Drug Cefazolin  is an antibioticbelonging to the first generation of the group cephalosporins. Cefazolin is administered only by injection, because when taken orally (as tablets), it is destroyed in the gastrointestinal tract, not having time to be absorbed into the blood and have an antibacterial effect. The antibiotic has a wide spectrum of action, therefore it can be used for treating various microbes that are sensitive to it. Cefazolin is used to treat organs of almost all systems, for example, respiratory, urinary, genital, skin, joints, etc.

Forms of release and name

The antibiotic Cefazolin is available only in the form of a dry powder, intended for the preparation of a solution for intramuscular or intravenous. The powder is packed in glass vials and hermetically sealed.

In Latin, the name of the drug is written as follows - cefazolin, which is the international name of the antibiotic. Commercial names may differ from the international one, since each pharmaceutical company may produce the drug with the active ingredient cefazolin, but give it a memorable and simple name. For example, the antibiotic cefazolin is available under the following commercial names - Amzolin, Antsef, Atraltsef, Woolmizolin, Zolin, Zolfin, Intrazolin, Ifisol, Kefzol, Lysolin, Natsef, etc. However, there are antibiotics, whose name coincides with the international name of the substance, for example, Cefazolin-AKOS, Cefazolin-Sandoz, etc. All of these drugs are the same - the antibiotic Cefazolin, which is used standardly, regardless of the name and the manufacturer. Only the quality of the product itself, produced by various pharmaceutical plants, may differ.

Dosage

Today, various pharmaceutical concerns produce Cefazolin in the following dosage options:

• 250 mg;
• 500 mg;
• 1 g (1000 mg).

That is how many (250, 500 or 1000) milligrams of powder are in one bottle.

Therapeutic effects and action spectrum of cefazolin

Cefazolin belongs to semisynthetic antibiotics from the group of beta-lactams. These antibiotics kill pathogenic bacteria, destroying their cell wall. Cefazolin is able to destroy many types of microorganisms, therefore, it is an antibiotic. wide spectrum  actions. Compared with other drugs from the group of cephalosporins of the first generation, it is the safest drug, because it has minimal toxicity.

Main and main therapeutic effect  Cefazolin - is the destruction of the pathogenic microorganism that caused the infectious-inflammatory disease. Accordingly, the drug effectively cures infections and inflammations caused by microbes, on which Cefazolin has a destructive effect.

Today, Cefazolin is effective against the following pathogens:

• Staphylococcus aureus (Staphylococcus aureus);
• Epidermal Staphylococcus (Staphylococcus epidermidis);
• Beta-hemolytic streptococci from group A;
• Pus Streptococcus (Streptococcus pyogenes);
• Diplococcus pneumonia (Diplococcus pneumoniae);
• Hemolytic Streptococcus (Streptococcus hemolyticus);
• Viridal Streptococcus (Streptococcus viridans);
• E. coli (Escherichia coli);
• Klebsiella (Klebsiella spp.);
• Proteus (Proteus mirabilis);
• Enterobacter aerogenes;
• Hemophilic bacillus (Haemophilus influenzae);
• Salmonella (Salmonella spp.);
• Shigella (Shigella disenteriae, etc.);
• Neisseria (Neisseria gonorrhoeae and Neisseria meningitidis);
• Corynebacterium (Corynebacterium diphtheriae);
• The causative agent of anthrax (Bacillus anthracis);
• Clostridium (Clostridium pertringens);
• Spirochetes (Spirochaetoceae);
• Treponema (Treponema spp.);
• Leptospira (Leptospira spp.).

  This means that Cefazolin is able to cure an infection of any organ caused by the above pathogenic microorganisms. Unfortunately, due to the frequent and unreasonable use of antibiotics, their spectrum of action is steadily decreasing, since persistent types of microorganisms appear. Therefore, after 5 years, this list of bacteria that are harmful to Cefazolin can change significantly.

The antibiotic does not act on the Pseudomonas aeruginosa, mycobacterium, fungi and protozoa (trichomonas, chlamydia, etc.).

Indications for use

Due to the fact that Cefazolin detrimental effect on many pathogens, it is used to treat infections of various organs. To date, indications for the use of Cefazolin are the following infectious and inflammatory diseases:

• acute and chronic bronchitis;
• infected bronchiectasis;
• pneumonia caused by bacteria (not fungi or viruses);
• bronchopneumonia;
• infections chestdeveloped after surgery (for example, after puncture, etc.);
• pleural empyema;
• lung abscess;
•   middle ear;
• acute and chronic pyelonephritis;
• cystitis;
• urethritis;
• skin infections;
• carbuncles;
• infected gangrene;
• infection on the wound or burn surface;
• infection of the skin or soft tissue after surgery;
• eye infection;
• septic;
• biliary tract infections;
• post-abortion infection;
• uterine infection;
• pelvic abscess;
• peritonitis.

  The above pathologies are amenable to successful treatment with Cefazolin. However, the antibiotic can also be used to prevent the development of infection before and after surgery for removal of the uterus, gallbladder, operations on the heart, bones and joints.

Injections Cefazolin - instructions for use

Cefazolin is administered intramuscularly or intravenously, pre-dissolving the required dose of powder in water, lidocaine or novocaine. The dosage and frequency of Cefazolin injections are determined by the severity of the person’s condition and the potential danger of infection.

Injections are placed in parts of the body where the muscular layer is well developed, for example, in the thigh, shoulder, buttock, etc. Intravenous Cefazolin may be injected in the form of injections or drip.

The powder should be diluted in the required human dosage. For example, if you want to enter 0, 5 g, then take a bottle with the appropriate dosage of Cefazolin powder. You can not take a bottle with a dosage of 1 g and divide it in half to get a dose of 500 mg. But to get a dose of 1 g, you can take two vials of 500 mg or four 250 mg each.

Intravenous injections Cefazolin at a dosage of less than 1 g is administered as a slow injection. The solution is injected into a vein within 3 to 5 minutes. If cefazolin is administered intravenously at a dosage of more than 1 g, then an IV should be used. The antibiotic solution in this case is injected for at least 30 minutes.

Antibiotic solutions must be prepared immediately before use. A quality solution should be transparent and free from any impurities, suspended particles, sediment or turbidity. A slight yellowish tint of the finished solution is allowed, which is the norm and does not indicate damage to the drug. If the resulting solution is not transparent, it can not be used. Also, do not use the solution prepared in advance. In exceptional cases, it is allowed to store the finished solution in the refrigerator for no longer than 2 days.

The dosage of cefazolin is determined by the severity of the pathology. Adults who do not suffer from renal insufficiency should receive an antibiotic in the following dosages:
1.   Mild infections caused by cocci (staphylococci, streptococci) require the use of Cefazolin 500 mg - 1 g every 12 hours. You can enter 500 mg every 8 hours. The maximum daily dose is 1.5 - 2 g.
2.   Acute uncomplicated urinary tract infections (urethritis, etc.) - Cefazolin is administered at 1 g every 12 hours. The daily dose of the antibiotic is 2 g.
3.   caused by pneumococci requires the administration of Cefazolin 500 mg every 12 hours. The daily dosage of the antibiotic is 1 g.
4.   Severe or moderate infections require the use of Cefazolin, 500 mg - 1 g every 6 - 8 hours. The daily dose is 3 to 4 g.
5.   Life-threatening infections are treated with 1 to 1.5 g of Cefazolin every 6 hours. At the same time a person receives 4 - 6 g of antibiotic per day.

It is possible to increase the dosage of Cefazolin to 12 g per day in case of a serious condition of a person, when there is a question of life and death. Elderly people who do not have a dysfunction receive Cefazolin in the usual adult dosage.

To prepare the solution for intramuscular injection, 2 - 3 ml of sterile water, 0.5% lidocaine or 2% novocaine are injected into the powder vial. After that, the vial is shaken vigorously, until the powder is completely dissolved and a clear liquid is formed.

