Universal reference book for medicines
Product name: SEYDON-SANOVEL (SEIDON-SANOVEL)

Active substance: clarithromycin

Type: Macrolide antibiotic

Manufacturer: SANOVEL PHARMACEUTICAL PRODUCTS Ind.
(Turkey)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

PHARMACHOLOGIC EFFECT
Semisynthetic antibiotic group of macrolides.
Suppresses the synthesis of proteins in a microbial cell, interacting with the 50S ribosomal subunit of bacteria. Acts mainly bacteriostatically, as well as bactericidal.
It is 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 Mycobacterium tuberculosis).
PHARMACOKINETICS
When administered orally, clarithromycin is well absorbed from the digestive tract.
Eating slows down absorption, but does not affect the bioavailability of the active substance.
Clarithromycin penetrates well into biological fluids and body tissues, where it reaches a concentration 10 times greater than in plasma.

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

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

It is excreted in the urine in unchanged form and in the form of metabolites.

INDICATIONS
Treatment of infectious and inflammatory diseases caused by pathogens sensitive to clarithromycin: infections of the upper respiratory tract and ENT organs (tonsillopharyngitis, otitis media, acute sinusitis);
infection of the lower respiratory tract (acute bronchitis, exacerbation of chronic bronchitis, community-acquired bacterial and atypical pneumonia); odontogenic infections; infections of the skin and soft tissues; mycobacterial infections (M.avium complex, M. kansasii, M.marinum, M. leprae) and their prophylaxis in AIDS patients; eradication of Helicobacter pylori in patients with duodenal ulcer or stomach ulcer (only in combination therapy).
DOSING MODE
Individual.
When administered orally for adults and children over 12 years of age, the single dose is 0.25-1 g, the frequency of admission 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.

Patients with impaired renal function (QC less than 30 ml / min or serum creatinine level more than 3.3 mg / dl) should be reduced by a factor of 2 or doubled between doses.

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

SIDE EFFECT
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, eructation, flatulence, increased bilirubin concentration in the blood, increased activity of ALT, ACT, GGT, LSG, LDH, cholestasis, hepatitis , incl. Cholestatic and hepatocellular; frequency unknown - acute pancreatitis, discoloration of the tongue and teeth, hepatic insufficiency, cholestatic jaundice.
Allergic reactions: often - a rash;
infrequently - anaphylactoid reaction, hypersensitivity, bullous dermatitis, pruritus, urticaria, maculopapular rash; frequency unknown - anaphylactic reaction, angioedema, Stevens-Johnson syndrome, toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptomatology (DRESS syndrome).
From the nervous system: often - headache, insomnia;
infrequently - loss of consciousness, dyskinesia, dizziness, drowsiness, tremor, anxiety, increased excitability;frequency unknown - convulsions, psychotic disorders, confusion, depersonalization, depression, disorientation, hallucinations, nightmares, paresthesia, mania.
On the part of the skin: often - intense sweating;
frequency is unknown - acne, hemorrhages.
From the senses: often - dysgeusia, perversion of taste;
infrequently - vertigo, hearing impairment, ringing in the ears; frequency is unknown - deafness, agesia, parosmia, anosmia.
From the cardiovascular system: often - vasodilation;
infrequently - cardiac arrest, atrial fibrillation, prolongation of QT interval on ECG, extrasystole, atrial flutter;frequency unknown - ventricular tachycardia, incl. type "pirouette".
From the side of the urinary system: infrequently - increased concentration of creatinine, a change in the color of urine;
frequency unknown - renal failure, interstitial nephritis.
From the side of metabolism and nutrition: infrequently - anorexia, decreased appetite, increased urea concentration, a change in the albumin-globulin ratio.

From the musculoskeletal system: infrequently - muscle spasm, musculoskeletal stiffness, myalgia;
frequency unknown - rhabdomyolysis, myopathy.
On the part of the respiratory system: infrequently - asthma, epistaxis, thromboembolism of the pulmonary artery.

On the part of the hematopoiesis system: infrequently - leukopenia, neutropenia, eosinophilia, thrombocythemia;
frequency unknown - agranulocytosis, thrombocytopenia.
From the coagulation system of the blood: infrequently - increase in the value of MHO, lengthening of prothrombin time.

