Cefazolin Sandoz

General characteristics. Structure:

With lyophilisate for preparation of solution for intravenous and intramuscular administration contains in 1 bottle:
Active ingredient: Cefazolin in the form of sodium salt of 1 g.

Pharmacological properties:

Pharmacokinetics. Absorption
After introduction C max in oil in plasma it is reached in 30-75 min.

Tab. Concentration (mkg/ml) in serum after introduction in oil

 Dose   of 30                         min. 1 h 2 h 4 h 6 h 8 h  
500 mg                    36.2 37.9        15.5 6.3      3
1 g               60.1 63.8        54.3 29.3       13.2 7.1 

Tab. Concentration (mkg/ml) in serum later in/in introductions in a dose of 1 g

5 min.  are 15                min. 30 min. 1 h 2 h 4 h old  
188.4     135.8    106.8      73.7   45.6   16.5 

Distribution
Linkng of cefazolin with proteins of plasma - about 65-92%. Cefazolin very well gets into fabrics, including skeletal muscles, a myocardium, a bone tissue, bile and tissues of a gall bladder, an endometria and a vagina.

Cefazolin gets through a placental barrier, is emitted with breast milk. In insignificant quantities gets into cerebrospinal fluid and intraocular liquid.
 
Metabolism and removal
Cefazolin is not metabolized. The most part of the entered dose is exposed to glomerular filtering and is removed with urine in microbiological active form. A small part is removed with bile. T 1/2 of plasma makes about 2 h.

At patients with renal failures T 1/2 can be longer. 
 Semi-synthetic tsefalosporinovy antibiotic of the I generation for parenteral administration. As well as all others beta лактамные antibiotics, possesses bactericidal action, influencing synthesis of a cell wall of microorganisms.

Has a broad spectrum of activity.

It is active in the relation:
Gram-positive aerobes: ◾Staphylococcus spp. (sensitive to Methicillinum).
Streptococcus spp. 
Streptococcus pneumoniae.

Gram-negative aerobes: ◾Branhamella catarrhalis. 
Citrobacter koseri. 
Escherichia coli. 
Haemophilus influenzae. 
Klebsiella spp. 
Neisseria gonorrhoeae. 
Proteus mirabilis.

Anaerobov: Clostridium perfringens. 
Fusobacterium spp. 
Peptostreptococcus spp. 
Prevotella spp. 
Veilonella spp.

 

Microorganisms with intermediate sensitivity:
Anaerobe bacterias.
Eubacterum spp.

It is not active in the relation:
Gram-positive aerobes: Enterococcus spp. 
Staphylococcus spp. (resistant to Methicillinum)
Listeria monocytogenes.

Gram-negative aerobes: ◾Acinetobacter baumanii. 
Aeromonas spp. 
Alcaligenes denitrificans. 
Bordetella spp. 
Campylobacter spp. 
Citrobacter freundii. 
Enterobacter spp. 
Legionella spp. 
Morganella morganii. 
Proteus vulgaris. 
Providencia spp. 
Pseudomonas spp. 
Serratia spp. 
Vibrio spp. 
Yersinia enterocolitica.

Anaerobov: Bacteroides spp. 
Clostridium difficile.

Other microorganisms: Chlamydia spp. 
Mycobacterium spp. 
Mycoplasma spp. 
Rickettsia spp.

Resistant to Streptococcus pneumoniae penicillin have cross resistance to cephalosporins, such as cefazolin.

Indications to use:

Bacterial infections of upper and lower respiratory tracts.
Infections of urinary tract, including: Acute pyelonephritis.

Infections of skin and soft tissues, including: Wound and burn fevers.

- Endocarditis.
- Septicaemia.
- Infections of abdominal organs and biliary tract.
- Infections of bone and connecting fabrics, including - Osteomyelitis.

- Syphilis.
- Gonorrhea.
- Mastitis.
- Prevention of an infection at surgical interventions.

Route of administration and doses:

Cefazolin Sandoz is intended for in/in (in the form of injections and infusions) and introductions in oil.

Doses depend on sensitivity of the activators which caused an infection, and weights of a course of a disease.
vzrosly:

Tab. The standard doses applied to treatment of adults

Indications                                              Dose                 Frequency               Daily
                                                                                         introductions             dose  
Infections of easy severity      of 500 mg               each 8           h 1.5 g
                                                               1 g                    every 12th            p 2g 
Uncomplicated infections
urinary tract                            of 1 g                    every 12th            p 2g 
Infections of average degree
weights and heavy infections               of 1 g                     each 6-8       h 3-4 g 
Infections, life-threatening          from 1 g to 1.5 g     each 6          h 4-6 g 

Doses to 12 g were in rare instances applied.