For intravenous injection, Cefazolin powder is dissolved in sterile water. At the same time at least 10 ml of water is necessary to ensure the administration of the drug within 3 to 5 minutes. It is allowed to dilute the antibiotic in at least 4 ml of water, based on 1 g of powder.

The solution for intravenous infusion (dropper) is prepared using 100-150 ml of the primary solvent. The following drugs are used as a solvent:

• sterile saline;
• 5% or 10% glucose solution;
• glucose solution in saline;
• glucose solution in ringer's solution;
• 5% or 10% solution of fructose on water for injection;
• ringer's solution;
• 5% sodium bicarbonate solution.

  Most commonly, intramuscular injections of Cefazolin are used in domestic conditions. Therefore, we consider in detail how to properly dilute the powder in solutions of anesthetics Lidocaine and Novocain.

Cefazolin with Novocain and Cefazolin with Lidocaine - how to breed?

For dilution of Cefazolin powder, 2% Novocain or 0.5% Lidocaine will be required, which are sold in pharmacies in sealed ampoules. Also need sterile syringes. The method of preparation of the solution of Cefazolin on Novocain or Lidocaine for intramuscular administration:
1.   Carefully file and break off the tip of the ampoule with a 2% solution of Novocain or 0.5% Lidocaine.
2.   Open a sterile syringe, put the needle on and lower it into the ampoule with Novocain or Lidocaine.
3.   Dial the required amount of Novocain or Lidocaine into a syringe (2 or 4 ml).
4.   Remove the syringe from the ampoule with Novocain or Lidocaine.
5.   Remove the metal cap from the vial of Cefazolin powder.
6.   To pierce a rubber cap of a bottle with Cefazolin with a needle of a syringe.
7.   Gently squeeze the entire contents of the syringe into the vial of powder.
8.   Without taking out the syringe, shake the bottle so that the powder is completely dissolved.
9.   Dial ready solution  into a syringe.
10.   Remove the syringe from the rubber stopper and turn it upside down with a needle.
11.   Tap with your finger on the surface of the syringe in the direction from the piston to the needle so that air bubbles gather at the base.
12.   Press on the plunger of the syringe to release air.
13.   Make an intramuscular injection.

The amount of Lidocaine or Novocain is determined by the dosage of Cefazolin. To dilute 500 mg of Cefazolin, you will need 2 ml of Novocain or Lidocaine. And for dilution of 1 g of Cefazolin, 4 ml of Novocain or Lidocaine is needed.

Cefazolin injections - instructions for use for children

Cefazolin in infants can be used only if there is an urgent need and a threat to the life of the child. In this case, the antibiotic is used only under the supervision of a physician.

The dosage of cefazolin in children is determined by the severity of the pathology and the body weight of the child. It is by weight that the daily dose of the antibiotic is calculated, which is divided into 2-4 administrations. If the child suffers from renal failure, then the glomerular filtration rate (CC), determined according to the Reberg test, also affects the dosage.

Cefazolin dosages for non-renal children are as follows:

• In light and moderate infections, the daily dosage is calculated at the rate of 25-50 mg of antibiotic per 1 kg of the child's weight. The resulting amount is divided into 2 - 4 administrations per day.
• In severe infections, the dosage is calculated on the basis of 100 mg of Cefazolin per 1 kg of the child's weight. The calculated daily dosage is divided into 3 - 4 administrations.
• Newborns and prematurely weighing less than 2 kg receive Cefazolin in a single amount of 20 mg per 1 kg, every 12 hours. That is, the daily dose of the antibiotic is 40 mg per 1 kg of body weight.
• Children older than 7 days, and with a mass of more than 2 kg, the daily dose of the drug is determined at the rate of 60 mg per 1 kg of weight.

  In newborns and children under 1 month, the rate of excretion of Cefazolin is low, therefore, it is not recommended to exceed the recommended dosage.

If the child suffers from renal failure, the algorithm for determining the dosage of Cefazolin is the following:
1.   Calculate the dose by body weight, as for a child not suffering from kidney disease.
2.   Conduct a Rehberg test and evaluate creatinine clearance.
3.   Calculate the dose of Cefazolin, which can be administered to the child, according to the ratios shown in the table:

  However, the first dose of Cefazolin for children suffering from renal failure is fully administered. And then all subsequent ones are reduced to the required amount, depending on creatinine clearance.

Cefazolin injections for children - how to breed?

Children injections of Cefazolin should be diluted exclusively in solutions of Novocain or Lidocaine. And it is better to choose the anesthetic that has the best analgesic effect in this particular child. In most cases, lidocaine has a more pronounced analgesic effect, so it is recommended to use this particular drug to prepare a solution of Cefazolin for injections. If there is an opportunity, one injection of Cefazolin with Novocain can be given to the child, and one with Lidocaine, so that the baby himself can estimate which solution has the best analgesic effect.

Cefazolin powder for intramuscular injections for children is diluted immediately before use. A dose of an antibiotic less than 500 mg is diluted in 2 ml of Novocain or Lidocaine. A dose of more than 500 mg requires 4 ml of Lidocaine or Novocain. The sequence of actions for breeding Cefazolin is as follows:
1.   Open the ampoule with Lidocaine or Novocain, lower the tip of the syringe needle into the solution.
2.   Gather the required amount of solution - 2 or 4 ml of Novocain or Lidocaine.
3.   Pierce the bottle cap with Cefazolin powder with a needle.
4. Pour Novocain or Lidocaine into the vial and, without removing the needle, vigorously mix the contents to obtain a solution.
5.   Gently draw the entire contents of the vial into the syringe.
6.   Remove the syringe from the vial and make an intramuscular injection.

Use during pregnancy

Cefazolin crosses the placenta and affects the fetus, so the antibiotic can only be used if there is absolute evidence when there is a threat to the life of the mother. To date, it is not clear exactly what effect Cefazolin has on the fetus, therefore, when deciding on the use of antibiotics by pregnant women, it is necessary to carefully weigh the ratio of the possible risk / intended benefit.

To date, Cefazolin has been tested only on pregnant rats. Moreover, the drug in large doses did not cause teratogenic effects, that is, did not lead to the formation of congenital deformities of the fetus. However, such controlled studies on pregnant women, for obvious reasons, were not conducted.

Cefazolin also penetrates into breast milk, although there it is detected in small concentrations. However, if necessary, its use during lactation should transfer the child to the artificial mixture at the time of treatment.

How to prick the antibiotic Cefazolin?

Intramuscularly should be administered Cefazolin only in those parts of the body where the person has a well developed muscular layer. This is usually the front and side of the thigh, buttocks, shoulders or abdominals. Since the injection is very painful, and a thickening is often formed at the injection site, it is recommended to change the areas of injection in turns. For example, one injection is placed in the buttock, the second - in the thigh, the third - in the shoulder, the fourth - in the abdominals. Then they begin again with the buttocks, and so alternate the places of Cefazolin administration until the very end of the course of treatment.

Intramuscular injection should be done slowly - at least 3 - 5 minutes, gradually introducing the medication. The needle should be inserted deep into the muscle, so that the medicine does not fall into the subcutaneous fatty tissue. After the introduction of Cefazolin, the injection site should not be heated, as this may lead to the development of aseptic inflammation. When performing injections of Cefazolin, the general requirements for the implementation of these medical procedures should be observed:
1.   Treat the injection site with an antiseptic (70% alcohol, etc.).
2.   Use only a sterile syringe with a sterile needle.
3.   Release the air from the syringe with the prepared solution.
4.   Position the needle vertically to the skin surface and insert it deep into the muscle.
5. Slowly press on the plunger, injecting the medication for 3-5 minutes.
6.   Having entered all solution, to take out a needle, holding it for the edge, put on the syringe.
7.   Treat the injection site with an antiseptic.

