Ceftriaxone powder 1000mg #1

Ceftriaxone instruction

You can buy Ceftriaxone antibiotic here

Composition

The drug includes Ceftriaxone - an antibiotic from the class of cephalosporins (β-lactam antibiotics, whose chemical structure is based on 7-ACS).

What is Ceftriaxone?

According to Wikipedia, Ceftriaxone is an antibiotic whose bactericidal action is due to its ability to disrupt peptidoglycan synthesis of bacterial cell walls.
The substance is a slightly hygroscopic fine crystalline powder of yellowish or white color. One bottle contains 0.25, 0.5, 1 or 2 grams of sterile sodium salt of Ceftriaxone.

Form of issue

Powder 0.25 / 0.5 / 1/2 g for cooking:
    solution d / u;
    solution for infusion therapy.
Ceftriaxone is not available in tablets or syrup.

pharmachologic effect

Bactericidal. Preparation of the third generation from the group of antibiotics "Cephalosporins".

Pharmacodynamics and pharmacokinetics

A universal antibacterial agent whose mechanism of action is due to the ability to suppress the synthesis of the bacterial cell wall. The drug exhibits greater resistance to most β-lactamases Gram (+) and Gram (-) microorganisms.
Active in relation to:
    Gram (+) aerobics - St. aureus (including for penicillinase-producing strains) and Epidermidis, Streptococcus (pneumoniae, pyogenes, viridans group);
    Gram (-) aerobes - Enterobacter aerogenes and cloacae, Acinetobacter calcoaceticus, Haemophilus influenzae (including penicillinase-producing strains) and parainfluenzae, Borrelia burgdorferi, Klebsiella spp. (including pneumoniae), Escherichia coli, Moraxella catarrhalis and diplococcus genus Neisseria (including penicillinase-producing strains), Morganella morganii, vulgar proteus and mirabilis protease, Neisseria meningitidis, Serratia spp., some Pseudomonas aeruginosa strains;
    anaerobes - Clostridium spp. (exception - Clostridium difficile), Bacteroides fragilis, Peptostreptococcus spp.
In vitro (the clinical value remains unknown), activity is noted for strains of the following bacteria: Citrobacter diversus and freundii, Salmonella spp. (including in relation to Salmonella typhi), Providencia spp. (including in relation to Providencia rettgeri), Shigella spp .; Bacteroides bivius, Streptococcus agalactiae, Bacteroides melaninogenicus.
Methicillin-resistant Staphylococcus, many strains of Enterococcus (including Str. Faecalis) and Streptococcus Group D to cephalosporin antibiotics (including Ceftriaxone) are stable.

Pharmacokinetic parameters:

    bioavailability - 100%;
    Т Сmax at introduction of Ceftriaxone iv in - at the end of infusion, with intramuscular injection - 2-3 hours;
    communication with plasma proteins - from 83 to 96%;
    T1 / 2 with a / m introduction - from 5.8 to 8.7 hours, with IV introduction - from 4.3 to 15.7 hours (depending on the disease, the age of the patient and the state of his kidneys).
In adults, the concentration of Ceftriaxone in CSF when administered at 50 mg / kg after 2-24 hours is many times higher than the MIC (minimum inhibitory concentration) for the most common pathogens of meningococcal infection. The drug penetrates well into the cerebrospinal fluid with inflammation of the membranes of the brain.

Ceftriaxone is excreted unchanged:

    kidneys - by 33-67% (in newborn babies this figure is at the level of 70%);
    with bile in the intestine (where the drug is inactivated) - by 40-50%.
Hemodialysis is ineffective.

