keeping down the lipid levels! — a look at the drugs available
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KEEPING DOWN THE LIPID lEVELS! - Alook at the d rugs available
COlESTIPOl ('Colestid'. recently launch ed bV Upjohn)
o Ph armacologyColeSl ipol hydr ochlor ide, a new hypolipidemit drug a two -year "!lIdy.
Cooper, E.E. et al . Soulhern Medical Jou rnal 68, 30 ) ( 197 5).
Enhancement or cnoteseronurncver in ratsby a <;atalo~ic "'-eroid (peN) and abile acid sequesiram (CoICSlipol·HO). HOllOOan. T. e r at. Biochemical
Pharmacology 24, H99 (I 9151.Effects of candicidin. cotesuoot and triparanol on sserol bic>synlhesis and
lipoprotein dist ribution in hamsters Wang. G M. et al. Federano n
Proceooillgs 34, a 12 (l97S)The effec ts of colestipol o n the I1'"Ielal.lolism of very-low -density lipop roteins in
ma n, WilllUm, J,1.. el al . Jou rnal of Laboraw ry and Clin ical Medicine s a :
lOOl\(l976l.Effect of candicidinand cojcsupot on the testesand prostateglands of BIO
&7.20 namsters. Geng Mei W ang et at. lnvesugauve Urology 14, 66(19 76)
Effectsof role.\.lipol hydrochlorides and neomycin su lfate on Cholesterol
turnover in !he rat. Ph illips. W .A, et aL Lip ids 12, 10 ( 1977 )
Prepa ration on"ClcoJ~tipol hydrochloride and its d ispos ilion in the human,dog and raL Thomas. R.C . et ai, Atherosclerosis 29, 9 ( 1978)
o And clinica l trialsExperience wilh a new chojesrerol-lowenn g resin. coJestipo t M uts. E. el al
Acta Clinica Belg sca 30, 409 ( 19 75)
l ..ong-term effects o f cojesuoot(v· 26. 597 A)o n plasma lip ids in famili al type
It hype rbeLafipop rute inaemia. Fellin , R. et at Atherosc lerosis 22: 43Iil975)
Hypo cho les te rolemic acti vity ofrole.'tipel in diabetes Bandisode. M.s. et aL
Cu=nt Th erape utic Research 18: 276 ( 19751
Cotesnnct. Clofibrate . chotesryrarmne and ccrn binatjon thcrap y in the
treatment of familial hyperbcLatipoproteiruemia Stein , E.A. et aL South
Arr ican Medical Journal 49: 1252 ( 1975)
C..olcstipol hyd roch loride. a new hypohpidemic drug, a two-year study.
Cooper. f .E.et al. So uthe rn Medi<.:al Jo umal 68 : 303 ( 1.,751
Lo ng-term treatment of hyperc holesterolemia with cote.,'ipol hydrochloride.Ryan . J.R, et aL Clinical Pharmaco log y and Therapeutics 17 : 8 3 ( 19751
Cbolesterot-Icwering effect of ro lestipo! bydrochloride given twice daily in
hypercholesterolemic patients, Gundersen. 1<. et al , Athe rosclerosis 25,
J 03 «976)
CoI=ipel in familial type II hypc rhpoproteinaernla, A th ree·yea r tr ial.
Har vengt. C et al. Cli nica l Pharmacology and Therapeu~ 20: 310(1976)
Results of colCSl.ipoltherapy in type 11 hyperlipopro~inettlia Lees. A.M et at.AUteroscle rosis 24: 129 ( 1976)
Clo fib rate·induced low dCTI&ity lipop rote in ekv~tjQn -c- rherapeuuc
implications and treatment by wle.~t ipol resi n. Rose, HG . et at.Atherosclerosis. 23, 4 (3(1 9761
Pedialr ic familial type II hype rhpoproICinemia ,Therapy with diet and
wlestipol. G lueck. CJ, et a t Pediat rics 51, 68 (1 976)
fllc effect of wlestipol on digitoxin pla:;ma levels. Bever. R,J, et al.
