页数：16页文件大小：1.08 MB来源： 药理学ppt课件
本课件为药理学课程中的《药理学总论-绪言》，围绕药理学总论-绪言、What is a drug、A goal of、One exampl等部分展开，逐页梳理概念、机制与临床应用要点，适合预习、课堂对照与考前复习。
药理学总论-绪言 Pharmacology A Very Basic Intro
What is a drug?-any chemical agent whichaffects any biological process
Sources of Drugs Animals Plants Minerals Synthetic Microbes Genetic engineering drugs
A goal of Genomics is to find and expressgenes that code for unknown peptides withsignificant biological properties, like receptorsor enzymes. In a reverse Pharmacologyapproach this peptide, e.g. a receptor, is thenused to "fish" for a natural ligand . Withreceptor and ligand in hand the biological roleof the receptor needs to be determined. Finally,screening for synthetic ligands as well as leadoptimization can lead to new drug candidates. In contrast, the classical approach to drugdiscovery starts with the identification of aligand that has biological activity that in turn isused to "fish" for the corresponding receptor.
One example for a Genomics strategy aims atidentifying drug targets based on molecularhomology within Gene-families. One of the mostimportant families of drug-targets for thepharmaceutical industry is the family of G-proteincoupled receptors (GPCRs). Of the top 200 bestselling prescription drugs, more than 20%interact with GPCRs, providing worldwide sales ofover $20 billion. The characteristic motif of the GPCR family is the seven distinct hydrophobicregions, each of 20 to 30 amino acids that formthe transmembrane domain of these integralmembrane proteins. This key amino-acidsequence motif can be found within all types of GPCRs and can be used to identify DNA-sequences that code for GPCRs.
What is pharmacology ?-the study ofhowdrugseffect biological systems
What is Pharmacology ?Pharmacology Pharmacokinetics Pharmacodynamics What the body does to drug What the drug does to body Pharmacotherapeutics Pharmacocognosy The study of the use of drugs Identifying crude materials as drugs Toxicology
From Chemistto First In Man…approximately 7–10 years How a Drug becomes a drug…
H. Haarmann University of Maryland, 2002Basic & Clinical Evaluation of New Drugs1. Drug discovery & Drug screening Chemistry In Vitro Studies Function in cells, tissues, and at receptors2. Preclinical safety & toxicity testing In Vivo
Animal studies Pharmacology and Behavioral Pharmacology Potency and Efficacy–ED50Toleranceand Tachyphylaxis(快速耐受) Toxicity–Acute and Chronic LD50Teratogenicity = birth defects Carcinogenicity = cancerous3. Evaluation of drug in humans
Evaluating Drugs in Humans The Food and Drug Administration (FDA) Phases of a Clinical Trials Phase IPhase IIPhase IIIPhase IV
Drug Nomenclature
Chemical name（化学名）-*Generic name（非专利名）
Trade name（商品名）Chemical Name: 2-(4-isobutylphenyl)-propionic acid Generic Name: ibuprofen（布洛芬）Trade Names: Advil, Aches-N
Pain, Brufen, Emodin, Haltran, Medipren, Midol 200, Motrin, Nuprin, Rufen, Trendar, Wal
Profen*preclinical nomenclature = company abbrev-123456 (e.g. WAY-100635, MK-869)
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