Suport ChFarm 2015 Aminoglicozide Amfenicoli
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Transcript of Suport ChFarm 2015 Aminoglicozide Amfenicoli
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ANTIBIOTICE AMINOGLICOZIDICEAMINOZIDE, AMINOCICLITOLI
Streptomyces sp.
Structural: aminooze legate glicozidic de un aglicon aminociclitol;
de ex. Streptomicina= streptobiozamina + agliconul streptidina
Mecanism actiune antimicrobiana:
Bactericide prin inhibarea sintezei proteice
Spectru antimicrobian:
bacili Gram-negativ aerobi: Enterobacter, E. coli, Klebsiella, Proteus,
Ps. aeruginosa, Salmonella, Serratia, Shigella
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Streptomicina
Aglicon streptidina
streptobiozamina
L-streptoza
N-metil-L-glucozamina
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Indice terapeutic mic; periodic, dozarea aminoglicozidelor în plasmã
Actiune sinergicã beta-lactamice; glicopeptide
R adv: Ototoxicitate (leziuni cohleare si vestibulare), nefrotoxicitate,
reactii alergice, bloc neuromuscular (apnee)
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AMINOGLICOZIDE - Clasificare
aglicon streptidinic STREPTOMICINE
STREPTOMICINA
DIHIDROSTREPTOMICINA
aglicon dezoxistreptaminic
NEOMICINE (Negamicine)
GENTAMICINE
KANAMICINE
TOBRAMICINE (Brulamicina)
PAROMOMICINA
AMIKACINA
NETILMICINA
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AMINOGLICOZIDE cu AGLICON STREPTidiNIC
Streptomycinum (dci): “streptomycini sulfas” (fr X)
Streptomyces griseus, S. bikinensis
PF: SULFAT DE STREPTOMICINA (Antibiotice) pulb sol inj 1g (i.m.)
STREVITAL (Antibiotice)- pulb sol inj 1 g
DIHIDROSTREPTOMICINA “Dihydrostreptomycini sulfas”
-CHO -CH2-OH
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Streptomicina - IT
• Infectii Mycobacterium tuberculosis
• Infectii non-tuberculoase cu germeni a caror sensibilitate la streptomicina
este dovedita (endocardite, meningite, septicemii etc.)
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AMINOGLICOZIDE cu AGLICON DEZOXISTREPTAMINIC
NEOMICINE (NEGAMICINE)
A, B, C: NEOMYCINI SULFAS (FR X)
Streptomyces fradiae
Spectru antimicrobian: streptomicinei (bacil Koch, G-)
Activitate antibioticã mai intensã în mediu alcalin
p.o.: infectii digestive cu germeni sensibili (1-2g/zi)
pregãtirea interventiilor pe colon (4 g/zi 2-3 zile)
Extern: neomicinã+ bacitracinã + polimixinã B sulfat + corticosteroizi
(ung, pulb, sol, spray): inf. dermatologice, oculare, ale urechii interne
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R.a.: frecvent reactii alergice (local);
sdr. de malabsorbtie, disbacteriozã sau candidozã intestinalã (O)
P.F.
NEGAMICIN- cp
BANEOCIN (Sandoz) – pulb cutanata; ung = Neomicinã (5 mg; 5000 UI)
+ Zn-bacitracinã (5 mg; 250 UI)
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Neomicinã + corticosteroizi
NEOPREOL – ung (+prednisolon+unturã de peste)
NIDOFLOR – ung (+ nistatin+triamcinolon acetonid)
PANDERM ung (nistatin+triamcinolon+gramicidin)
FLUMETAZON PIVALAT N – ung, cremã
FLUOCINOLON N – ung, cremã
LOCACORTEN with NEOMYCIN
MAXITROL – suspensie si ung oftalmice ( + Dexametazona)
OPHTAMETASONE N = solutie oculara, otica, nazala
(+Betametazona)
ANTIBIOPTAL – colir (+Cloramfenicol)
NEOSPORIN - ung oftalmic ( + polimixin B sulfat + bacitracin zinc)
PIMAFUCORT ung, crema (+ hidrocortizon+ natamicina)
DERMESONE N, SYNALAR N
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FRAMICETINA = NEOMICINA B
FRAMYCETIN (DCI)
IT: infectii ORL, dermatologice – germ Gram-negativ;
Forma farm: preparate topice (solutii apoase uz extern, unguente etc)
PF: SOFRAMYCINE, ISOFRAMICOL
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GENTAMICINE GENTAMYCINI SULFAS (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/ ticarcilinã/ benzilpenicilinã)
topic: arsuri infectate, inf. osoase, oculare
Cind.: alergie; tratamente de lungã duratã tulpini rezistente
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P.F.
