Table Of ContentLACINILC  .LOVVSCITUEPAREHT 23,  NO.  6,200l 
 weiveR of  Oxymetholone:  A  17a-Alkylated 
Anabolic-Androgenic   dioretS
Andrew  M.   ,sotulvaP MD,’   revilO  ,ztluF BS,2   wehttaM J.  Monberg,  BS,2 
and   linA  qktooV PharmD2 
‘Northside   ylimaF Medicine,  Chicago,   ,sionillI and   SSECCA2  lacideM Group,   ,dtL
 notgnilrA Heights,   sionillI
 TCARTSBA
Background:   enolohtemyxO  -a5-lyhtem-71-]enelyhtemyxordyh[-2-yxordyh-B71(
 )eno-3-natsordna  si a   detalyklaa71  cinegordna-cilobana  diorets  dna a   citehtnys  -avired
 evit of   .enoretsotset  tI has   neeb  devorppa  yb the   SU  dooF  dna  gurD  noitartsinimdA for 
the   tnemtaert of   saimena  desuac  yb  tneicifed red   llec  .noitcudorp
Objectives:   sihT  weiver  sezirammus the   ,scitenikocamrahp  tnerruc  dna  erutuf  lacinilc
 ,snoitacilppa  dna  esrevda effects  of   .enolohtemyxo  tnaveleR  seiduts were   deifitnedi  gnisu
a  search  of   @ENILDEM  hguorht March  2001,   detnemelppus  yb  ecnerefnoc  stcartsba  dna
 .snoitatneserp
Results:   esuaceB of   sti  cilobana  ,seitreporp  enolohtemyxo has   neeb  deiduts for  the 
 tnemtaert of   detaicossa-VIH  ,gnitsaw  nibmorbtitna  III  ,ycneicifed  cirtaidep growth   -mi
 ,tnemriap  dna  degamad  ,muidracoym  htiw  gniyrav degrees  of   .sseccus  yticixototapeH  si
a   rojam  esrevda effect   detaicossa  htiw the   esu of   ,enolohtemyxo  htiw  citatselohc  ecidnuaj
the   tsom  tnatropmi  citapeh  edis effect.  Less   nommoc  citapeh  edis effects   detaicossa  htiw
the   esu of   cinegordna-cilobana  sdiorets  edulcni  sisoilep  sitapeh  dna  noitamrof of   citapeh
 .sromut  llA  cinegordna-cilobana  sdiorets  nac  esuac  cinegordna  edis effects,   gnidulcni
 ,enca  ,msitusrih  riah  ,ssol  cillahp/larotilc  ,tnemegralne  lacov  ,segnahc  elitcere  eussit  -mits
 ,noitalu  ,aitsamocenyg  ,aehrronema  dna  segnahc  ni  odibil  dna  lauxes  .ycnetop
 :snoisulcnoC  sA  si the  case   htiw  ynam  cinegordna-cilobana  ,sdiorets few   -ikocamrahp
 citen  dna  ytilibarelot  seiduts were   demrofrep  erofeb  s’enolohtemyxo  lavorppa  ni the 
1960s.   tI has   ,devorp  ,revewoh  ot  eb  na  etairporppa  tnemtaert  eciohc for   detceles  stneitap
 htiw  ,aimena  fi  ylluferac  .derotinom
Key  words:   ,enolohtemyxo  cinegordna-cilobana  ,diorets  ,enoretsotset  ,gnitsaw  .aimena
 nilC( Ther:   )108-987:32;1002
 detpeccA for   noitacilbup  hcraM  ,72  .1002
Printed  in  the   .ASU Reproduction  in  whole  or  part   si not  permitted. 
 lKC.91$/10/8192-9410 789
LAClNlLC  ’SCITUEPAREHT
 NOITCUDORTNI  :enoret  yeht  desaercni  negortin  ,noitneter
 detalumits  ,siseioporhtyre and   devorpmi
With   eht  noitalosi  fo  enoretsotset  ni  ’,5391  lateleks  muiclac  .ekatpu  yehT  ,osla  -woh
 srehcraeser  nageb  ot  erolpxe  laitnetop  -pa  ,reve  dessessop  cinegordna  ,stceffe  -ni
 snoitacilp  fo  enoretsotset  ypareht  desab  gnidulc  4.noitaziliriv
 no its   cilobana and   cinegordna  .seitreporp  ehT  lykla-a71  sevitavired  fo  -sotset
 ylraE  seiduts  fo  yllaro  ro  yllaretnerap  enoret  etutitsnoc an   tnatropmi class   fo
 deretsinimda  enoretsotset  erew  -cusnu  cinegordna-cilobana  sdiorets  erugiF(  .)1
 ,lufssec  ni  trap  esuaceb  dipar  citapeh  -ba  noitcudortnI  fo  eht  lykla-a71  tneutitsbus
 noitpros and   noitadarged  aiv  esahp  I  otni  eht  enoretsotset  elucelom  stneverp
 msilobatem  detluser  ni  citueparehtbus  cilobatem  noitavitcani  hguorht  noitadixo
 stnuoma  fo  eht  enomroh  gnihcaer  tegrat  fo  eht  yxordyh-71  puorg  ot  eht  otek-71
tissues.   oT  emocrevo this   ,noitatimil  -set  .puorg  sihT  egnahc  swols  msilobatem  fo
 enoretsot  seugolana  erew  depoleved that   eseht  ,sdnuopmoc  gnisaercni  rieht  -iffe
had   rewols  citapeh  msilobatem and   -orp  ycac  nehw  deretsinimda  3.yllaro
 decud  regnol  cimetsys  .erusopxe  rehtruF  enolohtemyxO  -yh[-2-yxordyh&71(
 snoitacifidom  erew  demia at   gniretla  eht  -mitsordna_a5-lyhtem-71-lenelyhtemyxord
 cinegordna-cilobana  oitar  rof(  devorpmi  )eno-3 is  an   yllaro  evitca  detalykla-a71
