Zinnat - instructions for use, dose, side effects, contraindications

Component	Quantity in% (w / w)	Quantity in one dose (g / 5 ml)
Active substance:
Cefuroxime axetil¹	3,55³	0,150²
Excipients:
Stearic acid¹	20,19	0,852
Sucrose	72,56	3,062
Flavor of tutti-frutti	2,37	0,100
Acesulfame potassium	0,50	0,021
Aspartame	0,50	0,021
Povidon-KZO	0,31	, 0,013
Xanthan gum	0,02	0,001

1. Cefuroxime axetil and stearic acid are present as a complex of stearic acid - cefuroxime axetil 15% (SACA), the amount of which depends on the quantitative content of cefuroxime axetil in the original substance.

2. Equivalent to 125 mg of cefuroxime.

3. Equivalent to 2.96% (w / w) of cefuroxime.

Description:

The granules are white or almost white in color. When diluted, a suspension is formed from white to light yellow with a characteristic fruity odor.

Pharmacotherapeutic group:Antibiotic-cephalosporin

ATX: & nbsp

J.01.D.C.02 Cefuroxime

Pharmacodynamics:

Mechanism of action

Cefuroxime Axstile is a prodrug of cefuroxime, an antibiotic of the second generation cephalosporins group with bactericidal action. Cefuroxime is active against a wide range of pathogens, including strains producing beta-lactamases. Cefuroxime has resistance to the action of bacterial ß-lactamases, therefore it is effective against ampicillin-resistant or amoxicillin-resistant strains. The bactericidal effect of cefuroxime is associated with the suppression of bacterial cell wall synthesis as a result of binding to the main target proteins.

Pharmacodynamic effects

The prevalence of acquired bacterial resistance to cefuroxime varies depending on the region and over time, in certain types of microorganisms, resistance can be very high. It is preferable to have local sensitivity data, especially when treating severe infections.

Cefuroxime is usually active in vitro against the following microorganisms:

Bacteria, usually sensitive to cefuroxime

Gram-positive aerobes

Staphylococcus aureus (strains sensitive to methicillin)¹

Koagulazonegatnvnye staphylococci (strains sensitive to methicillin)

Streptococcus pyogenes¹

Beta-hemolytic streptococci

Gram-negative aerobes

Haemophilus influenzae¹, including ampicillin-resistant strains

Haemophilus parainfluenzae¹

Moraxetla catarrhalis¹

Neisseria gonorrhoeae¹, including strains that produce and do not produce penicillinase

Gram-positive anaerobes

Peptostreptococcus spp.

Propionibacterium spp.

Spirochetes

Barrelia burgdorferi^¹

Bacteria for which it is probable acquired resistance to cefuroxime

Gram-positive aerobes

Streptococcus pneumoniae^¹

Gram-negative aerobes

Citrobacter spp., with the exception of C. freundii

Enterobacter spp., with the exception of E. aerogenes and E. cloacae

Escherichia coli¹

Klebsiella spp., including Klebsiellapneumoniae¹

Proteus mirabilis

Proteus spp., with the exception of P. penneri andP. vulgaris

Providencia spp.

Gram-positive anaerobes

Clostridium spp., with the exception of C. difficile

Gram-negative anaerobes

Bacteroides spp., with the exception of AT. fragilis

Fusobacterium spp.

Bacteria possessing natural resistance to neuroxime

Gram-positive aerobes

Enterococcus spp., including E. faecal is and E. faecium

Listeria monocytogenes

Gram-negative aerobes

Acinetobacter spp.

Burkholderia cepacia

Campylobacter spp.

Citrobacter freundii

Enterobacter aerogenes

Enterobacter cloacae

Morganella morganii

Proteus penneri

Proteus vulgaris

Pseudomonas spp., including Pseudomonas aeruginosa

Serratia spp.

Stenotrophomonas maltophilia

Gram-positive anaerobes

Clostridium difficile

Gram-negative anaerobes

Bacteroides fragilis

Other

Chlamydia spp.

Mycoplasma spp.

Legionella spp.

¹ - for these bacteria, the clinical efficacy of cefuroxime has been demonstrated in clinical studies.

