Clarithromycin-OBL, pills 500 mg 14 pcs.

Composition

1 coated tablet contains:

Active ingredient:

clarithromycin 500 mg,

excipients:

croscarmellose sodium,

sodium lauryl sulfate,

microcrystalline cellulose,

povidone (polyvinylpyrrolidone low molecular weight medical),

magnesium stearate,

colloidal silicon dioxide (aerosil),

hypromellose (hydroxypropylmethylcellulose),

macrogol (polyethylene glycol 6000),

titanium dioxide,

hyprolose (hydroxypropylcellulose),

quinoline yellow dye,

vanillin.

Pharmacological action

Pharmacotherapeutic group:

antibiotic, macrolide.

Pharmacodynamics:

Clarithromycin is a second-generation bacteriostatic broad-spectrum macrolide antibiotic. Disrupts microbial protein synthesis (binds to the 50S subunit of the microbial cell ribosome membrane). It acts on extracellularly and intracellularly located pathogens. Active in relation to:

Streptococcus agalactiae (Streptococcus pyogenes, Streptococcus viridans, Streptococcus pneumoniae), Haemophilus influenzae (parainfluenzae), Haemophilus ducreyi, Neisseria gonorrhoeae, Neisseria meningitidis, Listeria monocytogenes, Legionella pneumophila, Mycoplasma pneumoniae, Helicobacter pylori (CamPylobacter), CamPylobacter jejuni, Chlamidia pneumoniae, Moraxella catarrhalis, Bordetella pertussis, Propionibacterium acne, Mycobacterium avium, Mycobacterium leprae, Mycobacterium kansasii, Mycobacterium marinom, Staphylococcus aureus, Ureaplasma urealyticum, Toxoplasma gondii, Corynebacterium spp., Borrelia burgdorferi, Pasteurella multocida, some anaerobes (Eubacterium spp., Peptococcus spp., Propionibacterium spp., Clostridium perfringens, Bacteroides melaninogenicus), less than Active against Mycobacterium tuberculosis.

Pharmacokinetics:

Absorption is fast. Food slows down absorption without significantly affecting bioavailability. Binding to plasma proteins is more than 90%. After a single dose,2 peaks of the maximum concentration of the drug in the blood plasma are recorded.

The second peak is due to the ability of the drug to concentrate in the gallbladder, followed by gradual or rapid entry into the intestine and absorption. The time to reach the maximum concentration of the drug in blood plasma with oral administration of 250 mg is 1-3 hours.

After oral administration,20% of the dose taken is rapidly hydroxylated in the liver by cytochrome CYP3A4, CYP3A5, and CYP3A7 enzymes to form the main metabolite,14-hydroxyclarithromycin, which has pronounced antimicrobial activity against Haemophilus influenzae.

It is an inhibitor of the isoenzymes CYP3A4, CYP3A5 and CYP3A7.

With regular intake of 250 mg/day, the steady-state concentrations of the unchanged drug and its main metabolite are 1 and 0.6 mcg / ml, respectively; the half-life is 3-4 hours and 5-6 hours, respectively. When the dose is increased to 500 mg / day, the steady-state plasma concentrations of the unchanged drug and its metabolite are 2.7-2.9 and 0.83-0.88 mcg / ml, respectively; the half-life is 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).

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 mg and 1200 mg,37.9% and 46% are excreted by the kidneys,40.2% and 29.1% by the intestines, respectively.

Indications

-Lower respiratory tract infections (including bronchitis, pneumonia).

– Upper respiratory tract infections (including pharyngitis, sinusitis).

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

– Mycobacterial infections caused by Mycobacterium avium and Mycobacterium intracellulare. Localized infections caused by Mycobacterium fortuitum and Mycobacterium kansasii.

– Prevention of the spread of infection caused by the Mycobacterium avium complex (MAC infection) in HIV-infected patients with a CD4 lymphocyte count of no more than 100 / µl.

– Eradication of Helicobacter pylori in order to reduce the frequency of relapses of gastric and duodenal ulcers.

– Odontogenic infections.

Use during pregnancy and lactation

The use of the drug during pregnancy (II and III trimesters) is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

Clarithromycin is excreted in breast milk, so if it is necessary to prescribe the drug during lactation, stop breastfeeding.

