Tseftriakson

• Structure
• Release form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications to Tseftriakson's use
• Contraindications
• Side effects
• Application instruction of Tseftriakson. What to part Tseftriakson for injections with?
• Overdose
• Interaction
• Terms of sale
• Storage conditions
• Period of validity
• Special instructions
• Analogs
• With alcohol
• At pregnancy and a lactation
• Responses
• With antibiotics

Structure

Is a part of medicine tseftriakson — an antibiotic from a class of cephalosporins (β-laktamny antibiotics of which chemical structure 7-ATsK is the cornerstone).

What is Tseftriakson?

According to Wikipedia, tseftriakson is an antibiotic which bactericidal action is caused by its ability to break synthesis of a peptidoglikan of bacterial cell walls.

Substance represents poorly hydroscopic fine-crystalline powder of yellowish or white color. Rolled into one drug contains 0,25, 0,5, 1 or 2 grams of sterile sodium salt of a tseftriakson.

Release form

Powder 0,25/0,5/1/2 of for preparation:

• solution for and;
• solution for infusional therapy.

Tseftriakson in tablets or syrup is not issued.

Pharmacological action

Bactericidal. Generation drug III from group of antibiotics "Cephalosporins".

Pharmacodynamics and pharmacokinetics

Universal antibacterial agent which mechanism of action is caused by ability to suppress synthesis of a bacterial cell wall. Drug Gram (+) and Gram (-) of microorganisms shows big resistance in the attitude towards the majority β-лактамаз.

It is active in the relation:

• Gram (+) aerobes — St. aureus (including concerning the strains producing a penicillinase) and Epidermidis, Streptococcus (pneumoniae, pyogenes, viridans groups);
• Gram(s) of aerobes — Enterobacter aerogenes and cloacae, Acinetobacter calcoaceticus, Haemophilus influenzae (including concerning the strains producing a penicillinase) and parainfluenzae, Borrelia burgdorferi, Klebsiella spp. (including pneumoniae), Escherichia coli, Moraxella catarrhalis and diplococcuses of the sort Neisseria (including the strains producing a penicillinase), Morganella morganii, vulgar a protea and a protea of mirabilis, Neisseria meningitidis, Serratia spp., some strains of a pyocyanic stick;
• anaerobe bacterias — Clostridium spp. (an exception — Clostridium difficile), Bacteroides fragilis, Peptostreptococcus spp.

In vitro (clinical value remains to unknown) is noted activity concerning strains of the following bacteria: Citrobacter diversus and freundii, Salmonella spp. (including concerning Salmonella typhi), Providencia spp. (including concerning Providencia rettgeri), Shigella spp.; Bacteroides bivius, Streptococcus agalactiae, Bacteroides melaninogenicus.

Steady against Staphylococcus Methicillinum, many strains of Enterococcus (including Str. faecalis) and Streptococcus of group D (including to a tseftriakson) are steady against tsefalosporinovy antibiotics.

Pharmacokinetic parameters:

• bioavailability — 100%;
• Cmax t at Tseftriakson's introduction in/in — at the end of infusion, at introduction intramusculary — 2-3 hours;
• communication with plasma proteins — from 83 to 96%;
• T1/2 at introduction in oil — from 5,8 to 8,7 hours, at in introduction — from 4,3 to 15,7 hours (depending on a disease, age of the patient and a condition of his kidneys).

At adults concentration of a tseftriakson in liquor at introduction of 50 mg/kg in 2-24 hours repeatedly exceeds MOC (minimum overwhelming concentration) for the most widespread causative agents of a meningococcal infection. Drug well gets into liquor at an inflammation of covers of a brain.

Tseftriakson in not changed look is brought:

• kidneys — for 33-67% (newborn babies have this indicator at the level of 70%);
• with bile in intestines (where drug is inactivated) — for 40-50%.

The hemodialysis is inefficient.

