Fastclav Dt

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 (nonbeta-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 Neiseria 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), Neisseira menintitidis, and Staphylococcus aureus (penicillinase- and non-penicillinase-producing strains).

- Surgical Prophylaxis: Prophylaxis against infections in abdominal, pelvic, orthopedic, cardiac, pulmonary, esophageal and vascular surgery where there is increased risk for infection.

Clavulanic acid is a beta lactamase inhibitor used to enhance the effectiveness of beta lactam antibiotics.

Clavulanic acid combined with other antibiotics is indicated to prevent the development of drug-resistant strains of bacteria and promotes their therapeutic antibacterial effects.

The following conditions, when they produced beta-lactamases, have been treated with a combination of amoxicillin and clavulanic acid or ticarcillin and clavulanic acid:

Acute otitis media caused by H. influenzae and M. catarrhalis

Sinusitis due to H. influenzae and M. catarrhalis

Lower respiratory tract infections due to Haemophilus influenzae, S.aureus, Klebsiella species, and Moraxella catarrhalis

Skin and skin structure infections caused by Staphylococcus aureus, Escherichia coli, and Klebsiella species

Urinary Tract Infections due to E. coli, Klebsiella species of bacteria, and Enterobacter species of bacteria, S.marcescens, or S.aureus

Gynecologic infections due to a variety of bacteria, including P.melaninogenicus, Enterobacter species, E.Coli species, Klebsiella species, S. aureus, S.epidermidis

Septicemia due to a variety of bacteria, including Klebsiella species, E.Coli species, S.aureus, or Pseudomonas species

Bone and joint infections due to S.aureus

Intraabdominal infections due to E.Coli, K.pnemoniae, or B.fragilis group

A note on susceptibility

It should be noted that it is only to be administered in infections that are confirmed or highly likely to be caused by susceptible bacteria. Culture and susceptibility tests should be performed if possible and used in selecting whether this antibiotic is prescribed. When beta-lactamase enzyme production is not detected during microbiological testing, clavulanic acid should not be used. When these tests are not available patterns of local infection and susceptibility may be used to determine the appropriateness of using clavulanic acid. Ticarcillin with clavulanate has shown particular efficacy in mixed infections in addition to empiric therapy before determining the susceptibility of causative organisms. The ticarcillin-clavulanic acid combination may prove to be an effective single-agent antibiotic therapy to treat infections where a regimen of several drugs may normally be used.

Fastclav Dt 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 Fastclav Dt 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

Fastclav Dt dosage

Oral :

INFECTIONS DOSAGE DURATION

Tablet

(May be administered without regard to meals)

Adolescents & adults(13 years & above)

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

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

Uncomplicated urinary tract infection 125-250 mg twice daily 7-10 days

Uncomplicated gonorrhea 1000 mg single dose - - -

Lyme disease 500 mg twice daily 20 days

Paediatric patients (Upto12 years)

(Who can swallow tablets whole)

Pharyngitis or Tonsillitis 125 mg twice daily 5-10 days Acute otitis media 250 mg twice daily 10 days

Acute bacterial maxillary sinusitis 250 mg twice daily 10 days

Suspension

(Must be administered with food. Shake the bottle

well before each use)

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

Injection :

Adult: 750 mg three times daily by IM or IV injection. In severe infections, dose can be increased upto 1.5 gm three times daily by IV injection. The frequency may be increased to four times daily, if necessary, giving total daily doses of 3 to 6 gms.

Children (above 3 months of age): 30 - 100 mg/kg/day given in 3 or 4 equally divided doses. A dose of 60mg/kg/day is appropriate for most infections.

Neonate: 30 - 100 mg/kg/day given in 2 or 3 equally divided doses.

Surgical prophylaxis: 1.5 gm by IV injection at induction of anaesthesia; up to 3 further doses of 750 mg may be given by IV/IM injection every 8 hours for high risk procedures.

Sequential therapy in adults

Pneumonia: 1.5 gm IV injection twice daily for 2-3 days, followed by 500 mg twice daily (oral) for 7-10 days.

