Fibrinolytics and antifibrinolytics [with 50 tables]
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Sprache: | English |
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Berlin [u.a.]
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2001
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Schriftenreihe: | Handbook of experimental pharmacology
146 |
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245 | 1 | 0 | |a Fibrinolytics and antifibrinolytics |b [with 50 tables] |c contributors F. Bachmann ... Ed.: F. Bachmann |
264 | 1 | |a Berlin [u.a.] |b Springer |c 2001 | |
300 | |a XXVI, 599 S. |b Ill., graph. Darst. | ||
336 | |b txt |2 rdacontent | ||
337 | |b n |2 rdamedia | ||
338 | |b nc |2 rdacarrier | ||
490 | 1 | |a Handbook of experimental pharmacology |v 146 | |
650 | 7 | |a Fibrinolytic Agents |2 cabt | |
650 | 0 | 7 | |a Fibrinolytikum |0 (DE-588)4017042-1 |2 gnd |9 rswk-swf |
650 | 0 | 7 | |a Pharmakologie |0 (DE-588)4045687-0 |2 gnd |9 rswk-swf |
650 | 0 | 7 | |a Antifibrinolytikum |0 (DE-588)4142667-8 |2 gnd |9 rswk-swf |
655 | 7 | |0 (DE-588)4143413-4 |a Aufsatzsammlung |2 gnd-content | |
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689 | 0 | |5 DE-604 | |
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689 | 2 | 1 | |a Antifibrinolytikum |0 (DE-588)4142667-8 |D s |
689 | 2 | |5 DE-604 | |
689 | 3 | 0 | |a Antifibrinolytikum |0 (DE-588)4142667-8 |D s |
689 | 3 | 1 | |a Pharmakologie |0 (DE-588)4045687-0 |D s |
689 | 3 | |5 DE-604 | |
689 | 4 | 0 | |a Fibrinolytikum |0 (DE-588)4017042-1 |D s |
689 | 4 | 1 | |a Pharmakologie |0 (DE-588)4045687-0 |D s |
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Datensatz im Suchindex
_version_ | 1819633345650229248 |
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adam_text | FIBRINOLYTICS AN
D
ANTIFIBRINOLYTICS
CONTRIBUTOR
S
F. BACHMANN
, D.C. BERRIDGE
, C. BODE
, H
. BOUNAMEAUX
,
F.J. CASTELLINO, J.H. CHESEBRO
, A.C
. CHIU, D. COLLEN,
G.J. DEL ZOPPO
, W. DIETRICH
, P. DONNER
, J.J. EMEIS
, L. FLOHE
,
V. FUSTER
, R. GALLO, W.A. GUNZLER
, V. GUREWICH
, E
. HABER
,
S.B. HAWLEY, R. HAYES, T. HERREN
, XL. HOOVER-PLOW, J. HORROW,
T. KOOISTRA, E.K.O
. KRUITHOF, H.R
. LIJNEN, VJ
. MARDER
,
L.A. MILES, K. PETER
, E.F. PLOW, V.A. PLOPLIS, A
. REDLITZ
,
M.S. RUNGE
, CM
. SAMAMA
, M.M. SAMAMA
, A.A
. SASAHARA
,
W.-D. SCHLEUNIG, G.V.R.K. SHARMA
, O. TABY, E.J. TOPOL,
M. VERSTRAETE
, S. XU
E
EDITOR
:
F. BACHMANN
SPRINGER
CONTENTS
SECTION I: MOLECULAR BIOLOGY, BIOCHEMISTRY, PHYSIOLOGY, AND PHARMACOLOGY
OF THE PLASMINOGEN-PLASMIN ENZYME SYSTEM
CHAPTER 1
THE FIBRINOLYTIC SYSTEM AND THROMBOLYTIC AGENTS
F.
BACHMANN.
WITH 1 FIGURE 3
A. THE FIBRINOLYTIC SYSTEM 3
B. MECHANISMS WHICH LEAD T
O TH
E LYSIS OF A THROMBU
S 5
C. PATHOPHYSIOLOGY OF THE FIBRINOLYTIC SYSTEM 7
I. DECREASE
D FIBRINOLYTIC ACTIVITY AND
DEE
P VENOUS THROMBOSIS 7
1. FAMILIAL THROMBOPHILI
A WITH HIGH PAI-1 LEVELS 7
2. ACQUIRE
D ASSOCIATION OF HYPOFIBRINOLYSIS AN
D
DEE
P VENOUS THROMBOSIS 7
II. IMPAIRE
D FIBRINOLYSIS AND CORONAR
Y HEAR
T DISEASE 9
D. THROMBOLYTIC THERAPY 10
I. BASIC CONSIDERATION
S 10
1. THE PROTEOLYTIC STATE AND BLEEDING COMPLICATIONS 10
2. THROMBIN GENERATIO
N AND REOCCLUSION 10
3. DELAY T
O TREATMEN
T 10
4. PLATELET ACTIVATION 11
5. CONTRAINDICATION
S FOR THROMBOLYTIC THERAPY 11
6. FIBRIN SPECIFICITY 11
7. ANTIGENICITY 12
8. TREATMENT OF ELDERLY PATIENTS 12
E. MILESTONES IN THROMBOLYTIC THERAP
Y OF
ACUT
E MYOCARDIAL INFARCTION 13
I. FIRST GENERATIO
N AGENT
S 13
II. SECOND GENERATIO
N AGENT
S 13
III. THIRD GENERATIO
N AGENT
S 13
IV. THE FUTUR
E OF THROMBOLYTIC THERAP
Y 15
XII CONTENTS
LIST OF ABBREVIATION
S AN
D ACRONYM
S 15
REFERENCE
S 15
CHAPTE
R 2
PLASMINOGEN AND STREPTOKINASE
F.J.
CASTELLINO
AN
D V.A.
PLOPLIS
.
