Thieme: Color Atlas of Pharmacology

374 Subject Index 

Subject Index 

A 

Abarelix 230 

Abatacept 288 

Abciximab 150, 151 

ABC transporter 28, 29, 34 

Abel, John J. 3 

Absorption of drugs 12,13, 22, 23 

exponential characteristics 46, 47 

oral administration 12, 13, 44, 45, 48 

velocity 48 

Absorption quotient 22 

Acamprosate 304 

Acarbose 246, 247 

Accumulation, drug 50, 51, 52–53 

Accumulation equilibrium 50, 51 

Acebutolol 11 

ACE inhibitors 120, 126, 127, 158 

congestive heart failure 316,317 

hypertension 308, 309 

Acetaldehyde 304, 305 

Acetaminophen 184, 185 

intoxication/poisoning 294 

in migraine 326, 327 

Acetazolamide 162, 163 

Acetylcholine (ACh) 88, 102, 104, 107 

actions 104, 105, 174, 300, 301 

binding to nicotinic receptor 66, 67 

degradation 104,105, 106, 107 

as neurotransmitter 102, 104, 174 

receptors 104, 105, 174, 300 

see also Muscarinic ACh receptors; Nicotinic 

ACh receptors 

release 104, 105, 108, 109, 174, 175 

storage 104, 174 

structure 105, 297 

synthesis 104, 174 

Acetylcholinesterase 104, 105, 106, 176 

inhibitors 106, 178 

phosphorylated, reactivators 296, 297 

Acetylcoenzyme A104 

N-Acetylcysteine 294 

Acetylsalicylic acid 6, 142, 150, 185 

absorption, dosage and actions 186 

adverse effects 186 

contraindications 144 

in/after myocardial infarction 314,315 

migraine 326, 327 

platelet aggregation inhibition 150, 151 

presystemic effects 150 

N-Acetyltransferase 280 

Aciclovir 269, 270, 271 

Acid–base balance 168 

Acid-labile drugs 12 

Acid neutralization 168 

Acrolein 282 

ACTH 220, 221, 226, 228 

Action potential 136, 137 

cardiac 136, 137 

muscle 176, 177, 178 

Active principle 4, 10 

Active secretion 42, 43 

Active transport 26, 27 

Acute coronary syndrome 314–315 

see also Myocardial infarction 

Acylaminopenicillins 254, 255 

Acyl transferases 40 

Adalimumab 344, 345 

Addiction 

alcohol 304 

amphetamines 96 

opioids 194,196, 199 

Addison disease 226 

Adefovir dipivoxil 270 

Adenohypophyseal hormones 112, 220, 221 

Adenylate cyclase 68, 69 

Aδ-fibers 180, 188 

Adipokines 338 

Administration of drugs 12–19 

buccal/sublingual 18,19, 22 

dermatological 16–17 

inhalation 14–15,18, 19 

oral 12–13,18, 19,44, 45 

parenteral 44 

routes 18, 19 

ADP receptor antagonists 150, 151 

Adrenal cortex 226 

Adrenaline see Epinephrine 

Adrenergic synapse 88, 89 

Adrenoceptors 88, 89 

subtypes 90–91 

subtype selectivity, sympathomimetics 94, 95 

α-Adrenoceptors, agonists/antagonists 98, 99 

α 1-Adrenoceptors 90, 91 

blockers 98, 99 

sympathomimetics 98, 99 

α2-Adrenoceptors 88, 90, 91 

agonists/sympathomimetics 98, 99 

β-Adrenoceptors 

antagonists/sympatholytics see β-blockers 

genetic variants 80 

receptor subtypes 100, 101 

β2-Adrenoceptors 90, 91 

agonists 90, 128, 340, 342 

epinephrine interaction 94, 95 

Adrenocortical insufficiency 226 

Adrenocorticotropic hormone (ACTH) 220, 221,226, 

228 

Adriamycin (doxorubicin) 282 

Adverse drug effects (ADEs) 8, 72–79 

allergy/hypersensitivity reactions 74–75 

cutaneous reactions 76–77 

increased sensitivity 72, 73 

lack of selectivity 72, 73 

overdosage 72, 73 

in pregnancy/lactation 78–79 

see also individual drugs 

Aerosols 14 

Affinity of drug 58, 62 

enantioselectivity 64, 65 

Afterload 112,124, 126, 130, 310 

Agonists 62–63, 68, 69 

prolonged stimulation by 92, 93 

aus: Luellmann, Color Atlas of Pharmacology (ISBN 9783137817048) © 2011 Georg Thieme Verlag KG