Indications to Tseftriakson's use

In the summary it is specified that indications to Tseftriakson's use are the infections caused by bacteria, sensitive to drug. Intravenous infusions and pricks of medicine are appointed for treatment:

• infections of an abdominal cavity (including at an empyema of a gall bladder, an angiocholitis, peritonitis), ENT organs and respiratory tracts (a pleura empyema, pneumonia, bronchitis, abscess of lungs, etc.), bone and joint tissue, soft tissues and skin, an urogenital path (including pyelonephritis, a pyelitis, prostatitis, cystitis, an epididymite);
• epiglottiditis;
• the infected burns/wounds;
• infectious defeats of maxillofacial area;
• bacterial septicaemia;
• sepsis;
• bacterial endocarditis;
• bacterial meningitis;
• syphilis;
• shankroida;
• tick-borne borreliosis (Lyme's illness);
• uncomplicated gonorrhea (including in cases when the disease is caused by microorganisms which allocate a penicillinase);
• salmonellosis / salmonellonositelstva;
• typhoid.

Drug is used also for perioperatsionny prevention and for treatment of patients with the weakened immunity.

What Tseftriakson at syphilis is applied to?

In spite of the fact that at various forms of syphilis drug of the choice is penicillin, its efficiency in certain cases can be limited.

To use of antibiotics cephalosporins resort as to reserve option at intolerance of drugs of group of penicillin.

Valuable properties of drug are:

• existence in its composition of chemicals which possess ability to suppress formation of cellular membranes and mukopeptidny synthesis in walls of cells of bacteria;
• ability to get quickly into bodies, liquids and body tissues and, in particular, into liquor which at patients with syphilis undergoes a set of specific changes;
• possibility of use for treatment of pregnant women.

Medicine in cases when a disease-producing factor is Treponema pallidum as distinctive feature of Tseftriakson — high treponemotsidny activity is the most effective. The positive effect is shown especially brightly at administration of drug in oil.

Treatment of syphilis using drug yields good results not only at early stages of a course of a disease, but also in the started cases: at neurosyphilis, and also at the secondary and latent syphilis.

As Tseftriakson's T1/2 makes about 8 hours, medicine can be applied equally successfully both at stationary, and at the out-patient scheme of treatment. The drug is enough to be administered to the patient of 1 times a day.

For preventive treatment means is entered within 5 days, at primary syphilis — a 10-tidnevny course, the early latent and secondary syphilis are treated in 3 weeks.

At not started neurosyphilis forms to the patient for 20 days enter once 1-2 g of Tseftriakson, at late stages of an illness enter medicine on 1 g/days within 3 weeks then maintain an interval lasting 14 days and within 10 days carry out treatment by a similar dosage.

At acute generalized meningitis and a syphilitic encephalomeningitis the dose is raised to 5 g/days.

Pricks Tseftriakson: from what drug is appointed at quinsy at adults and children?

In spite of the fact that the antibiotic is effective at various damages of a nasopharynx (including at quinsy and at antritis), it is seldom used, as a rule, as choice drug, in particular, in pediatrics.

At quinsy medicine is allowed to be entered through a dropper into a vein or in the form of usual pricks in a muscle. However in most cases to the patient appoint intramuscular injections. Solution is prepared just before use. Ready mix at the room temperature remains stable within 6 hours after preparation.

To children at quinsy Tseftriakson appoint in exceptional cases when acute quinsy is complicated by severe suppuration and inflammatory process.

The suitable dosage is defined by the attending physician.

During pregnancy drug is appointed when antibiotics of group of penicillin are not effective. Though medicine gets through a placental barrier, it has no significant effect on health and fetation.

Treatment of antritis by means of Tseftriakson

At antritis antibacterial agents are drugs of the first line. Completely getting into blood, Tseftriakson is late in the inflammation center in the necessary concentration.

As a rule, medicine is appointed in a combination with Mucolyticums, vasoconstrictors, etc.

How to prick drug at antritis? Usually sick Tseftriakson appoint to enter into a muscle twice a day 0,5-1 g. Before an injection powder is mixed with Lidocaine (preferably to use one-percentage solution) or water for and.

Treatment lasts not less than 1 week.

