Vilprafen 500mg/5ml 20g granules for suspension for oral administration
pharmachologic effect
Antibiotic, macrolide.
Composition and release form Vilprafen 500 mg/5 ml 20 g granules for the preparation of suspension for oral administration
Granules for preparing a suspension - 1 vial:
- Active ingredients: josamycin propionate - 6.307 g;
- Excipients: sodium citrate - 0.1125 g, methyl parahydroxybenzoate - 0.0795 g, propyl parahydroxybenzoate - 0.0105 g, simethicone - 0.075 g, hyprolose - 0.3 g, Avicel RC-591 [microcrystalline cellulose, sodium carmellose] - 0.6 g, strawberry flavor - 0.05 g, betacarotene - 0.015 g, sucrose starch powder 3% - 10.2005 g, mannitol - 2.25 g.
5 ml of the finished suspension contains 500 mg of josamycin.
15 g - Colorless glass bottles with a capacity of 100 ml (1) (complete with dosage syringe and syringe holder) - cardboard packs.
Description of the dosage form
Granules for the preparation of a suspension for oral administration are yellow, with the smell of strawberries; after dissolving in water, a yellow suspension with the smell of strawberries is formed.
Characteristic
Antibiotic of the macrolide group, produced by Streptomyces narbonensis var. Josamyceticus.
Directions for use and doses
When taken orally by adults and children over 14 years of age - 1-2 g/day in 2-3 divided doses. Children under 14 years of age - 30-50 mg/kg/day in 3 divided doses. The duration of treatment depends on the indications for use.
Pharmacodynamics
Antibiotic of the macrolide group. It has a bacteriostatic effect due to inhibition of protein synthesis by bacteria. When high concentrations are created at the site of inflammation, it has a bactericidal effect.
Highly active against intracellular microorganisms: Chlamydia trachomatis and Chlamydia pneumonuae, Mycoplasma pneumoniae, Mycoplasma hominis, Ureaplasma urealyticum, Legionella pneumophila; against gram-positive aerobic bacteria: Staphylococcus aureus, Streptococcus pyogenes and Streptococcus pneumoniae (pneumococcus), Corynebacterium diphtheriae; gram-negative aerobic bacteria: Neisseria meningitidis, Neisseria gonorrhoeae, Haemophilus influenzae, Bordetella pertussis; against some anaerobic bacteria: Peptococcus, Peptostreptococcus, Clostridium perfringens.
Josamycin is also active against Treponema pallidum.
Pharmacokinetics
After oral administration, josamycin is rapidly absorbed from the gastrointestinal tract. Cmax is achieved 1-2 hours after administration. 45 minutes after taking a dose of 1 g, the average concentration of josamycin in plasma is 2.41 mg/l.
Plasma protein binding does not exceed 15%.
An equilibrium state is achieved after 2-4 days of regular use.
Josamycin is well distributed in the body and accumulates in various tissues: in the lungs, lymphatic tissue of the palatine tonsils, organs of the urinary system, skin and soft tissues. Particularly high concentrations are determined in the lungs, tonsils, saliva, sweat and tear fluid. The concentration of josamycin in human polymorphonuclear leukocytes, monocytes and alveolar macrophages is approximately 20 times higher than in other cells of the body.
Josamycin is biotransformed in the liver to less active metabolites.
Excreted mainly in bile, excretion in urine is less than 20%.
Indications for use Vilprafen 500 mg/5 ml 20 g granules for the preparation of suspension for oral administration
Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to josamycin: infections of the upper respiratory tract and ENT organs (including pharyngitis, tonsillitis, paratonsillitis, otitis media, sinusitis, laryngitis); diphtheria (in addition to treatment with diphtheria antitoxin); scarlet fever (with hypersensitivity to penicillin); lower respiratory tract infections (including acute bronchitis, bronchopneumonia, pneumonia, including atypical form, whooping cough, psittacosis); oral infections (including gingivitis and periodontal disease); infections of the skin and soft tissues (including pyoderma, boils, anthrax, erysipelas / with hypersensitivity to penicillin /, acne, lymphangitis, lymphadenitis); infections of the urinary tract and genital organs (including urethritis, prostatitis, gonorrhea; with increased sensitivity to penicillin - syphilis, lymphogranuloma venereum); chlamydial, mycoplasma (including ureaplasma) and mixed infections of the urinary tract and genital organs.
