INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo FLOXAPEN 250 (capsules)
FLOXAPEN S (syrup)
SCHEDULING STATUS:
S4

PROPRIETARY NAMES
(and dosage form):

FLOXAPEN 250 (capsules)
FLOXAPEN S (syrup)

COMPOSITION:
Floxapen 250        :   Gelatin capsules containing flucloxacillin sodium equivalent to 250 mg flucloxacillin.
Floxapen S:   Powder for preparing citrus-flavoured syrup.
When dispensed as directed, each 5 mL of the syrup contains flucloxacillin sodium equivalent to 125 mg flucloxacillin.
The powder contains 0,13% m/m sodium benzoate B.P. as a preservative.

PHARMACOLOGICAL CLASSIFICATION:
A.20.1.2 Penicillins

PHARMACOLOGICAL ACTION:
Floxapen is a semi-synthetic penicillin derived from 6-amino-penicillanic acid and is the latest of the series of penicillinase stable penicillins.
(a) Bacteriology
Floxapen exhibits bactericidal activity against all Gram-positive organisms (with the exception of Strep. faecalis) e.g. Haemolytic streptococci, staphylococci, streptococcus pneumoniae and N. gonorrhoeae.
Floxapen’s anti-staphylococcal activity is not affected by penicillinase and as Floxapen is active against virtually all strains ofStaph. aureus (methicillin-resistant strains being the only exception), it is particularly indicated in the treatment of staphylococcal infections.
The MIC’s of benzylpenicillin against staphylococci are lower than those of flucloxacillin except in the case of the penicillinase-producing staphylococci.
(b) Absorption
Floxapen is extremely well absorbed orally. A single 250 mg dose achieves an average peak serum level virtually equal to that achieved by an equivalent IM injection. The peak serum level is achieved half to one hour after administration. Floxapen should be taken 1 hour before meals to ensure that maximum absorption is achieved.
(c) Excretion
Approximately 60% of an oral dose and 90% of an intramuscular and intravenous dose of Floxapen is excreted unchanged in the active form into the urine within 6 hours.
(d) Probenecid
Even higher Floxapen serum levels may be achieved after oral administration in patients with normal renal function by the simultaneous administration of a renal blocking agent such as probenecid. Probenecid should not be given in the presence of abnormal renal function.

INDICATIONS:
Infections caused by susceptible organisms, including:
Skin and soft tissue infections         Orthopaedic infections
Infected wounds and burns         Septicaemia
Otitis media         Meningitis
Urinary tract infections         Endocarditis
Respiratory tract infections caused by penicillinase-producing organisms         Enterocolitis

CONTRA-INDICATIONS:
Flucloxacillin is a penicillin and should not be given to patients with a history of hypersensitivity to beta-lactam antibiotics (e.g. penicillins, cephalosporin) or any of the excipients of Floxapen.
Floxapen is contra-indicated in patients with a previous history of flucloxacillin associated jaundice/hepatic dysfunction.
Not to be used in the eye, either sub-conjunctivally or topically. Babies born of hypersensitive mothers in the neonatal period. Safety in pregnancy has not yet been established.

WARNINGS:
Before initiating therapy with flucloxacillin, careful inquiry should be made concerning previous hypersensitivity reactions to beta-lactams. Cross-sensitivity between penicillins and cephalosporins is well documented. Serious and less frequently fatal hypersensitivity reactions (anaphylaxis) have been reported in patients receiving beta-lactam antibiotics.
Floxapen should be used with caution in patients with evidence of hepatic dysfunction. Special caution is essential in the newborn because of the risk of hyperbilirubinemia, as there is a potential for high serum levels of flucloxacillin due to a reduced rate of renal excretion.

DOSAGE AND DIRECTIONS FOR USE:
Oral
Each dose should be taken 1 hour before meals.
Adults: 250 mg (1 capsule or 10 mL syrup) 4 times a day preferably 1 hour before meals.
Children 2-10 years: 125 mg (5 mL syrup) 4 times a day preferably 1 hour before meals.
Children 2 months-2 years: 62,5 mg (2,5 mL syrup) 4 times a day preferably 1 hour before meals.

