Clarbact, pills 500 mg, 10 pcs.

Composition

Each coated tablet contains:

• Active ingredient: Clarithromycin-500 mg.
• Excipients: microcrystalline cellulose, corn starch, pregelatinated starch, polyvinylpyrrolidone, purified talc, sodium starch glycolate, colloidal silicon dioxide, stearic acid, magnesium stearate.
• Shell composition: isopropyl alcohol, hydroxypropylmethylcellulose, titanium dioxide, purified talc, polyethylene glycol 6000, methylene chloride, lemon flavor, peppermint powder.

Pharmacological action

An antibiotic of the second generation macrolide group with a broad spectrum of antimicrobial action. It has a bacteriostatic effect. Disrupts microbial protein synthesis by binding to the 50S subunit of the microbial cell ribosome membrane.

Clarithromycin Active against Streptococcus agalactiae (Streptococcus pyogenes, Streptococcus viridans, Sreptococcus 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, 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

Suction

 After oral administration, absorption is rapid. Food slows down absorption without significantly affecting bioavailability. The bioavailability of clarithromycin in suspension is equivalent to or slightly higher than that of tablets.

After a single dose,2 Cmax peaks are recorded. The second peak is due to the ability of the drug to concentrate in the gallbladder, followed by a gradual or rapid release. The time to reach Cmax when taken orally at a dose of 250 mg is 1-3 hours.

Distribution and metabolism

Binding to plasma proteins is more than 90%.

After oral administration,20% of the dose taken is rapidly hydroxylated in the liver with the participation of cytochrome P 450 isoenzymes to form the main metabolite – 14-hydroxyclarithromycin, which has a pronounced antimicrobial activity against Haemophilus influenzae.

With regular intake of 250 mg/day, the Css of the unchanged drug and its main metabolite is 1 and 0.6 mcg / ml, respectively; T1 / 2 is 3-4 hours and 5-6 hours, respectively. When the dose is increased to 500 mg/day, the Css of the unchanged drug and its metabolite in plasma is 2.7-2.9 and 0.83-0.88 mcg / ml, respectively; T1/2 – 4.8-5 hours and 6.9-8.7 hours, respectively. In therapeutic concentrations, it accumulates in the lungs, skin, and soft tissues (where concentrations are 10 times higher than the level in the blood serum).

Deduction

It is excreted by the kidneys and feces (20-30% – unchanged, the rest-in the form of metabolites). With a single dose of 250 mg and 1.2 g,37.9 and 46% are excreted in the urine, with fecal masses-40.2 and 29.1%, respectively.

Indications

Treatment of infectious diseases caused by drug-sensitive microorganisms:

• infections of the lower respiratory tract (bronchitis, pneumonia);
• infections of the upper respiratory tract (pharyngitis, sinusitis);
• ear infections;
• infections of 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;
• for Helicobacter pylori eradication and reduction of recurrence of duodenal ulcer.

Use during pregnancy and lactation

 Use during pregnancy and lactation

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

Therefore, during pregnancy, Klarbact is prescribed only in the absence of alternative therapy, if the intended benefit exceeds the possible risk to the fetus.

Clarithromycin is excreted in breast milk, so the drug should be used with caution during lactation.

 Use in children

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

Contraindications

• severe hepatic impairment;
• severe renal impairment;
• concomitant use of ergot alkaloids;
• concomitant use of cisapride, pimozide, astemizole, terfenadine;
• hypersensitivity to macrolide antibiotics.

Side effects

From the digestive system: most often – nausea, dyspepsia, abdominal pain, vomiting and diarrhea; possible pseudomembranous colitis (moderate to life – threatening), taste disorders and transient increase in liver enzyme activity, glossitis, stomatitis, candidiasis of the oral mucosa, discoloration of the tongue during treatment with clarithromycin, discoloration of teeth (in most cases reversible); rarely – hepatitis with increased liver enzymes in the blood, the development of cholestasis and jaundice (these liver injuries in some cases were severe and usually reversible); in some cases, hepatic failure with a fatal outcome.

 From the central nervous system and peripheral nervous system: possible transient headache, dizziness, anxiety, fear, fear, insomnia, nightmares, tinnitus, confusion, disorientation, hallucinations, psychosis and depersonalization; rarely-paresthesia.