Tab. Recommendations about the dosing mode at patients with a renal failure

 KK                            Creatinine of serum      the Daily dose      the Interval between
(ml/min. / 1.73 m 2 )     (mg / 100 ml)                                                       introductions (h)  
                               ≥55 ≤1.5                                 A usual dose        Without changes 
                            35-54 1.6-3 0                              Usual dose          of 12 h 
                            11-34 3.1-4.5                              50% of usual
                                                                               doses                       of 12 h 
≤10                                 ≥4.6                               25% of usual
                                                                                 doses                     of 24 h 

 

Prevention of a postoperative infection
The drug is administered in/in or in oil 1-2 g in an initial dose for 0.5-1 h before operation.

At long operations (2 hours and longer) in/in or in oil 500 more mg-1 of during operation are entered. The dose and time of introduction depend on type and duration of operation.

After operation during 24 h enter in/in or in oil 0.5-1 g with an interval of 6-8 h.

If potential infections constitute big danger to the patient (for example, after heart operation or serious orthopedic operation, such as full replacement of a joint), it is recommended to continue postoperative administration of drug during 24-48 h.

- To patients of advanced age: dose adjustment is not required.
- To children at the age of 1 month is also more senior:

At treatment of infections easy and moderate severity the daily dose makes 25-50 mg/kg of body weight, divided into 3-4 introductions.

At the heavy course of infections the daily dose can be increased to the maximum recommended dose - 100 mg/kg of body weight.

Tab. Recommendations about the dosing mode at treatment of children with a renal failure
 
 KK                             cefazolin Dose                 Interval between introductions
(ml/min. / 1.73 m 2 )      (mg/kg)                                 (h)  
>                              50 7 (to 500 mg on introduction)   from 6 to 8 
                           25-50 7                                           12 
                           10-25 7                                          from 24 to 36 
<                             10 7                                          from 48 to 72 

 

In an initiation of treatment to children to whom the hemodialysis is carried out the drug is administered in a dose 7 mg/kg of body weight. Since during dialysis concentration of cefazolin in a blood plasma decreases by 35-65%, between procedures of dialysis the drug is administered in a dose at the rate of 3-4 mg/kg (an interval between procedures of dialysis of 72 h).

Duration of treatment depends on the course of a disease. According to the principles of therapy by antibiotics the drug Cefazolin Sandoz is recommended to continue treatment, at least, within 2-3 days after disappearance of a feverish state and/or receiving confirmation on an activator eradikation.

Preparations of solutions for intramuscular introduction
1 g dissolve in 4 ml, 500 mg - in 2 ml of 0.5% of solution of lidocaine or Water for injections . The maximum dose for introduction in oil 1 g are entered deeply into a muscle.

At treatment of children aged till 1 year it is not necessary to apply lidocaine as solvent.
 
Preparation of solutions for intravenous administration
Cefazolin solution with lidocaine is not applied for in/in introductions.
For intravenous administration in the form of injections 
Cefazolin Sandoz is dissolved in water for injections or 0.9% chloride Sodium solution : dissolution of 1 g of powder requires not less than 4 ml of solution. In the way slow it is possible to enter up to 1 g of cefazolin into injections (3-5 min.).

The drug in higher daily doses (4-6 g in 2-3 introductions) is administered in the way to infusions.
 
For intravenous infusion
For preparation of solution for in/in infusion drug dissolve 0,9% of solution of sodium of chloride or 5% of solution of a dextrose in 50-100 ml. Infusion duration - 20-30 min.

During cultivation bottles need to be stirred up vigorously before full dissolution of drug. Only transparent and colourless solutions are used.

Features of use:

At purpose of Cefazolin Sandoz it is necessary to consider a possibility of development of a cross allergy with other cephalosporins and occasionally found cross allergic reactions to penicillin (especially at patients with allergic diathesis, bronchial asthma or a pollinosis).

In the presence of heavy persistent diarrhea it is necessary to consider probability of development of the pseudomembranous colitis connected with the carried-out therapy by antibiotics. As this state can pose a threat for the patient's life, it is necessary to stop immediately treatment by cefazolin and to appoint the corresponding treatment. Use of the drugs exerting impact on a peristaltics contraindicated.

At treatment of patients with arterial hypertension and heart failure it is necessary to consider the content of sodium in solutions for injections (48 mg on 1 g of cefazolin).

Athletes need to consider that if during treatment cefazolin solution with lidocaine was applied, doping tests can yield positive takes.

