Cefaclor (as cefaclor monohydrate) ….. 375 mg
Excipients: q.s ………………………………. 1 tablet
Slow-release film-coated tablet.
Product description: A capsule-shaped, yellow, film-coated tablet, plain on both sides and undamaged edges.
Box of 1 blister x 10 slow-release film-coated tablets.
ATC code: J01DC04
Kefcin 375 SR with the active ingredient Cefaclor is a semi-synthetic second-generation cephalosporin antibiotic with the bactericidal action resulting from inhibition of cell-wall synthesis.
Cefaclor is in vitro active against Gram-positive cocci similar to that of cephalexin but is reported to be more active against Gram-negative bacteria especially Haemophilus influenzae and Moraxella catarrhalis, including beta-lactamase-producing strains of H. influenzae and M. catarrhalis. It may be less resistant to beta-lactamase-producing and penicillinase-producing staphylococci than cephalexin.
Cefaclor is active against the following organisms in vitro, isolated from the patient:
Aerobes, Gram-positive: Staphylococci, including coagulase-positive, coagulase-negative, and penicillinase-producing strains; staphylococci exhibit cross-resistance between cefaclor and methicillin-type antibiotics. Streptococcus pneumonia; Streptococcus pyogenes (group A beta-hemolytic streptococci); Propionibacterium acnes; Corynebacterium diphtheriae.
Aerobes, Gram-negative: Moraxella catarrhali; Haemophilus influenzae (including beta-lactamase-producing, ampicillin-resistant strains); Escherichia coli; Proteus mirabilis; Klebsiella spp.; Citrobacter diversus; Neisseria gonorrhoeae;
Anaerobes: Bacteroides spp. (excluding Bacteroides fragilis); Peptococcus; Peptostreptococcus.
Cefaclor has no activity against Pseudomonas spp. or Acinobacter spp., methicillin-resistant staphylococci and all strains of enterococci (eg, Enterococcus faecalis as well as most of Enterobacter spp.), Serratia spp., Morganella morganii, Proteus vulgaris and Providencia rettgeri.
Resistance:
Resistance to cefaclor is primarily through hydrolysis of beta-lactamases, alteration of penicillin-binding proteins (PBPs) and decreased permeability.
These mechanisms of drug resistance are mostly due to genetic alterations or mutations in chromosome or transmittance via a plasmid or transposon.
Currently, some strains of susceptible bacteria have become resistant to cefaclor and second-generation cephalosporin antibiotics, particularly penicillin-resistant strains of Streptococcus pneumoniae, extended spectrum beta-lactamase-producing (ESBL) strains of Klebsielle pneumoniae and E. coli.
Absorption
Administered one hour after the end of the meal, the relative bioavailability of cefaclor SR is 91 to 94%, compared to standard cefaclor. It is therefore recommended to take this medicine in a meal or at most one hour after.
Distribution
Following administration of 375 mg, 500 mg and 750 mg tablets to fed subjects, average peak serum concentrations of 4, 8 and 11 micrograms/ml respectively, were obtained within 2.5 to 3 hours. No drug accumulation was noted when this was given twice daily.
Metabolism and excretion
There is no evidence of metabolism in humans. Plasma half-life in healthy subjects is independent of dosage form and averages 1 hour. Elderly subjects with normal, mildly diminished renal function, do not require dosage adjustment, since higher peak plasma concentrations and AUC had no apparent clinical significance.
Cefaclor should be used with caution in machine users, drivers, workers at height, and other cases.
Pregnancy
Although animal studies have shown no evidence of impaired fertility or harm to the foetus due to cefaclor, there are no adequate and well-controlled studies in pregnant women. Cefaclor should be used during pregnancy only if clearly needed.
Breast-feeding
Small amounts of cefaclor have been detected in breast milk following administration of single 500 mg doses. Average levels of about 0.2 micrograms/ml or less were detected up to 5 hours later. Trace amounts were detected at one hour. As the effect on nursing infants is not known, caution should be exercised when cefaclor is administered to a nursing woman.
