Klaritsit

General characteristics. Structure:

Active ingredient: klaritromitsina of 500 mg; 250 mg.

Other components: starch corn, cellulose microcrystallic, starch prezhelatinizirovanny, sodium of a kroskarmeloz, talc, magnesium stearate, stearic acid, silicon dioxide colloid anhydrous, a covering for drawing a cover of Opadry II Yellow.

Pharmacological properties:

Pharmacodynamics. Klaritsit – an antibiotic of group of macroleads, semi-synthetic derivative erythromycin. The changed structure of a molecule does drug more bioavailable, stable in acid medium, increases concentration in fabrics, expands an antimicrobic range, prolongs an elimination half-life that gives the chance to appoint drug once a day and that to improve process of treatment of patients. Drug suppresses protein synthesis in a microbic cell, interacting with 50S a ribosome subunit of bacteria.
Klaritsit it is active relatively the majority of strains of such microorganisms:
– aerobic gram-positive – Staphylococcus aureus, Streptococcus agalactiae, Streptococcus pyogenes, alpha and hemolitic streptococci (viridans group), Streptococcus pneumoniae, Streptococci (the C, F groups, G), Listeria monocytogenes;
– aerobic gram-negative – Haemophilus influenzae (parainfluenzae), Neisseria gonorrhoeae, Helicobacter pylori, Legionella pneumophila, Moraxella (Branhamella) catarrhalis;
– mycobacteria – Mycobacterium leprae, Mycobacterium chelonae, Mycobacterium fortuitum, Mycobacterium kansasii, the Mycobacterium avium complex which part Mycobacterium avium and Mycobacterium intracellulare are;
– other microorganisms – Mycoplasma pneumoniae, Chlamydia pneumonіae (trachomatis), Campylobacter jejuni, Borrelia burgdorferi, Treponema pallidum.
Products beta lactamelements do not influence activities of drug.

Pharmacokinetics. After oral administration of Klaritsit it is quickly absorbed, reaching the maximum concentration in 2 – 3 hours. Biological availability makes about 68%. After absorption drug gets in the most part of fabrics, except TsNS. In tonsillar and pulmonary fabrics are observed above concentration of drug, than in other fabrics; concentration in fabrics are higher, than in serum.
80% of drug contact proteins. It is metabolized by a liver with formation of the main metabolite of a 14-gidroksiklaritromitsin which antimicrobic activity, than invariable substances has such or on 1 – 2 orders smaller (depending on a species of microorganism). It is excreted with urine – 36% of a dose, with a stake – 52%. The elimination half-life depends on a dose: at a dose of 250 mg each 12 hours – 3 – 4 hours, at a dose of 500 mg each 12 hours – 5 – 7 hours.

Indications to use:

The infections caused by microorganisms, sensitive to Klaritromitsin:
- infections of ENT organs (pharyngitis, sinusitis, tonsillitis);
- respiratory infections (bronchitis, pneumonia of a negospitaln, gospitaln);
- infections of skin and soft tissues (folliculitis, erysipelatous inflammation, streptoderma, staphyloderma);
- widespread or are localized the mikobakterialny infections caused by mycobacteria, sensitive to effect of drug, including in HIV-positive patients with quantity of CD4 of lymphocytes that smaller or 100/mm3 is equal;
- dontogenous infections.

Klaritsit at the same time apply with drugs to braking of acidity of a gastric juice for H.pylori eradikation at treatment of a duodenal ulcer.

Route of administration and doses:

For adults and children aged from 12 years the average dose for intake makes 250 mg 2 times a day. In case of requirement of Klaritsit it is possible to appoint 500 mg 2 times a day. Duration of a course of treatment – 5 – 14 days, except for not hospital pneumonia and sinusitis that treatments within 6 – 14 days need.
The dosage for patients with damages of kidneys and a liver defines the doctor respectively to a step of insufficiency of function.
The patient with a heavy renal failure (clearance of creatinine less than 30 ml/minutes.) Klaritsit's dose should be adjusted. The following doses are offered:

Dose at clearance of creatinine> 30 ml/minutes.
The corrected dose at clearance of creatinine <30 ml/minutes.
 
On 500 mg 2 times a day
Initial dose – 500 mg, then on 250 mg 2 times a day
 
On 250 mg 2 times a day
250 mg of 1 times a day

At treatment of mikobakterialny infections the dose for adults is recommended makes 500 mg 2 times a day.

Treatment of widespread mikobakterialny infections at patients on AIDS needs to be continued before improvement of a clinical and microbiological state. Klaritsit apply together with other germicides.

Treatment of not tuberculosis mikobakterialny tuberculosis infections should be extended the decision of the doctor.

The recommended dose for prevention of mikobakterialny infections – 500 mg 2 times a day.

For treatment of dontogenous infections the dose – 250 mg 2 times a day within 5 days is recommended.

For H.pylori eradikation пропонуються following schemes of treatment.

