Tsepotil

General characteristics. Structure:

Active ingredient: 50 mg or 100 mg of a tsefpodoksim in 5 ml of ready suspension.

Excipients: cellulose microcrystallic, sodium carboxymethylcellulose, citric acid anhydrous, sodium citrate anhydrous, sodium lauryl sulfate, Natrium benzoicum, silicon dioxide colloid, aspartame, croscarmellose sodium, cream vanilla, fragrance of "frutta tutta", fragrance orange, sucrose.

Pharmacological properties:

Pharmacodynamics. Tsepotil is beta лактамным an antibiotic of group of cephalosporins III of generation. Works bakteritsidno. The mechanism of action of Tsepotil is based on inhibition of synthesis of mukopeptid of a wall of a bacterial cell. Tsepotil is steady against action of the majority β-лактамаз.

It is highly active concerning the following gram-positive microorganisms: Streptococcus pneumoniae, Streptococci of group A (Streptococcus pyogenes), group B (Streptococcus agalactiae), C, F and G groups, and also Streptococcus mitis, Streptococcus sanguis and Streptococcus salivarius, Corynebacterium diphtheriae; gram-negative microorganisms: Haemophilus influenzae (including strains the producing and not producing β-lactamelements), Haemophilus parainfluenzae (including strains the producing and not producing β-lactamelements), Branhamella catarrhalis (including strains the producing and not producing β-lactamelements), Neisseria meningitidis, Neisseria gonorrhoeae, Escherichia coli, Klebsiella spp. (including Klebsiella pneumoniae, Klebsiella oxytoca), Proteus mirabilis.

Tsepotil is moderately active in the relation Methicillinum - the sensitive stafilokokk, strains which are producing and which are not producing a penicillinase (Staphylococcus aureus and Staphylococcus epidermidis).

Tsepotil is steady against the following microorganisms: Enterococcus spp., Methicillinum - resistant staphylococcus (Staphylococcus aureus and Staphylococcus epidermidis), Staphylococcus saprophyticus, Pseudomonas spp. (including Pseudomonas aeruginosa) and Clostridium difficile, Bacteroides fragilis and their versions.

Pharmacokinetics. Absorption. After intake on an empty stomach 100 mg of a tsefpodoksim of a proksetil of 51,5% are soaked up in intestines and hydrolyzed to an active metabolite - a tsefpodoksim. Absorption of drug increases during meal.

Cmax of a tsefpodoksim in a blood plasma is reached in 2-3 h after reception. After administration of drug in a dose of 100 mg of Cmax makes 1,2 mkg/ml, after administration of drug in a dose of 200 mg - 2,5 mkg/ml. At reception of 100 mg and 200 mg of drug of 2 times/days more than 14 days pharmacokinetic parameters of a tsefpodoksim in a blood plasma remain invariable.

Distribution. Tsefpodoksim contacts proteins of serum, is preferential with albumine for 40%.

Tsefpodoksim's concentration the exceeding minimum inhibiting concentration (MIK90) for the majority of widespread microorganisms are reached in a parenchyma of lungs, a mucous membrane of bronchial tubes, pleural liquid, almonds, intersticial liquid and in prostate tissues. Tsefpodoksim also well gets into renal fabric where concentration above MIK90 for the majority of widespread causative agents of diseases of an urinary path in 3-12 h after a single dose of a dose of 200 mg are reached.

Removal. T1/2 of drug is equal to 2,4 h. About 80% of drug are removed with urine in not changed look.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to drug:

— infections of upper and lower respiratory tracts, including sinusitis, tonsillitis, pharyngitis, an acute bronchitis, a recurrence or exacerbations of chronic bronchitis, bacterial pneumonia;

— infections of skin and soft tissues, such as abscess, contaminated wounds, furuncles, folliculites, paronychias, anthrax;

— infections of upper and lower urinary tract, including cystitis and acute pyelonephritis;

— gonorrhea, uncomplicated gonorrheal urethritis.

Route of administration and doses:

Tsepotil it is necessary to accept during food. Duration of treatment depends on disease severity and is established individually.

Average courses of treatment and the recommended doses for adults and children are more senior than 12 years are presented in the table:

Indication	Dose	Therapy duration
Upper respiratory tract infections Sinusitis	on 100 mg each 12 h on 200 mg each 12 h	5-10 days
Lower respiratory tract infections	on 100-200 mg each 12 h, depends on weight of an infection	10-14 days
Infections of skin and soft tissues	on 200 mg each 12 h	7-14 days
Uncomplicated infections of the lower urinary tract	on 100 mg each 12 h	7-10 days
Uncomplicated infections of upper urinary tract	on 200 mg each 12 h	7-14 days
Uncomplicated gonorrheal urethritis	200 mg	once

 

To children aged up to 9 years purpose of drug Tsepotil in the form of powder for preparation of suspension of 50 mg / 5 ml or 100 mg / 5 is recommended to ml.

The recommended average dose for children - 8 mg/kg/days, divided into 2 equal parts, is accepted with a 12-hour interval.

Children aged from 9 up to 12 years can appoint drug both in the form of suspension, and in the form of tablets in a dose of 100 mg of 2 times/days.

Tsepotil babies should not appoint younger than 15 days as there is no experience of use in this age group.

Dose adjustment is not required from elderly patients with normal function of kidneys.

