Pharmacodynamics
The drug is used to treat bacterial infections; The bacteriostatic activity of josamycin, like other macrolide antibiotics, is due to inhibition of protein synthesis by bacteria. When high concentrations are created at the site of inflammation, it has a bactericidal effect.
Josamycin is highly active against intracellular microorganisms (Chlamydia trachomatis and Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycoplasma hominis, Ureaplasma urealyticum, Legionella pneumophila), gram-positive bacteria (Staphylococcus aureus, Streptococcus pyogenes and Streptococcus pneumoniae (pneumococcus), gram-negative bacteria (Neisseria meningitidis, Neisseria gonorrhoeae , Haemophilus influenzae, Bordetella pertussis, Helicobacter pylori), as well as against some anaerobic bacteria (Peptococcus, Peptostreptococcus, Clostridium perfringens).
Pharmacological properties of the drug Vilprafen
Pharmacodynamics . Josamycin is a broad-spectrum macrolide antibiotic. Active against gram-positive and gram-negative microorganisms, including obligate anaerobes. The drug is also active against mycoplasmas and chlamydia. Pharmacokinetics After oral administration, the drug is rapidly absorbed into the gastrointestinal tract. The maximum concentration in blood plasma is achieved 1 hour after administration. 45 minutes after taking 1 g of the drug, the average concentration of josamycin in the blood plasma is 2.4 mg/l. Josamycin penetrates well through biological membranes and accumulates in various tissues and organs: pulmonary, lymphatic, skin and soft tissues, tonsils, and organs of the urinary system. Binding to plasma proteins does not exceed 15%. Josamycin is metabolized in the liver and is slowly excreted in bile and in small amounts (≤15%) in urine.
Side effects
From the gastrointestinal tract: rarely - loss of appetite, nausea, heartburn, vomiting and diarrhea. In cases of persistent severe diarrhea, the possibility of developing life-threatening pseudomembranous colitis due to antibiotics should be kept in mind.
Hypersensitivity reactions: in extremely rare cases, allergic skin reactions (eg urticaria) are possible.
From the liver and biliary tract: in some cases, a transient increase in the activity of liver enzymes in the blood plasma was observed, in rare cases accompanied by a violation of the outflow of bile and jaundice.
From the hearing system: in rare cases, dose-dependent transient hearing impairment has been reported.
Vilprafen
Vilprafen (INN josamycin) is a macrolide antibiotic. It exhibits bacteriostatic and, in high concentrations, bactericidal action. Effective in the treatment of infections caused by staphylococci (including those producing penicillinase), streptococci, corynebacteria, neisseria, Haemophilus influenzae, bordetella, rickettsia, treponema, mycoplasma, chlamydia, some types of shigella, ureaplasma, clostridia. It has virtually no effect on enterobacteria, therefore it does not introduce an imbalance into the natural microflora of the gastrointestinal tract. Can be used in cases of resistance to erythromycin. Resistance to Vilprafen itself develops less frequently and more slowly than to other macrolides. One of the advantages of the drug is its lipophilicity, which ensures rapid penetration of the active substance in therapeutic concentrations into cells and tissues. When using tablet forms of josamycin, its concentration in white blood cells, epithelial cells, macrophages, phagocytes and monocytes is 20 times higher than in the interstitial space. This property of the drug makes it an ideal means of combating chlamydial infections, because The life cycle of these bacteria takes place inside the cell. Compared to other antibiotics, Vilprafen has a very high cure rate for chlamydia - 97% (azithromycin - 55%, doxycycline - 50%). The wide range of therapeutic effects of Vilprafen allows its use in the treatment of mixed bacterial infections, incl. caused by representatives of anaerobic microflora. The drug is practically devoid of teratogenic and embryotoxic effects, which makes it available to pregnant women and provides effective prevention of chlamydia in the neonatal period.
In addition to infections of the genitourinary tract, Vilprafen is used in the treatment of infections of the ENT organs, respiratory tract, oral cavity, soft tissues, and dermatological infections. After oral administration, it is quickly and completely absorbed from the digestive tract. The presence of food masses in the intestines does not affect the bioavailability of the drug (i.e. it can be taken regardless of meals, which is very convenient). The maximum concentration of the active substance in the blood is observed 1-2 hours after administration. It undergoes metabolic transformations in the liver, and the resulting metabolites have less therapeutic activity than the original substance. It is excreted from the body through the biliary (with bile) and genitourinary (with urine) tract. It has a small number of side effects, mainly from the digestive tract (appetite disturbance, nausea, dyspepsia, abdominal cramps, impaired choleretic function). When prescribing Vilprafen, it is necessary to take into account the possibility of adverse interactions with co-administered medications. Thus, this antibiotic slows down the elimination of the antiallergic drugs astemizole and terfenadine, which can lead to the development of severe ventricular arrhythmias. Vilprafen also potentiates the side effects of theophylline, digoxin, and ergot alkaloids (vasoconstrictor effect). And the other side of the coin: Vilprafen can reduce the effectiveness of penicillin and cephalosporin antibiotics, and in combination with lincomycin, the effectiveness of both drugs decreases. For elderly patients, Vilprafen is prescribed in lower doses. ECG monitoring is mandatory in persons concomitantly taking digoxin.