Indications for use of Ceftriaxone

The annotation states that the indications for the use of Ceftriaxone are infections caused by drug-sensitive bacteria. Intravenous infusions and injections of medication are prescribed for treatment of:
    infections of the abdominal cavity (including with empyema of the gallbladder, angiocholite, peritonitis), ENT organs and respiratory tract (empyema of the pleura, pneumonia, bronchitis, abscess of the lungs, etc.), bone and joint tissue, soft tissues and skin, urogenital tract (including pyelonephritis, pyelitis, prostatitis, cystitis, epididymitis);
    epiglottitis;
    infected burns / wounds;
    infectious lesions of the maxillofacial region;
    bacterial septicemia;
    sepsis;
    bacterial endocarditis;
    bacterial meningitis;
    syphilis;
    chancroid;
    tick-borne borreliosis (Lyme disease);
    uncomplicated gonorrhea (including in cases when the disease is caused by microorganisms that release penicillinase);
    salmonellosis / salmonella;
    typhoid fever.
The drug is also used for perioperative prevention and for the treatment of patients with weakened immunity.

What is Ceftriaxone used for syphilis?

Despite the fact that with various forms of syphilis, the drug of choice is penicillin, its effectiveness in some cases may be limited.
To the use of antibiotics-cephalosporins resorted to as a reserve option for intolerance of drugs of the penicillin group.

Valuable properties of the drug are:

    the presence in its composition of chemicals that have the ability to inhibit the formation of cell membranes and mukopeptide synthesis in the walls of bacterial cells;
    the ability to quickly penetrate into the organs, fluids and tissues of the body and, in particular, into the cerebrospinal fluid, which undergoes a number of specific changes in patients with syphilis;
    the possibility of application for the treatment of pregnant women.
The drug is most effective in cases when the causative agent of the disease is Treponema pallidum, since the distinctive feature of Ceftriaxone is a high treponemicide activity. The positive effect is particularly pronounced when the drug is injected.
Treatment of syphilis with the drug gives good results not only in the early stages of the disease, but also in neglected cases: with neurosyphilis, as well as with secondary and latent syphilis.
Because T1 / 2 of Ceftriaxone is approximately 8 hours, the drug can be equally successful in both the inpatient and outpatient treatment regimens. The drug should be administered only once a day.
For preventive treatment, the drug is administered for 5 days, with primary syphilis - a 10-day course, early latent and secondary syphilis are treated for 3 weeks.
When the forms of neurosyphilis are not released, the patient is given single-dose for 1-2 g of Ceftriaxone for 20 days, in the late stages of the disease, the drug is administered 1 g / day. for 3 weeks, after which a 14-day interval is maintained and treated in the same dosage for 10 days.
With acute generalized meningitis and syphilitic meningoencephalitis, the dose is increased to 5 g / day.

Prizes Ceftriaxone: from what the drug is prescribed for angina in adults and children?

Despite the fact that the antibiotic is effective for various lesions of the nasopharynx (including angina and sinusitis), it is usually rarely used as a drug of choice, especially in pediatrics.
With angina, the drug is allowed to enter through a dropper in a vein or in the form of usual injections in the muscle. However, in the vast majority of cases, the patient is prescribed intramuscular injections. The solution is prepared immediately before use. The finished mixture at room temperature remains stable for 6 hours after preparation.
Children with angina Ceftriaxone is prescribed in exceptional cases, when acute angina is complicated by severe suppuration and inflammation.
The appropriate dosage is determined by the attending physician.
During pregnancy, the drug is prescribed in cases where the antibiotics of the penicillin group are not effective. Although the drug penetrates the placental barrier, it does not have a significant effect on the health and development of the fetus.

Treatment of sinusitis with Ceftriaxone

In genyantritis, antibacterial drugs are first-line drugs. Completely penetrating into the blood, Ceftriaxone lingers in the focus of inflammation in the right concentrations.
Typically, the drug is prescribed in combination with mucolytics, vasoconstrictors, etc.
How to stain a drug with genyantritis? Usually, the patient is prescribed to inject Ceftriaxone twice a day with 0.5-1 g twice daily. Before injection, the powder is mixed with lidocaine (preferably a 1% solution is used) or with water.
Treatment lasts at least 1 week.