Infectious and parasitic diseases: infrequently - cellulitis, candidiasis, gastroenteritis, secondary infections (including vaginal);
frequency unknown - pseudomembranous colitis, erysipelas.
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.

CONTRAINDICATIONS
A history of prolongation of the QT interval, ventricular arrhythmia or ventricular pirouette tachycardia;
hypokalemia (risk of QT interval prolongation); severe hepatic insufficiency, which occurs simultaneously with renal insufficiency; Cholestatic jaundice / hepatitis in anamnesis, developed with the use of clarithromycin; porphyria;I trimester of pregnancy; lactation period (breastfeeding); simultaneous reception of clarithromycin with astemizole, cisapride, pimozide, terfenadine; with ergot alkaloids, for example, ergotamine, dihydroergotamine; with midazolam for oral administration; with inhibitors of HMG-CoA reductase (statins), which are largely metabolized by the isoenzyme CYP3A4 (lovastatin, simvastatin), with colchicine; with ticagrelor or ranolazine; increased sensitivity to clarithromycin and other macrolides.
PREGNANCY AND LACTATION
Application 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 exceeds the potential risk to the fetus.

If necessary, use during lactation should stop breastfeeding.

APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with impaired renal function (QC less than 30 ml / min or serum creatinine level more than 3.3 mg / dl) should be reduced by a factor of 2 or doubled between doses.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe liver failure, hepatitis (in history).

APPLICATION FOR CHILDREN
At present, there is insufficient data on the efficacy and safety of the use of clarithromycin in children under 6 months of age.

SPECIAL INSTRUCTIONS
Caution should be used clarithromycin in patients with moderate to severe renal insufficiency;
hepatic insufficiency of moderate and severe degree, with IHD, severe heart failure, hypomagnesemia, severe bradycardia (less than 50 beats per minute); concomitantly with benzodiazepines, such as alprazolam, triazolam, midazolam for IV administration; simultaneously with other ototoxic drugs, especially aminoglycosides; simultaneously with drugs that are metabolized by CYP3A isoenzymes (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), concomitantly with statins whose metabolism does not depend on the isoenzyme CYP3A (including fluvastatin), concomitantly with blockers of slow calcium channels that are metabolized by the iso-ferment comrade CYP3A4 (including verapamil, amlodipine, diltiazem); simultaneously with Class IA antiarrhythmic agents (quinidine, procainamide) and class III (dofetilide, amiodarone, sotalol).
Between antibiotics from the group of macrolides cross resistance is observed.

Treatment with antibiotics changes the normal flora of the intestine, so the development of superinfection caused by resistant microorganisms is possible.

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

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

DRUG INTERACTION
Clarithromycin inhibits the activity of the isoenzyme CYP3A4, which leads to a slowing of the metabolic rate of astemizole when they are used simultaneously.
As a result, the QT interval increases and the risk of ventricular arrhythmia such as pirouette increases.
Simultaneous reception of clarithromycin with lovastatin or simvastatin is contraindicated due to the fact that these statins are largely metabolized by the isoenzyme CYP3A4, and combined use with clarithromycin increases their serum concentrations, which increases the risk of myopathy, including rhabdomyolysis.
There have been reports of rhabdomyolysis in patients taking clarithromycin in conjunction with these drugs. If it is necessary to use clarithromycin, stop taking lovastatin or simvastatin 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 CYP3A isoenzymes (eg, fluvastatin). In case of need for joint intake, it is recommended to take the lowest dose of statin. It should monitor the development of signs and symptoms of myopathy. With simultaneous use with atorvastatin, the concentration of atorvastatin in the blood plasma is moderately increased, the risk of myopathy is increased.
Preparations that are inducers of CYP3A (for example, rifampicin, phenytoin, carbamazepine, phenobarbital, St. John's wort) are capable of inducing the metabolism of clarithromycin, which can lead to a sub-therapeutic concentration of clarithromycin and a decrease in its effectiveness.
It is necessary to monitor the plasma concentration of the inducer CYP3A, which can increase due to the inhibition of CYP3A by clarithromycin.
When combined with rifabutin, the concentration of rifabutin in the blood plasma increases, the risk of uveitis increases, the concentration of clarithromycin in the blood plasma decreases.