Acute exacerbations of chronic bronchitis: 750 mg twice daily (IM or IV injection) for 2-3 days, followed by 500 mg twice daily (oral) for 5-10 days. (Duration of both parenteral and oral therapy is determined by the severity of the infection and the clinical status of the patient.)

Other recommendations

In Gonorrhoea: Adult: 1.5g as a single dose (as 2 x 750mg injections intramuscularly with different sites, e.g. each buttock).

In Meningitis: Adults: 3gm IV injection three times daily. Children (above 3 months of age): 200-240 mg/kg/day by IV injection in 3 or 4 divided doses reduced to 100 mg/kg/day after 3 days or on clinical improvement. Neonate: 100 mg/kg/day by IV injection reduced to 50 mg /kg/day.

In bone and joint infections: Adult: 1.5 gm IV injection four times daily. Children (above 3 months of age): 150 mg/kg/day (not to exceed the maximum adult dose) in equally divided doses every 8 hours.

In impaired renal function: A reduced dose must be employed when renal function is impaired. Dosage in adults should be determined by the degree of renal impairment and the susceptibility of the causative organism according to the table below -

Creatinine clearance (ml/min) Dose Frequency

> 20 750 mg - 1.5 gm q8h

10-20 750 mg q12h

< 10 750 mg q24h*

* Since Cefuroxime is dialyzable, patients on hemodialysis should be given a further dose at the end of the dialysis.

In paediatric patients with renal insufficiency, the frequency of dosing should be modified consistent with the recommendations for adults.

Directions for reconstitution:

Shake the bottle well to loosen the powder. Add required amount (with the help of supplied measuring cup) of boiled and cooled water to the dry mixture in the bottle. Shake the bottle vigorously until all the powder is in suspension.

Note: Shake the bottle vigorously before each use. Keep the bottle tightly closed. The reconstituted suspension should be stored in a cool and dry place, preferably in a refrigerator and used within 10 days after reconstitution.

Kilbac 250 IM/IV Injection :

Intramuscular injection : Add 1 ml of supplied water for injection BP to the vial and shake.

Intravenous injection: Add 2 ml of supplied water for injection BP to the vial and shake. The solution should be slowly injected directly into a vein over a 3 to 5 minute period.

Kilbac 750 IM/IV Injection :

Intramuscular injection : Add 3 ml of supplied water for injection BP to the vial and shake.

Intravenous injection: Add 8 ml of supplied water for injection BP to the vial and shake. The solution should be slowly injected directly into a vein over a 3 to 5 minute period.

Kilbac 1.5 IV Injection :

Intravenous injection: Add 16 ml of supplied water for injection BP to the vial and shake. The solution should be slowly injected directly into a vein over a 3 to 5 minute period.

Pharmaceutical precaution

Cefuroxime tablet, powder for suspension and vial (for injection) should be kept in a cool (15° - 30°C) and dry place and protected from light.

Side Effects

Generally Cefuroxime is 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 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

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

Interaction

No potentially hazardous interactions have been reported.

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

Pregnancy: While all antibiotics should be avoided in the first trimester if possible. However, Cefuroxime has been safely used in later pregnancy to treat urinary and other infections.

Nursing mothers: Cefuroxime is excreted into the breast milk in small quantities. However, the possibility of sensitizing the infant should be kept in mind

Contraindication

Cefuroxime is contraindicated in patients with known allergy to Cephalosporins.

Acute Overdose

Excessively large doses of all Cephalosporins can cause cerebral irritation and may cause convulsions. This complication is unlikely to occur in routine practice unless the patient is in renal failure. Hemodialysis or peritoneal dialysis can remove Cefuroxime.

Storage Condition

Tablet: Store below 30° C, protected from light and moisture.

Suspension: Store below 25° C, protected from light and moisture.

Injection: Store below 25° C, protected from light and moisture. Use reconstituted solution immediately. The reconstituted solution is stable for 2 hours at room temperature and for 12 hours when refrigerated at 2° - 8° C.

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