In patients receiving cefaclor and warfarin concomitantly, regular monitoring of prothrombin time should be considered, with adjustment of dosage if necessary.
The extent of absorption of cefaclor (a slow-release film-coated tablet) is diminished if magnesium hydroxide or aluminium hydroxide-containing antacids are taken within 1 hour of administration. H2 blockers do not alter either the rate or extent of absorption.
The renal excretion of cefaclor is inhibited by probenecid.
The majority of adverse reactions were mild and transient. Drug-related adverse reactions requiring discontinuation of therapy occurred in 1.7% of patients. The following adverse reactions were reported in clinical trials. Incidence rates were less than 1%, except as stated:
Gastro-intestinal: Diarrhoea (3.4%), nausea (2.5%), vomiting and dyspepsia.
Hypersensitivity: Rash, urticaria or pruritus occurred in approximately 1.7% of patients. One serum sickness-like reaction (0.03%) was reported among the 3,272 patients treated with cefaclor (slow-release film-coated tablet) during the controlled clinical trials.
Serum sickness-like reactions (erythema multiforme minor, rashes or other skin manifestations accompanied by arthritis/arthralgia, with or without fever) have been reported with cefaclor. Lymphadenopathy and proteinuria are infrequent, there are no circulating immune complexes and no evidence of sequelae. Occasionally, solitary symptoms may occur, but do not represent a serum sickness-like reaction. Serum sickness-like reactions are apparently due to hypersensitivity and have usually occurred during or following a second (or subsequent) course of therapy with cefaclor. Such reactions have been reported more frequently in children than in adults. Signs and symptoms usually occur a few days after initiation of therapy and usually subside within a few days of cessation of therapy. Antihistamines and corticosteroids appear to enhance resolution of the syndrome. No serious sequelae have been reported.
Haematological and lymphatic systems: Eosinophilia.
Genitourinary: Vaginal moniliasis (2.5%) and vaginitis (1.7%).
The following adverse effects have been reported, but causal relationship is uncertain:
Central nervous system: Headache, dizziness and somnolence.
Hepatic: Transient elevations in AST, ALT and alkaline phosphatase.
Renal: Transient increase in BUN or creatinine.
Laboratory tests: Transient thrombocytopenia, leucopenia, lymphocytosis, neutropenia and abnormal urinalysis.
In addition to the adverse reactions listed above that have been observed in patients taking cefaclor, the following have been reported in patients treated with cefaclor:
Erythema multiforme, fever, anaphylaxis (may be more common in patients with a history of penicillin allergy), Stevens-Johnson syndrome, positive direct Coombs' test and genital pruritus. Symptoms of pseudomembranous colitis may appear either during or after antibiotic treatment. Anaphylactoid events may present as solitary symptoms, including angioedema, asthenia, oedema (including face and limbs), dyspnoea, paraesthesias, syncope, orvasodilatation.
Rarely, hypersensitivity symptoms may persist for several months.
The following reactions have been reported rarely in patients treated with cefaclor:
Toxic epidermal necrolysis, reversible interstitial nephritis, hepatic dysfunction, including cholestasis, increased prothrombin time in patients receiving cefaclor and warfarin concomitantly, reversible hyperactivity, agitation, nervousness, insomnia, confusion, hallucinations, hypertonia, aplastic anaemia, agranulocytosis and haemolytic anaemia.
The following adverse reactions have been reported in patients treated with other beta-lactam antibiotics:
Colitis, renal dysfunction and toxic nephropathy.
Several beta-lactam antibiotics have been implicated in triggering seizures, particularly in patients with renal impairment when the dosage was not reduced. If seizures associated with drug therapy should occur, the drug should be discontinued. Anticonvulsant therapy can be given if clinically indicated.
Please inform your doctor of all undesirable effects upon drug administration.
