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Logo ORELOX 100 (Tablets)
ORELOX-JUNIOR (Suspension)

SCHEDULING STATUS:
S4

PROPRIETARY NAME
(and dosage form):

ORELOX 100 (Tablets)
ORELOX-JUNIOR (Suspension)

COMPOSITION:
100 mg Tablets:
Each tablet contains 130,45 mg of cefpodoxime proxetil equivalent to 100 mg of
cefpodoxime.
Paediatric Suspension:
Each 5 mL of suspension contains 52,18 mg of cefpodoxime proxetil equivalent to 40 mg of cefpodoxime.
(Preservative : Potassium Sorbate 0,17%)
Contains aspartame 20 mg/5 mL.

PHARMACOLOGICAL CLASSIFICATION:
A. 20.1.1 Broad and medium spectrum antibiotics.

PHARMACOLOGICAL ACTION:
Orelox (cefpodoxime proxetil) is a semisynthetic beta-lactam -antibiotic belonging to the third generation oral cephalosporin group. Orelox is the prodrug of the bactericidal antibiotic cefpodoxime.
Cefpodoxime possesses in vitro bactericidal activity against a broad spectrum of Gram positive and Gram negative bacteria. In vitro sensitivity does not necessarily imply in vivo efficacy. Cefpodoxime is stable in the presence of the majority of beta-lactamases. The mechanism of action is bactericidal through inhibition of bacterial cell wall biosynthesis enhanced by a high affinity for proteins at the cytoplasmic membrane.

- SENSITIVE STRAINS: (Sensitivity tests must be performed)
- Gram positive organisms:
  - Streptococcus pneumoniae
  - Streptococci of Groups A (S. pyogenes), B (S. agalactiae), C, F and G.
  - Other streptococci (S. mitis, S. sanguis and S. salivarius)
  - Propionibacterium acnes
  - Corynebacterium diphtheriae
  - Methicillin-sensitive S. aureus, penicillinase and non-penicillinase producing strains.
- Gram negative organisms:
  - Haemophilus influenzae, beta-lactamase and non-beta-lactamase producing strains
  - Haemophilus para-influenzae, beta-lactamase and non-beta-lactamase producing strains
  - Moraxella catarrhalis (Branhamella catarrhalis), beta-lactamase and non-beta-lactamase producing strains
  - Neisseria gonorrhoeae, beta-lactamase and non beta-lactamase producing strains
  - Escherichia coli
  - Klebsiella pneumoniae; Klebsiella oxytoca
  - Proteus mirabilis
The following organisms are not sensitive: Group D streptococci, Methicillin-resistant staphylococci (S. aureus and S. epidermidis), Staphylococcus saprophyticus, Corynebacteria, groups J and K, Listeria monocytogenes, Pseudomonas aeruginosa and Pseudomonas spp., Acinetobacter baumanii, Clostridium difficile, Bacteroides fragilis and related species.
PHARMACOKINETICS: The bioavailability of Orelox is increased when the product is administered with meals, or when there is a decrease in gastric pH. An increase in gastric pH results in decreased bioavailability.
Absorption: After oral administration, cefpodoxime proxetil is absorbed in the gastrointestinal tract and rapidly hydrolysed by non-specific esterases in the gastrointestinal wall to cefpodoxime, the active acid.
Distribution: In Adults: After oral administration of a single dose of 100 mg of cefpodoxime, the maximum plasma concentration (Cmax) obtained is 1 to 1,2 mg/L, and after administration of a dose of 200 mg of cefpodoxime, the maximum plasma concentration (Cmax) obtained is 2,2 to 2,5 mg/L. In both cases the time (Tmax) taken to reach the maximum concentration is 2 to 3 hours.
Following administration of 100 and 200 mg twice daily for 14,5 days, the pharmacokinetic parameters of cefpodoxime remain unchanged, indicating that there is no accumulation of the active principle.
The binding of cefpodoxime to plasma proteins is about 40%. This binding is principally to albumin and is of the non-saturable type.
In Children: After oral administration of a single 5 mg/kg dose (200 mg maximum) of cefpodoxime to subjects between 4 and 12 years of age, the maximum plasma concentration (Cmax) is on average 2,6 mg/L. The time taken to reach the maximum concentration (Tmax) is 2 to 4 hours. The average plasma concentrations observed 8 and 12 hours after administration (residual) are 0,39 and 0,08 mg/L respectively.
Diffusion in fluids and tissues:Orelox diffuses well in lung parenchyma, bronchial mucosa, pleural fluid and tonsils.
Metabolism and elimination: The main metabolite is cefpodoxime, resulting from the hydrolysis of cefpodoxime proxetil.
The elimination half-life of cefpodoxime is 2,4 hours. 80% of unchanged cefpodoxime is excreted in the urine.

INDICATIONS:
In Adults:
Orelox 100 is indicated for use in the short-term treatment of upper and lower respiratory tract infections due to susceptible micro-organisms:
- Acute bronchitis and acute exacerbations of chronic bronchitis
- Pharyngitis and tonsillitis
- Community-acquired bronchopneumonia
- Acute sinusitis
In Children:Orelox-Junior is indicated for use in the short-term treatment of infections due to susceptible micro-organisms:
Upper and lower respiratory tract infections:
- Otitis media
- Tonsillitis and pharyngitis
- Pneumonia

CONTRA-INDICATIONS:
Known sensitivity to cephalosporin antibiotics.
Safety of use in pregnancy and lactation has not been established.
Orelox-Junior must not be given to children with phenylketonuria, since the formulation contains aspartame (20 mg/5 mL).

