DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

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Maprotiline (LUDIOMIL) 100–150 O NE 0/+ 3+ 2+ 2+ 2+ 0/+ + 2+ 2+Nortriptyline (PAMELOR) 75–150 O NE 0 + + + + 0/+ + 2+ 2+Protriptyline (VIVACTIL) 15–40 O NE 2+ 2+ 0/+ + 2+ 0/+ + 2+ 3+Selective Serotonin Reuptake Inhibitors(±)-Citalopram (CELEXA) 20–40 O 5-HT 0/+ 0 0/+ 0 0 3+ 0 3+ 0(+)- Escitalopram (LEXAPRO) 10–20 O 5-HT 0/+ 0 0/+ 0 0 3+ 0 3+ 0(±)-Fluoxetine (PROZAC) 20–40 O 5-HT + 0/+ 0/+ 0 0 3+ 0/+ 3+ 0/+Fluvoxamine (LUVOX) 100–200 O 5-HT 0 0 0/+ 0 0 3+ 0 3+ 0(–)-Paroxetine (PAXIL) 20–40 O 5-HT + 0 0/+ 0 0/+ 3+ 0 3+ 0(+)-Sertraline (ZOLOFT) 100–150 O 5-HT + 0 0/+ 0 0 3+ 0 3+ 0NHCH 3CHAPTER 15DRUG THERAPY OF DEPRESSION AND ANXIETY DISORDERSClCl(Continued)401
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Goodman & Gilman’sThe Pharmacolog
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Goodman & Gilman’sThe Pharmacolog
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viiiCONTENTS22. Treatment of Centra
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xiiCONTRIBUTORSBruce A. Chabner, MD
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xivCONTRIBUTORSJonathan M. Meyer, M
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xviCONTRIBUTORSRobert H. Tukey, PhD
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4SECTION IGENERAL PRINCIPLESbegan i
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6SECTION IGENERAL PRINCIPLESTARGETS
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its mission cannot possibly be acco
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10SECTION IGENERAL PRINCIPLESHMG-Co
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12SECTION IGENERAL PRINCIPLESit to
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14SECTION IGENERAL PRINCIPLESviolat
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16SECTION IGENERAL PRINCIPLESyears.
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18SECTION IGENERAL PRINCIPLESDRUGDO
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20SECTION IGENERAL PRINCIPLEScompou
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22SECTION IGENERAL PRINCIPLESgroups
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24SECTION IGENERAL PRINCIPLESphysic
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26SECTION IGENERAL PRINCIPLESdivers
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28SECTION IGENERAL PRINCIPLESphase
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30SECTION IGENERAL PRINCIPLESDivisi
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32SECTION IGENERAL PRINCIPLESconsis
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34SECTION IGENERAL PRINCIPLEStherap
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36SECTION IGENERAL PRINCIPLESMainte
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38SECTION IGENERAL PRINCIPLESThe ne
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42 signaling compounds are termed a
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44 receptors, but because the endog
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46 ligand-receptor complex, LR*. Th
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48 agonist plus an effective concen
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50SECTION IGENERAL PRINCIPLESPRESCR
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52 constrained by compartmentation
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54A. Activation by Ligand Binding o
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56 Second MessengersSECTION IGENERA
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58 markedly stimulates Ca 2+ flux,
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60 voltage-gated (Jegla et al., 200
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62SECTION IA(a) UnligandedreceptorI
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64 from the complex allowing the p5
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66 upon binding ligand. Other membe
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68 FADD/TRAF2, and caspase 8, which
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70 of cyclic GMP are also increased
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72 Vo NK, Gettemy JM, Coghlan VM. I
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74100ADeathSECTION I% of Population
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76SECTION IGENERAL PRINCIPLESisofor
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78SECTION IGENERAL PRINCIPLESantago
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80SECTION IGENERAL PRINCIPLESarrhyt
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82SECTION IGENERAL PRINCIPLESThe in
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84SECTION IGENERAL PRINCIPLESGastri
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86SECTION IGENERAL PRINCIPLESTable
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Page 114 and 115:
90TherapeuticeffectMetabolismTExcre
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92Clearance organs(liver, kidney)Co
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94Passive transport (downhill trans
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96SECTION IGENERAL PRINCIPLESNoncom
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Table 5-1Regulation of Transporter
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100ExtracellularSECTION IGENERAL PR
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Table 5-2Families in the Human Solu
Page 128 and 129:
Table 5-3The ATP Binding Cassette (
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Table 5-4ABC Transporters Involved
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108SECTION IGENERAL PRINCIPLESIn th
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110SECTION IGENERAL PRINCIPLESthe u
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112SECTION IGENERAL PRINCIPLESOC +B
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114SECTION IGENERAL PRINCIPLEStrans
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116SECTION IGENERAL PRINCIPLESincre
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118SECTION IGENERAL PRINCIPLESHaseg
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120SECTION IGENERAL PRINCIPLESmulti
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124SECTION IGENERAL PRINCIPLESconst
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126SECTION IGENERAL PRINCIPLESorall
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Table 6-2Major Reactions Involved i
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130SECTION IGENERAL PRINCIPLESco-ad
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132SECTION IGENERAL PRINCIPLESreact
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134SECTION IGENERAL PRINCIPLESSN-38
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136SECTION IGENERAL PRINCIPLESnon-c
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Table 6-4Indications and Unwanted S
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140SECTION IGENERAL PRINCIPLESsyndr
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142SECTION IGENERAL PRINCIPLESthe t
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146SECTION IGENERAL PRINCIPLESstres
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148SECTION IGENERAL PRINCIPLESsubst
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150SECTION IGENERAL PRINCIPLESEthni
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152Monogenic traitMultigenic traitS
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154SECTION IGENERAL PRINCIPLESlikel
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15625060Common genetic formSECTION
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158AgeneCYP3A5*1 allele123456789101
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Table 7-3Examples of Genetic Polymo
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162warfarinCYP2C9hydroxywarfarin5SE
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164SECTION IGENERAL PRINCIPLESin a
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166SECTION IGENERAL PRINCIPLESBIBLI
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168SECTION IGENERAL PRINCIPLESRosne
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172 regulation of sacral parasympat
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174 third lumbar segment. The axons
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176 ganglia, the ratio of pregangli
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Table 8-1Responses of Effector Orga
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Table 8-1Responses of Effector Orga
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182 While these criteria are applic
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184 those vesicles in close proximi
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186HemicholiniumAcCoA + CholineChol
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188 in transmitter release comes fr
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190 Subtypes of Nicotinic Acetylcho
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Table 8-3Characteristics of Muscari
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194 and inhibition of excitable mem
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196SECTION IINEUROPHARMACOLOGYcorre
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Table 8-5Characteristics of Plasma
