AVELOKS  tablets 400 mg №5

Description for AVELOKS ® tablets 400 mg:

AVELOKS ® (AVELOX ®)

MOXIFLOXACINUM J01M A14

Structure and Composition:

Table. n / a 400 mg, № 5
 Moxifloxacin 400 mg

Other ingredients: microcrystalline cellulose, croscarmellose sodium, lactose monohydrate, magnesium stearate, red iron oxide (E172), hypromellose, macrogol 4000, titanium dioxide.

№ UA/4071/01/01 from 01/23/2006 to 23/01/2011

pp info. 400 mg vial. 250 ml, № 1
 Moxifloxacin 400 mg

Other ingredients: sodium chloride, sodium hydroxide, hydrochloric acid, water for injection.

№ UA/4071/02/01 of 30.05.2008 to 30.05.2013

Pharmacological properties: moxifloxacin (1-cyclopropyl-7 {(S, S) -2,8-diaza-bicyclo [4.3.0] non-8-ye}-6-fluoro-8-methoxy-1 ,4-dihydro- 4-oxo-3-quinolinecarboxylic acid hydrochloride) - antibacterial fluoroquinolone broad-spectrum. Bactericidal action of the drug due to inhibition of bacterial topoisomerases II and IV, which leads to disruption of DNA biosynthesis of the bacterial cell and its demise. The activity of moxifloxacin is dependent on its concentration in blood plasma: the minimum bactericidal concentrations correspond to the minimum bacteriostatic. Mechanisms of resistance of microorganisms, inactivate penicillins, cephalosporins, aminoglycosides, macrolides, tetracyclines, and do not affect the antibacterial efficacy of moxifloxacin. Cross-resistance between the drug and the listed antibiotics Aveloks not say. Also not reported cases of resistance plasmid. The overall incidence of resistance is very small (10-7-10-10). Resistance to moxifloxacin develops slowly by multiple mutations.
Multiple effects of moxifloxacin on microorganisms at concentrations below the minimal inhibitory (MIC) is accompanied by a slight increase in MIC. Between antibacterial agents of quinolones, usually celebrate cross-resistance. However, some Gram-positive and anaerobic organisms that are resistant to other quinolones, are sensitive to moxifloxacin. Moxifloxacin is active in vitro against a broad spectrum of gram-negative and gram-positive bacteria, anaerobes, acid-fast bacilli and atypical forms such as Micoplasma, Chlamydia, Legionella. Moxifloxacin is effective against bacteria resistant to β-lactam and macrolide antibiotics.
Go to the drug sensitive:
Gram-positive microorganisms - Staphylococcus aureus (including methicillin-sensitive strains), Streptococcus pneumoniae (including strains resistant to penicillin and macrolides), Streptococcus pyogenes (group A);
gram-negative bacteria - Haemophillus influenzae (including strains producing β-lactamase), Haemophillus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis (including strains producing β-lactamase), Escherichia coli, Enterobacter cloacae;
atypical forms - Chlamydia pneumoniae, Mycoplasma pneumoniae, Legionella pneumoniae.
For moxifloxacin relatively sensitive:
Gram-positive bacteria - Streptococcus milleri, Str. mitior, Str. agalactiae, Str. dysgalactiae, Staphylococcus cohnii, S. epidermidis (including metitsillinrezistentnye strains), S. haemolyticus, S. hominis, S. saprophyticus, S. simulans, Corynebacterium diphtheriae;
gram-negative bacteria - Bordetella pertussis, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter intermedius, Enterobacter sakazaki, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia stuartii;
anaerobes - Bacteroides distasonis, Bacteroides eggerthii, Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides uniformis, Fusobacterium spp., Porphyromonas spp., Porphyromonas anaerobius, Porphyromonas asaccharolyticus, Porphyromonas magnus, Prevotella spp., Propionibacterium spp., Clostridium perfringens, Clostridium ramosum ;
atypical forms - Legionella pneumophila, Caxiella burnettii.
Susceptibility to moxifloxacin is confirmed by clinical data.
Moxifloxacin is less active with respect to Pseudomonas aeruginosa, Pseudomonas fluorescens, Burkholderia cepacia, Stenotrophomonas maltophilia.
With oral moxifloxacin is absorbed rapidly and almost completely. Absolute bioavailability is nearly 91%.
At doses ranging from 50 to 1200 mg in a single application and a dose of 600 mg per day for 10 days, the pharmacokinetics is linear. Stable blood concentrations achieved after three days of application. After receiving a single 400 mg dose maximum plasma concentration achieved within 0.5-4 h and is 3.1 mg / liter. When administered simultaneously with food moxifloxacin noted a slight increase in time to reach maximum concentration (2 h) and a slight decrease in maximum concentration (approximately 16%), and the duration of absorption does not change. However, these data do not have clinical significance, and the drug can be taken irrespective of food intake.
Moxifloxacin is rapidly distributed in tissues and organs, binds to plasma proteins (mainly albumin) for about 45%. The volume of distribution is about 2 l / kg. High concentrations of the drug in excess of plasma concentrations are achieved in lung tissue (alveolar macrophages), mucosa of the bronchi, nose, sinuses, and especially in areas of inflammation. In the interstitial fluid and saliva of moxifloxacin determined in a free, not protein-bound state, in higher concentrations than in plasma.
Moxifloxacin does not Biotransformation microsomal cytochrome P450 in the liver and excreted by the kidneys as unchanged and as inactive glucuronides and sulfosoedineny. 45% of unchanged drug is excreted in the urine and feces. The half-life of the drug is approximately 12 h. The average total body clearance after taking a dose of 400 mg of 179-246 ml / min. Approximately 19% of a single dose is excreted unchanged in the urine and 25% - in the feces.
Do not set age (children did not learn), and sex differences in the pharmacokinetics of moxifloxacin. There were no significant changes in the pharmacokinetics of moxifloxacin in patients with impaired renal function (creatinine clearance 30 ml / min • 1,73 m2) and are on hemodialysis, continuous and long-term ambulatory peritoneal dialysis have been identified. In patients with mild and moderate hepatic impairment (stage A and B in Child-Pugh classification) does not change the pharmacokinetics of the drug. Data on the use in cases of severe liver dysfunction (stage C according to Child-Pugh) do not.

