Bactericidas / Bacteriostticos
Antibiticos / Quimioterpicos
Resistente x Sensvel
Antimicrobianaos
antimicrobianaos
aa
antimicrobianaos
aa
Teste de Sensibilidade
Amostra de S.
pneumoniae com halo de
oxacilina 20 mmreportar
como sensveis penicilina e
aos -lactmicos que no
foram testados por esta
tcnica devido falta de
padronizao.
Effects of bacteriostatic versus bactericidal antibiotics on
logarithmically growing bacterial culture.
Log Number of Viable Bacteria
Drug Control
Addition
+ Bacteriostatic Agent
+ Bactericidal Agent
Time
Evolution of resistance to antibiotics
Antibiotic Year deployed Resistance observed
Sulfonamides 1930s 1940s
Penicilin 1943 1946
Streptomycin 1943 1959
Chloramphenicol 1947 1959
Tetracycline 1948 1953
Erythromycin 1952 1988
Vancomycin 1956 1988
Methicillin 1960 1961
Ampicillin 1961 1973
Cephalosporins 1960s late 1960s
Progression of antibiotics required for efficacy in
staphylococcal infections
H
HOOC N S
Penicillin 1946
NH2 O N
O
COOH
Progression of antibiotics required for efficacy in
staphylococcal infections
O
H
N
Methicillin 1961 S
O O N
O
COO
H
Progression of antibiotics required for efficacy in
staphylococcal infections
Sugar
O
Cl
O O
HO Cl OH
O O H
H
Vancomycin 1986 O
N
N
N
N
NH H
H H O N
HN O O O
HO
NH2
OH
O OH
HO
Progression of antibiotics required for efficacy in
staphylococcal infections
O
Zyvox 1999 O
O
O N N
N
F
Antibiotic sales in 1997
DRUG $ MILLIONS
Cephalosporins
Recephin (Roche) 933
Ceftin (GlaxoWellcome) 640
Ceclor (Lilly) 542
Fortaz (GlaxoWellcome) 449
Claforan (Hofmann LaRoche) 335
Macrolides
Bixin (Abbott) 1,150
Zithromax (Pfizer) 619
-Lactamase inhibitors
Augmentin (GlaxoSmithKline) 1,354
Primaxin (Merck) 555
Unasyn (Pfizer) 619
Penicillins
Amoxil (GlaxoSmithKline) 406
Quinolones
Ciprofloxacin (Bayer) 1,290
Antibiotic market in 1995
Class Wordwide sales Representative Infections that have
($ millions) drugs developed resistance
Cephalosporins 8,446 Cefalor, cefuroxime Bronchitis,
pneumonia meningitis
Penicillins 4,413 Amoxicilin, Ampicillin Pneumonia,
septicemia, bronchitis
Fluoroquinolones 3,309 Ciprofloxacin, ofloxacin
Meningitis
Macrolides 2,927 Clarithromycin, erythromycin
Meningitis
Tetracyclines 744 Minocycline Urinary tract
infections, pelvic
inflammatory disease
Aminoglycosides 729 Gentamicin Intestinal infections,
septicemia
Glycopeptides 462 Vancomycin Intestinal infections
All other 1,873 Imipenem, rifampin Bronchitis,
systemic antibiotic tuberculosis
Bacteria that are common causes of infections
Infections Gram-negative pathogens Gram-positive pathogens
Membrana Plasmtica
Ribossomos
cidos Nuclicos
Metabolismo Intermedirio
aa
antimicrobianaos
aa
Sites of action of antibacterial drug classes
cefalospornicos de 1, 2, 3, 4 e 5 geraes
Infeces estreptoccicas
Infeces leves e moderadas do trato respiratrio superior e da pele. Infeces
venreas: sfilis, bejel (sfilis endmica).
Profilaxia da glomerulonefrite aguda e doena reumtica.
Profilaxia de recorrncias da febre reumtica (doena reumtica de origem auto-
imune, em resposta do organismo a infeces pelo estreptococo).
Penicilina G (Bezentacil)
POSOLOGIA
2.5
0.0
0 1 2 3 4 5 6 7 8
Time (h)
Cefalosporinas
O
H H
S
N
H N
NH 2 CH 3
O
COOH
H
O OH
N
O
O
H
OH
Clavunalato
O cido clavulnico um beta-lactmico, estruturalmente
relacionado s penicilinas, que possui a capacidade de
inativar uma grande variedade de enzimas beta-
lactamases, comumente produzidas por microrganismos
resistentes s penicilinas e s cefalosporinas.
N. gonorrhoeae;
Outros
Chlamydia trachomatis; Mycobacterium scrofulaceum;
Cryptosporiduim Mycoplasma hominis
E. Coli Salmonella sp
Shigella sp
Entamoeba hystolitica
T. pallidum;
Mycobacterium avium - intacellulare Toxoplasma gondii
Mycobacterium kansasii; Ureaplasma urealyticum;
Mycobacterium leprae Yersina sp
Mycoplasma pneumoniae; Babesia microti
N. gonorrhoeae;
MACROLDEOS
Eritromicina Claritromicina
Clorafenicol Espiramicina
Azitromicina Miocamicina
Diritromicina Roxitromicina
Azitromicina
Nome comercial: Zitromax
Contra-indicaes:
Uso em adultos
REAES ADVERSAS
APRESENTAES
Otorrinolaringologia
Pneumologia
Dermatologia
Odontoestomatologia
Infeces genitais
Profilaxia da meningite meningoccica.
ROXITROMICINA
Contra-indicaes:
Tetraciclina
Doxiciclina
Doziciclina
Minociclina
TETRACICLINAS
- Acne vulgaris: como adjuvante de tratamento.
- Actinomicoses causadas por Actinomyces israelii.
- Infeco geniturinria causada por N. gonorrhoeae e por
Chlamydia trachomatis.
- Gengivoestomatite causada por Fusobacterium
fusiformisans.
- Granuloma inguinal causada por Calymmatobacterium
granulomatis.
- Linfogranuloma venreo por Chlamydia sp.
TETRACICLINAS
- Otite mdia, faringite, pneumonia e sinusite causadas por H.
influenzae e Klebsiella sp.
- Tifo causada por Rickettsias.
- Sfilis causada por Treponema pallidum.
- Infeco bacteriana do aparelho urinrio causada por
Escherichia coli e Klebsiella sp.
- Infeco retal menor causada por Chlamydia trachomatis.
- Enterocolites causadas por Shigella sp.
TETRACICLINAS
Contra-indicaes:
POSOLOGIA
Uso em Adultos
Uso em Adultos
eosinofilia
anorexia
hiperatividade psicomotora/agitao
Principles of Pharmacology - The Pathophysiologic Basis of Drug Therapy Fig 32.6 (cont.)
Structure of folic acid, PABA analogues (sulfonamides), and folate analogues
(dihydrofolate reductase inhibitors)
Principles of Pharmacology - The Pathophysiologic Basis of Drug Therapy Fig 32.6 (cont.)
Folate synthesis and
function
Principles of Pharmacology - The Pathophysiologic Basis of Drug Therapy Fig 33.10 (cont.)
Structure of antimicrobial
drugs targeting the 50S
ribosomal subunit