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200 by activation of β 2adrenergic
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202SECTION IIHOHOCH 3 OHOHOHHO H OH
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Table 8-6Characteristics for Adrene
Page 230 and 231:
Table 8-7Representative Agents Acti
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208α 1A α 2A β 1NH 2NH 2NH 2SECT
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210 uncoupling of G-protein signali
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212 and atenolol, which antagonize
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214 to inhibit its own release. NPY
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216 Furchgott RF. Endothelium-deriv
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218 Nucleotides as Regulators of Ce
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220 M 1through M 5muscarinic recept
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222 difficult to observe with admin
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224 The difficulty in developing su
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226 neurotransmitter release, the p
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228 parasympathetic postganglionic
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230 sympathetic cholinergic fibers,
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Table 9-3Muscarinic Receptor Antago
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234 efficient, resulting in the del
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236 Chapple C, Khullar V, Gabriel Z
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Page 264 and 265:
240 In the 1950s, a series of aroma
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242 tertiary amine physostigmine ex
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Table 10-1Chemical Classification o
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246 The sites of action of anti- Ch
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248 tolerance reassessments, and re
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250 animals after long- term exposu
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252 When the diagnosis of myastheni
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254 Gallo MA, Lawryk NJ. Organic ph
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256 the inhibitory amino acids (γ-
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258 abundance in muscle, along with
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260 and the remainder of the muscle
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262SECTION IINEUROPHARMACOLOGYmyeli
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Table 11-2Classification of Neuromu
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266 Preventing Trauma During Electr
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268 reduced renal function (pancuro
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270 that are selective for M 1musca
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272 and its metabolites are elimina
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274 gastric emptying. Although the
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276 Volle RL. Nicotinic ganglion-st
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278Adrenergic AgonistsDirect-acting
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280SECTION IITable 12-1Chemical Str
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282 when both types of receptors ar
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284 falls (epinephrine reversal). A
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286 increase of 20-30% in oxygen co
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288 Therapeutic Uses and Status. NE
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290 may occur, particularly in pati
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292HONOHHNH 3 COCOOHNHC(CH 3 ) 3HOH
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294 agonist that has twice the pote
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296 these receptors is high, althou
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298 CNS. Amphetamine is one of the
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300 treatment of attention-deficit/
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302 syndrome and idiopathic autonom
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304 transient or may respond to adj
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306Alkylating agentCH 3OCH 2 CHNCH
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308 Syncopal episodes also have occ
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310 ingestion of tyramine-containin
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312OOOOHHNOOHHNOBISOPROLOLBETAXOLOL
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314 Billman, 2000; Brodde and Miche
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316 The β receptors mediate activa
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318 treatment for patients with all
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320 for an individual patient shoul
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322SECTION IINEUROPHARMACOLOGYTable
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324SECTION IINEUROPHARMACOLOGYTable
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326 nadolol is its relatively long
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328 or membrane-stabilizing activit
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330 and possibly papaverine-like re
Page 363 and 364:
332 Gupta S, Wright HM. Nebivolol:
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336SECTION IINEUROPHARMACOLOGYNH 2N
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Table 13-1Serotonin Receptor Subtyp
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340SECTION IINEUROPHARMACOLOGY5-HT
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Table 13-3Some Actions of 5-HT in t
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344 suppressant in the management o
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346HNHNSECTION IICH 2H 3 CNHSO 2 CH
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Table 13-6Natural and Semisynthetic
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350 mCPP, an active metabolite of t
Page 384 and 385: 352 Oby AADC, the same enzyme that
Page 386 and 387: 354ND1 receptor familyD2 receptor f
Page 388 and 389: 356SECTION IINEUROPHARMACOLOGYMesoc
Page 390 and 391: 358 receptor agonist and a weak D 1
Page 392 and 393: 360 Delgado PL, Charney DS, Price L
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Page 396 and 397: 364 system and integrate somatic an
Page 398 and 399: 366 from the bloodstream into the b
Page 400 and 401: 368A Ion channels α 1 subunits for
Page 402 and 403: Table 14-1Subtypes of Ca 2+ Channel
Page 404 and 405: 372SECTION IINEUROPHARMACOLOGYselec
Page 406 and 407: 374Presynapticneuron11 107Neurotran
Page 408 and 409: 376SECTION IINEUROPHARMACOLOGYParav
Page 410 and 411: (including penicillin and pentylene
Page 412 and 413: 380 (NMDA) receptors and non- NMDA
Page 414 and 415: Table 14-4Subtypes of Muscarinic Re
Page 416 and 417: 384 thence to adenylyl cyclase. α
Page 418 and 419: 386HistamineNH 2HNNSECTION IIH 1 H
Page 420 and 421: 388β-LPHSignal peptideJP ACTH γ-L
Page 422 and 423: 390 Oglutamate (NMDA)-mediated neur
Page 425 and 426: 392 (e.g., ethanol) can exert relat
Page 427 and 428: 394 Bleich S, Romer K, Wiltfang J,
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Page 431 and 432: 398 disease, especially myocardial
Page 433: 400SECTION IINEUROPHARMACOLOGYTable
Page 439: (±)-Mirtazapine (REMERON) 15-45 O
Page 442 and 443: same time, selective inhibitors of
Page 444 and 445: of the studies included in the meta
Page 446 and 447: Table 15-3Disposition of Antidepres
Page 448 and 449: anorgasmia, and ejaculatory delay;
Page 450 and 451: benzodiazepines and β adrenergic a
Page 452 and 453: Rush AJ, Trivedi MH, Wisniewski SR,
Page 454 and 455: Pharmacotherapy of Psychosisand Man
Page 456 and 457: of substance-induced psychoses, rem
Page 458 and 459: Antipsychotic agents with greater w
Page 460 and 461: monitoring for agranulocytosis has
Page 463: Atypical Antipsychotic AgentsAripip
Page 467: Table 16-2Potencies of Antipsychoti
Page 470 and 471: antimuscarinic activity, but is rar
Page 472 and 473: symptoms of psychosis. The behavior
Page 475: Iloperidone 2D6 and 3A4 convert ilo
Page 479 and 480: pass many preclinical in vivo assay
Page 481 and 482: Table 16-4Neurological Side Effects
Page 483 and 484: antipsychotic agent. That clonazepa
Page 485 and 486:
serum triglycerides may change 70-8
Page 487 and 488:
and dosage adjustment can minimize
Page 489 and 490:
inhibit glutamatergic neurotransmis
Page 491 and 492:
maternal levels, and are not associ
Page 493 and 494:
safely to reverse the syndrome of n
Page 495 and 496:
hygroscopic and less irritating to
Page 497 and 498:
Goodwin FK, Fireman B, Simon GE, et
Page 499 and 500:
Schou M, Amdisen A, Thomsen K, et a
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Hypnotics and SedativesS. John Mihi
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Table 17-1Benzodiazepines: Names an
Page 505 and 506:
REM cycles, the number of shifts to