Agranulocytosis 184, 218, 224 

AIDS see entries beginning HIV 

Akathisia 218 

Albumin 32 

Alcohol 304 

abuse 304–305 

elimination, time course 46, 70 

metabolism 304 

tinctures using 4 

Alcohol dehydrogenase 46, 70, 304 

Aldesleukin (interleukin 2) 284 

Aldosterone 120, 160, 165, 166, 226 

antagonists 164, 165, 316, 317 

structure 227 

Alendronate 334, 335 

Alfuzosin 98 

Aliskiren 126 

Alkylating cytostatic drugs 282, 283 

Alkylation reactions 36, 37 

Allergy (drug-induced) 74–75, 76 

penicillin 252, 253 

Allergy mediators, antagonists 340, 341 

Allethrin 274 

Allopurinol 282, 336, 337 

Allosteric antagonism 62 

Allosteric synergism 62 

Allyl amines 266 

α-Phase (distribution phase) 48 

Alteplase 148,149 

Alzheimer disease 106 

Amantadine 270, 320, 321 

Amebic infections 258, 259, 278 

Amfebutamon (bupropion) 300 

Amiloride 164,165 

Amino acids 118, 119 

p-Aminobenzoic acid (PABA) 256, 257, 265 

γ-Aminobutyric acid see GABA 

ε-Aminocaproic acid 148 

Aminoglycosides 260, 261, 262, 263 

p-Aminomethylbenzoic acid (PAMBA) 148 

6-Aminopenicillanic acid 252, 253 

Amiodarone 136 

Amitriptyline 212, 213 

Amlodipine 124 

Amorolfine 266 

Amoxicillin 254, 255 

AMPA receptors 118, 119 

Amphetamine 96, 210, 211, 298 

Amphiphilic structure, local anesthetics 188, 189, 

190, 192, 193 

Amphotericin B266, 267 

Ampicillin 254, 255 

Amprenavir 272 

Anabolic steroids 230–231 

Anakinra 288, 344, 345 

Analgesics/analgesia 181, 184–185 

antipyretic 184, 185, 318 

NSAIDs 184, 185, 187 

opioids see Opioids 

sites ofaction 181 

Analogue substances 10 

Anandamide 118,298, 339 

Anaphylactic reaction 74, 75, 76 

Anaphylactic shock 74,340 

Subject Index 375 

Anastrozole 238, 239 

Androgens 230–231 

receptors and antagonists 230 

Androstenedione 238, 239 

Anemia, drug treatment 138–141 

Anesthesia 178, 200 

balanced 200, 201 

general 200–201 

see also General anesthetics 

local see Local anesthetics 

regional (spinal) 200 

Angina pectoris 122, 310–311 

Angiogenesis inhibitors 286, 287 

Angiotensin-converting enzyme (ACE) 37,126, 158, 

308 

inhibitors see ACE inhibitors 

Angiotensin II 37,126, 158 

receptors 126 

Angiotensin II receptor antagonists 120, 121,126, 

127, 316, 317 

Animal experiments 8, 9 

Anisostreptase 148, 149 

Antacids 140, 168 

Antagonism 

allosteric 62 

functional 62 

Antagonists 62, 63 

Anthelmintics 274, 275 

Anthracycline antibiotics 282 

Anthraquinone derivatives 170, 173 

Antiallergic therapy 340–341 

Antiandrogens 230–231 

Antianemics 138–141 

Antianginal drugs 122, 123, 312–313 

classes 312, 313 

use, acute and prophylactic 122, 312 

Antiarrhythmic drugs 124, 134–135 

in cardiac glycoside intoxication 133 

K + channel blocking 136, 137 

of local anesthetic type 134, 135 

of Na + channel-blocking type 134, 135, 136–137 

Antibacterial drugs (antibiotics) 250–265 

adverse effects 252, 254, 256, 258, 260, 262 

bactericidal effect 250, 251, 252 

bacteriostatic effect 250, 251, 256 

broad-/narrow-spectrum 250 

cell growth inhibition 256–257 

cell wall synthesis inhibitors 252–255 

colitis due to 254 

cytostatic 282 

DNA function inhibitors 258–259 

in inflammatory bowel disease 346 

mechanism of action 250, 251 

pore formers 256, 257 

protein synthesis inhibitors 260–261 

resistance to 250, 251 

in septic shock 318 

tetrahydrofolate synthesis inhibitors 256, 257 

Antibodies 74,288, 289 

Anticancer drugs 280–287 

cell proliferation signaling interference 284–285 

resistance 286, 287 

supportive therapy 282 

targeted pharmacotherapy 286, 287 

see also Cytostatic agents 



Anticholinergics 320 

Anticoagulants, oral 144, 145 

Anticonvulsants see Antiepileptic drugs 

Antidepressants 210–213 


latency and mechanism of action 210, 211 

SSRIs 116,210, 212, 213 

tricyclic 210, 212, 213 

Antidiabetic drugs, oral 246–247 

Antidiarrheal agents 172–173 

Antidiuretic hormone (ADH; vasopressin) 160, 164, 

165, 220, 221 

deficiency/excess 166 

Antidotes 294–297 

Antiemetics 112, 328–329 

ondansetron 116, 117, 282 

Antiepileptic drugs 175, 322–325 


indications 322, 323 

mechanism of action 322, 324, 325 

in pregnancy 78, 324 

Antiestrogen active principle 236, 237, 238 

Antifungal drugs 266–267 

Antigens 74,288, 289, 344, 346 

Antihistamines 114, 115, 168, 169 

antiemetic action 328, 329 

in atopy/allergies 340, 341 

in sleep disorders 330 

unwanted effects 114 

Antihypertensive agents 98,120, 308 

ACE inhibitors 308, 309 

β-blockers 308, 309 

calcium antagonists 124, 125, 308, 309 

diuretics 158, 308, 309 

Antileprotic drugs 264, 265 

Antimalarials 276–277 

Antimetabolites 266, 269 

virustatic 268, 269, 270 

Antimigraine therapy 326–327 

Antimycobacterial drugs 264–265 

Antiparasitic drugs 274–275 

Antiparkinsonian drugs 110, 112, 320–321 

Antiplatelet drugs 314 

see also Acetylsalicylic acid 

Antipsychotic drugs see Neuroleptics 

Antipyretic analgesics 184, 185, 318 

Antiretroviral drugs 272–273 

Antithrombin III 142, 146 

Antithrombotics 142–151 

fibrinolytics 148–149 

heparin 134, 142, 146–147 

hirudin 147 

platelet aggregation inhibitors 150–151 

vitamin Kantagonists 144–145 

Antithyroid drugs 224–225 

Antitubercular drugs 264, 265 

Antiviral drugs 268–273 

hepatitis viruses 270, 271 

herpes viruses 268, 270, 271 

influenza viruses 270, 271 

Anxiolytics 331 

Apomorphine 112 

Apoptosis 280, 335 

Apparent volume of distribution (Vapp) 30, 46 

Appetite center 338 

Appetite suppressants 338, 339 

Aprepitant 118, 282, 328, 329 

Aquaporins 26, 27,160, 164 

Arachidonic acid 182, 184, 187 

2-Arachidonylglycerol 298 

Arachnicides 274 

Area under plasma level–time curve (AUC) 48, 49 

Arecoline 106, 107 

Argabatroban 146 

Aripiprazole 218 

Aromatase 230, 231, 238, 239 

inhibitors 238–239 

Artemisinin derivatives 276, 277 

Arteriolar resistance 310 

Arteriolar vasodilators 120 

Arthus reaction 74 

Asthma see Bronchial asthma 

Atenolol 11, 100 

Atherosclerosis 154, 302, 308, 309, 314 

Atomoxetine 96 

Atopy 340–341 

Atorvastatin 28, 156 

Atosiban 128 

Atovaquone 276 

ATP-binding cassettes 28, 29, 34 

ATP-dependent transporter 26 

Atracurium 178, 179 

Atrial fibrillation 133, 134, 142 

Atrial flutter 134 

Atrioventricular (AV) node, drugs affecting 134, 135 

Atropa belladonna 6, 7, 109 

Atropine 6, 7, 110 


intoxication/poisoning 110 


organophosphate poisoning 296 

receptors 72 

Attention deficit hyperactivity disorder (ADHD) 97 

Autoantibodies 76 

Autoimmune disorders, treatment 288 

Autonomic nervous system (ANS) 86, 300, 301 

Autophosphorylation 284 

Axolemma 190, 191 

Axoplasm 190, 191 

Azathioprine 80, 282, 289, 290, 344, 346 

Azithromycin 262 

Azole antifungal drugs 266, 267 

Aztreonam 254, 255 

B 

Bacitracin 254 

Baclofen 174,175, 304 

Bacterial cell membrane, pore forming antibiotics 

256, 257 

Bacterial cell wall 252 

synthesis inhibitors 252–255 

Bacterial infections 250 

Bacterial infection treatment 250–265 

see also Antibacterial drugs (antibiotics) 

Bacterial replication 259 

Bactericidal effect 250, 251, 252 

Bacteriostatic effect 250, 251, 256 

Balanced anesthesia 200, 201 


Barbiturate 331 

Baroreceptor reflex 98, 99 

Basiliximab 288, 289 

Bateman function 48, 49 

Benign prostatic hypertrophy 98,110, 230 

Benzbromarone 336 

Benzocaine 192, 193 

Benzodiazepines 175, 206–209 

activity/effects 206 

antagonists 206, 207 

biotransformation 208, 209 

dependence potential 208 

epilepsy 322, 324, 325 

half-lives 208, 209 

hypnotic action 330, 331 

mechanism ofaction 206, 207 

pharmacokinetics 208–209 

prolonged use, effects 206 

Benzothiadiazines 162 

Benztropine 110, 111, 320, 321 

Benzyl benzoate 274, 275 

Benzylpenicillin see Penicillin G(benzylpenicillin) 

Berlin blue (ferric ferrocyanide) 296, 297 

β-Blockers 10,100–101 

adverse effects 100, 101 

angina pectoris 312, 313 

β1, in hypertension 308, 309 

congestive heart failure 316,317 

effect on heart 130 


migraine 326 

myocardial infarction 314 

selectivity 100, 101 

sinus tachycardia 134 

structures 11,101 

therapeutic effects 100,101 

in thyrotoxic crisis 224 

unwanted effects 100, 101 

β-Lactamases 252, 255 

β-Lactam ring/antibiotics see β-Lactam ring/ 

antibiotics 

β-Phase (elimination phase) 48 

Betaxolol 11 

Betel chewing 106 

Bevacizumab 284, 285, 286, 287 

Bicarbonate 162 

Biguanides 246, 247 

Bilharziasis 278, 279 

Biliary colic 108, 128 

Binding forces (drug–receptor) 60–61 

Bioallethrin 274 

Bioavailability 45, 48 

Bioequivalence 48 

Biogenic amines 112–119 

Biological weapons 296 

Biosimilars 10 

Biotransformation ofdrugs 34–35, 44, 76 

benzodiazepines 208, 209 

reactions 36–37 

Biperiden 320 

Bipolar disorder 210, 214 

Bisacodyl 170 

Bisoprolol 11, 100 

Bisphosphonates 334, 335 

Bivalirudin 146 

Bleeding, drug-induced 144, 146 

Bleomycin 282 

Blood–brain barrier 24, 25 

Bloodletting 294 

Blood loss, management 152, 153 

Blood pressure 308, 309 

Blood–tissue barriers 24–25, 30 

Blood transfusion 152, 153 

Blood volume 166 

B-lymphocytes 288, 289 

Bmax (maximum binding) 58 

Body mass index (BMI) 338, 339 

Body weight 30, 338 

Bone, structure/remodeling 334, 335 

Bone density 334, 335 

Bone marrow, erythropoiesis 138, 139 

Bone marrow depression 280, 282 

Bortezomib 284, 285 

Bosentan 120 

Botulinum toxin 178 

Breast cancer 236, 237, 238 

trastuzumab action 286, 287 

British Anti-Lewisite (BAL; dimercaprol) 294, 295 

Bromazepam 209 

Bromocriptine 128, 220, 320, 321 

Bronchial asthma 342–343 

β2-Sympathomimetics 128, 129, 340, 342, 343 

bronchodilators 128, 129 

drug action mechanisms 341 

glucocorticoids 44, 340, 342, 343 

pathophysiology 342, 343 

theophylline 129, 340 

treatment algorithm 342, 343 

Bronchial carcinoma 302, 303 

Bronchial epithelium 14,15 

Bronchial mucus 14 

Bronchial musculature 341 

Bronchial secretion, inhibition 108 

Bronchodilatation 90, 342, 343 

Bronchodilators 128, 129 

Brotizolam 330, 331 

Buccal route of administration 18, 19, 22 

Buchheim, Rudolf 3 

Budesonide 346 

Bufetonin 298 

Bulk laxatives 170 

Bupranolol 11 

Bupropion 300 

Buserelin 220, 230 

N-Butylscopolamine 108, 111, 128, 129 

Butyrophenones 216, 218, 219 

C 


Calcifediol 248 

Calcineurin 290 

inhibitors 289, 290, 291 

Calcitonin 248, 249, 334, 335 

Calcium (Ca 2+ ) 

chelation, tetracyclines 260, 262 

effect on clotting 142, 143 

electromechanical coupling 178, 248 

electrosecretory coupling 248 

heart conduction 130, 131, 132, 136, 137 



Calcium (Ca 2+ ) 

homeostasis, drugs maintaining 248–249 

normal levels 248 

parathyroid hormone effect 248, 249 

vitamin Dhormone action 248, 249 

Calcium antagonists (Ca 2+ channel blockers) 120, 

124–125 

angina pectoris 312, 313 

catamphiphillic 124, 125 

dihydropyridine derivatives 124, 125 

hypertension 308, 309 

vasoselective 124 

Calcium channels 92, 130 

Calcium chelators 142 

Calmodulin 90 

Cancer, drug treatment 280–287 

see also Anticancer drugs 

Candida albicans 266 

Cannabinoid(s) 298 

Cannabinoid receptors 298 

agonists and antagonists 298 

CB1 blockade 338, 339 

Canrenone 164 

Capillary endothelium 24, 42, 43 

Capsaicin 118 

Capsules 12,13 

Captopril 126 

Carbachol 106, 107 

Carbamates 106 

Carbamazepine 322, 323, 324 

Carbapenems 254, 255 

Carbetocin 128 

Carbidopa 320, 321 

Carbimazole 225 

Carbonic anhydrase (CAH) inhibitor 162, 163 

Carboplatin 282 

Carcinogenic effects 280 

Cardiac arrest 110,134 

Cardiac arrhythmia, drug-induced 132, 262 

Cardiac catheterization 314, 315 

Cardiac drugs 130–137 

Cardiac failure see Heart failure 

Cardiac glycosides 130, 132–133 

atrial flutter/fibrillation 133, 134 

congestive heart failure 316 

intoxication 132, 133 

Cardiac impulse 134, 135 

Cardiac inhibition, by local anesthetics 192 

Cardioacceleration 110 

Cardiogenic shock 318 

Cardiosteroids 132–133 

Cardiostimulation 90 

Cardiovascular disease 308 

Carrier proteins 22, 26, 27, 28 

Carteolol 11 

Carticaine 192, 193 

Carvedilol 100 

Case–control study 82 

Caspofungin 266, 267 

Castor oil 170 

Catecholamine(s) 

actions 90–91 

cardiac effects 91, 92 

controlled-volume therapy 318 

effects on smooth muscle 90, 91 

low lipophilicity 94 

metabolic effects 92, 93 

see also Dopamine; Epinephrine; Norepinephrine 

Catecholamine O-methyltransferase (COMT) 88, 94, 

95, 113 


CD 3288 

CD 28 288 

CD 80/86 288 

Cefalexin 254 

Celecoxib 186 

Celiprolol 11 

Cell membrane 

drug permeation 26–27 

drug target 20 

functional membrane proteins 22 

phospholipid bilayer 20, 21, 26, 27 

Cell proliferation signaling pathway 285 

interference, anticancer drugs 284–285 

Central muscle relaxants 174, 175 

Central nervous system (CNS) 