Pharmacokinetics:

Suction

Optimal absorption is achieved when taking the drug while eating.

The maximum serum concentrations of cefuroxime (2.1 mg / L for a dosage of 125 mg, 4.1 mg / L for a dosage of 250 mg,7.0 mg / L for a dosage of 500 mg) are observed after about 2-3 hours when taking the drug in a tablet dosage form with food. The rate of absorption of cefuroxime from the suspension is lower than that of tablets, so the maximum serum drug concentrations are lower, and systemic bioavailability is also reduced (by 4-17%).

After ingestion of cefuroxime, the auxetil is absorbed from the gastrointestinal tract and rapidly hydrolyzed in the mucosa of the small intestine and in the blood with the release of cefuroxime.

Distribution

With proteins of blood plasma, 33-50% of the drug binds and depends on the technique of determination.

Metabolism

Cefuroxime is not metabolized.

Excretion

The half-life is 1-1.5 hours. Cefuroxime Excreted by glomerular filtration and tubular secretion. With simultaneous administration of probenecid, the area under the concentration-time curve increases by 50%.

Patients with impaired renal function

The pharmacokinetics of cefuroxime were studied in patients with renal dysfunction of varying severity. The half-life of cefuroxime increases as the function of the kidneys decreases, which is the basis for the recommendations for correcting the dosing regimen for this group of patients (see the section "Dosing and Administration").In patients on hemodialysis, at least 60% of the total amount of cefuroxime present in the body at the time of onset of dialysis will be removed within a 4-hour dialysis period. Thus, an additional single dose of cefuroxime should be administered after completion of the hemodialysis procedure.

Indications:

The drug is indicated for the treatment of infectious and inflammatory diseases caused by bacteria susceptible to cefuroxime:

- upper respiratory tract infections, ENT organs, such as otitis media, sinusitis, tonsillitis and pharyngitis;

- infections of the lower respiratory tract, for example, pneumonia, acute bacterial bronchitis and exacerbation of chronic bronchitis;

- urinary tract infections, such as pyelonephritis, cystitis and urethritis;

- infections of the skin and soft tissues, for example, furunculosis, pyoderma and impetigo;

- gonorrhea, acute uncomplicated gonorrhea urethritis and cervicitis;

- treatment of borreliosis (Lyme disease) in the early stages and prevention of late stages of the disease in adults and children over 12 years.

The sensitivity of bacteria to neuroxime varies depending on the region and over time.Wherever possible, local sensitivity data should be taken into account (see section "Pharmacological properties").

Contraindications:

- Hypersensitivity to cephalosporin antibiotics, penicillins, carbapenems and aspartame;

- phenylketonuria;

- Children's age is up to 3 months.

Carefully:With caution should be used for kidney failure, diseases of the gastrointestinal tract (including in the history and with ulcerative colitis), pregnancy, lactation.

Pregnancy and lactation:

Pregnancy

There is no experimental evidence of embryopathic and teratogenic effects of cefuroxime axetil, but as with other medications, it should be carefully administered during the first months of pregnancy:

Lactation

Cefuroxime excretes in breast milk - so caution should be exercised when prescribing it to lactating women.

Dosing and Administration:

The standard course of therapy is about 7 days (from 5 to 10 days). For optimal absorption, the Zinnat suspension® should be taken with food.

Adults

With most infections	- 250 mg twice a day day
With infections urogenital systems (cystitis, urethritis)	- 125 mg twice at day
When pyelonephritis	- 250 mg twice at day
With infections lower divisions respiratory pathways of light and medium gravity, eg bronchitis	- 250 mg twice at day
With more heavy infections lower divisions respiratory paths or suspicion of pneumonia	- 500 mg twice at day
When uncomplicated gonorrhea	- 1 g once
In case of illness	- 500 mg twice
Lyme in adults	at day during
and children over 12	20 days
years

Special patient groups

Children

No clinical trial data available regarding the use of the drug Zinnat ® in children younger than 3 months. If a fixed dose is preferred, then for most infections it is recommended to take 125 mg twice a day day. Children aged 2 years and older with otitis media or with more severe infections are prescribed 250 mg twice a day day; the maximum daily dose is 500 mg. When treating children, it may be necessary to calculate the dose depending on body weight and age. For most infections, the dose for children aged 3 months to 12 years is 10 mg / kg twice a day day, but not more than 250 mg per day.With otitis media and heavier infections, the recommended dose is 15 mg / kg twice a day day, but not more than 500 mg per day.

