Pharmacodynamics and pharmacokinetics
The pharmacological effect of the drug is based on blocking the biosynthesis of microbial cell walls. The antibiotic Cefazolin is active against gram-positive (Streptococcus spp., Staphylococcus spp.) and gram-negative bacteria (Klebsiella spp., Escherichia coli, Treponema spp., Haemophilus influenzae, Proteus mirabilis, Neisseria gonorrhoeae, Enterobacter aerogenes).
The drug is poorly absorbed from the gastrointestinal tract when used internally, therefore it is used for intravenous and intramuscular injections . After intramuscular injections at a dosage of 0.5 g, the maximum concentration is observed after 1-2 hours. Plasma protein binding is approximately 85%.
The active substance of the drug penetrates bone tissue, as well as pleural , ascitic and synovial fluid , but is not detected in the nervous system.
The half-life of the drug is approximately 1.8 hours. The drug is excreted unchanged in the urine.
With intramuscular injections, about 80% of the dose is eliminated after 24 hours. In case of renal dysfunction, the plasma half-life increases.
pharmachologic effect
First generation cephalosporin antibiotic for parenteral use. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. It has a wide spectrum of action, is active against gram-positive (Staphylococcus spp., Staphylococcus aureus (non-producing and producing penicillinase; including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis) and gram-negative (Neisseria meningitidis, Neisseria gonorrhoeae, Shigella spp., Salmonella spp ., Escherichia coli, Klebsiella spp., Treponema spp., Leptospira spp.) microorganisms.
Active against Haemophilus influenzae, some strains of Enterobacter and Enterococcus.
Ineffective against Pseudomonas aeruginosa, indole-positive strains of Proteus spp., Mycobacterium tuberculosis, Serratia spp., anaerobic microorganisms, methicillin-resistant strains of Staphylococcus spp.
Indications for use of Cefazolin
Indications for use of Cefazolin are as follows:
- infections of the biliary and urinary tract ;
- infectious diseases of the respiratory tract;
- inflammation in the abdominal cavity and pelvic organs;
- blood poisoning;
- peritonitis and sepsis ;
- skin infections after burns, surgeries and wounds;
- inflammation of the lining of the heart;
- and joint infections ;
- venereal diseases;
- infectious skin diseases;
- mastitis.
For what purpose the drug will be effective in each individual case, it is necessary to consult a specialist. Only a doctor knows the exact indications for the use of Cefazolin. For example, he may recommend a drug for sore throat , skin infections , or blood poisoning .
The medicine is also used in veterinary practice for cats. Injections help with blood poisoning , peritonitis , meningitis , as well as many infectious diseases .
special instructions
Patients with a history of allergic reactions to penicillins or carbapenems may have increased sensitivity to cephalosporin antibiotics.
During treatment with cefazolin, it is possible to obtain positive direct and indirect Coombs tests, as well as a false positive urine reaction to sugar.
When prescribing the drug, exacerbation of diseases of the gastrointestinal tract, especially colitis, is possible.
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Side effects
Using the medication may cause the following side effects:
- organs of the digestive system: diarrhea , nausea, vomiting;
- chemotherapeutic effect: candidiasis , pseudomembranous colitis ;
- allergies : urticaria , eosinophilia , itching , fever ;
- local reactions: pain at the site of intramuscular injection.
In rare cases, there is a transient increase in the activity of liver transaminases , anaphylactic shock , arthralgia , angioedema , leukopenia (reversible), thrombocytopenia , neutropenia , renal dysfunction .
Side effects of the drug
Cefazolin injections cause a local painful reaction: a strong burning sensation at the injection sites that lasts for several minutes. This effect does not require discontinuation of the drug. Other side effects:
- dyspepsia: nausea, stomach cramps, loss of appetite;
- stool disorder;
- fungal infections of the skin and mucous membranes;
- changes in blood count: thrombocytopenia, leukopenia, increased liver transaminases;
- aching pain in the joints.
