CEFEPIME-ELSaad 1000
-
Chemical Name:
Cefepime (HCl) -
Therapeutic Category:
Antimicrobial -
Pharmacologic Category:
Antibiotic, Cephalosporin (Fourth Generation) -
Pharmaceutical Form:
Vial -
Composition:
Cefepime (HCl) 1000mg
CEFEPIME- ELSaad
Cefepime hydrochloride
1-COMBOSITION:
CEFEPIME- ELSaad 500 -Vial: Each vial contains: Cefepime hydrochloride equivalent to 500 mg Cefepime.
CEFEPIME- ELSaad 1000-Vial: Each vial contains: Cefepime hydrochloride equivalent to 1000 mg Cefepime.
CEFEPIME- ELSaad 2000-Vial: Each vial contains: Cefepime hydrochloride equivalent to 2000 mg Cefepime.
2-PHARMACOLOGY:
Cefepime hydrochloride is a semi-synthetic, broad-spectrum, fourth generation cephalosporin antibiotic for parenteral administration.
Cefepime hydrochloride is a bactericidal agent that acts by inhibition of cell-wall synthesis.
Cefepime hydrochloride is highly resistant to hydrolysis by most beta-lactamases and exhibits rapid penetration into gram-negative bacterial cells . Cefepime hydrochloride has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections:.
Aerobic Gram-Negative:
Enterobacter spp.
Escherichia coli
Klebsiella pneumoniae
Proteus mirabilis
Pseudomonas aeruginosa
Aerobic Gram-Positive:
Staphylococcus aureus(methicillin-susceptible strains only).
Streptococcus pneumoniae
Streptococcus pyogenes
Cefepime has been shown to have in vitro activity against most strains of the following microorganisms:
Aerobic Gram-Positive:
Staphylococcus epidermidis (methicillin-susceptible strains only).
Staphylococcus saprophyticus
Streptococcus agalactiae
Viridans group streptococci
Aerobic Gram-Negative
Acinetobacter calcoaceticus subsp. / woffi
Citrobacter diversus
Citrobacter freundii
Enterobacter agglomerans
Haemophilus influenzae ( including beta-lactamase producing strains)
Hafnia alvei
Klebsiella oxytoca
Moraxella catarrhalis (including beta-lactamase producing strains)
Morganella morganii
Proteus vulgaris
Providencia rettgeri
Providencia stuartii
Serratia marcescens
3-PHARMACOKINETICS :
Maximum peak plasma concentrations of Cefepime observed in healthy adult male volunteers following single 30-minute infusions (IV) of Cefepime 500 mg, 1000 mg, and 2000 mg. are C max , ىg/mL 39.1 for 500 mg, 81.7 for 1000 mg and 163.9 for 2000 mg.
AUC, hr. ىg/mL are 70.8 for 500 mg, 148.5 for 1000 mg and 284.8 for 2000 mg.
Elimination of Cefepime is principally via renal excretion with an average half-life of 2.0 (±0.3) hours and total body clearance of 120.0 (±8.0) mL/min in healthy volunteers. Cefepime pharmacokinetics are linear over the range 250 mg to 2000 mg. There is no evidence of accumulation in healthy adult male volunteers receiving clinically relevant doses for a period of 9 days.
Following intramuscular (IM) administration, Cefepime is completely absorbed. The
C max plasma concentrations of Cefepime at various times following a single IM injection are :
C max, ىg/mL 13.9 for 500 mg, 29.6 for 1000 mg and 57.5 for 2000 mg.
T max, hr 1.4 for 500 mg 1.6 for 1000 mg and 1.5 for 2000 mg.
AUC, hr. ىg/mL 60.0 for 500 mg, 137.0 for 1000 mg and 262.0 for 2000 mg.
Distribution: The average steady state volume of distribution of Cefepime is 18.0 (±2.0)L. The serum protein binding of Cefepime is approximately 20% and is independent of its concentration in serum.
Cefepime is excreted in human milk. A nursing infant consuming approximately 1000 mL of human milk per day would receive approximately 0.5 mg of Cefepime per day.
Data suggest that Cefepime does cross the inflamed blood-brain barrier.
