Claritrosin, tablets 500mg 5 pcs

Pharmgroup:

Macrolide antibiotic.

Pharmaceutical action:

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

. (Streptococcus pyogenes, Streptococcus viridans, Streptococcus pneumoniae), Haemophilus influenzae (parainfluenzae), Haemophilus ducreyi , Neisseria donorrhoeae, Neisseria meningitidis, Listeria monocytogenes, Legionella pneumophila, Mycoplasma pneumoniae, Helicobacter (Campilobacter) pylori, Campilobacter jejuni, Chamidia pneumoniae (trachomastis), Moraxella (Branhamella) catarrhalis, Bordetella pertussis, Propionibacterium acnes, Mycobacterium avium, Mycobacterium leprae, Staphylococcus aureus, Ureaplasma urealyticum, Toxoplasma gondii, Corynebacterium spp., Borrelia burgdorferi, Pasteurlla multocida, some anaerobes (Eubacterium spp., Peptococcus spp., Propionibacterium spp., Clostridium perfringens, Bacteroides melaninogenicus) and all mycobacteria except M. tuberculosis.

Pharmacokinetics:

Absorption is rapid. Food slows absorption without significantly affecting bioavailability. Bioavailability of 250 mg tablets is 50%, in the form of suspension is equivalent or slightly higher than when taken as tablets. The binding to plasma proteins is 65-75%. After a single use two Cmax peaks are registered.

The second peak is due to the ability of the drug to accumulate in the gallbladder followed by gradual or rapid entry into the intestine and absorption. TCmax when taking 250 mg is 2-3 h, for prolonged-acting LF it is 6 h.

After oral administration 20-30% of the accepted dose of clarithromycin is rapidly hydroxylated in the liver by cytochrome isoenzymes CYP3A4, CYP3A5 and CYP3A7 to form the main metabolite – 14 (R)-hydroxyclarithromycin, which has marked antimicrobial activity against Haemophilus influenzae. It is an inhibitor of CYP3A4, CYP3A5 and CYP3A7 isoenzymes.

When taking regularly 250 mg/day, Css of unchanged drug and its main metabolite are 1 and 0.6 mcg/ml, respectively; T1/2 is 3-4 and 5-6 hours, respectively. In dose increase up 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 and 6.9-8.7 h, respectively; for prolonged action LP (500 mg/day) – 5.3 and 7.7 h; 1000 mg/day – 5.8 and 8.9 h, respectively.

Therapeutic concentrations are accumulated in the lungs, skin and soft tissues (in which concentrations are 10 times higher than serum concentrations).

It is excreted by the kidneys and intestines (20-30% – in unchanged form, the rest – as metabolites). In a single administration of 250 and 1200 mg, 37.9 and 46% is excreted by the kidneys, and 40.2 and 29.1% by the intestine, respectively.
In CKD, TCmax, Cmax and AUC of clarithromycin and its metabolite are increased.

Indications

Claritrosin is indicated for treatment of infections caused by sensitive microorganisms. These diseases include:
– Lower respiratory tract infections (bronchitis, pneumonia).
– Upper respiratory tract infections (pharyngitis, sinusitis), otitis.
– Skin and soft tissue infections (folliculitis, boils).
– Disseminated 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 eradication of H.pylori and reduction of recurrence rate of duodenal ulcer.

Active ingredient

Composition

1 tablet:

– Clarithromycin 500 mg.

Auxiliary substances:

Cellulose microcrystalline,

polyvinylpyrrolidone (povidone),

dairy sugar (lactose),

p> potato starch,

aerosil (colloidal silicon dioxide),

magnesium stearate,

talc;

coating:

oxypropyl methylcellulose (hypromellose) or hydroxypropyl methylcellulose, titanium dioxide (titanium dioxide) polyethylene oxide 4000 (polyethylene glycol 4000), treopelin O.

How to take, the dosage

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

If necessary, 500 mg 2 times a day can be prescribed. Duration of treatment course is 6-14 days.

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

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

In patients with renal insufficiency, with creatinine clearance less than 30 ml/min, the dose of Claritrosin should be reduced by half. Maximum duration of the course in patients in this group should not exceed 14 days.

Interaction

Concomitant administration increases blood concentrations of drugs metabolized in the liver with the help of cytochrome P450 enzymes – indirect anticoagulants, carbamazepine, theophylline, astemizole, cisapride, terfenadine (2-3 times), triazolam, midazolam, cyclosporine, disopyramide, phenytoin, rifabutin, lovastatin, digoxin, ergot alkaloids and others.