Contraindications
Severe liver dysfunction, hypersensitivity to erythromycin and other macrolide antibiotics.
Application of Vilprafen 500 mg/5 ml 20 g granules for the preparation of suspension for oral administration during pregnancy and lactation
Use during pregnancy and lactation is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus or child.
When treating with macrolides and simultaneous use of hormonal contraceptives, non-hormonal contraceptives should be additionally used. Josamycin is not prescribed to premature babies. When used in newborns, it is necessary to monitor liver function.
special instructions
If pseudomembranous colitis develops, josamycin should be discontinued and appropriate therapy should be prescribed. Drugs that reduce intestinal motility are contraindicated.
In patients with renal failure, adjustment of the dosage regimen is required in accordance with CC values.
Josamycin is not prescribed to premature babies. When used in newborns, it is necessary to monitor liver function.
The possibility of cross-resistance to various macrolide antibiotics should be taken into account (for example, microorganisms that are resistant to treatment with antibiotics related in chemical structure may also be resistant to josamycin).
Overdose
Symptoms: increased side effects, especially from the gastrointestinal tract (there is no data on specific symptoms of poisoning).
Side effects Vilprafen 500mg/5ml 20g granules for suspension for oral administration
From the digestive system: rarely - lack of appetite, nausea, heartburn, vomiting, diarrhea, pseudomembranous colitis; in some cases - increased activity of liver transaminases, impaired bile outflow and jaundice.
Allergic reactions: rarely - urticaria.
Other: in some cases - dose-dependent transient hearing impairment.
Drug interactions
Bacteriostatic antibiotics may reduce the bactericidal effect of other antibiotics, such as penicillins and cephalosporins (simultaneous use of josamycin with penicillins and cephalosporins should be avoided).
With the simultaneous use of josamycin with lincomycin, the effectiveness of both drugs may be reduced.
Josamycin slows down the elimination of theophylline to a lesser extent than other macrolide antibiotics.
Josamycin slows the elimination of terfenadine or astemizole, which increases the risk of life-threatening arrhythmias.
There are isolated reports of increased vasoconstrictor effects with simultaneous use of macrolide antibiotics and ergot alkaloids. There was 1 case of ergotamine intolerance when taking josamycin.
With the simultaneous use of josamycin and cyclosporine, it is possible to increase the concentration of cyclosporine in the blood plasma up to nephrotoxic.
With the simultaneous use of josamycin and digoxin, an increase in the level of the latter in the blood plasma is possible.
In rare cases, during treatment with macrolides, the contraceptive effect of hormonal contraceptives may be insufficient.
Vilprafen Solutab 1000 mg No. 10 dispersible tablet.