If the research of the analysis of urine on the content of glucose is made using Benedict's solution, solution of Felinga or tablets of Klinitest, then results can be false positive though cefazolin does not influence results of a research of urine on the content of glucose with use of a fermental method.

Both indirect, and forward reaction of Koombs can be false positive, including at newborns whose mothers received cephalosporins.
Influence on ability to driving of motor transport and to control of mechanisms
Drug does not exert impact on ability to control of motor transport and other mechanisms.

Side effects:

Allergic reactions
Hyperthermia, urticaria, skin itch, rash, Quincke's disease.

Seldom - an exudative mnogoformny erythema (including Stephens-Johnson's syndrome), a Lyell's disease, a bronchospasm, an acute anaphylaxis.
 
From the alimentary system
Appetite loss, diarrhea, abdominal pain, nausea and vomiting (in most cases these symptoms are poorly expressed and disappear in time or after treatment), dysbacteriosis .

Seldom - tranzitorny hepatitis, cholestatic jaundice , a pseudomembranous coloenteritis , tranzitorny increase in level of hepatic transaminases, bilirubin and/or LDG and ShchF .
 
From an urinary system
Tranzitorny increase in level of an urea nitrogen of blood and creatinine of serum .

Seldom - a renal failure (at treatment by high doses).
 
From TsNS
Dizziness, febricula, fatigue, dreadful dreams, nervousness or concern, sleeplessnesses, drowsiness, weakness, feeling of heat, change in perception of color, confusion of consciousness , encephalopathy and epileptiform attacks (at patients with a renal failure), aseptic meningitis.
 
Laboratory indicators
Tranzitornye - a leukocytosis, a granulocytosis, a monocytosis, a lymphocytopenia, a basophilia, an eosinophilia, a granulocytopenia, a neutropenia, a leukopenia, thrombocytopenia, increase in a prothrombin time.

Seldom – decrease in hemoglobin and/or a hematocrit, anemia, an agranulocytosis, aplastic anemia, a pancytopenia, hemolitic anemia.
 
Local reactions
Phlebitis in the place in/in injections, morbidity in an injection site at introduction in oil.
 
Others
Stethalgia, exudate in a pleural cavity, cough, rhinitis, a hypoglycemia, a hyperglycemia, a vaginitis, thrombophlebitis, superinfection, candidiasis.

Interaction with other medicines:

It is not necessary to apply cefazolin together with the antibacterial drugs having the bacteriostatic mechanism of action (tetracyclines, streptocides, erythromycin , chloramphenicol ) as the researches in vitro showed that between them there is an antagonism.

Combined use with probenetsidy (at the accompanying use of a probenetsid the renal clearance of cefazolin decreases) is not recommended.

At simultaneous use of cefazolin with peroral anticoagulants or high doses of heparin control of parameters of coagulability of blood is necessary.

Cefazolin pharmaceutical is incompatible with aminoglycosides (a mutual inactivation).

At simultaneous use with aminoglycosides and diuretics the risk of development of toxic reactions increases (control of parameters of function of kidneys is necessary).

Contraindications:

- Hypersensitivity to cefazolin.
- Hypersensitivity to other tsefalosporinovy antibiotics.
- Newborns up to 1 month (safety of use is not established).

With care:
- Renal failure.
- Intestines diseases, including - Colitis.
Use at pregnancy and feeding by a breast

Purpose of cefazolin at pregnancy is admissible only if the expected advantage for mother exceeds potential risk for a fruit.

Cefazolin in small amounts is emitted in breast milk. In need of purpose of drug in the period of a lactation, it is necessary to resolve an issue of the breastfeeding termination.

Overdose:

Symptoms: pain, inflammatory reactions and phlebitis in an injection site, dizziness, a headache, paresthesias, is possible development of spasms (especially at patients with diseases of kidneys). Laboratory indicators: the increased level of creatinine, an urea nitrogen of blood, enzymes of a liver and bilirubin, positive reaction of Koombs, a thrombocytosis and thrombocytopenia, an eosinophilia, a leukopenia, increase in a prothrombin time.

Treatment: to immediately stop administration of drug, to carefully control the vital functions of an organism and the corresponding laboratory indicators. Performing symptomatic therapy. In hard cases carrying out a hemodialysis is possible. Peritoneal dialysis is not effective.

Storage conditions:

To store in the place protected from light, at a temperature not above 25 °C, ready solutions - at a temperature of 2-8 °C. Period of validity: 3 years. To store ready solutions no more than 24 hours. To store in places unavailable to children. Not to use after expiry date.

Issue conditions:

According to the recipe

Packaging:

In a bottle of 1 g of lyophilisate. In a cardboard pack 1 bottle.