Cefuroxime axetil

510.47

510.47

259-560-1

DTXSID0022775

White to almost white crystalline powder|White powder

2941905990

214.36000

0.85

white to off-white

1.6±0.1 g/cm3

175-180 °C

1.665

DMSO: soluble 1mg/mL

-20°C

9.95X10-16 mm Hg at 25 °C (est)

Peritoneal-rat LD50: 950 mg/kg; peritoneal-mouse LD50: 510 mg/kg

Thermal decomposition emits toxic nitrogen oxides and sulfur oxide fumes

Henry's Law constant = 2.81X10-21 atm-cu m/mol at 25 °C (est)

NONH for all modes of transport

3

R36/37/38:Irritating to eyes, respiratory system and skin .

S24/25

The warehouse is low-temperature, ventilated and dry

Stable under recommended storage conditions.

SRP: Expired or waste pharmaceuticals shall carefully take into consideration applicable DEA, EPA, and FDA regulations. It is not appropriate to dispose by flushing the pharmaceutical down the toilet or discarding to trash. If possible return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.|SRP: At the time of review, regulatory criteria for small quantity disposal are subject to significant revision, however, household quantities of waste pharmaceuticals may be managed as follows: Mix with wet cat litter or coffee grounds, double bag in plastic, discard in trash.

The Approved Drug Products with Therapeutic Equivalence Evaluations identifies currently marketed prescription drug products, including cefuroxime axetil, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act.

|Danger|H317 (100%): May cause an allergic skin reaction [Warning Sensitization, Skin]|P261, P272, P280, P285, P302+P352, P304+P341, P321, P333+P313, P342+P311, P363, and P501|Aggregated GHS information provided by 18 companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Personal protective equipment: Respiratory protection: Respiratory protection is not required. Where protection from nuisance levels of dusts are desired, use type N95 (US) or type P1 (EN 143) dust masks. Use respirators and components tested and approved under appropriate government standards such as NIOSH (US) or CEN (EU). Hand protection: Handle with gloves. Gloves must be inspected prior to use. Use proper glove removal technique (without touching glove's outer surface) to avoid skin contact with this product. Dispose of contaminated gloves after use in accordance with applicable laws and good laboratory practices. Wash and dry hands. Eye protection: Use equipment for eye protection tested and approved under appropriate government standards such as NIOSH (US) or EN 166(EU). Skin and body protection: Choose body protection in relation to its type, to the concentration and amount of dangerous substances, and to the specific work-place., The type of protective equipment must be selected according to the concentration and amount of the dangerous substance at the specific workplace.

Not flammable or combustible.

Suitable extinguishing media: Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide. Special protective equipment for firefighters: Wear self contained breathing apparatus for fire fighting if necessary.

Personal precautions: Avoid dust formation. Avoid breathing vapors, mist or gas. Environmental precautions: Do not let product enter drains. Methods and materials for containment and cleaning up: Sweep up and shovel. Keep in suitable, closed containers for disposal.

SRP: Local exhaust ventilation should be applied wherever there is an incidence of point source emissions or dispersion of regulated contaminants in the work area. Ventilation control of the contaminant as close to its point of generation is both the most economical and safest method to minimize personnel exposure to airborne contaminants. Ensure that the local ventilation moves the contaminant away from the worker.|Provide appropriate exhaust ventilation at places where dust is formed.

moderately toxic

Drugs that reduce gastric acidity may result in a lower bioavailability of Ceftin compared with that of fasting state and tend to cancel the effect of postprandial absorption.|Oral probenecid administered shortly before or concomitantly with cefuroxime usually slows the rate of tubular secretion of cefuroxime and produces higher and more prolonged serum concentrations of cefuroxime. This effect is usually used to therapeutic advantage in the treatment of gonorrhea. Peak serum concentrations of cefuroxime and the half-life of the drug are reportedly increased by up to 30% when probenecid is administered concomitantly; the area under the concentration-time curve (AUC) of cefuroxime is increased by about 50%. Concomitant administration of probenecid also reportedly decreases the apparent volume of distribution of cefuroxime by about 20%.|Cefuroxime axetil may affect gut flora, leading to decreased estrogen reabsorption and reduced efficacy of oral contraceptives containing estrogen and progestin.|The manufacturers state that cefuroxime should be used with caution in patients receiving diuretics because concurrent use of these drugs may increase the risk of adverse renal effects.|In vitro studies indicate that the antibacterial activity of cefuroxime and aminoglycosides may be additive or synergistic against some organisms including Enterobacter, Escherichia coli, Klebsiella, Proteus mirabilis, and Serratia marcescens. Concurrent use of aminoglycosides and certain cephalosporins reportedly may increase the risk of nephrotoxicity during therapy. Although this effect has not been reported to date with cefuroxime, the possibility that nephrotoxicity may be potentiated should be considered if the drug is used concomitantly with an aminoglycoside.