When combined with clarithromycin, concentrations in the plasma of phenytoin, carbamazepine, valproic acid may increase.

Strong inducers of cytochrome P450 isoenzymes such as efavirenz, nevirapine, rifampicin, rifabutin and rifapentin can accelerate the metabolism of clarithromycin and thus reduce the concentration of clarithromycin in the plasma 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 with respect to different bacteria, the therapeutic effect may decrease with the combined use of clarithromycin and enzyme inducers.
The concentration of clarithromycin in plasma decreases with the use of etravirine, while the concentration of the active metabolite of 14-OH-clarithromycin increases.
Since 14-OH-clarithromycin has a low activity against MAC infections, the overall activity against their pathogens may change, therefore alternative treatment should be considered for MAC treatment.
A pharmacokinetic study showed that the simultaneous intake of ritonavir at a dose of 200 mg every 8 hours and clarithromycin at a dose of 500 mg every 12 hours led to a marked suppression of the metabolism of clarithromycin.
With the simultaneous intake of 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 decreased significantly. Ritonavir should not be taken together with clarithromycin in doses exceeding 1 g / day.
Clarithromycin, atazanavir, saquinavir are substrates and inhibitors of CYP3A, which determines their bi-directional interaction.
When taking saquinavir together with ritonavir, the potential effect of ritonavir on clarithromycin should be considered.
With simultaneous application with zidovudine, the bioavailability of zidovudine decreases somewhat.

Colchicine is a substrate for both CYP3A and P-glycoprotein.
It is known that clarithromycin and other macrolides are inhibitors of CYP3A and P-glycoprotein. When co-administered with clarithromycin and colchicine, inhibition of P-glycoprotein and / or CYP3A can lead to an increase in the effect of colchicine. It should monitor the development of clinical symptoms of colchicine poisoning. Post-marketing reports on cases of colchicine poisoning during its simultaneous administration with clarithromycin are registered, more often in elderly patients. Some of these cases occurred in patients with renal insufficiency. As reported, some cases ended in a fatal outcome. Simultaneous use of clarithromycin and colchicine is contraindicated.
When joint use of midazolam and clarithromycin (oral 500 mg twice per day), there was an increase in midazolam AUC: 2.7 times after iv administration of midazolam and 7 times after oral administration.
Simultaneous reception of clarithromycin with midazolam for oral administration is contraindicated. If clarithromycin is used in / in the form of midazolam, the patient's condition should be carefully monitored for possible dose adjustment. The same precautions should also be applied to other benzodiazepines that are metabolized by CYP3A, including triazolam and alprazolam. For benzodiazepines, excretion of which does not depend on CYP3A (temazepam, nitrazepam, lorazepam), clinically significant interaction with clarithromycin is unlikely.
With the combined use of clarithromycin and triazolam, there may be an effect on the central nervous system, such as drowsiness and confusion.
With this combination, it is recommended to monitor the symptoms of a CNS disorder.
With simultaneous use with warfarin, it is possible to increase the anticoagulant effect of warfarin and increase the risk of bleeding.

