keeping down the lipid levels! — a look at the drugs available

2
from our files KEEPING DOWN THE LIPID lEVELS !- A look at the d rugs available COlESTIPOl ('Colestid '. recentl ylaunch ed bV Upjohn) o Ph armacology ColeSlipol hydrochloride, 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 "'-eroid (peN) and a b ile acid sequ esiram (CoICSlipol· HO). HOllOOan. T. er at. Biochemical Pharmacology 24, H99 (I 9151. Effects of candicidin. cotesuoot and triparanol on sserol bic>synlhesis and lipoprotein distribution 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-densit y lipoproteins in ma n, Will lUm, 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 Wanget at. lnvesugauve Urology 14, 66 (19 76) Effectsof role.\.lipol hydrochlor ides and neomycin su lfate on Cholesterol turnover in !he rat. Phillips. W .A, et aL Lipids 12, 10 ( 19 77 ) Preparation hydrochloride and its disposilion in the human, dog and raL Thomas. R.C. et ai, Atherosclerosis 29, 9 (1978) o And c lini ca l tri als Experience wilh a new choje sre rol-lowenng resin. coJestipo t M uts. E. el al Acta Clinica Belg sca 30, 40 9 ( 19 75 ) l..ong-term effects of cojesuoot (v ·26. 597 A)o n plas ma lip ids in famili al type It hype rbeLafi poprute inaemia. Fellin, R. et at Atherosclerosis 22: 43 I il975) Hypo cho les te role m ic acti vity ofrole.'t ipel in diabetes Bandisode. M.s. et aL C u=nt Therape utic Research 18: 276 ( 19751 Cotesnnct. Clofibrate . chotesryrarmne and ccrn bin atjon thcrap y in the treatment of familial hyperbcLatipoproteiruemia Stein, E.A. et aL South Arr ican Medical Journal 49: 1252 (1975) C..olcstipol hyd rochl or ide. a new hypohpidemic drug, a two-year study. Cooper. f .E. et al. Southern Med i<.:al Jo um a l 68 : 303 ( 1.,751 Lo ng-term treatment of hypercholesterolemia with cote.,'ipol hydrochloride. Ryan. J.R, et aL Clinical Pharmaco logy and Therapeutics 17: 83 (19751 Cbolesterot-Icwering e ffect of ro lestipo! bydrochloride given twice daily in hypercholesterolemic patients, Gundersen. 1< . et al, Atherosclerosis 25, J 03 «976) CoI=ipel in familial type II hypc rhpoproteinaernla, A th ree· yea r tr ial. Har vengt. C et al. Clinical Pharmacology and 20: 310 (1976) Results of colCSl.ipoltherapy in type 11 Lees. A.M et at. AUterosclerosis 24: 129 ( 197 6) Clofibrate·induced low dCTI&ity lipop rote in -c- rherapeuuc implications and treatment by resi n. Rose, HG . et at. Atherosclerosis. 23, 4 (3(19761 Pedialr ic fa m ilial type II hype rhpoproICinemia , Therapy with diet and wlest ipol. G lueck. CJ , et at Pediatrics 51, 68 (1976) fllc effect of wlestipol on digitoxin pla:;ma levels. Bever. R,J, et al. Arzneimittel.ForschulJ8 26, 1891 (19761 Long-term lherapy of diet -resistant hypercholesterolemia with cotesupot. Mishkel. M.A. et al. Current The ra peutic Resea rch 22, 398 t 197 7) Colestipol in the treatment of diabctic patien ts with hypercnoleaero jerma. OunlSCh. G Fortschrme der Medi1 .in 9S: 1492 (19171 Cole Slipol, clofibra te. and pl!ytoste rols in oombined ther "py of hyperlipidemia, Gru ndy. S.M. et a l. Jo u rnal of Laboratory and Clinical Mal icine 89, 3S4 (I9 17) treatment of ltypcrcltolcsterolemia for up to 8yr. Ryan. J.R. erat. Cl inical Pharmacology and Theratn:utics 2 1; 116 {191 1) Type II hyperlipeproteinaemia Treatment with colWipel and Sauvanet. J.