Ceftriaxone: instructions for use in injections

What helps with ceftriaxone injections, indications and contraindications

The product may be in the form of a yellow or white powder. The components include ceftriaxone, which is classified as a cephalosporin. The medication can be used for intravenous administration; the container contains 0.25, 0.5, 1 and 2 g of the active ingredient. The product is considered a unique antibacterial drug; it is active against gram-positive and gram-negative substances.

The instructions indicate the following indications for the use of Ceftriaxone:

inflammatory processes in the peritoneum, angiocholitis, concentration of purulent processes in the area of the gallbladder,
respiratory diseases - bronchitis, abscess, pneumonia, pleurisy with accumulation of pus,
damage to bones, joints, soft tissues and skin, urination,
infection of damaged blood vessels,
sepsis, viral septicemia, meningitis,
syphilis, chancroid, tick-borne borreliosis,
salmonellosis, mild gonorrhea, typhoid fever.

The drug is used as a preventive measure to prevent the occurrence of re-infections after surgery, after treatment with weak immunity.

Ceftriaxone is contraindicated in patients:

with an allergy to the composition of the medication,
for prematurely born babies with hyperbilirubinemia,
liver or kidney failure,
enteritis, colitis.

The medicine is not used during pregnancy and breastfeeding.

How to dilute Ceftriaxone with Lidocaine and water

To dilute 1 g of Ceftriaxone with 2% Lidocaine and water you need:

Open an ampoule containing 2 ml of water for injection and draw the contents into a 5 ml syringe.
Open the ampoule with 2 ml of 2% Lidocaine and add the solution to the same syringe.
Remove the protective cap from Ceftriaxone and pierce the rubber cap with a needle.
Inject the entire contents of the syringe into the bottle.
Shake the mixture of antibiotic and solvent vigorously until the solution becomes completely clear (the needle and syringe do not detach).

Then you should fill the syringe with the entire solution or the required amount, change the needle and inject into the buttock muscle (upper outer quadrant). It is best to prepare Ceftriaxone with Lidocaine and water for one injection, but it happens that only half of the prepared solution is used. Then the remainder in the bottle is placed in the refrigerator.

Watch the video on how to dilute Ceftritaxone:

Side effect of Ceftriaxone injections

Unusual reactions of the body are reflected in:

eosinophilia, fever,
rashes on the skin, severe scabies,
clinical picture similar to urticaria and edema,
exudative erythema multiforme,
anaphylactic shock,
dizziness and pain in the head,
oliguria, flatulence, stomatitis,
gag reflex and nausea, glossitis,
dysbacteriosis, pseudomembranous enterocolitis,
leukocytosis, hematuria, unexpected nosebleeds.

Laboratory testing reveals a decrease in the number of white blood cells, lymphocytes, platelets, and so on. During injections, inflammatory processes on the internal surfaces of the vessel, pain, etc. can be noted.

The drug affects liver activity criteria and urea content. The drug can cause the development of hyperbilirubinemia and glucosuria. Intramuscular injections cause pain in the muscles, rashes on the skin, and dizziness.

Is it better to dilute Ceftriaxone with Novocaine or Lidocaine?

It is better to dilute Ceftriaxone with Lidocaine than Novocaine, this is explained by the properties of the second painkiller:

reduces the effectiveness of the antibiotic;
acts weaker;
Lidocaine more often causes allergic reactions, including the immediate type - angioedema.

If you are intolerant to Lidocaine and need to use intramuscular injections, the doctor may allow dilution of the antibiotic with 4 ml of a 0.5% solution of Novocaine.

In such cases, a preliminary test is required. It is carried out with 0.5 ml of a ready-made mixture of Ceftriaxone with an anesthetic. This amount is injected under the skin of the forearm and then the reaction is assessed hourly. Novocaine can also be used in the treatment of animals.

It is strictly forbidden to change the solvent yourself; it is especially dangerous to use solutions with calcium (for example, Ringer), as insoluble salts are formed. You cannot inject Ceftriaxone at the same time (in the same syringe) with other antibiotics.