Many people use intramuscular injections of Cefazolin (especially children) needles for intravenous injection, seeking to reduce pain sensations. However, this can not be done, since a thin needle for intravenous injection quite often slips out and goes into the thickness of the muscles, staying there for many years and causing inconvenience to the person. Surgeons often encounter similar phenomena when they have to get needles from syringes from the buttocks and thighs, which broke off and went into the "muscle" a few years ago. In addition, the use of a thinner needle does not reduce the pain of the introduction of Cefazolin.

How much prick Cefazolin?

The duration of Cefazolin use depends on the severity of the infection and the speed of recovery. The course of treatment lasts from 7 to 14 days. Do not use Cefazolin injections for less than 5 days or more than 15 days, since in this case there is a high risk of developing antibiotic-resistant types of microorganisms. These resistant microorganisms can again cause an infection, which will have to be treated again, only with the use of another, even stronger antibiotic. Unfortunately, there is a great risk that, to another antibiotic, the microorganism may be resistant. In this case, the prognosis for life is unfavorable, since there are very few antibiotics in the world that can cope with resistant microbes. And if they do not help, then you can only rely on the sick.

That is why the use of antibiotics, including Cefazolin, must be treated responsibly. You can not throw injections as soon as the person becomes better, considering the treatment is over. A minimum of 5 days of Cefazolin injections should be made, overcoming pain and reluctance. This is especially true of children. After all, a child is faster and easier than an adult can “acquire” resistant types of microbes that will constantly cause infections that are difficult to treat.

Side effects

Mostly side effects  Cefazolin organs concern gastrointestinal tract, or limited to hypersensitivity. If a person suffers hypersensitivity to any other medication, then the risk of developing it to cefazolin is also high. In addition, relatively often develops an increased sensitivity to the antibiotic in people who have a tendency to allergic reactions, hay fever, urticaria, etc.

Blood system  Rarely enough, Cefazolin can lead to a decrease in the number of neutrophils, platelets and leukocytes in the blood. This decrease in blood cells is reversible, their normal number is restored after discontinuation of the drug. Were isolated cases of blood clotting and hemolytic formation.

Urinary system.  An increase in the concentration of urea and creatinine in the blood is possible according to laboratory tests. With the use of large doses of antibiotic may impair the functional activity of the kidneys. In this case, the dosage of Cefazolin is reduced, and further treatment is carried out under constant control of the concentration of urea and creatinine in the blood.

Local reactions.  Main local reaction  is a strong pain when administered antibiotic. In some cases, a seal may form at the injection site. In rare cases, intravenous administration of an antibiotic can trigger the development of phlebitis.

Other organs and systems.  Cefazolin may cause side effects such as dizziness, a feeling of pressure in the chest, convulsions, the addition of another infection, candidiasis (candidal stomatitis or vaginitis). With the development of candidiasis or the addition of another infection, it is necessary to resolve the issue of the further feasibility of using Cefazolin.

Contraindications

If you are allergic to any other antibiotics from the cephalosporins group, Cefazolin is strictly prohibited for use. If a person is allergic to penicillin antibiotics, then Cefazolin is administered carefully, preparing a kit for dealing with anaphylactic shock, since there is cross-allergenicity between these two groups of drugs.

Also, the antibiotic is contraindicated for use during pregnancy and breastfeeding. Cefazolin is not administered to infants up to 1 month since there is no scientifically confirmed information about its safety for newborns.

Analogs

Today, the antibiotic Cefazolin is available under various names, but all of these drugs are synonymous because they contain the same active ingredient. All synonyms of Cefazolin are a powder designed to prepare a solution for intramuscular or intravenous administration. The following synonyms of Cefazolin are available on the domestic pharmaceutical market:

• Amzolin;
• Antsef;
• Atralcef;
• Woolmizolin;
• Zolin;
• Zolfin;
• Intrazolin;
• Ifizol;
• Kefzol;
• Lysolin;
• Natsef;
• Orisolin;
• Orpin;
• Prozolin;
• Reflin;
• Totacef;
• Cesolin;
• Cefazolin-Biohemi;
• Cefazolin-Vatham;
• Cefazolin-KMP;
• Cefazolin Nycomed;
• Cefazolin-Sandoz;
• Cefazolin-Teva;
• Cefazolin-Elf;
• Cefazolin-AKOS;
• Cefazolin-Ferein;
• Cefazolin sodium;
• Cefamezin;
• Cefaprim;
• Cefesol;
• Cefzolin;
• Cefopride

  Only antibiotics from the group of the first generation of cephalosporins, which are intended for oral administration or injection, can be attributed to the analogues of Cefazolin. That is, analogues are antibiotics that have the same spectrum of action as Cefazolin and belong to the same group and generation. Cefazolin analogues include the following drugs:

• Granules, capsules, powder, and cephalexin tablets;
• Cefalotin powder;
• Capsules Ecocephron.

  Cefazolin

Latin name

Cefazolin

Chemical name

(6R-trans) -3- [methyl] -8-oxo-7 - [(1H-tetrazol-1-ylacetyl) amino] -5-thia-1-azabicyclo-oct-2-ene-2-carboxylic acid (and as sodium salt)

Gross formula

C 14 H 14 N 8 O 4 S 3

Pharmacological group

Cephalosporins

Nosological classification (ICD-10)

CAS code

25953-19-9

Characteristic

Semisynthetic antibiotic of group I cephalosporins for parenteral use.

It is used in the form of sodium salt, which is a white or yellowish-white crystalline powder with a bitter salty taste; easily soluble in water, slightly soluble in methanol and ethanol, practically insoluble in benzene, acetone, chloroform. Molecular weight 476.5.

Pharmacology

Pharmacological action - broad spectrum antibacterial, bactericidal.

It interacts with specific penicillin-binding proteins on the surface of the cytoplasmic membrane, inhibits the synthesis of the peptidoglycan cell wall layer (inhibits transpeptidase, inhibits the formation of cross-linking peptidoglycan chains), releases autolytic enzymes of the cell wall, causing its damage and the death of bacteria.

Established in the world Neisseria gonorrhoeae, Shigella spp., Salmonella spp., Escherichia coli, Klebsiella spp., Proteus mirabilis, Enterobacter aerogenes, Haemophilus influenzae. It is also active against Spirochaetaceae and Leptospiraceae.

Cefazolin-resistant most indole-positive strains of Proteus spp. (Proteus vulgaris), Enterobacter cloacae, Morganella morganii, Providencia rettgeri, Serratia spp., Pseudomonas aeruginosa, Mycobacterium tuberculosis, anaerobic microorganisms, methicillin-resistant strains of Staphylococcus spp., Many strains of cococcus socs, many strains of cocococcus spp.

In the digestive tract is destroyed. After i / m administration to volunteers, 0.5 or 1 g of C max was reached after 1 h and was 37 and 64 μg / ml; after 8 h, serum concentrations were 3 and 7 μg / ml, respectively. With the on / in the introduction of a dose of 1 g C max - 185 µg / ml, the concentration in serum after 8 h - 4 µg / ml. T 1/2 of blood is about 1.8 hours at a IV and 2 hours after the i / m administration. Studies in hospitalized patients with infectious diseases  showed that C max values ​​are roughly equivalent to those observed in healthy volunteers. Penetrates joints, cardiovascular tissue, abdominal cavity, kidneys and urinary tract, placenta, middle ear, respiratory tract, skin and soft tissues. The concentration in the tissue of the gallbladder and bile is significantly higher than in the serum. In synovial fluid, the level of cefazolin becomes comparable to serum levels approximately 4 hours after administration. Bad passes through the BBB. Passes through the placental barrier, is found in the amniotic fluid. Secreted (in small quantities) into breast milk. Distribution volume - 0.12 l / kg. Plasma protein binding - 85%.

