According to the instructions, Levofloxacin is an antimicrobial drug from the class of fluoroquinolones. On sale represented by a solution for infusion, tablets. Capsules are available in two dosage forms: 250 and 500 mg. The price of the medication is quite high: for a package containing 10 capsules, pharmacies ask for more than 500 rubles. One ampoule with a solution for injective administration costs 120 rubles, but it should be understood: like any other medicine against microbial infection, Levofloxacin is used in a course, so you will have to purchase as many ampoules as the doctor will prescribe. It is impossible to discontinue use prematurely, this can trigger a relapse of the disease.
Levofloxacin: tablets
An instruction explaining how to use the drug is necessarily invested by the manufacturer in the package with the medication. It is reasonable to get acquainted with it in advance in order to avoid a negative response of the body due to incorrect reception. It is equally important to follow the recommendations of the doctor who prescribed the medication.
"Levofloxacin" was named after the main component that has a therapeutic effect - levofloxacin. The substance is contained inside a capsule, the coating of which is a thin film. The amount of active ingredient in one tablet must be indicated both on the outside of the package and in the Levofloxacin instructions: 250 or 500 mg. In addition to this compound in the manufacture of capsules used:
- polysorbate;
- carmellose;
- hypromellose;
- cellulose;
- calcium stearate;
- talc;
- titanium dioxide;
- dyes.
The instructions "Levofloxacin" describes the tablets. All items in the package must be the same, round, convex on both sides. If you cut them across, you can see two layers: inside the tablet consists of a white (sometimes light yellowish) substance, and on the outside is a colored shell. The shade depends on the manufacturer. There are currently pinkish and yellowish capsules on sale. In the instructions for Levofloxacin, the manufacturer indicates what shade the specimens should be.
general information
Levofloxacin belongs to the class of antibacterial drugs manufactured industrially. The tool, as noted in the instructions for "Levofloxacin", is completely synthetic. The main advantage is a wide range of effectiveness. The drug belongs to the class of fluoroquinolones, the active component is one of ofloxacin isomers.
Once in the body of a sick person, Levofloxacin quickly affects pathological life forms, inhibiting the activity of DNA gyrase, fourth topoisomerase, prevents cross-linking of molecular breaks, blocks supercoiling, and slows down DNA production. Under the influence of the active component, the morphology of the cytoplasm, membranes, and walls of bacterial cells changes.
Experiments and clinical studies have shown the high effectiveness of Levofloxacin in relation to a wide range of pathological microscopic life forms. The instructions for the use of Levofloxacin tablets (500 mg, 250 mg) indicate the effectiveness of the drug when infected with certain types:
- entero-staphylococci;
- corynebacteria;
- listeria;
- helico-, citro-, entero-, acinetobacter;
- gardnerell;
- eikenell;
- Klebsiella;
- moraxell;
- morganell;
- neyssery;
- Proteus;
- pseudomonads;
- salmonella.
Levofloxacin is effective against bacteroids, clostridia, peptostreptococci, bartonella, chlamydia, legionella, mycoplasma, mycobacteria, ureaplasma.
In the instructions for use with Levofloxacin tablets (500 mg, 250 mg), the manufacturer indicates moderate sensitivity to the active component from certain varieties of corynebacteria, entero-, staphylococci, campylobacter.
Resistance to Levofloxacin is characterized by methicillin-resistant staphylococci, alkaligenes, and some mycobacteria.
Sustainability mechanism
The instructions for Levofloxacin (500 mg, 250 mg - the amount of active ingredient in one tablet) mention that pathological microorganisms can obtain drug resistance as a result of a step-by-step gene mutation involving the two topoisomerases mentioned above (DNA gyrase, fourth topoisomerase). Reducing the sensitivity to antimicrobial compounds can be achieved by mechanisms:
- efflux;
- effects on penetration cell barriers.
The second option is more characteristic of some types of pseudomonads.
The instruction for use of Levofloxacin (500 mg, 250 mg) states that the drug shows a result different from most antimicrobial drugs known to medicine, therefore it does not provoke cross-resistance with other medicines of this group.
What is going on in the body?
Instructions for use "Levofloxacin" (500 mg, 250 mg) explains how the active component is absorbed, distributed throughout the body, in what quantities it is observed and in what ways it is excreted. In particular, it is mentioned that absorption takes a minimum of time and absorption is close to 100%. The quality of this process is not controlled by food intake. The bioavailability of the active substance is estimated at 99-100%.
