Vilprafen Solutab, 1000 mg, 10 pcs.

Active substance:

josamycin 500 mg, 

Excipients: 

methyl cellulose;

MCC;

silicon dioxide colloidal anhydrous;

polysorbate 80;

sodium carboxymethyl cellulose;

talc;

magnesium stearate;

macrogol 6000;

titanium dioxide (E171);

aluminum hydroxide;

poly- (ethacrylate methyl methacrylate) -30% dispersion

Vilprafen solutab - bactericidal, bacteriostatic, antibacterial.

Pharmacodynamics

The drug is used to treat bacterial infections; the bacteriostatic activity of josamycin, like other macrolides, is due to inhibition of bacterial protein synthesis. When creating high concentrations of inflammation in the focus, it has a bactericidal effect.

Josamycin 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 diphtheriae ), Gram-negative bacteria  (Neisseria meningitidis, Neisseria gonorrhoeae, Haemophilus influenzae, Bordetella pertussis),  as well as against some anaerobic bacteria  (Peptococcus, Peptostreptococcus, Clostridium perfringens) . Slightly affects enterobacteria, therefore, little changes the natural bacterial flora of the gastrointestinal tract. Effective for resistance to erythromycin. Resistance to josamycin develops less frequently than to other antibiotics from the macrolide group.

Pharmacokinetics

After oral administration, josamycin is rapidly and completely absorbed from the digestive tract, food intake does not affect bioavailability. Serum Cmax of josamycin is reached 1–2 hours after administration. About 15% of josamycin binds to plasma proteins. Particularly high concentrations of the substance are found in the lungs, tonsils, saliva, sweat and tear fluid. Concentration in sputum exceeds the concentration in plasma by 8–9 times. Accumulates in bone tissue. Passes the placental barrier, is secreted into breast milk. Josamycin is metabolized in the liver to less active metabolites and excreted mainly with bile. Excretion of the drug with urine less than 20%.

Acute and chronic infections caused by drug-sensitive microorganisms, for example:

• infections of the upper respiratory tract and ENT organs - tonsillitis, pharyngitis, paratonsillitis, laryngitis, otitis media, sinusitis, diphtheria (in addition to treatment with diphtheria toxoid), as well as scarlet fever in case of hypersensitivity to penicillin;
• lower respiratory tract infections - acute bronchitis, exacerbation of chronic bronchitis, pneumonia (including caused by atypical pathogens), whooping cough, psittacosis;
• dental infections - gingivitis and periodontal disease;
• infections in ophthalmology - blepharitis, dacryocystitis;
• infections of the skin and soft tissues - pyoderma, furunculosis, anthrax, erysipelas (with increased sensitivity to penicillin), acne, lymphangitis, lymphadenitis, venereal lymphogranuloma;
• infections of the genitourinary system - prostatitis, urethritis, gonorrhea, syphilis (with increased sensitivity to penicillin), chlamydial, mycoplasma (including ureaplasma) and mixed infections.

Perhaps according to indications.

It is the drug of choice for the treatment of chlamydial infections in pregnant women.

• severe liver dysfunction;
• children weighing less than 10 kg;
• hypersensitivity to the components of the drug;
• hypersensitivity to antibiotics of the macrolide group.

From the digestive tract: rarely - loss of appetite, nausea, heartburn, vomiting, dysbiosis, diarrhea. In the case of persistent severe diarrhea, one should bear in mind the possibility of developing life-threatening pseudomembranous colitis against the background of antibiotics.

Allergic reactions: in extremely rare cases - urticaria.

On the part of the auditory apparatus: in rare cases, dose-dependent transient hearing impairment.

Other: very rarely - candidiasis.

Other antibiotics.  Since bacteriostatic antibiotics can reduce the bactericidal effect of other antibiotics such as penicillins and cephalosporins, co-administration of josamycin with these types of antibiotics should be avoided. Josamycin should not be prescribed together with lincomycin, because mutual reduction of their effectiveness is possible.

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 josamycin has a lesser effect on theophylline secretion than other macrolide antibiotics.

Antihistamines.  After co-administration of josamycin and antihistamines containing terfenadine or astemizole, a slowdown in the elimination of terfenadine and astemizole can be noted, which in turn can lead to the development of life-threatening cardiac arrhythmias.

Ergot alkaloids.  There are individual reports of increased vasoconstriction after co-administration of ergot alkaloids and macrolide antibiotics. One case of the patient's lack of tolerance to ergotamine when taking josamycin was noted. Therefore, the concomitant use of josamycin and ergotamine should be accompanied by appropriate observation of patients.

Cyclosporin.  The combined administration of josamycin and cyclosporine can cause an increase in the level of cyclosporin in the blood plasma and the creation of a nephrotoxic concentration of cyclosporin in the blood. Plasma cyclosporine concentration should be regularly monitored.

Digoxin.  With the joint administration of josamycin and digoxin, an increase in the level of the latter in blood plasma is possible.

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 contraceptives.

Inside, tablets - without chewing, washed down with a small amount of water, the suspension is prescribed between meals (the contents of the vial are pre-shaken): 1-2 g per day in 2-3 doses.

The duration of treatment for streptococcal infections is at least 10 days.

For the treatment of ordinary and spherical acne - 500 mg 2 times a day for 2-4 weeks, then - 500 mg 1 time per day for 8 weeks.

Newborns and children under 14 years of age - 30-50 mg / kg per day in 3 divided doses.

To date, there is no evidence of specific symptoms of poisoning.

In case of an overdose, the onset of the symptoms described in the “Side effects” section should be assumed, especially from the gastrointestinal tract.

If you missed one dose, you must immediately take a dose of the drug, but if it is time to take the next dose, you should return to the usual treatment regimen. Do not take a double dose. A break in treatment or premature discontinuation of the drug reduces the likelihood of treatment success.

The possibility of cross-resistance to various macrolide antibiotics should be considered (for example, microorganisms that are resistant to treatment with antibiotic-related antibiotics may also be resistant to josamycin)

Tablets