Instructions for Ceftriaxone injections

Ceftriaxone injections, according to the instructions for use, adults are prescribed the following dosage:

for children over 12 years of age and adults – from 1 to 2 g per day, once or half the dose with an interval of 12 hours,
in the presence of severe disease - up to 4 g per day,
for the treatment of gonorrhea - intramuscular single injection of 250 mg of the drug,
for the purpose of prophylaxis before surgery - 1-2 g of the drug half an hour to three hours before surgery,
prescribed to children two weeks old - once a day, for each kg of weight from 20 to 50 mg.

For children weighing over 50 kg, a dosage similar to adults is recommended. Otherwise, the dose is calculated based on body weight - from 20 to 75 mg per kg per day.

The dosage, which requires the use of Ceftriaxone in large volumes (more than 50 mg), is prescribed in the form of a dropper. Treatment is carried out for half an hour or more. Therapy for viral meningitis begins with a dose of 100 mg per kg per day. Once the pathogen and its susceptibility to the antibiotic have been established, the treatment program can be revised downward.

The duration of treatment is interconnected with the type of pathogenic microflora and the distinctive features of symptoms. With gram-negative harmful substances, the effect can be achieved in four days, and in the case of combating enterobacteria - in 14 days.

The medication is diluted with a 1-2% mixture of Lidocaine or a special liquid for injections. Ceftriaxone instructions for use of injections : the last alternative is used for patients with an allergy to the anesthetic. In other situations, preference is given to mixtures containing Lidocaine or Novocaine due to painful injections and discomfort.

The antibiotic is produced exclusively for parenteral use, and the product is simply not available in the form of tablets and suspensions. The difficulty lies in the reaction of body tissues to the composition of the ingredients.

Ceftriaxone injections

How to dilute 2 lidocaine to 1 percent

Lidocaine is used to dilute the antibiotic Ceftriaxone at a concentration of 1%, but such a percentage of the solution is rarely available in pharmacies, so you can dilute 2% to 1%; for this, take 2 ml of water for injection for 2 ml of 2% Lidocaine.

The instructions for the drug indicate that the volume of the solvent should be 3.5 ml, and if you dilute a 2% solution, you will end up with 4 ml. This difference (0.5 ml) does not affect the treatment process in any way. A slightly larger volume is even better, since Ceftriaxone is quite difficult to dissolve.

Lidocaine Water for injections

Is it possible to inject without Lidocaine?

Ceftriaxone can be injected without Lidocaine in the following cases:

intolerance (allergy);
contraindications to painkillers: liver disease, circulatory failure, heart block, old age, pregnancy, lactation;
intravenous injections and drips (Lidocaine is prohibited as it can cause heart rhythm disturbances).

For dilution then only water for injection is used in an amount of 4 ml (2 ampoules). Antibiotic injections into the buttock without pain relief are very painful.

Ceftriaxone analogs

Replacement therapy is carried out using the following medications:

Ifitsef;
Loraxone;
Medakson;
Thorocef;
Hizon;
Cefaxon;
Cephogram;
Tsefson;
Ceftriabol.

The doctor replaces the medicine. Concomitant use of the drug with other antimicrobial agents is not permitted due to the risk of unexpected bleeding. A similar effect can be observed when combined with anticoagulants. Treatment with loop diuretics can cause kidney damage.

According to the instructions for use in adults, intramuscular ceftriaxone should be used with caution. Violation of the dosage can lead to a high degree of central nervous system excitation and a febrile state.

Where to store lidocaine for dilution

Lidocaine ampoules for dilution of 1% or 2% concentration are stored in a place protected from light at room temperature (from 15 to 25 degrees). Exactly the same conditions are needed for vials of Ceftriaxone and water for injection.

We recommend reading the article about the combined use of Azithromycin and Ceftriaxone. From it you will learn about which antibiotic is stronger, the compatibility of drugs, and for what diseases they can be combined. And here is more information about the rules for using Ciprofloxacin and Ceftriaxone.

