Klacid pills 250 mg 10 pcs
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Active ingredients
Clarithromycin
Release form
Pills
Composition
Tablets, film-coated 1 tab. Active substance: Clarithromycin 250 mg adjuvants core pills 250 mg: croscarmellose sodium; MCC; pregelatinized starch; silicon dioxide; Povidone; stearic acid; magnesium stearate; talc; quinoline yellow E104 tablet shell 250 mg: hypromellose; hyprolosis; propylene glycol; sorbitan monooleate; titanium dioxide; sorbic acid; vanillin; quinoline yellow (E104) core pills 0.5 g: croscarmellose; MCC; silicon dioxide; Povidone; stearic acid; magnesium stearate; talc shell pills 0.5 g: hypromellose; hydroxypropylcellulose; propylene glycol; sorbitan monooleate; titanium dioxide; sorbic acid; vanillin; quinoline yellow (E104)
Pharmacological effect
Clarithromycin is a semisynthetic antibiotic of the macrolide group and has an antibacterial effect by interacting with the 50S ribosomal subunit of sensitive bacteria and inhibiting protein synthesis. Clarithromycin has demonstrated high in vitro activity against standard and isolated cultures of bacteria. Highly effective against many aerobic and anaerobic, gram-positive and gram-negative microorganisms. Clarithromycin in vitro is highly effective against Legionella pneumophila, Mycoplasma pneumoniae and Helicobacter (Campilobacter) pylori. Enterobacteriaceae and Pseudomonas as well as other non-decomposing lactose negative bacteria are insensitive to klaritromitsinu.Pokazano that clarithromycin has antibacterial activity against the following pathogens: gram-positive aerobic microorganisms - Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Listeria monocytogenes; aerobic gram-negative microorganisms: Haemophilus influenzae, Haemophilus parainftuenzae, Moraxella catarrhalis, Legionella pneumophila, Neisseria gonorrhoeae; other microorganisms are Mycoplasma pneumoniae, Chlamydia pneumoniae (TWAR), Chlamydia trachomatis; mycobacteria - Mycobacterium leprae, Mycobacterium kansasii, Mycobacterium chelonae, Mycobacterium fortuitum; Mycobacterium avium complex (MAC) - a complex that includes: Mycobacterium avium, Mycobacterium intracellulare. Beta-lactamase products do not affect the activity of clarithromycin. Most of the methicillin-oxacillin-resistant strains are resistant to the clarithicin, and they are resistant to the body. The sensitivity of H. pylori to clarithromycin was studied on isolates of H. pylori isolated from 104 patients before the start of therapy with the drug. In 4 patients, H. pylori strains resistant to clarithromycin were isolated, in 2 patients - strains with intermediate resistance, in the remaining 98 patients H. pylori isolates were sensitive to clarithromycin.Clarithromycin has an in vitro effect on most strains of the following microorganisms (however, the safety and effectiveness of using clarithromycin in clinical practice has not been confirmed by clinical studies and the practical significance remains unclear): - aerobic gram-positive microorganisms - Streptococcus agalactiae, Streptococci (groups C, F, G) , Viridans group streptococci; - aerobic gram-negative microorganisms - Bordetella pertussis, Pasteurella multocida; - anaerobic gram-positive microorganisms - Clostridium perfringens, Peptococcus niger, Propionibacterium acnes; - anaerobic g Negative microorganisms - Bacteroides melaninogenicus; - Spirochetes - Borrelia burgdorfer, Treponema pallidum; - Campylobacter - Campylobacter jejuni. The main metabolite of clarithromycin in the human body is a microbiologically active metabolite - 14-hydrosycrophyl; - a -fe-alpha; Microbiological activity of the metabolite is the same as that of the original substance, or 1-2 times weaker in relation to most microorganisms. The exception is H.influenzae, in relation to which the efficiency of the metabolite is 2 times higher. The parent substance and its main metabolite have either an additive or a synergistic effect on H. influenzae in vitro and in vivo depending on the culture of bacteria. Sensitivity studies Quantitative methods that require measuring the diameter of the growth inhibition zone of microorganisms give the most accurate estimates of the sensitivity of bacteria to antimicrobial agents. One of the recommended sensitivity procedures uses discs impregnated with 15 μg of clarithromycin (Kirby-Bauer diffusion test); The test results are interpreted depending on the diameter of the zone of growth inhibition of the microorganism and the value of the IPC of clarithromycin. The value of BMD is determined by the method of dilution of the medium or diffusion in agar. Laboratory tests give one of 3 results: - stable - we can assume that the infection is not amenable to treatment with this drug; - moderately sensitive - therapeutic effect is ambiguous, and possibly increasing the dosage can lead to sensitivity; - sensitive - it can be considered that the infection is treatable with clarithromycin.
