Description
FORMULATION
Each film – coated tablet contains:
Cefixime (as trihydrate)
Equivalent to anhydrous cefixime ………………………… 200 mg
PHARMACOLOGICAL CLASSIFICATION: ANTIMICROBIAL AGENT – BROAD AND MEDIUM SPECTRUM ANTIBIOTIC
PHARMACOLOGICAL ACTION
Mechanism of Action
Cefixime is a semi-synthetic third-generation cephalosporin beta-lactam antibiotic for oral administration. It is highly stable in the presence of beta-lactamase enzymes. Cefixime acts by binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, resulting in the inhibition of the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins. As a result, many organisms resistant to penicillins and some cephalosporins due to the presence of beta-lactamases may be susceptible to cefixime.
Cefixime is orally active antibiotic which has in-vitro bactericidal activity against a wide variety of Gram-positive and Gram-negative organisms including Streptococcus pneumoniae, Streptococcus pyogenes, Escherichia coli, Proteus mirabilis, Klebsiella species. Haemophilus influenza (beta-lactamase positive and negative), Moraxella (Branhamella) catarrhalis (beta-lactamase positive and negative).
Cefixime is stable in the presence of beta-lactamase enzymes. Most strains of enterococci (Streptococcus faecelis, group D Streptococci) and staphylococci (including coagulase positive and negative strains and methicillin resistant strains) are resistant to Cefixime. In addition, most strains of Enterobacter and Pseudomonas, Bacteroides fragilis, Listeria monocytogenes and Clostridia are resistant to Cefixime.
PHARMACOKINETICS
Only 40 to 50% of an oral dose is absorbed from the gastrointestinal tract, whether taken before or after meals. The rate of absorption may be decreased in the presence of food. Cefixime is better absorbed from oral suspension than from tablets. Absorption is fairly slow; peak plasma concentrations of 2 to 3 micrograms per mL and 3.7 to 4.6 micrograms per mL have been reported between 2 and 6 hours after single doses of 200 and 400 mg, respectively. The plasma half-life is usually about 3 to 4 hours and may be prolonged when there is renal impairment. About 65% of cefixime is bound to plasma proteins.
Information of the distribution in body tissues and fluids is limited. It crosses the placenta. Relatively high concentrations may be achieved in the bile and urine. About 20% of an oral dose (or 50% of an absorbed dose) is excreted unchanged in the urine within 24 hours. Up to 60% may be eliminated by nonrenal mechanisms; there is no evidence of metabolism but some are probably excreted in the feces from bile. It is not substantially removed via hemodialysis.
INDICATIONS
Cefixime is indicated for the treatment of the following infections when caused by susceptible microorganisms.
- Upper respiratory infections: e.g. bacterial pharyngitis, tonsillitis, otitis media, sinusitis.
- Lower respiratory tract infections: e.g. bronchitis.
- Urinary Tract Infections: e.g. acute cystitis
- Uncomplicated gonorrhea
DOSAGE AND DIRECTIONS FOR USE
Adults
The recommended dose of Cefixime is 400 mg daily. This may be given as 400 mg once daily or as 200 mg every 12 hours. For the treatment of uncomplicated cervical/urethral gonococcal infections, a single oral dose of 400 mg is recommended.
Children
The recommended dose is 8 mg/kg/day. This may be administered as a single dose or may be given in two divided doses as 4 mg/kg every 12 hours. In typhoid, the dose is 20 mg/kg/day in two divided doses or as a single dose in the treatment of infections due to S. pyogenes. A therapeutic dosage of Cefixime should be administered for at least 10 days.
CONTRAINDICATIONS
Allergy to cephalosporins. Cefixime is contraindicated with renal impairment with a creatinine clearance below 60 mL/min.
WARNINGS
Cefixime should be given with caution to patients who have shown hypersensitivity to other medicines. Cephalosporins should be given with caution to penicillin-sensitive patients as there is some evidence of partial cross-allergenicity between the penicillins and the cephalosporins. Patients have had severe reactions (including anaphylaxis) to both classes of drugs. If an allergic effect occurs with Cefixime, the drug should be discontinued and the patient should be treated with appropriate agents if necessary.
Cefixime should be administered with caution in patients with markedly impaired renal function. Prolonged use of Cefixime may result in the overgrowth of non-susceptible organisms. Cefixime has been shown to alter the normal flora of the colon and may permit overgrowth of Clostridia. Studies indicate a toxin(s) produced by Clostridium difficile is the primary cause of antibiotic associated pseudomembranous colitis. The product should be discontinued if diarrhea occurs.
SIDE EFFECTS AND SPECIAL PRECAUTIONS
Pregnancy and Lactation: Safe use in human pregnancy has not been established and it is not known whether cefixime is excreted in human breast milk.
Interactions: No significant interactions have been reported to date. A false positive reaction for glucose in the urine may occur with Benedict’s of Fehling’s solution or with copper sulphate test tablets, but not with tests based on enzymatic glucose oxidase reactions. A false positive direct Coombs test has been reported during treatment with cephalosporin antibiotics, therefore, it should be recognized that a positive Coombs test may be due to the medicine.
Gastrointestinal Disturbances: The most frequent side effects seen with cefixime are diarrhea and stool changes. Moderate to severe diarrhea has been reported. Other gastrointestinal side effects seen less frequently are nausea, abdominal pain, dyspepsia, vomiting, and flatulence. Pseudomembranous colitis has been reported.
Central Nervous System: Headache and dizziness.
Hypersensitivity Reactions: Allergy in the form of rash, pruritus, urticaria, drug fever and arthralgia have been observed. These reactions usually subsides upon the discontinuation of therapy.
Hematological and Clinical Chemistry: thrombocytopenia, leukopenia, and eosinophilia have been reported. These reactions were infrequent and reversible. Changes in liver and renal function tests have been observed.
Miscellaneous: Other possible reactions include genital pruritus and vaginitis.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
No specific antidote exists. Cefixime is not removed from the circulation in significant quantities by dialysis. Treatment shall be symptomatic and supportive.
DRUG INTERACTIONS
| Carbamazepine | Elevated carbamazepine levels have been reported when administered concomitantly with cefixime. Drug monitoring when these drugs are given together is advised. |
| Warfarin /other anticoagulants | Increased prothrombin time, with or without clinical bleeding, has been reported when cefixime is given concomitantly |
| Probenecid | Concomitant administration of probenecid reportedly increases peak serum concentration and AUC of cefixime and decreases renal clearance and Vd of the drug. |
| Salicylates | Concomitant administration of 650 mg oral dose of aspirin and a 400 mg oral dose of cefixime in healthy adult men may result in a 20-25% decrease in peak serum concentration of cefixime and AUC of the drug but did not affect protein binding, serum t 1/2 or renal clearance. This effect may not be clinically important since serum concentrations of cefixime remained higher than the MIC values reported for most susceptible organisms. However, some clinicians state that this effect may be clinically important in certain infections. |
STORAGE
Store at temperatures not exceeding 30°C.
AVAILABILITY
Alu/Alu Blister Pack of 10’s (Box of 30’s).
Manufactured by
AKUMS DRUGS & Pharmaceuticals Ltd.
19-21, Sector-6A, I.I.E., SIDCUL, Ranipur,
Haridwar-249403, India
Distributed by
The Cathay Drug Co., Inc.
2/F Vernida I Condominium., 120 Amorsolo St.
Legaspi Village, Makati City
Date of revision: July 4, 2019
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