Contraindications

Ceftriaxone is not prescribed with known hypersensitivity to cephalosporin antibiotics or ancillary components of the drug.
Relative contraindications:
    the period of newborns if the child has hyperbilirubinemia;
    prematurity;
    renal / hepatic impairment;
    enteritis, NJC or colitis associated with the use of antibacterial agents;
    pregnancy;
    lactation.

Side effects of Ceftriaxone

Side effects of the drug appear as:
    hypersensitivity reactions - eosinophilia, fever, itching, urticaria, edema, skin rash, multiform (in some cases, malignant) exudative erythema, serum sickness, anaphylactic shock, chills;
    headache and dizziness;
    oliguria;
    disturbances in the function of the digestive system (nausea, vomiting, flatulence, taste disturbance, stomatitis, diarrhea, glossitis, sladge formation in the gallbladder and pseudocholithiasis, pseudomembranous enterocolitis, dysbacteriosis, candidomycosis and other superinfections);
    disorders of hemopoiesis (anemia, including hemolytic, lympho-, leuko-, neutro-, thrombocyto-, granulocytopenia, thrombotic and leukocytosis, hematuria, basophilia, nosebleeds).
If the drug is administered intravenously, there may be inflammation of the venous wall, as well as tenderness along the veins. The introduction of the drug into the muscle is accompanied by soreness at the injection site.
Ceftriaxone (injections and intravenous infusion) can also have an effect on laboratory performance. The patient decreases (or increases) prothrombin time, increases the activity of alkaline phosphatase and liver transaminase, as well as urea concentration, hypercreatininemia, hyperbilirubinemia, glucosuria develop.
Reviews of the side effects of Ceftriaxone, suggest that with the introduction of the drug in almost 100% of patients complain of severe soreness of the injection, some note muscle pain, dizziness, chills, weakness, pruritus and rash.
The easiest way to tolerate injections, if you dilute the powder with anesthetic. In this case, it is necessary to make a trial both on the drug itself and on the anesthetic.

Instructions for the use of Ceftriaxone

In the manufacturer's instructions and Vidal's guide, it is indicated that the drug can be injected into a vein or into a muscle.
Dosage for adults and for children over 12 years - 1-2 g / day. Antibiotic is administered once or every 12 hours in a half dose.
In particularly serious cases, and also if the infection is provoked by a mildly sensitive agent to Ceftriaxone, the dose is increased to 4 g / day.
In gonorrhea, a single injection of 250 mg of the drug into the muscle is recommended.
For prophylactic purposes, before the infected or presumably infected operation, depending on the degree of danger of infectious complications, the patient should take 1-2 g of Ceftriaxone once for 0.5-1.5 hours before surgery.
For children of the first 2 weeks of life, the medicine is administered 1 r./day. The dose is calculated by the formula 20-50 mg / kg / day. The highest dose is 50 mg / kg (which is associated with the underdevelopment of the enzyme system).
The optimal dosage for children under 12 years (including infants) is also selected depending on the weight. The daily dose varies from 20 to 75 mg / kg. Children weighing more than 50 kg, Ceftriaxone administered at the same dose as adults.
Exceeding the 50 mg / kg dose should be administered as an intravenous infusion lasting at least 30 minutes.
In bacterial meningitis, treatment starts with a single injection of 100 mg / kg / day. The highest dose is 4 g. Once the pathogen is isolated and its sensitivity to the drug is determined, the dose is reduced.
Reviews about the drug (in particular, about its use in children) allow us to conclude that the remedy is very effective and affordable, but its significant drawback is severe soreness at the injection site. As for the side effects, in the opinion of the patients themselves, they are no more , than when using any other antibiotic.

How many days to stab the drug?

The duration of treatment depends on which pathogenic microflora is caused by the disease, and also on the characteristics of the clinical picture. If the pathogen is a Gram (-) diplococcus of the genus Neisseria, the best results can be achieved in 4 days, if the enterobacteria are sensitive to the drug, for 10-14 days.

