Vilprafen tablets 500mg, No. 10

• Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to josamycin: infections of the upper respiratory tract and ENT organs (including pharyngitis, tonsillitis, paratonsillitis, otitis media, sinusitis, laryngitis);

• diphtheria (in addition to treatment with diphtheria antitoxin);

• scarlet fever (with increased sensitivity to penicillin);

• infections of the lower respiratory tract (including acute bronchitis, bronchopneumonia, pneumonia, including atypical form, whooping cough, psittacosis);

• oral cavity infections (including gingivitis and periodontal disease);

• infections of the skin and soft tissues (including pyoderma, boils, anthrax, erysipelas / with hypersensitivity to penicillin /, acne, lymphangitis, lymphadenitis);

• infections of the urinary tract and genital organs (including urethritis, prostatitis, gonorrhea; with hypersensitivity to penicillin - syphilis, lymphogranuloma venereum);

• chlamydial, mycoplasma (including ureaplasma) and mixed infections of the urinary tract and genitals.

When taken orally for adults and children over 14 years old - 1-2 g / day in 2-3 doses. Children under the age of 14 - 30-50 mg / kg / day in 3 divided doses. The duration of treatment depends on the indications for use.

Film-coated tablets

1 tab. josamycin

• Severe liver dysfunction,

• hypersensitivity to josamycin and other macrolide antibiotics.

pharmachologic effect

Antibiotic of the macrolide group. It has a bacteriostatic effect due to inhibition of protein synthesis by bacteria. When high concentrations are created 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; in relation to 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; for 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. Cmax is achieved within 1-2 hours after administration. 45 minutes after taking a dose of 1 g, the average plasma concentration of josamycin is 2.41 mg / l. Plasma protein binding does not exceed 15%. The equilibrium state is achieved after 2-4 days of regular intake. Josamycin is well distributed in the body and accumulates in various tissues: in the lung, lymphatic tissue of the tonsils, organs of the urinary system, skin and soft tissues. Especially high concentrations are found in the lungs, tonsils, saliva, sweat and lacrimal 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%.

Side effect

From the digestive system: rarely - lack of appetite, nausea, heartburn, vomiting, diarrhea, pseudomembranous colitis; in some cases - increased activity of hepatic transaminases, impaired outflow of bile and jaundice. Allergic reactions: rarely - urticaria. Others: in some cases - dose-dependent transient hearing impairment.

Application during pregnancy and lactation

Application during pregnancy and lactation is possible only in cases where the intended benefit to the mother outweighs the potential risk to the fetus or child. When treating with macrolides and the simultaneous use of hormonal contraceptives, non-hormonal contraception should be additionally used.

Application for violations of liver function

Contraindicated in severe liver dysfunction.

Application for impaired renal function

In patients with renal insufficiency, the dosage regimen must be adjusted in accordance with the CC values.

Application in children

Josamycin is not prescribed for premature babies. When used in newborns, it is necessary to monitor liver function.

special instructions

If pseudomembranous colitis develops, josamycin should be discontinued and appropriate therapy should be prescribed. Drugs that reduce intestinal motility are contraindicated. In patients with renal insufficiency, the dosage regimen must be adjusted in accordance with the CC values. Josamycin is not prescribed for premature babies. When used in newborns, it is necessary to monitor liver function. Consideration should be given to the possibility of cross-resistance to various antibiotics of the macrolide group (for example, microorganisms that are resistant to treatment with chemically related antibiotics may also be resistant to josamycin).

Drug interactions

Bacteriostatic antibiotics can reduce the bactericidal effect of other antibiotics, such as penicillins and cephalosporins (concomitant use of josamycin with penicillins and cephalosporins should be avoided). With the simultaneous use of josamycin with lincomycin, the effectiveness of both drugs may decrease. Josamycin slows down the excretion of theophylline to a lesser extent than other antibiotics of the macrolide group. Josamycin slows down the elimination of terfenadine or astemizole, which increases the risk of life-threatening arrhythmias. There are separate reports of increased vasoconstrictor action with the simultaneous use of antibiotics of the macrolide group and ergot alkaloids. There was 1 case of intolerance to ergotamine while taking josamycin.With the simultaneous use of josamycin and cyclosporine, it is possible to increase the concentration of cyclosporine in the blood plasma up to nephrotoxic. With the simultaneous use of josamycin and digoxin, an increase in the level of the latter in the blood plasma is possible. In rare cases, against the background of treatment with macrolides, the contraceptive effect of hormonal contraceptives may be insufficient.