Sporidex Cefalexin Oral Suspension

Sporidex® Suspension

125 mg/5 mL & 250 mg/5 mL

(Cefalexin Oral Suspension BP)

For the Use Only of a Registered Medical Practitioner

 

COMPOSITION

Sporidex Suspension 125mg /5 ml

When constituted as directed:

Each 5 mL of the constituted suspension contains:

Cefalexin Monohydrate Ph. Eur.

equivalent to anhydrous Cefalexin 125mg

 

Sporidex Suspension 250mg /5 mL

When constituted as directed:

Each 5 mL of the constituted suspension contains:

Cefalexin Monohydrate Ph. Eur.

equivalent to anhydrous Cefalexin 250mg

Excipients: Sucrose, Sodium Benzoate, Xanthan Gum, Colloidal Anhydrous Silica, Orange Flavour, Pineapple Flavour, Sunset Yellow Supra.

 

DESCRIPTION

Sporidex Suspension contains cefalexin, which is a semisynthetic cephalosporin antibiotic intended for oral administration. It is (6R,7R)-7-[[(2R)-2-Amino-2- phenylacetyI]amino-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid monohydrate. Cefalexin has the molecular formula C16H17N3O4S.H2O and the molecular weight is 365.4.

 

INDICATIONS1,2

Sporidex Suspension is indicated for the treatment of the following infections when caused by susceptible strains of the designated microorganisms:

• Respiratory tract infections caused by Streptococcus pneumoniae and Streptococcus pyogenes (Penicillin is the usual drug of choice in the treatment and prevention of streptococcal infections, including the prophylaxis of rheumatic fever. Cefalexin is generally effective in the eradication of streptococci from the nasopharynx; however, substantial data establishing the efficacy of cefalexin in the subsequent prevention of rheumatic fever are not available at present).

• Otitis media due to Streptococcus pneumoniae, Haemophilus influenzae, Staphylococcus aureus, Streptococcus pyogenes, and Moraxella catarrhalis.

Skin and skin structure infections caused by Staphylococcus aureus and/or Streptococcus pyogenes.

• Bone infections caused by Staphylococcus aureus and/or Proteus mirabilis.

• Genitourinary tract infections, including acute prostatitis, caused by Escherichia coli, Proteus mirabilis, and Klebsiella pneumoniae.

• Dental infections caused by susceptible bacteria.

Note — Culture and susceptibility tests should be initiated prior to and during therapy. Renal function studies should be performed when indicated.

To reduce the development of drug-resistant bacteria and maintain the effectiveness of cefalexin and other antibacterial drugs, cefalexin should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.

 

DOSE AND METHOD OF ADMINISTRATION1,2

Sporidex Suspension may not be able to deliver all approved dose regimens; other approved dosage forms and strengths of cefalexin should be used in such cases. The general dosage recommendation is presented below.

Sporidex Suspension is administered orally.

 

Adults

The adult dosage ranges from 1 to 4 gram daily in divided doses. The usual adult dose is 250 mg every 6 hours. For the following infections, a dosage of 500 mg may be administered every 12 hours: streptococcal pharyngitis, skin and skin structure infections and uncomplicated cystitis in patients over 15 years of age. Cystitis therapy should be continued for 7 to 14 days. For more severe infections or those caused by less susceptible organisms, larger doses may be needed. If daily doses of cefalexin greater than 4 gram are required, parenteral cephalosporins, in appropriate doses, should be considered.

 

Pediatric Patients

The usual recommended daily dosage for pediatric patients is 25 to 50 mg/kg in divided doses. For streptococcal pharyngitis in patients over 1 year of age and for skin and skin structure infections, the total daily dose may be divided and administered every 12 hours.

In severe infections, the dosage may be doubled.

In the therapy of otitis media, clinical studies have shown that a dosage of 75 to 100mg/kg/day in 4 divided doses is required.

In the treatment of beta-hemolytic streptococcal infections, a therapeutic dosage of cefalexin should be administered for at least 10 days.

 

Elderly and Patients with Impaired Renal Function

As for adults. Reduce dosage if renal function is markedly impaired.

 

Directions for Constitution of Cefalexin Oral Suspension

Tap bottle to loosen powder, then add boiled and cooled water up to the mark by adding more water, if necessary.

The constituted suspension should be stored in a refrigerator at a temperature between 2 to 8°C and used within 10 days of constitution.

