Antibiotic ceftriaxone tablets

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Selection of ceftriaxone analogues in various release forms

Ceftriaxone is an antibiotic widely used throughout the world and belongs to the group of cephalosporin drugs. This drug is used only for parenteral administration and does not have a tablet form.

Table of contents:

The principle of action of the substance is to block the production of murein, which leads to the death and destruction of harmful microorganisms.

Ceftriaxone: analogues in tablets

Since this drug can only be introduced into the body through the blood, the relevant question is: what can replace ceftriaxone?

For oral use only drugs are used: Cephalexin, Cefadroxil, Cefaclor, Cefuroxime-acetyl, Cefditoren, Cefixime, Ceftibuten (Cedex), Cefpodoxime.

Nowadays, large pharmaceutical companies produce many substitutes for ceftriaxone in oral form: Pancef, Zinnat, Vertsef, Suprax, Cefspan.

Ceftriaxone: analogues in injections

If it is necessary to achieve an effective result in the fastest way, drugs analogous to ceftriaxone are used in the form of injections.

When prescribing treatment, it is important to remember that cephalosporin drugs are time-dependent antibacterial agents and repeated injections of the drug throughout the day are necessary to maintain the effective concentration of the active substance in the blood.

Analogues of ceftriaxone include Torocef, Cefazolin.

Analogues are used in the same cases as the original antibiotic. They have similar indications, contraindications for use and side effects. If the drug is administered intramuscularly, the active substance quickly reaches a high level in the blood due to good absorption. The highest concentration is achieved after 3 hours. When administered parenterally, the bioavailability of ceftriaxone analogues reaches maximum limits.

The conditions for preparing solutions and the indications for analogue drugs are the same as for ceftriaxone. They must be introduced immediately after preparation so that the solution does not have time to oxidize.

Moreover, the color of the solutions varies from pale yellow to yellow-orange and depends on the concentration of the active substance, as well as the duration of storage of the freshly prepared medicine. The color of the drug solutions does not affect the body's tolerance of this drug.

Ceftriaxone substitutes are much more expensive in price than the original.

Cefazolin

Cefazolin is a 1st generation cephalosporin that has a pronounced antimicrobial effect on the human body. It is a powder for intramuscular and intravenous use.

When administered parenterally, the substance is actively absorbed into the internal environment of the body. The half-life is about 10 hours (which is caused by the binding of 9/10 of the active substance to plasma proteins). Cefazolin is successfully used for the treatment of infectious processes of the urinary tract, as well as the reproductive system (syphilis, gonorrhea, prostatitis, cystitis, pyelonephritis, urethritis).

Since ceftriaxone is excreted not only in the urine, but also in the bile, in case of impaired renal function (with a healthy liver), there is no need to change the daily dose, while cefazolin requires a dosage reduction in patients with impaired renal function or liver disease.

But the cost of this analogue is % higher than that of ceftriaxone (the price of a bottle of ceftriaxone 1 g, N1 IV, IM reaches about 30 rubles, the cost of cefazolinrub.).

Ceftriaxone: analogues in suspension

Suspensions are liquid forms of a medicinal substance in which solid particles do not completely sediment, but float in the liquid as a suspension. Such substances can be used by both adults and children.

Important: the presence of allergic reactions, diseases of the liver, kidneys, biliary tract, taking medications for other concomitant pathologies and recent use of antibiotics must be reported to your doctor.

Taking antibiotics such as Ixim Lupine, Cedex, Pancef and others (based on cephalosporin components) in the form of a suspension often causes side effects. For example, nausea, abdominal pain, diarrhea, headache and dizziness, vomiting. In general, these effects are moderate and disappear when you stop taking the antibiotic. Using Cedex as an example, let us consider the properties of ceftriaxone analogues in suspension.

Tsedex is applicable for children from 6 months. Dosage – 9 mg of antibiotic per kg of child’s weight.

This drug is prescribed for:

  • urinary system infections;
  • respiratory tract diseases (sinusitis, bronchitis, pneumonia, scarlet fever, tonsillitis);
  • bacterial otitis, gastroenteritis and enteritis.

The price of drugs in this category is significantly higher than the cost of the original. So, in Russian pharmacies you can buy Ixim Lupine (0.4, N1) rub., Tsedex - rub., Panzef - rub. This significantly exceeds the cost of the original product, but it works much more carefully and efficiently.

Rocephin or ceftriaxone: which is better?

Rocephin is an antibiotic of Swiss origin, the active substance of which is ceftriaxonadinodium salt. It is produced in the form of a high concentration powder and is used parenterally. On sale (medicinal types used for intramuscular administration) come together with a solvent - lidocaine 1%. Although the drug must be used in the same way as ceftriaxone, Rocephin has a number of important differences:

  1. No pain after using the drug (ceftriaxone injection causes pain that lasts for several minutes).
  2. There is no need to purchase additional solvent.
  3. The quality and level of purification of the drug from Switzerland is much higher than that of ceftriaxone.
  4. The side effects are the same as those of domestically produced ceftriaxone.

The cost of rocephin is an order of magnitude higher than the price of ceftriaxone (which is explained by the higher quality of the imported product). It is hardly possible to purchase a Swiss drug for less than rubles, while the most budget-friendly versions of ceftriaxone can be purchased for less than 30 rubles (1 g bottle, N1).

Azaran or ceftriaxone: which is better?

The drug from Serbia Azaran is based on the active substance Ceftriaxone. This is due to the similarity of contraindications to the use of this antibiotic.