Metabolism and Excretion: Cefepime is metabolized to N- methylpyrrolidine (NMP) which is rapidly converted to the N-oxide (NMP-N-oxide). Urinary recovery of unchanged Cefepime accounts for approximately 85% of the administered dose.. Because renal excretion is a significant pathway of elimination, patients with renal dysfunction and patients undergoing hemodialysis require dosage adjustment.
4-INDICATIONS
Cefepime- ELSaad is indicated in the treatment of the following infections caused by susceptible strains of the designated microorganisms.
-Pneumonia (moderate to severe), including cases associated with concurrent bacteremia.
-Uncomplicated and Complicated Urinary Tract Infections (including pyelonephritis),
including cases associated with concurrent bacteremia
-Uncomplicated Skin and Skin Structure Infections .
-Complicated Intra-abdominal Infections (used in combination with metronidazole)
- Empiric Therapy for Febrile Neutropenic Patients. Cefepime- ELSaad as monotherapy is indicated for empiric treatment of febrile neutropenic patients. In patients at high risk for severe infection (including patients with a history of recent bone marrow transplantation, with hypotension at presentation, with an underlying hematologic malignancy, or with severe or prolonged neutropenia), antimicrobial monotherapy may not be appropriate.
5-CONTRAINDICATIONS:
(Cefepime hydrochloride) is contraindicated in patients who have shown immediate hypersensitivity reactions to (Cefepime hydrochloride) or the cephalosporin class of antibiotics, penicillins or other beta-lactam antibiotics.
6-PRECAUTIONS:
-Before therapy, careful inquiry should be made to determine whether the patient has had previous hypersensitivity reactions to cefepime, or other cephalosporins.
if an allergic reaction occurs, discontinue the drug and serious acute hypersensitivity reactions may require treatment, as clinically indicated
-As with other antimicrobials, prolonged use of Cefepime hydrochloride may result in overgrowth of nonsusceptible microorganisms. Should superinfection occur during therapy, appropriate measures should be taken.
-Cefepime hydrochloride should be prescribed with caution in individuals with a history of gastrointestinal disease, particularly colitis.
-Mild cases of pseudomembranous colitis usually respond to drug discontinuation alone.
-Many cephalosporins, including cefepime, have been associated with a fall in prothrombin activity.. prothrombin time should be monitored specially in patients with renal or hepatic impairment
-The daily dose of cefepime hydrochloride should be adjusted in patients with renal impairment
7-DRUG INTERACTIONS :
Renal function should be monitored carefully if high doses of aminoglycosides are to be administered with Cefepime hydrochloride because of the increased potential of nephrotoxicity and ototoxicity of aminoglycoside antibiotics. Nephrotoxicity has been reported following concomitant administration of other cephalosporins with potent diuretics such as furosemide.
8-PREGNANCY AND NURSING MOTHERS:
This drug should be used during pregnancy only if clearly needed.
Caution should be exercised when Cefepime- ELSaad is administered to a nursing women.
9-SIDE EFFECTS :
It may rarely cause :
Local reactions, pain and/or inflammation, rash, and very rarely some gastrointestinal disturbances including headache, nausea.
10-DOSAGE AND ADMINISTRATION :
Adults
|
Type of Infection
|
Dose
|
Frequency
|
Duration (Days)
|
|
Moderate to Severe Pneumonia (including cases associated With concurrent bacteremia)
|
1000-2000 mg IV
|
Q 12h
|
10
|
|
Mild to Moderate Uncomplicated or Complicated Urinary Tract Infections
|
500-1000mg IV/IM
|
Q 12h
|
7-10
|
|
Severe Uncomplicated or Complicated Urinary Tract Infections, including pyelonephritis
|
2000 mg IV
|
Q12h
|
10
|
|
Moderate to Severe Uncomplicated Skin and Skin Structure Infections
|
2000 mg IV
|
Q12h
|
10
|
|
Complicated Intra-abdominal Infections (used in combination with metronidazole)
|
2000 mg IV
|
Q12h
|
7-10
|
|
Empiric therapy for febrile neutropenic patients
|
2000 mg IV
|
q8h
|
7
|
Pediatric Patients (older than 2 months) :
The maximum dose for pediatric should not exceed the recommended adult dose. The usual recommended dosage in pediatric patients up to 40 kg in weight for uncomplicated and complicated urinary tract infections (including pyelonephritis), uncomplicated skin and skin structure infections, pneumonia, and as empiric therapy for febrile neutropenic patients is 50 mg/kg/dose, administered q12h (q8h for febrile neutropenic patients), for durations as given above.