Shortly after ingestion of 500 mg of the active substance in the blood plasma orally, the concentration of levofloxacin reaches 4.0-6.4 μg / ml. On average, it takes no more than 80 minutes to reach this level. As studies with doses of 50-1000 mg showed, the kinetics of the drug is linear. Equilibrium plasma levels are achievable on the second day, if you use Levofloxacin tablets according to the instructions 500 mg 1-2 times a day.
“Levofloxacin” binds to plasma proteins by 30-40%. Studies have shown good ability to penetrate into tissues, internal organs. The highest concentrations of Levofloxacin are found in:
- lungs;
- bronchial tubes;
- bones;
- spinal fluid;
- genitourinary organs;
- sputum;
- white blood cells;
- macrophages of the alveoli;
- prostate gland.
In the instructions for the use of Levofloxacin tablets, the manufacturer indicates that with a single and repeated ingestion of 500 mg of the active component, the distribution volume is estimated at 100 l.
With a single oral administration of 500 mg of the antimicrobial component, the highest rates of levofloxacin were found in the bronchial mucosa, the fluid of the epithelial lining. To achieve maximum levels, one and four hours were required, and the parameters were 8.3 and 10.8 μg / ml.
In the instructions for Levofloxacin 500 mg tablets, the manufacturer mentions that a five-day use of such doses allows achieving an average content of the active component in the body in the amount of 97.9 μg / ml in macrophages of the alveoli. The parameter was fixed on average 4 hours after the last dose of the composition. For the fluid lining the epithelium, the amount of levofloxacin was estimated at 9.94 μg / ml.
"Levofloxacin": tissues, organs and their features
In lung tissue with a single use of the drug in an amount of 500 mg, the highest level was observed after 4-6 hours, reaching 11.3 μg / g. Penetration is estimated at 2-5 units relative to plasma.
A three-day course of Levofloxacin tablets 500 mg (the options for using the drug as food once and twice a day were analyzed) allows you to get the concentration of the active component in the alveoli fluid in the amount of 40 μg / ml (one dose per day), 6.7 μg / ml ( two a day). Penetration is assessed per unit relative to blood plasma.
Studies have proven high ability to penetrate the spongy, cortical tissue of the bones. Penetration relative to plasma is estimated at 0.1-3, specific indicators depend on the site, especially bone tissue. The greatest amount of antimicrobial drug when using 500 mg was observed two hours after the oral administration of the drug. Localization - the proximal femur, spongy tissue of the bone. Parameters - about 15.1 mcg / g.
“Levofloxacin” can penetrate into the fluid of the spinal cord, but the process is slow, the level of penetration is low.
A three-day course of daily intake of 500 mg of antimicrobial compound allows you to get the concentration of the active component in the prostate in the amount of 8.7 μg / g with a penetration of about 1.84 relative to blood plasma.
Metabolism and elimination
About 5% of oral Levofloxacin is metabolized. Transformation products are excreted by the kidneys. The active component of the drug belongs to stereochemically stable substances, chiral transformations are not characteristic of it.
Elimination of the main dose of the accepted composition occurs through the kidneys. The half-life is seven hours, hourly deviations up or down are possible. After drug administration, 85% of the substance is orally excreted in the first two days. Less than 4% of Levofloxacin leaves the body with intestinal contents within 72 hours from the time of administration. The clearance as a whole after a single entry into the body of 500 mg is estimated at 175 ml / min with possible deviations up and down by 29.2 ml / min.
The experiments showed that injections into a vein and oral administration in kinetics are similar, there are no significant differences, which means that these two forms are mutually replaceable.
Are there any differences?
The instructions for use of Levofloxacin indicate that the drug equally affects the male and female body. There are no differences in kinetics when taking the medication by people of a young, middle, old age. An exception is the effect of creatinine clearance.
If renal failure is established, dosage adjustment and patient monitoring are required, as the kinetics of the pharmaceutical product may change. The worse the kidneys work, the lower the clearance, the longer the half-life of the drug from the body. The manufacturer in the instructions for use "Levofloxacin" gives the exact kinetics for a single dose of 500 mg of the drug.
When will it help?