Page 507 and 508:
agents are considerably more effect
Page 509 and 510:
patients and in patients with chron
Page 512 and 513:
depression in the neonate. Abuse by
Page 514 and 515:
Flumazenil is available only for in
Page 517 and 518:
The carbonyl group at position 2 ta
Page 519 and 520:
Absorption, Fate, and Excretion. Fo
Page 521 and 522:
Meprobamate. Meprobamate a bis-carb
Page 523 and 524:
Side effects of hypnotic agents may
Page 525 and 526:
Lader M, File S. The biological bas
Page 527 and 528:
Opioids, Analgesia, andPain Managem
Page 529 and 530:
Table 18-1Actions and Selectivities
Page 531 and 532:
Proorphanin485OrphaninProdynorphinP
Page 533 and 534:
addressHOOOHNHN- OOCLeu-enkephalin(
Page 535 and 536:
played by the organ systems with wh
Page 537 and 538:
PAG OPIATE ACTIONPeriaqueductalgray
Page 539 and 540:
Factors Exacerbating Opiate-Induced
Page 541 and 542:
ful anti-nausea and anti-emetic dru
Page 543 and 544:
cells of the immune system and indi
Page 546 and 547:
The principal benzylisoquinolines a
Page 548 and 549:
conjugated morphine can be found in
Page 550 and 551:
503R 2N R 1R 3Compound R 1 R 2 R 3M
Page 552 and 553:
by effects on the circular and long
Page 554 and 555:
treatment of acute intoxication, ar
Page 556 and 557:
PentazocinePentazocine was synthesi
Page 558 and 559:
peripheral sites led to the develop
Page 560 and 561:
produces a demonstrable antitussive
Page 562 and 563:
A buccal fentanyl “film” is FDA
Page 564 and 565:
Table 18-6Guidelines for the Use of
Page 566 and 567:
Table 18-8Summary of Drug Target an
Page 568 and 569:
while they may be physically depend
Page 570 and 571:
in subcellular fractions of mouse b
Page 572 and 573:
Supernaw RB. CYP2D6 and the efficac
Page 574 and 575:
General Anesthetics andTherapeutic
Page 576 and 577:
nonsteroidal anti-inflammatory drug
Page 578 and 579:
The inhalational anesthetics inhibi
Page 580 and 581:
SSNNH 3 C H 3 C OH 3 C H 3 CHO HTHI
Page 583 and 584:
Context-Sensitive t 1 (min)21501005
Page 585 and 586:
Pharmacokinetics and Metabolism. Th
Page 587 and 588:
Pharmacokinetics and Metabolism. Th
Page 589 and 590:
F A /F I10.5NitrousOxideDesfluraneS
Page 591 and 592:
Minute volume (liters/min) Pa CO2 (
Page 593 and 594:
long-term nephrotoxicity following
Page 595 and 596:
the cobalt I (Co + ) form of vitami
Page 597 and 598:
intubated and mechanically ventilat
Page 599 and 600:
for gas transport may be increased,
Page 602 and 603:
substantial hypoventilation, with t
Page 604 and 605:
and left-to-right shunting of cardi
Page 606 and 607:
factors, however, are insufficient
Page 608 and 609:
failure associated with orthotopic
Page 610 and 611:
Bannenberg GL, Vieira HL. Therapeut
Page 612 and 613:
Mazze RI, Woodruff RE, Heerdt ME. I
Page 614 and 615:
Local AnestheticsWilliam A. Cattera
Page 616 and 617:
with K + channels requires higher c
Page 618 and 619:
569CHAPTER 20Figure 20-3. The local
Page 620 and 621:
the vasoconstriction, leads to hypo
Page 622 and 623:
Lidocaine is dealkylated in the liv
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BIOLOGICAL TOXINS: TETRODOTOXINAND
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• those with a long (400-450 minu
Page 628 and 629:
levels. In different clinical situa
Page 630 and 631:
dose of systemically administered m
Page 632 and 633:
Pharmacotherapyof the EpilepsiesJam
Page 634 and 635:
mendelian. The classification of ep
Page 636 and 637:
models—together with careful atte
Page 638 and 639:
seizures arise from the reciprocal
Page 640 and 641:
HYDANTOINSPhenytoinPhenytoin (diphe
Page 642 and 643:
drug allergy. Although rare, they n
Page 644 and 645:
concentrations in the range of ther
Page 646 and 647:
Chemistry. Valproic acid (n-dipropy
Page 648 and 649:
clonazepam at any dosage. The initi
Page 650 and 651:
Pharmacological Effects and Mechani
Page 652 and 653:
Therapeutic Use. A double-blind, pl
Page 654 and 655:
Unfortunately, such a study has not
Page 656 and 657:
Huguenard JR, McCormick DA. Thalami
Page 658 and 659:
Treatment of Central NervousSystem
Page 660 and 661:
(such as the mitochondrial cofactor
Page 662 and 663:
Glu+Glu +DASNpcTo spinal cordand br
Page 664 and 665:
drug in plasma usually peak between
Page 666 and 667:
These agents are better tolerated a
Page 668 and 669:
confusion. Other side effects are c
Page 670 and 671:
Aggregation of Aβ is an important
Page 672 and 673:
progresses, the involuntary movemen
Page 674 and 675:
alterations of single amino acids,
Page 676 and 677:
Beier MT. Treatment strategies for
Page 678 and 679:
Ethanol and MethanolMarc A. Schucki
Page 680 and 681:
CH 3 OHMethanolH 3 C CH 2 OHEthanol
Page 682 and 683:
More recent research has added deta
Page 684 and 685:
similar to mild alcohol withdrawal,
Page 686 and 687:
other factors such as age, nicotine
Page 688 and 689:
patients with chronic alcoholism. A
Page 690 and 691:
may be responsible for some of the
Page 692 and 693:
Table 23-3Oral Medications for Trea
Page 694 and 695:
Davies AG, Pierce-Shimomura JT, Kim
Page 696 and 697:
ethanol in PC12 cells. J Pharmacol
Page 698 and 699:
Drug AddictionCharles P. O’BrienT
Page 700 and 701:
mucosa, producing higher cocaine le
Page 702 and 703:
Conditioned tolerance (situation-sp
Page 704 and 705:
(Mendelson and Mello, 1979), thus n
Page 706 and 707:
Deliberate abusers of high doses of
Page 708 and 709:
systems. Although this research has
Page 710 and 711:
Pharmacological Interventions. Opio
Page 712 and 713:
on reinforcing cocaine-free urine t
Page 714 and 715:
use does not always result in frank
Page 716 and 717:
treatment are necessary. There prob
Page 718 and 719:
MODULATION OFCARDIOVASCULAR FUNCTIO
Page 720 and 721:
Regulation of Renal Functionand Vas
Page 722 and 723:
This latter equation succinctly exp
Page 724 and 725:
TubularlumenIntercellular spaceInte
Page 726 and 727:
the cell. The Na + -P isymporter is
Page 728 and 729:
Table 25-2Inhibitors of Carbonic An
Page 730 and 731:
Acetazolamide can provide symptomat
Page 732 and 733:
Table 25-4Inhibitors of Na + -K + -
Page 734 and 735:
nonosmotic vasopressin release, and
Page 736 and 737:
Fractional excretion of Na + (%)25.
Page 738 and 739:
LumenDISTAL CONVOLUTED TUBULEInters
Page 740 and 741:
60 mV(+) (-)(-)15 mVLATE DISTAL TUB
Page 742 and 743:
Table 25-7Mineralocorticoid Recepto
Page 744 and 745:
antagonists. Therefore, these drugs
Page 746 and 747:
InterstitialspaceCA inhibitorsTight
Page 748 and 749:
The most desirable course of action
Page 750 and 751:
All currently available diuretics p
Page 752 and 753:
Regulation of Vasopressin Secretion
Page 754 and 755:
are typical heptahelical GPCRs. Man
Page 756 and 757:
For maximum concentration of urine,
Page 758 and 759:
Table 25-8Vasopressin Receptor Agon
Page 760 and 761:
Chlorpropamide, an oral sulfonylure
Page 762 and 763:
is 10-40 μg daily either as a sing
Page 764 and 765:
Table 25-9Vasopressin Receptor Anta
Page 766 and 767:
adverse effects listed for tolvapta
Page 768 and 769:
Plotkin MD, Kaplan MR, Verlander JW
Page 770 and 771:
Renin and AngiotensinRanda Hilal-Da
Page 772 and 773:
AVasodilatorsNaClReabsorptionbyProx
Page 774 and 775:
an apparent molecular weight of 170
Page 776 and 777:
The Mas receptor mediates the effec
Page 778 and 779:
those of the lung and skeletal musc
Page 780 and 781:
BradykininACEInactivepeptidesDRIAng
Page 782 and 783:
three times daily or 25 mg twice da
Page 784 and 785:
cardiac index increase, as do indic
Page 786 and 787:
BIPHENYLMETHYL DERIVATIVESR 2THIENY
Page 788 and 789:
failure (McMurray et al., 2003; Coh
Page 790 and 791:
(Parving et al., 2008). The long- t
Page 792 and 793:
Nguyen G, Danser AH. Prorenin and (
Page 794 and 795:
Treatment of MyocardialIschemia and
Page 796 and 797:
(ACE) inhibitors (see Chapter 26) a
Page 798 and 799:
decrease in blood pressure. Pulmona
Page 800 and 801:
drug has a t 1/2of 1-3 minutes. The
Page 802 and 803:
a nitrate, fluids and α-adrenergic
Page 804 and 805:
hospitals where emergency PCI is no
Page 806 and 807:
binds to the cytoplasmic bridge bet
Page 808 and 809:
Absorption, Fate, and Excretion. Al
Page 810 and 811:
exertional angina (Gibbons et al.,
Page 812 and 813:
Combination Therapy and New Anti-An
Page 814 and 815:
effects of pentoxifylline on lower-
Page 816 and 817:
Table 27-5Classification of Antihyp
Page 818 and 819:
have an arylsulfonamide structure a
Page 820 and 821:
furosemide and bumetanide, in patie
Page 822 and 823:
agents. The pharmacology of these d
Page 824 and 825:
parotid gland swelling and pain. Po
Page 826 and 827:
pharmacology of these drugs is pres
Page 828 and 829:
ACE inhibitors in the treatment of
Page 830 and 831:
maximum recommended dose of hydrala
Page 832 and 833:
glomerular filtration are maintaine
Page 834 and 835:
to rapidly treat patients merely on
Page 836 and 837:
Horiuchi M, Akishita M, Dzau VJ. Re
Page 838 and 839:
Pharmacotherapy of CongestiveHeart
Page 840 and 841:
Inotropic agents, digoxinHeart fail
Page 842 and 843:
Table 28-1Causes of Diuretic Resist
Page 844 and 845:
Table 28-3Vasodilator Drugs Used to
Page 846 and 847:
containing these two compounds in c
Page 848 and 849:
weighed against the increased likel
Page 850 and 851:
signaling in the myocardium, reduci
Page 852 and 853:
enhance myocardial contractility. E
Page 854 and 855:
positive inotropy, although β 2rec
Page 856 and 857:
AldosteroneXanthineoxldaseCholester
Page 858 and 859:
Stage AHigh riskwith nosymptomsStag
Page 860 and 861:
Ellison DH. Diuretic resistance: Ph
Page 862 and 863:
