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Pharmacological properties

Moxifloxacin (1-cyclopropyl-7 {(s, s) -2,8-diaza-bicyclo [4.3.0] non-8-уе} -6-fluoro-8-methoxy-1,4-dihydro-4-oxo -3-quinoline carboxylic acid hydrochloride) is an antibacterial drug with a wide spectrum of fluoroquinolone series. the bactericidal effect of the drug is due to the inhibition of bacterial topoisomerases ii and iv, which leads to disruption of the DNA biosynthesis of the microbial cell and its death. the activity of moxifloxacin depends on its concentration in blood plasma: the minimum bactericidal concentrations correspond to the minimum bacteriostatic. mechanisms of resistance of microorganisms that inactivate penicillins, cephalosporins, aminoglycosides, macrolides and tetracyclines do not affect the antibacterial effectiveness of moxifloxacin. there is no cross-resistance between the drug avelox and the listed antibiotics. cases of plasmid resistance were also not noted. the overall incidence of resistance is very small (10-7-10-10). resistance to moxifloxacin develops slowly through numerous mutations.

The repeated effect of moxifloxacin on microorganisms in concentrations below the minimum inhibitory (MIC) is accompanied by only a slight increase in MIC. Among antibacterial agents of the quinolone group, as a rule, cross-resistance is noted. However, some gram-positive and anaerobic microorganisms that are resistant to other quinolones are sensitive to moxifloxacin. In vitro moxifloxacin is active against a wide range of gram-negative and gram-positive microorganisms, anaerobes, acid-resistant bacteria and such atypical forms as Micoplasma, Chlamydia, Legionella. Moxifloxacin is effective against bacteria resistant to β-lactam and macrolide antibiotics.

Sensitive to the drug:

gram-positive microorganisms - Staphylococcus aureus (including strains sensitive to methicillin), Streptococcus pneumoniae (including strains resistant to penicillin and macrolides), Streptococcus pyogenes (group A);

gram-negative microorganisms - Haemophillus influenzae (including strains producing β-lactamases), Haemophillus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis (including strains producing β-lactamases), Escherichia coli, Enterobacter cloacae;

atypical forms - Chlamydia pneumoniae, Mycoplasma pneumoniae, Legionella pneumoniae.

To moxifloxacin are relatively sensitive:

gram-positive microorganisms - Streptococcus milleri, Str. mitior, Str. agalactiae, Str. dysgalactiae, Staphylococcus cohnii, S. epidermidis (including methicillin-resistant strains), S. haemolyticus, S. hominis, S. saprophyticus, S. simulans, Corynebacterium diphtheriae;

gram-negative microorganisms - 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., Porphyromonomorphus str. ;

atypical forms - Legionella pneumophila, Caxiella burnettii.

Sensitivity to moxifloxacin is confirmed by clinical data.

Moxifloxacin is less active with respect to Pseudomonas aeruginosa, Pseudomonas fluorescens, Burkholderia cepacia, Stenotrophomonas maltophilia.

When taken orally, moxifloxacin is absorbed rapidly and almost completely. Absolute bioavailability reaches almost 91%.

In a dose range of 50 to 1200 mg with a single use and at a dose of 600 mg / day for 10 days, the pharmacokinetics are linear. A stable concentration in the blood is reached after 3 days of use. After a single dose of 400 mg of the drug, the maximum concentration in the blood plasma is reached within 0.5-4 hours and is 3.1 mg / l. When taking moxifloxacin at the same time with food, there is a slight increase in the time to reach the maximum concentration (by 2 hours) and a slight decrease in the maximum concentration (by about 16%), while the duration of absorption does not change. However, these data are not of clinical importance and the drug can be taken regardless of food intake.

Moxifloxacin is rapidly distributed in tissues and organs, binds to blood plasma proteins (mainly with albumin) by about 45%. The volume of distribution is about 2 l / kg body weight.High concentrations of the drug, exceeding the concentration in blood plasma, are achieved in the lung tissue (alveolar macrophages), the mucous membrane of the bronchi, nasal sinuses and especially in the foci of inflammation. In interstitial fluid and saliva, moxifloxacin is determined in a free, non-protein bound state at a higher concentration than in blood plasma.

Moxifloxacin is not biotransformed by the microsomal cytochrome P450 system in the liver and is excreted from the body by the kidneys both unchanged and in the form of inactive sulfo compounds and glucuronides. 45% of the unchanged drug is excreted in urine and feces. The half-life of the drug is approximately 12 hours. The average total clearance after taking a dose of 400 mg is 179–246 ml / min. About 19% of a single dose is excreted unchanged with urine and 25% with feces.

