CLARITHROMYCIN-TEVA 500 mg 14 pcs. film-coated tablets

Clarithromycin-teva 500 mg 14 pcs. film-coated tablets

pharmachologic effect

Clarithromycin is a semisynthetic broad-spectrum macrolide antibiotic.
The antibacterial effect of clarithromycin is carried out by suppressing protein synthesis due to binding to the 50s subunit of bacterial ribosomes. Clarithromycin has pronounced activity against a wide range of aerobic and anaerobic gram-positive and gram-negative organisms. The minimum inhibitory concentration (MIC) of clarithromycin is half that of erythromycin for most microorganisms. The 14-hydroxy metabolite of clarithromycin also has antimicrobial activity. The minimum inhibitory concentrations of this metabolite are equal to or greater than the MIC of clarithromycin; against H. influenzae, the 14-hydroxy metabolite is twice as active as clarithromycin.

Clarithromycin is active in vitro against the following organisms - gram-positive aerobic bacteria: Staphylococcus aureus (methicillin sensitive), Streptococcus agalactiae, Streptococcus pyogenes, Streptococcus pneumonia, Streptococcus viridans and Listeria monocytogenes; gram-negative aerobic bacteria: Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella (Branhamella) catarrhalis, Neisseria gonorrhoea, Legionella pneumophila, Bordetella pertussis, Helicobacter pylori, Campylobacter jejuni; predominantly intracellular microorganisms: Mycoplasma pneumonia, Ureaplasma urealyticum, Chlamydia trachomatis, Chlamydia pneumonia, Mycobacterium avium, Mycobacterium leprae, M. kansaii, M. chelonae, M. marinum, M. fortitum; anaerobic microorganisms: Bacteroides fragilis, Clostridium perfringens, Propionibacterium acnes, Peptococcus species; Peptostreptococcus species. In addition, the drug is active against Toxoplasma species.

Clarithromycin has bactericidal activity against certain bacterial strains: Haemophilus influenzae; Streptococcus pneumoniae; Streptococcus pyogenes; Streptococcus agalactiae; Moraxella (Branhamella) catarrhalis; Neisseria gonorrhoeae; Helicobacter pylori and Campylobacter spp.

Composition and release form Clarithromycin-teva 500 mg 14 pcs. film-coated tablets

Tablets - 1 tablet:

Active substance: clarithromycin 500 mg.
Excipients: povidone, microcrystalline cellulose, croscarmellose sodium, colloidal silicon dioxide, magnesium stearate.
Shell composition: opadry II 31F58914 white (hypromelose, lactose monohydrate, titanium dioxide (E171), macrogol 4000, sodium citrate).

14 pcs. - blisters (1) - cardboard packs.

Description of the dosage form

White film-coated tablets, oblong, biconvex, scored on one side.

Directions for use and doses

Inside. Adults: the usual dose is 250 mg 2 times / day for 7 days, if necessary, the dose can be increased to 500 mg 2 times / day for a period of up to 14 days for severe infections.

Children over 12 years of age: dosage regimen as for adults.

For the treatment of duodenal ulcers caused by H. pylori (adults):

Triple therapy regimen (1-14 days): clarithromycin 500 mg 2 times a day; lansoprazole 30 mg 2 times/day; amoxicillin 1000 mg 2 times/day.

Triple therapy regimen (7 days): clarithromycin 500 mg 2 times a day; lansoprazole 30 mg 2 times/day; Metronidazole 400 mg 2 times/day.

Triple therapy regimen (7 days): clarigromycin 500 mg 2 times a day; omeprazole 40 mg/day; amoxicillin 1000 mg 2 times/day or metronidazole 400 mg 2 times/day.

Triple therapy regimen (10 days): clarithromycin 500 mg 2 times/day is prescribed with amoxicillin 100 mg 2 times/day and omeprazole 20 mg/day.

Dual therapy regimen (14 days): clarithromycin 500 mg 3 times a day, omeprazole orally 40 mg 1 time a day.

