Tài liệu Color Atlas of Pharmacology (Part 1): History of Pharmacology pptx

ccc cece cece ence nee nee n cence eeneennees Drug Administration Dosage Forms for Oral, and Nasal Applicaftions_.... cc cece ccc cece c cence nee eens eee eeneeneees Lullmann, Color Atl

Color Atlas of

Pharmacology

2nd edition, revised and expanded

Heinz Luillmann, M D

Professor Emeritus

Department of Pharmacology

University of Kiel

Germany

Klaus Mohr, M D

Professor

Department of Pharmacology

and Toxicology

Institute of Pharmacy

University of Bonn

Germany

Albrecht Ziegler, Ph D

Professor Department of Pharmacology University of Kiel

Germany

Detlef Bieger, M.D

Professor Division of Basic Medical Sciences Faculty of Medicine

Memorial University of Newfoundland

St John’s, Newfoundland Canada

164 color plates by Jurgen Wirth

EY

Stuttgart - New York - 2000

IV

Library of Congress Cataloging-in-Publication

Data

Taschenatlas der Pharmakologie English

Color atlas of pharmacology / Heinz Lullmann [et al.] ; color

plates by Jurgen Wirth — 2nd ed., rev and expanded

p cm

Rev and expanded translation of: Taschenatlas der Pharmakologie

3rd ed 1996

Includes bibliographical references and indexes

ISBN 3-13-781702-1 (GTV) — ISBN 0-86577-843-4 (TNY)

1 Pharmacology Atlases

I Lullmann, Heinz IL Title

[DNLM: 1 Pharmacology Atlases

17 T197c 1999a]

RM301.12.T3813 1999

615'.1—dc21

DNLM/DLC

for Library of Congress

Illustrated by Jurgen Wirth, Darmstadt, Ger-

many

This book is an authorized revised and ex-

panded translation of the 3rd German edition

published and copyrighted 1996 by Georg

Thieme Verlag, Stuttgart, Germany Title of the

German edition:

Taschenatlas der Pharmakologie

Some of the product names, patents and regis-

tered designs referred to in this book are in

fact registered trademarks or proprietary

names even though specific reference to this

fact is not always made in the text Therefore,

the appearance of a name without designation

as proprietary is not to be construed as a

representation by the publisher that it is in the

public domain

This book, including all parts thereof, is legally

protected by copyright Any use, exploitation

or commercialization outside the narrow lim-

its set by copyright legislation, without the

publisher’s consent, is illegal and liable to

prosecution This applies in particular to pho-

tostat reproduction, copying, mimeographing

or duplication of any kind, translating, prepa-

ration of microfilms, and electronic data pro-

cessing and storage

©2000 Georg Thieme Verlag, Ruidigerstrasse 14,

D-70469 Stuttgart, Germany

Thieme New York, 333 Seventh Avenue, New

York, NY 10001, USA

Typesetting by Gulde Druck, Tibingen

Printed in Germany by Staudigl, Donauwérth

ISBN 3-13-781702-1 (GTV)

ISBN 0-86577-843-4 (TNY) 123456

2 Pharmacology Handbooks, manuals, etc

2 Pharmacology Handbooks QV

99-33662 CIP

Important Note: Medicine is an ever-chang- ing science undergoing continual develop- ment Research and clinical experience are continually expanding our knowledge, in par- ticular our knowledge of proper treatment and drug therapy Insofar as this book mentions any dosage or application, readers may rest as- sured that the authors, editors and publishers have made every effort to ensure that such ref- erences are in accordance with the state of knowledge at the time of production of the book

Nevertheless this does not involve, imply, or express any guarantee or responsibility on the part of the publishers in respect of any dosage instructions and forms of application stated in the book Every user is requested to examine carefully the manufacturers’ leaflets accompa- nying each drug and to check, if necessary in consultation with a physician or specialist, whether the dosage schedules mentioned therein or the contraindications stated by the manufacturers differ from the statements made in the present book Such examination is particularly important with drugs that are either rarely used or have been newly released

on the market Every dosage schedule or ev- ery form of application used is entirely at the user’s own risk and responsibility The au- thors and publishers request every user to re- port to the publishers any discrepancies or in- accuracies noticed

