Rotomox - instructions for use, dose, side effects, contraindications

Composition:1 tablet contains:
Active substance: moxifloxacin hydrochloride 436.80 is equivalent to moxifloxacin 400.00 mg.
Excipients: corn starch 188.46 mg, sodium methyl parahydroxybenzoate 0.015 mg, microcrystalline cellulose 55.00 mg, talc 7.00 mg, silicon colloidal dioxide 4.00 mg, magnesium stearate 14.00 mg, sodium carboxymethyl starch 24.00 mg.
Shell composition: Opaglass (shellac 60.0%, carnauba wax 25.0%, ethanol 10.0%, beeswax white 5.0%) - 0.035 mg; Opaprai pink (polyvinyl alcohol 58.0%, talc 3.0%, titanium dioxide 30.0%, macrogol 6.3%, lecithin 1.7%, ferric oxide red oxide 1.0%) - 0.70 mg.

Description:Oblong, biconvex tablets, covered with a film shell of pink color, with a risk on one side. On a cross-section the nucleus is from white to light yellowish-greenish color.

Pharmacotherapeutic group:Protivomicrobial agent-fluoroquinolone.

ATX: & nbsp

J.01.M.A.14 Moxifloxacin

Pharmacodynamics:Antimicrobial drug group of fluoroquinolones. Has a bactericidal effect.
The mechanism of action is due to the inhibition of bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, which leads to a disruption in the synthesis of DNA from the microbial cell.
In vitro, the drug is active against a wide range of gram-negative and gram-positive bacteria, anaerobic, acid-fast and atypical bacteria.
Effective against bacteria resistant to beta-lactam and macrolide antibiotics.
To moxifloxacin are sensitive aerobic gram-positive bacteria: Enterococcus faecalis, Staphylococcus aureus (including strains that are sensitive to methicillin), Streptococcus anginosus, Streptococcus constellatus, Streptococcus pneumoniae (including penicillin-resistant strains and macrolides), Streptococcus pyogenes (Group A);
gramotritsatelnye aerobic bacteria: Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (. including strains producing and not producing beta-lactamase), Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis (including strains that produce beta-lactamase ), Proteus mirabilis;
anaerobic bacteria: Bacteroides fragilis, Bacteroides thetaiotaomicronron, Clostridium perfringens, Peptostreptococcus spp .; also Chlamydia pneumoniae, Mycoplasma pneumoniae.
According to in vitro studies on moxifloxacin are also sensitive:
aerobic gram-positive bacteria: Staphylococcus epidermidis, Streptococcus agalactiae, Streptococcus group, viridans, aerobic gram-negative bacteria: Citrobacter freundii, Klebsiella oxytoca, Legionella pneumophila;
anaerobic bacteria: Fusobacterium spp., Prevotella spp.
There is no cross-resistance with penicillins, cephalosporins, aminoglycosides, macrolides and tetracyclines. The overall incidence of resistance is low.
In vitro studies have shown that resistance to moxifloxacin develops slowly as a result of a number of consecutive mutations.Between drugs from the group of fluoroquinolones develops cross-resistance. However, some Gram-positive and anaerobic microorganisms resistant to other fluoroquinolones are susceptible to moxifloxacin.