blood–tissue barrier 24, 25 

cardiac glycosides affecting 132, 133 

nicotinic ACh receptors 300 

Cephalosporins 254 

Cerivastatin 156 

Cetirizine 114,115 

Cetuximab 284, 285 

C-fibers 180, 188 

Chagas disease 278 

Channels, drug transport 26, 27 

Chelating agents, in poisonings 294, 295 

Chiral molecules 64 

Chloramphenicol 261, 262 

Chlorguanide 276 

Chloride channel 66, 206, 207 

Chloroquine 276 

Chlorphenothane (DDT) 274, 275 

Chlorpromazine 216, 219 

Chlorthalidone 162 

Cholecalciferol (vitamin D) 248, 249 

Cholesterol, metabolism 154, 155 

Cholesterol-lowering drugs 154, 155 

Cholestyramine 156, 172, 346 

Choline 104 

Choline acetyltransferase 104, 105 

Cholinergic synapse 104–105 

Choline-transporter (CHT) 104 

Cholinoceptors 102, 104 

Chronic inflammatory bowel disease 256, 346–347 

Chronic myelogenous leukemia 286, 287 

Chronicobstructive pulmonary disease (COPD) 108, 

342 

Chylomicrons 154, 155 

Ciclosporin 288, 290, 291 

Cilastatin 254 

Ciliated epithelium 22, 23 

Cilostozol 120 

Cimetidine 114,115,168 

Cinacalcet 248, 249 

Ciprofloxacin 258 

Cirrhosis 304, 305 

Cisplatin 282 


Citalopram 212 

Citrate 142 

Clarithromycin 262 

Clavulanic acid 254, 255 

Clindamycin 262–263 

Clinical testing of new drugs 8, 9 

Clinical trials 8, 9 

placebo-controlled 82 

Clofazimine 264, 265 

Clofibrate 156 

Clomethiazole 324 

Clomifene 234, 236, 237 

Clonazepam 174 

Clonidine 98, 99 

Clopidogrel 44,150, 151 

Clostridium difficile 254 

Clotting, blood 142, 143 

Clotting factors 142, 144, 146 

Clozapine 218, 219 

Coagulation cascade 142, 143, 146 

Coated tablets 12 

Cocaine 96, 298 

Codeine 194 

Colchicine 6, 7, 336, 337 

Colchicum autumnale 6, 7, 336 

Colestipol 156 

Colloids 152, 153 

Colon cancer 286, 287 

Competitive antagonists 62, 63 

Complement, activation 74,75 

Compliance (patient) 50, 51, 52 

Concentration–binding curves 58–59 

Concentration–effect curves 56–57 

Concentration–effect relationship 56–57, 70, 71 

Concentration of drugs 46–47 

after irregular intake 50, 51 

after repeated dosing 50, 51 

as function oftime 46–47 

measurement ofeffect as function of56, 57 

time course 48–49 

Conduction anesthesia 188 

Congeneric drugs 10–11 

Congestive heart failure 126, 158, 316–317 

Conjugation ofdrugs 36, 37 

Conjugation reactions 40, 41 

Connexins 22 

Conotoxin 192–193 

Constipation 169 

Contact dermatitis 74,75 

Contraceptives, oral 234–235 

Controlled drug legislation 196, 298 

Controlled-volume catecholamine therapy 318 

Convallaria majalis 6 

Copper, chelation 294 

Coronary arteries 310, 311 

Coronary heart disease 100 

prognosis improvement, drugs 312 

smoking and 302, 303 

see also Angina pectoris; Myocardial infarction 

Coronary sclerosis 310, 311,312, 313 

Coronary spasm 122, 124, 310 

drugs for, and prevention 312, 313 

Corticotropin-releasing hormone (CRH) 220, 221, 

228 

Cortisol 226, 227, 228, 229 

Co-trimoxazole 256, 257 

Coumarins 142, 144, 145 

Counter-regulatory responses, diuretics 158, 159 

Counter-transport 44 

Covalent bonding 60 

COX-1150, 184, 186 

COX-2 182, 184, 186 

induction, in septic shock 318 


Crohn disease 256, 346–347 

Cromoglycate (cromolyn) 114,340, 341 

Crystalline zinc insulin 240 

Curare 178 

Cushing syndrome 226, 228 

Cutaneous reactions, to drugs 76–77 

Cyanide poisoning 296, 297 

Cyanocobalamin see Vitamin B 12 

Cyclic AMP (cAMP) 68, 69, 90, 92 

Cyclic GMP (cGMP) 120, 122 

Cyclooxygenases 150, 182, 184, 186–187 

nonselective inhibitors 186, 187 

see also COX-2 

Cyclophilin 290 

Cyclophosphamide 344 

CYP1A2 39 

CYP2C9 39 

CYP2D 634, 39, 80 

CYP3A4 38, 39, 262, 290 

CYP3A4 oxidase 44 

Cyproterone 230, 231 

Cystinuria 294, 295 

Cytarabine 282, 283 

Cytochrome oxidase 34, 44, 76 

Cytochrome P450 34, 44 

drug interactions and 38, 39 

drug metabolism 38–39 

genes and isoenzymes 38, 39 

inhibition, by macrolides 262 

substrates, inhibitors and inducers 38, 39 

see also entries beginning CYP 

Cytokines 318, 319 

synthesis inhibition 288, 289 

Cytoplasmic kinases 284 

Cytostatic agents 280, 281, 289 


alkylating 282, 283 

combination therapy 282 

emesis due to, control 116, 118 

as immunosuppressive drugs 289, 290 

mechanism of action 280–283 


Cytostatic antibiotics 282 

Cytotoxic antiproliferative drugs 289 

Cytotoxic reaction (type 2reaction) 74,75 

D 

Dabigatran 146 

Daclizumab 288, 289 

Danaparoid 146 

Dantrolene 175, 178 

Dapsone 264, 265 

Daptomycin 256, 257 

Darifenacin 108, 111 




Dasatinib 286 

Daunorubicin 282 

DDT (chlorphenothane) 274, 275 

Deadly nightshade (Atropa belladonna) 6,7,109 

Dealkylation reaction 36, 37 

Decamethonium 176 

Decarbaminoylation 106,107 

Defensins 346 

Delayed hypersensitivity (type IV) reactions 74,75, 

288, 289 

Dendritic cells 346 

Dephosphorylation, 

indirect parasympathomimetics 106, 107 

Depolarization 

cardiac 130, 136, 137 

nerves, local anesthetic effect 188, 189 

Depolarizing muscle relaxants 176, 177 

Depressive illness, treatment 210–213 

Dermatitis, contact 74,75 

Dermatological agents 16–17 

Dermatophyte infections 266 

Descending antinociceptive system 180 

Desensitization 68 

receptors 92, 93 

Desferoxamine 294, 295 

Desflurane 202 

Desmopressin 164, 165 

Desmosomes 22, 76 

Dexamethasone 227, 282 

Dextran 152 

Diabetes mellitus 240–247 

insulin therapy see Insulin 

oral antidiabetic drugs 246–247 

type I240, 242–243 

type II 240, 244–245, 338 

Diacylglycerol (DAG) 68, 69 

Diamorphine 196 

Diarrhea 172 

Diastereomers 64 

Diazepam 208, 209, 331 

Didanosine 272 

Diethylcarbamazepine 278 

Diethylstilbestrol 78 

Diffusion barriers 20, 22, 24 

for eye drops 332, 333 

Diffusion of drugs 26, 27, 42 

Digitalis 6, 7 

Digitoxin 133, 316 

Digoxin 6, 7, 133, 316 

Dihydrofolate (DHF) 256, 257 

Dihydropyridine derivatives 124, 125 

Diltiazem 125, 312 

Dimercaprol (BAL) 294, 295 

Dimercaptopropanesulfonic acid 294, 295 

4-Dimethylaminophenol 296 

Diphenhydramine 115 

Diphenolmethane derivatives 170 

Dipole–dipole interaction 60, 61 

Dipole–ion interaction 60, 61 

Dipyrone (metamizole) 184, 185 

Disease-modifying agents,rheumatoid arthritis 344 

Disintegration ofdrugs 12 

Disse spaces 24 

Dissociation constant 42 

Dissociative anesthesia 204 

Dissolution of drugs 12 

Distribution ofdrugs 18–19,22–33, 30–31, 48 

blood–tissue barriers 24–25 

external barriers of body 22–23 

membrane permeation 26–27 

modes 30–31 

plasma protein binding 32–33 

transporters 28–29 

Diuretics 158–165 


antihypertensive therapy 158, 308, 309 

congestive heart failure 158, 316, 317 

counterregulatory responses 158, 159 

loop 162, 163 


osmotic 160 

potassium-sparing 164, 165 

renal actions, NaCl reabsorption 158, 160, 161 

sulfonamide type 162–163 

thiazide 162, 163, 308, 309 

Divalent metal transporter 140 

DNA function inhibitors 258–259 

DNA strand breakage, induction 282 

DNA synthesis inhibition 

antibacterial drugs 258–259 

cytostatic drugs 280, 282, 283 

Dobutamine, enantioselectivity 64 

Docetaxel 280 

Domperidone 326, 327, 329 

Donepezil 106 

L-Dopa 88, 89, 112, 320, 321 

Dopa decarboxylase 320, 321 

Dopamine 88, 89, 96, 112–113 

Parkinson disease 320, 321 

release 97,112,113 

substrates and inhibitors 96, 97 

Dopamine receptors 112, 113, 216 

antagonists 112, 113, 216 

D 1 112, 113 

D2 113, 216 

agonists 112, 113, 220, 221, 320 

antagonists 216 


neuroleptic affinity profiles 219 

Dopamine transporter (DAT) 112 

Dorzolamide 162 

Dose, drug accumulation and 50, 51, 52, 53 

Dose–effect relationship 54, 55 

Dose–frequency relationship 54, 55 

Dose-linear kinetics 70, 71 

Dose–response curves 72, 73 

Dose–response relationship 54–55 

Doxorubicin (Adriamycin) 282 

Doxycycline 260 

Dropsy, plants treating 6 

Drug(s) 

absorption see Absorption ofdrugs 

accumulation 50, 51, 52–53 

actions 20–21 

enantioselectivity 64–65 

quantification 54–57 

sites 20–21 

administration see Administration of drugs 


approval 8, 9 

binding to plasma proteins 30, 31, 32–33 

biotransformation, in liver 34–35, 36–37, 44 

clearance rates 32 

concentration see Concentration ofdrugs 

delivery 

dermatological agents 16,17, 232 

inhalational drugs 14,15 

oral drugs 12,13 

development 8, 9 

diffusion barriers see Diffusion barriers 

distribution see Distribution of drugs 

elimination see Elimination ofdrugs 

essential 10 

free, concentration 32, 33 

metabolism see Metabolism of drugs 

names, diversity 10 

new, value 10 

penetration inrespiratory tract 14, 15 

permeation 24, 25, 26–27 

reabsorption 40, 41, 42, 43 

sales strategy 10 

targets 20–21 

time course, plasma levels see Time course 

toxicity inpregnancy/lactation 78–79 

see also Adverse drug effects (ADEs) 

