Description
Release form
Tablets
Packaging
50 units
Pharmacological action
Rosart – a lipid-lowering drug from the group of statins. Selective competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) – reductase – enzyme, converting HMG-CoA to mevalonate, a precursor of cholesterol.
Increases the number of low density lipoprotein receptors (LDL) on the surface of hepatocytes, which leads to increased uptake and catabolism of LDL, inhibition of very low density lipoprotein synthesis (VLDL), reducing the total number of LDL and VLDL. Reduces elevated cholesterol-LDL cholesterol-high-density non-lipoprotein (non-HDL) cholesterol, cholesterol-VLDL, total cholesterol, triglycerides (TG), TG-VLDL, apolipoprotein B (ApoV), lowers the ratio of total LDL-cholesterol, LDL-cholesterol / HDL cholesterol, non-HDL cholesterol / HDL cholesterol, ApoV / apolipoprotein AI (ApoA-I), increases the concentration of HDL cholesterol, ApoA-I level.
Hypolipidemic effect is directly proportional to the size of the prescribed dose. The therapeutic effect appears within 1 week after the start of therapy, after 2 weeks it reaches 90% of the maximum, by 4 weeks it reaches a maximum and after that it remains constant. Effective in adult patients with hypercholesterolemia with or without hypertriglyceridemia (regardless of race, gender or age), including in patients with diabetes mellitus and familial hypercholesterolemia. In 80% of patients with type IIa and IIb hypercholesterolemia (Fredrickson classification) with an average baseline LDL cholesterol of about 4.8 mmol / L while taking the drug at a dose of 10 mg, LDL cholesterol reaches values less than 3 mmol / L. In patients with homozygous familial hypercholesterolemia, taking the drug at a dose of 20 mg and 40 mg, the average decrease in LDL cholesterol is 22%.
The additive effect is observed in combination with fenofibrate (in relation to lowering the concentration of triglycerides (TG) and in nicotinic acid in lipid lowering doses (in relation to lowering the concentration of HDL cholesterol). 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) – reductase – an enzyme that converts HMG-CoA to mevalonate, a precursor of cholesterol.
Increases the number of low lipoprotein receptors density (LDL) on the surface of hepatocytes, which leads to increased uptake and catabolism of LDL, inhibition of the synthesis of very low density lipoproteins (VLDL), reducing the total amount of LDL and VLDL. It reduces the high content of LDL cholesterol, high-density non-lipiprotein cholesterol (non-HDL), VLDL cholesterol, total cholesterol, triglycerides (TG), VL-VLDL, apolipoprotein B (ApoV), lowers the ratio of LDL cholesterol / HDL cholesterol, total cholesterol, L-cholesterol / non-HDL / HDL cholesterol, ApoV / apolipoprotein AI (ApoA-I), increases the concentration of HDL cholesterol, ApoA-I level.
Hypolipidemic effect is directly proportional to the size of the prescribed dose. The therapeutic effect appears within 1 week after the start of therapy, after 2 weeks it reaches 90% of the maximum, by 4 weeks it reaches a maximum and after that it remains constant. Effective in adult patients with hypercholesterolemia with or without hypertriglyceridemia (regardless of race, gender or age), including in patients with diabetes mellitus and familial hypercholesterolemia. In 80% of patients with type IIa and IIb hypercholesterolemia (Fredrickson classification) with an average baseline LDL cholesterol of about 4.8 mmol / L while taking the drug at a dose of 10 mg, LDL cholesterol reaches values less than 3 mmol / L. In patients with homozygous familial hypercholesterolemia, taking the drug at a dose of 20 mg and 40 mg, the average decrease in LDL cholesterol is 22%.
