Klacid pills 500 mg 14 pcs
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Active ingredients
Clarithromycin
Release form
Pills
Composition
Clarithromycin 500 mg. Adjuvants: croscarmellose - 65.6 mg, microcrystalline cellulose - 183.9 mg, silicon dioxide - 12 mg, povidone - 25.5 mg, stearic acid - 21 mg, magnesium stearate - 12.6 mg, talc - 29.4 mg.
Pharmacological effect
Semisynthetic macrolide antibiotic. Suppresses the synthesis of proteins in the microbial cell, interacting with the 50S ribosomal subunit of bacteria. It is mainly bacteriostatic and 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. Also active against Toxoplasma gondii, Mycobacterium spp. (except Mycobacterium tuberculosis).
Pharmacokinetics
When ingested, clarithromycin is well absorbed from the gastrointestinal tract. Meal slows down the absorption, but does not affect the bioavailability of the active substance. Clarithromycin well penetrates 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-hydrochloridromycin. At a dose of 250 mg T1 / 2 is 3-4 hours, at a dose of 500 mg - 5-7 hours. Excreted in the urine in unchanged form and in the form of metabolites.
Indications
Treatment of infectious and inflammatory diseases caused by causative agents that are sensitive to clarithromycin: infections of the upper respiratory tract and upper respiratory tract (tonsillofaringitis, otitis media, acute sinusitis); lower respiratory tract infections (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; Helicobacter pylori eradication in patients with duodenal ulcer or stomach ulcer (only as part of combination therapy).
Contraindications
A history of prolongation of the QT interval, ventricular arrhythmia, or ventricular tachycardia such as pirouette; hypokalemia (risk of prolonged QT interval); severe liver failure, occurring simultaneously with renal insufficiency; a history of cholestatic jaundice / hepatitis,developed with the use of clarithromycin; porphyria; I trimester of pregnancy; lactation period (breastfeeding); simultaneous administration of clarithromycin with astemizole, cisapride, pimozide, terfenadine; with ergot alkaloids, for example, ergotamine, dihydroergotamine; with oral midazolam; 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.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
Use in the first trimester of pregnancy is contraindicated. Use in the second and third trimesters of pregnancy is possible only in cases where the intended benefit to the mother outweighs the potential risk to the fetus. If you need to use during lactation, breastfeeding should be stopped.
Dosage and administration
Individual. When taken orally for adults and children over 12 years old, 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 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 2 times or doubled the interval between doses .Maximum daily Daily doses: for adults - 2 g, for children - 1 g
Side effects
On the part of the digestive system: often - diarrhea, vomiting, dyspepsia, nausea, pain in the abdomen; infrequently - esophagitis, gastroesophageal reflux disease, gastritis, proctalgia, stomatitis, glossitis, abdominal distension, constipation, dry mouth, belching, flatulence, increased bilirubin concentration in the blood, increased activity of ALT, ACT, GGT, Alkaline, LDH, cholestasis, hepatitis including cholestatic and hepatocellular; frequency is unknown - acute pancreatitis, discoloration of the tongue and teeth, liver failure, cholestatic jaundice. Allergic reactions: often - rash; infrequently - anaphylactoid reaction, hypersensitivity, bullous dermatitis, pruritus,urticaria, maculo-papular rash; frequency is 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 is unknown - convulsions, psychotic disorders, confusion, depersonalization, depression, disorientation, hallucinations, nightmares, paresthesia, mania. On the part of the skin: often - sweating; frequency is unknown - acne, hemorrhage. From the side of the sense organs: often - dysgeusia, taste perversion; infrequently - vertigo, hearing loss, ringing in the ears; frequency is unknown - deafness, agevziya, parosmia, anosmia. For the cardiovascular system: often - vasodilation; infrequently - cardiac arrest, atrial fibrillation, prolongation of the QT interval on an ECG, extrasystole, atrial flutter; frequency is unknown - ventricular tachycardia, incl. pirouette type. From the urinary system: infrequently - increasing the concentration of creatinine, changing the color of urine; frequency unknown - renal failure, interstitial nephritis. Metabolism and nutrition: infrequently - anorexia, loss of appetite, increased urea concentration, change in albumin-globulin ratio. Musculoskeletal system: infrequently - muscle spasm, bone and muscle stiffness, myalgia; frequency is unknown - rhabdomyolysis, myopathy. On the part of the respiratory system: infrequently - asthma, nasal bleeding, pulmonary embolism. On the side of the hematopoietic system: infrequently - leukopenia, neutropenia, eosinophilia, thrombocythemia; frequency unknown - agranulocytosis, thrombocytopenia. From the blood coagulation system: infrequently - increase in the MHO value, prolongation of prothrombin time. Infectious and parasitic diseases: infrequently - cellulitis, candidiasis, gastroenteritis, secondary infections (including vaginal); frequency is 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 whole body side: infrequently - indisposition, hyperthermia, asthenia, chest pain, chills, fatigue.
