Wilprafen granules for oral suspension 500mg/5ml, 20g

Composition

>of 1 fl. contains: Active ingredients: josamycin propionate – 6,307 g. Auxiliary substances:  sodium citrate – 0.1125 g, methyl parahydroxybenzoate – 0.0795 g, propyl parahydroxybenzoate – 0.0105 g, simethicone – 0.075 g, hyprolose – 0.3 g, avicel RC-591[microcrystalline cellulose, sodium carmellose] – 0.6 g, strawberry flavor – 0.05 g, betacarotene – 0.015 g, starch powder sucrose 3% – 10.2005 g, mannitol – 2.25 g. 5 ml of the finished suspension contains 500 mg of josamycin.

Pharmacological action

An antibiotic of the macrolide group. It has a bacteriostatic effect due to inhibition of protein synthesis by bacteria. When creating high concentrations in the focus of inflammation, it has a bactericidal effect.

Highly active against intracellular microorganisms: Chlamydia trachomatis and Chlamydia pneumonuae, 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.

Indications

Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to josamycin: upper respiratory tract and ENT infections (including pharyngitis, tonsillitis, paratonsillitis, otitis media, sinusitis, laryngitis); diphtheria (in addition to treatment with diphtheria antitoxin); scarlet fever (with hypersensitivity to penicillin); lower respiratory tract infections (including acute bronchitis, bronchopneumonia, pneumonia, including atypical form, whooping cough, psittacosis); infections of infections of the oral cavity (including gingivitis and periodontal diseases); skin and soft tissue infections (including pyoderma, boils, anthrax, erysipelas /with hypersensitivity to penicillin/, acne, lymphangitis, lymphadenitis); urinary tract and genital infections (including urethritis, prostatitis, gonorrhea; with hypersensitivity to penicillin-syphilis, venereal lymphogranuloma); chlamydia, mycoplasma (including ureaplasma) and mixed infections of the urinary tract and genitals.

Recommendations for use

The recommended daily dose of josamycin 50 mg / kg of body weight should be divided into 2 doses: 25 mg / kg in the morning and 25 mg / kg in the evening, not exceeding 1 g in each dose. The duration of treatment is determined by the doctor depending on the nature and severity of the infection and usually lasts at least 5-7 days. If you miss the next appointment, you should not take a double dose of the drug. According to WHO recommendations, the duration of treatment for streptococcal tonsillitis should be at least 10 days.

Contraindications

-Hypersensitivity to josamycin, excipients, and other macrolides;- use of the drug simultaneously with taking ergotamine, dihydroergotamine, cisapride, pimozide, ivabradine or colchicine ; – use of the drug by the mother during lactation of a child receiving cisapride therapy;- severe liver function disorders; – sucrose/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption. With caution: In patients with renal insufficiency, josamycin therapy should be carried out taking into account the results of appropriate laboratory tests (determination of endogenous creatinine clearance). Josamycin is not recommended for use in conjunction with the following medications: – Ebastinee, – dopamine receptor agonists: bromocriptine, cabergoline, lisuride, pergolide, – triazolam, – halofantrine, – disopyramide, – tacrolimus, – terfenadine and astemizole. Caution is required when josamycin is co-administered with the following medications: carbamazepine, cyclosporine, indirect anticoagulants, sildenafil, theophylline, aminophylline, digoxin.

Side effects

Disorders of the gastrointestinal tract: Nausea, vomiting, abdominal pain, diarrhea, pseudomembranous colitis, gastralgia, stomatitis, constipation. Skin and subcutaneous tissue disorders: Erythematous maculopapular rashes, erythema multiforme, bullous dermatitis, Stevens-Johnson syndrome, Lyell’s syndrome. Immune system disorders: Hypersensitivity reactions in the form of severe pruritus, urticaria, facial edema, angioedema( angioedema), difficulty breathing, anaphylactoid reactions and anaphylactic shock; Serum sickness. Liver and biliary tract disorders: Increased activity of transaminases and alkaline phosphatase, jaundice, cholestatic or cytolytic hepatitis. Vascular system disorders: Purpura, cutaneous vasculitis. Metabolic and nutritional disorders: Decreased appetite. If the listed reactions occur, as well as reactions that are not specified in the instructions, you should consult a doctor.

