Zefclav Dry

Uses

Cefadroxil Monohydrate (Cefadroxil Monohydrate) is used for the treatment of patients with infection caused by susceptible strains of the designated organisms in the following diseases:

*Upper respiratory tract infections caused by Streptococcus pyogenes (Group A beta-hemolytic Streptococci) and Streptococcus pneumoniae.

* Urinary tract infections caused by E. coli, Proteus mirabilis, and Klebsiella species.

* Skin and soft tissue infections caused by Staphylococci (including penicillinase producing strains) and Streptococci.

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.

Zefclav Dry is also used to associated treatment for these conditions: Bacterial Infections, Infection and inflammatory reaction due to internal prosthetic device, implant, and graft, Skin and Subcutaneous Tissue Bacterial Infections, Streptococcal Pharyngitis, Streptococcal tonsillitis, Urinary Tract InfectionAcute 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 Zefclav Dry works

Like all beta-lactam antibiotics, cefadroxil binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, causing the inhibition of 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 cefadroxil 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

Zefclav Dry dosage

The bioavailability and consequent chemotherapeutic effects of Cefadroxil are unaffected by foods. It may, therefore, be taken with meals or on an empty stomach. Administration with food may be helpful in diminishing potential gastrointestinal complaints occasionally associated with oral cephalosporin therapy.IndicationAdult (dose)Children (Dose)

Upper respiratory tract Infections

1 gm per day in single (q.d.) or divided doses (b.i.d.) for 10 days 12 hourly

30 mg/kg/day in a single or in equally divided doses every 12 hours

Urinary Tract Infections

1 or 2 gm per day in single (q.d.) or divided doses (b.i.d.)

30 mg/kg/day in equally divided doses every 12 hours

For all other UTIs

2 gm per day in divided doses (b.i.d)

30 mg/kg/day in equally divided doses every 12 hours

Skin & soft tissue Infections

1 gm per day in single (q.d.) or divided doses (b.i.d.)

30 mg/kg/day in equally divided doses every 12 hours

Prophylaxis against bacterial endocarditis

2 gm 1 hour prior to the procedure

50 mg/kg 1 hour prior to the procedure

Direction for Reconstitution of suspension

For 100 ml suspension and 100 ml DS suspension: Add 65 ml (13 measuring spoonful) of boiled and cooled water to the dry mixture in the bottle. For ease of preparation add water to the bottle in two portions. Shake well after each addition until all the powder is in suspension.

For 60 ml suspension: Add 40 ml (8 measuring spoonful) of boiled and cooled water to the dry mixture in the bottle. For ease of preparation add water to the bottle in two portions. Shake well after each addition until all the powder is in suspension.

Paediatric Drops: Add 10 ml (2 measuring spoonful) to the bottle and shake vigorously.

Note: Shake both oral suspension and paediatric drops well before each use. Keep the bottle tightly closed. The reconstituted suspension should be stored in a cool and dry place, preferably in refrigerator and unused portion should be discarded after 14 days.

Side Effects

Generally cefadroxil is well tolerated. However, the most commonly reported side effects are gastrointestinal disturbances and hypersensitivity phenomena. Side effects including nausea, vomiting, diarrhoea, dyspepsia, abdominal discomfort, fever, dizziness, headache, arthralgia may also occur.

Toxicity

Nausea, vomiting, diarrhoea, allergic rashes may occur

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

History of hypersensitivity to penicillins or any other β-lactam drugs. History of GI disease (particularly colitis), severe allergies or asthma. Renal impairment. Pregnancy and lactation.

Interaction

There is no known clinically important drug interactions with Cefadroxil.

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

Cefadroxil is well absorbed on oral administration; food does not interfere with its absorption.

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

1.5 hours

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

Over 90% of the drug is excreted unchanged in the urine within 24 hours. Cefadroxil was detected in the placenta and breast milk.

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

Cefadroxil (Cefadroxil Monohydrate) is widely used as a first-line oral antibiotic for the treatment of uncomplicated urinary tract infections in pregnant women.

Contraindication

Cefadroxil is contraindicated in patients with a history of hypersensitivity to any of the ingredients.

Acute Overdose

If amounts >250 mg/kg is ingested, gastric lavage or simulation of vomiting is appropriate.

Storage Condition

Store between 20-25°C. Reconstituted powder for suspension: Store between 2-8°C.

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