Sol.inj. 40 mg/ml, fiole 1 ml si 2ml
GENTAMICIN KRKA; LYRAMYCIN
Sol/ ung. oftalmice
GENTAMICIN SULPHATE (Eipico Med) – colir 0.3%
GARASONE – colir, ottoguttae (+Betametasone)
Prep. dermatologice (ung., cremã) + corticosteroizi
FLUOCINOLON G crema (+ fluocinolon acetonid)
DIPROGENTA (betametazon dipropionat)
BELOGENT ung crema (+betametazona)
TRIDERM ung crema (+betametazon + clotrimazol)
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KANAMICINE (A) KANAMYCINI SULFAS (FR X)
aplicatii locale
i.m.: util. restrânsã în inf. grave; înlocuitã de gentamicinã
O: sterilizarea preoperatorie a intestinului
Cind.: nefropatii; tratamente de lungã duratã rezistentã microbianã
KANAMICINA SULFAT UNG OFTALMIC 1%
KANAMICINA SULFAT H – ung oftalmic (+hidrocortizon)
UNGUENT OFTALMIC CU KANAMICINA SI HIDROCORTIZON
PAN KANAMICINE- flac.inj. 1g
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TOBRAMICINA (BRULAMICINA)
Ind.terap.: gentamicinei
BRULAMICIN, NEBCIN – pulb sterila inj )
TOBRADEX – unguent si suspensie oftalmica (+Dexametazona)
TOBREX – SOL OFTALMICA 0.3 %; UNG OFTALMIC 0.3%
TOBROM, TOBISOL – COLIR 0.3%
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DIBEKACINA
PF: DEBEKACYL, ICACINE – solutie injectabila
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AMIKACINA
(P)– sol.inj; 7-10 zile, sub controlul functiei renale si al audiogramei
AMIKOZIT (Zentiva) – sol inj 50 mg/ml; 250 mg/ml fiole 2 ml
BIODACYNA – sol inj 1g/ 4 ml
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SISOMICINA : SISOLLINE – solutie injectabila
↑ A (enterococi) > gentamicinei
NETILMICINA :
NETROMYCINE (Schering Plough) – sol.inj. 100 mg/ml (flac 1.5 ml; 2 ml)
25 mg/ml flac 2 ml
NETTACIN (SIFI Italia) – sol oftalmica 0.3 %, flac unidoza
NETTAVISC – ung oftalmic 3 mg/g
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PAROMOMICINA
PF: HUMATIN – capsule 250 mg
HUMACORT ung. (Cloramfenicol+ Paromomicina + Hidrocortizon)
Fortimicina A : ASTROMICINE Spectru analog Amikacinei ; foarte activa asupra Ps. Aeruginosa
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ISEPAMICINA Bactericid: bacili aerobi Gram-negativ; stafilococ meticilino-sensibil
H. influenzae, Campylobacter, Listeria monocytogenes,
Yersinia, Proteus, E. coli, Salmonella, Shigella
Ind. terap:
R.a., Cind: analoge aminoglicozidelor
ISEPACIN-ISEPALLINE – sol.inj.