 ytilibarelot and   ,)ycaciffe  gnisaercni  ni  cinegordna-cilobana  diorets  tsrif  -ed
 oviv  ,efil-flah and   gnitatilicaf  -artsinimda  debircs  yb  dlogniR  te a1.5   tI has  a   ylluf
 3y*.noit  sihT  krow  detluser  ni  eht  -leved  detarutas  gnir-A  ,erutcurts  hcihw  yam  -er
 tnempo  fo >120   citehtnys  enoretsotset  ecud  eht risk   fo  yticixototapeh  erugiF(
 .seugolana  ehT  stceffe  fo  eseht  -moc  6.)2  ,oslA  enolohtemyxo  stibihxe  rehgih
 sdnuop  erew  ralimis  ot  esoht  fo  -sotset  cilobana  ytivitca and   rewol  cinegordna  -ca
 HO  HO
H   enolohtemyxO H   enolordnaxO
o&;H2’cH2’6cH2cH;c?&_CH3 
 enolordnaN  etaonaceD  I;  lolozonatS
 erugiF 1.   serutcurtS  fo  ylnommoc  desu  cinegordna-cilobana  .sdiorets
790
W.3 
_CH3 
_ 
OH  SchZinzer 
from 
; H 
E 
modified, 
as 
HO 
OH  permission, 
Hydroxylase  Decarboxylase  with 
I 
H  ;I 
Reprinted 
oxymetholone. 
of 
Ketoreductase 
metabolism 
: H 
Hepatic 
2. 
HO.’ 
o~:l_I..=i.--;‘~~o~~~~tase 
Figure
LACINILC  ”SCITUEPAREHT
 ytivit  derapmoc  htiw  ,enoretsotsetlyhtem  ralimis  enoretsotset  si  yletelpmoc  debrosba
 ,enoretsotset  dna  enoretsotset  etanoiporp  nehw  deretsinimda  41.yllaro  ehT  -erutcurts
 7.)elbaT(  ytivitca  pihsnoitaler  dna  lacinilc  -irepxe
 ,yltnerruC  enolohtemyxo  si  devorppa  ecne  htiw  enolohtemyxo  tseggus that   ti  si
 yb the   SU  dooF  dna  gurD  noitartsinimdA  llew  debrosba after   laro  .noitartsinimda
 )ADF( for  the   tnemtaert of   saimena  desuac  nO  gniretne the   ,maertsdoolb  -ohtemyxo
 yb  tneicifed red   llec  .noitcudorp  nI  -da  enol  seogrednu  htob phase   I  dna phase   II
 ,noitid  deriuqca or   latinegnoc  citsalpa  3.msilobatem  hguohtlA  enolohtemyxo  -ni
 ,aimena  ,sisorbifoleym  dna  citsalpopyh teracts   htiw the   emorhcotyc  054P (CYP) 
 saimena  eud  ot the   noitartsinimda of   metsys  ni  ,ortiv  ti  si  ton  dezilobatem  yb
 cixotoleym  sgurd  netfo  dnopser  ot  siht these   .semyzne  5l  stI  noitcaretni  htiw
 8.noitacidem Researchers   osla  evah  -duts CYP2D6,   ,A3PYC  ,2AlPYC or   91C2PYC
 dei  enolohtemyxo  ni the   tnemtaert of   stluser  ni weak   noitibihni  dna  smees  ot  evah
a   yteirav of   ,snoitidnoc  gnidulcni  -VIH  elttil  lacinilc  5i.ecnacifingis  rehtruF  lacinilc
 detaicossa  9,gnitsaw  nibmorhtitna  III  -ifed  seiduts are   deriuqer  ot  elur  tuo  lla  elbissop
 O‘,ycneic growth   tnemriapmi  ni  -lihc  detaler-PYC  gurd  51.snoitcaretni
 21,11,nerd  dna  degamad  muidracoym  ni  ehT  yramirp phase   I  cilobatem  -caer
heart   31.eruliaf  snoit  evlovni  noitadixo at   ,2C  noitcuder at 
 sihT  weiver  sezirammus the   -ocamrahp  ,3C  dna  noitalyxordyh at  C17.16   -xorppA
 ,scitenik  tnerruc  dna  erutuf  lacinilc  -ilppa  yletami 5%  of   enolohtemyxo has   neeb
 ,snoitac  dna  esrevda effects  of   -htemyxo  derevocer  ni  eniru as   setagujnoc of   -ulg
 .enolo  tnaveleR  selcitra were   deifitnedi  cinoruc  71.dica  owT  rojam  detagujnocnu
 gnisu a  search  of   @ENILDEM  hguorht  cidica  setilobatem were   retal  detalosi  ni
March  2001,   detnemelppus  yb  ecnerefnoc  ,eniru  dna 5   ronim  cidica  ,setilobatem 4 
 stcartsba  dna  .snoitatneserp of   meht  lausunu seco   ,sdiorets  evah  neeb
characterized.‘*J9   ehT effects  of  these 
 setilobatem  evah  ton  neeb  ,denimreted  tub
 SCITENIKOCAMRAHP
 yeht are   ylekilnu  ot  eb  detaler  ot  -otapeh
 detimiL  noitamrofni  si  elbaliava  no the   cixot effects   ni  91.snamuh
 citenikocamrahp  eliforp of   .enolohtemyxo  nI  ,snamuh  laner  noitercxe of   negortin
 hguohtlA  ekatpu  seiduts of   enolohtemyxo  gnirud  cilobatem  sisatsoemoh  nac  tciderp
 evah  ton  neeb  ,detcudnoc the   yllarutcurts the   cilobana  ytivitca of   cinegordna-cilobana
 .elbaT  cinegordna-cilobanA  soitar of   ylnommoc  desu  cinegordna-cilobana  sdiorets  ni  -ina
 lam  93v7.sledom
 negordnA  cinegordnA  ytivitcA  cilobanA  ytivitcA
 enolohtemyxO 0.45  3.2 
 enolordnaxO 0.24  3.22 
 enolorlcnaN  etaonaced  14.0-13.0  29.4-92.3
 lolozonatS 0.3   2.3-0.2
Values are relative to methyltestosterone,  testosterone, or testosterone propionate. 
