Ceftriaxone

Ceftriaxone is a 3rd generation cephalosporin antibiotic. It has bactericidal properties that develop when the membrane binding of bacterial cells is slowed down.

The drug acetylates transpeptidases associated with the walls, while destroying the cross-peptidoglycan cross-linking, which helps strengthen the strength of the cell walls. The drug demonstrates a large range of antimicrobial effects, which includes a variety of anaerobic bacteria with aerobes, as well as gram-positive and negative bacteria.

[1], [2], [3], [4], [5], [6], [7], [8], [9]

Indications Ceftriaxone

Used for such disorders:

• respiratory tract infections (for example, the development of pneumonia);
• lesions of the upper respiratory tract;
• diseases associated with the urethra, kidneys and genitals (among them gonorrhea);
• meningitis ;
• infection of the subcutaneous layer and epidermis;
• abnormalities in the peritoneal organs (for example, peritonitis);
• infections in people with reduced immunity;
• GVH lesions;
• infections affecting bones with joints;
• wound injuries;
• sepsis (common infection);
• disseminated tick-borne borreliosis (early or late stages of pathology).

In addition, it is prescribed to prevent the appearance of infections after operations in the field of gastrointestinal diseases, urethra, digestive or gynecological organs (only with possible or diagnosed contamination).

[10], [11], [12], [13]

Release form

The release of the therapeutic substance is in the form of an injection lyophilisate - 500 or 1000 mg.

[14], [15], [16], [17], [18], [19], [20], [21]

Pharmacodynamics

The drug demonstrates the effect on such microbes: streptococci from categories A, B and C, and in addition G, epidermal staphylococci, pneumococci and Staphylococcus aureus with enterobacteria. In addition, the list includes bacteria Morgana, E. Coli, Klebsiella with chopsticks influenza, moraxella cataris and H.parainfluenzae. At the same time, the drug acts on salmonella, meningococci, common protea with gonococci, providence, yersinia, serration with pale treponema and shigella. In addition, acinetobacteria, peptococci, citrobacteria with bacteroids, fuzobakterii, peptostreptokokki, clostridia, Aeromonas spp. And actinomycetes.

[22], [23], [24], [25], [26], [27],

Pharmacokinetics

The injected substance is absorbed completely and at high speed. Bioavailability values are almost 100%. Plasma Cmax values are recorded after 90 minutes. Reversibly synthesized with plasma albumin - 85-95%.

Medication stays inside the body for a long time. At the minimum level for the development of antimicrobial effects, the substance is determined inside the blood for 24 hours. Without complications, it passes inside the bone tissues, organs and fluids (synovia, pleural and peritoneal).

The term half-life is 5.8-8.7 hours; it is significantly prolonged in people older than 75 years of age (16 hours), as well as children (6.5 days) and newborns (up to 8 days).

Excreted together with the urine in the active form (about 50% for 48 hours). Part of the drug is excreted in the bile. In case of insufficiency of the kidneys, the rate of excretion is reduced, due to which the drug can accumulate inside the body.

[28], [29], [30], [31], [32], [33], [34], [35], [36], [37], [38]

Dosing and administration

The drug is administered intravenously or intramuscularly. Before starting therapy, it is required to exclude the presence of intolerance by performing a skin test.

Adolescents older than 12 years old and weighing more than 50 kg, as well as adults, need to be administered 1-2 g of medication 1 time per day (with 24-hour intervals). In the case of a weak effect of a drug or a severe form of infection, the daily portion may be increased to 4000 mg.

Newborns before the 14-day period (also premature) need to be administered 20-50 mg / kg 1 time per day. Infants older than 2 weeks of age and children under 12 years of age use 20-80 mg / kg of the substance 1 time per day.

A portion of 50+ mg / kg is administered intravenously via infusion (the procedure lasts at least half an hour).

It is necessary to continue treatment with an antibiotic for another 48-72 hours after the normalization of temperature and the results of laboratory tests.

[48], [49], [50]

Use Ceftriaxone during pregnancy

Ceftriaxone can pass through the placenta, but the safety of its use in pregnancy has hardly been studied.

The active drug element in small quantities is excreted with the mother's milk, which is why breastfeeding is canceled during therapy.

[39], [40], [41], [42], [43], [44], [45]

Contraindications

It is contraindicated to use medication for intolerance against cephalosporins (if hypersensitivity to penicillins is noted, the likelihood of cross-exposure should be taken into account).