predictors of adverse cardiovascula
Page 864 and 865:
Anti-Arrhythmic DrugsKevin J. Samps
Page 866 and 867:
InwardOutwardNa + currentCa 2+ L-ty
Page 868 and 869:
As a result, impulses spread along
Page 870 and 871:
Table 29-1Drug-Induced Cardiac Arrh
Page 872 and 873:
anatomicbarrierfunctionalbarrierFig
Page 874 and 875:
ANormal rhythm1 secFAtrial flutter
Page 876 and 877:
experimental arrhythmias by increas
Page 878 and 879:
Table 29-3Major Electrophysiologic
Page 880 and 881:
Verapamil and Diltiazem. The major
Page 882 and 883:
Table 29-4Patient-Specific Anti-Arr
Page 884:
Table 29-5Pharmacokinetic Character
Page 888 and 889:
such as dimethyl sulfoxide. Amiodar
Page 890 and 891:
are hypothyroid. Digitoxin undergoe
Page 892 and 893:
to inactive metabolites. The latter
Page 894 and 895:
N-acetyl procainamide rise to 30 g/
Page 896 and 897:
Quinidine metabolism is induced by
Page 898 and 899:
the treatment of patients with recu
Page 900 and 901:
Blood Coagulation andAnticoagulant,
Page 902 and 903:
851Endothelial cellsPAI-1PAI-2t-PAP
Page 904 and 905:
degradation, α 2-antiplasmin rapid
Page 906 and 907:
OH 2 COSO 3-4OH365O12ONHCOCH 3(or -
Page 908 and 909:
effect (see the warfarin “Clinica
Page 910 and 911:
or protamine zinc insulin), but unt
Page 912 and 913:
anticoagulant proteins C and S are
Page 914 and 915:
Table 30-2Frequencies of CYP2C9 Gen
Page 916 and 917:
until the heparin-induced thrombocy
Page 918 and 919:
which results from two factors: 1)
Page 920 and 921:
is a vasodilator that, in combinati
Page 922 and 923:
Table 30-4Features of GPIIb/IIIa An
Page 924 and 925:
are γ-carboxylated in the primary
Page 926 and 927:
Antithrombotic Trialists’ Collabo
Page 928 and 929:
Drug Therapy forHypercholesterolemi
Page 930:
Table 31-1Characteristics of Plasma
Page 934 and 935:
Another ACAT enzyme, ACAT-1, is exp
Page 936 and 937:
More than 900 mutations of the LDL
Page 938 and 939:
risk factors. This pivotal role of
Page 940 and 941:
Table 31-4Classification of Plasma
Page 942 and 943:
Table 31-6Assessing 10-Year Risk of
Page 944 and 945:
Can Cholesterol Levels Be Lowered T
Page 946 and 947:
catalyzes an early, rate-limiting s
Page 948 and 949:
Table 31-10Dose (mg) of Statins Req
Page 950 and 951:
and their active metabolites. Atorv
Page 952 and 953:
Mechanism of Action. The bile-acid
Page 954 and 955:
reversible side effects include tox
Page 956 and 957:
been reported to potentiate the act
Page 958 and 959:
American Heart Association; World H
Page 960 and 961:
and pravastatin across doses (STELL
Page 962 and 963:
Inflammation,Immunomodulation, andH
Page 964 and 965:
Histamine, Bradykinin, andTheir Ant
Page 966 and 967:
Table 32-1Characteristics of Histam
Page 968 and 969:
of acid, and moderate bronchospasm
Page 970 and 971:
receptor can elicit maximal vasodil
Page 972 and 973:
H 3 COCH 3CH 3H C O CH 2 CH 2 NH C
Page 974 and 975:
Table 32-2Preparations and Dosage o
Page 976 and 977:
Motion Sickness, Vertigo, and Sedat
Page 978 and 979:
Thioperamide was the first “speci
Page 980 and 981:
HMW-Kininogen927AngiotensinogenReni
Page 982 and 983:
and kallidin from the kininogens ar
Page 984 and 985:
inflammation appears to involve inc
Page 986 and 987:
ACE inhibitors are widely used drug
Page 988 and 989:
Slater EE, Merrill DD, Guess HA, et
Page 990 and 991:
Lipid-Derived Autacoids:Eicosanoids
Page 992 and 993:
dominates in the acute release of A
Page 994 and 995:
of epidermal LOXs in normal skin fu
Page 996 and 997:
COOH943OOHOOHO11-hydro-TxB 2dehydro
Page 998 and 999:
can couple to both elevation of int
Page 1000 and 1001:
at their sites of biosynthesis or t
Page 1002 and 1003:
Cardiac output generally is increas
Page 1004 and 1005:
aqueous humor outflow of the eye vi
Page 1006 and 1007:
Analogous to the eicosanoids, PAF i
Page 1008 and 1009:
Stomach. In addition to contracting
Page 1010 and 1011:
Shinmura K, Tamaki K, Sato T, et al
Page 1012 and 1013:
Anti-Inflammatory, Antipyretic,and
Page 1014 and 1015:
IL-1 comprises two distinct polypep
Page 1016 and 1017:
and analgesic but largely devoid of
Page 1018 and 1019:
(CELEBREX) currently is the only CO
Page 1021:
Sulindac Peak C p1-2 hours; 8 hours
Page 1025:
Naproxen Peak C p1 hour 250 mg 5 mg
Page 1029 and 1030:
and physical therapy, generally is
Page 1031 and 1032:
might induce expression of COX-2. H
Page 1033 and 1034:
PG-induced inhibition of both the r
Page 1035 and 1036:
is related to the GI and hepatic pa
Page 1037 and 1038:
ingestion of anti-inflammatory dose
Page 1039 and 1040:
monitoring of serum salicylate leve
Page 1041 and 1042:
It has been suggested that COX inhi
Page 1043 and 1044:
Adverse Effects and Drug Interactio
Page 1045 and 1046:
Absorption, Distribution, and Elimi
Page 1047 and 1048:
oxide or aluminum hydroxide. Naprox
Page 1049 and 1050:
dose-dependent relief from inflamma
Page 1051 and 1052:
the chosen agent should be prescrib
Page 1053 and 1054:
inflammatory mediators that lower t
Page 1055 and 1056:
Drug Interactions. Allopurinol incr
Page 1057 and 1058:
first presumes that the small secre
Page 1059 and 1060:
Arber N, Eagle CJ, Spicak J, et al.
Page 1061 and 1062:
current in rat sensory neurons: Who
Page 1063 and 1064:
Immunosuppressants, Tolerogens,and
Page 1065 and 1066:
of mAbs and the introduction of the
Page 1067 and 1068:
H 3 CH 3 CHH 3 C2H 3 C CH 3 HO CHCH
Page 1069 and 1070:
capsules and a 100-mg/mL oral solut
Page 1071 and 1072:
component in whole blood and contri
Page 1073 and 1074:
the treatment of polyomavirus nephr
Page 1075 and 1076:
Toxicity. The major side effect of
Page 1077 and 1078:
antagonists are in development and
Page 1079 and 1080:
In a large phase II clinical trial,
Page 1081 and 1082:
Interleukin-2. Human recombinant IL
Page 1083 and 1084:
A CASE STUDY: IMMUNOTHERAPYFOR MULT
Page 1085 and 1086:
Each of the agents mentioned in thi
Page 1087 and 1088:
Opelz G, Vanrenterghem Y, Kirste G,
Page 1089 and 1090:
PulmonaryPharmacologyPeter J. Barne
Page 1091 and 1092:
1033Cigarette smoke(and other irrit
Page 1093 and 1094:
Delivery DevicesSeveral ways of del
Page 1095 and 1096:
1037Cellmembraneβ 2 agonistMethylx
Page 1097 and 1098:
2Receptor Polymorphisms. Several si
Page 1099 and 1100:
INFLAMMATORY CELLSCell number( apop
Page 1101 and 1102:
Table 36-3Side Effects of Theophyll
Page 1103 and 1104:
NORMALAChVagusnerveVagusnerveResist
Page 1105 and 1106:
Chemistry. The adrenal cortex secre
Page 1107 and 1108:
INFLAMMATORY CELLSEosinophilSTRUCTU
Page 1109 and 1110:
Table 36-4Side Effects of Inhaled C
Page 1111 and 1112:
AllergenCold air1053ExercisePAFAspi
Page 1113 and 1114:
IL-4, IL-13FcεRIMast cellFcεRII/C
Page 1115 and 1116:
frequency in vitro. Because inflamm
Page 1117 and 1118:
Naloxone. Naloxone is a competitive
Page 1119 and 1120:
which the inhibition of PDE5 prolon
Page 1121 and 1122:
Hawkins G, McMahon AD, Twaddle S, e
Page 1123 and 1124:
Szczeklik A, Stevenson DD. Aspirin-
Page 1125 and 1126:
Hematopoietic Agents:Growth Factors
Page 1127 and 1128:
ERYTHROPOIETIN1069SCF / FLTotipoten
Page 1129 and 1130:
proliferation, and maturation are d
Page 1131 and 1132:
daily for the 10 days preceding sur
Page 1133 and 1134:
chemotherapy will increase granuloc
Page 1135 and 1136:
intake, malabsorption, blood loss,
Page 1137 and 1138:
Table 37-3Iron Requirements for Pre
Page 1139 and 1140:
NormalIron DepletionIron-DeficientE
Page 1141 and 1142:
Table 37-5Average Response to Oral
Page 1143 and 1144:
Before initiating iron dextran ther
Page 1145 and 1146:
common practice to describe megalob
Page 1147 and 1148:
linked to a central cobalt atom and
Page 1149 and 1150:
vitamins and minerals also can be g
Page 1151 and 1152:
PteroylMonoheptaglutamate10933 6OCO
Page 1153 and 1154:
Leucovorin should never be used for
Page 1155 and 1156:
Clark SF. Iron deficiency anemia: D
Page 1157 and 1158:
Sheridan WP, Begley CG, Juttner CA,
Page 1159 and 1160:
Hormones and HormoneAntagonistsChap
Page 1161 and 1162:
Introduction To Endocrinology:The H
Page 1163 and 1164:
SON, PVN(AVP, OXY)HypothalamusAVP,O
Page 1165 and 1166:
chromosome 17 (17q22), which also c
Page 1167 and 1168:
HypothalamusAnteriorpituitaryTarget
Page 1169 and 1170:
postnatal growth retardation is unr
Page 1171 and 1172:
mixed GH- and prolactin-secreting a
Page 1173 and 1174:
OHN1115NH 2CH 2OHOHDopamineNHNQuina
Page 1175 and 1176:
incidence of leukemia. Despite this
Page 1177:
Table 38-3Structures of Gonadotropi
Page 1180 and 1181:
results from peripheral production
Page 1182 and 1183:
Page 1184 and 1185:
acids. It is synthesized as a large
Page 1186 and 1187:
Gillam MP, Molitch ME, Lombardi G,
Page 1188 and 1189:
Thyroid and Anti-Thyroid DrugsGrego
Page 1190 and 1191:
6. recycling of the iodine within t
Page 1192 and 1193:
residues, only two to five of which
Page 1194 and 1195:
with a very high affinity (the equi
Page 1196 and 1197:
DopamineGlucocorticoidsRetinoidsHig
Page 1198 and 1199:
histone deacetylases and other prot
Page 1200 and 1201:
which T 3enhances the velocity of c
Page 1202 and 1203:
tablets and as a lyophilized powder
Page 1204 and 1205:
commonly begun with a loading dose
Page 1206 and 1207:
Table 39-4Anti-thyroid CompoundsPRO
Page 1208 and 1209:
Measurements of the course of organ
Page 1210 and 1211:
β Adrenergic receptor antagonists
Page 1212 and 1213:
Table 39-6Commonly Used Iodine-Cont
Page 1214 and 1215:
of 131 I therapy and only resumed 3
Page 1216 and 1217:
Chemotherapy in Thyroid CancerAdvan
Page 1218 and 1219:
thyroid-related hormones. J Clin En
Page 1220 and 1221:
Sera N, Ashizawa K, Ando T, et al.