SKIN AND SOFT TISSUE INFECTIONS
Up to 8 g daily in divided doses, six to eight hourly, one hour before meals.
Renal impairment
For patients with a creatinine clearance value <10 mL/min, consider a dose reduction or extension of dose interval. For patients with a creatinine clearance value >10 mL/min, no dose adjustment is necessary.
Floxapen is not significantly removed by dialysis and hence no supplementary dosage is needed during or at the end of dialysis.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Hypersensitivity reactions:
If any hypersensitivity reaction occurs, the treatment should be discontinued.
Rash, urticaria, purpura, fever, eosinophilia; sometimes angioneurotic oedema, and less frequently anaphylactic shock. Certain reactions (fever, arthralgia, myalgia) sometimes develop more than 48 hours after the start of treatment. Erythema multiforme has been reported less frequently.
If a skin rash occurs, treatment should be discontinued and administration of an antihistamine considered. An anaphylactic reaction after administration of a penicillin can occur. If this happens treatment should be stopped and appropriate treatment with adrenaline, corticosteroids and antihistamines commenced immediately.
Gastrointestinal reactions:
Minor gastrointestinal disturbances may occur during treatment e.g. nausea, diarrhoea.
Pseudomembranous colitis has been reported less frequently. If this condition develops, Floxapen treatment should be discontinued and appropriate therapy e.g. oral vancomycin should be initiated. Prolonged use may occasionally result in the overgrowth of non-susceptible organisms.
Hepatic effects:
Hepatitis and cholestatic jaundice have been reported. This may be delayed for up to two months post-treatment. Less frequently, deaths have been reported.
Renal effects:
Interstitial nephritis may occur but is reversible when treatment is discontinued.
Haematological effects:
Neutropenia (including agranulocytosis) and thrombocytopenia may occur but are reversible when treatment is discontinued.
SPECIAL PRECAUTIONS:
Serious and less frequently, fatal anaphylactic reactions have been reported. Although anaphylaxis is more frequent following parenteral therapy, it has occurred in patients on oral therapy. These reactions are more likely to occur in individuals with a history of beta-lactam hypersensitivity. If an allergic reaction occurs, Floxapen should be discontinued and the appropriate therapy instituted. Serious anaphylactoid reactions may require emergency treatment with adrenaline; corticosteroids and antihistamines. Oxygen and airway management, including intubation, may also be required.
Hepatitis, predominantly of a cholestatic type has been reported and less frequently, deaths have occurred. Reports have been more frequent with increasing age or following prolonged treatment. Floxapen should be used with caution in patients with evidence of hepatic dysfunction.
Special caution is essential in the newborn because of the potential of high serum levels of flucloxacillin due to a reduced rate of renal excretion.
During prolonged treatments, regular monitoring of hepatic and renal functions is recommended. Dosage should be adjusted in renal impairment.
Electrolyte disturbance, infrequent disturbance in the form of hypernatraemia may occur. Each gram of flucloxacillin sodium contains respectively 2,2 mmol of sodium.
Prolonged use may occasionally result in overgrowth of non-susceptible organisms.
Use in pregnancy
Floxapen should only be used in pregnancy when the potential benefits outweigh the potential risks associated with pregnancy.
Use in lactation
Floxapen is excreted in breast milk. With the exception of the risk of sensitization, there are no known detrimental effects to the infant.
INTERACTIONS:
Floxapen should not be administered simultaneously with bacteriostatic medications. On the other hand, combination with aminoglycosides may result in a synergistic effect. If prescribed concurrently, the two antibiotics should not be mixed in the same container as precipitation may occur. Probenecid decreases the renal tubular secretion of flucloxacillin. Concurrent use may result in increased and prolonged blood levels of flucloxacillin.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
Problems with overdosage are unlikely to occur. If encountered, gastro-intestinal symptoms and disturbances of the fluid and electrolyte balance may be evident. They may be treated symptomatically with attention to the water/electrolyte balance. Flucloxacillin cannot be removed from the circulation by haemodialysis.
As with all penicillins, oral administration can cause gastrointestinal symptoms such as transient diarrhoea, nausea and colic which are dose-related and as a result of local irritation and not toxicity.

IDENTIFICATION:
Floxapen 250 :        Black/caramel capsules overprinted “Floxapen 250”.
Floxapen S :        Pinkish-white, free-flowing powder. Orange coloured suspension.

PRESENTATION:
Floxapen 250 :        Amber glass bottles containing 20 or 100 x 250 mg flucloxacillin capsules.
Floxapen S : Bottles containing powder for reconstitution to 100 mL of 125 mg/5 mL flucloxacillin syrup.

STORAGE INSTRUCTIONS:
Bottles of Floxapen 250 should be kept tightly closed in a cool (below 25° C) dry place.
Once dispensed, Floxapen S must be used within 7 days; if stored in a cool (below 25°C) place or 14 days if stored in a refrigerator (5°C).

REGISTRATION NUMBERS:
Floxapen 250        :         E/20.1.2/89
Floxapen S        :         E/20.1.2/95
Zimbabwe:
Floxapen 250        :         78/7.1.2/1099 PP
Floxapen S        :         78/7.1.2/1097 PP

NAME AND BUSINESS ADDRESS OF THE APPLICANT:
GlaxoSmithKline South Africa (Pty) Limited
57 Sloane Street
Bryanston
2021

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
16.10.1990

Floxapen and the GSK logo are trademarks.

In-line with MDS-008

GOOD OLD PRINTING CT: 592 3868        P3865/0903

Updated on this site: April 2005
Source: Hospital Pharmacy

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