Pharmacological properties of the drug Vilprafen
Pharmacodynamics . Josamycin is a broad-spectrum macrolide antibiotic. Active against gram-positive and gram-negative microorganisms, including obligate anaerobes. The drug is also active against mycoplasmas and chlamydia. Pharmacokinetics After oral administration, the drug is rapidly absorbed into the gastrointestinal tract. The maximum concentration in blood plasma is achieved 1 hour after administration. 45 minutes after taking 1 g of the drug, the average concentration of josamycin in the blood plasma is 2.4 mg/l. Josamycin penetrates well through biological membranes and accumulates in various tissues and organs: pulmonary, lymphatic, skin and soft tissues, tonsils, and organs of the urinary system. Binding to plasma proteins does not exceed 15%. Josamycin is metabolized in the liver and is slowly excreted in bile and in small amounts (≤15%) in urine.
Vilprafen
Vilprafen (INN josamycin) is a macrolide antibiotic. It exhibits bacteriostatic and, in high concentrations, bactericidal action. Effective in the treatment of infections caused by staphylococci (including those producing penicillinase), streptococci, corynebacteria, neisseria, Haemophilus influenzae, bordetella, rickettsia, treponema, mycoplasma, chlamydia, some types of shigella, ureaplasma, clostridia. It has virtually no effect on enterobacteria, therefore it does not introduce an imbalance into the natural microflora of the gastrointestinal tract. Can be used in cases of resistance to erythromycin. Resistance to Vilprafen itself develops less frequently and more slowly than to other macrolides. One of the advantages of the drug is its lipophilicity, which ensures rapid penetration of the active substance in therapeutic concentrations into cells and tissues. When using tablet forms of josamycin, its concentration in white blood cells, epithelial cells, macrophages, phagocytes and monocytes is 20 times higher than in the interstitial space. This property of the drug makes it an ideal means of combating chlamydial infections, because The life cycle of these bacteria takes place inside the cell. Compared to other antibiotics, Vilprafen has a very high cure rate for chlamydia - 97% (azithromycin - 55%, doxycycline - 50%). The wide range of therapeutic effects of Vilprafen allows its use in the treatment of mixed bacterial infections, incl. caused by representatives of anaerobic microflora. The drug is practically devoid of teratogenic and embryotoxic effects, which makes it available to pregnant women and provides effective prevention of chlamydia in the neonatal period.
In addition to infections of the genitourinary tract, Vilprafen is used in the treatment of infections of the ENT organs, respiratory tract, oral cavity, soft tissues, and dermatological infections. After oral administration, it is quickly and completely absorbed from the digestive tract. The presence of food masses in the intestines does not affect the bioavailability of the drug (i.e. it can be taken regardless of meals, which is very convenient). The maximum concentration of the active substance in the blood is observed 1-2 hours after administration. It undergoes metabolic transformations in the liver, and the resulting metabolites have less therapeutic activity than the original substance. It is excreted from the body through the biliary (with bile) and genitourinary (with urine) tract. It has a small number of side effects, mainly from the digestive tract (appetite disturbance, nausea, dyspepsia, abdominal cramps, impaired choleretic function). When prescribing Vilprafen, it is necessary to take into account the possibility of adverse interactions with co-administered medications. Thus, this antibiotic slows down the elimination of the antiallergic drugs astemizole and terfenadine, which can lead to the development of severe ventricular arrhythmias. Vilprafen also potentiates the side effects of theophylline, digoxin, and ergot alkaloids (vasoconstrictor effect). And the other side of the coin: Vilprafen can reduce the effectiveness of penicillin and cephalosporin antibiotics, and in combination with lincomycin, the effectiveness of both drugs decreases. For elderly patients, Vilprafen is prescribed in lower doses. ECG monitoring is mandatory in persons concomitantly taking digoxin.
Use of the drug Vilprafen
The recommended dose for adults and children weighing 40 kg is 1 g (initial); then the drug is prescribed 1–2 g per day (2–4 tablets) in 2–3 doses. In severe cases of the disease, the dose can be increased to 3 g. The recommended dose for children over 5 years old weighing ≤40 kg is 40–50 mg/kg body weight per day, divided into several doses. If precise dosing is not possible, the drug for children is used in the form of a suspension. Take the tablets without chewing with a small amount of liquid between meals. The duration of treatment is determined by the doctor. According to WHO recommendations regarding the use of antibiotics, the duration of treatment for streptococcal infections is at least 10 days.
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
Special instructions for the use of the drug Vilprafen
If pseudomembranous colitis develops, the drug must be discontinued and appropriate therapy prescribed. In patients with impaired liver and biliary tract function, treatment is carried out taking into account the results of laboratory tests (for therapy lasting more than 15 days). During pregnancy and breastfeeding . Despite the current lack of data regarding the embryotoxic effect of josamycin, the use of the drug during pregnancy and lactation is permissible in exceptional cases after assessing the risk/benefit ratio of therapy. Use in children. The drug can be used in children over 5 years of age. For children under 5 years of age, as well as when precise dosing is impossible, the drug is prescribed in the form of a suspension. no negative effects on reaction speed when driving vehicles or operating machinery .
Drug interactions Vilprafen
Since bacteriostatic antibiotics, such as josamycin and bactericidal antibiotics, can interact with each other, the need for simultaneous use of Vilprafen with these antibiotics must be carefully considered. When used simultaneously with lincomycin, the effectiveness of Vilprafen may be reduced. After simultaneous use of Vilprafen and antihistamines that contain terfenadine or astemizole, a slowdown in the elimination of antihistamines may be observed, which in turn can cause life-threatening cardiac arrhythmias. When using Vilprafen together with ergot alkaloids, the possibility of developing a pronounced vasoconstrictor effect should be taken into account. The simultaneous administration of Vilprafen and cyclosporine may lead to an increase in the level of cyclosporine in the blood plasma, which in turn can cause renal dysfunction. With the simultaneous use of Vilprafen and digoxin, an increase in the level of digoxin in the blood plasma is possible.