The additive effect is observed in combination with fenofibrate (in relation to a decrease in triglyceride (TG) concentration and with nicotinic acid in lipid lowering doses (in relation to a decrease in HDL cholesterol). antibacterial activity, has a bacteriostatic effect: binding to the 50S subunit of ribosomes, inhibits translocation and transpeptidation reactions, the formation of peptide bonds between amino acids and the peptide chain, inhibits protein synthesis by ribosomes, as a result of which inhibits the growth and reproduction of bacteria. Good penetration into the cell ensures the effectiveness of roxithromycin against intracellular pathogens (including Chlamydia trachomatis, Chlamydia pneumoniae, Ureaplasma urealyticum, Legionella pneumophila, Mycoplasma pneumoniae). In vitro
are susceptible to the preparation: Streptococcus agalactiae, Streptococcus pneumoniae, Neisseria meningitidis, Listeria monocytogenes, Mycoplasma pneumoniae, Chlamydiat rachomatis, Chlamydia psittaci, Ureaplasma urealyticum, Legrellrellella rhellella rhellella rhellella rhella rgellophella Haemophilus ducreyi. The following microorganisms demonstrated in vitro variable sensitivity: Streptococcus pyogenes (group A beta-hemolytic streptococcus), Staphylococcus aureus, Haemophilus influenzae, Staphylococcus epidermidis.
Roxithromycin is also effective against anaerobic microorganisms: Bacleroides oralis, Bacteroides melaninogenicus, Bacteroides urealiticus Clostridium perfringens Eubacterium spp., Peptococcus spp., Peptostreptoctscus spp., acrioneticettsettsettsettsettsettsettiiettsi contsettsettsi etumtactiettsi contsettsi contsettsi contsettsettsi etumtacti conumttsettsi contsettsettsi ticumtsettsi contsettsettsettsettsettsettsettsettsi contsettsettsettsettsettsettsettsettsettsettsettsettsettsittsettsettsitsettsii
Resistant to the preparation: Bacleroides fragilis, Clostridium difficile, Pseudomonas spp. Acinetobacter spp., Enterobacteriaceae family.
Pharmacokinetics
Quickly absorbed from the gastrointestinal tract after oral administration. Roxithromycin is stable in the acidic environment of the stomach, eating 15 minutes after taking the pill does not affect absorption. Cmax after oral administration of 150 mg – 6.6 mg / L, the time to reach the maximum concentration (TCmax) – 2.2 hours, after 300 mg – 9.6 mg / L and 1.5 hours, respectively. In children, Cmax (with 2-fold administration of 2.5 mg / kg / day) is 8.7-10.1 mg / l and is achieved after 2 hours. Admission with an interval of 12 hours ensures the preservation of effective blood concentrations for 24 h. The equilibrium concentration (Css) in plasma when taken 150 mg 2 times a day for 10 days is reached after 2-4 days and is 9.3 mg / l when taken 300 mg 1 time per day for 11 days – 10, 9 mg / l. Communication with plasma proteins is 96%. It is characterized by high penetration into the tissues, especially into the lungs, palatine tonsils and prostate gland. Roxithromycin also penetrates well into cells (macrophages) and body fluids. Almost does not penetrate the blood-brain barrier. Roxithromycin in small quantities is excreted in breast milk. Distribution volume – 31.2 l.
It is partially metabolized in the liver, most (more than 50% of the active substance) is excreted by the intestine unchanged, about 12% is excreted by the kidneys and about 15% by the lungs. The half-life of roxithromycin after a single dose of 150 mg is an average of 12 hours.
With insufficiency of liver function, T1 / 2 and Cmax increase.
Indications
Infectious and inflammatory diseases, caused by microorganisms sensitive to roxithromycin: infections of the upper and lower respiratory tract and ENT organs (tonsillitis, pharyngitis, sinusitis, scarlet fever, diphtheria, pertussis, otitis media, pneumonia, bacterial infections in COPD, acute bronchitis and exacerbation of chronic, panbroncholitis, bronchiectasis) urogenital system (urethritis, endometritis, cervicitis, vaginitis, including genital infections, except gonorrhea), skin and soft tissues (erysipelas, phlegmon, boils, folliculitis, impetigo, pyoderma), oral cavity (periodontitis), bones ( P eriostitis, chronic osteomyelitis), migratory erythema, trachoma, brucellosis). Prevention of meningococcal meningitis in people in contact with the sick. Prevention of bacteremia in patients with endocarditis after dental interventions.
Contraindications
Hypersensitivity (including to other macrolides), breast age (up to 2 months), concurrent use of ergotamine or dihydroergotamine.
