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CLASE DE ANTIBIOTICE
Egidia Miftode
Istoria introducerii n practic a antibioticelor
Anul introducerii
Clase de antibiotice
1935
Sulfonamide
Beta-lactamine (Penicilina)
1941
1944
Aminoglicozide
Cloramfenicol
1949
Tetracicline
1950
Macrolide/lincosamide/streptogramine
1952
Glicopeptide
1956
Rifamicine
1957
Nitroimidazoli
1959
Quinolone
1962
Trimetoprim
1968
Oxazolidinone
2000
Lipopeptide
2003
PENICILINE
Clasificarea penicilinelor:
1. Peniciline naturale (Penicilina G i V)
2. Peniciline rezistente la penicilinaze (Peniciline de grup M)
3. Aminopeniciline (Grup A)
4. Peniciline antipseudomonas (carboxipeniciline i acil peniciline)
PENICILINE NATURALE
DOZE-ADULT/ZI
1-20 mil.UI, im/iv, 4/6/12h
DOZE-COPIL/ZI
50000-200000 U/kg
PENICILINA V
EXTENCILLINE
(BENZATHINE PEN G)
50000-100000 U/kg
600000 U/15 zile sau
1,2 mill.U/lun
INDICAII
1) Angine, scarlatin
2) Pneumonie , meningit, sepsis
3) Endocardit
4) Sepsis, meningit
5) Difterie
6) Antrax
7) Colita pseudomembranoas
8) Diferite infecii cutanate sau
sistemice
9) Sifilis
10) Leptospiroz
11) Boala Lyme
12) Meningit, sepsis
PENICILINE-REZISTENTE LA PENICILINAZE
DOZE-ADULT
2-4 g/zi (po:6/8h;im,iv:4-12h)
4-12 g/zi (im,iv: 4-6h)
1-4 g/zi (6-8h)
DOZE-COPIL
50-100 mg/zi
100-200 mg/kg/zi
50-100 mg/kg/zi
AMINOPENICILINELE
Tabel 4. Doze de aminopeniciline
ANTIBIOTIC
AMPICILINA
DOZE-ADULT
Po: 2-4 g/zi
Im, iv: 4-12 g/zi
DOZE-COPIL
100 mg/zi
100-300 mg/zi
AMOXICILINA
BACAMPICILINA
METAMPICILINA
PIVAMPICILINA
AMOXICILINA- acid clavulanic
AMPICILINA-sulbactam
25-200 mg/kg/zi
50-100 mg/kg/zi
50-200 mg/kg/zi
50-100 mg/kg/zi
30-40 mg/kg/zi
30-40 mg/kg/zi
INDICAII
Pneumonie
Meningit,
Sepsis
Endocardit
Antrax
Difterie
Leptospiroz
Boala Lyme
Profilaxia unor infecii stomatologice
DOZE-ADULT
250 mg/kg/zi
12,4-18,6g/zi
DOZE-COPIL
75-100 mg/kg/zi
150-300mg/kg/zi
MEZLOCILINA
PIPERACILINA
PIPERACILINA+tazobactam
Tabel 7. Activitatea
antipseudomonas
6-15 g/zi
6-15 g/zi
4,5-13,5 g/zi
antibacterian
100-300 mg/kg/zi
100-300 mg/kg/zi
100-300 mg/kg/zi
indicaiile
penicilinelor
SPECTRU
ANTIMICROBIAN
AL
INDICAII
PENICILINELOR
ANTIPSEUDOMONAS
TICARCILINA:
Proteus
Enterobacter
Infecii severe cu germeni sensibili
Serratia
Infecii polimicrobiene: biliare,
Pseudomonas
digestive, genito-urinare.