792
A.M. PAVLATOS ET AL. 
 .sdiorets  enolohtemyxO has   neeb  nwohs  .ainepotycobmorht  tnemevorpmI  retfa
 ot  eb  roirepus  ot  enoretsotsetlyhtem  ni  tnemtaert  htiw  enolohtemyxo  derrucco  ni
 smret  fo  negortin  02.noitneter  tneitapretnI all  4   fo  eseht  .stneitap
and   tneitapartni  ytilibairav  ekam  ti  -iffid  ehT  tifeneb  fo  negordna  ypareht was 
 tluc  ot  enimreted a   esnopser-esod  ,evruc  nees  ni 3   stneitap  htiw  deriuqca  citsalpa
 enolohtemyxO has   neeb  nwohs  ot  esaercni  32,aimena  ni  mohw a   tcerid  pihsnoitaler
 yraniru  niteioporhtyre  slevel up   ot  02.dlof-5 was   devresbo  neewteb  enolobtemyxo  esod
and   doolb  llec  .stnuoc  ehT  rebmun  fo  -htyre
 ,setycor  ,slihportuen and   steletalp  deirav
 LACINILC  SESU
 htiw  enolohtemyxo  ,egasod  htiw  eht  -xe
Acquired   dna  latinegnoC Anemia   noitpec  fo  eht  teletalp  tnuoc  ni 1   .tneitap
 ehT  esu  fo  enolohtemyxo  ni 5   nerdlihc
 enolohtemyxO has   neeb  tsom  -roht  htiw  citsalpa  aimena was   debircsed  ni  -na
 ylhguo  deiduts  ni  eht  tnemtaert  fo  citsalpa  rehto  tes  fo  esac  ”.stroper  llA 5   ,nerdlihc
 .aimena  ynaM  fo  eht  stceffe  fo  -htemyxo  gnidulcni 2   ohw  erew  yrotcarfer  ot  -sotset
 ,enolo  ,revewoh  erew  yllanigiro  detroper  enoret  ,tnemtaert had  a   yrotcafsitas  enob
 ni  dehsilbup  esac  seiduts  gnivlovni small   worram and   lacinilc  .esnopser  -htemyxO
 srebmun  fo  ;stneitap  emos  fo  eseht  era  enolo  deraeppa  ot  evah  retaerg  -orhtyre
 dessucsid  ni this   .noitces  esuaceB  fo small   gnitalumits-citeiop  tceffe than   -sotset
 tneitap  ,srebmun  emos  fo  eseht  esac stud-   ,enoret an   noitavresbo that   deerga  htiw
 sei  did  ton  evirra at   yllacitsitats  -ifingis  suoiverp data.25,26 
 tnac  .snoisulcnoc  ,sselehtenoN  yeht  -med  nI a   ,dezimodnar  revossorc  lacinilc  lairt
 etartsno  eht  yteirav  fo uses   fo  -yxo  gnivlovni 143   72,stneitap  enolohtemyxo
 enolohtem that   evah  neeb  .derolpxe was  1   fo 4   cinegordna-cilobana  sdiorets
 noissimeR  fo  ,aimena as   detacidni  yb  desu  ot  taert  aimena  ni  stneitap  gniviecer
 sesaercni  ni  nibolgomeh  ot ~12   ,Ld/g  -ni  .sisylaidomeh  ehT  nem  erew  detaert  htiw
 sesaerc  ni  etycoluciter  ,tnuoc and   -mi  enolordnan  ,etaonaced  ,enoretsemyxoulf
 tnemevorp  ni  srebmun  fo  slihportuen and   ,enolohtemyxo  ro  enoretsotset  ,etahtnane
 ,steletalp has   neeb  detartsnomed  retfa  saerehw  eht  nemow  deviecer all  drugs   -xe
 tnemtaert  htiw  .enolohtemyxo  sesaercnI  tpec  enoretsotset  .etahtnane  nI all,   %71  fo
 ni  enob  worram  ytiralullec  gnirud  -simer  eht  nem  dednopser  ot  tnemtaert  htiw
 nois  evah  neeb  .devresbo  tnenamreP  -er  enolohtemyxo  esaercni(  ni  tircotameh  fo
 ,snoissim as   llew as   snoissimer lasting  up   ,)%58  derapmoc  htiw  %4  fo  nemow  -vah
 ot 5   sraey  retfa  noitassec  fo  ,ypareht  evah  gni  hcus an   .esaercni  laretneraP  -cilobana
 neeb  12.detnemucod  cinegordna  diorets  ypareht was   retteb  -lot
 ehT  esnopser  ot  enolohtemyxo  -nimda  detare than   laro  .ypareht  saerehW  eht  laro
 deretsi  rof  3r  shtnom was   deiduts  ni 45   snoitaraperp  erew  reisae  ot  retsinimda and 
 stneitap  htiw  evitarefilorpopyh  ro  -negera had   rewef  edis  stceffe  ,ge(  ,amotameh
 evitare  22.aimena  stneitaP  htiw  -ullecopyh  ,)niap  yeht  osla  erew  detaicossa  htiw a 
 ral  worram had   eht  tseb  ,esnopser  htiw 13   yltnacifingis  rehgih  ecnedicni  fo  revil  -xot
 laitrap  ro  lluf  snoissimer  ni 18   .sesac A   ytici and   gniziliriv  stceffe  P( <   .)50.0  larO(
