Medzyme/Medzyme Vial

Medzyme/Medzyme Vial

cefuroxime

Manufacturer:

Medhaus

Distributor:

Medhaus
Full Prescribing Info
Contents
Medzyme: Cefuroxime axetil.
Medzyme Vial: Cefuroxime sodium.
Action
Medzyme: Pharmacological Classification: Antibacterial.
Pharmacology: Cefuroxime is a second-generation cephalosporin antibiotic with similar or less activity than first-generation cephalosporins against gram-positive cocci, but relatively resistant to beta-lactamases produced by Gram-negative bacteria.
Pharmacokinetics: After oral administration, cefuroxime axetil is absorbed from the gastrointestinal tract and rapidly hydrolyzed in the intestinal mucosa and blood to release cefuroxime into the circulation.
Following administration of cefuroxime axetil tablets, peak serum levels (2.9 mg/mL for a 125 mg dose, 4.4 mg/mL for a 250 mg dose, 7.7 mg/mL for a 500 mg dose and 13.6 mg/mL for a 1 g dose) occur approximately 2.4 hours after dosing when taken with food.
Absorption of cefuroxime axetil suspension is enhanced in the presence of food. The rate of absorption of cefuroxime from the suspension compared with the tablets is reduced, leading to later, lower peak serum levels and slightly reduced systemic bioavailability (4-17% or less). The serum half-life is between 1 and 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 concentration time curve by 50%. Serum levels of cefuroxime are reduced by dialysis. Cefuroxime passes the blood-brain barrier when the meninges are inflamed.
Medzyme Vial: Pharmacology: The bactericidal action of cefuroxime results from inhibition of bacterial cell-wall synthesis by binding to bacterial essential target proteins, penicillin-binding proteins.
Cefuroxime has a well-characterized and effective antibacterial activity against a wide range of common pathogens including beta-lactamase-producing strains of both Gram-positive and Gram-negative bacteria. Cefuroxime has good stability against many beta-lactamase produced by bacteria, especially enterobacteria.
Antibacterial spectrum: Cefuroxime is active against aerobic and anaerobic Gram-negative and Gram-positive cocci including penicillinase producing Staphylococci and active against Gram-negative intestinal bacteria. Cefuroxime has high potency and thus low MIC-values for Streptococci (group A, B, C and G), Gonococci and Meningococci.
The drug was originally presented to have low MIC-values for beta-lactamase producing Gonococci, Moraxella catarrhalis, Haemophilus influenzae and Klebsiella spp. In Vietnam, this has now changed and many bacteria are resistant. Strains of Enterobacter, Bacteroides fragilis and indole-positive Proteus have decreased sensitivity.
Clostridium difficile, Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Legionella spp. are not susceptible to Cefuroxime.
Methicillin-resistant strains of Staphylococcus aureus, Staphylococcus epidermidis are also resistant against cefuroxime. Listeria monocytogenes and most strains of Enterococci are resistant to cefuroxime.
The data from 1997 and 1999 ASTS reports have shown that cefuroxime still has useful activity against Salmonella with susceptibility of 100% of the testes isolates in Hue central hospital in 1996.
The current pathogenic bacterial resistance against cefuroxime has been reported to increase as follows: Shigella flexneri has been reported to be resistant in 11% of the isolates studied in 1998; Proteus mirabilis, 28.6% in 1997; Citrobacter 46.7% in 1997; E.coli, 33.5% in 1998; Klebsiella spp., 57% in 1997; Enterobacter, 59% in 1998; Streptococcus viridans, 31% in 1996; S. aureus, 33% in 1998.
Recent studies in Vietnamese healthy children, colonised with Haemophilus influenzae, also indicated a surprisingly high rate of cefuroxime resistance. Haemophilus influenzae was totally resistant against cefuroxime in 27% of the studied isolates (ASTS Information No. 4/1999 on pathogenic bacterial resistance against antibiotics). This is a serious situation, showing that broad-spectrum antibiotics must be restricted only for use in patients with severe infections.
Pharmacokinetics: Peak plasma concentrations about 27 μg/ml occurred at 45 minutes after an I.M. dose of 750 mg, and peak plasma concentrations about 50 μg/ml at 15 minutes after an I.V. dose of 750 mg. Therapeutic serum concentrations with measurable amounts are present 8 hours after a dose. 50% cefuroxime in the circulation is bound to plasma proteins. The plasma half-life is about 70 minutes and is prolonged with renal impairment and in neonates.