Ceftriaxone should be diluted with a 1% lidocaine solution or diluted with a 2% solution of water for injection. This helps reduce the pain of injections in the buttock. For intravenous administration, only water or saline solution and glucose are used.

Pneumonia is one of the most common infections. Community-acquired pneumonia annually affects every sixth of 1000 inhabitants of the planet [1]. Nosocomial (nosocomial) pneumonia develops in 0.5–1.5% of hospitalized patients and in 10–30% of patients on mechanical ventilation [2]. In the USA, 300 thousand cases of nosocomial pneumonia are registered annually [3], in the UK – 50 thousand [4]. In Russia, the incidence of pneumonia is 396.7 per 100 thousand population [5]; in certain categories of patients it significantly exceeds the average. For example, among elderly people the incidence of community-acquired pneumonia reaches 44/1000, and among those living in organized groups – 68–114/1000 [6]. A high incidence of community-acquired pneumonia is also observed in population groups suffering from chronic diseases, especially cardiovascular diseases, chronic obstructive pulmonary disease, alcoholism, HIV infection and other immunodeficiency conditions, and malignant neoplasms.

In 1999, 747,390 cases of pneumonia were officially registered in Russia, of which 486,785 were in adults, 30,422 were in adolescents aged 15–17 years, and 230,183 were in children under 15 years of age [5]. However, according to experts, taking into account the large number of unreported cases and diagnostic errors, the actual number of episodes of the disease was 1,882,409 in adults, and 2,533,971 in the general population [5].

Pneumonia occupies one of the first places in the structure of mortality. In economically developed countries, they are in 4th–5th place among all causes of death after cardiovascular, oncological, cerebrovascular diseases, as well as chronic obstructive pulmonary disease, and in 1st place among the causes of death from infectious diseases [7, 8]. The mortality rate in patients with mild community-acquired pneumonia usually does not exceed 5%, but in severe cases of the disease it can reach 25–50% [9, 10]. A particularly high mortality rate is observed in patients over 60 years of age and young children, and, according to WHO, in Russia the mortality rate of children under 1 year of age (25.1 per 1000 population) is 2–4 times higher than that in other economically developed countries [ eleven]. Despite the success of chemotherapy, mortality from community-acquired pneumonia is increasing. Over the past 30 years it has increased from 1 to 9%. Mortality rates for nosocomial pneumonia range from 16 to 80% [10, 12–14].

Pneumonia results in significant direct and indirect medical costs. They cause temporary disability lasting an average of 25.6 days (12.8–45) [15]. Costs associated with community-acquired pneumonia reach $24 billion per year in the United States [16]. The annual cost of antimicrobial agents alone for outpatients with community-acquired pneumonia in the country is approximately $100 million [17]. Respiratory tract infections, primarily pneumonia, account for about half of the costs of antibiotics in hospital intensive care units [18]. At the same time, the cost of antibacterial drugs is only a small part of the cost of treatment as a whole. For example, in the USA, 92% of all costs for community-acquired pneumonia are the cost of hospitalization [19]. In case of nosocomial pneumonia, the main part of the financial costs is due to an increase in the patient's length of stay in the hospital, in general, and in the intensive care unit, in particular. For example, in a study conducted in China, the treatment costs of one patient with nosocomial infection were approximately 90% higher than those of a control patient [20]. Additional costs in case of development of nosocomial infection largely depended on its location and were maximum in pneumonia. The cost of treating nosocomial pneumonia was more than 4 times higher than the cost of treating nosocomial urinary tract infections (31,940 versus 17,349 yuan). The development of nosocomial infection was associated with an extension of hospitalization by an average of 25.53 days.

Similar findings were found in studies conducted in other countries. In the USA, the average lengthening of hospitalization due to nosocomial pneumonia was 7–30 days [21], in Germany – 24.17 [22]. Moreover, in the latter case, 14.03 days were spent in the intensive care unit, where the cost of treatment is significantly higher than in therapeutic departments.