Contraindications

* hypersensitivity to macrolide drugs·

* concomitant administration of clarithromycin with the following drugs: astemizole, cisapride, pimozide and terfenadine

· * porphyria;

* pregnancy (I trimester)

· * lactation;

* children under 12 years of age.

With caution: Renal and / or hepatic insufficiency. When taking medications that are metabolized by the liver, it is recommended to measure their concentration in the blood.

Side effects

From the nervous system: headache, dizziness, anxiety, fear, insomnia, “nightmare” dreams; rarely-disorientation, hallucinations, psychosis, depersonalization, confusion.

From the digestive system: nausea, vomiting, gastralgia, diarrhea, stomatitis, glossitis, increased activity of “hepatic” transaminases, cholestatic jaundice, rarely-pseudomembranous enterocolitis.

From the sensory organs: tinnitus, changes in taste (dysgeusia); in isolated cases – hearing loss that passes after discontinuation of the drug.

Hematopoietic and hemostatic disorders: rarely-thrombocytopenia (unusual bleeding, hemorrhage).

Allergic reactions: skin rash, pruritus, malignant exudative erythema (Stevens-Johnson syndrome), anaphylactoid reactions.

Other services: development of microbial resistance.

Interaction

Concomitant use of clarithromycin with cisapride, pimozide, terfenadine, astemizole is contraindicated, as this leads to an increase in the concentration of these drugs in blood plasma by 2-3 times, which can cause prolongation of the QT interval, cardiac arrhythmia, including ventricular tachycardia, ventricular fibrillation.

When taken concomitantly, clarithromycin increases the blood concentration of drugs metabolized in the liver by cytochrome P450 enzymes: indirect anticoagulants, carbamazepine, theophylline, triazolam, midazolam, cyclosporine, vinblastine, disopyramide, phenytoin, rifabutin, simvastatin, lovastatin, digoxin, alprazolam, valproic acid, cilostazol, methylprednisolone, omeprazole, quinidine, ergot alkaloids, sildenafil, tacrolimus.

Concomitant administration of clarithromycin and zidovudine in HIV-infected patients resulted in a decrease in the steady-state concentration of zidovudine (an interval of at least 4 hours is required between drug administration).

Concomitant administration of ritonavir (200 mg every 8 hours) and clarithromycin (500 mg every 12 hours) slowed the metabolism of clarithromycin (Cmax of clarithromycin increased by 31%, Cmin – by 182%, AUC – by 77%). A significant slowdown in the formation of 14-hydroxyclarithromycin was observed.

When taking ritonavir, clarithromycin should not be administered simultaneously at a dose of more than 1 g per day. In this case, patients without impaired renal function do not need to adjust the dose of clarithromycin. This is of great importance when using this combination in patients with impaired renal function: in patients with creatinine clearance from 30 to 60 ml / min, the dose of clarithromycin is reduced by 50% (up to 500 mg once a day).

Cross-resistance between clarithromycin, lincomycin and clindamycin may occur.

How to take, course of administration and dosage

Inside, adults and children over 12 years of age-250-500 mg 2 times a day. The duration of treatment is 6-14 days.

In the treatment of infections caused by Mycobacterium avium,500 mg is prescribed orally 2 times a day. The duration of treatment is 6 months or more.

For eradication of Helicobacter pylori in patients with peptic ulcer of the stomach and duodenum 12, clarithromycin is prescribed 250-500 mg twice a day as part of a combination therapy. The duration of treatment is 7-14 days.

In patients with chronic renal insufficiency (creatinine clearance less than 30 ml / min or serum creatinine concentrations greater than 3.3 mg / 100 ml) – 250 mg/day (once), in severe infections-250 mg 2 times a day. The maximum duration of treatment in patients of this group is 14 days.

Overdose

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

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

Special instructions

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

With caution, it is prescribed against the background of drugs that are metabolized by the liver (it is recommended to measure their concentration in the blood).

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

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

Yellow film-coated tablets, biconvex in shape, oblong with rounded edges, with a risk.

The cross-section shows two layers, the inner layer is white or almost white in color.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 20 °C

Shelf life

2 years

Active ingredient

Clarithromycin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Skin Infections, Tonsillitis, Gastrointestinal Infections Caused by Helicobacter Pylori, Sinusitis, Gastric and Duodenal Ulcers, Otitis Media, Boils, Sore Throats, Colds, Pharyngitis, Bronchitis

Weight

Weight: 24 gr.