Arzneimittel.Fo rschulJ8 26, 1891 (1 9761
Long-te rm lherapy of diet -resistant hype rcholesterolemia with cotesupot.Mishkel. M.A. et al. Current The rapeutic Resea rch 22, 398 t 197 7)
Coles tipol in the treatment of diabctic patien ts with hypercnoleaero jerma.
OunlSCh. G Fortschrme der Med i1.in 9S: 1492 (19171
ColeSlipol, clofibra te. and pl!ytoste rols in oombined ther" py of
hyperlipidemia, Gru ndy. S.M. e t a l. Jo u rnal of Labora to ry and ClinicalMal icine 89, 3S4 (I917)
Cole.~tipol treatment o f ltypcrclto lcstero lemia for up to 8yr. Ryan. J.R . er a t.
Cl inical Pharmacology and Th eratn:ut ics 2 1; 116 {191 1)
Type II hyperl ipeproteinaemia Treatmen t with colWipel and p~«)fe n .
Sau vanet. J.-P . er at. La Nou velle Prcsse Medicale 7: 186 2 (1978)
Long· ter m trial with colesupol plus clofibra te in famil ialhypercho lesterolemia. Fellin , R,ee al. Athe rosclerosis 29: 24 1 ( 1978 )
Co\estipolltydrocb\Ofide for treatment o f hy percholesterolemia in a family
practice Five·y"" r study. Ruo ff, G . Jo urnal of the American GeriatricsSoc iety 26: 121(1 918)
Th e crrec of rolesl,po) hydrochloride or cholesry rarmn eon the bioavai)ability
and pharmacokinelics of clofibralt: . 79th annual meeting of the American
Soc ieWo f Clinical Pl1ar macology and The rapy. De Sante. K.A ,et aL
Cl inical Ph~rmaco logy and Th erape utics 23 : I r2 ( 19781
PROBUCOL! 'lorel co;' Dow , a not he r new introduction)
Long-term oral ad min istration of probucol (4 .4' -isopropy lidened itbiolbisl 2,6·
di+durylphenoIHDH-58I ) in the management o f hypercho les tero lemia
Harr is . R-S.e t aI. J<lurnal o r tile Ame rican Geriatrics Society 22, 16 10 914 )
Safety and efficac y of probocol during one ycarof itdministration. J\:ash, DT.
Journal o f Clinical PlIar maco logy 14: 470 ( 1974)The addruve effect of probuco! on d iel in hype rlipide mia. Brow n, H B. e t al.
Clinical Pharmacology and Therapeu tics 16: 44 (19 74 )
Safety and emcacy or crobocor d uring one year o f admin istrat ion. Nash, DT.
Jo urna lof Clinical Pharmaco log y 14 ,4 70 (197 41
T reat men t of se vere and mild hypereholcS\e rolaemi a with probucol and
neomycin. Mietlinen . T.A . er al. Postgraduate Medical Journal 5 1, 71(Suppl e M. 1975)
Proo ucol. A ne w chclesterollowermg d ru g. Nash , D .T, Journal of Medicine
6: 305(1975)
Long-term lly poeltoles~ rolernicdrug therap y w ith probuool(D H 58 ! ) in
hu ma n sub.it:cts. Ca nosa . FL el aL Clinical Phar maw logy andTh erapeutiCS 17, 230 ( 1'175 )
Probuco! - ~ew cholcsu:rol· lo wering dru g effective i~ patients with type- !!