Pharmacokinetics:After oral administration moxifloxacin absorbed quickly and almost completely. Absolute bioavailability is about 91%.
After a single dose of 400 mg of moxifloxacin, the maximum concentration (Cmax) is reached within 0.5-4 hours and is about 3 μg / ml.
Moxifloxacin is rapidly distributed in tissues and organs and binds to blood proteins (mainly albumins) by about 45%. The distribution volume is approximately 2 l / kg. High concentrations of moxifloxacin, exceeding those in plasma, are created in lung tissue, in alveolar macrophages, bronchial mucosa, in the mucous membrane of the nasal sinuses, in foci of inflammation (in the contents of blisters in skin lesions). In the interstitial fluid and in the saliva moxifloxacin is determined in a free, non-protein-bound form at a concentration higher than in the plasma. In addition, high concentrations of the drug are determined in the tissues of the abdominal cavity, peritoneal fluid and female genital organs.
Moxifloxacin undergoes biotransformation of the 2nd phase and is excreted from the body by the kidneys, as well as the intestines both in unmodified form and in the form of inactive sulfo compounds and glucuronides. Moxifloxacin does not undergo biotransformation by the microsomal system of cytochrome P450.
The half-life of the drug is approximately 12 hours. The average total clearance after administration in a dose of 400 mg is from 179 to 246 ml / min. About 22% of a single dose (400 mg) is excreted unchanged by the kidneys, about 26% by the intestine.
Pharmacokinetics in special clinical cases:
There were no significant changes in the pharmacokinetics of moxifloxacin in patients with impaired renal and hepatic function (Child-Pugh class A, B).

Indications:Infectious-inflammatory diseases caused by micro-organisms sensitive to moxifloxacin:
- Acute sinusitis;
- exacerbation of chronic bronchitis;
- community-acquired pneumonia;
- skin and soft tissue infections;
- complicated intra-abdominal infections;
- uncomplicated infections of the pelvic organs.

Contraindications:- hypersensitivity to moxifloxacin, other quinolones and components of the drug;
- Pregnancy;
- lactation period;
- Children and adolescence (up to 18 years);
- epilepsy;
severe diarrhea;
- damage to the tendons during the previous treatment with quinolones;
- syndrome of congenital or acquired lengthening of the Q-T interval;
- pronounced bradycardia, severe heart failure with a decrease in the left ventricular ejection fraction, ventricular arrhythmias (when quinolones are used in the anamnesis);
- simultaneous reception of drugs that extend the Q-T interval (antiarrhythmic drugs of class IA, III);
- pronounced electrolyte imbalance (uncorrectable hypokalemia);
- severe hepatic insufficiency (Child-Pugh class C).

Carefully:Convulsive syndrome (in the anamnesis), atherosclerosis of cerebral vessels, cerebral circulatory disorders (in the anamnesis), organic diseases of the central nervous system, psychoses and other mental disorders in the anamnesis, myocardial ischemia, simultaneous administration of drugs prolonging the QT interval (including tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungals, imidazole derivatives, cisapride), myasthenia gravis,- pseudomembranous colitis, simultaneous administration of glucocorticosteroids, in women and elderly patients, with liver cirrhosis, glucose-6-phosphate dehydrogenase deficiency, diabetes mellitus, renal and / or hepatic insufficiency (Child-Pugh class A, B) hemodialysis, hepatic porphyria, diseases accompanied by a risk of developing ventricular arrhythmia, electrolyte imbalance (eg, hypokalemia, hypomagnesemia).

Dosing and Administration:The recommended dosage regimen of moxifloxacin is 400 mg (1 tablet) once a day. Do not exceed the recommended dose. The tablet should be swallowed whole, not liquid, squeezed with enough water, regardless of food intake.
Duration of therapy.
The duration of treatment is determined by the localization and severity of the infection, as well as clinical effect.
Exacerbation of chronic bronchitis: 5 days.
Acute sinusitis: 7 days.
Uncomplicated skin and soft tissue infections: 7 days.
Community-acquired pneumonia: 7-14 days.
Complicated infections of the skin and subcutaneous structures: 7-21 days.
Complicated intra-abdominal infections: 5-14 days.
Uncomplicated infections of the pelvic organs: 14 days.
Do not exceed the recommended duration of treatment.
Elderly patients
Changes in the dosing regimen in elderly patients are not required.
Violation of liver function
Patients with impaired liver function (class A, B by Child-Pugh) do not need to change the dosage regimen.
Renal insufficiency
In patients with impaired renal function (including with creatinine clearance <30 ml / min), as well as in patients on continuous hemodialysis and long-term outpatient peritoneal dialysis, changes in the dosing regimen are not required.

