Roksitromitsin

General characteristics. Structure:

Active ingredient: 150 mg of a roksitromitsin.

Excipients: corn starch, sodium citrate, guar gum, polyethyleneglycol 6000, the water purified the talc purified of magnesium stearate, sodium glikolit starch, sodium carboxymethylcellulose, a gidroksipropilmetiltsellyuloza, diethyl phthalate, titanium dioxide.

Semi-synthetic antibiotic from group of macroleads of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. Pharmacological action - antibacterial (bacteriostatic). The mechanism of action is caused by disturbance of protein synthesis of microorganisms.

Drug is active concerning aerobic gram-positive bacteria: Streptococcii of group A and B, including Str. pyogenes, Str. agalactiae, Str. mitis, saunguis, viridans. Streptococcuspneuinoniae; Enterococcus spp. (are moderately sensitive), Staph. aureus (Methicillinum - sensitive, are moderately sensitive), Staph. epidermidis (Methicillinum - sensitive, are moderately sensitive), Bacillus cereus, Corynebacterium diphteriae, Listeria monocytogenes;

Aerobic gram-negative bacteria: Bordetella pertussis, Campylobacter coli, Campylobacter jejuni, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (is moderately sensitive), Helicobacter pylori, Legionella pneumophilia, Moraxella catarrhalis, Neisseria gonorrhoeae (is moderately sensitive), Neisseria meningitidis, Pasteurela multocida, Vibrio cholerae (is moderately sensitive);

Anaerobnykhbaktery: Actinomyces spp., Bacteroides oralis, Bacteroides urealiticus, Clostridium spp. (kromecl. difficile), Eubacterium spp., Peptococcus spp., Peptostreptococcus spp., Porphyromonas spp., Prevotella melaninogenica, Propionibacterium acnes;

Drug is also active in the relation: Borrelia burgdorfer, Chlamidia pneumoniae, Chlamidia psittaci, Chlamidia trachomatis, Cryptosporidium spp., Mycobacterium avium complex (is moderately sensitive), Mycobacterium tuberculosis. Mycoplasma pneumoniae, Rickettsia conorri, Rickettsia richttsii, Toxoplasma gondii, Ureaplasma urealyticum (is moderately sensitive).

Kpreparatuustoychiva: Enterobacteriaceae, Pseudomonas, Acinetobacter, Bacteriodes fragilis, Mycobacterium hominis.

Drug has the antiinflammatory activity caused by antioxidant properties and inhibition of production of cytokines.

Pharmacokinetics. It is quickly soaked up from a GIT and it is found in plasma in 15 min. (existence of food slows down absorption speed, but does not influence its completeness). Cmax is reached in 1,5-2 h and at a dose of 0,15 g makes 6,6 mg/l. Linkng with proteins of plasma - to 96%, is quickly distributed in tissues of airways (especially easy), almonds, a prostate gland, ovaries, kidneys, a liver. At reception in a dose of 0,15 g 2 times a day equilibrium concentration is reached in 2-4 days. It is removed in not changed look and in the form of metabolites generally through a GIT, partially easy (15%), kidneys (to 10%) and with breast milk (less than 0,05%). Average T1/2 - 10,5 h, at children aged from 1 month up to 13 years is T1/2 to 20 h. Does not kumulirut.

Indications to use:

Roksitromitsin apply to treatment of the infections caused by microorganisms, sensitive to a roksitromitsin.

- Respiratory infection and ENT organs: tonsillitis, pharyngitis, sinusitis, diphtheria, whooping cough, average otitis, atypical pneumonia, chronic obstructive diseases of lungs, bronchitis (acute and aggravation of chronic), pan-bronchitis, bronchiectasia;

- Infections of skin and soft tissues, in that number ordinary eels;

Dontogenous infections:

- The acute gastroenterocolitis (caused by Campylobacter jejuni);
- The ulcer of a duodenum and chronic gastritis (caused by H. pylori);
- The infections caused by Mycoplasma, Chlamidya, Legionella;
- Chronic prostatitis;
- Prevention of rheumatic fever;
- Infections of urinogenital system (urethritis not gonococcal, chlamydial gynecologic infections);
- Osteomyelitis, prevention of a spotted fever;

Other infectious diseases caused by microorganisms, sensitive to a roksitromitsin, at patients with the known hypersensitivity to penicillinic antibiotics.

Route of administration and doses:

Inside, to food, without chewing, washing down with water. The adult on 150 mg 2 times a day or 300 mg once, at a heavy renal failure - 150 mg/days.

Duration of a course is defined individually depending on weight of an infectious disease (of 5-12 days at acute respiratory diseases and ENT organs and up to 2-2,5 months at chronic osteomyelitis).

To children - 5-8 mg/kg/days in 2 receptions within no more than 10 days.

Features of use:

With care appoint to patients with a liver failure: only according to vital indications with periodic control of function of a liver and correction of the mode of dosing.

With care appoint to patients 65 years are more senior.

Side effects:

From a nervous system and sense bodys: dizziness, headache, weakness, indisposition, vision disorder and sense of smell, sonitus, taste change.

From bodies of a GIT: abdominal pain, dyspepsia, anorexia, meteorism, nausea, vomiting, lock or diarrhea, pancreatitis symptoms.

Allergic reactions: rash, itch, urticaria, bronchospasm, acute anaphylaxis.

Others: eczema, superinfection, oral and vaginal candidiasis.

Interaction with other medicines:

Roksitromitsin is incompatible with ergotaminpodobny drugs (probably development of an ergotism and necrosis of tissues of extremities).

Increases digoxin absorption, bioavailability of an omeprazol.

The probability of toxic effects of warfarin, theophylline, cyclosporine, astemizol, Disopyramidum and terfenadin increases. at co-administration with roksitromitsiny, as well as with other macroleads.

Ethambutolum: a synergism at combined use concerning Mycobacterium avium.

Sulfadiazinum, Pyrimethaminum: a synergism at combined use concerning protozoa.

Forces out Disopyramidum from complexes with proteins of plasma, increases concentration in serum of an astemizol and Pimozidum (is followed by lengthening of an interval of QT an ECG or heavy arrhythmias).

Contraindications:

• Hypersensitivity to a roksitromitsin (and including to other macroleads);
• Period of pregnancy and lactation;
• Porphyria;
• The expressed abnormal liver function;
• Children's age up to 2 months.
• Concomitant use of the drugs containing ergotamine, diergotamine, or other Secalecornutum alkaloids.

Storage conditions:

List B. To store in the place protected from moisture and light, at a temperature not above +25 °C. To store in the place, unavailable to children. Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

10 tablets in bank of polymeric. 1 bank together with a leaf insert in a pack. 10 tablets in a blister strip packaging. 1 k.ya.a. together with a leaf insert in a pack.