Product Index

Composition

NOVACLOX-500 I.V./I.M.
Each vial contains:
Amoxycillin Sodium, IP, equivalent to Amoxycillin anhydrous ..............250 mg
Cloxacillin Sodium, IP, equivalent to Cloxacillin ...........................................250 mg

Each FFS vial contains:
Sterile Water for Injection, IP...................5 ml

Dosage Form/s

I.V./I.M.injection

Pharmacology

Amoxycillin is bactericidal against non-beta-lactamase-producing Gram-positive organisms and selected Gram-negative pathogens. Cloxacillin is a beta-lactamase-resistant penicillin active against Gram-positive organisms, including beta-lactamase (penicillinase)-producing strains of Staphylococci. It is highly active against Staphylococcus aureus, Streptococcus pyogenes, Streptococcus viridans and Streptococcus pneumoniae. It is also effective against penicillinase-producing gonococci and against Neisseria meningitidis and Haemophilus influenzae.

Indications

Respiratory Tract Infections
Tonsillar abscess, otitis media, suppurative sinus infection, acute and chronic bronchitis, bronchiectasis, bronchopneumonia, pleurisy, empyema, lung abscess, emphysema, bronchiolitis.

Gynaecological Infections
Septic abortion, puerperal infections, caesarean sections and other gynaecological surgeries.

Urinary Tract Infections
Acute and chronic pyelonephritis, cystitis, urethritis.

Skin and Soft Tissue Infections

Recurrent boils, carbuncles, impetigo, cellulitis and other infected dermatoses.

Bone Infections
Osteomyelitis and septic arthritis.

Serious Infections
Septicaemia, bacterial endocarditis, brain abscess and bacterial meningitis.

Dosage and Administration

Adults
1-2 vials every 6-8 hours.
Dose may be given via the I.M./I.V. routes.

Paediatric
Aged 1 month to 2 years: 0.25-0.5 vial every 6-8 hours
Aged 2 to 10 years: 0.5-1 vial every 6-8 hours.
Dose may be given via the I.M./I.V. routes.

Contraindications

A history of allergic reaction to any of the penicillins is a contraindication.

Warnings and Precautions

Serious, and occasionally fatal, hypersensitivity (anaphylactic) reactions have been reported in patients on penicillin therapy. Although anaphylaxis is more frequent following parenteral therapy, it has occurred in patients on oral penicillins. These reactions are more likely to occur in individuals with a history of penicillin hypersensitivity and/or a history of sensitivity to multiple allergens. There have been reports of individuals with a history of penicillin hypersensitivity who have experienced severe reactions when treated with cephalosporins.

Before initiating therapy with this medicine, careful inquiry should be made concerning previous hypersensitivity reactions to penicillins, cephalosporins or other allergens. If an allergic reaction occurs, this medicine should be discontinued and appropriate therapy instituted.

Candidiasis and other superinfections may occur, especially in debilitated and malnourished patients, or those with low resistance to infection due to corticosteroids, immunosuppressors or irradiation. If superinfection occurs, institute appropriate measures.

Pseudomembranous colitis has been reported with nearly all antibacterial agents, including this medicine, and may range in severity from mild to life-threatening. Therefore, it is important to consider this diagnosis in patients who present with diarrhoea subsequent to the administration of antibacterial agents.

Treatment with antibacterial agents alters the normal flora of the colon and may permit overgrowth of clostridia. Studies indicate that a toxin produced by Clostridium difficile is a primary cause of “antibiotic-associated colitis”. After the diagnosis of pseudomembranous colitis has been established, appropriate therapeutic measures should be initiated. Mild cases of pseudomembranous colitis usually respond to drug discontinuation alone. In moderate-to-severe cases, consideration should be given to management with fluids and electrolytes, protein supplementation, and treatment with an antibacterial drug clinically effective against C. Difficile colitis.

The possibility of superinfections with mycotic or bacterial pathogens should be kept in mind during therapy. If superinfections occur, this medicine should be discontinued and appropriate therapy instituted.

Prescribing NOVACLOX-500 I.V./I.M. 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.

As with any potent drug, periodic assessment of renal, hepatic and haematopoietic function should be made during prolonged therapy.

White blood cell counts and differential cell counts should be obtained prior to initiation of therapy and at leastweekly during therapy with penicillinase-resistant penicillins.

Periodic urinalysis should be performed, and blood urea nitrogen, creatinine, AST and ALT concentrations should be determined during therapy with the penicillinase-resistant penicillins. Dosage alterations should be considered if these values become elevated.

Drug Interactions
Probenecid decreases the renal tubular secretion of amoxycillin. Concurrent use of amoxycillinand probenecid may result in increased and prolonged blood levels of amoxycillin.

Aminoglycosides and penicillins are physically and/or chemically incompatible and can mutually inactivate each other in vitro. In vitro mixing of penicillinase-resistant penicillins and aminoglycosides should be avoided during concomitant therapy, and the drugs should be administered separately. Penicillins can also inactivate aminoglycosides In vitroin serum samples from patients receiving both drugs, which could produce falsely decreased results in serum aminoglycoside assays of the serum samples.