Side effects:Allergic reactions: urticaria, rash, itching, anaphylactic / anaphylactoid reactions, angioedema, including facial edema, larynx (potentially life-threatening), Stevens-Johnson syndrome, toxic epidermal, necrolysis, anaphylactic shock.
From the digestive system: abdominal pain, nausea, vomiting, diarrhea, increased activity of "liver" transaminases, flatulence, constipation, lack of appetite, stomatitis, glossitis, transient liver dysfunction,
discoloration of the tongue, jaundice, gastroenteritis, pseudomembranous colitis, hepatitis (mostly cholestatic), fulminant hepatitis.
From the nervous system: headache, pain, dizziness, insomnia or drowsiness, pathological dreams; hallucinations, feelings of anxiety, increased muscle tone, impaired coordination of movements, agitation; amnesia, paresthesia, hypesthesia, hypersthesia, dysesthesia, tremor, disorientation, psychomotor hyperactivity, emotional lability, speech disorders, attention disturbance, convulsions, confusion, depression, depersonalization, psychotic reactions with behavioral disorders with self-harm.
From the sense organs: visual impairment, (blurred vision, decreased visual acuity), a violation of taste sensitivity, loss of taste sensitivity, tinnitus, impaired sense of smell, anosmia.
From the cardiovascular system: prolongation of the Q-T interval (often in patients with concomitant hypokalemia), palpitations, nonspecific arrhythmias, tachycardia, increased and decreased blood pressure, pain in (chest, fainting,vasodilation / (blood flushes to the face), ventricular tachyarrhythmias, polymorphic ventricular tachycardia, cardiac arrest (predominantly in persons with predisposing arrhythmias, such as clinically significant bradycardia, acute myocardial ischemia).
From the respiratory system: shortness of breath, asthmatic condition.
From the musculoskeletal system: arthralgia, myalgia, tendinitis, back pain, leg pain, arthritis, tendon ruptures, increased symptoms of myasthenia gravis.
From the genitourinary system: vaginal candidiasis, vaginitis, abdominal pain, facial edema, peripheral edema, renal dysfunction, renal failure.
Laboratory indicators: anemia, leukopenia, neutropenia, thrombocytopenia, leukocytosis, increased prothrombin time, increased / decreased international normalized ratio, eosinophilia, thrombocytosis, changes in thromboplastin and prothrombin concentration, increased activity of gamma-glutamintransferase, lactate dehydrogenase, alkaline phosphatase, amylase, increased bilirubin concentration, decreased prothrombin time, hyperglycemia, hyperlipidemia, hyperuricemia.
Other: candidiasis, general discomfort, asthenia, sweating.

Overdose:There are limited data on the overdose of moxifloxacin. In case of an overdose, one should be guided by the clinical picture and carry out symptomatic maintenance therapy with ECG monitoring.

Interaction:With the simultaneous use of moxifloxacin and glucocorticosteroids, the risk of developing tendovaginitis and rupture of the tendon increases.
No dosage regimen correction is required when combined with atenolol, ranitidine, calcium-containing additives, theophylline, oral contraceptives, glibenclamide, itraconazole, digoxin, morphine, probenecid.
Antacids, multivitamins and minerals
The use of moxifloxacin concomitantly with antacid agents, multivitamins and minerals can lead to impaired moxifloxacin absorption due to the formation of chelate complexes. In this regard, antacids, preparations containing vitamins, magnesium, aluminum, iron or zinc salts, sucralfate should be taken at least 4 hours before or 4 hours after ingestion of moxifloxacin.
Warfarin
When combined with warfarin prothrombin time and other parameters, blood clotting does not change. However, in patients receiving concomitant treatment with these drugs, it is necessary to monitor the INR (international standardized ratio) and, if necessary, adjust the dose of oral anticoagulants.
Digoxin
Moxifloxacin and digoxin has no significant effect on the pharmacokinetic parameters of each other. With the appointment of repeated doses, moxifloxacin, the maximum concentration of digoxin increased. approximately 30%, and the minimum concentration of digoxin did not change.
Activated carbon
With simultaneous oral administration of activated carbon and moxifloxacin, the systemic bioavailability of moxifloxacin is reduced by more than 80% as a result of inhibition of its absorption.
Dairy products and food intake
Absorption of moxifloxacin does not change with simultaneous intake of food (including dairy products).
Drugs that extend the Q-T interval
The potential interactions of moxifloxacin, resulting in the risk of developing additive action, to an increase in the Q-T interval: with drugs that extend the Q-T interval (incl.antiarrhythmic drugs of class IA, III tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungals, imidazole derivatives, cisapride).