-P. er at. La Nou ve lle Prcsse Medicale 7: 186 2 (1978) Long·ter m trial with colesupol plus clofibrate in familial hypercholesterolemia. Fellin, R, ee al. Athe rosclerosis 29: 24 1(1978) Co\estipolltydrocb\Ofide for treatment of hy percholesterolemia in a family pr actice Five·y"" r study. Ruo ff, G . Jo urnal of the American Geriatrics Soc 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 Pl1armacology and The rapy. De Sante. K.A , et aL Cl inical and Therape utics 23 : I r2 (19781 PROBUCOL! 'lorelco;' Dow, another new introduct ion) Lon g-term oral ad min istration of probucol (4 .4'-isopropylideneditbiolbisl 2,6· di+d urylphen oIHD H-58I ) in the management of hypercholesterolemia Ha rr is . R -S. e t aI. J<lurnal or tile Ame rican Geriatrics Society 22, 16 1 0 914 ) Saf ety and efficacy of probocol during one ycarof itdministration. J\:ash, DT. Journal of Clinical PlIar maco logy 14: 470 (1974) The addruve effect of probuco! on diel in hype rlipide mia. Brow n, H B. et al. Clinical Pharmacology and Therapeutics 16: 44 (19 74 ) Safety and emcacy or crobocor during one year of administration. N ash , DT . Journal of Clinical Pharmacology 14 ,4 70 (197 41 T reat ment of se vere and mild hypereholcS\erolaemi a with probucol and neomycin. Mietlinen. T.A. er al. Postgraduate Medical Journal 51, 71 (Suppl e M . 1975) Proo ucol. A ne w chclesterollowermg drug. Nash , D .T, Journal of Medicine 6: 305(19 75) Long-term therapy w ith prob uool(D H 58 ! ) in hu ma n sub.it:cts. Canosa . FL el aL Clinical Phar maw logy and Therapeut iCS 17, 230 ( 1'175) Probuco!- cholcsu:rol·lowering dru g effective patients with type- !! hyperh poproleinemia, Said. A,F. er ai, C1 ini<.:al Pharmaco logy an d Therapeu tics 10: 690 ( 1'1761 Probucol. Drugs of the Future IL 12 8 ( 19 77) An ove rvie w of the biochemical phar macology of probuooL Barnhart. J. W. er al. li p ids 12 : 29 ( 19 77 ) Probucor. a new antihypcrlipidemic. Russo, C. Currenl Prescribing 3, 7r ( 19 771 Proburo l f or hyper<:boleste rolemia, Medical Lener 19: 41( 1917) D iet an d pru buool in lo wer ing Cholesterol concemreuons- add itive e/Teets on COl\CCn\l,llions in patie nts with familial type 2 hyperlipuprolelJ\emia, Lclorier. J . CI aI, Arch ives o f In ternal 137: 142 9(19 77) ProbucolIw reieol in treatment or hype rlipemia, Murphy. B F. Journalof tile Ame rican Med ical Assoc iatioo 238, 2 53 7 (1 97 7) Diet and pro bucol in lower ing cecicaerot concent rations. Letc nee. J. CI al. Archive.;of Internal Medicine 137, 1429 (1917) !'robuw ] Drugs o fToday 14 ,33 (19781 EFfect of probucol on ck,fib rale resistanl familial hypercholC'Sterol emia , Le t.orfer. J. et al. A nnals of the Royal Coll ege of Physicians and Surgeons or Can ada I ( 35(1'17M) Combi ned of the Sludy ofprobuool al lmg fday in eight centers, Taylor. H.L. et at. Qini"",1 Pharmacorogy and Therapeutics 23: I J I ( 191 8 1 Prob uOJ1: a review of us pharmacological pro perties and therapeutic use in palie Ols with hyperchuleslerol aemia, Heel. R.C. CI at. Drugs 15: 409 \197M) INPHARMA 17t h June, 19 78 pt 9

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Page 1: KEEPING DOWN THE LIPID LEVELS! — A look at the drugs available

from our files

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

Page 2: KEEPING DOWN THE LIPID LEVELS! — A look at the drugs available

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)