Each vial contains: Cefazolin (as sodium), BP 1 g (equivalent to Cefazolin).
Fazef (Cefazolin) in lyophilized form is supplied in vial equivalent to 1 g of cefazolin.
Cefazolin (Fazef) is a semi-synthetic cephalosporin for parenteral administration. It is the sodium salt of 3-{[(5-methyl-1,3,4-thiadiazol-2-yl)thio]-methyl}-8-oxo-7-[2-(1H-tetrazol-1-yl) acetamido]-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid.
Pharmacology: Pharmacodynamics/Pharmacokinetics: After intramuscularly administration of Cefazolin (Fazef) to normal volunteers, the mean serum concentration were 37 mcg/mL at 1 hour and 3 mcg/mL at 8 hours following a 500 mg dose, and 64 mcg/mL at 1 hour and 7 mcg/mL at 8 hours following a 1 gram dose.
Studies have shown that the following intravenous administration of Cefazolin for injection to normal volunteers, mean serum concentrations peaked at approximately 4 mcg/mL at 8 hours for a 1 gram dose.
The serum half-life of Cefazolin (Fazef) is approximately 1.8 hours following I.V. administration and approximately 2.0 hours following I.M administration.
In a study (using normal volunteers) of constant intravenous infusion with dosage of 3.5 mg/kg for 1 hour (approximately 250 mg) and 1.5 mg/kg the next 2 hours (approximately 100 mg), Cefazolin (Fazef) produced a steady serum level at the third hour of approximately 28 mcg/mL.
Studies in patients hospitalized with infections indicate that Cefazolin (Fazef) produces a mean peak serum level approximately equivalent to those seen in normal volunteers.
Bile levels in patients without obstructive biliary disease can reach or exceed serum levels by up to five times; however, in patients with obstructive biliary disease, bile levels of Cefazolin (Fazef) are considerably lower than serum level (<1.0 mcg/mL).
In synovial fluid, the Cefazolin (Fazef) level becomes comparable to that reached in serum at about 4 hours after drug administration.
Studies of cord blood show prompt transfer of Cefazolin (Fazef) across the placenta. Cefazolin (Fazef) is present in very low concentrations in the milk of nursing mothers.
Cefazolin (Fazef) is excreted unchanged in the urine. In the first 6 hours approximately 60% of the drug is excreted in the urine and this increased to 70% to 80% within 24 hours. Cefazolin for injection achieves peak urine concentration of approximately 2400 mcg/mL and 4000 mcg/mL respectively following 500 mg and 1g intramuscular doses.
In patients undergoing peritoneal dialysis (2L/hr), Cefazolin (Fazef) produced mean serum levels of approximately 10 and 30 mcg/mL after 24 hours instillation of a dialyzing solution containing 50 mg/L and 150 mg/L respectively. Mean peak levels were 29 mcg/mL (range 13-144 mcg/mL) with 50 mg/L (three patients), and 72 mcg/mL (range 26-142 mcg/mL) with 150 mg/L (six patients).
Intraperitoneal administration of Cefazolin (Fazef) is usually well tolerated.
Controlled studies on adult normal volunteers, receiving 1 gram 4 times a day for 10 days, monitoring CBC, SGOT, SGPT, bilirubin, alkaline phosphatase, BUN, creatinine, and urinalysis, indicated no clinically significant changes attributed to Cefazolin (Fazef).
Cefazolin (Fazef) is indicated in the treatment of the following serious infections due to susceptible organisms: Respiratory tract infections due to Streptococcus pneumoniae. Klebsiella species, Haemophilus influenzae, Staphylococcus aureus (penicillin-sensitive and penicillin- resistant) and group A beta-hemolytic streptococci. Injectable benzathine penicillin is considered to be the drug choice in treatment and prevention of streptococcal infections, including the prophylaxis of rheumatic fever. Cefazolin (Fazef) is effective in the eradication of streptococci from the nasopharynx; however, data establishing the efficacy of Cefazolin (Fazef) in the subsequent prevention of rheumatic fever are not available at present.
Urinary tract infections due to Escherichia coli, Proteus mirabilis, Klebsiella species and some strains of enterobacter and enterococci.
Skin and skin structure infections due to Staphylococcus aureus (Penicillin-sensitive and penicillin-resistant), group A beta-hemolytic streptococci and other strains of streptococci.
Biliary tract infections due to Escherichia coli, various strains of streptococci, Proteus mirabilis, Klebsiella species and Staphylococcus aureus. Genital infections (i.e., prostatitis, epididymitis) due to Escherichia coli, Proteus mirabilis, Klebsiella species and some strain of enterococci.
