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CONTINUARE ANTIBIOTICECONTINUARE ANTIBIOTICE
Prof. Dr. Rodica Cinca
III. MACROLIDEIII. MACROLIDE
CARACTERISTICI COMUNE:
• INEL LACTONIC
• SPECTRU ANTIMICROBIAN LARG
• DIFUZIE TISULARA BUNA (utile in infectii cu germeni
intracelulari: chlamidia, mycoplasma, legionella)
• TOXICITATE ↓, TOLERANTA ↑
• COMPLIANTA TERAPEUTICA BUNA – MAI ALES “NOILE
MACROLIDE”
CLASIFICARE:
1. MACROLIDE ADEVĂRATE
• INEL LACTONIC CU 14 ATOMI
- COMPUŞI NATURALI: - ERITROMICINA
- OLEANDOMICINA
- COMPUŞI SEMISINTETICI: - ROXITROMICINA
- CLARITROMICINA
- DIRITROMICINA
• INEL LACTONIC CU 15 ATOMI
- AZITROMICINA
• INEL LACTONIC CU 16 ATOMI
- COMPUŞI NATURALI - JOSAMICINA
- SPIRAMICINA
- COMPUŞI SEMISINTETICI: - ROKITAMICINA
• INEL LACTONIC CU 17 ATOMI
- COMPUŞI SEMISINTETICI: - LANKACIDINA
2. SINERGISTINE
- PRISTINAMICINA
- VIRGINAMICINA
• Macrolide "vechi": - ERITROMICINA
- OLEANDOMICINA
- JOSAMICINA
- SPIRAMICINA
• Macrolide "noi": - ROXITROMICINA
- CLARITROMICINA
- DIRITROMICINA
- AZITROMICINA
- ROKITAMICINA
• ERITROMICINA
MA: inhiba sinteza ribozomiala a proteinelor
bacteriene prin fixarea pe subunitatea 50 S
ribozomială => bacteriostatic la doze ↓;
bactericid la doze ↑.
Obs.: NU se asociază cu Cloramfenicolul pentru
că au acelaşi loc de acţiune.
SA: CG+; CG-; BG+; Actinomicete, Mycoplasma,
Chlamidia, Ricketzia.
Obs.: ERITROMICINA ESTE ATB DE
ÎNLOCUIRE LA BOLNAVII CU ALERGIE LA
PENICILINE !!!
FC: adm. orală → abs. duodenala.
Distributie buna în ţesuturi
(cu excepţia LCR).
UT: boli cu germeni sensibili:
angine streptococice
pneumonie interstiţială cu Mycoplasme,
Legionella, Chlamidii,
profilaxia RAA
sifilis
erizipel
boli sexuale cu chlamidii (cervicite, uretrite).
Adm.: - oral la 6 ore
MACROLIDE “NOI”
• Bd% crescuta fata de macrolidele vechi
• SA: “larg” – asemanator macrolidelor “vechi” +
Toxoplasmoza gondi, H.Py., C. Jejuni,
Mycobacterium avium (SIDA); BG –
(Salmonela, Shigella, Jersinia)
• Complianta terapeutica buna (1-2 prize/zi)
• RA: - rare
• FA: - adm. orala → distributie buna in tesuturi
si celule; se c% in pulmon; renal → efect
postantibiotic (72 ore)
• UT: infectii cu germeni sensibili
• Adm.:
ROXITROMICINA – Rulid cp.
CLARITROMICINA – Klacid cp.; fl.; sirop
AZITROMICINA – Zitaromax cp.
SPIRAMICINA – Rovamycine cp; fl.; sirop
IV. LINCOSAMIDEIV. LINCOSAMIDE
- LINCOMICINA
- CLINDAMICINA
LINCOMICINA
SA: streptococi; stafilococi; anaerobi
(Bacterioides fragilis)
UT: infectii osteoarticulare cu stafilococ; profilaxia
endocarditei infectioase
Administrare: oral si parenteral (i.m., i.v. perfuzie)
CLINDAMICINA
SA: ! bacteroides fragilis
V. GLICOPEPTIDEV. GLICOPEPTIDE
- VANCOMICINA
- TEICOPLANINA
VANCOMICINA – VANCOCINE fl.