Contraindications

Tseftriakson do not appoint at the known hypersensitivity to tsefalosporinovy antibiotics or auxiliary components of drug.

Relative contraindications:

• the neonatality period in the presence at the child of a hyperbilirubinemia;
• prematurity;
• renal / liver failure;
• the enteritis, NYaK or colitis associated using antibacterial agents;
• pregnancy;
• lactation.

Side effects of Tseftriakson

Side effects of drug are shown in a look:

• hypersensitivity reactions — eosinophilias, fevers, a skin itch, the small tortoiseshell, hypostases, rash on skin, multiformny (in certain cases malignant) an exudative erythema, a serum disease, an acute anaphylaxis, a fever;
• headache and dizziness;
• oligurias;
• dysfunctions of digestive organs (nausea, vomiting, a meteorism, taste disturbance, stomatitis, diarrhea, a glossitis, forming of a sladzh in a gall bladder and a pseudo-cholelithiasis, a pseudomembranous coloenteritis, dysbacteriosis, a candidiasis and other superinfections);
• disturbances of a hemogenesis (anemia, including hemolitic; lympho-, leucio-, neytro-, trombotsito-, granulocytopenia; trombo-and a leukocytosis, a hamaturia, a basophilia, bleedings from a nose).

If medicine is entered intravenously, the inflammation of a venous wall, and also morbidity on the vein course are possible. Administration of drug in a muscle is followed by morbidity in the place of a prick.

Tseftriakson (pricks and in/in infusion) can also exert impact on laboratory indicators. At the patient the prothrombin time decreases (or increases), activity of an alkaline phosphatase and transaminases of a liver, and also concentration of urea increases, the giperkreatininemiya, a hyperbilirubinemia, a glucosuria develop.

About side effects of Tseftriakson, allow to draw a conclusion that at administration of drug in oil nearly 100% of patients complain of strong morbidity of a prick, some note muscular pain, dizziness, a fever, weakness, an itch and rash.

Pricks are the easiest transferred if to dissolve powder with anesthetic. At the same time it is necessary to take surely samples both on drug, and on anesthetic.

Application instruction of Tseftriakson. What to part Tseftriakson for injections with?

In the instruction of the producer and the reference book Vidal is specified that the drug can be administered in a vein or in a muscle.

The dosage the adult and for children is more senior than 12 years — 1-2 g/days. The antibiotic is entered once or 1 time at 12 o'clock in a half dose.

In especially serious cases, and also if the infection is provoked by the activator, moderately sensitive to Tseftriakson, the dose is raised to 4 g/days.

At gonorrhea single introduction to a muscle of 250 mg of drug is recommended.

In the preventive purposes before the infected or allegedly infected operation depending on degree of danger of infectious complications the patient in 0,5-1,5 hours prior to surgical intervention should enter 1-2 g of Tseftriakson once.

For children of the first 2 weeks of life medicine is entered by 1 rubles/days. The dose is calculated on a formula of 20-50 mg/kg/days. The highest dose — 50 mg/kg (that is connected with underdevelopment of fermental system).

The optimum dosage to children till 12 flyings (including babies) is also selected depending on weight. The daily dose varies ranging from 20 to 75 mg/kg. To children whose weight more than 50 kg, Tseftriakson appoint in the same dose, as the adult.

The dose exceeding 50 mg/kg should be entered in the form of intravenous infusion lasting at least 30 minutes.

At bacterial meningitis treatment begin 100 mg/kg/days with single introduction. The highest dose — 4 g. As soon as it is allocated the activator and its sensitivity to drug is defined, the dose is reduced.

(In particular, about its use for children) allow to draw a conclusion on drug that means is very effective and available, but its essential shortcoming is strong morbidity in the place of a prick. As for side effects, them, according to patients it is, no more, than when using any other antibiotic.

How many days to prick drug?

Duration of treatment depends on what pathogenic microflora caused a disease, and also from features of a clinical picture. If the activator are Gram (-) diplococcuses of the sort Neisseria, the best results manage to be achieved in 4 days if sensitive to enterobakteriya drug — in 10-14 days.

