Clarbact, 500 mg 10 pcs

A second-generation macrolide group antibiotic with a broad spectrum of antimicrobial action. It has bacteriostatic action. It disrupts protein synthesis of microorganisms – it binds to 50S subunit of the ribosome membrane of the microbial cell.

Clarithromycin is active against Streptococcus agalactiae (Streptococcus pyogenes, Streptococcus viridans, Streptococcus pneumoniae), Haemophilus influenzae (parainfluenzae), Haemophilus ducreyi, Neisseria gonorrhoeae, Neisseria meningitidis, Listeria monocytogenes, Legionella pneumophila, Mycoplasma pneumoniae, Helicobacter (Campilobacter) pylori, Campilobacter jejuni, Chlamidia pneumoniae (trachomatis), Moraxella (Branhamella) catarrhalis, Bordetella pertussis, Propionibacterium acnes, Staphylococcus aureus, Ureaplasma urealyticum, Toxoplasma gondii, Corynebacterium spp., Borrelia burgdorferi, Pasteurella multocida, some anaerobes (Eubacterium spp., Peptococcus spp., Propionibacterium spp., Clostridium perfringens, Bacteroides melaninogenicus) and all mycobacteria (including Mycobacterium avium, Mycobacterium leprae) except Mycobacterium tuberculosis.

Pharmacokinetics

Intake

After oral administration, absorption is rapid. Food slows absorption without significantly affecting bioavailability. The bioavailability of clarithromycin in suspension form is equivalent or slightly higher than when taken as tablets.

Two Cmax peaks are recorded after a single dose. The second peak is due to the ability of the drug to concentrate in the gallbladder with subsequent gradual or rapid release. Time to reach Cmax when administered orally in a dose of 250 mg is 1-3 hours.

Distribution and metabolism

The binding to plasma proteins is more than 90%.

After oral administration 20% of the taken dose is quickly hydroxylated in the liver with the participation of cytochrome P450 isoenzymes to form the main metabolite – 14-hydroxyclarithromycin, which has strong antimicrobial activity against Haemophilus influenzae.

In regular administration of 250 mg/day the Css of unchanged drug and its main metabolite are 1 and 0.6 mcg/ml, respectively; T1/2 is 3-4 h and 5-6 h, respectively. When increasing the 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 is 4.8-5 h and 6.9-8.7 h, respectively. In therapeutic concentrations it accumulates in the lungs, skin and soft tissues (concentrations in them are 10 times higher than in blood serum).

Extracted by the kidneys and in the feces (20-30% – unchanged, the rest – as metabolites). With a single use in doses of 250 mg and 1.2 g, 37.9% and 46% were excreted in the urine, 40.2% and 29.1% in the faeces, respectively.

Indications

The treatment of infectious diseases caused by microorganisms sensitive to the drug:

Active ingredient

Composition

How to take, the dosage

The drug is taken orally.

In adults, the average dose is 250 mg 2 times a day. If necessary, 500 mg 2 times a day may be prescribed. Duration of treatment is 6-14 days.

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

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

In patients with renal insufficiency (CKD less than 30 ml/min) the drug dose should be reduced by half. The maximum duration of treatment in patients in this group is 14 days.

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Interaction

Concomitant use of clarithromycin increases blood concentrations of drugs that are metabolized in the liver with participation of cytochrome P450 isoenzymes: indirect anticoagulants, carbamazepine, theophylline, triazolam, midazolam, cyclosporine, disopyramide, phenytoin, rifabutin, lovastatin, digoxin, ergot alkaloids.

When used concomitantly with clarithromycin, there is a significant increase in plasma concentrations of cisapride, pimozide, astemizole and terfenadine (2-3 times), with possible prolongation of QT interval and development of cardiac arrhythmias, including ventricular paroxysmal tachycardia, ventricular fibrillation and ventricular flutter or fibrillation (this combination is contraindicated).

Rare cases of acute skeletal muscle necrosis have been reported to coincide with concomitant administration of clarithromycin and the HMG-CoA reductase inhibitors lovastatin and simvastatin.

