Cimex

Cimex

cefuroxime

Manufacturer:

Multicare

Distributor:

Zuellig
Full Prescribing Info
Contents
Cefuroxime salts.
Description
Each film-coated tablet contains cefuroxime axetil equivalent to cefuroxime 500 mg. Each 5 mL of powder for oral suspension contains cefuroxime axetil 125 mg or 250 mg. Cefuroxime axetil is a semisynthetic broad-spectrum cephalosporin antibiotic given orally. Cimex tablet and suspension contains cefuroxime axetil, which is bactericidal against many pathogens, including many β-lactamase strains.
Each 750-mg and 1.5-g vial contains cefuroxime sodium 750 mg and 1.5 g, respectively.
Action
Pharmacology: Pharmacodynamics: Tablet: Cefuroxime axetil is the acetyloxyethyl ester of cefuroxime. Cefuroxime axetil belongs to the 2nd generation of cephalosporins, and compared to the 1st generation of cephalosporins are not only active against gram-positive but also gram-negative organism. The mechanism of action of cefuroxime axetil, similar to all cephalosporins and it acts by combining with the penicillin bound proteins (PBP) part of the bacterial cell wall resulting in the lysis of the cell wall and as a consequence causing cell death and therefore having a bactericidal action. Axetil is the prodrug of the active compound cefuroxime. When given orally, cefuroxime axetil is hydrolyzed to cefuroxime by nonspecific esterases in the intestinal mucosa. Cefuroxime is distributed throughout the extracellular fluid. The axetil part is metabolized to acetaldehyde and acetic acid.
Suspension: Cefuroxime is bactericidal and has similar spectrum of antimicrobial action and pattern resistance to cefamandole. It is more resistant to hydrolysis by β-lactamases than cefamandole, and therefore may be more active against β-lactamase-producing strains of Haemophilus influenzae and Neisseria gonorrheae.
Pharmacokinetics: Tablet: Following oral administration, 30-50% of the drug is absorbed. Around 50% of the serum cefuroxime is protein bound. The Cmax following oral administration of 250 mg and 500 mg of cefuroxime axetil in normal healthy adults is reported to be 4.1 and 7 mcg/mL and the tmax ranges from 2-3 hrs. The mean elimination t½ is approximately 1.2 hrs for all dose. Cefuroxime is eliminated unchanged in the urine, and 50% of the administered dose is recovered in the urine in 12 hrs. The serum t½ is therefore prolonged in patients with reduced renal function. However, no special precaution is necessary in patients with renal impairment or on renal dialysis or in the elderly at doses up to normal maximum of 1 g/day.
Suspension: Cefuroxime axetil is absorbed from the GIT and is rapidly hydrolyzed in the intestinal mucosa and blood to cefuroxime; absorption is enhanced in the presence of food. Peak plasma concentration are reported about 2-3 hrs after an oral dose. Up to 50% of cefuroxime in the circulation is bound to plasma proteins. The plasma t½ is about 70 min and is prolonged in patients with renal impairment and in neonates.
Cefuroxime is widely distributed in the body including pleural fluid, sputum, bone, synovial fluid and aqueous humor, but only achieves therapeutic concentrations in the cerebrospinal fluid when the meninges are inflamed. It crosses the placenta and has been detected in breast milk.
Cefuroxime is excreted unchanged, by glomerular filtration and renal tubular secretion and high concentrations are achieved in the urine. Probenecid competes for renal tubular secretion with cefuroxime resulting in higher and more prolonged plasma concentrations of cefuroxime. Small amounts of cefuroxime are excreted in bile. Plasma concentration are reduced by dialysis.
Microbiology: Tablet: Antibacterial Activity: Aerobic Gram-Positive Microorganisms: Staphylococcus aureus (including β-lactamase-producing strain, but not methicillin-resistant strains), Streptococcus pneumoniae, Streptococcus pyogenes.
Aerobic Gram-Negative Microorganisms: Escherichia coli, Haemophilus influenzae (including β-lactamase producing strain), Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Neisseria gonorrheae (β-lactamase negative strains only).
In vitro activity is present against the following organisms: Staphylococcus epidermidis, Morganella morganii, Neisseria gonorrheae (β-lactamase-producing strains only), Proteus mirabilis.