At a renal failure there is no need for dose adjustment if KK more than 40 ml/min. At KK of 39-10 ml/min. the interval between administrations of drug has to be increased to 24 h. At KK less than 10 ml/min. the interval between receptions has to be increased to 48 h. For the patients who are on a hemodialysis the frequency of dosing has to be 3 times a week after a hemodialysis.

Rules of preparation of suspension. For preparation of suspension it is necessary to turn and stir up a bottle to fluff up powder. To add boiled cold water to a tag on a bottle and to intensively shake up bottle contents within one minute. Then it is necessary to make sure whether the final volume of drug reaches a tag and to shake up bottle contents before formation of homogeneous suspension.

It is necessary to store suspension after dissolution in the refrigerator at a temperature of 2 °C - 8 °C.

Features of use:

Use at pregnancy and feeding by a breast. Use of drug at pregnancy and in the period of a lactation is contraindicated.

Special instructions. Before purpose of drug it is necessary to define lack of allergic reaction to cephalosporins, penicillin and other antibiotics. At the patients having allergic reaction to other cephalosporins the possibility of cross allergic reaction to Tsepotil has to be taken into account. Tsepotil the patients having in the anamnesis cases of reaction of hypersensitivity to cephalosporins should not appoint.

As well as in case of use of other cephalosporins, in isolated cases development of false positive reaction of Koombs is possible.

Against the background of administration of drug obtaining false positive results when determining glucose in urine with use of reactants of Benedict and Felinga is possible.

At use of peroral antibiotics there is a change of the normal intestinal microflora leading to growth of clostridiums with the subsequent development of pseudomembranous colitis.

Influence on ability to driving of motor transport and to control of mechanisms. Considering side effects of medicine it is necessary to be careful when driving and potentially dangerous mechanisms.

Side effects:

From the alimentary system: often (more than 1%) - nausea, an abdominal pain, diarrhea; seldom (less than 1%) - a loss of appetite, distortion and loss of taste, an eructation, vomiting, abdominal distention, dyspepsia, gastritis, gastrointestinal frustration, pseudomembranous colitis, dysbacteriosis, candidosis stomatitis, ulcers of an oral cavity.

From TsNS: often - a headache; seldom - dizziness, sleeplessness, concern, hallucinations, nervousness, disorder of attention, confusion of consciousness, nightmares, paresthesias, a sonitus, an indisposition, fatigue, weakness, migraine.

From an organism in general: often - vaginal fungal infections; seldom - fever, a fever, generalized and local pains (stethalgias, in spin, a mialgiya), dryness in a mouth and in a throat, thirst, the increased perspiration, dehydration, fungal, bacterial, parasitic infections, abnormal microbiological indicators.

From cardiovascular system: seldom - tachycardia, congestive heart failure, a vazodilatation, arterial hypertension or hypotension.

From system of a hemopoiesis: seldom - anemia, an eosinophilia, a leukocytosis, a lymphocytosis, a granulocytosis, a basophilia, a monocytosis, a thrombocytosis, the lowered hematocrit, a leukopenia, a neutropenia, a lymphocytopenia, thrombocytopenia, positive reaction of Koombs, increase in a prothrombin time.

From respiratory system: seldom - cough, a bronchospasm, nasal bleeding.

Allergic reactions: seldom - a Quincke's edema, a small tortoiseshell, an acute anaphylaxis.

Dermatological reactions: seldom - skin rash, an itch, fungal dermatitis, dryness and a peeling of skin, vezikulobullezny rash, a toxic epidermal necrosis, Stephens-Johnson's syndrome, a mnogoformny erythema.

From an urinary system: seldom - a hamaturia, a proteinuria, a dysuria, the speeded-up urination, a nocturia.

From laboratory indicators: reversible changes of laboratory indicators (short-term moderate increase in activity of hepatic transaminases - nuclear heating plant, ALT, ShchF, GGT, LDG, a hyperbilirubinemia, small increase in level of urea and creatinine), a hyperglycemia, a hypoglycemia, a hypoalbuminemia, a hypoproteinemia, a hyperpotassemia and a hyponatremia.

Interaction with other medicines:

Blockers of histamine H2 receptors and antacids reduce bioavailability of a tsefpodoksim. Therefore antacids and blockers histamine H2 receptors, such as ranitidine, have to be accepted later 2-3 h after reception of a tsefpodoksim.

Probenetsid reduces renal excretion of a tsefpodoksim, also as well as other cephalosporins.

Contraindications:

— rare hereditary diseases of tolerance of a galactose with a syndrome of the lowered absorption of a glucose/galactose;

— pregnancy;

— lactation period;

— hypersensitivity to antibiotics of a tsefalosporinovy and penicillinic row.

Overdose:

Symptoms: developing of encephalopathy, especially at patients with a renal failure is possible.

Treatment: gastric lavage, symptomatic and maintenance therapy.

Storage conditions:

Drug should be stored in dry, protected from light, the place, unavailable to children, at a temperature not above 25 °C. A period of validity - 2 years. After dissolution suspension should be stored in the refrigerator at a temperature of 2 °C - 8 °C.

Issue conditions:

According to the recipe

Packaging:

Bottles of dark glass of 50 ml (1) - a box cardboard.
Bottles of dark glass of 100 ml (1) - a box cardboard.