Klacid CP coated pills retard 500mg N14
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Active ingredients
Clarithromycin
Release form
Pills
Composition
1 tablet contains: clarithromycin 500 mg Auxiliary substances: anhydrous citric acid - 128 mg, sodium alginate - 120 mg, sodium calcium alginate - 15 mg, lactose - 115 mg, povidon-K30 - 30 mg, talc - 30 mg, stearic acid - 21 mg, magnesium stearate - 10 mg. The composition of the film shell: hypromellose - 9.81 mg, macrogol 400 - 3.27 mg, macrogol 8000 - 3.27 mg, titanium dioxide - 1.64 mg, dye yellow (quinoline yellow) - 1.23 mg, sorbic acid - 0.16 mg.
Pharmacological effect
Semisynthetic macrolide antibiotic. Suppresses the synthesis of proteins in the microbial cell, interacting with the 50S ribosomal subunit of bacteria. Acts 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. It is also active against Toxoplasma gondii, Mycobacterium spp. (except Mycobacterium tuberculosis).
Pharmacokinetics
When ingested, clarithromycin is well absorbed from the gastrointestinal tract. Eating slows down the 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 of 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 unchanged and in the form of metabolites.
Indications
Infections of the lower respiratory tract (including bronchitis, pneumonia). Infections of the upper respiratory tract (including pharyngitis, sinusitis). Infections of the skin and soft tissues (including folliculitis, erysipelas).
Contraindications
Severe renal dysfunction (with CC less than 30 ml / min). These patients are prescribed quick-release clarithromycin. Simultaneous reception of astemizole, cisapride, pimozide, terfenadine. Porphyria. Pregnancy. Lactation (breastfeeding). Hypersensitivity to macrolide antibiotics.
Precautionary measures
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 includingcholestatic and hepatocellular; frequency is unknown - acute pancreatitis, discoloration of the tongue and teeth, liver failure, cholestatic jaundice. 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 - intense sweating; frequency unknown - acne, hemorrhage. From the senses: often - dysgeusia, taste perversion; infrequently - vertigo, hearing loss, ringing in the ears; frequency is unknown - deafness, ageusia, parosmia, anosmia. Since 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. like pirouette. On the part of 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, increase in urea concentration, change in the albumin-globulin ratio. On the part of the musculoskeletal system: infrequently - muscle spasm, musculoskeletal stiffness, myalgia; frequency is unknown - rhabdomyolysis, myopathy. On the part of the respiratory system: infrequently - asthma, nasal bleeding, pulmonary thromboembolism. From the hematopoietic system: infrequently - leukopenia, neutropenia, eosinophilia, thrombocythemia; frequency is unknown - agranulocytosis, thrombocytopenia. On the part of the blood coagulation system: infrequently - an increase in the value of MHO, prolongation of prothrombin time.
Use during pregnancy and lactation
Use in the first trimester of pregnancy is contraindicated. Use 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.
Dosage and administration
Adults Klacid CP prescribed 500 mg (1 tab.) 1 time / day. In severe infections, the dose is increased to 1 g (2 tab.) 1 time / day. Tablets should be taken with food, swallowing whole, not breaking and not chewing.
Side effects
Since the cardiovascular system is rare - ventricular arrhythmia, including ventricular tachycardia (with an increase in the QT interval). From the digestive system, nausea, abdominal pain, vomiting, diarrhea, gastralgia, pancreatitis, glossitis, stomatitis, oral candidiasis, discoloration of the tongue and teeth. rarely - pseudomembranous enterocolitis. Teeth discoloration is reversible and is usually restored by professional cleaning by a dentist. Liver dysfunction was rarely observed, incl. increased liver enzyme activity, hepatic cell and / or cholestatic hepatitis with or without jaundice. These abnormal liver functions can be severe, but usually they are reversible. Very rarely, there were cases of liver failure and death mainly due to severe concomitant diseases and / or concomitant drug therapy. For the CNS, transient headaches, dizziness, anxiety, insomnia, nightmares, tinnitus, depersonalization, hallucinations, convulsions, feeling of fear. rarely - psychosis, confusion. in some cases - hearing loss (with the discontinuation of clarithromycin, hearing was restored), a change in smell (usually accompanied by taste-distortion). Allergic reactions urticaria, skin flushes, pruritus, anaphylaxis, Stevens-Johnson syndrome. On the hematopoietic system, leukopenia, thrombocytopenia. For laboratory parameters, an increase in creatinine levels in the blood. rarely - hypoglycemia (while taking hypoglycemic drugs). Other development of resistance of microorganisms.