Septicemia due to Streptococcus pneumoniae, Staphylococcus aureus (penicillin-sensitive and penicillin resistant), Proteus mirabilis, Escherichia coli, and Klebsiella species.
Endocarditis due to Staphylococcus aureus (penicillin-sensitive and penicillin-resistant) and group A beta-hemolytic streptococci.
Appropriate culture and susceptibility studies should be performed to determine susceptibility of the cause organism to Cefazolin (Fazef).
Perioperative prophylaxis: The prophylactic administration of Cefazolin (Fazef) preoperatively, intraoperatively and postoperatively may reduce the incidence of certain postoperative infections in patients undergoing surgical procedures which are classified as contaminated or potentially contaminated (eg, vaginal hysterectomy, and cholecystectomy in high-risk patients such as those over 70 years of age, with acute cholecystitis, obstructive jaundice or common duct bile stones).
The perioperative use of Cefazolin (Fazef) may also be effective in surgical patients in whom infection at the operative site would present a serious risk (e.g., during open-heart surgery and prosthetic arthroplasty).
The prophylactic administration of Cefazolin (Fazef) should usually be discontinued within 24-hour period after the surgical procedure. In surgery where the occurrence of infection may be particularly devastating (e.g., during open-heart surgery and prosthetic arthroplasty), the prophylactic administration of Cefazolin (Fazef) may be continued for 3 to 5 days following the completion of surgery.
If there are signs of infection, specimens for cultures should be obtained for the identification of the causative organism so that appropriate therapy may be instituted. (See Dosage & Administration.)
Usual Adult Dosage: See Table 1.
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Perioperative Prophylactic Use: Perioperative Prophylactic Use: To prevent postoperative infection in contaminated or potentially contaminated surgery, recommended doses are: a. 1 g I.V or I.M administered 1/2 hour to 1 hour prior to start the surgery.
b. For lengthy operative procedures (e.g., 2 hours or more). 500 mg to 1g I.V or I.M during surgery (administration modified depending on the duration of the operative procedure).
c. 500 mg to 1 gram I.V or I.M every 6 to 8 hours for 24 hours postoperatively. It is important that (1) the preoperative dose be given just (1/2 to 1 hour) prior to start the surgery so that adequate antibiotic levels are present in the serum and tissues at the time of initial surgical incision; and (2) Cefazolin (Fazef) be administered, if necessary, at appropriate intervals during surgery to provide sufficient levels of the antibiotic at the anticipated moments of greatest exposure to infective organisms.
In surgery where the occurrence of infection may be particularly devastating (e.g., open-heart surgery and prosthetic arthroplasty), the prophylactic administration of Cefazolin (Fazef) may be continued for 3 to 5 days following the completion of surgery.
Dosage Adjustment for Patients with Reduced Renal Function: Cefazolin (Fazef) may be used in patients with reduced renal function with the following dosage adjustments: Patients with a creatinine clearance of 55 mL/min or greater or a serum creatinine of 1.5 mg % or less can be given full doses. Patients with creatinine clearance rates of 35 to 54 ml/ min. or serum creatinine of 1.6 to 3.0 mg % can also be given full doses but dosage should be restricted to at least 8-hours intervals. Patients with creatinine clearance rates of 11 to 34 mL/min. or serum creatinine of 3.1 to 4.5 mg % should be given ½ the usual dose every 12 hours. Patients with creatinine clearance rates of 10 mL/min. or serum creatinine clearance rates of 10 mL/min. or less or serum creatinine of 4.6 mg % or greater should be given ½ the usual dose every 18 to 24 hours. All reduced dosage recommendations apply after an initial loading dose appropriate to the severity of the infection. Patients undergoing peritoneal dialysis (see Pharmacology under Actions).
Pediatric Dosage: In pediatric patients a total daily dosage of 25 to 50 mg per kg approximately 10 to 20 mg per pound) of body weight, divided into three or four equal doses, is effective for most mild to moderately severe infections. Total daily dosage may be increased to 100 mg per kg (45 mg per pound) of body weight for severe infections. Since safety for use in premature infants and in neonates has not been established, the use of Cefazolin (Fazef) in these patients is not recommended. (See Table 2 & 3.)