Interaction

The use of the following drugs together with josamycin is contraindicated due to the possibility of serious side effects: – Ergotamine, dihydroergotamine The result of interaction is the risk of severe vasoconstriction (ergotism) with the possible development of limb necrosis (due to inhibition of hepatic metabolism and elimination of ergot alkaloids). – Cisapride, Pimozidethe interaction increases the risk of developing life-threatening arrhythmias, including ventricular tachycardia of the “pirouette”type. – Ivabradin E As a result of interaction, the concentration of ivabradine in blood plasma increases and associated side effects (due to inhibition of hepatic metabolism of ivabradine). – Colchicine interaction results in an increased risk of colchicine side effects, including potentially fatal ones. The use of the following drugs together with josamycin is not recommended: – Ebastine Increased risk of life-threatening arrhythmias in patients with congenital long QT syndrome. – Dopamine receptor agonists (bromocriptine, cabergoline, lisuride, pergolide)An increase in the concentration of dopamine receptor agonists in blood plasma with a potential increase in their activity, the appearance of symptoms of overdose. – Triazolamnew cases of increased side effects of triazolam (behavioral disorders). – Halofantrine Increases the risk of ventricular arrhythmias, including ventricular tachycardia of the “pirouette” type (“torsades de pointes”). If possible, you should stop taking josamycin. If it is not possible to stop taking medications at the same time, monitoring of the QT interval and ECG is necessary. – Disopyramid Eincrease the risk of developing side effects of disopyramide: severe hypoglycemia, increased QT interval duration and life-threatening arrhythmias, including ventricular tachycardia of the “pirouette” type. It is necessary to monitor clinical and laboratory data, as well as regular ECG monitoring. – Tacrolimus Increased plasma concentrations of tacrolimus and creatinine as a result of inhibition of tacrolimus metabolism in the liver. – Terfenadine and astemizole Concomitant use of josamycin and antihistamines containing terfenadine or astemizole may increase the risk of life-threatening arrhythmias. The use of the following drugs together with josamycin requires caution: – Carbamazepine It is possible to increase the concentration of carbamazepine in blood plasma and develop symptoms of overdose due to inhibition of its hepatic metabolism. It is recommended to monitor the patient’s condition and the concentration of carbamazepine in the blood plasma. It may be necessary to reduce the dose of carbamazepine. – Cyclosporine concomitant use of josamycin and cyclosporine may cause increased levels of cyclosporine and creatinine in blood plasma and increase the risk of nephrotoxicity. Cyclosporine plasma concentrations and renal function should be monitored regularly. The dose of cyclosporine should be adjusted during co-use with josamycin, as well as after discontinuation of josamycin. – Indirect anticoagulants may increase the effect of indirect anticoagulants, increase the risk of bleeding. Frequent monitoring of international normalized relations (INR) is necessary. It may be necessary to reduce the dose of indirect anticoagulants during co-use with josamycin, and in some cases after discontinuation of josamycin. – Sildenafil: It is possible to increase the concentration of sildenafil in the blood plasma, increase the risk of arterial hypotension. If co-use is necessary, it is recommended to take the lowest dose of sildenafil. – Theophylline and aminophylline Caution should be exercised when using josamycin together with theophylline or aminophylline, as there is a risk of increasing the concentration of theophylline in blood plasma, especially in children. – Digoxin With the combined use of josamycin and digoxin, an increase in the level of the latter in blood plasma is possible. – Other antibacterial drugsas bacteriostatic antibiotics in vitro can reduce the antimicrobial effect of bactericidal antibiotics, their simultaneous use should be avoided. Josamycin should not be used concomitantly with lincosamides due to the possible mutual decrease in effectiveness.

Overdose

To date, there are no data on specific symptoms of overdose. In case of overdose, symptoms should be expected, especially from the gastrointestinal tract (in particular, nausea, diarrhea).

Treatment: in case of overdose, the unabsorbed drug should be removed from the gastrointestinal tract (gastric lavage, taking activated charcoal, etc. ) and symptomatic therapy should be performed.

Special instructions

If pseudomembranous colitis develops, josamycin should be discontinued and appropriate therapy should be prescribed. Medications that reduce intestinal motility are contraindicated.

In patients with renal insufficiency, dosage adjustment is required in accordance with the values of creatinine clearance.

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

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

Storage conditions

Store at a temperature not exceeding 25 °C.

Store the suspension at room temperature.

Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package. The shelf life of the suspension is 7 days from the moment of preparation.

Active ingredient

Josamycin

Conditions of release from pharmacies

By prescription

Dosage form

suspension for external use