LD50 Rabbit oral 200 mg/kg|LD50 Mouse sc 1840 mg/kg|LD50 Mouse ip 510 mg/kg|LD50 Rat sc 2500 mg/kg|LD50 Rat ip 950 mg/kg

Prior to initiation of cefuroxime therapy, careful inquiry should be made concerning previous hypersensitivity reactions to cephalosporins, penicillins, or other drugs. Cefuroxime axetil /is/ contraindicated in patients who are hypersensitive to cefuroxime or other cephalosporins and should be used with caution in patients with a history of hypersensitivity to penicillins. Use of cephalosporins should be avoided in patients who have had an immediate-type (anaphylactic) hypersensitivity reaction to penicillins.

Anti-Bacterial Agent|Ceftin tablets and oral suspension /are indicated for/ acute bacterial otitis media caused by Streptococcus pneumoniae, Haemophilusinfluenzae(including beta-lactamase-producing strains), Moraxellacatarrhalis (including beta-lactamase-producing strains), or Streptococcus pyogenes. /Included in US product label/|Ceftin tablets and oral suspension /are indicated for/ pharyngitis/tonsillitis caused by Streptococcus pyogenes. NOTE: The usual drug of choice in the treatment and prevention of streptococcal infections, including the prophylaxis of rheumatic fever, is penicillin given by the intramuscular route. Ceftin Tablets are generally effective in the eradication of streptococci from the nasopharynx; however, substantial data establishing the efficacy of cefuroxime in the subsequent prevention of rheumatic fever are not available. Please also note that in all clinical trials, all isolates had to be sensitive to both penicillin and cefuroxime. There are no data from adequate and well-controlled trials to demonstrate the effectiveness of cefuroxime in the treatment of penicillin-resistant strains of Streptococcus pyogenes. /Included in US product label/|Ceftin tablets /are indicated for/ acute bacterial maxillary sinusitis caused by Streptococcus pneumoniaeorHaemophilusinfluenzae (non-beta-lactamase-producing strains only). NOTE: In view of the insufficient numbers of isolates of beta-lactamase-producing strains of Haemophilusinfluenzae and Moraxellacatarrhalis that were obtained from clinical trials with Ceftin Tablets for patients with acute bacterial maxillary sinusitis, it was not possible to adequately evaluate the effectiveness of Ceftin Tablets for sinus infections known, suspected, or considered potentially to be caused by beta-lactamase-producing Haemophilusinfluenzae or Moraxellacatarrhalis. /Included in US product label/|For more Therapeutic Uses (Complete) data for Cefuroxime axetil (15 total), please visit the HSDB record page.

Patients should be advised that antibacterials (including cefuroxime) should only be used to treat bacterial infections and not used to treat viral infections (e.g., the common cold). Patients also should be advised about the importance of completing the full course of therapy, even if feeling better after a few days, and that skipping doses or not completing therapy may decrease effectiveness and increase the likelihood that bacteria will develop resistance and will not be treatable with cefuroxime or other antibacterials in the future.|To reduce development of drug-resistant bacteria and maintain effectiveness of cefuroxime and other antibacterials, the drug should be used only for the treatment or prevention of infections proven or strongly suspected to be caused by susceptible bacteria. When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing. In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.|Prior to initiation of cefuroxime therapy, careful inquiry should be made concerning previous hypersensitivity reactions to cephalosporins, penicillins, or other drugs. Cefuroxime axetil /is/ contraindicated in patients who are hypersensitive to cefuroxime or other cephalosporins and should be used with caution in patients with a history of hypersensitivity to penicillins. Use of cephalosporins should be avoided in patients who have had an immediate-type (anaphylactic) hypersensitivity reaction to penicillins.|Prescribing Ceftin in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.|For more Drug Warnings (Complete) data for Cefuroxime axetil (18 total), please visit the HSDB record page.

Substances that inhibit the growth or reproduction of BACTERIA. (See all compounds classified as Anti-Bacterial Agents.)

