Last Updated on February 19, 2017 by Dr.Derek Fhisher

Levaquin Levofloxacin 250, 500, 750 mg
Most popular brand: Levaquin
Active ingredient: Levofloxacin
Available dosage forms: 250, 500, 750 mg
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Levofloxacin general information

Dearth of hygiene is among the most ordinary factors behind bacterial infections. In the event the sputum buildup is because of bronchitis or possibly a chest infection, the individual ought to go for an expectorant. For sinus infections, have a nasal spray to maintain the sinuses moist. So, once the person coughs, it’s quite easy to get rid of the phlegm from the body.

First let’s look with an infection. So it’s your responsibility to know about potential tendon problems connected with fluoroquinolone use. Normally the pain is fast and intense. Expensive and traumatic tests aren’t required.

For those who have pneumonia and are rather healthy, request a z-pack. The body has its very own mechanism of managing bacteria. It contains immunoglobulins and glycoproteins, which need to be thrown away from the body, to remove the infection. It’s also a robust antioxidant.

Cancer is really a serious medical condition that’s characterized by development of the tumor because of abnormal and uncontrolled cell division. Therefore, it makes sense to utilize antibiotics to do away with prostate infection. The consumption of said foods ought to be completely avoided, in the event the function is influenced by infection. It might even cause dehydration or nutritional deficiencies.

Metronidazole dosage, and the length of treatment might vary according to age of the individual, sort of infection, and difficulty of the condition. In the event the state of the patient will not improve, the physician may recommend a stronger antibiotic and even raise the duration of remedy. In extreme instances, surgery may be bound to treat sinusitis if timely treatment isn’t received. The dose is usually adjusted taking into regard the answer to the therapy.

Chlamydia also happens to be considered a disease which gets transmitted sexually. Also known as as prostatitis, this kind of infection causes inflammation of the prostate gland, that’s located under the bladder. In the aforementioned situation, very frequently, segments of tapeworms are passed out within the stool. Bacteria existing in the abdominal cavity, could travel into the little bowel by means of a hole within the intestine.

Red meat is just a rich generator of iron. Tuna is, in addition, abundant with iron. Green beans are likewise a rich generator of iron. Chickpeas are also a great generator of iron.

By understanding what a healthful body is regularly attempting to do is considerably more valuable than panicking. Changing your habits will enable your body to operate at its very best level. Avoid touching the sores and after that touching different sections of the human body or things around you. Rest as much as feasible eat a great deal of vitamin rich foods.

When buying an expectorant, be sure that ingredients, for example bromhexine and guaifenesin are found in it, because they are very effectual in eliminating phlegm. The cream or gel works ideal for acne rosacea as the vaginal gel is advised for vaginitis. If you just follow the above-mentioned remedies, ordinarily, it should boost your mouth’s taste. Almonds also have a wonderful quantity of iron.

Diverticulitis is the following stage of diverticulosis. Fecal impaction too is a potential side effect. This condition might be caused because of a variety of reasons. Green peas are also full of iron content.

With antibiotics, there’s usually always alternatives. In that situation, a physician needs to be contacted for more treatment. Inside this case one needs to consult the physician in order for the array of medicines may be changed. It’s available in a similarity to tablets, capsules, and injections.

Levofloxacin (Levofloxacin): instruction, and the use of a formula

Code CAS

substance Characteristics Levofloxacin

The synthetic chemotherapeutic agent, a fluorinated karboksihinolon free of impurities S – enantiomer of a racemic compound ; PM ofloxacin. Bright yellowish – white to yellow – white crystalline powder or crystals. The molecular weight of 370.38. The easily soluble in water at pH 0,6 – 6,7. The molecule exists in at values ​​Amphion pH. respective environment of the small intestine. It has the ability to form stable compounds with many metals ions. The ability to form chelates in vitro decreases in the following order: Al +3> Cu +2> Zn +2> Mg +2> Ca +2.

Pharmacology

Mode of action – antibacterial broad-spectrum bactericidal.

It has a wide spectrum of action. It inhibits bacterial topoisomerase IV and DNA – gyrase (topoisomerase type II) ; enzymes required for replication, transcription, repair and recombination of the bacterial DNA. The concentrations equivalent to or somewhat exceeding inhibitory concentrations, often has a bactericidal effect. In vitro resistance to levofloxacin resulting from spontaneous mutations rarely formed (10 & minus; 9 & minus; 10 & minus; 10). Despite the fact that between levofloxacin and other fluoroquinolones was observed cross-resistance, some resistant to other fluoroquinolones may be susceptible microorganisms to levofloxacin. Some strains of Pseudomonas aeruginosa can be fast enough to acquire resistance during treatment with levofloxacin, as well as the use of other drugs in this class.