Since the fundamental part of both drugs is the same substance, the effect of the drug on the human body is absolutely similar.

The differences lie in the level of purification and the cost of the product (for example, Ceftriaxone can be bought for about 30 rubles (1 g, N1), while for a similar package of Azaran you need to spend at least 250 rubles).

An imported product is more reliable and is made from a pure product, which cannot be said about the domestic one. The choice of drug is a purely personal matter for everyone, but you should proceed from the desired result and resources: if you plan to use a high-quality and expensive product with a high level of purification and you have the opportunity to pay for the entire course of treatment, Azaran is preferable. If consumers are interested in a budget option, in which the main goal is recovery with minimal financial costs, they can use ceftriaxone (which is not much inferior to its foreign analogue).

Ceftriaxone analogues for children

It is administered both intramuscularly (IM) and intravenously (IV). The doctor must determine the daily norm individually for each child (based on the child’s weight, age and illness). Typically, the dose is set based on the ratio according to which there are mg of the active component per kg of weight.

In such cases, the antibiotic is administered parenterally. Almost always, the doctor can choose an oral analogue of the “painful” injection (ceftriaxone). The main active ingredients in this drug are Cefixime (Ixim Lupine, Suprax) and Ceftibuten (Cedex).

If we look at the price range, drugs based on cefixime are cheaper. So, for example, the price of Suprax reaches ., the price of Cedex (the active component of which is Ceftibuten) reaches .

A little about generics

Generics are more affordable substitutes (copies) of expensive tablets that operate on the same principle as the originals.

For ceftriaxone, along with synonyms, there are many generics. Sometimes such analogues, made on the basis of the original, are even better suited. Generics (analogues) of ceftriaxone have multicomponents, based on various types of active substance:

Antibiotics, the main active substance of which is ceftazidime, are used for severe infectious diseases (meningitis, osteomyelitis, sepsis, pneumonia, kidney abscess, bacterial urethritis, pyelonephritis, prostatitis). Also, these drugs are widely used for diseases of the pelvis, gastrointestinal tract and ear infections, diseases of the skin and soft tissues. An antibiotic is used even for newborns, but during pregnancy additional consultation with a specialist is necessary (there are many risks).

Medicines such as Bacperazone, Sulcef are based on two active components: Cefeperazone and Sulbactam. The second of them is not an active antibacterial agent, but its benefit lies in stimulating the effect of the antibiotic on sensitive strains of microorganisms. These drugs have a wide range of effects on the body (in particular, they eliminate some harmful bacterial cells that are not affected by ceftriaxone).

Third generation substitutes for this drug, due to their enhancement with inhibitors (beta-lactamase), are active against many pathogenic bacteria. But the drugs must be used carefully, since the unreasonable use of these drugs can have a detrimental effect on health.

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Ceftriaxone - instructions, list of cheaper analogues

Antibiotics are available to fight infections. They belong to different groups, and have their own characteristics in terms of their potency. In our article we will talk about a third-generation antibacterial drug, which belongs to the clinical-pharmacological group of cephalosporins, it is called “Ceftriaxone”.

In addition to the main characteristics of ceftriaxone, we will consider analogues, highlight which of them are cheaper, and determine by what parameters they replace ceftriaxone.

Ceftriaxone - instructions

To find analogues for ceftriaxone, you first need to find out how the drug “works” and what is its peculiarity.

How does ceftriaxone work?

The spectrum of action of ceftriaxone is impeccable. This antibacterial agent comes into play when many antibiotics cannot help, or the bacterial process is already at a stage at which there is a high probability of complications.

The drug has excellent resistance to beta-lactamases, so the therapeutic effect always occurs very quickly.

Research data have shown that some bacteria still resist ceftriaxone, these include methicillin-resistant staphylococci, enterococci, and group D streptococci.

Composition, release form and price

The active substance is ceftriaxone (in the form of sodium salt). The drug is presented as an injection powder, which is in hermetically sealed bottles. Bottles of 500 mg, 1 and 2 grams are available. The price for one bottle of ceftriaxone (Russia) is 20, 25 and 27 rubles, respectively.

There is also ceftriaxone on the market from manufacturers in India, Portugal, Ukraine, and China. Their prices need to be clarified.

Indications

Ceftriaxone successfully cures the following pathologies, provided the bacteria are sensitive to it:

Contraindications and side effects

The main contraindication is individual immunity to the composition, as well as hypersensitivity to drugs from the group of penicillins, cephalosporins and carbapenems. The first trimester of pregnancy also prohibits ceftriaxone.

  • Relative contraindications include severe liver and kidney diseases, hyperbilirubinemia in newborns and premature babies.
  • Among the “side effects” are allergic reactions on the skin, candidiasis, serum sickness, bronchospasm, anaphylactic shock, and impaired liver function.
  • There are also problems with the digestive, urinary and hematopoietic systems. Very rarely, nosebleeds and dizziness occur.

Ceftriaxone injections are painful, so it is recommended to dilute it with lidocaine. But despite this, very often the injection site bothers the patient. A slight infiltrate and pain appear. Some patients cannot tolerate intramuscular ceftriaxone injections at all due to pain. In such cases, it is administered intravenously.

Dosages

The drug is dosed based on the patient’s age, the severity of the disease and the pathology itself.

The average dosage for adults is as follows: the drug is administered intramuscularly or intravenously once a day, 1–2 grams. If necessary, the dose is increased to 4 grams, then the drug is administered every 12 hours. The duration of therapy is determined only by the treating doctor.