Following oral administration of cefuroxime axetil in pediatric patients with acute otitis media with effusion or with chronic or recurrent otitis media with effusion, cefuroxime is distributed into middle ear effusions. In a study in pediatric patients 1-4 years of age with acute otitis media with effusion who received a single 15 mg/kg dose of cefuroxime as cefuroxime axetil oral suspension, cefuroxime concentrations in middle ear effusions 2-5 hours after a dose ranged from 0.2-3.6 ug/mL; concurrent serum concentrations were 2.8-7.3 ug/mL.|In pharmacokinetic studies of cefuroxime axetil oral suspension in children, the drug was administered postprandially or with food; no data are available regarding absorption of the suspension in fasting children. Following oral administration to children 3 months to 12 years of age (mean age: 23 months) of a single 10-, 15-, or 20-mg/kg dose of commercially available cefuroxime axetil oral suspension concomitantly with milk or milk products, peak serum cefuroxime concentrations are attained approximately 3.6, 2.7, or 3.1 hours after the dose, respectively, and average 3.3, 5.1, or 7 mcg/mL, respectively.|Results of a study in healthy adults indicate that cefuroxime axetil oral suspensions containing 125 mg/5 mL or 250 mg/5 mL are bioequivalent. In healthy adults who received a 250-mg dose of cefuroxime axetil given as a suspension containing 125 mg/5 mL or 250 mg/5 mL with food, peak plasma concentrations of cefuroxime were 2.4 or 2.2 aug/mL, respectively, and were attained 3 hours after the dose.|Following oral administration in adults of a single 125-mg, 250-mg, 500-mg, or 1-g dose of commercially available cefuroxime axetil tablets immediately following a meal, peak serum cefuroxime concentrations are attained approximately 2-3 hours after the dose and average 2.1, 4.1, 7, or 13.6 ug/mL, respectively; serum concentrations 6 hours after the dose average 0.3, 0.7, 2.2, or 3.4 ug/mL, respectively. AUC of the drug in these individuals averaged 6.7, 12.9, 27.4, or 50 mcg-h/mL, respectively.|For more Absorption, Distribution and Excretion (Complete) data for Cefuroxime axetil (13 total), please visit the HSDB record page.

Following oral administration, cefuroxime axetil is rapidly hydrolyzed to cefuroxime by nonspecific esterases in the intestinal mucosa and blood; the axetil moiety is metabolized to acetaldehyde and acetic acid. Cefuroxime is not metabolized and is excreted unchanged principally in urine by both glomerular filtration and tubular secretion.

In neonates and children, the serum half-life of cefuroxime is inversely proportional to age.6 25 30 Following oral administration of cefuroxime axetil oral suspension in children 3 months to 12 years of age, the serum half-life of cefuroxime averages 1.4-1.9 hours.|In adults, the serum or plasma half-life of cefuroxime following oral administration of commercially available cefuroxime axetil tablets or oral suspension ranges from 1.2-1.6 hours.|Because cefuroxime is renally excreted, the serum half-life is prolonged in patients with reduced renal function. In a study of 20 elderly patients (mean age = 83.9 years) having a mean creatinine clearance of 34.9 mL/min, the mean serum elimination half-life was 3.5 hours.

Cefuroxime is usually bactericidal in action.Like other cephalosporins, the antibacterial activity of the drug results from inhibition of mucopeptide synthesis in the bacterial cell wall.

/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/|/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/|/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/

