Vilprafen, 500 mg 30 pcs.

Pharmacotherapeutic group: antibiotic, macrolide.

ATX code: J01FA07

Pharmacological properties

Pharmacodynamics.

An antibacterial drug from the group of macrolides. Mechanism of action is connected with disruption of protein synthesis in a microbial cell due to the reversible binding to 50S-subunit of ribosome. In therapeutic concentrations, as a rule, it has a bacteriostatic effect, slowing down the growth and reproduction of bacteria. At high concentrations in the center of inflammation it has a bactericidal effect.

Josamycin is active against Gram-positive bacteria (Staphylococcus spp. including methicillin-sensitive strains of Staphylococcus aureus), Streptococcus spp, including Streptococcus pyogenes and Streptococcus pneumoniae, Corynebacterium diphtheriae, Listeria monocytogenes, Propionibacterium acnes, Bacillus anthracis, Clostridium spp. Peptococcus spp., Peptostreptococcus spp.), Gram-negative bacteria (Neisseria meningitidis, Neisseria gonorrhoeae, Moraxella catarrhalis, Bordetella spp. Brucella spp., Legionella spp., Haemophilus ducreyi, Haemophilus influenzae, Helicobacter pylori, Campylobacter jejuni), Bacteroides fragilis sensitivity may be variable), Chlamydia spp, including C. trachomatis, Chlamydophila spp. including Chlamydophila pneumoniae (formerly called Chlamydia pneumoniae), Mycoplasma spp. including Mycoplasma pneumoniae, Mycoplasma hominis, Mycoplasma genitalium, Ureaplasma spp. Treponema pallidum, Borrelia burgdorferi.

As a rule it is not active against Enterobacteriaceae, so it has little effect on the microflora of the gastrointestinal tract. Retains activity with resistance to erythromycin and other 14- and 15-member macrolides. Resistance to jozamycin is less common than to the 14- and 15-member macrolides.

Pharmacokinetics.

After oral administration, jozamycin is rapidly absorbed from the gastrointestinal tract; food intake does not affect bioavailability. Maximum concentration of giovamycin in plasma is reached in 1 hour after intake. When administered in a dose of 1 g, maximum concentration in blood plasma is 2-3 mcg/ml. About 15% of giovamycin is bound to plasma proteins. Jozamycin is well distributed in organs and tissues (except brain) creating concentrations exceeding the plasma level and remaining at therapeutic levels for a long time. Especially high concentrations of josamycin are found in lungs, tonsils, saliva, sweat and lacrimal fluid. Concentration in sputum exceeds concentration in plasma by 8-9 times. It passes the placental barrier and is secreted into breast milk. Josamycin is metabolized in the liver to less active metabolites and is excreted mainly with bile. The half-life of the drug is 1-2 h, but it may be prolonged in patients with liver dysfunction. Renal excretion of the drug does not exceed 10%.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

Infections of the upper respiratory tract and ENT organs:
tonsillitis, pharyngitis, paratonsillitis, laryngitis, otitis media, sinusitis, diphtheria (in addition to treatment with diphtheria anatoxin), scarlet fever (in case of hypersensitivity to penicillin).

Infections of the lower respiratory tract:
acute bronchitis, acute exacerbation of chronic bronchitis, community-acquired pneumonia, including that caused by atypical pathogens, whooping cough, psittacosis.

Infections in dentistry:
gingivitis, pericoronitis, periodontitis, alveolitis, alveolar abscess.

Infections in ophthalmology:
blepharitis, dacryocystitis

Skin and soft tissue infections:
folliculitis, furunculitis, furunculosis, abscess, anthrax, rye, acne, lymphangitis, lymphadenitis, phlegmon, panaricosis, wound (including postoperative) and burn infections.

Infections of the urogenital system:
urethritis, cervicitis, epididymitis, prostatitis caused by chlamydia and/or mycoplasmas, gonorrhea, syphilis (with hypersensitivity to penicillin), venereal lymphogranuloma.

Diseases of the gastrointestinal tract associated with H. pylori
Gastric and duodenal ulcer, chronic gastritis, etc.

Active ingredient

Composition

Active ingredients:

Josamycin – 500 mg

Acompanying ingredients to a tablet weight of 640 mg:

Microcrystalline cellulose – 101.0 mg,

Polysorbate 80 – 5.0 mg,

colloidal silica – 14.0 mg,

sodium carmellose – 10.0 mg,

magnesium stearate – 5.0 mg,

methylcellulose – 0.12825 mg,

polyethylene glycol 6000 – 0.3846 mg,

talc – 2.0513 mg,

titanium dioxide – 0.641 mg,

aluminum hydroxide – 0.641 mg,

copolymer of methacrylic acid and its esters – 1.15385 mg.

