Zinnat
Producer: Glaxo Operetaions UK Limited (Glakso Opereyshns YuK Limited) Great Britain
Code of automatic telephone exchange: J01DC02
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Tablets, film coated white or almost white color, oval, biconvex, on the one hand "GXES5" is engraved; on cross section - a kernel of white or almost white color.
Active ingredient: a tsefuroksima aksetit 150.36 mg,
what corresponds to the maintenance of a tsefuroksim of 125 mg
Excipients: cellulose microcrystallic - 47.51 mg, croscarmellose sodium - 20 mg, sodium lauryl sulfate - 2.25 mg, the vegetable oil hydrogenated - 4.25 mg, silicon dioxide colloid - 0.63 mg.
Structure of a film cover: a gipromelloza - 5.55 mg, propylene glycol - 0.33 mg, methylparahydroxybenzoate - 0.06 mg, пропилпарагидроксибензоат - 0.04 mg, dye opaspry - 1.52 mg (a gipromelloza of 3%, titanium dioxide of 36%, Natrium benzoicum of 0.1%).
Tablets, film coated white or almost white color, oval, biconvex, on the one hand "GXES7" is engraved; on cross section - a kernel of white or almost white color.
Active ingredient: a tsefuroksima aksetit 300.72 mg,
what corresponds to the maintenance of a tsefuroksim of 250 mg
Excipients: cellulose microcrystallic - 95.03 mg, croscarmellose sodium - 40 mg, sodium lauryl sulfate - 4.5 mg, the vegetable oil hydrogenated - 8.5 mg, silicon dioxide colloid - 1.25 mg.
Structure of a film cover: a gipromelloza - 7.4 mg, propylene glycol - 0.44 mg, methylparahydroxybenzoate - 0.07 mg, пропилпарагидроксибензоат - 0.06 mg, dye opaspry - 2.03 mg (a gipromelloza of 3%, titanium dioxide of 36%, Natrium benzoicum of 0.1%).
Granules for preparation of suspension for intake in the form of grains of irregular shape, various size, but no more than 3 mm, white or almost white color; at cultivation suspension from white till light yellow color with a characteristic fruit smell is formed.
Active ingredient: a tsefuroksima aksetit 150 mg,
what corresponds to the maintenance of a tsefuroksim of 125 mg
Excipients: stearic acid - 852 mg, sucrose - 3.062 g, tutti-frutt fragrance - 100 mg, to potassium atsesulfa - 21 mg, aspartame - 21 mg, K30 povidone - 13 mg, gum xanthane - 1 mg.
Pharmacological properties:
Tsefuroksima aksetit is a predecessor of a tsefuroksim who treats tsefalosporinovy antibiotics of the II generation. Tsefuroksim is active concerning a wide range of activators, including the strains producing β-lactamelements. Tsefuroksim has resistance to action bacterial β-лактамаз therefore ampicillin - resistant or amoxicillin - resistant strains is effective in the relation.
Bactericidal action of a tsefuroksim is connected with suppression of synthesis of a cell wall of bacteria as a result of linkng with the main proteins targets.
In vitro tsefuroksy is active concerning the following microorganisms: gram-negative aerobes (Haemophilus influenzae / including ampicillin - resistant strains/, Haemophilus parainfluenzae, Moraxella catarrhalis, Neisseria gonorrhoeae / including the strains which are producing and not producing a penicillinase/, Escherichia coli, Klebsiella spp., Proteus mirabilis, Providencia spp., Providencia rettgeri; gram-positive aerobes (Staphylococcus aureus / including the strains producing a penicillinase, but excepting Methicillinum - resistant strains/, Staphylococcus epidermidis / including the strains producing a penicillinase, but excepting Methicillinum - resistant strains/, Streptococcus pyogenes and other beta and hemolitic streptococci, Streptococcus pneumoniae, Streptococcus of group B / Streptococcus agalactiae/; anaerobe bacterias (gram-positive and gram-negative cocci / including Peptococcus spp. and Peptostreptococcus spp./, gram-positive sticks / including Clostridium spp. except Clostridium difficile, Propionibacterium spp./, gram-negative sticks / including Bacteroides spp. and Fusobacterium spp./, gram-negative spirochetes / Borrelia burgdorferi/).
The following microorganisms are not sensitive to a tsefuroksim: Clostridium difficile, Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Listeria monocytogenes, Methicillinum - resistant strains of Staphylococcus aureus and Staphylococcus epidermidis, Legionella spp., Enterococcus faecalis, Morganella morganii, Proteus vulgaris, Enterobacter spp., Citrobacter spp., Serratia spp., Bacteroides fragilis.
