CARBAPENEMNOCarbapenemNHOH3COCOOHSNH2Thienamycin (1977)Thienamycin :- trch t moi trng nuoi cay Streptomyces cattleya. - hoat tnh khang khuan rong - hoat tnh tren Pseuomonas - khang !ai "-!actamase #$%$% '% $%IMIPENEMAcid [hydroxy-1 ehy! (R) " #$[[(iminomehy!amino-2) ehy!"hio"-3oxo-7-a%a-1bicyc!o [3&2&'"hepen-2 carboxy!ic-2 ((R)$S)&NHOH3COCOOHSNH2Thienamycin (1977)NHOH3COCOOHSNHNH*mipenemben%y! +ormimida- $han (enem )anhom '**% + '& ca,n thiet cho hoat tnh khang khuan.- '-. /#0 thay )1 '-. /20 + (enici!!in )a ce(ha!os(orin khang en3ym cu+a 45- 6mino-&-thioethy! /cysteamin0 + )7 tr 8 hoat tnh tren Pseuomonas.- N-9ormimioy!(han t+ :e,n )e, ma;t hoa hoc.IMIPENEMNHOH3COCOOHSNHNH(S)IMIPENEMPho khang khuan (ho khang khuan rat rong> :ao go,m:-'a,u khuan gram ng: #ta(hy!ococcus nhay metici!!in /#ta(hy!ococcus khang metici!!in ?e, khang )i imi(enem0> #tre(ococcus /ke ca+ nhom @0> Pneumococcus> Anterococcus.-'a,u khuan gram am: $eisseria-Trc khuan gram ng: '!ostriium> Listeria monocytogenesB- Trc khuan gram am: H. infuenzae> E. coli> 5!e:sie!!a> Proteus mirabilis> Antero:acter> 'itro:acter> #erratia> Proteus vulgaris> Bacteroides fragilis> 6cineto:acter> P. aeruginosae.NHOH3COCOOHSNHNHIMIPENEM- C4 cham. - @eD :7 (han hu+y :+i ehyro(e(tiase + ong than khi s+ ung thng ket h( imi(enem )i ci!astin /chat c che en3ym ehyro(e(tiase0 ?e gii han s chuyen hoa nay.cilastinNHOH3COCOOHSNHNHNHOOCO2HSNHON,eropenemNHOOCO2HSHNNH*mipenem MONOBACTAM$'**%*%*$%2*E& 8Fnocardicin 1$'%8#*8-*$%$$*''**%%8'%8'#$%8$G/#0 /#0Aztreonam Pho khang khuan-63treonam khong co hoat tnh tren )i khuan gram /G0. -%oat tnh tren )i khuan gram am tng ?ng )i ce(ha!os(orin CCC: Antero:acterie H. infuenzae> Pseuomonas Neisseria menigitidisBNHNSNH2NNOOCOOHO SO3HA%reonamNHNSNH2NNOOCOOHO SO3HOCONH2Car.monamNHNSNH2NNOOCOOHO SO3HTi/emonamNHNSNH2NNOOO OCO2NaOximonamCai thien tac !ong tre"n Entero#acteriaceaema$nh tre"n gram a"m % #e&n '(i )*+actama,e(2-carbamoyloxymethyl) 2,2-dimethylHC-A.T /0C C-E. )*1ACTAMA2E 3A4I C/5N6- $hie,u !oai )i khuan co kha+ naIng tiet ra cac en3ym :eta !actamase (han hu+y cac khang sinh ho :eta !actamine. # sa+n sinh cac en3ym nay co the !a t nhien hay tie( nhan ?c.- Jen :eta !actamase :ao go,m (enici!inase )a ce(ha!os(orinase.,ore han 2'' 0-!acama1e1 are c.rren!y 2no3n and /ro.ped ino +o.r c!a11e1) A) 4) C) and 5) ba1ed on heir amino acid 1e6.ence and /enera! caa!yic properie1&Typica!!y c!a11 A0-!acama1e1 exhibi a hi/her aci7iy o3ard1 penici!!in1 han o3ard1 cepha!o1porine& Some o+ he c!a11 A0-!acama1e1 are a!1o aci7e a/ain1 he ne3 /eneraion1 o+ cepha!o1porine1 and carbapenem1&-'hat c che :eta !actamase G cac (enici!!in: m+ rong (ho khang khuan cu+a nh=ng chat nay !en cac )i khuan tiet men (enici!!inase.-#au khi gaKn )i men (enici!!inase> cac chat nay se= :7 (han hu+y.C5 C-E. TA0C 3O7N6 Acid c+a'uc+anic 8,uicide inhi#itor9Thu ?c t Streptomyces clavuligerus'au truc c!a)am /oLa(enam05hong co nhom the + '.M 2/'80 !a N '%-'%&-*%.Oc s+ ung + ang muoi ka!i c!a)uc!anat'ac (hoi h(: aci c!a)uc!anic P amoLici!!in> aci c!a)uc!anic P ticarci!in c+a'u+anate : mero;enem (ang nghin cu)NOCH HHOCH2OHHH COOH-'a+i thien tren nh=ng ma,m nhay ca+m sa+n Luat :eta !actamase nh Neiserria gonor!oeae %aemo(hi!us E. coli #a!mone!!aB.A< c+a'uc+anic : ticarci++inPhoi h( nay gia taIng tac ?ong tren #ta(hy!ococcus "#$% Streptococcus n!a&y ca'm v()ip!o*i !(&p acid clavuclanic + ticarcillin so v()i ,#% ne*u c!- s.' du&ng mo/t m0n! ticarcillin1.Pho khang khuan cua ;ho=i h($; B< c+a'uc+anic : amo>ici++in-@aDn chat cu+a (enam> :an tong h( t . 6P6-'au truc tng t (enici!!in nhng khong co nhom the + '. /mat '-0> - # + )7 tr F ?c oLy hoa thanh #*&> -'au h1nh '& )a 'Q giong (enici!!in2u+#actam(2S,5R)-3,3-Dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptae-2-carboxylic acid 4,4-dioxide Pho=i h($; ,u+#actam*am;ici++inNSH HHOH COOHCH3CH3OO- Oay !a aDn chat cu+a su!:actam )a am(ici!!in- %oat tnh tren ca,u khuan gram ng> gram amM trc khuan gram ng> gram am- Oc ung trong tai-mu+i-hong> ho ha(> sinh uc> aB tren nh=ng ma,m nhay ca+m2u+tamici++inNSCH3CH3OOOONSOH3CH3COOOHNONH2S.!amici!!in- @aDn chat cu+a su!:actam ma mot nhom methy! mang nhom the tria3o!y!- Oay !a chat c che :eta!actamase khong thuan ngh7ch (ho rong- #+ ung i ang (hoi h( ta3o:actam - (i(eraci!!inTazo#actamNSH HHOH COOHCH2CH3OONNN