Description Zaxime® is an oral broad spectrum ß-lactam antibiotic of third generation cephalosporins.
Clinical pharmacology Zaxime ® kills bacteria by interfering in the synthesis of the bacterial cell wall. Zaxime ® binds with high affinity to penicillin binding proteins (PBP) in bacterial cytoplasmic membrane and by acylation of membrane-bound transpeptidase enzymes, prevents cross-linkage of peptidoglycan chains, which is necessary for bacterial cell wall strength and rigidity. Also cell division and growth are inhibited and elongation of susceptible bacteria and lysis frequently occur. Rapidly dividing bacteria are those most susceptible to the action of Zaxime ®. Antibacterial activity Zaxime® has a high degree of stability in the presence of beta-lactamases (penicillinases and cephalosporinases) and, therefore, has excellent activity against a wide spectrum of gram-negative bacteria, including penicillinase-producing strains of N.gonorrhoeae and most enterobacteriaceae (Citrobacter, E.coli Enterobacter, Klebsiella, Morganella, Proteus, Providencia, and Serratia species). Zaxime ® has the most activity of oral cephalosporins against Streptococcus pyogenes, S.pneumonia, and all gram-negative bacilli, including beta-lactamase producing strains of H.influenza, M.catarrhalis and N.gonorrhoeae. Zaxime ® is not as active against gram-positive cocci as are the first and second generation cephalosporins. It has a little activity against Staphylococci and has no activity against pseudomonas species. Pharmacokinetics Oral absorption ~60% Presystemic metabolism -- Plasma half – life 2.5-3.8 h Mean Range 3h Volume of distribution 0.1 l.kg -1 Plasma protein binding 70%
Indication 1-Bronchitis. 2-Bacterial exacerbation of bronchitis. 3-Otitis media. 4-Uncomplicated gonorrhea. 5-Bacterial pharyngitis and tonsillitis. 6-Bacterial urinary tract infections.
Contraindication Zaxime® is contraindicated in patients who have shown hypersensitivity to Cefixime or cephalasporin group of antibiotics.
Precaution • Before Zaxime® administration, previous hypersensitivity reactions to cephalosporins or penicillins must be determined because of cross hypersensitivity among ß-lactams. • Risk-benefit should be considered when history of bleeding disorders, gastrointestinal disease specially ulcerative colitis, regional enteritis or antibiotic associated colitis (Zaxime® may cause pseudomembranous colitis) and hepatic function impairment exist. • For patients with renal function impairment (creatinine clearance <20mL/min) one half the usual adult dose should be used at the same dosing intervals. • Long-term therapy with Zaxime® may allow for the overgrowth of Candida albicans, resulting in oral candidiasis. • Therapy should be continued for at least 10 days in group a beta-hemolytic streptococcal infections to help prevent the occurrence of acute rheumatic fever or glomerulonephritis. Pregnancy Pregnancy category B. Zaxime ® cross the placenta. There are no well-controlled studies in pregnant women. Therefore Zaxime ® should be used during pregnancy only if clearly needed. Breast feeding It is not known whether Zaxime ® is distributed into breast milk. Consideration should be given to discontinuing nursing temporarily during treatment with this drug.
Dosage Usual adult dose • Bronchitis, bacterial exacerbation of bronchitis, pharyngitis, tonsillitis or uncomplicated urinary tract infections: 200 mg every 12 hours or 400 mg once a day. • Uncomplicated cervical or urethral gonorrhea: 400 mg as a single dose. Usual pediatric dose • Bronchitis, bacterial exacerbation of bronchitis, Otitis media, pharyngitis, tonsillitis or uncomplicated urinary tract infections: Children 50 kg of body weight and over: the same as adult dose. Infants and children 6 months to 12 years of age and up to 50 kg of body weight: 4 mg per kg of body weight every 12 hours or 8 mg per kg of body weight once a day. Infants up to 6 months of age: dosage has not been established. Usual geriatric dose Dosing is the same as adult dose. Note: As the oral suspension form of Zaxime ® results in higher peak blood concentrations than the tablet when administrated at the same dose, therefore the tablet should not be substituted for the oral suspension in the treatment of Otitis media.