Page 1222 and 1223:
Estrogens and ProgestinsEllis R. Le
Page 1224 and 1225:
H 3 CH 3 C O16α-OHaseH 3 CH 3 C OO
Page 1226 and 1227:
The gonadotropins (LH and FSH) regu
Page 1228 and 1229:
ERα (Hewitt and Korach, 2003) and
Page 1230 and 1231:
both coagulation and fibrinolytic p
Page 1232 and 1233:
Besides co-activators and co-repres
Page 1234 and 1235:
4-hydroxycatechols, are converted t
Page 1236 and 1237:
content of the bile. Transdermal es
Page 1238 and 1239:
of transcription factors in the two
Page 1240 and 1241:
Agents Similar to Progesterone (Pre
Page 1242 and 1243:
Group for the PEPI Trial, 1995); th
Page 1244 and 1245:
If administered for one or several
Page 1246 and 1247:
Progestin-Only Contraceptives. Seve
Page 1248 and 1249:
with the long-acting preparations,
Page 1250 and 1251:
BIBLIOGRAPHYAnderson GL, Limacher M
Page 1252 and 1253:
Meis PJ, Klebanoff M, Thom E, et al
Page 1254 and 1255:
AndrogensPeter J. SnyderTESTOSTERON
Page 1256 and 1257:
have been identified: type I, which
Page 1258 and 1259:
Other changes also may result from
Page 1260 and 1261:
Testosterone(HISTERONE, others)OH12
Page 1262 and 1263:
undesirable effects occur shortly a
Page 1264 and 1265:
does not transiently increase sex s
Page 1266 and 1267:
King DS, Sharp RL, Vukovich MD, et
Page 1268 and 1269:
ACTH, Adrenal Steroids, andPharmaco
Page 1270 and 1271:
ZonaGlomerulosaAng IIK +ACTHZonaeFa
Page 1272 and 1273:
increases in the steroidogenic capa
Page 1274 and 1275:
Cushing’s disease) and an ectopic
Page 1276 and 1277:
HSP70SGRSGRHSP90SGRGRE GRECBGSIPTra
Page 1278 and 1279:
CH 2 OH21CH 2 OHCH 2 OHCH 2 OH1219C
Page 1280 and 1281:
to other vasoactive substances. Hyp
Page 1282 and 1283:
synthetic congeners are administere
Page 1284 and 1285:
Table 42-4Available Preparations of
Page 1286 and 1287:
Cataracts. Cataracts are a well-est
Page 1288 and 1289:
Traditional replacement regimens ha
Page 1290 and 1291:
Studies with other forms of renal d
Page 1292 and 1293:
Coombs test) are treated with predn
Page 1294 and 1295:
Axelrod L. Perioperative management
Page 1296 and 1297:
Endocrine Pancreas andPharmacothera
Page 1298 and 1299:
proportion to the nutrient load ing
Page 1300 and 1301:
The pancreatic α cell, which has c
Page 1302 and 1303:
• Impaired glucose tolerance (IGT
Page 1304 and 1305:
predominance of CD8+ cells (insulit
Page 1306 and 1307:
glucose production and promote hepa
Page 1308 and 1309:
Table 43-4Goals of Therapy in Diabe
Page 1310 and 1311:
1 SAspLysSA chainGly21AsnSSArg Arg1
Page 1312 and 1313:
abdomen currently is the preferred
Page 1314 and 1315:
INSULIN SECRETAGOGUES AND ORALHYPOG
Page 1316 and 1317:
may be more frequent in patients ta
Page 1318 and 1319:
Page 1320 and 1321:
patients in clinical trials and has
Page 1322 and 1323:
exendin-4 causes glucose-dependent
Page 1324 and 1325:
Therapeutic Uses. α-Glucosidase in
Page 1326 and 1327:
Type 2 Diabetes1267AssessA1CDiabete
Page 1329:
ParenteralInsulin a Glucose utiliza
Page 1332 and 1333:
Glucose, mmol/L131211109876543Gluco
Page 1334 and 1335:
Murphy R, Ellard S, Hattersley AT.
Page 1336 and 1337:
Agents Affecting Mineral IonHomeost
Page 1338 and 1339:
PhosphatePhosphate is an essential
Page 1340 and 1341:
inhibits renin secretion). Simultan
Page 1342 and 1343:
22128123 25119HO3 7provitamin D 3(7
Page 1344 and 1345:
mucosal compartments. Thus, net cal
Page 1346 and 1347:
Fibroblast Growth Factor 23 and Klo
Page 1348 and 1349:
Stromal cell/osteoblastRANKLRANKOPG
Page 1350 and 1351:
The amount of vitamin D necessary t
Page 1352 and 1353:
(15-25 μg/kg of body weight) to mi
Page 1354 and 1355:
Therapeutic Indications for Vitamin
Page 1356 and 1357:
Pyrophosphate Bisphosphonate Medron
Page 1358 and 1359:
Absorption, Fate, and Excretion. Ph
Page 1360 and 1361:
% change lumbar spine BMD1614121086
Page 1362 and 1363:
alendronate to PTH treatment provid
Page 1364 and 1365:
Ballock RT, O’Keefe RJ. The biolo
Page 1366 and 1367:
Okazaki M, Ferrandon S, Vilardaga J
Page 1368 and 1369:
Drugs AffectingGastrointestinal Fun
Page 1370 and 1371:
Pharmacotherapy of Gastric Acidity,
Page 1372 and 1373:
PROTON PUMP INHIBITORSChemistry; Me
Page 1374 and 1375:
mainstay in the treatment of pathol
Page 1376 and 1377:
Pharmacokinetics. Misoprostol is ra
Page 1378 and 1379:
In the hope of providing more rapid
Page 1380 and 1381:
GERD and Pregnancy. Heartburn is es
Page 1382 and 1383:
of acid-suppressant agents, usually
Page 1384 and 1385:
Treatment of Disorders of BowelMoti
Page 1386 and 1387:
achalasia of the esophagus (impaire
Page 1388 and 1389:
1327OHHNNH 2OCH 3NNHNCH 3HCLCH 3OHN
Page 1390 and 1391:
Rate(liters/day)Flow9.0H 2OUptake6.