Impaired Hepatic Function – No adjustment is necessary for patients with impaired hepatic function.
Impaired Renal Function : In patients with impaired renal function (creatinine clearance Cefepime- ELSaad should be adjusted to compensate for the slower rate of renal elimination. The recommended initial dose should be the same as in patients with normal renal function. The recommended maintenance doses in patients with renal insufficiency are presented in the Table.
|
Creatinine
Clearance
( mL / min )
|
Maintenance doses
|
||||
|
> 60
Normal
|
500 mg q 12 h
|
1000mg q 12 h
|
2000mg q 12 h
|
2000mg q 8h
|
|
|
30 – 60
|
500 mg q 24 h
|
1000mg q 24 h
|
2000mg q 24 h
|
2000mg q 12 h
|
|
|
11- 29
|
500 mg q 24 h
|
500 mg q 24 h
|
1000mg q 24 h
|
2000mg q 24 h
|
|
|
< 11
|
250 mg q 24 h
|
250 mg q 24 h
|
500 mg q 24 h
|
1000mg q 24 h
|
|
|
|
|
|
|
|
|
In patients undergoing hemodialysis, approximately 68% of the total amount of Cefepime- ELSaad present in the body at the start of dialysis will be removed during a 3-hour dialysis period. A repeat dose, equivalent to the initial dose, should be given at the completion of each dialysis session.
ADMINISTRATION :
For Intravenous Infusion : constitute the 1000mg or 2000mg with 50 or 100 mL of a compatible IV fluid. Alternatively, constitute the 500 mg, 1000mg, or 2000mg vial, and add an appropriate quantity of the resulting solution to an IV container with one of compatible IV fluids The resulting solution should be administered over approximately 30 minutes.
Intramuscular Administration : For IM administration, Cefepime- ELSaad should be constituted with one of the following diluents: Sterile Water for Injection, 0.9% Sodium Chloride, 5% Dextrose Injection, 0.5% or 1.0% Lidocaine Hydrochloride.
Preparation of Solutions of Cefepime
|
Single Dose Vials for Intravenous / Intramuscular
Administration
|
Amount of Diluent to be added
(mL )
|
Approximate
Available
Volume
(mL)
|
Approximate
Cefepime
Concentration
(mg / mL)
|
|
500 mg (IV)
|
5.0
|
5.6
|
100
|
|
500 mg (IM)
|
1.3
|
1.8
|
280
|
|
1000mg (IV)
|
10.0
|
11.3
|
100
|
|
1000mg (IM)
|
2.4
|
3.6
|
280
|
|
2000mg (IV)
|
10.0
|
12.5
|
160
|
11-COMPATIBILITY AND STABILITY :
Intravenous : Cefepime- ELSaad is compatible at concentration between 1 and 40 mg/mL with the following IV infusion fluids : 0.9% Sodium Chloride Injection, 5% and 10% Dextrose Injection, M/6 Sodium Lactate Injection, lactated Ringers.
These solutions may be stored up to 24 hours at controlled room temperature 20° – 25° C or 7 days in a refrigerator 2° – 8° C
Solutions of Cefepime- ELSaad, like those of most beta-lactam antibiotics, should not be added to solutions of ampicillin at a concentration greater than 40 mg/ mL, and should not be added to metronidazole, vancomycin, gentamicin, tobramycin, netilmicin sulfate or aminophylline because of potential interaction. However, if concurrent therapy with Cefepime- ELSaad is indicated, each of these antibiotics can be administered separately.
Intramuscular : Cefepime- ELSaad constituted as directed is stable for 24 hours at controlled room temperature 20° – 25° C , or 7 days in a refrigerator 2° – 8° C with the following diluents: Sterile Water for Injection, 0.9% Sodium Chloride Injection, 5% Dextrose Injection, or 0.5% or 1% Lidocaine Hydrochloride.
12-PACKAGING:
-1 Vial.
-100 Vials
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