Overdose
Symptoms: Taking a large dose of clarithromycin can cause symptoms of disorders of the gastrointestinal tract.In one patient with bipolar disorder in the history after taking 8 g of clarithromycin, changes in mental state, paranoid behavior, hypokalemia and hypoxemia are described. Treatment: in case of overdose, remove the unabsorbed drug from the gastrointestinal tract and conduct symptomatic therapy. Hemodialysis and peritoneal dialysis do not have a significant effect on the level of clarithromycin in serum, which is characteristic of other drugs of the macrolide group.
Interaction with other drugs
Clarithromycin inhibits the activity of CYP3A4 isoenzyme, which leads to a slower rate of metabolism of astemizol with their simultaneous use. As a consequence, an increase in the QT interval and an increase in the risk of developing ventricular arrhythmias such as pirouette occurs. Simultaneous administration of clarithromycin with lovastatin or simvastatin is contraindicated due to the fact that these statins are significantly metabolized by the CYP3A4 isoenzyme, and their combined use with clarithromycin increases their serum concentrations resulting in a CYP3A4 isoenzyme, and their combined use with clarithromycin increases their serum concentrations leads to increased risk of myopathy, including rhabdomyolysis. Cases of rhabdomyolysis have been reported in patients taking clarithromycin together with these drugs. If you need to use clarithromycin, you should stop taking lovastatin or simvastatin for the duration of therapy. Clarithromycin should be used with caution when combined therapy with other statins. It is recommended to use statins that are not dependent on the metabolism of CYP3A isoenzymes (for example, fluvastatin). If necessary, the joint reception is recommended to take the lowest dose of a statin. The development of signs and symptoms of myopathy should be monitored. With simultaneous use with atorvastatin, plasma plasma levels of atorvastatin increase moderately, and the risk of myopathy increases. Preparations that are inducers of CYP3A (for example, rifampicin, phenytoin, carbamazepine, phenobarbital, St. John's wort), are able to induce the metabolism of clarithromycin, and I do not work on the body of the human body. and reduce its effectiveness. It is necessary to control the plasma concentration of the inducer CYP3A,which can be increased due to inhibition of CYP3A clarithromycin. When used together 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. . Strong inducers of isoenzymes of the cytochrome P450 system, such as efavirenz, nevirapine, rifampicin, rifabutin and rifapentin, are able to accelerate the metabolism of clariter Omsicin and, thus, reduce the concentration of clarithromycin in plasma and weaken its therapeutic effect, and at the same time increase the concentration of 14-OH-clarithromycin, a metabolite that 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 co-administration of clarithromycin and enzyme inducers. The concentration of clarithromycin in plasma 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, overall activity against their pathogens may change, therefore alternative treatment should be considered for MAC treatment. A pharmacokinetic study showed that co-administration of ritonavir at a dose of 200 mg every 8 hours and clarithromycin at a dose of 500 mg every 12 hours resulted in a marked suppression of the metabolism of clarithromycin. When co-administered with ritonavir, Cmax of clarithromycin increased by 31%, Cmin 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 bidirectional interaction. When taking saquinavir together with ritonavir, the potential effect of ritonavir on clarithromycin should be considered. When used simultaneously with zidovudine, zidovudine bioavailability decreases slightly. Colchicine is a substrate of 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. The development of the clinical symptoms of colchicine poisoning should be monitored. Post-marketing reports of cases of colchicine poisoning with its simultaneous use with clarithromycin, more often in elderly patients, have been registered. Some of the cases described occurred in patients with renal insufficiency. Some cases have been reported to be fatal. Simultaneous use of clarithromycin and colchicine is contraindicated. When combined use of midazolam and clarithromycin (orally 500 mg 2 times / day), an increase in the AUC of midazolam was noted: 2.7 times after intravenous injection of midazolam and 7 times after oral administration. Simultaneous use of clarithromycin with midazolam for oral use is contraindicated. If intravenous midazolam is used with clarithromycin, the patient’s condition should be carefully monitored for possible dose adjustment. The same precautions should be applied to other benzodiazepines that are metabolized by CYP3A, including triazolam and alprazolam. For benzodiazepines, the elimination of which does not depend on CYP3A (temazepam, nitrazepam, lorazepam), clinically significant interaction with clarithromycin is unlikely. When combined with 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 a CNS disorder. When used simultaneously with warfarin, the anticoagulant effect of warfarin and the increased risk of bleeding can be increased. Digoxin is supposed to be 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 glycosidic intoxication are possible. Occurrence of ventricular tachycardia like pirouette is possible with the combined use of clarithromycin and quinidine or disopyramide.With simultaneous use of clarithromycin with these drugs, ECG monitoring should be regularly monitored for an increase in the QT interval, and serum concentrations of these drugs should