Instructions for the medical use of the drug Vilprafen Solutab Trading name Vilprafen Solutab International Nepatent name Josamycin Disma of tablet dispersed 1000 mg. The tablet contains an active substance - josamycin 1000.0 mg, equivalent to Josamycin 1067. 66 mg, auxiliary substances: cellulose microcrystallic , giplose (lm ), sodium docusate, aspartame, colloidal anhydrous silicon dioxide, strawberry flavor 052311 AR 0551, magnesium stearate. Description White or white with a yellowish tint, oblong-shaped tablets, sweet, with the smell of strawberries, with the inscription “IOSA” and a line mark on one side and the inscription “1000” on the other. Pharmacotherapeutic group Antibacterial drugs for systemic use. Macrolides, lincosamides and streptogramins. Macrolides. Josamycin. ATC code J01FA07 Pharmacological properties Pharmacokinetics After oral administration, josamycin is quickly and completely absorbed from the gastrointestinal tract; food intake does not affect bioavailability. The maximum serum concentration of josamycin is achieved 1-2 hours after administration. About 15% of josamycin is bound to plasma proteins. Particularly high concentrations of the substance are found in the lungs, tonsils, saliva, sweat and tear fluid. The concentration in sputum exceeds the concentration in plasma by 8-9 times. Accumulates in bone tissue. Crosses the placental barrier and is secreted into breast milk. Josamycin is metabolized in the liver to less active metabolites and excreted mainly in bile. Excretion of the drug in urine is less than 20%. Pharmacodynamics Vilprafen Solutab is used to treat bacterial infections; its bacteriostatic activity is due to inhibition of bacterial protein synthesis. When high concentrations are created at the site of inflammation, it has a bactericidal effect. The drug is highly active against intracellular microorganisms (Chlamydia trachomatis and Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycoplasma hominis, Ureaplasma urealyticum, Legionella pneumophila); gram-positive bacteria (Staphylococcus aureus, Streptococcus pyogenes and Streptococcus pneumoniae (pneumococcus), Corynebacterium diphteriae), gram-negative bacteria (Neisseria meningitidis, Neisseria gonorrhoeae, Haemophilus influenzae, Bordetella pertussis), as well as against some anaerobic bacteria (Peptococcus, Peptostreptococcus, Clostrid ium perfringens). It has a slight effect on enterobacteria, and therefore little changes the natural bacterial flora of the gastrointestinal tract. Effective against resistance to erythromycin. Resistance to Vilprafen Solutab develops less frequently than to other macrolide antibiotics. Indications for use Acute and chronic infections caused by microorganisms sensitive to the drug: - tonsillitis, pharyngitis, paratonsillitis, laryngitis, otitis media, sinusitis - diphtheria (in addition to treatment with diphtheria antitoxic serum) - scarlet fever, in case of hypersensitivity to penicillin - acute bronchitis, exacerbation of chronic bronchitis - pneumonia (including those caused by atypical pathogens) - psittacosis - gingivitis and periodontal diseases - blepharitis, dacryocystitis - pyoderma, furunculosis, anthrax, erysipelas (with hypersensitivity to penicillin) - acne, lymphangitis, lymphadenitis, inguinal lymphogranuloma - prostatitis, urethritis, gonorrhea, syphilis (with hypersensitivity to penicillin) - chlamydial, mycoplasma (including ureaplasma) and mixed infections Method of administration and dosage Vilprafen Solutab dispersible tablets can be taken in two different ways: they can be swallowed whole with a drink water or dissolve in water before use. The tablets should be dissolved in at least 20 ml of water. Before administration, the resulting suspension should be mixed thoroughly. The recommended daily dose for adults and adolescents over the age of 14 years is from 1 g to 2 g of the drug. If necessary, the dose can be increased to 3 g per day. The daily dose should be divided into 2-3 doses. The daily dose for children from 5 to 14 years is prescribed based on the calculation of 40 - 50 mg/kg body weight daily, divided into 2-3 doses. In the case of ordinary and globular acne, it is recommended to prescribe Vilprafen Solutab at a dose of 500 mg twice a day for the first 2-4 weeks, then 500 mg of the drug once a day as maintenance treatment for 8 weeks. The duration of treatment is determined by the doctor. In accordance with the recommendations of the World Health Organization on the use of antibiotics, the duration of treatment for streptococcal infections should be at least 10 days. Side effects Rarely - loss of appetite, nausea, heartburn, vomiting, dysbacteriosis, flatulence, diarrhea, pseudomembranous colitis Very rarely - skin allergic reactions - transient increase in the activity of liver enzymes in the blood plasma, in rare cases accompanied by impaired outflow of bile and jaundice, cholestatic hepatitis - dose-dependent transient hearing impairment - candidiasis - hypovitaminosis Contraindications - hypersensitivity