ROXITERO [Roxithromycin] 150 mg Film-coated tablets
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ROXITERO
instructions for
the medical use of the medicinal product
Tradename
Roxitero, Рокситеро
International non-proprietary name or generic name
Roxithromycin, Рокситромицин
Composition
Each film coated
tablet contains:
Active substance: roxithromycin 150 mg.
Excipients: lactose monohydrate, starch, Avicel 102, PVP K-30,
primogel, talc, magnesium stearate.
Tablets.
Antibiotic, macrolide.
Pharmacodynamics
Semisynthetic antibiotic from the macrolide group with a broad spectrum
of antibacterial activity. It has a bacteriostatic effect: by binding to the
50S ribosome subunit, it suppresses the reactions of translocation and
transpeptidation, the formation of peptide bonds between amino acids and the
peptide chain, inhibits protein synthesis by ribosomes, as a result of which it
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 susceptible to the
drug: Streptococcus agalactiae, Streptococcus pneumoniae, Neisseria meningitidis,
Listeria monocytogenes, Mycoplasma pneumoniae, Chlamydiat rachomatis, Chlamydia
psittaci, Ureaplasma urealyticum, Legionobella pneumacteris, The following
microorganisms have shown variable sensitivity in vitro: 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., Peptostreptococcus spp., Propionibactenum acnes; Rickettsia rickettsii,
Rickettsia conorii. Resistant to the drug: Bacleroides fragilis, Clostridium
difficile, Pseudomonas spp .; Acinetobacter spp., Family Enterobacteriaceae.
It is rapidly absorbed from the gastrointestinal tract after oral
administration. Roxithromycin is stable in the acidic environment of the
stomach, food intake 15 minutes after taking the tablet does not affect
absorption. Cmax after oral administration of 150 mg - 6.6 mg / l, the time to
reach the maximum concentration - 2.2 hours, after taking 300 mg - 9.6 mg / l
and 1.5 hours, respectively. In children, Cmax (with a 2-fold intake of 2.5 mg
/ kg / day) is 8.7-10.1 mg / l and is achieved after 2 hours. Reception with an
interval of 12 hours ensures the preservation of effective concentrations in
the blood for 24 h. Equilibrium concentration (Css) in plasma when taking 150
mg 2 times a day for 10 days is achieved after 2-4 days and is 9.3 mg / l; when
taking 300 mg once a day for 11 days - 10.9 mg / l. The connection with blood
plasma proteins is 96%. It is characterized by high tissue penetration,
especially into the lungs, palatine tonsils and the prostate gland.
Roxithromycin also penetrates well into cells (macrophages) and body fluids.
Practically does not penetrate the blood-brain barrier. Roxithromycin is
excreted in breast milk in small amounts. The volume of distribution is 31.2
liters. Partially metabolized in the liver, most (more than 50% of the active
substance) is excreted unchanged by the intestines, 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 12 hours on average. If liver function is
insufficient, T1 / 2 and Cmax increase.
Mild to moderate infections caused by pathogens
sensitive to roxithromycin:
In
adults
• upper respiratory tract infections:
pharyngitis, tonsillitis, acute sinusitis;
• lower respiratory tract infections: pneumonia
(including pneumonia caused by "atypical" pathogens, including
Chlamydia psittaci, Chlamydia pneumoniae, Moraxella catarrhalis, Legionella
pneumophila), bronchitis;
• infections of the skin and soft tissues;
• infections of the genitourinary tract caused
by Chlamydia trachomatis and Ureaplasma urealyticum;
• infections in odontology, infections of the
oral cavity and teeth.
In
children
• upper respiratory tract infections:
tonsillitis, pharyngitis, acute sinusitis;
• lower respiratory tract infections: pneumonia
(including pneumonia caused by "atypical" pathogens, including
Chlamydia psittaci, Chlamydia pneumoniae, Moraxella catarrhalis, Legionella
pneumophila), bronchitis;
• infections of the skin and soft tissues.
• hypersensitivity to roxithromycin, other
macrolides or other components of the drug;
• liver failure;
• renal failure;
• pregnancy;
• lactation period;
• children under 12 years of age.
Method of administration and dosage
Inside
before eating, drinking plenty of water.
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, the single and daily dose does not change.
In
case of renal failure, it is prescribed in a dose of 150 mg 2 times a day.
In
patients with severe hepatic impairment (for example, with cirrhosis of the
liver with jaundice or ascites), the dose should be reduced by 2 times, that
is, 150 mg once a day.
The
duration of the course depends on the indications for use, the severity of the
infectious process and the activity of the pathogen.
Special instructions and precautions
When prescribing to patients with hepatic impairment, caution should be
exercised, dose adjustments should be made, and liver function should be
monitored.
Use with caution in patients with renal impairment.
With the joint appointment of terfenadine, astemizole, cisapride,
pimozide, it is necessary to monitor the ECG indicators.
