Klaritromitsin

General characteristics. Structure:

Active ingredient: 250 mg of a klaritromitsin.

Excipients: sodium krakhmalglikolit, microcrystallic cellulose, starch corn, the talc purified magnesium stearate, PVP K-30, polyethyleneglycol 6000, propylene glycol, Tabcoatpink dye (a gidroksipropilmetiltsellyuloz, polyethyleneglycol, titanium dioxide, E 127 erythrosine, talc).

Semi-synthetic antimicrobic drug with pronounced bacteriostatic action.

Pharmacological properties:

Pharmacodynamics. Klaritromitsin represents semi-synthetic derivative erythromycin. In a cell of susceptible bacteria кларитромицин shows antimicrobic activity, connecting 50S a ribosome subunit and suppressing, thus, protein synthesis. Nature of antimicrobic action of a klaritromitsin preferential bacteriostatic. Klaritromitsin shows antibacterial activity concerning the following range of microorganisms:

Gram-positive bacteria: Streptococcus agalactiae, Streptococcus pyogenes, Streptococcus viridans, Streptococcus pneumoniae, Listeria monocytogenes, Staphylococcus aureus.

Gramotritsalny bacteria: Haemophilus influenzae, Haemophilus parainfluenzae, Neisseria gonorrheae, Legionella pneuophila, Pasteurella multocids, Helicobacter pylori, Campylobacter jejuni, Moraxella (Branthamela) catarrhalis, Bordetella pertussis.

Other microorganisms: Chlamydia pneumoniae (TWAR), Chlamydia trachomatis, Borrelia burgoferi, the Mycobacterium avium (MAC) complex consisting of Mycobacterium avium, Mycobacterium intracellular, Mycobacterium leprae, Mycobacterium chelonae, Mycobacterium fortuitum, Mycobacterium kansasii.

Anaerobnyemikroorganiza: Clostridium perfringes, Peptococcus niger, Propionibacterium acnes, Bacteroides melaninogenicus.

Mycoplasmas: Mycoplasma pneumoniae.

The metabolite of a klaritromitsin 14-gidroksiklaritromitsin also has therapeutic significant antimicrobic activity.

Pharmacokinetics. Klaritromitsin at intake is quickly and actively soaked up, its biological availability makes about 50%. Drug and its stable metabolite does not kumulirutsya. Meal just before purpose of drug slows down the beginning of absorption of a klaritromitsin a little, but does not influence its biological availability and formation of an active metabolite of a 14-gidroksiklaritromitsin. Thus, кларитромицин it can be appointed without communication with meal.

At purpose of drug 2 times a day on 250 mg the maximum equilibrium concentration (Relish) of a klaritromitsin in plasma was reached in 2-3 days and averaged 1 mkg/ml for a klaritromitsin and 0,6 mkg/ml for a 14-gidroksiklaritromitsin, at the same time elimination half-lives of initial connection and its metabolite made 3-4 and 5-6 hours, respectively.

At purpose of drug 2 times a day on 500 mg equilibrium Smaks of a klaritromitsin and its hydroxylated metabolite in plasma averaged 2,7-2,9 mkg/ml and 0,88-0,83 mkg/ml, respectively. The elimination half-life of initial connection at purpose of a dose of 500 mg made 5-7 hours whereas for a 14-gidroksiklaritromitsin this value made 7-9 hours.

After purpose of higher doses of a klaritromitsin further increase in Smaks and duration of an elimination half-life is noted that testifies to nonlinear character of pharmacokinetics of a klaritromitsin.

At single appointment inside adult 250 mg or 1200 mg of a klaritromitsin with urine are allocated to 37,9% of the appointed upper dose appointed the lower and 46,0% from. Allocation of a klaritromitsin with a stake makes 40,2% and 29,1% of these doses, respectively.

Klaritromitsin and him 14 hydroxymetabolite are quickly distributed on all fabrics and liquids of an organism. After intake concentration of a klaritromitsin in fabrics (especially in lungs) is several times higher, than in a blood plasma.

Indications to use:

Klaritromitsin is shown for treatment of the infectious diseases caused by sensitive microorganisms. Treat these diseases:

Infections of a lower part of respiratory tracts (bronchitis, pneumonia). Infections of an upper part of respiratory tracts (pharyngitises, sinusitis). Infections of skin and soft tissues (folliculites, phlegmons, erysipelatous inflammation).