MA: - inhiba sinteza peretelui bacterian
- afecteaza permeabilitatea membranei
citoplasmatice
- afecteaza sinteza ARN bacterian
SA: CG + (streptococi, stafilococi); BG +
UT: “ATB de rezerva” pentru:
- infectii stafilococice severe
- colita pseudomembranoasa cu Clostridium
- peritonita stafilococica
RA: ototoxicitate; nefrotoxicitate
Adm.: i.v.
TEICOPLANINA – TARGOCID
asemanator Vancomicinei
SA: CG+ (streptococo,stafilococ)
BG+
Uneori mai activ de 2 - 3 ori decat Vancomicina
VI. POLIPEPTIDE CICLICEVI. POLIPEPTIDE CICLICE
- COLIMICINA
- POLIMIXINA
SA: active pe CG- si BG-
VII. ATB CU SPECTRU LARGVII. ATB CU SPECTRU LARG
- TETRACICLINE
- CLORAMFENICOL
TETRACICLINELE
Tetracicline “vechi”
- TETRACICLINA
- CLORTETRACICLINA
- OXITETRACICLINA
Tetracicline “noi”
- DOXICICLINA
- MINOCICLINA
TETRACICLINA
(Tetraciclina caps)
DOXICICLINA
(Vibramicin caps; fl)
• abs. influentata de alimentatie
• c% biliara modesta
• NU patrunde in LCR
• complianta terapeutica ↓
(T1/2 6 ore)
• abs. neinfluentata de
alimentatie
• c% biliara buna
• patrunde modest in LCR
• complianta terapeutica buna
(T1/2 = 18 – 20 ore)
MA: impiedica sinteza proteica si replicarea bacteriana
SA: Gonococ; Brucella; Yersinia; V. holeric; Chlamidia;
Treponema; Richettzia;
M. pneumonie; Leptospira, Borellia
RA: dismicrobisme: candidoze, tulburari dentare si
osoase
Adm.: Tetraciclina caps 0,250 g oral la 6 ore
Doxiciclina caps 0,100 g oral monodoza (DA + DI)
fl. i.v.
CLORAMFENICOLI
- CLORAMFENICOL
- TIAMFENICOL
CLORAMFENICOL
FC: absorbtie intestinala 80-90%, difuzie buna in
tesuturi si organe (LCR) metabolizare hepatica
(inutilizabil in insuf. hepato-biliare)
MA: idem Macrolide
SA: CG-: H.I.; Salmonella; Shigella
CG+: streptococ, stafilococ, pneumococ
BG+: b. difteric
anaerobi: Richettzi, Clamidia, Mycoplasma
UT:
“ATB de rezerva”
• febra tifoida si paratifoida A ↔(alternativa la trat. cu
Ceftriaxona si Ciprofloxacina)
• Meningita cu pneumococ sau bacili Gram negativi ↔
(scheme de tratament)
• encefalite, abcese cerebrale cu anaerobi
• infectii genito-urinare si abdominale cu anaerobi
RA: Toxicitate hematopoetica (inhibitia
hematopoetica sau aplazie medulara ireversibila)
• “sindromul cenuisiu” al n-n prin deficit de
glucuronoconjugaza, hepatica;
• dismicrobisme: suprainfectii cu Candida
CHINOLONECHINOLONE
GENERATIA I
• ACID NALIDIXIC
GENERATIA II
• ACID OXALINIC CINOXACINA
• ACID PIPEMIDIC ROXACINA
! GENERATIA III - FLUOROCHINOLONELE
• NORFLOXACINA (NOLICIN) DIFLOXACINA
• ENOXACINA (ENOXOR) LOMEXACINA
• OFLOXACINA (TARIVID) FLEROXACINA
• PEFLOXACINA (PEFLOX) TEMAFLOXACINA
• CIPROFLOXACINA (CIPRINOL)
• Absorbtie orala 50-95% → Bd % mare
• Complianta terapeutica buna (T1/2) = 11 ore)
• Vd mare → cp mari in LCR, plamani, oase, bila,,
prostata
• SA “ultralarg”
MA:
(necesara in spiralarea cromozomului bacteria plesneste ca o
de AND bacterian) “fasole coapta”
ADN
BACTERIE
CHINOLONELE BLOCHEAZA
AND-GIRAZA