Installed in vitro and confirmed in clinical studies of efficacy against gram-positive aerobic ; Enterococcus faecalis, Staphylococcus aureus (methicillin-susceptible strains), Staphylococcus epidermidis (methicillin-susceptible strains) , Staphylococcus saprophyticus, Streptococcus pneumoniae (including multidrug strains ; MDRSP, see “Application».), Streptococcus pyogenes . Gram-negative aerobic ; Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Legionella pneumophila, Moraxella catarrhalis, Proteus mirabilis, Pseudomonas aeruginosa . Serratia marcescens and other microorganisms ; Chlamydia pneumoniae, Mycoplasma pneumoniae.

For most

(≥ 90%) strains of the following microorganisms in vitro set minimum inhibitory concentration of levofloxacin (2 mg / ml or less), but the efficacy and safety in the clinical application of levofloxacin therapy of infections caused by these agents has not been established in adequate and well-controlled studies: gram-positive aerobes ; Staphylococcus haemolyticus, Streptococcus (group C / F), Streptococcus (group G), Streptococcus agalactiae, Streptococcus milleri . Streptococcus viridans ; Gram-negative aerobic ; Acinetobacter lwoffii, Acinetobacter baumannii, Bordetella pertussis, Citrobacter (diversus) koseri, Citrobacter freundii, Enterobacter aerogenes, Enterobacter sakazakii, Klebsiella oxytoca, Morganella morganii, Pantoea (Enterobacter) agglomerans, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Pseudomonas fluorescens ; Gram-positive anaerobes ; Clostridium perfringens.

It may be effective against microorganisms resistant to aminoglycosides, macrolides and beta – lactam antibiotics (including penicillin).

The effectiveness of levofloxacin in the treatment of community-acquired bacterial pneumonia was studied in two prospective, multicenter clinical trials. In the first randomized trial involving 590 patients with community-acquired bacterial pneumonia, a comparative study of the efficacy of levofloxacin 500 mg once a day orally or intravenously for 7 – 14 days and cephalosporins with a total duration of treatment of 7 – 14 days; if the presence of the causative agent of an atypical pneumonia anticipated or confirmed, the comparison group, patients could receive further erythromycin or doxycycline. The clinical effect (cure or improvement) 5 – 7th day after levofloxacin was 95% compared with 83% in the control group. In the second study, involving 264 patients treated with levofloxacin 500 mg once a day orally or in / over 7 – 14 days, the clinical effect was 93%. In both studies, the effectiveness of levofloxacin in the treatment of atypical pneumonia caused by Chlamydia pneumoniae, Mycoplasma pneumoniae and Legionella pneumoniae was respectively 96%, 96% and 70%. The degree of microbiological eradication rates in both studies was according to the agent: H.influenzae ; 98%, S.pneumoniae ; 95%, S.aureus ; 88%, M.catarrhalis ; 94%, H.parainfluenzae ; 95%, K.pneumoniae ; 100%.

Six additional studies have been conducted to assess the effectiveness of levofloxacin in the treatment of community-acquired pneumonia caused by Streptococcus pneumoniae, especially penitsillinoustoychivye strains. The total number of clinically examined patients with community-acquired pneumonia of mild to severe, caused by S.pneumoniae, in all 8 studies (2 prospective multicenter and 6 extra) was 250 patients in the group treated with levofloxacin, and 41 patients in the comparison group. The clinical effect (improvement or recovery) among the 250 patients treated with levofloxacin, was 245/250 (98%), while in the group treated with an alternative therapy nehinolonovuyu ; 39/41 (95%). Throughout the 8 studies in 18 patients with community-acquired pneumonia treated with levofloxacin and 4 patients treated with nehinolonovuyu therapy were identified penitsillinoustoychivye strains of S.pneumoniae (the minimum inhibitory concentration for penicillin & ge; 2 ug / ml). Of these 18 patients treated with levofloxacin, under clinical supervision until the end of treatment were 15 people with community-acquired pneumonia caused by strain penitsillinoustoychivye S.pneumoniae . clinical effect (improvement or recovery) was obtained in 15 of them. Of these 15 patients, 6 patients were diagnosed with bacteremia and 5 patients ; severe degree of the disease. Of the 4 patients control group (receiving nehinolonovuyu therapy) with community-acquired pneumonia caused by penitsillinoustoychivye S.pneumoniae, have held three clinical assessment of treatment effectiveness; of these 3 patients received clinical benefit; All three had bacteremia and severe disease.

