O,n, Pharmarok,nel. 19 (2 ): 94-12S. 1990 03 1z.s963/90f000S.009~/S 16.00/0
C Adll InlnTUltlOnal Llmll«l All n&hll ran-vnI. ~. ,
Clinical Pharmacokinetics of Drugs Used in the Treatment of Gastrointestinal Diseases (Part II) Karsten Lauritsen, Laurils S. Laursen and Jorgen Rask-Madsen Department of Medical (fastroenterology, Oden~ IJnivenity Hospital, Oden ~, and Departmcnt of Gaslroe nl crology G, Bispcbjef) Hospital, University of Copenhagen. Copenhagen, Ornmark
Contents
g. Anti-Inflammatory Salicylates ........................... .. ............... _.......... ,................. 94 g.1 Sulfasalazinc ........ ,............................................... .. .............. _................ ...9S g.2 Clsalazlnc ............................................................................................ _............................ 97 g.) Othcr Azobond Prodrugs of S-Am inosaliC)hc ACId ....................... _............................. 9g g.4 Mesaluine ....... ,........... ................. .. ............................................ 98 9. NonSpe1:1fic Anlidlarrhoeal Agents ................................................................................... 100 9. 1 Diphenoxylale ....................................................................... ,................. ,..................... 100 9.2 Loperamide ........................................................................... .. ............................. 101 10. Lauti ves and CathanlC$ .................................................................... ..... 101 ............. ,....... ,.................. .. ..10) Appendix ............... .................... ......
Part I of this anicle, which appeared in the previous issue of tile Journal. cove red th e following agen ts: histamine H2-rcceptor antagon ists (cimetidine. ranitidine. famotidine. nizatidine); muscarinic- M I-receptor antagonists (pirt nzepine): protOn pump inhibitors (omeprazole); site-protecllve agents (colloidal bismuth $ubcit11l te, sum lfale): antacids and prostaglandin analotues: antiemetics and prokinetic;s (metoclopramide, domperidone, cisapride): a nd an tispasmodics. In Pan II . we consider the an ti-i nflammatory salicyla tes, nonspe'n«k ML Achem SR. Cimelldllle'-Hl~ylhne intaKlIon: cffeas o f . Ind Clmelodllle~. ThfflipeullC Dru, Monllon". 1: 426-434. 1985 Conrad KA . Mlycnohn M. 81lss M. C"imelodine docs nOI aller lbuproflon k,netlCli.f\cr. sonale dose. Bnll~ Journal orO'nlal PllarnHlcolosy 18; 62-4-626. 1984 COrTocher R. 8amNI1I LM. Call1ml)Chl P. Tnu R. G,relll M. CI al. EfTeet of I1In llldlne on the Ibsorpllon of ISpmn . DIJHIIOn 37: 17S-183, 1987 COI,I~'IOI,I P. Fleury B. 8010~ M, iklbcder AM. Vlncon G. CI al. Pharmao:oclll~IKlue: de ralrool Iprts perfu$lon Intl1lVfl_ Ile'use de IrolS heurcs avec el sans clm~lId lne clln dl. sUJCIS Ioams non alroohqucs. GaWotnlerolOJlf Olnlque: ft BloIo'Ique: 8: 103- 108. 19S4 COWIn GO. Das KM . Eastwood MA. Further slI.Id ies of 51,11· phnallzlnc metabolism In the U'nlment of Ultt-rallwf cohtls. Bnll~ MedlCll Journll 2: 1057-1059. 1977 Co_ SR. Krobolh PD. Andcrsotl PH. Smith RB. Meehanlsm for tM inlrractlon btl~n tlllZoIam Ind C1rN1.ichnc. Blophar. mlttl,lllCS Ind Dru, OIsposlllon 7: 567-575. 1986 Crilchl Kclly JG. Salem SAM. Kinne) CD. Shanks RG. ~kDc>1I1 lXi. Effects of ranludlne on the dlspoSllIon of melOprolol, 8f1ush Journal ofChnleal Pharmacolos) 19: 219_224. 1985 Kendall MJ . Laughcr SJ. Wlll ,ns \111. . Rallltldlllc. Clmelldlnc and
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mCloprolol: a pharmacoklllcllc IIItcracnon siudy. GaSlrocnterolog) 90: 1490. 1'186a Kendall MJ. Lobo J . Wllk'M MR . Ralllud,nc. c>mendllle and nlfeoliles and Olher prodrup of 5·ammosahcylic aCId. 0;n;ca1 Pharmaroklllellc$ 10: 285·J02, 1985 Kl oll U. Lacl of effccl of nllatldlne on drUI melabollsm. Scan· d,naVlan Journal of GaSlTOcls of mldazolam, ClinIcal PharmacolOSy and Therapeuncs 38: 652· 655. 19853 Klotz U. A"'cla P. Rosenkranz 8. Famotldlnc. a ne .... H!