Not biotransformed. It is mainly excreted by the kidneys in unchanged form: during the first 6 hours - approximately 60%, after 24 hours - 70-80%. After i / m administration in doses of 500 and 1000 mg, the maximum concentration in urine is 2400 and 4000 μg / ml, respectively.

Carcinogenicity, mutagenicity, effects on fertility, teratogenicity

Mutagenic and long-term animal studies have not been conducted to assess potential carcinogenicity.

In reproduction studies in rats, mice and rabbits, when administered in doses up to 25 times higher than MRDC, there was no evidence of an effect on fertility and of embryotoxic action.

Application

Infectious and inflammatory diseases caused by susceptible microorganisms: upper and lower infections respiratory tract, ENT organs (including otitis media), urinary and biliary tract infections, organs of the small pelvis (including gonorrhea), skin and soft tissues, bones and joints (including osteomyelitis), endocarditis, sepsis, peritonitis, mastitis, wound, burns and postoperative infections, syphilis. Prevention of surgical infections in the pre- and postoperative period.

Contraindications

Hypersensitivity to cephalosporins and other beta-lactam antibiotics, children up to 1 month (efficacy and safety have not been established).

Restrictions on the use of

Renal failure, intestinal diseases (including history of colitis).

Use during pregnancy and lactation

When pregnancy is prescribed only for health reasons (adequate and strictly controlled studies have not been conducted).

If necessary, use during breastfeeding stop breastfeeding (cefazolin penetrates into breast milk).

Side effects

Allergic reactions: hyperthermia, skin rash, urticaria, pruritus, bronchospasm, eosinophilia, angioedema, arthralgia, anaphylactic shock, erythema multiforme, malignant exudative erythema (Stevens-Johnson syndrome).

From the side nervous system: cramps.

On the part of the genitourinary system: in patients with kidney disease during treatment with large doses (6 g / day) - impaired renal function (in these cases, reduce the dose).

On the part of the gastrointestinal tract: anorexia, nausea, vomiting, diarrhea, abdominal pain, pseudomembranous enterocolitis, transient increase in liver transaminase activity (AST, ALT), alkaline phosphatase, LDH; rarely - cholestatic jaundice, hepatitis.

From the side of blood formation organs: leukopenia, neutropenia, thrombocytopenia / thrombocytosis, hemolytic anemia.

With long-term treatment: dysbacteriosis, superinfection caused by antibiotic-resistant strains, candidiasis (including candidal stomatitis).

Other: hypercreatininemia, an increase in PV; reactions at the injection site: with i / m administration - pain at the injection site; with a / in the introduction - phlebitis.

Interaction

Not recommended for use simultaneously with anticoagulants and diuretics, including furosemide, ethacrynic acid (with simultaneous use with loop diuretics, tubular secretion of cefazolin is blocked).

Synergism of antibacterial action is observed in combination with aminoglycoside antibiotics. Aminoglycosides increase the risk of kidney damage. Pharmaceutically incompatible with aminoglycosides (mutual inactivation).

Drugs blocking tubular secretion, slow down the excretion, increase the concentration in the blood and increase the risk of toxic reactions.

Dosage and administration

V / m, in / in (drip or jet). The dosage regimen and the duration of the course of treatment are determined individually, taking into account the indications, the severity of the infection, the sensitivity of the pathogen. The average daily dose for adults is 1-4 g (maximum daily dose is 6 g), the frequency of administration is 2-3 times a day (up to 3-4 times / day). For the prevention of postoperative infectious complications - in / in 1 g for 0.5-1 h before surgery, 0.5-1 g during surgery, 0.5-1 g every 8 h during the first days after surgery. The average duration of treatment is 7-10 days. The average daily dose for children is determined at the rate of 20-50 mg / kg / day, in severe cases - up to 100 mg / kg / day. In case of violation of the renal excretory function, the dosing regimen is established taking into account creatinine clearance.

Cefesol ®

    Cefazolin refers to drugs that affect different kinds  microorganisms and having antibacterial activity. It is used in the treatment of infections that are caused by unicellular microorganisms that have a single-layer membrane and do not have one: pneumonia, nonspecific inflammation of the lung tissue, infections of the respiratory tract, purulent pleurisy, inflammation of the abdominal cavity, infection of the blood, urinary tract infections, inflammation of the inner lining of the heart, inflammation bone marrow resulting from all sorts of open injuries, septicotoxemia (burn infection), infection of the urinary tract by pathogenic microbial flora, pyodermatitis (infections of the skin and soft tissues), inflammatory and dystrophic diseases of the osteo-articular apparatus, and degeneration of the bone tissue of a systemic nature.

Composition and release form

  Cefazolin is produced in the form of a white or white powder with a yellowish tint to make an infusion solution. 1 bottle contains cefazolin (in the form of sodium salt, soluble in water) 0.5 g, 1 g, 2 g.

Pharmacodynamics

  Cefazolin is a first-generation semisynthetic antibiotic with a wide range of action that bactericidally affects gram-positive and gram-negative bacteria, inhibiting cell wall biosynthesis. Used for intravenous and subcutaneous administration.

Suppresses the synthesis of natural organic compounds by living organisms. It is active against staphylococci, which form and do not form penicillinase, pneumococci, Salmonella, gram-negative bacilli that do not form a spore, beta-hemolytic streptococci of serological group A, an acute infectious disease caused by Leffler's bacillus, motionless Gram-negative diplocks.

In case of infection of the respiratory tract of moderate severity caused by pneumococci and urinary tract infections, cefazolin is prescribed 1 g twice a day. In the treatment of gram-negative microorganisms, the medicine is prescribed in the amount of 1 g three times a day. In the case of severe infections (blood poisoning, inflammation of the inner lining of the heart, inflammation of the abdominal cavity, purulent pleurisy, inflammation of the joints and bones, urinary tract infections with complications), the dose of the drug per day can be a maximum of 6g in three doses. For children, cefazolin is prescribed in a volume of from 20 mg / kg to 50 mg / kg. In the case of a severe course of the disease, the daily pediatric dosage may be increased to 100 mg / kg. The duration of drug therapy is on average 10 days.

In cases of disease of the excretory system in adults, the dose of cefazolin should be reduced and the time between injections should be increased. The smallest dose of medication for these patients may be 0.5 g.

For patients suffering from kidney disease, in the presence of urea nitrogen in the blood 50 mg% and the rate of purification of the body from the drug by the kidneys 70 ml / min, the amount of cefazolin in the case of moderate infection is half a gram twice a day, with severe course  diseases -1.25 g twice a day (half-life is three to five hours).

In the case of the presence of urea nitrogen in the blood of 50 mg% and clearance of 40 ml / min, the amount of cefazolin in the case of moderate infection is 0.25 g twice a day, in severe cases, 0.6 g twice a day (the half-life is 12 hours ).

If urea nitrogen is equal to 75 mg% and clearance is 20 ml / min, the amount of cefazolin with an average severity of infection is 150 mg once a day, and with severe forms  400g of infection once a day (half-life is 30 hours).

In the presence of urea nitrogen in the blood in an amount of 75 mg% and a clearance of 5 ml / min, the amount of the drug in the case of therapy of the average form of the infection course is 75 mg once a day, with a severe form — 200 mg per day 9 the half-life is forty hours) .

In cases of kidney disease in children, a single dose of cefazolin is administered first, and subsequent doses of medication change depending on the degree of renal failure. For children who have a moderate renal dysfunction with creatine clearance 40 ml / min, the amount of cefazolin should be equal to 60% of the daily dose of the drug used for normal kidney function, and divided into 2 stages of administration. In the case of creatine clearance of 20 ml / min, the amount of cefazolin equals a quarter of the norm and is divided into two stages of administration. In severe forms of the infection in the kidneys with creatine clearance of 5 ml / min daily dose is 10% of the norm with a daily interruption in the introduction of the drug.

