Producer: CJSC Verteks Russia
Code of automatic telephone exchange: J01FA09
Release form: Firm dosage forms. Capsules.
General characteristics. Structure:
Active ingredient: 250 mg of a klaritromitsin.
Excipients: sugar milk, starch corn, polyvinylpirrolidone, sodium lauryl sulfate, calcium октадеканоат. Gelatinous solid capsules: gelatin, water, sodium lauryl sulfate, methylparaben, propylparaben, titanium dioxide.
Makrolidny bacteriostatic antibiotic of a broad spectrum of activity.
Pharmacodynamics. The Makrolidny bacteriostatic antibiotic of the second generation from group of macroleads of a broad spectrum of activity. Breaks synthesis of protein of microorganisms (connecting 50S subunit of a membrane of ribosomes of a microbic cell). It is active in the relation: Streptococcus agalactiae (Staphylococcus pyogenes, Staphylococcus viridans, Staphylococcus pneumoniae), Haemophilus influenzae (parainfluenzae), Haemophilus ducreyi, Neisseria gonorrhoeae, Neisseria meningitidis, Listeria monocytogenes, Legionella pneumophila, Mycoplasma pneumoniae, Helicobacter (Campylobacter) pylori, Campylobacter jejuni, Chlamidia pneumoniae (trachomatis), Moraxella (Branhamella) catarrhalis, Bordetella pertussis, Propionibacterium acnes, Mycobacterium avium, Mycobacterium leprae, Staphylococcus aureus, Ureaplasma urealyticum, Toxoplasma gondii, Corynebacterium spp., Borrelia burgdorferi, Pasteurella multocida, some anaerobe bacterias (Eubacterium spp., Peptococcus spp., Propionibacterium spp., Clostridium perfringens, Bacteroides melaninogenicus) and mycobacteria, except M. Tuberculosis.
Pharmacokinetics. Absorption is bystry. Food slows down absorption, significantly without influencing bioavailability. Bioavailability of a klaritromitsin in the form of suspension is equivalent or is slightly higher, than at reception in the form of tablets. Communication with proteins of plasma — more than 90%. After a single dose 2 peaks of the maximum concentration are registered. The second peak is caused by ability of drug to concentrate in a gall bladder with the subsequent gradual or bystry release. Time of achievement of the maximum concentration at oral administration of 250 mg — 1-3 h.
After intake of 20% of the accepted dose quickly it is hydroxylated in a liver by P450 cytochrome enzymes with formation of the main metabolite — a 14-gidroksiklaritromitsin having the expressed antimicrobic activity concerning Haemophilus influenzae.
At regular reception on 250 mg/days equilibrium concentration of not changed drug and its main metabolite — 1 and 0,6 mkg/ml, respectively; an elimination half-life — 3-4 h and 5-6 h, respectively. At increase in a dose up to 500 mg/days equilibrium concentration of not changed drug and its metabolite in plasma — 2,7-2,9 and 0,83-0,88 mkg/ml, respectively; an elimination half-life — 4,8-5 h and 6,9-8,7 h, respectively. In therapeutic concentration collects in lungs, skin and soft tissues (in them concentration by 10 times exceed level in blood serum).
It is allocated with kidneys and with a fecal masses (20-30% — in not changed form, the rest — in the form of metabolites). At a single dose of 250 mg and 1,2 g kidneys allocate 37,9 and 46%, with a fecal masses — 40,2 and 29,1%, respectively.
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), otitises.
Infections of skin and soft tissues (folliculites, 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 is shown for elimination of H. pylori and decrease in frequency of a recurrence of an ulcer of a duodenum.
Route of administration and doses:
For adults the average dose for intake makes 250 mg of 2 times/days. If necessary it is possible to appoint 500 mg of 2 times/days. Duration of a course of treatment — 6-14 days.
To children drug appoint 7,5 mg/kg of mass of bodies/days in a dose. The maximum daily dose — 500 mg. Duration of a course of treatment — 7-10 days.
For treatment of the infections caused by Mycobacterium avium кларитромицин appoint inside — 1 g 2 times/days. Duration of treatment can make 6 months and more.