Pharmacokinetics. Absorption
After intake by tsefuroksy aksetit slowly it is soaked up from a GIT and quickly hydrolyzed in a mucous membrane of intestines and blood with release of a tsefuroksim. Tsefuroksima aksetit optimum is soaked up on condition of administration of drug right after food.
After reception of the tablets Cmax of a tsefuroksim (2.9 mg/l for a dose of 125 mg and 4.4 mg/l for a dose of 250 mg) are observed approximately in 2.4 h at administration of drug after food.
After reception of Cmax suspension of a tsefuroksim (2-3 mg/l for a dose of 125 mg and 4-6 mg/l for a dose of 250 mg) are observed approximately in 2-3 h after administration of drug after food.
Distribution
Linkng of a tsefuroksim with proteins of a blood plasma makes 33-50%.
Tsefuroksim gets through GEB, gets through a placenta and is allocated with breast milk.
Metabolism
Tsefuroksim is not metabolized in an organism.
Removal
It is allocated by glomerular filtering and canalicular secretion. Serumal levels of a tsefuroksim decrease at dialysis.
T1/2 makes 1-1.5 h.
Indications to use:
Treatment of the infectious and inflammatory diseases caused by microorganisms, sensitive to drug:
— upper respiratory tract infections, ENT organs (sinusitis, tonsillitis, pharyngitis, average otitis);
— lower respiratory tract infections (acute bacterial bronchitis and exacerbation of chronic bronchitis, pneumonia);
— infections of urinary tract (pyelonephritis, cystitis, urethritis);
— infections of skin and soft tissues (furunculosis, pyoderma, impetigo);
— gonorrhea, acute uncomplicated gonorrheal urethritis and cervicitis;
— treatment of a disease of Lyme at an early stage and prevention of late stages of this disease at adults and children is more senior than 12 years.
Tsefuroksim is also issued in the form of sodium salt (drug Zinatsef®) for parenteral administration. Within performing step therapy transition from a parenteral form to a peroral form of a tsefuroksim is recommended.
Step therapy is shown in treatment of pneumonia and at an exacerbation of chronic bronchitis.
Route of administration and doses:
Tablets
The standard course of therapy makes 7 days (can vary from 5 to 10 days). For optimum absorption drug should be accepted after food.
Adults
Dosing mode
Tablets
The standard course of therapy makes 7 days (can vary from 5 to 10 days). For optimum absorption drug should be accepted after food.
Adults
Indications Dose
(tablets and suspension
for intake)
Majority of infections of 250 mg 2
Infections of urinary tract of 125 mg 2
Slight and medium-weight infections
lower respiratory tracts, for example
bronchitis of 250 mg 2
Heavier infections of lower
respiratory tracts or at suspicion
on pneumonia of 500 mg 2
Pyelonephritis of 250 mg 2
Uncomplicated gonorrhea of 1 g once
Borreliosis (Lyme's disease) at adults
and 12 years of 500 mg 2 within 20 days are more senior than children
Children since 3 years
The majority of infections of 125 mg (1 tablet on 125 mg) 2 Maximum daily dose - 250 mg
Average otitis or heavier infections of 250 mg (1 tablet on 250 mg or 2 tablets on 125 mg) 2 Maximum daily dose - 500 mg
Suspension for intake
The drug Zinnat® in the form of suspension for intake is recommended for use for children since 3 months. There is no experience of use of the drug Zinnat® for children aged is younger than 3 months.
If purpose of the fixed dose is preferable, then at the majority of infections 2 Children are recommended to accept on 125 mg at the age of 2 years and is more senior at average otitis or at heavier infections appoint 2 on 250 mg; the maximum daily dose makes 500 mg.
At treatment of babies and children happens it is necessary to calculate a dose depending on the body weight and age. At the majority of infections the dose for babies and children aged from 3 months up to 12 years makes 10 mg/kg 2, but no more than 250 mg / At average otitis and heavier infections the recommended dose is equal on 15 mg/kg 2, but no more than 500 mg /
Doses depending on age and the body weight of the child for dosing of Зиннат® 125 suspension of mg / 5 by ml the measured spoons on 5 ml attached to packaging are given in the following tables.
The dose at the rate of 10 mg/kg of body weight appointed at the majority of infections
Age the Body weight (kg) the Single dose (mg) at Number of measured spoons (5
(approximately) reception 2 разав days of ml) in one dose
3-6 months 4-6 40-60 1/2
6 months-2 of year 6-12 60-120 1/2-1
2-12 years from 12 and more than 20 125 1
The dose at the rate of 15 mg/kg of body weight appointed at average otitis and heavier
Age the Body weight (kg) the Single dose (mg) at Number of measured spoons (5
(approximately) reception of body weight of ml) in one dose
3-6 months 4-6 60-90 1/2
6 months-2 of year 6-12 90-180 1-1.5
2-12 years from 12 and more than 20 180-250 1.5-2
Step therapy
Tsefuroksim is issued also in the form of sodium salt (drug Zinatsef®) for parenteral administration that allows to appoint consistently same antibiotic when transition with parenteral to peroral therapy is necessary. The drug Zinnat® is effective after parenteral use of the drug Zinatsef® for treatment of pneumonia and an exacerbation of chronic bronchitis.