to macrolide antibiotics and other components of the drug - severe liver dysfunction Drug interactions Vilprafen Solutab has a slight effect on the cytochrome P450 system, suppressing metabolism and increasing the plasma concentration of indirect anticoagulants, carbamazipine, valproic acid acids, disopyramide. Vilprafen Solutab / other antibiotics Since bacteriostatic antibiotics can reduce the bactericidal effect of other antibiotics, such as penicillins and cephalosporins, co-prescribing the drug with these types of antibiotics should be avoided. It should not be prescribed together with lincomycin, as a mutual decrease in their effectiveness is possible. Vilprafen Solutab / xanthines Some representatives of macrolide antibiotics slow down the elimination of xanthines (theophylline), which can lead to possible intoxication. Clinical and experimental studies indicate that Vilprafen Solutab has less effect on the release of theophylline than other macrolide antibiotics. Vilprafen Solutab / antihistamines After co-administration of the drug and drugs containing terfenadine and astemizole, a slowdown in the elimination of terfenadine or astemizole may be observed, which in turn can lead to the development of life-threatening cardiac arrhythmias caused by prolongation of the QT interval. Vilprafen Solutab / serotonin 5-HT 4 receptor agonists Co-administration of Vilprafen Solutab and drugs containing cisapride may result in a slower elimination of cisapride, which in turn can lead to the development of life-threatening cardiac arrhythmias caused by prolongation of the QT interval. Vilprafen Solutab / ergot alkaloids There are individual reports of increased vasoconstriction after co-administration of ergot alkaloids and macrolide antibiotics. Therefore, the concomitant use of Vilprafen Solutab and ergotamine should be accompanied by appropriate monitoring of patients. Vilprafen Solutab / cyclosporine Co-administration of the drug Vilprafen Solutab and cyclosporine can cause an increase in the level of cyclosporine in the blood plasma and the creation of a nephrotoxic concentration of cyclosporine in the blood. Plasma concentrations of cyclosporine should be regularly monitored. Vilprafen Solutab / digoxin When Vilprafen Solutab and digoxin are co-administered, the level of the latter in the blood plasma may increase. Vilprafen Solutab / hormonal contraceptives In rare cases, the contraceptive effect of hormonal contraceptives may be insufficient during treatment with macrolides. In this case, it is recommended to additionally use non-hormonal contraception. Antacids slightly reduce the absorption of josamycin in the gastrointestinal tract. Special instructions In patients with renal failure, treatment should be carried out taking into account the results of appropriate laboratory tests. The possibility of cross-resistance to various macrolide antibiotics should be taken into account. In the case of persistent severe diarrhea, one should keep in mind the possibility of life-threatening pseudomembranous colitis developing against the background of antibiotics. Pregnancy and lactation Use during pregnancy and breastfeeding is permitted according to indications. WHO Europe recommends josamycin as the drug of choice for the treatment of chlamydial infection in pregnant women. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms The drug does not affect the ability to drive vehicles or potentially dangerous mechanisms. Overdose Symptoms: increased side effects. Treatment: supportive and symptomatic therapy. Ensuring sufficient fluid intake into the body. Release form and packaging 5 tablets are placed in a blister pack made of polyvinyl chloride/polyvinyl dichloride film and aluminum foil. 2 blister packs together with instructions for medical use in the state and Russian languages are placed in a cardboard pack. Storage conditions Store in a dry place, protected from light, at a temperature not exceeding 25°C. Keep out of the reach of children! Shelf life: 2 years Do not use after expiration date! Conditions for dispensing from pharmacies By prescription Manufacturer Famar Lyon, 29 Avenue Charles de Gaulle, 69230 Saint-Genis-Laval, France Marketing authorization holder Astellas Pharma Europe B.V., the Netherlands Silviusweg 62, 2333 VE Leiden, the Netherlands Address of the receiving organization in the territory of the Republic of Kazakhstan, claims from consumers regarding product (product) quality: Representative office of Astellas Pharma Europe B.V. in the Republic of Kazakhstan Almaty, 050559, Al-Farabi Ave. 15, PFC "Nurly Tau", building 4B, office No. 20 Phone Fax www.astellas.ru, e-mail
Wilprafen®
The use of the following drugs in combination with josamycin is contraindicated due to the potential for serious side effects:
— Ergotamine, dihydroergotamine
The result of the interaction is the risk of severe vasoconstriction (ergotism) with the possible development of limb necrosis (due to inhibition of hepatic metabolism and elimination of ergot alkaloids).
