Clacid, pills 500mg 14pcs

Composition

The Klacid antibiotic contains: active ingredient: clarithromycin-500 mg, additional ingredients: sodium calcium alginate, sodium alginate, lactose, hydrophosphate of anhydrous citric acid, stearic acid, povidone KZO, magnesium stearate.

Pharmacological action

Klacid is a semi-synthetic antibiotic of the macrolide group. It has an antibacterial effect by interacting with the 50S ribosomal subunit of bacteria and suppressing protein synthesis in the microbial cell.

Clarithromycin showed high activity in vitro against standard and isolated bacterial cultures. Highly effective against many aerobic and anaerobic gram-positive and gram-negative microorganisms.

Clarithromycin is highly effective in vitro against Legionella pneumophila, Mycoplasma pneumoniae and Helicobacter (CamPylobacter) pilori. Enterobacteriaceae and Pseudomonas as well as other non-lactose-degrading gram-negative bacteria are not sensitive to clarithromycin.

Clarithromycin has been shown to have an antibacterial effect against the following pathogens: aerobic gram – positive microorganisms – Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Listeria monocytogenes; aerobic gram – negative microorganisms – Haemophilus influenzae, Haemophilus parainftuenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, Legionella pneumophila; other microorganisms – Mycoplasma pneumoniae, Chlamydia pneumoniae (TWAR), Chlamydia trachomatis; Mycobacteria-Mycobacterium leprae, Mycobacterium kansasii, Mycobacterium chelonae, Mycobacterium fortuitum; Mycobacterium avium complex (MAC) – Mycobacterium avium, Mycobacterium intracellulare.

Beta-lactamase production does not affect the activity of clarithromycin. Most strains of staphylococci that are resistant to methicillin and oxacillin are also resistant to clarithromycin.

Helicobacter PYLORI The sensitivity of Helicobacter pylori to clarithromycin was studied on isolates of Helicobacter pylori isolated from 104 patients before starting therapy with the drug. Helicobacter pylori strains resistant to clarithromycin were isolated in 4 patients, strains with intermediate resistance were isolated in 2 patients, and Helicobacter pylori isolates were sensitive to clarithromycin in the remaining 98 patients. Clarithromycin exerts its effects in vitro against most strains of the following microorganisms (however, the safety and effectiveness of using clarithromycin in clinical practice has not been confirmed in clinical studies and practical significance remains unclear): aerobic gram – positive microorganisms Streptococcus agalactiae, Streptococcus (groups C, F, G), Streptococcus viridans group; aerobic gram – negative microorganisms Bordetella pertussis, Pasteurella multocida; anaerobic gram-positive microorganisms – Clostridium perfringens, Peptococcus niger, Propionibacterium acnes; anaerobic gram-negative bacteria – Bacteroides melaninogenicus; Borrelia burgdorferi, Treponema pallidum, Campylobacter jejuni.

The main metabolite of clarithromycin in the human body is the microbiologically active metabolite 14-hydroxyclarithromycin. The microbiological activity of the metabolite is the same as that of the parent substance, or 1-2 times weaker against most microorganisms. The exception is Hemophilus influenzae, for which the effectiveness of the metabolite is 2 times higher. The parent substance and its main metabolite have either an additive or synergistic effect against Haemophilus influenzae in vitro and in vivo, depending on the bacterial culture.

Sensitivity studies

Quantitative methods that require measuring the diameter of the microbial growth retardation zone provide the most accurate estimates of the sensitivity of bacteria to antimicrobial agents. One of the recommended sensitivity testing procedures uses discs soaked in 15 micrograms of clarithromycin (Kirby-Bauer diffusion test); the test results are interpreted depending on the diameter of the microbial growth retardation zone and the clarithromycin BMD value. The MPC value is determined by dilution of the medium or diffusion in agar. Laboratory tests give one of three results: 1) “stable” – it can be considered that the infection does not respond to treatment with this drug; 2)”medium – sensitive” – the therapeutic effect is ambiguous, and it is possible that an increase in dosage may lead to sensitivity; 3)”sensitive” – it can be considered that the infection can be treated with clarithromycin.

