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Antibiotice Si Chimioterapice Antimicrobiene

This document discusses antibiotics and antimicrobial chemotherapy. It describes how antibiotics are naturally produced by microorganisms and have antimicrobial effects, while chemotherapeutics are semisynthetic and synthetic substances with selective inhibitory effects on pathogens. It provides classifications of antibiotics based on chemical structure such as beta-lactams, aminoglycosides, and macrolides. It also discusses mechanisms of antibiotic and chemotherapeutic action, mechanisms of natural and acquired microbial resistance, and provides examples of penicillin antibiotics.

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0% found this document useful (0 votes)
132 views22 pages

Antibiotice Si Chimioterapice Antimicrobiene

This document discusses antibiotics and antimicrobial chemotherapy. It describes how antibiotics are naturally produced by microorganisms and have antimicrobial effects, while chemotherapeutics are semisynthetic and synthetic substances with selective inhibitory effects on pathogens. It provides classifications of antibiotics based on chemical structure such as beta-lactams, aminoglycosides, and macrolides. It also discusses mechanisms of antibiotic and chemotherapeutic action, mechanisms of natural and acquired microbial resistance, and provides examples of penicillin antibiotics.

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tabella25
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© © All Rights Reserved
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ANTIBIOTICE SI CHIMIOTERAPICE

ANTIMICROBIENE
 Antibioticele(AB)- substante naturale
produse de diverse microorganisme cu
efect antimicrobian asupra agentilor
biologici patogeni
 Chimioterapicele sunt substante
semisintetice si sintetice cu efect selectiv
inhibitor asupra agentilor biologici
patogeni.
ANTIBIOTICE ANTIMICROBIENE
Clasificarea dupa structura chimica

1.Betalactamine 2.Aminoglicozide 3.Macrolide


Dibactami:
Streptomicina Eritromicina
Peniciline nat.
Peniciline antistafilococice Kanamicina Oleandomicina
Aminopeniciline Gentamicina Spiramicina
Carboxipeniciline
Neomicina Roxitromicina
Ureidopeniciline
Amidinopeniciline Tobramicina Fluritromicina
Carbapenemi Amikacina Azitromicina
Cefalosporine
 Monobactami
Claritromicina
Tribactami
Structura betalactaminelor
ANTIBIOTICE ANTIMICROBIENE
Clasificarea dupa structura chimica

4. Lincosamide Lincomicina, Clindamicina

5. Glicopeptide Vancomicina, Daptomicina

6. AB cu spectru larg Tetracicline, Amfenicoli

7. Grupul rifanpicinei Rifampicina, Rifaximin

8. AB polipeptidice Polimixinele , Bacitracina


CHIMIOTERAPICE ANTIMICROBIENE

 Chinolone si fluorochinolone
 Sulfamide antibacteriene
 Diaminopirimidine, trimetoprim
 Derivati de nitrofuran
 Derivati de formaldehida
 Derivati de imidazol
 Alte antimicrobiene: linezolid, spectinomicina,
fosfomicina, acid fusidic.
BACTERIILE SI LOCUL
INFECTIILOR
Cav. bucala Piele/Tes. moi Oase si Articulatii
Peptococcus S. aureus S. aureus
Peptostreptococcus S. pyogenes S. epidermidis
Actinomyces S. epidermidis Streptococci
Pasteurella N. gonorrhoeae
Gram-negative rods

Abdomen Tract Urinar T. Resp. Sup


E. coli, Proteus E. coli, Proteus S. pneumoniae
Klebsiella Klebsiella H. influenzae
Enterococcus Enterococcus M. catarrhalis
Bacteroides sp. Staph saprophyticus S. pyogenes

