Roksilid

General characteristics. Structure:

Active ingredient: roxithromycin;

1 tablet contains a roksitromitsin (in terms of 100% substance, anhydrous and free from solvents) 150 mg;

excipients: cellulose microcrystallic, povidone, кросповидон, silicon dioxide colloid anhydrous, talc, magnesium stearate, сепифилм 752 white.

Pharmacological properties:

Pharmacodynamics. Roksitromitsin is a semi-synthetic antibiotic of group of macroleads. The antibacterial range of a roksitromitsin includes gram-positive and gram-negative aerobic and anaerobic microorganisms.

Are sensitive to a roksitromitsin:

aerobic bacteria – staphylococcus (excepting metitsilinstoyky strains), streptococci, Corynebacterium spp., Bacillus cereus, Listeria monocytogenes, Neisserria gonorrhoeae, N.meningitidis, Bordetella pertussis, Helicobacter pylori, Gardnerella vaginalis, Branhamella (Moraxella) catarrhalis and Legionella pneumophila.

Sensitivity of strains of Haemophilus influenzae non-constant;

anaerobic bacteria – Bacteroides oralis, B.melaninogenicus, B.ureolyticus, Clostridium perfringens, Eubacterium spp., Peptococcus spp., Peptostreptococcus spp. and Propionibacterium acnes.

Bacteroides fragilis, Clostridium difficile usually resistant to a roksitromitsin.

Roksitromitsin active Chlamidia trachomatis, Ureaplasma ureolyticus, Mycoplasma pneumoniae, Rickettsia rickettsii and R.conorii is also relative.

Roksitromitsin acts bacteriostatically, inhibiting synthesis of protein of a bacterial wall.

Pharmacokinetics. Roksitromitsin easily is soaked up and defined in plasma in 15 min.; after oral administration of a dose of 150 mg the maximum concentration in plasma are reached within 2 h and average 6,6 mg/l. Administration of drug at an interval of 12 h provides concentration, effective against sensitive microorganisms, in blood for days. After reusable reception with a 12-hour interval equilibrium concentration are reached for 2-4 days. Well gets into fabrics (lungs, almonds, a prostate), liquids of an organism and in macrophages. The antibiotic is exposed to partial metabolism in a liver, the main part is removed with excrements (about 50%) in not changed look and partially – in the form of metabolites, to 12% is removed by kidneys, to 15% – lungs. The elimination half-life after one-time administration of drug makes about 10,5 h.

Pharmaceutical characteristics.

Main physical and chemical properties: tablets, coated, white color, a round form with a biconvex surface.

Indications to use:

The infections caused by microorganisms, sensitive to a roksitromitsin:

- ENT organs and airways (tonsillitis, pharyngitis, sinusitis, average otitis, pneumonia, bronchitis);

- skin and soft tissues;

- urogenital infections, including caused by chlamydias;

- dontogenous infections;

- prevention of a spotted fever at persons who were in contact with the patient.

Route of administration and doses:

The pill Roksilid® needs to be taken in 15 min. prior to food, without chewing and washing down with enough liquid.

Adult: on 300 mg/days (on 150 mg each 12 h or on 300 mg once before food).

To children with body weight more than 40 kg: depending on a type of the activator and weight of infectious process, on 150 mg 2 times a day (i.e. at most 300 mg/days).

Duration of treatment is 5-10 days depending on indications and the clinical answer. At streptococcal infections of a throat the course of treatment makes not less than 10 days. For some patients at not gonococcal urogenital infections for full treatment the course of treatment up to 14 days can be necessary.

For patients with a heavy liver or renal failure (the clearance of creatinine is less than 0,25 ml / c) a dose it is necessary to lower: one tablet on 150 mg each 24 h before food.

For patients of advanced age dose adjustment is not necessary.

Features of use:

Use during pregnancy or feeding by a breast. Drug should not be used during pregnancy and feeding by a breast.

Children. Drug is not used at children with body weight to 40 kg.