WITH 3 FIGURE
S 25
A
. PRIMAR
Y STRUCTUR
E OF HUMA
N PLASMINOGE
N 25
B. GEN
E ORGANIZATIO
N OF HUMA
N PLASMINOGE
N 28
C. THE ACTIVATIO
N OF HUMA
N PLASMINOGE
N 29
I. GENERA
L CONSIDERATION
S 29
II
. ACTIVATIO
N OF HUMA
N PLASMINOGE
N BY TWO-CHAIN UROKINAS
E
AND TISSUE-TYP
E PLASMINOGE
N ACTIVATO
R 33
1. MECHANIS
M OF ACTIVATIO
N OF HUMA
N PLASMINOGE
N 33
2. POSITIVE AND NEGATIV
E ACTIVATIO
N EFFECTORS 34
III
. ACTIVATIO
N OF HUMA
N PLASMINOGE
N BY
SINGLE-CHAIN UROKINAS
E 35
IV. ACTIVATIO
N OF HUMA
N PLASMINOGE
N BY STREPTOKINAS
E 36
1. STRUCTURA
L AN
D ACTIVATIO
N FEATURE
S OF STREPTOKINASE
S ..
. 36
2. MECHANIS
M OF ACTIVATIO
N OF HUMA
N PLASMINOGE
N
BY HUMA
N HOST-DERIVE
D STREPTOKINAS
E 39
3. FUNCTIONA
L REGION
S OF HUMA
N PLASMINOGE
N AN
D
HUMAN-DERIVE
D STREPTOKINAS
E THA
T
MEDIAT
E ACTIVATIO
N 41
V. ACTIVATIO
N OF HUMA
N PLASMINOGE
N BY STAPHYLOKINAS
E 42
D. SPONTANEOU
S AN
D INDUCE
D PHENOTYPE
S OF
PLASMINOGE
N DEFICIENCY 43
LIST OF ABBREVIATION
S 44
REFERENCE
S 45
CHAPTE
R 3
TISSUE-TYPE PLASMINOGEN ACTIVATOR (TPA
)
F.
BACHMANN.
WITH 2 FIGURES 57
A
. MILESTONE
S IN TISSUE-TYPE PLASMINOGE
N ACTIVATO
R
(TPA
) RESEARC
H 57
B. SOURCE
S OF TPA 58
C. METABOLIS
M OF TPA 59
D. STRUCTUR
E AN
D BIOCHEMISTR
Y OF TPA 60
I. GEN
E STRUCTUR
E OF TPA 60
1. TRANSLATE
D REGION
S 60
2. 5
AN
D 3
FLANKIN
G REGION
S 60
3. POLYMORPHISMS 62
II
. PROTEI
N STRUCTUR
E OF TPA 62
1. PRIMAR
Y AMIN
O ACI
D SEQUENC
E 62
CONTENTS XIII
A) THE FINGER DOMAI
N 63
B
) THE EPIDERMA
L GROWT
H FACTOR DOMAIN 63
C) THE KRINGLE DOMAIN
S 64
D
) THE PROTEAS
E (CATALYTIC) DOMAI
N 65
2. CRYSTAL STRUCTUR
E OF TH
E PROTEAS
E DOMAIN 65
3. GLYCOSYLATION OF TPA 65
III.
ENZYMATIC PROPERTIE
S OF TPA 66
1. ENZYME KINETICS IN THE ABSENC
E AND PRESENCE
OF FIBRIN 66
2. DIFFERENCES BETWEEN SC-TPA AND TC-TPA 67
3. LOCALIZATION OF TH
E EPITOPE
S IN FIBRIN THAT ENHANC
E
THE RAT
E OF PLASMINOGEN ACTIVATION BY TPA 68
IV. INTERACTION
S OF TPA WITH SERPINS 68
E
. THE TPA RECEPTOR
S 70
I. ACTIVATION RECEPTOR
S 70
II. CLEARANC
E RECEPTOR
S 71
1. THE MANNOS
E RECEPTO
R 71
2. THE LD
L RECEPTOR-RELATE
D PROTEIN
(LRP, A
2
-MACROGLOBULIN RECEPTOR
) 72
F. PATHOPHYSIOLOGY OF TPA 72
I. INTRAVASCULAR FUNCTION OF TPA 72
II
. OTHE
R FUNCTIONS OF TPA 74
LIST OF SYMBOLS AND ABBREVIATION
S 75
REFERENCES 76
CHAPTE
R 4
URINARY-TYPE PLASMINOGEN ACTIVATOR (UPA
)
W.A.
GUNZLE
R
AND L.
FLOHE
.
WITH 2 FIGURES 91
A
. MILESTONE
S IN UPA RESEARC
H 91
B. NOMENCLATUR
E OF UPA FORMS 92
C. SOURCE
S OF UPA 93
D. ASSAY OF UPA 93
E. BIOCHEMISTR
Y OF UPA 94
I. THE UPA GEN
E 94
II. THE UPA STRUCTUR
E 95
III
. NON-PROTEI
N COMPONENT
S OF UPA 97
IV. PROTEOLYTI
C CONVERSION
S OF UPA 9S
V. UPA ACTIVITY 99
F. PHYSIOLOGY OF UPA 100
I. INTRAVASCULA
R AND INTRATUBULA
R FUNCTION
S OF UPA 102
II. ROL
E OF UPA IN TISSUE REMODELIN
G AND CELL MIGRATION ...
. 102
LIST OF ABBREVIATION
S 103
REFERENCE
S 103
XIV CONTENTS
CHAPTE
R 5
THE INHIBITORS OF THE FIBRINOLYTIC SYSTEM
E.K.O
.
KRUITHOF.
WITH 1 FIGURE IL
L
A
. INTRODUCTIO
N ..
.
B. OH-ANTIPLASMIN
I. GEN
E AN
D PROTEI
N STRUCTUR
E
II. TARGET ENZYM
E SPECIFICITY .