Pharmacokinetics

In clinical trials involving healthy volunteers, clarithromycin was administered once in doses of 75 mg,125 mg,250 mg and 500 mg in a volume of 100 ml as an infusion for 30 minutes, as well as in doses of 500 mg,750 mg or 1000 mg in 250 ml for more than 60 minutes. Clarithromycin cssmax ranged from 5.16 mcg / ml to 9.4 mcg / ml after infusion of 500 mg and 1000 mg clarithromycin for 60 minutes, respectively. The cmax of 14-hydroxyclarithromycin was 0.66 mcg / ml after 500 mg infusion and 1.06 mcg/ml after 1000 mg clarithromycin use for 60 minutes. At steady state, the terminal T1/2 of clarithromycin depends on the dose of the drug and ranges from 3.8 h to 4.5 h with doses of 500 mg to 1000 mg per 60 minutes, respectively. T1 / 2 of 14-hydroxyclarithromycin after use of the same doses of 500 mg and 1000 mg for 60 minutes is 7.3 hours and 9.3 hours, respectively, which confirms approximately the same dependence, which increases with increasing dose of clarithromycin.

At steady state, the AUC values changed disproportionately with increasing dose, i. e., there was a non-linear dependence of the AUC values from 22.29 h × mcg / ml to 53.26 h×mcg / ml at doses of 500-1000 mg per 60 minutes, respectively. The AUC of 14-hydroxyclarithromycin ranged from 8.16 h × mcg / ml to 14.76 h×mcg/ml at the same doses over 60 min of infusion.

In 7-day clinical trials, clarithromycin was administered repeatedly in doses of 125 mg and 250 mg as a 100 ml infusion for more than 30 minutes and in doses of 500 mg and 750 mg in a volume of 250 ml for more than 60 minutes every 12 hours. In this study, steady-state Cmax values increased from 5.5 mcg / ml at 500 mg to 8.6 mcg/ml at 750 mg. At steady state, the terminal T1 / 2 of 500 mg and 750 mg clarithromycin after more than 60 minutes of infusion was 5.3 hours and 4.8 hours, respectively. Cmax of 14-hydroxyclarithromycin at steady state after 500 mg and 750 mg dosages increased from 1.02 mcg / ml to 1.37 mcg / ml. The terminal T1/2 phase for this metabolite in the 500 mg or 750 mg groups was 7.9 hours and 5.4 hours, respectively.

The pharmacokinetics of 14-hydroxyclarithromycin were dose-independent.

Patients

Clarithromycin and its metabolite 14-hydroxyclarithromycin are well distributed in the body’s tissues and fluids.

Indications

Infectious and inflammatory diseases caused by clarithromycin-sensitive microorganisms in adults and children over 12 years of age:

• infections of the lower respiratory tract (such as bronchitis, pneumonia);
• infections of the upper respiratory tract (such as pharyngitis, sinusitis);
• infections of skin and soft tissues (such as folliculitis, inflammation of the subcutaneous tissue, face);
• disseminated or localized mycobacterial infections caused by Mycobacterium avium and Mycobacterium intracellulare;
• localized infections caused by Mycobacterium chelonae, Mycobacterium fortuitum and Mycobacterium kansasii;
• prevention of infection caused by Mycobacterium avium complex (MAC) in HIV-infected patients with the content of the CD4 lymphocytes (T helper lymphocytes) no more than 100 to 1 mm 3;
• H. pylori eradication and reduction in relapse rate of duodenal ulcer;
• odontogenic infection.

Use during pregnancy and lactation

The safety of using clarithromycin during pregnancy and lactation has not been established. The use of clarithromycin during pregnancy (especially in the first trimester) is possible only if there is no alternative therapy, and the potential benefit to the mother exceeds the potential risk to the fetus. If it is necessary to take it during lactation, breastfeeding should be discontinued.

