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

Excipients (core): cellulose microcrystalline - 127,50 mg; sodium carboxymethyl starch - 9.00 mg; Povidone (polyvinylpyrrolidone) 9.00 mg; magnesium stearate - 3.00 mg; silicon dioxide colloidal - 1,50 mg.

Auxiliary substances (shell): opedraj II White - 10,00 mg, incl. polyvinyl alcohol - 4.69 mg; Macrogol-3350 - 2.36 mg; talc - 1.74 mg; titanium dioxide -1.21 mg.

Description:Tablets of cylindrical biconvex form, covered with a film shell of white or almost white color, on the fracture are visible two layers - a core of white or almost white color and a film membrane.

Pharmacotherapeutic group:antibiotic-macrolide.

ATX: & nbsp

J.01.F.A Macrolides

J.01.F.A.06 Roxithromycin

Pharmacodynamics:Semisynthetic antibiotic from the group of macrolides, which has a broad spectrum of antibacterial activity. It has a bacteriostatic effect: binding to the 50S subunit of the ribosomes, suppresses the translocation and transpeptidation reactions, the process of formation of peptide bonds between amino acids and the peptide chain, inhibits

protein synthesis by ribosomes, which inhibits the growth and multiplication of bacteria. Good penetration into the cell ensures the efficacy of roxithromycin against intracellular pathogens (including Chlamydia trachomatis, Chlamydia pneumoniae, Ureaplasma urealyticum, Legionella pneumophila, Mycoplasma pneumoniae).

In vitro sensitive to the drug: Streptococcus agalactiae, Streptococcus pneumoniae, Neisseria meningitidis, Listeria monocytogenes, Mycoplasma pneumoniae, Chlamydia trachomatis, Chlamydia psittaci, Ureaplasma urealyticum, Legionella pneumophila, Helicobacter pylori, Gardnerella vaginalis, Bordetellci pertussis, Moraxella catarrhalis, Haemophilus ducreyi. The following microorganisms demonstrated variable in vitro sensitivity: Streptococcus pyogenes (group A beta-hemolytic streptococcus), Staphylococcus aureus, Haemophilus influenzae, Staphylococcus epidermidis.

Roxithromycin is also effective against anaerobic microorganisms: Bacteroides oralis, Bacteroides melaninogenicus, Bacteroides urealiticus; Clostridium perfringens; Eubacterium spp., Peptococcus spp., Peptostreptococcus spp., Propionibacterium acnes; Rickettsia rickettsii, Rickettsia conorii.

The drug is resistant: Bacteroides fragilis, Clostridium difficile, Pseudomonas spp., Acinetobacter spp., Family Enterobacteriaceae.

Pharmacokinetics:Quickly absorbed from the gastrointestinal tract after oral administration. Roxithromycin stable in the acidic environment of the stomach, eating 15 minutes after taking the pill does not affect suction. The maximum concentration e of the blood plasma (Cmax) after ingestion of 150 mg to 6.6 mg / l, the time to reach the maximum concentration (TCmax) is 2.2 hours, after taking 300 mg to 9.6 mg / l and 1.5 h respectively. In children, Cmax (at a 2-fold intake of 2.5 mg / kg / day) - 8.7-10.1 mg / l and is achieved after 2 hours. Receiving at an interval of 12 h ensures the maintenance of effective concentrations in the blood within 24 h. Equilibrium concentration (Css) in plasma with the admission of 150 mg twice a day for 10 days is achieved after 2-4 days and is 9.3 mg / l; when taken 300 mg once a day for 11 days - 10.9 mg / l. The connection with plasma proteins is 96%. It is characterized by high penetration into tissues, especially into the lungs, palatine tonsils and the prostate gland. Roxithromycin also penetrates well into cells (macrophages) and body fluids. Virtually does not penetrate the blood-brain barrier. Roxithromycin in small amounts is excreted in breast milk. The volume of distribution - 3 1.2 liters.

Partially metabolized in the liver, most (more than 50% of the active substance) is excreted intestine unchanged, about 12% is excreted by the kidneys and about 15% - by the lungs.The half-life of roxithromycin after a single dose of 150 mg is an average of 12 hours.

If the liver function is insufficient, the half-life and the maximum concentration in the plasma increase.

Indications:

Infections of mild to moderate severity caused by roxithromycin-sensitive pathogens:

In adults

- Infections of the upper respiratory tract: pharyngitis, tonsillitis, acute sinusitis.