 etelpmoc  noissimer was   deton  ylno  ni  snoitaraperp  hcus as   enolohtemyxo  -med
 stneitap  ohw  did  ton  evah  .ainepotycnap  etartsno  rehgih  yticixototapeh than   -rap
 fO 7   stneitap  htiw  ,sisorbifoleym 4  had   laretne  seipareht  esuaceb  rehgih  gurd
793
LACINILC  ’SCITUEPAREHT
 snoitartnecnoc are   detneserp  ot the   revil  ,enol  ,revewoh  did  ton  evorpmi  rehtie the 
 no  tsrif pass.)   ehT  srotagitsevni  dedulcnoc  ytilauq of   esnopser or   mret-trohs  .lavivrus
that   laro  cinegordna-cilobana  sdiorets
 dluohs  eb  devreser for   esu  ni  sisylaid  -ap
Myelojihosis 
 stneit who  are   elbanu  ot  etarelot  laretnerap
 .snoitaraperp  nevelE  stneitap  htiw  decnavda  -ifoleym
 thgie-ytneif  stneitap  htiw  cinorhc  -er  sisorb were   deiduts  ni a   retnecitlum
 yrotcarf  aimena  morf  enob  worram  eruliaf  evitcepsorp  .yduts 3o   noitazilamroN of  the 
were   deiduts  erofeb  dna after   tnemtaert  larehpirep  doolb or   laitnatsbus  -evorpmi
 htiw  .enolohtemyxo 2o   niteioporhtyrE  -xe  tnem  3>( g   )Ld/nibolgomeh was   devresbo
 noiterc was   decnahne  dlof-5>  evoba the  after  9  of  15   sesruoc of   .enolohtemyxo
expected   tircotameh  level  ni 70%  of   -ap  ehT  deen for   doolb  snoisufsnart ceased 
 .stneit  nI 23%  of   ,stneitap red   llec  ssam  yletelpmoc  ni  lla 5   stneitap who  had   -er
was   desaercni  yb  .%02~  ,enolohtemyxO  deriuq  meht  erofeb the   .lairt  nehW  -yxo
 ,revewoh  did  ton  evorpmi the   noitidnoc of   enolohtem  tnemtaert was   decuder or   -ni
 stneitap who   deriuqer  tneuqerf red   llec  ,detpurret 4   stneitap  ,despaler  hguohtla 2 
 .snoisufsnart  ehT  srotagitsevni  -mocer of   meht  dednopser  ot a   dewener  esruoc of 
 dednem that  the   esu of   enolohtemyxo  eb  .enolohtemyxo Based   no these   ,sgnidnif
 devreser for   stneitap  htiw  erom  etaredom  enolohtemyxo  yam  eb of   eulav  ni  -da
degrees  of   enob  worram  eruliaf  dna  -pmys  decnav cases  of   sisorbifoleym  htiw  -ena
 citamot  .aimena  saim  gniriuqer  .noisufsnart
 enolohtemyxO was   deretsinimda for   2~
 shtnom  ot 7   stneitap  htiw  elkcis  llec  -ena
Myelosuppression 
 82.aim  xiS  stneitap showed  a   dlof-5>  -ni
crease   ni  yraniru  ,niteioporhtyre  htiw  na  muihtiL  etanobrac  sulp  enolohtemyxo
 esaercni  ni red   llec  ssam  gnignar  morf was   derapmoc  htiw  muihtil  enola  ni the 
17%   ot 75%   evoba the   lortnoc  .eulav  ehT  tnemtaert of   decudni-yparehtomehc  -oleym
 srohtua  detseggus that   enolohtemyxo  .noisserppus 31   eno-ytneveS  stneitap were 
 thgim  eb  lufesu  ni  detceles  tluda  stneitap  dedulcni  ni the   muihtil  ,puorg 63   ni the 
 htiw  elkcis  llec  esaesid  ni  mohw  ereves  tnemtaert-denibmoc  ,puorg  dna 79   ni the 
 aimena was   gnitubirtnoc  ot the   ytidibrom  lortnoc  .puorg  hguohtlA the   noitidda of 
of  the   .esaesid  enolohtemyxo  did  ton  yllaitnatsbus  nessel
 nI  rehtona  ,yduts 134   stneitap  htiw  -ca  noisserppusoleym  ni  tsom  ,stneitap  ti  -mi
 deriuq  citsalpa  aimena were   dezimodnar  devorp  ’stneitap  etiteppa  dna  ydob  .thgiew
 ot  eviecer  etycohpmylitna  nilubolg  dna  ehT  ytirojam of   stneitap  ni the   muihtil
 enolosinderplyhtem  htiw or   tuohtiw  -yxo  dna  lortnoc  spuorg  tsol  ,thgiew whereas 
 92.enolohtem  ehT  esnopser rate  at  4  those   gniviecer  enolohtemyxo  deniag
 shtnom was   yltnacifingis greater   ni the   thgiew  naidem(  ydob  thgiew  ,niag 1.25   ;gk
 stneitap  gniviecer  enolohtemyxo (57%  P < 0.001). 
