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Levaquin

Levaquin
Levaquin is indicated for infectious and inflammatory diseases caused by sensitive microorganisms.

Brand: Levofloxacin

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: January 2024
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Levaquin 750 mg
180 pills - 750 mg
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Levaquin 500 mg
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Levaquin 250 mg
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Product description

Pharmacological action of the Levaquin

Buy Levaquin in Canada

Levofloxacin is a synthetic antibacterial drug with a broad spectrum of action from the group of fluoroquinolones, containing levofloxacin as an active substance - the levorotatory isomer of ofloxacin. Levofloxacin blocks DNA gyrase, disrupts supercoiling and cross-linking of DNA breaks, inhibits DNA synthesis, and causes deep morphological changes in the cytoplasm, cell wall and membranes.

Levofloxacin is active against most strains of microorganisms both in vitro and in vivo.

Aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus faecalis, Enterococcus spp, Listeria monocytogenes, Staphylococcus coagulase-negative methi-S (I), Staphylococcus aureus methi-S, Staphylococcus group), Staphylococcus spp. and G, Streptococcus agalactiae, Streptococcus pneumoniae peni I / S / R, Streptococcus pyogenes, Viridans streptococci peni-S / R.

Aerobic gram-negative microorganisms: Acinetobacter baumannil, Acinetobacter spp, Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Enterobacter cloacae, Enterobacter cloacae, Enterobacter cloacae, Enterobacter coli, Enterobacter cloacae, Enterobacter coli, Enterobacter cloacae, Spp. Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella oxytoca, Klebsiella pneumoniae, Klebsiella spp, Moraxela catarrhalis (3 + / p-, Morganella morganii, Neisseria gonorrhoeae Pasurella Pasurella Pasurella Pasurella Pasurella conisseria meningisit, Neisseria meningisit mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Providencia spp, Pseudomonas aeruginosa, Pseudomonas spp, Salmonella spp, Serratia marcescens, Serratia spp.

Anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Bifidobacterium spp., Bifidobacterium spp. Veilonella spp.

Other microorganisms: Bartonella spp, Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella pneumophila, Legionella spp, Mycobacterium spp, Mycobacterium leprae, Micobacterium tuberculosis, Mycoplasma hominia, Ucoplasma pneumonia.

Pharmacokinetics

Levofloxacin is rapidly and almost completely absorbed after oral administration. Food intake has little effect on the rate and completeness of absorption. The bioavailability of 500 mg of levofloxacin after oral administration is almost 100%. After taking a single dose of 500 mg of levofloxacin Cmax is 5.2-6.9 μg / ml, the time to reach Cmaxis 1.3 h, T1/2 is 6-8 h.

Plasma protein binding is 30-40% ... It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, genitourinary organs, bone tissue, cerebrospinal fluid, prostate gland, polymorphonuclear leukocytes, alveolar macrophages.

In the liver, a small portion is oxidized and / or deacetylated. It is excreted from the body mainly by the kidneys by glomerular filtration and tubular secretion. After oral administration, approximately 87% of the dose is excreted unchanged in the urine within 48 hours, less than 4% in the feces within 72 hours.

Indications for Levofloxacin

Levaquin for the treatment of inflammation

Infectious and inflammatory diseases caused by sensitive microorganisms:

  • acute sinusitis;

  • exacerbation of chronic bronchitis;

  • community-acquired pneumonia;

  • complicated urinary tract infections (including pyelonephritis);

  • uncomplicated urinary tract infections;

  • prostatitis;

  • infections of the skin and soft tissues;

  • septicemia / bacteremia associated with the above indications;

  • intra-abdominal infection.

Dosage regimen of the drug Levaquin

Levaquin tablet appearance

The drug is taken orally 1 or 2 times a day. Do not chew the tablets and drink a sufficient amount of liquid (from 0.5 to 1 cup), can be taken before meals or between meals. Doses are determined by the nature and severity of the infection, as well as the sensitivity of the suspected pathogen.

