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Chapter 39 Antineoplastic Agents Department of Pharmacology, Yunyang Medical College Lu Juan( 卢娟 )

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Presentation on theme: "Chapter 39 Antineoplastic Agents Department of Pharmacology, Yunyang Medical College Lu Juan( 卢娟 )"— Presentation transcript:

1 Chapter 39 Antineoplastic Agents Department of Pharmacology, Yunyang Medical College Lu Juan( 卢娟 )

2 Teaching outline TTo master the categories of antineoplastic drugs and the basic mechanisms. TTo understand the principles of combination of antineoplastic drugs, the pharmacologic actions, clinical applications and adverse reactions.

3 Overview Cancer incidence and treatment measures The development history of cancer chemotherapy Novel anticancer drug

4 1.Systemic tumor 2.Some solid tumor which have good effect to chemotherapy 3.the consolidation and adjuvant therapy as post-operation and radiotherapy 4.the palliative treatment of Late, extensive transfer and recurrent tumors 5.Neo-adjuvant chemotherapy the adaptation syndrome of antineoplastic drugs:

5 Five-year survival rate % Before chemotherapy post chemotherapy Choriocarcinoma 20 85~90 Malignant mole 20 >90 Acute leukemia 0 50 …

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7 眼科检查:双眼瞳孔区可见白色反光,双眼底可见肿瘤

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9 Pharmacological Basis

10 1 、 Proliferating cell population ---Targeting of therapy Rapidly growing tumors, the GF is greater, and sensitive to drugs. 2 、 Group of non-proliferating cells Including three parts of quiescent cells, no proliferation cells (already differentiated cells) and dead cells, in which quiescent cells are not sensitive to drugs is a source of tumor recurrence. composition of tumor cells : GF ( growth fraction ) Proliferating cell population Whole-cell group GF =

11 Cell cycle, including : Resting (G 0 phase) Proliferating cycle: Presynthesis(G 1 phase) DNA synthesis(S phase) Premitotic(G 2 phase) Mitosis(M phase)

12 G 2 (19%) M(2%) S (39%) G 1 (40%) no proliferation cells Dead cells (G 0 ) Proliferating cell population sensitive to drugs. Group of non-proliferating cells a source of tumor recurrence.

13 一. the relationship between Cell proliferation cycle and the anti-cancer drugs

14 Classification of antineoplastic agents  cell cycle specific agents, CCSA  cell cycle non-specific agents, CCNSA According to the role of cycles or phases

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16 G 2 (19%) M(2%) S (39%) G 1 (40%) no proliferation cells Dead cells (G 0 ) Proliferating cell population sensitive to drugs. Group of non-proliferating cells a source of tumor recurrence.

17 二. The relationship between biochemistry and antineoplastic agents

18 Classification of antineoplastic agents According to the biochemical mechanism of action  Drugs that affecting nucleic acid biosynthesis  Drugs that damaging structure and function of DNA directly  Drugs that inhibiting synthesis of RNA by interfering with transcription process  Drugs that affecting synthesis and functions of proteins  Drugs that affecting the balance of hormones  Other

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20 Classification of antineoplastic agents  Alkylating agents  Antimetabolites  antitumor antibiotics  plant alkaloids  Hormonal agents According to the chemical structure and source

21 三. A dverse reactions

22 (一) Recent toxicities 一 common toxicities bone marrow depression——is the most common serious adverse reactions Gastrointestinal reactions Hair follicle damage

23 (二) Recent toxicities 一 Specific toxicities Renal toxicity and bladder toxicity Pulmonary toxicity Cardiotoxicity Neurotoxicity Ototoxicity Immunosuppression Hepatotoxicity

24 (三) Long-term toxicity Infertility, mutagenic, teratogenic carcinogenesis : Second primary tumor

25 Commonly used anti-cancer drugs 一. Alkylating agents ( cell cycle non- specific agents ) cyclophosphamide 二. Antimetabolites ( cell cycle specific agents ) methotrexate,MTX

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27 三. antitumor antibiotics ( cell cycle non-specific agents ) ADM 四. plant alkaloids vinblastine,VLB vincristine,VCR

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29 Camptothecine

30 Podophyllotoxin

31 paclitaxel

32 五. Hormones 六. other

33 四. The principles of using drugs

34 Best Wishes for Your Success in Final Examination


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