III
. A
2
-ANTIPLASMI
N DEFICIENCIES
11
11
13
14
C. PLASMINOGEN ACTIVATO
R INHIBITO
R TYPE 1 114
I. GEN
E STRUCTUR
E 114
II. PROTEI
N STRUCTUR
E 115
III
. TARGET ENZYM
E SPECIFICITY OF PAI-1 116
IV. DEFICIENCIES, KNOCKOUT
, AN
D OVEREXPRESSIO
N IN MICE
V. ROLE OF PAI-1 IN CELL MIGRATIO
N
VI
. DISTRIBUTIO
N OF PAI-1 IN VIVO
VII
. GEN
E REGULATIO
N OF PAI-1
VIII
. PAI-1 AS A MARKE
R FOR VASCULAR AN
D ARTERIA
L DISEASE
16
16
17
18
18
18
19
IX. PAI-1 AN
D TH
E ACUT
E PHAS
E RESPONS
E
X. PAI-1 AN
D SEPTICEMI
A
D. PLASMINOGEN ACTIVATO
R INHIBITO
R TYPE 2 119
I. GEN
E AN
D PROTEI
N STRUCTUR
E 119
II. TARGET ENZYM
E SPECIFICITY 120
III
. DISTRIBUTIO
N OF PAI-2 IN VIVO 120
IV. GEN
E REGULATIO
N OF PAI-2 121
V. THE PHYSIOLOGICAL ROL
E OF PAI-2 121
E. PLASMINOGEN ACTIVATO
R INHIBITOR
S IN PREGNANCY 121
F. THERAPEUTI
C APPLICATION
S OF PAI-1 AN
D PAI-2 122
I. PAI-1 123
II. PAI-2 123
G. OTHE
R PROTEAS
E INHIBITOR
S OF TH
E FIBRINOLYTIC SYSTEM 123
H. INHIBITOR
S OF PLASMINOGE
N BINDIN
G T
O FIBRIN O
R CELL SURFACES 124
I. HISTIDINE-RIC
H GLYCOPROTEI
N 124
II. LIPOPROTEIN(A
) 125
III
. CARBOXYPEPTIDASE
S 126
I. CONCLUSIONS 126
LIST OF ABBREVIATION
S 127
REFERENCE
S 127
CHAPTE
R 6
ASSEMBLY OF THE PLASMINOGEN SYSTEM ON CELL SURFACES
E.F.
PLOW,
A
.
REDLITZ
,
S.B.
HAWLEY,
S.
XUE
,
T.
HERREN
,
J.L.
HOOVER-PLOW,
AN
D L.A
.
MILES
.
WITH 3 FIGURES 141
A
. INTRODUCTIO
N 141
B. PLASMINOGEN RECEPTOR
S 142
CONTENTS XV
I. GENERA
L CHARACTERISTIC
S 142
II
. NATUR
E OF PLASMINOGEN RECEPTOR
S 143
III
. REGULATIO
N OF PLASMINOGEN RECEPTOR
S 145
C. TPA RECEPTOR
S 148
I. GENERA
L CHARACTERISTIC
S 148
II
. RECOGNITIO
N OF TPA 148
III
. CELLULAR DISTRIBUTIO
N OF TPA RECEPTOR
S 148
1. ENDOTHELIA
L CELLS 148
2. CIRCULATING BLOOD CELLS 149
3. CELLS OF NEURONA
L ORIGIN 149
4. VASCULAR SMOOTH MUSCLE CELLS 149
5. TUMOR CELLS 149
D. UROKINAS
E RECEPTOR
S 150
I. GENERA
L CHARACTERISTIC
S 150
II
. THE UROKINAS
E RECEPTOR
, UPA
R 150
1. CELLULAR DISTRIBUTIO
N OF UPA
R 150
2. RECOGNITIO
N SPECIFICITY OF UPA
R 150
3. THE UPA
R GEN
E 151
4. THE UPA
R PROTEI
N 151
5. REGULATIO
N OF UPA
R EXPRESSIO
N 153
6. NON-PROTEOLYTI
C FUNCTION
S OF UPA
R 153
III
. OTHE
R UPA RECEPTOR
S 154
E
. FUNCTIONA
L CONSEQUENCE
S OF RECEPTO
R OCCUPANCY 155
I. KINETIC CONSEQUENCE
S 155
1. PLASMINOGEN RECEPTOR
S 155
A) ENHANCE
D PLASMINOGEN ACTIVATION 156
B
) AMPLIFICATION LOOP
S 156
C) PROTECTIO
N OF PLASMIN ACTIVITY 156
D
) ENHANCEMEN
T OF PLASMIN ACTIVITY 156
2. UPA RECEPTOR
S 156
3. TPA RECEPTOR
S 157
II
. FUNCTIONA
L CONSEQUENCE
S 157
LIST OF ABBREVIATION
S 158
REFERENCE
S 158
SECTION II: CLINICAL US
E OF THROMBOLYTIC AGENTS
IN ACUTE MYOCARDIAL INFARCTION
CHAPTER 7
STREPTOKINASE AND ANISOYLATED LYS-PLASMINOGEN STREPTOKINASE
ACTIVATOR COMPLEX
V.J.
MARDER
AND F.
BACHMANN.
WITH 2 FIGURES 173
A
. INTRODUCTIO
N 173
I. PHARMACOLOGY 173
1. STREPTOKINAS
E (SK) 173
XVI CONTENTS
2. ANISOYLATE
D LYS-PLASMIN(OGEN
) STREPTOKINAS
E ACTIVATO
R
COMPLE
X (APSAC
, ANISTREPLASE
) 174
II
. TH
E PROTEOLYTI
C STAT
E 174
III.
FACTORS INFLUENCING TH
E LYSIS OF THROMB
I AN
D EMBOL
I 176
B. THERAPEUTI
C RESULT
S IN ACUT
E MYOCARDIA
L INFARCTION 177
I. STREPTOKINAS
E 177
1. EARL
Y STUDIE
S WITH INTRAVENOU
S STREPTOKINAS
E 177
2. INTRACORONAR
Y ADMINISTRATIO
N 178
3. HIGH-DOS
E INTRAVENOU
S ADMINISTRATIO
N
OF STREPTOKINAS
E 179
A) DOSE-RANGIN
G STUDIE
S AN
D ANTI-S
K ANTIBODIE
S ...
. 179
B
) PATENC
Y VS RECANALIZATIO
N RAT
E 180
C) MORTALIT
Y REDUCTIO
N 182
D
) DELA
Y T
O TREATMEN
T 183
E
) BLEEDIN
G COMPLICATIO
N 185
F) PATIEN
T SELECTION
, CONTRAINDICATION
S 187
G) OTHE
R SIDE EFFECTS 188
H) LABORATOR
Y MONITORIN
G 188
I) RETHROMBOSI
S 188
II
. ANISOYLATE
D LYS-PLASMIN(OGEN
) STREPTOKINAS
E ACTIVATO
R
COMPLE
X (APSAC
, ANISTREPLASE
) 189
1. RANDOMIZE
D CLINICAL TRIALS 189
2. PRE-HOSPITA
L TREATMEN
T 189
LIST OF ABBREVIATION
S 193
REFERENCE
S 193
CHAPTE
R 8
TISSUE-TYPE PLASMINOGEN ACTIVATOR (TPA
)
D.