 

USE IN SPECIAL POPULATIONS1

Pregnancy

Teratogenic effects — US FDA Pregnancy Category B— Reproduction studies have been performed on mice and rats using oral doses of cefalexin monohydrate 0.6 and 1.5 times the maximum daily human dose (66 mg/kg/day) based upon mg/m2, and have revealed no harm to the fetus. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

 

Lactation

The excretion of cefalexin in human breast milk increased up to 4 hours following a 500mg dose. The drug reached a maximum level of 4 µg/mI, then decreased gradually and had disappeared 8 hours after administration. Caution should be exercised when cefalexin is administered to a nursing woman.

 

Pediatrics

The safety and effectiveness of cefalexin in pediatric patients has been established in reported clinical trials.

 

Geriatrics

Of the 701 subjects in 3 published clinical studies of cefalexin, 62% were of age 65 years and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.

This drug is known to be substantially excreted by the kidney and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection and it may be useful to monitor renal function.

 

CONTRAINDICATIONS1,2

Sporidex Suspension is contraindicated in patients with known allergy to the cephalosporin group of antibiotics or any inactive ingredient of the formulation.

 

WARNINGS AND PRECAUTIONS1,2
BEFORE THERAPY WITH CEFALEXIN IS INSTITUTED, CAREFUL INQUIRY SHOULD BE MADE TO DETERMINE WHETHER THE PATIENT HAS HAD PREVIOUS HYPERSENSITIVITY REACTIONS TO CEFALEXIN, CEPHALOSPORINS, PENICILLINS, OR OTHER DRUGS. IF THIS PRODUCT IS TO BE GIVEN TO PENICILLIN-SENSITIVE
PATIENTS, CAUTION SHOULD BE EXERCISED BECAUSE CROSS-HYPERSENSITIVITY AMONG BETA-LACTAM ANTIBIOTICS HAS BEEN CLEARLY DOCUMENTED AND MAY OCCUR IN UP TO 10% OF PATIENTS WITH A HISTORY OF PENICILLIN ALLERGY. IF AN ALLERGIC REACTION TO CEFALEXIN OCCURS, DISCONTINUE THE DRUG. SERIOUS ACUTE HYPERSENSITIVITY REACTIONS MAY REQUIRE TREATMENT WITH EPINEPHRINE AND OTHER EMERGENCY MEASURES, INCLUDING OXYGEN, INTRAVENOUS FLUIDS, INTRAVENOUS ANTIHISTAMINES. CORTICOSTEROIDS, PRESSOR AMINES AND AIRWAY MANAGEMENT, AS CLINICALLY INDICATED.

There is some clinical and laboratory evidence of partial cross allergenicity of the penicillins and the cephalosporins. Patients have been reported to have had severe reactions (including anaphylaxis) to both drugs.

Any patient who has demonstrated some form of allergy, particularly to drugs, should receive antibiotics cautiously. No exception should be made with regard to cefalexin.

 

Clostridium difficile associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including cefalexin and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficlie.

C. difficile produces toxins A and B which contribute to the development of CDAD. Hypertoxin producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy.
CDAD must be considered in all patients who present with diarrhea following antibiotic use. Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial agents.

If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C. difficiie may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of C. difficlie and surgical evaluation should be instituted as clinically indicated.

 

General

Prescribing cefalexin in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.

Patients should be followed carefully so that any side effects or unusual manifestations of drug idiosyncrasy may be detected. If an allergic reaction to cefalexin occurs, the drug should be discontinued and the patient treated with the usual agents (e.g., epinephrine or other pressor amines, antihistamines, or corticosteroids).

Prolonged use of cefalexin may result in the overgrowth of non susceptible organisms. Careful observation of the patient is essential. If superinfection occurs during therapy, appropriate measures should be taken.

Positive direct Coombs’ tests have been reported during treatment with the cephalosporin antibiotics. In hematologic studies or in transfusion cross-matching procedures when antiglobulin tests are performed on the minor side or in Coombs’ testing of newborns whose mothers have received cephalosporin antibiotics before parturition, it should be recognized that a positive Coombs’ test may be due to the drug. Cefalexin should be administered with caution in the presence of markedly impaired renal function. Under such conditions, careful clinical observation and laboratory studies should be made because safe dosage may be lower than that usually recommended.

Indicated surgical procedures should be performed in conjunction with antibiotic therapy.

Broad-spectrum antibiotics should be prescribed with caution in individuals with a history of gastrointestinal disease, particularly colitis.

Cephalosporins may be associated with a fall in prothrombin activity. Those at risk include patients with renal or hepatic impairment, or poor nutritional state, as well as patients receiving a protracted course of antimicrobial therapy and patients previously stabilized on anticoagulant therapy. Prothrombin time should be monitored in patients at risk and exogenous vitamin K administered as indicated.

Effects of cefalexin on ability to drive and use machines are not known.

Sporidex Suspension contains sucrose. Patients with rare hereditary problems of fructose intolerance, glucose/galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine.

Sporidex Suspension contains approximately 2.3 g of sucrose per 5 ml for Cefalexin oral Suspension 125 mg/5 ml and 2.2 g of sucrose per 5 ml for Cefalexin oral Suspension 250 mg/5 ml. This should be taken into account in patients with diabetes mellitus.

 

Information for Patients

Patients should be counseled that antibacterial drugs including cefalexin should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold). When cefalexin is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may (1) decrease the effectiveness of the immediate treatment and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by cefalexin or other antibacterial drugs in the future.

Diarrhea is a common problem caused by antibiotics which usually ends when the antibiotic is discontinued. Sometimes after starting treatment with antibiotics, patients can develop watery and bloody stools (with or without stomach cramps and fever) even as late as two or more months after having taken the last dose of the antibiotic. If this occurs, patients should contact their physician as soon as possible.

 

DRUG INTERACTIONS1

Metformin: In healthy subjects given single 500 mg doses of cefalexin and metformin, plasma metformin mean C, and AUC increased by an average of 34% and 24%, respectively and metformin mean renal clearance decreased by 14%. No information is reported about the interaction of cefalexin and metformin following multiple doses of either drug. The clinical significance of this study is unclear, particularly as no cases of “lactic acidosis” have been reported in association with concomitant metformin and cefalexin treatment. Although not observed in this study, adverse effects could potentially arise from co-administration of cefalexin and metformin by inhibition of tubular secretion via organic cationic transporter systems. Accordingly, careful patient monitoring and dose adjustment of metformin is recommended in patients concomitantly taking cefalexin and metformin.

 

Probenecid: As with other beta-lactams, the renal excretion of cefalexin is inhibited by probenecid.

 

Drug/Laboratory Test Interactions

As a result of administration of cefalexin a false-positive reaction for glucose in the urine may occur. This has been reported with Benedicts and Fehling’s solutions.

 

UNDESIRABLE1,2

Gastrointestinal. Onset of pseudomembranous colitis may occur during or after antibacterial treatment (see WARNINGS AND PRECAUTIONS). Nausea and vomiting have been reported rarely. The most frequent side effect has been diarrhea. It was very rarely severe enough to warrant cessation of therapy. Dyspepsia, gastritis and abdominal pain have also occurred. As with some penicillins and some other cephalosporins, transient hepatitis and cholestatic jaundice have been reported rarely.

Hypersensitivity: Allergic reactions in the form of rash, urticaria, angioedema and, rarely, erythema multiforme, Stevens-Johnson syndrome, or toxic epidermal necrolysis have been reported. These reactions usually subsided upon discontinuation of the drug. In some of these reactions, supportive therapy may be necessary. Anaphylaxis has also been reported.

Other reactions have included genital and anal pruritus, genital moniliasis, vaginitis and vaginal discharge, dizziness, fatigue, headache, agitation, confusion, hallucinations, arthralgia, arthritis and joint disorder. Reversible interstitial nephritis has been reported rarely. Eosinophilia, neutropenia, thrombocytopenia, hemolytic anemia and slight elevations in AST and ALT have been reported.

In addition to the adverse reactions listed above, the following adverse reactions and altered laboratory tests have been reported for cephalosporin class antibiotics:

Adverse reactions; Fever, colitis, aplastic anemia, hemorrhage, renal dysfunction and toxic nephropathy.

Several cephalosporins are 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.

Altered Iaboratoty tests: Prolonged prothrombin time, increased BUN, increased creatinine, elevated alkaline phosphatase, elevated bilirubin elevated LDH, pancytopenia, leukopenia and agranulocytosis.

 

OVERDOSE1,2

Signs and symptoms

Symptoms of oral overdose may include nausea, vomiting, epigastric distress, diarrhea and hematuria. If other symptoms are present, it is probably secondary to an underlying disease state, an allergic reaction, or toxicity due to ingestion of a second medication.

 

Treatment

In the event of severe overdose, general supportive care is recommended, including close clinical and laboratory monitoring of haematological, renal and hepatic functions and coagulation status until the patient is stable.

Unless 5 to 10 times the normal dose of cefalexin has been ingested, gastrointestinal decontamination should not be necessary.

Protect the patient’s airway and support ventilation and perfusion. Meticulously monitor and maintain, within acceptable limits, the patient’s vital signs, blood gases, serum electrolytes, etc. 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. Repeated doses of charcoal over time may hasten elimination of some drugs that have been absorbed. Safeguard the patient’s airway when employing gastric emptying or charcoal.