It is suggested that digoxin is a substrate for P-glycoprotein.
It is known that clarithromycin inhibits P-glycoprotein. With simultaneous use with digoxin, a significant increase in the concentration of digoxin in the blood plasma and the risk of developing glycosidic intoxication.
Possible occurrence of ventricular tachycardia of the "pirouette" type when combined use of clarithromycin and quinidine or disopyramide.
With the simultaneous use of clarithromycin with these drugs, ECG monitoring should be performed regularly to increase the QT interval, and serum concentrations of these drugs should be monitored. In post-marketing applications, cases of hypoglycemia were reported with the combined use of clarithromycin and disopyramide. It is necessary to monitor the concentration of glucose in the blood with the simultaneous use of clarithromycin and disopyramide. It is believed that an increase in the concentration of disopyramide in the blood plasma is possible due to the inhibition of its metabolism in the liver under the influence of clarithromycin.
The simultaneous administration of fluconazole 200 mg daily and clarithromycin 500 mg 2 times / day caused an increase in the mean equilibrium concentration of Clarithromycin (C min ) and AUC by 33% and 18%, respectively.
At the same time, the combined administration did not significantly affect the average equilibrium concentration of the active metabolite of 14-OH-clarithromycin. Correction of the dose of clarithromycin in the case of concurrent administration of fluconazole is not required.
Clarithromycin and itraconazole are substrates and inhibitors of CYP3A, which determines their bi-directional interaction.
Clarithromycin can increase the concentration of itraconazole in plasma, while itraconazole can increase the plasma concentration of clarithromycin.
When used simultaneously with methylprednisolone - the clearance of methylprednisolone decreases;
with prednisone - cases of development of acute mania and psychosis are described.
With simultaneous application with omeprazole, the concentration of omeprazole is significantly increased and the concentration of clarithromycin in the blood plasma is slightly increased;
with lansoprazole - glossitis, stomatitis and / or the appearance of a dark color of the tongue are possible.
With simultaneous use with sertraline - theoretically can not exclude the development of serotonin syndrome;
with theophylline - it is possible to increase the concentration of theophylline in the blood plasma.
While the use of terfenadine may slowing metabolism of terfenadine and increase its concentration in blood plasma, which may lead to an increase in QT interval and an increased risk of ventricular arrhythmias such as "pirouette".
Inhibition of CYP3A4 isoenzyme activity of clarithromycin under the influence leads to slower rate of metabolism of cisapride with their simultaneous use. Because of this increase cisapride concentrations in blood plasma and increases the risk of life-threatening cardiac arrhythmias, including ventricular arrhythmias such as "pirouette".
Primary metabolism of tolterodine is carried out with the participation of CYP2D6. However, part of the population devoid of CYP2D6, the metabolism occurs with the participation of CYP3A. In this population suppression of CYP3A results in significantly higher concentrations of tolterodine in serum. Therefore, in patients with low CYP2D6-mediated metabolism may require dose reduction in the presence of tolterodine CYP3A inhibitors, such as clarithromycin.
When the joint application of clarithromycin and oral hypoglycemic agents (e.g., sulfonylurea derivatives) and / or insulin may experience severe hypoglycemia. The simultaneous use of clarithromycin with some hypoglycemic agents (e.g., nateglinide, pioglitazone, repaglinide and rosiglitazone) can lead to inhibition of CYP3A isozymes clarithromycin, which may lead to hypoglycemia. It is believed that while the use of tolbutamide there is a possibility of hypoglycemia.
In an application with fluoxetine, the case of toxic effects, caused by the action of fluoxetine.
At simultaneous reception of clarithromycin with other ototoxic drugs, especially aminoglycosides, care should be taken to control the function of the vestibular and auditory aids both during treatment and after its completion.
When applied simultaneously with cyclosporin increased cyclosporin concentration in blood plasma, there is risk of increasing the side effects.
With the simultaneous use ergotamine, dihydroergotamine described cases amplification side effects of ergotamine and dihydroergotamine. Post-marketing studies show that the combined use of clarithromycin with ergotamine or dihydroergotamine, the following effects associated with acute poisoning drugs group ergotamines: vasospasm, ischemia of the extremities and other tissues including the central nervous system. The simultaneous use of clarithromycin and ergot alkaloids contraindicated.
Each of these PDE inhibitors metabolized, at least partially, with the participation of CYP3A. However, clarithromycin is able to inhibit CYP3A. The combined use of clarithromycin with sildenafil, tadalafil or vardenafil may result in increased inhibitory effects on the PDE. In these combinations should consider reducing the dose of sildenafil, tadalafil and vardenafil.
With simultaneous application of clarithromycin and calcium channel blockers that are metabolized isoenzyme CYP3A4 (e.g., verapamil, amlodipine, diltiazem), caution because there is the risk of hypotension. Clarithromycin plasma concentrations, as well as calcium channel blockers, may be increased while the application.Hypotension, bradyarrhythmias and lactic acidosis are possible while taking clarithromycin and verapamil.
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