Description
Latin name
RULID
Release form
Coated tablets.
10 pcs 10 pcs Packaging
.
Pharmacological action
Pharmacodynamics
Semi-synthetic antibiotic of the macrolide group for oral administration.
Usually sensitive to the drug: Bordetella pertussis. Borrelia burgdorferi. Moraxella (Branhamella) catarrhalis. Campylobacter coli. Campylobacter jejuni. Chlamydia trachomatis, psittaci and pneumoniae. Clostridium perfringens. Corynebacterium diptheriae. Enterococcus. Gardnerella vaginalis. Methi-S-Staphylococcus. Neisseria meningitidis. Helicobacter pylori. Legionella pneumophilia. Lysteria monocytogenes obiluncus. Mycoplasma pneumoniae. Pasteurella multocida. Peptostreptococcus. Porphyromonas. Propionibacterium acnes. Rhodococcus equi. Streptococcus pneumoniae. Streptococcus spp.
Moderately susceptible to the preparation: Haemophilus influenzae. Ureaplasma urealyticum. Vibrio cholerae.
Resistant to the drug: Acinetobacter spp. Bacteroides fragilis. Enterobacteriaceae. Methi-R Staphylococcus. Pseudomonas spp. Fusobacterium. Mycoplasma hominis. Nocardia.
Pharmacokinetics
Absorption and distribution of
Roxithromycin is rapidly absorbed after oral administration. Roxithromycin is more stable than other macrolides in the acidic environment of the stomach. Taking the drug 15 minutes before a meal does not affect the pharmacokinetics. After taking the drug in a dose of 150 mg, the maximum concentration in the blood averages 6.6 mg / l and is achieved after 2.2 hours. Taking the drug with an interval of 12 hours ensures the preservation of effective blood concentrations throughout the day. The half-life after a single dose of 150 mg is 10.5 hours. After a single dose of 300 mg of roxithromycin, the average maximum concentration in the blood is 9.7 mg / l and is achieved after 1.5 hours. With repeated administration of roxithromycin (150 mg twice a day, for 10 days), an equilibrium state in the plasma is reached between 2-4 days, making C max 9.3 mg / L. Reception of 300 mg of roxithromycin every 24 hours for 11 days provided With max at the level of 10.9 mg / L. Roxithromycin penetrates well into many tissues, especially the lungs, palatine tonsils and prostate gland. The drug also penetrates well into cells, especially into neutrophilic leukocytes and monocytes, stimulating their phagocytic activity. Binding to blood proteins is 96%, is saturable and decreases at concentrations of roxithromycin above 4 mg / L.
Metabolism and excretion
Roxithromycin is metabolized only partially, more than half of the active substance is excreted unchanged mainly with feces, as well as with urine. In adults with normal kidney and liver function, 65% of roxithromycin is excreted in feces. Less than 0.05% of the accepted dose of roxithromycin passes into breast milk.
Pharmacokinetics in special clinical cases
In renal failure, excretion of roxithromycin and its metabolites through the kidneys is approximately 10% of the dose taken. The dose of the drug does not change with renal failure. In severe liver failure, the elimination half-life lengthens (25 hours) and C max increases.
Indications
Upper respiratory tract infections: acute pharyngitis, tonsillitis, sinusitis
lower respiratory tract infections: pneumonia (including that caused by such “atypical” pathogens as Chlamydia psittaci, Chlamydia pneumoniae, Legamella, Mohrella, Mohamella, Mohrella, Mohrella, Moraxella, Mohrella, Mohamella, Moraxella and Moraxella mohlefella etc., bronchitis, bacterial infections in chronic obstructive pulmonary diseases
skin and soft tissue infections
genital infections (except gonorrhea), including: urethritis, cervicovaginitis
infections in odontology.
Contraindications
Hypersensitivity to
macrolides simultaneous administration of drugs such as ergotamine and dihydroergotamine
combined use with ergotamine derivatives and ergotamine-like vasoconstrictors is not allowed, as it can lead to tissue necrosis.
