clarithromycin | Claritrosin tablets 500mg 5 pcs

Release form

Tablets.

Pharmacological action

Farmgroup: antibiotic-macrolide.

Pharmaceutical action: Claritrosin is a second-generation macrolide bacteriostatic antibiotic from the broad-spectrum macrolide group. It disrupts the synthesis of protein of microorganisms (binds to the 50S subunit of the membrane of the ribosome of the microbial cell).

Active in relation to: Streptococcus agalactiae (Streptococcus pyogenes, Streptococcus viridans, Streptococcus pneumoniae), Haemophilus influenzae (parainfluenzae), Haemophilus ducreyi, Neisseria donorrheobilioeoplegloema Campina lerieriaephilioema Campina , Chamidia pneumoniae (trachomastis), Moraxella (Branhamella) catarrhalis, Bordetella pertussis, Propionibacterium acnes, Mycobacterium avium, Mycobacterium leprae, Staphylococcus aureus, Ureaplasma perfferma burgundum Peptococcus spp., Propionibacterium spp., Clostridium perfringens, Bacteroides melaninogenicus) and all mycobacteria except M. tuberculosis.

Pharmacokinetics: Absorption - Fast. Food slows down absorption, without significantly affecting bioavailability. The bioavailability of tablets 250 mg - 50%, in the form of a suspension is equivalent to or slightly higher than when taken in tablet form. Communication with plasma proteins - 65-75%. After a single dose, 2 peaks of Cmax are recorded. The second peak is due to the ability of the drug to accumulate in the gall bladder, followed by a gradual or rapid entry into the intestine and absorption. TCmax when taking 250 mg - 2-3 hours, for sustained release LF - 6 hours.

After oral administration, 20-30% of the dose taken, clarithromycin is rapidly hydroxylated in the liver with isoenzymes of cytochrome CYP3A4, CYP3A5 and CYP3A7 with the formation of the main metabolite - 14 (R ) -hydroxyclarithromycin with pronounced antimicrobial activity against Haemophilus influenzae. It is an inhibitor of isoenzymes CYP3A4, CYP3A5 and CYP3A7.

With regular intake of 250 mg / day, the Css of the unchanged drug and its main metabolite are 1 and 0.6 μg / ml, respectively, T1 / 2 - 3-4 and 5-6 hours, respectively. With an increase in dose to 500 mg / day, Css of unchanged drug and its metabolite in plasma is 2.7-2.9 and 0. 83-0.88 μg / ml, respectively, T1 / 2 - 4.8-5 and 6.9-8.7 hours, respectively, for sustained release drugs (500 mg / day) - 5.3 and 7.7 hours, 1000 mg / day - 5.8 and 8.9 hours, respectively. At therapeutic concentrations, it accumulates in the lungs, skin, and soft tissues (in them, concentrations are 10 times higher than serum).

It is excreted by the kidneys and intestines (20-30% - in unchanged form, the rest - in the form of metabolites). With a single dose of 250 and 1200 mg, 37.9 and 46% are excreted by the kidneys, 40.2 and 29.1%, respectively, by the intestines.

In chronic renal failure, TCmax, Cmax, and AUC of clarithromycin and its metabolite increase.

Indications

Claritrosin is indicated for the treatment of infectious diseases caused by susceptible microorganisms. These diseases include: - Infections of the lower respiratory tract (bronchitis, pneumonia).

- Upper respiratory tract infections (pharyngitis, sinusitis), otitis media.

- Infections of the skin and soft tissues (folliculitis, erysipelas).

- Common or localized mycobacterial infections caused by Mycobacterium avium and Mycobacterium intracellulare.

Localized infections caused by Mycobacterium chelonae, Mycobacterium fortuitum and Mycobacterium kansasii.

Claritrosin is indicated for the elimination of H. pylori and a decrease in the frequency of relapse of a duodenal ulcer.

Contraindications

Clarithromycin is contraindicated in patients with hypersensitivity to macrolide antibiotics.

Do not prescribe ergot derivatives for clarithromycin.

When treating with clarithromycin, it is forbidden to take cisapride, pimozide, astemizole and terfenadine (see also the section Interaction with other medicines).

In patients taking these drugs simultaneously with clarithromycin, there is an increase in their concentration in the blood. In this case, prolongation of the QT interval and the development of cardiac arrhythmias are possible, including ventricular paroxysmal tachycardia, ventricular fibrillation, and ventricular flutter or fibrillation.

Severe impairment of liver and / or kidney function.

Use during pregnancy and lactation

Pregnancy and lactation

Use of the drug Claritrosin during pregnancy and lactation is possible only if the expected benefit to the mother outweighs the potential risk to the fetus.