COLLEN
.
WITH 2 FIGURE
S 209
A
. INTRODUCTIO
N 209
B. DEVELOPMEN
T OF TPA AS A THROMBOLYTI
C AGEN
T 212
I. ISOLATIO
N AN
D PURIFICATION OF TPA 212
II. CLONING AN
D EXPRESSIO
N OF TH
E TPA CDN
A 214
III
. EXPERIMENTA
L CORONAR
Y THROMBOSI
S MODEL
S FOR AM
I 215
IV. FIRST ADMINISTRATIO
N OF TPA T
O PATIENT
S WITH AM
I 215
C. CLINICAL TRIALS WITH TPA IN AM
I 216
I. EARLY CLINICAL STUDIES IN AM
I 216
II. TPA TRIALS, 1986-1989 218
III
. TPA TRIALS, 1990-1995 220
IV. FURTHE
R ATTEMPT
S T
O IMPROV
E TH
E EFFICACY OF THROMBOLYSI
S
AND T
O REDUC
E TH
E INCIDENC
E OF REOCCLUSIO
N 221
LIST OF ABBREVIATION
S 222
REFERENCE
S 223
CONTENTS XVII
CHAPTE
R 9
UROKINASE AND SINGLE-CHAIN UROKINASE-TYPE PLASMINOGEN ACTIVATOR
(PRO-UROKINASE)
V.
GUREWICH
231
A
. HISTORY 231
B. NOMENCLATUR
E 232
C. BIOCHEMISTRY OF PRO-UK/U
K (SC-UPA/TC-UPA) 232
I. THE INTRINSIC ACTIVITY OF PRO-UK (SC-UPA) 233
II. FIBRINOLYSIS BY PRO-UK/U
K (SC-UPA/TC-UPA) 234
III. CONTRASTIN
G PROPERTIE
S OF PRO-UK AND TPA 235
IV. PRO-UK/U
K AND PLATELETS 237
D. PHARMACOKINETIC
S 238
E. CLINICAL STUDIES IN ACUT
E MYOCARDIAL INFARCTION 239
I. UROKINAS
E 239
1. CONTROLLED TRIALS OF UK VS CONTROL
S 239
2. PREHOSPITAL VS IN-HOSPITAL THROMBOLYSIS WITH UK 240
3. COMPARATIV
E TRIALS OF UK VS SK OR TPA 240
II. PRO-UROKINAS
E 241
1. EARLY DOSE-FINDING STUDIES 241
2. RANDOMIZE
D TRIALS OF PRO-UK VS SK 243
3. RANDOMIZE
D TRIAL OF PRO-U
K VS TPA 245
HI. NON-SPECIFIC PLASMINOGEN ACTIVATION 245
IV. COMBINATION
S OF PRO-U
K AND UK OR TPA 246
1. EARLY DOSE-FINDING STUDIES OF PRO-UK AND UK 246
2. EARLY DOSE-FINDING STUDIES OF PRO-UK AND TPA 247
3. LARGER CLINICAL TRIAL WITH PRO-UK AND TPA 247
V. BOLUS ADMINISTRATION OF PRO-UK 248
VI. HEPARI
N AND PRO-UK 248
F. SECOND GENERATIO
N PRO-UK 24S
G. CONCLUSIONS 249
LIST OF ABBREVIATION
S 251
REFERENCES 251
CHAPTE
R 10
COMPARATIVE EVALUATIONS OF TPA VS SK WITH PARTICULAR REFERENCE
TO THE GUSTO-I TRIAL
A.C.
CHI
L
AND E.J. TOI OT . WITH 1 FIGURE 261
A. INTRODUCTION 261
B. EVOLUTION OF THROMBOLYTIC THERAPIE
S 261
I. RATIONALE FOR THROMBOLYSIS 2M
II. EARLY ANGIOGRAPHIC PATENCY TRIALS. TPA VS SK 2M
III. ADJUNCTIVE THERAPIES
: HEPARIN AND ASPIRIN 263
I
V MAJOR COMPARATIV
E THROMBOLYTIC TRIALS 264
XVIII CONTENTS
C. THE GUSTO-
I TRIAL 268
I. DESIGN OF TH
E TRIAL 268
II
. PRIMAR
Y RESULT
S OF GUSTO-
I 271
III
. THE GUSTO-
I ANGIOGRAPHI
C SUBSTUDY 274
IV. FURTHE
R ANALYSIS OF GUSTO-
I RESULT
S 278
V. OTHE
R GUSTO-
I SUBSTUDIE
S 278
VI
. EPILOGU
E 281
LIST OF ABBREVIATION
S AN
D ACRONYM
S 281
REFERENCE
S 282
CHAPTE
R 11
CONJUNCTIVE THERAPY TO REDUC
E THE OCCURRENCE OF CORONARY
REOCCLUSION AFTER THROMBOLYTIC TREATMENT OF AMI
R.
HAYES,
R.
GALLO
,
V.
FUSTER,
AN
D J.
CHESEBRO.
WITH 8 FIGURE
S 287
A
. INTRODUCTIO
N 287
B. THE ROL
E OF THROMBI
N AN
D PLATELET
S IN THROMBU
S FORMATIO
N ...
. 287
C. EVIDENC
E FOR TH
E EFFICACY OF THROMBOLYTI
C THERAP
Y 289
I. IMPORTANC
E OF ACHIEVIN
G PATENC
Y OF TH
E INFARCT
RELATE
D ARTER
Y 290
II
. LIMITATION
S OF THROMBOLYTI
C THERAP
Y 292
III
. THE ROL
E OF PLATELET
S AN
D THROMBI
N IN RESISTANC
E 292
T
O THERAP
Y 292
1. THROMBI
N 292
2. PLATELET
S 295
D. ANTITHROMBOTI
C THERAP
Y 296
I. THROMBI
N INHIBITIO
N 296
1. HEPARI
N 296
2. LOW-MOLECULAR-WEIGHT HEPARI
N 300
3
. HIRUDI
N 301
4. HIRULO
G 304
5. ARGATROBA
N 304
6. EFEGATRA
N 305
II. ANTIPLATELE
T AGENT
S 305
1. ASPIRI
N 305
2. GLYCOPROTEI
N ILB/III
A ANTAGONIST
S 306
3. OTHE
R DRUG
S INHIBITIN
G PLATELE
T FUNCTIO
N 308
4. PHYSICAL COUJUNCTIV
E THERAP
Y 309
E
. OUTLOO
K 309
LIST OF ABBREVIATION
S 309
REFERENCE
S 311
CONTENTS XIX
THROMBOLYTIC TREATMENT OF OTHER CLINICAL THROMBOEMBOLIC CONDITIONS
CHAPTE
R 12
NEW CONCEPTS IN THROMBOLYSIS OF PULMONARY EMBOLISM
A.A
.