PIPERACILINA: spectrul AMPI +
Serratia marcescens
Enterobacter cloacae
Citrobacter
Bacteroides fragilis
Pseudomonas
Proteus
Klebsiella
MONOBACTAMI
AZTREONAM
Tabel 8. Spectru antimicrobian al aztreonam
SPECTRU ANTIMICROBIAN AL
AZTREONAM
Coci Gram negativ aerobi:
- N. gonorrhoeae
- N. meningitidis
Bacili Gram negativ aerobi:
- Salmonella
- Shigella
- Haemophilus
- E. coli
Sensibilitate inconstant sau moderat:
Pseudomonas
Enterobacter
Citrobacter
INDICAII
Klebsiella
CARBAPENEME
Tabel 9. Dozele de carbapeneme
DRUG
IMIPENEM
MEROPENEM
ERTAPENEM
ADULT
2 g/zi, iv
3 g/zi, iv
1g/zi, im, iv
CHILD
30-60 mg/kg/d
40 mg/kg/d
sp)
ANAEROBI GN (Bacillus fragilis)
GP=Gram pozitiv, GN=Gram negativ
CEFALOSPORINE
CEFALOSPORINE DE PRIM GENERAIE
Tabel 11. Dozele de cefalosporine de prima generaie (C1G)
ANTIBIOTIC
CEFAZOLIN
CEFADROXYL
CEFALEXINE
DOZE-ADULT
1-6 g/zi IV, im (la 6-8h)
1-2 g/zi po
1-2g/zi po (la 6 h)
DOZE-COPIL
60mg/kg/zi (la 8 h)
30 mg/kg/zi (la 12 h)
25-50 mg/kg/zi (la 6 ore)
INDICAII
Infecii respiratorii, ORL
Infecii urinare
Infecii ale pielii
DOZE-ADULT
3-6 g/zi
1,5-4,5 g/zi, iv,im
500 mg/zi, po
DOZE-COPIL
50-100 mg/kg/zi
50mg/kg q8h iv, 10-15mg/kg x2 po
10-15mg/kgx2 (max 1 g/d)
30-60 mg/kg/zi
80-160 mg/kg/zi (la 6h)
INDICAII
Otite
Sinuzite
Angine (n caz de eec al terapiei cu
penicilina G sau recurene)
DOZE-ADULT
4 g/zi
3-8 g/zi
3-6 g/zi
2 g/zi(<65ani), 1g/zi (>65ani)
2-12 g/zi
2-6 g/zi
DOZE-COPIL
30-60 mg/kg/zi
50-100 mg/kg/zi
50-100 mg/kg/zi
50-75 mg/kg/zi
30-60 mg/kg q8h
400 mg/zi po
200-400 mg/zi
400 mg/zi
600mg/zi (div 1 sau 2 prize)
INDICAII
C3G parenterale
INFECII SEVERE:
Sepsis
Meningite
Infecii bronhopulmonare
Infecii nosocomiale
Infecii la neutropenici
Antibioprofilaxie n chirurgie
C3G orale:
Infecii ORL recidivante
Infecii
bronhopulmonare
recidivante
Infecii urinare
DOZE-ADULT
2-4g/zi, iv
2-4g/zi, iv
DOZE-COPIL
150mg/kg/zi (la 8 h)
INDICAII
INFECII SEVERE:
Sepsis
Infecii neuro-meningee
Infecii bronhopulmonare
Infecii nosocomiale
Infecii la neutropenici
Infecii urinare
LINCOSAMIDE
Tabel 19. Dozele de lincosamide
ANTIBIOTIC
CLINDAMCINA
LINCOMICINA
DOZE-ADULT
DOZE-COPIL
0,6-2,4 g/zi, po, im, iv (la 8-25 mg/kg, po
6-8h)
15-40mg/kg, parenteral
0,6-1,8g/zi im., iv po 30-60 mg/kg/d, po
(la8h)
10-20 mg/kg/d, im/iv
INDICAII
Infecii osoase i articulare
Staphylococcus
Streptococcus (excepie enterococcus)
Infecii
cu
anaerobi
(excepie
meningita)
Profilaxia endocarditei infecioase n
caz de alergie la penicilin.
AMINOGLICOZIDE
Tabel 21. Dozele de aminoglicozide
ANTIBIOTIC
1. AMIKACINA
2. DIBEKACINA
3. GENTAMICINA
4. NETILMICINA
5. SISOMICINA
6. TOBRAMICINA
7. KANAMICINA
8. STREPTOMICINA
9. ISEPAMICINA
DOZE-ADULT
15 mg/kg/zi (12-24h)
3 mg/ kg/zi (12-24h)
3 mg/kg/zi (8, 12, 24h)
4-7 mg/ kg/zi (8, 12, 24h)
3 mg/ kg/zi (8, 12, 24h)
3-5 mg/ kg/zi (8, 12, 24h)
15 mg/kg/zi (12h)
0,5-1 g/zi (24h)
15 mg/kg q24h
DOZE-COPIL
15 mg/kg/zi
2-4 mg/kg/zi
6-9 mg/kg/zi
3-5 mg/kg/zi
3 mg/kg/zi
15mg/kg/zi
30-50 mg/kg/zi
-
INDICAII
! N ASSOCIERE!