S.A.: ultralarg:CG+; CG-; BG- aerobi si anaerobi
Mycoplasma, Chlamydia, Rickettsia
UT: infectii urinare joase; infectii de prostatita
(prostatitele acute si cronice); infectii cu
transmitere sexuala (uretrite acute, cervicite
acute, rectite acute, faringite acute gonococi);
infectii gastrointestinale; infectii osteoarticulare;
osteomielite acute si cronice cu BG-; infectii
respiratorii: bronsite cronice (ciprofloxacina)
Adm.: orala 2 prize; 1 priza
i.v. perfuzie
SULFAMIDE
Cu actiune generala
- Sulfodiazina
- Sulfametazina
Cu actiune urinara
- Sulfametin
- Sulfametoxazol
Cu actiune intestinala
- Salazopirin
Cu actiune antileproasa
- Sulfone
Cu actiune antimalarica
- Fansidar
Cotrimoxazol = Biseptol; Bactrim; Septrim;
Eusaprim
(Sulfametoxazol + Trimetoprim)
FC.: conc. in plamani, prostata, rinichi
SA.: BG-;Pneumocistis carini, Toxoplasma gondi,
Nocardia
UT.: - infectii urinare
- infectii genitale
- infectii digestive
- Pneumocistoza
NITROFURANII
• Cu actiune intestinala
Furazolidon
• Cu actiune urinara
Nitrofurantoin
NITROIMIDAZOLII
Metronidazolul (Flagyl)
SA.:
- tricomonas, giardia lamblia, entamoeba histolytica
(antiparazitar)
- anaerobi: G +: clostridium perfringes si difficile;
gardnerella vaginalis
G -: bacteroides fragilis, fusobacterium,
veilonella
UT.: boli parazitare; infectii cu anaerobi (colono-rectale,
gineco-obstetricale)
Pr.: Metronidazol – Flagyl comp. orale, vaginale; fiole
Ornidazol – Tiberal comp.; fiole
Tinidazol – Fasigyn comp.; suspensie orala; fiole.
Macrolide

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Macrolide

  • 2.
  • 3. III. MACROLIDEIII. MACROLIDE CARACTERISTICI COMUNE: • INEL LACTONIC • SPECTRU ANTIMICROBIAN LARG • DIFUZIE TISULARA BUNA (utile in infectii cu germeni intracelulari: chlamidia, mycoplasma, legionella) • TOXICITATE ↓, TOLERANTA ↑ • COMPLIANTA TERAPEUTICA BUNA – MAI ALES “NOILE MACROLIDE”
  • 4. CLASIFICARE: 1. MACROLIDE ADEVĂRATE • INEL LACTONIC CU 14 ATOMI - COMPUŞI NATURALI: - ERITROMICINA - OLEANDOMICINA - COMPUŞI SEMISINTETICI: - ROXITROMICINA - CLARITROMICINA - DIRITROMICINA • INEL LACTONIC CU 15 ATOMI - AZITROMICINA • INEL LACTONIC CU 16 ATOMI - COMPUŞI NATURALI - JOSAMICINA - SPIRAMICINA - COMPUŞI SEMISINTETICI: - ROKITAMICINA • INEL LACTONIC CU 17 ATOMI - COMPUŞI SEMISINTETICI: - LANKACIDINA 2. SINERGISTINE - PRISTINAMICINA - VIRGINAMICINA
  • 5. • Macrolide "vechi": - ERITROMICINA - OLEANDOMICINA - JOSAMICINA - SPIRAMICINA • Macrolide "noi": - ROXITROMICINA - CLARITROMICINA - DIRITROMICINA - AZITROMICINA - ROKITAMICINA
  • 6. • ERITROMICINA MA: inhiba sinteza ribozomiala a proteinelor bacteriene prin fixarea pe subunitatea 50 S ribozomială => bacteriostatic la doze ↓; bactericid la doze ↑. Obs.: NU se asociază cu Cloramfenicolul pentru că au acelaşi loc de acţiune. SA: CG+; CG-; BG+; Actinomicete, Mycoplasma, Chlamidia, Ricketzia. Obs.: ERITROMICINA ESTE ATB DE ÎNLOCUIRE LA BOLNAVII CU ALERGIE LA PENICILINE !!!