Page 1392 and 1393:
Table 46-3Classification and Compar
Page 1394 and 1395:
effluent is clear. To avoid net tra
Page 1396 and 1397:
visceral pain (Eutamene et al., 200
Page 1398 and 1399:
In patients suspected of having bil
Page 1400 and 1401:
et al., 2001). For patients with va
Page 1402 and 1403:
NK 2receptors; it is not available
Page 1404 and 1405:
Table 46-6Receptor Specificity of A
Page 1406 and 1407:
Table 46-813455-HT 3Antagonists in
Page 1408 and 1409:
R3Bile AcidCholic acidR12CH 3CH 3R3
Page 1410 and 1411:
Sartor RB. Probiotic therapy of int
Page 1412 and 1413:
Pharmacotherapy of InflammatoryBowe
Page 1415 and 1416:
Intestinal lumenBacteriaAntibiotics
Page 1417 and 1418:
sulfapyridine(metabolite)sulfasalaz
Page 1419 and 1420:
(Greenberg et al., 1994; McKeage an
Page 1421 and 1422:
improve significantly (generally wi
Page 1423 and 1424:
Mesalamine and glucocorticoids are
Page 1425 and 1426:
Chemotherapy of MicrobialDiseasesCh
Page 1427 and 1428:
General Principles ofAntimicrobial
Page 1429 and 1430:
of even polar drugs (Quagliarello a
Page 1431 and 1432:
and liver dysfunction, which may le
Page 1433 and 1434:
viability assay (Hanna and D’Aqui
Page 1435 and 1436:
enzyme (Harshey and Ramakrishnan, 1
Page 1437 and 1438:
suggest this approach may be as eff
Page 1439 and 1440:
Resistance Due to Enhanced Excision
Page 1441 and 1442:
Arion D, Kaushik N, McCormick S, et
Page 1443 and 1444:
Wilson W, Taubert KA, Gewitz M, et
Page 1445 and 1446:
Chemotherapy of MalariaJoseph M. Vi
Page 1447 and 1448:
microenvironment. For the patient,
Page 1449 and 1450:
1387Table 49-2Regimens for the Prev
Page 1451:
Table 49-3Regimens for the Treatmen
Page 1455:
Doxycycline P falciparum from Oral:
Page 1459:
Quinine sulfate P. falciparum from
Page 1463 and 1464:
Table 49-4Regimen for Presumptive S
Page 1465 and 1466:
H 2 CCHHON1397H 3 COOHHCNNHF 3 CClC
Page 1467 and 1468:
failures are rare. However, when at
Page 1469 and 1470:
purine and pyrimidine synthesis. In
Page 1471 and 1472:
MauritaniaSenegalPortugalMoroccoWes
Page 1473 and 1474:
therapeutic doses, and thick smears
Page 1475 and 1476:
based on patient age, severity of i
Page 1477 and 1478:
for 3 months after mefloquine use b
Page 1479 and 1480:
and teeth, tetracyclines should not
Page 1481 and 1482:
Clinical suspicion of malariaor his
Page 1483 and 1484:
and antimalarial drugs in discovery
Page 1485 and 1486:
Krishna S, White, NJ. Pharmacokinet
Page 1487 and 1488:
Chemotherapy of ProtozoalInfections
Page 1489 and 1490:
recovered from all mammalian specie
Page 1491 and 1492:
this infection (Bern et al., 2007;
Page 1493 and 1494:
2007, Chappuis et al., 2005; Priott
Page 1495 and 1496:
individuals with amebic colitis or
Page 1497 and 1498:
microaerophilic bacteria such as He
Page 1499 and 1500:
approved in India as the first oral
Page 1501 and 1502:
and oocytes of C. parvum and inhibi
Page 1503 and 1504:
lungs depends on both the size of p
Page 1505 and 1506:
treatment of African trypanosomiasi
Page 1507 and 1508:
Donnelly H, Bernard EM, Rothkotter
Page 1509 and 1510:
Vöhringer HF, Arastéh K. Pharmaco
Page 1511 and 1512:
Chemotherapy of HelminthInfectionsJ
Page 1513 and 1514:
or with hookworms. In rare instance
Page 1515 and 1516:
streams and rivers, O. volvulus inf
Page 1517 and 1518:
been reported and higher doses of t
Page 1519 and 1520:
inhibition of first-pass CYP-mediat
Page 1521 and 1522:
general population; comparable stud
Page 1523 and 1524:
Chemistry. Ivermectin exists as an
Page 1525 and 1526:
Anthelmintic Action. After rapid an
Page 1527 and 1528:
Therapeutic Uses. Pyrantel pamoate
Page 1529 and 1530:
with onchocercal ocular involvement
Page 1531 and 1532:
Sulfonamides, Trimethoprim-Sulfamet
Page 1533 and 1534:
such a combination would yield syne
Page 1535 and 1536:
treatment of an established deep in
Page 1537 and 1538:
The synergistic interaction between
Page 1539 and 1540:
Table 52-2Structural Formulas of Se
Page 1541 and 1542:
concentrations in cerebrospinal flu
Page 1543 and 1544:
Antimicrobial Activity. Enzymes cap
Page 1545 and 1546:
Penicillins, Cephalosporins, andOth
Page 1547 and 1548:
GlycopeptidepolymerNAMpenicillinsce
Page 1549 and 1550:
1500 1000 1500 2000 2300Base pairsS
Page 1551 and 1552:
microorganisms, including Clostridi
Page 1553 and 1554:
Gonococcal Infections. Gonococci gr
Page 1555 and 1556:
This is their valid clinical use. D
Page 1557 and 1558:
Table 53-1Chemical Structures and M
Page 1559 and 1560:
Untoward Reactions to PenicillinsHy
Page 1561 and 1562:
toxic concentrations of procaine. I
Page 1563 and 1564:
Table 53-2Names, Structural Formula
Page 1565 and 1566:
the bile (neither is available in t
Page 1567 and 1568:
manifest cross-reactivity to a memb
Page 1569 and 1570:
Aztreonam generally is well tolerat
Page 1571 and 1572:
Spratt BG. Resistance to antibiotic
Page 1573 and 1574:
AminoglycosidesConan MacDougalland
Page 1575 and 1576:
1507CHAPTER 54NEOMYCIN BAMINOGLYCOS
Page 1577 and 1578:
consequently, gentamicin-resistant
Page 1579 and 1580:
Table 54-2Algorithm for Dose Reduct
Page 1581 and 1582:
ionic balance of the endolymph (Neu
Page 1583 and 1584:
• To provide synergistic bacteria
Page 1585 and 1586:
the infusion, which falls to ~20 μ
Page 1587 and 1588:
Appel GB. Aminoglycoside nephrotoxi
Page 1589 and 1590:
Protein Synthesis Inhibitorsand Mis
Page 1591 and 1592:
Bacteroides spp., Propionibacterium
Page 1593 and 1594:
Intra-abdominal Infections. Increas
Page 1595 and 1596:
most anaerobic bacteria, including
Page 1597 and 1598:
Drug Interactions. Chloramphenicol
Page 1599 and 1600:
with the fully methylated ribosomal
Page 1601 and 1602:
of acute exacerbations of chronic b
Page 1603 and 1604:
These strains would not display a b
Page 1605 and 1606:
which are more likely to be a probl
Page 1607 and 1608:
membranes. The permeability of the
Page 1609 and 1610:
of enterococci, primarily Enterococ
Page 1611 and 1612:
Antimicrobial Activity. Daptomycin
Page 1613 and 1614:
antibiotic in developing nations be
Page 1615 and 1616:
Oliva ME, Rekha A, Yellin A, et al.
Page 1617 and 1618:
Chemotherapy of Tuberculosis,Mycoba
Page 1619 and 1620:
mRNA30SMycobacteriumRNA PolymeraseD
Page 1621 and 1622:
Table 56-2Population Pharmacokineti
Page 1623 and 1624:
pyrazinamide was administered for d
Page 1625 and 1626:
AFastSlow15573BNumber of subjectsCp
Page 1627 and 1628:
Lewis, 1999). The following species
Page 1629 and 1630:
TMC-207 (R207910)TMC-207 is a diary
Page 1631 and 1632:
Mechanisms of Resistance. Mutations
Page 1633 and 1634:
employees of high-risk congregate s
Page 1635 and 1636:
disease, which has early hypopigmen
Page 1637 and 1638:
Diacon AH, Pym A, Grobusch M, et al
Page 1639 and 1640:
Antifungal AgentsJohn E. BennettThe
Page 1641 and 1642:
Table 57-1Pharmacotherapy of Mycose
Page 1643 and 1644:
due to decreased production of eryt
Page 1645 and 1646:
Table 57-3Interaction of Azole Anti
Page 1647 and 1648:
bound to plasma proteins. Neither a
Page 1649 and 1650:
the maintenance dose. There are no
Page 1651 and 1652:
Extracellular spaceMannoproteinGluc
Page 1653 and 1654:
Absorption, Distribution and Excret
Page 1655 and 1656:
mild penile irritation. Cross-aller
Page 1657 and 1658:
ButenafineButenafine hydrochloride
Page 1659 and 1660:
terreus infection. Antimicrob Agent
Page 1661 and 1662:
Antiviral Agents (Nonretroviral)Edw
Page 1663 and 1664:
Aattachmentrelease1595buddingBuncoa
Page 1665 and 1666:
ONHNH N N2 NOH CH 2OCH 2 CH 2ACYCLO
Page 1667 and 1668:
The principal dose-limiting toxicit
Page 1669 and 1670:
CNS or eye has not been well charac
Page 1671 and 1672:
of foscarnet and ganciclovir synerg
Page 1673 and 1674:
Ganciclovir therapy (5 mg/kg every
Page 1675 and 1676:
NH H NH 2 3 C21607OAMANTADINEOHNCOO
Page 1677 and 1678:
Table 58-3Pharmacological Character
Page 1679 and 1680:
A B1uncoatingnucleus1golgi3glycopro
Page 1681 and 1682:
IFN can cause myelosuppression and
Page 1683 and 1684:
tubing with ribavirin. Techniques t
Page 1685 and 1686:
Entecavir triphosphate is a weak in
Page 1687 and 1688:
Therapeutic Uses. Tenofovir is appr
Page 1689 and 1690:
Lai CL, Lim SG, Brown NA, et al. A
Page 1691 and 1692:
Antiretroviral Agents andTreatment
Page 1693 and 1694:
to occur at approximately three bas
Page 1695 and 1696:
A reservoir of long-lived quiescent
Page 1697 and 1698:
1. Triphosphate competeswith native
Page 1700 and 1701:
Like all available antiretroviral d
Page 1702 and 1703:
and cross-resistance. TAMs associat
Page 1704 and 1705:
less potent and substantially more
Page 1706 and 1707:
lamivudine, abacavir, and efavirenz
Page 1708 and 1709:
Mechanisms of Action and Resistance
Page 1710 and 1711:
DaughterDNA strand1641ParentRNA str
Page 1712 and 1713:
Therapeutic Use. Nevirapine (VIRAMU
Page 1714 and 1715:
efavirenz and nevirapine, and any p
Page 1716:
Table 59-4Pharmacokinetic Propertie
Page 1719 and 1720:
1649NONCONH 2OHNNO CH 2 CONH C(CH 3
Page 1721 and 1722:
occurs less frequently at codon 84.
