Wilprafen - instructions for use, dose, side effects, contraindications

Active substanceJosamycinJosamycin

Similar drugsTo uncover

Wilprafen®

pills inwards

Astellas Farma Europe BV Netherlands

Wilprafen®

granules inwards

Astellas Farma Europe BV Netherlands

Wilprafen® solutab®

pills inwards

Astellas Farma Europe BV Netherlands

Dosage form: & nbspGranules for preparation of suspension for oral administration

Composition:

Component	Number per 1 bottle, g			Amount per 5 ml of suspension, mg
Dosage	125 mg / 5ml	250mg / 5ml	500 mg / 5ml	125 mg / 5ml	250 mg / 5ml	500mg / 5ml
Active substance
Josamycin propionate *	1,577* (1.50 million. ME)	3,1545* (3.0 million. ME)	6,307* (6.0 million. ME)	131,417* (125 thousand. ME)	262,875* (250 thousand. ME)	525,5* (500 thousand. ME)
Excipients
Sodium citrate	0,1125	0,1125	0,1125	9,375	9,375	9,375
Methylparahydroxybenzoate	0,0795	0,0795	0,0795	6,625	6,625	6,625
Propyl parahydroxybenzoate	0,0105	0,0105	0,0105	0,875	0,875	0,875
Simethicone	0,075	0,075	0,075	6,250	6,25	6,25
Giprolase	0,180	0,225	0,300	15,000	18,75	25,00
Avicel RC-591 [microcrystalline cellulose, carmellose sodium]	0,570	1,200	0,600	47,500	100,00	50,00
Aromatic Strawberry	0,0375	0,0375	0,050	3,125	3,125	4,167
Canthaxanthine 10%	-	0,0075	-	-	0,625	-
Betacarotene	-	-	0,015	-	-	1,25
Powdered starch sucrose (3%)	10,108	7,848	10,2005	842,333	654,00	850,042
Mannitol	2,250	2,250	2,250	187,5	187,5	187,5

* Based on the theoretical activity of 951 IU / mg.

Description:

125 mg / 5 ml: White granules with the smell of strawberries.

After the granules are dissolved in water, a white suspension with a strawberry smell is formed.

250 mg / 5 ml: Pink granules with the smell of strawberries.

After the granules are dissolved in water, a pink suspension with the smell of strawberry is formed.

500 mg / 5 ml: Yellow granules with the smell of strawberries.

After the granules are dissolved in water, a yellow suspension with the smell of strawberry is formed.

Pharmacotherapeutic group:Antibiotic-macrolide

ATX: & nbsp

J.01.F.A.07 Josamycin

Pharmacodynamics:

Antibacterial drug from the group of macrolides. The mechanism of action is associated with a violation of protein synthesis in a microbial cell due to reversible binding to 50Ssubunit of the ribosome. In therapeutic concentrations, as a rule, has a bacteriostatic effect, slowing the growth and multiplication of bacteria. When creating high concentrations in the focus of inflammation, a bactericidal effect is possible.

Josamycin is active against gram-positive bacteria (Staphylococcus spp., in t.ch. methicillin-sensitive strains Staphylococcus aureus, Streptococcus spp., in t.ch. Streptococcus pyogenes and Streptococcus pneumoniae, Corynebacterium diphtheriae, Listeria monocytogenes, Propionibacterium acnes, Bacillus anthracis, Clostridium spp., Peptococcus spp., Peptostreptococcus spp.), gram of negative bacteria (Neisseria meningitidis, Neisseria gonorrhoeae, Moraxella catarrhalis, Bordetella spp., Brucella spp.. Legionella spp., Haemophilus ducreyi, Haemophilus influenzae, Helicobacter pylori, Campylobacter jejuni), sensitivity Bacteroides fragilis can be variable, Chlamydia spp., in t.ch. C. trachomatis, Chlamydophila spp., in t.ch. Chlamydophila pneumoniae (formerly called Chlamydia pneumoniae), Mycoplasma spp., in t.ch. Mycoplasma pneumoniae, Mycoplasma hominis, Mycoplasma genitalium, Ureaplasma spp., Treponema pallidum, Borrelia burgdorferi. As a rule it is not active against enterobacteria, therefore it negatively affects the microflora of the gastrointestinal tract. In a number of cases, it remains active in the resistance to erythromycin and other 14-and 15-member macrolides (streptococci, staphylococci).Resistance to josamycin is less common than to 14-and 15-member macrolides.

