头孢菌素类抗生素(英文PPT)Cephalosporin Antibiotics

1st Generation Cephalosporins
OH
HH
N
S
H2N
O
源自文库
N
O
C H3
C O2H
Indications: UTI, pharyngitis and tonsillitis due to group A b-hemolytic Streptococcus, skin and skin structure infections.
G2
PO: Cefaclor, Loracarbef, Cefprozil, Cefuroxime Parenteral: Cefmetazole, Cefotetan, Cefonacid,
Cefamandol, Cefoxitin
G3
PO: Cefpodoxime, Cefixime, Cefdinir, Ceftitbuten Parenteral: Cefotaxime, Ceftizoxime, Ceftriaxone,
IM/IV use only, adjust dose as a function of creatinine clearance with 80% excreted renally unchanged, 86% protein bound
N N
N
H
N
S
O O
N
SN
N
CO2H
S CH3
Cefazolin - Ancef®, Kefzol®, Zolicef®
Indications: Respiratory tract infections, GU infections, skin and skin structure infections, Biliary tract infections, bone and joint infections, Septicemia, endocarditits; pre-, post- or intraoperative prophylaxis. Used for staph or strep infection in patients with mild hypersensitivity to penicillins! NOT for meningitis (can’t cross BBB).
Gram(+) aerobic bacteria - limited Gram(-)
Oral use only, 10% protein bound, >90% excreted renally unchanged
One of the Top 200
Indications: Oral - Respiratory tract infections, Otitis media, skin and skin structure infections, Bone infections, GU infections, UTI;
Parenteral – Septicemia; pre-, post- or intraoperative prophylaxis
Oral or IV/IM use, 17% protein bound, >90% excreted renally unchanged
Generally all are inactivated by b-lactamases
and skin structure infections, Osteomyelitis, UTI,
N
H
N
S
S
Septicemia, pre-, post- or intraoperative prophylaxis
O
N
O
O CH3
IV/IM use only, 50% protein bound, 70% excreted renally unchanged
Ceftazidime, Cefaperazone
G4 - Cefepime
Cephalosporin Deactivation
H ROCHN
H S
H
ROCHN
Esterase
H S
N
O
O
N
OH
O
CO2H
O
CO2H
H ROCHN
H S
Spontaneous Lactonization
N O
O O
CO2H
O
Methicillin substitute.
Cephapirin - Cefadyl®
Comparatively resistant to Staph. penicillinase
Generally all are inactivated by b-lactamases
1st Generation Cephalosporins
Oral use only, 20% protein bound, >90% excreted renally unchanged
Prolonged half-life allows once-a-day dosing
C e fa d ro x il - D u ric e f®
Indications: Respiratory tract infections, skin
头孢菌素类抗生素（英文PPT） Cephalosporin Antibiotics
Cephalosporin Antibiotics
Cephalosporin Antibiotics
G1
PO: Cephalexin, Cephradine, Cephadroxil Parenteral: Cefapirin, Cefazolin
C e p h ra d in e - V e lo s e f®
Indications: Respiratory tract infections, Otitis media, skin and skin structure infections, Bone
infections, Gram (-) UTI. Used for staph or strep infection in patients with mild hypersensitivity to penicillins!
Deactivated Cephalosporin
1st Generation Cephalosporins
HH
N
S
H2N
O
N
O
CH3
CO2H
Cephalexin - Keflex®, Biocef®, Keftab®
Partial hydrogenation
HH
N
S
H2N
O
N
O
C H3
C O2H