If you are allergic to the drug, in rare cases, Quincke's edema develops, skin itching, fever, and urticaria are possible. In case of overdose, cardiotoxic shock, arrhythmia, and vomiting develop.
Instructions for the use of Cefazolin injections (Method and dosage)
When Cefazolin injections are prescribed, the instructions for use indicate that the dosage and duration of the course may vary depending on the disease and the individual sensitivity of the patients. Daily dosage for adults is from 1 to 6 g. Injections are given 2-3 times daily. Therapy is designed for a maximum of 7-10 days.
The drug is administered intramuscularly or intravenously . Depending on this, they decide how to dilute Cefazolin. When intramuscularly , the medicine is diluted with water or sodium chloride solution. For intravenous injections, sodium chloride is mainly used. In this case, the drug is administered slowly. Administration time is approximately 5 minutes.
If a patient is placed on a drip , the antibiotic is usually diluted with glucose, and sodium chloride is used only in rare cases.
For the treatment of inflammation of the lining of the heart, joints, purulent pleurisy , bones, abdominal cavity, blood poisoning , 1 g of the drug is administered 3 times every day. In case of kidney dysfunction, the dosage should be halved.
The drug cannot be combined in the same syringe with other antibiotics .
In addition to water and sodium chloride, the medicine is also sometimes diluted with Novocaine . It is topical anesthetic This drug has been used in medical practice for quite a long time, so there is an established scheme for diluting Cefazolin with Novocaine . The latter is taken at a concentration of 0.25%. Before diluting this drug with Novocaine It is enough just to add 2-3 ml to the antibiotic and then shake well. The result is a ready-made solution for single use.
For some indications, the drug is also used in veterinary practice instead of using tablets. In this case, it is diluted in Lidocaine or Novocaine . The dosage for cats depends on the weight of the pet, it is calculated so that 10 mg is per 1 kg. Therapy lasts 5-10 days. Before using the medicine, you should consult your veterinarian.
Cefazolin Akos is often used as an analogue of the drug for humans . It is also administered through intramuscular and intravenous injections (stream and drip). Instructions for use of Cefazolin Akos reports that the average daily dosage for adults is 1 g. They need to be administered 2 times a day. The maximum dose per day should not exceed 6 g. If necessary, the frequency of use can be increased to 3-4 times a day. The average duration of therapy is 7-10 days.
The average daily dosage for children is 25-30 mg/kg, and in case of severe infections - 100 mg/kg.
In case of renal dysfunction, doses are adjusted.
For intramuscular injections, an antibiotic in a dose of 500 mg is mixed with 2 ml of water, 1 g is diluted in 2.5 ml of water. For intravenous administration, the medicine is mixed with 5 ml of water and administered for 3-5 minutes.
Cefazolin 1g For Injection
Cefazolin 1g for injection
Active ingredient: Cefazolin Dosage form : Powder Pharmacotherapeutic group: Antibiotics of the cephalosporin group. Composition Active ingredient: Cefazolin 1 bottle contains cefazolin sodium in terms of cefazolin 1 g. Dosage form. Powder for injection. Pharmacotherapeutic group Antibacterial agents for systemic use. First generation cephalosporins. Cefazolin. ATC code J01D B04. Indications of infection of the ENT organs and lower respiratory tract; biliary tract infections; genitourinary tract infections, including prostatitis, epididymitis; gynecological infections; skin and soft tissue infections; infectious lesions of bones and joints; eye tissue infections; peritonitis; septicemia; bacterial endocarditis; prevention in the pre- and postoperative period in order to reduce the risk of postoperative infections during transvaginal hysterectomy and cholecystectomy, as well as during abdominal surgical interventions (for example, open-heart surgery or joint replacement). Contraindications Hypersensitivity to drugs of the cephalosporin group and other beta-lactam antibiotics. Children up to 1 month of age (efficacy and safety of use have not been established). Kidney failure. Intestinal diseases (including a history of colitis). Before starting use, a skin test is performed to determine the tolerability of the drug and lidocaine. Method of administration and dosage The drug is used for adults and children over 1 month of age. Prescribed intramuscularly or intravenously, depending on the type and severity of the disease and kidney function. The drug is administered intravenously either slowly (over 3-5 minutes) or as an intravenous infusion. The drug in a dose of 1 g is administered mainly intravenously. After the symptoms of the disease or signs of a bacterial infection disappear, treatment with the drug should be continued for at least 48-72 hours. For infections caused by beta-hemolytic streptococci, the duration of treatment is at least 10 days.