transport 24, 25, 26, 27, 48 

transporters 28–29 

uptake into blood 24 

barriers to22–23 

Drug eruptions, fixed (exanthemas) 76, 77 

Drug-induced vomiting 328, 329 

Drug interactions 28, 32, 34 

antiepileptics 324 

cytochrome P450 and 38, 39 

Drug–receptor interactions 60–71 

binding forces 60–61 

mechanisms 62, 63 

Drugs of abuse 196 

Drug vehicles, dermatological agents as 16,17 

Duloxetine 108, 116 

Duodenal ulcers, treatment 168, 169 

Dusting powders 16,17 

Dutasteride 230, 231 

E 

EC50 56 

Ecstasy (MDMA) 96, 298 

Ectoparasitic infestation, treatment 274–275 

Edema, diuretic actions 158, 159 

EDTA 142, 294, 295 

Efalizumab 292, 293 

Efavirenz 272 

Efflux pumps 22 

Efflux transporters 28, 29 

Eicosanoids 182–183 

Electrolyte disorders 166–167 

Electrolyte loss, cardiac glycosides causing 132 

Electromechanical coupling 130, 178, 248 

Electrosecretory coupling 248 

Electrostatic attraction 60, 61 

Elimination of drugs 34–45, 46 

exponential characteristics 46, 47 

increased/impaired during therapy 52, 53 


kidney role 42–43, 46 

liver role 34–35, 46 

time course 48 

Embryo–fetal alcohol syndrome 304, 305 

Emesis see Vomiting 

Emetic center 328, 329 

Emulsion 16, 17 

Enalaprilat 126 

Enantiomers 64, 65 

Enantioselectivity, drug action 64–65 

Endocannabinoids 338, 339 

Endocytosis, receptor-mediated 26, 27, 92 

Endocytotic activity 24 

Endoneural space 190 

Endoparasitic infestation, treatment 274–275 

Endoplasmic reticulum 34, 35 

Endothelial cells 24 

Endothelin (ET) receptors 120 

Endothelium-derived relaxant factor (EDRF) 122 

Enfuvirtide 272 

Enoxacin 258 

Entacapone 320, 321 

Entamoeba histolytica 258, 259, 278 

Entecavir 270 

Enteral absorption 22 

Enteric coated tablets 12,13 

Enterochromaffin-like (ECL) cells 114, 116 

Enterohepatic circulation 40–41 

Enzyme induction 34 

Ephedrine 96 

Epidophyllotoxins 282 

Epilepsy 206, 322 

childhood 324 

see also Antiepileptic drugs 

Epinephrine 88, 94, 98 

actions 88, 89, 301 

affinity for receptors 94 

anaphylactic shock 340 

cardiac arrest 134 

interaction with β2-adrenoceptors 94, 95 

release, nicotine effect 301, 302 

structure–activity relationship 94, 95 

Epirubicin 282 

Epithelium, thickness, drug uptake 22 

Eplerenone 164, 316 

Epoxidation reactions 36, 37 

Epsom salt 170 

Eptifibatide 150 

Equilibrium dissociation constant (KD) 58 

Erectile dysfunction 120 

Ergometrine 128 

Ergot alkaloids 128, 129, 326, 327 

Erlotinib 284, 285 

Erythema, toxic 76, 77 

Erythromycin 261, 262 

Erythropoiesis, and erythropoietin 138, 139 

Escherichia coli Nissle 346 

Esmolol 11 

Essential drugs 10 

Ester hydrolysis 36, 37 

Estradiol 230, 231, 232, 233 

chronic administration 236 

synthesis, aromatase role 238, 239 

transdermal delivery 232 



Estrogen 232–233 

bone resorption reduction 334, 335 

conjugated 232 

exogenous, oral contraceptive 234, 235 

formation inhibition 238 

preparations 232 

receptors and antagonists 236, 237 

Etanercept 344, 345 

Ethambutol 264, 265 

Ethanol see Alcohol 

Ethinylestradiol 232, 233 

Ethosuximide 322, 323, 324 

Etomidate 204, 205 

Etoposide 282 

Etoricoxib 186 

Euonymus europaeus 6 

European plants 6, 7 

Everolimus 290 

Exemestane 238, 239 

Exenatide 246, 247 

Extracellular fluid volume (EFV) 158, 166 

Extracts, from plants 4 

Eye drops, diffusion barriers 332, 333 

Ezetimibe 156 

F 

Fab fragments 133 

Famotidine 168 

“Fast acetylators” 80 

Fe 2+ compounds 140 

Fe 3+ salts 140 

Febrile convulsions 324 

Felbamate 322 

Felodipine 124 

Felypressin 164, 165, 190 

Fenestrations 24, 30 

Fenoterol 340 

Fentanyl 4, 198, 200 

Fentanyl patches 196 

Ferric ferrocyanide 296, 297 

Ferroportin 140 

Fetal alcohol syndrome 304, 305 

Fetal damage, by drugs 78, 79 

Fexofenadine 114 

Fibric acid agents 156 

Fibrinolytics 142, 148–149 

Fick’s law 46 

Fight-or-flight actions 86, 87 

Filariasis 278 

Finasteride 230, 231 

First-pass elimination 14,18, 44 

Fixed drug eruptions 76, 77 

FK-binding protein 290, 291 

Fluconazole 266 

Flucytosine 266, 267 

Fludrocortisone 226 

Flumazenil 206, 207, 294, 330 

Fluoroquinolones 258, 259 

5-Fluorouracil 282, 283 

Fluoxetine 116, 117, 212, 213 

Fluphenazine 216, 218, 219 

Flutamide 230 

Folic acid 138, 139 

Follicle-stimulating hormone (FSH) 220, 221, 232, 

233, 238 

oral contraceptive effect 234 

Follicular growth 232–233, 234 

Follow-on preparations 10 

Fondaparinux 142, 146 

Formestane 238, 239 

Formoterol 340, 342 

Fosaprepitant 328 

Foscarnet 270, 271 

Fulvestrant 236 

Fungal infection treatment 266–267 

Furosemide (frusemide) 162 

G 

GABA 118, 119, 206 

enhanced inhibition, benzodiazepines 206, 207 

mechanism of action 118,119, 207 

receptors see GABA, receptors (below) 

structure 322 

GABA, receptors 118, 206, 207 

activation, injectable anesthetics 205 

GABAA receptors 66,118,119,174,203, 206, 

207 

antiepileptic action 322, 325 

GABAB receptors 118, 119, 175 

GABAergic neurons 206, 207 

antiepileptic drug action 322, 323, 325 

GABAmimetics 322, 325 

Gabapentin 322, 323, 325 

Galantamine 106 

Galen, Claudius 2 

Gallopamil 124 

γ-Aminobutyric acid see GABA 

Ganciclovir 269, 270 

Ganglia 88 

Gas exchange disorders, opioid effect 194 

Gastric lavage 294 

Gastric secretion, inhibition 108, 168 

Gastric ulcers, treatment 168, 169 

Gastrointestinal tract 

drugs acting on 168–173 

flora 346, 347 

mucosal barrier 346, 347 

opioid action 194, 195 

Gelatin colloids 152, 153 

Gelatin polymers 152, 153 

General anesthesia 200–201 

General anesthetics 200 

inhalational 200, 202–203 

injectable 200, 204–205 


Generic drugs 10 

Genetic polymorphism 80, 81 

of biotransformation 34 

Ghrelin 338 

Glatiramer acetate 288 

Glaucoma 100, 332–333 

angle-closure 110, 332 

open-angle 332 

Glibenclamide 247 

Glitazones 246 

Glomerular filtration 42, 43 

Glucagon-like peptide-1 (GLP-1) 246 


Glucocorticoids 226–227 


asthma/COPD 342, 343 

atopy/allergies 340 

circadian administration 228–229 

cytokine production inhibition 288, 289 

effect on cortisol synthesis 228, 229 

inflammatory bowel disease 346 

pharmacodynamics 226 

presystemic elimination 44 

receptors 226 

replacement therapy 226 

rheumatoid arthritis 344 

Glucuronic acid 40, 41 

β-Glucuronidases 40, 41 

Glucuronides 40, 41 

Glutamic acid 118, 119, 322 

receptor(s) 118,119,322 

receptor antagonist 322 

Glycemic control 242 

Glyceryl trinitrate (GTN) 122, 123, 312 

Glycine 174, 175 

Glycine receptor 203 

activation 205 

Glycoprotein IIb/IIIa antagonists 150, 151, 315 

Goiter 222, 223, 225 

Gold compounds 344, 345 

Gonadotropin(s), secretion increase 234 

Gonadotropin releasing hormone (GnRH) 