For patients with normal or moderately reduced renal function (creatinine clearance> 50 ml / min.), The following dosage regimen is recommended: sinusitis: 500 mg once a day for 10-14 days; exacerbation of chronic bronchitis: 250 mg or 500 mg once a day - 7-10 days; community-acquired pneumonia: 500 mg 1-2 times a day - 7-14 days. uncomplicated urinary tract infections: 250 mg once a day - 3 days; prostatitis: 500 mg - 1 time per day - 28 days; complicated urinary tract infections, including pyelonephritis: 250 mg once a day for 7-10 days; infections of the skin and soft tissues: 250 mg once a day or 500 mg 1-2 times a day - 7-14 days; septicemia / bacteremia: 250 mg or 500 mg 1-2 times a day for 10-14 days; intra-abdominal infection: 250 mg or 500 mg once a day - 7-14 days (in combination with antibacterial drugs acting on the anaerobic flora).

Patients after hemodialysis or continuous ambulatory peritoneal dialysis do not require additional doses.

Patients with impaired liver function do not require a special selection of doses, since levofloxacin is metabolized in the liver only to an extremely insignificant extent.

As with the use of other antibiotics, it is recommended to continue treatment with Levofloxacin for at least 48-78 hours after normalization of body temperature or after laboratory-confirmed recovery.

Contraindications for use

  • hypersensitivity to levofloxacin or other quinolones;

  • renal failure (with creatinine clearance less than 20 ml / min - due to the impossibility of dosing this dosage form);

  • epilepsy;

  • tendon lesions during previous treatment with quinolones;

  • children and adolescents (up to 18 years old);

  • pregnancy and lactation.

Itcaution should be used within the elderly due to the high likelihood of a concomitant decrease in renal function, as well as with a deficiency of glucose-6-phosphate dehydrogenase.

Application during pregnancy and lactation

Contraindicated during pregnancy and lactation.

Application for impaired liver function

Patients with impaired liver function do not require a special selection of doses, since levofloxacin is metabolized in the liver only to an extremely insignificant extent.

Application for impaired renal function

Contraindicated in renal failure (with creatinine clearance less than 20 ml / min. - due to the impossibility of dosing this dosage form).

Patients after hemodialysis do not require additional doses.

Use in children

Levofloxacin cannot be used to treat children and adolescents (under 18 years of age) due to the likelihood of damage to the articular cartilage.

Use in elderly patientselderly patients

When treating, it should be borne in mind that patients in this group often suffer from impaired renal function (see section "Method of administration and dosage").

Special instructions

Levofloxacin cannot be used to treat children and adolescents due to the likelihood of damage to the articular cartilage.

When treating elderly patients, it should be borne in mind that patients in this group often suffer from impaired renal function (see section "Dosage and Administration").

In severe pneumococcal pneumonia, levofloxacin may not provide optimal therapeutic benefits. Hospital infections caused by certain pathogens (P. aeruginosa) may require combination treatment.

During treatment with Levofloxacin, a seizure attack may develop in patients with previous brain damage caused, for example, by stroke or severe trauma.

Despite the fact that photosensitization is very rare when using levofloxacin, in order to avoid it, patients are not recommended to be exposed unnecessarily to strong solar or artificial ultraviolet radiation.

If pseudomembranous colitis is suspected, levofloxacin should be discontinued immediately and appropriate treatment initiated. In such cases, you can not use drugs that inhibit intestinal motility.

Rarely observed when using Levofloxacin, tendonitis (primarily inflammation of the Achilles tendon) can lead to tendon rupture. Elderly patients are more prone to tendinitis. Treatment with glucocorticosteroids is likely to increase the risk of tendon rupture. If tendonitis is suspected, treatment with Levofloxacin should be stopped immediately and appropriate treatment for the affected tendon should be initiated.

Patients with deficiency of glucose-6-phosphate dehydrogenase (hereditary metabolic disorder) can react to fluoroquinolones by destroying red blood cells (hemolysis). In this regard, the treatment of such patients with levofloxacin should be carried out with great caution.