/CASE REPORTS/ Thrombotic thrombocytopenic purpura (TTP) or Moschcowitz's syndrome is characterized by platelet and von Willebrand factor (vWF) deposition in arterioles and capillaries throughout the body, which results in organ ischemia. The diagnostic pentad characterizing TTP consists of thrombocytopenia, microangiopathic hemolytic anemia (MAHA), fever, neurologic manifestations, and renal insufficiency. In terms of type, TTP can be either idiopathic or secondary. The causes of secondary TTP include pregnancy, infections, pancreatitis, collagen vascular disease, cancer, bone marrow transplantation, and drugs (including cephalosporins). Postoperative TTP has been reported after vascular surgery, renal and liver transplantations, and orthopedic, urologic, and abdominal surgical procedures. Therapeutic plasma exchange (TPE) therapy has reduced the mortality rates, but sometimes patients may have to receive immunosuppressive drugs including vincristine (VCR). This report describes a 42-year-old woman with TTP after prophylactic usage of cefuroxime axetil in relation to a liposuction procedure who was treated successfully with plasma exchange and VCR. The patient fully recovered after 17 TPEs and three doses of VCR. At this writing, her TTP still is in remission after 6 months of follow-up evaluation.|/CASE REPORTS/ A 39-year-old woman was diagnosed with anaphylactic shock a few minutes after taking a 500 mg tablet cefuroxime of axetil and was admitted to the emergency department with dizziness, facial angioedema, generalized skin rash, and inferior cardiac ischemia. Skin testing confirmed the involvement of cefuroxime as the cause of the anaphylactic reaction, and the reaction was defined as probable according to the Naranjo probability scale. We then performed skin testing to study cross-reactivity between different beta-lactam antibiotics. In addition to this initial assessment, a structure-activity relationship (SAR) analysis was done. It showed that the patient was sensitized to beta-lactam antibiotics presenting a methoxyimino group, but not to similar compounds lacking this chemical group (eg, amoxicillin or penicillin G or V). Challenge with amoxicillin under intensive medical monitoring was tolerated up to a cumulated dose of 1 g, administered intravenously over 2 hours. This study demonstrates that SAR analysis could be useful to predict potential adverse reactions to related antibiotics and to select alternative strategies when antibiotic administration is essential. CONCLUSIONS: An SAR-based approach could help physicians and pharmacists provide allergic patients with relevant advice and propose viable alternatives regarding drug therapy.|/CASE REPORTS/ ... A case of toxic epidermal necrolysis (TEN) that developed eighteen days of the initiation of cefuroxime axetil therapy for urinary tract infection in a 73-year-old woman with chronic renal failure and no previous history of allergic diathesis /is presented/. The condition was associated with severe granulocytopenia and followed by gastrointestinal hemorrhage, severe sepsis and multiple organ failure syndrome development. Despite intensive medical treatment the patient died. The present report underlines the potential of cefuroxime to simultaneously induce life threatening adverse effects such as TEN and severe granulocytopenia. Further on, because the patient was also taking furosemide for chronic renal failure, the possible unfavorable interactions between the two drugs could be hypothesized. Therefore, awareness of the possible drug interaction is necessary, especially when given in conditions of their altered pharmacokinetics as in case of chronic renal failure.|/CASE REPORTS/ Linear immunoglobulin A (IgA) bullous dermatosis (LABD) is a rare autoimmune blistering disorder. The disease may be either idiopathic or druginduced. Over the past 30 years, approximately one hundred LABD cases have been described as induced by a wide range of drugs, chiefly antibiotics. ... The case of 37-year-old woman who developed pruritic bullous lesions spread all over the body three weeks after her last dose of cefuroxime axetil /is reported/. Antibiotic therapy was started due to rhino-sinusitis. In most reported cases of drug-induced LABD, skin lesions occur within the time of drug administration. However, the onset of disease may be even after discontinuation of treatment. It seems that in such cases, other clinical conditions (like infection) act, as cofactors of immunologic response.|/CASE REPORTS/ A sixty-one year old female with a past history of asthma was admitted to the emergency department because of vertigo, nausea, vomiting, chest pain and generalized erythema after taking an oral dose of cefuroxime axetil. Electrocardiography showed ST segment elevation in inferior leads. After coronary angiography, type 2 variant of Kounis Syndrome is diagnosed. ... The present report ... shows that atopic people expressing an amplified mast cell degranulation may have more serious hemodynamic decompensation during hypersensitivity reactions.

acetoxyethylcefuroxime

Table: cefuroxime Axetil Preparations [Table#8125]|Table: cefuroxime Sodium Preparations [Table#8126]|Parenteral: Injection (frozen), for IV infusion: 30 mg (of cefuroxime) per mL (1.5 g), Zinacef Iso-osmotic in Sterile Water Injection (Glaxy, Baxter; GlaxoSmithKline).|Parenteral: Injection (frozen), for IV infusion: 15 mg (of cefuroxime) per mL (750 mg) in 2.8% Dextrose, Zinacef in Iso-osmotic Dextrose Injection (Galaxy, Baxter; GlaxoSmithKline).

A simple and precise liquid chromatographic method for the determination of cefuroxime axetil in pharmaceutical tablets, human serum and urine has been developed and validated. Cefuroxime axetil and indapamide (internal standard) were separated by a reversed phase column (Supelco Hypersil 5 microm, 150 mm x 4.6 mm i.d., C18) using a mobile phase consisting of KH2PO4 (0.1 M) and acetonitrile (70:30 v/v) (at pH 4.0). The mobile phase was pumped at 1.0 mL min(-1) flow rate and cefuroxime axetil was detected by ultraviolet detection at 281 nm within an average analysis time of 11 min. Flow injection analysis was performed for pharmaceutical tablet analysis using a carrier stream of methanol:water (10:90v/v) with a flow rate of 1.0 mL min(-1). The LOD and LOQ concentrations of the HPLC method were 1.35 x 10(-7) and 4.08 x 10(-7)M for the HPLC analysis and 1.31 x 10(-7) and 4.00 x 10(-7)M for FIA. The results of the analysis of the tablet formulation obtained by using these methods were statistically comparable with each other and with an additional spectrophotometric method. There was no significant difference between all these methods.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients