Cefazolin Sodium Powder For Injection 0.5g / 1.0g Antibiotic Drugs
Cefazolin Sodium equivalent to Cefazolin 500 mg or 1 g activity.
A 20.1.1 - Broad spectrum antibiotic.
Cefazolin (cefazolin sodium) is a broad-spectrum bactericidal,
semi-synthetic cephalosporin for parenteral administration.
Chemically cefazolin is the sodium salt of
Cefazolin given intravenously or intramuscularly produces notably
high serum levels. Serum binding occurs at a rate of 74%. Cefazolin
is resistant to degradation in the body, is virtually not
inactivated in the liver, and is primarily excreted in the urine
unchanged. Following intramuscular injection of cefazolin 500 mg,
63+17% of the dose was recovered within 6 hours and approximately 80%
to 100% within 24 hours. Peak urine concentrations of approximately
1000 micrograms/mL and 4000 micrograms/mL are achieved after
intramuscular administration of 500 mg and 1 g doses, respectively.
When cefazolin is administered to patients with unobstructed
biliary tracts, high concentrations well over serum levels occur in
the gallbladder tissue and bile. In the presence of obstruction,
however, concentration in the bile is considerably lower than the
serum level. Tissue distribution of cefazolin is greatest in the
kidney, liver and lungs. The concentration of cefazolin in the
joint space when the synovial membrane is inflammed is comparable
to the concentration found in the serum due to the ease with which
the antibiotic crosses the inflammed membrane.
Cefazolin is bactericidal against a wide range of gram-positive and
In vitro sensitivity of gram-positive organisms include:
Penicillinase and Non-penicillinase-producing Staphylococci,
beta-haemolytic Streptococci. Streptococcus pneumoniae and
Clostridia perfringens. Methicillin-resistant staphylococci are
uniformly resistant to cefazolin.
In vitro sensitivity of gram-negative organisms include:
Some strains of Neisseria gonorrhoea, Escherichia coli, Klebsiella
pneumoniae, Proteus mirabilis, Salmonella typhosa, Shigella,
Corynebacterium diptheriae, Bacillus subtilis.
Most strains of Enterobacter cloacae and indole positive Proteus
(P. vulgaris), Enterococcus faecalis Morganella morganii (formerly
Proteus morganii), Providencia rettgeri (formerly Proteus rettgeri)
are resistant. Almost uniformly resistant to cefazolin are
Serratia, Pseudomonas and Acinetobacter calcoaceticus. In vitro
sensitivity does not necessarily imply in vivo efficacy.
Cefazolin is indicated in the treatment of the following infections
when due to susceptible micro-organisms.
Respiratory tract infections:
Tonsillitis, pharyngitis, pneumonia, bronchitis, pulmonary abscess,
empyema, pleurisy, sinusitis, laryngitis and otitis media.
Skin, soft-tissue and postoperative infections:
Lymphangitis, abscesses, cellulitis, decubitus ulcers, mastitis.
(Surgical procedures should be performed where indicated).
Gastrointestinal tract infections:
Genitourinary tract infection:
Pyelonephritis, cystitis and adnexitis.
Bacteremia, septicemia, endocarditis, osteomyelitis, peritonitis,
Appropriate culture and susceptibility studies should be performed
to determine susceptibility of the causative organism to Cefazolin.
If the tests show that the causative organism is resistant of
Cefazolin, other appropriate therapy should be instituted.
Patients hypersensitive to cephalosporins and its derivatives, or
any components of the formulation.
DOSAGE AND DIRECTIONS FOR USE
The following dosages are recommended, for administration of
constituted Cefazolin preferably by intravenous infusion or
alternatively by slow intravenous injection (over 3 to 5 minutes)
or by intramuscular injection.
For the treatment of mild-to-moderately severe bacterial
infections, 1,5 to 2 g per day in equally divided doses, two or
three times daily. For the treatment of severe bacterial infection,
3-4 g per day in equally divided doses two or three times daily.
Higher and/or more frequent doses (up to 6 g daily) may be given in
very severe, life-threatening infections, but in rare instances,
doses of up to 12 grams have been used.
