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OMAR MOHAMUD SALAH NO; 0085 15/1/2010

PHRMACOLOGY ASSIGNMENT

Cephalosporins:
These are any of a group of broad-spectrum, penicillinase-resistant antibiotics from
Acremonium, related to the penicillins in both structure and mode of action. Those used
medicinally are semisynthetic derivatives of the natural antibiotic cephalosporin C. First-
generation cephalosporins have a broad range of activity against gram-positive organisms
and a narrow range of activity against gram-negative organisms; second-, third-, and
fourth generation agents are progressively more active against gram-negative organisms
and less active against gram-positive organisms.

Mode of action

Cephalosporins are bactericidal and have the same mode of action as other beta-lactam
antibiotics (such as penicillins) but are less susceptible to penicillinases. Cephalosporins
disrupt the synthesis of the peptidoglycan layer of bacterial cell walls. The peptidoglycan
layer is important for cell wall structural integrity. The final transpeptidation step in the
synthesis of the peptidoglycan is facilitated by transpeptidases known as penicillin
binding proteins (PBPs). PBPs bind to the D-Ala-D-Ala at the end of muropeptides
(peptidoglycan precursors) to crosslink the peptidoglycan.

Classification of cephalosporins: Cephalosporins are grouped into "generations" based
on their spectrum of antimicrobial activity in to four groups’ mentioned below.

First generation

First generation cephalosporins are moderate spectrum agents. They are effective
alternatives for treating staphylococcal and streptococcal infections and therefore are
alternatives for skin and soft-tissue infections, as well as for streptococcal pharyngitis.

The first generation cephalosporins are Cefadroxil, Cephalexin, Cephaloridine,
Cephalothin, Cephapirin, Cefazolin, and Cephradine. Cefazolin

Second generation

The second generation cephalosporins have a greater gram-negative spectrum while
retaining some activity against gram-positive bacteria. They are useful agents for treating
upper and lower respiratory tract infections, sinusitis and otitis media. These agents are
also active against E. coli, Klebsiella and Proteus, which makes them potential
alternatives for treating urinary tract infections caused by these organisms.The second
generation cephalosporins are Cefaclor, Cefoxitin, Cefprozil, Cefuroxime.

Third generation

Third generation cephalosporins have a broad spectrum of activity and further increased
activity against gram-negative organisms. Some members of this group (particularly
those available in an oral formulation) have decreased activity against gram-positive
organisms. The parenteral third generation cephalosporins (ceftriaxone and cefotaxime)
OMAR MOHAMUD SALAH NO; 0085 15/1/2010
PHRMACOLOGY ASSIGNMENT

have excellent activity against most strains of Streptococcus pneumoniae, including the
vast majority of those with intermediate and high level resistance to penicillin.

The third generation cephalosporins are Cefdinir, Cefixime, Cefpodoxime, Ceftibuten,
Ceftriaxone, Cefotaxime.

Fourth generation

Fourth generation cephalosporins are extended spectrum agents with similar activity
against gram-positive organisms as first generation cephalosporins. They also have a
greater resistance to beta-lactamases than the third generation cephalosporins. Many can
cross blood brain barrier and are effective in meningitis.

The fourth generation cephalosporins are Cefepime, Cefluprenam, Cefozopran,
Cefpirome, Cefquinome.

Pharmacokinetics

Absorption: Only few cephalosporins (cephatoxin, cephradin, cephadroxil and
cephachlor) are acid stable and thus effective when administered OP. They are
usually well absorbed, the others are administered IV or IM, with plasma
concentrations peaking ~ 30 min after injection.

Distribution: cephalosporins are widely distributed through most body fluids and
tissuesincluding lug, kidney, joints, bones and they are poor penetration in to
cerebrospinal fluid.

Excretion:

Most cephalosporins are excreted by renal tubular secretion although glomulecular
filtration is important in some cases biliary elimination of newer
cephalosporins is significant.

Side effect
• Deahrria with 2nd and 3rd generation
• Hypersensitivity
• Intramuscular injection may can be painful
• Nausea vomiting and dearrhea
• IV may lead to phlebitis
OMAR MOHAMUD SALAH NO; 0085 15/1/2010
PHRMACOLOGY ASSIGNMENT

Clinical use of cephalosporins:

Cephalosporins are used to treat a wide variety of bacterial infections, such as respiratory
tract infections (pneumonia, strep throat, tonsillitis, and bronchitis), skin infections and
urinary tract infections. They are sometimes given with other antibiotics. Cephalosporins
are also commonly used for surgical prophylaxis - prevention of bacterial infection
before, during, and after surgery.

Cephalosporins are active against these organisms

o Salmonella,
o Klebsiella
o Shigella,
o Enterobacter
o Streptococcus,
o Staphylococcus