The following tables show the dose, depending on the age and body weight child for dosing a suspension of Zinnat® 125 mg / 5 mL with a 5-ml measuring spoon attached to the package.

Dose at the rate of 10 mg / kg body weight,

prescribed for most infections

Age		Weight		One-time	Number
		body weight (kg) (approx.mately)		dose (mg) at admission 2 times in day	dimensional spoons (5 ml) in one dose
3 months -		4-6		40-60	1/2
6 months
6 months - 2 years		6-12		60-120	1/2-1
2 years -	from 12 and		125		1
12 years	more than 20

Dose at the rate of 15 mg / kg body weight, prescribed for otitis media and more serious infections

Age	Weight bodies (kg) (Prib)liziticular)	One-time dose (mg) at admission 2 times in day	Number dimensional spoons (5 ml) in one dose
3 months -	4-6	60-90	1/2
6 months
6 months -	6-12	90-180	1-1, 1/2
2 years
2 years - 12 years	from 12 and more 20	180-250	1 ,1/2-2

Cefuroxime is also available as a sodium salt (Zinacef® preparation) for parenteral administration. This allows you to switch from parenteral administration of cefuroxime to oral administration in the presence of clinical indications.

Patients with impaired renal function

The excretion of cefuroxime occurs mainly by the kidneys.

It is recommended to reduce the dose cefuroxime in patients with severe renal dysfunction to compensate for delayed excretion (see table below).

Creatinine clearance	T1 / 2 (hours)	Recommended dose
> 30 ml / min	1,4- 2,4	No dose adjustment is required.
10-29 ml / min	4,6	The standard single dose every 24 hours.
<10 ml / min	16,8	The standard single dose is every 48 hours.
During hemodialysis	2-4	At the end of each dialysis session, take one additional standard single dose.

Method of preparing the suspension

- Shake the vial of granules several times.

- Pour 20 ml of water into the measuring cup to the mark (this amount of water is sufficient to prepare a 50 ml slurry).

- Pour the measured amount of water into the vial and close the vial with a lid.

- Turn the vial over and vigorously shake it (about 1.5 minutes) to mix the preparation well.

Turn the bottle back to its original position and shake vigorously. Before each use of the drug should be vigorously shaken vial with suspension.

When taking the drug in each serving of the suspension, you can add cold fruit juice or milk, and this slug should be used immediately. Do not dilute the entire volume of the suspension with juice or milk immediately.

Side effects:

The undesirable reactions presented below are listed in accordance with the damage to organs and organ systems. Frequency of occurrence is defined as follows: very often (> 1/10),

often (≥ 1/100 and <1/10), infrequently (≥1 / 1,000 and <1/100), rarely (≥1 / 10,000 and <1/1 000), very rarely (<1/10 000 , including individual cases). Frequency categories were formed on the basis of clinical studies of the drug and post-registration surveillance.

Frequency of occurrence of undesirable reactions

Infectious and parasitic diseases

Often: excessive growth of fungi of the genus Candida.

Violations of the blood and lymphatic system

Often: eosinophilia.

Infrequent: positive Coombs test, thrombocytopenia, leukopenia (sometimes pronounced).

Very rarely: hemolytic anemia.

Cephalospores are absorbed on the surface of the cell membrane of erythrocytes, binding to antibodies to cephalosporins, which leads to a positive result of the Coombs test (which may affect cross-compatibility) and, in very rare cases, hemolytic anemia.

Disturbances from the nervous system

Often: headache, dizziness.

Disorders from the gastrointestinal tract

Often: gastrointestinal disorders, including diarrhea, nausea, abdominal pain.

Infrequently: vomiting.

rarely: pseudomembranous colitis (see section "Special instructions").

Disturbances from the liver and bile ducts

Often: a temporary increase in the level of liver enzymes ALT (alanine aminotransferase), ACT (aspartate aminotransferase), LDH (lactate dehydrogenase).