The efficacy of levofloxacin in infectious skin lesions and skin structure was studied in an open, randomized, comparative study, involving 399 patients treated with levofloxacin 750 mg / day (intravenously. And then inside) or the reference drug for 10 & plusmn ; 4.7 days. Surgical manipulation with complicated infections (excision of necrotic tissue and drainage) shortly before or during antibiotic therapy (as part of combination therapy) were conducted in 45% of patients treated with levofloxacin, and 44% of the comparison group of patients. Among patients who were followed up for 2 – 5 days after drug treatment, the clinical effect was 116/138 (84.1%) in the group treated with levofloxacin and 106/132 (80.3%) in the comparison group

The efficacy of levofloxacin demonstrated in a multicenter, randomized, open-label study in the treatment of nosocomial pneumonia and in a multicenter, randomized, double-blind study in the treatment of chronic bacterial prostatitis.

The clinical effect of levofloxacin in the form of a 0.5% eye drops in a randomized, double-blind, multicenter, controlled trial in the treatment of bacterial conjunctivitis was the end of treatment (6 – 10 days) 79%. The degree of microbiological eradication rates were 90%.

Once inside quickly and completely absorbed from the gastrointestinal tract. absolute bioavailability tablets of 500 mg and 750 mg of levofloxacin is 99%. C max is achieved through the 1 –. 2 hours when taken concomitantly with food significantly increases the time to reach C max (1 hour) and slightly reduced C max (14%), thus levofloxacin can be administered independently from the meal. After the on / in a single administration to healthy volunteers at a dose of 500 mg (infusion over 60 min) C max was 6.2 ± 1.0 pg / ml, at a dose of 750 mg (infusion over 90 minutes ) ; 11,5 & plusmn; 4,0 ug / ml. The pharmacokinetics of levofloxacin is linear and predictable with single and repeated administration in and / in. Constant plasma concentration is reached after 48 hours upon receipt of 500 – 750 mg 1 time per day. When multiple doses in healthy volunteers values ​​of C max were: the oral administration of 500 mg / day ; 5.7 ± 1.4 pg / ml, 750 mg / day ; 8.6 ± 1.9 pg / ml; with a / in the introduction of 500 mg / day ; 6.4 ± 0.8 pg / ml, 750 mg / day ; 12.1 ± 4.1 ug / ml. The plasma concentration profile of levofloxacin after / in the introduction is similar to that after oral administration of an equivalent dose.

The average volume of distribution is 74 – 112 l after single and repeated administration of doses of 500 mg and 750 mg. Widely distributed in the body tissues, it is well into the pulmonary tissue (lung concentration 2 – 5-fold higher concentrations in plasma). In vitro in the range of concentrations of the relevant clinical significance (1 – 10 ug / ml), binding to plasma proteins (primarily to albumin) is 24 – 38% and does not depend on the concentration of levofloxacin.

stereochemically stable in plasma and urine, is not converted into its enantiomer, D – ofloxacin. The body is almost not metabolised. Excreted mainly unchanged in urine (about 87% of the dose within 48 h), a minor amount ; faeces (less than 4% for 72 hours). Less than 5% is determined in urine as metabolites (desmethyl nitrogen oxide) possessing low specific pharmacological activity. T 1/2 is 6 – 8 hours after single and repeated oral administration or /.

The Cl is 144 – 226 ml / min, renal Cl ; 96 – 142 ml / min, excretion is carried out by glomerular filtration and tubular secretion. Concomitant use of cimetidine or probenecid reduces the renal Cl respectively at 24 and 35%, indicating that the secretion of levofloxacin proximal tubules departments. levofloxacin crystals were found in freshly urine.

The pharmacokinetics of levofloxacin are not dependent on age, sex and race of the patient.

After administration of 500 mg orally to healthy volunteers – men T 1/2 was on average 7.5 hours compared to 6.1 hours for women; differences were associated with the peculiarities of renal function in men and women and had no clinical significance.

Pharmacokinetics depending on race studied by analysis of covariance data of 72 subjects: 48 white and 24 other races; there were no differences in terms of total clearance and volume of distribution.

The pharmacokinetics of levofloxacin in elderly patients does not have significant differences, taking into account individual differences in creatinine clearance values. After a single oral 500 mg levofloxacin T 1/2 in healthy elderly patients (66 – 80 years) was 7.6 hours compared to 6 hours in younger patients; differences are explained by the variability of renal function and not clinically significant. Dose adjustment in elderly patients is not required.

Renal failure: in patients with renal impairment (Cl creatinine < 50 ml / min) significantly reduced the clearance of levofloxacin and increased T 1/2 . to prevent the accumulation of dose adjustment is required. Hemodialysis and long ambulatory peritoneal dialysis do not take levofloxacin from the body and so when their conduct does not require administration of additional doses.

Hepatic impairment: pharmacokinetics study in patients with liver disease have not been conducted. Since levofloxacin metabolism is insignificant, is not expected to influence the pharmacokinetics of liver damage.

