Wilprafen pills 500mg, 10pcs

Composition

Active Ingredients:

Josamycin-500 mg

Auxiliary ingredients to the mass of 640 mg tablets:

microcrystalline cellulose – 101,0 mg,

Polysorbate 80 – 5.0 mg,

silicon dioxide colloid – 14.0 mg,

carmellose sodium – 10.0 mg,

magnesium stearate – 5.0 mg,

cellulose – 0,12825 mg

polyethylene glycol 6000 – 0,3846 mg,

talc – 2,0513 mg,

titanium dioxide – 0,641 mg

of aluminium hydroxide 0,641 mg,

copolymer of methacrylic acid and its esters – 1,15385 mg.

Pharmacological properties

Pharmacotherapeutic group:  an antibiotic, a macrolide.

ATX code: J01FA07

Pharmacological properties

Pharmacodynamics .

An antibacterial drug from the macrolide group. The mechanism of action is associated with a violation of protein synthesis in the microbial cell due to reversible binding to the 50S subunit of the ribosome. In therapeutic concentrations, as a rule, it has a bacteriostatic effect, slowing down the growth and reproduction of bacteria. When creating high concentrations in the focus of inflammation, it has a bactericidal effect.

Josamycin is active against gram-positive bacteria (Staphylococcus spp., including methicillin-sensitive strains 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), sensitivity Bacteroides fragilis can be variable), Chlamydia spp., including C. trachomatis, Chlamydophila spp., including Chlamydophila pneumoniae (previously 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 enterobacteria, so it has little effect on the microflora of the gastrointestinal tract. It remains active against resistance to erythromycin and other 14-and 15-membered macrolides. Resistance to josamycin is less common than to 14-and 15-membered macrolides.

Pharmacokinetics.

After oral use, josamycin is rapidly absorbed from the gastrointestinal tract, and food intake does not affect bioavailability. The maximum concentration of josamycin in plasma is reached 1 hour after use. When taken at a dose of 1 g, the maximum concentration in blood plasma is 2-3 mcg/ml. About 15% of josamycin binds to plasma proteins. Josamycin is well distributed in organs and tissues (with the exception of the brain), creating concentrations that exceed plasma and remain at the therapeutic level for a long time. Josamycin creates particularly high concentrations in the lungs, tonsils, saliva, sweat, and tear fluid. The concentration in sputum exceeds the concentration in plasma by 8-9 times. Passes the placental barrier, is secreted into breast milk. Josamycin is metabolized in the liver to less active metabolites and is mainly excreted in the bile. The half-life of the drug is 1-2 hours, but may be prolonged in patients with impaired liver function. Renal excretion of the drug does not exceed 10%.

Indications

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

Upper respiratory tract and ENT infections: tonsillitis, pharyngitis, paratonsillitis, laryngitis, otitis media, sinusitis, diphtheria (in addition to treatment with diphtheria toxoid), scarlet fever (in case of hypersensitivity to penicillin).

Lower respiratory tract infections: acute bronchitis, exacerbation of chronic bronchitis, community-acquired pneumonia, including those 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, furuncle, furunculosis, abscess, anthrax, erysipelas, acne, lymphangitis, lymphadenitis, phlegmon, panaritium, wound (including postoperative) and burn infections.

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

Diseases of the gastrointestinal tract associated with H. Pylori Ulcer of the stomach and duodenum, chronic gastritis, etc.

Use during pregnancy and lactation

It is allowed to use during pregnancy and lactation after a medical assessment of the benefit/risk. The WHO European Office recommends josamycin as the drug of choice for the treatment of chlamydia infection in pregnant women.

Contraindications

• hypersensitivity to josamycin and other components of the drug
• hypersensitivity to other macrolides;
• severe liver function disorders:
• children weighing less than 10 kg.

Side effects

Adverse reactions are listed by frequency of their registration, in accordance with the following gradation: very often: from >1/10, often from >1/100 to < 1/10, uncommon: from >1/1000 to < 1/100, rare: from >1/10, OOO to <1/1000, very rare from <1/10 000.