The extended or localized mikobakterialny infections caused by Mycobacterium avium and Mycobacterium intracellulare. The localized infections caused by Mycobacterium chelonae, Mycobacterium fortuitum and Mycobacterium kansasii.

Klaritromitsin appoint for prevention of spread of the infection caused by the Mycobacterium avium (MAC) complex, the HIV-positive patient with the maintenance of lymphocytes of CD4 (T-helper lymphocytes) of no more than 100 in 1 mm3.

Klaritromitsin is shown for N.'s eradikation of pylori (only as a part of a combination therapy).

Route of administration and doses:

Inside, without chewing, washing down with a small amount of liquid. Irrespective of meal.

To adults and children is more senior 12 летКларитромицин each 12 h appoint in an average dose 250 mg.

At sinusitis, heavy infections and at the diseases caused by Haemophilus influenzae, drug is appointed on 500 mg by each 12 h. The maximum daily dose - 2 g. A course of treatment - 8-14 days.

For Helicobacter pylori eradikation at patients with a peptic ulcer of a duodenum or stomach Klaritromitsin appoint in a dose 250-500 mg of 2 times/days as a part of a combination therapy. The course of treatment makes 7 days.

Tablets should not be broken. They should be swallowed entirely, washing down with a small amount of liquid.

For treatment and prevention of the widespread infection caused by Mycobacterium avium complex, to adults and children 12 years are more senior each 12 h appoint drug in a dose of 500 mg. If necessary increase in a dose is possible. Treatment of the infection caused by Mycobacterium avium complex, long.

Patients with renal failures (KK less than 30 ml/min. or level of serumal creatinine more than 3.3 mg/dl) should reduce a dose twice or to double an interval between receptions.

The dose decline for elderly people is not required.

Features of use:

At purpose of drug it is necessary to consider that among antibiotics of group of macroleads there is a cross resistance.

Patients with abnormal liver functions of easy and average degree do not have need to reduce a drug dose if function of kidneys is normal. Patients with heavy renal failures should reduce a dose.
Treatment by antibiotics changes normal flora of intestines therefore development of the superinfection caused by resistant microorganisms is possible.

The patient has to be warned that at heavy persistent diarrhea which can be caused by pseudomembranous colitis he should see a doctor.

It is recommended to measure concentration of theophylline, carbamazepine, digoxin, a lovastatin, a simvastatin, a triazolam, midazolam, Phenytoinum, cyclosporine, a takrolimus and alkaloids of an ergot in serum at their use along with klaritromitsiny.

It is necessary to control periodically a prothrombin time at the patients receiving кларитромицин along with warfarin or other peroral anticoagulants.

Klaritromitsin's use in the I trimester of pregnancy is contraindicated. Use of Klaritromitsinaa in II and III trimesters of pregnancy is possible only when the expected advantage for mother exceeds potential risk for a fruit. In need of use of drug in the period of a lactation it is necessary to stop breastfeeding.

Influence on ability to driving of motor transport and to control of mechanisms
Drug does not exert impact on the speed of psychomotor reactions during the driving or work with mechanisms.

Side effects:

Complaints from digestive tract are most often noted (dyspepsia: nausea, abdominal pains, vomiting and diarrhea; pseudomembranous colitis). Headaches, changes of taste and passing increase in activity of enzymes of a liver belong to other side reactions.

There are messages on exceptional cases of hepatitis with increase in level of enzymes of a liver in blood serum and development of a cholestasia and jaundice. These injuries of a liver in certain cases were heavy and, as a rule, reversible. The liver failure with a lethal outcome was in exceptional cases observed. It was connected with serious basic diseases and/or a concomitant use of other medicines.

At reception of a klaritromitsin allergic reactions which intensity varied from a small tortoiseshell and skin rash, to an anaphylaxis and Stephens-Johnson's syndrome were inside observed.

There are messages on decrease in hearing during treatment klaritromitsiny which was in most cases recovered after drug withdrawal. Also it is reported about taste perception changes.

There are messages on development of a glossitis, stomatitis, candidiasis of a mucous membrane of an oral cavity and language discoloration during treatment klaritromitsiny. It is reported also about discoloration of teeth at the patients receiving кларитромицин. Discoloration of teeth in most cases was reversible.

The hypoglycemia was in rare instances noted; in a number of these cases the gipoklikemiya developed at the patients accepting during treatment klaritromitsiny hypoglycemic means for oral administration or insulin.