Indications for use are infectious, inflammatory processes initiated by pathological microscopic life forms that are sensitive to Levofloxacin. The instructions for use indicate the following diagnoses:
- sinusitis;
- pyelonephritis;
- infection of the genitourinary system with and without complications;
- exacerbations of bronchitis;
- chronic prostatitis, provoked by bacteria;
- community-acquired pneumonia;
- infection of the skin, soft tissues.
In case of tuberculosis, Levofloxacin is used as an element of complex therapy. The manufacturer in the instructions for use of "Levofloxacin" indicates the possibility of taking the composition as a prophylactic and therapeutic for anthrax, if the transmission route is airborne.
The use of "Levofloxacin" should be subject not only to instructions, but also to national, local recommendations, rules, and guidelines regarding antimicrobial medicines. To maximize the effectiveness of the course of treatment, you should first check the sensitivity of microorganisms to the active component, only then prescribe a program.
Strongly impossible!
Instructions for use "Levofloxacin" contains the following contraindications:
- hypersensitivity, immunity of quinolones in general, levofloxacin in particular;
- Too high sensitivity to other substances used in the manufacture of the drug;
- epilepsy;
- pseudoparalytic myasthenia gravis.
You can not use the composition if the medical history contains references to previous treatment with quinolones, which caused damage to the tendons.
It is not allowed to use the composition during the period of gestation, breastfeeding, as well as until reaching adulthood. This is due to the effect on bone tissue. The use of tablets during pregnancy can lead to damage to the growth points of the cartilage of the embryo, a similar effect can cause levofloxacin, which enters the body of a baby with breast milk. Until adulthood, “Levofloxacin” is contraindicated, since the skeleton is still developing, which means that irreversible disturbances of the cartilage growth points are possible.
You can, but very carefully
The instructions for use of "Levofloxacin" indicate the groups of patients for whom the drug is permitted, but its use requires special care. The following health conditions and characteristics are mentioned:
- predisposition to cramps;
- glucose-6-phosphate dehydrogenase deficiency;
- organic disorders of the central nervous system;
- the use of medications that lower the threshold of convulsions;
- impaired renal function;
- risk factors that increase the QT interval;
- diabetes mellitus corrected by hypoglycemic agents for oral use;
- history of severe negative response to fluoroquinolones;
- mental disorders in the medical history;
- porphyria.
How to use?
In the instructions for use, "Levofloxacin" is recommended for use 1-2 times a day. It is not necessary to disrupt the integrity of the tablet, chew or dissolve the capsule. The tablet is washed abundantly with water. You can use the medication before meals, between those.
The doctor chooses the dosage, focusing on the particular health, diagnosis, severity of the course of the disease, the sensitivity of the pathogen to Levofloxacin. It is possible to use the medication first by injecting into a vein with a gradual transition to the oral form. Dose adjustment when changing the form is not required, since the bioavailability of the capsule format is close to 100%.
With normal renal functionality, with a small deviation from the norm (creatinine clearance - from 50 ml / min or more), Levofloxacin is indicated in the following doses:
- sinusitis - a two-week course, a daily single dose of 500 mg;
- exacerbation of bronchitis - 10-day course, daily single use of 500 mg;
- community-acquired pneumonia - a two-week course, 500 mg daily once or twice;
- infection of the urinary system without complications - three-day intake, 250 mg daily;
- chronic prostatitis - a four-week course, 500 mg daily;
- infection of the urinary system with complications - a two-week course, daily use of 500 mg;
- pyelonephritis - a ten-day program, 500 mg daily;
- tuberculosis - daily use once or twice 500 mg of an antibacterial agent - the duration of such treatment can reach a quarter of a year.
In case of infection of the skin and soft tissues, Levofloxacin is used in a two-week course of 500 mg once or twice daily.
As a prophylactic and therapeutic agent for anthrax, Levofloxacin is indicated in an eight-week course. Tablets are taken once a day, the dosage is 500 mg.
If dose reduction due to renal failure is necessary, Levofloxacin, available in 250 mg format, is used: each copy is equipped with a risk that allows the capsule to be divided into two parts of 125 mg.
Some features
The reviews and instructions for “Levofloxacin” indicate that the drug is suitable for the treatment of elderly patients, does not require special adjustments if the creatinine clearance is 50 ml / min or more.