Thus, adequate initial treatment of respiratory tract infections can prevent the development of conditions requiring hospitalization and complications of the disease, leading to a reduction in days of disability and disability, as well as a significant reduction in direct and indirect economic costs.

Monotherapy is indicated for most patients with pneumonia. Indications for prescribing combination antibacterial therapy include [23]:

pneumonia in the intensive care unit with a severe course due to an unknown pathogen, especially complicated by sepsis;
pneumonia against the background of severe immunodeficiency;
pneumonia caused by microbial associations beyond the spectrum of action of available antibacterial drugs;
pneumonia caused by weakly sensitive strains of microorganisms;
pneumonia caused by P. aeruginosa
.

When choosing a specific drug, the following factors must be taken into account [23]:

antimicrobial activity (bactericidal drugs have an advantage);
stability to beta-lactamases;
portability;
age-related changes in the pharmacokinetics of drugs (it is necessary to ensure good penetration of the drug into sputum and lung tissue);
ease of use for the patient (it is advisable that the frequency of administration does not exceed twice a day, otherwise the risk of non-compliance with the treatment regimen increases).

Unfortunately, many antibacterial agents widely used to treat pneumonia do not meet these requirements [23]. Thus, natural penicillins are not active against a number of potential pathogens of pneumonia (staphylococci, gram-negative bacteria), and in recent years the level of resistance of pneumococci to them has increased significantly. Aminopenicillins (ampicillin, amoxicillin) are destroyed by beta-lactamases. First generation cephalosporins (cephalothin, cefazolin, cephalexin) are not active against most gram-negative pneumonia pathogens and are destroyed by beta-lactamases of gram-negative bacteria. Aminoglycosides penetrate poorly into the lung tissue and are characterized by high toxicity. Their activity decreases during purulent processes. Tetracyclines have a bacteriostatic effect, are potentially toxic and are poorly tolerated by patients. Sulfonamides are also bacteriostatic and have an unfavorable side effect profile. In addition, high levels of pathogen resistance to sulfonamides, including co-trimoxazole, are now widely observed.

Antibiotics that best meet the above requirements include third-generation cephalosporins, primarily ceftriaxone. Third-generation cephalosporins began to attract special attention in the era of the spread of an “epidemic” of antibiotic resistance in the world of one of the main causative agents of respiratory infections – Streptococcus pneumoniae

, which causes 15–35% of community-acquired pneumonia and 10–20% of nosocomial pneumonia [24].
Penicillin-resistant strains of S. pneumoniae, the prevalence of which in some regions has reached 80% or more [25], in most cases remain sensitive to cefotaxime and ceftriaxone [26, 27]. In addition, these drugs are active against other common pathogens of lower respiratory tract infections - Haemophilus influenzae, Moraxella catarralis
and methicillin-sensitive staphylococci.

One of the ceftriaxone preparations presented on the domestic pharmaceutical market is Novosef (Eczacibashi Pharmaceuticals, Turkey), which is available in bottles of 0.5 and 1 g for intramuscular and intravenous administration of each dosage.

Ceftriaxone differs from cefotaxime, another third-generation cephalosporin, by more favorable pharmacokinetic properties:

long half-life, allowing it to be administered once a day, dose-dependent binding to plasma proteins;
almost complete bioavailability when administered intramuscularly;
very good tissue penetration (including through the blood-brain barrier);
dual path of excretion, and therefore dose adjustment is required only in patients with simultaneous renal and hepatic insufficiency [28, 29].

Ceftriaxone is widely distributed throughout the body, reaching high concentrations in organs and tissues. For more than a day after administration, its concentrations far exceed the minimum inhibitory (MIC) for most sensitive microorganisms in more than 60 tissues and fluids, including the lungs and pleural fluid [30].

A wide spectrum of antibacterial activity, favorable pharmacokinetic properties, good tolerability and ease of use of ceftriaxone have made it, despite the parenteral route of administration, one of the most widely used antibiotics for the treatment of respiratory tract infections not only in hospitalized but also outpatients. In some countries, such as Italy, ceftriaxone is one of the most widely used antibiotics [31].

