Suprax Information
Suprax (Cefixime)
Suprax (Cefixime) Description
Suprax (Cefixime) is a semisynthetic, cephalosporin antibiotic for oral administration. Chemically, it is ()-7-[2-(2-Amino-4-thiazolyl)glyoxylamido]-8-oxo-3-vinyl-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 7-()-[-(carboxymethyl) oxime] trihydrate.
Molecular weight = 507.50 as the trihydrate. Chemical Formula is CHNOS.3HO
The structural formula for cefixime is:
Suprax (Cefixime) is available for oral administration as 400 mg film coated tablets and as powder for oral suspension which when reconstituted provides either 100 mg/5 mL or 200 mg/5 mL of cefixime as trihydrate.
Inactive ingredients contained in the 400 mg tablets are: dibasic calcium phosphate, hypromellose, titanium dioxide, lactose monohydrate, polyethylene glycol, triacetin, magnesium stearate, microcrystalline cellulose and pregelatinized starch.
The powder for oral suspension contains the following inactive ingredients: strawberry flavor, sodium benzoate, sucrose, colloidal silicon dioxide and xanthan gum.
Suprax (Cefixime) Clinical Pharmacology
Suprax (Cefixime) , given orally, is about 40%-50% absorbed whether administered with or without food; however, time to maximal absorption is increased approximately 0.8 hours when administered with food. A single 200 mg tablet of cefixime produces an average peak serum concentration of approximately 2 mcg/mL (range 1 to 4 mcg/mL); a single 400 mg tablet produces an average peak concentration of approximately 3.7 mcg /mL (range 1.3 to 7.7 mcg /mL). The oral suspension produces average peak concentrations approximately 25%-50% higher than the tablets, when tested in normal volunteers. Two hundred and 400 mg doses of oral suspension produce average peak concentrations of 3 mcg/mL (range 1 to 4.5 mcg/mL) and 4.6 mcg/mL (range 1.9 to 7.7 mcg/mL), respectively, when tested in normal volunteers. The area under the time versus concentration curve is greater by approximately 10%-25% with the oral suspension than with the tablet after doses of 100 to 400 mg, when tested in normal volunteers. This increased absorption should be taken into consideration if the oral suspension is to be substituted for the tablet. Because of the lack of bioequivalence, tablets should not be substituted for oral suspension in the treatment of otitis media. (See Cross-over studies of tablet versus suspension have not been performed in children.
Peak serum concentrations occur between 2 and 6 hours following oral administration of a single 200 mg tablet, a single 400 mg tablet or 400 mg of cefixime suspension. Peak serum concentrations occur between 2 and 5 hours following a single administration of 200 mg of suspension.
Approximately 50% of the absorbed dose is excreted unchanged in the urine in 24 hours. In animal studies, it was noted that cefixime is also excreted in the bile in excess of 10% of the administered dose. Serum protein binding is concentration independent with a bound fraction of approximately 65%. In a multiple dose study conducted with a research formulation which is less bioavailable than the tablet or suspension, there was little accumulation of drug in serum or urine after dosing for 14 days. The serum half-life of cefixime in healthy subjects is independent of dosage form and averages 3-4 hours but may range up to 9 hours in some normal volunteers. Average AUCs at steady state in elderly patients are approximately 40% higher than average AUCs in other healthy adults.
In subjects with moderate impairment of renal function (20 to 40 mL/min creatinine clearance), the average serum half-life of cefixime is prolonged to 6.4 hours. In severe renal impairment (5 to 20 mL/min creatinine clearance), the half-life increased to an average of 11.5 hours. The drug is not cleared significantly from the blood by hemodialysis or peritoneal dialysis. However, a study indicated that with doses of 400 mg, patients undergoing hemodialysis have similar blood profiles as subjects with creatinine clearances of 21-60 mL/min. There is no evidence of metabolism of cefixime .
Adequate data on CSF levels of cefixime are not available.
Suprax (Cefixime) Indications And Usage
To reduce the development of drug resistant bacteria and maintain the effectiveness of Suprax (Cefixime) and other antibacterial drugs, Suprax (Cefixime) should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antimicrobial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.
Suprax (Cefixime) is indicated in the treatment of the following infections when caused by susceptible strains of the designated microorganisms:
Appropriate cultures and susceptibility studies should be performed to determine the causative organism and its susceptibility to cefixime; however, therapy may be started while awaiting the results of these studies. Therapy should be adjusted, if necessary, once these results are known.
* Efficacy for this organism in this organ system was studied in fewer than 10 infections.