Forced diuresis, peritoneal dialysis, hemodialysis, or charcoal hemoperfusion have not been established as beneficial for an overdose of cefalexin; however, it would be extremely unlikely that one of these procedures would be indicated.

The oral median lethal dose of cefalexin in rats is >5000 mg/kg.

 

PHARMACODYNAMIC AND PHARMACOKINETIC PROPERTIES2

Pharmacodynamic effects

Mechanism of action

In vitro tests demonstrated that cephalosporins are bactericidal because of their inhibition of cell-wall synthesis.

 

Antibacterial activity

Cefalexin is active against most strains of the following microorganisms both in vitro and in clinical infections as described in the INDICATIONS section.

 

Aerobes, Gram-positive

Staphylococcus aureus (including penicillinase-producing strains)

Streptococcus pneumoniae (penicillin-susceptible strains)

Streptococcus pyogenes

 

Aerobes, Gram-negative

Escherichia coli

Haemophilus influenzae

Klebsiella pneumoniae

Moraxella (Branhamella) catarrhalis

Proteus mirabilis

Note — Methicillin-resistant staphylococci and most strains of enterococci (Enterococcus faecalis [formerly Streptococcus faecalis]) are resistant to cephalosporins, including cefalexin. It is not active against most strains of Enterobacter spp., Morganella morganii and Proteus vulgaris. It has no activity against Pseudomonas spp. or Acinetobacter calcoaceticus. Penicillin resistant Streptococcus pneumoniae is usually cross-resistant to beta-lactam antibiotics.

 

Pharmacokinetics

Cefalexin is acid stable and may be given without regard to meals. It is rapidly absorbed after oral administration. Following doses of 250 mg, 500 mg and 1 gram, average peak serum levels of approximately 9, 18 and 32mg/liter, respectively, were obtained at 1 hour. Measurable levels were present 6 hours after administration. Cefalexin is excreted in the urine by glomerular filtration and tubular secretion. Studies showed that over 90% of the drug was excreted unchanged in the urine within 8 hours. During this period, peak urine concentrations following the 250 mg, 500 mg and 1 gram doses were approximately 1000, 2200 and 5000 mg/liter, respectively.

Cefalexin is almost completely absorbed from the gastro-intestinal tract and 75 to 100% is rapidly excreted in active form in the urine. Absorption is slightly reduced if the drug is administered with food. The half-life is approximately 60 minutes in patients with normal renal function. Haemodialysis and peritoneal dialysis will remove cefalexin from the blood.

Peak blood levels are achieved one hour after administration and therapeutic levels are maintained for 6 to 8 hours. Approximately 80% of the active drug is excreted in the urine within 6 hours. No accumulation was seen with dosages above the therapeutic maximum of 4 gm/day.

The half-life may be increased in neonates due to their renal immaturity, but there is no accumulation when given at up to 50 mg/kg/day.

 

PRECLINICAL SAFETY1,2

Carcinogenicity/mutagenicity/impairmentof fertility

Lifetime studies in animals have not been performed to evaluate the carcinogenic potential of cefalexin. Tests to determine the mutagenic potential of cefalexin have not been performed. In male and female rats, fertility and reproductive performance were not affected by cefalexin oral doses up to 1.5 times the highest recommended human dose based upon mg/m2.

The daily oral administration of cefalexin to rats in doses of 250 or 500 mg/kg prior to and during pregnancy, or to rats and mice during the period of organogenesis only, showed no adverse effect on fertility, foetal viability, foetal weight, or litter size.

Cefalexin showed no enhanced toxicity in weanling and newborn rats as compared with adult animals.

 

STORAGE

Store below 25°C, protected from moisture.

Keep the constituted suspension in refrigerator (2-8°C) and use within 10 days.

KEEP ALL MEDICINES OUT OF THE REACH OF CHILDREN

 

SUPPLY

HDPE bottle of 100 mL.

 

REFERENCES

1 US Prescribing Information of KEFLEX® capsules, Advancis Pharmaceutical Corporation USA, November 2006 accessed online from http://dailymed.nim.nih .gov/dailymed/druglnfo.cfm?id=6490#nim34067-9 on December 7, 2010.

2 UK Summary of Product Characteristics of KEFLEX® tablets, capsules and granules for suspension, Flynn Pharma Limited, UK, revised in September2005.

Information compiled in December 2010

 

Manufactured in India by

Sun Pharmaceutical Ind. Ltd.

Industrial Area – 3

Dewas -455 001

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