Scheme of treatment by three drugs:

500 mg of Klaritsit 2 times a day along with reception of a corresponding dose of inhibitor of a proton pomp (for example, a lansoprazola, a pantoprazola, an omeprazola) and 1000 mg of amoxicillin 2 times a day within 10 days.

Scheme of treatment by two drugs:

500 mg of Klaritsit 3 times a day along with reception of a corresponding dose of inhibitor of a proton pomp (for example, a pantoprazola, an omeprazola) within 14 days, then to accept inhibitor of a proton pomp (пантопразол, омепразол) in the corresponding dose during the next 14 days.

Features of use:

Use during pregnancy or feeding by a breast.
During pregnancy appoint drug only after careful assessment of comparison of advantage and risk, especially in the first trimester of pregnancy. Data about use of drug in the period of a lactation are absent. Klaritsit and its active metabolite are found in breast milk.

Children.
To children up to 3 years drug in this dosage form is not appointed. To children from 4 to 12 years drug appoint 7,5 mg/kg of body weight in a daily dose; the maximum daily dose – 500 mg, duration of a course of treatment – 7 – 10 days.

Klaritsit it is necessary to take with caution the patient with disturbances of functions of a liver and/or kidneys, and also to patients of advanced age.
Drug can be accepted with food. Reception with food reduces speed, but not degree absorption.

Ability to influence the speed of reactions when driving motor transport or other mechanisms.
Influence on ability to manage vehicles and mechanisms it is not established.

Side effects:

Nausea, vomiting, taste changes, pain in epigastric area, diarrhea, tranzitorny increase in activity of hepatic transaminases, allergic reactions are possible (a small tortoiseshell, an enanthesis, in isolated cases – an acute anaphylaxis and Stephens-Johnson's syndrome); temporary side effects from the central nervous system (a headache, dizziness, feeling of alarm, sleeplessness, alarming dreams, a ring in ears, consciousness misting, a disorientation, hallucinations, psychoses and depersonalization); glossitis, stomatitis, fungal infections mucous mouth and decolouration of language; hypoglycemia; leukopenia and thrombocytopenia; pseudomembranous colitis. It is similar to the others of makrolidny antibiotics at Klaritsit's use prolongation of a QT interval, tachycardia and tremblings/ventricular fibrillations are possible.

During treatment by Klaritsit there can be superinfections caused by resistant bacteria or fungi; in that case it is necessary to refuse treatment by drug.

Interaction with other medicines:

At simultaneous use of Klaritsit with theophylline, carbamazepine, astemizoly, alkaloids of horns, triazolamy, midazolam, cyclosporine observe increase in contents of the last in a blood plasma.

Simultaneous use of Klaritsit and terfenadin led to increase by 2 – 3 times of concentration of an acid metabolite of a terfenadin in blood serum, and also lengthenings of an interval of QT on an ECG that was not followed by emergence of clinically significant symptoms. Simultaneous use of these drugs should be avoided.

Simultaneous use of Klaritsit with tsizapridy, Pimozidum can lead to lengthening of an interval of QT and cardiac arrhythmia.

At simultaneous use of Klaritsit with quinidine or Disopyramidum chances of blinking/trembling of ventricles. Control of level of these drugs in blood during treatment by Klaritsit is necessary.

At Klaritsit's reception along with digoxin concentration of digoxin in blood serum can increase that demands in such cases to control of its level.

At simultaneous use of Klaritsit and a rifambutin or rifampicin Klaritsit's concentration in blood serum decreases (more as by 50%).

At simultaneous use with Klaritsit effect of warfarin amplifies. Therefore patients who accept warfarin need to control a prothrombin time.

At a concomitant use of Klaritsit and inhibitors of HMG-CoA reductase, for example a lovastatina or a simvastatina, it was very seldom observed рабдомиолиз.

Simultaneous use of Klaritsit and zidovudine by HIV-positive patients can entail decrease in constant levels of a zidovudine in blood. But such is interaction it is not observed in HIV-positive children at simultaneous use of Klaritsit in the form of suspension and a zidovudine or a dideoksinozin.

Ritonavir slows down Klaritsit's metabolism.

Contraindications:

Klaritsit it is contraindicated to patients who have hypersensitivity to macroleads. In case of allergic reactions or hypersensitivity reaction it is necessary to carry out an emergency maintenance therapy.

Overdose:

At overdose gastrointestinal disturbances (nausea, vomiting, diarrhea), disturbance of a mental state, a hypopotassemia, an anoxemia are possible.
Therapeutic measures at overdose the substances directed to removals from an organism with the help a gastric lavage the probe and holding the general supporting actions. Hemodialysis or peritoneal dialysis ineffective.

Storage conditions:

Store in the place, unavailable to children, in original packaging at a temperature from 15 °C to 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated yellow color, a round form, with a notch, 250 mg; 500 mg.