The toxic symptoms following an overdose of cefaclor may include nausea, vomiting, epigastric distress, and diarrhea. The severity of the epigastric distress and the diarrhea are dose-related. If other symptoms are present, it is probable that they are secondary to an underlying disease state, an allergic reaction, or the effects of other intoxication.
In managing overdosage, consider the possibility of multiple drug overdoses, interaction among drugs, and unusual drug kinetics in your patient. Unless 5 times the normal dose of cefaclor has been ingested, gastrointestinal decontamination will not be necessary. Protect the patient's airway and support ventilation and perfusion. Absorption of drugs from the gastrointestinal tract may be decreased by giving activated charcoal, which, in many cases, is more effective than emesis or lavage; consider charcoal instead of or in addition to gastric emptying. Forced diuresis, peritoneal dialysis, hemodialysis have not been established as beneficial for an overdose of cefaclor.
Store in dry places, not exceeding 300C, protect from light.
24 months from the manufacturing date.
Before instituting therapy with cefaclor, every effort should be made to determine whether the patient has had previous hypersensitivity reactions to cefaclor, the cephalosporins, penicillins or other drugs. Cefaclor should be given cautiously to penicillin-sensitive patients and to any patient who has demonstrated some form of allergy, particularly to drugs.
If an allergic reaction to cefaclor occurs, the drug should be discontinued and the patient treated with the appropriate agents.
Pseudomembranous colitis has been reported with virtually all broad-spectrum antibiotics, including macrolides, semi-synthetic penicillins and cephalosporins. It is important, therefore, to consider its diagnosis in patients who develop diarrhoea in association with the use of antibiotics. Such colitis may range in severity from mild to life-threatening. Mild cases usually respond to drug discontinuance alone. In moderate to severe cases, appropriate measures should be taken.
Prolonged use of cefaclor may result in the overgrowth of non-susceptible organisms. If superinfection occurs during therapy, appropriate measures should be taken.
A false-positive reaction for glucose in the urine may occur with Benedict's or Fehling's solutions or with copper sulphate test tablets.
The medicinal product contains mannitol which can cause mild laxative status.
Kefcin 375 SR is indicated in the treatment of the following infections when caused by susceptible strains of the designated organisms:
Acute bronchitis and acute exacerbations of chronic bronchitis caused by Streptococcus pneumoniae, Haemophilus influenzae (including beta-lactamase producing strains), Haemophilus parainfluenzae, Moraxella catarrhalis (including beta-lactamase producing strains) and Staphylococcus aureus.
Pharyngitis and tonsillitis caused by Streptococcus pyogenes (group A streptococci).
Pneumonia caused by S. pneumoniae, H. influenzae (including beta-lactamase producing strains) and M. catarrhalis (including beta-lactamase producing strains).
Uncomplicated lower urinary tract infections, including cystitis and asymptomatic bacteriuria, caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and Staphylococcus saprophyticus.
Skin and skin structure infections caused by S. pyogenes (group A streptococci), S. aureus (including beta-lactamase producing strains) and Staphylococcus epidermidis (including beta-lactamase producing strains).
Bacteriological studies, to determine the causative organism and its susceptibility to cefaclor, should be performed. Once these results become available, antimicrobial therapy should be adjusted accordingly.
A known history of hypersensitivity to the cephalosporin antibiotics or any ingredients of the drug.
Cefaclor is administered orally. The tablets should not be cut, crushed or chewed. The drug should be taken with meals.
Adults and the elderly:
Pharyngitis, tonsillitis, skin and skin structure infections: 375 mg twice daily.
Lower urinary tract infections: 375 mg twice daily or 500 mg once daily.
Bronchitis: 375mg or 500mg twice daily.
Pneumonia: 750mg twice daily. The therapy should be 14 days.
Elderly subjects with normal renal function do not require dosage adjustment.
The safety and efficacy of cefaclor (slow-release film-coated tablet) in children have not been established.
In the treatment of infections caused by S. pyogenes (group A streptococci), a therapeutic dosage should be administered for at least 10 days.
Or as directed by the physician.
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