Wilprafen^® (Tablets, Granules) Instructions for Use

ATC Code

J01FA07 (Josamycin)

Active Substance

Josamycin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antibiotic of the macrolide group

Pharmacotherapeutic Group

Antibiotic-macrolide

Pharmacological Action

An antibiotic of the macrolide group. It exerts a bacteriostatic effect by inhibiting bacterial protein synthesis. When high concentrations are achieved at the site of inflammation, it exerts a bactericidal effect.

It is highly active against intracellular microorganisms: Chlamydia trachomatis and Chlamydia pneumoniae, 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. C_max is reached 1-2 hours after administration. Forty-five minutes after a 1 g dose, the average plasma concentration of josamycin is 2.41 mg/L.

Binding to plasma proteins does not exceed 15%.

Steady state is achieved after 2-4 days of regular administration.

Josamycin is well distributed in the body and accumulates in various tissues: in the lung tissue, lymphatic tissue of the palatine tonsils, organs of the urinary system, skin, and soft tissues. Particularly high concentrations are found 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.

It is excreted mainly in the bile; excretion in the urine is less than 20%.

Indications

Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to josamycin: infections of the upper respiratory tract and ENT organs (including pharyngitis, tonsillitis, peritonsillitis, otitis media, sinusitis, laryngitis); diphtheria (as an adjunct to treatment with diphtheria antitoxin); scarlet fever (in case of hypersensitivity to penicillin); infections of the lower respiratory tract (including acute bronchitis, bronchopneumonia, pneumonia, including atypical forms, whooping cough, psittacosis); oral infections (including gingivitis and periodontal diseases); skin and soft tissue infections (including pyoderma, furuncles, anthrax, erysipelas /in case of hypersensitivity to penicillin/, acne, lymphangitis, lymphadenitis); infections of the urinary tract and genital organs (including urethritis, prostatitis, gonorrhea; in case of hypersensitivity to penicillin – syphilis, venereal lymphogranuloma); chlamydial, mycoplasmal (including ureaplasmal) and mixed infections of the urinary tract and genital organs.

ICD codes

Dosage Regimen

Administer the drug orally.

For adults and children over 14 years, the total daily dose is 1-2 g.

Divide the total daily dose into 2-3 doses.

For children under 14 years, calculate the dose based on body weight.

The total daily dose for children is 30-50 mg per kg of body weight.

Divide the total daily dose for children into 3 equal doses.

For severe infections, increase the total daily dose for adults to 2-3 g.

In severe infections, divide the higher dose into 2-3 doses.

For the treatment of sexually transmitted infections like urethritis, administer a single dose of 1-2 g.

For gonorrhea, take a single dose of 1 g.

For syphilis, the total daily dose is 1.5-2 g divided into 2-3 doses.

The typical treatment duration for syphilis is 10-15 days.

For chlamydial, mycoplasmal, and ureaplasmal infections, the typical treatment course is 7-14 days.

For streptococcal infections, continue treatment for at least 10 days to prevent complications.

Take the tablets or granules between meals for optimal absorption.

Adhere strictly to the prescribed dosage and duration of therapy.

Do not discontinue treatment prematurely, even if symptoms improve.

In patients with renal impairment, adjust the dosage based on creatinine clearance values.

For patients with severe renal insufficiency, reduce the dosing frequency or the total daily dose.

Adverse Reactions

From the digestive system rarely – loss of appetite, nausea, heartburn, vomiting, diarrhea, pseudomembranous colitis; in some cases – increased activity of liver transaminases, impaired bile flow, and jaundice.

Allergic reactions rarely – urticaria.

Other in some cases – dose-dependent transient hearing impairment.

Contraindications

Severe liver dysfunction, hypersensitivity to josamycin and other antibiotics of the macrolide group.

Use in Pregnancy and Lactation

Use during pregnancy and lactation is only possible in cases where the intended benefit to the mother outweighs the potential risk to the fetus or child.

When treating with macrolides and simultaneously using hormonal contraceptives, non-hormonal contraceptive methods should be additionally used.

Use in Hepatic Impairment

Contraindicated in severe liver dysfunction.

Use in Renal Impairment

In patients with renal insufficiency, dose adjustment is required according to the creatinine clearance values.

Pediatric Use

Josamycin is not prescribed to premature infants. When used in newborns, liver function should be monitored.

Special Precautions

In case of pseudomembranous colitis development, Josamycin should be discontinued and appropriate therapy instituted. Drugs that reduce intestinal motility are contraindicated.

In patients with renal insufficiency, dose adjustment is required according to the creatinine clearance values.

Josamycin is not prescribed to premature infants. When used in newborns, liver function should be monitored.

The possibility of cross-resistance to various antibiotics of the macrolide group should be considered (for example, microorganisms resistant to treatment with chemically related antibiotics may also be resistant to josamycin).

Drug Interactions

Bacteriostatic antibiotics may reduce the bactericidal effect of other antibiotics, such as penicillins and cephalosporins (concomitant use of josamycin with penicillins and cephalosporins should be avoided).

With simultaneous use of josamycin and lincomycin, the effectiveness of both drugs may be reduced.

Josamycin slows 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 an increased vasoconstrictor effect with the simultaneous use of macrolide antibiotics and ergot alkaloids. One case of ergotamine intolerance during josamycin administration has been reported.

With simultaneous use of josamycin and cyclosporine, an increase in the plasma concentration of cyclosporine up to nephrotoxic levels is possible.

With simultaneous use of josamycin and digoxin, an increase in the plasma level of the latter is possible.

In rare cases, during treatment with macrolides, the contraceptive effect of hormonal contraceptives may be insufficient.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.