WARNINGS:
Preliminary enquiry as to an allergic diathesis and particularly hypersensitivity of beta-lactam antibiotics should precede treatment with Orelox.
The use of Orelox is strictly contra-indicated in subjects with a previous history of immediate type hypersensitivity to cephalosporins.
Orelox should be used with extreme caution in patients sensitive to penicillin and other beta-lactam antibiotics as cross-allergy may develop. Strict medical supervision is required throughout the treatment.
Hypersensitivity reactions (anaphylaxis) observed with Orelox, can be serious and occasionally fatal. Treatment should be stopped immediately, should an allergic reaction occur.

DOSAGE AND DIRECTIONS FOR USE:
In Adults:
The dosage depends on the condition being treated.
Tonsillitis, pharyngitis and acute bronchitis:
One tablet every 12 hours with meals (200 mg/day).
As is the case with all beta lactam antibiotics in the treatment of beta-haemolytic streptococcal infections, a therapeutic dose has to be administered for at least 10 days.
Acute sinusitis, acute exacerbations of chronic bronchitis, pneumonia:
Two tablets every 12 hours with meals (400 mg/day).
Elderly patients:Where renal function is normal, it is not necessary to adjust the dose.
Renal Insufficiency in adults and children:
When the creatinine clearance is above 40 mL/min, it is not necessary to adjust the dose. For values below 40 mL/min, the daily dosage regimen should be reduced by half and administered as a single daily dose for values 10-39 mL/min, every second day for values below 10 mL/min, and after each dialysis session for haemodialysis patients.
In Children: The dosage depends on the weight of the child being treated. The average dose is 8 mg/kg/day administered in two doses at 12 hourly intervals with meals.
The following table may be used as a dosage guide.
        WEIGHT (kg)         DOSE
        Between 10 and 15 kg         5 mL every 12 hours
        > 15 kg         10 mL every 12 hours
The use of Orelox-Junior in children under one year of age is currently not indicated since insufficient clinical data is available at present.
Directions and reconstitution of the Suspension:
Remove the screw-cap by simultaneously pushing and turning it. Remove the desiccant plug by pulling the tear-tab, and discard. The indented calibration mark represents the final volume. Half fill the bottle with water and shake vigorously (about 30 seconds). Fill up with water to the calibration mark and shake again to disperse all granules. A total of 45 mL water is required to make up the 50 mL suspension and a total of 90 mL water is required to make up the 100 mL suspension.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
The following side-effects have been reported:
- Gastrointestinal disorders: Diarrhoea, nausea, vomiting and abdominal pains. Diarrhoea, particularly if severe and/or persistent, occuring during treatment or initial weeks following treatment may be symptomatic of Clostridium difficile associated disease, the most severe form of which is pseudo-membranous colitis. The diagnosis of this rare but possibly fatal condition should be confirmed by colonoscopy and/or histology. This occurrence requires immediate cessation of administration and treatment with appropriate specific antibiotic therapy.
- Headache, dizzy sensations, tinnitus, parethesia, asthenia.
- Allergic disorders: cutaneous eruptions and pruritus, urticaria and purpura. Cases of bullous erruptions have been reported.
- Anaphylactic reactions: eg angioedema, bronchospasm, malaise, possibly culminating in shock may rarely occur (see warnings).
- Abnormalities in clinical laboratory tests: elevations of ASAT, ALAT and alkaline phosphatase, increase of blood urea and creatinine.
- Haematological disorders: reduction of haemoglobin, thrombocytosis, thrombocytopenia, leucopenia and eosinophilia. Neutropenia and more rarely agranulocytosis may occur during treatment with cefpodoxime particularly if given over long periods.
Use with care in patients with renal impairment.
A positive Coombs' test has been reported during treatment with cephalosporins.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
See side-effects and special precautions.
Treatment should be symptomatic and supportive.
In cases of overdosage, particularly in patients with renal insufficiency, there is a risk of reversible encephalopathy for several cephalosporins.

IDENTIFICATION:
Orelox 100:
Biconvex, cylindrical, practically white tablets, 9 mm in diameter with "208" and beneath "A" engraved on one side. A broken tablet shows a pale yellow core surrounded by a white film-coating.
Orelox-Junior:
Pale, yellow granules for reconstitution. The reconstituted suspension is pale yellow in colour and has a banana flavour and odour.

PRESENTATION:
Orelox 100: Blister pack of 10 tablets.
Orelox-Junior: 150 mL amber glass bottle containing granules for reconstitution up to 100 mL of suspension or 75 mL amber glass bottle containing granules for reconstitution up to 50 mL of suspension.

STORAGE INSTRUCTIONS:
Orelox 100:
Store in a cool, dry place, below 25°C.
Protect from light and humidity.
Orelox-Junior:
Before reconstitution: Store in a cool, dry place below 25°C.
Protect from light and humidity.
After reconstitution: Use within 10 days.
Store in a refrigerator (2 to 8°C).
Shake before use.
Keep out of reach of children.

REGISTRATION NUMBERS:
Orelox 100:         Z/20.1.1/7
Orelox Junior:         27/20.1.1/0564

NAME AND BUSINESS ADDRESS OF APPLICANT:
Aventis Pharma (Pty) Ltd
2 Bond Street
Midrand
1685

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
28 March 1996

Product licensed from Sankyo Co. Ltd.

Aventis Pharma (Pty) Ltd
2 Bond Street
Midrand
1685

                        OX2-B0501
               
Highland Print
Updated on this site: June 2003
Source: Community Pharmacy

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