(gonadorelin) 220, 221, 230 

analogues 220 


pulsatile delivery 234 

superagonists 220, 221, 230, 231 

Goserelin 220, 230 

Gout 6, 336–337 

GP IIb/IIIa antagonists 150, 151, 315 

G-protein 66, 67, 68, 69, 90, 92 

G-protein-coupled receptor family 68 

G-protein-coupled receptors 66, 67, 92, 93, 94 

mode ofaction 68–69 

Gram-negative bacteria 252, 253, 256, 262 

Gram-positive bacteria 252, 253, 254, 318 

Grapefruit juice 44 

Graves’ disease 224, 225 

Griseofulvin 266, 267 

Growth factors 284 

Growth hormone 220 

Growth hormone release-inhibiting hormone 

(GHRIH) 220, 221 

Growth hormone-releasing hormone 

(GHRH) 220, 221 

Gut flora 346, 347 

Gyrase inhibitors 258, 259 

H 

H1 antihistamines 114, 115, 340 

H2 antihistamines 114, 115, 168, 169 

Half-life (t1/2) 46, 70 

Hallucinogens 298–299 

Haloperidol 218, 219 

Halothane 202, 203 

Haptens 74,76 

Hashish 298 


Hay fever 340 

Heart 

action potential 136, 137 

calcium antagonists effect on124, 125 

conduction 130, 131,134, 135 

contraction and relaxation 130, 131 

drugs influencing 130, 131 

macrolide adverse effect 262 

Heart failure 100, 316 

compensatory mechanisms 316, 317 

congestive 126, 158, 316–317 

Helicobacter pylori 168, 169 

Helleborus niger 6 

Hemoglobin, impaired synthesis 138 

Hemosiderosis 140 

Hemostasis 142, 143 

Heparan sulfate 146 

Heparin 134, 142, 146–147 

Heparin-induced thrombocytopenia (HIT) 146 

Hepatitis B, drug treatment 270, 271 

Hepatitis C, drug treatment 270 

Hepatitis viruses, drug treatment 270, 271 

Hepatocytes 34, 35 

Hepcidin 140 

Hephaestin 140 

HER1 and HER2 284, 285, 286 

Herbal products, sleep disorders 330 

Heroin 196, 199 

Herpes simplex viruses 268, 269 

High-density lipoprotein (HDL) 154, 155 

Hirudin and derivatives 142, 146, 147 

Histamine 74,114–115 

Histamine receptors 114 


see also Antihistamines 

History, ofpharmacology 2–3 

Histotoxic hypoxia 296 

HIV infection treatment 272–273 

HIV protease inhibitors 272, 273 

HIV replication, inhibition 272, 273 

H + /K + ATPase 26 

HMG-CoA reductase inhibitors (statins) 156, 157 

Hohenheim, Theophrastus von 2 

Homatropine 111 

Homeopathy 82, 83, 330 

Hormone–receptor complexes 66, 67 

Hormones 20, 220–249 

Human chorionic gonadotropin (HCG) 234, 236 

Human epidermal growth factor receptor 284, 285, 

286, 287 

Human immunodeficiency virus (HIV) see entries 

beginning HIV 

Human menopausal gonadotropin (HMG) 234 

Hydrocyanic acid, poisoning 296, 297 

Hydrogel 16, 17 

Hydrolysis, of drugs 36, 37 

Hydrophilic (aqueous) cream 16,17 

Hydrophilic drugs 16,17, 30 

Hydrophobic interactions 60, 61 

Hydrophobicity 32 

Hydroxychloroquine 344 

Hydroxycobalamin 138, 296 

Hydroxycoumarins 144,145 

4-Hydroxycoumarins 144, 145 



Hydroxyethyl starch 152, 153 

Hydroxylation, hepatic 34, 35 

17-α-Hydroxyprogesterone caproate 232 

5-Hydroxytryptamine see Serotonin 

Hydroxyurea 282 

Hyperacidity 168, 169 

Hypercalcemia 248 

Hyperglycemia 162, 242 

Hyperglycemic coma 240, 242 

Hyperinsulinemia 244 

Hyperkalemia 166, 316 

Hyperlipoproteinemia 154–157 

Hypernatremia 166, 167 

Hyperparathyroidism 248 

Hypersensitivity reactions 74, 75 

delayed (type IV) 74,75, 288, 289 

to penicillin 252, 253 

Hypertension 100, 308–309 

see also Antihypertensive agents 

Hyperthyroidism 100, 222, 224–225 

Hyperuricemia 162, 336 

Hypnotics 330–331 

Hypoglycemia 226, 242, 246, 247 

Hypokalemia 162, 166, 170 

Hyponatremia 166, 167 

Hypophyseal hormones 220–221 

Hyposensitization therapy 340 

Hypotension 120, 121, 318,319 

Hypothalamic releasing hormones 220, 221 

Hypothyroidism 222 

Hypovolemic shock 152, 153, 318 

I 

Idarubicin 282 

Idoxuridine 268, 269 

IgA antibodies 346 

IgE antibodies 74, 75, 340 

Illusions, drugs causing 298 

Imatinib 284, 285, 286, 287 

Imidazole derivatives 266, 267 

Imipenem 254, 255 

Imipramine 211, 212, 213 

Immune-complex vasculitis 74,75 

Immune response 74,75, 288, 289 

inhibition 288–291 

Immunogens 74 

Immunosuppressive drugs 288–291, 346 

Incretin mimetics 246, 247 

Indinavir 272 

Infiltration anesthesia 188 

Inflammatory bowel disease 256, 346–347 

Inflammatory mediators 

inflammatory bowel disease 346, 347 

rheumatoid arthritis 344, 345 

septic shock 318, 319 

Inflammatory reactions/response 344, 345, 346 

glucocorticoid therapy 226 

Infliximab 344, 345, 346 

Influenza viruses, drug treatment 270, 271 

Inhalation, drug application by 14–15,18, 19 

Inhalational anesthetics 200, 202–203 

Injectable general anesthetics 200, 204–205 

Inositol trisphosphate (IP 3)68, 69, 90, 91 

Inotropic agents 132, 316 

Insecticides 274, 275, 296 

Insomnia 330 

Insulin 

amino acid sequence variations 240, 241 

control of release from injection site 240, 241 

conventional therapy (fixed-dose) 242, 243 

extended-action 240 

formulations, and dosage forms 240 

hypoglycemia due to242 

intensified therapy 242, 243 

long-acting analogues 240, 242, 243 

presystemic actions 242, 243 

rapidly-acting analogues 240, 242, 243 

receptors 244 

recombinant 240 

replacement methods 242, 243 

resistance 244 

secretory capacity decrease 244 

solutions and suspensions 240 

structure 241 

synthesis 240 

Insulin aspart 240 

Insulin detemir 240 

Insulin glargine 240 

Insulin glulisine 240 

Insulin-like growth factor 1(IGF-1) 220 

Insulin lispro 240, 241 

Integrins 292, 293 

Interferon alfa 268, 270, 271, 284 

Interferons 268 

Interleukin 1(IL-1) 288 

antagonist 344 

Interleukin 2(IL-2) 284, 288, 290, 291 

International Nonproprietary Name (INN) 10 

International Normalized Ratio (INR) 144 

Interneurons 174, 175 

Interstitial fluid 30 

Intestinal mucosa–blood barrier 22 

Intestinal tract see Gastrointestinal tract 

Intracellular fluid 30 

Intramuscular injection 18, 19 

Intravenous administration 18, 19 

Intrinsic activity 62 

enantioselectivity 64 

Intrinsic factor 138 

Intrinsic sympathomimetic activity (ISA) 100 

Inverse agonists 62 

Iodine 

administration 222, 224 

deficiency 222 

Iodine-131 ( 131 I) 224 

Iodized salt prophylaxis 222 

Ion channels 

G-protein action and 68, 69 

ligand-gated 66, 67 

Ionic interaction 60, 61 

Ipecac syrup 294 

Ipratropium 108, 110, 111, 128, 134 

Irinotecan 282 

Iron 

administration and fate 140, 141 

chelation 294, 295 

overload 140 

Iron deficiency anemia 138, 140–141 

Irritant laxatives 170, 173 


Isoflurane 202, 203 

Isoniazid 264, 265 

Isoproterenol 94 

Isosorbide dinitrate 122, 123, 312 

Isosorbide mononitrate 122, 123, 312 

Isoxazolylpenicillins 254 

Isradipine 124 

Itraconazole 28, 266 

Ivabradin 130, 134 

Ivermectin 278 

J 

JC virus infection 292 

K 

Kainate receptors 118, 119 

Kala-azar 278 

K + channels see Potassium (K + )channels 

Keratinized squamous epithelium (skin) 22, 23 

Ketamine 204, 205 

Ketoconazole 38 

Ketolides 262 

Kidney 

drug excretion 42–43, 46 

NaCl reabsorption 158, 160, 161 

Kinetosis, prophylaxis 110 

L 

β-Lactamases 252, 255 

β-Lactam ring/antibiotics 252, 253, 254 

atypical 254, 255 

Lactation, drug toxicity during 78, 79 

Lactic acidosis 246, 247 

Lactulose 170 

Lamivudine 270, 271, 272 

Lamotrigine 322 

Lanreotide 220 

“Laughing gas” (nitrous oxide) 202, 203 

Law ofmass action 58 

Laxatives 169–170, 171 

habituation 170, 171 


in poisoning 294 

types 170, 173 

Lead, chelation 294, 295 

Leflunomide 344 

Leishmaniasis 278, 279 

Lepirudin 146 

Leprosy, drug treatment 264, 265 

Letrozole 238, 239 

Leukemia, chronic myelogenous 286, 287 

Leukocytes 

B-lymphocytes 288, 289 

migration mechanism/inhibitors 292, 293 

see also T-lymphocytes 

Leukotrienes 182, 183 

receptor blockade 340, 341, 342 

Leuprorelin 220, 230 

Levaracetam 324 

Levobunolol 11 

Levodopa (L-Dopa) 88, 89, 112, 320, 321 

Lidocaine 192, 193 

Ligand-gated ion channels 66, 67 

Ligand-operated enzyme 66, 67 

Ligand–receptor complexes 66, 67 

Lincosamides 262–263 

Lindane 274, 275 

Linezolide 260, 261 

Lipid bilayers 20, 21, 26, 27 

Lipid-lowering agents 154–157 

Lipophilic (oily) cream 16, 17 

Lipophilic drugs 16,17, 22, 30 

Lipophilicity, inhalational anesthetics 202, 203 

Lipophilic ointment (oil ointment) 16,17 

Lipoproteins, metabolism 154, 155 

Lithium ions 214,215, 224 

adverse effects and indications 214 

Lithium salts, in thyrotoxicosis 224 

Liver 

cirrhosis 304, 305 

drug biotransformation 34–35, 46 

drug elimination 34–35, 46, 47 

drug uptake 24, 25 

Local anesthetics 188–193 

adverse effects 188, 192–193 

amide-type orester-type 190 

cardiac effects/inhibition 192 

chemical structure 190, 193 

concentration, diffusion and effect 190, 191 

forms and administration 188 


pH value 190, 193 

vasoconstrictors with 190 

Loop diuretics 162, 163 

Loop ofHenle 160 

Loperamide 172 

Lorazepam 330 

Losartan 126 

Lotions 16,17 

Lovastatin 156, 157 

Low-density lipoproteins (LDL) 154, 155, 156 

Low-molecular-weight heparin 142, 146 

Lugol’s solution 224 

Luteinizing hormone (LH) 220, 221, 232, 233, 234 

Lyell syndrome (toxic epidermal necrolysis) 76, 77 

Lymphokines 74 

Lypressin 164 

Lysergic acid derivatives 128 

Lysergic acid diethylamide (LSD) 128, 298, 299 

M 


Macrolides 261, 262, 263 

Malaria, drug treatment/prevention 276–277 

Malignant neuroleptic syndrome 216 

Malignant tumor chemotherapy 280–287 

Mania 214–215 

Mannitol 160 

Maraviroc 272 