Lullmann, Color Atlas of Pharmacology © 2000 Thieme

Preface

The present second edition of the Color Atlas of Pharmacology goes to print six years after the first edition Numerous revisions were needed, highlighting the dramatic continuing progress in the drug sciences In particular, it appeared necessary to in- clude novel therapeutic principles, such as the inhibitors of platelet aggregation from the group of integrin GPIIB/IIIA antagonists, the inhibitors of viral protease, or

the non-nucleoside inhibitors of reverse transcriptase Moreover, the re-evaluation

and expanded use of conventional drugs, e.g., in congestive heart failure, bronchial

asthma, or rheumatoid arthritis, had to be addressed In each instance, the primary

emphasis was placed on essential sites of action and basic pharmacological princi- ples Details and individual drug properties were deliberately omitted in the interest

of making drug action more transparent and affording an overview of the pharmaco- logical basis of drug therapy

The authors wish to reiterate that the Color Atlas of Pharmacology cannot replace a textbook of pharmacology, nor does it aim to do so Rather, this little book is desi- gned to arouse the curiosity of the pharmacological novice; to help students of me- dicine and pharmacy gain an overview of the discipline and to review certain bits of

information in a concise format; and, finally, to enable the experienced therapist to

recall certain factual data, with perhaps some occasional amusement

Our cordial thanks go to the many readers of the multilingual editions of the Color Atlas for their suggestions We are indebted to Prof Ulrike Holzgrabe, Wiirzburg,

Doc Achim Meifner, Kiel, Prof Gert-Hinrich Reil, Oldenburg, Prof Reza Tabrizchi, St John’s, Mr Christian Klein, Bonn, and Mr Christian Riedel, Kiel, for providing stimula-

ting and helpful discussions and technical support, as well as to Dr Liane Platt-

Rohloff, Stuttgart, and Dr David Frost, New York, for their editorial and stylistic gui-

dance

Heinz Ltillmann

Klaus Mohr

Albrecht Ziegler

Detlef Bieger

jtirgen Wirth

Fall 1999

VỊ

Contents

General Pharmacology

History of Pharmacology ccc cece eee e cee cence eee ee eee eeneenns Drug Sources Drug and Active Principle cv vs Drug Development ccc cece cece ence nee nee n cence eeneennees Drug Administration Dosage Forms for Oral, and Nasal Applicaftions_

Dosage Forms for Parenteral Pulmonary_

Rectal or Vaginal, and Cutaneous Application_

Drug Administration by Inhalation_

Dermatalogic À€nfS - Q n n HH HE kh From Application t0 Distribution n een eees Cellular Sites of Action Potential Targets of Drug ACHON ccc e nee n cence eens Distribution in the Body External Barriers of the Body c2 222 Blood-Tissue BaTTÌ€TS c c Q Q n ĐH HH HH HH kh nha Possible Modes of Drug Distribution

Binding to Plasma Proteins ccc cece ccc e cece een een eeeeneees Drug Elimination The Liver as an Excretory Organ 0 ccc cece ccc teen eee e eee eeneenns Biotransformation 0f DrugS cv EnterohepatiC CVCÏ@ c c Q Q HQ ng HH ng ko kh nha The Kidney as Excretory OFgan ccc ccc ccc ccc c cence nee eneeneeens Elimination of Lipophilic and Hydrophilic Substances

Pharmacokinetics Drug Concentration in the Body as a Function of Time First-Order (Exponential) Rate PTOC€SS€S

Time Course of Drug Concentration in Plasma

Time Course of Drug Plasma Levels During Repeated Dosing and During Irregular Intake