How to take, the dosage

The recommended daily dosage for adults and adolescents over 14 years of age is 1 to 2 g of josamycin, the standard dose is 500 mg x 3 p/day. The daily dose should be divided into 2-3 doses. If necessary, the dose may be increased to 3 g per day.

The duration of treatment is usually determined by the physician, being from 5 to 21 days, depending on the nature and severity of the infection. According to the WHO recommendations, the duration of treatment of streptococcal tonsillitis should be at least 10 days.

In the regimens of anti-Helicobacter therapy, josamycin is prescribed in a dose of 1 g 2 times a day for 7-14 days in combination with other drugs in their standard dosages (famotidine 40 mg/day or ranitidine 150 mg 2 p/day + josamycin 1 g 2 p/day + metronidazole 500 mg 2 p/day; omeprazole 20 mg (or lansoprazole 30 mg, or pantoprazole 40 mg, or esomeprazole 20 mg, or rabeprazole 20 mg) 2 p/day + amoxicillin 1 g 2 p/day + josamycin 1 g 2 p/day; omeprazole 20 mg (or lansoprazole 30 mg or pantoprazole 40 mg or esomeprazole 20 mg or rabeprazole 20 mg) 2 p/day + amoxicillin 1 g 2 p/day + jozamycin 1 g 2 p/day + bismuth tricali dicitrate 240 mg 2 p/day; famotidine 40 mg/day + furazolidone 100 mg 2 p/day + josamycin 1 g 2 p/day + bismuth tricalium dicitrate 240 mg 2 p/day).

In case of gastric mucosal atrophy with achlorhydria confirmed by pH-metry: Amoxicillin 1 g 2 p/day + jozamycin 1 g 2 p/day + bismuth tricalium dicitrate 240 mg 2 p/day.

In cases of common and globular acne, we recommend prescribing giovamycin at a dose of 500 mg twice daily for the first 2-4 weeks, followed by 500 mg of giovamycin once daily as maintenance treatment for 8 weeks.

Interaction

– other antibiotics
Since bacteriostatic antibiotics in vitro may reduce the antimicrobial effect of bactericidal antibiotics, coadministration should be avoided. Josamycin should not be co-administered with lincosamides, since there may be a mutual reduction in their efficacy.

– Xanthines
Some members of the macrolide group slow the elimination of xanthines (theophylline), which may lead to signs of intoxication, Clinical and experimental studies indicate that giosamycin has less effect on the elimination of theophylline than other macrolides.

– Antihistamines
The risk of life-threatening arrhythmias may increase with co-administration of josamycin and antihistamines containing terfenadine or astemizole.

– Ergot alkaloids
There have been isolated reports of increased vasoconstriction after co-administration of ergot alkaloids and macrolide antibiotics, including a single observation with jozamycin.

– cyclosporine
Co-administration of jozamycin and cyclosporine may cause elevated plasma levels of cyclosporine and increase the risk of nephrotoxicity. Plasma concentrations of cyclosporine should be monitored regularly.

– Digoxin
When co-administering jozamycin and digoxin, the plasma level of the latter may increase.

Special Instructions

In case of persistent severe diarrhea it is necessary to keep in mind the possibility of development of life-threatening pseudomembranous colitis against the background of Gesamycin.

In patients with renal insufficiency the treatment should be carried out taking into account the results of appropriate laboratory tests (determination of endogenous creatinine clearance).

The possibility of cross-resistance to different antibiotics from the group of macrolides should be taken into account (microorganisms resistant to treatment with chemically related antibiotics may also be resistant to jozamycin).

Influence on the ability to drive and operate machinery
No effect of the drug on the ability to drive and operate machinery
has been noted.

Contraindications

Side effects

Unwanted reactions are listed by their frequency of registration according to the following grading: very common: >1/10, common: >1/100 to < 1/10, infrequent: >1/1000 to < 1/100, rare: >1/10 LLC to <1/1000, very rare from <1/10 000.

Gastrointestinal tract side:

Hypersensitivity reactions:

Hepatic and biliary tract disorders: Very rare – hepatic dysfunction, jaundice

Senses: In rare cases, dose-dependent, transient hearing impairment has been reported

Other: Very rare – purpura

Overdose

Pregnancy use

Similarities