With the development of superinfection, allergic reactions, you should
immediately stop taking the drug and prescribe appropriate therapy.
Influence
on the ability to drive vehicles and mechanisms
Due to the possibility
of dizziness, caution is required when driving and working with equipment.
Application during pregnancy
and during breastfeeding
Contraindicated
for use during pregnancy. If it is necessary to use the drug during lactation,
the issue of stopping breastfeeding should be resolved.
Interaction with other medicinal
products
Roxithromycin is not prescribed concurrently with drugs containing
ergotamine or dihydroergotamine (vasoconstrictor ergot alkaloids). This
combination can provoke arterial spasm and cause severe ischemia with the
development of necrosis of the extremities.
With the simultaneous use of antibiotics of the macrolide group (such as
erythromycin) with terfenadine, there was an increase in the risk of developing
severe complications from the cardiovascular system, including atrial
fibrillation and other ventricular arrhythmias. Although no such reactions have
been observed with roxithromycin, this concomitant use is contraindicated.
The use of drugs such as astemizole, cisapride, or pimozide, which are
metabolized by the isoenzyme CYP3A, has been associated with prolongation of
the QT interval and / or cardiac arrhythmias (usually with the development of
pirouette-type ventricular tachycardia) as a result of an increase in plasma
concentrations due to interaction with inhibitors this isoenzyme, including
some antibiotics from the macrolide group. Therefore, the combined use of these
drugs with roxithromycin is contraindicated.
Simultaneous use with indirect anticoagulants (warfarin) can lead to an
increase in prothrombin time. It is recommended to regularly determine the
international normalized ratio (INR) while using roxithromycin with indirect
anticoagulants.
Roxithromycin can displace disopyramide from its connection with plasma
proteins, leading to an increase in its concentration in blood plasma. ECG
monitoring and, if possible, determination of the concentration of disopyramide
in blood plasma is recommended.
When taken simultaneously with digoxin, an increase in its absorption is
possible, which can lead to the development of glycosidic intoxication. It can
manifest itself with symptoms such as nausea, vomiting, diarrhea, headache,
dizziness; intoxication with cardiac glycosides can also cause cardiac
conduction disturbances or cardiac arrhythmias. Therefore, in patients taking
roxithromycin and digoxin (or other cardiac glycosides), it is recommended to
regularly monitor the ECG and determine the plasma concentrations of cardiac
glycoside. This is necessary when symptoms of an overdose of cardiac glycosides
appear.
Roxithromycin, like other macrolides, should be used with caution in
patients receiving class IA and III antiarrhythmics (ECG monitoring is
required), since macrolides, including roxithromycin, as well as these antiarrhythmic
drugs, can prolong the QT interval and there is a possibility of summation of
the effects of prolongation the QT interval of these drugs.
With the simultaneous use of some macrolides with dopamine receptor
agonists - ergot alkaloids (including bromocriptine, cabergoline, lisuride,
pergolide), an increase in plasma concentrations of the latter was observed,
which can enhance their pharmacodynamic effect and increase the risk of
developing their side effects. Care should be taken with the simultaneous use
of roxithromycin and dopamine receptor agonists - ergot alkaloids.
Roxithromycin, like other macrolide antibiotics, can increase the area
under the concentration-time curve and T1 / 2 of midazolam, and therefore the
effects of midazolam can be enhanced and prolonged in patients treated with
roxithromycin.
The simultaneous use of roxithromycin and theophylline or cyclosporine
can cause an increase in plasma concentrations of the latter, which, as a rule,
does not require a correction of the dosage regimen.
From the digestive system: nausea, vomiting, abdominal pain, diarrhea
(sometimes with blood), anorexia, flatulence, pancreatitis, pseudomembranous
colitis.
From the liver: increased activity of "hepatic"
transaminases (ALT (ALT) and AST (ACT) and / or alkaline phosphatase), acute
cholestatic or hepatocellular hepatitis (sometimes with the development of
jaundice).
From the nervous system: dizziness, headache, paresthesia, changes in taste,
impaired smell, hallucinations, temporary hearing loss, hypoacusia (incomplete
hearing loss), vertigo.
Allergic reactions: rash, redness, purpura, urticaria, angioedema,
bronchospasm, eosinophilia, anaphylactic shock, erythema multiforme.
Others: development of superinfection, candidiasis is possible.
If any of the side
effects indicated in the instructions are aggravated, or you notice any other
side effects not listed in the instructions, inform your doctor.
Symptoms: Possible increased dose-related side effects.
Treatment: gastric lavage, symptomatic therapy. There is no specific antidote.
Store in a dry and dark place, at a temperature not exceeding 25°C.
Keep out of the reach of children!
2 years. Do not use after the
expiration date printed on the package.
Dispensed by prescription.
Release form
10 tablets in aluminum foil blister. 1 blister with instructions for use
in a cardboard box.