Special instructions:In some cases, after the first use of the drug may develop allergic reactions of varying severity. In these cases, the use of moxifloxacin should be abolished and the necessary medical measures taken.
During treatment with moxifloxacin, inflammation and rupture of the tendon can develop, especially in elderly patients and in patients taking glucocorticosteroids in parallel. At the first signs of pain or inflammation of the tendons, patients should stop treatment and immobilize the affected limb.
When moxifloxacin is used, prolongation of the Q-T interval may be noted in some patients. Because women, compared to men, have a longer interval, they may be more sensitive to drugs that extend the Q-T interval. Elderly patients are also more prone to drugs that extend the Q-T interval.
There is a direct relationship between an increase in the concentration of moxifloxacin and an increase in the QT interval (risk of developing ventricular arrhythmias, including torsade de pointes). As a consequence, this is not.should exceed the recommended dose (400 mg / day).
Moxifloxacin should be avoided in patients with established QT interval elongation, patients with severe bradycardia, severe heart failure with a decrease in the left ventricular ejection fraction, ventricular arrhythmias (with quinolones in the history), and patients who use antiarrhythmic drugs of class IA, III, in patients with uncorrectable hypokalemia.
Because of the risk of developing an additive effect on the QT interval, moxifloxacin should be used with caution simultaneously with drugs that extend the Q: T interval (including tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungals, imidazole derivatives, cisapride), patients with myocardial ischemia, in women and elderly patients, with diseases accompanied by a risk of ventricular arrhythmia, electrolyte imbalance (eg, hypokalemia, hypomagnesemia).
The use of broad-spectrum antimicrobials, including moxifloxacin, is associated with a risk of developing pseudomembranous colitis.This diagnosis should be kept in mind in patients who have severe diarrhea with moxifloxacin. In this case, you should cancel the drug and prescribe the appropriate therapy. Preparations that inhibit the intestinal peristalsis are contraindicated in the development of severe diarrhea.
When moxifloxacin was taken, cases of fulminant hepatitis, potentially leading to liver failure, were reported.
The use of drugs quinolone series is associated with a possible risk of seizures. With the simultaneous use of moxifloxacin with non-steroidal anti-inflammatory drugs, the risk of seizures increases. Moxifloxacin should be used with caution in patients with myasthenia gravis in connection with possible exacerbation of the disease.
The drug does not have a photosensitizing effect, however, during the treatment with the drug, it is recommended to avoid ultraviolet irradiation including. direct sunlight.

Effect on the ability to drive transp. cf. and fur:The drug may impair a patient's ability to engage in potentially hazardous activities,requiring increased attention and speed of psychomotor reactions.

Form release / dosage:Film-coated tablets 400 mg.

Packaging:For 5 tablets coated with a film sheath in a contour mesh package made of PVC / aluminum foil.
For 1 or 2 contour pack together with instructions for use in a cardboard box.

Storage conditions:In the dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.

Shelf life:3 years.
Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001866

Date of registration:02.10.2012 / 14.07.2016

Expiration Date:02.10.2017

The owner of the registration certificate:Rowecq LimitedRowecq Limited United Kingdom

Manufacturer: & nbsp

BELCO PHARMA India

ROSLEKS PHARM, LLC Russia

Representation: & nbspROUTEC LIMITEDROUTEC LIMITEDUnited Kingdom

Information update date: & nbsp2016-08-21

Illustrated instructions

Instructions

Rotomox (Rotomox)