Duration of parenteral and peroral courses of treatment is defined by severity of an infection and a clinical picture.
Pneumonia
The drug Zinatsef® (tsefuroksy in the form of sodium salt) in a dose of 1.5 g 2-3 (in/in or in oil) during 48-72 h, then - the drug Zinnat® (a tsefuroksima aksetit) inside in a dose of 500 mg 2 within 7-10 days.
Exacerbation of chronic bronchitis
The drug Zinatsef® (tsefuroksy in the form of sodium salt) in a dose of 750 mg 2-3 (in/in or in oil) during 48-72 h, then - a course of treatment the drug Zinnat® (a tsefuroksima aksetit) orally in a dose of 500 mg 2 within 5-10 days.
Features of use:
Care should be shown at purpose of drug to patients with allergic reaction to a beta laktamnye antibiotics in the anamnesis.
In the course of treatment it is necessary to control function of kidneys, especially at the patients receiving drug in a high dose.
During administration of drug of Zinnat® false positive reaction of urine to glucose is possible.
As well as when using other antibiotics, long administration of drug of Zinnat® can lead to the overgrowth of mushrooms of the sort Candida. Long reception can cause growth of other resistant microorganisms (enterococcis and Clostridium difficile) that can demand the treatment termination.
Pseudomembranous colitis was observed when using antibiotics of a broad spectrum of activity therefore it is necessary to carry out differential diagnosis of pseudomembranous colitis at patients with the heavy diarrhea which arose in time or after a course of treatment antibiotics.
Yarisha-Gerksgeymer's reaction was observed at borreliosis (Lyme's disease) at administration of drug of Zinnat® and is caused by bactericidal activity of drug concerning Borrelia burgdorferi spirochete infestant. Patients have to be informed that these symptoms are a typical consequence of use of antibiotics at this disease.
If the clinical effect is not reached during 72 h from an initiation of treatment, the parenteral course of therapy has to be continued.
Before step therapy apply for information in the available reference books concerning sodium salt of a tsefuroksim (drug Zinatsef®).
Tablets of the drug Zinnat® cannot be broken and crumbled. Therefore this dosage form is not applied to treatment of patients with difficulties of swallowing, including small children who cannot swallow the whole tablet.
It is necessary to consider the content of sucrose in Zinnat® suspension at treatment of patients with a diabetes mellitus.
5 ml of the prepared Zinnat® suspension contain 0.25 grain units (GU).
Influence on ability to driving of motor transport and to control of mechanisms
As aksetit a tsefuroksim can cause dizziness, it is necessary to warn patients about precautionary measures during the driving or work with moving mechanisms.
Side effects:
The undesirable phenomena given below are listed depending on anatomo-physiological classification and frequency of occurrence. Frequency of occurrence is defined as follows: very often (≥1/10), it is frequent (≥1/100 and <1/10), infrequently (≥1/1 000 and <1/100), is rare (≥1/10 000 and <1/1 000), is very rare (<1/10 000, including separate cases). Categories of frequency were created on the basis of clinical trials of drug and post-registration observation.
Infections: often - superinfection sort Candida mushrooms.
From hemopoietic and lymphatic system: often - an eosinophilia; infrequently - false positive reaction of Koombs (cephalosporins are absorbed on a surface of a cellular membrane of erythrocytes, contacting antibodies to cephalosporins that results in false positive result of test of Koombs and seldom or never - to hemolitic anemia), thrombocytopenia, a leukopenia (sometimes heavy); very seldom - hemolitic anemia.
From immune system: hypersensitivity reactions: infrequently - skin rash; seldom - urticaria, an itch; very seldom - medicinal fever, a serum disease and an anaphylaxis.
From a nervous system: often - a headache, dizziness.
From the alimentary system: often - diarrhea, nausea, abdominal pains; infrequently - vomiting; seldom - pseudomembranous colitis.
From a liver and biliary tract: often - tranzitorny increase in level of enzymes of a liver of ALT, ACT, LDG; very seldom - jaundice (preferential cholestatic), hepatitis.
From skin and a hypodermic fatty tissue: very seldom - a mnogoformny erythema, Stephens-Johnson's syndrome, a toxic epidermal necrolysis.
Interaction with other medicines:
The drugs reducing acidity of a gastric juice can reduce bioavailability of a tsefuroksim when comparing it with observable after administration of drug on an empty stomach, and also level effect of the increased absorption of drug after meal.