From the sensory organs: possible hearing loss (recovers after discontinuation of the drug), changes in taste perception, usually occurring together with a violation of taste.

From the cardiovascular system: rarely-increased QT interval, ventricular arrhythmia (including ventricular paroxysmal tachycardia, fluttering or flickering of the ventricles).

From the urinary system: rarely-increased serum creatinine, interstitial nephritis, renal failure.

From the hematopoietic system: in some cases – thrombocytopenia, leukopenia.

Allergic reactions: urticaria, skin rash, anaphylactic reactions, Stevens-Johnson syndrome are possible when ingested.

Other: rarely-hypoglycemia (in some cases with simultaneous administration of oral hypoglycemic agents or insulin).

Interaction

 When used concomitantly, clarithromycin increases the blood concentration of drugs metabolized in the liver with the participation of cytochrome P 450 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 the concentration of cisapride, pimozide, astemizole and terfenadine (2-3 times) in blood plasma, while prolongation of the QT interval and the development of cardiac arrhythmias, including ventricular paroxysmal tachycardia, ventricular fibrillation and flutter or ventricular fibrillation (this combination is contraindicated).

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

There have been reports of increased plasma digoxin concentrations in patients receiving concomitant digoxin and clarithromycin tablets. In such patients, it is necessary to constantly monitor the content of digoxin in the serum in order to avoid digitalis intoxication.

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

Concomitant use of clarithromycin and ergotamine (ergot alkaloids) can lead to acute ergotamine intoxication, which is manifested by severe peripheral vasospasm and impaired sensitivity.

Concomitant administration of oral zidovudine and clarithromycin tablets to HIV-infected adults may lead to a decrease in zidovudine Css. Given that clarithromycin is likely to alter the absorption of concomitantly administered zidovudine, this interaction is largely avoided when taking clarithromycin and zidovudine at different times of the day (with an interval of at least 4 hours).

Concomitant administration of clarithromycin and ritonavir increases the serum concentration of clarithromycin. Clarithromycin dose adjustment is not required in these cases for patients with normal renal function. However, in patients with creatinine clearance between 30 and 60 ml/min, the dose of clarithromycin should be reduced by 50%. If creatinine clearance is less than 30 ml/min, the dose of clarithromycin should be reduced by 75%. Concomitant treatment with ritonavir should not be administered clarithromycin in doses greater than 1 g/day.

How to take it, course of administration and dosage

 The drug is taken orally.

For adults, the average dose is 250 mg 2 times / day. If necessary, you can prescribe 500 mg 2 times a day. The duration of treatment is 6-14 days.

Children are prescribed the drug at a dose of 7.5 mg / kg of body weight per 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, the drug is prescribed orally for 1 g 2 times a day.The duration of treatment may be 6 months or more.

In patients with renal insufficiency (creatinine clearance less than 30 ml/min), the dose of the drug should be reduced by 2 times. The maximum duration of treatment in patients of this group is 14 days.

Overdose

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

Treatment: Immediate gastric lavage and symptomatic treatment are necessary. Hemodialysis and peritoneal dialysis do not significantly change the level of clarithromycin in the blood serum.

Special instructions

 In the presence of chronic liver diseases, it is necessary to regularly monitor the activity of liver enzymes.

Use caution when taking drugs that are metabolized in the liver; it is recommended to determine their concentration in blood plasma.

When co-administered with warfarin or other indirect anticoagulants, prothrombin time should be monitored.

Concomitant use with terfenadine, cisapride, or astemizole is not recommended for patients with a history of heart disease.

Attention should be paid 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, superinfection may develop (the growth of insensitive bacteria and fungi).

Form of production

Klarbakt tablets.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Clarithromycin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Pregnant women as prescribed by a doctor, Adults as prescribed by a doctor, Children over 12 years of age, Children as prescribed by a doctor

Indications

Sore Throat, Skin Infections, Otitis Media, Respiratory Tract Infections, Bronchitis, Colds, Stomach and Duodenal Ulcers, Tonsillitis

Weight

Weight: 16 gr.