[39/69]   sv 40%   ;]56/62[ P < 0.04).  The 
 tnemevorpmi  ni  esnopser rate  was   erom
 detaleR-VIH Wasting 
 decnuonorp  ni  nemow  htiw  wol  lihportuen
 stnuoc  naht  ni  elbarapmoc  nem (78%   sv  hguohtlA  cinegordna-cilobana  sdiorets
 ;%72 P < 0.03).   noitiddA of   -ohtemyxo  evah  neeb  desu for   sraey  ni  gnitsaw  -noc
794
.M.A  SOTALVAP  TE  .LA
 snoitid  hcus as   citorhpen  ,emordnys  nI a   keew-21  tolip  43,yduts 32   -VIH
 cinorhc  revil  ,esaesid and   33923,recnac  rieht  evitisop  nem  deviecer  enolohtemyxo  ni
 esu  ni  VIH  noitcefni is   ylevitaler  .wen  noitidda  ot  gniogno  ralucsumartni  -cejni
 enolohtemyxO was   deretsinimda  enola  snoit  fo  .enoretsotset  ’stneitaP  naem  ydob
and   ni  noitanibmoc  htiw  nefitotek  a( his-   thgiew  desaercni  ylthgils  morf  %001  ot
 ,enimat  tsinogatna  htiw  romut-itna  -orcen  %401  fo  laedi  ydob  .thgiew  reviL  -cnuf
sis   ahpla-rotcaf  )ytivitca  ot  stneitap  htiw  noit  tset  ,stluser  doolb  dipil  ,slevel  VIH
 detaler-VIH wasting   ni an   ,lebal-nepo RNA   ,retit and  CD4+   stnuoc  erew  -inom
 evitcepsorp  9.lairt  ytrihT  stneitap  erew  ,derot and   on  tnacifingis  esrevda  stceffe
 ylmodnar assigned   ot  enolohtemyxo  erew  .devresbo At   pu-wollof  ,stisiv  -ap
 yparehtonom  n( =   )41  ro  enolohtemyxo  stneit  detroper  yltnacifingis less   ,aixerona
plus   nefitotek  n( =   ,)61 and   eht  stluser  ,noisserped and   eugitaf than   erofeb  -taert
 erew  derapmoc  htiw  esoht  ni a   puorg  fo  tnem  P( <   .)50.0
30   detaertnu  slaudividni  ohw  tem  eht  eggneH  te aP5   detcudnoc an   sisylana  fo
 noisulcni  .airetirc  nI  noitidda  ot  ydob  eht  yticixototapeh  fo  enolohtemyxo  ni 30 
 ,thgiew  eht  yksfomaK  elacs  a(  erusaem  fo  stneitap  htiw  decnavda  VIH  esaesid  -nu
 ytilauq  fo  )efil was   desu  ot  rehtruf  -ulave  gniogred  mret-gnol  enolohtemyxo  -taert
 eta  eht  esnopser  ot  .ypareht  .tnem  nI  eht  s’yduts  laitini  ,esahp  hcihw
 ehT  naem gain   ni  ydob  thgiew was  8.2  kg   detsal 30   ,skeew 2   dednilbnon  spuorg  -er
 )%5.41(  ni  eht  enolohtemyxo  puorg  P(  c  deviec  rehtie  enolohtemyxo  enola  ro
 ,)lOO.O 6.1  kg   )%9.01(  ni  eht  -noitanibmoc  enolohtemyxo plus   .nefitotek  retfA  eht
 ypareht  puorg  P( <   ,)500.0 and   8.1- kg   laitini  ,esahp 25   fo  eht  lanigiro 30   stneitap
 thgiew(  )ssol  ni  detaertnu  .slortnoc  ehT  erew  dewollof  ni an   lebal-nepo  .esahp
 naem  emit  ot  kaep  ydob  thgiew was  19.6   ytnewT  stneitap  deunitnoc  tnemtaert  rof
 skeew  htiw  enolohtemyxo  ,yparehtonom  lr  raey at  an   egareva  enolohtemyxo  esod
 derapmoc  htiw 20.8   skeew  htiw  -anibmoc  fo 50   .d/gm  ehT  tsom  nommoc  yrotarobal
 noit  .ypareht  ehT  naem  yksfonraK  ,erocs  ytilamronba  gnirud  eht  laitini  esahp was  a 
 hcihw  serusaem  eht  ytiliba  ot  mrofrep  -ca slight   noitavele  ni  esarefsnartlymatulg-y
 seitivit  fo  yliad  gnivil  no a   elacs  morf  %0  )TGG(  ni  %73  )11(  fo  ;stneitap  retfa  -noc
 )tsewol(  ot  %001  ,)tsehgih(  devorpmi  gnillort  rof  gnidnuofnoc  ,selbairav this 
 yllauqe  ni  htob  ,spuorg  morf  %65  erofeb  detnuoma  ot an   noitavele  fo  TGG  ni  %71
 tnemtaert  ot  %76  retfa 20   skeew  fo  -taert  )5(  fo  detaert-enolohtemyxo  .stneitap  -giS
 tnem  P(  c  .)50.0  sgnidniF  no  rehto  -ytilauq  tnacifin  snoitavele  ni  latot  niburilib  erew
 efil-fo  serusaem  erew  evitisop as   .llew  deton  ni  %01  )3(  fo  .stneitap  enO  tneitap
 ehT  efil-yliad-fo-seitivitca  erocs  devorpmi  depoleved a   revil  romut that   dluoc  evah  neeb
 ni  %86  fo  stneitap  ni  htob  tnemtaert  spuorg  sisoilep  .sitapeh  mureS  nimubla  -artnecnoc
 P( <   ,)50.0  saerehw  noitirtun/etiteppa  snoit  erew  desaercni  ni  %02  )6(  fo  .stneitap
 serocs  devorpmi  yb  %19  ni  htob  spuorg
 P(  c  .)10.0  ehT  srotagitsevni  detroper that 
 enolohtemyxo was   llew  detarelot and   -orp Antithrombin  ZZZD eficiency 