Adverse reactions Allergic reactions: skin rash, itching, eosinophilia, Quincke's edema, arthralgia, anaphylactic shock. In these cases, it is necessary to stop administering the drug and carry out desensitizing therapy. In patients with kidney disease, when treated with increased doses of cefazolin (about 6 g), signs of renal failure may appear. In these cases, the dose of the drug is reduced and treatment is carried out under the control of the dynamics of urea nitrogen and creatinine in the blood. A transient increase in blood urea nitrogen levels may occur without clinical symptoms of renal dysfunction. From the digestive system: nausea, vomiting, anorexia, diarrhea, pseudomembranous colitis, transient increase in the activity of liver transaminases and alkaline phosphatase, transient hepatitis, cholestatic jaundice. With long-term treatment, dysbiosis, superinfection caused by antibiotic-resistant strains, and candidiasis may develop. When administering the drug intramuscularly, in rare cases, phlebitis and pain at the injection site are observed. Anal-genital itching, genital candidiasis and vaginitis may occur. From the hematopoietic system: neutropenia, leukopenia, thrombocytopenia. Overdose Symptoms. Neurotoxic phenomena: dizziness, paresthesia, headache, tachycardia, increased convulsive readiness, clonic-tonic seizures, vomiting (especially in patients with renal failure due to the possibility of drug accumulation). Treatment. You should stop administering the drug and take anticonvulsant measures, if necessary. Therapy is symptomatic; there is no specific antidote. Hemodialysis may be used. Peritoneal dialysis is not effective in this case. Use during pregnancy or breastfeeding During pregnancy, it is prescribed only for health reasons (adequate and strictly controlled studies have not been conducted). If it is necessary to use the drug during lactation, stop breastfeeding (cefazolin passes into breast milk). Children There is no experience of use in children under 1 month. Features of use The drug should be used with caution in patients who have established hypersensitivity to penicillins, due to proven partial cross-allergenicity between penicillin and cephalosporin antibiotics. There is evidence of severe anaphylactic reactions with fatal outcomes with the simultaneous administration of antibiotics of both groups. If severe anaphylactic reactions develop, the drug is discontinued and emergency therapeutic measures are taken. As with the use of most antibacterial drugs, pseudomembranous colitis may develop from mild forms to life-threatening conditions. Therefore, it is necessary to correctly assess the cause of diarrhea during treatment with the drug, conduct additional tests to confirm the diagnosis and prescribe treatment. The drug is not recommended to be administered intrathecally, as this may cause severe toxic reactions from the central nervous system, including seizures. In patients with reduced renal function, it is necessary to select an individual dosage and intervals between administrations of cefazolin, depending on the severity of functional renal impairment. In case of unstable renal function, constant monitoring of the level of the drug in the blood serum is necessary to ensure the safety of the drug. False-positive results from laboratory tests for sugar in urine may occur if they are performed using Benedict's solution, Fehling's solution or Clinitest® tablets. At the same time, the drug does not affect the results of tests for sugar content in urine produced using enzymatic methods. In addition, false-positive direct and indirect Coombs test results may occur, for example, in infants whose mothers were treated with cefazolin.
