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Cefaclor
Description
Cefaclor 250: Capsule Purple opaque and white opaque capsule with "hovid"
printed on one end and "CFC250" on the other end of the capsule.
Cefaclor 500 Capsule: Purple opaque and grey opaque capsule with "hovid"
printed on one end and "CFC500" on the other end of the capsule.
Cefaclor 125 mg / 5 ml Granules: Pink, strawberry flavoured granules.
Composition
Cefaclor 250 Capsule: Cefaclor (as monohydrate) 250 mg / capsule
Cefaclor 500 Capsule: Cefaclor (as monohydrate) 500 mg / capsule
Cefaclor 125 mg / 5 ml Granules: Cefaclor (as monohydrate) 125 mg / 5 ml
Actions and Pharmacology
Bactericidal; its action depends on ability to reach and bind
penicillin-binding proteins located in bacterial cytoplasmic membranes.
Cefaclor inhibits bacterial septum and cell wall synthesis, probably by
acylation of membrane-bound transpeptidase enzymes. This prevents
cross-linkage of peptidoglycan chains, which is necessary for bacterial cell
wall strength and rigidity. Also, cell devision and growth are inhibited,
and elongation of susceptible bacteria and lysis frequently occur. Rapidly
dividing bacteria are those most susceptible to the action of cefaclor.
Cefaclor has comparable activity in vitro against most Gram-positive cocci
but is more active against Gram-negative bacteria including Escherichia
coli, Klebsiella pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis and
Haemophilus influenzae.
Pharmacokinetics
Cefaclor is well absorbed from the gastro-intestinal tract. The presence of
food may delay the absorption of cefaclor, but the total amount absorbed is
unchanged. Oral administration of doses of 250, 500 and 1000 mg produce peak
plasma concentrations of about 7, 13 and 23 pg per ml respectively at 0.5 to
1 hour. A plasma half-life of 0.5 to 1 hour has been reported; it may be
slightly prolonged in patients with renal impairment. About 25% is bound to
plasma proteins. Cefaclor appears to be widely distributed in the body; it
crossed the placenta and low concentrations have been detected in breast
milk. It is rapidly excreted by the kidneys; up to 85% of a dose appears
unchanged in the urine within 8 hours; the greater part within 2 hours. High
concentrations of cefaclor are achieved in the urine within 8 hours of a
dose; peak concentrations of 600, 900, and 1900 pg per ml have been reported
after doses of 250, 500 and 1000 mg respectively. Probenecid delays
excretion. Some cefaclor is removed by haemodialysis.
Indications
Cefaclor is indicated for the treatments of the followings caused by
susceptible organisms:
• Bronchitis
• Otitis media
• Pharyngitis, bacterial
• Tonsillitis
• Pneumonia, bacterial
• Skin and soft tissue infections
• Urinary tract infections, bacterial
Contraindications
• Contraindicated in patients with previous allergic reaction (anaphylaxis)
to penicillins, penicillin derivatives, penicillamine, or cephalosporins.
Precautions
• Caution should be exercised to patients with previous hypersensitivity
reactions to cefaclor, cephalosporins, penicillins, penicillin derivatives,
or penicillamine.
Risk-benefit should be considered when the following medical problems exist:
• history of bleeding disorders
• history of gastrointestinal disease, especially ulcerative colitis,
regional enteritis, or antibiotic-associated colitis; pseudomembranous
colitis has been reported with cephalosporins
• hepatic function impairment
• renal function impairment
Prolonged use of Cefaclor may result in the overgrowth of nonsusceptible
organisms. If superinfection occurs during therapy, appropriate measures
should be taken. Positive direct Coombs' tests have been reported during
treatment with the cephalosporin antibiotics.
Use in pregnancy and lactation
Animal studies have shown no evidence of impaired fertility or
teratogenicity. However, since there are no adequate or wellcontrolled
studies in human, caution should be exercised when prescribing for the
pregnant patient. Small amounts of cefaclor have been detected in breast
milk. As the effect on nursing infants is not known, caution should be
exercised when cefaclor is administered to a nursing woman.
Main Side/Adverse Effects
Incidence less frequent or rare include hypoprothrombinemia,
pseudomembranous colitis, allergic reactions (anaphylaxis), erythema
multiforme or Stevens-Johnson syndrome, hearing loss, haemolytic anemia,
hypersensitivity reactions (symptoms including morbilliform eruptions,
pruritus, urticaria, positive Coomb's tests), renal dysfunction, serum
sickness-like reactions, seizures and thrombophlebitis.
Other incidences include:
• Gastrointestinal reactions, headache, oral candidiasis and vaginal
candidiasis.
• Eosinophilia, genital pruritus, monoliasis or vaginitis, thrombocytopenia,
reversible interstitial nephritis.
• Central nervous system (CNS): reversible hyperactivity, agitation,
nervousness, insomnia, confusion, hypertonia, dizziness, hallucinations and
somnolence have been reported rarely.
• Hepatic: slight elevations of ST (SGOT), ALT (SGPT) or alkaline
phosphatase values.
• Hematopoletic: transient lymphocytosis, leukopenia and rarely, haemolytic
anemia, aplastic anemia, agranulocytosis and reversible neutropenia.
• Increased prothrombin time.
• Renal: slight elevations in blood urea (BUN) or serum creatinine or
abnormal urinalysis.
Drug Interactions
• The extent of absorption of cefaclor is decreased with concurrent use of
aluminium hydroxide or magnesium-containing antacids.
• Concurrent use of cefaclor and oral anticoagulants will increase the
anticoagulant effect. There have been rare reports of increased prothrombin
time in patients receiving cefaclor and warfarin concomitantly.
• Renal excretion of cefaclor is inhibited by probenecid.
• A false-positive reaction for glucose in the urine may occur with
Benedict's of Fehling's solutions or with copper sulphate test tables.
Overdose
Symptoms of nausea, vomiting, epigastric distress and diarrhoea would be
anticipated.
Treatment for overdosage
Activated charcoal may aid in decreasing the absorption of cefaclor.
Patients in whom intentional overdose is confirmed or suspected should be
referred for psychiatric consultation.
Dosage and Administration
Cefaclor Capsule:
Usual adult and adolescent dose:
Oral, 250 mg to 500 mg every 8 hours up to 2 g per day; however, 4 g per day
have been administered.
For the treatment of acute gonococcal urethritis, a single dose of 3 g
combined with probenecid, 1 g, is given.
Usual paediatric dose: Refer to Cefaclor Granules.
Cefaclor Granules:
Usual adult and adolescent dose: Refer to Cefaclor Capsule.
Usual paediatric dose:
Oral,
Infants and children 1 month of age and older: 20 mg per kg of body weight
daily in 3 divided doses. Doses up to 40 mg per kg of body weight per day
have been used but maximum dose should not exceed 1 g per day.
Infants up to 1 month of age: Safety and efficacy have not been established.
Note: The information given here is limited. For further information,
consult your doctor or pharmacist.
Storage
Store below 25°C .
Protect from light and moisture.
Granules - After reconstitution, the suspension should be stored in
refrigerator and be used within 10 days.
Presentation/Packing
Capsule - Bottle of 100's; blister packs of 10 x 10's
Granules - Bottle of 60 ml |
