Zimbaktar

General characteristics. Structure:

Active agent: кларитромицин 250 mg; 500 mg.

Pharmacological properties:

Semi-synthetic antibiotic of group of macroleads. Suppresses protein synthesis in a microbic cell, interacting with 50S a ribosome subunit of bacteria. Works generally bacteriostatically, and also bakteritsidno.
It is active concerning gram-positive bacteria: Streptococcus spp., Staphylococcus spp., Listeria monocytogenes, Corynebacterium spp.; gram-negative bacteria: Helicobacter pylori, Haemophilus influenzae, Haemophilus ducreyi, Moraxella catarrhalis, Bordetella pertussis, Neisseria gonorrhoeae, Neisseria meningitidis, Borrelia burgdorferi; anaerobic bacteria: Eubacterium spp., Peptococcus spp., Propionibacterium spp., Clostridium perfringens, Bacteroides melaninogenicus; intracellular microorganisms: Legionella pneumophila, Chlamydia trachomatis, Chlamydophila pneumoniae, Ureaplasma urealyticum, Mycoplasma pneumoniae.
Mycobacterium spp is active also concerning Toxoplasma gondii. (except Mycobacterium tuberculosis).

Pharmacokinetics. At intake кларитромицин it is well absorbed from a GIT. Meal slows down absorption, but does not influence bioavailability of active agent.
Klaritromitsin well gets into biological liquids and body tissues where reaches concentration by 10 times bigger, than in plasma.
About 20% of a klaritromitsin are at once metabolized with formation of the main metabolite of a 14-gidroklaritromitsin.
At a dose of 250 mg of T1/2 makes 3-4 h, at a dose of 500 mg - 5-7 h.
It is removed with urine in not changed look and in the form of metabolites.

Indications to use:

Treatment of the infectious and inflammatory diseases caused by activators, sensitive to a klaritromitsin: infections of upper parts of respiratory tracts and ENT organs (tonzillofaringit, average otitis, acute sinusitis); infections of lower parts of respiratory tracts (acute bronchitis, exacerbation of chronic bronchitis, community-acquired bacterial and atypical pneumonia); infections of skin and soft tissues; mikobakterialny infections (M.avium complex, M.kansasii, M.marinum, M.leprae) and their prevention at patients AIDS; Helicobacter pylori eradikation at patients with a peptic ulcer of a duodenum or stomach (only as a part of a combination therapy).

Route of administration and doses:

Individual. At intake for adults and children 12 years a single dose are more senior makes 0.25-1 g, the frequency of reception of 2 times/days.
For children the daily dose makes 15 mg/kg/days in 2 receptions.
Duration of treatment depends on indications.
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.
Maximum daily doses: for adults - 2 g, for children of 1 g.

Features of use:

Between antibiotics from group of macroleads cross resistance is observed.

Treatment by antibiotics changes normal flora of intestines therefore development of the superinfection caused by resistant microorganisms is possible.

It must be kept in mind that heavy persistent diarrhea can be caused by development of pseudomembranous colitis.

At simultaneous use with klaritromitsiny it is recommended to control concentration in a blood plasma of theophylline, carbamazepine, digoxin, a lovastatin, a simvastatin, a triazolam, midazolam, Phenytoinum, cyclosporine and alkaloids of an ergot.

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

Use in pediatrics

Now there are not enough data on efficiency and safety of use of a klaritromitsin for children aged up to 6 months.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, abdominal pain, stomatitis, glossitis; seldom - pseudomembranous colitis; in some cases - increase in activity of enzymes of a liver, cholestatic jaundice.

From TsNS: dizziness, confusion of consciousness, sensation of fear, sleeplessness; dreadful dreams.

Allergic reactions: small tortoiseshell, anaphylactic reactions; in some cases - Stephens-Johnson's syndrome.

Others: temporary changes of flavoring feelings.

Interaction with other medicines:

Klaritromitsin oppresses activity of an isoenzyme of CYP3A4 that leads to delay of speed of metabolism of an astemizol at their simultaneous use. Thereof there is an increase in an interval of QT and increase in risk of development of ventricular arrhythmia like "pirouette".

At simultaneous use with atorvastatiny concentration of an atorvastatin in a blood plasma moderately increases, the risk of development of a myopathy increases.

At simultaneous use with warfarin strengthening of anticoagulating effect of warfarin and increase in risk of development of bleedings is possible.

