INDEX Note: Page numbers in bold refer to a text discussion of the entry abatacept, 636, 695 release cotransmitters, 497 acquired immuno deficiency syndrome abciximab (ReoPro), 233 synthesis and metabolism, 498–501 (AIDS), 3, 387, 414, 542, ABC transporters, 263 vesicles, 500 590–591, 638, 659, 678–9 polymorphisms, 263 acetylcholine receptors, 501–4 HIV infection, 382, 659 substrates, 263 muscarinic (mAChR), 189, 321, acrylamide derivatives, 335 absorption, 21, 31–44 339, 360, 478, 486, 498, action potential, 468 rate, 39, 74 503, 524, 604 activator protein 1 (AP-1), 630 time constant, 74 muscarinic agonists acyclovir, 15, 655–6 absorption distribution metabolism and (parasympathomimetics), Acyl-CoA-cholesterol-acyltransferase elimination (ADME), 671, 695, 504, 506–7 (ACAT), 448 700–707 muscarinic antagonists inhibitors, 448–9 absorption distribution metabolism (parasympatholytics), 338, 498, adalimumab, 239, 627, 636, 695 excretion and toxicity 504, 506–7 adamantanes, 656–7 (ADMET), 701 muscarinic autoreceptors, 501 adaptation, 42, 118, 121–9, 580, 582, 648 abuse see dependence muscle-type receptor, 503 adaptor protein, 112, 113, 118, 218, 219, acamprosate, 128–9 nicotinic, 112, 126, 140, 179, 180, 182, 231, 434 acarbose, 458, 460 184, 186–7, 504–6 addiction, 7, 122–9, 583, 584 acceptable daily intake (ADI), 669 nicotinic (nAChR), 501–3 adefovir, 659 ACE see angiotensin-converting enzyme nicotinic agonists, 504 adenine nucleotide translocase (ANT), (ACE) nicotinic antagonists, 504 411, 436 acebutol, 325, 492–3 nicotinic autoreceptors, 501 adenosine, 157, 190, 192, 336, 501, aceclidine, 504 COPYRIGHTEDacetylcholinesterase (AChE), 65,MATERIAL 137, 359, 553–64, 656 acetylation, 62, 67, 135 497–8, 507, 692 adenosine deaminase (ADA), 304, 419, 555–6 histone acetyltransferase, 135 inhibitors (AChEIs), 499–500, 505, 526 ADA deficiency syndrome, 563 histone deacetylase, 135 acetylcholine transporters, 360 adenosine diphosphate (ADP), 554–64 acetylcholine (ACh), 190, 194, 496–501, vesicular ACh transporter 1 (VAChT1), adenosine kinase, 556 512, 513, 515 498, 500 adenosine monophosphate (AMP), 555–64 binding protein, 116, 179 acetyl-CoA, 67, 440, 441, 497, 499, 653 adenosine triphosphate (ATP), 190, ganglionic neurotransmission, 479, 503, 506 acetyl-CoA transporter (ACATN), 499 553–64 precursors, 499 acetylprocainamide, 338 adenylate kinase, 555 release, 118, 321, 351, 475, 479, acidification, 56, 161, 169, 355–6, 381, adenylyl cyclase, 195–6 487, 488, 501, 512, 580 475, 684 adesleukin, 638 General and Molecular Pharmacology: Principles of Drug Action, First Edition. Edited by Francesco Clementi and Guido Fumagalli. © 2015 John Wiley & Sons, Inc. Published 2015 by John Wiley & Sons, Inc. 0002534462.indd 714 5/11/2015 2:38:20 PM INDEX 715 adherent junctions see junctions adrenocorticotrope hormone (ACTH), 190, amisulpride, 517–18 adhesion molecules, 219, 220, 222, 227, 221, 481, 489, 494, 523, 567, amitriptyline, 35, 49, 71, 338, 486, 515, 229, 233, 324, 466, 473, 523, 570, 574 517–18, 682 628, 634, 636 adverse reactions, 7, 36, 259, 262, 290, amoxicillin, 34, 642 adhesive receptors, 225–6 291, 682, 698 AMPA receptors see glutamate receptors drug targeting, 