The age-related (not studied in children) and gender differences in the pharmacokinetics of moxifloxacin have not been established. Significant changes in the pharmacokinetics of moxifloxacin in patients with impaired renal function (creatinine clearance 30 ml / min · 1.73 m2) and those on continuous hemodialysis and long-term outpatient peritoneal dialysis were not detected. In patients with minor and moderate impaired liver function (stages A and B according to the Child-Pugh classification), the pharmacokinetics of the drug does not change. Data on the use in cases of severe hepatic impairment (Child-Pugh stage C) are not available.

Indications

Treatment of bacterial infections caused by drug-sensitive microorganisms.

Infectious diseases of the respiratory tract:

chronic bronchitis during exacerbation;

community-acquired pneumonia, the causative agents of which are strains of microorganisms with multiple antibiotic resistance;

acute sinusitis;

Uncomplicated infections of the skin and soft tissues.

Uncomplicated inflammatory diseases of the pelvic organs (including infectious diseases of the upper genital area in women, including salpingitis and endometritis).

Complicated infectious diseases of the skin and subcutaneous structures (including infected diabetic foot).

Complicated intra-abdominal infections, including polymicrobial infections (such as abscess formation).

Streptococcus pneumonie with multiple antibiotic resistance, including penicillin-resistant strains and strains resistant to two or more antibiotics of groups such as penicillins (with minimal inhibitory activity ≥2 μg / ml), second-generation cephalosporins (cefuroxime), macrolides, tetracyclines and trimethoprim / sulfamethoxazole.

Application

Adults 400 mg 1 time per day for any infections.

Therapy duration

The duration of therapy is determined by the severity of the infection and the clinical effect. At the initial stages of treatment, the Avelox solution can be used for infusion, and then, if indicated, the drug can be prescribed orally in tablets to continue therapy.

Exacerbation of chronic bronchitis - 5 days.

Community-acquired pneumonia - 10 days.

Acute sinusitis - 7 days.

Uncomplicated infections of the skin and soft tissues - 7 days.

Uncomplicated inflammatory diseases of the pelvic organs - 14 days.

Complicated infections of the skin and subcutaneous structures - the total duration of staged therapy with moxifloxacin (iv administration of the drug followed by oral administration) is 7-21 days.

Complicated intra-abdominal infections - the total duration of step therapy (iv drug administration followed by oral administration) is 5-14 days.

According to clinical studies, the duration of therapy with tablets and r-rum for Avelox infusions was up to 21 days (in the treatment of complicated infections of the skin and subcutaneous structures).

In elderly patients and in patients with impaired liver function, the dosage regimen does not change.

In patients with impaired renal function (including creatinine clearance of 30 ml / min · 1.73 m2) and those on continuous hemodialysis and long-term outpatient peritoneal dialysis do not need dose adjustment.

The use for the treatment of patients of different ethnic groups - there is no need to change the dosage regimen.

Tablets should be taken without chewing, drinking plenty of water, regardless of food intake.

The moxifloxacin infusion solution is used both for antibacterial monotherapy and in combination with other compatible drugs. The moxifloxacin solution remains stable for 24 hours at room temperature and when using the following solvents: water for injection, sodium chloride solutions 0.9%, sodium chloride 1M, glucose 5%, 10% and 40%, solution xylitol 20%, ringer Ringer and Ringer lactate, drugs Aminofusin 10% and Ionosteril D5. The infusion solution should be administered iv slowly for 60 minutes. The maximum dose is 600 mg once or 400 mg 1 time per day for 7-21 days. In / in appoint Avelox in a dose of 400 mg once a day. The drug can be used iv during the entire course of treatment or at the initial stages of treatment, followed by switching to taking moxifloxacin in the form of tablets.

Contraindications

Hypersensitivity to moxifloxacin (or to any component of the drug); to other quinolones; children and adolescents (up to 18 years); the drug is contraindicated in patients with epilepsy, during pregnancy and lactation.

Side effects

Moxifloxacin tolerance is good in most patients. during clinical trials of moxifloxacin, most side effects (90%) were mild or moderate. the frequency of discontinuation of treatment with the use of infusion r-ra Avelox in connection with the development of side effects did not exceed 3.8%.

With a developmental frequency of ≥1% 10%

On the part of the cardiovascular system - prolongation of the Q – T interval in patients with concomitant hypokalemia.

From the gastrointestinal tract - abdominal pain, nausea, diarrhea, vomiting, dyspepsia symptoms, changes in liver tests.

From the side of the central nervous system, sensory organs - dizziness, headache.

With a development rate of ≥0.1% 1%

General reactions - asthenia, hyperhidrosis, general weakness, pain in the chest area.