-rcceplor anlagOnlSI. does nOI aff..rt hepallc ell milia lion of dlazcpam or tubular SCdom.ztd. ~bo con uolled. dotIbIc:-bhnd. dose l"Iu,,, nl clinICal tnll. GastroenteroloiJy 9J: 12H-126l1987 MlClllels M. Her>dn kl R. He)'ums S. Rao.:h OlmmullOflJs.y of the . n tod iarrhoeal ~mode. L.k ScH:TICe$ 21: 45 1-459. 1917 M.chiels M. Ucndnks 11.. Heyhnll J . On the phannIKOlr.IIH:" ... of dom ~ridone .n Ini mals Ir>d min: II . Ti$$ue d'Slnbu h o n. plaantal ar>d mil k lr ansfer of domperidol'l< in lhe: Wistar ral. EUropelln Jourmcl of Dnaa Metabol.sm ,r>d Piurm.acol"ncllCS 6: J7-48. 198 1 MICh iels M. MonlMllu J. Her>dnks R. Gccm 11.. Wotstenboflhs R. et II. Pil.arrn;t(ol"netlCS Ir>d 11_ d."nbunon of the I'H:W Il§lroklnctlC qent Clsapride In ral. rabbi l ar>d dol.- Annel· millel·Fonch un, J7: 1159- 11 67. 1987 MilJl10n M . Cha u N P. N,uyen· Ph uoc BK. Sa uvage M. l.q:uy F. el al. lI.a m udlnc upon mcal Ir>ducnl pSlric KCrrlioo. oral pharmacokil'H:ucs .r>d plasma conanll'1llion effeel relauonihlps. Bri hsh Journ.1 of ClinICal PhlrrnxolOl)' 14: 187·19J. 19821 M...,on M. VIIH:r J . Ba uer P. Bonlils S . E ffect of pi rrnuplI\C on mcal-sllmulated IC1d ~lIon ,r>d pSlnn releasc In nonnal ma n, Scdll'Ulvllin Journal of Gu!fOI:mC'fOloCy 17 (Suppl. 72~ 14S-151. 1982b Ml lialy G W. DNmmer O H. Mar1hall A. Smal111o'ood II.A. loUIS WJ . Hla)I pres$ure hquid e hroml tOlflphlC ~lerrnl l'Ul1l0n of ranitidlne - I new H2 rettp\.Of anlllOnlst in plasml.r>d unne. Joumalof PhI~I Scoenca69: 1155-1131. 1980 Mi llaly G W. Mlnno AT . We~r LK. JOI'H:$ 08. LouiS WJ. el a1. H ia)l dose o r antacid (Mylantl II ) rrducn bioiIvallabi lil y ofranitidine. British Medial JournI1 28S: 998-999. 1982 Mi llal)' G W. Pnc hard PJ. Smallwood RA. Veomans NO. loUIS WJ . Sim u ltaneous hia)l·~rforml nce hquid e hromllOlflphIC IlUIlysis of omepruoic ar>d liS s.ulphone.r>d sul p'lIdc 1IIC1lboIl1es In h uman pluma and unnc. Journal ofChromatOlflphy 278: J II-119. 191) Miller OD. MlICklin M. Cimetodlno·lmlpramlne InICfac'llon: a case rrpon. Ammcan Jo u rnal o f Psych iatry 140: 33 1·132, 1983 Mil ler D O. Sawyer JO. Du ffy J P. Cimetid ine's eff~1 on steadystale SCTUm nonnptylinc oonc:enlraIIOns. Druj Intcllitence Ind Chntall Pharmacy 17: 904-903. 198) M.ller R. Pharmacokl nellCS ar>d bloa. ... ilabolily o f flIn llodlnc .n humans. Joul'IIIIl or Phannaceul lcal Sacnces 11: 1)76-1J7i.
.ncr
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Miners )0. A" wood J. B,,1,eu OJ. I)o::termll'Ulnts of acetaminophen metabolism: effect of inducers ar>d in hIbi tors of dru, mellbolism o n ac:cUlmi nophen's metabolic palh ways. Cl inical PharmaoolOl)' ar>d Thra~ul1CS 33: 48Q.486. 19114 Miners JO. Attwood J . Will' LMH . Bu.... en DJ . In nuence of CI·
mehchnc. sulp'unpyI'1llOM. ar>d ClpR'ue ""~Inc on lheobromIne IIICtabollsm In man. Dru& Metabolism and o.S[lO!i'\lon I): 398-601. 1985 M ltchard M. Hams A. Mullinter B M. Rlnn ,d,nc druC Inlerac_ lions - a literalure rrVlew. Pharmacolosy and Thl"l"lljX'ulies 32: 29).)2S. 1987 M llclM'lI Me. Schen ker S. Speq KV , Sclrc\lve In hlblton of acetamlnoplocn O.Klallon and to.IClty by elmelid,ne and Other hl~l . Imine H;!-rettptOf anlllOfl'sts /II rtlV ar>d /11 >lIfO In tIM' ral and In man. Journal ofOmoc:alln ...·sI.IJlIIQrl 11; )8)'J91. 1984 M llclM'lI SC. Idk J R. Smllh II. L TIM' metabohsm or (I~) CI' mctld lne In man. XenobcotlCl 12: 211),292. 198211 M itchell SC. Idk JR. SmIth II. L lI.educllve metaboli sm o f CI· metldlne sulpho.id DlsPOSIloon 10: 289--290. 1982b M llelM'lI SC. Wanne R H. Id~ J R. Smllh RL C'lIIClidlnc pre_ ~Imcnt dccn:u:s CI~ne sulpho~odIl00n In man. III.CS MedICal Scot:nce: Drut Melabollsm ar>d TOllcolosy 9: 10281029. 19111 Mlwa M. Tant M. MIWI T. In h lblllon OfP51rlC ~"on by, new H l~ntllOnisl. VM- 11 170. 111 healthy 5ubJI'Cts. Inlerna_ IlOn.1 Journal o f Cl, nlCal PharrnaeolOl)' Therapy and TO~I· colOI)' 22: 214-217. 1984 MO,lavman P. Fedder IL V1asscs PH. 1I.0tmen$Ch HH . ROttI M L et . 1. C,melid , ne don lIOIallCl" mOfll'Une dlsposuoon In man. Bn tlih Journal of Clinical Phlrrnacolosy 14; 809-813. IQII2
