Rulid, pills 150 mg, 10 pcs.

Composition

Active ingredient:

roxithromycin – 150 mg.

Auxiliary substances:

hydroxypropyl cellulose,

poloxamer,

povidone KZO,

colloidal silicon dioxide,

magnesium stearate,

talc,

corn starch.

Shell composition:

hypromellose,

anhydrous glucose,

titanium dioxide,

propylene glycol.

Pharmacological action

Pharmacodynamics

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 perfringens. Corynebacterium diptheriae. Enterococcus. Gardnerella vaginalis. Methi-S-Staphylococcus. Neisseria meningitidis. Helicobacter pylori. Legionella pneumophilia. Lysteria monocytogenes obiluncus. Mycoplasma pneumoniae. Pasteurella multocida. Peptostreptococcus. Porphyromonas. 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

Suction and distribution

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 does not affect the pharmacokinetics. After taking the drug at a dose of 150 mg, the maximum concentration in the blood averages 6.6 mg / l and is reached in 2.2 hours. Taking the drug at intervals of 12 hours ensures that effective blood concentrations are maintained throughout the day.

The half-life after a single dose of 150 mg is 10.5 hours. After a single dose of 300 mg of roxithromycin, the average maximum blood concentration is 9.7 mg / l and is reached in 1.5 hours. With repeated administration of roxithromycin (150 mg twice daily, for 10 days), the equilibrium state in plasma is reached between 2-4 days, amounting to a max of 9.3 mg/l. Taking 300 mg of roxithromycin every 24 hours for 11 days resulted in a max C of 10.9 mg / l.

Roxithromycin penetrates well into many tissues, especially the lungs, tonsils and prostate. The drug also penetrates well into cells, especially neutrophilic leukocytes and monocytes, stimulating their phagocytic activity. Binding to blood proteins is 96%, is saturable and decreases at concentrations of roxithromycin above 4 mg/l.

Metabolism and elimination

Roxithromycin is only partially metabolized, more than half of the Active ingredient is excreted unchanged mainly in the faeces, as well as in the urine. In adults with normal renal and hepatic function,65% of roxithromycin is excreted in the faeces. Less than 0.05% of the administered dose of roxithromycin passes into breast milk.

Pharmacokinetics in special clinical cases

In patients with renal insufficiency, renal excretion of roxithromycin and its metabolites is approximately 10% of the dose taken. The dose of the drug does not change in case of renal failure. In severe hepatic insufficiency, the elimination half-life is prolonged (25 h) and increases with max.

Indications

• Infections of the upper respiratory tract: acute pharyngitis, tonsillitis, sinusitis;
• infections of the lower respiratory tract: pneumonia (including caused by such “atypical” pathogens like Chlamydia psittaci, Chlamydia pneumoniae, Moraxella (Branhamella) catarrhalis, Legionella pneumophilia, etc., bronchitis, bacterial infections in chronic obstructive pulmonary disease;
• infections of skin and soft tissues;
• infection of the genital (except for gonorrhea), including: urethritis, cervicovaginitis;
• infection in dentistry.

Use during pregnancy and lactation

Roxithromycin is contraindicated in pregnancy.

Small amounts of roxithromycin pass into breast milk, so it is necessary to stop breastfeeding or taking the drug.

Contraindications

• Hypersensitivity to macrolides;
• simultaneous administration of drugs such as ergotamine and dihydroergotamine;
• combined use with ergotamine derivatives and ergotamine-like vasoconstrictors is not allowed, as it can lead to the development of “ergotism” and necrosis of limb tissues.

Use with caution in patients with severe hepatic insufficiency.

Side effects

Anaphylactic reactions: angioedema, bronchospasm, weakness, anaphylactic shock (rare).

Skin reactions: rash, redness, urticaria.

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

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

Possible: slight changes in taste and olfactory sensations.

In some cases: symptoms of pancreatitis, dizziness, headache, paresthesia were observed.

Possible: development of superinfection due to the growth of insensitive microorganisms.

Interaction

Concomitant administration of terfenadine is not recommended, due to an increase in the concentration of the latter with simultaneous administration of macrolide antibiotics, which can lead to the development of severe ventricular arrhythmias.

Although this complication was not observed with roxithromycin, and no pharmacokinetic interactions or ECG changes were shown in studies on volunteers, the combination of roxithromycin and terfenadine is not recommended.

The use of drugs such as astemizole, cisapride, pimozide may lead to prolongation of the QT interval and / or severe cardiac arrhythmias as a result of an increase in their serum concentration, as a result of the competitive influence for the CYP3A isozyme between the above drugs and macrolide antibiotics.

Interaction with warfarin, carbamazepine, ranitidine, antacids and oral contraceptives is absent.

When roxithromycin is co-administered with vitamin K antagonists, it is recommended to monitor prothrombin time or the international normalized ratio (INR).

Roxithromycin can replace the protein bound disopyramide, leading to an increase in serum levels of disopyramide.

It is recommended to monitor the ECG and, if possible, determine the level of disopyramide in the serum.

When taken concomitantly with digoxin, it is possible to increase the absorption of the latter. It is recommended to monitor the electrocardiogram and serum cardiac glycoside levels.

This is mandatory when symptoms of an overdose of cardiac glycosides appear.

Roxithromycin may increase the half-life of midazolam, leading to an increase or prolongation of its action.

How to take, course of administration and dosage

Adults are prescribed 150 mg of roxithromycin orally at 12-hour intervals. The daily dose is 300 mg. It is possible to prescribe 300 mg once a day.

Use in children

Children (body weight over 40 kg) are prescribed 150 mg of roxithromycin orally 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!

Use in elderly patients

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

Use in patients with renal insufficiency

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

Use in patients with hepatic insufficiency

In patients with hepatic insufficiency,150 mg is prescribed once.

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 once or twice a day before meals. The tablet should be washed down with a sufficient amount of water.

Overdose

In case of overdose, gastric lavage and symptomatic therapy are necessary.

There is no specific antidote.

Special instructions

Use in patients with hepatic insufficiency and elderly patients

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

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

Form of production

Film-coated tablets

Storage conditions

Store at a temperature not exceeding +25°C. Keep out of reach of children.

Shelf

life is 3 years.

Active ingredient

Roxithromycin

Conditions of release from pharmacies

By prescription

Dosage form

of the tablet

Indications

Pneumonia, Vaginal Infections, Skin Infections, Bronchitis, Urinary Tract Infections, Tonsillitis, Sinusitis

Weight

Weight: 11 gr.