ChFarm 2012 Suport AB Peptid Aminoglicozid Amfenicoli

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    22-Jun-2015

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ANTIBIOTICE GLICOPEPTIDICE VANCOMICINA VANCOMYCIN (DCI)Glicopeptid triciclic cu structur complex; Streptococcus orientalisProduse farmaceuticeVANCOMYCIN HYDROCHLORIDE, VANCOCINVANCO-TEVA, VANMIXAN, VANCOLED EDICIN, LYPHOCIN (flc. pulb sterila inj.)TEICOPLANINActinoplanes teichomyetiusStructur, mec. act., spectrul de activitate antibiotic vancomicinaR.a.: rash cutanat (doze mari); reactii alergice; ototoxicitate sczutTARGOCID flc. inj.ANTIBIOTICE GLICOPEPTIDICEBacillus subtiliscomplex de polipeptide; remarcabil omogenitate a structurii ciclicealb-cenusie; caracter bazic sulfatiNefrotoxicitate accentuatAplicatii locale: conjunctivite, ulcere corneene, piodermite, eczeme, plgi traumatice si chirurgicale infectateANTIBIOTICE CU STRUCTURA POLIPEPTIDICABACITRACINABACITRACINUMForme farmaceutice: unguent, pulbere externa, spray, unguent oftalmicBacitracin + neomicin (negamicin)NEGAMICIN B ungNEOBASEPT pulbBANEOCIN pulbBIVACYN pulb, ung oft, sprayENBECIN ung, spraySANTADERM pulb, ung(OROPIVALONE BACITRACINA compr pt supt (+tixocortol)Acid cis-1,2-epoxipropilfosfonic sare cu trometaminaE. coli, S. aureus, Serratia, Klebsiella, Citrobacter, Enterococcus, Enterobacter spp.; inhibitor al sintezei peretelui bacterianFosfomycin Tromethamine *PF: MONUROL : (P) sare disodic(O) sare de calciu si cu trometaminaANTIBIOTICE AMINOGLICOZIDICEAMINOZIDE, AMINOCICLITOLIStreptomyces sp.Structural:aminooze legate glicozidic de un aglicon aminociclitol; de ex. Streptomicina= streptobiozamina + agliconul streptidinaMecanismactiune antimicrobiana:bactericide prin inhibarea sintezei proteiceSpectru antimicrobian: Enterobacter, E. coli, Klebsiella, Proteus,Ps. aeruginosa, Salmonella, Serratia, ShigellaRezistenta bacterianIndice terapeutic micR adv: ototoxicitate, nefrotoxicitate, reactii alergiceAMINOGLICOZIDE- Clasificareaglicon streptidinic STREPTOMICINESTREPTOMICINADIHIDROSTREPTOMICINAaglicon dezoxistreptaminicNEOMICINE (Negamicine)GENTAMICINEKANAMICINETOBRAMICINE (Brulamicina)PAROMOMICINAAMIKACINANETILMICINAStreptomicina * Aglicon streptidinastreptobiozaminaL-streptozaN-metil-L-glucozaminaAMINOGLICOZIDE cu AGLICON STREPTidiNIC Streptomycinum (dci):streptomycini sulfas (fr X)Streptomyces griseus, S. bikinensisPF: SULFAT DE STREPTOMICINA flac inj (i.m.)STREPANCIL STREVITALDIHIDROSTREPTOMICINADihydrostreptomycini sulfas-CHO -CH2-OHRelatii structura chimica - actiuneAMINOGLICOZIDE cu AGLICON DEZOXISTREPTAMINICNEOMICINE (NEGAMICINE) A, B, C: NEOMYCINI SULFAS (FR X)Streptomyces fradiaeSpectru antimicrobian: streptomicinei (bacil Koch, G-)Activitate