Pharmacokinetics
The drug is rapidly absorbed in the digestive tract. Absolute bioavailability is about 50%. With repeated doses of the drug cumulation was not detected, and the nature of the metabolism in the human body has not changed.Eating immediately before taking the drug increased the bioavailability of the drug by an average of 25%. Clarithromycin can be used before or during meals. In vitro In in vitro studies, the binding of clarithromycin to plasma proteins is 70% in a concentration from 0.45 to 4.5 μg / ml. At a concentration of 45 μg / ml, the binding decreases to 41%, probably as a result of saturation of the binding sites. This is observed only at concentrations that are several times higher than the therapeutic one. Patients When prescribing clarithromycin in a dose of 250 mg 2 times a day, the maximum Css clarithromycin and 14-hydroxylarithromycin in plasma were reached in 2–3 days and were 1 and 0.6 μg / ml, respectively. T1 / 2 of the initial preparation and its main metabolite were 3-4 hours and 5-6 hours, respectively. When prescribing clarithromycin in a dose of 500 mg 2 times a day, the maximum Css clarithromycin and 14-hydroxylarithromycin in plasma were reached after administration of the 5th dose and amounted to on average, 2.7–2.9 and 0.88–0.83 mcg / ml, respectively. The T1 / 2 of the initial preparation and its main metabolite were 4.5–4.8 h and 6.9–8.7 h, respectively. In an equilibrium state, the level of 14-hydroxylaritromycin does not increase in proportion to the doses of clarithromycin, and T1 / 2 of clarithromycin and its main metabolite increase with increasing dose. The nonlinear nature of the pharmacokinetics of clarithromycin is associated with a decrease in the formation of 14-OH- and N-demethylated metabolites with the use of higher doses, which indicates the nonlinearity of the metabolism of clarithromycin when receiving high doses. About 37.9% is excreted in urine after taking 250 mg and 46% after taking 1200 mg of clarithromycin, through the intestine - about 40.2 and 29.1%, respectively. Clarithromycin and its 14-OH metabolite are well distributed in tissues and body fluids . After oral administration of clarithromycin, its content in the cerebrospinal fluid remains low (with normal BBB permeability 1–2% of the level in the blood serum). The content in the tissues is usually several times higher than the content in the serum.
Indications
lower respiratory tract infections (such as bronchitis, pneumonia), upper respiratory infections (such as pharyngitis, sinusitis), skin and soft tissue infections (such as folliculitis, inflammation of the subcutaneous tissue, erysipelas), mycobacterial infections caused by Mycobacterium avium and mycobacterium intracellulare. Localized infections caused by Mycobacterium chelonae, Mycobacterium fortuitum and Mycobacterium kansasii, prevention of the spread of infection caused by the Mycobacterium avium complex (MAC).HIV-infected patients with a CD4 lymphocyte content (T-helper lymphocytes) of no more than 100 in 1 mm3; to eliminate H. pylori and reduce the frequency of recurrence of duodenal ulcer; odontogenic infections.
Contraindications
hypersensitivity to macrolide drugs; simultaneous use of clarithromycin with the following drugs: astemizole, cisapride, pimozide, terfenadine, ergotamine, dihydroergotamine (see "Interaction"); porphyria; Pregnancy; lactation period; children under 3 years old (see "Special instructions ").
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
The safety of clarithromycin in pregnant and lactating women has not been studied. It is known that clarithromycin is excreted in breast milk. Therefore, the use of clarithromycin during pregnancy and lactation is recommended only in cases where there is no safer alternative, and the risk associated with the disease itself exceeds the possible harm to the mother and fetus.