  • 7. FC: adm. orală → abs. duodenala. Distributie buna în ţesuturi (cu excepţia LCR). UT: boli cu germeni sensibili: angine streptococice pneumonie interstiţială cu Mycoplasme, Legionella, Chlamidii, profilaxia RAA sifilis erizipel boli sexuale cu chlamidii (cervicite, uretrite). Adm.: - oral la 6 ore
  • 8. MACROLIDE “NOI” • Bd% crescuta fata de macrolidele vechi • SA: “larg” – asemanator macrolidelor “vechi” + Toxoplasmoza gondi, H.Py., C. Jejuni, Mycobacterium avium (SIDA); BG – (Salmonela, Shigella, Jersinia) • Complianta terapeutica buna (1-2 prize/zi) • RA: - rare • FA: - adm. orala → distributie buna in tesuturi si celule; se c% in pulmon; renal → efect postantibiotic (72 ore) • UT: infectii cu germeni sensibili
  • 9. • Adm.: ROXITROMICINA – Rulid cp. CLARITROMICINA – Klacid cp.; fl.; sirop AZITROMICINA – Zitaromax cp. SPIRAMICINA – Rovamycine cp; fl.; sirop
  • 10. IV. LINCOSAMIDEIV. LINCOSAMIDE - LINCOMICINA - CLINDAMICINA LINCOMICINA SA: streptococi; stafilococi; anaerobi (Bacterioides fragilis) UT: infectii osteoarticulare cu stafilococ; profilaxia endocarditei infectioase Administrare: oral si parenteral (i.m., i.v. perfuzie) CLINDAMICINA SA: ! bacteroides fragilis
  • 11. V. GLICOPEPTIDEV. GLICOPEPTIDE - VANCOMICINA - TEICOPLANINA VANCOMICINA – VANCOCINE fl. MA: - inhiba sinteza peretelui bacterian - afecteaza permeabilitatea membranei citoplasmatice - afecteaza sinteza ARN bacterian SA: CG + (streptococi, stafilococi); BG +
  • 12. UT: “ATB de rezerva” pentru: - infectii stafilococice severe - colita pseudomembranoasa cu Clostridium - peritonita stafilococica RA: ototoxicitate; nefrotoxicitate Adm.: i.v. TEICOPLANINA – TARGOCID asemanator Vancomicinei SA: CG+ (streptococo,stafilococ) BG+ Uneori mai activ de 2 - 3 ori decat Vancomicina
  • 13. VI. POLIPEPTIDE CICLICEVI. POLIPEPTIDE CICLICE - COLIMICINA - POLIMIXINA SA: active pe CG- si BG-
  • 14.
  • 15. VII. ATB CU SPECTRU LARGVII. ATB CU SPECTRU LARG - TETRACICLINE - CLORAMFENICOL TETRACICLINELE Tetracicline “vechi” - TETRACICLINA - CLORTETRACICLINA - OXITETRACICLINA Tetracicline “noi” - DOXICICLINA - MINOCICLINA
  • 16. TETRACICLINA (Tetraciclina caps) DOXICICLINA (Vibramicin caps; fl) • abs. influentata de alimentatie • c% biliara modesta • NU patrunde in LCR • complianta terapeutica ↓ (T1/2 6 ore) • abs. neinfluentata de alimentatie • c% biliara buna • patrunde modest in LCR • complianta terapeutica buna (T1/2 = 18 – 20 ore)
  • 17. MA: impiedica sinteza proteica si replicarea bacteriana SA: Gonococ; Brucella; Yersinia; V. holeric; Chlamidia; Treponema; Richettzia; M. pneumonie; Leptospira, Borellia RA: dismicrobisme: candidoze, tulburari dentare si osoase Adm.: Tetraciclina caps 0,250 g oral la 6 ore Doxiciclina caps 0,100 g oral monodoza (DA + DI) fl. i.v.