— Cisapride, pimozide
As a result of the interaction, the risk of developing life-threatening arrhythmias, including ventricular tachycardia of the “pirouette” type, increases.
— Ivabradin
As a result of the interaction, the plasma concentration of ivabradine and associated side effects increase (due to inhibition of the hepatic metabolism of ivabradine).
— Colchicine
The interaction results in an increased risk of colchicine side effects, including potentially fatal ones.
The use of the following drugs in combination with josamycin is not recommended:
— Ebastine
Increased risk of life-threatening arrhythmias in patients with congenital long QT syndrome.
— Dopamine receptor agonists (bromocriptine, cabergoline, lisuride, pergolide)
An increase in the concentration of dopamine receptor agonists in the blood plasma with a potential increase in their activity and the appearance of overdose symptoms.
— Triazolam
Several cases of increased side effects of triazolam (conduct disorder).
— Halofantrine
Increased risk of ventricular arrhythmias, including ventricular tachycardia of the “torsades de pointes” type. If possible, josamycin should be discontinued. If it is not possible to cancel concomitant use of drugs, monitoring of the QT interval and ECG is necessary.
— Disopyramide
Increased risk of side effects of disopyramide: severe hypoglycemia, increased duration of the QT interval and life-threatening arrhythmias, including ventricular tachycardia of the “pirouette” type. Monitoring of clinical and laboratory data, as well as regular ECG monitoring, is necessary.
— Tacrolimus
Increased plasma concentrations of tacrolimus and creatinine as a result of inhibition of tacrolimus metabolism in the liver.
— Terfenadine and astemizole
During combined use of josamycin and antihistamines containing terfenadine or astemizole, the risk of developing life-threatening arrhythmias may be increased.
The use of the following drugs together with josamycin requires caution:
— Carbamazepine
It is possible to increase the concentration of carbamazepine in the blood plasma and develop overdose symptoms due to inhibition of its hepatic metabolism. It is recommended to monitor the patient's condition and the concentration of carbamazepine in the blood plasma. A dose reduction of carbamazepine may be required.
— Cyclosporine
Co-administration of josamycin and cyclosporine may cause an increase in plasma levels of cyclosporine and creatinine and increase the risk of nephrotoxicity. Plasma concentrations of cyclosporine and renal function should be regularly monitored. The dose of cyclosporine should be adjusted during co-administration with josamycin, as well as after discontinuation of josamycin.
— Indirect anticoagulants
It is possible to enhance the effect of indirect anticoagulants and increase the risk of bleeding.
Frequent monitoring of the international normalized ratio (INR) is necessary. It may be necessary to reduce the dose of indirect anticoagulants during co-administration with josamycin, and also in some cases after discontinuation of josamycin.
— Sildenafil
It is possible to increase the concentration of sildenafil in the blood plasma, increasing the risk of arterial hypotension. If co-administration is necessary, it is recommended to take the lowest dose of sildenafil.
— Theophylline and aminophylline
Caution should be exercised when using josamycin together with theophylline or aminophylline, because there is a risk of increased plasma theophylline concentrations, especially in children.
— Digoxin
When administered together, josamycin and digoxin may increase the level of the latter in the blood plasma.
— Other antibacterial drugs
Since bacteriostatic antibiotics in
vitro
may reduce the antimicrobial effect of bactericidal antibiotics, their simultaneous use should be avoided. Josamycin should not be used simultaneously with lincosamides due to a possible mutual decrease in effectiveness.