Dosage and administration
Inside, regardless of the meal. Usually, adults are prescribed 250 mg of clarithromycin 2 times a day. In more severe cases, the dose is increased to 500 mg 2 times a day. Typically, the duration of treatment is from 5–6 to 14 days. Patients with creatinine Cl less than 30 ml / min are prescribed half the usual dose of clarithromycin, i.e. 250 mg 1 time per day, or for more severe infections - 250 mg 2 times per day. The treatment of such patients is continued for no more than 14 days. In case of mycobacterial infections, 500 mg of the drug is prescribed 2 times a day. In case of common infections caused by MAC in AIDS patients: treatment should be continued until there is clinical and microbiological evidence of its benefits. Clarithromycin should be prescribed in combination with other antimicrobial drugs. In infectious diseases caused by mycobacteria, except tuberculosis: the duration of treatment is determined by the doctor. To prevent infections caused by MAC. The recommended dose of clarithromycin for adults is 500 mg 2 times a day. For odontogenic infections, the dose of clarithromycin is 250 mg 2 times a day for 5 days. For eradication of H.pyloriCombined treatment with three drugsClarithromycin in a dose of 500 mg 2 times a day in combination with lansoprazole in a dose of 30 mg2 times a day and amoxicillin at a dose of 1000 mg 2 times a day for 10 days. Clarithromycin at a dose of 500 mg 2 times a day in combination with amoxicillin at a dose of 1000 mg 2 times a day and omeprazole at a dose of 20 mg / day for 7–10 days. Combined treatment with two drugs: Clarithromycin at a dose of 500 mg 3 times a day in combination with omeprazole at a dose of 40 mg / day for 14 days, with an appointment in the next 14 days of omeprazole at a dose of 20–40 mg / day. Clarithromycin in a dose of 500 mg 3 times a day in combination with lansoprazole at a dose of 60 mg / day for 14 days. For complete healing of ulcers may require an additional decrease in the acidity of gastric juice.
Side effects
The most common adverse events on the gastrointestinal tract, including diarrhea, vomiting, abdominal pain and nausea. Other adverse reactions included headache, taste impairment, and transient increases in liver enzymes. Postomarketing experience When treated with clarithromycin, liver dysfunctions, including increased activity of liver enzymes, and hepatocellular and / or cholestatic hepatitis, accompanied or not accompanied by jaundice, were rarely observed. Hepatic dysfunction can be severe and usually reversible. In very rare cases, deaths from liver failure were recorded, which were usually observed in the presence of serious comorbidities and / or simultaneous use of other HPs. Some cases of increased serum creatinine levels were described, but their relationship with the drug was not established. Allergic reactions were described during oral administration of clarithromycin. which ranged from urticaria and small rashes to anaphylaxis and Stevens-Johnson syndrome / toxic epidermal necrolysis. There are bscheniya of transient effects on the CNS, including dizziness, anxiety, insomnia, bad dreams, tinnitus, confusion, disorientation, hallucinations, psychosis and depersonalisation; their causal relationship with the drug has not been established. When treating clarithromycin, cases of hearing loss are described; hearing was usually restored after cessation of treatment. There are also cases of olfactory impairment, which are usually combined with taste perversion. When treating clarithromycin, glossitis, stomatitis, oral thrush and a change in the color of the tongue are described. There have been cases of discoloration of teeth in patients who received clarithromycin.These changes are usually reversible and can be eliminated by the dentist. Rare cases of hypoglycemia have been described, some of which have been reported in patients who received oral hypoglycemic agents or insulin. QT interval, ventricular tachycardia and ventricular tachycardia of the type “pirouette.” Rare cases of pancreatitis and seizures are described. There are reports of interstitial development Rita klaritromitsinom.V in the treatment of clinical cases of colchicine toxicity described when it is combined with clarithromycin, especially in the elderly. Some of them were observed in patients with renal insufficiency; A few deaths have been reported in such patients (see Interaction, Colchicine; Contraindications). Immunocompromised children In patients with AIDS and other immunodeficiencies receiving clarithromycin in higher doses for a long time to treat mycobacterial infections, it is often difficult to differentiate the adverse effects of the drug from the symptoms of HIV infection or intercurrent diseases. The main adverse events in patients taking clarithromycin orally at a dose of 1 g were nausea, rv ota, taste perversion, abdominal pain, diarrhea, rash, abdominal distension, headache, hearing loss, constipation, increased AST and ALT levels. Dyspnea, insomnia and dry mouth were also less common. In this group of patients with depressed immunity, significant deviations of laboratory parameters from standard values in specific tests (sharp increase or decrease) were recorded. Based on this, approximately 2-3% of patients who took clarithromycin orally at a dose of 1 g / day had significant deviations from normal laboratory values, such as an increase in AST, ALT, and a decrease in the number of leukocytes and platelets. A smaller number of patients also showed an increase in the blood urea nitrogen level.
