Avelox, 400 mg pills, 5 pcs.

Composition

1 tablet contains:

Active ingredient: moxifloxacin hydrochloride 436.8 mg (corresponds to moxifloxacin base-400 mg)

Pharmacological action

Avelox is a broad-spectrum antibacterial bactericidal drug,8-methoxyfluoroquinolone. The bactericidal effect of moxifloxacin is due to the inhibition of bacterial topoisomerases II and IV, which leads to disruption of the processes of replication, repair and transcription of microbial cell DNA biosynthesis and, as a result, to the death of microbial cells.

The minimum bactericidal concentrations of the drug are generally comparable with its MIC.

Mechanisms of resistance

Mechanisms leading to the development of resistance to penicillins, cephalosporins, aminoglycosides, macrolides and tetracyclines do not affect the antibacterial activity of moxifloxacin. There is no cross-resistance between these groups of antibacterial drugs and moxifloxacin. So far, no cases of plasmid resistance have been observed. The overall frequency of resistance development is very low (10-7-10-10). Resistance to moxifloxacin develops slowly through multiple mutations. Repeated exposure of moxifloxacin to microorganisms at concentrations below MIC is accompanied by only a slight increase in it. There are cases of cross-resistance to quinolones. However, some gram-positive and anaerobic microorganisms resistant to other quinolones remain sensitive to moxifloxacin.

It was found that the addition of a methoxy group at position C8 to the moxifloxacin molecule structure increases the activity of moxifloxacin and reduces the formation of resistant mutant strains of gram-positive bacteria. The addition of a bicycloamine group at position C7 prevents the development of active efflux, a mechanism of resistance to fluoroquinolones.

Moxifloxacin is active in vitro against a wide range of Gram-negative and gram-positive microorganisms, anaerobes, acid-resistant bacteria and atypical bacteria such as Mycoplasma spp., Chlamydia spp., Legionella spp., as well as bacteria resistant to beta-lactam and macrolide antibiotics.

Effect on human intestinal microflora

In two studies conducted on volunteers, the following changes in the intestinal microflora were noted after oral administration of moxifloxacin: a decrease in concentrations of Escherichia coli, Bacillus spp., Bacteroides vulgatus, Enterococcus spp., Klebsiella spp., as well as anaerobes Bifidobacterium spp., Eubacterium spp., Peptostreptococcus spp. These changes were reversible within two weeks. No Clostridium difficile toxins were detected.

Indications

Infectious and inflammatory diseases in adults caused by drug-sensitive microorganisms:

• acute sinusitis,
• exacerbation of chronic bronchitis;
• community-acquired pneumonia (including that caused by strains with multiple antibiotic resistance);
• uncomplicated infections of skin and soft tissues;
• complicated infections of skin and subcutaneous structures (including infected diabetic foot);
• complicated intra-abdominal infections including polymicrobial infections, including intra-abdominal abscesses;
• uncomplicated inflammatory diseases of the pelvic organs (including salpingitis and endometritis).

Use during pregnancy and lactation

Avelox is contraindicated in childhood and adolescence, during pregnancy and lactation.

Contraindications

Hypersensitivity to Avelox, epilepsy, severe diarrhea.

With caution. Convulsions (history), liver failure (class C on a scale child-Pyuga), prolongation of Q-T interval; bradycardia, myocardial ischemia, concomitant use of drugs that slow cardiac conduction (including antiarrhythmic drugs of class Ia, II, III, tricyclic antidepressants, neuroleptics); patients on hemodialysis (lack of experience); diarrhea, pseudomembranous colitis; concomitant use of corticosteroids.

Side effects

Cardiovascular system: prolongation of the QT interval (often in patients with concomitant hypokalemia, infrequently in other patients); infrequently-tachycardia, palpitations and vasodilation (flushing of blood to the face); rarely-hypotension, hypertension, syncope; ventricular tachyarrhythmias; very rarely-non-specific arrhythmias (including extrasystole), polymorphic ventricular tachycardia (Torsade de Pointes) or cardiac arrest, mainly in individuals with conditions predisposing to arrhythmias, such as clinically significant bradycardia, acute myocardial ischemia.

Respiratory system: infrequently-shortness of breath (including asthmatic condition).

Digestive system: often — nausea, vomiting, abdominal pain, diarrhea, transient increase in transaminases; infrequently — anorexia, constipation, dyspepsia, flatulence, gastroenteritis (except erosive gastroenteritis), increased levels of amylase, bilirubin, liver function disorders (including increased LDH levels), increased levels of GGT and alkaline phosphatase, rarely — dysphagia, stomatitis, pseudomembranous colitis (in very rare cases associated with threatening conditions). life — threatening complications), jaundice, hepatitis (mainly cholestatic), very rarely-lightning-fast hepatitis, potentially leading to life-threatening liver failure.

The nervous system: often — dizziness, headache, infrequently — confusion, disorientation, vertigo, drowsiness, tremor, paresthesia/dysesthesia, sleep disorders, rarely — hypesthesia, abnormal dreams, coordination disorders (including gait disorders due to dizziness, in very rare cases leading to injuries as a result of a fall, especially in elderly patients), seizures with various clinical manifestations ( including “grand mal”seizures), attention disorders, speech disorders, amnesia, very rarely — hyperesthesia.

