Roxithromycin
Roxithromycin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Roxithromycin
ATX code: J01FA06
Active ingredient: roxithromycin (roxithromycin)
Manufacturer: Ozone, LLC (Russia)
Description and photo updated: 22.11.2018
Prices in pharmacies: from 155 rubles.
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Roxithromycin is a semi-synthetic antibacterial drug from the macrolide group with a wide spectrum of activity.
Release form and composition
Dosage form of Roxithromycin - film-coated tablets: round biconvex, shell and core color - white, engraving "164" on one side (in a cardboard box 1-5 or 10 blisters of 10, 25 or 30 tablets or 1 can 10, 20, 30, 40, 50 or 100 tablets).
Composition of 1 tablet:
- active substance: roxithromycin - 150 mg;
- auxiliary components: poloxamer - 0.15 mg; povidone K30 - 4.2 mg; talc - 2.25 mg; colloidal silicon dioxide - 1.875 mg; corn starch - up to 210 mg; hyprolosis - 19.65 mg; magnesium stearate - 1.875 mg;
- shell: titanium dioxide - 0.27 mg; dextrose - 1.12 mg; hypromellose - 2.78 mg; propylene glycol - 0.83 mg.
Pharmacological properties
Pharmacodynamics
Roxithromycin is a semi-synthetic macrolide antibiotic with a broad spectrum of antibacterial activity. It has a bacteriostatic effect - inhibits the growth and reproduction of bacteria, which is associated with the main effects of the substance: binding to the 50S ribosome subunit, suppression of the transpeptidation and translocation reaction, the formation of peptide bonds between the peptide chain and amino acids, inhibition of protein synthesis by ribosomes.
The efficacy of roxithromycin in relation to intracellular pathogens (including Mycoplasma pneumoniae, Ureaplasma urealyticum, Chlamydia pneumoniae, Chlamydia trachomatis, Legionella pneumophila) is ensured due to good cell penetration.
The following are susceptible to the action of roxithromycin: Neisseria meningitidis, Mycoplasma pneumoniae, Listeria monocytogenes, Chlamydia Trachomatis, Ureaplasma urealyticum, Chlamydia psittaci, Legionella pneumophila, Gardnerella vaginalis.
The following microorganisms have variable sensitivity: Staphylococcus aureus, Streptococcus pyogenes (group A beta-hemolytic streptococcus), Staphylococcus epidermidis, Haemophilus influenzae.
Roxithromycin is also effective in relation to anaerobic microorganisms: Eubacterium spp., Peptostreptococcus spp., Peptococcus spp., Propionibacterium acnes, Rickettsia conorii, Rickettsia rickettsii, Bacteroides melaninogenic oralis.
Resistant to the action of the drug: family Enterobacteriaceae, Bacteroides fragilis, Acinetobacter spp., Pseudomonas spp., Clostridium difficile.
Pharmacokinetics
After oral administration, roxithromycin is rapidly absorbed from the gastrointestinal tract. Shows stability in the acidic environment of the stomach, food intake 15 minutes after taking the pill has no effect on absorption. With max (maximum concentration of the substance) after oral administration of 150 or 300 mg of roxithromycin is 6.6 or 9.6 mg / l, the time to reach C max is 2.2 or 1.5 hours, respectively.
In children, C max (with a double dose of 2.5 mg / kg per day) is achieved after 2 hours and ranges from 8.7 to 10.1 mg / l.
When taken with a break of 12 hours, effective blood concentrations are maintained for 24 hours.
C ss (equilibrium concentration) in plasma when taken 2 times a day at 150 mg for 10 days is 9.3 mg / l and is achieved in 2-4 days; when taken 1 time per day, 300 mg for 11 days, C ss is 10.9 mg / l.
Communication with blood plasma proteins - 96%. Roxithromycin is characterized by high tissue penetration, especially into the lungs, prostate gland and palatine tonsils. The substance also penetrates well into body fluids and cells (macrophages). It is excreted in breast milk in insignificant quantities. It practically does not penetrate through the blood-brain barrier. The volume of distribution is 31.2 liters.