Interaction
Vilprafen/other antibiotics. Since bacteriostatic antibiotics can reduce the bactericidal effect of other antibiotics, such as penicillins and cephalosporins, co-administration of josamycin with these types of antibiotics should be avoided. Josamycin should not be prescribed together with lincomycin, because a mutual decrease in their effectiveness is possible.
Vilprafen/xanthines. Some representatives of macrolide antibiotics slow down the elimination of xanthines (theophylline), which can lead to possible intoxication. Clinical experimental studies indicate that josamycin has less effect on theophylline release than other macrolide antibiotics.
Vilprafen/antihistamines. After co-administration of josamycin and antihistamines containing terfenadine or astemizole, there may be a slowdown in the elimination of terfenadine and astemizole, which, in turn, can lead to the development of life-threatening cardiac arrhythmias.
Vilprafen/ergot alkaloids. There are individual reports of increased vasoconstriction following coadministration of ergot alkaloids and macrolide antibiotics. There was one case of patient's lack of tolerance to ergotamine while taking josamycin.
Therefore, the concomitant use of josamycin and ergotamine should be accompanied by appropriate monitoring of patients.
Vilprafen/cyclosporine. Co-administration of josamycin and cyclosporine may cause an increase in the level of cyclosporine in the blood plasma and the creation of nephrotoxic concentrations of cyclosporine in the blood. Plasma concentrations of cyclosporine should be regularly monitored.
Vilprafen/digoxin. When administered together, josamycin and digoxin may increase the level of the latter in the blood plasma.
Vilprafen/hormonal contraceptives. In rare cases, the contraceptive effect of hormonal contraceptives may be insufficient during treatment with macrolides. In this case, it is recommended to additionally use non-hormonal contraception.
Drug interactions Vilprafen
Since bacteriostatic antibiotics, such as josamycin and bactericidal antibiotics, can interact with each other, the need for simultaneous use of Vilprafen with these antibiotics must be carefully considered. When used simultaneously with lincomycin, the effectiveness of Vilprafen may be reduced. After simultaneous use of Vilprafen and antihistamines that contain terfenadine or astemizole, a slowdown in the elimination of antihistamines may be observed, which in turn can cause life-threatening cardiac arrhythmias. When using Vilprafen together with ergot alkaloids, the possibility of developing a pronounced vasoconstrictor effect should be taken into account. The simultaneous administration of Vilprafen and cyclosporine may lead to an increase in the level of cyclosporine in the blood plasma, which in turn can cause renal dysfunction. With the simultaneous use of Vilprafen and digoxin, an increase in the level of digoxin in the blood plasma is possible.
Directions for use and doses
Inside, swallow whole, with a small amount of water. The recommended daily dose for adults and adolescents over 14 years of age is 1 to 2 g of josamycin. The daily dose should be divided into 2-3 doses. The initial recommended dose is 1 g of josamycin. In the case of acne vulgaris and globulus, it is recommended to prescribe josamycin at a dose of 500 mg 2 times a day for the first 2-4 weeks, then 500 mg josamycin once a day as maintenance treatment for 8 weeks. To achieve optimal serum concentrations, individual doses should be taken between meals.
Usually the duration of treatment is determined by the doctor. In accordance with the recommendations of the World Health Organization on the use of antibiotics, the duration of treatment for streptococcal infections should be at least 10 days.
If one dose is missed, you must immediately take a dose of the drug. However, if it is time for the next dose, do not take the “forgotten” dose, but return to your normal treatment regimen. You should not take double the dose.
A break in treatment or premature discontinuation of the drug will reduce the likelihood of treatment success.
Use of the drug Vilprafen
The recommended dose for adults and children weighing 40 kg is 1 g (initial); then the drug is prescribed 1–2 g per day (2–4 tablets) in 2–3 doses. In severe cases of the disease, the dose can be increased to 3 g. The recommended dose for children over 5 years old weighing ≤40 kg is 40–50 mg/kg body weight per day, divided into several doses. If precise dosing is not possible, the drug for children is used in the form of a suspension. Take the tablets without chewing with a small amount of liquid between meals. The duration of treatment is determined by the doctor. According to WHO recommendations regarding the use of antibiotics, the duration of treatment for streptococcal infections is at least 10 days.
special instructions
In patients with renal failure, treatment should be carried out taking into account the results of appropriate laboratory tests.
The possibility of cross-resistance to various macrolide antibiotics should be taken into account (for example, microorganisms that are resistant to treatment with antibiotics related in chemical structure may also be resistant to josamycin).
Although there is no information about embryotoxic effects, Vilprafen should be prescribed to pregnant and breastfeeding women only after a careful assessment of the risk-benefit ratio of treatment.
Special instructions for the use of the drug Vilprafen
If pseudomembranous colitis develops, the drug must be discontinued and appropriate therapy prescribed. In patients with impaired liver and biliary tract function, treatment is carried out taking into account the results of laboratory tests (for therapy lasting more than 15 days). During pregnancy and breastfeeding . Despite the current lack of data regarding the embryotoxic effect of josamycin, the use of the drug during pregnancy and lactation is permissible in exceptional cases after assessing the risk/benefit ratio of therapy. Use in children. The drug can be used in children over 5 years of age. For children under 5 years of age, as well as when precise dosing is impossible, the drug is prescribed in the form of a suspension. no negative effects on reaction speed when driving vehicles or operating machinery .