 detom  thgiew gain   ni  citcehcac  stneitap  evah  neeb  lareves  esac  stroper  fo
There 
 htiw  decnavda  VIH  .noitcefni  ehT  -idda  eht  noituloser  fo  ibmorht  ni  stneitap
 noit  fo  nefitotek  did  ton  ecudorp  rehtruf  detaert  htiw  enolohtemyxo  ni  -anibmoc
 thgiew gain.   noit  htiw  tnalugaocitna  O‘.ypareht  oT  eht
795
LACINILC  ”SCITUEPAREHT
 tseb of   ruo  ,egdelwonk there   evah  neeb  on phase,  there  was  a   yllacitsitats  tnacifingis
 seiduts of   enolohtemyxo  tnemtaert for   -na  ecnereffid  ni growth  rate   neewteb the 
 nibmorhtit  III  .ycneicifed  ehT  stluser of   yparehtonom  dna  ypareht-noitanibmoc
the  case  reports,   ,revewoh  yam  tnarraw  spuorg (4.7%   sv  ;%1.8  P c   .)50.0 These  re- 
 rehtruf  .noitagitsevni  stlus  etacidni that   ti  si  elbissop  ot  esaercni
 enob  noitazilarenim  yldipar  ni  -alubmanon
 yrot  citoropoetso  nerdlihc  htiw  tnettimretni
Zmpaired  Growth   ni Children 
 enolohtemyxo  dna  ediroulf  .ypareht
 ehT effects  of   enolohtemyxo  ni  -htworg
retarded,   thgiewrednu  nerdlihc were   -ni
Damaged  Myocardium   ni Heart  Failure 
 detagitsev  ni a   ,dnilb-elbuod  -obecalp
 dellortnoc  .yduts  1  1  evif-ytnewT  nerdlihc  A  llams  yduts reported  the  effects  of 
were   dezimodnar  ot  enolohtemyxo  dna 29   enolohtemyxo  no the   laudiser  -oym
 ot  .obecalp  retfA 12   shtnom of   ,tnemtaert  muidrac of  the   detalid  gniliaf  Itraeh
a   yllacitsitats  tnacifingis  ecnereffid  ni  evlewT  stneitap  deviecer  enolohtemyxo
 naem  thgieh  esaercni was   devresbo  ni the  for  3   .shtnom  segnahC  ni  tfel  ralucirtnev
 enolohtemyxo  puorg  derapmoc  htiw the  (LV)   ecnamrofrep were   detaulave  desab
 obecalp  puorg (8.2   sv 5.6   ;mc  P <   .)20.0  no  yhpargoidracohce  dna  amsalp  -necnoc
 ,ylralimiS a   yllacitsitats  tnacifingis  -reffid  snoitart of   1airta  citeruirtan  editpep  )PNA(
 ecne  ni  ydob  thgiew  niag was   deton  -eb  dna  niarb  citeruirtan  editpep (BNP). 
 neewt the   enolohtemyxo  puorg  derapmoc  stnemevorpmI  ni LV   snoisnemid  tuohtiw
 htiw the   obecalp  puorg (2.81   sv 1.75   ;gk  cilotsaid  noitcnufsyd were   .devresbo  -nU
 P <  0.01).   erehT were   on  tnacifingis  -eb  ,yldetcepxe LV   ssam decreased   htiw
 puorg-neewt  secnereffid  ni  enob age   -fe  .enolohtemyxo  nI  ,noitidda  tnacifingis  -er
fects.   nI  siht  ,yduts  wol doses   92.0-11.0(  snoitcud  ni  naem  amsalp  PNA  82-(
 )d/gk/gm of   enolohtemyxo  decudorp a   )Lm/gp  dna  PNB  25-(  )Lm/gp were   nees
 thgils  tub  tnacifingis  esaercni  ni growth   ni  P( c  0.001).   ehT  snoitcuder  ni LV   ssam
 ezisrednu  nerdlihc  tuohtiw  gnisuac a   -gis  dna  amsalp  PNB  slevel  detcelfer  -cuder
 tnacifin  esaercni  ni  lateleks age   susrev  noit  ni LV   niarts  dna  tnemevorpmi  ni LV 
 thgieh age.   laidracoym  .noitcnuf  ehT effects  of   -yxo
 ehT effect   no  enob growth  of   -yxo  enolohtem were   ralimis  ni  stneitap  htiw
 enolohtem  htiw  dna  tuohtiw  ediroulf was   yhtapoymoidrac  dna  emulov  ,daolrevo
 deiduts  ni  yrotalubmanon  citoropoetso  gnitseggus the   ytilibacilppa of   -yxo
 *‘.nerdlihc  ytnewT  stneitap  deviecer  -moc  enolohtem  ot  htob  seirogetac of   .stneitap
 noitanib  ypareht  htiw  enolohtemyxo  dna
 ,ediroulf  dna 20   deviecer  enolohtemyxo ADVERSE  EFFECTS 
 .yparehtonom  retfA 18   ,shtnom the   naem
rate  of   enob growth   denimreted(  yb  -oidar Hepatotoxicity 
 cihparg  gnilacs of  the   gnol  sixa of  the   SO
 )siclac  htiw the   noitanibmoc  ypareht was   yticixototapeH  si a   suoires  esrevda
8.7%,  whereas   enolohtemyxo  -rehtonom effect   detaicossa  htiw the   esu of   -a71
 ypa  desaercni the  rate  of   enob growth   yb  detalykla  cinegordna-cilobana  .sdiorets
7.0%.   sihT  ecnereffid was   ton  yllacitsitats  citatselohC  ecidnuaj  si the   rojam  citapeh
 .tnacifingis  gniruD a   htnom-21  pu-wollof  edis effect   dna  si  htob dose   dna  noitarud  -ed
796
A.M. PAVLATOS ET AL. 