hyperh poproleinemia, Said. A,F . er ai, C1ini<.:al Pharmaco logy an dTherapeu tics 10: 690 ( 1'1761
Probucol. Drugs of the Future I L 128 ( 19 77)
An ove rvie w of the b iochemical phar macology of pro buooL Barnhart. J. W. eral. lip ids 12 : 29 ( 1977 )
Probucor.a new antihypcrlipidemic. Russo, C. Currenl Prescrib ing 3, 7r( 19 771
Pro buro l for hyper<:boleste rolemia , Medical Lener 19: 41 ( 1917)
Diet and pru buool in lo wer ing Cholesterol concemreuons- add itive e/Teets
on pla.~macholesterul COl\CCn\l,llions in patie nts with familial type 2hyperlipuprolelJ\emia , Lclo rier. J . CI aI, Arch ives o f In ternal ~edicine
137: 142 9(1977)
Probuco l Iw reieol in treatment or hype rlipemia , Murp hy. B F. Journa l o f tileAme rican Med ica l Assoc iat ioo 238, 2537 (1 97 7)
Diet and pro bucol in lower ing cecicaerot concent rations. Letcnee. J. CI al.Archive.; o f In ternal Medicine 137 , 1429 (19 1 7)
!' robuw ] Drugs o fToday 14 ,33 (1 9781
EFfectof probucol on ck,fib rale resistanl familial hypercholC'Sterolemia ,
Le t.orfer. J. et al. Annals of the Royal Coll ege of Physicians and Surgeonsor Can ada I ( 35(1'17M)
Combined r~lts of the Sludy ofprobuool a l l mg fday in eight centers ,
Taylor. H.L. et at.Qini"",1 Pharmacorogy and Th erapeutics 23: I J I( 191 81
Prob uOJ1: a review of us pharmacological pro perties and therapeu tic use in
palie Ols with hyperchuleslero laemia, Heel. R.C. CI at. Drugs 15: 409\1 97M)
INPHARMA 17t h June, 1978 pt 9
CHOlESTYRAMINE ('Cuemid '; Merck Sharp& Dohm e, 'Quest ran': Bris t ol)
o PharmacologyIn vivo effectof bile sens and cholestyramineon intestinalanaerobic bacteria.
William:<, R.C er aJ. Gastroenterology 69 483{197SJ.Failure of chole5\)'ramine to p~ent eue san injur}'to IllOU-I:t:pstJic m\llCOS&.
Ea...-t....ood , G ,L Gastroenttto!oey 68, 1466 1191S).Effectol' cholestyramirleon ~ue poob ol'cbolesterol: A preliminuy rcpo n..
KUokbodkaT. S.J. d aI. Pnx:minr of !be Soc iety for upmmenlaJBiolojy and .'Iledicitlt 148: 393 ( 19751,
Cho~ramine- iDduccd inhibition of salic)'larosulfapyriditlt (sulfa.<;aLalinc)metabolism by rat inlCninal microl'lo.... Picniaszek. H.J. et at. Journal ofPharlllaC()logy and E ~ perimental Therapeutics 198: 240 I 1976).
Bion aib bihty of prednisolone durinj simulllUleOllS treatment withcholeo;ty ramine. Audcw et al. G~1rOCnterology 1 1 1110 (1916).
E!Teaof tholc:styramine on absorptioon or nicotinicacid and clofibrate HahnK ·J. etal . Naunyn-5chmiedebefJ 's "' rchivesolPhu~ 29'4 R8 'lSuppl, 1916).
EffectS or d!olesQ'ramine and iJeaI by-pau ce serum cbolesteroI and fCQISlCrofd$ ill patients ....ith familial untho~IOl:ic Iypc IIh~rcholesterolemia. Mieltinen, T..... AmericaJI Jourml or CardiolOCY39, 308(911).
Interruption or the enterohepanc circulation or phenprocoumon bychole~tyramine. Meinertt . T . et a1. Q inical PharmacololY andTherapeutics 21: 7J IlJ977l
Jnnueece of isoproIerenolandcholeslyramine on acu~ pSU'ic mooosaJuleerote~ Ritchie, W.P. el l--!. GlISlroenteroioD 7J: 62 (11177).
Tbeeffea of choayramine on the f~ ncretion ol'biJeacidsand neunl~$ in fvnilial hypercholc5tcrolaemia.. MQ<lta(l$. C.O. et I--!.Atherosclerosis 26: J29 111117}.
Inn~nc.e o(choles!yrami/lC on lbechmination ol EMO 26 644.~ novel '~llIirheumati<: substance. leopold . G. et AI . rliaunyn·Schmiedebe"a"sArchives of Pharmacology 291: 62 ISuppl. 2, 1971),
Effect of cholcstyramine on pepsin activity in vitro. Liebman. W.M. et aI.IRCS Medic.al Sc:ienoc: Qinical Pllannagology and Therapeutics 6: lOS(1 918 ).
o And clinical use in hyPe rlipidaemiaColeslirNII, clor.bra~. cho!eslyramine and combln'lUon therapy in !be
trelunenl o( f~mil ial hyperbetalipopfO(rinacmilL S~in . f ,A. ell--! , SouthAfrican Medical JOUrnal 411 , r251 1111'S).