[46], [47]

Side effects Ceftriaxone

The main side signs are:

• infectious lesions: mycosis, covering the genitals, fungal infections of a secondary nature and infections that are provoked by the activity of resistant microbes;
• lymphatic and blood dysfunction: leuko-, thrombocyto or granulocytopenia, eosinophilia, elevated PTV values, hemolytic anemia, agranulocytosis, coagulation disorders and increased creatinine levels;
• digestive problems: glossitis, blockage of gallstones, diarrhea, pancreatitis, stomatitis and nausea. Occasionally enterocolitis pseudomembranous character (triggered by clostridium differential activity) develops;
• impaired hepatobiliary function: cholelithiasis, deposits of Ca salts inside the gallbladder and an increase in blood values of liver enzymes (ALT, alkaline phosphatase and AST);
• lesions of the subcutaneous layers and the epidermis: edema, erythema polyforme, rash, exanthema, PETN, urticaria, dermatitis of allergic origin and itching;
• problems with urinary function: hematuria, oliguria, kidney failure, glucosuria and the formation of calculi inside the kidneys;
• systemic disorders: headache, fever, chills, anaphylactoid or anaphylactic symptoms, and dizziness;
• local manifestations: sometimes inflammation of the venous wall occurs. This violation can be avoided by injecting the drug in the i / m way at low speed (for 2-4 minutes). It must be taken into account that intramuscular administration without the use of lidocaine will be extremely painful;
• Changing laboratory test data: False positive Coombs test. Like other antibiotics, ceftriaxone can lead to a false positive test for galactosemia and for detection of sugar inside urine. Because of this, during the period of therapy, glucosuria must be determined using an alternative enzyme method.

Overdose

With Ceftriaxone intoxication, hemodialysis or peritoneal dialysis does not give results. The drug has no antidote. In case of poisoning, symptomatic medical measures are performed.

[51], [52], [53], [54], [55], [56]

Interactions with other drugs

Does not possess pharmaceutical compatibility with vancomycin, aminoglycosides, amsacrine, and also fluconazole.

Bacteriostatic type antibiotics weaken the ceftriaxone bactericidal activity.

In vitro studies have revealed antagonism between the drug and chloramphenicol.

Combination with NSAIDs and other substances that slow platelet aggregation, increases the risk of bleeding.

The drug may reduce the therapeutic effect of hormonal contraceptives. When using Ceftriaxone and for a month after the end of therapy, non-hormonal contraceptives should be used additionally.

The combination of large portions of medication with potent diuretics (for example, with furosemide) does not lead to the appearance of disorders of the renal function.

It does not have drug compatibility with solutions that contain other antibiotics.

It is forbidden to dilute the drug in solutions containing the element Ca (among those of Hartmann or Ringer). When they interact can form insoluble substances. You can not mix the drug with fluids for parenteral nutrition, which include Ca. Also, they can not be prescribed in combination, regardless of the age of the patient. You can not enter them through different in / in the application system.

[57], [58], [59], [60], [61], [62], [63]

Storage conditions

Ceftriaxone is required to be stored in a dry place closed to small children. Temperature indicators - no more than 25 ° C.

[64], [65], [66], [67], [68], [69]

Shelf life

Ceftriaxone is allowed to apply for a 2-year term since the release of the therapeutic substance.

[70], [71], [72], [73]

Application for children

It is forbidden to prescribe to premature babies (until the 41st week - both the gestational period and the period from the moment of birth are taken into account) and in the case of hyperbilirubinemia in the newborn (especially premature), because the drug can displace bilirubin from albumin synthesis, which is why bilirubin-induced encephalopathy appears.

It cannot be used for intravenous injection with calcium-containing fluids in newborns under the age of 28 days (also when administered by the parenteral method). This is due to the high probability of precipitation of the Ca salts of the drug.

[74], [75], [76], [77], [78], [79], [80], [81], [82], [83], [84], [85], [86]

Analogs

Analogs of drugs are drugs Hazaran and Rocetin with Lendazin.

[87], [88], [89], [90], [91], [92], [93], [94], [95], [96]

Reviews

Ceftriaxone is now considered a fairly popular drug. Patients in their reviews mainly note the qualitative effect of the drug, which allows to quickly alleviate the state of health immediately from the first day of treatment.

Of the minuses, most comments mention a very strong painfulness of the injections performed - both during the procedure itself and for some time after its completion. In the case of intravenous administration, pain is observed along the vein.

[97], [98], [99], [100], [101], [102], [103], [104], [105]