If ceftriaxone is not suitable for the patient, then analogues are selected, and they can be not only in injection form, but also tablets, syrup, or suspension.

Are there any analogues for ceftriaxone?

Let’s say ceftriaxone is not suitable for the patient, what then can you choose? The main point of searching for an analogue is determining sensitivity to the antibiotic. To do this, it is necessary to carry out bacterial culture, where suitable analogues will be determined.

Most often, ceftriaxone is changed to rocephin, cefotaxime, cefazolin and azoline.

Rocephin

The drug is produced in Switzerland, it only comes in powder form. The package contains a solvent (lidocaine). The difference between ceftriaxone is that lidocaine is not included in the package, and, therefore, it will have to be purchased separately. Vials of Rocephin powder are dosed at 250, 500 or 1000 mg. The drug is administered intramuscularly or intravenously.

The active substance of Rocephin is ceftriaxone (disodium derivative). Hence the conclusion that rocephin and ceftriaxone are completely identical in structure.

If we look at the indications for use in detail, they are no different. In terms of the degree of purification, Swiss preparations are always at the top, but their prices are not surprisingly higher. For example, the price for one bottle of Rocephin (500 mg) is 550 rubles, which is 10 times more expensive than ceftriaxone (Russia).

Attentive patients note that Rocephin has more side effects. The following should be noted here: our manufacturer warns about the main possible reactions, and the Swiss one lists all undesirable effects.

Cefotaxime

The active substance of the drug is cefatoxime. The drug in question belongs to semisynthetic antibiotics (third generation cephalosporins). It is used only parenterally. The spectrum of action of cefotaxime is similar to ceftriaxone. It also negatively affects the gastrointestinal tract, so it is used only by injection.

Cefotaxime is not involved in the displacement of bilirubin from its connection with albumin, this makes it possible to use the drug from the first days of life.

The cost of cefotaxime is the same as that of ceftriaxone.

Cefazolin

The drug belongs to the first generation cephalosporins, just like ceftriaxone is used for parenteral administration. It is believed that cefazolin has a smaller spectrum of effects on pathogenic microflora, because It has no effect on some gram-negative bacteria. But, if culture shows that the bacteria is sensitive to cefazolin, you can safely use this remedy.

As for indications and contraindications, they are largely similar to ceftriaxone. A big plus in the direction of cefazolin is the possibility of its use during breastfeeding, when many antibiotics are contraindicated.

Cefazolin 500 mg (1 bottle) produced in Russia and Belarus is cheaper than ceftriaxone, its price is only 13 rubles.

Azaran

This drug is produced in Serbia and Yugoslavia. It is a structural analogue of ceftriaxone, therefore, all the main criteria are the same. It is believed that azaran has a high degree of purification; it is 10 times more expensive than ceftriaxone.

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Analogues for internal reception

If the bacterial process is moderate, then ceftriaxone can not be prescribed parenterally, but analogues in tablets, capsules or suspensions can be used.

Amoxiclav or ceftriaxone

The antibiotic consists of two active ingredients - amoxicillin and clavulanic acid. The latter is aimed at preventing the inactivation of amoxicillin, which can occur under the influence of beta-lactamases.

The drug is used not only for parenteral administration, but also comes in tablet form, as well as powder for preparing a suspension.

  1. Amoxiclav belongs to the penicillins, which are weaker in their therapeutic effect than other groups of antibacterial agents.
  2. When it comes to indications, it should immediately be noted that these are those infections that are sensitive to amoxiclav. If necessary, amoxiclav is prescribed to pregnant women.
  3. It is impossible to say right away which is better - amoxiclav or ceftriaxone; the severity and severity of the clinical picture remains an important point. For example, a patient has lacunar tonsillitis. Objectively: high body temperature, purulent plaque on the tonsils, sharp sore throat, general intoxication. Prescribe amoxiclav tablets and observe.

If by the end of the second day of treatment there is no improvement, the purulent plaque increases, it is better to immediately replace it with a macrolide (azithromycin) or cephalsporin (cephalexin). In particularly difficult cases, they switch to intramuscular or intravenous administration of ceftriaxone or cefazolin.

Cephalexin or ceftriaxone

The active ingredient of the drug is cephalexin. The antibiotic belongs to the first generation of the cephalosporin series. It is a good alternative to ceftriaxone for oral use. It is well accepted by the walls of the stomach, quickly adsorbed, and within an hour reaches its maximum in the blood.

The antibacterial effect is especially pronounced in the liver and kidney tissues, where the highest concentration of cephalexin is observed. The withdrawal period from the body is 6 hours.

According to the instructions, cephalexin is prescribed from the infant period, it is indicated “up to 12 months” at a dose of 2.5 ml. There is no clear information from what month of life the treatment is possible, so all the nuances of treating children are discussed with a pediatrician.

Cephalexin is an inexpensive drug, the price for various forms is as follows - capsules 500 mg No. 16 (Serbia) - 80 rubles, granules for preparing a suspension 250 mg / 5 ml 40 g - 66 rubles.

If you try to compare prices, then most likely cephalexin will be cheaper. So, for example, one bottle of 250 mg suspension (66 rubles) will be enough for a child’s course of treatment. The price for one bottle of ceftriaxone 500 mg is 20 rubles (one injection). The course of injections is at least 5 days. So consider it cheaper. Therefore, it is difficult to clearly determine what will be economical; it all depends on the severity of the bacterial process.

Suprax or ceftriaxone?

