Clarithrosin
Claritrosin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Clarithrosin
ATX code: J01FA09
Active ingredient: clarithromycin (Clarithromycin)
Producer: Sintez, LLC (Russia)
Description and photo updated: 30.11.2018
Prices in pharmacies: from 53 rubles.
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Clarithrosin is an antibiotic from the macrolide group.
Release form and composition
Dosage form - film-coated tablets: round, biconvex, yellow, in cross-section - almost white or white (in cell contour packs containing 5 or 10 tablets, in a cardboard box 1-2 packs and instructions for the use of Clarithrosin).
Composition of 1 tablet:
- active substance: clarithromycin - 250 or 500 mg;
- auxiliary components: microcrystalline cellulose, colloidal silicon dioxide (aerosil), sodium carboxymethyl starch, magnesium stearate, lactose monohydrate, potato starch, povidone (polyvinylpyrrolidone), talc;
- film shell: macrogol 4000, titanium dioxide, hypromellose, tropeolin O dye.
Pharmacological properties
Pharmacodynamics
The active substance of Clarithrosin is clarithromycin, a semi-synthetic macrolide antibiotic with a broad spectrum of action. It interacts with the 50S ribosomal subunit of sensitive bacteria and inhibits protein synthesis, which causes the antibacterial effect of the drug.
The coated tablets are a homogeneous crystalline base that provides a sustained release of clarithromycin as the drug passes through the gastrointestinal tract.
In vitro, the drug is highly active against standard and isolated cultures of bacteria: many anaerobic and aerobic gram-negative and gram-positive microorganisms, including Mycoplasma pneumoniae and Legionella pneumophila.
Clarithromycin is resistant to gram-negative bacteria that do not degrade lactose, including Enterobacteriaceae and Pseudomonas.
Clarithrosin has an antibacterial effect on the following pathogens:
- anaerobes: Peptococcus niger, Bacteroides melaninogenicus, Propionibacterium acnes, Clostridium perfringens;
- gram-negative aerobic microorganisms: Moraxella (Branhamella) catarrhalis, Haemophilus influenzae, Campylobacter jejuni, Legionella pneumophila, Haemophilus parainfluenzae, Helicobacter pylori, Pasteurella multocida, Neisseria gonorrhoeae;
- gram-positive aerobic microorganisms: Listeria monocytogenes, Streptococcus pyogenes, Staphylococcus aureus, Streptococcus viridans, Streptococcus agalactiae, Streptococcus pneumoniae;
- mycobacteria: Mycobacterium chelonae, Mycobacterium leprae, Mycobacterium intracellulare, Mycobacterium fortuitum, Mycobacterium avium, Mycobacterium avium complex (MAC), Mycobacterium kansasii;
- intracellular microorganisms: Borrelia burgdorferi, Mycoplasma pneumoniae, Chlamydia trachomatis, Chlamydophila (Chlamydia) pneumoniae.
The production of β-lactamases does not affect the effect of clarithromycin. Most strains of staphylococci that are resistant to oxacillin and methicillin are also resistant to clarithromycin.
The activity of Clarithrosin in vitro has also been noted against strains of the following microorganisms (however, the efficacy and safety of the use of clarithromycin in clinical practice has not been established):
- gram-negative anaerobic bacteria: Bacteroides melaninogenicus;
- gram-positive anaerobic microorganisms: Peptococcus niger, Clostridium perfringens, Propionibacterium acnes;
- gram-negative aerobic microorganisms: Pasteurella multocida and Bordetella pertussis;
- gram-positive aerobic microorganisms: Streptococci groups C, F, G and Viridans, Streptococcus agalactiae;
- spirochetes: Treponema pallidum and Borrelia burgdorferi;
- Campylobacter jejuni.
The main metabolite of the drug is 14-hydroxyclarithromycin, which has a microbiological activity that is similar to clarithromycin or 2 times weaker in relation to most microorganisms, with the exception of Haemophilus influenzae - in its relation 14-hydroxyclarithromycin is 2 times more active.
Clarithromycin and its metabolite against Haemophilus influenzae in vitro and in vivo have an additive or synergistic effect depending on the culture of bacteria.
Pharmacokinetics
From the gastrointestinal tract, clarithromycin is absorbed quickly and well. Its bioavailability is 50–55%. Concomitant food intake slows down absorption, but does not significantly affect bioavailability.