It is forbidden to combine solutions of cefazolin and other antibiotics in one syringe or in one solution for injections. The period of therapy depends on the degree of the disease.

Side effects

  The use of cefazolin may have the following undesirable effects: allergic reactions  in the form of nettle rash on the skin, scabies, increasing the concentration of one of the types of leukocytes - non-dividing granulocyte, formed in the bone marrow, chills, fever, scabies, bronchospasm, Quincke swelling, shock, faintness, vomiting, constipation, diarrhea, increased gas formation in the abdominal cavity, colic in the abdomen, changing the microflora of the body, inflammation of the oral mucosa, inflammation of the tongue, acute severe disease of the colon, reducing the number of leukocytes, granulocytes, neutrophil granulocytes, tr mbocytes, accelerated destruction of erythrocytes in the blood, kidney disease (increase in the number of nitrogen-containing products of protein metabolism, increased concentration of urea and creatinine in the blood, itching of the anus, local itching in the external genitalia, inflammation of the inner lining of the veins, pain along the affected vein , hardening of the tissue and pain in the area of ​​the injection, re-infection with a new infection in the presence of an incomplete infection process, inflammation caused by Candida fungi.

In patients with kidney disease, in the case of drug therapy in doses exceeding 6g, there is a risk of developing impaired renal function, which is characterized by retention of the elements of nitrogen metabolism, and as a result of an imbalance of acid-base water balance. With intravenous administration, local pain is possible, there is a risk of inflammation of the inner walls of the vein.

In the case of intramuscular injection, pain is observed.

Cefazolin and alcohol

  When taking the drug alcohol is strictly contraindicated.

Contraindications

  In the case of cefazolin therapy, undesirable effects may occur:
  - in case of sensitivity to drugs of the cephalosporins group;
  - the period of pregnancy;
  - children's age of a newborn up to one month;
  - breastfeeding period.

During pregnancy

  Cefazolin is not recommended for use during pregnancy. The use of the drug during breastfeeding is possible if the benefits it brings are higher than the perceived risk for the newborn baby.

special instructions

  In the event of allergy after the start of cefazolin, it is recommended to suspend drug therapy and apply treatment to reduce the body's sensitivity to the drug. If in the course of drug therapy exacerbation of kidney disease is detected, it is recommended to reduce the dose of cefazolin and conduct further drug therapy, constantly monitoring the amount of urea nitrogen and creatinine in the blood.

The combined use of cefazolin with diuretic drugs and drugs that prevent the formation of blood clots, is not recommended. In the case of kidney disease, it is necessary to reduce the volume of the drug and increase the intervals between drug injections, depending on the degree of kidney damage. If stable kidney function is not observed, the concentration of the drug in the blood should be checked for safe use. The initial dose of cefazolin should be 500mg.

If patients are allergic to penicillin, then it is possible to assume their reaction to the use of cefazolin. Possible manifestation of cross-reactive antigens with other antibiotics of the cephalosporin group, and often with antibiotics. penicillin group. For patients with gastrointestinal problems, cefazolin should be given carefully.

In the case of cefazolin therapy, a Kumbus test and a false positive reaction to the determination of the glucose level in the urine analysis may occur. The safe use of cefazolin in premature babies and children in the first month of life has not been scientifically proven. For patients suffering from colitis, it is recommended to prescribe cefazolin with caution. The effect of cefazolin on driving and other means requiring increased concentration is not scientifically proven.

Interaction

The use of cefazolin with diuretic drugs and drugs that prevent the formation of blood clots, is not recommended. The mutually reinforcing effect of the antimicrobial action in the case of simultaneous use of the drug with antibiotics of the antiparasitic direction, vancomycin, rifampicin has been scientifically proven. Increasing the blood concentration of cefazolin provokes furosemide.
  Antibacterial antibiotics provoke a violation of the kidney in the case of joint use with cefazolin. The use of lidocaine for the preparation of a solution for intravenous administration is not recommended. Kidney removal of waste products is reduced by the combined use of cefazolin with probenecid.
  False positive results of tests on the concentration of sugar in the urine in the case of their use with the use of Benedict's solution, Fehling's solution, or Klinitest in the form of tablets are possible. Along with this, no effect of cefazolin on the analyzes of the level of sugar in the urine, carried out using enzymatic methods.

Overdose

  In case of exceeding the volume of injected cefazolin, migraine may occur, loss of orientation. With an increase in the dose of the drug for patients suffering from kidney disease, manifestations of seizures, vomiting, and rapid heartbeat are possible. If patients have a poisoning and if an overdose of the drug is observed, accelerated elimination of the drug can be achieved by hemodialysis.

Price

  The cost of 1 bottle of cefazolin 1g is 13-23 rubles and 89-102 rubles, depending on the manufacturer.

Analogs

• Antsef
• Zolin
• Zolfin
• Intrazolin
• Ifizol
• Kefzol
• Lysolin
• Natsef
• Orizolin
• Orpin
• Reflin
• Totatsef
• Cesolin
• Cefazolin sodium
• Cefazolin Sandoz
• Cefazolin Elf
• Cefazolin "Biohemi"
• Cefazolin-AKOS
• Cefazolin-Ferein
• Cefazolin sodium salt
• Cefamezin
• Cefaprim
• Cefesol
• Cefopride

Amzolin; Antsef; Atralcef; Woolmizolin; Zolin; Zolfin; Intrazolin; Ifizol; Kefzol; Lysolin; Natsef; Orisolin; Prozolin; Reflin; Totacef; Cesolin; Cefazolin; Cefazolin Biohemi; Cefazolin Watham; Cefazolin sodium; Cefazolin sodium; Cefazolin Nycomed; Cefazolin Sandoz; Cefazolin Elf; Cefazolin-Akos; Cefazolin-KMP; Cefazolin-Teva; Cefazolin-Ferein; Cefazolin sodium salt; Cefazolin sodium; Cefamezin; Cefaprim; Cefesol; Cefzolin; Cefopride

Cefazolin - I cephalosporin antibiotic of the first generation for parenteral use, possessing a wide spectrum and powerful bactericidal action. It is indicated for a variety of infections caused by susceptible microorganisms: infections of the respiratory tract and ENT organs (bronchitis, pneumonia, bronchopneumonia, empyema and lung abscess, otitis media, tonsillitis, mastoiditis), infections of the genitourinary system (pyelonephritis, cystitis, urethritis, prostatitis, gonorrhea ), infections of skin and soft tissues (cellulitis, mastitis, erysipelas, carbuncles, wound and burn infections), infections of bones and joints (osteomyelitis, septic arthritis), infections of the biliary tract, gynecological and obstetric infections (septic abortion, infections uterus, salpingitis and pelvic abscesses), bacterial endocarditis, systemic septic infections (sepsis, septicemia, peritonitis). It is used to prevent infections during surgical interventions in the pre- and postoperative period.

Active-active substance:
Cefazolin / Cefazolin.

Dosage Forms:
Injection solution (powder for preparing injection solution).

