Plevilox - instructions for use, doses, side effects, contraindications

Composition:Active substance: moxifloxacin hydrochloride, 436.4 mg equivalent to moxifloxacin 400.0 mg.
Excipients: lactose monohydrate, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, hydroxypropylmethylcellulose, red iron oxide dye.

Description:Oval tablets of red-brown color, convex form on both sides, covered with a film membrane with a risk on one side.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone.

ATX: & nbsp

J.01.M.A.14 Moxifloxacin

Pharmacodynamics:Moxifloxacin acts bactericidal, affecting the replication of bacterial DNA (the target are topoisomers II and IV, which carry out changes in the spatial configuration of the DNA molecule at various stages of its replication). Interacting with topoisomerase IV, causes the rupture of the DNA molecule after replication. It is active against many strains of microorganisms both in vitro and in vivo.
Gram-positive aerobic bacteria are sensitive to moxifloxacin: Streptococcus pneumonia (including strains resistant to penicillin and macrolides), Streptococcus pyogenes (group A), Streptococcus mitis, Streptococcus agalactiae, Streptococcus dysgalactiae, Staphylococcus aureus (including methicillin-sensitive strains), Staphylococcus cohnii, Staphylococcus epidermidis (including methicillin-sensitive strains), Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus, Staphychococcus simulans, Corynebacterium diphtheriae; Gram-negative aerobic bacteria: Haemophillus influenzae (including strains producing and non-producing beta-lactamases), Haemophilias parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis (including strains producing and non-producing beta-lactamases), Escherichia coli, Enterobacter cloacae, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter intermedius, Enterobacter sakazaki, Bordetella pertussis, Klebsiella oxytoca, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia stuartii; anaerobic bacteria: Bacteroides distasonis, Bacteroides eggerthii, Bacteroides ffagilis, Bacteroides ovatus, Bacteroides thetaiotaomicronron, Bacteroides uniformis, Fusobacterium spp., Porphyromonas spp. (including Porphyromonas anaerobius, Porphyromonas asaccharolyticus, Porphyromonas magnus), Prevotella spp., Propionibacterium spp., Clostridium perffingens, Clostridium ramosus; as well as Chlamydia pneumonia, Mycoplasma pneumonia, Coxiella bumettii. Moxifloxacin less active against Pseudomonas aeruginosa, Pseudomonas fluorescens, Burkholdera cepacia, Stenotrophomonas maltophilia. Mechanisms that lead to the development of resistance to penicillins, cephalosporins, aminoglycosides, macrolides and tetracyclines do not interfere with the antibacterial activity of moxifloxacin.
Cross-resistance between these groups of antibacterial drugs and moxifloxacin is not noted. The overall incidence of resistance is low. Resistance to moxifloxacin develops slowly by multiple mutations.
There are cases of cross-resistance to other quinolones.However, some Gram-positive and anaerobic microorganisms resistant to other fluoroquinolones are susceptible to moxifloxacin.

Pharmacokinetics:Moxifloxacin well absorbed from the gastrointestinal tract, eating does not have a significant effect on absorption, bioavailability is about 90%. After ingestion of a single dose of 400 mg, the maximum concentration in the plasma is achieved after 0.5-4 hours and is 3.1 mg / l. Constant concentration in the plasma is achieved on the third day of treatment. Moxifloxacin is rapidly distributed in tissues and organs and binds to blood proteins (mainly albumins) by approximately 40% (30-50%). High concentrations of the drug, exceeding the concentration in the plasma, are created in the lung tissue (including in the alveolar macrophages), in the bronchial mucosa, in the sinuses, in the foci of inflammation. In the interstitial fluid and in saliva, the drug is determined in a free, non-protein-binding form at a concentration higher than in the plasma.
Biotransformed to inactive sulfo compounds and glucuronides (conjugation of sulfate and glucuronide reaches approximately 38% and 14%, respectively, from a single dose taken internally). It is not biotransformed with microsomal hepatic enzymes of the P450 system.
It is excreted by the kidneys in an unchanged form and in the form of inactive metabolites; about 45% of the unchanged drug is excreted by the kidneys and through the gastrointestinal tract. The half-life (T_1/2) is approximately 12 hours. The average total clearance after taking the drug inside at a dose of 400 mg is from 179 to 246 ml / min.
Pharmacokinetics in special cases
There were no differences in pharmacokinetic parameters of moxifloxacin depending on sex and age. Studies of the pharmacokinetics of the drug in children have not been conducted. There were no significant changes in the pharmacokinetics of moxifloxacin in patients with impaired renal function (including creatinine clearance <30 mL / min / 1.73 square meters) and in patients on continuous hemodialysis and long-term outpatient peritoneal dialysis. In patients with minor and moderate hepatic impairment (class A and B on the Scidl-Piug scale) no studies have been performed.