Tseftriakson's pricks: application instruction. What to dilute drug with?

For cultivation of an antibiotic Lidocaine solution (1 or 2%) or water for injections are used (for and).

When using water for it is also necessary to consider that injections of drug in oil are very painful therefore if solvent is water, unpleasant feelings will be as during a prick, and some time after it.

Water for cultivation of powder is taken usually when use of Lidocaine is impossible because of existence at the patient of an allergy to it.

Optimal variant — one-percentage solution of Lidocaine. For and it is better to use water as a supportive application, at drug cultivation by Lidocaine of 2%.

Whether it is possible to part with Novocaine Tseftriakson?

Novocaine when using it for cultivation of drug reduces activity of an antibiotic, along with it increasing probability of development in a sick acute anaphylaxis.

If to make a start from responses of patients, then in them it is noted that Lidocaine is better, than Novocaine, kills pain at Tseftriakson's introduction.

Besides, use not of freshly cooked solution of Tseftriakson with Novocaine, promotes strengthening of pain during an injection (solution keeps stability within 6 hours after preparation).

How to part Tseftriakson Novokainom?

If as solvent nevertheless Novocaine is used, it on 1 g of drug is taken of 5 ml. If to take smaller amount of Novocaine, powder can be dissolved not completely, and the hypodermic needle will be hammered with medicine lumps.

Cultivation by Lidocaine of 1%

For an injection in a muscle of 0,5 g of drug dissolve in 2 ml of one-percentage solution of Lidocaine (contents of one ampoule); on 1 g of drug take 3,6 ml of solvent.

The dosage of 0,25 g is parted similar to that, as well as 0,5 g, that is contents of 1 ampoule of 1% of Lidocaine. After that ready solution is gathered in different syringes on a half of volume in everyone.

Medicine is entered deeply into a gluteus (no more than 1 g in each buttock).

The drug divorced Lidocaine is not intended for intravenous administration. It is allowed to be entered strictly into a muscle.

How to part Tseftriakson Lidokainom's pricks of 2%?

For cultivation of 1 g of drug take 1,8 ml of water for and and two-percent Lidocaine. To part 0,5 g of drug, also mix 1,8 ml of Lidocaine from 1,8 ml of water for and, but for dissolution use only a half of the turned-out solution (1,8 ml). For cultivation of 0,25 g of drug take 0,9 ml of the solvent prepared similarly.

Tseftriakson: how to part to children for intramuscular introduction?

The given technique of carrying out intramuscular injections is practically not used in pediatric practice as Tseftriakson with novocaine can cause the strongest acute anaphylaxis in the child, and in a combination with lidocaine — can promote developing of spasms and disturbance of cardiac performance.

For this reason optimum solvent in case of use of drug for children is usual water for and. The impossibility of use of anesthetic at children's age demands slower and accurate introduction of medicine to lower pain during a prick.

Cultivation for in/in introductions

For in/in introductions of 1 g of drug dissolve in 10 ml of the distilled water (sterile). The drug is administered slowly within 2-4 minutes.

Cultivation for intravenous infusion

When carrying out infusional therapy the drug is administered during at least half an hour. For preparation of solution of 2 g of powder part in 40 ml of solution, free from Ca: Dextrosums (5 or 10%), NaCl (0,9%), fructose (5%).

In addition

Tseftriakson is intended only for parenteral administration: producers do not let out a tablet and suspension for the reason that an antibiotic contacting to body tissues, shows high activity and strongly irritates them.

Doses for animals

The dosage for cats and for dogs is selected taking into account the body weight of an animal. As a rule, it makes 30-50 mg/kg.

If the bottle of 0,5 g is used, it is necessary to enter into it 1 ml of two-percent Lidocaine and 1 ml of water for and (or 2 ml of Lidocaine of 1%). Having intensively stirred up medicine before full dissolution of lumps, he is taken in the syringe and entered to a sick animal into a muscle or under skin.