If renal function is impaired, dosage adjustment is usually not required, with the exception of patients with severe renal impairment (KC

When taking ritonavir concomitantly for patients with impaired renal function, a dose adjustment is recommended according to the following scheme: for patients with CC 30-60 ml/min, the dose of clarithromycin should be reduced by 50%. For patients with CC less than 30 ml/min, the dose of clarithromycin should be reduced by 75%. When using clarithromycin and ritonavir together, dosages of clarithromycin should not exceed 1 g/day.

Pharmacokinetics

Clarithromycin is quickly and well absorbed from the gastrointestinal tract after oral administration. The microbiologically active metabolite 14-hydroxyclarithromycin is formed after the first passage through the liver. Food intake does not affect the bioavailability of clarithromycin; however, it slightly slows down the onset of absorption of clarithromycin and the formation of the 14-hydroxy metabolite. The pharmacokinetics of clarithromycin is nonlinear; in this case, the equilibrium concentration is achieved 2 days after starting the drug.

Clarithromycin is excreted in the urine and also in feces, mainly through bile. When taking 250 mg of clarithromycin 2 times a day, 15-20% of the administered dose is excreted unchanged in the urine. When taking 500 mg 2 times a day, urinary excretion is about 36%. 14-hydroxyclarithromycin is the main metabolite found in urine, accounting for about 10-15%.

When taking 500 mg of clarithromycin 3 times a day, the plasma concentration of clarithromycin is higher than when taking this dose 2 times a day.

The content of clarithromycin in tissues, including glandular and pulmonary tissue, is several times higher than in circulating blood. At therapeutic concentrations, clarithromycin is 80% bound to plasma proteins.

Clarithromycin penetrates gastric mucus. The level of clarithromycin in gastric mucus and tissue increases during combination therapy with omeprazole. Clarithromycin passes into breast milk

Indications for use Clarithromycin-teva 500 mg 14 pcs. film-coated tablets

Infections caused by microorganisms sensitive to clarithromycin:

lower respiratory tract infections (including acute and chronic bronchitis, pneumonia);
upper respiratory tract infections (including sinusitis and pharyngitis);
skin and soft tissue infections;
duodenal ulcer for eradication of Helicobacter pylori (as part of complex therapy with proton pump inhibitors).

Contraindications

Simultaneous administration with ergot derivatives;
simultaneous administration of the following drugs: cisapride, pimozide, terfenadine;
children under 12 years of age;
pregnancy and lactation period.
hypersensitivity to macrolide antibiotics.

With caution: patients with impaired liver and kidney function.

Application of Clarithromycin-teva 500 mg 14 pcs. film-coated tablets during pregnancy and breastfeeding

The safety of clarithromycia during pregnancy and lactation has not been studied.

The drug passes into breast milk. If necessary, use during lactation should stop breastfeeding.

Use in children

Contraindication: children under 12 years of age.

special instructions

Taking clarithromycin tablets in children under 12 years of age is not recommended.

When clarithromycin and warfarin are co-administered, prothrombin time should be regularly monitored.

When clarithromycin and digoxin are co-administered, the level of digoxin concentration in the blood serum should be monitored.

Overdose

Symptoms: gastrointestinal symptoms; one of the patients, when taking 8 g of clarithromycin, had a case of mental state disturbance, paranoid behavior, hypoglycemia, hypoxemia.

Treatment: gastric lavage, maintenance therapy. Hemodialysis or peritoneal dialysis is ineffective, as for other macrolides.

Side effects Clarithromycin-teva 500 mg 14 pcs. film-coated tablets

Clarithromycin is generally well tolerated by patients

From the gastrointestinal tract: nausea, vomiting, dyspepsia, diarrhea, abdominal pain, stomatitis, glossitis, pancreatitis, oral candidiasis, discoloration of the tongue and teeth; rarely - pseudomembranous enterocolitis. Tooth discoloration is reversible and can usually be restored with special treatment at a dental clinic. As with other antibiotics from the macrolide group, liver function disorders are possible, incl. increased activity of liver enzymes, hepatocellular and/or cholestatic hepatitis with or without jaundice. These liver problems can be severe, but are usually reversible. Very rare cases of liver failure and death have been observed, mainly due to severe concomitant diseases and/or concomitant drug therapy.

From the blood system: in exceptional cases - leukopenia and thrombocytopenia; increase in serum creatinine level.