Pharmaceutical characteristics: basic physical and chemical properties: white or white powder with a yellowish tint. Incompatibility Lidocaine cannot be used to prepare a solution for intravenous administration (stream or drip). Shelf life: 3 years. Storage conditions Store at a temperature not exceeding 25 ° C in a dry place, protected from light. Keep out of the reach of children. The shelf life of a freshly prepared solution is 24 hours at a temperature of 15-30 ° C and 96 hours when stored in the refrigerator (2-8 ° C). A solution of the drug in water for injection, in 0.9% sodium chloride solution or in 5% glucose solution, if frozen immediately after preparation, is stored for 12 weeks if stored in the freezer at a temperature below -20 ° C. Thaw the drug for use without heating. Do not refreeze! Packaging 1g per bottle, No. 50 per cardboard box. Vacation category Prescription
Overdose
Administration of the drug in high doses may cause dizziness , headache and paresthesia . People with chronic kidney failure neurotoxic effects . Convulsions, tachycardia and vomiting are noted.
In case of toxic reactions and signs of overdose, the elimination of the drug can be accelerated through the use of hemodialysis .
Contraindications
Hypersensitivity, neonatal period (up to 1 month).
With caution:
Renal failure, intestinal diseases (including a history of colitis), children under 1 year of age.
Use during pregnancy and lactation:
During pregnancy, it is prescribed only for health reasons (no strictly controlled studies have been conducted).
FDA category of effect on the fetus is B.
If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped (cefazolin passes into breast milk).
Interaction
When the drug is combined with aminoglycosides , Rifampicin , Vancomycin , a synergistic antimicrobial effect is observed . Aminoglycosides increase the likelihood of kidney damage. The drug is incompatible with them.
It is undesirable to combine the medication with anticoagulants and diuretics .
Interaction with agents that inhibit tubular secretion increases the level of the active substance of the drug in the blood, increases the likelihood of toxic reactions and slows down the elimination time.
Analogues of Cefazolin
Level 4 ATC code matches:
Cephalexin
The following analogues of Cefazolin are known:
- Cefazex;
- Cefazolin-Astrapharm;
- Cefazolin Acos;
- Reflin;
- Cesolin;
- Cefazolin-Pharmex;
- Cefamezine.
All of these medications are sold in powder form. Common analogues are not available in tablets.
Cefazolin price, where to buy
The price of Cefazolin injections can vary greatly depending on the seller. Ampoules of medicine (1 g) can cost from 20 rubles. The maximum price of Cefazolin for 1 bottle of 1 g reaches 120 rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Cefazolin-AKOS por.
d/prig. solution for intravenous and intramuscular injection. 1g 50pcs Sintez AKO OJSC RUR 892 order
Pharmacy Dialogue
- Cefazolin (vial 1g i.v. i.m. individual pack) Biosynthesis OJSC
42 RUR order
- Cefazolin (vial 1g intravenous i.m. individual pack) Kraspharma OJSC
38 rub. order
- Cefazolin (vial 1g IM, IV) Lecco JSC
28 RUR order
- Cefazolin-Akos (vial 1g i.v. i.m. individual pack) Synthesis OJSC
31 rub. order
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Pharmacy24
- Cefazolin-Darnitsa 1g N5 PrAT Pharmaceutical company Darnitsa, Ukraine
73 UAH order - Cefazolin-Darnitsa 0.5 g No. 5 powder PrAT” Pharmaceutical company “Darnitsa”, Ukraine
55 UAH order
- Cefazolin 0.5 g N10 powder PAT "Kievmedpreparat", Ukraine
94 UAH order
- Cefazolin 1 g N5 solution for injection AT Lekhim-Kharkiv, Ukraine
55 UAH order
- Cefazolin 1 g No. 1 injection solution AT "Lekhim-Kharkiv", Ukraine
12 UAH order
PaniPharmacy
- Cefazolin bottle Cefazolin powder for injection 0.5g bottles No. 5 Ukraine, Darnitsa ChAO
60 UAH.order
- Cefazolin por. d/in 1g No. 5 Ukraine, Lekhim-Kharkov
71 UAH order
- Cefazolin bottle Cefazolin pores. d/r-ra d/in. 1g fl. No. 10 Ukraine, Kievmedpreparat OJSC
124 UAH order
- Cefazolin bottle Cefazolin pores. d/r-ra d/in. 0.5g fl. No. 10 Ukraine, Kievmedpreparat OJSC
93 UAH order
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