Chapter 39 Antineoplastic Agents

Department of Pharmacology, Yunyang Medical College

Lu Juan( 卢娟 )

Teaching outline

To master the categories of antineoplastic dr

ugs and the basic mechanisms.

To understand the principles of combination

of antineoplastic drugs , the pharmacologic acti

ons , clinical applications and adverse reactions .

Overview

Cancer incidence and treatment measuresThe development history of cancer chemotherapyNovel anticancer drug

1.Systemic tumor 　

2.Some solid tumor which have good effect t

o chemotherapy

3.the consolidation and adjuvant therapy as

post-operation and radiotherapy

4.the palliative treatment of Late, extensive t

ransfer and recurrent tumors

5.Neo-adjuvant chemotherapy

the adaptation syndrome of antineoplastic drugs:

Five-year survival rate%

Before chemotherapy post chemotherapy

Choriocarcinoma 20 85~90 Malignant mole 20 >90 Acute leukemia 0 50 …

眼科检查：双眼瞳孔区可见白色反光，双眼底可见肿瘤

Pharmacological Basis

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 prolifera

tion 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 populationWhole-cell groupGF =

Cell cycle, including ：Resting (G0 phase)

Proliferating cycle:

Presynthesis(G1 phase)

DNA synthesis(S phase)

Premitotic(G2 phase)

Mitosis(M phase)

G2

(19%)

M(2%)S (39%)

G1(40%)

no proliferation cells

Dead cells

(G0)

Proliferating cell populationsensitive to drugs.

Group of non-proliferating cellsa source of tumor recurrence.

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

Classification of antineoplastic agents

cell cycle specific agents, CCSA

cell cycle non-specific agents, CCNSA

According to the role of cycles or phases

G2

(19%)

M(2%)S (39%)

G1(40%)

no proliferation cells

Dead cells

(G0)

Proliferating cell populationsensitive to drugs.

Group of non-proliferating cellsa source of tumor recurrence.

二．The relationship between biochemistry and antineoplastic agents

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

Classification of antineoplastic agents

Alkylating agents

Antimetabolites

antitumor antibiotics

plant alkaloids

Hormonal agents

According to the chemical structure and source

三．Adverse reactions

（一） Recent toxicities 一 common toxicities

bone marrow depression——is the most

common serious adverse reactions Gastrointestinal reactions

Hair follicle damage

（二） Recent toxicities 一 Specific toxicities Renal toxicity and bladder toxicity

Pulmonary toxicityCardiotoxicityNeurotoxicityOtotoxicityImmunosuppressionHepatotoxicity

（三） Long-term toxicity

Infertility, mutagenic, teratogenic

carcinogenesis ： Second primary tumo

r

Commonly used anti-cancer drugs

一．Alkylating agents （ cell cycle non-specific agents ）

cyclophosphamide

二．Antimetabolites （ cell cycle specific agents ）

methotrexate,MTX

三． antitumor antibiotics （ cell cycle non-specific agents ） ADM

四．plant alkaloids vinblastine ,VLB vincristine,VCR

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Camptothecine

Podophyllotoxin

paclitaxel

五． Hormones

六．other

四．The principles of using drugs

Best Wishes for Your Success in Final Examination

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