Those taking the composition noted that in case of impaired liver functionality, the drug was also prescribed in standard doses. The manufacturer explains this by the fact that the metabolism of the antimicrobial agent mainly proceeds in the kidneys, and only a small percentage of the liver accounts for it.
In the reviews left by the doctors, instructions for using Levofloxacin, the effectiveness of the medication is indicated only with course use. Like other antimicrobial substances, levofloxacin only works when taken during the period of the disease and another 2-3 days after stabilization. If recovery is confirmed by laboratory tests, the tablets continue to be used for a couple of days to prevent relapse. Stopping prematurely can provoke superinfection.
Side effects: what do the reviews say?
The instructions to Levofloxacin (500 mg, 250 mg) indicate that the drug can provoke a negative response of the body, as well as the average frequency of occurrence of various negative effects. In practice, as many people taking the medication say, the drug is well tolerated, although you can’t do without troubles. So, many people were sick and dizzy while using the substance. It is indicated in the reviews on Levofloxacin, the instruction (500 mg, 250 mg) also confirms the high likelihood of such a phenomenon that patients encountered temporary discomfort from the gastrointestinal tract: stool was broken, nausea, and vomiting disturbed. Another common negative effect of taking is sleep disturbance.
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Special cases
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Strains of microscopic pathological life forms can become resistant to the active component of the drug. Sustainability indicators vary significantly in different areas, a lot depends on time. Before you start using, you should find out how resistant the strains are, common in the area, region, country to antimicrobial substance. In the absence of a pronounced effect when taking the composition against a background of a serious illness, it is important to make a microbiological diagnosis in a timely manner, determine the pathogen, and establish the degree of sensitivity to Levofloxacin.
From the accumulated medical statistics it is known that the risk of resistance to Levofloxacin of Staphylococcus aureus resistant to methicillin is especially high. If infection with this particular microorganism is expected, Levofloxacin should not be used until laboratory tests confirm the effectiveness of the drug in a particular case.
Quinolones in general, Levofloxacin in particular, can provoke a convulsive state in persons who are predisposed to this. The use of the drug requires accuracy if a person has previously suffered a head injury or is forced to undergo therapy with drugs that lower the threshold of brain preparedness for convulsions.
Diagnoses and Levofloxacin
Against the background of prima, there is a risk of prolonged loose stool containing blood. This may indicate colitis, provoked by one of the forms of clostridia. If such a complication is suspected, the patient's condition is transferred to antibiotic treatment:
- metronidazole;
- teicoplanin;
- vancomycin.
You can not use tools that can slow down the peristalsis of the gastrointestinal tract.
With the use of Levofloxacin, tendonitis is possible. This is rarely observed, but can cause tendon rupture. As a rule, if a side effect develops, then in the first two days from the start of administration. Possible bilateral tendonitis. To a greater extent, the risk of this condition is inherent in elderly patients, as well as those taking glucocorticosteroids.
If the symptoms make it possible to suspect tendonitis, antibiotic therapy is stopped, a course of restoration of tendon integrity is started, immobilizing the damaged area.
Drug reactions
It is known that Levofloxacin can provoke a hypersensitivity reaction that is potentially life-threatening to the patient. With hints of such an allergic response, it is necessary to stop treatment and get to the doctor as quickly as possible.
From medical practice, several cases of bullous reactions, necrolysis of the skin, Steven-Johnson syndrome, which developed against the background of the use of Levofloxacin, are known. With any skin manifestations of intolerance, sensitivity to the drug, with disturbing conditions of the mucosa, the medication is not used, they seek the help of a doctor.
In a very small percentage of cases, patients taking Levofloxacin experience a photosensitivity reaction. To minimize the risk of such a phenomenon, during therapy, two days after its completion, it is recommended to avoid strong exposure to ultraviolet light, that is, do not spend time in sunlight, do not visit solariums.
The use of the drug is associated with the likelihood of developing superinfection. To a greater extent, this is characteristic of long courses of treatment, when colonies of life forms that are not sensitive to levofloxacin begin to multiply actively in the body. Perhaps a change in the composition of human microflora, the appearance of superinfection. With prolonged treatment, it is recommended that regular studies be conducted to determine the level of susceptibility of levofloxacin with pathological microorganisms. If superinfection is established, the doctor adjusts the therapeutic program taking into account its features.