INDICATIONS: Treatment of bacterial infections caused by microorganisms sensitive to the drug.
Respiratory infections:
• chronic bronchitis during exacerbation;
• community-acquired pneumonia, which are the causative agents of strains of microorganisms with multiple antibiotic resistance;
• acute sinusitis;
Uncomplicated skin and soft tissue.
Uncomplicated inflammatory disease of the pelvic organs (including infectious diseases of the upper genital women, including salpingitis and endometritis).
Complicated infections of skin and subcutaneous structures (including the infected diabetic foot).
Complicated intra-abdominal infections, including polymicrobic infections (such as abscess formation).
Streptococcus pneumonie with multiple resistance to antibiotics, including strains resistant to penicillin and resistant strains to two or more antibiotic groups such as penicillin (minimum inhibitory activity at ≥ 2 mg / ml), the second-generation cephalosporins (cefuroxime), macrolides, tetracyclines and trimethoprim / sulfamethoxazole.

USE: Adults: 400 mg 1 time per day for any infections.
Duration of therapy
Duration of therapy is determined by the severity of infection and clinical effect. In the initial stages of treatment can be applied pp Aveloksa for infusion, and then to continue the therapy when indicated the drug may be appointed into tablets.
Exacerbation of chronic bronchitis - 5 days.
Community-acquired pneumonia - 10 days.
Acute sinusitis - 7 days.
Uncomplicated skin and soft tissue - 7 days.
Uncomplicated inflammatory disease of the pelvic organs - 14 days.
Complicated infections of skin and subcutaneous structures - the total duration of moxifloxacin sequential therapy (w / w of the drug, followed by oral administration) is 7-21 days.
Complicated intra-abdominal infections - the total duration of sequential therapy (w / w of the drug, followed by oral administration) is 5-14 days.
According to clinical studies the duration of therapy, pills and p-rum infusion Aveloks was up to 21 days (for the treatment of complicated skin infections and subcutaneous structures).
In elderly patients the dosage regimen is not changed.
In patients with hepatic impairment the dosage regimen is not changed.
Patients with impaired renal function (including creatinine clearance at ≤ 30 ml / min • 1,73 m2) and are on hemodialysis, continuous and long-term ambulatory peritoneal dialysis dose adjustment is not necessary.
Used to treat patients of different ethnic groups - to change the dosing regimen is not necessary.
The tablets should be taken without chewing, drinking plenty of water regardless of food intake.
Infusion pp moxifloxacin is used as an antibiotic for monotherapy and in combination with other compatible drugs. Pp moxifloxacin is stable for 24 hours at room temperature using the following solvents: water for injection, p-ry of sodium chloride 0.9%, sodium chloride, 1M, 5% glucose, 10% and 40%, p-p xylitol 20%, Valium Ringer and Ringer lactate, 10% of drugs Aminofuzin Ionosteril and D5. Infusion pp should be entered in / slow for 60 minutes. The maximum dose is 600 mg one-time or 400 mg once a day for 7-21 days. In / Aveloks appoint a dose of 400 mg 1 time per day. The drug can be used in / for the entire course of treatment or during the initial stages of treatment with the subsequent transition to the reception of moxifloxacin in tablet form.

CONTRAINDICATIONS: Hypersensitivity to moxifloxacin (or to any component of the drug), to other quinolones, childhood and adolescence (18 years), the drug is contraindicated in patients with epilepsy, pregnancy and lactation.

