Rulid tablets 150mg, No. 10

• upper respiratory tract infections: acute pharyngitis, tonsillitis, sinusitis;

• lower respiratory tract infections: pneumonia (including caused by such atypical pathogens as Chlamydia psittaci, Chlamydia pneumonia, Moraxella (Branhamella) catarrhalis, Legionella pneumophilia, etc.), bronchitis, bacterial infections in chronic obstructive pulmonary diseases;

• infections of the skin and soft tissues;

• genital infections (other than gonorrhea), including urethritis, cervico-vaginitis;

• infections in odontology.

Adults are prescribed 150 mg of roxithromycin by mouth with an interval of 12 hours. The daily dose is 300 mg. Perhaps the appointment of 300 mg once a day.

Children (body weight over 40 kg) are prescribed 150 mg of roxithromycin by mouth with an interval of 12 hours. The daily dose is 300 mg.

This dosage form is not used in children under 4 years of age!

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

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

In patients with hepatic impairment, 150 mg is prescribed as a single dose.

The duration of taking roxithromycin depends on the indication for use, the severity of the infectious process and the activity of the pathogen.

Roxithromycin is taken orally 1 or 2 times a day before meals.

The tablet should be taken with a sufficient amount of water.

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.

• Simultaneous administration of drugs such as ergotamine and dihydroergotamine;

• hypersensitivity to macrolides.

  Combined use with ergotamine derivatives and ergotamine-like vasoconstrictors is not allowed, as it can lead to the development of 'ergotism' and necrosis of the tissues of the extremities.

  Use with caution in patients with severe hepatic impairment.

pharmachologic effect

Semisynthetic antibiotic of the macrolide group for oral administration. Usually sensitive to the drug: Bordetella pertussis; Borrelia burgdorferi; Moraxella (Branhamella) catarrhalis; Campylobacter coli, Campylobacter jejuni, Chlamydia trachomatis, psittaci and pneumoniae, Clostridium spp. (including Clostridium perfringens); Corynebacterium diptheriae; Enterococcus spp., Gardnerella vaginalis; Methi - S - Staphylococcus; Neisseria meningitidis; Helicobacter pylori; Legionella pneumophilia, Lysteria monocytogenes obiluncus; Mycoplasma pneumoniae; Pasteurella multocida; Peptostreptococcus spp., Porphyromonas spp., Propionibacterium acnes; Rhodococcus equi, Streptococcus pneumoniae, Streptococcus spp.

Moderately sensitive to the drug: Haemophilus influenzae, Ureaplasma urealyticum, Vibrio cholerae.

Resistant to the drug: Acinetobacter spp, Bacteroides fragilis; Enterobacteriaceae; Methi-R Staphylococcus; Pseudomonas spp; Fusobacterium; Mycoplasma hominis, Nocardia.

Pharmacokinetics

In adults

Roxithromycin is rapidly absorbed after oral administration. Roxithromycin is more stable than other macrolides in the acidic environment of the stomach. Taking the drug 15 minutes before meals has no effect on pharmacokinetics. After taking the drug at a dose of 150 mg, Cmax in the blood averages 6.6 mg / l and is achieved after 2.2 hours. Taking the drug with an interval of 12 hours ensures that effective blood concentrations are maintained throughout the day. T1 / 2 after a single dose of 150 mg is 10.5 hours.

After a single dose of 300 mg of roxithromycin, the average Cmax in the blood is 9.7 mg / l and is reached after 1.5 hours.

With the repeated appointment of roxithromycin (150 mg 2 times / day, for 10 days), the equilibrium state in plasma is achieved between 2-4 days, amounting to Cmax 9.3 mg / l.

Taking 300 mg of roxithromycin every 24 hours for 11 days provided a Cmax of 10.9 mg / L.

Roxithromycin penetrates well into many tissues, especially the lungs, palatine tonsils and the prostate gland. The drug also penetrates well into cells, especially into neutrophilic leukocytes and monocytes, stimulating their phagocytic activity.

Binding to blood proteins is 96%, is saturated and decreases at concentrations of roxithromycin above 4 mg / l.

Roxithromycin is metabolized only partially, more than half of the active substance is excreted unchanged, mainly in the feces, as well as in the urine. In adults with normal renal and hepatic function, 65% of roxithromycin is excreted in the feces.

In renal failure, the excretion of roxithromycin and its metabolites through the kidneys is approximately 10% of the dose taken. The dose of the drug does not change in renal failure.

In severe liver failure, T1 / 2 is lengthened (25 hours) and Cmax increases.

Less than 0.05% of the taken dose of roxithromycin passes into breast milk.

Side effect

Anaphylactic reactions: angioedema, bronchospasm, weakness, rarely anaphylactic shock.

Skin reactions: rash, redness, urticaria.

Gastrointestinal reactions: nausea, vomiting, abdominal pain, diarrhea (very rarely with blood).

Liver reactions: increased liver enzymes (ALT, ACT, ALP). Cholestatic or hepatocellular acute hepatitis.

Small changes in taste and smell are possible.

In some cases, symptoms of pancreatitis were observed.

Dizziness, headache, paresthesia.

Superinfection may develop due to the growth of insensitive microorganisms.

Application during pregnancy and lactation

Roxithromycin is contraindicated in pregnancy. Small amounts of roxithromycin pass into breast milk, therefore breastfeeding or taking the drug must be discontinued.

Application for violations of liver function

In patients with hepatic impairment, 150 mg is prescribed as a single dose.

Application for impaired renal function

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

Application in children

Children (body weight over 40 kg) are prescribed 150 mg of roxithromycin by mouth with an interval of 12 hours. The daily dose is 300 mg.

Use in elderly patients

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

special instructions

When prescribing the drug to patients with hepatic insufficiency, special care is required, monitoring of liver function and dose adjustment.

When the drug is prescribed to patients with renal insufficiency, as well as to elderly patients, there is no need to adjust the dose.

Overdose

In case of an overdose, gastric lavage and symptomatic therapy are necessary. There is no specific antidote.

Drug interactions

Simultaneous administration of terfenadine is not recommended, due to an increase in the concentration of the latter while taking macrolide antibiotics, which can lead to the development of severe ventricular arrhythmias. Although this complication has not been noted with roxithromycin, and studies in volunteers have not shown any pharmacokinetic interactions or changes in the ECG, the combination of roxithromycin and terfenadine is not recommended.

Taking drugs such as astemizole, cisapride, pimozide can lead to prolongation of the QT interval and / or severe arrhythmias of the heart, as a result of an increase in their serum concentration, as a result of a competitive effect for the CYP 3A isoenzyme between the above drugs and macrolide antibiotics.

There is no interaction with warfarin, carbamazepine, ranitidine, antacids and oral contraceptives.

With the simultaneous appointment of roxithromycin with vitamin K antagonists, it is recommended to monitor the prothrombin time or the international normalized ratio (INR).

Roxithromycin can replace protein bound disopyramide, leading to an increase in serum disopyramide levels. ECG monitoring and, if possible, determination of serum disopyramide levels are recommended.

When taken simultaneously with digoxin, an increase in the absorption of the latter is possible. It is recommended to monitor the electrocardiogram and serum levels of cardiac glycoside. This is necessary when symptoms of an overdose of cardiac glycosides appear.

Roxithromycin can increase the half-life of midazolam, leading to an increase and lengthening of its action.