Wilprafen® [Josamycin]

Pharmacological properties

Josamycin is an antibiotic of the broad-spectrum macrolide group; it is active against gram-positive and gram-negative microorganisms, including obligate anaerobes. the drug is used to treat bacterial infections; the bacteriostatic activity of josamycin, like other macrolides, is due to inhibition of bacterial protein synthesis.

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), Corynebacterium diphteriae), Gram-negative bacteria (Neisseria meningitidis, Neisseria gonorrhoeae, Haemophilus influenzae, Bordetella perococcus peptocens, Peptocris peptissis) Slightly affects enterobacteria, therefore, little changes the natural bacterial flora of the gastrointestinal tract. Effective for resistance to erythromycin. Resistance to josamycin develops less frequently than to other antibiotics of the macrolide group.

Pharmacokinetics Josamycin is acid resistant, therefore, after oral administration, the drug is rapidly absorbed in the digestive tract. C_max Wilprafen in plasma is reached after 1 hour, and Wilprafen Solutab 1–2 hours 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: in the pulmonary and lymphatic tissues, tonsils, urinary organs, skin and soft tissues. Plasma protein binding does not exceed 15%. Josamycin is metabolized in the liver and slowly excreted in the bile, and in a small amount (less than 15%) in the urine.

Indications

Infectious diseases caused by microorganisms sensitive to josamycin:

• infections of the ENT organs;
• respiratory tract infections;
• dental infections;
• infections of the skin and soft tissues;
• infections of the genitourinary system.

The use of Wilprafen and Wilprafen Solutab is also recommended for allergic reactions to penicillin.

Application

Wilprafen. the recommended dose of Wilprafen for adults is 1–2 g (2–4 tablets) in 2–3 doses. in severe cases of the disease, the dose can be increased to 3 g or more.

The recommended dose for children over 5 years old is 50 mg / kg body weight per day, divided into several doses. To achieve a clear dosage, other dosage forms of the drug are used.

The tablets should be swallowed whole, without chewing, with a small amount of liquid. The drug is used between meals.

The duration of treatment is determined by the doctor. According to WHO recommendations for the use of antibiotics, the duration of treatment for streptococcal infections is at least 10 days.

Wilprafen Solutab. The recommended daily dose for adults is 1.5–2 g. In severe cases, the dose can be increased to 3 g. The daily dose is divided into 2–3 doses.

The recommended dose for children (over 5 years of age) is 40-50 mg / kg / day, divided into 2-3 doses. Dispersible tablets can be taken in 2 ways: 1) swallow whole, washed down with water; 2) pre-dissolve the tablet in water. Tablets should be dissolved in at least 20 ml of water. Stir the resulting suspension thoroughly before use.

The duration of treatment is determined by the doctor. Therapy should be continued for another 48 hours after the disappearance of the symptoms of the disease and normalization of body temperature.

Contraindications

Hypersensitivity to the components of the drug and other antibiotics of the macrolide group, severe dysfunction of the liver and biliary tract. due to the content of aspartame solutab in Wilprafen, the drug is contraindicated in patients with phenylketonuria.

Side effects

From the digestive tract: anorexia, stomach discomfort, nausea, abdominal discomfort, vomiting, diarrhea, stomatitis, constipation, loss of appetite, pseudomembranous colitis.

From the side of the immune system: angioedema (Quincke) and anaphylactic reactions.

On the part of the skin and subcutaneous tissue: urticaria and other skin reactions, bullous dermatitis, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, purpura, facial edema.

From the hepatobiliary system: impaired liver function, which is usually manifested, but not limited to, cholestatic reactions with moderate liver damage; jaundice.

special instructions

In the case of pseudomembranous colitis, the drug must be discontinued and appropriate therapy prescribed.

As a rule, with a treatment duration of more than 15 days in patients with diseases of the liver and biliary tract, it is necessary to control liver function.

In patients with impaired liver function, the drug should be prescribed with caution and the concentration of the drug in the blood plasma should be determined.

The possibility of cross-resistance to various macrolide antibiotics should be taken into account (for example, microorganisms that are resistant to treatment with antibiotic-related antibiotics may also be resistant to josamycin).

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 the doctor has evaluated the risk / benefit ratio of therapy.

Children. The drug is used in children over the age of 5 years due to the lack of the possibility of a clear dosage of josamycin in the dosage form of a tablet in children under the age of 5 years. In children under the age of 5 years, the drug is used in the form of a suspension.

There was no negative effect on the reaction rate when driving vehicles and working with other mechanisms.

Interactions

Since bacteriostatic antibiotics, such as josamycin, and bactericidal antibiotics can interact with each other, the need for simultaneous use of josamycin with these drugs should be carefully considered.

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

After the simultaneous use of josamycin and antihistamines that contain terfenadine or astemizole, it is possible to slow the elimination of antihistamines, which, in turn, can cause life-threatening heart rhythm disturbances.

With the combined use of josamycin with ergot alkaloids, the possibility of developing a pronounced vasoconstrictor effect should be taken into account.

The simultaneous use of josamycin and cyclosporine can lead to an increase in the level of cyclosporin in the blood plasma, which, in turn, can cause impaired renal function.

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

Josamycin may induce an increase in plasma theophylline levels by increasing T_½ theophylline. In case of theophylline-induced toxicity, additional doses of theophylline should be adjusted accordingly in order to control plasma concentration.

Josamycin can enhance the effects of triazolam, which can cause drowsiness. In case of an overdose of triazolam, a temporary discontinuation of the drug is recommended.

Josamycin may enhance the effects of bromocriptine mesylate and cause drowsiness, dizziness, ataxia, and other complications. In the case of bromocriptine intoxication with mesylate, a temporary cessation of its use is recommended.

Josamycin can enhance the effects of oral anticoagulants, such as warfarin and its derivatives, which are antagonists of vitamin K. Josamycin reduces the production of vitamin K by intestinal bacteria.In the event of bleeding, withdrawal of josamycin and / or oral anticoagulants and the administration of vitamin K may be recommended (respectively, the severity of bleeding or coagulopathy based on the prothrombin index).

Overdose

With an overdose, nausea, abdominal pain, diarrhea are possible. symptomatic treatment.

Storage conditions

In the dark place at a temperature of no higher than 25 ° C.

ALL / 2017/0003 / UA / Dec / 2017 / Morion / 15000