-Infecii urinare
-Endocardita infecioas
-Infecii bronho-pulmonare
-Infecii cu Listeria
-Infecii cu germeni multirezisteni
(terapie de primo intenie)
-Bruceloz
-Tuberculoz
Brucella
KANAMICINA: M. tuberculosis
CICLINELE
Tabel 23. Dozele de cicline
ANTIBIOTIC
Prima generaie:
TETRACICLINA
OXITETRACICLINA
ROLITETRACICLINA
A 2-a Generaie:
LIMECICLINA
METACICLINA
A 3- a generaie:
DOXICICLINA
MINOCICLINA
DOZE-ADULT
1-2g (6h), po
1-2g (12h),iv
300mg,im
25-50 mg/kg/zi
10-20 mg/kg/zi
10-15 mg/kg/zi
2-4 mg/kg/zi
2-4 mg/kg/zi
INDICAII
Bruceloz
Infecii bronho-pulmonare cu
pneumoniae, Chlamydia
Holer
Infecii genitale cu Chlamydia
Profilaxia i tratamentul malariei.
Boala Lyme
Boala zgrieturii de pisic
Mycoplasma
MACROLIDE
Tabel 25. Dozele de macrolide
ANTIBIOTIC
14 atomi C:
ERITROMCINA
CLARITROMCINA
DIRITROMICINA
ROXITROMCINA
15 atomi C
Azalide:
AZITROMICINA
16 atomi C:
SPIRAMICINA
JOSAMICINA
SINERGISTINE:
PRISTINAMICINA
VIRGINIAMICINA
DOZE-ADULT
DOZE-COPIL
25-50 mg/kg/zi
300-600 mg/zi
5-8 mg/k/zi
500 mg/zi, po
10 mg/kg/zi
50000 UI/k/zi
30-50 mg/k/zi
3 g/zi, po
3g
50-100 mg/kg
50-100 mg/kg
INDICAII
Bronit
Pneumonie atipic
Pneumonia cu Legionella
Infecii ale pielii
Infecii digestive
(Campylobacter,
Criptosporidium),
Infecii genitale,
Toxoplasmoz (n sarcin)
Angiomatoza bacilar
Pelioza hepatic
Infecii n stomatologie
Vibrio sp.
Toxoplasma
gondii
(spiramicina,
roxitromicina, claritromicina)
Mycobacterii atipice, Helicobacter pylori
(claritromicina)
SINERGISTINE:
Staphylococcus oxa-R
Pneumococ
anaerobi GP
GP=Gram-pozitiv; GN=gGam-negativ
GLICOPEPTIDE
Tabel 27. Dozele de glicopeptide
ANTIBIOTIC
VANCOMCINA
ADULT
1,5-2 g iv (12h)
TEICOPLANIN
ORITAVANCIN
DALBAVANCIN
200-400 mg/zi
COPIL
0-30 zile (vrst): 15 mg/kg/zi
> 30 zile (vrst): 10 mg/kg/zi
10 mg/kg/zi
CLORAMFENICOL
Tabel 28. Activitatea antibacterian i indicaiile cloramfenicolului
SPECTRU ANTIMICROBIAN
coci GP:
S. aureus
S. epidermidis
S. pneumoniae
Peptococcus-Peptostreptococcus
coci GN i cocobacili:
N. gonorrhoeae
Pasteurella multocida
H. influenzae
Brucella spp
Bordetella pertussis
Bacili GP:
Corynebacterium diphteriae
Listeria monocytogenes
Clostridium spp
Prpionibacterium acnes
INDICAII
abces cerebral
empiem subdural
meningit
febr tifoid
infecii
determinate
rickettsii
de
Actinomyces israelii
Actinobacillus actinomycetemcomitans
Bacili GN:
E. coli, S. typhi,
Proteus mirabilis
Enterobacteriaceae au sensibilitate variabil)
Chlamydia, Mycoplasma, rickettsii
(alte
QUINUPRISTIN I DALFOPRISTIN
Tabel
29.
Activitatea
quinupristin/dalfopristin
SPECTRU
ANTIMICROBIAN
Quinupristin i dalfopristin
E. faecium
S. aureus (inclusiv MRSA)
S. pneumoniae (inclusiv PRP)
Lactobacillus spp,
Leukonostoc spp
Bacteroides spp
Moraxella
L. monocytogenes
Prevotella
My. pneumoniae
antibacterian
indicaiile
INDICAII
al
FOSFOMICINA
Fosfomicina este activ pe Staphylococcus (i pe Staphylococcus
meticilino-rezistent), bacili gram negativ.