Suprax (Cefixime) Clinical Studies
In clinical trials of otitis media in nearly 400 children between the ages of 6 months to 10 years, was isolated from 47% of the patients, from 34%, from 15% and from 4%.
The overall response rate of to cefixime was approximately 10% lower and that of or approximately 7% higher (12% when beta-lactamase positive strains of are included) than the response rates of these organisms to the active control drugs.
In these studies, patients were randomized and treated with either cefixime at dose regimens of 4 mg/kg BID or 8 mg/kg QD, or with a standard antibiotic regimen. Sixty-nine to 70% of the patients in each group had resolution of signs and symptoms of otitis media when evaluated 2 to 4 weeks post-treatment, but persistent effusion was found in 15% of the patients. When evaluated at the completion of therapy, 17% of patients receiving cefixime and 14% of patients receiving effective comparative drugs (18% including those patients who had resistant to the control drug and who received the control antibiotic) were considered to be treatment failures. By the 2 to 4 week follow-up, a total of 30%-31% of patients had evidence of either treatment failure or recurrent disease.
Suprax (Cefixime) Contraindications
Suprax (Cefixime) is contraindicated in patients with known allergy to the cephalosporin group of antibiotics.
Suprax (Cefixime) Warnings
Anaphylactic/anaphylactoid reactions (including shock and fatalities) have been reported with the use of cefixime.
Antibiotics, including Suprax (Cefixime) , should be administered cautiously to any patient who has demonstrated some form of allergy, particularly to drugs.
Treatment with broad spectrum antibiotics, including Suprax (Cefixime) , alters the normal flora of the colon and may permit overgrowth of clostridia. Studies indicate that a toxin produced by is a primary cause of severe antibiotic-associated diarrhea including pseudomembranous colitis.
Pseudomembranous colitis has been reported with the use of Suprax (Cefixime) and other broad-spectrum antibiotics (including macrolides, semisynthetic penicillins, and cephalosporins); therefore, it is important to consider this diagnosis in patients who develop diarrhea in association with the use of antibiotics. Symptoms of pseudomembranous colitis may occur during or after antibiotic treatment and may range in severity from mild to life-threatening. Mild cases of pseudomembranous colitis usually respond to drug discontinuation alone. In moderate to severe cases, management should include fluids, electrolytes, and protein supplementation. If the colitis does not improve after the drug has been discontinued, or if the symptoms are severe, oral vancomycin is the drug of choice for antibiotic-associated pseudomembranous colitis produced by . Other causes of colitis should be excluded.
Suprax (Cefixime) Precautions
Prescribing Suprax (Cefixime) in the absence of a proven or strongly suspected bacterial infection of a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
The possibility of the emergence of resistant organisms which might result in overgrowth should be kept in mind, particularly during prolonged treatment. In such use, careful observation of the patient is essential. If superinfection occurs during therapy, appropriate measures should be taken.
The dose of Suprax (Cefixime) should be adjusted in patients with renal impairment as well as those undergoing continuous ambulatory peritoneal dialysis (CAPD) and hemodialysis (HD). Patients on dialysis should be monitored carefully. (See
Suprax (Cefixime) should be prescribed with caution in individuals with a history of gastrointestinal disease, particularly colitis.
Cephalosporins may be associated with a fall in prothrombin activity. Those at risk include patients with renal or hepatic impairment, or poor nutritional state, as well as patients receiving a protracted course of antimicrobial therapy, and patients previously stabilized on anticoagulant therapy. Prothrombin time should be monitored in patients at risk and exogenous vitamin K administered as indicated.
Carbamazepine
Warfarin and Anticoagulants
A false-positive reaction for ketones in the urine may occur with tests using nitroprusside but not with those using nitroferricyanide.
The administration of cefixime may result in a false-positive reaction for glucose in the urine using Clinitest, Benedict’s solution, or Fehling’s solution. It is recommended that glucose tests based on enzymatic glucose oxidase reactions (such as Clinistix or TesTape) be used. A false-positive direct Coombs test has been reported during treatment with other cephalosporin antibiotics; therefore, it should be recognized that a positive Coombs test may be due to the drug.
Safety and effectiveness of cefixime in children aged less than six months old have not been established.
The incidence of gastrointestinal adverse reactions, including diarrhea and loose stools, in the pediatric patients receiving the suspension, was comparable to the incidence seen in adult patients receiving tablets.