The maximum concentration (C max) is recorded in no more than 3 hours. After a single dose of Clarithrosin, two peaks of C max are noted, the second is due to the ability of clarithromycin to concentrate in the gallbladder and then be released (gradually or quickly).
It binds to plasma proteins by 65–75%. When carrying out therapy using Clarithrosin in a daily dose of 250 mg, the steady-state concentration (C ss) of clarithromycin and 14-hydroxyclarithromycin is 1 and 0.6 μg / ml, respectively, the half-life (T ½) is 3-4 and 5-6 hours; in a daily dose of 500 mg: C ss - 2.7-2.9 and 0.83-0.88 μg / ml, T ½ - 4.8-5 and 6.9-8.7 hours, respectively.
The drug accumulates in the lungs, soft tissues and skin, where it creates concentrations 10 times higher than in blood serum.
Approximately 20% of the dose taken is rapidly hydrolyzed in the liver with the participation of cytochrome P 450 isoenzymes, such as CYP3A4, CYP3A5 and CYP3A7, resulting in the formation of metabolites, including the main active 14-hydroxyclarithromycin.
It is excreted by the kidneys and through the intestines: 20-30% - unchanged, the rest - in the form of metabolites. After a single dose of 250 mg or 1200 mg, 37.9 or 46% are excreted by the kidneys, 40.2 or 29.1%, respectively, through the intestines.
Pharmacokinetics in special cases:
- functional disorders of the liver: under the condition of normal renal function, the equilibrium concentration and clearance of clarithromycin are similar to those in healthy volunteers, therefore, dose adjustment is not required. C ss of 14-hydroxyclarithromycin is lower than in healthy patients;
- functional disorders of the kidneys: increase in C max and C min (maximum and minimum concentrations) in plasma, AUC (area under the concentration-time curve) and half-life of clarithromycin and 14-hydroxyclarithromycin, decrease in the constant of elimination and excretion by the kidneys. The severity of changes in these parameters depends on the degree of impaired renal function;
- advanced age: the concentration of clarithromycin and 14-hydroxyclarithromycin increases, their excretion decreases. These changes are associated not with age, but mainly with age-related changes in renal function and creatinine clearance;
- HIV infection: when using clarithromycin in doses of more than 1000 mg per day, required for the treatment of mycobacterial infections, a significant increase in the plasma concentration of the drug and an increase in its T ½ are possible - these changes are consistent with the known nonlinearity of the pharmacokinetics of clarithromycin;
- simultaneous use of omeprazole in a daily dose of 40 mg: while taking clarithromycin 500 mg 3 times a day, the AUC and T ½ of omeprazole increase by 89 and 34%, respectively, and the C max, C min and AUC of clarithromycin also increase by 10, 27 and 15, respectively % compared to patients receiving clarithromycin alone. With combination therapy, 6 hours after taking Clarithrosin, the equilibrium concentration of clarithromycin in the gastric mucosa is 25 times higher, in the stomach tissues - 2 times higher than in patients not taking omeprazole.
Indications for use
Clarithrosin is indicated for the treatment of infectious and inflammatory diseases caused by sensitive pathogens, such as:
- odontogenic infections;
- infections of the skin and soft tissues (including folliculitis and erysipelas);
- infections of the lower and upper respiratory tract (sinusitis, tonsillitis, pharyngitis, bronchitis, community-acquired pneumonia);
- common mycobacterial infections caused by Mycobacterium intracellulare and Mycobacterium avium.
In addition, Clarithrosin is used to prevent the spread of infection caused by the Mycobacterium avium complex, as well as to eradicate Helicobacter pylori and reduce the frequency of recurrence of duodenal ulcers.
Contraindications
Absolute:
- children under 3 years old;
- lactation period;
- deficiency of sucrase / isomaltase, fructose intolerance, glucose-galactose malabsorption;
- porphyria;
- severe chronic renal failure [creatinine clearance (CC) less than 30 ml / min];
- severe functional disorders of the liver;
- concomitant use of the following drugs: astemizole, cisapride, pimozide, terfenadine, ergotamine and other ergot alkaloids, midazolam in oral dosage forms, alprazolam, triazolam;
- hypersensitivity to any component of Clarithrosin or other macrolides.
The antibiotic Clarithrosin should be used with caution in patients with myasthenia gravis, renal and hepatic insufficiency, during pregnancy, as well as in the case of the simultaneous use of colchicine or drugs metabolized by the liver.