The following dosage chart is a useful guide* to Cefazolin therapy
|AGE AND WEIGHT||TOTAL DAILY DOSE**|
|100%||Adult (65 kg)||1,5 g to 6 g|
|75%||12 years (40 kg)||1,125 g to 4,5 g|
|50%||7 years (23 kg)||750 mg to 3 g|
|25%||1 year (10 kg)||375 mg to 1,5 g|
|20%||4 months (6,5 kg)||300 mg to 1,2 g|
For in-between ages, in-between percentages are used e.g. at 10
years, 66% and at three years 33% of the adult dose.
*Using the Percentage Method based on the following formula:
|Surface area of child||x 100||= Percentage of adult dose|
|Surface area of adult|
**The recommended total daily dose should be administered in two or
three equally divided doses. The maximum range is for very severe
The intravenous route by drip infusion is preferable when high
doses are to be administered.
Safety and effectiveness for use in premature infants and infants
under one month of age has not been established.
Cefazolin may be nephrotoxic if given in excessive doses (more than
6g daily in patients with normal renal function) or if administered
without appropriate dosage reduction in patients with renal
impairment. Although Cefazolin is generally well tolerated in
patients with impaired renal function it is nevertheless desirable
to adjust the dosage as follows to prevent the accumulation of high
Dosage adjustment for adults:
|> 55||Full doses|
|35 TO 54||Full doses, but restricted to at least 8 hour intervals|
|11 TO 34||Half the usual dose every 12 hours|
|< 10||Half the usual dose every 18 to 24 hours|
Dosage adjustment for children:
|70 to 40||60% of normal daily dose in equally divided doses every 12 hours|
|40 to 20||25% of normal daily dose in equally divided doses every 12 hours|
|20 to 5||10% of normal daily dose every 24 hours.|
All reduced dosage recommendations apply after an initial loading
dose appropriate to the severity of the infection. Patients
undergoing peritoneal dialysis: (See PHARMACOLOGICAL ACTION).
Treatment should be continued for a minimum of 48 to 72 hours
beyond the time that the patient becomes asymptomatic or evidence
of bacterial eradication has been obtained.
A MINIMUM OF 10 DAYS TREATMENT IS RECOMMENDED FOR ANY INFECTION
CAUSED BY GROUP-A beta-HAEMOLYTIC STREPTOCOCCI TO HELP PREVENT THE
OCCURRENCE OF ACUTE GLOMERULONEPHRITIS OR ACUTE RHEUMATIC FEVER.
For administration by intravenous infusion: Use sterile water for injection. Add 2 mL to the 500 mg vial and 4
mL to the 1 g vial. Withdraw the entire contents and add to one of
the following intravenous solutions:
0,9% sodium chloride injection
5% or 10% dextrose injection
5% dextrose in lactated Ringers injection
5% dextrose in 0,9% sodium chloride injection (also may be used
with 5% dextrose and 0,45% or 0,2% sodium chloride injection)
Lactated Ringers Injections
5% or 10% invert sugar in sterile water for injection
For administration by direct intravenous injection: After constitution with 2 mL (500 mg) or 4 mL (1 g) of water for
injection, dilute in a minimum of 10 mL of water for injection.
Inject solution slowly over 3-5 minutes either directly into a vein
or through the tubing for a patients receiving the parenteral
fluids mentioned above.
For administration by intramuscular injection: Add 2 mL (500 mg) or 4 mL (1 g) of sterile water for injection,
bacteriostatic water for injection or 0,9% sodium chloride
injection. Withdraw the entire contents to the vial.
Constituted solutions are stable for 24 hours when kept at room
temperature not exceeding 25°C, or for 96 hours when kept in a
SIDE-EFFECTS AND SPECIAL PRECAUTIONS
As with all other cephalosporins, Cefazolin has the potential for
producing allergic reactions, such as rash, pruritus, urticaria,
angioedema eosinophilia, drug fever and anaphylaxis were observed.
Leukopenia, neutropenia, thrombocytopenia, thrombocythemia and
positive direct and indirect Coombs' tests have occurred.
Transient rises in AST (SGOT), ALT (SGPT) and alkaline phosphatase
levels have been observed rarely. Transient hepatitis and
cholestatic jaundice have been reported rarely.
