Vilpramycin Sar^® (Tablets) Instructions for Use

Marketing Authorization Holder

Promomed Rus LLC (Russia)

Manufactured By

Biokhimik, JSC (Russia)

ATC Code

J01FA07 (Josamycin)

Active Substance

Josamycin (Rec.INN registered by WHO)

Dosage Form

Vilpramycin Sar®

Dispersible tablets 1000 mg: 5, 7, 10, 14 or 28 pcs.

Dosage Form, Packaging, and Composition

Dispersible tablets almost white or white with a yellowish tint or yellow, oval, biconvex with a score on one side, with a strawberry odor.

Excipients : microcrystalline cellulose – 564.53 mg, low-substituted hypromellose (LH 22) – 199.82 mg, docusate sodium – 10.02 mg, aspartame (E951) – 10.09 mg, colloidal silicon dioxide – 2.91 mg, strawberry flavor – 50.05 mg, magnesium stearate – 34.92 mg.

5 pcs. – contour cell packs (1) – cardboard packs.
5 pcs. – contour cell packs (2) – cardboard packs.
7 pcs. – polyethylene jars (1) – cardboard packs.
14 pcs. – polyethylene jars (1) – cardboard packs.
28 pcs. – polyethylene jars (1) – cardboard packs.

Clinical-Pharmacological Group

Antibiotic of the macrolide group

Pharmacotherapeutic Group

Antibiotic-macrolide

Pharmacological Action

An antibiotic of the macrolide group. It has a bacteriostatic effect due to the inhibition of bacterial protein synthesis. When high concentrations are created 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 concentration of josamycin in plasma is 2.41 mg/L.

Plasma protein binding does not exceed 15%.

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

Josamycin is well distributed in the body and accumulates in various tissues: in 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 into less active metabolites.

It is excreted mainly with bile; excretion in 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 (in addition 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 form, 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 orally. For adults and children over 14 years, the total daily dose is 1-2 g. Divide this dose into 2-3 equal administrations.

For children under 14 years, calculate the dose based on body weight. The total daily dose is 30-50 mg/kg. Divide this daily dose into 3 equal administrations.

Take tablets at regular intervals to maintain stable antibiotic concentrations. The duration of treatment is determined by the type and severity of the infection. Complete the full prescribed course, even if symptoms improve.

For severe infections, use the higher end of the recommended dosage range. Adjust the dosage regimen for patients with renal impairment based on creatinine clearance values.

Do not administer to premature infants. Monitor liver function in newborns. In case of renal failure, adjust the dose according to creatinine clearance.

Adverse Reactions

From the digestive system rarely – loss of appetite, nausea, heartburn, vomiting, diarrhea, pseudomembranous colitis; in some cases – increased activity of hepatic 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 failure, dose regimen adjustment is required according to 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 should be prescribed. Drugs that reduce intestinal motility are contraindicated.

In patients with renal failure, dose regimen adjustment is required according to 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 (simultaneous use of josamycin with penicillins and cephalosporins should be avoided).

With simultaneous use of josamycin with lincomycin, a decrease in the effectiveness of both drugs is possible.

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 simultaneous use of macrolide antibiotics and ergot alkaloids. One case of ergotamine intolerance while taking josamycin has been noted.

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.