T. Resp. Inf T. Resp. Inf Meninge


Comunitate spital S. pneumoniae
S. pneumoniae K. pneumoniae N. meningitidis
H. influenzae P. aeruginosa H. influenza
K. pneumoniae Enterobacter sp. Group B Strep
Legionella pneumophila Serratia sp. E. coli
Mycoplasma, Chlamydia S. aureus Listeria
MODUL DE ACTIUNE AL AB. SI CT.
 Actiune bactericida- intoxicarea
ireversibila a germenilor microbieni
la CMI.
- bactericida absoluta: afecteaza
germenii in stare de repaus si in faza
de multiplicare.(polimixine)
- bactericida degenerativa:
afecteaza germenii numai in faza de
multiplicare(peniciline, cefalosporine)
 Actiune bacteriostatica –inhibarea
multiplicarii germenilor (tetracicline,
sulfamide, macrolide etc)
Mecanismele de actiune
antimicrobiene
 Actiune asupra peretelui celular(inhibarea
sintezei peptidoglicanului)
 Actiune asupra membranei citoplasmatice
(modifica bariera osmotica)(polimixinele)
 Inhibarea sintezei proteice ribozomale
(tetracicline, macrolide)
 Actiune la nivelul nucleului: inhibarea ADN-
girazei, ARN-polimerazei,efect toxic asupra
ADN
Rezistenta la AB. si CT.
 Rezistenta microbiana- capacitatea
microorganismelor patogene de a se mentine
in stare activa si de a se multiplica si dezvolta
in prezenta unui anumit chimioterapic.
-Naturala: determinata genetic- B. Koch
- Dobandita: - genetic :
-transfer cromozomial,
- transfer extracromozomial
prin achizitie de plasmide
- non-genetic :
-existenta sub forma de
“persisteri” inactivi metabolic
- pierderea structurii tinta pt
medicamente : protoplasti
Mecanismele biochimice ale
rezistentei naturale si dobandite
 Producerea de enzime ce inactiveaza AB si CT
 Scaderea permeabilitatii peretelui sau membranei
citoplasmatice bacteriene pt antibiotic
 Producerea de enzime modificate( polimeraze,
transpeptidaze) care limiteaza sau anuleaza
actiunea antibacteriana a antibioticului la nivelul
enzimei tinta
 Alterarea tintei extracelulare prin modificarea
proteinelor ribozomale
PENICILINE
 AB naturale sau de semisinteza – au ca nucleu
comun acidul acidul 6-aminopenicilinamic= inel
tiazolidinic+inel beta-lactamic
 1928- Alexander Fleming –Penicilinum rubrum
 1933- Florey si Chain izoleaza penicilina
PENICILINE
Clasificare
Peniciline naturale Benzilpenicilina(G) Coci , bacili G+
Benzatin-benzilpenicilina Coci G-
Fenoximetilpenicilina
Peniciline Meticilina Stafilococcus aureus
Antistafilococice Oxacilina
Cloxacilina
Dicloxacilina
Flucloxacilina
Aminopeniciline Ampicilina, Amoxicilina Coci , bacili G+
Epicilina Coci G-, unii bacili G-

Peniciline cu spectru Ticarcilina, piperacilina, Coci , bacili G+


larg carbenicilina Coci G-, bacili G-
Pseudomonas A.
BENZILPENICILINA
 FARMACOCINETICA
Administrare i.m. , i.v.
T1/2 30-60 min, concentratii sgv.
active 6h.
Legare de prot. 50-60%
plasmatice
Distributie in tes. Vd=0.35 l , in LCR 5-10% din
concentr. Plasmatica
Traverseaza placenta, partial in
laptele matern
Eliminarea Renala, redusa la nou-nascuti,
batrani, probenecid
BENZILPENICILINA
Gram-pozitivi Gram-negativi
pen-susc S. aureus Neisseria sp.
S. pneumoniae
Grup streptococci Anaerobi
Streptococci viridans Clostridium sp
Enterococcus
Altele
Treponema pallidum (sifilis)
BENZILPENICILINA
 Mecanismul de actiune: bactericid degenerativ
Legarea de PBP(peniciline binding proteine)

Legarea covalenta de transpeptidazele peretelui


bacterian

Activarea autolizinelor bacteriene

Moarte celulara
BENZILPENICILINA
 Rezistenta bacteriana : beta-lactamaze
BENZILPENICILINA
 REACTII ADVERSE
- Convulsii la administrare intrarahidiana
- Reactii alergice :dermita de contact, soc
anafilactic, astm bronsic
- Anemie hemolitica dupa cure prelungite
- Nefrita interstitiala si necroza globulara la
doze mari
- Dureri la locul injectarii, infiltratii nodulare, abcese,
flegmoane
BENZILPENICILINA
 CONTRAINDICATII: susceptibilitate alergii, infectii
cu germeni rezistenti
 INDICATII TERAPEUTICE:
-inf cu pneumococ: pneumonii, meningite, septicemii
- infectii cu streptococ hemolitic: angine, otita, erizipel,
infectii puerperale
- endocardita lenta cu streptococ viridans, enterococ
- actinomicoza, tetanos, difterie, lues
- profilactic in RAA
BENZILPENICILINA
POSOLOGIA:
Adulti: infectii moderate 1-2 000 000UI/zi la 6ore
infectii grave 2-20 000 000UI/zi la 6 ore
Nou-nascuti 60 000UI/kg/zi - 4 prize
Sugar, copil mic :
- infectii usoare si medii
40 000 – 100 000 UI/kg/zi - 4 prize
-inf. grave 200 000-400 000/kg/zi 4 prize
PENICILINE INJECTABILE CU
EFECT RETARD
 Procainbenzilpenicilina
 Benzatinbenzilpenicilina

 Fenoximetilpenicilina(penicilina V)

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