Page 1723 and 1724:
6% of patients discontinued atazana
Page 1725 and 1726:
high-fat meals (Bardsley-Elliot and
Page 1727 and 1728:
HIV virusmembrane16571Nucleocapsidc
Page 1729 and 1730:
vitro. The Y143C/H/R mutation has a
Page 1731 and 1732:
Fischl MA, Stanley K, Collier AC, e
Page 1733 and 1734:
Perelson AS, Neumann AU, Markowitz
Page 1735 and 1736:
Chemotherapy ofNeoplastic DiseasesC
Page 1737 and 1738:
General Principles of CancerChemoth
Page 1739 and 1740:
Table 60-3Natural ProductsNONPROPRI
Page 1741 and 1742:
6-MERCAPTOPURINE6-THIOGUANINEInhibi
Page 1743 and 1744:
integrity. If a cell possesses norm
Page 1745 and 1746:
Pullarkat ST, Stoehlmacher J, Ghade
Page 1747 and 1748:
Cytotoxic AgentsBruce A. Chabner, J
Page 1749 and 1750:
CyclophosphamideO1-triazeno)-imidaz
Page 1751 and 1752:
Other repair enzymes are specific f
Page 1753 and 1754:
CLINICAL PHARMACOLOGYNitrogen Musta
Page 1755 and 1756:
Ethyleneimines and MethylmelaminesA
Page 1757 and 1758:
disease. Almost 50% of the compound
Page 1759 and 1760:
CisplatinAbsorption, Fate, and Excr
Page 1761 and 1762:
new agents have greater capacity fo
Page 1763 and 1764:
elements formed by amplification of
Page 1765 and 1766:
Modification of BaseCYTOSINE(Capeci
Page 1767 and 1768:
dUMPFdUMPthymidylatesynthaseN5-10me
Page 1769 and 1770:
incorporation into DNA by DNA polym
Page 1771 and 1772:
difluorodeoxyuridine (dFdU). Althou
Page 1773 and 1774:
After rapid extracellular dephospho
Page 1775 and 1776:
Deoxyadenosine also inactivates S-a
Page 1777 and 1778:
sometimes resulting in colicky abdo
Page 1779 and 1780:
Docetaxel causes greater degrees of
Page 1781 and 1782:
The precise sequence of events that
Page 1783 and 1784:
most potent antitumor agents known.
Page 1785 and 1786:
echocardiography, which reveals abn
Page 1787 and 1788:
H 2 N ONH 2NHNH 2 ON N OCH 3 H ON R
Page 1789 and 1790:
and mitomycin must be discontinued
Page 1791 and 1792:
L-ASP terminates the antitumor acti
Page 1793 and 1794:
discontinuation. Corticosteroids an
Page 1795 and 1796:
Asselin BL, Whitin JC, Coppola DJ,
Page 1797 and 1798:
Heizer WD, Peterson JL. Acute myelo
Page 1799 and 1800:
DNA following subchronic doxorubici
Page 1801 and 1802:
Targeted Therapies: Tyrosine Kinase
Page 1803 and 1804:
181614<2%2-10%>10%1733% of patients
Page 1805 and 1806:
IGF-1kinase activity and ability to
Page 1807 and 1808:
Metastatic Colon Cancer. Cetuximab
Page 1809 and 1810:
aflibercept (VEGF Trap), a recombin
Page 1811 and 1812:
classification as anti-angiogenics
Page 1813 and 1814:
NNONHMechanism of Action. Bortezomi
Page 1815 and 1816:
reduced to 5 mg daily for patients
Page 1817 and 1818:
Table 62-2Dose and Toxicity of Mono
Page 1819 and 1820:
complicate the patient’s course f
Page 1821 and 1822:
Corbin AS, La Rosée P, Stoffregen
Page 1823 and 1824:
Serafini P, De Santo C, Marigo I, e
Page 1825 and 1826:
Natural Products in CancerChemother
Page 1827 and 1828:
Table 63-1Clinical Uses for Anti-Es
Page 1829 and 1830:
factor V Leiden mutation and tamoxi
Page 1831 and 1832:
Aromatase activity is the product o
Page 1833 and 1834:
Mechanism of Action. In contrast to
Page 1835:
Table 63-2Structures of GnRH and De
Page 1838 and 1839:
ketoconazole inhibits both testicul
Page 1840 and 1841:
Sharifi N, Gulley JL, Dahut WL. And
Page 1842 and 1843:
Special Systems PharmacologyChapter
Page 1844 and 1845:
Ocular PharmacologyJeffrey D. Hende
Page 1846 and 1847:
Table 64-1Autonomic Pharmacology of
Page 1848 and 1849:
Table 64-2Effects of Pharmacologica
Page 1850 and 1851:
for compounds with limited solubili
Page 1852 and 1853:
Table 64-4Topical Antibacterial Age
Page 1854 and 1855:
Table 64-5Antiviral Agents for Opht
Page 1856 and 1857:
Use of Autonomic Agents in the EyeG
Page 1858 and 1859:
• in patients who have an increas
Page 1860 and 1861:
their chemistry and pharmacology ar
Page 1862 and 1863:
Table 64-8Vitreous Substitutes aVIT
Page 1864 and 1865:
necessary. Rifabutin, if used in co
Page 1866 and 1867:
Table 64-9Ophthalmic Effects of Sel
Page 1868 and 1869:
DarkLight1797[Ca 2+ ]DK [cGMP]LT [C
Page 1870 and 1871:
the need for surgical intervention
Page 1872 and 1873:
Morrow GL, Abbott RL. Minocycline-i
Page 1874 and 1875:
Dermatological PharmacologyCraig Bu
Page 1876 and 1877:
LamellarbodyTightjunctionScale desq
Page 1878 and 1879:
Table 65-2Vehicles for Topically Ap
Page 1880 and 1881:
to reserve this method for allergic
Page 1882 and 1883:
as monotherapy or in combination wi
Page 1884 and 1885:
Calcipotriene. Calcipotriene (DOVON
Page 1886 and 1887:
ECP is used for cutaneous T-cell ly
Page 1888 and 1889:
are irritants and may lead to micro
Page 1890 and 1891:
HEXACHLOROCYCLOHEXANELindane has be
Page 1892 and 1893:
gangrenosum, and Behçet’s diseas
Page 1894 and 1895:
active derivative, inhibits the enz
Page 1896 and 1897:
Table 65-10Biological Agents Common
Page 1898 and 1899:
sepsis, tuberculosis), including le
Page 1900 and 1901:
DRUGS FOR HYPERKERATOTICDISORDERSKe
Page 1902 and 1903:
Barry BW. Breaching the skin’s ba
Page 1904 and 1905:
Contraception andPharmacotherapy of
Page 1906 and 1907:
Table 66-2Brand Names and Formulati
Page 1908 and 1909:
Postcoital ContraceptionPostcoital
Page 1910 and 1911:
Available routes of estrogen admini
Page 1912 and 1913:
contraceptives containing progestin
Page 1914 and 1915:
withdrawal in women who do not. If
Page 1916 and 1917:
cavity, thorax, and even the perica
Page 1918 and 1919:
Nursing mothers constitute a second
Page 1920 and 1921:
β 2 agonistsNO donors1849β 2G s A
Page 1922 and 1923:
rate then is reduced to 1-2 mL/minu
Page 1924 and 1925:
Environmental Toxicology:Carcinogen
Page 1926 and 1927:
human exposure. The most common mod
Page 1928 and 1929:
InitiationPromotion1857MetabolicAct
Page 1930 and 1931:
termination of the trial (William e
Page 1932 and 1933:
Many of the toxic metals in the env
Page 1934 and 1935:
impulsivity, short attention span,
Page 1936 and 1937:
Exposure. Inorganic mercury cations
Page 1938 and 1939:
Toxicity to the nervous system is t
Page 1940 and 1941:
voluntarily replaced arsenic with o
Page 1942 and 1943:
but has very little or no benefit i
Page 1944 and 1945:
NaOONH 2(CH 2 ) 5NONR 2OCaexposure
Page 1946 and 1947:
the FDA but is approved for use in
Page 1948 and 1949:
Goldwater LJ. Mercury; a History of
Page 1950 and 1951:
Principles of Prescription OrderWri
Page 1952 and 1953:
to be equivalent to 5 mL and a “t
Page 1954 and 1955:
shorter due to limits and pressures
Page 1956 and 1957:
may be telephoned to a pharmacy onl
Page 1958 and 1959:
Even the most carefully prepared pr
Page 1960 and 1961:
ELECTRONIC PRESCRIBINGThe era of e-
Page 1962 and 1963:
Design and Optimizationof Dosage Re
Page 1964 and 1965:
percentage of the administered dose
Page 1966 and 1967:
The time required to achieve a maxi
Page 1968 and 1969:
estimated from the concentration of
Page 1970:
Table AII-1Pharmacokinetic DataKey:
Page 1974:
Alendronate a<0.7 b 44.9 ± 9.3 78
Page 1978:
Ambrisentan a— b — 99 — c —
Page 1982:
Aripiprazole a87 <1 >99 0.83 ± 0.1
Page 1986:
Bicalutamide a— 1.7 ± 0.3 96 R:
Page 1990:
Capecitabine a— 3 <60 145 (34%) L
Page 1994:
CefdinirCap: 16-21 a 13-23 b 89 c 1
Page 1998:
Cetirizine aRac: >70 b Rac: 70.9 ±
Page 2002:
Cinacalcet a~20 — b 93-97 ~18 ~17
Page 2006:
Clopidogrel a— b — Clo: 98 —
Page 2010:
CyclosporineSI: 28 ± 18 a,b <1 93
Page 2014:
Diazepam aPO: 100 ± 14 <1 98.7 ±
Page 2018:
Donepezil a— b 10.6 ± 2.7 92.6
Page 2022:
Duloxetine a42.8 (18.5-71.2) — >9
Page 2026:
Entacapone a42 ± 9 b Negligible 98
Page 2030:
Esomeprazole aEs: 89 (81-98) b Es/R
Page 2034:
Felodipine a15 ± 8 <1 99.6 ± 02 1
Page 2038:
5-Fluorouracil (5-FU)28 (0-80) a <1
Page 2042:
Furosemide a71 ± 35 71 ± 10 98.6
Page 2046:
Glipizide95 <5 98.4 0.52 ± 0.18 a
Page 2050:
Hydroxychloroquine a79 ± 12 27 45
Page 2054:
Imipenem/Cilastatin aImipenem 69 ±
Page 2058:
Isoniazid a— b RA: 7 ± 2 c ~0 RA
Page 2062:
Ivermectin a— <1 93.1 ± 0.2 2.06
Page 2066:
Levofloxacin a99 ± 10 61-87 24-38
Page 2070:
Lorazepam93 ± 10 <1 91 ± 2 1.1 ±
Page 2074:
Mercaptopurine a12 ± 7 b 22 ± 12
Page 2078:
Methylprednisolone82 ± 13 a 4.9 ±
Page 2082:
Minocycline a95-100 11 ± 2 76 1.0
Page 2086:
Moxifloxacin a86 ± 1 21.9 ± 3.6 3
Page 2090:
Nitrofurantoin87 ± 13 47 ± 13 62
Page 2094:
Oxcarbazepine a— O: <1 — O: 67.
Page 2098:
ParoxetineDose dependent a <2 95 8.
Page 2102:
Pramlintide a30-40% b - ~60 c Low:
Page 2106:
Pregabalin a≥90 b 90-99 0 0.96-1.
Page 2110:
Pseudoephedrine a~100 43-96 b — 7
Page 2114:
Rabebrazole a52 b 0 b 95-98 4.2 ±
Page 2118:
Remifentanil a— b Negligible 92 4
Page 2122:
Rivastigmine a72 (22-119) b Negligi
Page 2126:
Simvastatin a≤5 Negligible 94 7.6
Page 2130:
Spironolactone a— b <1 c >90 d 93
Page 2134:
Tamoxifen a— <1 >98 1.4 b,c 50-60
Page 2138:
Tolterodine aEM: 26 ± 18 EM: Negli
Page 2142:
Trimethoprim>63 63 ± 10 37 ± 5 1.
Page 2146:
Vancomycin— a 79 ± 11 30 ± 11 C
Page 2150:
Vincristine a— 10-20 Low 4.92 ±
Page 2154 and 2155:
IndexInformation in figures and tab
Page 2156 and 2157:
Adrenergic receptors (Cont.):beta,
Page 2158 and 2159:
AMAPRYL (glimepiride), 1257tAmatoxi
Page 2160 and 2161:
Angina pectoris (Cont.):variant (Pr
Page 2162 and 2163:
Anticholinesterase agents (Cont.):s
Page 2164 and 2165:
Aromatase inhibitors (Cont.):first
Page 2166 and 2167:
Azelastine hydrochloride, 922, 922t
Page 2168 and 2169:
Bile acids, 1346-1347Bile acid sequ
Page 2170 and 2171:
Butorphanolactions and selectivitie
Page 2172 and 2173:
Cardiovascular system (Cont.):opioi
Page 2174 and 2175:
Cetuximab (Cont.):therapeutic uses
Page 2176 and 2177:
CLOMID (clomiphene citrate),1841-18
Page 2178 and 2179:
CPVT. See Catecholaminergicpolymorp
Page 2180 and 2181:
DERMABOND (cyanoacrylate tissueadhe
Page 2182 and 2183:
Diiodohydroxyquin (iodoquinol),1153
Page 2184 and 2185:
Dose-response, 73-74, 74fDose-respo
Page 2186 and 2187:
Electrocardiographic toxicitymanife
Page 2188 and 2189:
Essential thrombocytosis, drugs for
Page 2190 and 2191:
Felodipine (Cont.):cardiovascular p
Page 2192 and 2193:
Fosinopril (Cont.):therapeutic uses
Page 2194 and 2195:
GlutathioneABC transporters and, 10
Page 2196 and 2197:
Hepatitisdrugs for, 1609-1617interf
Page 2198 and 2199:
Hydralazine (Cont.):site of action
Page 2200 and 2201:
Immunosuppression, 1006-1019biologi
Page 2202 and 2203:
Iridocyclitis, 233viral, 1783tIrino
Page 2204 and 2205:
β-Lactamase inhibitors, 1501Lactat
Page 2206 and 2207:
Loop diuretics, 682-686, 683tabsorp
Page 2208 and 2209:
Mefenamic acid, 989adverse effects
Page 2210 and 2211:
Metoprolol, 777absortion, fate, and
Page 2212 and 2213:
Multifocal atrial tachycardia, drug
Page 2214 and 2215:
α-Neoendorphin, actions andselecti
Page 2216 and 2217:
Nitrogen mustards, 1668t-1670t,1682
Page 2218 and 2219:
Olanzapinedosage of, 425tmetabolism
Page 2220 and 2221:
Oxygenases, 125tOxygenation, normal
Page 2222 and 2223:
Persistent hyperinsulinemichypoglyc
Page 2224 and 2225:
Pityrosporum ovale, 1830Pivoxicam,
Page 2226 and 2227:
Prescription writing (Cont.):date i
Page 2228 and 2229:
Proton pump inhibitors (Cont.):in c
Page 2230 and 2231:
Receptors (Cont.):affinity and, 44-
Page 2232 and 2233:
Riskadverse effects and publicaccep
Page 2234 and 2235:
Serotonin-norepinephrine reuptakein
Page 2236 and 2237:
SPORANOX (itraconazole), 1818SPRYCE
Page 2238 and 2239:
Sympathomimetic amines (Cont.):for
Page 2240 and 2241:
Thioridazinearrhythmias caused by,
Page 2242 and 2243:
Transporters (Cont.):resistance and
Page 2244 and 2245:
Valacyclovir (Cont.):mechanism of a
Page 2246 and 2247:
Vitamin B 12(Cont.):folic acid and,
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DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010