Ceftriaxone injections: instructions for use. Than to dilute a preparation?

To dilute the antibiotic used a solution of lidocaine (1 or 2%) or water for injection (d / u).
When using water, it should be borne in mind that IM injections of the drug are very painful, so if the solvent is water, discomfort will be both during the injection and some time after it.
Water for dilution of the powder is usually taken in those cases when the use of lidocaine is impossible because of the patient's allergy to it.
The optimal option is a 1% solution of lidocaine. Water d / and it is better to use as an adjuvant, while diluting the drug Lidocaine 2%.

Can I dilute with Novocaine Ceftriaxone?

Novocaine, when used to dilute the drug, reduces the activity of the antibiotic, while increasing the likelihood of anaphylactic shock in the patient.
If we start from the feedback of the patients themselves, they note that Lidocaine is better than Novocain, relieves pain when introducing Ceftriaxone.
In addition, the use of a freshly prepared solution of Ceftriaxone with Novocaine increases the pain during injection (the solution remains stable for 6 hours after preparation).

How to breed Ceftriaxone Novocaine?

If Novokain is still used as a solvent, 1 ml of the preparation is taken in the volume of 5 ml. If you take a smaller amount of Novocaine, the powder may not completely dissolve, and the needle of the syringe will be clogged with lumps of the drug.
Breeding with lidocaine 1%
For injection into the muscle, 0.5 g of the drug is dissolved in 2 ml of a 1% solution of lidocaine (the contents of one ampoule); 3.6 g of solvent is taken per 1 g of the preparation.
Dosage of 0.25 g is diluted in the same way as 0.5 g, that is, 1 ampoule content of 1% lidocaine. After that, the finished solution is collected into different syringes by half the volume in each.
The medicine is injected deep into the gluteus muscle (not more than 1 g in each buttock).
The drug diluted with lidocaine is not intended for intravenous administration. He can be injected strictly into the muscle.
How to dilute injections of Ceftriaxone Lidocaine 2%?
To dilute 1 g of the drug, take 1.8 ml of water d / and 2% of lidocaine. To dilute 0.5 g of the preparation, 1.8 ml of lidocaine with 1.8 ml of water are also mixed, but only half of the resulting solution (1.8 ml) is used for dissolution. To dilute 0.25 g of the preparation, 0.9 ml of a similarly prepared solvent is taken.

Ceftriaxone: how to breed for children for intramuscular injection?

The above procedure for conducting intramuscular injections is practically not used in pediatric practice, since Ceftriaxone with novocaine can cause a severe anaphylactic shock in a child, and in combination with lidocaine - may cause seizures and disrupt the work of the heart.
For this reason, the optimal solvent in the case of the use of the drug in children is ordinary water d / u. The impossibility of using an anesthetic in childhood requires an even slower and more accurate administration of the drug in order to reduce pain during the injection.

Dilution for intravenous administration

For IV administration, 1 g of the drug is dissolved in 10 ml of distilled water (sterile). The drug is injected slowly for 2-4 minutes.
Breeding for intravenous infusion
When carrying out the infusion therapy, the drug is administered for at least half an hour. To prepare the solution, 2 g of powder is diluted in 40 ml of a solution free from Ca: dextrose (5 or 10%), NaCl (0.9%), fructose (5%).

Additionally

Ceftriaxone is intended exclusively for parenteral administration: manufacturers do not release tablets and suspensions because the antibiotic is in contact with the tissues of the body, is highly active and strongly irritates them.