Margin of safety 72 

Mast cells, histamine release 114, 115 

Mast cell stabilizers 114, 340, 341, 342 

Matrix-type tablet 12,13 

Maximum binding (B max) 58 

Mcells 346 

Mebendazole 274, 275 

Mechlorethamine 282 

Meclozine 329 



Medroxyprogesterone 232 

Melatonin 330 

Membrane transport systems 20 

Menadione 144, 145 

Menopause 236, 238 

Menstrual cycle 232, 235 

Mepivacaine 192, 193 

6-Mercaptopurine 282 

Meropenem 254 

Mesalazine 256, 257, 346 

Mescaline 298 

Metabolic autoregulation 310, 311 

Metabolic disorders, in obesity 338 

Metabolic syndrome 244 

Metabolism of drugs 44 

catecholamine effects 92, 93 

by cytochrome P450 38–39 

genetic variants 80, 81 

phase I/II reactions 36, 37 

Metabotropic receptors 118, 119 

Metamizole (dipyrone) 184, 185 

Metformin 246, 247 

Methadone 196, 199 

Methemoglobin 296, 297 

Methimazole 225 

Methohexital 204, 205 

Methotrexate 282, 283, 344, 345, 346 

Methylene dioxyamphetamine (MDMA) 96, 298 

Methylphenidate 96 

Methylxanthines 340 

Metipranolol 11 

Metoclopramide 326, 327, 329 

Metoprolol 11, 100, 101, 326 

Metronidazole 258, 259, 278 

Midazolam 204, 205, 208, 209 

Mifepristone 236, 237 

Miglitol 246 

Migraine 100, 326–327 

Mineralocorticoids 226, 227 

Minimum alveolar concentration (MAC) 202 

Minipill 234, 235 

Minocycline 260 

Misoprostol 182 

Mitotic spindle damage, cytostatic drugs 280, 281 

Mivacurium 178 

Mixed-function oxidases orhydroxylases 34 

Moclobemide 96, 212 

Modafinil 96 

Molsidomine 122, 123, 312 

Monoamine oxidase (MAO) 88, 94,113 

Monoamine oxidase-B (MAO-B) 320 

Monoamine oxidase (MAO) inhibitors 96, 97, 213 

Monoanesthesia 200, 201 

Monobactams 254, 255 

Montelukast 340 

Mood disorders 210 

“Morning-after” pill 234 

Morphine 194 

adverse effects and overdose 72, 73 

controlled-release tablets 196 

distribution in brain 198, 199 

extraction from opium 4, 5, 194 

indications 196 

Morphine-6-glucuronide 196, 198, 199 

Morpholines 266 

Motion sickness 110, 328 

Motor end plate 300 

Motor function, drugs affecting 174–179 

Motor neurons 174, 175 

local anesthetic effect 188, 189 

Motor system 174, 175 

MRP2 (multidrug resistance-associated protein 2) 

34 

MTOR 290 

Mucociliary transport 14,15, 302 

Multidrug resistance proteins 28, 34 

Multiorgan failure 318, 319 

Multiple myeloma 284 

Multiple sclerosis 288, 292, 293 

Murein lattice 252, 253, 318 

Muromonab-CD 3288, 289 

Muscarinic ACh receptors 72, 102, 104, 105, 109 

antagonists 108, 109 

subtypes and actions 104 

Muscle paralysis 174, 178 

Muscle relaxants 176–177, 200, 201 

central 174, 175 

depolarizing 176,177 

nondepolarizing 178, 179 

poisons 178, 179 

Muscle spasm 174 

Mutagenic effects, drugs 280 

Mycobacterium infections 258, 264–265 

Mycobacterium leprae 258, 264, 265 

Mycobacterium tuberculosis 258, 264, 265 

Mycophenolate mofetil 289, 290 

Mydriatics 108 

Myocardial blood flow 310, 311 

Myocardial contraction and relaxation 130, 131 

Myocardial failure 316, 317 

Myocardial hypoxia 310, 311 

Myocardial infarction 186, 308, 314–315 

Myocardial oxygen demand/supply 310, 311,312, 

313 

Myometrial relaxants (tocolytics) 90, 92, 128, 129 

Myometrial stimulants 128, 129 

N 

Na + see Sodium 

Na2Ca-EDTA 294 

Na3Ca-pentetate 294 

Nabilone 298 

Na + /Ca 2+ exchangers 28, 130 

Na + channel see Sodium (Na + )channel 

NaCl reabsorption 158, 160, 161, 166 

Naftidine 266 

Na + /K + ATPase 26, 28, 160, 164 

cardiac glycoside action 132, 133 

direct inhibition 168 

Nalidixic acid 258 

Naloxone 198 

Naltrexone 198 

Nasal decongestants 98 

Natalizumab 292, 293, 346 

Nateglinide 246 

Natural products 4 

Nebivolol 100 

Nebulizer 14 


Nedocromil 340 

Nelfinavir 272 

Neomycin 262 

Neostigmine 106, 107 

Nephron 160, 161 

Nerve cells 88 

Nerve impulse, local anesthetic effect 188, 189 

Neuraminidase inhibitors 270 

Neurohypophyseal(NH) hormones 220, 221 

Neurokinin (NK) receptors 118, 119 

NK1 receptor antagonist 329 

Neuroleptanalgesia 200 

Neuroleptics 112, 216–219 

atypical 218,219 

classical 216, 219 

effects in schizophrenia 112, 113, 216, 217 

uses/dosages 218 

Neuromuscular blocking agents 176–179, 200 

Neuropathic pain 180 

Neurotransmitters 

acetylcholine as 102, 104, 174 

GABA 118, 119, 207 

glutamic acid 118, 119 

parasympathetic nervous system 102, 104 

serotonin as116 

spinal cord 174 

sympathetic nervous system 88 

transporters, substrates/inhibitors 96, 97 

Nevirapine 272 

Nicardipine 124 

Nicotine 300–303 

absorption and plasma levels 302 

actions/effects 300, 301 

dependence 300, 301 

withdrawal symptoms 300 

Nicotine patches/gum/spray 300 

Nicotinic ACh receptors 66, 67, 102, 104, 105, 

300 

localization 300, 301 

partial agonist 300 

Nicotinic acid 156 

Nifedipine 124, 125, 312 

Nilotinib 286 

Nimodipine 124 

Nitrate(s), organic see Organic nitrates 

“Nitrate pauses” 312 

“Nitrate tolerance” 122, 312 

Nitrazepam 209, 330 

Nitrendipine 124 

Nitric oxide 114, 120, 122 

Nitroglycerin 122, 123, 312 

Nitroimidazole derivatives 258, 259 

Nitrous oxide 202, 203 

NMDA receptors 118, 119, 203, 204, 322 

alcohol effect on 304 

antiepileptic drug action 322, 325 

blockade 205, 304 

Nociceptive impulses 180, 181 

Nociceptors 180 

NOD-like receptors (NLR) 346 

Noncovalent bonding 60 

Nondepolarizing muscle relaxants 178, 179 

Nonnucleoside reverse transcriptase inhibitors 

272 

Nonsteroidal anti-inflammatory drugs (NSAIDs) 

184, 185, 187 


in gout 336 

Norepinephrine (noradrenaline) 88, 98 

actions/functions 88, 89, 301 

affinity for receptors 94 

appetite reduction 338 

in heart failure 316 

mechanisms for increasing 96 

substrates and inhibitors 96, 97 

Norepinephrine (noradrenaline) transporter (NET) 

88, 89, 96 

inhibitors 96 

Norfloxacin 258 

Nuclear factor of activated Tcells (NFAT) 290, 291 

Nucleobase synthesis inhibition 282 

Nucleoside reverse transcriptase inhibitors 272 

Nucleotide synthesis, inhibition 282, 283 

Nystatin 266 

O 


Obesity 338–339 

diabetes mellitus and 244, 245, 328 

sequelae 338–339 

Obidoxime 296, 297 

Octreotide 220 

Ofloxacin 258 

Olanzapine 218, 219 

Omeprazole 168 

Onchocerciasis 278 

Ondansetron 116,117, 282, 328329 

Opioids (opiates) 194–199 

addiction 194, 196, 199 

administration/bioavailability 196, 197 

disposition rate 197 

effects (stimulant/damping) 194, 195 

endogenous 194, 195 

indications 196 

metabolism 197 

receptor(s) 172, 194, 195 

receptor antagonist 198 

side effects 194 

tolerance 194 

withdrawal symptoms/treatment 196 

Opipramol 212, 213 

Opium, morphine extraction from 4,5,194 

Opium tincture 4, 5, 172 

Oral administration 12–13,18, 19,44, 45, 48 

drug absorption 12,13, 44, 45, 48 

Oral antidiabetic drugs 246–247 

Oral contraceptives 234–235 

Oral dosage forms 12,13 

Oral mucosa 18, 22 

Oral rehydration solutions 172 

Organic nitrates 122–123, 128, 312, 313 

mechanism of action 122, 123, 313 

unwanted reactions 122 

Organophosphates 106, 296, 297 

Orlistat 338, 339 

Ornipressin 164, 165 

Oseltamivir 270 

Osmotic diuresis 160 

Osteoblasts 334, 335 



Osteoclasts 248, 334, 335 

Osteomalacia 324 

Osteoporosis 236, 237, 334–335 

Ototoxicity 254, 262, 263 

Overdosage 

adverse effects due to72, 73 

drugs counteracting 294 

Ovulation 232–233 


stimulation 234 

Oxacillin 254, 255 

Oxalate 142 

Oxazepam 208, 209, 331 

Oxazolidinones 260, 261 

Oxcarbazepine 324 

Oxidation reactions 36, 37 

Oxprenolol 11 

Oxygen 

in COPD 342 

myocardial demand/supply 310, 311,312, 313 

Oxymetazoline 98 

Oxytocin 128, 220, 221 

P 

PABA (p-aminobenzoic acid) 256, 257, 265 

Paclitaxel 280 

Pain 

mechanisms/pathways 180–181 

neuropathic 180 

opioid indications 196 

relief see Analgesics/analgesia 

Palifermin 282 

Pancuronium 178, 179 

Papaverine 194 

Paracelsus 2, 72 

Paraoxon 106, 107 

Parasitic infections, treatment 274–275 

Parasympathetic nervous system 86, 102–103 

activation, responses to 102, 103 

anatomy 102 

blockade 108–109 

heart function and 130 

neurotransmitters 102, 104 

stimulation 106, 109 

Parasympathetic nuclear regions, 

opioid stimulation 194 

Parasympatholytics 72, 108–111 



cardiac function and 130 


poisoning, antidotes 106 

sinus bradycardia 134 

Parasympathomimetics 106–107 


direct, or indirect 106, 107 

in glaucoma 332 

Parathyroid hormone 

(PTH; parathormone) 248, 249 

bone remodeling 334, 335 

deficiency 334 

Parecoxib 186 

Parkinson disease, treatment 110, 112, 320–321 

Parkinsonism 110, 218 

treatment 320, 321 

Paroxetine 212 

Partial agonists 62 

Passive diffusion 42 

Passive smoking 302, 303 

Passive transport 26, 27 

Paste (oil paste) 16, 17 

Patent protection 10 

Pegvisomant 220 

Pemphigus-like reactions 76 

Penbutolol 11 

D-Penicillamine 294, 295 

Penicillin(s) 252, 253 

extended activity spectrum 254 

Penicillinase 252, 253, 254 

resistance 254 

Penicillin derivatives 252, 254 

Penicillin G(benzylpenicillin) 252, 253 


dose/plasma level time course 70, 252 


Penicillin V(phenoxymethylpenicillin) 254, 255 

Penicillium notatum 252, 253 

Pentavalent antimonial compounds 278 

Pentobarbital 331 

Peptidases 36–37 

Peptidoglycan lattice 252, 253, 254 

Perchlorate 224 

Pergolide 320 

Perineurium 190 

Peristalsis 168, 171, 172 

Pernicious anemia 138 

Peroxisome proliferator-activated receptor (PPARα) 

