Sitex

Uses

Pharyngitis/tonsillitis caused by Streptococcus pyogenes

Acute bacterial otitis media caused by Streptococcus pneumoniae, Haemophilus influenzae (including beta lactamase-producing strains), Moraxella Catarrhalis (including beta-lactamase-producing strains) or Streptococcus pyogenes

Acute bacterial maxillary sinusitis caused by Streptococcus pneumoniae or Haemophilus influenzae (non-beta-lactamase-producing strains only)

Lower respiratory tract infections including pneumoniae, caused by Streptococcus pneumoniae, Haemophilus influenzae (including beta lactamase-producing strains), Klebsiella spp., Staphylococcus aureus (penicillinase- and non-penicillinase-producing strains), Streptococcus pyogenes, Escherichia coli

Acute bacterial exacerbations of chronic bronchitis and secondary bacterial infections of acute bronchitis caused by Streptococcus penumoniae, Haemophilus influenzae (beta-lactamase negative strains) or Haemophilus parainfluenzae (beta-lactamase negative strains)

Skin and Skin-Structure Infections caused by Staphylococcus aureus (penicillinase- and non-penicillinase-producing strains), Streptococcus pyogenes, Escherichia coli, Klebsiella spp. and Enterobacter spp.

Urinary tract infections caused by Escherichia coli or Klebsiella pneumoniae

Bone and Joint Infections caused by Staphylococcus aureus (penicillinase and non-penicillinase producing strains)

Gonorrhea: Uncomplicated and disseminated gonococcal infections due to Neisseria gonorrhoeae (penicillinase- and non-penicillinase-producing strains) in both males and females

Early Lyme disease (erythema migrans) caused by Borrelia burgdorferi

Septicemia caused by Staphylococcus aureus (penicillinase and non-penicillinase producing strains), Streptococcus pneumoniae, Escherichia coli, Haemophilus influenzae (including ampicillin-resistant strains), and Klebsiella spp.

Meningitis caused by Streptococcus pneumoniae, Haemophilus influenzae (including ampicillin resistant strains), Neisseria meningitidis and Staphylococcus aureus (penicillinase and non-penicillinase producing strains)

Switch therapy (injectable to oral) after surgery when patient’s condition is improved.

Sitex is also used to associated treatment for these conditions: Acute Bacterial Exacerbation of Chronic Bronchitis (ABECB), Animal bite, Bacterial Infections, Bloodstream Infections, Bone and Joint Infections, Gonorrhea, Impetigo, Lower Respiratory Tract Infection (LRTI), Lyme Disease, Maxillary Sinusitis, Meningitis, Skin and Subcutaneous Tissue Bacterial Infections, Urinary Tract Infection, Bacterial otitis media, Mild Streptococcal pharyngitis, Mild Streptococcal tonsillitis, Moderate Streptococcal pharyngitis, Moderate Streptococcal tonsillitisAcute Cystitis, Acute Uncomplicated Pyelonephritis, Bacterial Infections, Bacterial Pneumonia, Bacterial infection due to streptococcus, group A, Bloodstream Infections, Bone and Joint Infections, Bronchitis, Cysto-Urethritis, Gonorrhoea, Gynaecological infection, Haemophilus Influenzae, Infection Due to Escherichia Coli, Intraabdominal Infections, Lower Respiratory Infection, Lower Respiratory Tract Infection (LRTI), Moraxella catarrhalis, Otitis Media (OM), Pharyngitis, Proteus mirabilis, Sinusitis, Skin and skin structure infections, Streptococcus Pneumoniae, Tonsillitis, Upper Respiratory Tract Infection, Urinary Tract Infection, Skin and skin-structure infections, Susceptible Bacterial Infections

How Sitex works

Cefuroxime, 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 cefuroxime interferes with an autolysin inhibitor.

Clavulanic acid contains a beta-lactam ring in its structure that binds in an irreversible fashion to beta-lactamases, preventing them from inactivating certain beta-lactam antibiotics, with efficacy in treating susceptible gram-positive and gram-negative infections.

Dosage

Sitex dosage

Adolescents & adults:

Pharyngitis or Tonsillitis: 250 mg twice daily 5-10 days

Acute bacterial maxillary sinusitis: 250 mg twice daily 10 days

Acute bacterial exacerbation of chronic bronchitis: 250-500 mg twice daily 10 days

Secondary bacterial infections of acute bronchitis: 250-500 mg twice daily 5-10 days

Community acquired pneumonia: 250-500 mg twice daily 5-10 days

Uncomplicated skin & skin-structure infections: 250-500 mg twice daily 10 days

MDR Typhoid fever: 500 mg twice daily 10-14 days

Uncomplicated urinary tract infection: 250 mg twice daily 7-10 days

Uncomplicated gonorrhea: 1000 mg single dose

Lyme disease: 500 mg twice daily 20 days

Paediatric patients (3 months to 12 years)

Pharyngitis or Tonsillitis: 20 mg/kg/day in two divided doses 5-10 days

Acute otitis media: 30 mg/kg/day in two divided doses 10 days

Acute bacterial maxillary sinusitis: 30 mg/kg/day in two divided doses 10 days

Community acquired pneumonia: 30 mg/kg/day in two divided doses 5-10 days

MDR Typhoid fever: 30 mg/kg/day in two divided doses 10-14 days

Uncomplicated skin & skin-structure infections: 30 mg/kg/day in two divided doses 10 days

Uncomplicated urinary tract infection: 20 mg/kg/day in two divided doses 7-10 days

Cefaclav may be administered without regard to meals.

Direction for reconstitution of suspension:

Shake the bottle well to loosen the powder. Add 35 ml of boiled and cooled water to the dry powder of the bottle. For ease of preparation, add water to the bottle in two proportions. Shake the bottle well after each addition until all the powder is in suspension.