Cefazolin

Properties / Action:
Cefazolin is a semi-synthetic cephalosporin antibiotic of the first generation for parenteral use (administered intramuscularly or intravenously), which has a broad spectrum and a powerful bactericidal effect. Cefazolin belongs to the group of beta-lactams. Cefazolin has the same antibacterial spectrum as other first-generation injection cephalosporins, but it has been shown that it has important clinical and pharmacological advantages - it is the least toxic cephalosporin antibiotic of the first generation.
The mechanism of action of Cefazolin is similar to that of penicillins. Like all other beta-lactam antibiotics, cefazolin has a bactericidal effect, which is based on the inhibition of the synthesis of mucopeptides, the disruption of the synthesis of bacterial cell membranes, which leads to the lysis of fissionable bacteria.
Cefazolin antibacterial spectrum:
Cefazolin is particularly active against gram-positive, as well as against many gram-negative bacteria.
Gram positive cocci:

Staphylococcus aureus - Staphylococcus aureus (active against penicillinase-forming strains, highly resistant to beta-lactamase);

Staphylococcus epidermidis (staphylococci that show methicillin resistance, are resistant to Cefazolin),

beta hemolytic streptococci of group A; Streptococcus pyogenes, pneumoniae (Diplococcus), viridans, hemolyticus and other strains of Streptococcus (many strains of enterococci are resistant to Cefazolin).
Gram-negative cocci and sticks:

Escherichia coli - Escherichia coli (more active than other cephalosporins);

Klebsiella spp. (Klebsiella pneumoniae - more active than other cephalosporins);

Proteus mirabilis;

Enterobacter aerogenes;

Haemophilus influenzae;

Salmonella spp, including Salmonella typhi, flexneri;

Shigella spp, incl. Shigella disenteriae;

Paracolon spp;

Neisseria gonorrhoeae (including many penicillin-resistant strains), Neisseria meningitidis are usually sensitive;

is also active against Corynebacterium diphtheriae, Bacillus anthracis, Clostridium pertringens, Spirochaetoceae, Treponema spp., Leptospira spp.
Moderately sensitive to cefazolin:

Streptococcus faecalis; in vitro Cefazolin and gentamicin are synergistic with respect to Streptococcus faecalis.
Resistant to Cefazolin:

indole-positive strains of Proteus spp. (Proteus vulgaris, morganii);

Pseudomonas (P. aeruginosa);

Enterobacter cloacae;

Morganella morganii;

Providencia rettgeri;

Serratia spp .;

Acinetobacter;

Mycobacterium tuberculosis;

most anaerobic strains, some bacteroids, enterococci, viruses, fungi, protozoa.

Pharmacokinetics:
When taken orally, cefazolin is not absorbed. Cefazolin, administered intramuscularly or intravenously, creates high serum concentrations.
For intramuscular administration, Cefazolin is rapidly absorbed from the injection site. After i / m administration, blood concentrations are higher and last longer than after administration of most other cephalosporins.
Peak concentrations: after administration of 0.5 g and 1 g in blood, the following concentrations are achieved:

The half-life of plasma is about two hours.
After intravenous administration of 1 g, the maximum serum concentration at 188.4 µg / ml is reached after 5 minutes, decreasing after 4 hours to 16.5 µg / ml.
Due to the high and long-lasting blood levels, Cefazolin can be administered in a dose of 1 g at intervals of 12 hours, using a convenient two-dose schedule per day.
Approximately 70-90% of the administered dose is bound to plasma proteins.
Cefazolin easily penetrates the tissues of various organs, in particular the tonsils, gallbladder wall and appendix. Cefazolin is also found in high concentrations in physiological fluids. In the absence of obstruction of the biliary tract, 4 hours after the injection, its concentration in the bile surpasses those in the serum. Cefazolin reaches therapeutic concentrations in ascitic and pleural fluid, inflammatory exudate, lungs, liver, skin and soft tissues, joints, heart and peritoneum, middle ear. Very high concentrations of Cefazolin are created in the kidneys - after administration of 1 g of Cefazolin, its concentration in the urine is up to 4000 µg / ml. Cefazolin passes through the capillary membranes in the bones and reaches bactericidal concentrations in the fluid of the interstitial space of healthy and osteomelitic bone.
In the absence of infection of the meninges, Cefazolin is found in cerebrospinal fluid  in extremely insignificant concentrations, so we can assume that it does not pass through the blood-brain barrier.
Cefazolin levels in the fetal bloodstream are similar to those in the mother’s bloodstream. Cefazolin is found in the milk of lactating women in very low concentrations.
Cefazolin is not metabolized in the liver and excreted from the body unchanged.
Cefazolin is excreted mainly in the urine due to glomerular filtration and tubular secretion. The amount of Cefazolin excreted in the urine is 60–90% during the first 6 hours, and after 70 hours, 70–95% of the administered dose. The release of Cefazolin with bile occurs only to a small extent.
P1 / 2 plasma increases in patients with impaired renal function up to 20–40 hours.

Indications:
Due to its pharmacokinetic features, Cefazolin is indicated for a number of infections caused by pathogenic microorganisms sensitive to Cefazolin.
The range of indications for use of Cefazolin include:

infections of the respiratory tract and ENT organs, such as acute and chronic bronchitis, infected bronchiectasis, bacterial pneumonia and bronchopneumonia, postoperative infections of the chest, empyema and lung abscess, infections of ENT organs such as otitis media, tonsillitis and mastoiditis;

infections of the genitourinary system, such as acute and chronic pyelonephritis, cystitis, urethritis, prostatitis, gonorrhea;

infections of skin and soft tissues including cellulitis, mastitis, erysipelas, carbuncles, infected gangrene, wound, burn, and postoperative infections;

eye tissue infections;

infections of bones and joints, including osteomyelitis and septic arthritis;

biliary tract infection;

gynecological and obstetric infections, including septic abortion, infections of the uterus, salpingitis and pelvic abscesses;

bacterial endocarditis;

syphilis;

systemic septic infections: sepsis, septicemia, peritonitis;

prevention of infections in surgical interventions in the pre- and postoperative period (hysterectomy, cholecystectomy, open heart surgery, operations on the bones and joints); preoperative, intraoperative and postoperative Cefazolin may reduce the incidence of postoperative infections.

Dosage and administration:
Cefazolin is intended only for parenteral administration - intramuscularly and intravenously (jet or drip). Doses set individually, taking into account the severity and localization of infection, the sensitivity of the pathogen.
Preparation of solutions and use:
Intramuscularly Cefazolin is injected into the broad muscle mass. The solution for i / m injections is prepared by dissolving the dry matter with a 0.5% solution of lidocaine a or in 2-3 ml of water for injection.
For intravenous jet injection, the powder is dissolved in 10 ml of sterile water for injection (at least 4 ml of solvent per 1 gram of dry matter).
In both cases, after adding the solvent, the vial must be vigorously shaken to completely dissolve the powder.
Doses up to 1 g of cefazolin can be administered as a slow intravenous infusion (over 3-5 minutes). When using higher doses, infusion should be used (over a period of more than 20 and up to 30 minutes).
To prepare an infusion solution, you can use 100-150 ml of physiological solution (0.9% sodium chloride solution), 5% or 10% glucose or glucose solution with saline, as well as a glucose solution in Ringer's solution, 5% or 10% fructose solution on sterile water for injection, ringer's solution for injection and 5% sodium bicarbonate solution.
Use only freshly prepared and clear solutions. Unused solution is not suitable for later use. The possible yellowish color of the solution after dissolving the powder is not an indication of any change in the properties of the drug or differences in its therapeutic efficacy.
Dosing Instructions for Adults:

In very rare cases, Cefazolin doses of up to 12 g per day were used.
When prescribing Cefazolin to adult patients with renal failure:

Perioperative prophylaxis:
To prevent infections during surgery, the dosage of Cefazolin depends on the type and duration of the operation.

