Exef
(Cefotaxime Sodium)
Description: Broad-spectrum third generation cephalosporin for parenteral administration.In vitro studies indicate that the bacterial action of Cefotaxime results from inhibition of cell wall synthesis.
Cefotaxime is partially metabolized in humans by non-specific esterases which desacetylate the acetoxymethylside chain to form the desacetyl cefotaxime (DACM). Desacetylation is followed by formation of the lactone and subsequent conversion to open b-lactam ring structures (UP1) and (UP2).
The DACM has been shown to contribute to 10 to 15% of the bactericidal activity of the parent compound. UP1 and UP2 lack antibacterial activity.
Indications And Clinical Uses: Cefotaxime may be indicated for the treatment of infections caused by susceptible strains of the designated microorganisms in the diseases listed below:
Lower respiratory tract infections:pneumonia and lung abscess caused by S. pneumoniae, other streptococci (excluding enterococci, e.g., S. faecalis), S. aureus (penicillinase and non-penicillinase producing), E. coli, H. influenzae, (including ampicillin resistant strains) and unspecified Klebsiella species.
Urinary tract infections: caused by E. coli, unspecified Klebsiella species (including K. pneumoniae), P. mirabilis, indole positive Proteus, S. marcescens and S. epidermidis. Also, uncomplicated gonorrhea caused by N. gonorrhoeae including penicillin resistant strains.
Bacteremia/Septicemia: caused by E. coli, unspecified Klebsiella strains and S. marcescens.
Skin infections: caused by S. aureus (penicillinase and non-penicillinase producing), S. epidermidis, Group A streptococci, E. coli, P. mirabilis and indole positive Proteus. Intra-abdominal infections: caused by E. coli, and unspecified Klebsiella species.
Gynecological infections: including pelvic inflammatory disease, endometritis & pelvic cellulitis caused by E. coli, Group A streptococci and S. epidermidis; anaerobic bacteria including unspecified Peptococcus and Peptostreptococcus strains and some strains of B. fragilis. In several cases, although clinical cures were achieved, bacteriological follow-up was not available.
CNS infections: meningitis and ventriculitis caused by H. influenzae, N. meningitidis, S. pneumoniae, K. pneumoniae and E. coli. Cefotaxime is not active against L. monocytogenes.
Prophylactic use: The administration of cefotaxime perioperatively (preoperatively, intraoperatively and postoperatively) may reduce the incidence of certain infections in patients undergoing elective surgical procedures (e.g., abdominal or vaginal hysterectomy, gastrointestinal and genitourinary tract surgery) that may be classified as contaminated or potentially contaminated.
Caesarian Section: In patients undergoing caesarian section who are considered to be at increased risk of infection, intra-operative (after clamping the umbilical cord) and postoperative use of Cefotaxime may also reduce the incidence of certain postoperative infections. For patients undergoing gastrointestinal surgery, preoperative bowel preparation by mechanical cleansing as well as with a nonabsorbable antibiotic (e.g., neomycin) is recommended.
Dosage And Administration: Cefotaxime may be administered i.v. or i.m. after reconstitution.
Adults: To prevent postoperative infection in contaminated or potentially contaminated surgery, recommended doses are as follows: (a) 1 g i.m. or i.v. administered 1/2 to 1 1/2 hours prior to the initial surgical incision to ensure that adequate antibiotic levels are present in the serum and tissues at the start of surgery; (b) 1g i.m. or i.v. administered 1 1/2 to 2 hours following the first dose; for lengthy operative procedures, additional intraoperative doses may be administered, if necessary, at appropriate intervals (1 1/2 to 2 hours) during surgery; (c) 1g i.m. or i.v. administered within 2 hours following completion of surgery.
The total cumulative prophylactic dose should not exceed 6 g in a 12-hour period.Caesarian Section Patients: The first dose of 1 g is administered i.v. as soon as the umbilical cord is clamped. The second and third doses should be given as 1 g i.m. or i.v. at 6 and 12 hours after the first dose.
Neonates, Infants, and Children: The following dosage schedule is recommended. Neonates: 0 to 1week of age; 50 mg/kg i.v. every 12 hours, 1 to 4 weeks of age; 50 mg/kg i.v. every 8 hours.Infants and children (1 month to 12 years): For body weights less than 50 kg, the recommended daily dose is 50 to 100 mg/kg i.m. or i.v. of body weight divided into 4 to 6 equal doses, or up to 180 mg/kg/day for severe infections (including CNS infections). For body weights 50 kg or more, the usual adult dosage should be used.
The maximum daily dosage should not exceed 12 g.Administration of cefotaxime should be continued for a minimum of 48 to 72 hours after the Patient defervesces or after evidence of bacterial eradication has been obtained; a minimum of 10 days of treatment is recommended for infections caused by Group A beta-hemolytic streptococci in order to guard against the risk of rheumatic fever or glomerulonephritis;
Administration:
I.M.: Cefotaxime should be injected well within the body of a relatively large muscle such as the upper outer quadrant of the buttock (i.e., gluteus maximus); aspiration is necessary to avoid inadvertent i njection into a blood vessel.
I.V.: The i.v. route is preferable for patients with bacteremia, bacterial septicemia, or other severe or life-threatening infections, or for patients who may be poor risks because of lowered resistance resulting from such debilitating conditions as malnutrition, trauma, surgery, diabetes, heart failure,or malignancy, particularly if shock is present or impending.
Storage: Store below 25oC in dry form.Protect from light.
Availability:
EXEF 1g vial with a 5ml ampoule of sterile water for injection.
EXEF 500mg vial with a 5ml ampoule of sterile water for injection.
EXEF 250mg vial with a 5ml ampoule of sterile water for injection.
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