Situroxime

SITUROXIME
Kaplet
Cefuroxime 500 mg

Composition :
Each caplet contains:

Cefuroxime axetil	601.98	mg
equivalent to Cefuroxime	500	mg

Pharmacodynamic properties :
Bacteriology : Cefuroxime axetil is an oral prodrug of the bactericidal Cephalosporin antibiotic Cefuroxime, which is resistant to most β-lactamases and is active againts a wide range of gram positive and gram-negative organism. Cefuroxime axetil owes its in-viva bactericidal activity to the parent compound Cefuroxime. Cefuroxime is a well characterized and effective antibacterial agent which has bactericidal activity against a wide range of common pathogens, including β-Lactamase producing strains. Cefuroxime has good stability to bacterial β-Lactamase and consequently is active against many Ampicillin-resistant or Amoxycillin-resistant strains. The bactericidal action of Cefuroxime results-from inhibition of Cell wall synthesis by binding to essential target proteins.

Cefuroxime is usually active against the following organism in-vitro:

• Aerobes gram negative: H.influenzae (including Ampicillin-resistant strains) and H.parainfluenzae, Moraxella (Branhamella) catarrhalis, N.gonorrhoeae (including Penicillinase and non-penicillinase producing strains), E.coli, Klebsiella spp, P.mirabilis and P.rettgeri, Providencia spp.
• Aerobes gram positive: Staphylococcus aureus and staphylococcus epidermidis (including penicillinase producing strains but excluding Methicillin resistant strains), Streptococcus pyogenes (and other β-haemolytic Streptococci) Streptococcus Pneumoniae, Streptococcus agalactiae (group-B streptococcus). 
• Anaerobes : Gram positive and gram negative cocci (including Peptococcus and Peptostreptococcus spp), gram positive bacilli (including Clostridium spp) and gram negative bacilli (including Bacteroides and Fusobacterium spp). Propionibacterium spp. 
• Other organisms Borrelia burgdorferi.

Indications:
Cefuroxime axetil is indicated for the treatment of infections caused by susceptible bacteria. Indications include :

• Upper respiratory tract infections, for example : Ear, nose and throat infections (such as otitis media, sinusitis, tonsillitis and pharyngitis).
• Lower respiratory tract infections, for example : Pneumonia, acute bronchitis, and acute exacerbations of chronic bronchitis. Genitourinary tract infections, for example : Pyelonephritis, cystitis and urethritis.
• Skin and soft tissue infections, for example : Furunculosis, pyoderma and impetigo.
• Gonorrhoea, acute uncomplicated gonococcal urethritis and cervicitis.
• Treatment of early Lime disease and subsequent prevention of late Lyme disease in adults and children over 12 years old. Cefuroxime is also available as the sodium salt for parenteral administration. This permits the use of sequential therapy with the same antibiotics, when a change from parenteral to oral therapy is clinically indicated.
• Where appropriate Cefuroxime is effective when used following initial parenteral Cefuroxime sodium in the treatment of pneumonia and acute exacerbations of chronic bronchitis.

Contraindication :
Patients with known hypersensitivity to Cephalosporin antibiotics

Dosage and administration:
The usual course of therapy is 7 days (range 5 - 10 days). Cefuroxime axetil should be taken after food for optimum absorption.

•	Adults:
	Most infections	:	250 mg	twice daily
	Urinary tract infections	:	125 mg	twice daily
	Mild to moderate lower respiratory tract infections, e.g. bronchitis	:	250 mg	twice daily
	More severe lower respiratory tract infections or if pneumonia is suspected	:	500 mg	twice daily
	Pyelonephritis	:	250 mg	twice daily
	Uncomplicated gonnorrhoea	:	1000 mg	as single dose
	Lyme disease in adults and children over 12 years of age	:	500 mg	twice daily for 20 day
•	Sequential therapy:
	Pneumonia: 1.5 g Cefuroxime bd (i.v) for 48 - 72 hours followed by 500 mg bd Cefuroxime axetil oral therapy for 7 days. Acute exacerbations of chronic bronchitis: 750 mg Cefuroxime bd (i.v.) for 48 - 72 hours followed by 500 mg bd Cefuroxirne axetil oral therapy for 5 - 7 days.
•	Duration of both parenteral and oral therapy is determined by severity of the infection and the clinical status of the patients.
•	Children:
	Most infections	:	125 mg (1 x 125 mg caplet) twice daily to a maximum dose of 250 mg daily
	Children aged 2 years or older with otitis media or, where appropriate, with more severe infections.	:	250 mg (1 x 250 mg caplet or 2 x 125 mg caplets) twice daily to a maximum of 500 mg daily.

Cefuroxime caplets should not be crushed and are therefore unsuitable for treatment of patients, such as younger children who cannot swallowed caplets. In children, cefuroxime oral suspension may be used. There is no experience of using cefuroxime in children under the age of 3 months.

• In common with other antibiotics, Cefuroxime may affect the gut flora, leading to lower estrogen reabsorption and reduced efficacy of combined oral contraceptives. Concurrent administration of Probenecid increases the area under the mean serum concentration time curve by 50 %. Serum levels of Cefuroxime are reduced by dialysis.

Overdosage :
Overdosage of Cephalosporins can cause cerebral irritation leading to convulsions. Serum levels of Cefuroxime can be reduced by haemodialysis and peritoneal dialysis.

