chapter 39 antineoplastic agents department of pharmacology, yunyang medical college lu juan( 卢娟...
TRANSCRIPT
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 …
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.
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.
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
(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
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