It undergoes partial metabolism in the liver, more than 50% of the active substance is excreted unchanged by the intestines, about 15% - by the lungs, 12% - by the kidneys. After a single dose of 150 mg of roxithromycin, T 1/2 (half-life) averages 12 hours.
In case of insufficiency of hepatic function, C max and T 1/2 increase.
Indications for use
According to the instructions, Roxithromycin is prescribed for mild / moderate infections that are caused by pathogens sensitive to the action of the active substance:
- infections of soft tissues and skin;
- infections of the upper and lower respiratory tract - tonsillitis, pharyngitis, acute sinusitis, bronchitis, pneumonia (including pneumonia caused by atypical pathogens, including Chlamydia pneumoniae, Chlamydia psittaci, Legionella pneumophila, Moraxella catarrhalis);
- infections in odontology, infections of the teeth and oral cavity (in adults);
- infections of the genitourinary system caused by Ureaplasma urealyticum and Chlamydia trachomatis (in adults).
Contraindications
Absolute:
- combined use with ergot vasoconstrictor alkaloids (dihydroergotamine, ergotamine), cisapride, pimozide, astemizole, terfenadine;
- porphyria;
- age up to 12 years or body weight up to 40 kg;
- pregnancy and lactation;
- individual intolerance to the components of the drug, as well as other macrolides.
Relative (Roxithromycin is prescribed under medical supervision):
- hepatic / renal failure;
- combined use with the following drugs: warfarin, disopyramide, colchicine, digoxin, dopamine receptor agonists - ergot alkaloids (including bromocriptine, cabergoline, lisuride, pergolide), theophylline, cyclosporine;
- myasthenia gravis (Erb-Goldflam disease);
- congenital lengthening of the QT interval, conditions contributing to the development of cardiac arrhythmias (including uncorrected hypokalemia or hypomagnesemia, clinically significant bradycardia), concomitant therapy with class IA and III antiarrhythmic drugs;
- age from 65 years.
Instructions for the use of Roxithromycin: method and dosage
Roxithromycin tablets are taken orally with a sufficient amount of liquid, preferably before meals.
Recommended dosage regimen: 2 times a day (with a break of 12 hours), 1 tablet. Adults, excluding patients with renal insufficiency, may be prescribed 2 tablets per day in one dose.
In severe liver failure (in particular, in liver cirrhosis with ascites or jaundice) Roxithromycin should be taken once a day, 1 tablet.
The duration of the course is determined by the indications, the severity of the infectious process and the microorganism that caused the infection. Usually, the duration of taking the drug is in the range from 5 to 10 days, with infections caused by beta-hemolytic streptococcus - at least 10 days. The maximum duration of therapy is 10 days.
Side effects
- hepatobiliary system: increased activity of hepatic transaminases (aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase), acute hepatocellular or cholestatic hepatitis (in some cases with jaundice);
- digestive system: vomiting, nausea, abdominal pain, diarrhea (in some cases with blood), pseudomembranous colitis, pancreatitis;
- nervous system: paresthesia, headache, dizziness, changes in taste sensations (including ageusia), impaired smell (including anosmia), temporary hearing loss, vertigo, hypoacusia, hallucinations;
- allergic reactions: anaphylactic shock, exudative erythema multiforme, bronchospasm, urticaria, angioedema, eosinophilia;
- skin reactions: redness, rash, purpura;
- others: superinfection, candidiasis.
Overdose
In case of an overdose, there may be an increase in dose-dependent side effects.
Recommended: gastric lavage; symptomatic treatment. There is no specific antidote.
special instructions
In liver failure, Roxithromycin should be used with caution under the control of hepatic function, if necessary, dose adjustment is performed.
If allergic reactions and superinfection occur, Roxithromycin is immediately discontinued and appropriate treatment is prescribed.