The active ingredient in Suprax is cefixime. The drug has three forms: tablets, capsules and granules for preparing a suspension. Ceftriaxone does not have such forms, because Available for injection only. Both drugs represent the third generation cephalosporin series.

The introduction of antibiotics into a muscle or intravenously is justified when the infectious process has “crossed” all limits of what is permitted, i.e. when previous treatment did not help and the patient’s condition worsens. Ceftriaxone is certainly more effective than Suprax, it acts faster, and the spectrum of antibacterial action is wider.

  • Ceftriaxone is approved in pediatrics from the age of two weeks in newborns, suprax (suspension) is used only from 6 months.
  • If we consider side effects, then ceftriaxone has a minus here, and “side effects” often appear literally three days from the start of therapy.
  • When choosing one of these remedies, the doctor will, first of all, take into account the clinical picture of the disease, as well as the results of bacteriological studies.

Now let's focus on the price. The cost of suprax (granules for preparing a suspension for oral administration 100 mg/5 ml 30 g) is in the range of 550–600 rubles. Capsules (400 mg) No. 6 are sold at a price of 700 rubles.

Amoxicillin or ceftriaxone?

These drugs have many differences, the only thing they have in common is that they are antibiotics. Amoxicillin belongs to the penicillin series. The drug is therapeutically much weaker than ceftriaxone, and very often shows resistance to bacterial flora.

Recently, doctors have increasingly prescribed amoxicillin in combination with clavulanic acid, which helps resist the harmful effects of penicillinase. Such drugs, for example, include amoxiclav; it is more expensive than amoxicillin, but more effective.

  1. Ceftriaxone is administered intramuscularly and intravenously, and amoxicillin is prescribed orally. For this, there are tablets, capsules and powder for preparing a suspension.
  2. If the bacterial process goes away without complications, amoxicillin or amoxiclav can be used. In severe cases of the disease, ceftriaxone will be the drug of choice.
  3. The main thing is not to self-medicate; antibiotics have their own specific prescriptions, and the wisdom of adjusting therapy is not always spelled out in the instructions. Only the doctor’s experience will tell you how best to dose the antibacterial drug.

The price, depending on the form of amoxicillin, ranges from 55 to 100 rubles.

What analogues of ceftriaxone can be found in drug search engines?

Despite the fact that a doctor prescribes an antibiotic, patients still look for information on the Internet. Ceftriaxone analogues can also be represented by the following list:

This list can be continued for a long time, because... Today, pharmaceutical companies compete in the production of antibacterial agents. Of course, after reading this list, you should not run to the pharmacy and treat yourself.

You can choose one of the remedies only in exceptional cases, when the patient’s life is threatened by an infection, and there are no doctors nearby. Then the patient should be treated according to the instructions for use.

In our article, we looked at the antibacterial drug ceftriaxone, learned about its analogues and the features of their use. From the information presented, we can conclude that ceftriaxone is a powerful drug that acts quickly, but is manifested by many adverse reactions. The administration of ceftriaxone and its analogues requires strict dosages, because These drugs are used from early childhood.

An important point remains that ceftriaxone and its structural analogues should not be used in mild to moderate cases of the infectious disease. Therapy should always be prescribed with more gentle doses, and preferably in the form of tablets or suspensions. Only if they are ineffective do they resort to parenteral administration.

In order not to make a mistake with the use of antibiotics and then not to replace them, ask the doctor to refer you to a bacterial culture of the required material before treatment (for a sore throat - culture from the throat, ear - culture from the ear canal, etc. ).

The main aspect of therapeutic therapy always remains timeliness, then the dose and duration of taking antibacterial drugs will be minimal. Be healthy!

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Source: http://lor-explorer.com/lekarstva-ot-nasmorka/tseftriakson-deshevye-analogi-instruktsiya

Ceftriaxone: popular about antibiotics

Antibacterial drugs are a huge group of drugs, which includes dozens of items. For a person unprepared for pharmacological information loads, it is very difficult to navigate the terrain among this chemical diversity. And yet, probably, almost all consumers who have ever encountered the prescription of antibiotics - and this is almost 100% of our readership - have most likely heard of the drug Ceftriaxone. And some, undoubtedly, saw it, spread it and injected it into the thickness of the gluteal muscle.

Before you continue reading: If you are looking for an effective method of getting rid of a runny nose, pharyngitis, tonsillitis, bronchitis or colds, then be sure to look at this section of the site after reading this article. This information has helped so many people, we hope it will help you too! So, now back to the article.

There are many legends and rumors about Ceftriaxone. Some say that he is very “strong”. Others argue that it is extremely harmful. Still others claim that it is indispensable and can be used for any infection. And it’s true: Ceftriaxone occupies one of the honorable places in the list of frequently prescribed antibacterial drugs. It is prescribed for a variety of infections in adults, children and even pregnant women. Thousands of our fellow citizens dutifully dilute the white powder in transparent bottles, playing magic with needles and syringes, and then experience far from pleasant sensations during the administration of the finished medicine.

However, today here and there the voices of skeptics are heard, assuring that the painfulness of the procedure does not always justify the result of treatment.

There are increasingly loud statements claiming that injectable antibiotics can be successfully replaced by oral antibiotics, available in the form of tablets or suspensions for internal use.

How close to the truth are the followers of this theory? Is it really possible, with a calm heart, to replace Cephalosporin for injection with equally “strong” tablets? And in general, what kind of medicine is this, and why is it so popular both among doctors and among the masses? We will answer these and many other questions in an article devoted to the antibiotic Ceftriaxone.