Chloramphenicol, macrolides, sulphonamides and tetracyclines may interfere with the bactericidal effects of penicillin. This has been demonstrated In vitro; however, the clinical significance of this interaction is not well documented.

Drug/Laboratory Test Interactions

High urine concentrations of ampicillin may result in false-positive reactions when testing for the presence of glucose in urine using, Benedict's Solution or Fehling's Solution. Since this effect may also occur with amoxycillin, it is recommended that glucose tests based on enzymatic glucose oxidase reactions be used.

Following administration of ampicillin to pregnant women, a transient decrease in plasma concentration of total conjugated oestriol, oestriol-glucuronide, conjugated oestrone and oestradiol has been noted. This effect may also occur with amoxycillin.

Pregnancy

There are 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

Penicillins have been shown to be excreted in human milk. Amoxycillin use by nursing mothers may lead to sensitization of infants. Caution should be exercised when NOVACLOX-500 I.V./I.M.is administered to a nursing mother.

Paediatric Use

Because of incompletely developed renal function in newborns, penicillinase-resistant penicillins may not be completely excreted, resulting inabnormally high blood levels of the drugs. Frequent blood level monitoring of such drugs are advisable in this group.

Geriatric Use

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.

Undesirable Effects

As with other penicillins, it may be expected that untoward reactions will be essentially limited to sensitivity phenomena. They are more likely to occur in individuals who have previously demonstrated hypersensitivity to penicillins and in those with a history of allergy, asthma, hay fever or urticaria. The following adverse reactions have been reported as associated with the use of penicillins:

Gastrointestinal Nausea, vomiting, diarrhoea, and haemorrhagic/pseudomembranous colitis. Onset of pseudomembranous colitis symptoms may occur during or after antibiotic treatment.

Hypersensitivity Reactions Serum sickness-like reactions, erythematous maculopapular rashes, erythema multiforme, Stevens-Johnson syndrome, exfoliative dermatitis, toxic epidermal necrolysis, acute generalized exanthematouspustulosis, hypersensitivity vasculitis and urticaria have been reported.

NOTE These hypersensitivity reactions may be controlled with antihistamines and, if necessary, systemic corticosteroids. Whenever such reactions occur, amoxycillin should be discontinued unless, in the opinion of the physician, the condition being treated is life-threatening and amenable only to amoxycillin therapy.

Liver A moderate rise in AST (SGOT) and/or ALT (SGPT) has been noted, but the significance of this finding is unknown. Hepatic dysfunction, including cholestatic jaundice, hepatic cholestasis and acute cytolytic hepatitis, has been reported.

RenalCrystalluria has also been reported.

Haemic and Lymphatic Systems Anaemia, including haemolyticanaemia, thrombocytopenia, thrombocytopenic purpura, eosinophilia, leucopenia and agranulocytosis have been reported during therapy with penicillins. These reactions are usually reversible on discontinuation of therapy and are believed to be hypersensitivity phenomena.

Central Nervous System Reversible hyperactivity, agitation, anxiety, insomnia, confusion, convulsions, behavioral changes, and/or dizziness have been reported rarely.

Miscellaneous Tooth discolouration (brown, yellow or grey staining) has been, rarely, reported. Most reports occurred in paediatric patients. Discolouration was reduced or eliminated with brushing or dental cleaning in most cases.

Overdosage

In case of overdosage, discontinue medication, treat symptomatically, and institute supportive measures as required. If the overdosage is very recent and there is no contraindication, an attempt at emesis or other means of removal of drug from the stomach may be performed. A prospective study of 51 paediatric patients at a poison-control centre suggested that overdosages of less than 250 mg/kg of amoxycillin are not associated with significant clinical symptoms and do not require gastric emptying.

Interstitial nephritis resulting in oliguric renal failure has been reported in a small number of patients after overdosage with amoxycillin.

Crystalluria, in some cases leading to renal failure, has also been reported after amoxycillin overdosage in adult and paediatric patients. In case of overdosage, adequate fluid intake and diuresis should be maintained to reduce the risk of amoxycillincrystalluria.

Renal impairment appears to be reversible with the cessation of drug administration. High blood levels may occur more readily in patients with impaired renal function because of decreased renal clearance of amoxycillin. Amoxycillin may be removed from circulation by haemodialysis. Cloxacillin is only minimally removed (up to 5%) by haemodialysis and peritoneal dialysis.

Incompatibility

NOVACLOX-500 I.V./I.M.injectable solution should be used immediately after reconstitution. NOVACLOX-500 I.V./I.M.is compatible with intravenous infusion fluids commonly used.NOVACLOX-500 I.V./I.M.should not be added to blood or plasma or other proteinaceous fluids

Storage and Handling Instructions

Store in a cool, dry place. Protect from light.

Packaging Information

NOVACLOX-500 I.V./I.M.: 5ml FFS vial