaginase

L-asparagine

asparticacid

proteinsynthesis19AffectinghormonehomeostasisEstrogensandantiestrogenAndrogensandantiandrogenProgestogensglucocorticoid

201.ResistanceInherentlyresistantAcquiredresistanceMultidrugResistanceSectionII

Problemsassociatedwithchemotherapy21MultidrugResistanceTumorcellsmaybecomegenerallyresistanttoavarietyofcytotoxicdrugsonthebasisofdecreaseduptakeorretentionofthedrugsP-glycoprotein

22(1)shorttermtoxicity

Commonadverseeffects:

BoneMarrowToxicity:hormone,Bleomycin,asparaginase

(b)GastrointestinalTractToxicity(c)HairFollicleToxicity2.Toxicity23

Uncommonadverseeffects:(a)Pulmonarytoxicity:Bleomycin(b)Hepatotoxicity：L-Asparaginase

、Cyclophosphamide

(c)Renaltoxicity：Cyclophosphamide(d)Neurotoxicity：Vincristine、Cisplatin

(e)Allergicresponse：L-Asparaginase、Bleomycin、Paclitaxel

24(2)LongtermtoxicityTreatment-inducedtumorsInfertilityanddeformability25Thankyou！26TestWhatismechanismofantimicrobialactionandcorrespondingantimicrobialagents?Whatisthemechanismofbacterialresistancetoanantimicrobialagent?Whichdrugisfirstchosentotreatpenicillinallergicshock,andwhy?Whatarefeaturesinthreegenerationsofcephalosporins?Whatareantibacterialspectrumandclinicalusesoferythromycin?27Whatisantibacterialactionofquinolones?Whatiscompositionofco-trimoxazoleandadventageofco-trimoxazol?Whichspeciesareanticanceragentsdividedinto,accordin

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