1 gram is administered intravenously or intramuscularly 30 minutes to 1 hour before the start of surgery (the dose is sufficient with minor surgical interventions of short duration);

during prolonged surgical operations (more than 2 hours), in addition, from 0.5 to 1 g is administered intravenously or intramuscularly during the operation itself (depending on the duration, it can also be administered at certain intervals during the surgical operation);

during postoperative period  after the initial dose, doses from 0.5 g to 1 g are administered intravenously or intramuscularly with an interval of 6-8 hours within 24 hours;

if a potential infection may pose a threat to the patient (for example, after heart surgery or after extensive orthopedic surgery, such as arthroplasty), it is recommended to continue postoperative administration of Cefazolin for a period of 3 to 5 days.
It is important to observe the above terms so that during the surgical incision, sufficient concentrations of the antibiotic are already present in the patient’s serum and tissues.
Use in children with normal renal function:
Children are prescribed from 25 to 50 mg of Cefazolin per 1 kg of body weight per day, divided into 2-4 injections, with minor infections. In severe infections, the daily dose of Cefazolin can be increased to 100 mg / kg body weight. Newborn and premature babies aged 0 to 7 days, weighing less than 2 kg, a dose of 20 mg / kg every 12 hours is recommended (total daily dose of 40 mg / kg). Children older than 7 days and weighing more than 2 kg, a daily dose of 60 mg / kg is recommended. In newborns and infants less than 1 month old, the half-life of Cefazolin is generally higher than in older children. When prescribing Cefazolin to patients in this age group, in order to avoid an overdose of Cefazolin, it is necessary to monitor the levels of Cefazolin in serum.
Use in children with renal failure:
Children with creatinine clearance from 70 to 40 ml / min / 1.73 m 2 are given 60% of the standard dose of Cefazolin divided into two doses. Children with creatinine clearance ranging from 40 to 20 ml / min / 1.73 m 2 are given 25% of the standard dose of Cefazolin divided into two doses. When creatinine clearance between 20 and 5 ml / min / 1.73 m 2 is assigned 10% of the standard daily dose of Cefazolin at intervals of 24 hours. However, the usual loading dose should be administered first. Children undergoing hemodialysis receive 7 mg / kg body weight at the start of treatment. Due to the fact that serum levels of Cefazolin during dialysis are reduced by 35-65%, between dialysis sessions the size of the administered dose of Cefazolin should be from 3 to 4 mg / kg body weight (the duration between hemodialysis sessions is 72 hours).

Overdose:
Cefazolin or its cumulation in patients with kidney failure may cause neurotoxic effects. At the same time, increased convulsive readiness, clonicotonic convulsions, vomiting and tachycardia were noted. In the case of the development of toxic reactions in patients, as well as signs of an overdose of Cefazolin, its elimination from the body can be accelerated by hemodialysis. Peritoneal dialysis is ineffective.

Contraindications:
Cefazolin is absolutely contraindicated in patients with allergies to cephalosporin antibiotics. Patients allergic to penicillin Cefazolin can be administered with great caution, provided that there is everything necessary for resuscitation in the event of possible anaphylaxis, because between the two groups of beta-lactam antibiotics there is partial cross allergenicity, especially in patients with immediate type hypersensitivity to penicillins .

Use during pregnancy and lactation:
Cefazolin has the ability to penetrate the placental barrier. Cefazolin can be used during pregnancy only for absolute reasons. If the administration of Cefazolin is prescribed during pregnancy, it is necessary to carefully evaluate the degree of its beneficial effects in comparison with the risk. As with other beta-lactam antibiotics, there is no evidence of the toxic effect of Cefazolin on the embryo or fetus. Studies on the effect on reproductive function related to the possible teratogenic effect of Cefazolin in rats and mice in doses that were 25 times higher than the doses used in humans. However, well-controlled studies in pregnant women have not been conducted. Cefazolin concentrations in cord blood after its administration to the mother before a caesarean section ranged from 1/4 to 1/3 with respect to concentrations in the mother's blood.
Cefazolin is found in human milk, although in very low concentrations. With the introduction of Cefazolin, breastfeeding mothers should refrain from breastfeeding.

Side effects:
Side effects of cephalosporin antibiotics are limited mainly by disorders of the gastrointestinal tract and, in some cases, symptoms of hypersensitivity. The frequency of the latter phenomena is higher in individuals who have previously found increased sensitivity to various pharmaceutical preparations, as well as in patients with a tendency to allergies, asthma, hay fever, urticaria, etc.
From the side digestive system. Undesirable side effects from the gastrointestinal tract during treatment with Cefazolin may manifest as loss of appetite, glossitis, heartburn, abdominal pain, nausea and vomiting, diarrhea. Candidiasis and pseudomembranous colitis were noted as rare side effects. In rare cases, there may be a temporary increase in the levels of alkaline phosphatase, total bilirubin (cholestatic jaundice), ACT, and ALT (drug-induced hepatitis).
Allergic reactions. Cefazolin may cause allergic reactions. Cases of drug fever, skin rash (urticaria), pruritus, bronchospasm, eosinophilia have been reported; in isolated cases - angioedema, arthralgia, allergic nephritis, anaphylactic shock, erythema multiforme exudative (including Stevens-Johnson syndrome).
From the hemopoietic system. In some cases, reversible neutropenia and leukopenia, thrombocythemia, and the positive results of the direct and indirect Coombs test were noted when calculating blood corpuscles. There were sporadic cases of hypoprothrombinemia, which was reversible in the administration of vitamin K. In the treatment with cephalosporins, rare cases of hemolytic anemia were reported.
From the urinary system. When conducting therapy with Cefazolin, a transient increase in blood urea nitrogen levels, hypercreatininemia, may occur. Compared with cephaloridin or gentamicin, the effects of nephrotoxicity are practically not observed. Rarely, usually in the treatment with large doses (6 g), renal dysfunction (in these cases, the dose is reduced and the treatment is carried out under the control of the dynamics of urea nitrogen and creatinine in the blood).
Local reactions. Intramuscular injections of Cefazolin can be painful and cause hardening of the tissues at the injection site. Some patients after intravenous administration of Cefazolin had phlebitis (the frequency of phlebitis is insignificant).
Other side effects include dizziness, tightness in the chest, cramps; dysbacteriosis, superinfection, candidiasis - candidal stomatitis and vaginitis. Recent effects are due to the reproduction of Cefazolin-insensitive microorganisms. These side effects require the appropriate action to be taken, and the physician must carefully consider whether to discontinue or continue Cefazolin.

Special instructions and precautionary measures:
Prior to use, determine the sensitivity of the isolated pathogens.
All cephalosporins should be used with caution in patients with allergies to penicillin, carbapenems. There are clinical and laboratory data indicating partial cross-allergenicity between antibiotics of the penicillin and cephalosporin groups, and in rare cases severe reactions to the administration of one or both of these antibiotic groups have been reported (anaphylaxis after parenteral administration). In the event of signs of allergic reactions, Cefazolin administration should be discontinued and appropriate symptomatic treatment should be administered (epinephrine; GCS — prednisone, dexamethasone; antihistamines).
Cefazolin is used with caution in renal or hepatic insufficiency, bowel disease (including a history of colitis).
In patients with reduced renal function, it is necessary to select dosage levels and intervals between injections of Cefazolin, depending on the severity of renal functional impairment. In the event of an unstable kidney function, continuous monitoring of serum levels of Cefazolin will ensure the safety of the drug. Any simultaneous or subsequent prescription of other drugs with nephrotoxic effects (aminoglycoside antibiotics - kanamycin, streptomycin, gentamicin, etc.) enhances the toxic effect on the kidneys and requires careful monitoring of their function. Do not use cefazolin at the same time as "loop" diuretics.
In children in early infancy, Cefazolin can be used only when absolutely necessary and under direct medical supervision.
Prolonged use of any antibiotic can lead to the reproduction of microorganisms insensitive to it - superinfection. In such cases, it is necessary to take appropriate measures.
The use of cephalosporin antibiotics may distort the results of some laboratory tests. False-positive results of laboratory tests for sugar content in the urine may be observed if they are performed using a Benedict solution, Fehling solution or Klinitest. Distortion of results does not occur in the case of using enzymatic methods. False-positive results of the direct and indirect Coombs test were noted, for example in newborns whose mothers were treated with Cefazolin.
The solution is stable for 48 hours when stored in the refrigerator.