Rarely: jaundice (mostly cholestatic), hepatitis.

Violations from the skin and subcutaneous tissue

Rarely: erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (exanthematous necrolysis) (see also "Immune system disorders").

Violations from the immune system

Reactions hypersensitivity, including:

Infrequently: skin rash.

Rarely: hives, itching.

Rarely: drug fever, serum sickness and anaphylaxis.

Overdose:

Symptoms

Overdose of cephalosporins can cause increased excitability of the central nervous system with the development of seizures.

Treatment

Symptomatic. The serum level of cefuroxime can be reduced by hemodialysis and peritoneal dialysis.

Interaction:

Drugs that reduce the acidity of gastric juice can cause a decrease in the bioavailability of the Zinnat® suspension.

Like many antibiotics, Zinnat® may affect the gut flora, leading to lower estrogen reabsorption and, therefore, reduce the effectiveness of combined oral contraceptives. Simultaneous treatment with the "loop" diuretics slows tubular secretion and reduces renal clearance, increases the concentration in plasma and increases the half-life of cefuroxime. Simultaneous administration of cefuroxime and probenecid results in an increase of 50% in the area of cefuroxime under the pharmacokinetic curve. With simultaneous administration with aminoglycosides and diuretics, the risk of nephrotoxic effects increases.

In patients receiving cefuroxime axetil, a test with iron-sulphide potassium can give a false-negative result. Such patients are recommended to use methods using glucose oxidase or hexokinase to determine blood glucose.

Cefuroxime does not affect the results of determining the level of creatinine by an alkaline-picrate method.

Special instructions:

Care should be taken when prescribing patients with allergic reaction to cephalosporins, penicillins or carbapenems in the anamnesis.As with other antibiotics, the administration of cefuroxime axetil can lead to excessive growth of fungi of the genus Candida. Long-term use may cause the growth of other resistant microorganisms (e.g., enterococci and Clostridium difficile), which may require discontinuation of treatment. Cases of occurrence pseudomembranous colitis when taking antibiotics, the severity of which can range from mild to life-threatening. Therefore, a differential diagnosis of pseudomembranous colitis in patients with diarrhea that occurred during or after a course of antibiotic treatment. If diarrhea is prolonged or severe, or the patient experiences abdominal cramps, treatment with Zinnat® should be stopped immediately and the patient should be examined. It is necessary to take into account the content of sucrose in the preparation in the treatment of patients with diabetes mellitus. Patients should be given appropriate recommendations.

The prepared suspension of Zinnat® contains aspartame, which is source of phenylalanine (see section "Contraindications").

In the treatment of Zinnat® with Lyme disease, the occurrence of the Yarisch-Gersheimer reaction is possible, which is due to the bactericidal activity of the drug against the causative agent of the spirochete Borrelia burgdorferi. Patients should be informed that these symptoms are a typical consequence of the use of antibiotics in this disease, which occurs spontaneously. 5 ml of the prepared suspension of Zinnat® contains 0.25 bread units (XE).

Effect on the ability to drive transp. cf. and fur:Since cefuroxime axetil may cause dizziness, it is necessary to warn patients about precautions when driving a vehicle or working with moving machinery.

Form release / dosage:Granules for oral suspension, 125 mg / 5 ml.

Packaging:Vials of dark glass sealed with a membrane and closed with a screwed plastic lid with a device against opening the bottle by children. For 1 bottle together with a measuring cup, measuring spoon and instructions for medical use in a cardboard pack.

Storage conditions:

At a temperature of no higher than 30 ° C.

The prepared suspension should be stored in the refrigerator at a temperature of 2-8 ° C for not more than 10 days.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date stated on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N008779

Date of registration:28.06.2010 / 18.05.2012

Expiration Date:Unlimited

The owner of the registration certificate:GlaxoSmithKline Trading, ZAO GlaxoSmithKline Trading, ZAO Russia

Manufacturer: & nbsp

GLAXO OPERATIONS UK, Limited United Kingdom

Representation: & nbspGlaxoSmithKline Trading, ZAOGlaxoSmithKline Trading, ZAO

Information update date: & nbsp14.10.2017

Illustrated instructions

Instructions

Zinnat® (Zinnat®)