Pharmacokinetics:

After oral administration josamycin quickly absorbed from the gastrointestinal tract, eating does not affect bioavailability. The maximum concentration of josamycin in plasma is reached after 1 hour after administration. When taken in a dose of 1 g, the maximum concentration in the blood plasma is 2-3 μg / ml. About 15% of josamycin binds to plasma proteins. Josamycin it is well distributed in organs and tissues (with the exception of the brain), creating concentrations exceeding the plasma concentration and remaining at the therapeutic level for a long time.

Especially high concentrations josamycin creates in the lungs, tonsils, saliva, sweat and tear fluid. The concentration in the sputum exceeds the concentration in the plasma by 8-9 times. Passes the placental barrier, is secreted into breast milk. Josamycin metabolized in the liver to less active metabolites and excreted mainly with bile. The half-life of the drug is 1-2 hours, but it can lengthen in patients with impaired liver function. Excretion of the drug by the kidneys does not exceed 10%.

Indications:

Infectious and inflammatory diseases caused by microorganisms sensitive to josamycin:

- Infections of the upper respiratory tract and ENT organs:

tonsillitis, pharyngitis, paratonzillitis, laryngitis, otitis media, sinusitis, diphtheria (in addition to treatment with diphtheria toxoid), scarlet fever (as an alternative to beta-lactam antibiotics, if their use is not possible).

- Lower respiratory tract infections:

acute bronchitis, exacerbation of chronic bronchitis, community-acquired pneumonia, whooping cough, psittacosis.

- Infections of the skin and soft tissues:

folliculitis, furuncle, furunculosis, abscess, anthrax, mug, acne, lymphangitis, lymphadenitis, phlegmon, panaritium, wound (including postoperative) and burn infections.

- Infections of the oral cavity:

gingivitis, pericoronitis, periodontitis, alveolitis, alveolar abscess.

- Eye infections:

blepharitis, dacryocystitis.

- Infections of the genitourinary system:

non-gonococcal infections of the urogenital tract (including urethritis, cervicitis, epididymitis, prostatitis caused by chlamydia and / or mycoplasmas, syphilis (with hypersensitivity to penicillin), venereal lymphogranuloma).

- Diseases of the gastrointestinal tract associated with N. pylori:

peptic ulcer of stomach and duodenum, chronic gastritis, etc.

Contraindications:

- Hypersensitivity to josamycin, excipients, other macrolides;

- application of the drug simultaneously with the use of ergotamine, dihydroergotamine, cisapride, pimozide, ivabradine or colchicine (see section "Interaction with other medicinal products");

- the use of the drug by the mother during the breast-feeding period of a child receiving cisapride therapy (see the section on "Application during pregnancy and during breastfeeding");

- severe violations of liver function;

- deficiency of sugar / isomaltase, intolerance to fructose, glucose-galactose malabsorption.

Carefully:

In patients with renal insufficiency, dzhozamycin therapy should be performed taking into account the results of appropriate laboratory tests (determining the clearance of endogenous creatinine).

Jozamycin is not recommended for use with the following drugs:

- ebastin,

- dopamine receptor agonists: bromocriptine, cabergoline, lizard, pergolide,

- triazolam,

- halofantrine,

- disopyramide,

- tacrolimus,

- terfenadine and astemizole (see the section "Interaction with other medicinal products").

Care must be taken when using josamycin together with the following drugs: carbamazepine, ciclosporin, anticoagulants of indirect action, sildenafil, theophylline, aminophylline, digoxin.

Pregnancy and lactation:

Despite the fact that this dosage form is intended for children, information on the use of josamycin during pregnancy and lactation is given below.

Pregnancy

The use of the drug during pregnancy is possible if the intended benefit to the mother exceeds the potential risk to the fetus. The need for the drug during pregnancy should be evaluated by a doctor. Limited clinical observations suggest that the use of josamycin during pregnancy does not lead to an increase in the incidence of adverse pregnancy outcomes and is not associated with the occurrence of any specific developmental defects in the child. Pre-clinical studies did not reveal teratogenic and fetotoxic effects of josamycin.

The WHO European Office recommends josamycin as a drug of choice in the treatment of chlamydial infection in pregnant women.