Drug Interactions:
It is not recommended to prescribe Cefazolin at the same time as anticoagulants.
With simultaneous use with "loopback" diuretics (furosemide, ethacrynic acid), Cephazolin canalicular secretion is blocked (co-administration should be avoided).
Cefazolin's kidney clearance is reduced while co-administered with probenecid, which leads to increased and longer blood cefazolin concentrations.
Synergism of antibacterial action is observed when combined with aminoglycoside antibiotics, vancomycin ohm, rifampicin ohm. Aminoglycosides increase the risk of kidney damage. Pharmaceutically incompatible with aminoglycosides (mutual inactivation).
Cefazolin can cause disulfiram-like reactions while being used with ethanol.

Storage conditions:
Store in a dry, dark, out of reach of children at a temperature of 5 ° C.
Provided proper storage of the drug fully retains its activity until the expiration date indicated on the package.
Vacation conditions from pharmacies - prescription.

Structural formula

Russian name

Latin name of the substance Cefazolin

Cefazolinum ( kind of  Cefazolini)

Chemical name

(6R-trans) -3- [methyl] -8-oxo-7 - [(1H-tetrazol-1-ylacetyl) amino] -5-thia-1-azabicyclo-oct-2-en-2-carboxylic acid (as sodium salt)

Gross formula

C 14 H 14 N 8 O 4 S 3

Pharmacological group of substance Cefazolin

Nosological classification (ICD-10)

CAS code

25953-19-9

Characteristics of the substance Cefazolin

Semisynthetic antibiotic of group I cephalosporins for parenteral use.

It is used in the form of sodium salt, which is a white or yellowish-white crystalline powder with a bitter salty taste; easily soluble in water, slightly soluble in methanol and ethanol, practically insoluble in benzene, acetone, chloroform. Molecular weight 476.5.

Pharmacology

pharmachologic effect  - bactericidal, broad spectrum antibacterial.

It interacts with specific penicillin-binding proteins on the surface of the cytoplasmic membrane, inhibits the synthesis of the peptidoglycan cell wall layer (inhibits transpeptidase, inhibits the formation of cross-linking peptidoglycan chains), releases autolytic enzymes of the cell wall, causing its damage and the death of bacteria.

Installed   in vitro  and clinically confirmed activity against gram-positive microorganisms - Staphylococcus aureus  (including penicillin-producing strains), Staphylococcus epidermidis, Streptococcus pyogenes  (beta hemolytic streptococci of group A),   Streptococcus pneumoniae, Corynebacterium diphtheriae, Bacillus anthracis, a number of gram-negative bacteria - Neisseria meningitidis, Neisseria gonorrhoeae, Shigella spp., Salmonella spp.,Escherichia coli, Klebsiella spp., Proteus mirabilis, Enterobacter aerogenes, Haemophilus influenzae.  Active also in relation to Spirochaetaceae and Leptospiraceae.

Cefazolin-resistant most indole-positive strains Proteus spp. (Proteus vulgaris), Enterobacter cloacae, Morganella morganii, Providencia rettgeri, Serratia spp., Pseudomonas aeruginosa, Mycobacterium tuberculosis,  anaerobic microorganisms, methicillin-resistant strains Staphylococcus spp.,  many strains Enterococcus spp.

In the digestive tract is destroyed. After i / m administration to volunteers, 0.5 or 1 g of C max was reached after 1 h and was 37 and 64 μg / ml; after 8 h, serum concentrations were 3 and 7 μg / ml, respectively. With the on / in the introduction of a dose of 1 g C max - 185 µg / ml, the concentration in serum after 8 h - 4 µg / ml. T 1/2 of blood is about 1.8 hours at a IV and 2 hours after the i / m administration. Studies in hospitalized patients with infectious diseases have shown that C max values ​​are roughly equivalent to those observed in healthy volunteers. Penetrates joints, cardiovascular tissue, abdominal cavity, kidneys and urinary tract, placenta, middle ear, respiratory tract, skin and soft tissues. The concentration in the tissue of the gallbladder and bile is significantly higher than in the serum. In synovial fluid, the level of cefazolin becomes comparable to serum levels approximately 4 hours after administration. Bad passes through the BBB. Passes through the placental barrier, is found in the amniotic fluid. Secreted (in small quantities) into breast milk. Distribution volume - 0.12 l / kg. Plasma protein binding - 85%.

Not biotransformed. It is mainly excreted by the kidneys in unchanged form: during the first 6 hours - approximately 60%, after 24 hours - 70-80%. After i / m administration in doses of 500 and 1000 mg, the maximum concentration in urine is 2400 and 4000 μg / ml, respectively.

Carcinogenicity, mutagenicity, effects on fertility, teratogenicity

Mutagenic and long-term animal studies have not been conducted to assess potential carcinogenicity.

In reproduction studies in rats, mice and rabbits, when administered in doses up to 25 times higher than MRDC, there was no evidence of an effect on fertility and of embryotoxic action.

Use of Cefazolin

Infectious and inflammatory diseases caused by susceptible microorganisms: infections of the upper and lower respiratory tract, ENT organs (including otitis media), infections of the urinary and biliary tracts, pelvic organs (including gonorrhea), skin and soft tissues, bones and joints (including osteomyelitis), endocarditis, sepsis, peritonitis, mastitis, wound, burn and postoperative infections, syphilis. Prevention of surgical infections in the pre- and postoperative period.

Contraindications

Hypersensitivity to cephalosporins and other beta-lactam antibiotics, children up to 1 month (efficacy and safety have not been established).

Restrictions on the use of

Renal failure, intestinal diseases (including history of colitis).

Use during pregnancy and lactation

When pregnancy is prescribed only for health reasons (adequate and strictly controlled studies have not been conducted).

If necessary, use during breastfeeding stop breastfeeding (cefazolin penetrates into breast milk).

Side Effects of Cefazolin

Allergic reactions: hyperthermia, skin rash, urticaria, pruritus, bronchospasm, eosinophilia, angioedema, arthralgia, anaphylactic shock, erythema multiforme, malignant exudative erythema (Stevens-Johnson syndrome).

From the nervous system:  convulsions.

From the genitourinary system:  in patients with kidney disease during treatment with large doses (6 g / day) - impaired renal function (in these cases, reduce the dose).

On the part of the digestive tract:  anorexia, nausea, vomiting, diarrhea, abdominal pain, pseudomembranous enterocolitis, transient increase in liver transaminase activity (AST, ALT), alkaline phosphatase, LDH; rarely - cholestatic jaundice, hepatitis.

From the side of blood-forming organs:  leukopenia, neutropenia, thrombocytopenia / thrombocytosis, hemolytic anemia.

With long-term treatment:  dysbacteriosis, superinfection caused by antibiotic-resistant strains, candidiasis (including candidal stomatitis).

Other:  hypercreatininemia, an increase in PV; reactions at the injection site: with i / m administration - pain at the injection site; with a / in the introduction - phlebitis.

Interaction

Not recommended for use simultaneously with anticoagulants and diuretics, including furosemide, ethacrynic acid (with simultaneous use with loop diuretics, tubular secretion of cefazolin is blocked).

Synergism of antibacterial action is observed in combination with aminoglycoside antibiotics. Aminoglycosides increase the risk of kidney damage. Pharmaceutically incompatible with aminoglycosides (mutual inactivation).

Drugs blocking tubular secretion, slow down the excretion, increase the concentration in the blood and increase the risk of toxic reactions.

Route of administration

V / m, V / V.

Precautions substances cefazolin

Patients with a history of allergic reactions to penicillins, carbapenems, may have an increased sensitivity to cephalosporin antibiotics.

During treatment with cefazolin, it is possible to obtain positive (direct and indirect) Coombs samples and a false-positive reaction of urine to glucose.

Interactions with other active ingredients

Trade names

Title	Value Index Vyshkovsky ®