156 

Peroxisome proliferator-activated receptor (PPARγ) 

246 

P-glycoprotein 22, 28, 38, 44, 290 

Pharmacodynamics, genetic variants 80, 81 

Pharmacogenetics 80–81 

Pharmacokinetics 8, 46–53 

genetic variants 80, 81 

Pharmacovigilance 8 

Phase Ireactions (drug metabolism) 36, 37 

Phase I–IV studies (clinical testing) 8,9 

Phenobarbital 34, 322, 323 

Phenothiazines 216, 219 

Phenoxymethylpenicillin (penicillin V)254, 255 

Phenylephrine 98 

Phenytoin 322, 323, 324 

Philadelphia chromosome 286, 287 

Phosphate, vitamin Dhormone action 248, 249 

Phosphodiesterase inhibitors 120, 340 

Phospholipase C68, 69 

Phospholipids 20, 21, 26, 142 

membrane bilayer 20, 22 

Phosphorylation 66, 68, 284 

Photoallergic reactions 76, 77 

Photosensitivity 76, 77, 262 

Phototoxic reactions 76, 77 

Physicochemical properties, drugs 64 

Physostigmine 106, 107 

Phytomenadione 144, 145 

Pigmentation, asadverse effect 264 

Pilocarpine 106, 332 

Pindolol 11 


Pioglitazone 246 

Piperacillin 254, 255 

Pirenzepine 108 

Piretanide 162 

Placebo 82, 83 

Plants 

cutaneous reactions to 76, 77 

drug sources 4, 5, 6, 7 

Plasma, freeze-dried 152 

Plasmalemma 130, 174 

drug action at 20, 256, 257 

Plasma proteins 152 

drug binding 30, 31, 32–33 

Plasma substitutes 152, 153 

Plasma volume expanders 152–153 

Plasmin inhibitors 148, 149 

Plasminogen activators 148, 149 

Plasmodium falciparum 276 

Plasmodium infections, drug treatment 276–277 

Platelet(s), serotonin action 116 

Platelet aggregation 150 

inhibitors 150–151,182,186 

stimulation 182 

Platinum-containing anticancer drugs 282 

Poisoning, treatment 294–297 

Polidocanol 192 

Polyarthritis, chronic (rheumatoid arthritis) 288, 

294, 344–345 

Polyene antibiotics 266, 267 

Polymorphisms see Genetic polymorphism 

Polymyxins 256 

Polyvinylpyrrolidone 152 

Posaconazole 266 

Postganglionic synapses 88 

Post-marketing surveillance 8 

Postmenopausal osteoporosis 334, 335 

Postsynaptic membrane 104, 174 

Potassium (K + ) 

depletion 162, 166, 170 

homeostasis disorders 166 

Potassium (K + )channel(s) 

antiarrhythmics blocking 136, 137 

openers 120 

sulfonylurea drug action 246, 247 

Potassium-sparing diuretics 164, 165 

Potency 62 

Pralidoxime 296, 297 

Pravastatin 156 

Praziquantel 274,275, 278 

Prazosin 98 

Preclinical testing 8, 9 

Prednisolone 227 

Preganglionic axons 88 

Pregnancy 

antiepileptics in 78, 324 

drug toxicity 78–79 

vomiting, management 328 

Premature labor, prevention 90, 92, 128, 129 

Premedication drugs 201 

Presystemic elimination 44–45 

insulin 242, 243 

Prilocaine 192, 193 

Primary active transport 26, 27 

Primary adrenocortical insufficiency 226 

Probenecid 336, 337 

Probiotic bacteria 346 

Procaine 192, 193 

Proenkephalin 194, 195 

Progabide 322, 325 

Progestin preparations 232–233 

oral contraception 234 

Progestin receptor antagonist 236, 237 

Progressive multifocal leukoencephalopathy 292 

Proguanil 276 

Prolactin inhibitors 112 

Prolactin release-inhibiting hormone (PRIH) 220, 

221 

Promethazine 114 

Proopiomelanocortin 194,195 

Propofol 204, 205 

Propranolol 11,100,101, 326 

Propylthiouracil 225 

Prostacyclin 182, 183 

Prostaglandins 

myometrial stimulation 128 

origin and actions 182, 183 

PGE2 182 

PGF2α 182, 183 

Prostaglandin synthase inhibitors 344, 345 

Prostatic cancer 220, 230 

Prostatic hypertrophy 98,110, 230 

Protamine 146 

Proteasome inhibitors 284 

Protein binding see Plasma proteins 

Protein kinase A92 

Protein synthesis 260, 261 

inhibitors (bacterial) 260–261 

receptors regulating 66, 67 

Proton pump inhibitors 168, 169 

Pseudomembranous enterocolitis 254 

Psilocin 298 

Psilocybin 298 

Psoriasis, plaque-type 292, 293 

Psychedelics 298–299 

Psychopharmacologicals 206–219 

Psychosis, treatment 216–219 

Psychosomatic reactions 206 

Psychotomimetics 298–299 

Pulmonary hypertension 120 

Pupillary sphincter tonus, lowering 108 

Purine antimetabolites 282, 283 

Purine metabolism, gout and 336, 337 

Pyrazinamide 264, 265 

Pyrethroids 274, 275 

Pyrimethamine 276 

Pyrimidine antimetabolites 283 

Q 

QT interval prolongation 218, 258, 262 

Quinagolide 112 

Quinine 276 

R 

Rabeprazole 168 

Racecadotril 172 

Racemate 64, 65 

Radioiodine 224 




Raloxifene 236, 237, 334 

Raltegravir 272 

Ranibizumab 286 

Ranitidine 114, 115, 168, 169 

RANK ligand (RANKL) 334, 335 

Rapamycin (sirolimus) 289, 290, 291 

Rasagiline 320 

Rasburicase 336 

Reboxetine 212, 213 

Receptor-mediated endocytosis 26, 27, 92 

Receptors 20, 66 

desensitization 92, 93 

drug interactions see Drug–receptor interactions 

recycling 92 

types 66–67 

Recombinant insulin 240 

Recombinant tissue plasminogen activator (rt-PA) 

148, 149 

Recreational drugs 96, 298–305 

Rectal administration 18, 19 

5α-Reductase 231 


Reduction reactions 36, 37 

Regional anesthesia 200 

Rehydration solutions 172 

Renal colic 108, 128 

Renal failure prophylaxis, diuretics 158 

Renal tubular reabsorption ofdrugs 42, 43 

Renin 126 


Renin–angiotensin–aldosterone (RAA) system 120, 

126, 127, 166, 316 

inhibitors 126–127 

Repaglinide 246 

Resistance plasmids 250 

Respiratory depression, opioid-induced 194, 197 

Respiratory tract 22 

Retarded drug release 12,13 

Reteplase 148, 149 

Reverse transcriptase 272 


Rhabdomyolysis 156 

Rheumatoid arthritis 288, 294, 344–345 

Ribavirin 271 

Ricinoleic acid 170 

Rifabutin 258 

Rifampicin 258 


St John’s wort interaction 38, 39 

tuberculosis 264, 265 

Rifampin 258, 264, 265 

Rimonabant 298, 338, 339 

Risedronate 334, 335 

Risk–benefit analysis 72, 78 

Risperidone 218, 219 

Ritonavir 272 

Rivastigmine 106 

“River blindness” 278 

Rofecoxib 186 

Rosiglitazone 246, 247 

Roxithromycin 262 

S 

Salbutamol 129, 340 

Salicylic acid 6, 7 

Salix 6, 7 

Salmeterol 340, 342 

Saluretics see Diuretics 

Saquinavir 272, 273 

Sarcoplasmic reticulum 130 

“Sartans” 126 

Scabies 274, 275 

Schistosoma mansoni 278, 279 

Schistosomiasis 278 

Schizophrenia, treatment 216–219 

Schmiedeberg, Oswald 3 

Scopolamine 6, 110, 111, 328, 329 

Secondary active transport 26 

Second-submission successor preparations 10 

Seizures 322, 323, 324 

Selectins 292, 293 

Selective estrogen receptor modulators 

(SERM) 236, 237 

Selective norepinephrine reuptake inhibitors 

(SNRIs) 88, 212, 213 

Selective serotonin and norepinephrine reuptake 

inhibitors (SSNRI) 212, 213 

Selective serotonin reuptake inhibitors (SSRIs) 116, 

210, 212, 213 

Selegiline 96, 320, 321 

Sensory nerves, sensitivity tolocal anesthetics 188, 

189 

Septic shock 318–319 

Serine/threonine kinase 284, 285 

Serotonin 97, 116–117 

appetite reduction 338 

inactivation 116,117 


mechanism of action 116,117 

as neurotransmitter 116 

occurrence and functions 116 

promoters of effects 116, 117 

receptor(s) 116 

receptor agonists 116, 326, 327 

receptor antagonists (5HT 3)116,329 

substrates (indirect mimetics) 96, 97 

Sertraline 212 

Serum sickness 74 

Sevoflurane 202 

Sibutramine 116,338, 339 

Signal transduction 66, 68, 69, 284–285 

Sildenafil 120 

Simvastatin 156 

Sinoatrial node, drugs controlling 130, 134, 135 

Sinus bradycardia 134 

Sinus tachycardia 134 

Sirolimus 289, 290, 291 

Sitagliptin 246, 247 

Sitaxentan 120 

Skin protectants, dermatological agents as 16,17 

Skin reactions, to drugs 76–77 

SLC (‘solute carrier’) transport proteins 28, 29 

Sleep disorders 330–331 

“Slow acetylators” 80 

“Slow metabolizers” 80, 81 

Slow-release tablets 12,13 


Smoking 

cessation, aids for 300 

consequences 302–303 

see also Nicotine 

Smooth (sER) endoplasmic reticulum 34, 35 

Smooth muscle 

catecholamine effects 90, 91 

drugs influencing 128–129 

organic nitrates effect 122, 123 

relaxation, parasympatholytics 108, 109 

see also Vascular smooth muscle 

Sodium (Na + ) 

