Download - Atb
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ANTIBIOTICE SI CHIMIOTERAPICE
Prof. Dr. Rodica Cinca
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“Era antibioticelor” – debut in urma cu 6 decenii – a schimbat viziunea privind “moartea prin infectie”
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Utilizarea irationala si abuziva
numeroase reactii adverse schimbarea ecologiei microbiene
(“germeni de spital”)
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“Prescrierea ATB a devenit pentru Prescrierea ATB a devenit pentru medicii si pacientii zilelor noastre medicii si pacientii zilelor noastre un veritas viciuun veritas viciu”.
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• Automedicatia
• Patologia iatrogena postantibiotica
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“Inflatia” de ATB => “jungla terapeutica” se intalnesc 3 situatii:
• medicul constiincios si bine informat (balanta cost/beneficiu);
• medicul inconstient si putin informat;• medicul neinformat, plafonat.
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Important• prescrierea rationala a ATB;• “cand prescrie ATB medicul zilei de azi
trebuie sa se gandeasca la viitorul medicinei de maine”;
• “sanatatea nu are pret, dar are buget”
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CLASIFICARE:Dupa STRUCTURA CHIMICA: BETALACTAMINE GLICOPEPTIDE AMINOGLICOZIDE POLIPEPTIDE CICLICE MACROLIDE CICLINE LINCOSAMIDE RIFAMPICINEDupă SPECTRUL ANTIMICROBIAN: ATB cu spectru ÎNGUST; ATB cu spectru LARG; ATB cu spectru ULTRALARG.După MECANISMUL DE ACŢIUNE: ATB BACTERICIDE (omoară germenii); ATB BACTERIOSTATICE (împiedică multiplicarea germenilor).După ACŢIUNEA SELECTIVĂ ÎN INFECŢII LOCALIZATE• ATB intestinale (neabsorbabile);• Chimioterapice urinare.
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BETALACTAMINEBETALACTAMINE
N
Legatura amidica,locul de actiune al
betalactamazelor
3 4
2 1
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MECANISM DE ACTIUNE:MECANISM DE ACTIUNE:PERETEBACTERIAN
PBP+TRANSPEPTIDAZE
PBP+ATB
BACTERIE IMEDIATDUPA FORMARE BACTERIE ADULTA
BACTERIE TANARA
PERETEBACTERIAN
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CLASIFICAREA BETALACTAMINELOR
MONOBACTAMI: AZTREONAM
DIBACTAMI: - PENAMI (PENICILINE) - IBL + PENAMI - PENEMI - CARBAPENEMI - CEFEME (CEFALOSPORINE)
- CARBACEFEMETRIBACTAMI: SANFETRINEM
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DIBACTAMIPENAMI (PENICILINE)
1. PENICILINE BIOSINTETICE NATURALEA. BENZILPENICILINA – PENICILINA G f. 400.000 UI
actiune rapida 1.000.000 UI 5.000.000 UI
SA: CG +; CG -; BG +UT: boli provocate de germeni sensibiliFC: doar parenteral → c% plasmatica eficienta → difuzeaza bine
in tesuturi (exceptie LCR, ochi, seroase)RA: alergice → soc anafilacticAdm: i.m. din 6 in 6 ore; i.v. in perfuzieObservatie:! Cu ser fiziologic sau cu H2O distilata
!!! NU cu glucoza sau alte M in siringa
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B. FENOXIMETIPENICILINA – PENICILINA V, OSPEN – cp. 400.000 UI 1.000.000 UI
Asemanatoare Penicilinei G cu actiune mult mai slabaObservatie:- pe stomacul gol cu o ora inainte de masa;- doze duble fata de Penicilina G;- din 6 in 6 ore.
C. PROCAINPENICILINA – EFITARD fl 800.000 UIAsemanatoare Penicilinei G, dar de semidepoziti.m. monodoza
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D. BENZATINPENICILINA - MOLDAMIN, RETARPENBENZATINPENICILINA - MOLDAMIN, RETARPEN fl. 600.000 1.200.000
UIAsemanatoare Penicilinei G, dar de depoziti.m. 1 doza/saptamana – 2 – 3 saptamanai
Observatie:- NU dizolvata in H2O distilata- NU i.v. (pericol de embolie pulmonara)- NU la copii < 3 ani
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2. PENICILINE ANTISTAFILOCOCICE – PENICILINE “M”- METICILINA- OXACILINA- CLOXACILINA- DICLOXACILINA- NAFCILINA
OXACILINA – OXACILIN caps. 0,250; fl. 0,500SA: stafilococi meticilinosensibili producatori de BLUT: - infectii stafilococice ca monoterapie - infectii stafilococice grave (endocardite septice) in
asociere cu un AGFC: pe stomacul gol si parenteral → c% sanguine eficienteAdm: caps, fl.