From the central and peripheral nervous system: paresthesia, headache, disturbances of smell, changes in taste; dizziness, agitation, insomnia, nightmares, fear, ringing in the ears, confusion, disorientation, hallucinations, psychosis, depersonalization; reversible hearing loss; convulsions.

From the cardiovascular system: as with other macrolides, prolongation of the QT interval, ventricular tachycardia, polymorphic ventricular tachyarrhythmia (torsades de pointes).

From the musculoskeletal system: arthralgia, myalgia.

From the urinary system: isolated cases of increased plasma creatinine, interstitial nephritis, renal failure.

Allergic reactions: urticaria, angioedema, anaphylactic shock, in rare cases - Stevens-Johnson syndrome, toxic elidermal necrolysis.

Other: rarely - hypoglycemia in patients taking oral hypoglycemic drugs or insulin.

Drug interactions

When clarithromycin is co-administered with cisapride, pimozide and terfenadine, increased plasma concentrations of these drugs are observed, which can cause prolongation of the QT interval and cardiac arrhythmias, including ventricular tachycardia, ventricular fibrillation, arrhythmia and torsade de pointes; similar effects are observed when taking astemizole and other macrolides simultaneously.

Clarithromycin does not interact with oral contraceptives.

As with other macrolide antibiotics, concomitant use of clarithromycin and other drugs metabolized by cytochrome P450 (warfarin, ergot alkaloids, triazolam, midazolam, disopyramide, lovastatin, rifabutin, phenytoin, cyclosporine and tacrolimus) may be accompanied by an increase in serum concentrations of these drugs. blood.

With simultaneous use of clarithromycin and HMG-KoA reductase inhibitors (lovastatin, simvastatin), rhabdomyolysis may develop.

With the simultaneous administration of clarithromycin and theophylline, the concentration of theophylline in the blood serum and its toxicity increase.

The simultaneous administration of clarithromycin and warfarin or digoxin may be accompanied by an increase in the severity of their effects.

With the simultaneous administration of clarithromycin and carbamazepine, the effect of carbamazepine may be enhanced due to a decrease in the rate of excretion of carbamazepine.

When clarithromycin and zidovudine (orally) are taken simultaneously in HIV-infected adult patients, the steady-state concentration of zidovudine may decrease; this can be largely avoided by increasing the interval between doses of clarithromycin and zidovudine to 1-2 hours. For children, such an interaction was not observed.

When taking ritonavir and clarithromycin simultaneously, the values of the pharmacokinetic parameters for the latter increase: AUC, Cmax, Cmin. For patients with normal renal function, no dose adjustment is usually required due to the wide therapeutic dosage range of clarithromycin.

With the simultaneous use of clarithromycin and omeprazole, clarithromycin and lansoprazole, as well as clarithromycin and ranitidine, an increase in the concentration of drugs in the blood plasma is possible, but usually no dose adjustment is required.

With the simultaneous use of clarithromycin and hypoglycemic agents, including insulin, in rare cases, hypoglycemia may develop.

Clarithromycin-Teva tablets 500 mg 10 pcs. in Moscow

Clarithromycin is a semisynthetic antibiotic of the macrolide group and has an antibacterial effect by interacting with the 50S ribosomal subunit and inhibiting the protein synthesis of bacteria sensitive to it.

Clarithromycin demonstrated high activity in vitro against both standard laboratory strains of bacteria and those isolated from patients during clinical practice. Shows high activity against many aerobic and anaerobic gram-positive and gram-negative microorganisms. The minimum inhibitory concentrations (MICs) of clarithromycin for most pathogens are less than the MICs of erythromycin on average per Log2 dilution.

Clarithromycin in vitro

highly active against
Legionellapneumophila Mycoplasmapneumonia
e.
It has a bactericidal effect against Helicobacter pylori
; this activity of clarithromycin is higher at neutral pH. than with sour.

In addition, in vitro and in vivo

indicate that clarithromycin acts against clinically relevant mycobacterial species.
Enterobacteriaceae and Pseudomonasspp
. like other non-lactose-fermenting gram-negative bacteria, they are not sensitive to clarithromycin.