Indications/Uses
Tablet: Treatment of the following infections cause by sensitive bacteria: Lower respiratory tract infections eg, acute bronchitis, acute exacerbation of acute bronchitis and pneumonia; upper respiratory tract infection eg, ear, nose, throat infections eg, otitis media, sinusitis, tonsillitis or pharyngitis; peritonitis; uncomplicated genitourinary tract infections eg, pyelonephritis, cystitis and urethritis; gonorrhea eg, acute uncomplicated gonorrhea, urethritis and cervicitis; skin infections eg, furunculosis, pyodema and impetigo; bone and joint infections; urinary tract infection; meningitis.
Treatment of early Lyme disease and subsequent prevention of late Lyme disease in adults and children >12 years.
Suspension: Treatment of susceptible infections including those bone and joint infections, bronchitis (and other lower respiratory tract infections), gonorrhea, meningitis, otitis media, peritonitis, pharyngitis, sinusitis, skin infections (including soft tissue infections) and urinary tract infection. Prophylaxis for surgical infection.
Injection: Susceptible Strains: Streptococcus aureus (including penicillin-resistant strains, excluding methicillin-resistant strains), Staphylococcus epidermidis (excluding methicillin-resistant strains), Haemophilus influenzae (including ampicillin-resistant strains), parainfluenzae (including ampicillin-resistant strains), Klebsiella spp, Streptococcus pyogenes, Group B streptococcus, Streptococcus pneumoniae, Escherichia coli, Streptococcus viridans, Clostridium, Proteus mirabilis, Bacillus typhosus, Salmonella spp, Shigella spp, Neisseria gonorrheae (including β-lactamase-producing strains), Bordetella pertussis, Pneumoniae, Proteus vulgaris, Proteus morganii, Enterobacter spp, Citrobacter spp, Serratia spp, Streptococcus faecalis.
Acute or chronic bronchitis, bronchiectasis, bacterial pneumonia, pneumonial abscess, postoperational chest infection, otitis media, sinusitis, tonsillitis, pharyngitis, nephropyelitis, skin and soft tissue infections, cystitis, cellulitis, erysipelas, peritonitis, wound infection, myelitis, septic arthritis, gonorrhea, urinary tract infections, septicemia, meningitis, postoperational infections on areas eg, abdomen, pelvis, heart, lung, esophagus, blood vessels. Endometritis, perimetritis, suprapelvic infection. Surgical infection prophylaxis.
Dosage/Direction for Use
Tablet: Adults: Pharyngitis/Tonsillitis, Acute Sinusitis: 250-500 mg twice a day.
Acute Exacerbation of Chronic Bronchitis/Acute Bronchitis, Skin Infections: 250-500 mg twice daily.
Uncomplicated Gonorrhea: Single dose of 1 g is recommended.
Uncomplicated Urinary Tract Infection: 125 or 250-500 mg twice daily.
125 mg/5 mL Suspension: Adults: 5-20 mL (1-4 tsp) twice daily.
Children >2 years: 10 mL (2 tsp) or 15 mg/kg body weight twice daily. Maximum Dose: 20 mL daily; >3 months: 5 mL (1 tsp) or 10 mg/kg body weight twice daily. Maximum Dose: 10 mL (2 tsp) daily.
250 mg/5 mL Suspension: Adults: 5-10 mL (1-2 tsp) twice daily.
Children >2 years: 5 mL (1 tsp) or 15 mg/kg body weight twice daily. Maximum Dose: 10 mL (2 tsp) daily; >3 months: 2.5 mL (½ tsp) or 10 mg/kg body weight twice daily. Maximum Dose: 5 mL (1 tsp) daily.
IM/IV Injection: Adults: 750 mg of cefuroxime sodium is administered IV or IM every 8 hrs but in more severe infections, 1.5 g is administered IV every 8 hrs. If necessary, it is administered IV or IM every 6 hrs but it should not exceed 3-6 g/day.
Infants and Children: A daily dose of 30-100 mg/kg body weight is administered IV or IM in 3 or 4 divided doses. Usually 60 mg/kg daily is suitable.
Neonates: A daily dose of 30-100 mg/kg is administered IV or IM in 2 or 3 divided doses. Cimex should be used cautiously because t½ of cefuroxime sodium may be 3-5 times that of adults during 1 week after birth.
Gonorrhea: 1.5 g of cefuroxime sodium is administered IM or 750 mg of 1.5 g (potency) is administered to each side of buttock.