Lactation

It is established that macrolides are secreted with the mother's milk, and the concentration of the drug in milk is equal to or exceeds its concentration in the blood plasma. The main danger lies in the action of the drug on the intestinal microflora of the child. Thus, the reception of the drug Vilprafen ® according to indications during breastfeeding is allowed. The need for the drug during lactation should be evaluated by a doctor. If the child develops disorders from the gastrointestinal tract (diarrhea, candidiasis of the oral mucosa), breastfeeding should be stopped (or stop taking the medication). When cisapride is administered to newborns or infants who are naturally breastfed, the use of macrolides by the mother is contraindicated because of potential risk of interaction of drugs, dangerous development of ventricular tachycardia such as "pirouette" in a child.

Dosing and Administration:

Dosing regimen

The drug Vilprafen® is available in several dosage forms and dosages. The dosage form "granules for oral suspension" is specially formulated for children in 3 doses: 125 mg / 5 ml, 250 mg / 5 ml and 500 mg / 5 ml.

Together with the drug, the kit contains a special syringe with the marks and marks corresponding to the weight of the child. This syringe is used to accurately dispense and take the prepared suspension inside.

The recommended daily dosage of josamycin 50 mg / kg should be divided into 2 divided doses: 25 mg / kg in the morning and 25 mg / kg in the evening without exceeding the dose of 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 is not less than 5-7 days.

If you miss a regular dose, you should not take a double dose of the drug.

In accordance with the recommendations of the WHO, the duration of treatment of streptococcal tonsillitis should be at least 10 days.

Preparation of the suspension

(1) shake the contents of the bottle well

(2) Add chilled boiled water to a circular risk

(3) Shake well and allow to settle for a few minutes in order to thoroughly examine the liquid level

(4) Add water (if necessary) to circular risks on the vial The resulting foam should always be above this label

(5) Before use, the prepared suspension should be thoroughly shaken

Administration of the drug

(1) Place the attached syringe with divisions into a vial containing the finished suspension

(2) Draw the suspension into the syringe, pulling the syringe plunger to the mark corresponding to the weight of the child

(3) After use, rinse the syringe with water

(4) To attach the syringe holder, enclosed in the package, to one side of the vial, free of the applied information (preferably)

(5) After use, place the syringe in the holder on the vial

The dosage of the drug depends on the weight of the child:

- preparation Vilprafen® in a dose of 125 mg / 5 ml is intended for children with a body weight of 2-5 kg. To the preparation is attached a syringe with the deposited divisions from 2 to 5 kg. One division of this syringe corresponds to a weight of 0.5 kg and a dose of the preparation Vilprafen '* 12.5 mg per 1 kg of body weight.

- preparation Vildrafen® in a dose of 250 mg / 5 ml is intended for children with a body weight of 5-10 kg. The drug is supplied with a syringe with the deposited divisions from 2 to 10 kg. One division of this syringe corresponds to a weight of 1 kg and a dose of Wilprafen® 25 mg per 1 kg of body weight.

- preparation Vilprafen® in a dose of 500 mg / 5 ml is intended for children with a body weight of 10-40 kg. A syringe with the deposited divisions from 2 to 20 kg is applied to the preparation. One division of this syringe corresponds to a weight of 1 kg and a dose of Vilprrafen 50 mg per 1 kg of weight.

Always strictly adhere to the dosage prescribed by the doctor. If there is any doubt about the correctness of the use, consult your doctor.

The preparation Vilprafen® is taken internally in the form of a suspension, which is prepared immediately before use.

The syringe volume of the suspension, corresponding to the weight of the child, contains the dose of the drug for one dose.

Examples of dispensing of the suspension:

For a child weighing 4 kg, you should use the preparation Vildrafen® at a dose of 125 mg / 5 ml with the attached "2-5 kg" syringe. At one time, you need to dial this syringe suspension to the label "4 kg".

For a child weighing 6 kg, you should use the preparation Vildrafen® at a dose of 250 mg / 5 ml with the attached "2-10 kg" syringe. At one time, you need to dial this syringe suspension to the mark "6 kg".

For a child weighing 15 kg, use a preparation of Wilprafen® at a dose of 500 mg / 5 ml with the attached "2-20 kg" syringe. At one time, you need to dial this syringe suspension to the mark "15 kg".If the child's weight exceeds the weight indicated on the divisions of the syringe, dial the required volume of the suspension twice. For example, for a child weighing 30 kg, first dial a "2-20 kg" syringe to the "20 kg" label, then to the "10 kg" label.