The activity of clarithromycin against most strains of the microorganisms listed below has been proven both in vitro and in clinical practice for the diseases listed in the “Indications for Use” section.

Aerobic gram-positive microorganisms:

Staphylococcus aureus
Streptococcus pneumoniae
Streptococcus pyogenes
Listeriamonocytogenes

Aerobic gram-negative microorganisms:

Haemophilus influenzae
Haemophilus parainfluenzae
Mor ax ll a catarrhal is
Neisseria gonorrhoeae
Legionella pneumophila

Other microorganisms:

Mycoplasma pneumoniae
Chlamydia pneumoniae (TWAR)

Mycobacteria:

Mycobacterium leprae
Mycobacterium kansasii
Mycobacterium chelonae
Mycobacterium fortuitum
Mycobacterium avium complex (MAC) -
a complex including:
Mycobacterium avium
Mycobacterium intracellulare

The production of beta-lactamase does not affect the activity of clarithromycin. Most strains of staphylococci resistant to methicillin and oxacillin are also resistant to clarithromycin.

Helicobacter pylori

Sensitivity of H. pylori

to clarithromycin was studied on
H. pylori
isolated from 104 patients before the start of drug therapy. In 4 patients, clarithromycin-resistant strains of H. pylori were isolated; in 2 patients, strains with moderate resistance were isolated; in the remaining 98 patients, H. pylori isolates were sensitive to clarithromycin. Clarithromycin has an in vitro effect against most strains of the following microorganisms (however, the safety and effectiveness of the use of clarithromycin in clinical practice has not been confirmed by clinical studies and the practical significance remains unclear):

Aerobic gram-positive microorganisms:

Streptococcusagalactiae
Streptococcus (group C FG)
Viridansgroupstreptococcus

Aerobic gram-negative microorganisms:

Bordetella pertussis
Pasteurellamultocida

Anaerobic gram-positive microorganisms:

Clostridium perfringens

Peptococcus niger

Propionibacterium acnes

Anaerobic gram-negative microorganisms:

Bacteroides melaninogenicus

Spirochetes:

Borrelia burgdorferi
Treponema pallidum

Campylobacter:

Campylobacter jejuni

The main metabolite of clarithromycin in the human body is the microbiologically active metabolite 14-hydroxyclarithromycin (14-OH-clarithromycin).

The microbiological activity of the metabolite is the same as that of the parent substance or 1-2 times weaker against most microorganisms. The exception is H. influenzae

for which the effectiveness of the metabolite is twice as high.
The parent compound and its major metabolite have either additive or synergistic effects against both H. influenzae
in
vitro and in vivo
, depending on the bacterial strain.

Clarithromycin-Teva tablet p/o 500 mg N10 (Teva)

PharmacodynamicsClarithromycin is a second-generation bacteriostatic antibiotic from the group of broad-spectrum macrolides. Disturbs the protein synthesis of microorganisms (binds to the 50S subunit of the ribosomal membrane of the microbial cell). Acts on extra- and intracellularly located pathogens. 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 pylori (Campilo bacter), Campilobacter 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 ana erobes (Eubacterium spp., Peptococcus spp., Propionibacterium spp., Clostridium perfringens, Bacteroides melaninogenicus), is less active against Mycobacterium tuberculosis. Pharmacokinetics: Absorption is fast. Food slows absorption without significantly affecting bioavailability. Communication with 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 the blood plasma after oral administration of 250 mg is 1-3 hours. After oral administration, 20% of the dose taken is quickly hydroxylated in the liver by cytochrome enzymes CYP3A4, CYP3A5 and CYP3A7 with the formation of the main metabolite -14-hydroxyclarithromycin, which has a pronounced antimicrobial activity against Haemophilus influenzae. It is an inhibitor of the isoenzymes CYP3A4, CYP3A5 and CYP3A7. When taken regularly at 250 mg/day, the equilibrium 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 equilibrium concentration of the unchanged drug and its metabolite in plasma is 2.7-2.9 and 0.83-0.88 μg/ml, respectively; 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 (concentrations there are 10 times higher than the level in 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, and 40.2 and 29.1% by the intestines, respectively.