ORALUXE (F.C. Tablets / Dry Powder For Oral Suspension)
(Cefpodoxime Proxetil)

PROPERTIES
ORALUXE (Cefpodoxime Proxetil) is an orally administered, extended spectrum semi-synthetic antibiotic of the cephalosporin class, belonging to the third generation.
The bactericidal activity of ORALUXE results from its inhibition of cell wall synthesis. Cefpodoxime has a high degree of stability in the presence of beta-lactamases, both penicillinases and cephalosporins of gram-negative and gram-positive bacteria.
 

CLINICAL PHARMACOLOGY:
ORALUXE (Cefpodoxime Proxetil) is rapidly absorbed after oral administration. Measurable levels were present 12 hours after administration of 100 and 200 mg at 0.08 mg/l and 0.18mg/l respectively. Over 80 % of the drug is excreted unchanged in the urine. Increases in dosage generally produce a proportionate increase in Cefpodoxime urinary concentrations. Protein binding of Cefpodoxime ranges from 22 to 33 % in serum and from 21 to 29 % in plasma, and is very well diffused in the lung parenchyma, bronchial mucosa, pleural liquid. tonsils and interstitial liquid.
4 to 7 hours after oral administration of 100 mg Cefpodoxime, concentrations in the tonsils were 0.24 to 0.1 mg/gr. After administration of 200 mg Cefpodoxime, the concentrations in the interstitial fluid were 1.5 to 2 mg/l, in the lung tissues 0.6 to 0.2 mg/gr, in the pleural liquid 0.6 to 0.8 mg/l, and in the bronchial mucosa were around 1 mg/gr. All the above measured concentrations were superior to the MIC.
Cefpodoxime half-life is 2.4 hours and its absorption is about 40 to 50 % and is increased when administered with meals.
 

MICROBIOLOGY:
ORALUXE is active against the following organisms:
 

Gram-positive:
Staphylococcus aureus (including penicillinase - producing strains).
Staphylococcus saprophyticus.
Streptococcus (diplococcus) pneumoniae.
Streptococcus pyogenes, streptococcus agalactiae, and streptococcus spp.(group C,F,G).
Propionibacterium acnes.
Corynebacterium diphtheria.
 

Gram-negative:
Citrobacter diversus.
Escherichia coli.
Haemophilus influenzae.
Haemophilus parainfluenzae.
Klebsiella pneumoniae.
Klebsiella oxytoca.
Moraxella (Branhamella) catarrhalis.
Neisseria meningitidis.
Neisseria gonorrhoeae.
Pasteurella multocida. Peptosireptococcus magnus.
Proteus mirabilis.
Proteus vulgaris.
Providencia spp.
Salmonella spp.
Shigella spp.

INDICATIONS:
ORALUXE is recommended in adults and in children (age 5 months through 12 years) for treatment of the following infections:
- Tonsillitis, pharyngitis, sinusitis and otitis media.
- Acute, community acquired pneumonia, acute purulent bronchitis, acute bacterial exacerbation of chronic obstructive bronchitis.
- Acute, uncomplicated urethra and cervical gonorrhea caused by (neisseria gonorrhoeae).
- Acute, uncomplicated anorectal infections in women due to (neisseria gonorrhoeae).
- Uncomplicated urinary tract infections (cystitis).
- Uncomplicated skin and skin structure infections.
 

CONTRAINDICATIONS:
ORALUXE is contraindicated in patients with a known allergy to Cefpodoxime or to the cephalosporin group of antibiotics.
 

SIDE EFFECTS:
ORALUXE may, in some patients, cause: diarrhoea, abdominal pain, nausea, vomiting vaginal fungal infection, rash and headache.
 

PREGNANCY AND LACTATION:
Safe use of Cefpodoxime during pregnancy and lactation have not been established.
ORALUXE should be used during pregnancy only if clearly needed.
 

PRECAUTIONS:
- ORALUXE should be prescribed with caution in patients with renal impairment.
- ORALUXE should be prescribed with caution in individuals with previous history of allergy to betalactamase or receiving concurrent treatment with potent diuretics.
 