Cefuroxime is widely distributed in the body including pleural fluid, sputum, bone, synovial fluid and aqueous humor. The blood-brain barrier can be passed by cefuroxime when the meninges are inflamed. It crosses the placenta and has been detected in breast milk. Cefuroxime is not metabolized and is excreted unchanged to approximately 50% by glomerular filtration and 50% through the renal tubular secretion. High concentrations are achieved in the urine. Only very small amounts of cefuroxime are excreted in bile.
Indications/Uses
Used in the treatment of susceptible infections: bone and joint infections, bronchitis (and other lower respiratory tract infections), gonorrhea, meningitis (although treatment failures have been reported in H. influenza meningitis), otitis media, peritonitis, pharyngitis, sinusitis, skin infections (including soft tissue infections), and urinary tract infections. It is also used for surgical infection prophylaxis.
Dosage/Direction for Use
Medzyme: Suspension 125 mg and 250 mg: Children (more than 6 months): 125 mg: 1 teaspoonful twice daily.
250 mg (maximum): 2 teaspoonful daily.
Over 2 years old: 250 mg: 1 teaspoonful twice daily.
500 mg (maximum): 2 teaspoonful daily.
Or as prescribed by the physician.
500mg Film-coated Tablet: Adults: 500 mg twice daily.
Or as prescribed by the physician.
Medzyme Vial: Adults: For more severe infections, this dose should be increased to 1.5 g three or four times a day, IV injection. Total dose is 3g-6g daily.
Infants and Children: 30-100 mg/kg/day, given as three or four divided doses. A dose of 60 mg/kg/day will be appropriate for most infections.
Neonates: 30-100 mg/kg/day, given as two or three divided doses. In the first week of life, the serum half-life of Cefuroxime can be three to five times that in adults.
Gonorrhea: 1.5 g should be given as a single dose. This may be given as 2 x 750 mg injections into different sites, e.g. each buttock.
Prophylaxis: The usual dose is 1.5 g IV with induction of anesthesia for abdominal, pelvic and orthopedic operations, but may be supplemented with two 750 mg IM doses eight and sixteen hours later. In cardiac, pulmonary, esophageal and vascular operations, the usual dose is 1.5 g IV with induction of anesthesia continuing with 750 mg three times a day, IM t.i.d. for a further 24 to 48 hours. In total joint replacement, 1.5 g cefuroxime powder may be mixed dry with the methyl methacrylate cement.
Meningitis: Adults: 3 g I.V. every eight hours.
Infants and Children: 200 to 240 mg/kg/day I.V in three or four divided doses. This dosage may be reduced to 100 mg/kg/day IV after three days or when clinical improvement occurs.
Neonates: The initial dosage should be 100 mg/kg/day I.V. A reduction to 50 mg/kg/day IV may be made when clinically indicated.
Overdosage
Medzyme: Symptoms: Encephalopathy, convulsions and coma.
Management: Haemodialysis or peritoneal dialysis may reduce serum levels.
Medzyme Vial: Most agents cause only nausea, vomiting and diarrhea, although neuromuscular, hypersensitivity and seizures are possible, especially in patients with renal insufficiency.
Managing overdose: Protect the patient's airway and support ventilation and perfusion. If the patient develops convulsions, the drug should be promptly discontinued; anticonvulsant therapy may be administered if clinically indicated.
Haemodialysis may be helpful to aid in the removal of the drug from the blood but not usually indicated; otherwise most treatment is supportive or symptom-directed.
Contraindications
Medzyme: Hypersensitivity to cefuroxime or to other cephalosporins.
Medzyme Vial: Patients with known allergy to the cephalosporin group of antibiotics and penicillin.
Special Precautions
Medzyme: History of hypersensitivity to penicillin, and GI disease (particularly colitis). Renal impairment. Pregnancy and lactation.
Medzyme Vial: Careful inquiry should be made concerning previous allergic reactions of the patient to cephalosporins, penicillins and other drugs prior to initiation of cefuroxime therapy.
Dosage of cefuroxime should be reduced in patients with transient or persistent renal insufficiency because high and prolonged serum antibiotic concentrations can occur in such in individuals given usual doses.
Prolonged use of cefuroxime may result in the over-growth of non-susceptible organisms. Careful observation of the patient is therefore essential. If severe super-infection occurs during therapy, the drug treatment should be interrupted.