Suprax (Cefixime) Adverse Reactions
Most of adverse reactions observed in clinical trials were of a mild and transient nature. Five percent (5%) of patients in the U.S. trials discontinued therapy because of drug-related adverse reactions. The most commonly seen adverse reactions in U.S. trials of the tablet formulation were gastrointestinal events, which were reported in 30% of adult patients on either the BID or the QD regimen. Clinically mild gastrointestinal side effects occurred in 20% of all patients, moderate events occurred in 9% of all patients and severe adverse reactions occurred in 2% of all patients. Individual event rates included diarrhea 16%, loose or frequent stools 6%, abdominal pain 3%, nausea 7%, dyspepsia 3%, and flatulence 4%. The incidence of gastrointestinal adverse reactions, including diarrhea and loose stools, in pediatric patients receiving the suspension was comparable to the incidence seen in adult patients receiving tablets.
These symptoms usually responded to symptomatic therapy or ceased when cefixime was discontinued.
Several patients developed severe diarrhea and/or documented pseudomembranous colitis, and a few required hospitalization.
The following adverse reactions have been reported following the use of cefixime. Incidence rates were less than 1 in 50 (less than 2%), except as noted above for gastrointestinal events.
In addition to the adverse reactions listed above which have been observed in patients treated with cefixime, the following adverse reactions and altered laboratory tests have been reported for cephalosporin-class antibiotics:
Several cephalosporins have been implicated in triggering seizures, particularly in patients with renal impairment when the dosage was not reduced. (See and If seizures associated with drug therapy occur, the drug should be discontinued. Anticonvulsant therapy can be given if clinically indicated.
Suprax (Cefixime) Overdosage
Gastric lavage may be indicated; otherwise, no specific antidote exists. Cefixime is not removed in significant quantities from the circulation by hemodialysis or peritoneal dialysis. Adverse reactions in small numbers of healthy adult volunteers receiving single doses up to 2 g of cefixime did not differ from the profile seen in patients treated at the recommended doses.
Suprax (Cefixime) Dosage And Administration
Children weighing more than 50 kg or older than 12 years should be treated with the recommended adult dose.
Otitis media should be treated with the suspension. Clinical studies of otitis media were conducted with the suspension, and the suspension results in higher peak blood levels than the tablet when administered at the same dose. Therefore, the tablet should not be substituted for the suspension in the treatment of otitis media. (See
Efficacy and safety in infants aged less than six months have not been established.
In the treatment of infections due to , a therapeutic dosage of Suprax (Cefixime) should be administered for at least 10 days.
Suprax (Cefixime) may be administered in the presence of impaired renal function. Normal dose and schedule may be employed in patients with creatinine clearances of 60 mL/min or greater. Patients whose clearance is between 21 and 60 mL/min or patients who are on renal hemodialysis may be given 75% of the standard dosage at the standard dosing interval (i.e., 300 mg daily). Patients whose clearance is
After reconstitution the suspension may be kept for 14 days either at room temperature, or under refrigeration, without significant loss of potency. Keep tightly closed. Shake well before using. Discard unused portion after 14 days.
Suprax (Cefixime) How Supplied
Suprax (Cefixime) , Cefixime Tablets USP, 400 mg are white to off-white film coated capsule shaped tablets with beveled edges and a divided score line on each side, debossed with "Suprax (Cefixime) " across one side and "LUPIN" across other side containing 400 mg of cefixime as the trihydrate and are supplied as follows:
NDC 27437-201-01-Bottle of 100 tablets
NDC 27437-201-08-Bottle of 50 tablets
NDC 27437-201-10-Bottle of 10 tablets with CRC
Suprax (Cefixime) , Cefixime for Oral Suspension USP, 100 mg/5 mL is an off-white to pale yellow colored powder. After reconstituted as directed, each 5 mL of reconstituted suspension contains 100 mg of cefixime as the trihydrate and is supplied as follows:
NDC 68180-202-03 - 50 mL Bottle
NDC 68180-202-02 - 75 mL Bottle
NDC 68180-202-01 - 100 mL Bottle
Suprax (Cefixime) , Cefixime for Oral Suspension USP, 200 mg/5mL is an off-white to pale yellow colored powder. After reconstituted as directed, each 5 mL of reconstituted suspension contains 200 mg of cefixime as the trihydrate and is supplied as follows:
NDC 27437-206-05 - 25 mL Bottle
NDC 27437-206-06 - 37.5 mL Bottle
NDC 27437-206-03 - 50 mL Bottle
NDC 27437-206-02 - 75 mL Bottle
NDC 27437-206-01 - 100 mL Bottle
Suprax (Cefixime) References
**Clinitest and Clinistix are registered trademarks of Ames Division, Miles Laboratories, Inc. Tes-Tape is a registered trademark of Eli Lilly and Company.
Suprax (Cefixime)
Suprax (Cefixime) Package Label.principal Display Panel