also be monitored. With post-marketing use, cases of hypoglycemia have been reported with 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. Joint 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 minimum equilibrium concentration of clarithromycin (Cmin) 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. Correction of the dose of clarithromycin in the case of concomitant 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 acute mania and psychosis are described. When used simultaneously 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 colouration of the tongue are possible. If used concurrently with sertraline, it is theoretically impossible to exclude the development of serotonin syndrome; with theophylline - it is possible to increase the concentration of theophylline in the blood plasma. When used simultaneously with terfenadine, it is possible to slow the metabolism rate of terfenadine and increase its concentration in the blood plasma, which can lead to an increase in the QT interval and an increase in the risk of developing ventricular arrhythmias such as pirouette. the influence of clarithromycin leads to a slower rate of metabolism of cisapride with their simultaneous use.As a result, plasma cisapride concentration increases and the risk of developing life-threatening cardiac rhythm, including ventricular arrhythmias of the pirouette type, increases. The primary metabolism of tolterodine is mediated by CYP2D6. However, in a part of a population deprived of CYP2D6, metabolism occurs with the participation of CYP3A. In this population group, inhibition of CYP3A leads to significantly higher serum tolterodine concentrations. Therefore, patients with low CYP2D6-mediated metabolism may require a dose reduction of tolterodine in the presence of CYP3A inhibitors, such as clarithromycin. When combined with clarithromycin and oral hypoglycemic agents (eg, sulfonylurea derivatives) and / or insulin, severe hypoglycemia may occur. Simultaneous use of clarithromycin with certain hypoglycemic drugs (for example, nateglinide, pioglitazone, repaglinide, and rosiglitazone) can lead to inhibition of CYP3A isoenzymes by clarithromycin, which can lead to the development of hypoglycemia. It is believed that with simultaneous use with tolbutamide there is a likelihood of hypoglycemia. When used simultaneously with fluoxetine, a case of toxic effects due to fluoxetine has been described. When using clarithromycin with other ototoxic drugs, especially aminoglycosides, it is necessary to be careful and monitor the functions of the vestibular and hearing aids both during therapy, and after its termination. At simultaneous use with cyclosporin it rises to Oncentration of cyclosporine in the blood plasma, there is a risk of increased side effects. When used concomitantly with ergotamine, dihydroergotamine, cases of increased side effects of ergotamine and dihydroergotamine are described. Postmarketing studies show that with the combined use of clarithromycin with ergotamine or dihydroergotamine, the following effects associated with acute poisoning by drugs of the ergotamine group are possible: vascular spasm, ischemia of the extremities and other tissues, including the central nervous system. Simultaneous use of clarithromycin and ergot alkaloids is contraindicated. Each of these PDE inhibitors is metabolized, at least partially, with the participation of CYP3A. At the same time clarithromycin is able to inhibit CYP3A. The combined use of clarithromycin with sildenafil, tadalafil or vardenafil can lead to an increase in the inhibitory effect on PDE.With these combinations, the possibility of reducing the dose of sildenafil, tadalafil and vardenafil should be considered. When simultaneously using clarithromycin and calcium channel blockers that are metabolized by the CYP3A4 isoenzyme (for example, verapamil, amlodipine, diltiazem), care should be taken because there is a risk of arterial hypotension. Plasma concentrations of clarithromycin, as well as calcium channel blockers, may increase with simultaneous use. Hypotension, bradyarrhythmia and lactacidosis are possible with simultaneous administration of clarithromycin and verapamil.
special instructions
Precautions should use clarithromycin in patients with moderate to severe renal failure; moderate and severe liver failure, with coronary artery disease, severe heart failure, hypomagnesemia, severe bradycardia (less than 50 beats / min); concurrently 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; quinidine, rifabutin, sildenafil, tacrolimus, vinblastine; quinidine, rifabutin, sildenafil, tacrolimus, vinblastine; quinidine, rifabutin, sildenafil, tacrolimus, vinblastine; quinidine, rifabutin, sildenafil, tacrolimus, vinblastine, quinidine, rifabutin, sildenafil, tacrolimus, vinblastine; , phenytoin, carbamazepine, phenobarbital, St. John's wort); simultaneously with statins, whose metabolism does not depend on the CYP3A isoenzyme (including fluvastatin); simultaneously with blockers of slow calcium channels metabolized by the isoenzyme CYP3A4 (including verapamil, amlodipine, diltiazem); at the same time as class IA (quinidine, procainamide) and class III antiarrhythmic drugs (dofetilide, amiodarone, sotalol). Cross-resistance is observed between antibiotics from the group of macrolides. Antibiotic treatment changes normal intestinal flora, therefore, the development of superinfection caused by resistant microorganisms is possible. It should be borne in mind that severe persistent diarrhea may be caused by the development of pseudomembranous colitis. It should be monitored periodically rotrombinovoe time in patients receiving clarithromycin concurrently with warfarin or other oral anticoagulants.