At patients with a renal failure, at clearance of creatinine less than 30 ml/min., a dose of drug should be lowered twice. The maximum duration of a course at patients of this group has to make no more than 14 days.
Features of use:
In the presence of chronic diseases of a liver it is necessary to carry out regular control of enzymes of blood serum.
With care appoint against the background of the drugs which are metabolized a liver (it is recommended to measure their concentration in blood).
In case of joint appointment with warfarin or other indirect anticoagulants it is necessary to control a prothrombin time.
At heart diseases in the anamnesis the concomitant use with terfenadiny, tsizapridy, astemizoly is not recommended.
It is necessary to pay attention to a possibility of cross stability between klaritromitsiny and other antibiotics from group of macroleads, and also lincomycin and clindamycin.
At prolonged or repeated use of drug development of superinfection (growth of insensitive bacteria and mushrooms) is possible.
Use at pregnancy and a lactation. Safety of a klaritromitsin during pregnancy and feeding by a breast is not established. Therefore during pregnancy кларитромицин appoint only in case of lack of alternative therapy if the estimated advantage exceeds possible risk for a fruit.
Klaritromitsin gets into breast milk therefore in need of purpose of drug in the period of a lactation it is necessary to stop breastfeeding.
Complaints from digestive tract (nausea, dyspepsia, abdominal pains, vomiting and diarrhea) are most often noted. There are messages on development of pseudomembranous colitis from an average to life-threatening. Headaches, disturbances of taste and passing increase in activity of enzymes of a liver belong to other side reactions.
There are messages on exceptional cases of development of a parasthesia.
There are messages on exceptional cases of hepatitis with increase in level of enzymes of a liver in blood 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.
There are messages on exceptional cases of increase in concentration of creatinine in serum, development of intersticial nephrites, development of a renal failure.
There are messages on a hearing loss during treatment klaritromitsiny which was in most cases recovered after drug withdrawal. Also it is reported about taste perception changes, as a rule, arising together with taste disturbance.
There are messages on development of glossites, stomatitises, 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 hypoglycemia developed at the patients accepting during treatment klaritromitsiny hypoglycemic means for oral administration or insulin.
At reception of a klaritromitsin tranzitorny side effect on the central nervous system was observed: dizziness, alarm, fear, fear, sleeplessness, nightmares, sonitus, confusion of consciousness, disorientation, hallucinations, psychoses and depersonalization.
At treatment klaritromitsiny, as well as when using other macroleads, lengthening an interval of QT, ventricular arrhythmia, including a ventricular Bouveret's disease and trembling or ventricular fibrillation was extremely seldom observed.
Interaction with other medicines:
At a concomitant use increases concentration in blood of the drugs which are metabolized in a liver by means of enzymes of P450 cytochrome, indirect anticoagulants, carbamazepine, theophylline, an astemizol, tsizaprid, terfenadin (by 2-3 times), a triazolama, midazolam, cyclosporine, Disopyramidum, Phenytoinum, a rifabutin, a lovastatin, digoxin, ergot alkaloids, etc.
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.
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 (ergot derivatives) can lead to the acute ergotominovy intoxication which is shown a heavy peripheral vasospasm 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 (with an interval not less than 4 hours).
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 at patients with clearance of creatinine 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.
Klaritromitsin is contraindicated to patients with hypersensitivity to antibiotics from group of macroleads.
At treatment klaritromitsiny not to appoint ergot derivatives.
At treatment klaritromitsiny it is forbidden to accept цизаприд, Pimozidum, астемизол and терфенадин (see also section Interaction with other medicines). At the patients accepting these drugs along with klaritromitsiny increase in their concentration in blood is noted. At the same time lengthening of an interval of QT and development of cardiac arrhythmias, including a ventricular Bouveret's disease, fibrillation of ventricles and trembling or ventricular fibrillation is possible.
Heavy abnormal liver functions and/or kidneys.
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.
List B. In dry, protected from light, the place, unavailable to children, at a temperature not over 25 ºС. Period of validity 2 years. Not to use after expiry date.
According to the recipe
Capsules on 250 mg. On 7 capsules in a blister strip packaging. On 14 capsules in bank polymeric. Two planimetric packagings or to one bank together with the application instruction in a pack from a cardboard.