From the side of the cardiovascular system - tachycardia, increased blood pressure, palpitations, lengthening of the Q – T interval.

From the gastrointestinal tract - dry mouth, nausea, vomiting, flatulence, constipation, stomatitis, lack of appetite, oral candidiasis, glossitis, increased gamma-glutamyl transpeptidase and amylase.

On the part of the blood system and lymphatic system - leukopenia, a decrease in the level of prothrombin, eosinophilia, thrombocytopenia.

From the musculoskeletal system - arthralgia, myalgia.

From the side of the nervous system - insomnia, dizziness, nervousness, drowsiness, anxiety, tremor, paresthesia.

From the respiratory system - shortness of breath.

On the part of the skin - rashes, itching, sweating.

From the genitourinary system - vaginal candidiasis, vaginitis.

With a developmental frequency of ≥0.01% ≤0.1%

Common reactions are pelvic pain, facial swelling, back pain, changes in laboratory tests, allergic reactions, leg pain.

On the part of the cardiovascular system - lowering blood pressure, loss of consciousness, peripheral edema, vasodilation (rush to the face).

From the gastrointestinal tract - gastritis, discoloration of the tongue, dysphagia, jaundice (cholestatic predominates), diarrhea (caused by Clostridium difficile).

On the part of the blood and lymphatic system - a decrease in the level of thromboplastin, an increase in the level of prothrombin, thrombocytopenia, anemia.

From the side of metabolism - hyperglycemia, hyperlipidemia, hyperuricemia, increased LDH in combination with impaired hepatic tests.

From the musculoskeletal system - arthritis, tendon damage.

From the side of the nervous system - hallucinations, depersonalization, increased muscle tone, impaired coordination, agitation, amnesia, aphasia, emotional lability, sleep, speech, thinking process, decreased tactile sensitivity, pathological dreams, convulsions, confusion, depression.

From the respiratory system - bronchospasm.

On the part of the skin - rashes (maculopapular, pustular, purpura), urticaria.

On the part of the sensory organs - tinnitus, visual impairment, loss of taste, parosmia (including a change in the sensation of smell, decrease and loss of scent), amblyopia.

From the genitourinary system - impaired renal function (increased creatinine or urea).

With a development rate of 0.01%

Allergic reactions - anaphylactic reactions, anaphylactic shock (including life-threatening), angioedema (including life-threatening laryngeal edema).

From the gastrointestinal tract - pseudomembranous colitis (in rare cases, life-threatening), hepatitis (mainly cholestatic).

From the musculoskeletal system - tendon rupture.

On the part of the skin - Stevens-Johnson syndrome.

From the side of the nervous system - psychotic reactions.

From the cardiovascular system - ventricular tachyarrhythmia (very rare), ventricular fibrillation and flutter, and cardiac arrest mainly in people prone to arrhythmias.

On the part of laboratory indicators - an increase or decrease in the hematocrit and a decrease or increase in the content of red blood cells, leukocytosis, hypoglycemia, a decrease in hemoglobin, an increase in the level of alkaline phosphatase, AlAT, AcAT, bilirubin, uric acid, creatinine, urea.

The relationship of changes in these laboratory parameters with the use of moxifloxacin has not been established.

special instructions

In the case of the combined use of the infusion solution of Avelox and other drugs for iv administration, each of these drugs must be administered separately. administration of only transparent infusion solutions of moxifloxacin is allowed.

Special warnings and precautions

The use of quinolone drugs is associated with a possible risk of developing a seizure. Moxifloxacin should be used with caution in patients with central nervous system diseases predisposing to seizures or lowering the threshold for their occurrence. The drug should not be prescribed to patients with epilepsy.

In patients with moderate liver failure, dose adjustment of moxifloxacin is not performed. The use of the drug in patients with severe hepatic impairment (Child-Pugh, stage C) is not recommended due to the lack of sufficient clinical experience.

When using moxifloxacin, as well as during therapy with other quinolones and macrolides, the Q – T interval may slightly increase (up to 1.2% of the initial level). None of the 9,000 patients receiving moxifloxacin had cardiovascular complications or lethal cases associated with prolongation of the Q – T interval. However, moxifloxacin should be used with caution in patients with congenital or acquired diseases accompanied by prolongation of the Q – T interval, hypokalemia, or those receiving drugs that potentially slow cardiac conduction (for example, class Ia antiarrhythmic drugs (quinidine, procainamide) or class III (amiodarone, sotalol)) . The degree of lengthening of the Q – T interval may increase with increasing concentration of the drug, so the recommended dose should not be exceeded.

The 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.

Influence on the ability to drive vehicles and work with mechanisms

Despite the fact that moxifloxacin rarely causes adverse reactions from the central nervous system, patients should determine their individual response to the drug before driving vehicles and moving mechanisms.