WARNINGS
- There is a possible allergy (in 5 to 10 % of cases) in subjects sensitive to penicillins.
- If an allergic reaction to ORALUXE occurs, the drug should be discontinued immediately.
Serious acute hypersensitivity reactions may require emergency treatment measures. Pseudomembranous colitis has been reported with the use of cephalosporin (and other broad spectrum antibiotics): therefore, it is important to consider its diagnosis in patients who develop diarrhoea in association with antibiotic use. Treatment with broad spectrum antibiotics alters normal flora of the colon and may permit overgrowth of clostridia. Studies indicate that a toxin produced by clostridium difficile is one primary cause of antibiotic-associated colitis
Cholestyramine and colestipol resins have been shown to bind to the toxin in vitro.
Mild cases of colitis may respond to drug discontinuation alone. Moderate to severe cases should be managed with fluid, electrolyte, metronidazole and protein supplementation as indicated.
When the colitis is not relieved by drug discontinuation or when it is severe, oral vancomycin is the treatment of choice for antibiotic-associated pseudomembranous colitis produced by C. difficile. Other causes of colitis should also be considered.
 

DRUG AND FOOD INTERACTIONS:
- Antacids (aluminum hydroxide, sodium bicarbonate) and H2 Antagonist receptor (Ranitidine)
reduces peak plasma level by 24 to 42 % and the extent of absorption by 27 % to 32 %
respective.
- Pentagastrin reduces the gastric pH causing an increase of the bioavailability of the drug.
- Probenecid inhibit the excretion of Cefpodoxime and thus increases by 31 % the A.U.C. and by 20 % the peak plasma levels.
- Nutritional interaction: Studies indicated that the biodisponibility of the drug increases when it is taken with meals.
DRUG/LABORATORY INTERACTIONS:
- Positive direct Coomb's tests have been reported during treatment with the cephalosporin antibiotics.

DOSAGE AND ADMINISTRATION:
Note: It is advisable to take ORALUXE orally with food to enhance absorption.
ADULTS:
ORALUXE 400 mg daily, should be administered during meals in two divided doses (BID) in the following indications:
-Acute sinusitis.
-Acute and chronic purulent bronchitis, acute community-acquired bacterial pneumonia, acute
bacterial exacerbation of chronic obstructive bronchopneumonia.
ORALUXE 200 mg daily, should be administered during meals in two divided doses (BID) in the following indications:
- Tonsillitis, Pharyngitis.
- Uncomplicated urinary tract infections.
ORALUXE 200 mg as a single dose in uncomplicated gonorrhoea (men and women) and rectal gonococcal infections (women). ORALUXE 800 mg daily, should be administered during meals in two divided doses (BID) in skin and skin structure infections.
 

Dosage in renal impairment:
In patients with renal impairment (creatinine clearance <30 ml/min) the dosage of ORALUXE should be adjusted accordingly, to prevent drug accumulation. A dosage of ORALUXE 100 mg daily as a single dose is sufficient.
 

CHILDREN:
ORALUXE 10 mg/kg/day should be administered without regard to food in two divided doses (BID), in the following indications.
-Acute otitis media (maximum for 100 mg/day).
-Pharyngitis and/or tonsillitis (maximum to 100 mg/day).
According to the physician prescription the recommended duration of treatment vary from 7 to 14 days.
 

OVERDOSAGE:
No treatment is required other than general support and observation. For amounts greater than 50 mg/kg, induce gastric emptying (emesis induction or gastric lava).
 

PACKAGES AND COMPOSITION:
ORALUXE 100: 10 Film coated tablets. in an aluminum laminated foil, strip.
Each film coated tablet contains:
Cefpodoxime proxetil 130.45 mg corresponding to: Cefpodoxime 100 mg.
ORALUXE 200: 10 Film coated tablets. in an aluminum laminated foil, strip.
Each film coated tablet contains:
Cefpodoxime proxetil 260.09 mg corresponding to: Cefpodoxime 200 mg.
ORALUXE 50 mg/5 ml: Bottle of 60 ml dry powder suspension.
Each 5ml of reconstituted suspension contains:
Cefpodoxime proxetil 65.23 mg corresponding to: Cefpodoxime 50mg.
ORALUXE 100 mg/5 ml: Bottle of 60 ml dry powder suspension.
Each 5ml of reconstituted suspension contains:
Cefpodoxime proxetil 130.45 mg corresponding to: Cefpodoxime 100 mg.
 

STORAGE:
Store at room temperature. Keep out of the reach of children.
RECONSTITUTION FOR ORAL SUSPENSION:
Invert bottle and tab to loosen the powder. Add water, until the reconstituted suspension is at level with the mark on the bottle.
Following reconstitution the suspension is stable for 7 days at room temperature, or 14 days under refrigerator, (2 – 8)° C , keep container tightly closed.
Shake well before using.