Roxithromycin tablets 150mg, No. 10

Mild to moderate infections caused by pathogens sensitive to roxithromycin:

In adults

upper respiratory tract infections: pharyngitis, tonsillitis, acute sinusitis; lower respiratory tract infections: pneumonia (including pneumonia caused by 'atypical' pathogens, including Chlamydia psittaci, Chlamydia pneumoniae, Moraxella catarrhalis, Legionella pneumophila), bronchitis; infections of the skin and soft tissues; infections of the genitourinary tract caused by Chlamydia trachomatis and Ureaplasma urealyticum; infections in odontology, infections of the mouth and teeth.

In children

upper respiratory tract infections: tonsillitis, pharyngitis, acute sinusitis; lower respiratory tract infections: pneumonia (including pneumonia caused by 'atypical' pathogens, including Chlamydia psittaci, Chlamydia pneumoniae, Moraxella catarrhalis, Legionella pneumophila), bronchitis; infections of the skin and soft tissues.

Inside.

The drug should be taken before meals with a sufficient amount of liquid.

Adults and children over 12 years old (with a body weight of more than 40 kg): the standard dose is 150 mg 2 times a day, with an interval of 12 hours, or 300 mg once (for adults only).

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

In patients with renal impairment

In renal failure, roxithromycin is prescribed at a dose of 150 mg 2 times a day.

In patients with severe hepatic impairment

In patients with severe hepatic impairment (for example, with cirrhosis of the liver with jaundice or ascites), the dose should be reduced by 2 times, that is, 150 mg of roxithromycin once a day.

Duration of treatment

The duration of taking roxithromycin depends on the indication for use, the microorganism that caused the infection and the severity of the infectious 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 course 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.

Film-coated tablets, white, round, biconvex, engraved with '164' on one side; cross-sectional view: white.

1 tab. roxithromycin 150 mg

Excipients: hyprolose - 19.65 mg, poloxamer - 150 mcg, povidone K30 - 4.2 mg, colloidal silicon dioxide - 1.875 mg, magnesium stearate - 1.875 mg, talc - 2.25 mg, corn starch - up to 210 mg.

• Hypersensitivity to roxithromycin, other macrolides or other components of the drug;

• pregnancy;

• lactation period;

• porphyria;

• simultaneous intake of vasoconstrictor ergot alkaloids (ergotamine and dihydroergotamine);

• concomitant use of cisapride, pimozide, astemizole and terfenadine;

• children under 12 years of age or with a body weight of less than 40 kg (for this dosage form).

  Precautions: patients with hepatic impairment; patients with renal insufficiency, patients over 65 years old; patients with congenital prolongation of the QT interval, with conditions contributing to the occurrence of cardiac arrhythmias (uncorrected hypokalemia or hypomagnesemia, clinically significant bradycardia) and in patients receiving class IA and III antiarrhythmic drugs; with myasthenia gravis; when taken simultaneously with warfarin, disopyramide, digoxin, colchicine, dopamine receptor agonists - ergot alkaloids (including bromocriptine, cabergoline, lisuride, pergolide), cyclosporine, theophylline.

pharmachologic effect

Semisynthetic antibiotic from the macrolide group with a broad spectrum of antibacterial activity. It has a bacteriostatic effect: by binding to the 50S subunit of ribosomes, it suppresses the reactions of translocation and transpeptidation, the formation of peptide bonds between amino acids and the peptide chain, inhibits protein synthesis by ribosomes, as a result of which it inhibits the growth and reproduction of bacteria. Good penetration into the cell ensures the effectiveness of roxithromycin against intracellular pathogens (including Chlamydia trachomatis, Chlamydia pneumoniae, Ureaplasma urealyticum, Legionella pneumophila, Mycoplasma pneumoniae).

In vitro susceptible to the preparation: Streptococcus agalactiae, Streptococcus pneumoniae, Neisseria meningitidis, Listeria monocytogenes, Mycoplasma pneumoniae, Chlamydiat rachomatis, Chlamydia psittaci, Ureaplasma urealyticum, Legionobella pneumacterophila. The following microorganisms have shown variable sensitivity in vitro: Streptococcus pyogenes (group A beta-hemolytic streptococcus), Staphylococcus aureus, Haemophilus influenzae, Staphylococcus epidermidis.

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

Resistant to the drug: Bacleroides fragilis, Clostridium difficile, Pseudomonas spp .; Acinetobacter spp., Family Enterobacteriaceae.

Pharmacokinetics

It is rapidly absorbed from the gastrointestinal tract after oral administration. Roxithromycin is stable in the acidic environment of the stomach, food intake 15 minutes after taking the tablet does not affect absorption. Cmax after oral administration of 150 mg - 6.6 mg / l, the time to reach the maximum concentration (TCmax) - 2.2 hours, after taking 300 mg - 9.6 mg / l and 1.5 hours, respectively. In children, Cmax (with 2-fold intake of 2.5 mg / kg / day) is 8.7-10.1 mg / l and is achieved after 2 hours. Reception with an interval of 12 hours ensures the maintenance of effective concentrations in the blood for 24 h. Equilibrium concentration (Css) in plasma when taking 150 mg 2 times a day for 10 days is achieved in 2-4 days and is 9.3 mg / l; when taking 300 mg once a day for 11 days - 10.9 mg / l. The connection with blood plasma proteins is 96%. It is characterized by high tissue penetration, especially into the lungs,palatine tonsils and prostate gland. Roxithromycin also penetrates well into cells (macrophages) and body fluids. Practically does not penetrate the blood-brain barrier. Roxithromycin is excreted in breast milk in small amounts. The volume of distribution is 31.2 liters.