Ceftriaxone is highly effective against community-acquired pneumonia. In the recommendations of the All-Russian Society of Pulmonologists for the treatment of community-acquired pneumonia, it is considered as the drug of choice in hospitalized patients with both mild and severe cases of this disease [32]. In the latter case, ceftriaxone is recommended to be combined with macrolides. The place given to ceftriaxone in the treatment of community-acquired pneumonia in Russia is presented in Tables 1–3.

A significant place is given to third-generation cephalosporins, in particular ceftriaxone, in the updated version of the recommendations for the management of community-acquired pneumonia of the Infectious Diseases Society of America (IDSA), published in 2003 [34]. In combination with modern macrolides, it is recommended for patients hospitalized in the general ward, as well as for patients hospitalized in the intensive care unit, if they do not have risk factors for infection with P. aeruginosa

If the etiology of the disease is established, ceftriaxone is the drug of choice for infection caused by Escherichia coli

,
Haemophilus influenzae
, penicillin-resistant
S. pneumoniae
and strains of Klebsiella pneumoniae that do not produce extended-spectrum beta-lactamases [23].

In a number of countries (USA, Canada, Italy, etc.), ceftriaxone is widely used at home in the treatment of patients with severe pneumonia [35, 36]. This allows for excellent clinical results and high patient and physician satisfaction [35]. In addition, due to its ease of use, ceftriaxone is the drug of choice for the treatment of pneumonia in outpatients who, for whatever reason, cannot take antibiotics orally [32].

The effectiveness of ceftriaxone (as monotherapy or combination with other antibiotics) for community-acquired pneumonia of varying severity in adult patients and children has been shown in foreign and domestic clinical studies [35–42]. According to the results of an analysis of literature data on the use of ceftriaxone for lower respiratory tract infections (515 patients with pneumonia and 312 with other infections), published in 1987, the clinical effectiveness of the drug was 96%, bacteriological - 88% [43]. Side effects were observed in 4.6% of patients.

In another retrospective study of 1032 patients aged 16–100 years (mean age 71.9 years) with lower respiratory tract infections, ceftriaxone was the most effective (85.4%) of all antibiotics used [44]. The high efficacy and good tolerability of ceftriaxone in serious, difficult-to-treat community-acquired infections, including pneumonia, meningitis and acute otitis media (including those caused by strains with reduced sensitivity to beta-lactam antibiotics), was confirmed by the results of a recent analysis of randomized clinical trials. research [45].

Ceftriaxone is also widely used for the treatment of nosocomial pneumonia. Experts from the Commission on Antibiotic Policy under the Ministry of Health of Russia and the Russian Academy of Medical Sciences recommend its empirical prescription for pneumonia that developed in general departments in patients without risk factors (i.e., without previous antibiotic therapy or prophylaxis), and for “early” ventilator-associated pneumonia that occurred in patients in intensive care units [46].

The use of ceftriaxone may be limited by two factors: its relatively high price and the risk of the emergence and spread of antibiotic-resistant microorganisms. As for price, firstly, as mentioned above, the cost of an antibiotic for many respiratory tract infections is only a small part of the total cost of treatment. Secondly, the cost of parenteral drug therapy consists of the cost of a course dose of an antibiotic and the so-called “hidden” costs associated with its preparation and administration (solvents, syringes, needles, infusion systems, consumables, etc.), as well as the cost working hours of medical personnel.

A number of foreign pharmacoeconomic studies have shown that the costs associated with the preparation and administration of the drug can be equal to the cost of the drug itself or even exceed it [47]. The share of “hidden” costs in the total cost of treatment decreases with decreasing frequency of drug administration and is minimal with one injection per day [47]. In comparative pharmacoeconomic studies, the “hidden” costs of a single dose of ceftriaxone were 17–52% lower than those of short-acting antibiotics intended for 3–6 doses [48]. As a result, the cost of a course of treatment with ceftriaxone may be lower than the cost of a course of treatment with cheaper antibiotics - cefazolin, cefuroxime and cefotaxime [48, 49].