Accumulation: Dose, Dose Interval, and Plasma Level Fluctuation

Change in Elimination Characteristics During Drug Therapy

Quantification of Drug Action Dose-Response Relationship 0c c cece ese e cece eee vs Concentration-Effect Relationship - Effect Curves_

Concentration-Binding CUrVES cc cece cece cee c een een eeneeneees Drug-Receptor Interaction Types of Binding Forces cc ccc cece cece ene nee n eee e een eeneeens Agonists-AntagonistS 0 ccc cece ccc cee n cece eee ce eeeeeneeeeeneeeunes Enantioselectivity of Drug ACEIO' cv R€C€DfOT ÏVD€S LH H ng eee e HH Hà nh kh va Mode of Operation of G-Protein-Coupled Recepf0TS_

Time Course of Plasma Concentration and Effect Adverse Drug EffectS 0.0.0 0 cc cece ccc cece c cence nee eens eee eeneeneees

Lullmann, Color Atlas of Pharmacology © 2000 Thieme

Contents

Drug Alergy 0 ccc ccc ccc cence cece eee nent een tent eee eee eeneees Drug Toxicity in Pregnancy and Lactation -‹ Drug-independent Effects

Placebo - Homeopathy 0 ccc esc cece cence ence tenet eee eeneees Systems Pharmacology Drug Acting on the Sympathetic Nervous System

Sympathetic Nervous System 0 cc ccc ccc e cece eee e ne eeeeeneees Structure of the Sympathetic Nervous Sysfem Adrenoceptor Subtypes and Catecholamine Actions_ Structure - Activity Relationship of Sympathomimetics Indirect SympathomimeticsS 0 c cece cece cence neces eeneees œ-Sympathomimetics, œ-SympatholytiCS 8-Sympatholytics (ð-Blockers) .-< Types of 8-BlOCkeTS ĐH ng HE kh ka Antiadrenergics 0 0 ccc cece cece ccc e teen eee e ĐH tt nh va Drugs Acting on the Parasympathetic Nervous System

Parasympathetic Nervous SysSt€M 0c c cece cece neces ene enneees Cholinergic Synapse 0 cece ccc ccc ccc cence een ee teen e eee eeneees ParasympathomimefiCS - {c2 c2 212222 ParasympatholVfiCS - c c Q Q n ene eee e tent eeneees Nicotine

Ganglionic TransmiSSỈON_ SE nh Effects of Nicotine on Body Functions Consequences of Tobacco Smoking ‹- Biogenic Amines

Biogenic Amines - Actions and

Pharmacological Implicatlons cccc c2 R9yn00510 1 cá Vasodilators

MB 9o, ¬ na ad I8)š>x:10) 88Ï18Y-11 xi Calcium An†aðOnISfS HH HH HE hxa Inhibitors of the RAA SVSfGIT Q QQ Q n HH HH na Drugs Acting on Smooth Muscle Ÿ.ằẶ 2 Drugs Used to Influence Smooth Muscle Organs Cardiac Drugs

Overview of Modes of Action ccc cece cece ene ete n cence een ennes Cardiac GlyCOSIdES 6.0 ccc ccc ccc cece cence nent eee ene eeneees Antiarrhythmic Drugs 0 ccc ccc cee cece cence ence eee eee eee neeeee Electrophysiological Actions of Antiarrhythmics of

the Nat-Channel Blocking Type ccc ccc c cece ene ene ee een eeenees Antianemics

Drugs for the Treatment of Anemias [ron COIMDOUTS_ SH et een eens eeneees Antithrombotics

Prophylaxis and Therapy of Thromboses - Coumarin Derivatives —- HeparIn_ cv vs Fibrinolytic Therapy 0 ccc cece ccc ccc e cee cence tenet eeeenneees Intra-arterial Thrombus Formation

VII Contents

Inhibitors of Platelet Aggregation_ c eens Presystemic Effect of Acetylsalicylic Acid_ Adverse Effects of Antiplatelet Drugs - Plasma Volume Expanders c2 cv Drugs used in Hyperlipoproteinemias