Precautions: use in patients with severe hepatic impairment.
Use during pregnancy and lactation
Roxithromycin is contraindicated in pregnancy.
Small amounts of roxithromycin pass into breast milk, so you must stop breast-feeding or taking the drug.
Composition
1 tablet contains:
Active ingredient: roxithromycin – 150 mg.
Excipients: hydroxypropyl cellulose, poloxamer, povidone KZO, colloidal silicon dioxide, magnesium stearate, talc, corn starch.
Shell composition: hypromellose, anhydrous glucose, titanium dioxide, propylene glycol.
Dosage and Administration
Adults are prescribed 150 mg of roxithromycin orally with an interval of 12 hours. In this case, the daily dose is 300 mg. Perhaps the appointment of 300 mg once a day.
Use in children
Children (body weight over 40 kg) are prescribed 150 mg of roxithromycin inside with an interval of 12 hours. The daily dose is 300 mg. This dosage form is not used in children under 4 years old!
Use in elderly patients
In elderly patients, the dosage and daily dose of roxithromycin does not change.
Use in patients with renal failure
In the presence of renal failure, roxithromycin is prescribed in a dose of 150 mg 2 times a day.
Use in patients with liver failure
In patients with liver failure, 150 mg is prescribed once.
The duration of taking roxithromycin depends on the indications for use, the severity of the infectious process and the activity of the pathogen. Roxithromycin is taken orally once or twice a day before meals. The tablet should be washed down with a sufficient amount of water.
Side effects
Anaphylactic reactions: angioedema, bronchospasm, weakness., anaphylactic shock (rare).
Skin reactions: rash, redness, urticaria.
Gastrointestinal reactions: nausea and vomiting, abdominal pain, diarrhea (very rare with blood).
Reactions from the liver: increased liver enzymes (ALT, ACT, ALP), cholestatic or hepatocellular acute hepatitis.
Possible: slight changes in taste and olfactory sensations.
In some cases: symptoms of pancreatitis, dizziness, headache, paresthesia were observed.
Possibly: development of superinfection due to the growth of insensitive microorganisms.
Drug Interaction
Concomitant administration of terfenadine is not recommended, due to the increased concentration of the latter when co-administered with macrolide antibiotics, which may lead to the development of severe ventricular arrhythmias.
Although this complication was not observed in roxithromycin, and no pharmacokinetic interactions or changes in ECG have been shown in volunteer studies, the combination of roxithromycin and terfenadine is not recommended.
Taking drugs such as astemizole, cisapride, pimozide may lead to prolongation of the QT interval and / or severe cardiac arrhythmias as a result of an increase in their serum concentration, as a result of competitive effects on the CYP3A isozyme between the above drugs and macrolides.
There is no interaction with warfarin, carbamazepine, ranitidine, antacids and oral contraceptives.
When administering roxithromycin with vitamin K antagonists, it is recommended to monitor prothrombin time or International Normalized Ratio (INR).
Roxithromycin can replace protein bound disopyramide, leading to an increase in serum levels of disopyramide.
ECG monitoring and, where possible, serum disopyramide levels are recommended.
Increased absorption of digoxin when co-administered with digoxin. It is recommended to monitor the electrocardiogram and serum level of cardiac glycoside.
This is mandatory when symptoms of an overdose of cardiac glycosides occur.
Roxithromycin may increase the half-life of midazolam, leading to an increase and prolongation of its action.
Overdose
Gastric lavage and symptomatic therapy are necessary for overdose. There is no specific antidote.
Storage conditions
Store at a temperature not exceeding + 25 ° С.
Keep out of the reach of children.
The Expiration of
is 3 years.
Deystvuyuschee substances
roksitromitsin
Terms of sale of
pharmacies Prescription
dosage form
dosage form
tablets
Sanofi-Aventis, France