Mental disorders: infrequently-feelings of anxiety, increased psychomotor activity, agitation, rarely-emotional lability, depression (in very rare cases, behavior with a tendency to self-harm is possible), hallucinations, very rarely-depersonalization, psychotic reactions (potentially manifested in behavior with a tendency to self-harm).

Sensory organs: infrequently-taste disorders, visual disturbances (blurred vision, decreased visual acuity, diplopia, especially in combination with dizziness and confusion); rarely — tinnitus, impaired sense of smell, including anosmia, very rarely — loss of taste sensitivity.

Circulatory and lymphatic system disorders: infrequently-anemia, leukopenia (including neutropenia), trobocytopenia, thrombocytosis, prolongation of PV and decrease in INR, rarely-a change in the concentration of thromboplastin; very rarely-an increase in the concentration of prothrombin and a decrease in INR, a change in the concentration of prothrombin and INR.

Musculoskeletal system: infrequently-arthralgia, myalgia, rarely-tendinitis, increased muscle tone and convulsions, very rarely-tendon tears, arthritis, gait disorders due to damage to the musculoskeletal system.

Genitourinary system: often-candida superinfection, vaginitis; infrequently-dehydration (caused by diarrhea or decreased fluid intake); rarely-impaired renal function, renal failure (as a result of dehydration, which can lead to kidney damage, especially in elderly patients with concomitant renal impairment).

Skin and subcutaneous tissues: very rarely — bullous skin reactions (for example, Stevens-Johnson syndrome or potentially life-threatening toxic epidermal necrolysis).

Allergic reactions: infrequently — urticaria, pruritus, rash, eosinophilia, rarely-anaphylactic / anaphylactoid reactions, angioedema (including potentially life-threatening laryngeal edema), very rarely — anaphylactic shock (including life-threatening).

The body as a whole: infrequently — general malaise (including symptoms of poor health, non-specific pain and sweating); rarely-swelling.

Laboratory parameters: hyperlipidemia, hyperglycemia, hyperuricemia.

The incidence of the following adverse effects with the use of sequential therapy with moxifloxacin (at/in the introduction of the drug, followed by ingestion) than when taking the drug inside: often — increased level of GGT; rarely, ventricular tachyarrhythmia, hypotension, edema, pseudomembranous colitis (in rare cases associated with life threatening complications), seizures, with various clinical manifestations (including “grand mal”seizures), hallucinations, hepatic failure and renal dysfunction as a result of dehydration, which can lead to kidney damage, especially in elderly patients with concomitant renal dysfunction.

Interaction

Antacids, minerals, and multivitamins impair absorption (due to the formation of chelate complexes with polyvalent cations) and reduce the concentration of moxifloxacin in plasma (simultaneous administration is possible at intervals of 4 hours before or 2 hours after taking moxifloxacin). Concomitant use with other quinolones increases the risk of prolongation of the Q-T interval. Ranitidine reduces the absorption of moxifloxacin. It does not interact with probenecid, warfarin, oral contraceptives, theophylline, glibenclamide, morphine, itraconazole. Slightly affects the pharmacokinetic parameters of digoxin. Corticosteroids increase the risk of developing tendovaginitis or tendon rupture.

How to take it, course of administration and dosage

Avelox is taken orally at 400 mg 1 time a day. The tablet is swallowed whole, without chewing, regardless of the meal. The course of treatment for exacerbation of chronic bronchitis is 5 days, community-acquired pneumonia-10 days, acute sinusitis, skin and soft tissue infections-7 days. There is no need to change the dosage regimen in elderly patients with hepatic (groups A, B on the Child-Pugh scale) and/or renal (including those with a creatinine clearance of less than 30 ml/min/1.73 sq. m) insufficiency.

Overdose

No side effects were observed when using moxifloxacin at a dose of up to 1200 mg once and 600 mg for more than 10 days. In case of overdose, you should focus on the clinical picture and conduct symptomatic maintenance therapy with ECG monitoring. The use of activated carbon for the treatment of overdose with intravenous administration of the drug is of very limited importance.

Special instructions

During fluoroquinolone therapy, inflammation and tendon rupture may develop, especially in elderly patients and in patients receiving corticosteroids in parallel. At the first sign of pain or inflammation of the tendons, patients should stop treatment and immobilize the affected limb. There is a direct correlation between an increase in moxifloxacin concentration and an increase in the Q-T interval (risk of ventricular arrhythmias, including torsades de pointes). Therefore, the recommended dose (400 mg) and infusion rate (at least 60 minutes) should not be exceeded. If severe diarrhea develops during treatment, the drug should be discontinued.

Form of production

Tablets

Storage conditions

In a dry place, at a temperature not exceeding 25 °C

Shelf life

5 years

Active ingredient

Moxifloxacin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Adults as prescribed by a doctor

Indications

Skin Infections, Sinusitis, Bronchitis, Pneumonia, Urinary Tract Infections, Respiratory Tract

Infections Weight

Weight: 12 gr.