Precautions:

• Special care is indicated in patients who have experienced an allergic reaction to Penicillin or other β-lactams. As with other antibiotics, prolonged use of Cefuroxime axetil may result in the overgrowth of nonsusceptible organisms (e.g. Candida, Enterococci, Clostridium difficile) which may require interruption of treatment.
• Pseudomembranous colitis has been reported with the use of-broad-spectrum antibiotics, therefore, it is important to consider its diagnosis in patients who develop serious diarrhea during or after antibiotic use.
• The Jarisch-Herxheimer reaction has been seen following Cefuroxime treatment of Lyme disease. It results directly from the bactericidal activity of Cefuroxime on the causative organism of Lyme disease, the Spirochaeta Borrelia burgdorferi. Patients should be reassured that this a common and usually self-imiting consequence of antibiotic treatment of Lyme disease. With a sequential therapy regime, the timing of change to oral therapy is determined by severity of the infection, clinical status of the patients and susceptibility of the pathogens involved. If there is no clinical improvement within 72 hours, then the parenteral course of treatment must be reviewed.
• Please refer to the relevant prescribing information for Cefuroxime sodium before initiating sequental therapy. Use during pregnancy and lactation: There is no experimental evidence of embropathic or teratogenic effects attributable to Cefuroxime axetil but, as with all drugs, it should be administered with caution during the early months of pregnancy. Cefuroxime is excreted in human milk, and consequently caution should be exercised when Cefuroxime axetil is administered to a nursing mother.
• Effects on ability to drive and use machines : Not reported

Side Effects :

•	Blood and lymphatic system disorders :
	Common	:	Eosinophilia
	Uncommon	:	Positive Coombs tests, thrombocytopenia, leucopenia (sometimes profound)
	Very rare	:	Haemolytic anaemia. Cephalosporins as acIass tend to be absorbed anto the surface of red cells membranes and react with antibodies directed against the drug to produce a positive Coombs test (which can interfere with cross-matching of blood) and very rarely haemolytic anemia
•	Immune system disorders: Hypersensitivity reactions including :
	Uncommon	:	Skin rashes
	Rare	:	Urticaria, pruritus
	Very rare	:	Drug fever, serum sickness, anaphylaxis.
•	Nervous system disorders:
	Common	:	Headache
•	Gastrointestinal disorders :
	Common	:	Gastrointestinal disturbances including diarrhea, nausea.
	Uncommon	:	Vomiting
	Rare	:	Pseudomembranous colitis
•	Hepatobiliary disorders
	Common	:	Transient increases of hepatic enzyme levels (ALT/SGPT, AST/SGOT, LDH).
	Very rare	:	Jaundice (predominantly cholestatic), hepatitis.
•	Skin and subcutaneous tissue disorders :
	Very rare	:	Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (exanthematic necrolysis). See also Immune system disorders.
•	Infections and infestations:
	Common	:	Candida overgrowth form prolonged use.

Interactions :
Drugs which reduce gastric acidity may result in a lower bioavailability of Cefuroxime compared with that of the fasting state and tend to cancel the effect of enhanced post-prandial absorption. As a false negative result may occur in the ferricyanide test, it is recommended that either the Glucose oxidase or hexokinase methoda are used to determined blood/plasma Glucose levels in patients receiving Cefuroxime axetil. This antibiotic does not interfere in the alkaline picrate assay for creatinine.

• The following organisms are not susceptible to Cefuroxime : C. difficile, Pseudomonas spp, Campylobacter spp, Acinetobacter calcoaceticus, Listeria monocytogenes, Methicillin resistant strains of Staphylococcus aureus and Staphylococcus epidermidis, Legionella spp.
• Some strains of the following organisms are not susceptible to Cefuroxime : Enterococcus (Streptococcus) faecalis, Morganella morganii, P.vulgaris, Enterobacter spp, Citrobacter spp, Seratia spp, Bacteroides fragilis.

Pharmacokinetic properties: After oral administration, Cefuroxirne axetil is slowly absorbed from the gastrointestinal tract and rapidly hydrolysed in the intestinal mucosa and blood to release Cefuroxime into the circulation. Optimum absorption accurs when it is administered shortly after a meal. Peak serum levels (2 - 3 mg/L for a 125 mg dose, 4 - 6 mg/L for a 250 mg dose, 5 - 8 mg/L for a 500 mg dose, and 9 - 14 mg/L for a 1000 mg dose) occur approximately 2 - 3 hours after dosing when taken after food, unlike i. v. dosing which peaks immediately. The absorption of Cefuroxime from the suspension is more prolonged compared with caplets, leading to later, lower peak serum levels and slightly reduced systemic bioavailability (4 - 17 % less). Post peak levels, the serum half-life is between 1 - 1.5 hours. Protein binding has been variously stated as 33 - 50 % depending on the methodology used. Cefuroxime is not metabolized and is excreted by glomerular filtration and tubular secretion. Concurrent administration of Probenecid increases the area under the mean serum concentrations time curve by 50%. Serum levels of cefuroxime are reduced by dialysis,
Preclinical safety data: No additional data of relevance.

Storage :
Store at room temperature between (25 - 30)°C Keep away from light

Availabilily :
Box, 3 strips @ 10 caplets
Reg.No. DKL 1002503104A1

HARUS DENGAN RESEP DOKTER

Produced by :
PT. PRAFA
Citeureup, Bogor - Indonesia

for
PT. Pharmasi Binangkit
Majalengka - Indonesia

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