Monk J P. Cll$$OId SP. MI50pI'OItol: • prelomlnary rrv~w of 11$ pharrnacod)'namlC and pharrnacokinctie pro~rtlts. ar>d lher'~UIIC effICacy in the , rralmenl of ~p\.1C ulcer dlSCIsc. Drup J): 1-30. 1987 Morpn MV. Stambuk O. Famolldlne pharmacokinetICS folio"'· Ina 01'111 .nd Intravenous ao.:jml n lSU'lllOn In pallents Wllh h,tf dlscaK: results or a prelimllUlry study. Posltnduate MedICine Joul'llll1 62 (Su ppL 2): 29·17. 1986 Monc ha u_8H uchan t M. HoulII G. MaV IN P. Aleur>drr C. Ohu_ lIICau. D. Phlrmaeoklncll ... ar>d bloavaillblhly of ranilld ine in nOl'mlI subj«ts and CII'ThOlIC patH:nls. o.tes"ve o.SClset. ar>d ScH:nca JI : 11l-118. 1986 MonOd to~tcoIou of nllalldlne. SCln· d,lllvlln Journal ofGa5troc:ntm:olo&Y 22 (SuppL 136~ I'" 1987 MUirhead M. Bochner F. SomOlyl A. PhlnnacokllletlC dfUlln· Il"I"IICIIOns betllottn mlm lercnc and I'1Inllld ' ne In humans: al· teratlons .n rrnal Ir>d hepahC clearances and pstrointtshnal absorpllon. Journal of PharmacalOlY Ind e...~n mental Ther. a~ulla 244: 7}4-719. 1988 MUirhead M. SomOl),1 A. lI. oIln P. Bochner F. Effen oreullClI· dIne 0d hcpoIue d1'\O' cllmllllUOn: sludies wllh tnam· lercnc. Cl.nlCal PhlrmacoIo&y ~r>d Therapeu tlC1 4(): 400-407. 1986 Mulder CJJ . Tylp l GNJ. Welerm~ n IT. Ot: kker W. BIoi< p. el II. Doublc:-blir>d compa n IOn of slow·n:lelte 3-ammosahqlatt and sulfasaluine III rrmlnlon m ainte nance In ulcC'rall~C col· IllS. GutroenlaolocY 9S: 144~ 14S3. 1988 Mulkcy PM. Murp/l)' JE. Shletfer NH. S!eadY4111e thcoph)'lhne phannacoklllC:IICS dunn, ar>d Ifter lJIon·ltfm cII"cud,n.: admlmslraloon. Cllmcal Phlrm.acy 2: 4)9...«1 . 198} M ul~rsman G. Goll V P. Russell WL Ot:rrnOorf H. Lack or cli nica ll y S ,lni lica nl in .,lfO and III 1'1111 III leBClions belween ramlld ine ~nd sucral f. le. J oum~J or PharrnaaullCIl ScH:IICCS 13: 995-998. 1986 MunpU O. Talbert RL Ph illips C. JaITe D. Ludckn T M. Sucralfate Ind Wlrfann. Annals of Inlcrl'Ull MedOClne 98: SS7. 1983 MutKh ler E. Spahn H. Km:h W. The IIIlel'1l(llOn betWttn H ! rr«plOf InUilOnlSls . nd bell·adrrnoceplOf blockcn. Brit ish Jou rna l o fCl mical Phlrrnaoolol;y 17: SIS-HS. 1984 M )'C'rs B. E... ns DNW. Rhodes J. Evans BK. Hu&hc:s BR. el al. Metabolism and unlll!')' u~lIon of 3~mlno sahcylic acid In
Pharmacokinetics ofGaslromlCSllnal Drugs
hcallh) 'olunlc("~ "hcn ,,,en Inlra'~nously or relcaloCd for absorption al dlfferenl snes ,n Ihe gaslro,nlnllnal IflICI. GUI 2& I%-~. 1987 NlIC'wal J. o\ndel"sson T . Rodemar G. u.f»On R. ResJrdh eG. CI al Plurmacol"'ello of (1"'(") omepnlLo~ In pallenls ... nh Imp:urc-d renal funcllon Scand,na' Ian Journal ofGulroenler· 0101) 20 ISuppl 1131 J4 19&j 'lIC'wal J. o\ndeflown T. Rodemu G. u.rs.on R. R.,prdh CG. el al PharmlcolllK'lIN. (Iolel omcpralOle In pallCnl~ ",Ih 1m· pam'd renal funcllOn Cimini PharmarolOK) and Thcr:lprulln 40: 344.3)1. 1986 'aewal J . Hanle! M Rodemu G. Gonhard R. LundQ"~1 (;. el al Th ... dT«1 of 20ml OlllCpn/O~ d~lly on loCTUm p~lrln. 24-h InlfllPSlrlC" aCid II) and bile" ;acId Wr>CI:nlr.lllon In duodenal uk"n paller"'. Scand,n.".n Journal of Gamoenlero!os) 22 ~-11. 1987 ;0.;,,) E. C~po I. Degrcll I. S'abo G. Hlgh_performanee liquid chrOmalQ&f3phlC" 1»1) of 5·amln()§a h-amlno-WlhS.41 I 1981 lI.o.~·lcc L lIu, le,.ood \ T>rcr III. EadlC \tJ hplnn l,,·a.· mC'nl of n"lrame allach pl~.nla drug iC',cI d~1J Ccphalll~ ! 9. 1982 Ro"IC'~-JolIC'S D_ GralOgC'r "I (,melldl~ b, mll""lmUloCular admlnl~lraIlQn. C'fficx' and loafCl). \\Qrld (onfe..,1"\Ce on Chnoeal PharmarolQl) ar>d TheraptuIIC'S .... bl.lracl '0 J99. \l acMllian . London. 19!1O ItO) ,\K . Cuda M P Le"ne It ,\ Induction of Ih("()ph) IlonC' IO~· lell)' and Inh,blilon ofclnrancc rales by ranllldlnc, Amer"an Journal of MedlCln c 8S 5!s·S27. 1988 Ituffalo RL Thompson JF. $cpl JL OlalC'pam-c,mC'lId'~ drug Inleracll0n. a ch nle:!lI } ~llnlfle coI'liS. AIom of famOlld,ne' !umma~ of dala f1"()m tM linlted Stales. ltal~n Journal ofGaSlTOC'nlC'rolQl} 16 171-176.1984 K}an JR Chrl"mos .\'1. Varp! It . ManlC'1I G. Johnson CL C'I al T~ effect of 'anOUi dose rt"l,mcns of famQlldlne on b;oloal Ru~ns
n
nocturnal and mCal'Sllmulaled IIslne sec..,llun. Chnlul I"harmacQIOi) and TheOlpeUIlO 42_ 22S-lJl. 1987 R)de EM . l,ma JJ HI~\lIlablhl) Slud) on oral sulfaSoliazlne !USpenSlOn compar..:! to t.ablcl! In health) 'Qlunlttl"$. CU1ll'nt "TherapeullC Rnc-arch 29. 728.7)7. 1981 R)de M Ahnrch NO. The pharmacollnencs of oISollnlne' loOd,um m ~alth) ,oIun'C'C'n. after a sln&k' I \ ' dOiC ar>d aller oral dosn ""Ih and " .. houl food_ Eurupeao JQurnal ofCt,nlCal Pharm •• colOll) _14 481-488 . 1988 R)dc M GUSIl\'sson S. Hillary ""ClIun of 015.1la7lnC' loOdlum In humans. Europtan Journal of [)ru, Metabohsm and Pharo macoltneliC'S 12: 17·2~. 1987 R}lane~ GW \Iooo.ls CG. Lamb R The u~ of,nl""coous n.n· lI,dlllC' In SlrnloCd ch,ld..,n GastrocnlC'ro!oc) 92: 1606. 19,7 SaIC'm ItO Breland H[). Mishra St'ds. EpoiC'psla 24 28 ..... ~88, 1983 Salo~n M . Aantaa E. AaItQne'n L KanlO J. ImpOrtan C't' of the Inieraclton of mldalolam and Clmcl,d,nc ACla I"harmacologlca C'I To"coIOS'e:! ~8, 91-9~. 19'6 Sambol NC Uplon RA. Chn:"mo~ "'''. 1111 E. GC'C' W. CI al. In . nuenre of famoud,nc and com~ltdlne on lh~ dispoSl110n of phen}tOln and IIIdoc}'anlnC' grt't'n. Abslraet no. B6. (1,mcal Pharmacolos)' and Thcrapeul to 39, ~2~. 1986 Sandbt-fJ M. HaMson KA lklcrmlnallon of Ioalt~la/osulpha p)ndl~ b,oIOSlcal malC'nal~ l"haOlmacC'ullCI Suttle:! 10: [07·110. 1913 SandoclJ.(jC'n/tn II. larnC'TOI G. "'raal \\ Azod'SollloOd,um In lhC' IrI"almenl of ulreral"c colilli. A slud) of lo1cmnnc and relaPK'pn:,ennn& propentes. GaWOl"nterolos) 90: 102~-10JO, 1986 SandOC'l-Gcrvcn II. K)dc M. brocrol G Absorpltun and ~A' e..,llon of a slnll~ I·, dOloC of a/cd $ill sodium 10 subjects ""Ih IIroiIOm) Scandlna"an Journal of GastrornlC'T01os) 18 107III. 198) Sa,anne V PlcrOOIlO "'. Ma&noloa \11t. Scalabnnl P. M~la GS. Cl al SmllC' bedllmC' dose offamolld,~ asscssmC'n' of liS aOIl1('(..,101") aCtlUn b) ~~.hQur IIItrapS!nC pH monllonna. Jour. nal 0((1,nocal Pharmacolos) 17, "9().79J. 1987 Sall~ E. JaffC' Jp x'e.., ,l1InUIOC)lCpenla ,,"h comelld'ne and phCn}lo,n. Annals of Interna[ MediCine 93: I SI · 152. 1980 Schcn~c. S. l}tckc J. Johnson RF. Mor I. L. IkndC'rson Gf Hu· min placC'ntallranspon ofclm~ndlne Journalof(1lO"alln>nhpllon 80: 1~28·1~34. 1987 Schenta, JJ . Ccrra FH. CaliC'n G. 00: Glopper E. ROiC 1Q. CI al l'I1armiICQk,nellC and cI,nlcal sludo In pallC'nls " ',lh ClmCIId,ne .... nocla lC'd menial confu!lon UIIC'CI I 177.181.1979 Schenlll JJ. Cerra FB. Callen G\f. leiSIO, ME. F..,nch MA . C'I al .\gc. dl~a~. and ClmC'tldmC' dlSl)OllllOn III heallhy subjects and ch ro nlCall } III pallen IS. Cl,nlCll f'harmiICQlO&) and Ther. apl'ullc! ~9 7J7.743. 1981 Schornh~rd G. Oppermann J. Kohn FE. Metabolism and pharo marokmClle slud,Clo of ml~prOSlol. [)'&CloIl'e D'loCaloCS and ScICTI('('S JO iSuppl.); I 26S-128S. 1~8~ Schreder II Campbell [)ES. Absorption. m'olunlcer~ of d,Wd
C Adll InlnTUltlOnal Llmll«l All n&hll ran-vnI. ~. ,
Clinical Pharmacokinetics of Drugs Used in the Treatment of Gastrointestinal Diseases (Part II) Karsten Lauritsen, Laurils S. Laursen and Jorgen Rask-Madsen Department of Medical (fastroenterology, Oden~ IJnivenity Hospital, Oden ~, and Departmcnt of Gaslroe nl crology G, Bispcbjef) Hospital, University of Copenhagen. Copenhagen, Ornmark
Contents
g. Anti-Inflammatory Salicylates ........................... .. ............... _.......... ,................. 94 g.1 Sulfasalazinc ........ ,............................................... .. .............. _................ ...9S g.2 Clsalazlnc ............................................................................................ _............................ 97 g.) Othcr Azobond Prodrugs of S-Am inosaliC)hc ACId ....................... _............................. 9g g.4 Mesaluine ....... ,........... ................. .. ............................................ 98 9. NonSpe1:1fic Anlidlarrhoeal Agents ................................................................................... 100 9. 1 Diphenoxylale ....................................................................... ,................. ,..................... 100 9.2 Loperamide ........................................................................... .. ............................. 101 10. Lauti ves and CathanlC$ .................................................................... ..... 101 ............. ,....... ,.................. .. ..10) Appendix ............... .................... ......
Part I of this anicle, which appeared in the previous issue of tile Journal. cove red th e following agen ts: histamine H2-rcceptor antagon ists (cimetidine. ranitidine. famotidine. nizatidine); muscarinic- M I-receptor antagonists (pirt nzepine): protOn pump inhibitors (omeprazole); site-protecllve agents (colloidal bismuth $ubcit11l te, sum lfale): antacids and prostaglandin analotues: antiemetics and prokinetic;s (metoclopramide, domperidone, cisapride): a nd an tispasmodics. In Pan II . we consider the an ti-i nflammatory salicyla tes, nonspe'n«k ML Achem SR. Cimelldllle'-Hl~ylhne intaKlIon: cffeas o f . Ind Clmelodllle~. ThfflipeullC Dru, Monllon". 1: 426-434. 1985 Conrad KA . Mlycnohn M. 81lss M. C"imelodine docs nOI aller lbuproflon k,netlCli.f\cr. sonale dose. Bnll~ Journal orO'nlal PllarnHlcolosy 18; 62-4-626. 1984 COrTocher R. 8amNI1I LM. Call1ml)Chl P. Tnu R. G,relll M. CI al. EfTeet of I1In llldlne on the Ibsorpllon of ISpmn . DIJHIIOn 37: 17S-183, 1987 COI,I~'IOI,I P. Fleury B. 8010~ M, iklbcder AM. Vlncon G. CI al. Pharmao:oclll~IKlue: de ralrool Iprts perfu$lon Intl1lVfl_ Ile'use de IrolS heurcs avec el sans clm~lId lne clln dl. sUJCIS Ioams non alroohqucs. GaWotnlerolOJlf Olnlque: ft BloIo'Ique: 8: 103- 108. 19S4 COWIn GO. Das KM . Eastwood MA. Further slI.Id ies of 51,11· phnallzlnc metabolism In the U'nlment of Ultt-rallwf cohtls. Bnll~ MedlCll Journll 2: 1057-1059. 1977 Co_ SR. Krobolh PD. Andcrsotl PH. Smith RB. Meehanlsm for tM inlrractlon btl~n tlllZoIam Ind C1rN1.ichnc. Blophar. mlttl,lllCS Ind Dru, OIsposlllon 7: 567-575. 1986 Crilchl Kclly JG. Salem SAM. Kinne) CD. Shanks RG. ~kDc>1I1 lXi. Effects of ranludlne on the dlspoSllIon of melOprolol, 8f1ush Journal ofChnleal Pharmacolos) 19: 219_224. 1985 Kendall MJ . Laughcr SJ. Wlll ,ns \111. . Rallltldlllc. Clmelldlnc and
'15
mCloprolol: a pharmacoklllcllc IIItcracnon siudy. GaSlrocnterolog) 90: 1490. 1'186a Kendall MJ. Lobo J . Wllk'M MR . Ralllud,nc. c>mendllle and nlfeoliles and Olher prodrup of 5·ammosahcylic aCId. 0;n;ca1 Pharmaroklllellc$ 10: 285·J02, 1985 Kl oll U. Lacl of effccl of nllatldlne on drUI melabollsm. Scan· d,naVlan Journal of GaSlTOcls of mldazolam, ClinIcal PharmacolOSy and Therapeuncs 38: 652· 655. 19853 Klotz U. A"'cla P. Rosenkranz 8. Famotldlnc. a ne .... H!-rcceplor anlagOnlSI. does nOI aff..rt hepallc ell milia lion of dlazcpam or tubular SCdom.ztd. ~bo con uolled. dotIbIc:-bhnd. dose l"Iu,,, nl clinICal tnll. GastroenteroloiJy 9J: 12H-126l1987 MlClllels M. Her>dn kl R. He)'ums S. Rao.:h OlmmullOflJs.y of the . n tod iarrhoeal ~mode. L.k ScH:TICe$ 21: 45 1-459. 1917 M.chiels M. Ucndnks 11.. Heyhnll J . On the phannIKOlr.IIH:" ... of dom ~ridone .n Ini mals Ir>d min: II . Ti$$ue d'Slnbu h o n. plaantal ar>d mil k lr ansfer of domperidol'l< in lhe: Wistar ral. EUropelln Jourmcl of Dnaa Metabol.sm ,r>d Piurm.acol"ncllCS 6: J7-48. 198 1 MICh iels M. MonlMllu J. Her>dnks R. Gccm 11.. Wotstenboflhs R. et II. Pil.arrn;t(ol"netlCS Ir>d 11_ d."nbunon of the I'H:W Il§lroklnctlC qent Clsapride In ral. rabbi l ar>d dol.- Annel· millel·Fonch un, J7: 1159- 11 67. 1987 MilJl10n M . Cha u N P. N,uyen· Ph uoc BK. Sa uvage M. l.q:uy F. el al. lI.a m udlnc upon mcal Ir>ducnl pSlric KCrrlioo. oral pharmacokil'H:ucs .r>d plasma conanll'1llion effeel relauonihlps. Bri hsh Journ.1 of ClinICal PhlrrnxolOl)' 14: 187·19J. 19821 M...,on M. VIIH:r J . Ba uer P. Bonlils S . E ffect of pi rrnuplI\C on mcal-sllmulated IC1d ~lIon ,r>d pSlnn releasc In nonnal ma n, Scdll'Ulvllin Journal of Gu!fOI:mC'fOloCy 17 (Suppl. 72~ 14S-151. 1982b Ml lialy G W. DNmmer O H. Mar1hall A. Smal111o'ood II.A. loUIS WJ . Hla)I pres$ure hquid e hroml tOlflphlC ~lerrnl l'Ul1l0n of ranitidlne - I new H2 rettp\.Of anlllOnlst in plasml.r>d unne. Joumalof PhI~I Scoenca69: 1155-1131. 1980 Mi llaly G W. Mlnno AT . We~r LK. JOI'H:$ 08. LouiS WJ. el a1. H ia)l dose o r antacid (Mylantl II ) rrducn bioiIvallabi lil y ofranitidine. British Medial JournI1 28S: 998-999. 1982 Mi llal)' G W. Pnc hard PJ. Smallwood RA. Veomans NO. loUIS WJ . Sim u ltaneous hia)l·~rforml nce hquid e hromllOlflphIC IlUIlysis of omepruoic ar>d liS s.ulphone.r>d sul p'lIdc 1IIC1lboIl1es In h uman pluma and unnc. Journal ofChromatOlflphy 278: J II-119. 191) Miller OD. MlICklin M. Cimetodlno·lmlpramlne InICfac'llon: a case rrpon. Ammcan Jo u rnal o f Psych iatry 140: 33 1·132, 1983 Mil ler D O. Sawyer JO. Du ffy J P. Cimetid ine's eff~1 on steadystale SCTUm nonnptylinc oonc:enlraIIOns. Druj Intcllitence Ind Chntall Pharmacy 17: 904-903. 198) M.ller R. Pharmacokl nellCS ar>d bloa. ... ilabolily o f flIn llodlnc .n humans. Joul'IIIIl or Phannaceul lcal Sacnces 11: 1)76-1J7i.
.ncr
""
Miners )0. A" wood J. B,,1,eu OJ. I)o::termll'Ulnts of acetaminophen metabolism: effect of inducers ar>d in hIbi tors of dru, mellbolism o n ac:cUlmi nophen's metabolic palh ways. Cl inical PharmaoolOl)' ar>d Thra~ul1CS 33: 48Q.486. 19114 Miners JO. Attwood J . Will' LMH . Bu.... en DJ . In nuence of CI·
mehchnc. sulp'unpyI'1llOM. ar>d ClpR'ue ""~Inc on lheobromIne IIICtabollsm In man. Dru& Metabolism and o.S[lO!i'\lon I): 398-601. 1985 M ltchard M. Hams A. Mullinter B M. Rlnn ,d,nc druC Inlerac_ lions - a literalure rrVlew. Pharmacolosy and Thl"l"lljX'ulies 32: 29).)2S. 1987 M llclM'lI Me. Schen ker S. Speq KV , Sclrc\lve In hlblton of acetamlnoplocn O.Klallon and to.IClty by elmelid,ne and Other hl~l . Imine H;!-rettptOf anlllOfl'sts /II rtlV ar>d /11 >lIfO In tIM' ral and In man. Journal ofOmoc:alln ...·sI.IJlIIQrl 11; )8)'J91. 1984 M llclM'lI SC. Idk J R. Smllh II. L TIM' metabohsm or (I~) CI' mctld lne In man. XenobcotlCl 12: 211),292. 198211 M itchell SC. Idk JR. SmIth II. L lI.educllve metaboli sm o f CI· metldlne sulpho.id DlsPOSIloon 10: 289--290. 1982b M llelM'lI SC. Wanne R H. Id~ J R. Smllh RL C'lIIClidlnc pre_ ~Imcnt dccn:u:s CI~ne sulpho~odIl00n In man. III.CS MedICal Scot:nce: Drut Melabollsm ar>d TOllcolosy 9: 10281029. 19111 Mlwa M. Tant M. MIWI T. In h lblllon OfP51rlC ~"on by, new H l~ntllOnisl. VM- 11 170. 111 healthy 5ubJI'Cts. Inlerna_ IlOn.1 Journal o f Cl, nlCal PharrnaeolOl)' Therapy and TO~I· colOI)' 22: 214-217. 1984 MO,lavman P. Fedder IL V1asscs PH. 1I.0tmen$Ch HH . ROttI M L et . 1. C,melid , ne don lIOIallCl" mOfll'Une dlsposuoon In man. Bn tlih Journal of Clinical Phlrrnacolosy 14; 809-813. IQII2
Monk J P. Cll$$OId SP. MI50pI'OItol: • prelomlnary rrv~w of 11$ pharrnacod)'namlC and pharrnacokinctie pro~rtlts. ar>d lher'~UIIC effICacy in the , rralmenl of ~p\.1C ulcer dlSCIsc. Drup J): 1-30. 1987 Morpn MV. Stambuk O. Famolldlne pharmacokinetICS folio"'· Ina 01'111 .nd Intravenous ao.:jml n lSU'lllOn In pallents Wllh h,tf dlscaK: results or a prelimllUlry study. Posltnduate MedICine Joul'llll1 62 (Su ppL 2): 29·17. 1986 Monc ha u_8H uchan t M. HoulII G. MaV IN P. Aleur>drr C. Ohu_ lIICau. D. Phlrmaeoklncll ... ar>d bloavaillblhly of ranilld ine in nOl'mlI subj«ts and CII'ThOlIC patH:nls. o.tes"ve o.SClset. ar>d ScH:nca JI : 11l-118. 1986 MonOd to~tcoIou of nllalldlne. SCln· d,lllvlln Journal ofGa5troc:ntm:olo&Y 22 (SuppL 136~ I'" 1987 MUirhead M. Bochner F. SomOlyl A. PhlnnacokllletlC dfUlln· Il"I"IICIIOns betllottn mlm lercnc and I'1Inllld ' ne In humans: al· teratlons .n rrnal Ir>d hepahC clearances and pstrointtshnal absorpllon. Journal of PharmacalOlY Ind e...~n mental Ther. a~ulla 244: 7}4-719. 1988 MUirhead M. SomOl),1 A. lI. oIln P. Bochner F. Effen oreullClI· dIne 0d hcpoIue d1'\O' cllmllllUOn: sludies wllh tnam· lercnc. Cl.nlCal PhlrmacoIo&y ~r>d Therapeu tlC1 4(): 400-407. 1986 Mulder CJJ . Tylp l GNJ. Welerm~ n IT. Ot: kker W. BIoi< p. el II. Doublc:-blir>d compa n IOn of slow·n:lelte 3-ammosahqlatt and sulfasaluine III rrmlnlon m ainte nance In ulcC'rall~C col· IllS. GutroenlaolocY 9S: 144~ 14S3. 1988 Mulkcy PM. Murp/l)' JE. Shletfer NH. S!eadY4111e thcoph)'lhne phannacoklllC:IICS dunn, ar>d Ifter lJIon·ltfm cII"cud,n.: admlmslraloon. Cllmcal Phlrm.acy 2: 4)9...«1 . 198} M ul~rsman G. Goll V P. Russell WL Ot:rrnOorf H. Lack or cli nica ll y S ,lni lica nl in .,lfO and III 1'1111 III leBClions belween ramlld ine ~nd sucral f. le. J oum~J or PharrnaaullCIl ScH:IICCS 13: 995-998. 1986 MunpU O. Talbert RL Ph illips C. JaITe D. Ludckn T M. Sucralfate Ind Wlrfann. Annals of Inlcrl'Ull MedOClne 98: SS7. 1983 MutKh ler E. Spahn H. Km:h W. The IIIlel'1l(llOn betWttn H ! rr«plOf InUilOnlSls . nd bell·adrrnoceplOf blockcn. Brit ish Jou rna l o fCl mical Phlrrnaoolol;y 17: SIS-HS. 1984 M )'C'rs B. E... ns DNW. Rhodes J. Evans BK. Hu&hc:s BR. el al. Metabolism and unlll!')' u~lIon of 3~mlno sahcylic acid In
Pharmacokinetics ofGaslromlCSllnal Drugs
hcallh) 'olunlc("~ "hcn ,,,en Inlra'~nously or relcaloCd for absorption al dlfferenl snes ,n Ihe gaslro,nlnllnal IflICI. GUI 2& I%-~. 1987 NlIC'wal J. o\ndel"sson T . Rodemar G. u.f»On R. ResJrdh eG. CI al Plurmacol"'ello of (1"'(") omepnlLo~ In pallenls ... nh Imp:urc-d renal funcllon Scand,na' Ian Journal ofGulroenler· 0101) 20 ISuppl 1131 J4 19&j 'lIC'wal J. o\ndeflown T. Rodemu G. u.rs.on R. R.,prdh CG. el al PharmlcolllK'lIN. (Iolel omcpralOle In pallCnl~ ",Ih 1m· pam'd renal funcllOn Cimini PharmarolOK) and Thcr:lprulln 40: 344.3)1. 1986 'aewal J . Hanle! M Rodemu G. Gonhard R. LundQ"~1 (;. el al Th ... dT«1 of 20ml OlllCpn/O~ d~lly on loCTUm p~lrln. 24-h InlfllPSlrlC" aCid II) and bile" ;acId Wr>CI:nlr.lllon In duodenal uk"n paller"'. Scand,n.".n Journal of Gamoenlero!os) 22 ~-11. 1987 ;0.;,,) E. C~po I. Degrcll I. S'abo G. Hlgh_performanee liquid chrOmalQ&f3phlC" 1»1) of 5·amln()§a h-amlno-WlhS.41 I 1981 lI.o.~·lcc L lIu, le,.ood \ T>rcr III. EadlC \tJ hplnn l,,·a.· mC'nl of n"lrame allach pl~.nla drug iC',cI d~1J Ccphalll~ ! 9. 1982 Ro"IC'~-JolIC'S D_ GralOgC'r "I (,melldl~ b, mll""lmUloCular admlnl~lraIlQn. C'fficx' and loafCl). \\Qrld (onfe..,1"\Ce on Chnoeal PharmarolQl) ar>d TheraptuIIC'S .... bl.lracl '0 J99. \l acMllian . London. 19!1O ItO) ,\K . Cuda M P Le"ne It ,\ Induction of Ih("()ph) IlonC' IO~· lell)' and Inh,blilon ofclnrancc rales by ranllldlnc, Amer"an Journal of MedlCln c 8S 5!s·S27. 1988 Ituffalo RL Thompson JF. $cpl JL OlalC'pam-c,mC'lId'~ drug Inleracll0n. a ch nle:!lI } ~llnlfle coI'liS. AIom of famOlld,ne' !umma~ of dala f1"()m tM linlted Stales. ltal~n Journal ofGaSlTOC'nlC'rolQl} 16 171-176.1984 K}an JR Chrl"mos .\'1. Varp! It . ManlC'1I G. Johnson CL C'I al T~ effect of 'anOUi dose rt"l,mcns of famQlldlne on b;oloal Ru~ns
