KLAREKSID

Active material: Clarithromycin
When ATH: J01FA09
CCF: Macrolide antibiotics
When CSF: 06.07.01
Manufacturer: PLIVA HRVATSKA d.o.o. (Croatia)

Pharmaceutical form, composition and packaging

Pills, Film-coated white, oblong, lenticular.

Excipients: povidone, microcrystalline cellulose, Croscarmellose sodium, colloidal silicon dioxide, magnesium stearate.

The composition of the shell: опадрай II 31F58914 белый (gipromeloza, lactose monohydrate, Titanium dioxide (E171), macrogol 4000, sodium citrate).

10 PC. – blisters (1) – packs cardboard.
14 PC. – blisters (1) – packs cardboard.

Pills, Film-coated white, oblong, lenticular, with Valium on one side.

Excipients: povidone, microcrystalline cellulose, Croscarmellose sodium, colloidal silicon dioxide, magnesium stearate.

The composition of the shell: опадрай II 31F58914 белый (gipromeloza, lactose monohydrate, Titanium dioxide (E171), macrogol 4000, sodium citrate).

7 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (1) – packs cardboard.

DESCRIPTION OF ACTIVE SUBSTANCES

Pharmacological action

Semisynthetic macrolide antibiotics. It inhibits protein synthesis in the microbial cell, interacting with the 50S ribosomal subunit of bacteria. It operates mainly bacteriostatic, as well as bactericidal.

Active against 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.

It is also active against Toxoplasma gondii, Mycobacterium spp. (except Mycobacterium tuberculosis).

Pharmacokinetics

When administered clarithromycin is well absorbed from the gastrointestinal tract. Food intake delays absorption, but it does not affect the bioavailability of the active substance.

Clarithromycin penetrates well in biological fluids and tissues, where it reaches a concentration 10 times larger, than in plasma.

About 20% clarithromycin immediately metabolized to form the main metabolite 14-gidroklaritromitsina.

At a dose of 250 mg T_1/2 is 3-4 no, at a dose 500 mg – 5-7 no.

Return with urine unchanged and as metabolites.

Testimony

Treatment of infectious and inflammatory diseases, caused by susceptible pathogens clarithromycin: infections of the upper respiratory tract and ENT (tonzillofaringit, otitis media, ostryi sinusitis); infections of the lower respiratory tract (acute bronchitis, exacerbation of chronic bronchitis, community-acquired bacterial pneumonia and atypical); infections of skin and soft tissue; mycobacterial infection (M.avium complex, M.kansasii, M.marinum, M.leprae) and their prevention in AIDS patients; Helicobacter pylori eradication in patients with duodenal ulcer or stomach (Only a combination therapy).

Dosage regimen

Individual. When administered to adults and children over 12 s single dose of 0.25-1 g, frequency of administration 2 times / day.

For children, the daily dose is 15 mg / kg / day 2 admission.

The duration of treatment depends on the indication.

Patients with impaired renal function (CC less than 30 ml / min or serum creatinine 3.3 mg / dL) the dose should be reduced 2 times or double the interval between doses.

The maximum daily dose: for adults – 2 g, for children 1 g.

Side effect

From the digestive system: nausea, vomiting, diarrhea, abdominal pain, stomatitis, glossitis; rarely – psevdomembranoznыy colitis; in some cases – increase in liver enzymes, cholestatic jaundice.

CNS: dizziness, confusion, a sense of fear, insomnia; nightmares.

Allergic reactions: hives, anaphylactic reactions; in some cases – Stevens-Johnson syndrome.

Other: temporary changes in taste sensations.

Contraindications

Severe liver function impairment, hepatitis (history), porphyria, I trimester of pregnancy, simultaneous use with terfenadine, cizapridom, astemizolom, pimozidom, hypersensitivity to clarithromycin and other macrolide antibiotics.

Pregnancy and lactation

The use in the I trimester of pregnancy is contraindicated.

Application in II and III trimester of pregnancy is possible only in cases, when the intended benefits to the mother outweighs the potential risk to the fetus.