After opening the vial and preparing the suspension, the shelf life of the suspension at room temperature is 7 days.

Be careful! The dosage syringe is used exclusively for the oral administration of a suspension of the preparation of Vilprafen® and should not be used for dosing another drug.

Hs use other devices for dosing and injecting a suspension of the preparation Vilprafen® (syringe, spoon, pipette from another drug), in addition to this special syringe, corresponding to the specific dosage (i.e., supplied with the preparation).

Side effects:

Disorders from the gastrointestinal tract:

Nausea, vomiting, abdominal pain, diarrhea, pseudomembranous colitis, gastralgia, stomatitis, constipation.

Disturbances from the skin and subcutaneous tissue:

Erythematous maculopapular eruptions, erythema multiforme, bullous dermatitis, Stevens-Johnson syndrome, Lyell syndrome.

Immune system disorders:

Hypersensitivity reactions in the form of severe itching, hives, face edema, Quincke edema (angioedema), difficulty breathing, anaphylactoid reactions and anaphylactic shock;

Serum sickness.

Disorders from the liver and bile ducts:

Increased activity of transaminases and alkaline phosphatase, jaundice, cholestatic or cytolytic hepatitis.

Disorders from the vascular system:

Purpura, cutaneous vasculitis.

Metabolic and nutritional disorders:

Decreased appetite.

When these reactions occur, as well as a reaction that is not indicated in the instructions, it is necessary to consult a doctor.

Overdose:

To date, there is no evidence of specific symptoms of an overdose. In case of an overdose, the symptoms described in the "Side effect" section should be assumed, especially from the gastrointestinal tract (in particular, nausea, diarrhea).

Treatment: with an overdose, remove the unabsorbed drug from the gastrointestinal tract (gastric lavage, activated charcoal, etc.) and perform symptomatic therapy.

Interaction:

The use of the following drugs with josamycin is contraindicated in connection with the possibility of developing serious side effects:

- Ergotamine, dihydroergotamine

The result of the interaction is the risk of pronounced vasoconstriction (ergotism) with possible development of necrosis of the extremities (due to inhibition of hepatic metabolism and elimination of ergot alkaloids).

- Cisapride, pimozide

As a result of interaction, the risk of developing life-threatening arrhythmias increases, including ventricular pirouette tachycardia.

- Iwabradine

As a result of the interaction, the concentration of ivabradine in the blood plasma increases and the associated side effects (due to inhibition of hepatic metabolism of ivabradine).

- Colchicine

The result of the interaction is an increased risk of side effects of colchicine, including potentially fatal.

The use of the following drugs with josamycin is not recommended:

- Ebastin

Increased risk of life-threatening arrhythmias in patients with congenital long-interval syndrome QT.

- Dopamine receptor agonists (bromocriptine, cabergoline, lizard, pergolide)

Increase in the concentration of dopamine receptor agonists in blood plasma with a potential increase in their activity, the appearance of symptoms of an overdose.

- Triazolam

Several cases of increased side effects of triazolam (behavioral disorders).

- Halofantrine

Increased risk of ventricular arrhythmias, including ventricular tachycardia such as pirouette ("torsades de pointes") If possible, you should cancel the use of josamycin.If you can not cancel simultaneous medication, it is necessary to monitor the interval QT and ECG.

- Disopyramide

Increased risk of side effects of disopyramide: severe hypoglycemia, increasing the duration of the interval QT and life-threatening arrhythmias, including ventricular pirouette tachycardia. 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 astemisole

During the joint use of josamycin and antihistamines containing terfenadine or astemizole, the risk of developing life-threatening arrhythmias may be increased.

The use of the following drugs with josamycin requires caution:

- Carbamazepine

It is possible to increase the concentration of carbamazepine in the blood plasma and develop symptoms of an overdose due to the inhibition of its hepatic metabolism. It is recommended to monitor the patient's condition and the concentration of carbamazepine in the blood plasma. You may need to reduce the dose of carbamazepine.

- Cyclosporin

The joint administration of josamycin and cyclosporine may cause increased levels of cyclosporine and creatinine in the blood plasma and increase the risk of nephrotoxicity. It is necessary to regularly monitor the concentration of cyclosporine in the blood plasma and kidney function. The dose of cyclosporine should be adjusted during joint use with josamycin, and after discontinuing the use of josamycin.