 .tnednep  A  llams  rebmun of  case  reports   htiw  noitalyklaa71  gnidulcni(  -ohtemyxo
 evah  neeb  dehsilbup  gnitnemucod the   -co  )enol  evah  neeb  nwohs  ot  ecudorp  -fingis
 ecnerruc of   citatselohc  ecidnuaj  ni  -ap  tnaci  sesaercni  ni  amsalp  negonimsalp
 stneit treated   htiw  73T63.enolohtemyxo factor,   gnidael  ot  citylonirbif  34.ytivitca
 lanoitcnuF  revil  eruliaf  dna  citapeh  -orcen Based   no 1  case   ““,troper the   esu of   -yxo
 sis  evah  ton  neeb  devresbo  htiw  -a71  enolohtem  htiw  stnalugaocitna  yam  ton
 detalykla  cinegordna-cilobana  sdiorets  eb  yletulosba  ,detacidniartnoc  tub  rieht
 nehw a   elgnis  tnega was   ,desu  hguohtla  esu  seriuqer  luferac  gnitset  htiw  llams
 ADF  gnilebal  snoitaluger  eriuqer a   ssalc doses  of   tnalugaocitna  ot  enimreted the 
 tnemetats  tuoba these   .sksir  nI  ,noitidda  mumixam  detarelot dose  of   enolohtemyxo
 laro  snoitaraperp  hcus as   enolohtemyxo  ni  laudividni  .stneitap
 evah  rehgih  yticixototapeh  naht  laretnerap
 cinegordna-cilobana  ,sdiorets  esuaceb
 aimedipilrepyH
 rehgih  gurd  snoitartnecnoc are   detneserp
 ot the   revil  no  tsrif pass.   elbisreveR  aimedipilrepyh has   neeb  -er
 sisoileP  ,sitapeh  na  lausunu  citsyc  noisel ported  after  5   2/l weeks  of   enolohtemyxo
of  the   ,revil  si a  rare   edis effect   detaicossa  ypareht  ni a   tneitap  gniviecer  mret-gnol
 htiw  enolohtemyxo  93v83.esu  ehT  ecnerrucco  54.sisylaidomeh
of   sisoilep  sitapeh  si of  greater   lacinilc  -noc
 nrec after   noitaunitnocsid of   tnemtaert  naht
 nommoC Side  Effects  of 
 .erofeb  sisoileP  sitapeh  si a   gninetaerht-efil
Anabolic-Androgenic  Steroids 
 esrevda  ;tneve for   siht  ,nosaer the   ADF  -nam
dates   noisulcni of   etairporppa  sgninraw  ni  llA  cinegordna-cilobana  sdiorets  yam
the   gnibircserp  noitamrofni for   lla  -cilobana  esuac  cinegordna  edis effects   hcus as   ,enca
 cinegordna  .sdiorets  ,msitusrih  riah  ,ssol  cillahp/larotilc  -ne
 ngineB  dna  tnangilam  citapeh  romut  ,tnemegral  lacov  ,segnahc  elitcere  eussit
 noitamrof has   neeb  detaicossa  htiw the   ,ytilibalumits  ,aitsamocenyg  ,aehrronema
 esu of   detalyklaa71  cinegordna-cilobana  dna  segnahc  ni  odibil  dna  lauxes  .ycnetop
 .sdiorets  ehT  ecnedicni of   -enegiromut  nI  ,noitidda  cinegordna-cilobana  sdiorets
 sis appears   ot  esaercni  htiw the   noitarud  yam  erefretni  htiw  serusaem of   dioryht
 dna  tnetxe of   .erusopxe  romuT  noisserger  noitcnuf  dna  riapmi  etardyhobrac  -batem
has   derrucco after   noitassec of   -cilobana  .msilo  yehT  yam  etarelecca  enob  -arutam
 cinegordna  diorets  14,04.ypareht  ,noit  gnitluser  ni growth   .tnemriapmi  -lA
 snaicisyhP  gnibircserp  -ordna-cilobana  hguoht  ynam of  these   edis effects  are 
 eineg  sdiorets  dluohs  eb  trela  ot  -pmys  elbisrever  no  gurd  ,noitaunitnocsid  -rec
 smot of   yticixototapeh  htiw  mret-gnol  esu  niat effects,   hcus as  growth   ,tnemriapmi
 dna  rotinom  revil  noitcnuf  24.yllacidoirep  ,msitusrih  dna  larotilc or   cillahp  -egralne
 ,tnem  yam  eb  8.elbisreverri
Decreased   tnalugaocitnA Tolerance 
 EGASOD
 noisserppuS of   gnittolc factors   ,II V, 
 ,IIV  dna X   yb  cinegordna-cilobana  sdiorets  enolohtemyxO  si  detacidni for  the   -taert
 si a   nwonk-llew  dna  yllacinilc  tnacifingis  tnem of   saimena  desuac  yb  tneicifed red 
 edis effect.   cinegordna-cilobanA  sdiorets  llec  ,noitcudorp  gnidulcni  deriuqca  -salpa
797
LACINILC  ”SCITUEPAREHT