SIDE EFFECTS: tolerability of moxifloxacin in most patients is good. During clinical trials of moxifloxacin, most side effects (90%) were mild or moderate severity. The frequency of discontinuation of treatment with an infusion of p-ra Aveloks in connection with the development of side effects did not exceed 3.8%.
With a frequency of ≥ 1% ≤ 10%
Cardio-vascular system - the lengthening of the interval Q-T in patients with concomitant hypokalemia.
Gastrointestinal - abdominal pain, nausea, diarrhea, vomiting, dyspepsia symptoms, changes in liver tests.
The CNS, sensory organs - dizziness, headache.
With a frequency of ≥ 0,1% ≤ 1%
General reaction - fatigue, sweating, weakness, pain in the chest.
Cardio-vascular system - tachycardia, increased blood pressure, palpitations, lengthening the interval Q-T.
Gastrointestinal - Dry mouth, nausea, vomiting, flatulence, constipation, stomatitis, anorexia, oral candidiasis, glossitis, increased gamma-glutamyl and amylase.
In the blood and lymphatic systems - radiation, reduction in prothrombin, eosinophilia, thrombocytopenia.
On the part of the musculoskeletal system - arthralgia, myalgia.
Nervous system disorders - insomnia, dizziness, nervousness, drowsiness, anxiety, tremor, paresthesia.
The respiratory system - shortness of breath.
Of the skin - rash, itching, sweating.
Genitourinary - vaginal candidiasis, vaginitis.
With a frequency of ≥ 0,01% ≤ 0,1%
General reactions - pain in the pelvis, swelling of the face, back pain, changes in laboratory tests, allergic reactions, pain in the legs.
Cardio-vascular system - lowering blood pressure, loss of consciousness, peripheral edema, vasodilatation (flushing).
Gastrointestinal - gastritis, tongue discoloration, dysphagia, jaundice (cholestatic prevails), diarrhea (caused by Clostridium difficile).
In the blood and lymphatic system - reduction of thromboplastin, increased prothrombin, thrombocytopenia, and anemia.
On the part of metabolism - hyperglycemia, hyperlipidemia, hyperuricemia, increased LDH in conjunction with the violation of liver tests.
On the part of the musculoskeletal system - arthritis, damage to tendons.
The nervous system - hallucinations, depersonalization, increased muscle tone, poor coordination, agitation, amnesia, aphasia, emotional lability, sleep disturbance, speech, thought process, decreased tactile sensitivity, abnormal dreams, seizures, confusion, depression.
The respiratory system - bronchospasm.
Of the skin - rashes (maculopapular, pustular, purpura), urticaria.
From the senses - the noise in the ears, blurred vision, loss of taste, parosmiya (including changes in sensation of smell, reduction and loss of sense of smell), amblyopia.
Genitourinary - renal dysfunction (increased creatinine or urea).
With a frequency of ≤ 0,01%
Allergic reaction - anaphylaxis, anaphylactic shock (including life-threatening), angioedema (including laryngeal edema, a life-threatening).
Gastrointestinal disorders - pseudomembranous colitis (in rare cases life-threatening), hepatitis (predominantly cholestatic).
On the part of the musculoskeletal system - the tendon rupture.
Of the skin - Stevens - Johnson.
Nervous system disorders - psychotic reaction.
Cardio-vascular system - ventricular tachyarrhythmia (very rare), atrial fibrillation and ventricular flutter and heart failure mainly in people prone to arrhythmias.
From the laboratory parameters - increase or decrease in hematocrit values ​​and reduced or elevated levels of red blood cells, leukocytosis, hypoglycemia, decreased hemoglobin, increased alkaline phosphatase, ALT, AST, bilirubin, uric acid, creatinine, urea.
Relationship of these changes in laboratory parameters with the reception of moxifloxacin is not installed.