Claritrosin, instructions for use: method and dosage
Claritrosin tablets are taken orally. Meal time does not matter.
Adults and adolescents from 12 years old and / or weighing more than 33 kg, as a rule, the drug is prescribed at a dose of 250 mg 2 times a day (at intervals of 12 hours). The duration of the therapeutic course is 7-14 days.
Recommended dosage regimens for Clarithrosin according to indications:
- pharyngitis and tonsillitis caused by Streptococcus pyogenes: 250 mg 2 times a day for 10 days;
- acute sinusitis: 500 mg 2 times a day for 14 days;
- exacerbated chronic bronchitis: if the pathogen is Streptococcus pneumoniae or Moraxella catarrhalis - 250 mg 2 times a day for 7-14 days, Haemophilus parainfluenzae - 500 mg 2 times a day for 7 days, Haemophilus influenzae - 500 mg 2 times 7-14 days per day;
- community-acquired pneumonia: if the causative agent is Chlamydophila (Chlamydia) pneumoniae, Mycoplasma pneumoniae or Streptococcus pneumoniae - 250 mg 2 times a day for 7-14 days, Haemophilus influenzae - 250 mg 2 times a day for 7 days;
- uncomplicated infections of the skin and subcutaneous tissue caused by Streptococcus pyogenes or Staphylococcus aureus: 250 mg 2 times a day for 7-14 days;
- odontogenic infections: 250 mg 2 times a day for a 5-day course;
- prevention and treatment of infections caused by the Mycobacterium avium complex: 500 mg 2 times a day for 6 months or more. The maximum allowable dose is 1000 mg per day.
For the eradication of Helicobacter pylori, Clarithrosin is used in combination with omeprazole or amoxicillin and omeprazole / lansoprazole. Usually, one of the following treatment regimens is prescribed:
- clarithromycin 500 mg 3 times a day + omeprazole 40 mg a day for 14 days, in the next 14 days, omeprazole is used in a daily dose of 20 mg;
- clarithromycin 500 mg 2 times a day + omeprazole 20 mg 2 times a day + amoxicillin 1000 mg 2 times a day for 10 days;
- clarithromycin 500 mg 2 times a day + lansoprazole 30 mg 2 times a day + amoxicillin 1000 mg 2 times a day, the duration of therapy is 10 days.
Children 3-12 years old Claritrosin is prescribed in a daily dose of 15 mg / kg and divided into 2 doses. The maximum allowable dose is 1000 mg per day. The duration of therapy is 10 days.
In chronic renal failure with a CC of 290 μmol / l (3.3 mg / 100 ml), the dose of Clarithrosin is halved or the intervals between doses are doubled. Treatment in these patients should not exceed 14 days.
Side effects
- allergic reactions: skin flushing, urticaria, itching, skin rash, toxic epidermal necrolysis, Stevens-Johnson syndrome, anaphylactic reactions;
- from the digestive system: discoloration of the tongue and teeth, glossitis, stomatitis, candidiasis of the oral mucosa, nausea, vomiting, diarrhea, gastralgia, dyspepsia, pseudomembranous colitis, increased activity of hepatic transaminases, cholestatic jaundice, hepatocellular and cholestatic hepatitis, acute pancreatitis liver failure with a fatal outcome (mainly in cases of concomitant diseases or the simultaneous use of certain drugs);
- from the urinary system: hypercreatininemia, interstitial nephritis;
- from the hematopoietic system: leukopenia, thrombocytopenia (unusual bleeding, hemorrhage);
- from the nervous system: insomnia, headache, dizziness, convulsions, confusion, depersonalization, anxiety, hallucinations, nightmares, disorientation, fear, depression, psychosis;
- on the part of the cardiovascular system: lengthening of the QT interval on the electrocardiogram, flutter and fibrillation of the ventricles, ventricular tachycardia (including pirouette-type);
- from the senses: change in taste, noise / ringing in the ears, reversible hearing loss, impaired sense of smell;
- from the endocrine system: hypoglycemia;
- others: secondary infections (resistance of microorganisms), myalgia.
Overdose
Taking an excessive dose of Clarithrosin can lead to abdominal pain, diarrhea, nausea, vomiting, and confusion.
You should rinse the stomach as soon as possible after taking the drug. Further treatment is symptomatic. Hemodialysis and peritoneal dialysis are ineffective.
special instructions
In patients with chronic liver disease during therapy, the activity of enzymes in the blood serum should be regularly monitored.