Pseudomembranous colitis has been reported with the use of broad-spectrum antibiotics, one primary cause is Clostridium difficile, and therefore, it is important to consider this diagnosis and to treat with metronidazole patients who develop severe diarrhea in association with the use of antibiotics. Broad-spectrum antibiotics should therefore also be prescribed with extra caution in individuals with a history of gastro-intestinal disease, particularly colitis.
Effects on ability to drive and operate machines: The drug does not affect ability to drive and operate machines.
Use In Pregnancy & Lactation
Medzyme: Cefuroxime falls under the FDA's Pregnancy Category B, which means that it's generally safe for the unborn baby. Regardless, the patient should tell the doctor if she is pregnant or plan to become pregnant before taking this medication.
Limited information indicates that cefuroxime produces low levels in milk that are not expected to cause severe adverse effects in breastfed infants. Cefuroxime is acceptable in nursing mothers.
Medzyme Vial: As the safety during pregnancy has not yet been established, this drug should be used during pregnancy or suspected pregnancy only if the potential benefit justifies the potential risk.
It is reported that this drug is secreted in human milk. Thus, should be used with caution in lactating mothers.
Adverse Reactions
Medzyme: As with other cephalosporins, there have been rare reports of erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (exanthematic necrolysis) and hypersensitivity reactions including skin rashes, urticaria, pruritus, interstitial nephritis, drug fever, serum sickness and very rarely anaphylaxis.
Some patients receiving cefuroxime axetil have experienced gastrointestinal disturbances including diarrhea, nausea and vomiting. As with other broad spectrum antibiotics, there have been occasional reports of pseudomembranous colitis. Headache has also been reported.
There have been rare reports of thrombocytopenia and leucopenia. As with other cephalosporins, jaundice has been reported very rarely.
Medzyme Vial: Common: Local irritation and thrombophlebitis following intravenous injection, diarrhea, maculopapular rash.
Less common: anaphylactic reaction, Candida infection, eosinophilia, leucopenia, neutropenia, nausea, vomiting, urticaria, pruritus.
Rare: fever, haemolytic anemia, pseudomembranous colitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, cholestatic jaundice, slight elevation of AST, ALT, and nephrotoxicity with transient elevations of blood urea nitrogen/creatinine, interstitial nephritis.
Inform the doctor or pharmacist in case of any adverse reactions related to drug use.
Drug Interactions
Medzyme: Probenecid reduces the renal clearance of cefuroxime.
Medzyme Vial: Used concurrently, furosemide-diuretics or aminoglycoside antibiotics may increase renal disorder. Thus, in such cases, carefully monitor renal function, particularly, for the aged and the patients with a history of renal impairment.
High-dose probenecid decreases cefuroxime renal clearance, giving rise to higher and more prolonged plasma concentrations of cefuroxime.
Caution For Usage
Medzyme: Direction for Reconstitution: Medzyme 125 mg/5mL Granules for Suspension: To make 50 ml reconstituted suspension, shake the bottle well until granules loosen. Pour 25 mL water and shake vigorously until the powder is evenly suspended.
Medzyme 250 mg/5mL Granules for Suspension: To make 50 ml reconstituted suspension, shake the bottle well until granules loosen. Pour 25 mL water and shake vigorously until the powder is evenly suspended.
Shake well before each use. Replace cap securely after each opening. Store the reconstituted suspension in a refrigerator between 2°C and 8°C (36°F and 46°F). DISCARD AFTER 10 DAYS.
Medzyme Vial: Direction for Reconstitution: Intravenous: Dissolve cefuroxime (MEDZYME) in water for injections using at least 15 ml for 1.5 g.
For short intravenous infusion (e.g. rp to 30 minutes), 1.5 g may be dissolved in 50 mL water for injections. It is not desirable to use sodium bicarbonate injection as a diluent of this drug.
Storage
Store at temperatures not exceeding 30°C. Store the reconstituted suspension in a refrigerator between 2°C and 8°C (36°F and 46°F). Protect from light.
MIMS Class
Cephalosporins
ATC Classification
J01DC02 - cefuroxime ; Belongs to the class of second-generation cephalosporins. Used in the systemic treatment of infections.
Presentation/Packing
Medzyme: FC tab 500 mg x 40's. Granules for oral susp 125 mg/5 mL x 50 mL. 250 mg/5 mL x 50 mL.
Medzyme Vial: Powd for inj (vial) 750 mg x 10's. 1.5 g x 10's.
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