antibiotic mai intens n mediu alcalinp.o.: infectii digestive cu germeni sensibili (1-2g/zi)pregtirea interventiilor pe colon (4 g/zi 2-3 zile)Extern: neomicin+ bacitracin + polimixin B sulfat + corticosteroizi(ung, pulb, sol, spray): inf. dermatologice, oculare, ale urechii interneR.a.: frecvent reactii alergice (local); sdr. de malabsorbtie, disbacterioz sau candidoz intestinal (O)P.F.NEGAMICIN- cpNeomicin + bacitracinNEGAMICIN B ungNEOBASEPT - pulbBANEOCIN, BIVACYN, ENBECINNEOBACIN, SANTADERM Neomicin + corticosteroiziNEOPREOL ung (+prednisolon+untur de peste)NIDOFLOR ung (+ nistatin+triamcinolon acetonid)FLUMETAZON PIVALAT N ung, cremFLUOCINOLON N ung, cremLOCACORTEN with NEOMYCINMAXITROL suspensie si ung oftalmice ( + Dexametazona)OPHTAMETASONE N = solutie oculara, otica, nazala(+Betametazona)ANTIBIOPTAL colir (+Cloramfenicol)NEOSPORIN - ung oftalmic ( + polimixin B sulfat + bacitracin zinc)PIMAFUCORT, PANDERM, SEPTOZYLDERMESONE N, SYNALAR N GENTAMICINE GENTAMYCINISULFAS (FR X)i.m./ i.v.: infectii severe sau complicate (pielonefrite, septicemii, endocardite, inf. respiratorii, articulare, cutanate) cu germeni sensibili(Ps. aeruginosa, Enterobacter, Serratia, Proteus, Klebsiella); + beta-lactamine (carbenicilina/ ticarcilin/ benzilpenicilin)topic: arsuri infectate, inf. osoase, oculareCind.: alergie; tratamente de lung durat tulpini rezistenteP.F.Sol.inj.GENTAMYCIN, GENTAMICIN, GENTAMED,GARAMYCIN, GENTOGRAM, GEOMYCINESol/ ung. oftalmiceGENTOSEPT colirGARASONE colir, ottoguttae (+Betametasone)GENTAGEN, GENTICOL, GENTAMYCIN, GENTAMICIN SULPHATE, OPHTAGRAMPrep. dermatologice (ung., crem) + corticosteroiziFLUOCINOLON GDIPROGENTA (betametazon dipropionat)KANAMICINE (A) KANAMYCINI SULFAS (FR X)aplicatii localei.m.: util. restrns n inf. grave; nlocuit de gentamicinO: sterilizarea preoperatorie a intestinuluiCind.: nefropatii; tratamente de lung durat rezistent microbianUNGUENT OFTALMIC CU KANAMICINA 1%KANAMICINA SULFAT H ung oftalmic (+hidrocortizon)UNGUENT OFTALMIC CU KANAMICINA SI HIDROCORTIZONKANAMICINA- flac.inj.KANAMYCIN, KANAMICIN, KANTREX, KANAMYTREXTOBRAMICINA (BRULAMICINA)6-dezoxikanamicina BBRULAMICINNEBCIN pulb sterila injTOBRADEX unguent si suspensie oftalmica (+Dexametazona)TOBREX, TOBRIN DIBEKACINA 3,4 didezoxi Kanamicina BDEBEKACYL,ICACINE solutie injectabilaAMIKACINA :AMIKACINA :AMIKIN, AMIKOZIT, ORLOBINSISOMICINA :SISOLLINE solutie injectabilaNETILMICINA: NETROMYCIN sol.inj.PAROMOMICINAPF: HUMATIN capsule 250 mgHUMACORT ung. (Cloramfenicol+ Paromomicina + Hidrocortizon)Fortimicina A : ASTROMICINE ISEPAMICINAISEPACIN-ISEPALLINE sol.inj.SPECTINOMICINA.SPECTINOMYCIN (DCI)Streptomyces spectabilis; AminociclitolKIRIN flac inj. (doza terap. 