Click on icon to see table/diagram/image
Click on icon to see table/diagram/image
In pediatric patients with mild to moderate renal impairment (creatinine clearance of 70 to 40 mL/min), 60% of the normal daily dose given in equally divided doses every 12 hours should be sufficient. In patients with moderate impairment (creatinine clearance of 40 to 20 mL/min), 25% of normal daily dose given in equally divided doses every 12 hours should be adequate. Pediatric patients with severe renal impairment (creatinine clearance of 20 to 5 mL/min) maybe given 10% of the normal daily dose every 24 hours. All dosage recommendations apply after an initial loading dose.
Method of Administration: Intramuscular Administration: Reconstitute vials with Sterile Water for Injection according to the dilution table under Cautions for Usage. Shake well until dissolved. Cefazolin (Fazef) should be injected into large muscle mass. Pain on injection is infrequent with Cefazolin (Fazef).
Intravenous Administration: Direct (bolus) Injection: Following reconstitution according to the dilution table under Cautions for Usage, further dilute vials with approximately 5 mL Sterile Water for Injection. Inject the solution slowly over 3 to 5 minutes, directly or through tubing for patients receiving parenteral fluids.
Symptoms may include pain, phlebitis and inflammation at site of injection. Dizziness, headache, paresthesia may occur, seizures are possible, especially renally impaired patients. Laboratory tests may include elevation of bilirubin, BUN, creatinine, liver enzymes, positive Coombs' test and eosinophilia, leucopenia, thrombocytopenia, thrombocytosis and lengthening of prothrombin time.
Treatment should be symptomatic and supportive. It is recommended to monitor coagulation status, haematological, hepatic and renal functions until the patient stabilizes. In the event of seizures, immediately discontinue Cefazolin (Fazef) and use anticonvulsant therapy as appropriate and clinically justified. Combined haemodialysis and haemoperfusion may be useful, although no data is available on such use. Peritoneal dialysis is ineffective.
Cefazolin (Fazef) is contraindicated in patients with known allergy to the cephalosporin group of antibiotics.
As with other cephalosporins, Cefazolin (Fazef) tends to darken depending on storage conditions; within the stated recommendations, however, product potency is not adversely affected.
Before therapy with Cefazolin (Fazef) is instituted, careful inquiry should be made to determine whether the patient has had previous hypersensitivity reactions to cefazolin, cephalosporins, penicillins, or other drugs. If this product is given to penicillin-sensitive patients, caution should be exercised because cross-hypersensitivity among beta-lactam antibiotics has been clearly documented and may occur in up to 10% of patients with a history of penicillin allergy. If an allergic reaction to Cefazolin (Fazef) occurs, discontinue treatment with the drug. Serious acute hypersensitivity reactions may require treatment with epinephrine and other emergency reactions may require treatment with epinephrine and other emergency measures, including oxygen, IV fluids, IV antihistamines, corticosteroids, pressor amines, and airway management, as clinically indicated.
Pseudomembranous colitis has been reported with nearly all antibacterial agents, including cefazolin, and may range in severity from mild to life threatening. Therefore, it is important to consider this diagnosis in patients who present with diarrhea subsequent to the administration of antibacterial agents.
Treatment with antibacterial agents alters the normal flora of the colon and may permit overgrowth of clostridia. Studies indicate that toxin produced by Clostridium difficile is a primary cause of "antibiotic-associated colitis".
After the diagnosis of pseudomembranous colitis has been established, therapeutic measures should be initiated, Mild cases of pseudomembranous colitis usually respond to drug discontinuation alone. In moderate to severe cases, consideration should be given to management with fluids and electrolytes protein supplementation and treatment with an oral antibacterial drug clinically effective against C. difficile colitis.
General: Prolonged use of Cefazolin (Fazef) may result in overgrowth of nonsusceptible organisms. Careful clinical observation of the patient is essential.
When Cefazolin (Fazef) is administered to patients with low urinary output because impaired renal function, lower daily dosage is required (see Dosage & Administration).
As with other beta-lactam antibiotics, seizures may occur if inappropriately high doses are administered to patients with impaired renal function (see Dosage & Administration).
Cefazolin (Fazef) is administered to patients with impaired renal function (see Dosage & Administration).
Cefazolin (Fazef) as with all cephalosporins, should be prescribed with caution in individuals with a history of gastrointestinal disease, particular colitis.
Cephalosporins may be associated with a fall in prothrombin activity. Those at risk include patients with renal or hepatic impairment or poor nutritional state, as well as patients receiving a protracted course of antimicrobial therapy, and patients receiving a protracted course of antimicrobial therapy and patients previously stabilized on anticoagulant therapy. Prothrombin time should be monitored in patients at risk of exogenous vitamin K administered as indicated.