SASAHARA
AND G.V.R.K.
SHARMA.
WITH 5 FIGURES 325
A
. INTRODUCTIO
N 325
B. TREATMEN
T WITH THROMBOLYTIC THERAP
Y 327
C. ESTABLISHED CLINICAL EFFECT OF THROMBOLYTIC THERAPY 328
I. THROMBOLYTIC AGENT
S HASTE
N THROMBOEMBOLI
C
RESOLUTION 328
II. RESULTS OF PULMONARY ANGIOGRAPHY 328
III. RESULTS OF PERFUSION LUNG SCAN 328
IV. HEMODYNAMI
C OBSERVATION
S 329
V. THROMBOLYTIC THERAPY REMOVES PULMONARY
THROMBOEMBOL
I MORE COMPLETELY THAN
HEPARI
N THERAP
Y 330
VI
. THROMBOLYTIC AGENTS HASTE
N DISSOLUTION OF THROMBI
IN TH
E VENOUS SYSTEM OF THE LEGS 332
VII
. THROMBOLYTIC THERAPY CAN BE ADMINISTERE
D SAFELY 332
D. POSSIBLE UNESTABLISHE
D CLINICAL EFFECTS 334
I. THROMBOLYTIC AGENT
S MAY DECREAS
E MORTALITY FROM
PULMONARY EMBOLISM 334
II. THROMBOLYTIC THERAP
Y IMPROVE
S LONG-TERM
HEMODYNAMI
C STATUS 335
E. NEW THROMBOLYTIC REGIMENS 336
F. SURGICAL THERAP
Y 341
G. ADJUNCTIVE THERAP
Y 343
LIST OF ABBREVIATION
S 343
REFERENCES 344
CHAPTE
R 13
DEE
P VENOUS THROMBOSIS
H.
BOUNAMEAUX
349
A. INTRODUCTIO
N 349
B. TREATMEN
T REGIMENS 349
C. IMMEDIAT
E EFFECTS OF THROMBOLYTIC THERAP
Y OF DVT:
THE DEFINITE RISK 350
D. LATE EFFECTS OF THROMBOLYTIC THERAPY OF DVT:
THE POTENTIAL BENEFIT 352
E. THE BENEFIT-TO-RISK BALANCE 353
F. HOW T
O REDUCE THE RISK AND IMPROVE THE BENEFIT? 354
I. REDUCING HCMORRHAGI
C RISK 354
II. IMPROVING THROMBOLYTIC EFFICACY 355
G. MISCELLANEOUS VENOUS INDICATIONS 356
XX CONTENTS
I. PHLEGMASI
A CAERULE
A DOLEN
S 356
II
. SUPERIO
R O
R INFERIOR VENA CAVA SYNDROM
E 356
III
. DEE
P VENOU
S THROMBOSI
S OF TH
E UPPE
R LIMBS 356
IV. VENOUS THROMBOSI
S OF UNUSUA
L LOCALIZATIO
N 356
V. THROMBOSI
S OF CENTRA
L VENOUS CATHETER
S 357
H
. LABORATOR
Y MONITORIN
G 357
I. TREATMEN
T OF BLEEDIN
G 358
J. CONCLUSIONS AN
D PERSPECTIVE
S 358
LIST OF ABBREVIATION
S AN
D ACRONYM
S 359
REFERENCE
S 359
CHAPTE
R 14
PERIPHERAL ARTERIAL OCCLUSIONS
D.C.
BERRIDGE
363
A
. INTRODUCTIO
N 363
B. CURREN
T INDICATION
S 364
C. CONTRA-INDICATION
S 366
D. DRUG
S AVAILABLE 367
I. STREPTOKINAS
E 367
II. APSAC
, ANISTREPLAS
E (ACYLATED-PLASMINOGEN
-
STREPTOKINASE-ACTIVATO
R COMPLEX
) 367
III
. UROKINAS
E AN
D PRO-UROKINAS
E 368
IV. RECOMBINAN
T TISSUE PLASMINOGE
N ACTIVATO
R (TPA
) 368
V. STAPHYLOKINAS
E 368
E
. TECHNIQUES USE
D 368
I. SYSTEMIC ADMINISTRATIO
N 368
II. LOCAL LOW-DOS
E INTRA-THROMBOTI
C ADMINISTRATIO
N 369
III
. HIGH-DOS
E BOLU
S 369
IV. PULSE-SPRA
Y ADMINISTRATIO
N 370
V. ENCLOSE
D THROMBOLYSI
S 371
VI
. INTRA-OPERATIV
E LYSIS 372
F. COMPARATIV
E RESULT
S 373
I. STREPTOKINAS
E VS RECOMBINAN
T TISSUE
PLASMINOGE
N ACTIVATO
R 373
II
. UK VS RECOMBINAN
T TISSUE PLASMINOGE
N ACTIVATO
R 374
III
. PRO-U
K VS. UK 374
IV. SURGERY VS THROMBOLYSI
S 374
G. LONG-TERM RESULT
S 378
H. ADJUVAN
T TREATMEN
T 378
I. COMPLICATION
S 379
I. MAJOR HEMORRHAG
E 379
II. MINOR HEMORRHAG
E 379
III
. CEREBROVASCULA
R ACCIDEN
T 379
IV. DISTAL EMBOLIZATIO
N 380
V. PERICATHETE
R THROMBOSI
S 380
CONTENTS XXI
VI
. ALLERGIC REACTION
S 380
VII
. OTHE
R COMPLICATIONS 380
J. SUMMARY 381
LIST OF ABBREVIATION
S AND ACRONYMS 381
REFERENCES 381
CHAPTE
R 15
THROMBOTIC CEREBROVASCULAR DISEASE
G.J.