As well as other antibiotics, the drug Zinnat® can influence intestinal microflora that leads to decrease in a reabsorption of estrogen and, as a result, to decrease in efficiency of the oral hormonal combined contraceptives.
When carrying out the ferrotsianidny test the false-negative result therefore for determination of level of glucose in blood and/or plasma it is recommended to use glyukozooksidazny or hexokinase methods can be observed.
The drug Zinnat® does not influence quantitative definition of creatinine alkaline пикратным by method.
The concomitant use with "loopback" diuretics slows down canalicular secretion, reduces renal clearance, increases concentration in plasma and increases T1/2 of a tsefuroksim.
Simultaneous introduction of a tsefuroksim and probenetsid leads to increase in AUC by 50%.
At a concomitant use with aminoglycosides and diuretics the risk of emergence of nephrotoxic effects increases.
Contraindications:
— a fenilketonuriya (for suspension for intake);
— children's age up to 3 months (for suspension for intake);
— for tablets - children's age up to 3 years (for children from 3 months to 3 years the drug Zinnat® should be used in the form of suspension);
— hypersensitivity to antibiotics of group of cephalosporins.
With care
It is necessary to be careful at appointment to patients with a renal failure; gastrointestinal diseases (including in the anamnesis, and also at ulcer colitis); to pregnant women, in the period of a lactation.
Use of the drug ZINNAT® at pregnancy and feeding by a breast
The drug Zinnat® should be used if the potential advantage for mother exceeds potential risk for the child.
There are no experimental proofs of embriopatichesky or teratogenic effects of a tsefuroksim of an aksetil, but also as well as in case of use of other medicines, it is necessary to show care at appointment it on early durations of gestation.
It is necessary to be careful at appointment to his nursing mothers as drug is defined in breast milk.
Use for children
Children since 3 years
The majority of infections of 125 mg 2 Maximum daily dose - 250 mg
Average otitis or heavier infections of 250 mg 2 Maximum daily dose - 500 mg
The drug Zinnat® in the form of suspension for intake is recommended for use for children since 3 months. There is no experience of use of the drug Zinnat® for children aged is younger than 3 months.
If purpose of the fixed dose is preferable, then at the majority of infections 2 Children are recommended to accept on 125 mg at the age of 2 years and is more senior at average otitis or at heavier infections appoint 2 on 250 mg; the maximum daily dose makes 500 mg.
At treatment of babies and children happens it is necessary to calculate a dose depending on the body weight and age. At the majority of infections the dose for babies and children aged from 3 months up to 12 years makes 10 mg/kg 2, but no more than 250 mg / At average otitis and heavier infections the recommended dose is equal on 15 mg/kg 2, but no more than 500 mg /
Doses depending on age and the body weight of the child for dosing of Зиннат® 125 suspension of mg / 5 by ml the measured spoons on 5 ml attached to packaging are given in the following tables.
The dose at the rate of 10 mg/kg of body weight appointed at the majority of infections
Age the Body weight (kg) the Single dose (mg) at Number of measured spoons (5
(approximately) reception 2 разав days of ml) in one dose
3-6 months 4-6 40-60 1/2
6 months-2 of year 6-12 60-120 1/2-1
2-12 years from 12 and more than 20 125 1
The dose at the rate of 15 mg/kg of body weight appointed at average otitis and heavier
Age the Body weight (kg) the Single dose (mg) at Number of measured spoons (5
(approximately) reception of body weight of ml) in one dose
3-6 months 4-6 60-90 1/2
6 months-2 of year 6-12 90-180 1-1.5
2-12 years from 12 and more than 20 180-250 1.5-2
— children's age up to 3 months (for suspension for intake);
— for tablets - children's age up to 3 years (for children from 3 months to 3 years the drug Zinnat® should be used in the form of suspension).
Overdose:
Symptoms: the overdose by cephalosporins can cause increase in excitability of a brain with development of spasms.
Treatment: carry out symptomatic therapy. Serumal concentration of a tsefuroksim decrease at a hemodialysis and peritoneal dialysis.
Storage conditions:
Tablets should be stored at a temperature not above 30 °C. A period of validity - 3 years.
Granules for preparation of suspension should be stored at a temperature not above 30 °C. A period of validity - 2 years.
The prepared suspension should be stored in the refrigerator at a temperature of 2-8 °C no more than 10 days.
To store in the place, unavailable to children.
Issue conditions:
According to the recipe
Packaging:
5 - blisters (1) - packs cardboard.
5 - blisters (2) - packs cardboard.
10 - blisters (1) - packs cardboard.
10 - blisters (2) - packs cardboard.
1.25 - bottles of dark glass (1) complete with a dosing spoon and a measured glass - packs cardboard.