The pharmacokinetics of levofloxacin in children . After a single on / in the levofloxacin in dose of 7 mg / kg for children aged from 6 months to 16 years of drug is excreted more rapidly than in adults. Subsequent pharmacokinetic analysis showed that the dosing regimen of 8 mg / kg (250 mg dose) every 12 hours in children 6 months ; 17 years in a state of equilibrium will be attained values ​​AUC 0 – 24 and C max in the plasma that are comparable to those in adults at a dose of levofloxacin 500 mg every 24 hours

The pharmacokinetics of levofloxacin in patients with severe CAP does not differ from that in healthy volunteers.

Levofloxacin pharmacokinetics study in applying in the form of eye drops was conducted on 15 healthy volunteers. Levofloxacin concentrations in plasma were measured at various time intervals during the 15 – day course of preparation. Average plasma concentrations of levofloxacin after 1 h after instillation ranged from 0.86 ng / ml on the first day to 2.05 ng / ml on the fifteenth day. C max levofloxacin in plasma was 2.25 ng / ml and is achieved in the 4 – day after 2 days of the drug every 2 hours (up to 8 times per day). C max levofloxacin achieved a 15 – day, was more than 1000 times lower than the concentrations observed after oral administration of standard doses of levofloxacin. In studies in healthy volunteers (n = 30) showed that the average concentration of levofloxacin in the tear film, as measured at 4 and 6 hours after instillation was 17.0 ug / ml and 6.6 ug / ml, respectively.

In animal experiments, the introduction of immature rats and dogs, levofloxacin oral or / in the increased frequency and severity of osteoarthritis. Other fluoroquinolones cause the development of similar erosive changes in the joints, which have the primary weight-bearing, and other forms of arthropathy in immature animals of various species.

In immature dogs (age 4 – 5 months) oral administration of 10 mg / kg / day for 7 days or on / in a dose of 4 mg / kg / day for 14 days led to the development of arthropathy. Oral administration of 300 mg / kg / day for 7 days or / 60 mg / kg / day for 4 weeks induced arthropathy in immature rats.

In studies on mice levofloxacin exerted effect phototoxicity similar in severity to ofloxacin, but less pronounced compared to other quinolones.

Although some studies in rats at / in the introduction was observed crystalluria, urinary crystals are formed in the bladder, detected only after urination or have been associated with nephrotoxicity.

In experiments on mice, the stimulatory effect of quinolones in the CNS is enhanced by the simultaneous use of NSAIDs.

With the rapid on / in dogs at a dose of 6 mg / kg or more caused the hypotensive effect, presumably due to histamine release.

The study in vitro and in vivo levofloxacin within therapeutic concentrations had no inducing or inhibiting effect on the enzyme systems, thus fermentoposredovannogo not expected to affect the metabolism of other drugs.

carcinogenicity, mutagenicity, effects on fertility

The biological lifetime levofloxacin studies in rats did not show carcinogenic properties when administered orally daily for 2 years at doses up to 100 mg / kg / day (1.4 times excess MRDC (750 mg), based on body surface area ). Levofloxacin for each dosing regimen did not reduce the development time to UV – induced skin tumors in nude mice – albino (Skh – 1), and thus did not show fotokantserogennyh properties in experimental conditions. Levofloxacin concentration in the tissues of the skin of hairless mice was within 25 – 42 mg / g when used in the study on the maximum fotokantserogennost doses (300 mg / kg / day). For comparison, a human levofloxacin concentrations in the tissues of the skin in patients receiving 750 mg on average 11.8 g / g at C max in the plasma.

Do not showed mutagenic in the following assays: Ames test in bacteria S.Typhimurium and E.Coli, test with hypoxanthine – guanine Chinese hamster ovary cells, micronucleus test in mice, the test of dominant lethal mutations in mice, unscheduled DNA synthesis assay in rats, sister chromatid exchange test in mice. Revealed mutagenic activity in test in vitro for chromosomal aberrations (in the CHL cell line) and sister chromatid exchange (in CHL / IU cell line).

has no effect on fertility and reproductive performance in rats at oral dose of 360 mg / kg / day (4.2 times the MRDCH., Based on body surface area) or on / in a dose of 100 mg / kg / day (1.2 times higher than MRDCH., based on body surface area).

Application of the substance levofloxacin

According to the State Register (2011), levofloxacin oral and / in the introduction is indicated for the treatment of infections caused by susceptible to levofloxacin pathogens: lower respiratory tract (exacerbation of chronic bronchitis, community-acquired pneumonia), acute

Contraindications

Restrictions on the use

Application of pregnancy and breastfeeding

Category effects on the fetus by FDA ; C.

Interaction

Overdose

Dosing and Administration

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Cautions

Further Reading

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