233–4 affinity, 95, 96, 99, 101, 103, 104, 107, 108 amphetamines, 124, 126, 361, 366, 485, 515 adipocytes, 282, 393, 458, 460, 563, 586, agomelatine, 517 3,4-methylenedioxy-N- 609, 619 agonist, 102 ethylamphetamine (MDEA), 515 adrenocorticotropic hormone (ACTH), agonists 3,4-methylenedioxy-N- 190, 221, 481, 489, 494, 523, inverse, 107–8 methylamphetamine (MDMA), 567, 570, 574 partial, 104–5 122, 124, 366, 370, 515 administration routes, 31–43 Agouti-related peptide (ARP), 569 amphotericin B, 651–4, 661 dermal route, 37–8 AIDA, 550 ampicillin, 14, 34, 642, 679, 685 drip injection, 35 AIDS see acquired immuno deficiency amprenavir, 387, 393 drug delivery, 42–3 syndrome (AIDS) anacetrapib, 449–50 drug targeting, 43 A-kinase-anchoring protein (AKAP), 196, 198 anakinra, 628, 636, 695 enteral route, 33 Akt, 169, 170, 413 analgesia, 576–9 inhalation route, 36–7 alanine (β-), 365 anandamide (AEA), 112, 585–7, 587, 593–5 intradermal route, 36 Albright’s hereditary osteodystrophy, 194 anaphylaxis, 492, 573, 629 intramuscular route (i.m.), 36 albumin, 21, 50, 55, 59, 243, 290, 421, androgen receptor, 272, 281 intravascular route (i.v.), 35 614, 681 poly-Q tract polymorphism, 281 mucosal routes, 38 alcohol dehydrogenase, 65, 574 androgens, 272, 281, 283, 672 oral route, 33–5 alcoholism, 574 anesthetics, 12, 21, 31, 33, 37, 94, 319, parenteral routes, 35–6 aldehyde dehydrogenase, 514 321, 323–6, 336, 437, 491, 534, rectal route, 35 aldosterone, 167, 273, 280, 479, 493 540, 549, 567 subcutaneous route, 36 alefacept, 628, 636 general, 336, 534, 536–7, 540 sublingual route, 35 aleglitazar, 448 local, 3, 21, 33, 37, 94, 319, 323–6, 329, systemic administration, 31 alemtuzumab, 239, 628, 636, 695 437, 491 topical/regional routes, 31, 37 alfentanil, 573 angina, 492–3, 602 transcutaneous route, 37–8 alfuzosin, 492 angiotensin-converting enzyme (ACE), adrenal cortex, 280, 386 alkalinization of urine, 56, 169, 684 264, 381, 386, 567 adrenaline, 321, 371–2, 452, 478, 484–5, alkylamines, 527, 651 inhibitors, 15, 42, 264, 347, 349, 386, 492, 685 alkylating agents, 417 679–80 adrenal medulla, 168, 373, 478, 479, 496, allopurinol, 629, 683 angiotensin II, 15, 190, 199–200, 381, 386, 574, 620 allosteric modulators, 102, 103 479, 571, 603, 609 adrenergic and noradrenergic systems, agonist, 103 animal models, 15, 46, 163, 254, 275, 290, 480–481 antagonists, 103 298, 326, 328, 413, 442, 443, control of pituitary functions, 481 potentiators, 103 449, 461, 539, 569, 590, 592, depression, wakefulness and feeding almotriptan, 517 619, 637, 702 behavior, 481 alprazolam, 71, 157, 539, 685 animal testing see toxicity distribution, 480 alteplase, 694–5 antagonists, 102 functions, 480 alternative splicing, 115, 167, 203, 237, competitive, 102 adrenergic receptors, 487 286, 351, 456, 499, 566, 619 insurmountable, 102–3 α-adrenergic receptors, 190, 191, 194, 487 alternatives to animal experiments, 672 surmountable, 102 α1 agonists, 490 Alzheimer’s disease, 169, 505 antazoline, 527 α2 agonists, 491 amanita muscaria, 501 anthracenediones, 416, 423 α antagonists, 491 amantadine, 656 anthracyclines, 416, 422–3, 437, 679 β-adrenergic receptors, 190–192, 194, ambenonium, 500, 505 antiarrhythmic drugs, 320, 338 196, 198–200, 488 amidepsine, 440, 446 class II: β-adrenergic antagonists, 15, β1, 264 amikacin, 642, 647 251, 263, 264, 325, 349, 493 β2, 265 amiloride, 49, 320, 354–6, 399, 557, 600 class III: VGKC blockers, 320, 325 β2 agonists, 491 amineptine, 366 class IV antiarrhythmic: VGCC β antagonists, 15, 251, 263, 264, 325, amine transporters, 360 blockers, 320, 325 349, 493 aminoethyl-hydroxyindole, 509 class I: VGSC blockers, 323, 325 β1 polymorphisms, 264 aminoglycosides, 642–3, 647, 679 antibiotics, 4, 13, 14, 26, 36, 37, 49, 56, β2 polymorphisms, 265 aminopyridine, 147, 320, 336, 505 263, 422, 641–60 drugs and therapeutic use, 490–493 aminopyrine, 612 antineoplastic, 422 functions, 489 amiodarone, 49, 71, 320, 325, 338, 354–5, cytoplasmic membrane function localization, 489 681–3 inhibitors, 649–50 0002534462.indd 715 5/11/2015 2:38:20 PM 716 INDEX antibiotics (cont’d ) antiviral drugs, 654–60 association constant, 95 DNA synthesis and replication anti HBV, 659 astemizole, 337–8 inhibitors, 649 anti HCV, 658–9 asthma, 233, 264–5, 280, 290–291, 335, mechanism of action, 642–3 interferons, 659 339–40, 384, 491–3, 506–7, 524, peptidoglycan polymerization NS5B inhibitors, 658 526, 561–4, 570, 573, 600, inhibitors, 645 NS3/4 inhibitors, 658 615–16, 618, 620, 628, 636, 679 peptidoglycan synthesis inhibitors, anti HIV, 659 astrocyte, 362, 369, 466–7, 592, 598, 603 643–5 integrase inhibitors, 660 ataxia telangiectasia, 286 resistance, 650 protease inhibitors, 393 atenolol, 27, 57, 89, 98, 325, 346, 392, ribosomes, 647 reverse transcriptase inhibitors, 659 492, 493 transcription inhibitors, 646 virus entry inhibitors, 660 atorvastatin, 71, 440–441, 450, 685 translation inhibitors, 646–9 anti influenza virus, 656–7 ATP binding cassette, 263, 345, 493 antibodies, 636 mechanism of action, 654–5 atracurium, 504, 506 monoclonal (mAbs), 17, 113, 115, resistance, 656–60 atrial natriuretic peptide, 114 213–15, 233, 239, 417, 427–8, anxiety, 14, 363, 481, 493–4, 511, 517, atropine, 57, 491, 498, 504–8, 680 635, 639, 695 529, 532–4 methylnitrate, 506, 507 monoclonal humanized, 239 Apaf-1, 408, 411 autacoids see specific agents monoclonal therapeutic, 239 apamin, 339 autoimmunity, 626 polyclonal, 635 apolipoproteins, 443, 448, 540 autonomic nervous system, 343, 477–95, anticholinergic agents, 7, 34, 486, 498, apomorphine, 489, 494, 540 553, 609, 619 504, 507, 527, 680 apoptosis, 389, 558, 562–3 avasimibe, 449 antidepressants, 14, 15, 34, 35, 61, 259, regulators, 409 avidity, 48, 52, 81 263, 338, 364, 366, 370–372, apoptosis-inducing factor (AIF), 411 azacytidine (Vidaza), 426 481, 486, 511–12, 515, 515–19 apoptotic bodies, 407 azathioprine, 62, 262, 626–31, 635–6, 679 antidotes, 684 eat me signals, 408 azimilide, 325, 337–8 antiemetics, 65, 263, 338, 517 picnosis, 408 azithromycin, 634, 642, 683–4 antiepileptic drugs, 51, 320, 322–3, 325, apoptotic pathway, 408–11 azoles, 651–4 327, 369, 472, 530, 539 extrinsic pathway, 408, 409 aztreonam, 642 antifungal drugs, 338, 651–4 intrinsic mitochondrial pathway, acting on cytoplasmic membrane, 652–3 408, 411 bacitracin, 642 DNA and protein synthesis apraclonidine, 492 baclofen, 531, 533, 537–40