DEL ZOPPO
387
A
. INTRODUCTIO
N 387
B. FOCAL CEREBRA
L ISCHEMIA 388
I. CONSIDERATION
S FOR TISSUE SALVAGE 388
II. HEMORRHAGI
C TRANSFORMATION 389
III
. NEUROLOGICAL OUTCOM
E 390
C. PLASMINOGEN ACTIVATOR
S IN FOCAL CEREBROVASCULA
R ISCHEMIA 392
I. COMPLETE
D STROK
E 393
II. ACUT
E STROKE 394
1. CAROTID TERRITORY ISCHEMIA 394
A) ANGIOGRAPHY-CONTROLLE
D TRIALS 394
A)
INTRA-ARTERIA
L LOCAL INFUSION 394
P)
INTRAVENOU
S (SYSTEMIC) INFUSION 397
Y)
SINGLE PHOTON-EMISSION COMPUTE
D
TOMOGRAPHY (SPECT
) 400
B) SYMPTON-BASED (CLINICAL OUTCOME
) TRIALS 400
2. VERTEBROBASILA
R TERRITORY ISCHEMIA 408
A) ANGIOGRAPHY-CONTROLLE
D TRIALS 408
A)
INTRA-ARTERIA
L (LOCAL) INFUSION 408
P)
INTRAVENOU
S (SYSTEMIC) INFUSION 409
III.
OTHE
R CONDITIONS 409
1. RETINAL VASCULAR OCCLUSION 409
2. DURAL SINUS THROMBOSI
S 410
D. ONGOING STROK
E TRIALS WITH THROMBOLYTIC AGENT
S 410
E. CONCLUSION 411
LIST OF ABBREVIATION
S AND ACRONYMS 411
REFERENCES 412
THROMBOLYTIC AGENTS IN DEVELOPMENT, BIOCHEMISTRY, PHARMACOLOGY
-
EFFICACY IN ANIMAL EXPERIMENTS AND FIRST CLINICAL TRIALS
CHAPTE
R 16
STAPHYLOKINASE
H.R.
LIINEN
AND D. CO
N
IN
.
WITH 3 FIGURES 425
A. INTRODUCTIO
N 425
B. GEN
E AND PROTEIN STRUCTURE OF STAPHYLOKINASE 426
XXII CONTENTS
I. PRODUCTIO
N OF STAPHYLOKINAS
E 426
II
. GEN
E STRUCTUR
E OF STAPHYLOKINAS
E 427
III
. PROTEI
N STRUCTUR
E OF STAPHYLOKINAS
E 428
C. PLASMINOGE
N ACTIVATIO
N BY STAPHYLOKINAS
E 429
I. INTERACTIO
N WITH PLASMIN(OGEN
) 429
II
. KINETICS OF PLASMINOGE
N ACTIVATIO
N 431
III
. MECHANIS
M OF PLASMINOGE
N ACTIVATIO
N 431
D. FIBRIN-SPECIFICITY OF STAPHYLOKINAS
E 432
I. INHIBITIO
N OF PLASMIN-STAPHYLOKINAS
E COMPLE
X BY
A
2
-ANTIPLASMI
N 432
II
. EFFECT OF FIBRIN ON PLASMINOGE
N ACTIVATIO
N
BY STAPHYLOKINAS
E 433
III
. MOLECULA
R MECHANIS
M OF FIBRIN-SPECIFICITY IN PLASMA 433
E
. FIBRINOLYTIC PROPERTIE
S OF STAPHYLOKINAS
E IN PLASM
A IN VITR
O 435
I. FIBRINOLYTIC POTENCY AN
D FIBRIN-SPECIFICITY 435
II
. SPECIES-SPECIFICITY 437
F. THROMBOLYTI
C PROPERTIE
S OF STAPHYLOKINAS
E IN ANIMA
L MODEL
S ...
. 437
I. HAMSTER
S WITH PULMONAR
Y EMBOLIS
M 437
II
. RABBIT
S WITH JUGULA
R VEIN THROMBOSI
S 438
III
. RABBIT
S WITH ARTERIA
L THROMBOSI
S 438
IV. RABBI
T EMBOLI
C STROK
E MODE
L 438
V. BABOON
S WITH VENOU
S AN
D ARTERIA
L THROMBOSI
S 438
G. THROMBOLYTI
C PROPERTIE
S OF STAPHYLOKINAS
E IN PATIENT
S 439
I. ACUT
E MYOCARDIA
L INFARCTIO
N 439
II
. PERIPHERA
L ARTERIA
L OCCLUSION 440
H. PHARMACOKINETI
C PROPERTIE
S OF STAPHYLOKINAS
E 441
I. IN ANIMA
L MODEL
S 441
II
. IN PATIENT
S 441
I. IMMUNOGENICIT
Y OF STAPHYLOKINAS
E 442
I. IN ANIMA
L MODEL
S 442
II. IN PATIENT
S 442
III.
ATTEMPT
S T
O REDUC
E IMMUNOGENICIT
Y 443
J. CONCLUSION
S 443
LIST OF ABBREVIATION
S AN
D ACRONYM
S 444
REFERENCE
S 444
CHAPTE
R 17
DESMODUS
ROTUNDUS
(COMMON VAMPIRE BAT)
SALIVARY PLASMINOGEN ACTIVATOR
W.-D.
SCHLEUNING
AN
D P.
DONNER
.
WITH 5 FIGURES 451
A. INTRODUCTIO
N 451
B. NATURA
L HISTOR
Y OF VAMPIRE BATS 453
C. BIOCHEMISTRY 453
I. PURIFICATION 453
CONTENTS XXIII
II
. CLONING AND EXPRESSION 454
III
. DSPA GEN
E EXPRESSION IN HETEREOLOGOU
S HOST CELLS 455
IV. THREE-DIMENSIONA
L STRUCTUR
E OF THE PROTEAS
E DOMAIN 456
V. ENZYMOLOGY 456
D. PHARMACOLOGY 459
I. IN VITRO CLOT LYSIS 459
II
. CAROTI
D AND FEMORAL ARTER
Y THROMBOSIS IN RABBITS 461
III
. MYOCARDIAL INFARCTION IN DOGS 461
IV. EXPERIMENTA
L PULMONARY EMBOLISMS IN RATS 462
V. BLEEDING MODELS 463
E. PHARMACOKINETICS 464
F. TOXICOLOGY 466
G. PHASE I CLINICAL STUDIES 466
H. PHASE IB CLINICAL STUDIES 467
I. CONCLUSIONS AND PERSPECTIVES 467
LIST OF ABBREVIATION
S AND ACRONYM
S 468
REFERENCE
S 468
CHAPTE
R 18
THROMBUS-TARGETING OF PLASMINOGEN ACTIVATORS
C.