Effects on the ability to drive vehicles and use mechanisms

Side effects of Levofloxacin, such as dizziness or numbness, drowsiness and visual disturbances (see also the section "Side effects), can impair the reactivity and ability to concentrate. This may pose a certain risk. in situations where these abilities are of particular importance (for example, when driving a car, when servicing machines and mechanisms, when performing work in an unstable position)

Overdose

Symptoms of an overdose of Levofloxacin appear at the level of the central nervous system (confusion, dizziness, impaired consciousness and seizures In addition, gastrointestinal disorders (for example, nausea) and erosive lesions of the mucous membranes, prolongation of the QT interval may occur.

Treatment should be symptomatic. Levofloxacin is not excreted by dialysis (hemodialysis, peritoneal dialysis and standing peritoneal dialysis). There is no specific antidote.

Drug interaction

There are reports of a pronounced decrease in the threshold of convulsive readiness with the simultaneous use of quinolones and substances that can, in turn, lower the cerebral threshold of convulsive readiness. This also applies to the simultaneous use of quinolones and theophylline.

The effect of the drug Levofloxacin is significantly weakened when used simultaneously with sucralfate. The same happens with the simultaneous use of magnesium- or aluminum-containing antacids, as well as iron salts. Levofloxacin should be taken at least 2 hours before or 2 hours after taking these drugs. No interaction with calcium carbonate was found.

With the simultaneous use of vitamin K antagonists, it is necessary to control the blood coagulation system.

Excretion (renal clearance) of levofloxacin is slightly slowed down by cimetidine and probenicid. It should be noted that this interaction has practically no clinical significance. However, with the simultaneous use of drugs such as probenicid and cimetidine, which block a certain route of excretion (tubular secretion), treatment with levofloxacin should be carried out with caution. This applies primarily to patients with limited renal function.

Levofloxacin slightly increases the half-life of cyclosporine.

Taking glucocorticosteroids increases the risk of tendon rupture.

Side Effects of Levofloxacin Substance

Serious and clinically important adverse drug reactions, which are discussed in more detail in the Precautions section, include:

- effects on tendons;

- exacerbation of pseudoparalytic myasthenia gravis (myasthenia gravis);

- hypersensitivity reactions;

- other serious and sometimes fatal reactions;

- hepatotoxicity;

- action on the central nervous system;

- Clostridium difficile-associated diarrhea;

- peripheral neuropathy, which may be irreversible;

- lengthening of the QT interval;

- fluctuations in blood glucose levels;

- photosensitivity / phototoxicity;

- development of drug resistance of bacteria.

Hypotension was associated with rapid or bolus IV administration of levofloxacin. Levofloxacin should be injected slowly, over 60 to 90 minutes.

Crystalluria and cylindruria have been reported with fluoroquinolones, including levofloxacin. Therefore, during treatment with levofloxacin, it is necessary to maintain adequate hydration in patients in order to avoid the formation of excessively concentrated urine.

Experience

Clinical TrialsBecause clinical trials are conducted with a different set of conditions, the incidence of adverse reactions observed in these trials cannot be directly compared with those in other clinical trials and cannot predict the occurrence of adverse events in clinical practice.

Data are provided from 29 phase 3 pooled clinical trials (n = 7537). The average age of patients is 50 years (approximately 74% of patients are under 65 years of age), 50% are men, 71% are Caucasian, 19% are black. Patients received levofloxacin for the treatment of various infections at a dose of 750 mg once a day, 250 mg once a day, or 500 mg twice a day. The duration of therapy was usually 3-14 days (average 10 days).

The overall frequency, type and distribution of adverse reactions were similar in patients who received levofloxacin at a dose of 750 mg once a day, compared with patients who received 250 mg once a day or 500 mg twice a day. Therapy was discontinued due to drug-related side effects in 4.3% of patients overall, 3.8% of patients taking 250 and 500 mg doses, and 5.4% of patients taking 750 mg. The most common side effects leading to discontinuation of the drug at doses of 250 and 500 mg were gastrointestinal complaints (1.4%), nausea (0.6%), vomiting (0.4%), dizziness (0.3%) , headache (0.2%). The most common side effects leading to drug discontinuation at a dose of 750 mg were gastrointestinal disturbances (1.2%), nausea (0.6%), vomiting (0.5%), dizziness (0.3%), headache. pain (0.3%).