Administration Reconstitution direction for oral suspension • Add approximately half the total amount of water for reconstitution and shake well, then add more water towards indication line and shake well to get a soft suspension.
Patient consultation • Take Zaxime ® on a full or empty stomach or take with food if gastrointestinal irritation occurs. • Take the medicine in regular intervals and continue medicine for full time of treatment. • If you missed a dose, take as soon as possible, don't take if almost time for next dose and don't double doses. • If there wasn't improvement of symptoms within a few days, check with your physician. • Shake well before using. Warning • If Zaxime® is to be given to penicillin-sensitive patients, caution should be exercised because cross-hypersensitivity among ß-lactam antibiotics has been clearly documented and may occur in up to 7% of patients with a history of penicillin allergy. Interaction • The potential for increased nephrotoxicity exists when Zaxime ® is used with other nephrotoxic medications such as loop diuretics, especially in patients with preexisting renal function impairment. Renal function should be monitored carefully in patients receiving Zaxime® and aminoglycosides concurrently. Laboratory value alteration • Zaxime® may produce false-positive reaction for ketones in urine with tests using nitropruside, also may produce false positive or falsy elevated test results for glucose in the urine with copper reduction tests [Benedict's, Fehling’s]. • A positive Coombs reaction appears frequently in patients who receive large doses of Zaxime ®. • Zaxime ® may prolong prothrombin time. • Administration of Zaxime ® may change the following physiology/laboratory test values: Alanine aminotransferase (ALT [SGPT]), Alkaline phosphatase, Aspartate aminotransferase (AST [SGOT]), Lactate dehydrogenase (LDH), Serum bilirubin, Blood urea nitrogen (BUN), Serum Creatinine, Complete blood count (CBC), Platelet count.
Adverse reactions • Most of adverse reactions observed in clinical trials were of a mild and transient nature. The most commonly seen adverse reactions were gastrointestinal events. • The following adverse reactions have been reported but their incidence rates were less than 2%, except as noted above for gastrointestinal events. Those indicating need for medical attention. • Incidence less frequent or rare Hypoprothrombinemia (unusual bleeding or bruising), pseudomembranous colitis (abdominal or stomach cramps and pain, abdominal tenderness. Severe watery and bloody diarrhea, fever).
• Incidence rare Allergic reactions, specifically anaphylaxis, Erythema multiforme or Stevens Johnson syndrome (blistering, peeling or loosening of skin and mucous membranes, which may involves the eyes or the other organ systems) hearing loss, hemolytic anemia, immune, drug – induced (unusual tiredness or weakness, yellowing of the eyes or skin), hypersensitivity reactions, renal dysfunction, serum sickness-like reactions, seizures, thrombophlebitis. Those indicating need for medical attention only if they continue or are bothersome. • Incidence more frequent. Gastrointestinal reactions (abdominal cramps, mild diarrhea, nausea or vomiting) headache, oral candidiasis (sore mouth or tongue), vaginal candidiasis (vaginal itching and discharge).
Overdose In the case of Zaxime® overdosage, gastric lavage may be used to decrease the absorption of Zaxime®.It is not removed in significant quantities from the circulation by hemodialysis or peritoneal dialysis.
Storage and Stability Condition
Capsule & Tablet • Store below 25oC. • Protect from light and moisture.
• Prior to reconstitution, store below 25oC protect from light.
• After reconstitution, suspension is stable for one week in room temperature and two weeks in refrigerator.
• Protect from freezing. Packaging • Zaxime® Tablets Scored film coated tablets containing 200 or 400 mg of cefixime as trihydrate. Boxes of 10 and 20 tablets • Zaxime® Capsules Each capsule containing 200 or 400 mg of cefixime as trihydrate Boxes of 10 and 20 capsules • Zaxime® Oral suspension Dry powder, which after reconstitution contains 100mg/5mL of Cefixime as trihydrate. Bottles of 100mL. Last Updated: March 23, 2009