Lipid-Lowering AZentS ccc cece cece cece nee n cence eeneeneees Diuretics

Diuretics — AN OVErVieW HH NaCI Reabsorption in the Kidney OsmotIC DIUT€FlCS HQ ng HH HH nh kh khai Diuretics of the Sulfonamide Type ccc cece c ence teen nena eees Potassium-Sparing Diuretics 0 ccc cece cece cece eeeneeeeneeees Antidiuretic Hormone (/ADH) and DerivatiVes Drugs for the Treatment of Peptic Ulcers

Drugs for Gastric and Duodenal Ulcers -

Antidiarrheals

Antidiarrheal AZents 0.0 0 cece ccc cece cece ence nee nee eeeneeneeens Other Gastrointestinal Drugs 0 ccc cece cece cece cence eee eeneeens Drugs Acting on Motor Systems

Drugs Affecting Motor FunctiOn cà Muscle Relaxan†S_ - cQ Q HH HH HH kh va Depolarizing Muscle RelaxanfS Ặ{ŸẶ Antiparkinsonian Drugs 0 ccc ccc ccc cee cence nee eeeneeneenns Antiepileptics 0.0.0 ccc ccc ccc ccc cece ene nee nee n eee eene een eeneeens Drugs for the Suppression of Pain, Analgesics,

Pain Mechanisms and Pathways co Antipyretic Analgesics

Bia.) ST ((‹(‹(đaa nee n cence tense een eeeenees Antipyretic Analgesics and Antiinflammatory Drugs

Antipyretic AnalE€SICS ccc cece n cence eee eeeneeneeens Antipyretic Analgesics

Nonsteroidal Antiinflammatory

(Antirheumatic) AZentsS 2.0 cece ccc ccc ccc cence ene HH HH nha Thermoregulation and AnfÏDVTefiCS cu Local AnesthetlCS ng ng ng ng nu ng hà kh kh ya Opioids

Opioid Analgesics - Morphine Type 0 cece ccc ee cece een eeneees General Anesthetic Drugs

General Anesthesia and General Anesthetic Drugs Inhalational AnesthetiCS cQ Q Q HH na Injectable AnesthefiCS -c c Q Q n HH HH HH nha Hypnotics

SOpOTifics, HVDOICS cence nee n een een eeneennees Sleep-Wake Cycle and Hypnotics ccc cc ccc cece cence nee neen eens Psychopharmacologicals

BenzodiaZepin€S ccc cece cece cee nen eee nee nee e been eeneennees Pharmacokinetics of Benzodiazepines Therapy of Manic-Depressive lÏÏnes - Therapy of Schizophrenia 0 c ccc cece eee c ence ence ee eeeeeneenns Psychotomimetics (Psychedelics, Hallucinogens)

Lullmann, Color Atlas of Pharmacology © 2000 Thieme

Contents Hormones

Hypothalamic and Hypophyseal Hormones_ Thyroid Hormone TherapDYy - c2 22222222 Hyperthyroidism and Antithyroid Drugs Glucocorticoid TheTaDV ec cee eee eee teen e eee eeneees Androgens, Anabolic Steroids, Antiandrogens_

Follicular Growth and Ovulation, Estrogen and

Progestin Production 0 ccc ccc cece cece ence nent eee eeeenneees Oral ContraceptiveS 0.0 cc cece cece cence ence eee tent enneees Insulin TheraDV - ng HH HE nu kh huy Treatment of Insulin-Dependent

Diabetes Mellifus - ence eens eee eeneees Treatment of Maturity-Onset (Type II)

Diabetes Mellifus - ence eens eee eeneees Drugs for Maintaining Calcium HomeosfaSiS Antibacterial Drugs