Below are the side effects noted in clinical trials and observed with a frequency of> 0.1% in patients treated with levofloxacin (N = 7537). The most common adverse reactions (≥3%) were nausea, headache, diarrhea, insomnia, constipation, and dizziness.

From the nervous system and sensory organs: headache (6%), dizziness (3%), insomnia1 (4%); 0.1-1% - anxiety, agitation, confusion, depression, hallucinations, nightmares1, sleep disturbance1, anorexia, unusual dreams1, tremor, convulsions, paresthesia, vertigo, hypertension, hyperkinesis, impaired coordination of movements, drowsiness1, fainting.

From the side of the cardiovascular system and blood: 0.1-1% - anemia, arrhythmia, palpitations, cardiac arrest, supraventricular tachycardia, phlebitis, epistaxis, thrombocytopenia, granulocytopenia.

From the respiratory system: shortness of breath (1%).

From the digestive tract: nausea (7%), diarrhea (5%), constipation (3%), abdominal pain (2%), dyspepsia (2%), vomiting (2%); 0.1-1% - gastritis, stomatitis, pancreatitis, esophagitis, gastroenteritis, glossitis, pseudomembranous colitis, liver dysfunction, increased liver enzymes, increased alkaline phosphatase.

From the genitourinary system: vaginitis2 (1%); 0.1-1%: impaired renal function, acute renal failure, genital candidiasis.

On the part of the musculoskeletal system: 0.1-1% - arthralgia, tendonitis, myalgia, pain in skeletal muscles.

On the part of the skin: rash (2%), itching (1%); 0.1-1% - allergic reactions, edema (1%), urticaria.

Others: candidiasis (1%), reaction at the intravenous injection site (1%), chest pain (1%); 0.1–1%: hyperglycemia / hypoglycemia, hyperkalemia.

In clinical trials using multiple doses, ophthalmic disorders, including cataracts and multiple pinpoint opacities of the lens, have been observed in patients treated with fluoroquinolones, including levofloxacin. The relationship between these phenomena and the use of drugs has not been established.

1 N = 7274

2 N = 3758 (women)

Post-marketing studies

It is impossible to reliably assess the frequency of these phenomena and the causal relationship with drug intake, since messages were received spontaneously, from a population of unknown size.

From the nervous system and sensory organs: isolated reports of encephalopathy, EEG disorders, peripheral neuropathy (may be irreversible), psychosis, paranoia, isolated reports of suicidal attempts and suicidal thoughts, uveitis, visual impairment (including diplopia, decreased visual acuity, blurred vision, scotoma), hearing loss, tinnitus, parosmia, anosmia, loss of taste, perversion of taste, dysphonia, exacerbation of myasthenia gravis, pseudotumor of the brain.

From the side of the cardiovascular system and blood: isolated reports of torsade de pointes, prolongation of the QT interval, tachycardia, vasodilation, increased INR, prolongation of PT, pancytopenia, aplastic anemia, leukopenia, hemolytic anemia, eosinophilia.

From the digestive tract: liver failure (including fatal cases), hepatitis, jaundice.

From the musculoskeletal system: tendon rupture, muscle damage, including rupture, rhabdomyolysis.

On the part of the skin: bullous rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, photosensitivity / phototoxicity reactions.

Allergic reactions: hypersensitivity reactions (sometimes fatal), incl. anaphylactic / anaphylactoid reactions, anaphylactic shock, angioedema, serum sickness; isolated reports of allergic pneumonitis.

Others: leukocytoclastic vasculitis, increased activity of muscle enzymes, hyperthermia, multi-organ failure, interstitial nephritis.

When using levofloxacin in the form of 0.5% eye drops, the most frequently observed effects were: 1-3% - transient decrease in vision, transient burning sensation, pain or discomfort in the eye, sensation of a foreign body in the eye, fever, headache, pharyngitis, photophobia; <1% - allergic reactions, eyelid edema, dry eye, itchy eye.