Doses for animals

Dosage for cats and dogs is selected taking into account the body weight of the animal. As a rule, it is 30-50 mg / kg.
If a 0.5 g bottle is used, 1 ml of 2% Lidocaine and 1 ml of water should be added to it (or 2 ml of lidocaine 1%). After shaking the medicine vigorously until the lumps are completely dissolved, it is injected into the syringe and injected into the diseased animal into the muscle or under the skin.
Dosage to the cat (Ceftriaxone 0.5 g is usually used for small animals - for cats, kittens, etc.), if 1 kg of weight the doctor has prescribed 40 mg of Ceftriaxone is 0.16 ml / kg.
For dogs (and other large animals) take 1 gram vials. The solvent is taken in a volume of 4 ml (2 ml Lidocaine 2% + 2 ml water q / v). A dog weighing 10 kg, if the dose is 40 mg / kg, you need to enter 1.6 ml of the finished solution.
If Ceftriaxone is to be administered iv, sterile distilled water is used through the dilution catheter.

Overdose

Signs of drug overdose are convulsions and CNS excitation. Peritoneal dialysis and hemodialysis are ineffective to reduce the concentration of Ceftriaxone. The medicine does not have an antidote.
Therapy: symptomatic.

Interaction

In one volume, it is pharmaceutically incompatible with other antimicrobial agents.
Suppressing the microflora of the intestine, prevents the formation of vitamin K in the body. For this reason, the use of the drug in combination with agents that reduce platelet aggregation (sulphinpyrazone, NSAIDs) can provoke bleeding.
This same feature of Ceftriaxone helps to enhance the effect of anticoagulants when they are used together.
In combination with loop diuretics, the risk of developing nephrotoxicity increases.

Storage conditions

Protect from light. The optimum storage temperature is up to 25 ° C.
When applied without medical control, the drug can provoke complications, so the bottles with powder should be kept out of the reach of children.
Shelf life - 2 years.

special instructions

The drug is used in a hospital. In patients who are on hemodialysis, as well as with simultaneous severe hepatic and renal failure, the plasma concentrations of Ceftriaxone should be monitored.
With long-term treatment requires regular monitoring of the picture of peripheral blood and indicators that characterize the function of the kidneys and liver.
Sometimes (rarely) with ultrasound of the gallbladder, darkening can occur, which indicates the presence of sediment. Darkening disappears after discontinuation of treatment.
Weak patients and elderly patients in a number of cases it is advisable to prescribe in addition to Ceftriaxone vitamin K.
If the balance of water and electrolytes, as well as with arterial hypertension, the level of sodium in the blood plasma should be controlled. If the treatment is prolonged, the patient is shown a general blood test.
Like other cephalosporins, the drug has the ability to displace serum albumin-bound bilirubin, and therefore it is used with caution in newborns with hyperbilirubinemia (and, in particular, in premature infants).
The drug has no effect on the rate of neuromuscular conduction.

Compatibility with alcohol

Do not consume alcohol during treatment with the drug. The combination of "Ceftriaxone + ethanol" can provoke symptoms similar to the symptoms of severe poisoning, and in some cases lead to the death of the patient.

Ceftriaxone in pregnancy and breastfeeding

The drug is contraindicated in the first trimester of pregnancy. If it is necessary to appoint a nursing woman, the child should be transferred to the mixture.
Reviews of Ceftriaxone during pregnancy confirm that the drug really is a very powerful and very effective antibacterial agent that can not only cure the underlying disease, but also prevent the development of its complications.
Given that the drug (like other antibiotics) has side effects, it is prescribed only in cases where the potentially possible complications of the disease can harm more than the use of the drug (in particular, in infections of the urogenital tract, which are very susceptible to pregnant women).

Reviews of Ceftriaxone

Ceftriaxone - reviews of doctors confirm this fact - it is a potent antibiotic that helps to cure the disease in a short time and with a minimum of side effects. It is allowed to be used for children and during pregnancy (except for 1 trimester).
According to the patients themselves, the main disadvantage of the drug is that the injections are very painful.
In responses to Ceftriaxon injections, Emla cream, which is a local anesthetic, is recommended for children to facilitate the procedure of the mother (according to the advice of the attending physician). It is applied for about half an hour to the intended site of the injection.