- Infections of the lower respiratory tract: pneumonia (including pneumonia caused by "atypical" pathogens, incl. Chlamydia psittaci, Chlamydia pneumoniae, Moraxella catarrhalis, Legionella pneumophila), bronchitis.

- Infections of the skin and soft tissues.

- Urinary tract infections caused by Chlamydia trachomatis and Ureaplasma urealyticum.

- Infections in odontology, oral and dental infections.

- Children

- Infections of the upper respiratory tract: tonsillitis, pharyngitis, acute sinusitis.

- Infections of the skin and soft tissues.

Contraindications:- hypersensitivity to roxithromycin, other macrolides or other components of the drug;

- Pregnancy;

- lactation period;

- porphyria;

- simultaneous reception of vasoconstrictive ergot alkaloids (ergotamine and dihydroergotamine);

- simultaneous administration of cisapride, pimozide, astemizole and terfenadine;

- Children under 12 years of age or at a body weight of less than 40 kg (for this dosage form).

Carefully:patients with hepatic insufficiency; patients with renal insufficiency, patients older than 65 years; patients with congenital lengthening of the QT interval, with conditions that contribute to the occurrence of cardiac arrhythmias (uncorrected hypokalemia or hypomagnesemia, clinically significant bradycardia) and in patients receiving antiarrhythmic drugs of IA and III class; with myasthenia gravis; with simultaneous administration with warfarin, disopyramide, digoxin colchicine, dopamine receptor agonists - ergot alkaloids (including bromocriptine, cabergoline, lisuride, pergolide), cyclosporine, theophylline.

Pregnancy and lactation:Roxithromycin contraindicated in pregnancy. Roxithromycin in small amounts penetrates into breast milk. If you need to use the drug during lactation, you should decide whether to stop breastfeeding.

Dosing and Administration:

Inside.The drug should be taken before eating, squeezed with enough liquid.

Adults and children over 12 years of age (with a body weight of more than 40 kg): the standard dose is 150 mg twice a day, with an interval of 12 hours or 300 mg once (adults only).

In elderly patients

In elderly patients, a single and daily dose of roxithromycin does not change.

In patients with renal insufficiency

With renal insufficiency roxithromycin is prescribed in a dose of 150 mg 2 times a day In patients with severe hepatic insufficiency In patients with severe hepatic insufficiency (eg, with cirrhosis of the liver with jaundice or ascites), the dose should be reduced by a factor of 2, i.e., 150 mg of roxithromycin once a day.

Duration of treatment

The duration of reception of roxithromycin depends on the indication for use, the microorganism that caused the infection and the severity of the infection process. In adults, the usual course of treatment is 5-10 days; for infections caused by beta-hemolytic streptococcus, the course of treatment should be at least 10 days. In children, the usual duration of treatment is 5-10 days; for infections caused by beta-hemolytic streptococcus, the course of treatment should be at least 10 days.The duration of therapy should not exceed 10 days.

Side effects:

From the gastrointestinal tract: nausea, vomiting, abdominal pain, diarrhea (sometimes with blood), pancreatitis, pseudomembranous colitis.

From the side of the liver: increased activity of "hepatic" transaminases (alanine aminotransferase (ALT) and aspartate aminotransferase (ACT) and / or alkaline phosphatase), acute cholestatic or hepatocellular hepatitis (sometimes with the development of jaundice).

From the nervous system: dizziness, headache, paresthesia, changes in gustatory sensations (including aguezia), impaired sense of smell (including anosmia), hallucinations, temporary hearing loss, hypoacusia (incomplete hearing loss), vertigo.

Skin reactions: rash, redness, purpura.

Allergic reactions: urticaria, angioedema, bronchospasm, eosinophilia; anaphylactic shock, multiforme exudative erythema.

Other: possible development of superinfection, candidiasis.

Overdose:Symptoms: may increase dose-related side effects. Treatment: gastric lavage, symptomatic therapy. There is no specific antidote.

Interaction:Roxithromycin not simultaneously administered with preparations containing ergotamine or dihydroergotamine (vasoconstrictive ergot alkaloids). Such a combination can provoke arterial spasm and cause serious ischemia with the development of necrosis of the extremities.

With the simultaneous use of antibiotics, a group of macrolides (such as erythromycin) With terfenadine was an increase in the risk of severe complications of the cardiovascular system, including torsades de pointes and other ventricular arrhythmias. Although no such reactions were observed with roxithromycin, this joint use is contraindicated.