n
nocturnal and mCal'Sllmulaled IIslne sec..,llun. Chnlul I"harmacQIOi) and TheOlpeUIlO 42_ 22S-lJl. 1987 R)de EM . l,ma JJ HI~\lIlablhl) Slud) on oral sulfaSoliazlne !USpenSlOn compar..:! to t.ablcl! In health) 'Qlunlttl"$. CU1ll'nt "TherapeullC Rnc-arch 29. 728.7)7. 1981 R)de M Ahnrch NO. The pharmacollnencs of oISollnlne' loOd,um m ~alth) ,oIun'C'C'n. after a sln&k' I \ ' dOiC ar>d aller oral dosn ""Ih and " .. houl food_ Eurupeao JQurnal ofCt,nlCal Pharm •• colOll) _14 481-488 . 1988 R)dc M GUSIl\'sson S. Hillary ""ClIun of 015.1la7lnC' loOdlum In humans. Europtan Journal of [)ru, Metabohsm and Pharo macoltneliC'S 12: 17·2~. 1987 R}lane~ GW \Iooo.ls CG. Lamb R The u~ of,nl""coous n.n· lI,dlllC' In SlrnloCd ch,ld..,n GastrocnlC'ro!oc) 92: 1606. 19,7 SaIC'm ItO Breland H[). Mishra St'ds. EpoiC'psla 24 28 ..... ~88, 1983 Salo~n M . Aantaa E. AaItQne'n L KanlO J. ImpOrtan C't' of the Inieraclton of mldalolam and Clmcl,d,nc ACla I"harmacologlca C'I To"coIOS'e:! ~8, 91-9~. 19'6 Sambol NC Uplon RA. Chn:"mo~ "'''. 1111 E. GC'C' W. CI al. In . nuenre of famoud,nc and com~ltdlne on lh~ dispoSl110n of phen}tOln and IIIdoc}'anlnC' grt't'n. Abslraet no. B6. (1,mcal Pharmacolos)' and Thcrapeul to 39, ~2~. 1986 Sandbt-fJ M. HaMson KA lklcrmlnallon of Ioalt~la/osulpha p)ndl~ b,oIOSlcal malC'nal~ l"haOlmacC'ullCI Suttle:! 10: [07·110. 1913 SandoclJ.(jC'n/tn II. larnC'TOI G. "'raal \\ Azod'SollloOd,um In lhC' IrI"almenl of ulreral"c colilli. A slud) of lo1cmnnc and relaPK'pn:,ennn& propentes. GaWOl"nterolos) 90: 102~-10JO, 1986 SandOC'l-Gcrvcn II. K)dc M. brocrol G Absorpltun and ~A' e..,llon of a slnll~ I·, dOloC of a/cd $ill sodium 10 subjects ""Ih IIroiIOm) Scandlna"an Journal of GastrornlC'T01os) 18 107III. 198) Sa,anne V PlcrOOIlO "'. Ma&noloa \11t. Scalabnnl P. M~la GS. Cl al SmllC' bedllmC' dose offamolld,~ asscssmC'n' of liS aOIl1('(..,101") aCtlUn b) ~~.hQur IIItrapS!nC pH monllonna. Jour. nal 0((1,nocal Pharmacolos) 17, "9().79J. 1987 Sall~ E. JaffC' Jp x'e.., ,l1InUIOC)lCpenla ,,"h comelld'ne and phCn}lo,n. Annals of Interna[ MediCine 93: I SI · 152. 1980 Schcn~c. S. l}tckc J. Johnson RF. Mor I. L. IkndC'rson Gf Hu· min placC'ntallranspon ofclm~ndlne Journalof(1lO"alln>nhpllon 80: 1~28·1~34. 1987 Schenta, JJ . Ccrra FH. CaliC'n G. 00: Glopper E. ROiC 1Q. CI al l'I1armiICQk,nellC and cI,nlcal sludo In pallC'nls " ',lh ClmCIId,ne .... nocla lC'd menial confu!lon UIIC'CI I 177.181.1979 Schenlll JJ. Cerra FB. Callen G\f. leiSIO, ME. F..,nch MA . C'I al .\gc. dl~a~. and ClmC'tldmC' dlSl)OllllOn III heallhy subjects and ch ro nlCall } III pallen IS. Cl,nlCll f'harmiICQlO&) and Ther. apl'ullc! ~9 7J7.743. 1981 Schornh~rd G. Oppermann J. Kohn FE. Metabolism and pharo marokmClle slud,Clo of ml~prOSlol. [)'&CloIl'e D'loCaloCS and ScICTI('('S JO iSuppl.); I 26S-128S. 1~8~ Schreder II Campbell [)ES. Absorption. m'olunlcer~ of d,Wd