A look into the past

And we will begin our close acquaintance with Ceftriaxone with the history of its creation. It turns out that the drug, without which millions of doctors around the world cannot imagine their clinical practice today, has not existed for very long. Humanity owes its appearance to the pharmacists of the famous Swiss company Hoffman La Roche. It was through their efforts that a new third-generation cephalosporin was synthesized in 1978. Just four years later, the original drug, under the trade name Rocephin, began an ascent up the ladder of fame, which, apparently, is still not completed. By 1987, Rocephin had broken sales records for all other drugs produced by Hoffman La Roche. For its obvious merits, Ceftriaxone was included in the famous list of the World Health Organization, which includes all the drugs that currently exist and are most important for human health.

And today, Ceftriaxone continues to occupy one of the leading positions among antibiotics. What is the secret of his success? Of course, in a favorable ratio of wide spectrum of action and high safety. But first things first.

About cephalosporins

So, Ceftriaxone is an antibiotic, that is, a drug active against a number of bacteria. It belongs to the group of cephalosporins, uniting five generations of drugs, the structural formula of which is based on a beta-lactam ring. Let us recall that beta-lactams, along with cephalosporins, include penicillin antibiotics (for example, Amoxicillin), as well as lesser-known and much less commonly used carbapenems and monobactams. The main difference between cephalosporin antibiotics and penicillins is their greater resistance to beta-lactamases - special enzymes synthesized by bacteria that destroy the beta-lactam ring and, as a result, the drug itself.

Cephalosporins act bactericidal against infectious agents, destroying the cell wall of bacteria, which leads to its death. The first cephalosporin drug appeared in 1948. Since then, five generations of drugs have been synthesized, each of which has some significant advantage over the previous one. Thus, first-generation drugs are effective against predominantly gram-negative flora, which are mainly responsible for infections of the intestines and genitourinary tract. Second generation cephalosporins have a slightly wider spectrum of action, but they still cannot be called universal antibiotics. In addition, second-generation drugs (for example, Cefaclor, Cefuroxime) for internal use have extremely low bioavailability (about 60%). This means that when the medicine is administered, no more than 60% of the dose taken is absorbed into the blood and begins to work, and this property, of course, cannot be called a positive quality of the drugs. But starting from the third generation, scientists were able to synthesize drugs covering almost the entire spectrum of bacterial flora.

Cephalosporins of the third and higher generations are parenteral, that is, administered as injections for intramuscular or intravenous administration. And Ceftriaxone is a typical representative of this subgroup of antibiotics.

Composition and release forms of Ceftriaxone

The drug is a crystalline powder, usually white. A slight yellowish or orange tint is allowed. Ceftriaxone dissolves well in water and anesthetics to form a clear, slightly yellow or even amber solution. The drug is produced in the form of disodium salt, so sometimes the name of the drug looks more complicated: Ceftriaxone sodium. However, not all manufacturers indicate this nuance, and in most cases the medicine is simply called “Ceftriaxone” (in the Latin language that doctors use to write prescriptions, it is Ceftriaxonum).

The drug disintegrates quite quickly in dissolved form, so it, like many other antibiotics, is available in the form of a lyophilized powder for the preparation of an injection solution. For ease of dosing, there are several forms of release of Ceftriaxone: bottles of 1 gram (intended for the treatment of adult patients), as well as 0.5 g and even 0.25 g. The last two forms are used, as a rule, in pediatric practice. Note that there is no difference in composition between the different forms of release of Ceftriaxone, that is, if the pharmacy, for example, does not have a 1-gram dosage, it can be easily replaced with two bottles of 0.5 g each. However, such variations can make dilution difficult, and also complicate the calculation of the dose when it comes to the use of antibiotics in children.

Pharmacological properties

The bactericidal effect of Ceftriaxone is due to its ability to disrupt the biosynthesis of an important protein - a component of the bacterial cell wall. Being a beta-lactam antibiotic, Ceftriaxone remains resistant to the action of enzymes that destroy the beta-lactam ring, which distinguishes it extremely favorably from the same penicillins, for example, Amoxicillin.

The spectrum of action of Ceftriaxone is very wide. The drug is effective against infection with both gram-positive and gram-negative bacteria. Let us list the pathogens that are sensitive to it.

Enterobacteriaceae, Escherichia coli, Proteus, Klebsiella, Pseudomonas (Pseudomonas aeruginosa), Salmonella, which are responsible for many intestinal infections, as well as Haemophilus influenzae, Moraxella, which cause upper respiratory tract infections. Gonococci associated with gonorrhea, etc.

  • Gram-positive bacteria:

    Staphylococcus epidermidis, aureus, pneumococcus, streptococci - causative agents of infections of the upper and lower respiratory tract, including pneumonia, tonsillitis, etc.

  • Anaerobic bacteria:

    bacteroids, clostridia, peptostreptococci.

    • It is important that, for example, unlike second-generation oral cephalosporins, Ceftriaxone is absorbed quickly and completely: its bioavailability reaches 100%. Just 1–3 hours after administration, the maximum concentration of the antibiotic is reached in the blood, which certainly has a positive effect on its effectiveness. Half the dose of Ceftriaxone is excreted within the first two days after administration in the urine and/or bile.