Indications:Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:
-expansion of chronic bronchitis;
-hospital pneumonia;
- Acute sinusitis;
-infection of the skin and soft tissues.

Contraindications:-increased sensitivity to moxifloxacin, other quinolones or components of the drug;
-epilepsy;
- Severe diarrhea;
-diabetes;
- uncontrolled hypokalemia;
-baby and adolescence (up to 18 years);
-pregnancy;
-period of lactation.

Carefully:- with a convulsive syndrome in history, with diseases of the central nervous system (pronounced atherosclerosis of cerebral vessels, cerebral circulation disorders) predisposing to lower the threshold of convulsive readiness and the occurrence of convulsive seizures;
-in violation of liver function (class C on the Scale-Piug scale);
-in hypokalemia;
-lengthening the interval QT;
-in conditions predisposing to arrhythmia (including bradycardia, acute myocardial ischemia);
-if simultaneous administration of the drug, extending the interval of QT: antiarrhythmic drugs of class 1a (incl. quinidine, procainamide) and III (incl. amiodarone, sotalol), tricyclic antidepressants, neuroleptics);
- with pseudomembranous colitis;
-boiled, being on hemodialysis (insufficient experience of application);
- simultaneous reception of glucocorticosteroids.

Dosing and Administration:Inside, 400 mg once a day.
The tablet is swallowed whole, not liquid, squeezed with a small amount of water, regardless of food intake.
The course of treatment for exacerbation of chronic bronchitis-5 days, with acute sinusitis and infections of the skin and soft tissues-7 days, with community-acquired pneumonia-7-14 days.
In elderly patients, patients with minor violations of liver function (class A and B on the Scale-Pyuga scale), patients with impaired renal function (including with creatinine clearance <30 mL / min / 1.73 square meters) and patients on continuous hemodialysis and long-term outpatient peritoneal dialysis, changes in the dosing regimen are not required.

Side effects:Often -1-10%, rarely-0.1-1%, very rarely-0.01-0.1%.
From the digestive system: often - abdominal pain, symptoms of dyspepsia (nausea, vomiting, diarrhea), increased activity of "liver" transaminases; rarely - dry mouth, flatulence, constipation, candidiasis of the oral mucosa, anorexia, stomatitis, glossitis; extremely rare - gastritis, discoloration of the tongue, dysphagia, transient jaundice (mostly cholestatic), pseudomembranous colitis (in very rare cases, life threatening), hepatitis (mostly cholestatic).
From the nervous system: often - dizziness, headache; rarely - asthenia, insomnia or drowsiness, nervousness, anxiety, tremor, paresthesia; very rarely - hallucinations, depersonalization, increased muscle tone, impaired coordination of movements, agitation, amnesia, aphasia, emotional lability, sleep disturbance,
speech disorders, cognitive processes, hypoesthesia, awful dreams, convulsions, confusion, depression, psychotic reactions.
From the sense organs: often - a noise in the ears, a change in taste; very rarely - visual impairment, amblyopia, loss of taste sensitivity, parosmia (including changes in perception of odors, loss and loss of smell).
From the cardiovascular system: often - prolongation of the QT interval in patients with concomitant hypokalemia; rarely - tachycardia, increased blood pressure, palpitations; extremely rare - a decrease in blood pressure, fainting, peripheral edema, flushing of the blood to the face, gastric tachyarrhythmia, including fibrillation of ventricular flutter and cardiac arrest (predominantly in predisposed patients).
From the respiratory system: rarely shortness of breath; extremely seldom-asthmatic state.
From the musculoskeletal system: rarely - arthralgia, chest pain, myalgia; extremely rarely - back pain, pain in the legs, arthritis, pelvic pain, tendopathy.
From the genitourinary system: rarely - vaginal candidiasis, vaginitis; extremely rarely - pain in the lower abdomen, edema of the face peripheral edema, impaired renal function.
Allergic reactions: rarely - a rash, itching; extremely rare - rash (maculopapular, pustular, purpura), urticaria, Stevens-Johnson syndrome, angioedema (including laryngeal edema, life-threatening), anaphylactic shock.
Laboratory indicators: rarely - leukopenia, increased prothrombin time, eosinophilia, thrombocytosis, increased activity of gamma-glutamintransferase and amylase; extremely rare - a decrease in the concentration of thromboplastin, a decrease in prothrombin time, thrombocytopenia, anemia, hyperglycemia, hyperlipidemia, hyperuricemia, increased lactate dehydrogenase activity. The connection with the administration of the drug has not been proven: an increase or decrease in hematocrit, leukocytosis, erythrocytosis or erythropenia, a decrease in the concentration of glucose, hemoglobin, urea, an increase in the activity of alkaline phosphatase, bilirubin, creatinine.
Other: rarely - candidiasis, general discomfort, sweating, asthenia.