PRECAUTIONS: In case of combined use of an infusion of p-ra Aveloks and other drugs for / in the introduction, each of these drugs must be administered separately. Allowed the introduction of only transparent infusion of p-ditch moxifloxacin.
Special warnings and precautions
The use of quinolone drugs is associated with a number of possible risk of a convulsive seizure. Moxifloxacin should be used with caution in patients with diseases of the central nervous system, predisposing to the occurrence of seizures or lowering the threshold for their occurrence. It should not be prescribed the drug patients with epilepsy.
In patients with moderate impairment of liver function correction doses of moxifloxacin is not carried out. Use of the drug in patients with severe hepatic impairment (Child-Pugh on, step c) is not recommended due to lack of sufficient clinical experience.
In the application of moxifloxacin as well as during therapy with other quinolones and macrolides may be slightly (to 1.2% of baseline) increase the interval Q-T. None of the 9000 patients receiving moxifloxacin, there was no prolongation associated with Q-T cardiovascular complications and deaths. However, moxifloxacin should be used with caution in patients with congenital or acquired diseases, accompanied by a lengthening of the interval Q-T, hypokalemia, or receiving drugs, potentially slowing cardiac conduction (eg anti-arrhythmic drugs class IA (quinidine, procainamide) or class III (amiodarone, sotalol)) . The degree of lengthening the interval Q-T can be increased with increasing concentration of the drug, so do not exceed recommended dose.
Safety of moxifloxacin during pregnancy and lactation has not been established and its use is contraindicated. A small amount of the drug is excreted in breast milk.
Effect on ability to drive motor vehicles and machinery
Although moxifloxacin rarely causes adverse reactions from the CNS, patients should determine their individual response to medication before driving, and moving machinery.
Please be aware that the therapy fluoroquinolones, including moxifloxacin and, especially in elderly patients and patients receiving corticosteroids, may develop tenosynovitis and tendon rupture. When the pain and signs of inflammation at the site of tendon injury should stop taking the drug and reduce the burden on the affected limb.
Please note that the application of antibacterial broad-spectrum drugs carries a risk of pseudomembranous colitis. Cases of pseudomembranous colitis with the use of moxifloxacin is not registered, but must be used with caution to patients who have a history of severe diarrhea in the therapy with antibiotics