Clarithromycin is excreted in breast milk, so if you need to prescribe the drug Claritrosin during lactation, you should stop breastfeeding.

Special instructions

In the presence of chronic liver diseases, regular monitoring of serum enzymes is necessary.

Claritrosin is prescribed with caution against drugs metabolized by the liver (it is recommended to measure their concentration in the blood).

In the case of co-administration of Claritrosin with warfarin or other indirect anticoagulants, it is necessary to control prothrombin time.

With a history of heart disease, simultaneous administration with terfenadine, cisapride, astemizole is not recommended.

It is necessary to pay attention to the possibility of cross-resistance between clarithromycin and other macrolide antibiotics, as well as lincomycin and clindamycin.

With prolonged or repeated use of the drug Claritrosin, superinfection may develop (the growth of insensitive bacteria and fungi).

Composition

1 tablet: - Clarithromycin 500 mg.

Excipients: microcrystalline cellulose, polyvinylpyrrolidone (povidone), milk sugar (lactose), potato starch, aerosil (colloidal silicon dioxide), magnesium stearate, talc shell: hydroxypropylmethyl cellulose (hypromellose) or hydroxypropyltropylene (4,200) polyethylene glycol 4000), threopelin O.

Dosing and Administration

For adults, the average oral dose is 250 mg of Claritrosin 2 times / day.

If necessary, 500 mg 2 times / day can be prescribed. The duration of treatment is 6-14 days.

For children, the drug is prescribed at a dose of 7.5 mg / kg body weight / day. The maximum daily dose is 500 mg. The duration of treatment is 7-10 days.

For the treatment of infections caused by Mycobacterium avium, Clarithromycin is prescribed orally - 1 g 2 times / day. The duration of treatment may be 6 months or more.

In patients with renal failure, with creatinine clearance less than 30 ml / min, the dose of Claritrosin should be reduced by 2 times. The maximum duration of the course in patients of this group should be no more than 14 days.

Drug interaction

With a simultaneous administration, it increases the concentration in the blood of drugs metabolized in the liver by cytochrome P450 enzymes - indirect anticoagulants, carbamazepine, theophylline, astemizole, cisapride, terfenadine (2-3 times), triazolam, cyclazospam, m-cycle, disopyramide, phenytoin, rifabutin, lovastatin, digoxin, ergot alkaloids, etc.

Rare cases of acute skeletal muscle necrosis have been reported, coinciding in time with the simultaneous administration of clarithromycin and hydroxymethylglutaryl inhibitors - CoA reductase - lovastatin and simvastatin.

There are reports of an increase in the concentration of digoxin in the plasma of patients receiving both digoxin and clarithromycin tablets. In such patients, it is necessary to constantly monitor the content of digoxin in the serum in order to avoid digital intoxication.

Clarithromycin can reduce the clearance of triazolam and, thus, increase its pharmacological effects with the development of drowsiness and confusion.

The simultaneous use of clarithromycin and ergotamine (ergot derivatives) can lead to acute ergotomin intoxication, manifested by severe peripheral vasospasm and perverse sensitivity.

Co-administration of zidovudine orally with adult HIV-infected patients and clarithromycin tablets may decrease the equilibrium concentrations of zidovudine. Considering that clarithromycin probably alters the absorption of orally administered zidovudine, this interaction is largely avoided when taking clarithromycin and zidovudine at different hours of the day (with an interval of at least 4 hours).

With the simultaneous administration of clarithromycin and ritonavir, serum concentrations of clarithromycin increase. Dose adjustment of clarithromycin in these cases is not required for patients with normal renal function. However, in patients with creatinine clearance from 30 to 60 ml / min. the dose of clarithromycin should be reduced by 50%. With creatinine clearance less than 30 ml / min. The dose of clarithromycin should be reduced by 75%.

With simultaneous treatment with ritonavir, clarithromycin should not be prescribed in doses above 1 g / day.

Overdose of

Gastrointestinal symptoms likely to develop (nausea, vomiting, diarrhea) headache, confusion.

In case of overdose, immediate gastric lavage and symptomatic treatment are necessary. Hemodialysis and peritoneal dialysis do not lead to a significant change in the level of clarithromycin in blood serum.

Daily uyuschee substances

clarithromycin

Terms and conditions

prescription

Dosage form

tablets

Appointment

Adult on doctor's appointment, Children on doctor's appointment

Indications

From tonsillitis, From respiratory tract infections, From angina, From gastric and 12-duodenal ulcer, Cold, From otcut sinusitis, Bronchitis, Ot arynhyta, Here kozhy infections, gastrointestinal tract infections Here, v zvann h Helykobakter bench

Synthesis, Russian