    Indications for the use of Ceftriaxone according to the instructions

    The instructions for use of Ceftriaxone contain a fairly impressive list of indications for use. By the way, after reading this list, the reader may even get the feeling that the drug can easily cope with almost all existing bacterial infections. Unfortunately, this is not entirely true, but Ceftriaxone can indeed be successfully used for various pathologies - after all, its spectrum of activity provides wide possibilities. Among the indications for the use of Ceftriaxone:

    • infections of the upper and lower respiratory tract (acute bronchitis associated with bacterial infection, pneumonia, sinusitis, bacterial tonsillitis, acute otitis media);
    • peritonitis, biliary tract infections;
    • infections of joints and bone tissue;
    • skin infections (eg furunculosis);
    • urinary system infections, including pyelonephritis, inflammation of the bladder;
    • infections of the reproductive tract - inflammation of the prostate gland, testicles;
    • intestinal infections (salmonellosis and others).

    In addition, Ceftriaxone injections are used as part of combination antibiotic therapy for syphilis, gonorrhea (uncomplicated), bacterial meningitis, typhoid fever and other infectious diseases. The drug is also prescribed to prevent infections during surgical interventions. In such cases, it is not used as a course, as usual, but once.

    Despite the fact that the instructions for Ceftriaxone (as, indeed, for any other antibiotics) clearly indicate the diseases for which the drug can be effective, in no case should they be taken as instructions for action by the patient himself - too many nuances should be taken into account when prescription of medication. Why do doctors and pharmacists insist that patients themselves do not self-medicate with antibiotics?

    Antibacterial permissiveness: causes and consequences

    One of the most complex and, unfortunately, still unresolved problems of domestic medicine is the easy availability of the vast majority of prescription drugs. While throughout the civilized world hormonal, cardiovascular and, of course, antibacterial drugs are sold exclusively by prescription, in the countries of the former Soviet Union, for reasons that are not entirely clear, these potent drugs are practically freely available. Officially, antibiotics, of course, belong to the prescription group, but in reality, pharmacies in Russia and other CIS countries are unlikely to require a document confirming a doctor’s prescription.

    The role of a prescription, written out on a standard form and certified by a doctor’s seal, is often played by patient cards, pages from notebooks and miserable scraps of paper. Moreover, antibiotics are easily dispensed even without any written confirmation of the prescription, simply “by ear.” At the same time, all specialists, including pharmacists, are well aware of the possible consequences of such permissiveness.

    A particular danger lies in the use of antibacterial agents on the advice of friends, neighbors, acquaintances or from one’s own practical experience. Our compatriots boldly read the instructions for use (including Ceftriaxone) and, based on the indications set out in it, confidently draw conclusions about the nature of their disease and the advisability of taking antibiotics. But each case is individual and unique. Even if we are really talking about a bacterial infection, it is not at all necessary that its causative agent will show sensitivity to Ceftriaxone, since the possibilities of this drug, although great, are, unfortunately, not unlimited.

    Incorrect use of antibiotics can have dangerous consequences.

    First of all, an incorrectly prescribed drug (in this case, used without a doctor’s prescription) only aggravates the disease, since it does not have a therapeutic effect. Consequently, despite regular exhausting injections, the disease continues to progress and the patient’s condition continues to deteriorate.

    Secondly, inadequate antibiotic therapy is fraught with the development of new, antibiotic-resistant strains of bacteria, which complicates further treatment and worsens the prognosis. Often, antibacterial drugs, which usually cope with an infection without problems, turn out to be powerless against it due to the fact that the day before (some time ago) the patient incorrectly and haphazardly used other antibiotics.

    In addition, even after studying the annotation for the medicine inside and out, a consumer without a medical or pharmaceutical education will not be able to make an informed choice between, for example, the same Ceftriaxone and another antibiotic that is used for a given infectious disease. The doctor certainly makes this choice, and makes it taking into account a whole range of different nuances. Here are typical examples of the use of Ceftriaxone for various infectious diseases.

    Ceftriaxone for respiratory tract infections

    If the instructions indicate that Ceftriaxone is used for pneumonia or bacterial sore throat, this does not mean that this antibiotic is the drug of choice. For almost all respiratory tract diseases associated with bacterial infection, first-line antibiotics, that is, those prescribed first, are penicillins (Amoxicillin or its combination with clavulanic acid, for example, Augmentin). If the patient is allergic to penicillins, macrolides (azithromycin - Sumamed, clarithromycin - Fromilid, Klacid) are usually prescribed. And only in case of intolerance or ineffectiveness of drugs of these two groups does it come to cephalosporins and, in particular, Ceftriaxone.

    The reason why Ceftriaxone is not even relegated to the background lies in the much better tolerability of penicillins and macrolides. Unlike Ceftriaxone, alternative drugs can be used orally, in the form of tablets (capsules) or pediatric suspension. Then why do doctors often prescribe the antibiotic Ceftriaxone injections for pneumonia?

    Apparently, this is due to the association that has become established in the minds of our compatriots (including old-school doctors): good medicine must be injectable. According to followers of this a priori false theory, tablets are always less effective than injections. But in fact, the effectiveness in this case does not correlate in any way with the method of application. Modern antibiotics and their production technologies are capable of providing oral drugs with bioavailability approaching 100%, which is not inferior to the pharmacokinetic parameters of injectable forms. And if the doctor prescribes Ceftriaxone for you or, what’s worse, your child for tonsillitis or pneumonia, and not penicillin tablets (macrolides), you have every reason to seek advice from an alternative specialist. Because the use of injectable antibiotics is a last resort, which doctors around the world reserve only for patients who are allergic to or resistant to oral medications.