From the gastrointestinal tract:

• Often – stomach discomfort, nausea
• Infrequently – abdominal discomfort, vomiting, diarrhea
• Rarely-stomatitis, constipation, decreased appetite
• Very rare – pseudomembranous colitis

Hypersensitivity reactions:

• Rarely – urticaria, angioedema and anaphylactoid reaction.
• Very rarely – bullous dermatitis, erythema multiforme, including Stephen-Johnson syndrome.

From the liver and biliary tract: Very rarely-hepatic dysfunction, jaundice

Sensory disorders: Rare cases of dose-dependent, transient hearing loss have been reported

Other: very rare – purple

Interaction

– other antibiotics Since in vitro bacteriostatic antibiotics may reduce the antimicrobial effect of bactericidal ones, their co-use should be avoided. Josamycin should not be administered together with lincosamides, as their effectiveness may be mutually reduced.

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

– Antihistamines When josamycin is co-administered with antihistamines containing terfenadine or astemizole, the risk of life-threatening arrhythmias may increase.

– Ergot alkaloids There have been isolated reports of increased vasoconstriction after co-use of ergot alkaloids and macrolide antibiotics, including a single observation while taking josamycin.

– Cyclosporine concomitant use of josamycin and cyclosporine may cause an increase in the level of cyclosporine in blood plasma and increase the risk of nephrotoxicity. The plasma concentration of cyclosporine should be monitored regularly.

– Digoxin With the combined use of josamycin and digoxin, an increase in the level of the latter in blood plasma is possible.

How to take, course of use and dosage

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

Usually, the duration of treatment is determined by the doctor, ranging from 5 to 21 days, depending on the nature and severity of the infection. According to WHO recommendations, the duration of treatment for streptococcal tonsillitis should be at least 10 days.

In antihelicobacter therapy schemes, josamycin is prescribed at 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 r/day + amoxicillin 1 g 2 r/day + josamycin 1 g 2 r/day; omeprazole 20 mg (or lansoprazole 30 mg, or pantoprazole 40 mg, or esomeprazole 20 mg, or rabeprazole 20 mg) 2 r/day + amoxicillin 1 g 2 r/day + josamycin 1 g 2 r/day + bismuth tricalium dicitrate 240 mg 2 r/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 the presence of atrophy of the gastric mucosa with achlorhydria, confirmed by pH-metry: Amoxicillin 1 g 2 p/day + josamycin 1 g 2 p / day + bismuth tricalium dicitrate 240 mg 2 p / day.

In the case of common and globular acne, it is recommended to prescribe josamycin at a dose of 500 mg twice a day for the first 2-4 weeks, then 500 mg of josamycin once a day as a maintenance treatment for 8 weeks.

Overdose

To date, there are no data on specific symptoms of poisoning.

In case of overdose, the symptoms described in the section “Side effects” should be expected to occur, especially from the gastrointestinal tract.

Special instructions

In the case of persistent severe diarrhea, the possibility of developing life-threatening pseudomembranous colitis with josamycin should be borne in mind.

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

Consideration should be given to the possibility of cross-resistance to various macrolide antibiotics (microorganisms resistant to treatment with chemically related antibiotics may also be resistant to josamycin).

Effect on the ability to drive vehicles and work with mechanisms No effect of the drug on the ability to drive vehicles and work with mechanisms was observed.

Form of production

Film-coated tablets

Storage conditions

In a dark place, at a temperature not exceeding 25 °C

Shelf life

4 years

Active ingredient

Josamycin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as prescribed by a doctor, Children as prescribed by a doctor, Nursing mothers as prescribed by a doctor, Pregnant women as prescribed by a doctor

Indications

Pharyngitis, Laryngitis, Gastric and duodenal ulcers, Respiratory tract infections, Chlamydia, Gastritis, Otitis media, Chronic infections, Whooping cough, Pneumonia, Purulent wounds, Blepharitis