Abifloks - instructions for use of the drug, structure, Contraindications

Abiflox is an antimicrobial drug from the subspecies of fluoroquinolones. The drug has inhibitory properties on the DNA group of hydrase and topomerase IV, which leads to a failure in the production of pathogenic bacterial cells and leads to the destruction of the disease.

Abiflox: indications and dosage

Indications for the use of Abiflox are:

• treatment of inflammatory processes, caused by microorganisms susceptible to levofloxacin:
• inflammatory processes of the bronchopulmonary system (eg, pneumonia (serious illness, in which one or both lungs are affected. Bacteria may be the cause of inflammation in the lungs, fungi or viruses.));
• inflammatory processes of the urogenital tract (pyelonephritis (nonspecific inflammation of the renal pelvis, cups and parenchyma of kidney), prostatitis (inflammation of the prostate) and etc.);
• inflammation of the skin and soft tissues.

Abiflox is used as an infusion solution. The substance should be used for 3 hours after opening the vial. The solution does not require protection from light. The solution should be administered for a long time drip (100 ml of solution is injected throughout 1 o'clock).

After 3-4 days after the start of taking Abiflox, you should switch to taking oral forms of the drug. In severe stages of the disease, an increase in the standard dose is allowed.. Patients with kidney dysfunction with GFR have less 50 ml / min recommended reduction in the rate of medication:

• at GFR 50-20 ml/min - first dose - 250 mg per day, subsequent 125 mg for 24 o'clock, in severe infections – primary 500 mg for 24 o'clock, with subsequent doses 250 mg every 12 hours;
• at GFR 19-10 ml/min primary - 250 mg, subsequent - 125 mg for 48 hours, severe infections - primarily - 500 mg, subsequent - 125 mg every 12 hours;
• with GFR less 10 ml/min primary 250 mg, subsequent 125 mg, severe infections - primarily 500 mg, subsequent 125 for 24 o'clock.

When undergoing hemodialysis, additional doses of the drug should not be administered immediately after the end of the procedure.. The course of therapy is determined by the course of the disease, but the duration of treatment after leveling the temperature reactions should be carried out for 2-3 days.

Abiflox: overdose

When using large doses of Abiflox, the following types of symptoms develop:

• convulsions,
• fainting
• dizziness,
• increase in the QT interval during the passage of the ECG.

As a therapy against an overdose with Abiflox, treatment should be prescribed according to the identified symptoms.. No specific treatment has been developed. Hemodialysis is not effective for removing the active substance of the drug.

Abiflox: side effects

Possible negative reactions are transient and decrease after discontinuation of therapy. In case of individual intolerance develop:

• allergic reaction - immunopathological process, expressed by hypersensitivity of the body's immune system during repeated exposure to an allergen on an organism previously sensitized by this allergen.
• anaphylactic shock and anaphylaxis (rarely) - immediate allergic reaction, a state of sharply increased sensitivity of the body, developing with repeated exposure to the allergen.
• photosensitivity - the phenomenon of increasing the sensitivity of the body (most of the skin and mucous membranes) to the action of ultraviolet or visible radiation.
• dyspeptic manifestations - disruption of the normal functioning of the stomach, difficult and painful digestion.
• appetite and stool disorders - a pathological process in the small or large intestine. Sometimes diarrhea or constipation is a sign of stomach or duodenal disease..
• psevdomembranoznыy colitis (rarely) - acute inflammation of the colon, caused by Clostridium difficile and occurring while taking antibiotics or (less often) other medicines.
• hepatitis (rarely) - inflammatory diseases of the liver, usually of viral origin.
• elevated liver function tests (rarely).
• mycosis - a common fungal disease, caused by parasitic, pathogenic fungi.
• eozinofilija -the State of, in which there is an absolute or relative increase in the number of eosinophils.
• decrease in the level of leukocytes, Platelet, neutrophil.
• agranulocytosis - pathological condition, in which there is a decrease in the level of leukocytes (less than 1 109/l) due to granulocytes (less than 0.75 109/l) and monocytes, increases the body's susceptibility to bacterial and fungal infections.
• gemoliticheskaya anemia - a group of blood disorders, characterized by a shortening of the life cycle of red blood cells - erythrocytes.
• hypoglycemic phenomena (in patients with diabetes) - hypoglycemia is considered to be a decrease in plasma glucose concentration to a level below 2.2-2.8 mmol / l.
• emotional lability - a disorder and in a certain way even a pathology of the nervous system, moody.
• mental disorders - state of mind, different from normal, healthy.
• headache - a nonspecific symptom of various diseases and pathological conditions, pain in the head or neck.
• dizziness - a feeling of insecurity in determining one's position in space, apparent rotation of surrounding objects or one's own body, feeling of instability, disequilibrium, leaving the soil from under the feet.
• tinnitus.
• hearing loss.
• neuropathy - non-inflammatory nerve damage.
• loss of taste and smell.
• extrapyramidal disorder - a complex of neurological complications manifested by motor disorders, associated with the use of antipsychotic drugs (antipsychotic).
• visual impairment - reduced ability to see to such an extent, what causes problems, not removed by conventional means, such as glasses or medication.
• increased heart rate.
• lowering blood pressure.
• myocardial repolarization disorder - one of the cyclic phases of the functioning of the heart muscle (infarction), accompanied by the restoration of the electrical membrane charge.
• bronchospasm - constriction of the bronchi, caused by muscle contraction in response to a number of factors, eg, with bronchial asthma or bronchitis.
• allergic pneumonitis - non-infectious inflammatory process, allergic or idiopathic, affecting the interstitial tissue of the lung, extraalveolar connective tissue in the absence of alveolar exudation.
• renal failure - syndrome of violation of all functions of the kidneys, leading to water disturbance, electrolyte, nitrogen and other types of metabolism.
• tendon injury (Tendinitis) - dystrophy and inflammation of the tendon. It often accompanies other serious diseases of the body..
• arthralgia – joint pain, volatile, in the absence of objective symptoms of joint damage.
• myalgia - disease, that, primarily, occurs due to inflammation of the muscle fibers.
• raʙdomioliz - indrom, which is an extreme degree of myopathy and is characterized by the destruction of muscle tissue cells, a sharp increase in the level of creatine kinase and myoglobin, myoglobinuria, development of acute renal failure.
• burning.
• soreness and redness at the injection site.

Abiflox: Contraindications

The drug is not used in people with high sensitivity to levofloxacin or other types of quinolones. Abiflox is not recommended for patients with epilepsy., reactive manifestations from the tendons to the introduction of quinolones. Levofloxacin is not prescribed in the pediatric age group.

The effect of the drug on the reaction rate when driving a car and heavy machinery

Patients should take into account the possible adverse reactions of the nervous system when driving vehicles and heavy machinery.:

• sudden dizziness,
• prolonged drowsiness,
• blurred consciousness,
• vision and hearing problems,
• incoordination while walking.

Abiflox: use of the drug during pregnancy and lactation

Abiflox is not recommended for use during pregnancy and breastfeeding due to the risk of negative effects on the osteoarticular system of the fetus and newborn. If the drug is prescribed during lactation, it is necessary to stop breastfeeding for the entire period of therapy..

Abiflox: interactions with other drugs and alcohol

Abiflox: pharmachologic effect

Abiflox is an antimicrobial agent from the group of fluoroquinolones. The drug has an inhibitory effect on the complex of DNA hydrase and topomerase IV, which leads to disruption of bacterial cell synthesis and leads to the death of the microbial agent. Given the mechanism of action of the drug, it lacks cross-resistance between other groups of antimicrobials, but exists between groups of fluoroquinolones.

The drug is active in relation to grams (+) aerobic: Staph.saprophyticus, Strep, the group with the, G, Strep.agalactiae, Strep.pneumoniae, pyogenes;

aerobic grams (-) microorganisms: Burkholderia cepacia, Eikenella corrodens, H. influenzae, parainfluenzae, Klebsiella oxytoca, pneumoniae, Moraxella catarrhalis, Pasteurella multocida, Pr.vulgaris, Rettgeri Providence; anaerobic peptostreptococci, chlamydia, legionella, mycoplasmas, ureaplasma.