Carcinogenesis/Mutagenesis: Mutagenicity studies a long-term studies in animals to determine the carcinogenic potential of Cefazolin for injection (cefazolin for injection) have not been performed.
Use in Children: Safety and effectiveness for use in premature infants and neonates have not been established. See Dosage and Administration for recommended dosage in pediatric patients over 1 month.
Use in Pregnancy & Lactation: Pregnancy: Teratogenic Effects: Pregnancy and Category B: Reproduction studies have been performed in rats, mice and rabbits at doses up to 25 times the human dose and have revealed no evidence of impaired fertility or harm to the fetus due to Cefazolin (Fazef). There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Labor and Delivery: When cefazolin has been administered prior to caesarean section, drug levels in cord blood have been approximately one quarter to one third of maternal drug levels. The drug appears to have no adverse effect on the fetus.
Nursing Mothers: Cefazolin (Fazef) is present in very low concentrations in the milk of nursing mothers. Caution should be exercised when Cefazolin (Fazef) is administered to a nursing woman.
Pregnancy: Teratogenic Effects: Pregnancy and Category B: Reproduction studies have been performed in rats, mice and rabbits at doses up to 25 times the human dose and have revealed no evidence of impaired fertility or harm to the fetus due to Cefazolin (Fazef). There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Category B1.
Safety of this product for use during pregnancy has not been established in human clinical trials. Studies in animals are inadequate or lacking but available data shows no evidence of an increased occurrence of fetal damage. Studies of cord blood show prompt transfer of cefazolin across the placenta. Drug level in cord blood were approximately one quarter to one third of maternal drug levels.
Labor and Delivery: When cefazolin has been administered prior to caesarean section, drug levels in cord blood have been approximately one quarter to one third of maternal drug levels. The drug appears to have no adverse effect on the fetus.
Nursing Mothers: Cefazolin (Fazef) is present in very low concentrations in the milk of nursing mothers. Caution should be exercised when Cefazolin (Fazef) is administered to a nursing woman.
Lactation: Cefazolin is present in very low concentration in the milk of breast feeding mothers. Safety for use in lactating women has not been established.
The following reactions have been reported:
Gastrointestinal: Diarrhea, oral candidiasis (oral thrush), vomiting, nausea, stomach cramps, anorexia and pseudomembranous colitis. Onset of pseudomembranous colitis symptoms may occur during or after antibiotic treatment (See Warnings). Nausea and vomiting have been reported rarely.
Allergic: Anaphylaxis, eosinophilia, itching, drug fever, skin rash, Stevens-Johnson Syndrome.
Hematologic: Neutropenia, leukopenia, thrombocytopenia, thrombocythemia.
Hepatic: Transient rise in SGOT, SGPT and alkaline phosphatase levels has been observed. As with other cephalosporins, reports of hepatitis have been received.
Renal: As with other cephalosporins, reports of increased BUN and creatinine levels, as well as renal failure, have been received.
Local Reactions: Rare instance of phlebitis have been reported at site of injection. Pain at the site of injection after intramuscular administration has occurred infrequently. Some induration has occurred.
Other Reactions: Genital and anal pruritus (including vulvar pruritus, genital moniliasis and vaginitis).
Probenecid may decrease renal tubular secretion of cephalosporins when used concurrently, resulting in increased and more prolonged cephalosporin blood levels.
Drug/Laboratory Test Interactions: A false positive reaction for glucose in the urine may occur with the Benedict's solution, Fehling's solution or with Clinitest tablets, but not with enzyme-based test such as Clinistix.
Positive direct and indirect antiglobulin (Coombs) tests have occurred; these may also occur in neonates whose mothers received cephalosporins before delivery.
Preparation for Parenteral Solution: Parenteral drug products should be shaken well when reconstituted, and inspected visually for particulate matter prior to administration. If particulate matter prior to administration. If particulate matter is evident in reconstituted fluids, the drug solutions should be discarded.
When reconstituted or diluted according to instructions as previously mentioned, Cefazolin (Fazef) is stable for 24 hours at room temperature or for 10 days if stored under refrigeration (5°C or 41°F). Reconstituted solutions may range in color from pale yellow to yellow without a change in potency.
Single-Dose-Vials: For I.M. injection, I.V. direct (bolus) injection or I.V. infusions, reconstitute with Sterile Water for Injection according to the following table. Shake well. (See Table 4.)
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J01DB04 - cefazolin ; Belongs to the class of first-generation cephalosporins. Used in the systemic treatment of infections.
Fazef powd for inj 1 g
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