Renal Impairment: In patients with slightly impaired renal function, there is no need to reduce the dosage of cefuroxime sodium. But in case of severe renal function, (creatinine clearance between 10 and 20 mL/min) the dosage should only be given twice daily and in case of preterminal renal function (CrCl is low 10 mL/min) once daily. Patients undergoing hemodialysis should receive an additional 750 mg dose following each dialysis; those undergoing continuous peritoneal dialysis may be given 750 mg twice daily.
Perioperative Prophylaxis: Abdomen, Pelvis, Orthopedic Surgery: Usual Dose: 1.5 g of cefuroxime IV prior to the procedure; this may be supplemented by 750 mg (potency) IM after 8 and 16 hrs.
Heart, Lung, Esophagus, Vessel Surgery: Usual Dose: 1.5 g of cefuroxime IV prior to the procedure; this may be supplemented by 750 mg IM every 8 hrs for up to 24-84 hrs.
Total Joint Replacement: 1.5 g of cefuroxime powder may be mixed with the methylmethacrylate cement before addition of liquid monomer.
Meningitis: Adults: 3 g is administered IV every 8 hrs.
Infants and Children: A daily dose of 200-240 mg/kg body weight is administered IV in 3 or 4 divided doses; after clinical improvement for 3 days, dosage may be reduced to 100 mg/kg daily.
Neonates: An initial daily dose of 100 mg/kg is administered IV; after clinical improvement, dosage may be reduced to 50 mg/kg daily.
Overdosage
Tablet: Can cause cerebral irritation leading to convulsion. Serum levels can be reduced by haemodialysis and peritoneal dialysis.
Contraindications
Hypersensitivity to cephalosporins or with cefuroxime itself.
Injection: Patients with history of shock to cefuroxime sodium or cefuroxime axetil.
Special Precautions
Tablet: Cefuroxime axetil may be given safely to patients who are hypersensitive to penicillins. Special care is indicated in patients who have experienced anaphylactoid reactions with penicillin. Prolonged use of cefuroxime may result in overgrowth of susceptible organism. There is no evidence of embryogenic and teratogenic effect due to cefuroxime axetil. Should be administered with caution in pregnancy especially during the early period. Cefuroxime is excreted in milk. A Jarisch Herxheimer reaction has been reported following administration of cefuroxime in Lyme disease. Pseudomembranous colitis has been reported with cefuroxime. A false positive reaction for glucose in the urine may occur with copper reductive tests (Benedict's test). It is recommended that either the glucose oxidase or hexokinase methods be used to determine blood/plasma glucose level. Should be given with caution to patients receiving concurrent treatment with potent diuretics.
Suspensions: Care is also necessary in patients with history of allergy.
Cefuroxime should be given in cautions to patients with renal impairment; a dosage reduction may be necessary. Renal hematological status should be monitored especially during prolonged and high-dose therapy.
Injection: In principle, Cimex should not be administered in patients with history of hypersensitivity to cephem antibiotics, but if inevitable, cautious administration is required. Patients with history of hypersensitivity to penicillins or β-lactam antibiotics. Patients or whose parents, sisters or brothers are prone to suffer from allergic symptoms eg, bronchial asthma, exanthema, urticaria. Patients with severe renal disorder; poor oral ingestion, parenteral nutrition, poor general conditions and who are old aged (cautious monitoring is required since vitamin K deficiency may occur). Patients who are old aged or taking medicine eg, furosemide diuretics, aminoglycoside antibiotics.
General Precautions: In order to prevent appearance of resistant microorganisms, susceptibility should be determined. Also, the treatment should be continued only for the minimum period of time required.
In order to predict side effects eg, shock, patient's history should be taken in detail and skin reaction test should be performed.
Emergency measures have to be available in preparation for occurrence of shock and even after measures taken, the patient should be observed cautiously in stable condition.
It is desirable to perform laboratory tests (hepatic and renal function, blood) at regular intervals during treatment.
Cimex can be administered with aminoglycoside antibiotics and metronidazole but these should not be mixed in 1 injection.
In case of long-term dosage, overgrowth of insusceptible bacteria may occur.
Precautions on Application: As vascular pain, venous angialgia, thrombosis, phlebitis may rarely occur with large IV doses, caution should be taken on preparation of injectable solution, site of injection, method of administration and injection should be given as slowly as possible.
Cefuroxime should not be mixed with sodium bicarbonate.