The dosage to a cat (Tseftriakson of 0,5 g is usually used for small animals — for cats, kittens, etc.) if the doctor appointed to 1 kg of weight to enter 40 mg of Tseftriakson, makes 0,16 ml/kg.

For dogs (and other large animals) bottles take 1 g. Solvent take of 4 ml (2 ml of Lidocaine of 2% + 2 ml of water for and). The dog weighing 10 kg if the dose makes 40 mg/kg, needs to enter 1,6 ml of ready solution.

In need of Tseftriakson's introduction in/in through a catheter for cultivation use the sterile distilled water.

Overdose

Signs of overdose of drug are spasms and excitement of TsNS. The peritoneal dialysis and a hemodialysis are inefficient for decrease in concentration of Tseftriakson. Medicine has no antidote.

Therapy: symptomatic.

Interaction

In one volume pharmaceutical it is incompatible with other antimicrobic means.

Suppressing intestinal microflora, interferes with education in a vitamin K organism. For this reason use of drug in a combination with means which reduce aggregation of thrombocytes (Sulfinpyrazonum, NPVP) can provoke bleeding.

The same feature of Tseftriakson promotes strengthening of effect of anticoagulants at their combined use.

In combination with loopback diuretics the risk of development of nephrotoxicity increases.

Terms of sale

Acquisition requires the recipe in Latin.

The recipe on Latin (sample):
Rp.: Ceftriaxoni 0,5
D.t.d.N.10
S. In the enclosed solvent. In oil, 1 ruble/days.

Storage conditions

To protect from light. Optimum temperature of storage — to 25 °C.

At use without medical control drug can provoke complications therefore bottles with powder should be held in unavailable to children, the place.

Period of validity

2 years.

Special instructions

Drug is used in the conditions of a hospital. At patients who are on a hemodialysis and also at a simultaneous heavy liver and renal failure, it is necessary to keep indicators of plasma concentration of Tseftriakson under control.

At prolonged treatment regular supervision over a picture of peripheral blood and the indicators characterizing function of kidneys and a liver is required.

(Seldom) at ultrasonography of a gall bladder blackouts which indicate existence of a deposit can sometimes be noted. Blackouts disappear after the termination of a course of treatment.

In some cases it is reasonable to the weakened patients and elderly patients to appoint vitamin K in addition to Tseftriakson.

At disturbance of balance of water and electrolytes, and also at arterial hypertension it is necessary to control sodium level in a blood plasma. If prolonged treatment, is shown to the patient carrying out the general blood test.

As well as other cephalosporins, drug possesses ability to force out the bilirubin connected with a seralbumin in this connection it with care is applied at newborns with a hyperbilirubinemia (and, in particular, at premature children).

Drug does not exert impact on the speed of neuromuscular conductivity.

Tseftriakson's analogs: what it is possible to replace drug with?

Tseftriakson's analogs in pricks: Tseftriakson-LEKSVM (Kabi, Dzhodas, KMP, Pro-honey, Vial, Elf), Tseftriabol, Tsefson, Tsefakson, Torotsef, Hizon, Tsefogram, Medakson, Lorakson, Ifitsef.

Analogs in tablets: Pantsef, Supraks Solyutab, Tseforal Solyutab, Tsefpotek, Spektratsef.

Tseftriakson or Cefazolin — what is better?

Both drugs belong to Tsefalosporiny group, but Tseftriakson is an antibiotic of the III generation, and Cefazolin is a drug I of generation.

Important feature of tsefalosporinovy antibiotics of the I generation is that they are not effective concerning listeriya and enterococci, have a narrow action spectrum and low level of activity in the relation Gram (-) of bacteria.

Cefazolin is applied generally in surgery to perioperatsionny prevention, and also to treatment of infections of soft tissues and skin.

Appointment it for treatment of infections of urinogenital system and a respiratory path cannot be considered as reasonable that is connected with a narrow range of antimicrobic activity and high resistance to it among potential activators.

That it is better: Tseftriakson or Tsefotaksim?

Tsefotaksim and Tseftriakson are basic antimicrobic means of group of cephalosporins III of generation. Drugs are almost identical on the bactericidal properties.