It is reported about separate cases of thrombocytopenia.

At treatment klaritromitsiny lengthening of an interval of QT, ventricular arrhythmia, including a ventricular Bouveret's disease and a torsade de pointes of ventricles was extremely seldom observed.

At prolonged treatment of patients with AIDS and other immunodeficiency with high doses of a klaritromitsin (1000-2000 mg/days) concerning the infectious diseases caused by mycobacteria nausea, vomiting, taste disturbances, an abdominal pain, skin rash, diarrhea, a meteorism, a headache, locks, a hearing disorder, increase in level of aminotransferases of blood serum most often meet. Less often patients complained of sleeplessness, short wind and dryness in a mouth. Frequency of side reactions among the patients receiving doses of 1000 mg and 2000 mg was comparable, however among the patients receiving 4000 mg/days кларитромицин these reactions met by 3-4 times more often.

Interaction with other medicines:

The same as at reception of other antibiotics from group of macroleads, use of a klaritromitsin along with medicines, metaboliziruyemy system of P450 cytochrome (carbamazepine, такролимус, hexobarbital, alfentanil, Bromocriptinum, Valproatums, ловастатин, дисопирамид, Phenytoinum, cyclosporine), can be followed by increase in concentration of these drugs in serum and strengthening of their effects. At simultaneous use with klaritromitsiny there can be a need of control of serumal concentration of these drugs.

- It is reported about exceptional cases of an acute necrosis of the skeletal muscles matching on time co-administration of a klaritromitsin and inhibitors of gidroksimetilglutaril-SOA-reduktazy - a lovastatina and a simvastatina.

- There are messages on increase in concentration of digoxin in plasma of the patients receiving at the same time digoxin and tablets of a klaritromitsin. At such patients it is necessary to control constantly the content of digoxin in serum to avoid digitalis intoxication.

- Simultaneous use of a klaritromitsin with tsizapridy, Pimozidum, terfenadiny and astemizoly is contraindicated because of possible development of life-threatening cardiac arrhythmias.

Klaritromitsin can reduce clearance of a triazolam and, thus, increase its pharmacological effects with development of drowsiness and confusion of consciousness.

Simultaneous use of a klaritromitsin and ergotamine or dihydroergotamine is connected at some patients with the acute ergotaminovy intoxication which is shown a spasm of peripheral vessels and perverted by sensitivity.

Co-administration by the HIV-positive adult of a zidovudine orally and tablets of a klaritromitsin can lead to reduction of equilibrium concentration of a zidovudine. Considering what кларитромицин probably changes absorption of the zidovudine appointed at the same time orally, this interaction substantially manages to be avoided at reception of a klaritromitsin and zidovudine in various hours of days.

At co-administration of a klaritromitsin and ritonavir values of serumal concentration of a klaritromitsin increase. Dose adjustment of a klaritromitsin in these cases for patients with normal function of kidneys is not required. However patients with clearance of creatinine have from 30 to 60 ml/min., the dose of a klaritromitsin should be lowered by 50%. At clearance of creatinine less than 30 ml/min., a dose of a klaritromitsin should be lowered by 75%. At simultaneous treatment ritonaviry it is not necessary to appoint кларитромицин in doses over 1 g/days.

At co-administration of a klaritromitsin and omeprazol there is an increase in their concentration in plasma, however, dose adjustment of these drugs is not required. The most frequent side reactions arising at treatment klaritromitsiny and omeprazoly, are taste disturbance, nausea and vomiting. Less than at 1% of patients increase in serumal concentration of direct bilirubin, hepatic transaminases and creatinine can be noted.

Contraindications:

– heavy abnormal liver functions;
– hepatitis (in the anamnesis);
– porphyria;
– I trimester of pregnancy;
– hypersensitivity to a klaritromitsin and other antibiotics from group of macroleads.

Klaritromitsin it is not necessary to appoint the patient receiving терфенадин, цизаприд, Pimozidum or астемизол.

Overdose:

Development of symptoms from digestive tract (nausea, vomiting, diarrhea) is probable. At overdose the immediate gastric lavage and a symptomatic treatment is necessary.

The hemodialysis and peritoneal dialysis do not lead to considerable change of level of a klaritromitsin in blood serum.

Storage conditions:

List B. 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:

14 tablets in a blister strip packaging and in a cardboard pack.