Cefaclor

Generic name Cefaclor

Brand name Ceclor, Raniclor
Drug Classification Antimicrobial Agent
Subclassification 2ND GEN CEPHALOSPORINS
General chemistry
a semi-synthetic, broad-spectrum antibiotic derivative of cephalexin

Gen Mechanism of - Inhibits transpeptidation step of peptidoglycan synthesis.

action Active against H influenzae but not against serratia or B fragilis. Bind
to bacterial cell wall membrane, causing cell death.
- Cefaclor, like the penicillins, is a beta-lactam antibiotic. By
binding to specific penicillin-binding proteins (PBPs) located inside the
bacterial cell wall, it inhibits the third and last stage of bacterial cell
wall synthesis. Cell lysis is then mediated by bacterial cell wall
autolytic enzymes such as autolysins. It is possible that cefaclor
interferes with an autolysin inhibitor.

ABSORPTION
Absorption Well absorbed after oral administration, independent of food intake.
Onset Rapid onser after oral administration
Duration of action 6-12 hr (Oral)
Cmax
Tmax 30-60min (PO)
Steady state
Bioavailability 30-40%
First-pass
Protein Binding 23.5%
Distribution
Distribution Widely distributed; cross the placenta, and they are found in high
concentrations in synovial and pericardial fluids
Vd
Metabolism
Metabolism No appreciable biotransformation in liver
Metabolites
Excretion
Excretion Approximately 60% to 85% of the drug is excreted unchanged in the
urine within 8 hours, the greater portion being excreted within the
first 2 hours.
Total body
clearance
t1/2 30-60min (PO)
Indication Treatment of otitis media, pharyngitis & tonsillitis, acute bacterial
exacerbations of chronic bronchitis, secondary bacterial infections of
acute bronchitis, pneumonia, uncomplicated skin & skin structure
infections, lower UTI
Or
Lower respiratory infections, including pneumonia, bronchitis and
exacerbations of chronic bronchitis.

Upper respiratory infections, including pharyngitis, tonsillitis and

otitis media.

Skin and skin structure infections.

Urinary tract infections, including pyelonephritis and cystitis.

Cefaclor has been shown to be active against most strains of the

following organisms both in vitro and in clinical infections:

Staphylococci, including coagulase-positive and penicillinase-

producing strains (but not methicillin-resistant strains of Staph.
aureus). Streptococcus pyogenes (group A beta-haemolytic
streptococci). Streptococcus (Diplococcus) pneumoniae Escherichia
coli Proteus mirabilis Klebsiella sp Haemophilus influenzae
Neisseria gonorrhoeae (penicillinase-producing and non-penicillinase
producing strains). Moraxella (branhamella) catarrhalis
contraindication hypersensitivity to cephalosporin and penicillin
Adverse Effects Most common: diarrhea, rashes, pain, phlebitis at IV site; Life
threatening: seizures, pseudomembranous colitis, anaphylaxis, serum
sickness
Special Renal impairment; geriatric patients due to decrease in renal function
precautions In penicillin-sensitive patients, cephalosporin antibiotics should be
administered cautiously
Individuals with a history of gastrointestinal disease, particularly
colitis.
Drug interaction Antacid decrease absorption of cefaclor.
Probenecid decreases excretion, increases blood levels
Drug formulation
Dosage & PO (Adults): 250500mg q 8 hr or 375500 mg q 12 hr as extended-
Administrations release tablets
PO (Children >1 mo): 6.713.4 mg/kg q 8 hr or 1020 mg/kg q 12 hr
(up to 1 g/day).

OR
PO:
Adults-The usual adult dosage is 250 mg every 8 to 12 hours. For
bronchitis and pneumonia, the dosage is 250 mg administered 3
times daily. For more severe infections or those caused by less
susceptible organisms, doses may be doubled (500 mg 8 hourly).
Doses of 2 g/day should not be exceeded.

For skin and skin structure infections the dosage is 250 mg 2-3 times
a day.
 Children-The usual recommended daily dosage for children with mild
to moderate infections is 20 mg/kg/day in divided doses every 8
hours (maximum 1 g/day).

For streptococcal pharyngitis/tonsillitis and impetigo, 12 hourly

administration appears equally effective.

In more serious infections, otitis media, and infections caused by less

susceptible organisms, the recommended dosage is 40 mg/kg/day in
divided doses every 8 to 12 hours (maximum 2 g/day). For otitis
media, 12 hourly administration appears equally effective.
Storage Store at 20-25C.