homeostasis disorders 166, 167 

local anesthetic actions 188, 189 

transport in kidney 160, 161 

Sodium (Na + )channel 

blockade, local anesthetic action 188, 189, 192 

blocking antiarrhythmics 134, 135, 136–137 

cardiac glycoside action 132 

muscle depolarization 176,177 

Sodium chloride (NaCl) reabsorption 158, 160, 161, 

166 

Sodium nitroprusside 122, 123 

Sodium picosulfate 170 

Sodium thiopental 204, 205 

Sodium thiosulfate 296 

Solifenacin 108 

Somatic nervous system 86 

Somatomedin C220 

Somatostatin 220, 221 

Sorafenib 284, 285 

Sorbitol 160 

Spasmolysis 108, 128, 129 

Spinal anesthesia 188, 200 

Spinal cord, impulse transmission 174 

Spironolactone 164, 316 

Sprays, drug administration 14 

Squamous epithelium 22, 23 

Staphylococci, penicillin Gresistance 252, 253 

Statins 156, 157 

Status epilepticus 206, 322 

Stavudine 272 

Steady state concentration (Css) 50, 51, 52 

Steroid hormone, receptors 66, 67 

Stevens–Johnson syndrome 76 

St John’s wort 28, 38, 39, 210 

Streptokinase 148, 149 

Streptomyces 260, 261, 262 

Streptomyces hydroscopicus 290 

Streptomyces pilosus 294 

Streptomyces tsukubaensis 290 

Streptomycin 264, 265 

Stress incontinence 108 

Stroke 134 

Strontium ranelate 334 

Structure–activity relationships, 

sympathomimetics 94–95 

Strychnine 174, 175 

Subcutaneous injection 18,19 

Sublingual route, administration 18, 19,22 

Substance P118,119,328 

Successor preparations 10, 11 

Succinylcholine 176,177 

Sulbactam 254, 255 

Sulfadoxine 276 

Sulfamethoxazole 256, 257 

Sulfapyridine 256, 257 

Sulfasalazine 256–257, 344, 345 

Sulfonamides 256, 257 

Sulfonylurea drugs 246, 247 

Sulfotransferases 40, 41 

Sulfoxidation reactions 36, 37 

Sumatriptan 116, 117, 326, 327 

Sunitinib 284 

Suramin 278 

Surface anesthesia 188, 192 

Suxamethonium 177 

Sympathetic nervous system 86–101 

activation, response to 86, 87,120 

function and actions 86, 87 

heart function and 130 

neurotransmitters 88, 89 

structure 88–89 

Sympatholytics, cardiac function and 98, 99, 130 

α-Sympatholytics 98, 99 

Sympathomimetics 


direct-acting 94, 95 

indirect 94, 96–97 

structure–activity relationships 94–95 

α-Sympathomimetics 98, 99, 340, 341 

β2-Sympathomimetics 90, 128 

allergies 340 

asthma 340, 342, 343 

COPD 342 

T 


Tachyarrhythmias 100 

Tachykinins 118 

Tachyphylaxis 92, 96, 122 

Tacrolimus 290, 291 

Talinolol 11 

Tamoxifen 236, 237 

Tamsulosin 98 

Tardalafil 120 

Tardive dyskinesia 218,320 

Taxoids 280, 281 

Tazobactam 254 

Teicoplanin 254 

Telbivudine 270 

Telithromycin 262 

Temazepam 330, 331 

Temsirolimus 290 

Tenecteplase 148, 149 

Tenoposide 282 

Teratogenicity 78, 280 

Terbutaline 340, 341 

Terfenadine 114 

Teriparatide 248 

Testosterone 230, 231, 238 

Testosterone derivatives 230 

Testosterone undecanoate 230, 231 

Tetanus toxin 174, 175 

Tetracyclines 260, 261, 262 


therapeutic use, actions 263 

Δ 9 -Tetrahydrocannabinol (THC) 298, 338 



Tetrahydrofolate synthesis inhibitors 256, 257, 282 

Tetrahydrofolic acid (THF) 256, 282 

Thalidomide 78, 284 

Thallium salts, poisoning 296, 297 

Theophylline 128, 129, 340 

Therapeutic index 72 

Thiamazole 225 

Thiazide diuretics 162, 163, 308, 309 

Thioamides 224, 225 

Thiocyanate 296 

Thiopental 204, 205 

Thiopurine methyltransferase (TMPT) 80 

Thiourea-derivatives 224, 225 

Thrombocytopenia, heparin-induced 146 

Thromboembolism, prophylaxis 144 

Thrombosis 158 

arterial, or venous 142 

coronary 314, 315 

prophylaxis and therapy 142–151 

Thromboxane A2 182, 183, 186 

Thymidine kinase 270 

Thymoleptics see Antidepressants 

Thyroglobulin 224 

Thyroid hormones 222–223, 224 

receptors 66, 67, 222 

release 222, 224 

Thyroid peroxidase 224 

Thyroid-stimulating hormone (TSH) 220, 221, 222, 

223 

receptors, antibody action 224, 225 

Thyroid suppression therapy 222, 224 

Thyrotoxicosis 224–225 

Thyrotropin releasing hormone (TRH) 220, 221 

Thyroxine (T4) 222, 223, 224 

Tiagabine 322, 325 

Ticlopidine 150 

Tigecycline 262 

Tight junction 22 

Time course, of drug concentration 48–49, 70–71 

after irregular intake 50, 51 

after repeated dosing 50, 51 

dose-dependence of effect 70, 71 

Time–effect curves 70, 71 

Timidazole 258 

Tincture 4 

Tiotropium 111, 128, 129, 342 

Tirofiban 150 

Tissue plasminogen activator (t-PA) 148,149 

T-lymphocytes 74,75, 288, 289 

calcineurin inhibitor action 290, 291 

proliferation inhibition 290 

TH1, TH0and TH2 types 340, 341 

T-helper cells 288, 290, 291, 292, 340, 341 

Tobacco 302 

Tobramycin 261 

Tocolytics 90, 92, 128, 129 

Toll-like receptors (TLR) 318, 319, 346 

Tolonium chloride 296, 297 

Tolterodine 108 

Toluidine blue 296, 297 

Topoisomerase II (gyrase) inhibitors 258, 259 

Topotecan 282 

Torasemide 162 

Total clearance ofdrug (Cltot) 46 

Total intravenous anesthesia (TIVA) 204 

Toxic epidermal necrolysis (TEN) 76, 77 

Toxicity (drug) see Adverse drug effects (ADEs) 

Toxicological investigations 8 

Toxins 22, 172 

Trabectin 282 

Tramadol 196, 198 

Transcytosis 24, 26, 27 

Transdermal delivery 18, 19 

Transferrin 140 

Transpeptidase 252, 254 

Transplacental passage, of drugs 78, 79 

Transplant rejection, prevention 288, 290 

Transport proteins 20, 21 

Trastuzumab 284, 286, 287 

Tremor, essential 100 

Triamcinolone 227 

Triamterene 164, 165 

Triazolam 330, 331 

Triazole derivatives 266, 267 

Trichomonas vaginalis 258, 259 

Tricyclic antidepressants 210, 212, 213 

Triiodothyronine (T3) 222, 223 

Trimethoprim 256, 257 

Triptans 116, 326, 327 

Triptorelin 220, 230 

Tropical diseases, treatment 278–279 

Tropisetron 328 

Trypanosoma brucei 278, 279 

Trypanosoma cruzi 278 

Trypanosomiasis 278, 279 

Tuberculosis 264, 265 

Tubular reabsorption of drugs 42, 43 

Tumor necrosis factor α (TNFα) 344, 346 


Tyrosine kinase 66, 67, 284, 285 


Tyrothricin 256 

U 

Ubiquitin 284, 285 

Ulcerative colitis 256, 346–347 

Urate levels 336 

Urge incontinence 108 

Uric acid 337 

Uricolytics 336 

Uricostatic agents 336, 337 

Uricosurics 336, 337 

Urinary incontinence 108 

Urokinase 148, 149 

Urticaria 76 

V 

Valaciclovir 270 

Valganciclovir 270 

Valproate/valproic acid 322, 323 


migraine 326 

Vancomycin 254, 255 

van der Waals forces 32, 60, 61 

Vardenafil 120 

Varenicline 300 

Varicella-zoster virus 270, 271 


Varicosities, sympathetic nerve 88, 89 

Vascular disease, smoking causing 302 

Vascular endothelial growth factor 

(VEGF) 284, 285, 286, 287 

Vascular smooth muscle 

calcium antagonist actions 124, 125 

organic nitrate action 122, 123 

permeability 341 

tone decrease 120 

Vascular space 30 

Vasculitis, immune-complex 74,75 

Vasoconstriction 90, 98,116,341 

Vasoconstrictors 

with local anesthetics 190 

topical 98 

Vasodilatation 90 

histamine action 114 

serotonin role 116 

Vasodilators 120–125 

calcium antagonists 124–125 

counter-regulatory responses due to120, 121 

effect in cardiac disease 130 

organic nitrates 122–123 

Vasopressin see Antidiuretic hormone 

(ADH; vasopressin) 

Vasorelaxant mediators 120 

Vecuronium 178 

Venlafaxine 212, 213 

Venous vasodilators 120 

Verapamil 124, 125, 134, 312 

Very-low-density lipoprotein (VLDL) 154, 155 

Vesicular acetylcholine transporter (VAChT) 104 

Vesicular monoamine transporter (VMAT) 88, 89, 

112 

Vesicular transport (transcytosis) 24, 26, 27 

Vestibular toxicity 254, 262, 263 

Vigabatrin 322, 323, 325 

Vildagliptin 246 

Vinblastine 280 

Vinca alkaloids 280, 281 

Vincristine 280 

Viral infection treatment 268–273 

Viral replication 268, 269 

Virustatic antimetabolites 268, 269, 270 

Vitamin B 12 138, 139 

deficiency 138, 139 

Vitamin B12a 138, 296 

Vitamin D(cholecalciferol) 248, 249 

Vitamin Dhormone 248 

Vitamin K144–145 

Vitamin Kantagonists 144–145 

“Vitamin Kbomb” 144 

Volume depletion, acute 152, 153 

Volume of distribution 30 

apparent 30, 46 

Vomiting 280, 328–329 

drug-induced 194, 328, 329 

in pregnancy 328 

see also Antiemetics 

Voriconazole 266 

W 

Warfarin 144,145 

Water deficit 166,167 

Water disorders 166–167 

Water-soluble ointment 16, 17 

Weight loss 338, 339 

Wepfer, Johann Jakob 3 

Wernicke–Korsakoff syndrome 304 

Withdrawal reactions 78, 196, 300 

Worm infestations, drug treatment 274,275 

Wuchereria bancrofti 278, 279 

X 

Xylometazoline 98 

Z 

Zalcitabine 272 

Zaleplon 330, 331 

Zanamivir 270 

Ziconotide 192–193 

Zidovudine 272 

Ziprasidone 218 

Zolpidem 330, 331 

Zonulae occludentes 22, 190 

Zonula occludens 22 

Zopiclone 330, 331 

Z-substances 330

Thieme: Color Atlas of Pharmacology

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