When using Roxithromycin, including the period 2-3 weeks after the end of therapy, pseudomembranous colitis may occur. In mild cases, discontinuation of the drug and the use of ion-exchange resins (colestipol, colestyramine) are usually sufficient, in severe cases, replacement of fluid, protein and electrolyte loss, metronidazole / vancomycin therapy is prescribed. It is impossible to use drugs that slow down intestinal motility.
Influence on the ability to drive vehicles and complex mechanisms
The question of the possibility of driving vehicles during the period of therapy with Roxithromycin should be decided individually, which is associated with the likelihood of developing disorders from the nervous system, including hallucinations and dizziness.
Application during pregnancy and lactation
Roxithromycin is not prescribed during pregnancy / lactation.
Pediatric use
It is contraindicated to take the drug in patients under 12 years of age or with a body weight of up to 40 kg.
With impaired renal function
Roxithromycin therapy for renal failure should be carried out under medical supervision.
For violations of liver function
Roxithromycin therapy for liver failure should be carried out under medical supervision.
Use in the elderly
Roxithromycin therapy in patients over 65 years old should be carried out under medical supervision.
Drug interactions
- drugs that are metabolized using the CYP3A isoenzyme (astemizole, pimozide or cisapride): prolongation of the QT interval and / or heart rhythm disturbances (in most cases with ventricular tachycardia such as pirouette), which is associated with an increase in their plasma concentration; the combination is contraindicated;
- disopyramide: its plasma concentration increases, and therefore it is recommended, if possible, to determine the concentration of disopyramide in the blood plasma and monitor the ECG;
- preparations containing dihydroergotamine or ergotamine (vasoconstrictor ergot alkaloids): possible development of arterial spasm and severe ischemia with necrosis of the extremities; the combination is contraindicated;
- terfenadine: the likelihood of severe complications from the cardiovascular system, including atrial fibrillation and ventricular fibrillation and other ventricular arrhythmias, increases; the combination is contraindicated;
- indirect anticoagulants (warfarin): an increase in prothrombin time, and therefore during the period of therapy it is recommended to regularly determine the INR (international normalized ratio);
- class IA and III antiarrhythmic drugs: possible summation of the effects of prolonging the QT interval of Roxithromycin and these drugs; combined therapy requires caution (under the control of an electrocardiogram);
- digoxin: its absorption will increase, which can lead to glycosidic intoxication (manifested in the form of nausea, vomiting, diarrhea, headache, dizziness); intoxication with cardiac glycosides can also lead to cardiac conduction / rhythm disturbances; with combined use, including a combination with other cardiac glycosides, it is recommended to regularly monitor the electrocardiogram and determine the concentration of cardiac glycoside in plasma (these measures are required in case of symptoms of an overdose of cardiac glycosides);
- dopamine receptor agonists - ergot alkaloids (including bromocriptine, lisuride, cabergoline, pergolide): their plasma concentration increases and, as a result, the pharmacodynamic effect increases and the risk of their side effects increases; combination therapy requires caution (despite the lack of information confirming such an interaction);
- colchicine: its plasma concentration increases, while the risk of its adverse reactions, including nephrotoxic effects, increases; combination therapy requires caution (despite the lack of information confirming such an interaction);
- theophylline, cyclosporine: their plasma concentration increases, while correction of the dosage regimen is usually not required;
- midazolam: its T 1/2 and the area under the concentration-time curve increases, which can lead to an increase and lengthening of its effects.
Analogs
Roxithromycin analogs are Elrox, Rulid, Esparoxy, Xitrocin, Rulicin.
Terms and conditions of storage
Store in a place protected from light at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Roxithromycin
According to reviews, Roxithromycin is an effective antibiotic most often used in the treatment of ureaplasmosis and mycoplasmosis. In some cases, they indicate the development of side effects.
The price of Roxithromycin in pharmacies
The approximate price for Roxithromycin (10 tablets) is 147 rubles.
Roxithromycin: prices in online pharmacies
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Drug name Price Pharmacy |
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Roxithromycin 150 mg film-coated tablets 10 pcs. 155 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