Rare cases of acute skeletal muscle necrosis have been reported to coincide with concomitant administration of clarithromycin and the hydroxymethylglutaryl-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 derivatives) may lead to acute ergotomine intoxication manifested by severe peripheral vasospasm and perverse sensitization.
Simultaneous oral administration of zidovudine and clarithromycin tablets to HIV-infected adults may result in decreased equilibrium concentrations of zidovudine. Given that clarithromycin probably alters absorption of concomitantly administered oral zidovudine, this interaction is largely avoided when clarithromycin and zidovudine are taken at different hours 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 creatinine clearance between 30 and 60 ml/min, the clarithromycin dose should be reduced by 50%. If creatinine clearance is less than 30 ml/min. The clarithromycin dose should be reduced by 75%.

In concomitant treatment with ritonavir, clarithromycin should not be administered in doses greater than 1 g/day.

Special Instructions

Caution is advised when prescribing Claritrosin against drugs that are metabolized by the liver (it is recommended to measure their blood concentrations).

In case of co-administration of Claritrosin with warfarin or other indirect anticoagulants the prothrombin time must be monitored.

In a history of heart disease, concomitant use with terfenadine, cisapride, astemizole is not recommended.
Attention must be paid to the possibility of cross-resistance between clarithromycin and other antibiotics from the macrolide group, as well as lincomycin and clindamycin.

In prolonged or repeated use of Claritrosin it is possible to develop superinfection (growth of insensitive bacteria and fungi).

Contraindications

Clarithromycin is contraindicated in patients with hypersensitivity to macrolide antibiotics.
Do not prescribe ergot derivatives when treating with clarithromycin.

The treatment with clarithromycin should not take cisapride, pimozide, astemizole or terfenadine (see also section Interaction with other medicinal products).

Patients taking these drugs concomitantly with clarithromycin have increased blood concentrations. This may cause prolongation of the QT interval and development of cardiac arrhythmias, including ventricular paroxysmal tachycardia, ventricular fibrillation and ventricular flutter or fibrillation.
Severe liver function and/or renal impairment.

Side effects

Gastrointestinal complaints (nausea, dyspepsia, abdominal pain, vomiting, and diarrhea) are the most common. Pseudomembranous colitis has been reported to develop mild to life-threatening. Other adverse reactions include headaches, taste disorders, and a transient increase in liver enzyme activity. Rare cases of parasthesias have been reported.

There have been reports of rare cases of hepatitis with elevated blood levels of liver enzymes and the development of cholestasis and jaundice.

These liver damage has been severe in some cases and is usually reversible. In exceptional cases, hepatic failure with lethal outcome was observed.

There have been reports of rare cases of increased serum creatinine concentration, development of interstitial nephritis, and development of renal failure.

In case of oral clarithromycin administration allergic reactions have been observed, the intensity of which varied from urticaria and skin rash to anaphylaxis and Stevens-Johnson syndrome.

There have been reports of hearing loss during clarithromycin treatment, which in most cases recovered after Clarithrosine withdrawal. Changes in taste perception have also been reported, usually occurring in conjunction with impaired taste. Glossitis, stomatitis, oral candidiasis, and discoloration of the tongue during clarithromycin treatment have been reported. Tooth discoloration has also been reported in patients treated with clarithromycin. The discoloration of the teeth was in most cases reversible. Hypoglycemia has rarely been reported; in a number of these cases hypoglycemia has occurred in patients who received oral hypoglycemic agents or insulin during treatment with clarithromycin.
Individual cases of thrombocytopenia and leukopenia have been reported.

Transient central nervous system side effects have been observed with clarithromycin: dizziness, anxiety, fear, apprehension, insomnia, nightmares, tinnitus, confusion, disorientation, hallucinations, psychosis and depersonalization.

In treatment with clarithromycin, as with other macrolides, prolongation of the QT interval, ventricular arrhythmias, including ventricular paroxysmal tachycardia and ventricular flutter or fibrillation have been extremely rare.

Overdose

The development of gastrointestinal symptoms (nausea, vomiting, diarrhea); headache, confusion.

In case of overdose, immediate gastric lavage and symptomatic treatment are necessary. Hemodialysis and peritoneal dialysis do not significantly alter serum clarithromycin levels.

Similarities