Doze:
- 8-12 g/dzi iv (aduli)
- 100-200 mg/kg/zi (copii)
Reacii adverse: diaree, flebit chimic, hiperNa i hypoK-emia
hiperosmolaritate (atenie n insuficiena cardiac/renal).
FLUOROQUINOLONELE
Tabel 30. Clasificarea i activitatea antibacterian a fluoroquinolonelor
Clasificare biologic a fluoroquinolonelor
Grupa I: Spectru limitat
Acid nalidixic
Flumequine
Acid oxolinique
Acid piromedique
Acid pipemidique
Cinoxacine
Grupa II: Spectru larg
Pefloxacin
Enoxacin
Norfloxacin
Ciprofloxacin
Fleroxacin
Lomefloxacin
Ofloxacin
Clasificare microbiologic
Enterobacteriaceae
Enterobacteriaceae i:
H. influenzae
Neisseria spp
Staphylococcus coagulazo negativ
patogeni intracelulari
Mycoplasma spp
P. aeruginosa
Acinetobacter spp
Vibrio holerae
M. tuberculosis
M. leprae
Spectrul Grupei II
+
S. pneumoniae
Streptococcus spp
+/ANAEROBI
KETOLIDE
Utilizat n prezent este telithromycine.
Activitatea antibacterian:
Coci Gram pozitiv , inclusiv: Streptococcus pyogenes, S. aureus, S.
pneumoniae rezisteni la macrolide,
OXAZOLIDINONE
Activitatea antibacterian este reprezentat n principal de patogeni
bacterieni Gram pozitiv:
S. aureus meticilino rezistent (MRSA),
S. epidermidis,
pneumococi penicilino rezistent (PRP),
enterococ vanco- rezistent (VRE),
tulpini de enterococ vanco intermediare (VISA).
METRONIDAZOL I ALI NITROIMIDAZOLI
Metronidazolul este un agent bactericid a crui aciune const n:
activarea oxireducerii, efect toxic al produilor intermediari redui,
eliberarea produilor finali inactivi.
Doza depinde de infecie:
Giardiaz: 250 mg x2/zi 5-7 zile, sau 2g/zi 3 zile.
Infecii cu anaerobi:
i.v. - 15 mg/kg apoi 7,5 mg/kg (administrare la 6h)
p.o. 1-2 g/zi n 2-4 doze .
Activitate antimicrobian: Bacteroides fragilis, B. melaninigenicus,
Prevotella, Fusobacterium spp, anaerobi, coci gram-negativ i gram-positiv,
Cl. perfringens, Giardia lamblia, Entamoeba histolytica, Trichomonas
vaginalis
SULFONAMIDE I TRIMETOPRIM
ACTIVITATE ANTIMICROBIAN
Organisme Gram - pozitiv (S. aureus, S.
Sulfisoxazol
Sulfametoxazol
Sulfadoxina
LIPOPEPTIDE
Daptomicina este primul antibiotic aparinnd unei noi clase de
antibiotice, lipopeptidele ciclice.
Este indicat n infecii complicate ale pielii i esuturilor moi (4 mg/kg/24
ore, i.v. doz unic), endocardite (6 mg/kg/24 ore i.v.)
GLICILCICLINE
Tigeciclina este primul antibiotic al clasei, derivat din minociclin.
Este activ pe:
majoritatea bacililor Gram-negativ (cu excepia P. aeruginosa,
Proteus spp, Providentia spp) incluznd i tulpinile productoare de
ESBL i Acinetobacter spp multirezistente;
Coci Gram-pozitiv multi-drog rezisteni: MRSA i enterococ
rezistent la glicopeptide;
Bacterii intracelulare (Mycoplasma, Chlamydia, Legionella),
Anaerobi (i Bacteroides fragilis),
Mycobacterii cu cretere rapid (M. abscesus, M chelonae, M.
fortuitum).
