Drives

General characteristics. Structure:

Active agent: рокситромицин 150 mg.

Excipients: hydroxypropyl cellulose, half-oxameasures, K30 povidone, silicon dioxide colloid, magnesium stearate, talc, starch corn.

Structure of a cover: gipromelloza, dextrose anhydrous, titanium dioxide, propylene glycol.

Pharmacological properties:

Pharmacodynamics. Rulid - a semi-synthetic antibiotic of group of macroleads for oral administration. Are usually sensitive to drug: Bordetella pertussis; Borrelia burgdorferi; Moraxella (Branhamella) catarrhalis; Campylobacter coli, Campylobacter jejuni, Chlamydia trachomatis, psittaci and pneumoniae, Clostridium spp. (in t.ch.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.

Are moderately sensitive to drug: Haemophilus influenzae, Ureaplasma urealyticum, Vibrio cholerae.

Are steady against drug: Acinetobacter spp, Bacteroides fragilis; Enterobacteriaceae; Methi-R Staphylococcus; Pseudomonas spp; Fusobacterium; Mycoplasma hominis, Nocardia.

Pharmacokinetics. At adults: рокситромицин it is quickly soaked up after intake. Roksitromitsin is stabler than other macroleads in acid medium of a stomach. Administration of drug in 15 min. prior to food does not exert impact on pharmacokinetics. After administration of drug in a dose of 150 mg of Cmax in blood averages 6.6 mg/l and it is reached in 2.2 h. Administration of drug at an interval of 12 h provides preservation of effective concentration in blood within a day. T1/2 after a single dose of 150 mg makes 10.5 h.

After a single dose of 300 mg of a roksitromitsin average Cmax in blood makes 9.7 mg/l and is reached in 1.5 h.

At repeated purpose of a roksitromitsin (150 mg of 2 times/days, within 10 days) the equilibrium state in plasma is reached between 2-4 days, making Cmax of 9.3 mg/l.

Reception of 300 mg of a roksitromitsin each 24 h within 11 days provided Cmax at the level of 10.9 mg/l.

Roksitromitsin well gets into many fabrics, especially into lungs, into palatine tonsils and a prostate. Drug well gets also in cells, especially into neutrophilic leukocytes and monocytes, stimulating their phagocytal activity.

Linkng with blood proteins makes 96%, has saturable character and decreases at concentration of a roksitromitsin over 4 mg/l.

Roksitromitsin is metabolized only partially, more than a half of active agent is removed in an invariable view preferential with a stake, and also with urine. At adults with normal function of kidneys and a liver of 65% of a roksitromitsin it is removed with a stake.

At a renal failure removal of a roksitromitsin and its metabolites through kidneys makes about 10% of the accepted dose. The dose of drug does not change at a renal failure.

At a heavy liver failure of T1/2 it is extended (25 h) and Cmax increases.

Less than 0.05% of the accepted dose of a roksitromitsin get into breast milk.

Indications to use:

— upper respiratory tract infections: acute pharyngitises, tonsillitis, sinusitis;

— lower respiratory tract infections: pneumonia (including the caused such atypical activators as Chlamydia psittaci, Chlamydia pneumonia, Moraxella (Branhamella) catarrhalis, Legionella pneumophilia, etc.), bronchitis, bacterial infections at chronic obstructive diseases of lungs;

— infections of skin and soft tissues;

— genital infections (except gonorrhea), including uretrita, tserviko-vaginita;

— infections in odontology.

Route of administration and doses:

Adult appoint 150 mg of a roksitromitsin inside at an interval of 12 h. At the same time the daily dose makes 300 mg. Purpose of 300 mg once in days is possible.

To children (body weight over 40 kg) appoint 150 mg of a roksitromitsin inside at an interval of 12 h. The daily dose makes 300 mg.

This dosage form is not applied at children 4 years are younger!

At elderly patients the dosage and a daily dose of a roksitromitsin does not change.

In the presence of a renal failure рокситромицин it is appointed in a dose of 150 mg of 2 times/days.

At patients with a liver failure of 150 mg it is appointed once.

Duration of reception of a roksitromitsin depends on the indication to use, weight of infectious process and activity of the activator.

Roksitromitsin is accepted before meal orally by 1 or 2 times/days.

Rulid's tablet has to be washed down with enough water.

Features of use:

At purpose of drug Rulid extra care, control of function of a liver and correction of a dose is necessary for patients with a liver failure.

At purpose of drug the patient with a renal failure, and also the patient of advanced age, need for correction of a dose does not arise.

Side effects:

Anaphylactic reactions: Quincke's disease, bronchospasm, weakness, seldom acute anaphylaxis.

Skin reactions: rash, reddening, urtikariya.

Gastrointestinal reactions: nausea, vomiting, abdominal pains, diarrhea (it is very rare with blood).

Reactions from a liver: increase in liver enzymes (ALT, ACT, ShchF). Cholestatic or hepatocellular acute hepatitis.

Little changes of flavoring and olfactory feelings are possible.

Pancreatitis symptoms were in some cases observed.

Dizziness, headache, paresthesias.

Development of superinfection in view of growth of insensitive microorganisms is possible.

Interaction with other medicines:

The concomitant use of a terfenadin, in view of increase in concentration of the last is not recommended at a concomitant use of makrolidny antibiotics that can lead to development of heavy ventricular arrhythmias. Though this complication was not noted at a roksitromitsin, and in researches on volunteers any pharmacokinetic interactions or changes on an ECG were not shown, the combination of a roksitromitsin and a terfenadin is not recommended.

Reception of such drugs as астемизол, цизаприд, Pimozidum can lead to lengthening of an interval of QT and/or heavy arrhythmias of heart, as a result of increase in their serumal concentration, as a result of competitive influence for CYP 3A isoenzyme between the above-named drugs and makrolidny antibiotics.

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

At co-administration of a roksitromitsin with antagonists of vitamin K it is recommended to watch a prothrombin time or the international normalized relation (INR).

Roksitromitsin can replace a protein the connected Disopyramidum, leading to increase in serumal level of Disopyramidum. Monitoring of an ECG and, whenever possible, determination of level of Disopyramidum in serum is recommended.

At a concomitant use with digoxin increase in absorption of the last is possible. It is recommended to monitor the electrocardiogram and serumal level of cardiac glycoside. It is obligatory at emergence of symptoms of overdose of cardiac glycosides.

Roksitromitsin can increase a midazolam elimination half-life, leading to strengthening and lengthening of its action.

Contraindications:

— a concomitant use of drugs like ergotamine and dihydroergotamine;

— hypersensitivity to macroleads.

Combined use with derivatives of ergotamine and ergotaminopodobny vasoconstrictors is not allowed as can lead to development of "ergotism" and a necrosis of tissues of extremities.

With care to apply at patients with a heavy liver failure.

Overdose:

At overdose the gastric lavage and symptomatic therapy is necessary. 

The specific antidote does not exist.

Storage conditions:

At a temperature from 10 to 25 °C in dry protected from light and the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets on 150 mg.

10 tablets in the blister packaging on 1 blister with the application instruction place in a pack from a cardboard.