Others: In the treatment of meningitis, a slight or moderately visual disorder have been reported in children to whom Cimex was administered. When it cultivates cerebrospinal fluid after 18-36 hrs of administration, positive influenza may appear but its interaction with the clinical effect has not been known.
Use in Pregnancy: Tablet: Pregnancy Category B. Reproduction studies have been performed in rats and mice at doses up to 3200 mg/kg/day (23 times the recommended maximum human dose based on mg/m3) and have revealed no evidence of harm to the fetus due to cefuroxime axetil. There are however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Injection: As safety in human pregnancy has not been established, cefuroxime should not be administered to pregnant women or women of childbearing potential unless therapeutic benefit is considered to exceed the possible risk.
Use in Lactation: Tablet: Because cefuroxime axetil is excreted in human milk, consideration should be given in discontinuing nursing temporarily during drug treatment with cefuroxime axetil.
Injection: As cefuroxime is excreted in human milk, caution is required when Cimex is administered to a nursing mother.
Use In Pregnancy & Lactation
Use in Pregnancy: Tablet: Pregnancy Category B. Reproduction studies have been performed in rats and mice at doses up to 3200 mg/kg/day (23 times the recommended maximum human dose based on mg/m3) and have revealed no evidence of harm to the fetus due to cefuroxime axetil. There are however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Injection: As safety in human pregnancy has not been established, cefuroxime should not be administered to pregnant women or women of childbearing potential unless therapeutic benefit is considered to exceed the possible risk.
Use in Lactation: Tablet: Because cefuroxime axetil is excreted in human milk, consideration should be given in discontinuing nursing temporarily during drug treatment with cefuroxime axetil.
Injection: As cefuroxime is excreted in human milk, caution is required when Cimex is administered to a nursing mother.
Adverse Reactions
Tablet: These are usually mild in nature. Gastrointestinal disturbance including diarrhea, nausea and vomiting, and headache have been reported. Eosinophilia and transient increase of hepatic enzymes (SGPT, OT and LIH) have also been reported. Jaundice and Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis, serum sickness-like reactions, anaphylaxis and angioedema have been reported rarely.
Suspension: Gastrointestinal disturbances including diarrhea, nausea and vomiting have occurred in some patients taking cefuroxime. There have been reports of erythema multiforme, Stevens-Johnson syndrome and toxic epidermal syndrome.
Injection: Shock: Shock may rarely occur. Therefore, cautious monitoring is required and if any abnormal sign is detected, further administration should be discontinued and appropriate measures should be taken.
Skin: Stevens-Johnson syndrome (mucocutaneous ocular syndrome), erythema multiforme, toxic epidermal necrotic syndrome. These symptoms may rarely occur. Therefore, cautious monitoring is required and if any abnormal sign is detected, further administration should be discontinued.
Hypersensitivity: Pruritus, shivering, exanthema (erythema, wheal), fever, urticaria, lymph node tumidity, arthrodynia, anaphylactic reaction.
Kidney: Severe renal disorder (interstitial nephritis, acute renal failure) These symptoms may rarely occur. Therefore, cautious monitoring is required and if abnormal sign is acknowledged, further administration should be discontinued and appropriate measures taken.
Blood: Rarely, decreased hemoglobin concentration, anemia, granulocytopenia, leukopenia, thrombocytopenia, occasionally neutropenia, hypoeosinophilia, thrombophlebitis may occur. Also it has been reported that with administration of cephalosporin antibiotics, hemolytic anemia occurred.
Liver: Abnormal liver function eg, elevation of ALT, AST and ALP may occasionally occur and elevation of bilirubin, γ-GPT may rarely occur.
Gastrointestinal System: Severe enterocolitis with hemafecia eg, pseudomembranous enterocolitis may rarely occur. If abnormal pain and frequent diarrhea occur, appropriate measures eg, immediate discontinuation of cefuroxime sodium be taken. Also nausea, diarrhea, rarely vomiting, anorexia may occasionally occur.
Respiratory System: Since interstitial pneumonia, pulmonary infiltration with eosinophilia (PIE) syndrome accompanied with fever, cough, dyspnea, abnormal chest x-ray, eosinophilia may rarely occur with other cephems. In case that such symptoms occur, further administration should be discontinued and appropriate measures eg, administration of adrenal cortical hormone should be taken.
Superinfection: Candidiasis intertrigo may rarely occur.