Admission of such drugs as astemizole, Cisapride or pimozide which are metabolized via isoenzyme CYP3A, was associated with lengthening of the interval QT and / or disorders of cardiac rhythm (typically with the development of ventricular tachycardia type "pirouette") by increasing their plasma concentrations due to interactions with the inhibitors of this isozyme, including certain antibiotics from the group of macrolides. Therefore, the combined use of these drugs with roksitromitsinom contraindicated.Simultaneous use with indirect anticoagulants (warfarin) can lead to an increase in prothrombin time. It is recommended to regularly determine the international normalized ratio (MHO) with the simultaneous use of roxithromycin with indirect anticoagulants.

Roxithromycin may displace disopyramide from binding to plasma proteins, leading to an increase in its concentration in the blood plasma. It is recommended to monitor the ECG and, if possible, determine the concentration of disopyramide in the blood plasma. With simultaneous admission with digoxin, it is possible to increase its absorption, which can lead to the development of glycosidic intoxication. It can manifest as symptoms such as nausea, vomiting, diarrhea, headache, dizziness; Intoxication with cardiac glycosides can also cause cardiac conduction or cardiac rhythm disturbances. Therefore, in patients receiving roxithromycin and digoxin (or other cardiac glycosides), it is recommended to regularly monitor the ECG and determine plasma concentrations of the cardiac glycoside. This is necessary when there are symptoms of an overdose of cardiac glycosides.

Roxithromycin, like other macrolides, should be used with caution in patients receiving IA and III class antiarrhythmics (ECG control is required), since macrolides, including roxithromycin, as well as these antiarrhythmic drugs can extend the QT interval and there is the possibility of summing the effects of prolonging the QT interval of these drugs.

With the simultaneous use of certain macrolides with colchicine, plasma concentrations of colchicine were increased with an increased risk of developing side effects, including nephrotoxic effects. Caution should be exercised when roxithromycin and colchicine are used concomitantly, although there is still no evidence of such interaction.

With the simultaneous use of certain macrolides with dopamine receptor agonists - ergot alkaloids (incl. bromocriptine, cabergoline, lysuride, pergolide) there was an increase in plasma concentrations of the latter, which can enhance their pharmacodynamic action and increase the risk of their side effects. Caution should be exercised with the simultaneous use of roxithromycin and dopamine receptor agonists - alkaloidsergot, although to date there is no data with such an interaction.

Roxithromycin, like other macrolide antibiotics, can increase the area under the concentration-time curve and the half-life of midazolam, and the effects of midazolam may be enhanced and prolonged in patients treated with roxithromycin.

There is no convincing evidence of the interaction between roxithromycin and triazolam.

The simultaneous use of roxithromycin and theophylline or cyclosporine may cause an increase in plasma concentrations of the latter, which does not, as a rule, require correction of the dosing regimen.

With the simultaneous use of roxithromycin with carbamazepine, ranitidine, aluminum and magnesium hydroxides, oral contraceptives containing estrogens and gestagens, there was no clinically significant interaction.

Special instructions:

in patients with hepatic insufficiency the drug is used with caution, under the control of liver function and, if necessary, with dose adjustment. When prescribing the drug for patients with renal insufficiency, as well as for elderly patients, there is no need to adjust the dose.

With the development of superinfection, allergic reactions roxithromycin should immediately be abolished and appropriate therapy prescribed.

Like other macrolides, roxithromycin may weight the course of myasthenia gravis, therefore, the use of roxithromycin in such patients requires caution and monitoring of the patient's condition.

When using the drug, both in the background of taking, and after 2-3 weeks. after discontinuation of treatment, the development of diarrhea caused by Clostridium difficile (pseudomembranous colitis) is possible. In mild cases, it is sufficient to cancel the treatment and apply ion-exchange resins (colestramine, colestipol), in severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin or metronidazole. Do not use drugs that inhibit the intestinal motility.

Effect on the ability to drive transp. cf. and fur:When using the drug should be followed vehicles and activities that require increased concentration and speed of psychomotor reactions. In the case of adverse reactions from the nervous system (such as,dizziness of hallucinations) patients are not recommended to engage in potentially hazardous activities.

Form release / dosage:

Tablets, film-coated 150 mg.

Packaging:

For 10, 25, 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 10, 20, 30, 40, 50 or 100 tablets in cans of polymeric for medicines. One jar or 1, 2, 3, 4, 5 or 10 contour mesh packages together with the instruction for use are placed in a cardboard package (bundle).

Storage conditions:In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002578

Date of registration:13.08.2014

Date of cancellation:2019-08-13

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp11.06.2016

Illustrated instructions

Instructions

Roxithromycin (Roxithromycin)