 cit  ,aimena  latinegnoc  citsalpa  ,aimena  lanoitiddA  lacinilc  snoitacilppa of   -yxo
 ,sisorbifoleym  dna the   citsalpopyh  -ena  enolohtem are   yltnerruc  gnieb  ,detagitsevni
 saim  detaicossa  htiw  noitartsinimda of   dna research   seunitnoc  ni those  areas   ni
 cixotoleym  .sgurd  ehT  dednemmocer  hcihw the   gurd has   nwohs  .esimorp  ehT
 yliad dose  of   enolohtemyxo  si 1   ot 5   elbissop  tifeneb  ni  stneitap  htiw  -VIH
 gk/gm  ydob  thgiew per   yad  ni  nerdlihc  detaicossa  gnitsaw  si  gnieb  rehtruf  -ulave
 dna  stluda  htiw  saimena  desuac  yb  -ifed ated.   cilobanA  diorets  ypareht  yam  -ilicaf
 tneic red   llec  .noitcudorp  ehT  lausu  -ceffe tate   enob growth   dna  laidracoym  .riaper
 evit dose   si 1   ot 2   gk/gm per   ,yad  tub  ,revewoH  erutuf  lacinilc  snoitacilppa of 
 rehgih doses   yam  eb  ,deriuqer  dna the   enolohtemyxo  lliw  dneped  no  hguoroht
dose   dluohs  eb  .dezilaudividni  ehT  -er  noitaulave of   sti  ytilibarelot  dna  ycaciffe
 esnops  yam  ton  eb  ,etaidemmi  dna  ypareht  dna  tnemssessa of   sti  sksir  susrev  .stifeneb
 dluohs  eb  nevig a   muminim  lairt of  3   ot 6   enolohtemyxO  si  etairporppa  ni  ynam
 .shtnom  retfA  ,noissimer  emos  stneitap  stneitap  htiw  saimena  detaicossa  htiw red 
 yam  eriuqer  on  rehtruf  enolohtemyxo  llec  ,ycneicifed  dna  ti  yam  eb  na  noitpo
 ,ypareht whereas  others   yam  eriuqer a   -er for  the   tnemtaert of  other   .snoitidnoc  -lA
 decud  ecnanetniam dose.   A  ecnanetniam  hguoht other   ,stnega  hcus as   -ioporhtyre
dose   si  yllausu  deriuqer  ni  stneitap  htiw  ,nite  yam  eb preferred  for  the   tnemtaert of 
 latinegnoc  citsalpa  *.aimena  ,aimena  enolohtemyxo  yam  eb  lufesu  ni
 niatrec  tneitap  ,snoitalupop  ylralucitrap
those  who  are   elbanu  ot  etarelot  dradnats
 SNOISULCNOC
 .seipareht
 enolohtemyxO  si  na  yllaro  evitca  -cilobana
 cinegordna  diorets that  has   neeb  deiduts
 TNEMGDELWONKCA
 yllacinilc  ni  suoirav  sesaesid  ecnis the 
1960s.   sA  si the  case   htiw  ynam  -cilobana  sihT paper  was   detroppus  yb  na  -acude
 cinegordna  ,sdiorets  hcum of  the  data   lanoit  tnarg  morf  deminU  -ituecamrahP
 no  enolohtemyxo was   dehsilbup  ni the   ,slac  ,cnI  ,dleifreeD  .sionillI
1960s   dna few   citenikocamrahp  dna  -relot
 ytiliba  seiduts were   demrofrep  erofeb the 
 SECNEREFER
 s’gurd  lavorppa  yb the   .ADF  nI  ,noitidda
 ynam  snoitacilbup  evah  neeb case  reports   divaD  ,K  esnamegniD E,   duerF J,   rueuqaL
 ni  llams  srebmun of   ,stneitap  hcihw  -erp E.   rebii  senillatsirk  sehcilnnam  nomroh
 dedulc  tnemniatta of   yllacitsitats  tnacifingis aus   nedoh  ,)noretsotset(  remaskriw  sla aus 
 nrah  redo  niretselohc  setetiereb  -sordna
 .stluser  larO  cinegordna-cilobana  diorets
 .noret Hoppe  Seylers   Z Physiol  Chem. 
 snoitaraperp  hcus as   enolohtemyxo  evah
1935;233:281-282. 
 detartsnomed  rehgih  yticixototapeh  naht
 laretnerap  ,snoitaraperp  esuaceb  rehgih
 gurd  snoitartnecnoc are   detneserp  ot the   idihahS NT.   cilobanA  cinegordna  -roh
 revil  no  tsrif pass.   ruO  weiver of  the   -aretil  .senom Am   I. Med.  1977;62:546-548. 
 ,erut  ,revewoh  stseggus that   enolohtemyxo
 yam  eb  na  etairporppa  ypareht  ni  niatrec  rezniihcS  .W  msilobateM  fo  cilobana  -na
 stneitap who  are   ylluferac  detceles  dna  cinegord  .sdiorets  nilC  .mehC 1996;42: 
 .derotinom 1001-1020. 
798
Description:Results: Because of its anabolic properties, oxymetholone has been studied for    Key words: oxymetholone, anabolic-androgenic .. New York McGraw-Hill;.