Note: The reconstituted suspension must be stored at 2-8 °C temperature and should be used within 7 days after reconstitution. Shake the suspension well before each use. Keep the bottle tightly closed.

Cefuroxime & Clavulanic Acid may be administered without regard to meals.

Side Effects

Generally Cefuroxime and Clavulanic acid are well tolerated. However, a few side effects like nausea, vomiting, diarrhea, abdominal discomfort or pain may occur. As with other broad-spectrum antibiotics, prolonged administration of Cefuroxime and Clavulanic acid combination may result in overgrowth of nonsusceptible microorganisms. Rarely (<0.2%) renal dysfunction, anaphylaxis, angioedema, pruritis, rash and serum sickness like urticaria may appear.

Toxicity

Allergic reactions might be expected, including rash, nasal congestion, cough, dry throat, eye irritation, or anaphylactic shock. Overdosage of cephalosporins can cause cerebral irritation leading to convulsions.

LD50 information

Clavulanic acid has demonstrated low oral acute toxicity in adult rodents, having an LD50 of more than 2000 mg/kg. The toxicity of clavulanic acid on pre-weaning rats was also studied. Gastrointestinal disturbance and mortality occurred, even at lower clavulanic acid doses of 125 mg/kg.

Overdose information

Overdose information has been obtained for the combination of amoxicillin and clavulanic acid, as these drugs are frequently administered together in a single product. Changes in fluid and electrolyte balances and gastrointestinal symptoms may occur in the case of an overdose. Offer symptomatic treatment or gastrointestinal disturbances, while considering the importance of fluid and electrolyte balance. This drug may be removed by a session of hemodialysis. When coadministered with amoxicillin, crystalluria causing renal failure has been observed. Seizures may also occur in a case of overdose, or in a patient with renal failure.

Precaution

Cefaclav should be given with care to patients receiving concurrent treatment with potent diuretics & who have history of colitis.

Interaction

Probenecid: Concomitant administration of probenecid with Cefuroxime increases the area under the serum concentration versus time curve by 50%. The peak serum Cefuroxime concentration after a 1.5 gm single dose is greater when taken with 1 gm of probenecid than without probenecid.

Antacids: Drugs that reduce gastric acidity may result in a lower bioavailability of Cefuroxime and Clavulanic acids compared with that of fasting state and tend to cancel the effect of postprandial absorption.

Oral contraceptives: In common with other antibiotics, Cefuroxime may affect the gut flora, leading to lower estrogen re absorption and reduced efficacy of combined oral estrogen/ progesterone.

Volume of Distribution

A study in 4 healthy volunteers administered a radiolabeled dose of clavulanic acid determined a volume of distribution of 12L.Clavulanic acid is distributed to various tissues and interstitial fluid. Clinically significant concentrations have been measured in the gallbladder, abdomen, skin, fat, and muscle tissues. Bile, pus, synovial and peritoneal fluids are also found to have therapeutic concentrations of clavulanic acid. Studies of animals have demonstrated that clavulanic crosses the placenta.

Elimination Route

Absorbed from the gastrointestinal tract. Absorption is greater when taken after food (absolute bioavailability increases from 37% to 52%).

Clavulanic acid, when taken orally, is well absorbed in the gastrointestinal tract. After administration of radiolabeled clavulanic acid to four human subjects, a minimum of 73% absorption and the average absolute bioavailability was calculated at 64%. The mean Cmax in a group of 8 healthy research volunteers was 2.098 ± 0.441 micrograms/ml in a pharmacokinetic study. The same study reported a mean Tmax of 1.042 ± 0.80 hours. Tmax is reported to be 40-120 minutes according to another pharmacokinetic study.

Half Life

Approximately 80 minutes following intramuscular or intravenous injection.

The half-life of clavulanic acid is reported to be similar to amoxicillin, and last 45-90 minutes. A study of radiolabeled clavulanic acid administered to 4 healthy volunteers determined a half-life of 0.8 h.

Clearance

The clearance of clavulanic acid in a pharmacokinetic study of 4 healthy volunteers administered a radiolabeled dose of clavulanic acid was 0.21 l/min. Another resource indicates the average clearance of clavulanic acid is 12.20 liters/h/70 kg. Dose adjustments may be required in patients with renal failure.

Elimination Route

About 40 to 65% of the clavulanic acid is excreted as unchanged drug in urine during the first 6 hours following ingestion. The metabolites of clavulanic acid are found to be excreted in the urine and feces and as carbon dioxide in expired air. Clavulanate is cleared by both renal and non-renal processes. About 17% of radiolabeled dose of clavulanic acid was found to be exhaled in expired air and 8% of a dose was found to be excreted in the feces.

Pregnancy & Breastfeeding use

During pregnancy: While all antibiotics should be avoided in the first trimester if possible. However, Cefaclav can be safely used in later pregnancy to treat urinary and other infections.

During lactation: Cefaclav is excreted into the breast milk in small quantities. However, the possibility of sensitizing the infant should be kept in mind.

Contraindication

It is contraindicated in patients with known allergy to Cefuroxime and Clavulanic acid or to the cephalosporin group of antibiotics.

Acute Overdose

Signs and symptoms: Overdosage of Cefaclav can cause cerebral irritation leading to convulsions.

Management: Serum levels of Cefaclav can be reduced by haemodialysis and peritoneal dialysis.

Interaction with other Medicine

Concomitant administration of probenecid with Cefaclav increases the area under the serum concentration versus time curve by 50%. Drug that reduces gastric acidity may result in a lower bioavailability of Cefuroxime and tend to cancel the effect of postprandial absorption.

Storage Condition

Should be kept in a cool (15–30°C) and dry place and protected from light.

Innovators Monograph

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