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Pharmacodynamics (藥物作用分類 (Agonists (致效劑) (full efficacy), Partial agonists…
Pharmacodynamics
藥物作用分類
Agonists (致效劑)
full efficacy
Partial agonists (部分致效劑)
some efficacy
部分致效劑對完全致效劑的作用
Antagonists (拮抗劑)
zero efficacy
Noncompetitive antagonist
不同結合位
Competitive antagonist
相同結合位
Affinity (親和力)
Kd愈大,親和力愈弱
Efficacy (最大藥效)
藥物所能產生的最大反應
Potency (效價)
依藥物產生其最大效果的50%效用所需的濃度(EC50)或劑量(ED50)而定
Safety tests
acute toxicity
subacute or subchronic toxicity
chronic toxicity
effect on reproductive performance
carcinogenic potential
mutagenic potential
investigative toxicology
dose
Median effective dose (ED50)
Median lethal dose (LD50)
The therapeutic index
(TI)=LD50/ED50
越大越安全
藥物動力學與藥效學的關係
pharmacokinetics
dose-concentration
pharmacodynamics
concentration-effect
Dose-response relationships
Linear scale
Logarithmic scale
Characterization of receptor
Spare receptors
備用接受器
將訊息放大
Desensitization
去敏感性
目的: 保護細胞
Tachyphylaxis (快速耐受性)
藥物發展的階段
IND= investinational new drug
NDA= new drug application
藥物受器間交互作用與藥效學
Types of receptor- effector linkage
Ligand-gated ion channels
rapid
receptors
nicotinic
sodium influx
gama-aminobutyric acid (GABA)
chloride influx
G-protein coupled receptors
second messengers
Enzyme-liked receptors
Intracellular receptors
steroid hormone
藥效學
effects of drugs