The composition of the drug clarithromycin, indications for use, a detailed list of side effects. Clarithromycin

Clarithromycin (also Clarithromycin SR) is an antibiotic macrolide group with a wide range of applications. The drug has antibacterial properties, acting on a variety of harmful microorganisms.

The active ingredients of this medication come into contact with the bacterial structure, inhibiting protein synthesis in it, which is inevitable leads to its destruction..

Clarithromycin acts on bacteria such as moraxella, Helicobacter pylori, Staphylococcus aureus, Haemophilus influenzae, mycobacteria, etc. Based on this, it can be noted indications for the use of this drug: diseases respiratory tract- pneumonia, bronchitis, etc., pharyngitis, otitis and sinusitis, infectious processes localized on skin, mycobacterial infections, burns, general ulcer therapy duodenum.

An important area of ​​​​use is the treatment of diseases such as tonsillitis and pneumonia. The drug is a means second line and is used when the patient is contraindicated in the use of first-line drugs - Amoxicillin and other similar drugs.

In addition, Clarithromycin is used in the field of venereology, is used in the treatment of mycoplasmosis and urogenital chlamydia.

Antibiotic Clarithromycin dosage of 250, 500 mg: instructions for use

The dosage regimen should be prescribed by the attending physician, after completing all the necessary laboratory tests . Diagnosis also affects dosage, frequency, and duration. drug therapy, so you should not take Clarithromycin on your own, without a visit to the doctor.

The drug is available in several forms:

• Capsules 250 and 500 mg.
• Tablets. The content of the active active ingredient is 250 and 500 mg.
• Special powder for suspension preparation.
• Solution for infusion.

If we evaluate the effectiveness of these funds, then the tablets are no different from the capsules. As for the powder, it is used to prepare a suspension for children up to 12 years.

Adult patients and children over 12 years old appointed 250 to 500 mg twice a day. Dose in 500 mg stored in the body 12 hours, therefore, the reception of funds twice.

You can drink tablets or capsules with plain water or other liquids, but not with milk, as it can lead to improper absorption.

How to take with a bacterial infection, before or after a meal?

The antibiotic Clarithromycin is widely used in the treatment of gastroenterological diseases. Application scheme includes double dose of capsules or tablets in a day. The daily dose is 500 mg.

Reception is carried out after meal. The duration of therapy varies one to two weeks. Only the attending physician decides how many days to take the drug.

Taking the drug by pregnant women and children

Any antibiotic is quite aggressive on the body, so most of them are not prescribed to women during pregnancy and young children. Clarithromycin is widely used in the treatment of various diseases, not only in adults but also in children.

However, there is one small nuance. The drug in the form of capsules and tablets is prescribed only to those children whose age over 12 years old.

Dosage for children over 12 years old will be identical to the regimen for adults, i.e. 250 to 500 mg twice a day. Small children are given from 7.5 to 15 mg per kilogram of body weight. They are shown the drug in the form of a powder, with which a suspension is prepared. The suspension is administered orally using a dosing syringe containing 5 ml medicines that match 125 mg Clarithromycin.

The expediency of taking this particular drug is determined by the pediatrician. Average duration treatment is 6 to 14 days.

As for pregnant women, the question is ambiguous.

Some experts do not recommend the use of this drug during the period of gestation, but if there is infectious diseases reception may be allowed if the woman is in the third trimester of pregnancy.

When taking Clarithromycin in the first and second trimester, there is a real risk of intrauterine pathologies in the unborn child.

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Dosage of the drug

The average dosage is 500 mg per day. This dose is provided for both adults and children over 12 years of age. In this case, we are talking about oral administration, but if the patient for some reason cannot take this medicine inside, he is assigned the introduction of a substance intravenously with droppers. In this case, the dosage is also 500 mg per day. Intravenous administration continues for 2-5 days, after which the patient is transferred to tablets or capsules.

In the treatment of diseases caused by various mycobacteria, the maximum daily dose may be increased. up to 1 gram per day. If the disease is severe, the maximum dose is exactly doubled - up to 2 grams. With this regimen, treatment can continue up to six months.

If the patient is diagnosed with chronic renal failure, then the dosage of Clarithromycin should be no more than 250 mg. Accordingly, the drug is taken once.

Important! The maximum daily dose for children over 12 years of age should be no more than 1 gram.

Dosage for tuberculosis

Clarithromycin is a macrolide, which means it can be used in the treatment of tuberculosis. It is used only in complex therapy together with first-line drugs Isoniazid, Ethambutol, Rifampin etc.

Photo 1. Packing of the drug Isoniazid in the form of tablets with a dosage of 300 mg. Producer "Moskhimfarmpreparaty".

The dosage is 1 gram twice a day. The average duration of such therapy is six months.

There is a certain dependence of the dosage on the weight and age of a particular patient. For adult patients older than 18 years, dosage in the first 8 weeks - 25 mg per 1 kg of body weight. Then the course changes a little, and the dosage will be 35 mg per 1 kg of body weight.

Dosage for children - 15 mg per 1 kg of body weight.

Main contraindications

Despite the indisputable effectiveness, this drug can not be used in all cases. The main contraindications are:

• First and second trimester of pregnancy.
• lactation period.
• Individual intolerance to the substances included in the composition.
• Hepatitis.
• Cholestatic jaundice.
• liver failure in acute form running simultaneously with kidney failure.
• Allergy to lactose in a patient.
• potassium deficiency.
• Ventricular arrhythmia.

If you have any liver disease, there is a possibility of complications. That is why it is necessary to strictly follow the prescriptions established by the doctor.

Clarithromycin cannot be used in the treatment of angina and otitis media. in children.

It should also be noted that the drug interacts with other media.

medicines, excluding simultaneous reception with this agent:

• Heart preparations made on the basis of ergot.
• Ticagrelor, i.e., a blood thinner.
• Atorvastatin, Rosuvastatin and other cholesterol-lowering drugs.
• Terfenadine, pimozide and cisapride.

Simultaneous reception with these medicines may cause significant deterioration and lots of side effects .

Attention! Clarithromycin belongs to the category of antibiotics, therefore it is forbidden to drink alcohol with it.

The fact is that alcohol greatly weakens the effect of the drug on the body, as a result of which the patient does not receive the necessary treatment.

The antibiotic acts on the body quite aggressively. It negatively affects not only microorganisms and bacteria, but also healthy cells. If we add to this the use of alcoholic beverages, then the body will be doubly loaded. Very much, including the liver. If the organ is healthy, it will cope with all the loads, and if there are certain problems, then complications may arise.

Side effects

Individual characteristics and non-compliance with the dosage can cause a negative reaction from the body to taking Clarithromycin. Can be distinguished major side effects:

• Panic attacks.
• Sleep disturbance.
• Pain in the head.
• Dizziness.
• Constant feeling anxiety.
• Hallucinations (rare).
• Vomiting and diarrhea.
• Change in taste.
• Noise in ears. In very rare cases, there may be a partial loss of auditory activity after discontinuation of the drug.
• Various allergic reactions on the skin, feeling itchy.
• Anaphylactic reaction.

Reference. In some cases (about 0.1%) there may be a change in the composition of the blood. Fixed cases of change heart rate.

When taking the drug possible exacerbation chronic diseases liver and kidneys. People with these problems should be treated with extreme caution. As for the complex therapy of tuberculosis, the side effects are not much different from the usual cases. The most common are dizziness, ringing in the ears and partial hearing loss, which recovers quickly. But it's still worth following official instructions to reduce the likelihood of their occurrence.

Conclusion

If we talk about the specifics of taking Clarithromycin, then we can note several nuances.

The frequency of administration, dosage and duration of therapy determines only the attending physician. The dosage and duration of the drug will vary and depend on many factors; great importance has a specific disease, the patient has chronic ailments and other pathologies.

Photo 2. Packaging of the drug Clarithromycin in the form of tablets with a dosage of 500 mg. Producer "Rapharma".

With extreme caution it is worth using this drug during pregnancy. Doctors allow you to do this only in the third trimester of pregnancy, but the gynecologist makes the final decision on the advisability of taking it.

Women breastfeeding a child should stop breastfeeding if you start taking this medicine. The fact is that active ingredients drugs pass into the mother's milk, which can adversely affect the health of the baby.

The maximum daily dose should not exceed 2 grams, but such an amount is shown only in some, the most severe cases. The drug belongs to the group of antibiotics, so it can adversely affect the functioning of the heart, liver, kidneys and digestive system if the dose is exceeded.

With regard to use in the treatment of tuberculosis, Clarithromycin is perceived as a drug 2 rows, i.e., it can only be used as an aid. As a rule, the drug is taken together with Ethambutol or Rifabutin. With this method of therapy, the daily dose of the drug is 1 gram - 500 mg twice a day. Depending on the specific clinical picture disease treatment can last no more than six months, but there are cases when therapy continues throughout the patient's life. Share with your friends!

Pharmaceutics is a discipline that does not stand still. It undergoes permanent evolutionary processes aimed at finding new formulas and creating more effective and safe drugs. And another antibiotic, a representative of the macrolide group Clarithromycin, became another success for scientists.

It is impossible to say that Clarithromycin is very young: it was synthesized 36 years ago. And yet, not only has it not lost its relevance in the 21st century, but it has also strengthened its stable position among other antibacterial drugs.

Today, Clarithromycin is considered a first- and second-line drug for the treatment of many infectious diseases.

The popularity of the drug is high: without it today it is unthinkable to treat pathologies of the upper and lower respiratory tract, infections of the genitourinary tract, and even peptic ulcer stomach and duodenum. It is prescribed in children's and adult practice, including in old age. Let's take a closer look at Clarithromycin and find out thanks to what qualities he was able to achieve such a high position.

A bit of history

So, Clarithromycin was born thanks to the hard and persistent work of scientists from the Japanese company Taisho Pharmaceutical. It happened in 1980. Then experts made many attempts to create a remedy based on the good old erythromycin macrolide. This antibiotic with a unique spectrum of activity, including intracellular bacteria, was in great demand, but its use was limited by instability in the gastrointestinal tract: the acidic environment of the stomach and gastric contents significantly slow down the absorption process. Because of this, the drug had to be taken at least four times a day, and in fairly high dosages. In addition, erythromycin has been associated with significant gastrointestinal side effects such as nausea and stomach pain.

Japanese scientists tried to introduce a methyl group into the formula of Erythromycin, obtaining 6-O-methylerythromycin structurally very close to it. Tests have shown that the new substance, called Clarithromycin, has almost the same spectrum of antibacterial activity as Erythromycin, and at the same time is devoid of side effects traditional for the progenitor. Taisho Pharmaceutical quickly received a patent for a new antibiotic and launched a branded drug called Clarit for the Japanese market. Five years later, in 1985, Taisho, in collaboration with the American pharmaceutical giant Abbott, launched the first clarithromycin for the European and American market. In Russia, he received the name Klacid. Until 2004, Klacid had no competitors - it was produced as a brand, until the patent expired. And only after that, pharmacies were flooded with its analogues, or generics - drugs with the same active substance issued by companies not related to its creation. For consumers, this meant only one thing: the monopoly of Klacid, a rather expensive drug, was over forever, and from now on Clarithromycin becomes available to a wide range of patients. Well, now let's move on to a closer acquaintance with him.

>>Recommended: if you are interested effective methods getting rid of chronic rhinitis, pharyngitis, tonsillitis, bronchitis and constant colds, then be sure to look at this website page after reading this article. The information is based on personal experience the author and helped many people, we hope it will help you. Now back to the article.<<

How it works?

The principle of action of Clarithromycin is based on its bacteriostatic and bactericidal properties against a wide range of microorganisms. The drug binds strongly to a specific subunit of the microbe and irreversibly inhibits protein synthesis, which leads to the death of the bacterial cell.

Many gram-positive and gram-negative microorganisms are sensitive to Clarithromycin, including:

• Staphylococcus aureus, the causative agent of many respiratory diseases;
• pneumoniae streptococcus, responsible for the development of pneumonia and other diseases;
• pyogenic and other types of pathogenic streptococcus;
• hemophilic bacillus;
• moraxella;
• bordetella, the causative agent of whooping cough;
• legionella, which causes legionellosis;
• clostridia;
• mycobacteria;
• Pseudomonas aeruginosa and others.

Separately, I would like to emphasize that Clarithromycin is one of the few existing antibiotics that can penetrate into the bacterial cell.

This unique property inherent in macrolides allows the drug to remain active against intracellular pathogens that are indifferent to the action of most antibiotics. Indications for the use of Clarithromycin are also based on the spectrum of activity.

When is Clarithromycin used?

The antibiotic is a second-line drug for the treatment of many respiratory tract infections, including pneumonia, bacterial tonsillitis (tonsillitis). This means that patients who, for some reason, are contraindicated in drugs of choice - penicillin antibiotics, for example, Amoxicillin or its protected combination with clavulanic acid, are prescribed macrolides, and in most cases the choice falls on Clarithromycin (or Azithromycin).

The drug is also used for (including sinusitis), bacterial bronchitis, SARS, infections of the skin or soft tissues (for example, furunculosis), otitis media. An important field of application of Clarithromycin is venereology: macrolide antibiotics are indispensable for urogenital chlamydia and mycoplasmosis. The unique ability of Clarithromycin to have a bactericidal effect against Helicobacter pylori infection determines its use in gastroenterology for the treatment of peptic ulcer. In addition, the antibiotic is active against Bartonella, the bacteria that causes cat-scratch fever, and therefore it is prescribed to treat this disease.

Pharmacokinetic properties: studying the instructions for Clarithromycin

Pharmacokinetics studies the behavior of a drug in the human body: how and when it is absorbed, how it is excreted, and so on. It depends on the pharmacokinetic characteristics of the drug whether it is possible to take the drug (in our case, Clarithromycin) with food and how often it should be drunk.

The instructions for use of Clarithromycin indicate that the tablets are quickly absorbed from the gastrointestinal tract. Exactly half of the drug reaches the destination and begins to work - the remaining 50% are excreted from the body. Food greatly slows down the absorption of the drug, but its bioavailability is not affected. This means that even if you take a pill during a heavy meal, the entire dose taken will be absorbed.

A stable concentration of the drug in the blood plasma is achieved only after 2-3 days of continuous use, that is, approximately 72 hours after the start of treatment with Clarithromycin, its level will reach a constantly high value, which is necessary to obtain the most pronounced antibacterial effect.

Release forms

The drug is used orally (from the Latin per os - through the mouth) and parenterally - intravenously drip (in "droppers"). Clarithromycin is available as:

• capsules (500 and 250 mg);
• tablets of long, or prolonged action (500 mg each);
• conventional tablets (250 and 500);
• lyophilized powder, from which an infant suspension is prepared;
• solution for intravenous drip.

The average consumer, as a rule, is concerned about whether different forms of a drug differ in effectiveness. Indeed, why are Clarithromycin tablets better or worse than its capsules? Or what features do prolonged dosage forms have?

So, we answer. Tablets of various shapes and colors, coated or uncoated with shells or films, and capsules practically do not differ from each other, with the exception of visual characteristics. All these wisdoms - coatings or capsule shells - reflect only the features of the production of a pharmaceutical company. The exception is Clarithromycin extended-release tablets. When creating them, a special technology is used that allows for a slower release of the antibiotic into the blood. Thanks to this nuance, it is possible to achieve a constantly high concentration of the drug while reducing the frequency of its dosing.

Part tablets Clarithromycin includes an active ingredient clarithromycin , as well as additional components: MCC, potato starch, pregelatinized starch, low molecular weight PVP, colloidal silicon dioxide, magnesium stearate, sodium lauryl sulfate.

Part capsules Clarithromycin also contains the active ingredient clarithromycin , as well as additional components: corn starch, lactose monohydrate, povidone, croscarmellose sodium, calcium stearate, polysorbate 80. The hard capsule consists of gelatin and titanium dioxide.

Release form

Side effects

During the course of treatment, the following side effects may occur:

• nervous system: , fear, bad dreams, , feeling of anxiety; in rare cases - , disturbances of consciousness, psychosis ;
• digestion: vomit, nausea , gastralgia , cholestatic jaundice, , an increase in the activity of hepatic transaminases, in rare cases, pseudomembranous enterocolitis manifests itself;
• hematopoiesis, hemostatic system: in rare cases - thrombocytopenia ;
• sense organs: tinnitus, taste disturbance, isolated cases of hearing loss after the drug was canceled;
• allergy: and skin rash, anaphylactoid reactions, Stevens-Johnson syndrome;
• other actions: manifestation of resistance of microorganisms.

Instructions for use Clarithromycin (Method and dosage)

Instructions for use Clarithromycin Teva provides that adults and children over 12 years of age take, depending on the diagnosis, 250-500 mg twice a day. Therapy lasts from 6 to 14 days.

If the patient is diagnosed with a severe infection or oral administration of the drug is impossible for some reason, clarithromycin is given IV, the dose is 500 mg per day. The drug is taken for 2 to 5 days, after which, if possible, the patient is transferred to oral medication. In general, the treatment lasts up to 10 days.

If the remedy is prescribed for the treatment of diseases provoked by Mycobacterium avium, as well as severe infections (including those provoked haemophilus influenzae), shows the reception of 0.5-1 g of the drug twice a day. The largest daily dose is 2 g. Treatment can last about 6 months.

People with chronic renal failure receive a single dose of 250 mg per day, if a severe infection is diagnosed, 250 mg is prescribed twice a day. Treatment can last up to 14 days.

Overdose

If an overdose occurs, the patient may experience problems with the function of the gastrointestinal tract, impaired consciousness, headaches. In this case, gastric lavage is performed and, if necessary, symptomatic treatment is prescribed.

Interaction

Do not use Clarithromycin concomitantly with pimozide , Terfenadine and cisapride .

Taking with indirect anticoagulants, drugs that are metabolized in the liver with the help of cytochrome P450, as well as with , Cisapride, Carbamazepine, Terfenadine, , Triazolam, Disopyramide, Lovastatin, , Midazolam, ergot alkaloids, , Phenytoin concentration of these drugs in the blood increases.

Clarithromycin reduces absorption Zidovudine .

Cross-resistance may develop between Clarithromycin, and Lincomycin.

It reduces the rate of Astemizol, therefore, with simultaneous use, an increase in the QT interval may develop, the risk of ventricular arrhythmia of the "pirouette" type increases.

increases significantly the concentration in omeprazole and slightly - Clarithromycin.

If the drug is used concomitantly with pimozide , the concentration of the latter increases, which increases the likelihood of severe cardiotoxic effects.

Application with Tolbutamide increases the risk of hypoglycemia.

When used simultaneously with possible toxic effects.

Terms of sale

You can buy in a pharmacy with a doctor's prescription, a specialist gives a prescription in Latin.

Storage conditions

It is necessary to protect Clarithromycin from moisture and light, the storage temperature is not more than 25 ° C.

Keep out of reach of children.

Best before date

You can keep the medicine for 2 years. Do not apply after this period.

special instructions

If the patient is diagnosed with chronic diseases, he must definitely control the enzymes of the blood serum.

Carefully, the remedy is prescribed when taking drugs, the metabolism of which takes place in the liver.

There is cross-resistance between antibacterial drugs that belong to the group of macrolides.

During antibiotic therapy, normal intestines changes, so the likelihood of manifestation should be taken into account superinfection caused by resistant microorganisms.

It should be borne in mind that a severe manifestation may be associated with pseudomembranous colitis.

For children, to facilitate the administration of the drug, a suspension can be prescribed, the active substance of which is clarithromycin.

Analogues of Clarithromycin

The price of Clarithromycin analogues depends on their manufacturer and other factors. Analogues of this drug are means Clarithromycin Teva , Arvicin , , Clarexide , Zimbaktar , Clarithrosin , and etc.

children

In pediatrics, the drug can be used for children after 6 months of age. The most commonly used suspension for children, the active ingredient of which is clarithromycin. The application should be carried out strictly according to the scheme prescribed by the doctor.

During pregnancy and lactation

In the first trimester, this antibiotic should not be used. In the following months of pregnancy, it is possible to use the remedy only if the doctor correlates the expected benefits for the woman and harm to the fetus. During lactation, if you need to take medication, you need to stop breastfeeding.

Reviews about Clarithromycin

Patients leave different reviews about Clarithromycin online. It is often written that with the help of an antibiotic it was possible to get rid of the symptoms of infectious diseases in a few days. However, there are many opinions about the fact that the drug provokes the manifestation of a large number of side effects, in particular, headaches, digestive problems, imbalance of intestinal microflora. In most cases, it is noted that it is advisable to drink the medicine only on prescription and according to the scheme prescribed by the specialist.

Clarithromycin price, where to buy

The price of Clarithromycin 250 mg tablets is an average of 120 rubles per pack of 10 pcs. Price Clarithromycin 500 mg - an average of 240 rubles per pack. 10 pieces. You can buy a medicine in Ukraine (Kyiv, Kharkov, etc.) at a price of 50 UAH. For 10 pcs. The price of Clarithromycin IV (Klacid drug) averages 600 rubles.

• Internet pharmacies in Russia Russia
• Internet pharmacies of Ukraine Ukraine

ZdravCity

Clarithromycin tablets p.p.o. 500mg №10 Ozone Ozone LLC

Clarithromycin-Acrichin tab. p / o captivity. 250mg #10Micro Labs Limited

Clarithromycin caps. 250mg n14 Vertex JSC

Clarithromycin tablets p.p.o. 500mg №10 Dalhimpharm OJSC Dalhimfarm

Clarithromycin tab. po 250mg n10 Ozone LLC

Pharmacy Dialog

Clarithromycin SR tablets 500mg №7

Clarithromycin (caps. 250mg #14)

Antibiotics - macrolides and azalides.

Composition Clarithromycin

The active substance is Clarithromycin.

Manufacturers

Vertex CJSC (Russia)

pharmachologic effect

Antibacterial (bacteriostatic), antiulcer.

When taken orally, it is quickly and fairly completely absorbed.

Food slows absorption without significantly affecting bioavailability.

In plasma, it binds to serum proteins.

It is immediately oxidized in the liver to form the main metabolite 14-hydroxyclarithromycin (it has a pronounced antimicrobial activity against Haemophilus influenzae).

It penetrates well into body fluids and tissues, creating concentrations 10 times higher than the level in blood serum.

It is excreted in the urine in unchanged form and as metabolites. It is active against intracellular microorganisms (Mycoplasma pneumoniae, Legionella pneumophila, Chlamydia trachomatis and Chlamydia pneumoniae, Ureaplasma urealyticum), gram-positive (Streptococcus spp. and Staphylococcus spp., Listeria monocytogenes, Corynebacterium spp.) and gram-negative bacteria (Haemophilus influenzae and Haemophilus ducreyi, Moraxella catarrhalis, Bordetella pertussis, Neisseria meningitidis, Borrelia burgdorferi, Pasteurella multocida, Campylobacter spp., Helicobacter pylori), some anaerobes (Eubacterium spp., Peptococcus spp., Propionibacterium spp., Clostridium spp. , Bacteroides melaninogenicus), Toxoplasma gondii and all mycobacteria except V.tuberculosis.

Side effects of Clarithromycin

Nausea, vomiting, change in taste, pain in the abdomen, diarrhea, pseudomembranous colitis, stomatitis, glossitis, dizziness, headache, anxiety, fear, insomnia, nightmares, increased liver enzymes, cholestatic jaundice, allergic (urticaria, Stevens syndrome - Johnson and others) and anaphylactoid reactions.

Indications for use

Infections of the upper respiratory tract and ENT organs (tonsillopharyngitis, otitis media, acute sinusitis), lower respiratory tract (acute bronchitis, exacerbation of chronic bronchitis, bacterial and atypical pneumonia), skin and soft tissues, mycobacterial infection (M.avium complex, M. cansasii, M.marinom, M.leprae), peptic ulcer of the duodenum and stomach caused by Helicobacter pylori (combination therapy).

Contraindications Clarithromycin

Hypersensitivity, severe liver disease, porphyria, pregnancy and lactation.

Method of application and dosage

For adults, the average oral dose is 250 mg 2 times a day.

If necessary, you can assign 500 mg 2 times a day.

The duration of the course of treatment is 6-14 days.

For children, the drug is prescribed at a dose of 7.5 mg / kg / body weight / day.

The maximum daily dose is 500 mg.

The duration of the course of treatment is 7-10 days.

For the treatment of infections caused by Mycobacterium avium, clarithromycin is prescribed orally - 1 g 2 times a day.

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 the drug should be reduced by 2 times.

The maximum duration of the course in patients of this group should be no more than 14 days.

Overdose

Symptoms:

• nausea,
• vomiting,
• diarrhea. Treatment: gastric lavage,
• symptomatic therapy.

Hemodialysis and peritoneal dialysis are not effective.

Interaction

Increases the concentration in the blood of drugs metabolized in the liver with the participation of enzymes of the cytochrome complex P450:

• warfarin and other indirect anticoagulants,
• carbamazepine,
• theophylline,
• astemizole,
• cisapride,
• thiazolam,
• midazolam,
• cyclosporine,
• digoxin,
• ergot alkaloids, etc.
• reduces the absorption of zidovudine.

special instructions

It is prescribed with caution against the background of drugs metabolized by the liver (it is recommended to measure their concentration in the blood).

In the case of combination with warfarin or other indirect anticoagulants, it is necessary to control the prothrombin time.

Storage conditions

List B.

In a place protected from light, at room temperature.

Clarithromycin is an antibiotic from the group of macrolides, which has a bacteriostatic, and in high concentrations, a bactericidal effect associated with the suppression of protein synthesis in microorganism cells due to the binding of the drug to the 50S subunit of bacterial ribosomes. Sensitivity to clarithromycin is shown by many microorganisms, including intracellular (Chlamydia pneumoniae, Chlamydia trachomatis, (Mycoplasma pneumoniae, Ureaplasma urealyticum, Legionella pneumophila), gram-positive (Staphylococcus spp., Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus pyogenes), Corynebacterium spp. , Listeria monocytogenes) and gram-negative (Haemophilus parainfluenzae, Haemophilus influenzae, Haemophilus ducreyi, Helicobacter pylori, Moraxella catarrhalis, Pasteurella multocida, Neisseria meningitidis, Bordetella pertussis, Campylobacter spp., Borrelia burgdorferi) representatives of human bacterial microflora, a number of anaerobes (Mycoplasma pneumoniae, spp., Eubacterium spp., Clostridium perfringens, Propionibacterium spp., Toxoplasma gondii, Bacteroides melaninogenicus), as well as mycobacteria (Mycobacterium avium complex, including Mycobacterium intracellulare and Mycobacterium avium).

Clarithromycin is rapidly absorbed from the gastrointestinal tract, and if the drug was taken after a heavy snack, then, naturally, its absorption will be reduced.

However, in the end, this does not affect the bioavailability of this antibiotic: its stable concentration in the blood will be established on the 2-3rd day from the start of administration. Elderly patients take clarithromycin without any restrictions, unless, of course, they experience serious kidney problems. But liver problems do not affect the dosing regimen of clarithromycin in any way and do not require dose adjustment.

Clarithromycin is available in tablets. For adults and children over 12 years of age, a single dose is 250-500 mg twice a day. The duration of treatment is 1-2 weeks. The presence of a patient's history of chronic liver disease makes monitoring of serum enzymes mandatory when taking clarithromycin. Cross-resistance between this drug, clindamycin and lincomycin is likely, so some microorganisms resistant to the last two antibiotics may be insensitive to clarithromycin. Long-term and repeated use of the drug can provoke the resistance of both bacterial and fungal microflora, which can lead to a secondary infection. In such cases, the drug should be stopped and switched to a different method of antibiotic therapy.

Pharmacology

Semi-synthetic macrolide antibiotic. Suppresses the synthesis of proteins in the microbial cell, interacting with the 50S ribosomal subunit of bacteria. It acts mainly bacteriostatically, as well as bactericidal.

Active against gram-positive bacteria: Streptococcus spp., Staphylococcus spp., Listeria monocytogenes, Corynebacterium spp.; gram-negative bacteria: Helicobacter pylori, Haemophilus influenzae, Haemophilus ducreyi, Moraxella catarrhalis, Bordetella pertussis, Neisseria gonorrhoeae, Neisseria meningitidis, Borrelia burgdorferi; anaerobic bacteria: Eubacterium spp., Peptococcus spp., Propionibacterium spp., Clostridium perfringens, Bacteroides melaninogenicus; intracellular microorganisms: Legionella pneumophila, Chlamydia trachomatis, Chlamydophila pneumoniae, Ureaplasma urealyticum, Mycoplasma pneumoniae.

It is also active against Toxoplasma gondii, Mycobacterium spp. (except for Mycobacterium tuberculosis).

Pharmacokinetics

When administered orally, clarithromycin is well absorbed from the gastrointestinal tract. Eating slows down absorption, but does not affect the bioavailability of the active substance.

Clarithromycin penetrates well into biological fluids and tissues of the body, where it reaches a concentration 10 times higher than in plasma.

Approximately 20% of clarithromycin is immediately metabolized to form the main metabolite 14-hydroclarithromycin.

At a dose of 250 mg T 1/2 is 3-4 hours, at a dose of 500 mg - 5-7 hours.

It is excreted in the urine unchanged and as metabolites.

Release form

Tablets, film-coated, white, oval, biconvex.

Excipients: pregelatinized starch 100.8 mg, microcrystalline cellulose 68 mg, croscarmellose sodium 38 mg, povidone (K-30) 38 mg, colloidal silicon dioxide 7.6 mg, magnesium stearate 7.6 mg.

The composition of the film shell: Opadry II white 22 mg, including polyvinyl alcohol, titanium dioxide, macrogol, talc.

7 pcs. - blister packs (aluminum/PVC) (1) - cardboard packs.
7 pcs. - blister packs (aluminum/PVC) (2) - cardboard packs.
10 pieces. - blister packs (aluminum/PVC) (1) - cardboard packs.
10 pieces. - blister packs (aluminum/PVC) (2) - cardboard packs.
12 pcs. - blister packs (aluminum/PVC) (1) - cardboard packs.
12 pcs. - blister packs (aluminum/PVC) (2) - cardboard packs.

Dosage

Individual. When taken orally for adults and children over 12 years of age, a single dose is 0.25-1 g, the frequency of administration is 2 times / day.

For children under 12 years of age, the daily dose is 7.5-15 mg / kg / day in 2 divided doses.

In children, clarithromycin should be used in the appropriate dosage form intended for this category of patients.

The duration of treatment depends on the indications.

Maximum daily doses: for adults - 2 g, for children - 1 g.

Interaction

Clarithromycin inhibits the activity of the CYP3A4 isoenzyme, which leads to a slowdown in the rate of metabolism of astemizole with their simultaneous use. As a result, there is an increase in the QT interval and an increased risk of developing ventricular arrhythmia of the "pirouette" type.

Simultaneous administration of clarithromycin with lovastatin or simvastatin is contraindicated due to the fact that these statins are largely metabolized by the CYP3A4 isoenzyme, and combined use with clarithromycin increases their serum concentrations, which leads to an increased risk of myopathy, including rhabdomyolysis. Cases of rhabdomyolysis have been reported in patients taking clarithromycin concomitantly with these drugs. If clarithromycin is required, lovastatin or simvastatin should be discontinued for the duration of therapy.

Clarithromycin should be used with caution in combination therapy with other statins. It is recommended to use statins that do not depend on the metabolism of the CYP3A isoenzyme (for example, fluvastatin). If co-administration is necessary, it is recommended to take the lowest dose of the statin. The development of signs and symptoms of myopathy should be monitored. With simultaneous use with atorvastatin, the concentration of atorvastatin in the blood plasma moderately increases, and the risk of developing myopathy increases.

Drugs that are CYP3A inducers (eg, rifampicin, phenytoin, carbamazepine, phenobarbital, St. It is necessary to control the plasma concentration of the CYP3A inducer, which may increase due to inhibition of CYP3A by clarithromycin.

When combined with rifabutin, the concentration of rifabutin in the blood plasma increases, the risk of developing uveitis increases, and the concentration of clarithromycin in the blood plasma decreases.

When combined with clarithromycin, an increase in plasma concentrations of phenytoin, carbamazepine, valproic acid is possible.

Strong inducers of isoenzymes of the cytochrome P450 system, such as efavirenz, nevirapine, rifampicin, rifabutin and rifapentine, can accelerate the metabolism of clarithromycin and, thus, lower the plasma concentration of clarithromycin and weaken its therapeutic effect, and at the same time increase the concentration of 14-OH-clarithromycin - metabolite, which is also microbiologically active. Since the microbiological activity of clarithromycin and 14-OH-clarithromycin differs in relation to different bacteria, the therapeutic effect may be reduced when clarithromycin and enzyme inducers are used together.

Plasma concentration of clarithromycin decreases with the use of etravirine, while the concentration of the active metabolite 14-OH-clarithromycin increases. Since 14-OH-clarithromycin has low activity against MAC infections, the overall activity against their pathogens may change, so an alternative treatment should be considered for the treatment of MAC.

A pharmacokinetic study showed that co-administration of ritonavir 200 mg every 8 hours and clarithromycin 500 mg every 12 hours resulted in a marked suppression of clarithromycin metabolism. When co-administered with ritonavir, C max of clarithromycin increased by 31%, C min increased by 182% and AUC increased by 77%, while the concentration of its metabolite 14-OH-clarithromycin was significantly reduced. Ritonavir should not be co-administered with clarithromycin at doses greater than 1 g/day.

Clarithromycin, atazanavir, saquinavir are substrates and inhibitors of CYP3A, which determines their bidirectional interaction. When saquinavir is co-administered with ritonavir, the potential effect of ritonavir on clarithromycin should be considered.

With simultaneous use with zidovudine, the bioavailability of zidovudine is slightly reduced.

Colchicine is a substrate for both CYP3A and P-glycoprotein. Clarithromycin and other macrolides are known to be inhibitors of CYP3A and P-glycoprotein. When clarithromycin and colchicine are co-administered, inhibition of P-glycoprotein and/or CYP3A may lead to an increased effect of colchicine. The development of clinical symptoms of colchicine poisoning should be monitored. There have been post-marketing reports of cases of colchicine poisoning when taken concomitantly with clarithromycin, more often in elderly patients. Some of the reported cases have occurred in patients with renal insufficiency. Some cases have been reported to have resulted in death. The simultaneous use of clarithromycin and colchicine is contraindicated.

With the combined use of midazolam and clarithromycin (500 mg orally 2 times / day), an increase in the AUC of midazolam was noted: 2.7 times after intravenous administration of midazolam and 7 times after oral administration. Co-administration of clarithromycin with oral midazolam is contraindicated. If intravenous midazolam is used with clarithromycin, the patient should be carefully monitored for possible dose adjustments. The same precautions should be applied to other benzodiazepines that are metabolized by CYP3A, including triazolam and alprazolam. For benzodiazepines whose excretion is independent of CYP3A (temazepam, nitrazepam, lorazepam), a clinically significant interaction with clarithromycin is unlikely.

With the combined use of clarithromycin and triazolam, effects on the central nervous system, such as drowsiness and confusion, are possible. With this combination, it is recommended to monitor the symptoms of CNS disorders.

With simultaneous use with warfarin, it is possible to increase the anticoagulant effect of warfarin and increase the risk of bleeding.

It is assumed that digoxin is a substrate for P-glycoprotein. Clarithromycin is known to inhibit P-glycoprotein. With simultaneous use with digoxin, a significant increase in the concentration of digoxin in the blood plasma and the risk of developing glycoside intoxication are possible.

Perhaps the occurrence of ventricular tachycardia type "pirouette" with the combined use of clarithromycin and quinidine or disopyramide. While taking clarithromycin with these drugs, regular ECG monitoring should be carried out for an increase in the QT interval, and serum concentrations of these drugs should also be monitored. In post-marketing use, cases of hypoglycemia have been reported with the co-administration of clarithromycin and disopyramide. It is necessary to control the concentration of glucose in the blood while using clarithromycin and disopyramide. It is believed that it is possible to increase the concentration of disopyramide in the blood plasma due to inhibition of its metabolism in the liver under the influence of clarithromycin.

Co-administration of fluconazole at a dose of 200 mg daily and clarithromycin at a dose of 500 mg 2 times / day caused an increase in the average value of the minimum equilibrium concentration of clarithromycin (C min) and AUC by 33% and 18%, respectively. At the same time, co-administration did not significantly affect the average equilibrium concentration of the active metabolite 14-OH-clarithromycin. Dose adjustment of clarithromycin is not required in case of concomitant use of fluconazole.

Clarithromycin and itraconazole are substrates and inhibitors of CYP3A, which determines their bidirectional interaction. Clarithromycin may increase plasma concentrations of itraconazole, while itraconazole may increase plasma concentrations of clarithromycin.

With simultaneous use with methylprednisolone, the clearance of methylprednisolone decreases; with prednisone - cases of development of acute mania and psychosis are described.

With simultaneous use with omeprazole, the concentration of omeprazole increases significantly and the concentration of clarithromycin in the blood plasma slightly increases; with lansoprazole - glossitis, stomatitis and / or the appearance of a dark color of the tongue are possible.

With simultaneous use with sertraline, the development of serotonin syndrome cannot theoretically be excluded; with theophylline - it is possible to increase the concentration of theophylline in the blood plasma.

With simultaneous use with terfenadine, it is possible to slow down the rate of metabolism of terfenadine and increase its concentration in blood plasma, which can lead to an increase in the QT interval and an increased risk of developing ventricular arrhythmia of the "pirouette" type.

Inhibition of the activity of the isoenzyme CYP3A4 under the influence of clarithromycin leads to a slowdown in the rate of metabolism of cisapride with their simultaneous use. As a result, the concentration of cisapride in the blood plasma increases and the risk of developing life-threatening cardiac arrhythmias, including ventricular arrhythmias of the "pirouette" type, increases.

The primary metabolism of tolterodine is carried out with the participation of CYP2D6. However, in the part of the population lacking CYP2D6, metabolism occurs with the participation of CYP3A. In this population, suppression of CYP3A results in significantly higher serum concentrations of tolterodine. Therefore, in patients with low levels of CYP2D6-mediated metabolism, a dose reduction of tolterodine may be required in the presence of CYP3A inhibitors such as clarithromycin.

With the combined use of clarithromycin and oral hypoglycemic agents (for example, sulfonylurea derivatives) and / or insulin, severe hypoglycemia may occur. Concomitant use of clarithromycin with certain hypoglycemic drugs (eg, nateglinide, pioglitazone, repaglinide and rosiglitazone) may lead to inhibition of the CYP3A isoenzyme by clarithromycin, which may lead to the development of hypoglycemia. It is believed that with simultaneous use with tolbutamide, there is a possibility of developing hypoglycemia.

With simultaneous use with fluoxetine, a case of the development of toxic effects caused by the action of fluoxetine is described.

While taking clarithromycin with other ototoxic drugs, especially aminoglycosides, care must be taken and the functions of the vestibular and hearing aids should be monitored both during and after therapy.

With simultaneous use with cyclosporine, the concentration of cyclosporine in the blood plasma increases, there is a risk of increased side effects.

With simultaneous use with ergotamine, dihydroergotamine, cases of increased side effects of ergotamine and dihydroergotamine are described. Post-marketing studies show that when clarithromycin is co-administered with ergotamine or dihydroergotamine, the following effects associated with acute poisoning with ergotamine group drugs are possible: vascular spasm, ischemia of the extremities and other tissues, including the central nervous system. The concomitant use of clarithromycin and ergot alkaloids is contraindicated.

Each of these PDE inhibitors is metabolized, at least in part, with the participation of CYP3A. At the same clarithromycin is able to inhibit CYP3A. Co-administration of clarithromycin with sildenafil, tadalafil, or vardenafil may result in an increased inhibitory effect on PDE. With these combinations, dose reduction of sildenafil, tadalafil and vardenafil should be considered.

With the simultaneous use of clarithromycin and calcium channel blockers that are metabolized by the CYP3A4 isoenzyme (for example, verapamil, amlodipine, diltiazem), caution should be exercised, since there is a risk of arterial hypotension. Plasma concentrations of clarithromycin, as well as calcium channel blockers, may increase with simultaneous use. Arterial hypotension, bradyarrhythmia and lactic acidosis are possible while taking clarithromycin and verapamil.

Side effects

From the digestive system: often - diarrhea, vomiting, dyspepsia, nausea, pain in the abdomen; infrequently - esophagitis, gastroesophageal reflux disease, gastritis, proctalgia, stomatitis, glossitis, bloating, constipation, dry mouth, belching, flatulence, increased blood bilirubin concentration, increased activity of ALT, ACT, GGT, alkaline phosphatase, LDH, cholestasis, hepatitis , incl. cholestatic and hepatocellular; frequency unknown - acute pancreatitis, discoloration of the tongue and teeth, liver failure, cholestatic jaundice.

Allergic reactions: often - rash; infrequently - anaphylactoid reaction, hypersensitivity, bullous dermatitis, itching, urticaria, maculo-papular rash; frequency unknown - anaphylactic reaction, angioedema, Stevens-Johnson syndrome, toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms (DRESS syndrome).

From the nervous system: often - headache, insomnia; infrequently - loss of consciousness, dyskinesia, dizziness, drowsiness, tremor, anxiety, irritability; frequency unknown - convulsions, psychotic disorders, confusion, depersonalization, depression, disorientation, hallucinations, nightmares, paresthesia, mania.

From the side of the skin: often - intense sweating; frequency unknown - acne, hemorrhages.

From the senses: often - dysgeusia, taste perversion; infrequently - vertigo, hearing loss, ringing in the ears; frequency unknown - deafness, ageusia, parosmia, anosmia.

From the side of the cardiovascular system: often - vasodilation; infrequently - cardiac arrest, atrial fibrillation, prolongation of the QT interval on the ECG, extrasystole, atrial flutter; frequency unknown - ventricular tachycardia, incl. pirouette type.

From the urinary system: infrequently - an increase in the concentration of creatinine, a change in the color of urine; frequency unknown - renal failure, interstitial nephritis.

On the part of metabolism and nutrition: infrequently - anorexia, decreased appetite, increased urea concentration, changes in the albumin-globulin ratio

From the musculoskeletal system: infrequently - muscle spasm, musculoskeletal stiffness, myalgia; frequency unknown - rhabdomyolysis, myopathy.

From the respiratory system: infrequently - asthma, epistaxis, pulmonary embolism.

From the hemopoietic system: infrequently - leukopenia, neutropenia, eosinophilia, thrombocythemia; frequency unknown - agranulocytosis, thrombocytopenia.

From the blood coagulation system: infrequently - an increase in the value of MHO, prolongation of prothrombin time.

Local reactions: very often - phlebitis at the injection site, often - pain at the injection site, inflammation at the injection site.

On the part of the body as a whole: infrequently - malaise, hyperthermia, asthenia, chest pain, chills, fatigue.

Indications

Treatment of infectious and inflammatory diseases caused by pathogens sensitive to clarithromycin: infections of the upper respiratory tract and upper respiratory tract (tonsillopharyngitis, otitis media, acute sinusitis); infections of the lower respiratory tract (acute bronchitis, exacerbation of chronic bronchitis, community-acquired bacterial and atypical pneumonia); odontogenic infections; skin and soft tissue infections; mycobacterial infections (M.avium complex, M.kansasii, M.marinum, M.leprae) and their prevention in AIDS patients; eradication of Helicobacter pylori in patients with duodenal ulcer or gastric ulcer (only as part of combination therapy).

Contraindications

A history of QT prolongation, ventricular arrhythmia, or torsades de pointes; hypokalemia (risk of prolongation of the QT interval); severe liver failure occurring simultaneously with renal failure; cholestatic jaundice/hepatitis in history, developed during the use of clarithromycin; porphyria; I trimester of pregnancy; lactation period (breastfeeding); simultaneous administration of clarithromycin with astemizole, cisapride, pimozide, terfenadine; with ergot alkaloids, eg ergotamine, dihydroergotamine; with midazolam for oral administration; with HMG-CoA reductase inhibitors (statins), which are largely metabolized by the CYP3A4 isoenzyme (lovastatin, simvastatin), with colchicine; with ticagrelor or ranolazine; hypersensitivity to clarithromycin and other macrolides.

Application features

Use during pregnancy and lactation

Use in the first trimester of pregnancy is contraindicated.

Application in the II and III trimesters of pregnancy is possible only in cases where the intended benefit to the mother outweighs the potential risk to the fetus.

If necessary, use during lactation should stop breastfeeding.

Application for violations of liver function

Application for violations of kidney function

Use in children

special instructions

Clarithromycin should be used with caution in patients with moderate to severe renal impairment; liver failure of moderate and severe degree, with coronary artery disease, severe heart failure, hypomagnesemia, severe bradycardia (less than 50 bpm); simultaneously with benzodiazepines, such as alprazolam, triazolam, midazolam for intravenous administration; simultaneously with other ototoxic drugs, especially aminoglycosides; simultaneously with drugs that are metabolized by the CYP3A isoenzyme (including carbamazepine, cilostazol, cyclosporine, disopyramide, methylprednisolone, omeprazole, indirect anticoagulants, quinidine, rifabutin, sildenafil, tacrolimus, vinblastine; simultaneously with CYP3A4 inducers (including rifampicin , phenytoin, carbamazepine, phenobarbital, St. John's wort); simultaneously with statins, the metabolism of which does not depend on the CYP3A isoenzyme (including fluvastatin); simultaneously with blockers of slow calcium channels, which are metabolized by the CYP3A4 isoenzyme (including verapamil, amlodipine, diltiazem); simultaneously with class I A antiarrhythmic drugs (quinidine, procainamide) and class III (dofetilide, amiodarone, sotalol).

There is cross-resistance between macrolide antibiotics.

Antibiotic treatment alters the normal intestinal flora, so superinfection caused by resistant microorganisms is possible.

It should be borne in mind that severe persistent diarrhea may be due to the development of pseudomembranous colitis.

Prothrombin time should be monitored periodically in patients receiving clarithromycin concomitantly with warfarin or other oral anticoagulants.