BODE
,
K.
PETER,
M.S.
RUNGE
,
AND E
.
HABER
473
A
. INTRODUCTIO
N 473
B. THE PRINCIPL
E OF ANTIBOD
Y TARGETIN
G 474
I. ANTIFIBRIN ANTIBODIE
S 474
II
. ANTIPLATELE
T ANTIBODIE
S 474
III
. CHEMICA
L CONJUGATE
S OR RECOMBINAN
T FUSION PROTEIN
S ...
. 475
C. SYNTHESIS, PURIFICATION, AND CHARACTERIZATIO
N OF CHEMICA
L
ANTIBODY-PLASMINOGE
N ACTIVATO
R CONJUGATE
S 475
I. SYNTHESIS 475
II
. PURIFICATION 476
III
. CHARACTERIZATIO
N 476
1. ANTIFIBRIN-U
K CONJUGATE
S 477
2. ANTIFIBRIN-TPA CONJUGATE
S 477
3. ANTIFIBRIN-SCUPA CONJUGATE
S 478
4. ANTIPLATELET-U
K CONJUGATE
S 478
5. ANTIPLATELET-SCUP
A CONJUGATE
S 478
D. TARGETIN
G WITH BIFUNCTIONAL ANTIBODIE
S 479
I. PRINCIPAL CONSIDERATION
S 479
II. BISPECIFIC IGG (INTAC
T ANTIBODIES
) 479
III. BISPECIFIC (FAB )
2 480
IV. BISPECIFIC ANTIBODIE
S BY HYBRID-HYBRIDOM
A TECHNIQUE ...
. 480
V. DOUBL
E TARGETIN
G 481
E. EXPRESSIO
N AND CHARACTERIZATIO
N OF RECOMBINAN
T ANTITIBRIN
-
PLASMINOGEN ACTIVATO
R FUSION PROTEIN
S 481
XXIV CONTENTS
I. ANTIFIBRIN-SK CONSTRUCTS 481
II. ANTIFIBRIN-TPA CONSTRUCTS 481
III. ANTIFIBRIN-SCUPA CONSTRUCTS 482
F. OTHER APPROACHES OF TARGETING PLASMINOGEN ACTIVATORS
TO THROMBI 484
G. TARGETING THE THROMBIN INHIBITOR HIRUDIN TO FIBRIN 486
I. GENERAL CONSIDERATIONS 486
II. CHEMICAL CONJUGATES 486
III. RECOMBINANT FUSION PROTEIN 486
H. CONCLUSION AND OUTLOOK 487
LIST OF ABBREVIATIONS AND ACRONYMS 488
REFERENCES 488
CHAPTE
R 19
THE HUNT FOR THE IDEAL THROMBOLYTIC AGENT:
MUTANTS OF TPA AND UPA, CHIMERA OF BOTH MOLECULES, FIBROLASE
M.
VERSTRAETE.
WITH 3 FIGURES 493
A. MUTANTS AND VARIANTS OF SINGLE-CHAIN UROKINASE-TYPE
PLASMINOGEN ACTIVATOR 493
I. PLASMIN-RESISTANT MUTANTS OF SC-UPA 493
II. LOW-MOLECULAR-WEIGHT SC-UPA 493
III. MUTANT OF SC-UPA RESISTANT TO PAI-1 494
B. MUTANTS OF TISSUE-TYPE PLASMINOGEN ACTIVATOR (TPA) 494
I. MUTANTS WITH MODIFIED EPIDERMA
L GROWTH
FACTOR DOMAIN 494
II. MUTANTS WITH MODIFIED OR DELETED FINGER DOMAIN 495
III. DELETION OF THE FINGER AND EPIDERMAL GROWTH
FACTOR DOMAINS 495
IV. DELETION OF THE EPIDERMAL GROWTH FACTOR AND FINGER
DOMAINS AND OF GLYCOSYLATION SITES 496
V. MUTANTS CONSISTING OF KRINGLE 2 AND THE
PROTEASE DOMAIN 496
VI. MUTANT CONSISTING OF KRINGLE 2 WITH POINT MUTATION
IN LINKAGE TO PROTEASE LIGHT CHAIN 501
VII. MUTANT WITH MODIFICATIONS IN KRINGLE 1 503
VII. RECOMBINANT TNK-TPA 503
IX. UNGLYCOSYLATED PROTEASE DOMAINS OF TPA 510
C. CHIMERIC PLASMINOGEN ACTIVATORS 510
D. FIBROLASE 512
E. OTHE
R FIBRINOLYTIC AGENTS 512
LIST OF ABBREVIATIONS AND ACRONYMS 512
REFERENCES 513
CONTENTS XXV
CHAPTER 20
AGENTS WHICH INCREASE SYNTHESIS AND RELEASE OF TISSUE-TYPE
PLASMINOGEN ACTIVATOR
T.
KOOISTRA
AND J.J.
EMEIS
.
WITH 3 FIGURES 521
A. INTRODUCTIO
N 521
I. THE PLASMINOGEN/PLASMIN SYSTEM 521
II. INTRAVASCULAR FIBRINOLYSIS 521
III. TISSUE-TYPE PLASMINOGEN ACTIVATO
R (TPA) IN
THE CIRCULATION 522
IV. INVOLVEMENT OF THE ENDOTHELIU
M IN PLASMA FIBRINOLYSIS ...
. 523
B. REGULATION OF CONSTITUTIVE TPA SYNTHESIS 524
I. GENERA
L 524
II. INTRACELLULA
R SIGNALING AND ACTIVATION OF PROTEIN
KINASE C 525
III. RETINOID
S 526
IV. STEROI
D HORMONE
S 528
V. SODIUM BUTYRAT
E AND OTHE
R INHIBITOR
S OF HISTONE
DEACETYLASE 529
VI
. TRIAZOLOBENZODIAZEPINES 530
C. REGULATE
D SECRETION OF TPA 531
I. GENERA
L 531
II. THE ENDOTHELIA
L TPA STORAGE COMPARTMEN
T AND THE
CIRCULATORY REGULATION OF TPA 532
III. CELLULAR MECHANISMS INVOLVED IN REGULATED
TPA SECRETION 535
IV. COMPOUND
S AFFECTING REGULATED TPA SECRETION IN MAN ...