It is partially metabolized in the liver, most (more than 50% of the active substance) is excreted unchanged by the intestines, 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.

In case of insufficiency of liver function, T1 / 2 and Cmax increase.

Side effect

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

From 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 taste (including ageusia), impaired 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, erythema multiforme exudative.

Others: development of superinfection, candidiasis is possible.

Application during pregnancy and lactation

Roxithromycin is contraindicated in pregnancy.

Roxithromycin passes into breast milk in small amounts. If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be resolved.

Application for violations of liver function

Caution should be exercised when using in patients with impaired liver function.

Application for impaired renal function

Caution should be exercised when using in patients with impaired renal function.

Application in children

The drug is contraindicated in children under 12 years of age or with a body weight of less than 40 kg (for this dosage form).

Use in elderly patients

Use the drug with caution in patients over 65 years of age.

special instructions

In patients with hepatic impairment, the drug is used with caution, under the control of liver function and, if necessary, with a dose adjustment.

When prescribing the drug to patients with renal insufficiency, as well as to elderly patients, there is no need for dose adjustment.

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

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

When using the drug, both during administration and after 2-3 weeks, after stopping treatment, diarrhea caused by Clostridium difficile (pseudomembranous colitis) may develop. In mild cases, it is enough to discontinue treatment and use ion-exchange resins (cholestyramine, colestipol), in severe cases, it is shown to compensate for the loss of fluid, electrolytes and protein, the appointment of vancomycin or metronidazole. Do not use drugs that inhibit intestinal motility.

Influence on the ability to drive vehicles and work with mechanisms

When using the drug, care should be taken when driving vehicles and engaging in activities that require increased concentration of attention and speed of psychomotor reactions. In the event of adverse reactions from the nervous system (such as dizziness, hallucinations), patients are not recommended to engage in potentially hazardous activities.

Overdose

Symptoms: Possible increased dose-related side effects.

Treatment: gastric lavage, symptomatic therapy.

There is no specific antidote.

Drug interactions

Roxithromycin is not prescribed concurrently with drugs containing ergotamine or dihydroergotamine (vasoconstrictor ergot alkaloids). This combination can provoke arterial spasm and cause severe ischemia with the development of necrosis of the extremities.

With the simultaneous use of antibiotics of the macrolide group (such as erythromycin) with terfenadine, there was an increase in the risk of developing severe complications from the cardiovascular system, including atrial fibrillation and other ventricular arrhythmias. Although no such reactions have been observed with roxithromycin, this concomitant use is contraindicated.

The use of drugs such as astemizole, cisapride, or pimozide, which are metabolized by the isoenzyme CYP3A, has been associated with prolongation of the QT interval and / or cardiac arrhythmias (usually with the development of ventricular tachycardia of the 'pirouette' type) as a result of an increase in their plasma concentrations due to interaction with inhibitors this isoenzyme, including some macrolide antibiotics. Therefore, the combined use of these drugs with roxithromycin is 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 (INR) while using roxithromycin with indirect anticoagulants.

Roxithromycin can displace disopyramide from its connection with plasma proteins, leading to an increase in its concentration in blood plasma. ECG monitoring and, if possible, determination of the concentration of disopyramide in blood plasma is recommended.

When taken simultaneously with digoxin, an increase in its absorption is possible, which can lead to the development of glycosidic intoxication. It can manifest itself with symptoms such as nausea, vomiting, diarrhea, headache, dizziness; intoxication with cardiac glycosides can also cause cardiac conduction disturbances or cardiac arrhythmias. Therefore, in patients taking roxithromycin and digoxin (or other cardiac glycosides), it is recommended to regularly monitor the ECG and determine the plasma concentrations of cardiac glycoside. This is necessary when symptoms of an overdose of cardiac glycosides appear.

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

With the simultaneous use of some macrolides with colchicine, an increase in plasma concentrations of colchicine was observed with an increase in the risk of developing its side effects, including nephrotoxic effects. Caution should be exercised with the concomitant use of roxithromycin and colchicine, although to date there is no data on the presence of such an interaction.

With the simultaneous use of some macrolides with dopamine receptor agonists - ergot alkaloids (including bromocriptine, cabergoline, lisuride, pergolide), an increase in plasma concentrations of the latter was observed, which can enhance their pharmacodynamic effect and increase the risk of their side effects. Caution should be exercised with the simultaneous use of roxithromycin and dopamine receptor agonists - ergot alkaloids, although so far there is no data on the presence of such an interaction.

Roxithromycin, like other macrolide antibiotics, can increase the area under the concentration-time curve and T1 / 2 of midazolam; therefore, the effects of midazolam can be enhanced and prolonged in patients receiving roxithromycin treatment.

There is no conclusive evidence of an interaction between roxithromycin and triazolam.

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

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