It should be borne in mind that during therapy with fluoroquinolones, including moxifloxacin, especially in elderly patients and patients receiving corticosteroids, tendovaginitis and tendon rupture may develop. When pain and signs of tendon inflammation appear at the site of injury, it is recommended to stop taking the drug and reduce the load on the affected limb.

It should be borne in mind that the use of broad-spectrum antibacterial drugs is associated with a risk of pseudomembranous colitis. There have been no cases of pseudomembranous colitis with the use of moxifloxacin, but it is necessary to prescribe the drug with caution to patients who have a history of severe diarrhea during antibiotic therapy. In case of severe diarrhea, the drug should be discontinued and appropriate therapy prescribed.

In some cases, after the first dose of the drug, hypersensitivity and allergic reactions may develop. Very rarely, allergic reactions can progress up to the development of anaphylactic shock, even after the first dose. In such cases, moxifloxacin must be canceled and appropriate treatment measures taken (including anti-shock).

When using quinolones, photosensitivity reactions are noted, although moxifloxacin does not have phototoxic properties. Patients receiving the drug should avoid direct sunlight and ultraviolet radiation.

Children

The use of moxifloxacin in children and adolescents is not recommended, since the effectiveness and safety of the use of the drug have not been reliably established.

Interactions

Antacids, minerals and multivitamins. the combined use of moxifloxacin with antacids, minerals and multivitamins can cause a malabsorption of the drug due to the formation of chelate complexes with polyvalent cations contained in these drugs, and this in turn can lead to a decrease in their concentration in blood plasma. therefore, antacids, antiretroviral and other drugs containing calcium, magnesium, aluminum, iron should be taken at least 4 hours before or 2 hours after oral administration of moxifloxacin.

Ranitidine

The combined use of ranitidine and moxifloxacin slightly changes the absorption of the latter.

Calcium-containing preparations

With the combined use of moxifloxacin with high doses of calcium-containing preparations, no clinically significant effect on the absorption of moxifloxacin was detected, with the exception of a slight decrease in the absorption rate.

Theophylline

Moxifloxacin does not affect the pharmacokinetics of theophylline (and vice versa), therefore, does not interact with isoenzymes of cytochrome P450 subtype 1A2.

Warfarin

With the combined use of moxifloxacin with warfarin, prothrombin time and other indicators of blood coagulation do not change. But sometimes, in patients receiving anticoagulants simultaneously with fluoroquinolones, there have been cases of increased anticoagulant activity of antithrombotic drugs. Risk factors are the presence of infectious diseases (and the accompanying inflammatory process), the age and general condition of the patient. Therefore, in the case of the combined use of warfarin and moxifloxacin, it is necessary to correct the dose of oral antithrombotic drugs.

Oral contraceptives

Interactions between moxifloxacin and oral contraceptives were not observed.

Antidiabetic agents

No clinically significant interaction between glibenclamide and moxifloxacin has been established.

Itraconazole

When combined with moxifloxacin, the AUC of itraconazole does not change significantly. There was no significant mutual influence of the drugs, therefore, no change in the dosage regimen is necessary.

Digoxin

The pharmacokinetics of digoxin under the influence of moxifloxacin did not change and vice versa.

Morphine

With parenteral administration of morphine and simultaneous oral administration of moxifloxacin, a decrease in the bioavailability of the latter was not noted; maximum concentrationplasma moxifloxacin is slightly reduced (17%).

Atenolol

The pharmacokinetics of atenolol slightly changes under the influence of moxifloxacin. After taking a single dose of AUC, atenolol increases by 4%, and the maximum concentration in blood plasmareduced by 10%.

Probenecid

Probenecid does not affect the total and renal clearance of moxifloxacin, therefore, dose adjustment with combined use is not necessary.

The moxifloxacin infusion solution is incompatible with sodium chloride solutions of 10% and 20%, sodium bicarbonate 4.2% and 8.4%. The drug can not be administered simultaneously with other antibiotics.

Overdose

No side effects were noted with the use of Avelox in healthy volunteers in single doses up to 1.2 g or at a dose of 600 mg / day for 10 days.

In case of overdose, symptomatic therapy is carried out, combined with ECG monitoring, in accordance with the clinical situation. The use of activated carbon is advisable only in case of an overdose of moxifloxacin in the form of tablets, at an early stage this prevents the systemic exposure of moxifloxacin. After its iv administration, activated carbon slightly (by 20%) reduces the systemic exposure of the drug.

Storage conditions

In a dry, dark place at a temperature of 8-25 ° C. do not freeze.

Tags: Moxifloxacin