The higher clinical and/or cost effectiveness of ceftriaxone in patients with lower respiratory tract infections compared to second generation cephalosporins and cefotaxime has been shown in a number of foreign studies [50–53]. A study conducted in 9 therapeutic departments of Northern and Central Italy demonstrated that the use of ceftriaxone in patients with pneumonia and bronchopneumonia saves the hospital 15.18% of financial resources compared to the use of other third-generation cephalosporins and 14.76% compared to the use of broad-spectrum penicillins [53].

A Russian pharmacoeconomic study in elderly and senile patients with community-acquired pneumonia revealed an advantage of the ceftriaxone–amoxicillin/clavulanate regimen over a number of other antibiotics [42]. In moderate cases of the disease, this regimen was superior in cost effectiveness (cost-effectiveness ratio 42.3) to ampicillin (63.9, p

In patients with severe pneumonia, a Russian pharmacoeconomic analysis also confirmed the justification of using the ceftriaxone–amoxicillin/clavulanonate regimen, especially considering its high clinical efficacy (84.2%) and safety [42].

The cost of ceftriaxone treatment can be reduced by step therapy. A number of studies in adults and children with lower respiratory tract infections have shown the effectiveness of stepwise therapy, in which ceftriaxone was used at the first stage, and when the condition normalized, they switched to an oral cephalosporin - ceftibuten, cefpodoxime proxetil, cefetameta pivoxil [54–56]. Not inferior in clinical effectiveness to parenteral therapy, stepwise therapy made it possible to reduce the length of hospital stay and reduce treatment costs. For example, in one study, step therapy resulted in savings per patient of US$46.05 [55].

The use of ceftriaxone in severely ill patients on an outpatient basis reduces treatment costs by an average of 68–78% [57]. Interestingly, in Italy, where the practice of home treatment of various infections requiring parenteral antibiotic administration is widespread, and where ceftriaxone is used per capita much more often than in other countries, the level of bacterial resistance is lower than in the United States and most European countries [58].

Thus, during the 20 years that ceftriaxone has been on the global pharmaceutical market, its importance in the treatment of pneumonia not only does not decrease, but, on the contrary, increases.

Special instructions for the use of the drug Ceftriaxone

Use with extreme caution in patients with hypersensitivity to penicillins due to a possible cross-allergic reaction. If antibiotic use causes diarrhea, pseudomembranous colitis should be excluded; otherwise, ceftriaxone should be discontinued and appropriate treatment administered. With long-term treatment, the development of superinfection caused by microorganisms insensitive to ceftriaxone is possible. Echopositive precipitates of ceftriaxone calcium in the gallbladder disappear after the end of antibiotic therapy. The use of ceftriaxone in newborns, infants and young children is effective and safe when the recommended dosage regimens are followed. Ceftriaxone, like some other cephalosporins, can displace bilirubin from binding to plasma albumin, so it should be used with caution in newborns with hyperbilirubinemia. Ceftriaxone should not be used in newborns (especially premature infants) who are at risk of developing bilirubin encephalopathy. Ceftriaxone penetrates the placental barrier. The safety of its use during pregnancy has not been established. Caution is required when using it during breastfeeding. In patients taking ceftriaxone, the Coombs test may be false positive. During treatment, false positive results of the galactosemic test and non-enzymatic methods for determining glucose in urine are possible.

In what cases is hypertonic sodium chloride solution used?

A hypertonic solution is a concentrated sodium chloride solution that contains more salts than an isotonic solution. It is used for several indications. A hypertonic solution has a direct effect on the fluids in the body. It draws water out of cells. Therefore, it is prescribed to patients with cerebral edema. In addition, the solution helps increase blood pressure during blood loss.

It is often used to treat wounds - salt is a natural antiseptic. Patients with arthritis make compresses that relieve pain, reduce inflammation and swelling. For diseases of the oral cavity, it is recommended to rinse with a hypertonic solution, and for sinusitis, rinse the nose with it.