If necessary, use during lactation should stop breastfeeding.

Cautions

Between macrolide antibiotics observed cross-resistance.

Treatment with antibiotics alters the normal flora of the intestine, so it is possible the development of superinfection, caused by resistant microorganisms.

It will be appreciated, that severe persistent diarrhea may be due to the development of pseudomembranous colitis.

While the use of clarithromycin is recommended to monitor the plasma concentration of theophylline, karʙamazepina, digoksina, Lovastatin, simvastatin, triazolama, midazolama, phenytoin, Cyclosporine and alkaloids lpv.

Periodically monitor the prothrombin time in patients, receiving clarithromycin concurrently with warfarin or other oral anticoagulants.

Use in Pediatrics

Currently there is insufficient data on the efficacy and safety of clarithromycin in children under the age of 6 Months.

Drug Interactions

Clarithromycin oppressing activity izofermenta CYP3A4 , that leads to a slow metabolic rate astemizola when they are applying. As a consequence, increase the QT interval and increase the risk of ventricular arrhythmia types “pirouette”.

Together with the use of atorvastatin is appropriate moderately concentrations of atorvastatin in plasma, increased risk of myopathy.

If you are applying with warfarin may increase the antikoagulântnogo action of warfarin and increase the risk of bleeding.

Together with the use of Digoxin concentration possibly significant of Digoxin in the blood plasma and the risk of Glycoside intoxication.

It is believed, that may increase concentration in the blood plasma as a result dizopiramida inhibiting its metabolism in the liver under the influence of the ==. You run the risk of prolonging the QT interval, development of heart rhythm disorders types “pirouette”, increase insulin secretion and hypokalemia.

Together with the use of AZT a few reduced bioavailability of zidovudine; with itrakonazolom – significantly increases itrakonazola concentration in the blood plasma, believe, that there is a risk of amplifying side effects.

Together with the use of carbamazepine concentrations of carbamazepine in plasma, There is a risk of its side effects; with colchicine – cases of severe, life-threatening toxic reactions, colchicine-induced; with lanzoprazolom – possible Glossitis, stomatitis and/or appearance of dark coloring language; with methyl-prednisolone – reduced clearance of methylprednisolone; with midazolamom – Midazolam concentrations in plasma and amplified its effects.

Together with the use of omeprazole omeprazole concentration is greatly improved and slightly increases the concentration == in plasma.

If you are applying with pimozidom pimozida concentrations in plasma, There is a risk of severe cardiotoksicski action; with prednizonom – Describes the cases of acute mania and psychosis; with ritonavir – possibly significant increase of concentration of clarithromycin, However, this concentration of its metabolite 14-gidroksiklaritromicina significantly reduced; with rifabutinom – concentrations of rifabutin in plasma, increases the risk of uveitis, reduced the concentration == in plasma.

If you are applying with rifampicin decreases the concentration == in plasma; with sertralinom – Theoretically, one should not exclude the development of serotonin syndrome; theophylline – perhaps increasing the concentration of theophylline in plasma.

Together with the use of terfenadine possible slowing of metabolism terfenadine and increasing its concentration in the blood plasma, that could increase the QT interval and increase the risk of ventricular arrhythmia types “pirouette”.

It is believed, that, together with the use of tolbutamidom there is the likelihood of hypoglycemia.

Together with the use of phenytoin may increase concentration fenitoina plasma, the risk of toxicity.

Together with the use of fluoxetine case development of toxic effects, Fluoxetine-induced.

Oppression influenced izofermenta CYP3A4 activity == leads to slower speeds the metabolism of cisapride in their simultaneous use. As a consequence, increases the concentration of cisapride in plasma and increases the risk of life-threatening heart rhythm disorders, including jeludockove adults type “pirouette”.

At simultaneous application with cyclosporine increases the concentration of cyclosporine in the blood plasma, enhance the risk of side effects.

While the use of ergotamine, dihydroergotamine described cases increased side effects of ergotamine and dihydroergotamine.