There have been reports of increased plasma concentrations of digoxin in patients receiving concomitant digoxin and clarithromycin tablets. In these patients, serum digoxin levels should be monitored continuously to avoid digitalis intoxication.

Clarithromycin may decrease clearance of triazolam and thus increase its pharmacological effects with development of somnolence and confusion.

The concomitant use of clarithromycin and ergotamine (ergot alkaloids) may lead to acute ergotamine intoxication with severe peripheral vasospasm and impaired sensitivity.

The concomitant administration of oral zidovudine and clarithromycin tablets to HIV-infected adults may result in decreased Css of zidovudine. Given that clarithromycin likely alters absorption of concomitant oral zidovudine, this interaction is largely avoided when clarithromycin and zidovudine are taken at different times of the day (at least 4 hours apart).

The concomitant administration of clarithromycin and ritonavir increases serum concentrations of clarithromycin. No clarithromycin dose adjustment is required in these cases in patients with normal renal function. However, in patients with a creatinine clearance of 30 to 60 ml/min, the clarithromycin dose should be reduced by 50%. If CKR is less than 30 ml/min, the clarithromycin dose should be reduced by 75%. Clarithromycin doses greater than 1 g/day should not be administered concomitantly with ritonavir.

Special Instructions

In the presence of chronic liver disease, regular monitoring of liver enzymes activity is necessary.

With caution, use with the administration of drugs that are metabolized in the liver; it is recommended to determine their plasma concentrations.

Protrombin time should be controlled when combined with warfarin or other indirect anticoagulants.

In case of a history of heart disease, concomitant use with terfenadine, cisapride, astemizole is not recommended.

Possible cross-resistance between clarithromycin and other antibiotics from the macrolide group as well as lincomycin and clindamycin should be noted.

Long-term or repeated use of the drug may lead to superinfection (growth of insensitive bacteria and fungi).

Contraindications

Side effects

Digestive system disorders: most common – nausea, dyspepsia, abdominal pain, vomiting and diarrhea; pseudomembranous colitis (moderate to life-threatening), taste disorders and transient increase in liver enzyme activity, glossitis, stomatitis, candidiasis of the oral mucosa, color changes in the tongue during clarithromycin treatment, tooth discoloration (in most cases reversible) are possible; rarely – hepatitis with increased liver enzymes in the blood, development of cholestasis and jaundice (these liver damage in some cases were severe and usually reversible); in single cases – liver failure with lethal outcome.

CNS and peripheral nervous system disorders: transient headache, dizziness, anxiety, fear, apprehension, insomnia, nightmares, tinnitus, confusion, disorientation, hallucinations, psychosis and depersonalization are possible; paresthesias are rare.

Sensory organs: there may be hearing loss (recovered after discontinuation of the drug), changes in taste perception, usually occurring together with taste disorder.

Cardiovascular system: rarely – prolongation of the QT interval, ventricular arrhythmia (including ventricular paroxysmal tachycardia, ventricular flutter or fibrillation).

Urinary system disorders: rarely – increase in serum creatinine, interstitial nephritis, renal failure.

Hematopoietic system: in rare cases – thrombocytopenia, leukopenia.

Allergic reactions: with oral administration urticaria, skin rash, anaphylactic reactions, Stevens-Johnson syndrome are possible.

Others: rare – hypoglycemia (in some cases with concomitant use of oral hypoglycemic agents or insulin).

Overdose

Symptoms: nausea, vomiting, diarrhea, headache, confusion.

Treatment: immediate gastric lavage and symptomatic treatment are necessary. Hemodialysis and peritoneal dialysis do not significantly alter serum clarithromycin levels.

Pregnancy use

Pregnancy and lactation

The safety of clarithromycin in pregnancy and lactation has not been established.

Therefore, in pregnancy Claribact is only prescribed if there is no alternative therapy and if the expected benefits exceed the possible risk to the fetus.

Clarithromycin is excreted with breast milk, so caution should be exercised when using the drug during lactation.

Per pediatric use

The drug is indicated in the dose of 7.5 mg/kg body weight per day in children. Maximum daily dose is 500 mg. The duration of treatment is 7-10 days.

Similarities