After infusion, leofloxacin accumulates in bronchial secretions and bronchi, lung tissue, urine, minimal in cerebrospinal fluid. Preparation of 40% binds to blood proteins. Metabolized slightly in the liver. Half life – 6-8 hours. Eliminated through the kidneys 85%.

EUCAST Clinical MIC Limits for Levofloxacin (20.06.2006):

CLSI Recommended MIC and Disk Diffuse Limits for Levofloxacin (M100-S17, 2007):

Abiflox: pharmacokinetics

Absorption

There is no significant difference in the pharmacokinetics of levofloxacin after intravenous and oral administration..

After intravenous administration, the drug accumulates in the bronchial mucosa and bronchial secretion of lung tissue. (concentration in the lungs exceeds that in blood plasma), Urine. Levofloxacin enters the cerebrospinal fluid poorly.

Distribution

About 30 – 40% levofloxacin binds to serum protein. Cumulative effect of levofloxacin when administered 500 mg 1 once a day repeated use is practically absent. There is a slight, but the expected cumulative effect after application of doses according to 500 mg twice a day. Steady state is reached within 3 days.

Penetration into tissues and body fluids

Penetration into the bronchial mucosa, bronchial secretion of lung tissue (BSTL)

The maximum concentration of levofloxacin in the bronchial mucosa and bronchial secretion of the lungs after application 500 mg orally were 8,3 g / and g 10,8 g / ml respectively. These indicators were achieved within one hour after taking the drug..

Penetration into lung tissue

Maximum concentrations of levofloxacin in lung tissues after application 500 mg orally were approximately 11,3 g / g and were achieved through 4 – 6:00 after drug use. The concentration in the lungs exceeds that in the blood plasma.

Penetration into the contents of the bubble

Maximum concentrations of levofloxacin 4,0 – 6,7 g / ml per bubble content reached through 2 – 4:00 after drug administration 3 days of drug administration at doses 500 mg 1 once or twice a day, respectively.

Penetration into the cerebrospinal (spinal) fluid

Levofloxacin does not penetrate well into the CSF..

Penetration into prostate tissue

After application 500 mg levofloxacin 1 once a day for 3 days, the average concentrations in the prostate tissue reached 8,7 g / g, 8,2 g / and g 2,0 g / g respectively through 2:00, 6:00 on 24 o'clock; average prostate concentration ratio / plasma was 1,84.

Concentration in urine

Average concentration in urine 8 – 12:00 after a single oral dose 150 mg, 300 mg or 500 mg of levofloxacin were 44 mg / l, 91 mg / and l 200 mg / l, respectively.

Metabolism

Levofloxacin is metabolized to a very small extent, metabolites are dismethyl-levofloxacin and levofloxacin N-oxide. These metabolites are less than 5% quantities of preparation, which is excreted in the urine. Levofloxacin is stereochemically stable and is not subject to choral structure inversion.

Conclusion

After administration and administration, levofloxacin is excreted from the blood plasma relatively slowly. (half-life is 6 – 8:00). Excreted usually through the kidneys (85% of the administered dose).

There is no significant difference in the pharmacokinetics of levofloxacin after intravenous and oral administration., which indicates that, that these paths (oral and intravenous routes of administration) are interchangeable.

Abiflox: composition and properties

Structure

Active substance - levofloxacin. IN 100 ml of drug solution contains 500 mg levofloxacin.

Excipients:

• Glucose anhydride,
• eat at dinner,
• Citric acid anhydride,
• water for injection,
• dilute hydrochloric acid.

Product form

infusion solution according to 100 ml / 500 mg in bottles No. 1.

Storage conditions

Recommended storage mode up to 25 degrees Celsius. Stored out of direct sunlight, Do not freeze.

Abiflox: general information

• Sales form: over-the-counter
• Current in-about: Levofloxacin