In the case of joint administration of warfarin or other indirect anticoagulants, monitoring of prothrombin time is indicated.
Particular care should be taken with the combined use of drugs that are metabolized by liver enzymes. It is recommended to periodically check their blood concentrations.
If severe and / or prolonged diarrhea occurs while taking Clarithrosin or after its cancellation, the patient should be examined for the development of pseudomembranous colitis, a life-threatening complication that requires discontinuation of antibiotic therapy and appropriate treatment.
In some patients, while taking clarithromycin, a secondary infection develops due to the growth of insensitive microorganisms. In these cases, the appointment of adequate therapy is required.
Influence on the ability to drive vehicles and complex mechanisms
Due to the risk of developing negative phenomena from the nervous system, patients are advised to be careful when driving a car and performing tasks that require speed of reactions and increased attention.
Application during pregnancy and lactation
It is possible to use Claritrosin in pregnant women, but only if the benefits of the forthcoming therapy outweigh the potential risks.
The drug passes into breast milk. If a course of antibiotic therapy is required during lactation, breastfeeding should be discontinued.
Pediatric use
Claritrosin tablets are contraindicated in children under 3 years of age.
The maximum daily dose for children 3–12 years old is 1000 mg, the recommended daily dose is 15 mg / kg in 2 divided doses. The duration of therapy is 10 days.
With impaired renal function
It is contraindicated to use the antibiotic Clarithrosin in patients with severe functional impairment of the kidneys.
In chronic renal failure with a CC of 290 μmol / L (3.3 mg / 100 ml), the clarithromycin dose is halved or the intervals between doses are doubled. Treatment in these patients should not exceed 14 days.
For violations of liver function
It is contraindicated to use Clarithrosin in patients with severe liver dysfunction.
With hepatic insufficiency, the drug is taken with caution.
Use in the elderly
When treating elderly patients, care should be taken to take into account the possible age-related decrease in renal function and changes in creatinine clearance.
Drug interactions
Claritrosin is contraindicated to be used simultaneously with drugs primarily metabolized by the CYP3A isoenzyme, such as astemizole, cisapride, pimozide, terfenadine, ergotamine and other ergot alkaloids, midazolam in oral dosage forms, alprazolam, triazolam. This is due to the high risk of a mutual increase in the concentration of drugs in the blood, which is fraught with an increase or prolongation of both therapeutic and side effects.
Particular care should be taken with the combined use of drugs that are metabolized through other isoenzymes of cytochrome P 450, such as: cyclosporine, quinidine, lovastatin, carbamazepine, sildenafil, omeprazole, disopyramide, rifabutin, vinblastine, simvastatin, phenytoin, methylpredostlinizolovaya, the acid, tacrolimus, indirect anticoagulants (including warfarin). Dose adjustment of Clarithrosin and control of its concentration in the blood is required.
Possible drug interactions while using other drugs:
- pimozide, astemizole, terfenadine, cisapride: an increase in their plasma concentrations is possible, which can lead to a prolongation of the QT interval, the appearance of ventricular fibrillation, ventricular tachycardia and arrhythmias, including pirouette type;
- HMG-CoA reductase inhibitors (lovastatin, simvastatin): their concentrations increase, which increases the risk of rhabdomyolysis;
- theophylline, carbamazepine: their concentrations in the systemic circulation may increase;
- nevirapine, rifapentine, rifabutin, rifampicin, efavirenz: the concentration of clarithromycin in plasma decreases and its effect weakens, at the same time the concentration of 14-hydroxyclarithromycin increases;
- Colchicine: Possible enhancement of its action. It is necessary to monitor the patient's condition for the appearance of signs of intoxication, especially in patients with chronic renal failure and the elderly (deaths are known);
- preparations of the ergotamine group (ergotamine, dihydroergotamine): a significant increase in their concentration is possible, which is fraught with intoxication (vascular spasm, ischemia of the central nervous system, limbs and other tissues);
- quinidine, disopyramide: there is a risk of developing pirouette-type ventricular tachycardia. It is necessary to control their serum concentrations and monitor the electrocardiogram indicators for an increase in the QT interval;
- indirect anticoagulants: their effect may be enhanced;