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
Interaction with cytochrome P450 Clarithromycin is metabolized in the liver by the action of the cytochrome P4503A isoenzyme (CYP3A). This mechanism determines many interactions with other drugs. Clarithromycin can inhibit the biotransformation of other drugs under the action of this system, which can lead to an increase in their serum levels. The following drugs or classes of metabolism by the same CYP3A isoenzyme are assumed to be: , quinidine, rifabutin, sildenafil, simvastatin, tacrolimus, terfenadine, triazolam and vinblastine. Similar mechanisms of interaction, which are mediated by other cytochrome P450 isoenzymes, are characteristic of phenytoin, theophylline, and valproic acid. In clinical studies with a combination of theophylline or carbamazepine with clarithromycin, a small but statistically significant (less than 0.05) increase in serum levels of theophylline and carbamazepine was observed. CYP3A-mediated interactions were reported in clinical practice using erythromycin and / or clarithromycin. With the combined use of clarithromycin with HMG-CoA reductase inhibitors, such as lovastatin and simvastatin, in rare cases, rhabdomyolysis developed. At the same time Mr. applying clarithromycin with cisapride was an increase in the last levels. This can lead to prolongation of the QT interval and the development of cardiac arrhythmias, including ventricular tachycardia, ventricular fibrillation and polymorphic ventricular tachycardia of the "pirouette" type. Similar effects have been reported in patients receiving clarithromycin with pimozide (see “Contraindications.”) Macrolides caused a disturbance in the metabolism of terfenadine, which led to an increase in its plasma levels and was sometimes associated with the development of arrhythmias, includinglengthening of the QT interval, ventricular tachycardia, ventricular fibrillation and ventricular tachycardia of the “pirouette” type (see “Contraindications”). In one study in 14 healthy volunteers, the combined use of clarithromycin and terfenadine pills led to an increase in the serum level of acidic metabolite terfenadine by 2–3 times and lengthening of the QT interval, which was not accompanied by any clinical effects. In clinical practice, cases of ventricular tachycardia of the “pirouette” type have been recorded with clarithromycin combined with quinidine or disopyramide. When treating clarithromycin, serum levels of these drugs should be monitored. Ergotamine / dihydroergotamine. In clinical practice, the combination of clarithromycin with ergotamine or dihydroergotamine recorded cases of acute toxicity of the latter, which is characterized by vasospasm and ischemia of the limbs and other tissues, including the CNS. Interaction with other drugs. In patients treated with clarithromycin pills in combination with digoxin, an increase in serum concentrations of the latter was observed. It is advisable to monitor serum levels of digoxin. Colchicine. It is a substrate for CYP3A and P-glycoprotein. Clarithromycin and other macrolides are inhibitors of CYP3A and P-glycoprotein. When co-administered with colchicine and clarithromycin, inhibition of P-glycoprotein and / or CYP3A can lead to an increase in the effect of colchicine. Patients should be carefully monitored in order to identify the symptoms of the toxic effect of colchicine. Interaction with antiretroviral agents. Simultaneous oral administration of clarithromycin in pills with zidovudine in HIV-infected adult patients can lead to a decrease in Css zidovudine. No such interaction was observed in HIV-infected children who took the children's suspension of clarithromycin with zidovudine or dideoxyinosine. In a pharmacokinetic study, the combined use 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 significant inhibition of the metabolism of clarithromycin. Cmax of clarithromycin when combined with ritonavir increased by 31%, Cmin - by 182%, AUC - by 77%. A virtually complete inhibition of the formation of 14-hydroxylarithromycin was observed.Given the high therapeutic index of clarithromycin, a reduction in its dose is not required in patients with normal renal function. However, in patients with impaired renal function, dose adjustment is advisable. In patients with Cl creatinine 30–60 ml / min, the dose of clarithromycin is reduced by 50%, and in patients with Cl creatinine less than 30 ml / min - by 75%. In doses of more than 1 g / day, clarithromycin should not be used in combination with ritonavir.
special instructions
In the presence of chronic liver disease, it is necessary to regularly monitor serum enzymes. With caution prescribed against the background of drugs metabolized by the liver (see "Interaction"). In the case of co-administration with warfarin or other indirect anticoagulants, it is necessary to control P.V. Children preferably use dosage form powder for suspension for oral administration 125 mg / 5 ml and 250 mg / 5 ml.