At simultaneous use with digoxin perhaps substantial increase of concentration of digoxin in a blood plasma and risk of development of glikozidny intoxication.

Believe that increase in concentration of Disopyramidum in a blood plasma owing to inhibition of his metabolism in a liver under the influence of a klaritromitsin is possible. There is a risk of prolongation of an interval of QT, development of disturbances of a cordial rhythm like "pirouette", increases in secretion of insulin and a hypopotassemia.

At simultaneous use with a zidovudine bioavailability of a zidovudine decreases a little; with itrakonazoly - concentration of an itrakonazol in a blood plasma considerably increases, believe that there is a risk of strengthening of side effect.

At simultaneous use with carbamazepine concentration of carbamazepine in a blood plasma increases, there is a risk of strengthening of its side effect; with colchicine - cases of the heavy, life-threatening toxic reactions caused by effect of colchicine are described; with lansoprazoly - the glossitis, stomatitis and/or emergence of dark coloring of language are possible; with Methylprednisolonum - the clearance of Methylprednisolonum decreases; with midazolam - concentration of midazolam in a blood plasma increases and its effects amplify.

At simultaneous use with omeprazoly concentration of an omeprazol considerably increases and slightly concentration of a klaritromitsin in a blood plasma increases.

At simultaneous use with Pimozidum concentration of Pimozidum in a blood plasma increases, there is a risk of development of heavy cardiotoxic action; with Prednisonum - cases of development of an acute mania and psychosis are described; with ritonaviry - perhaps substantial increase of concentration of a klaritromitsin, at the same time concentration of its metabolite of a 14-gidroksiklaritromitsin considerably decreases; with rifabutiny - concentration of a rifabutin in a blood plasma increases, the risk of development of a uveitis increases, concentration of a klaritromitsin in a blood plasma decreases.

At simultaneous use with rifampicin concentration of a klaritromitsin in a blood plasma considerably decreases; with sertraline - theoretically it is impossible to exclude development of a serotoninovy syndrome; with theophylline - increase in concentration of theophylline in a blood plasma is possible.

At simultaneous use with terfenadiny delay of speed of metabolism of a terfenadin and increase in its concentration in a blood plasma is possible that can lead to increase in an interval of QT and increase in risk of development of ventricular arrhythmia like "pirouette".

Believe that at simultaneous use with Tolbutamidum there is a probability of development of a hypoglycemia.

At simultaneous use with Phenytoinum increase in concentration of Phenytoinum in a blood plasma, risk of development of toxic action is possible.

At simultaneous use with fluoxetine the case of development of the toxic effects caused by effect of fluoxetine is described.

Oppression of activity of an isoenzyme of CYP3A4 under the influence of a klaritromitsin leads to delay of speed of metabolism of a tsizaprid at their simultaneous use. Thereof concentration of a tsizaprid in a blood plasma increases and the risk of development of life-threatening disturbances of a cordial rhythm, including ventricular arrhythmias like "pirouette" increases.

At simultaneous use with cyclosporine concentration of cyclosporine in a blood plasma increases, there is a risk of strengthening of side effect.

At simultaneous use with ergotamine, dihydroergotamine cases of strengthening of side effect of ergotamine and dihydroergotamine are described.

Contraindications:

Heavy insufficiency of function of a liver, hepatitis (in the anamnesis), a porphyria, the I trimester of pregnancy, simultaneous use with terfenadiny, tsizapridy, astemizoly, Pimozidum, hypersensitivity to a klaritromitsin and other antibiotics of group of macroleads.

Use at pregnancy and feeding by a breast
Use in the I trimester of pregnancy is contraindicated.
Use in II and III trimesters of pregnancy is possible only when the estimated advantage for mother exceeds potential risk for a fruit.
In need of use in the period of a lactation it is necessary to stop breastfeeding.

Use at abnormal liver functions
It is contraindicated at heavy insufficiency of function of a liver, hepatitises (in the anamnesis).

Use at renal failures
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.

Use for children
Now there are not enough data on efficiency and safety of use of a klaritromitsin for children aged up to 6 months.

Overdose:

There are no data.

Storage conditions:

To store in the place, unavailable to children, at a temperature from 15 °C to 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets, покр. film cover, 250 mg: 14 pieces.

Tablets, покр. film cover, 500 mg: 14 pieces.