Drugs for Treating Bacterial Infections ‹- Inhibitors of Cell Wall Synthesis 0 ccc ccc cece cece neces eeneees Inhibitors of Tetrahydrofolate SynthesIs Inhibitors of DNA FunCHOn ng HE kh và Inhibitors of Protein Synthesis ccc cece cece cece neces eeneees Drugs for Treating Mycobacterial Infectlons Antifungal Drugs

Drugs Used in the Treatment of Fungal Infection_ Antiviral Drugs

Chemotherapy of Viral InfectionS ccc ccc cence cence eee eneees Drugs for Treatment of AIDS_ c2 Disinfectants

Disinfectants and AntisepticS 0 ccc cece c cece eee e eens eeneees Antiparasitic Agents

Drugs for Treating Endo- and Ectoparasitic Infestations Antimalarials 0.0.0 ccc ccc cece cece cece n cence nen ee nee tenant en ennenes Anticancer Drugs

Chemotherapy of Malignant Tumors_ -‹- Immune Modulators

Inhibition of Immune ReSpOnS€S_ cà Antidotes

Antidotes and treatment of poisonings_ - Therapy of Selected Diseases

[10123191 §k ~ M19)9Ìứaa eee e tenet eeteteneneeeennes Antianginal DruES -cc c n Q ng HE ky Acute Myocardial InfarCfiOn na HYPerteMSion di I8) 91201) Loaaaaidaidaadadiiiitẳiiẳiái e6 ee eee e eee en eee eee e eee eee (OTS) 110) B16) 1) (sa

Rheumatoid ArthrifiS ng HH HH HH nu khu khe hà và và MIBTAID€ Q c Q Q ng n ng ng n ng HE tà nà ko và ki và Common CoÌd_, ng HH SH nu khu kh kh và AIlerBlC DISOTC€TS cQ Q QQ Q nee nee e ng ng nh va Bronchial Asthma c Q HH ng nu HH kh huy 50-0 ä —ä

X Contents

Further Reading ng ng ng ng nu kh yi IMiiis8io[> VHHCaaiiỖẮỖŨỖŨỖẮỖỔỔŨỖŨÍỖŨÚŨÚẮẮỖỒẮŨỒỔŨẮỒ Index

Lullmann, Color Atlas of Pharmacology © 2000 Thieme

General Pharmacology

2 History of Pharmacology

History of Pharmacology

Since time immemorial, medicaments

have been used for treating disease in

humans and animals The herbals of an-

tiquity describe the therapeutic powers

of certain plants and minerals Belief in

the curative powers of plants and cer-

tain substances rested exclusively upon

traditional knowledge, that is, empirical

information not subjected to critical ex-

amination

The Idea

sys

q

`

T ˆ ` Fas

**

7 Ts

eA AS TA WS

' TY ea ve ye < ~ one |

Claudius Galen (129-200 A.D.) first at-

tempted to consider the theoretical

background of pharmacology Both the-

ory and practical experience were to

contribute equally to the rational use of

medicines through interpretation of ob-

served and experienced results

“The empiricists say that all is found by

experience We, however, maintain that it

is found in part by experience, in part by

theory Neither experience nor theory

alone is apt to discover all.”

The Impetus

Theophrastus von Hohenheim (1493-

1541 A.D.), called Paracelsus, began to

quesiton doctrines handed down from

antiquity, demanding knowledge of the

active ingredient(s) in prescribed reme-

dies, while rejecting the irrational con-

coctions and mixtures of medieval med-

icine He prescribed chemically defined substances with such success that pro- fessional enemies had him prosecuted

as a poisoner Against such accusations,

he defended himself with the thesis that has become an axiom of pharma- cology:

“If you want to explain any poison prop- erly, what then isn't a poison? All things are poison, nothing is without poison; the dose alone causes a thing not to be poi- son.”

Early Beginnings

Johann Jakob Wepfer (1620-1695) was the first to verify by animal experi- mentation assertions about pharmaco- logical or toxicological actions

“I pondered at length Finally I resolved to clarify the matter by experiments.”

Lullmann, Color Atlas of Pharmacology © 2000 Thieme

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