    Ceftriaxone for intestinal infections

    Another interesting indication for the use of Ceftriaxone, which is worth talking about in more detail, is use for various bacterial intestinal infections. Let's start with the fact that, as a rule, the use of antibiotics in such cases is inappropriate: all pathogens of intestinal infections, including the known salmonella, shigella, which causes dysentery, and other bacteria die on their own, going through a development cycle. This usually happens 7–10 days after the onset of the disease. Therefore, the official protocols of the world's leading gastroenterological associations indicate that the main method of treating intestinal infections involves symptomatic therapy, which consists mainly of compensating for the loss of fluid and minerals with vomiting and diarrhea. However, with high fever, severe bloody diarrhea, and severe intoxication, antibiotics can still be prescribed, provided, of course, that the disease is associated with bacterial pathogenic flora and not a viral infection, which is often responsible for traditional food poisoning.

    But let’s look at a case where an intestinal infection is truly of bacterial origin and requires the prescription of antibiotics. In such a situation, the drugs of choice are not cephalosporins, but, for example, fluoroquinolones, which have a wider spectrum of gram-negative activity. The first is preferred in pediatric practice, since fluoroquinolone antibiotics are not approved for use under the age of 18 years. However, some pediatric gastroenterologists still prefer less safe, but much more effective fluoroquinolones (short courses of treatment) to the use of the more “narrow” Ceftriaxone. Thus, with the second important indication for the administration of Ceftriaxone injections, which is prescribed in the instructions for use and, in general, does not raise objections, everything is not as clear as we would like.

    Ceftriaxone for sexually transmitted diseases

    Briefly but succinctly I would like to warn those who want to “self-cure” from “unpleasant diseases” with the help of Ceftriaxone. The annotation lists uncomplicated gonorrhea and even syphilis as indications for use, but it should be borne in mind that venereologists extremely rarely resort to treating these diseases with cephalosporins. They can be prescribed either at the earliest stages, during the first few days after tragic contact with an infected person, or as an additional antibiotic in a complex treatment regimen.

    Contraindications to the use of Ceftriaxone

    Having dealt with the indications, let's move on to the exact opposite - contraindications for the use of Ceftriaxone. First of all, an antibiotic cannot be used if you are hypersensitive to it, that is, if you have an allergy. This rule also applies to those patients who are allergic to other cephalosporin drugs. In addition, it is recommended to use Ceftriaxone with caution in people who have ever had an allergy to penicillins (Amoxicillin, Ampicillin, Augmentin or Amoxiclav, etc.).

    Carefully weighing the risks and expected benefits, Ceftriaxone is prescribed to people with renal and liver failure, severe diseases of the gastrointestinal tract, especially ulcerative colitis, and enteritis. Ceftriaxone should not be used to treat premature babies, as well as newborns with hyperbilirubinemia (jaundice).

    During pregnancy, Ceftriaxone is used in cases where the benefit outweighs the possible harm to the child. The antibiotic passes into breast milk, so it is better to stop breastfeeding during treatment.

    Dosing

    Now it’s time to figure out how to dose Ceftriaxone and, most importantly, how and how best to dilute it.

    The dosage of Ceftriaxone for adults is 1–2 g of the drug once a day. In case of severe infections, the dose can be increased to 4 g, then the frequency of administration is doubled (every 12 hours, that is, twice a day). The exact dose should be selected by the attending physician, based on the severity of the infection, as well as the type of pathogen, general health, and age of the patient. Taking these same factors into account, the duration of antibiotic therapy is also determined, so the question of how long to inject Ceftriaxone cannot be answered in one word: as a rule, it is prescribed for at least 5 days for mild infections, and up to 2-3 weeks for severe ones.

    The dose of Ceftriaxone for the treatment of children is determined depending on the child’s weight and age. Thus, newborns who are not yet two weeks old are prescribed 20–50 mg of antibiotic per 1 kilogram of weight per day. Children older than 3 weeks and up to 12 years of age can receive from 20 to 80 mg of Ceftriaxone per 1 kg of body weight, preferably twice a day.

    The child should not receive more than 2 g of Ceftriaxone per day.

    How to dilute Ceftriaxone?

    We have come to one of the most pressing issues faced by consumers who are forced to administer the drug at home, in an outpatient setting. So, how to properly dilute Ceftriaxone powder to obtain a dissolved medicine ready for use?

    First of all, we will need a solvent compatible with Ceftriaxone, which can be water for injection, as well as the anesthetics Lidocaine or Novocaine. It is known that antibiotic injections are very painful, so diluting Ceftriaxone (like another antibacterial drug) with water is too much of a challenge for the patient. At the same time, it is also inappropriate to use only anesthetics to prepare the solution: in this case, the activity of the drug may decrease. Therefore, both doctors and pharmacists agreed that the best painlessness/effectiveness ratio would be a solution prepared using equal parts of lidocaine and water for injection. Novocaine is used much less frequently.

    So, to dissolve 1 gram of Ceftriaxone you will need 2 ml of water for injection and 2 ml of lidocaine 2%.

    Please note that pharmacies also sell lidocaine in a concentration of 10%.

    Now let's look at the instructions step by step on how to turn Ceftriaxone powder into an injection solution using lidocaine and water.