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SPECTINOMICINA. SPECTINOMYCIN (DCI)*
Streptomyces spectabilis; Aminociclitol
Spectru antimicrobian:
Bacteriostatic : inhibarea reversibila a sintezei proteice
Neisseria gonorrhoeae
KIRIN flac inj.
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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 maxima
D-(-)-treo-cloramfenicol
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CHLORAMPHENICOLUM (FR X)Spectru antimicrobian
Antibiotic spectru larg; inhiba sinteza proteinelor
Bacteriostatic:
b. aerobe Gram-pozitive si Gram-negative
(stafilococi, streptococi; Bacillus anthracis, Clostridii; E coli)
anaerobi i.c. (Bacillus fragilis)
Chlamydia, Mycoplasma
Rickettsii
Bactericid: Haemophilus influenzae, Neisseria meningitidis,
Streptococcus pneumoniae, Salmonella typhi, S. paratyphi
Virusuri mari, spirochete
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Ind. terap.
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R adverse
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Contraindicatii
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Produse farmaceutice:
CLORAMFENICOL – CAPS 125 mg, 250 mg
CLORAMFENICOL HEMISUCCINAT – flac. inj. 1 g
BERLICETIN – compr. 250 mg
SIFICETINA – colir 0,4%
BETABIOPTAL – colir (+Betametazona)
ANTIBIOPTAL – colir (+Neomicina)
SOLUTIE AURICULARA CU CLORAMFENICOL SI FLUOCINOLON
TRICOMICON ovule (Cloramfenicol+ Metronidazol + Nistatin)
HUMACORT ung. (Cloramfenicol+ Paromomicina + Hidrocortizon)
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Optimizarea unor proprietati biofarmaceutice ale Cloramfenicolului
1. Optimizarea gustului amar Esteri cu acizi grasi la grupa alcoolica primara
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•PALMITAT DE CLORAMFENICOL
R: -CO-(CH2)14-CH3
CLORAMFENICOL PALMITAT suspensie orala
biodisponibilitate optima: pulbere amorfa 1-5 mm;
cristale aciculare < 10 mm
•STEARAT DE CLORAMFENICOL
R: -CO-(CH2)16-CH3
•PALMITOIL GLICOLAT DE CLORAMFENICOL (n=14)
•STEAROIL GLICOLAT DE CLORAMFENICOL (n=16)
R : -CO-CH2-O-CO-(CH2)n-CH3
stabilitatea, conc. serice
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2. Optimizarea solubilitatii in apa Esteri hidrosolubili cu acizi
dicarboxilici
Hemisuccinatul de cloramfenicol si sodiu :
CHLORAMPHENICOLI NATRII SUCCINAS (FR X)
R : -CO- CH2-CH2-COONa
pulbere alba, higroscopica; se solubilizeaza numai in momentul utilizarii;
CLORAMFENICOL HEMISUCCINAT DE SODIU
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Relatii structura chimica – activitate in seria derivatilor cloramfenicolului
Grupare functionala
Modulare structurala
Consecinte /Activitate, toxicitate
-NO2
paraCH3-CO- Cetofenicol A; T
CH3-SO2- Tiamfenicol A; durata actiuneAlte grupari (OH, OR, COOH, NH2, NH-R, NR2, CO-NH2, CN, X, Ar, alchil)
A/ inactivi
Alte pozitii pe nucleul aromatic
A
Nucleul benzenic
Ciclohexil, naftil, ciclopentil, chinolil, furil
A
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Grupare functionala
Modulare structurala
Consecinte /Activitate, toxicitate
Ar-1CH-OH Ar-1C=O Cloramfenicona
antifungic
C2-NH-COCHCl2 substituire inactivare-CO-CH2-N=N+=NAzidamfenicol
Hidrosolubilitatea(colir)
C2-NH-COCHBr2Bromamfenicol
A
CH2-OH esterificare Pro-drug-uri (in vivo, hidroliza enzimatica)
Cloramfenicol
Oxidare, reducere, eliminareAcetilare (rezistenta bacteriana)
Inactivare