- itraconazole: a mutual increase in plasma concentrations of drugs is possible. Careful monitoring of the patient's condition is required in order to enhance or prolong the effects of both drugs;
- tolterodine: it is possible to increase its concentration in patients with slow metabolism through the CYP2D6 isoenzyme, which requires a decrease in its dose;
- fluconazole (used in a daily dose of 200 mg simultaneously with clarithromycin in a daily dose of 1000 mg): it is possible to increase the equilibrium concentration and the area under the concentration-time curve of clarithromycin by 33 and 18%, respectively. Correction of the dosage regimen is not required;
- digoxin: there is a possibility of an increase in its concentration in the blood and the development of potentially fatal arrhythmias. Careful monitoring of serum levels is required;
- phosphodiesterase type 5 inhibitors (tadalafil, sildenafil, vardenafil): the inhibitory effect on the PDE5 enzyme may increase, which requires a decrease in the dose of the drug;
- verapamil: possible lowering of blood pressure, development of bradyarrhythmia and lactic acidosis;
- omeprazole: it is possible to increase its C max, AUC and T ½, respectively, by 30, 89 and 34%, there is a slight increase in the pH level in the stomach;
- atazanavir (used in a daily dose of 40 mg simultaneously with clarithromycin in a daily dose of 1000 mg): it is possible to increase the AUC of clarithromycin by 2 times and atazanavir by 28%, as well as a 70% decrease in the AUC of 14-hydroxyclarithromycin. For patients with CC 30–60 ml / min, it is necessary to halve the clarithromycin dose. Concomitantly with protease inhibitors, clarithromycin should not be used in daily doses of more than 1000 mg;
- ritonavir (used in a daily dose of 600 mg simultaneously with clarithromycin in a daily dose of 1000 mg): the metabolism of clarithromycin may decrease and the formation of 14-hydroxyclarithromycin may be completely suppressed. In chronic renal failure, a dose adjustment of Clarithrosin is required depending on the CC: 30-60 ml / min - by 50%, CC <30 ml / min - by 75%. Simultaneously with ritonavir, clarithromycin should not be used in daily doses exceeding 1000 mg;
- saquinavir (used in soft gelatin capsules of 1200 mg 3 times a day simultaneously with clarithromycin in a daily dose of 1000 mg): the C ss and AUC of saquinavir may increase by 187 and 177%, respectively, clarithromycin - by 40%. With short-term joint use of drugs in the indicated doses, the dosage regimen adjustment is not required;
- zidovudine in oral dosage forms: a decrease in its equilibrium concentrations is possible. It is recommended to observe at least 4-hour intervals between doses;
- midazolam and other benzodiazepines metabolized by the CYP3A isoenzyme (triazolam and alprazolam) in oral dosage forms: a significant decrease in their metabolism is possible. It is not recommended to use such combinations;
- midazolam and other benzodiazepines metabolized by the CYP3A isoenzyme (triazolam and alprazolam) in parenteral dosage forms: care must be taken and their doses must be adjusted if necessary;
- benzodiazepines, the excretion of which does not depend on CYP3A isoenzymes (nitrazepam, temazepam, lorazepam): a clinically significant interaction with clarithromycin is unlikely.
Analogs
Clarithrosin analogs are: Bacticap, Vilprafen, Zimbaktar, Klabaks, Clarbact, Clarithromycin, Claricin, Klacid, Lecoclar, Macropen, Rovamycin, Romiklar, Rulid, Fromilid, Elrox, Erythromycin, Esparoxy and others.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C in a dry, dark place out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Clarithrosin
There are no reviews of Clarithrosin on specialized forums and websites. Clarithromycin (an active substance that is part of many medications), patients speak of as an effective antibiotic that helps with a variety of diseases caused by sensitive microorganisms.
Negative messages contain complaints about the development of adverse reactions, including bitterness in the mouth, stomach pain, nausea, diarrhea, vomiting, dizziness, tachycardia, insomnia, candidiasis.
Price for Claritrosin in pharmacies
Approximate prices for Clarithrosin are: 46 rubles. for 10 tablets of 250 mg, 121 rubles. for 5 tablets of 500 mg.
Claritrosin: prices in online pharmacies
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Drug name Price Pharmacy |
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Clarithrosin 500 mg film-coated tablets 5 pcs. RUB 53 Buy |
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Clarithrosin 250 mg film-coated tablets 10 pcs. RUB 60 Buy |
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Clarithrosin 500 mg film-coated tablets 10 pcs. 142 RUB Buy |
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Clarithrosin tablets p.p. 250mg 10 pcs. 153 r Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