    1. Open both ampoules with solvent (water and lidocaine 2%) by pressing the dot located at the neck of the ampoule.
    2. Open the central round part of the aluminum shell located on the Ceftriaxone vial. Do not remove the shell rim!
    3. Wipe the rubber cap located under the central part of the aluminum shell with 70% alcohol (or 95% alcohol, or an alcohol solution of boric (salicylic) acid).
    4. Fill a 5 ml syringe alternately with water and lidocaine.
    5. Inject the resulting solution into the Ceftriaxone vial by piercing the rubber cap with a needle. It is better to administer in two stages: first, about half the solvent, then shake the bottle thoroughly, and then add the remaining solvent.
    6. Remove the needle from the cap and shake the vial with Ceftriaxone for several minutes until a clear solution is obtained.

    Dissolved Ceftriaxone has a light yellow color (sometimes only yellowish). It should not contain sediment or undissolved particles.

    How to inject a ready-made antibiotic correctly?

    A similar question may worry patients who receive Ceftriaxone on an outpatient basis, and, therefore, intramuscularly - after all, intravenous injections are prescribed only in hospital settings. In answering this, it should be noted:

    1. The prepared solution of Ceftriaxone cannot be stored, otherwise the effectiveness of the drug may be reduced.
    2. To administer the injection, you should not use the same needle with which the solvent was introduced into the bottle, but a new one. The syringe can be left the same, or you can change it.
    3. The intramuscular injection technique involves deep insertion of a needle into the left upper quadrant of the buttock. It is better to administer the antibiotic slowly. Before and after administration, the injection area must be treated with alcohol or an alcohol solution of boric (salicylic) acid.

    About following recommendations

    Having dealt with the technical issues, let's talk about the importance of observing dosages and the course of treatment during antibiotic therapy. The fact is that many patients, having felt relief after starting to use antibiotics, try to make adjustments to their further regimen. They begin to be tormented by the seditious thought that further introduction of “these strong and dangerous antibiotics” is unnecessary. What are the consequences of unauthorized withdrawal or even reduction of the dosage of antibacterial drugs?

    Imagine a colony of bacteria developing during an infectious process. It is heterogeneous: among the family of microbes there are those who are stronger, and there are also weak “instances”. When an antibiotic begins to act, those microbes whose vitality is already running low are immediately targeted. They are unable to fight for existence, and die in the first days, or even hours, of treatment. The patient feels relief and may mistakenly believe that the antibiotics’ mission has been completed. And make a mistake.

    While the patient voluntarily stops antibiotic therapy or reduces its dosage, the selected, strong and courageous bacteria that survived the first blow are activated and enter the battle. The consumer, as if nothing had happened, rests on his laurels, while microbes multiply rapidly in his body, which means the infectious disease progresses. When the patient or the doctor comes to their senses and understands that treatment should be started again, the previous antibiotic will most likely be unable to resist the disease, since the bacterial strains have already “acquainted” with it and have developed resistance.

    Side effects

    Of course, antibiotics have side effects, including Ceftriaxone. We list the most common adverse events associated with treatment with this drug:

    • neurological reactions: headache, sometimes dizziness. Occurs in less than 1% of cases;
    • cardiovascular reactions: heartbeat;
    • hematopoietic disorders: increased number of eosinophils (in 6% of patients), platelets (in 5% of patients), decreased number of leukocytes, rarely - anemia (drop in hemoglobin) and other blood picture disorders;
    • digestive disorders: diarrhea (no more than 2.7% of patients), nausea, vomiting, taste disturbances, flatulence in less than 1% of cases;
    • dysfunction of the genitourinary system: changes in some renal parameters. Note that these reactions are observed quite rarely (usually in less than 1% of patients);
    • allergies: uncommon (in 1% of patients or less) - itching, urticaria, fever.

    Sometimes, while taking Ceftriaxone, a fungal infection (candidiasis) develops. This effect occurs rarely, in less than 1% of cases. Weak patients who suffer from chronic diseases are predisposed to it.

    For those who are worried about the possible development of dysbiosis due to the use of antibiotics and Ceftriaxone in particular, we note that in an extremely small proportion of patients, the drug can help loosen stools, but not due to the hypothetically altered flora, but due to stimulation of intestinal motility. The only dangerous intestinal consequence of antibiotic therapy may be colitis associated with rapid growth of clostridia bacteria. However, this complication occurs very rarely, as a rule, in patients with immunodeficiency (HIV-infected, cancer patients, etc.).

    Ceftriaxone analogs

    Ceftriaxone is the international name of the drug under which it is produced throughout the world. Many pharmaceutical companies, especially domestic ones, do not introduce trade names, and then the antibiotic is sold under its international “name”. This is done, for example, by Russian companies LECKO, Kraspharma, Sintez, Biokhimik, as well as some Indian manufacturers. The price of different drugs under the same name Ceftriaxone is usually low. Along with this, the pharmacy assortment also includes higher-quality analogues of Ceftriaxone, which are much more expensive than domestic and Indian ones. These include:

    • - an original drug produced by Hoffman La Roche. It has impeccable quality and a corresponding price;
    • Tercef - Bulgarian Ceftriaxone, combining acceptable quality and reasonable price;
    • Lendacin, a drug produced in Slovenia (KRKA);
    • Medakson, an analog produced in Cyprus.

    It should be noted that there are no analogues of Ceftriaxone in tablets, just as there are no other third-generation cephalosporin antibiotics with a similar spectrum. And when the doctor prescribes this particular drug, you have practically no choice - to inject or not to inject, unless, of course, you doubt the doctor’s competence. Inject with confidence, follow the dosage and get better immediately!

    The article above and comments written by readers are for informational purposes only and do not encourage self-medication. Consult a specialist regarding your own symptoms and illnesses. When taking any medicine, you should always use the instructions that come with the medicine and your doctor's advice as a guide.

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