Patients should appoint drug with care with a heavy liver failure. In need of administration of drug it is necessary to carry out regular control of function of a liver and to carry out correction of doses. There is a cross resistance with erythromycin. As well as for other antibiotics at prolonged use or at repeated administration of drug development of microorganisms, steady against a roksitromitsin, or fungal infections is possible (mycoses). In the presence patients have hypopotassemias, disturbances of AV conductivity, arrhythmia or the extended QT interval use of a roksitromitsin should be carried out carefully, carrying out regular ECG control. In case of long diarrhea or at suspicion on existence of an intestinal disease (pseudomembranous colitis) it is necessary to cancel administration of drug. It is not necessary to accept the drugs braking an intestines peristaltics. In the presence of heavy hypersensitivity reactions (for example an anaphylaxis) it is necessary to cancel immediately administration of drug and to hold such events of ambulance as reception of antihistamines, corticosteroids, sympathomimetics, and if necessary – artificial ventilation of the lungs.

Ability to influence the speed of reactions at control of motor transport or work with other mechanisms. During treatment it is necessary to refuse control of motor transport and work with other mechanisms.

Side effects:

From bodies of a GIT: nausea, vomiting, anorexia, lock/diarrhea, pain in epigastriums, a meteorism, tranzitorny increase in hepatic transaminases and an alkaline phosphatase, cholestatic hepatitis or a hepatocellular acute hepatitis, pancreatitis symptoms, a pseudomembranous coloenteritis.

From a nervous system and sense bodys: insanity, headache, weakness, change of taste and/or sense of smell, sonitus, paresthesias.

Allergic reactions: itch, rash, dermahemia, urticaria, eczema, Quincke's disease, bronchospasm, acute anaphylaxis.

Others: development of superinfection, candidiasis of an oral cavity and vagina, eosinophilia, giperkreatininemiya, pigmentation of nails.

Interaction with other medicines:

Theophylline: at a concomitant use elimination of theophylline decreases and manifestation of its side effects amplifies. Regular control of size of serumal theophylline, especially is recommended if prior to reception of a roksitromitsin it made 15 mg/l or more.

Antagonists of vitamin K (the means braking coagulability of blood): increase in a prothrombin time is possible.

Digoxin: at a concomitant use of a roksitromitsin (as well as other macroleads) increase in level of concentration of digoxin in blood and increase in its by-effects is possible. It takes place and at reception of other cardiac glycosides. Midazolam: at a concomitant use area size under a pharmacokinetic curve and semi-removal time for midazolam therefore the effect of midazolam can amplify and be extended increases.

Disopyramidum: at a concomitant use the size of linkng of Disopyramidum with proteins therefore the level of free drug in blood increases decreases.

Terfenadin: at a concomitant use of a terfenadin and some macroleads increase in level of a terfenadin in blood serum is possible. It can lead to development of heavy arrhythmia (up to Torsades de pointes). Despite the lack of similar observations in relation to a roksitromitsin, the concomitant use is not recommended. Astemizol, цизаприд, Pimozidum: at a concomitant use the serumal level of these substances increases. Because of danger of development of disturbances of a cordial rhythm the concomitant use is not recommended.

Cyclosporine: at a concomitant use perhaps slight increase of level of cyclosporine in blood serum. Generally correction of doses is not required. There is no interaction with antacids, H2 antagonists of receptors, carbamazepine and warfarin.

Increases toxicity of ergotamine and ergotaminopodobny vasoconstrictors (the risk of development of an ergotism and necrosis of tissues of extremities increases).

Contraindications:

Hypersensitivity to a roksitromitsin or any other component of drug. Heavy abnormal liver functions. Pregnancy, feeding period breast. Children with body weight it is less than 40 kg.

Overdose:

Symptoms: abdominal pain, nausea, vomiting, diarrhea, anorexia, lock, increase in activity of hepatic transaminases, weakness.

Treatment: gastric lavage, absorbent carbon inside. In hard cases: actions for recovery of a water and electrolytic state. The specific antidote is absent. The hemodialysis is inefficient.

Storage conditions:

Period of validity. 2 years. To store in the place, unavailable to children, in original packaging, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging, on 1 blister strip packaging in a pack.