Transient rise in blood urea levels have been observed without
clinical evidence of renal impairment. Interstitial nephritis and
other renal disorders have been reported rarely. Most patients
experiencing these reactions had been seriously ill and were
receiving multiple drug therapies. The role of cefazolin in the
development of nephropathies has not been determined.
Symptoms of pseudomembranous colitis may appear either during or
after antibiotic therapy. Nausea and vomiting have been reported
rarely. Anorexia, diarrhoea and oral candidiasis have been
Cefazolin is well tolerated when administered by intravenous
infusion, and the incidence of phlebitis with Cefazolin is low.
Although pain was infrequently reported after intramuscular
injection, it was seldom severe. Cefazolin rarely produced
tenderness, induration or fever.
Other reactions include genital and anal pruritis, genital
candidiasis and vaginitis.
In patients with a history of cephalosporin or penicillin allergy,
Cefazolin should be used with caution. There is evidence of partial
cross-allergenicity of the penicillins and the cephalosporins and
there are instances of patients who have had fatal anaphylactoid
reactions after parenteral use. These require immediate emergency
Any patient who has demonstrated some form of allergy, particularly
to medicine, should receive antibiotics cautiously and then only
when absolutely necessary.
Pseudomembranous colitis has been reported with cephalosporins and
may range from mild to life-threatening. Therefore, it is important
to consider this diagnosis in patients who present with diarrhoea
after the administration of Cefazolin. Should colitis be diagnosed,
therapeutic measures should be initiated.
Intrathecal administration of Cefazolin is not recommended. There
have been reports of severe central nervous system toxicity
including seizures when cefazolin was administered intrathecally.
A reduced dose may be appropriate in patients with impaired renal
function (See DOSAGE AND DIRECTIONS FOR USE).
Prolonged use of cefazolin may cause overgrowth of nonsusceptible
organisms in which case appropriate measures should be taken.
Cefazolin should be used with caution in patients with a history of
gastrointestinal disease, especially colitis.
Probenecid may cause prolonged cephalosporin blood levels.
False-positive reactions for glucose in the urine may occur if
copper reduction test methods are used. Glucose tests should
therefore be based on enzymatic glucose oxidase reactions.
Concomitant administration of cephalosporins and aminoglycoside
antibiotics has been associated with increased nephrotoxicity.
Positive direct and indirect antiglobulin (Coombs') test have
occurred; those may also occur in neonates whose mothers received
cephalosporins before delivery. Safety of cefazolin during
pregnancy has not been established. Cefazolin has been found to
readily cross the placental barrier into the cord blood and
Safety in lactation has no been established.
Cefazolin is present in very low concentrations in the milk of
Safety and effectiveness for use in premature infants and infants
under one month of age have not been established. See DOSAGE AND
DIRECTIONS FOR USE for recommended dosage in children over one
As experience in premature infants and neonates is limited the use
of Cefazolin in these patients should only be undertaken with
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
Inappropriately large doses of parenteral cephalosporins may cause
dizziness, paresthesias and headache. Seizures may occur following
overdosage with some cephalosporins, particularly in patients with
renal impairment in whom accumulation is likely to occur.
Dosage reduction is necessary when renal function is impaired. (See
DOSAGE AND DIRECTIONS FOR USE). If seizures occur, the drug should
be promptly discontinued; anticonvulsant therapy may be
administered if clinically indicated. Haemodialysis may be
considered in cases of overwhelming overdosage.
Laboratory abnormalities that may occur after an overdose include
elevations in creatinine, BUN, liver enzymes and bilirubin, a
positive Coombs' tests, thrombocytosis, thrombocytopenia,
eosinophilia, leukopenia and prolongation of the prothrombin time.
Treatment of overdosage should be symptomatic and supportive.
White to off-white crystalline powder.
Cefazolin is available in sterile vials containing 500 mg and 1 g
of cefazolin activity as the sodium salt. Cartons contain 5 vials.
Store in a cool dry place. Temperature should not exceed 25°C.
Constituted solutions should be used within 24 hours.
Keep out of reach of children.