Chole'\lyramine, cloflbr.llle and nicotinic aci<lassingieor combined treatmentof type lIa and Ub hyperlip<.>proleinaemia IProctedings of an international
symposium at S....edlSilSociety or Mldical ScieDces.. Stoxtholm. 8.11October. 19141Oro. L et aI. POS\&raduate Med>l:aI JQ<lnW S1: 16 ISuppi.8, 1975J.
Type Ila hyperbpllJ'l'OUi-=mia.. ADevaluKion of four therapeutic Il:&imens.Watermeyer. G.S el al. South Arrican Medical Journal 411: 63111 91$).
Cornpanson of treatmenll; (or congenital non'ObslrucUve oontlaemolytichyperbili rub ina~mia. Payne. R.B. et at. Archives of Disea.....in ChildhoodSO: 191 (191S).
Cboiestylllmine and hyper1ipidemill, Pladlllier. A. et aI. La Revue deMedecine 11, '94 (1916).
Trealment or h~holesxerolemia Vl'ith SocboleJ - a Ioni·lerm c1:inic&l trial
and com~ ....ith dKMestyramine. Nikkilae. E." . et aI.Atherosck-rt>sl< 24: 401 (1916).
Therapeutic failu~ in ramilial type II hyperlipoprolCinemia. Witte~ L .... etaI. Metabolism 2S: 1017 (1916).
A comparative study or thc effectsof chokstyramine and neomycin in thetreatment or type II hyperlipoproteinaemia, Schade, R.W.B. et al. ACIll
Medica Scandinaviclo 199: 11' (1976).Cbolcslyramine: An effective. lWioeodaily <!osage rqimeD. Blum, C .B, et ai ,
Annals oflptunal Medicine 8S: 281 (191M.Dose-dfect reIatioII of eholeRyrallUtIt in dlild ren and youlli adults WIth
familialhypercllolc$ttrolKrnia. Farah. I.R. et I--!. Larx::et I: '9 (1977).A comparison or choleslyramine and Ilil::otinic acid in !be tRalmenl of fanulial
type II b~rlipoprolCinaemia. .'\tann, U .etal . Bnti$/)Journal ofamicaJP llannaoology 4, 30'11911).
Interruption of lbc emerohepauc circulation of phcnprocounlOp by<,:ho.lles;tyramine, .'\teinero , T. et at Clinical PharmacologyandTherapeutics 1!: 1J 1(1971).
Doescholesty ramine impair the bioavailabilityof prednisolone~ Audetat. V.et &I .Schwcile rftche .'\tediriDi5lche Wocbcnscbrifl 101, '2111911).
Decn:ased bioavailabililY of digo.unprod~ by dicw'y fibre anddlolesty~DJine. Brown. D.O. et aI. Ametican Journalof CvdioJocy J\l :211 1119111
Ellea or cbolestyn m,ne on digo~in abso~n and ucrWon in maD. Hall.W.H. ellli American JQ<lrnaI orCllrdioiogy 39: 11J (971).
The effector cholc;Lyramin<:(·Queslran'). 8g IWice-dilily. on serum lipcprcteincencemrauens in lype II hyperbpoproleinaemia. Olsson. AG.Pharmalherapeutica I: 583 (1917).
Clwlestyn.mine and ilealby·pass ip the treatment orramilialbypercbo\esle:rolaemia. MietIineIl.. T.A. etal. EuropeanJou mlli ofQinicaiInvestigation1: SMOlin).
Enhanoed elimination of warfarin durina lnatment ....ith chokslyn. mine.Jahncnen, E. et al. Briti5lt JOIUlllliof Oi llJCal PllarmacolocY 5: 4310 9181.
Acu~ eITecl5 of cholestyramim on serum lipoprotein concentrations in typeIV hyperlipoproteinacmia, Olsson. A,G, et al. AtherosclcfOliis 211: SJ·6 1(1918)