Contraindications

• hypersensitivity to clarithromycin, macrolides and other components of the drug;
• simultaneous use of clarithromycin with the following drugs: astemizole, cisapride, pimozide, terfenadine;
• concomitant use of clarithromycin with ergot alkaloids, for example, ergotamine, dihydroergotamine;
• concomitant use of clarithromycin with midazolam for oral use;
• concomitant use of clarithromycin with inhibitors of HMG-COA reductase (statins), which are largely metabolized by CYP3A4 (lovastatin or simvastatin), in connection with the increased risk of myopathy, including rhabdomyolysis;
• concomitant use of clarithromycin and colchicine;
• couse of clarithromycin with ticagrelor or ranolazine;
• prolonged QT interval in history (was congenital or acquired QT prolongation) or ventricular arrhythmias, including ventricular tachycardia type “pirouette”;
• hypokalaemia (risk of QT interval prolongation);
• severe liver failure, occurring simultaneously with renal insufficiency;
• cholestatic jaundice/hepatitis in history, which developed in the application of clarithromycin;
• breastfeeding;
• age to 18 years (efficacy and safety not established).

Side effects

From the cardiovascular system: rarely-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. Tooth discoloration is reversible and is usually repaired by professional brushing at the dentist.

Rarely, liver function disorders were observed, including increased activity of liver enzymes, hepatic cell and / or cholestatic hepatitis with or without jaundice. These liver function disorders can be severe, but they are usually reversible. Very rare cases of liver failure and death were observed, mainly against the background of severe concomitant diseases and/or concomitant drug therapy.

From the central nervous system: transient headaches, dizziness, anxiety, insomnia, nightmares, ringing in the ears, depersonalization, hallucinations, convulsions, fear; rarely – psychosis, confusion; in some cases – hearing loss (when stopping taking clarithromycin, hearing was restored), changes in the sense of smell (usually accompanied by distortions of taste sensations).

Allergic reactions: urticaria, hyperemia of the skin, pruritus, anaphylaxis, Stevens-Johnson syndrome.

From the hematopoietic system: leukopenia, thrombocytopenia.

On the part of laboratory parameters: increased blood creatinine; rarely-hypoglycemia (with simultaneous use of hypoglycemic drugs).

Other: development of microbial resistance.

How to take, course of use and dosage

The average oral dose for adults is 250 mg 2 times / day. If necessary, you can prescribe 500 mg 2 times a day.

The duration of treatment is 6-14 days.

For the treatment of infections caused by Mycobacterium avium, Klacid is prescribed orally-1 g 2 times a day. The duration of treatment may be 6 months or more.

Overdose

Symptoms: Taking a large dose of clarithromycin may cause symptoms of gastrointestinal disorders. One patient with a history of bipolar disorder after taking 8 g of clarithromycin described changes in mental state, paranoid behavior, hypokalemia and hypoxemia.

Special instructions

Caution should be exercised when prescribing the drug to patients with impaired liver function. In the presence of chronic liver diseases, it is necessary to conduct regular monitoring of serum enzymes.

Caution should also be exercised when prescribing the drug to patients with mild to moderate renal impairment. For severe renal impairment (creatinine clearance less than 30 ml/min), fast-release clarithromycin (250 mg or 500 mg tablets) should be prescribed.

When co-administered with warfarin or other indirect anticoagulants, prothrombin time should be monitored.

Form of production

Film-coated tablets

Storage conditions

In a dark place, at a temperature not exceeding 30 °C

Shelf life

1 year

Active ingredient

Clarithromycin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children as prescribed by a doctor, Children over 12 years of age, Adults as prescribed by a doctor

Indications

Stomach and Duodenal Ulcers, Tonsillitis, Gastrointestinal Infections Caused by Helicobacter Pylori, Sinusitis, Bronchitis, Otitis Media, Colds, Respiratory Tract Infections, Skin Infections, Boils, Sore Throat