2. Inhibiteurs%%de%la%transcriptase%inverse%:!
h0!$!d!:$&.??'+!K!?'+!63&>3+C+!0)6?C3+.*.A)'+!?'+!0)6?C3(.*.A)'+!'(!?'+!030!0)6?C3+.*.A)'+]!
!
2.1 %%%Inhibiteurs%nucléosidiques%(INTI)%:%
2.1.1 Structure%:%
On%a%une%modification%chimique%du%sucre%:!!(3)+!*C>3)%/)!*)!hZ!'0!d\%
=3('!K! 9'03:3/.%!K! >%3*).(! %C6'0(L! *C%./'! *'! ?\$*C0.0'! b! >%3! &C*.6$&'0(! $/'6! .0(%3*)6(.30! *)! ,'%!
"#3+>#$(']!
!
2.1.2 Mecanisme%d’action%:%
Molécules%analogues%de%nucléosides%naturels%:%
! Zidovudine%K!9#[&.*.0'!!
! Didanosine%!!K!8*C0.0'!
! Lamivudine%K!6[(.*.0'!
G?+! /30(! j(%'! >#3+>#3%[?C+!*$0+!?'+!6'??)?'+!.0:'6(C'+!'(!+$.0'+!>$%!)0'!k.0$+'!6'??)?$.%'!'(!
(%$0+:3%&C+!'0!0)6?C3(.*'!triphosphate!b!6'(('!C($>'!'+(!indispensable!B'0(.(C!$6(./'E!
Ils% entrent% en% compétition!B^!?$!:3.+!+)7+(%$(!'(!.0#.7.(')%E!$/'6!?'+!0)6?C3+.*'+!(%.>#3+>#$('+!
0$()%'?+! ! $)! +.('! $6(.:! *'! ?$! (%$0+6%.>($+'! .0/'%+'! '(! bloque% l'élongation!*)!HC03&'!/.%$?!82=!>$%!
.0(CH%$(.30]!
N'!+30(!*'+!.0#.7.(')%+!63&>C(.(.:+%relativement%spécifiques!*'!?$!(%$0+6%.>($+'!.0/'%+'!B'0/.%30!,QQ!
:3.+!;!.0#.7.(')%!/.+Y^Y/.+! *'! ?$! (%$0+6%.>($+'! .0/'%+'! *)! OGZ! A)'! /.+Y^Y/.+! *'! ?l82=! >3?[&C%$+'!
6'??)?$.%']E!
2306!?l$6(./.(C!*'+!6'??)?'+!*'!?l3%H$0.+&'!'+(!>%C+'%/C']!!
!5&>j6#'!*306!?l.0:'6(.30!*'!03)/'??'+!6'??)?'+!&$.+!'+(!sans%effet%sur%le%réservoir!*'!/.%)+!*Cm^!
.0(CH%C+]!!
!
2.1.3 Pharmacocinétique%:%
! "%.06.>$?'&'0(&per&osL!/3.%'!GO!B>3)%!?'+!$663)6#'&'0(+L!(%$0+&.++.30!&$('%03!:3'($?'!^!OGZE!
! R.3*.+>30.7.?.(C!*'!nQYoVW!
I$.+!**.!K!&$)/$.+'!7.3*.+>30.7.?.(C!6$%!.0+($7?'!'0!&.?.')!$6.*'!
5X.+('!:3%&'!H$+(%3@;L!&$.+!$)++.!'0!+3?)(.30!!
630(.'0(!*'+!+'?+!*'!NhdYL!8?M!>3)%!($&>300'%!'(!*.&.0)'%!?$!*CH%$*$(.30!
*C6$?'%!*'!J#!$/'6!?'+!$)(%'+!&C*.6$&'0(+!
!
! 8++'<!>')!?.C+!$)X!>%3(C.0'+!>?$+&$(.A)'+!BVQWE!
! 2.+(%.7)(.30!$++'<!7300'!*$0+!(3)+!?'+!(.++)+!'(!*$0+!?$!RZ5!B+)%(3)(!849E!
!
! (!p!K!
!P!,#! >3)%! 849!!'(! (,DJ!.0(%$6'??)?$.%'!b!dYT#! !VQQYnQQ!&HDm! '0! J! ^! d! >%.+'+! B!cc!
37+'%/$06'!ccE!
b!,JY,o#!>3)%!9'03:3/.%!'(!(,DJ!.0(%$6'??)?$.%'!b!,JYVQ#!!!,!+')?'!>%.+'Dm!
!
! "')!&C($73?.+C+!
! 5?.&.0$(.30!%C0$?'!'0(%'!nQYoQW!+3)+!:3%&'! 030! &C($73?.+C'! B+$):! 849! A).! '+(! &C($73?.+C! >$%!
H?)6)%3630m)H$.+30!!$(('0(.30!.?!>')(![!$/3.%!)0'!63&>C(.(.30!>3++.7?'!$/'6!*\$)(%'+!>%3*).(+E!!
!