Vitamin Deficiency: Symptoms of vitamin K deficiency (hypoprothrombinemia, hemorrhage tendency) and vitamin B deficiency (glossitis, stomatitis, anorexia, neuritis) may rarely occur.
Others: Palsy may rarely occur. In the treatment of meningitis, especially in children, slight acoustic disorders occurred.
Drug Interactions
Tablet: Cefuroxime axetil is not bioequivalent and is therefore not substitutable on a mg/mg basis. Before therapy with cefuroxime axetil is instituted, careful inquiry should be made to determine whether the patients has had previous hypersensitivity reactions to cefuroxime axetil, other cephalosporins, penicillin or other drugs. If Cimex is to be given to penicillin-sensitive patients, caution should be exercised because cross-hypersensitivity among β-lactam antibiotics have been clearly documented and may occur up to 10% of patients with history of penicillin allergy. If a clinically significant allergic reaction to cefuroxime axetil occurs, discontinue the drug and institute appropriate therapy, serious acute hypersensitivity reactions may require treatment with epinephrine and other emergency measures, including oxygen, IV fluids, and IV antihistamines, corticosteroids, pressor amines and airway management as clinically indicated.
Pseudomembranous colitis has been reported with nearly all antibacterial agents, including cefuroxime and may range from mild to life-threatening. Therefore, it is important to consider this diagnosis in patients who present with diarrhea, subsequent to the administration of antibacterial agents.
Treatment with antibacterial agents alters the normal flora of the colon and may permit overgrowth or clostridia. Studies indicate that a toxin by Clostridium difficile is 1 primary cause of antibiotic-associated colitis.
After diagnosis of pseudomembranous colitis has been established, appropriate therapeutic measures should be initiated. Mild cases of pseudomembranous colitis usually respond to drug discontinuation alone. In moderate to severe cases, consideration should be given in the management with fluids and electrolytes, protein supplementation and treatment with an antibacterial drug effective against Clostridium difficile.
Suspension: Probenecid reduces the renal clearance of cefuroxime.
Injection: When cefuroxime combines with diuretics like furosemide or aminoglycoside antibiotic, renal disorder could be increased. Therefore, caution for renal function is required. When cefuroxime is administered to old aged or patients with history of renal disorder, monitoring of renal function is required.
Interference with Laboratory Test: Caution should be taken as urine test using Benedict's reagent, Fehling's reagent, Clinitest, except for testape reaction, may give false-positive results.
Caution should be taken as direct Coombs' test may give false-positive results.
As with the decreasing of copper level, urine test results can be changed.
Caution For Usage
Suspension: Direction for Reconstitution: 125 mg/5 mL Suspension: To make 70 mL, 50 mL and 10 mL reconstituted suspension, mix thoroughly the contents with 30 mL, 24 mL and 5 mL, respectively of water and shake well until powder is evenly suspended.
250 mg/5 mL Suspension: To make 70 mL, 50 mL and 10 mL reconstituted suspension, mix thoroughly the contents with 28 mL, 22 mL and 5 mL, respectively of water and shake well until powder is evenly suspended.
Injection: Preparation of Injection Solution: IM Injection: Use suspension of cefuroxime sodium 250 mg with 11 mL of sterile water for injection.
IV Injection: Cefuroxime sodium 250 mg is dissolved in 2 mL, 750 mg is dissolved in 6 mL, 1.5 g is dissolved in 15 mL of sterile water for injection. When the drip IV injection is used, 1.5 g of cefuroxime sodium is dissolved in 50 mL of sterile water for injection and infused over 30 min. Cefuroxime should not be used with sodium bicarbonate solution. Use immediately after preparation. Discard any unused portion of the solution.
Storage
Store at temperatures not exceeding 30°C.
Tablet/Suspension: Protect from light.
The reconstituted suspension is stable for 7 days at temperatures not exceeding 30°C and 14 days under refrigeration (2-8°C).
MIMS Class
ATC Classification
J01DC02 - cefuroxime ; Belongs to the class of second-generation cephalosporins. Used in the systemic treatment of infections.
Presentation/Packing
FC tab 500 mg (white colored, biconvex, with breakline on one side and "Lupin" inscription on the other side) x 50's. Powd for oral susp 125 mg/5 mL x 50 mL, 70 mL. 250 mg/5 mL x 50 mL. Powd for inj (vial) 750 mg x 1's, 10's. 1.5 g x 1's, 10's.
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