  • 18.
  • 19. CLORAMFENICOLI - CLORAMFENICOL - TIAMFENICOL CLORAMFENICOL FC: absorbtie intestinala 80-90%, difuzie buna in tesuturi si organe (LCR) metabolizare hepatica (inutilizabil in insuf. hepato-biliare) MA: idem Macrolide SA: CG-: H.I.; Salmonella; Shigella CG+: streptococ, stafilococ, pneumococ BG+: b. difteric anaerobi: Richettzi, Clamidia, Mycoplasma
  • 20. UT: “ATB de rezerva” • febra tifoida si paratifoida A ↔(alternativa la trat. cu Ceftriaxona si Ciprofloxacina) • Meningita cu pneumococ sau bacili Gram negativi ↔ (scheme de tratament) • encefalite, abcese cerebrale cu anaerobi • infectii genito-urinare si abdominale cu anaerobi RA: Toxicitate hematopoetica (inhibitia hematopoetica sau aplazie medulara ireversibila) • “sindromul cenuisiu” al n-n prin deficit de glucuronoconjugaza, hepatica; • dismicrobisme: suprainfectii cu Candida
  • 21. CHINOLONECHINOLONE GENERATIA I • ACID NALIDIXIC GENERATIA II • ACID OXALINIC CINOXACINA • ACID PIPEMIDIC ROXACINA ! GENERATIA III - FLUOROCHINOLONELE • NORFLOXACINA (NOLICIN) DIFLOXACINA • ENOXACINA (ENOXOR) LOMEXACINA • OFLOXACINA (TARIVID) FLEROXACINA • PEFLOXACINA (PEFLOX) TEMAFLOXACINA • CIPROFLOXACINA (CIPRINOL)
  • 22. • Absorbtie orala 50-95% → Bd % mare • Complianta terapeutica buna (T1/2) = 11 ore) • Vd mare → cp mari in LCR, plamani, oase, bila,, prostata • SA “ultralarg”
  • 23. MA: (necesara in spiralarea cromozomului bacteria plesneste ca o de AND bacterian) “fasole coapta” ADN BACTERIE CHINOLONELE BLOCHEAZA AND-GIRAZA
  • 24. S.A.: ultralarg:CG+; CG-; BG- aerobi si anaerobi Mycoplasma, Chlamydia, Rickettsia UT: infectii urinare joase; infectii de prostatita (prostatitele acute si cronice); infectii cu transmitere sexuala (uretrite acute, cervicite acute, rectite acute, faringite acute gonococi); infectii gastrointestinale; infectii osteoarticulare; osteomielite acute si cronice cu BG-; infectii respiratorii: bronsite cronice (ciprofloxacina) Adm.: orala 2 prize; 1 priza i.v. perfuzie
  • 25. SULFAMIDE Cu actiune generala - Sulfodiazina - Sulfametazina Cu actiune urinara - Sulfametin - Sulfametoxazol Cu actiune intestinala - Salazopirin Cu actiune antileproasa - Sulfone Cu actiune antimalarica - Fansidar
  • 26. Cotrimoxazol = Biseptol; Bactrim; Septrim; Eusaprim (Sulfametoxazol + Trimetoprim) FC.: conc. in plamani, prostata, rinichi SA.: BG-;Pneumocistis carini, Toxoplasma gondi, Nocardia UT.: - infectii urinare - infectii genitale - infectii digestive - Pneumocistoza
  • 27. NITROFURANII • Cu actiune intestinala Furazolidon • Cu actiune urinara Nitrofurantoin
  • 28. NITROIMIDAZOLII Metronidazolul (Flagyl) SA.: - tricomonas, giardia lamblia, entamoeba histolytica (antiparazitar) - anaerobi: G +: clostridium perfringes si difficile; gardnerella vaginalis G -: bacteroides fragilis, fusobacterium, veilonella UT.: boli parazitare; infectii cu anaerobi (colono-rectale, gineco-obstetricale) Pr.: Metronidazol – Flagyl comp. orale, vaginale; fiole Ornidazol – Tiberal comp.; fiole Tinidazol – Fasigyn comp.; suspensie orala; fiole.