Use during pregnancy and lactation
Should not be prescribed during pregnancy (the safety of roxithromycin in the fetus in humans has not been determined). At the time of treatment, breastfeeding should be discontinued (passes into breast milk).
Special instructions
In patients with liver failure, the drug is used with caution, under the control of liver function and, if necessary, with dose adjustment.
When prescribing the drug to patients with renal failure, as well as elderly patients, there is no need for dose adjustment.
With the development of superinfection, allergic reactions, roxithromycin should be discontinued immediately and appropriate therapy should be prescribed.
Like other macrolides, roxithromycin can aggravate the course of myasthenia gravis, and therefore, the use of roxithromycin in such patients requires caution and monitoring of the patient’s condition.
When using the drug, both on the background of taking it, and after 2-3 weeks, after discontinuation of treatment, diarrhea may develop, caused by Clostridium difficile (pseudomembranous colitis). In mild cases, it is sufficient to cancel the treatment and use of ion-exchange resins (colestyramine, colestipol), in severe cases, compensation for the loss of fluid, electrolytes and protein, the appointment of vancomycin or metronidazole is indicated. Do not use drugs that inhibit intestinal motility.
Effect on the ability to drive vehicles and work with mechanisms
When using the drug, care should be taken when driving vehicles and engaging in activities that require increased concentration and speed of psychomotor reactions. In case of adverse reactions from the nervous system (such as dizziness, hallucinations), patients are not recommended to engage in potentially dangerous activities.
Composition
Active ingredient: roxithromycin 150 mg
Excipients: hyprolose – 19.65 mg, poloxamer – 150 ?g, povidone K30 – 4.2 mg, colloidal silicon dioxide – 1.8 mg, 1.875 – 1.875 g talc – 2.25 mg maize starch – 210 mg.
Shell composition: hypromellose – 2.78 mg, dextrose – 1.12 mg, titanium dioxide – 270 ?g, propylene glycol – 830 ?g.
Dosage and Administration
Inside. The drug should be taken before meals, drinking plenty of fluids.
Adults and children over 12 years of age (with a body weight of more than 40 kg): the standard dose is 150 mg 2 times a day, with an interval of 12 hours or 300 mg once (for adults only).
In elderly patients, a single and daily dose of roxithromycin does not change.
In renal failure, roxithromycin is prescribed in a dose of 150 mg 2 times a day.
In patients with severe hepatic insufficiency (for example, with cirrhosis with jaundice or ascites), the dose should be reduced by 2 times, that is, 150 mg of roxithromycin once a day.
Duration of treatment
The duration of taking roxithromycin depends on the indications for use, the microorganism that caused the infection and the severity of the infection process. In adults, the usual duration of treatment is 5-10 days for infections caused by beta-hemolytic streptococcus, the course of treatment should be at least 10 days. In children, the usual duration of treatment is 5-10 days for infections caused by beta-hemolytic streptococcus, the course of treatment should be at least 10 days. The duration of therapy should not exceed 10 days.
Side effects of the
From the gastrointestinal tract: nausea, vomiting, anorexia, constipation / diarrhea (very rare with blood), abdominal pain, flatulence, transient increase in liver transaminases and alkaline phosphatase activity, cholestatic hepatitis or hepatocellular acute hepatitis, symptoms of pancreatitis, pseudomembranous enterocolitis.
From the nervous system and sensory organs: dizziness, headache, weakness, malaise, blurred vision, change in taste and / or smell, tinnitus, paresthesia.
Allergic reactions: itching, rash, flushing of the skin, urticaria, eczema, angioedema, bronchospasm, anaphylactic shock.
Others: development of superinfection, candidiasis of the oral cavity and vagina, eosinophilia, hypercreatininemia, nail pigmentation.
Overdose
Symptoms: Dose-related side effects may increase.
Treatment: gastric lavage, symptomatic therapy.
Storage Conditions
In a dark place at a temperature not exceeding 25 ° C.
shelf life
3 years
Deystvuyushtee substance
Roxithromycin
Conditions of release from drugstores
Prescription
Dosage form
tablets
Indications
Indications
Urinary tract infections, Infections, Skin infections, cations, Pharyngitis, Sinusitis, Pneumonia
Ozon, Russia