- Anticoagulants of indirect action

It is possible to increase the effect of anticoagulants of indirect action, increase the risk of bleeding.

Frequent control of the international normalized relationship (INR) is necessary.It may be necessary to reduce the dose of indirect anticoagulants during the joint application with josamycin, and also in some cases - after discontinuing the use of josamycin.

- Sildenafil

It is possible to increase the concentration of sildenafil in blood plasma, increase the risk of arterial hypotension. In case of need of joint reception it is recommended take the smallest dose of sildenafil.

- Theophylline and aminophylline

Caution should be exercised in the joint use of josamycin with theophylline or aminophylline, t. there is a risk of increasing the concentration of theophylline in the blood plasma, especially in children.

- Digoxin

With the joint administration of josamycin and digoxin, an increase in the level of the latter in the blood plasma is possible.

- Other antibacterial drugs

Because bacteriostatic antibiotics in vitro can reduce the antimicrobial effect of bactericidal antibiotics, their simultaneous use should be avoided. Josamycin It should not be used simultaneously with lincosamides in connection with the possible mutual decrease in efficacy.

Special instructions:

With almost all antibacterial agents, including josamycin, there are cases of the development of pseudomembranous colitis, which can pose a threat to life. The possibility of occurrence of this undesirable phenomenon should be borne in mind in patients with diarrhea on the background or after taking dzhozamycin. Careful collection of anamnesis is necessary, since diarrhea caused by Clostridium difficile, can develop within 2 months after the end of the course of antibiotic therapy. In the case of pseudomembranous colitis, the drug is canceled and the necessary treatment is prescribed. Drugs that inhibit intestinal peristalsis are contraindicated in this situation.

In patients with renal insufficiency, dzhozamycin therapy should be performed taking into account the results of appropriate laboratory tests (determining the clearance of endogenous creatinine).

The possibility of cross-resistance to various antibiotics from the macrolide group should be taken into account: microorganisms resistant to treatment with antibiotic related chemical structures may also be resistant to josamycin. This drug contains sodium in an amount of less than 1 mmol per 5 ml of suspension (or dose, calculated at 5 kg).

Particular issues of violation of the international normalized relationship (INR)

Numerous cases of an increase in the activity of anticoagulants of indirect action are noted in patients taking antibiotics. Risk factors are the presence of an infectious disease (and concomitant inflammatory process), the age and general condition of the patient. In this regard, it is difficult to determine the significance of individual factors - an infectious disease or antibiotic used for its therapy, in changing the value of INR. Nevertheless, it is necessary to take into account the possible influence of a number of antimicrobial agents: fluoroquinolones, macrolides, tetracyclines, co-trimoxazole and some cephalosporins.

This medication contains methyl parahydroxybenzoate and propyl parahydroxybenzoate, which can cause allergic reactions (most likely delayed type).

Effect on the ability to drive transp. cf. and fur:

The effect of the drug on the ability to drive vehicles and work with mechanisms has not been noted.

Form release / dosage:

Granules for the preparation of a suspension for ingestion 125 mg / 5 ml, 250 mg / 5 ml and 500 mg / 5 ml.

Packaging:

Dosages of 125 mg / 5 ml and 250 mg / 5 ml:

For 15 g granules in a 100 ml colorless glass vial with a circular 60 ml risk with a screwed plastic lid with a first-opening control ring and a polyethylene stop valve.

One bottle together with the instructions for use and a plastic dispensing syringe with the syringe holder is placed in a cardboard box.

Dosage 500 mg / 5 ml:

For 20 g of granules in a 100 ml colorless glass vial with a circular risk of 60 ml with a screwed plastic lid with a first-opening control ring and a polyethylene stop valve.

One bottle together with the instructions for use and a plastic dispensing syringe with the syringe holder is placed in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Store the suspension at room temperature.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiry date printed on the package. Shelf life of the suspension is 7 days from the date of preparation.

Terms of leave from pharmacies:On prescription

Registration number:LP-004305

Date of registration:22.05.2017

Expiration Date:22.05.2022

The owner of the registration certificate:Astellas Farma Europe BVAstellas Farma Europe BV Netherlands

Manufacturer: & nbsp

FAMAR LYON France

Representation: & nbspASTELLAS PHARMA YUROP BV ASTELLAS PHARMA YUROP BV Netherlands

Information update date: & nbsp22.06.2017

Illustrated instructions

Instructions

Wilprafen® (Wilprafen®)