REZISTENA LA ANTIBIOTICE
MEDICAIA ANTIFUNGIC
Tabel 1. Clasificarea antifungicelor
Clasificare
Inhibitori ai mitozei fungilor
Poliene
Substitute de pirimidin
Azoli
- Imidazoli
- Triazoli
Reprezentani antifungici
Griseofulvina
Nistatin, amfotericina B
Flucitozina
Miconazol, clotrimazol, ketoconazol
Fluconazol, itraconazol, voriconazol,
posaconazol
Naftifina, terbinafina
Tolnaftat
Caspofungin
Alilamine
Tiocarbamai
Inhibitori de beta 1-3 glucan
sintetaz
Inhibitori ai sintezei chitinei
Dimetil morfoline
Nikomicina
Amorolfina
DOZE
INDICAII
-Amfotericina B
1mg/kg (T=2-2,5g)
Flucitozina
Imidazoli
-Ketoconazol
-Itraconazol
200 mg/zi x 2
200mgx3/zi primele 3
zile
-Fluconazol
50-100 mg o dat/ zi
Candidoza orofaringian
100-400 mg
Candidoza esofagian
400 mg/ zi -2 luni (dup Meningita criptococozic
terapia iniial cu Amf
B+flucitozin
-Voriconazol
-Posaconazol
400mg x 2/zi
-Caspofungin
Terbinafina
T=doza total.
Candidoza vaginal
Micoze profunde
- Aspergillus sp (i rezistent la
AmfB, Candida sp, Fusarium sp
MEDICAIA ANTIVIRAL
n tabelul de mai jos sunt redate principalele antivirale (cu excepia
antiretroviralelor care sunt expuse n capitolul Infecia cu HIV/boala SIDA
i a antiviralelor utilizate n hepatite care sunt detaliate la capitolul
corespunztor), mecanismele se aciune, indicaiile i efectele adverse.
Tabel 1. Caracteristici ale antiviralelor
DROG ANTIVIRAL
MECANISM
VIRUS
DOZE
DE ACIUNE
AFECTAT
Acycl. triphosphate inhib ADN H. simplex, varicella-zoster, 10 mg/
ACYCLOVIR
polimeraza viral
cytomegalovirus (CMV)
kg/zi,po/iv.
!EFECTE ADVERSE:nefropatie reversibil, tulburri GI, flebit, cefalee, encefalopatie.
La fel ca Acyclovir
La fel ca Acyclovir
VALACYCLOVIR
! E.A.: La fel ca Acyclovir + microangiopatia trombotic.
Ganciclovir triph.inhib
CMV,
5 mg/kg/zi
GANCICLOVIR
ADN polimeraza viral..
posibil:HS, VZ, HHV8
! E.A.: suppresia mduvei osoase (granulocitopenie) frecvent, insuficien renal, febr, cefalee, encefalopatie,
flebit, rash.
Pencicl.triph
inhib
ADN
PENCICLOVIR
polimeraza viral.
Topic, fr absorbie sistemic important!
! E.A.: fr.
La fel ca Penciclovir.
Herpes simplex, varicellaFAMCICLOVIR
zoster
! E.A.: cefalee greuri, diaree, interaciuni cu medicamente ce inhib sau necesit oxidare hepatic rar.
inhib ADN polimeraza viral,
CMV, acyclovir
60mg/kg/zi
FOSCARNET
revers transcriptaza.
HSV rezistent, VZV
la 8h
! E.A.: Insuficien renal, dezechilibre electrolitice (hipocalcemie -frecvent), greuri, vrsturi frecvent
anemie, ulcere genitale, convulsii rar.
Interfereaz cu ARN mesager viral Febra Lassa, hantavirus,
0.5/0.6 g
RIBAVIRINA
hepatita C (cronic)
x2 /zi, po
! E.A.: Anemie frecvent, iritaii ale ochilor, pielii, CRS (bronhospasm frecvent)
inhib ADN viral i revers Hepatit B (cronic), HIV - 1 100 mg/zi,
LAMIVUDINA
transcriptaza
po
! E.A.: Acidoz lactic, hepatomegalie cu steatoz rar.
Blochez o protein a canalului Virusul gripal A
100mg/zi,
AMANTADINA
ionic, alternd pH-ul intracelular
2.2mg/k/zi
! E.A.: greuri i anorexie frecvent, disfuncie SNC rar, deces prin hiperdoz rar.
La fel ca amantadine
La fel ca amantadine
200mg/zi,
RIMANTADINA
5mg/kg/zi
! E.A.: greuri i anorexie frecvent, disfuncie SNC mai rar dect amantadina
Interfer cu sinteza proteinelor Hepatita B i C (posibil D), Vezi
cap.
INTERFERON ALFA
virale.
HHV8, Papillomavirus
Hepatite
(Peginterferon)
! E.A.: simptome influenza-like, tulburri GI, depreie, suppresia mduvei osoase- frecvent, fenomene
autoimmune- rar.