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, there is an increase in the QT interval and an increase in the risk of developing ventricular arrhythmias such as pirouette. Simultaneous use 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 together with these drugs. In case of need of use of clarithromycin, lovastatin or simvastatin should be discontinued for the duration of therapy. Clarithromycin should be used with caution when combined 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, the concentration of atorvastatin in the blood plasma increases moderately, the risk of myopathy increases. CYP3A inducer drugs (for example, rifampicin, phenytoin, carbamazepine, phenobarbital, St. John's wort) can induce clarithromycin metabolism, which can lead to a subtherapeutic concentration of clarithromycin and a decrease in its effectiveness. It is necessary to control the plasma concentration of the inducer CYP3A, 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 uveitis increases, the concentration of clarithromycin in the blood plasma decreases. When combined with clarithromycin, it is possible to increase plasma concentrations of phenytoin, carbamazepine, valproic acid. Strong inductors isozymes of cytochrome P450, such as efavirenz, nevirapine, rifampicin, rifabutin and rifapentine able to accelerate clarithromycin metabolism and thus lowering the concentration of clarithromycin in plasma and reduce 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 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 14-OH-clarithromycin increases.Since 14-OH-clarithromycin has low activity against MAC infections, the overall activity against their pathogens may change, so 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 bi-directional interaction. When taking saquinavir with ritonavir, consider the potential effect of ritonavir on clarithromycin. With simultaneous use with zidovudine slightly decreases the bioavailability of zidovudine. 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. The simultaneous use of clarithromycin and colchicine is contraindicated. With the combined use of midazolam and clarithromycin (by mouth, 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. The combined use of clarithromycin and triazolam may affect the central nervous system, such as drowsiness and confusion. With this combination, it is recommended to monitor monitor the symptoms of CNS disorders. With simultaneous use with warfarin may increase the anticoagulant action of warfarin and increase the risk of bleeding. Digoxin is assumed 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 glycoside intoxication may occur. Occurrence of ventricular tachycardia of the pirouette type 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. The 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 value of the 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 dose of clarithromycin in the case of concomitant use of fluconazole is not required. Clarithromycin and itraconazole are substrates and inhibitors of CYP3A, which determines their bidirectional interaction.Clarithromycin can increase the plasma concentration of itraconazole, while itraconazole can increase the plasma concentration of clarithromycin. With simultaneous use with methylprednisolone, the clearance of methylprednisolone decreases; with prednisone - described cases of acute mania and psychosis. 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 coloring of the tongue are possible. With simultaneous use with sertraline - theoretically it is impossible to exclude the development of serotonin syndrome; 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 the rate of metabolism of terfenadine and increase its concentration in the blood plasma, which can lead to an increase in the QT interval and an increased risk of developing ventricular arrhythmias such as pirouette. Inhibition of CYP3A4 isoenzyme activity under the influence of clarithromycin leads to a slower rate of cisapride metabolism with their simultaneous use. As a result, plasma cisapride concentration increases and the risk of developing life-threatening cardiac rhythm, including ventricular arrhythmias such as pirouette, 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, in patients with a low level of CYP2D6-mediated metabolism, it may be necessary to reduce the dose of tolterodine in the presence of CYP3A inhibitors, such as clarithromycin. When combined with clarithromycin and oral hypoglycemic agents (for example, 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 when used with tolbutamide there is a likelihood of hypoglycemia. With simultaneous use with fluoxetine described a case of toxic effects due to the action of fluoxetine. When simultaneously taking clarithromycin with other ototoxic drugs, especially aminoglycosides, care must be taken to monitor the functions of the vestibular and hearing aids, both during therapy and after its termination. With simultaneous use with cyclosporine, the concentration of cyclosporine in the blood plasma increases, there is a risk of increasing side effects. When used concomitantly with ergotamine, dihydroergotamine, there are cases of increased side effects of ergotamine and dihydroergotamine. 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. The 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. With simultaneous use of clarithromycin and calcium channel blockers, which are metabolized by 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. 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 ischemic heart 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); simultaneously with 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. Prothrombin time should be periodically monitored in patients receiving clarithromycin simultaneously with warfarin or other oral anticoagulants.