. 536
1. THE OCCURRENCE OF REGULATED TPA SECRETION IN MAN. . . . 536
2. ADRENERGI
C AGENT
S 538
3. VASOPRESSIN 539
4. DDAV
P 539
5. ACETYLCHOLINE AND METHACHOLINE 541
6. BRADYKININ AND SUBSTANCE P 541
7. COAGULATION ACTIVATION PRODUCTS 542
8. CAM
P 542
9. MISCELLANEOUS COMPOUND
S 542
10. ABNORMA
L RELEASE OF TPA 543
D. INCREASE OF TPA ACTIVITY BY INHIBITION OF PAI-1 543
LIST OF ABBREVIATION
S AND SYMBOLS 544
REFERENCES 544
XXVI CONTENTS
AUTIFIBRINOLYTIC AGENTS
CHAPTER 21
STRUCTURE, PHARMACOLOGY, AND CLINICAL USE OF ANTIFIBRINOLYTIC AGENTS
CM
.
SAMAMA,
W.
DIETRICH,
J.
HORROW,
O.
TABY,
AND M.M.
SAMAMA.
WITH 3 FIGURES 559
A. INTRODUCTION 559
B. PHARMACOLOGY AND CLINICAL USE OF EACA AND TA 559
I. E-AMINOCAPROIC ACID (EACA) 561
1. PHARMACOLOGY 561
2. NON-CARDIAC SURGERY 561
A) UROLOGIC SURGERY 561
B) ORAL SURGERY 561
C) LIVER TRANSPLANTATION 562
3. USE IN CARDIAC SURGERY 562
4. ADVERSE EFFECTS 562
II. TRANEXAMIC ACID 564
1. PHARMACOLOGY 564
2. NONSURGICAL APPLICATIONS 564
3. NONCARDIAC SURGERY 565
4. CARDIAC SURGERY 565
5. ADVERSE EFFECTS 565
C. PHARMACOLOGY OF APROTININ 567
I. STRUCTURE 567
II. PHARMACOLOGY 567
III. PHARMACOKINETICS 568
IV. CLINICAL USE 568
1. HISTORY 568
2. MODE OF ACTION OF APROTININ
(CLINICAL POINT OF VIEW) 569
3. EFFICACY OF APROTININ TREATMENT 571
4. MISCELLANEOUS USES 572
A) ORTHOTOPIC LIVER TRANSPLANTATION (OLT) AND
ELECTIVE LIVER RESECTION 572
B) ORTHOPEDIC SURGERY 574
5. SIDE EFFECTS OF APROTININ THERAPY 574
D. CONCLUSION 575
LIST OF ABBREVIATIONS AND ACRONYMS 576
REFERENCES 576
SUBJECT INDEX
587
|
any_adam_object | 1 |
author_GND | (DE-588)122154223 |
building | Verbundindex |
bvnumber | BV013337254 |
classification_rvk | XI 1701 |
ctrlnum | (OCoLC)643203049 (DE-599)BVBBV013337254 |
discipline | Medizin |
format | Book |
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genre | (DE-588)4143413-4 Aufsatzsammlung gnd-content |
genre_facet | Aufsatzsammlung |
id | DE-604.BV013337254 |
illustrated | Illustrated |
indexdate | 2024-12-23T15:25:54Z |
institution | BVB |
isbn | 3540661263 |
language | English |
oai_aleph_id | oai:aleph.bib-bvb.de:BVB01-009095375 |
oclc_num | 643203049 |
open_access_boolean | |
owner | DE-355 DE-BY-UBR DE-19 DE-BY-UBM DE-12 DE-188 DE-578 |
owner_facet | DE-355 DE-BY-UBR DE-19 DE-BY-UBM DE-12 DE-188 DE-578 |
physical | XXVI, 599 S. Ill., graph. Darst. |
publishDate | 2001 |
publishDateSearch | 2001 |
publishDateSort | 2001 |
publisher | Springer |
record_format | marc |
series | Handbook of experimental pharmacology |
series2 | Handbook of experimental pharmacology |
spellingShingle | Fibrinolytics and antifibrinolytics [with 50 tables] Handbook of experimental pharmacology Fibrinolytic Agents cabt Fibrinolytikum (DE-588)4017042-1 gnd Pharmakologie (DE-588)4045687-0 gnd Antifibrinolytikum (DE-588)4142667-8 gnd |
subject_GND | (DE-588)4017042-1 (DE-588)4045687-0 (DE-588)4142667-8 (DE-588)4143413-4 |
title | Fibrinolytics and antifibrinolytics [with 50 tables] |
title_auth | Fibrinolytics and antifibrinolytics [with 50 tables] |
title_exact_search | Fibrinolytics and antifibrinolytics [with 50 tables] |
title_full | Fibrinolytics and antifibrinolytics [with 50 tables] contributors F. Bachmann ... Ed.: F. Bachmann |
title_fullStr | Fibrinolytics and antifibrinolytics [with 50 tables] contributors F. Bachmann ... Ed.: F. Bachmann |
title_full_unstemmed | Fibrinolytics and antifibrinolytics [with 50 tables] contributors F. Bachmann ... Ed.: F. Bachmann |
title_short | Fibrinolytics and antifibrinolytics |
title_sort | fibrinolytics and antifibrinolytics with 50 tables |
title_sub | [with 50 tables] |
topic | Fibrinolytic Agents cabt Fibrinolytikum (DE-588)4017042-1 gnd Pharmakologie (DE-588)4045687-0 gnd Antifibrinolytikum (DE-588)4142667-8 gnd |
topic_facet | Fibrinolytic Agents Fibrinolytikum Pharmakologie Antifibrinolytikum Aufsatzsammlung |
url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=009095375&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
volume_link | (DE-604)BV002390716 |
work_keys_str_mv | AT bachmannfedor fibrinolyticsandantifibrinolyticswith50tables |