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3. AMPICILINE: PENICILINE “A”AMPICILINE: PENICILINE “A”- AMPICILINAAMPICILINA- AMOXICILINAAMOXICILINA
AMPICILINA – AMPICILINAAMPICILINA – AMPICILINA caps. 0,250 g fl. 0,250 g; 0,5 gSA: CG +; CG -; BG –UT: boli provocate de acesti germeniFC: oral si parenteral → c% biliara inalta = ATB biliar;
se concentreaza renalAdm: oral din 6 in 6 ore i.m. din 6 in 6 ore i.v. perfuzie
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AMOXICILINA – AMOXICILINAAMOXICILINA – AMOXICILINA caps 0,250 g; 0,5g; fl. 0,250 g
SA: Bd% net superioara Ampicilinei; asemanatoare AmpicilineiUT: idem Ampicilina cu eficacitate mult mai mare
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4. CARBOXIPENICILINELECARBOXIPENICILINELE• CARBENICILINACARBENICILINA• TICARCILINATICARCILINAActive indeosebi pe piocianic
TICARCILINA – TICARCILINATICARCILINA – TICARCILINA fl. 1 g, 3 gSA: piocianic, proteus, enterobacter, seratiaUT: infectii cu germeni sensibiliAdm: i.m., i.v., i.v. perfuzie
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5. UREIDOPENICILINELEUREIDOPENICILINELE• MEZLOCILINAMEZLOCILINA• AZLOCILINAAZLOCILINA• PIPERACILINAPIPERACILINA
PIPERACILINA: PIPERACILPIPERACILINA: PIPERACIL fl. 2 g, 3 g, 4 gSA: piocianic, proteus, enterobacter, seratia, enterocociUT: infectii severe urinare, biliare, osoase, meningialeAdm: i.m., i.v.
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INHIBITORII DE BETALACTAMAZE (IBL)
• ACIDUL CLAVULINIC• SULBACTAM• TAZOBACTAMATB minore, scazute
N
N
O
O
Leg. betalactam
Leg. betalactam ATBATB
minorminor
BACTERIABACTERIA
BLBL
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Principalele prod. comerciale IBL + BETALACTAMINEIBL + BETALACTAMINE
1. ACID CLAVULANIC + AMOXICILINA = ACID CLAVULANIC + AMOXICILINA = AUGMENTIN, AUGMENTIN, AMOXIKLAV AMOXIKLAV susp., caps., fl., la 8 ore
2. ACID CLAVULANIC + TICARCILINA = ACID CLAVULANIC + TICARCILINA = TIMETINTIMETIN fl. (i.m., i.v.) la 6 ore
3. SULBACTAM + AMPICILINA SULBACTAM + AMPICILINA SULTAMICILINASULTAMICILINA == UNASYN UNASYN
susp, caps, fl.(i.m., i.v.) la 8 ore
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PENEMIPENEMIRITIPENEMRITIPENEM fl. si caps
CARBAPENEMICARBAPENEMIIMIPENEMI – CILASTATINA : IMIPENEMI – CILASTATINA : TIENEMTIENEMSA: “ultralarg” – toate bacteriileMA: asemanator – se fixeaza pe PBP2 → efect bactericid rapid si
intensFc: difuzeaza bine in tesuturi, LCR (90%), urinaAdm: i.v., i.v. perfuzie
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CEFEME – CEFALOSPORINECEFEME – CEFALOSPORINE
MA: idem PenicilineSA: difera de la o generatie la alta
GENERATIA IGENERATIA I
CEFACEFAZOLINAZOLINA (KEFAZOL) CEFA (KEFAZOL) CEFAZEDONAZEDONACEFACEFALOTINALOTINA (KEFLIN) (KEFLIN) CEFACEFAPIRINAPIRINASpectru “largit” ca si spectrul Penicilinei G
Oxacilinei Ampicilinei
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GENERATIA IIGENERATIA II
CEFUCEFUROXIMAROXIMA (ZINNAT) (ZINNAT) CEFOCEFOTIAMTIAMCEFACEFAMANDOLMANDOL (MANDOL) (MANDOL) CEFOCEFOTEMTEMSpectru “larg” ca si spectrul Penicilinei G
Oxacilinei Ampicilinei Gentamicinei Metronidazol
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GENERATIA IIIGENERATIA III
CEFOCEFOTAXIMATAXIMA (CLAFORAN) (CLAFORAN) CEFTCEFTAZIDIMAAZIDIMACEFTCEFTRIAXONARIAXONA (ROCEPHIN) (ROCEPHIN) CEFOCEFOPERAZONAPERAZONA
(CEFOBID)(CEFOBID)Spectru “ultralarg” ca si spectrul Penicilinei G
OxacilineiAmpicilineiGentamicineiMetronidazolTicarcilina
GENERATIA IVGENERATIA IV
CEFPIROMACEFPIROMA CEFEPIMACEFEPIMASpectrul “foarte larg” ce include si enterococul
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“CACIULA CIOBANULUI”
G
OP
ACEF gen. I
CEF gen. II
CEF gen. III
BACTEROIDESFRAGILIS
PIOCIANIC
ENTEROCOC
PIOCIANIC
SPECTRUL ANTIBACTERIAN AL CELOR 3 GEN. DE CEF
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CARBACEFEMECARBACEFEMELORACARBEFLORACARBEF
MONOBACTAMIMONOBACTAMIAZTREONAMAZTREONAM – piocianic
TRIBACTAMITRIBACTAMISANFETRINEMSANFETRINEM – spectru “ultralarg” G + si G -, aerobi si anaerobi
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II. AMINOGLICOZIDE (AGZ)II. AMINOGLICOZIDE (AGZ)
SA: BG - aerobi CG +
RA: ototoxicitate nefrotoxicitate !!!Adm: parenterala
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GENERATIA IGENERATIA ISTREPTOMICINASTREPTOMICINA – activa pe BKKANAMICINAKANAMICINANEOMICINANEOMICINASPECTINOMICINASPECTINOMICINA
GENERATIA IIGENERATIA IIGENTAMICINAGENTAMICINATOBRAMICINATOBRAMICINA
GENERATIA IIIGENERATIA IIIAMIKACINAAMIKACINA