2 g Spectinomicin)AMFENICOLI/FENICOLI /ANTIBIOTICE ARILALCHILICECHLORAMPHENICOLUM * (FR X)FR X: 2,2-dicloro-N-[(1R, 2R)-1-hidroxi-2-hidroximetil-1-[(4-nitrofenil)-etil]-acetamida(+) eritro-cloramfenicol si (+) treo-cloramfenicol;D-(-)-treo-cloramfenicol= activitate antibiotica maximaD-(-)-treo-cloramfenicolCHLORAMPHENICOLUM (FR X)Spectru antimicrobian largBacteriostatic: b. aerobe Gram-pozitive si Gram-negative (stafilococi, streptococi; Bacillus anthracis, Clostridii; E coli) anaerobi i.c. (Bacillus fragilis)Chlamydia, MycoplasmaRickettsiiBactericid: Salmonella typhi, S. paratyphi , Haemophilus influenzae,Neisseria meningitidis, Streptococcus pneumoniae, Virusuri mari, spirocheteProduse farmaceutice:CLORAMFENICOL draj. 125 mg, 250 mgCLORAMFENICOL HEMISUCCINAT flac. inj. 1 gBERLICETIN compr. 250 mgSIFICETINA colir 0,4%BETABIOPTAL colir (+Betametazona)ANTIBIOPTAL colir (+Neomicina)SOLUTIE AURICULARA CU CLORAMFENICOL SI FLUOCINOLONTRICOMICON ovule (Cloramfenicol+ Metronidazol + Nistatin)HUMACORT ung. (Cloramfenicol+ Paromomicina + Hidrocortizon)Optimizareaunor proprietati biofarmaceuticeale Cloramfenicolului1. Optimizarea gustului amar Esteri cu acizi grasi la grupa alcoolica primaraPALMITAT DE CLORAMFENICOLR: -CO-(CH2)14-CH3CLORAMFENICOL PALMITAT suspensie oralabiodisponibilitate optima: pulbere amorfa 1-5 mm; cristale aciculare < 10 mmSTEARAT DE CLORAMFENICOLR: -CO-(CH2)16-CH3PALMITOIL GLICOLAT DE CLORAMFENICOL (n=14)STEAROIL GLICOLAT DE CLORAMFENICOL (n=16)R : -CO-CH2-O-CO-(CH2)n-CH3 stabilitatea, conc. serice2. Optimizarea solubilitatii in apa Esteri hidrosolubili cu acizidicarboxiliciAnalogi structurali ai cloramfenicoluluiTHIAMPHENICOLUM NO2 -SO2-CH3THIOPHENICOLenantiomerul D-(-)-treo activ; spectru de activitate identic cu cel al Cloramfenicoluluimai solubil, mai putin toxic decit Cloramfenicolulabsenta R.A. anemie aplasticaintensitatea actiunii < Cloramfenicolul; durata de actiune > Cloramfenicolul(O) 1-1,5 g/zi: infectii cai biliare ; digestive, respiratoriiRelatii structura chimica activitatein seria derivatilor cloramfenicoluluiGruparefunctionalaModularestructuralaConsecinte /Activitate, toxicitate-NO2paraCH3-CO- Cetofenicol A;TCH3-SO2- Tiamfenicol A; durata actiuneAlte grupari(OH, OR, COOH, NH2, NH-R, NR2, CO-NH2, CN, X, Ar, alchil)A/ inactiviAlte pozitii pe nucleularomaticANucleulbenzenicCiclohexil, naftil, ciclopentil, chinolil, furilAGruparefunctionalaModularestructuralaConsecinte /Activitate, toxicitateAr-1CH-OH Ar-1C=O CloramfeniconaantifungicC2-NH-COCHCl2substituire inactivare-CO-CH2-N=N+=NAzidamfenicolHidrosolubilitatea(colir)C2-NH-COCHBr2BromamfenicolACH2-OH esterificare Pro-drug-uri (in vivo, hidroliza enzimatica) CloramfenicolOxidare, reducere, eliminareInactivare

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