Overdose:Symptoms: possibly a decrease in activity, drowsiness, vomiting, diarrhea, general body tremor, convulsions.
Treatment: gastric lavage (in the first two hours after an overdose), observation, symptomatic therapy with ECG monitoring. There is no specific antidote. It is necessary to ensure a sufficient supply of fluid in the body while maintaining the appropriate diuresis.

Interaction:Antacids, minerals, multivitamins impair absorption (due to the formation of chelate complexes with polyvalent cations) and reduce the concentration of moxifloxacin in plasma (simultaneous reception is possible with an interval of 4 hours before or 2 hours after taking moxifloxacin).
With simultaneous use of moxifloxacin and antiarrhythmic drugs of class Ia (incl. quinidine, procainamide) and III (incl. amiodarone, sotalol), as well as drugs that can extend the QT interval (cisapride, erythromycin, tricyclic antidepressants, antipsychotics), an additive effect is possible with respect to the prolongation of the QT interval.
Ranitidine reduces the absorption of moxifloxacin.
Moxifloxacin does not interact with probenicide, warfarin, oral contraceptives, theophylline, glibenclamide, morphine, itraconazole.
Moxifloxacin and digoxin do not significantly affect the pharmacokinetic parameters of each other.
The simultaneous use of moxifloxacin and glucocorticosteroids increases the risk of developing tendovaginitis and rupture of tendons.
With the simultaneous administration of quinolones and cyclosporine, the nephrotoxic effect of cyclosporin can be enhanced.
With the simultaneous use of quinolones and non-steroidal anti-inflammatory drugs, the risk of side effects from the central nervous system, including convulsions, may increase.
When combined quinolones with other antimicrobial agents (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole), synergy is usually observed.

Special instructions:In order to reduce the risk of developing resistance to moxifloxacin and to maintain the effectiveness of antibacterial agents moxifloxacin It is necessary to prescribe only for the treatment of infections caused by strains sensitive to the drug.
During the period of treatment, ECG monitoring (QT interval prolongation, ventricular arrhythmias) is necessary. The degree of elongation of the QT interval may increase with increasing drug concentration, therefore, do not exceed the recommended dose. The prolongation of the QT interval is associated with an increased risk of ventricular arrhythmias, including flicker-flutter.
Against the background of therapy with fluoroquinolones, including moxifloxacin, especially in elderly patients receiving glucocorticosteroids, tendonitis and tendon rupture are possible. At the first symptoms of pain or inflammation in the site of damage, stop taking the medication and unload the affected limb.
In the case of the development of severe diarrhea against the background of treatment with moxifloxacin, it is necessary to cancel the drug and prescribe the appropriate therapy.
In some cases, severe allergic reactions, including life-threatening anaphylactic shock, can develop. In these cases moxifloxacin it is necessary to cancel and appoint the necessary (including anti-shock) drugs: glucocorticosteroids, norepinephrine, antihistamines.
Moxifloxacin does not possess phototoxic properties. Nevertheless, patients receiving moxifloxacin, should avoid direct sunlight and ultraviolet irradiation.

Effect on the ability to drive transp. cf. and fur:Although moxifloxacin rarely causes adverse reactions from the central nervous system, patients should know their reaction to the drug before driving the car / moving mechanisms.

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

Packaging:5 or 10 tablets per blister. 1 blister for 5 or 10 tablets together with instructions but in a cardboard box. 3, 6 or 10 blisters of 10 tablets together with instructions for use in a cardboard box.

Storage conditions:In a dry place, protected from light, at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:2 years.
Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003574/08

Date of registration:07.05.2008 / 07.04.2016

Expiration Date:Unlimited

The owner of the registration certificate:Plethiko Pharmaceuticals Co., Ltd. Plethiko Pharmaceuticals Co., Ltd. India

Manufacturer: & nbsp

PLETHICO PHARMACEUTICALS, Ltd. India

Representation: & nbspREZLOV ZAO REZLOV ZAO Kazakhstan

Information update date: & nbsp2016-10-22

Illustrated instructions

Instructions

Plevilox (Plevilox)