Abaktal - instructions for use, doses, side effects, contraindications

Excipients: lactose monohydrate 79.5 mg, corn starch 32.00 mg, povidone 32.00 mg, sodium carboxymethyl starch 32.00 mg, talc 27.00 mg, silicon dioxide colloidal anhydrous 2.00 mg, magnesium stearate 7.00 mg;

shell composition: hypromellose 13,166 mg, titanium dioxide 2,090 mg, talc 0,854 mg, macrogol-400 1,790 mg, carnauba wax 0.100 mg.

Description:From white to slightly yellowish color, oval, biconvex tablets, covered with a film membrane.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A.03 Pefloxacin

Pharmacodynamics:

Pefloxacin is a synthetic antimicrobial drug from the group of fluoroquinolones.It acts bactericidal, inhibiting the DNA-gyrase enzyme and the replication of bacterial DNA; also disrupts the replication of the A-subunit of ribonucleic acid and the synthesis of proteins by a bacterial cell. With respect to gram-negative bacteria, it acts on cells that are in both the rest phase and in the fission phase, against gram-positive bacteria-only on cells that are in the process of mitotic division. The postantibiotic effect is characteristic.

Pefloxacin has a broad spectrum of antimicrobial action.

The following microorganisms are sensitive to pefloxacin: Aeromonas hydrophila, Campylobacter jejuni, Citrobacter spp., Enterobacter spp., Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Klebsiella spp., Legionella pneumophila. Moraxella catarrhalis, Morganella morganii, Pasteurella multocida, Proteus mirabilis, indole-positive Proteus. Providencia stuartii, Salmonella spp., Serratia spp., Shigella spp., Vibrio cholerae.

Moderate sensitivity to drug have the: Streptococcus spp., Besides Streptococcus pneumoniae; Acinetobacter spp., Neisseria gonorrhoeae, Neisseria meningitidis, Staphylococcus aureus, Chlamydia trachomatis.

Sustainability have the: Clostridium perfringens, Enterococcus spp., Gardnerella vaginalis, gram-negative anaerobic microorganisms, spirochetes (Treponema spp., Borrelia spp., Leptospira spp.), Pseudomonas aeruginosa, Mycoplasma spp., Ureaplasma urealyticum and Mycobacterium tuberculosis.

Pharmacokinetics:

Absorption

Absorption is high: during 20 minutes after ingestion 90% Pefloxacin is absorbed in the gastrointestinal tract-intestinal tract (GIT). After a single oral intake of 200 or 400 mg pefloxacin per day, healthy volunteers for 1-1.5 hours maximum concentrations (C_mOh) in blood plasma were 2.5 and 4.3 μg / ml, respectively.

With repeated use of 400 mg pefloxacin twice a day, maximum and residual concentrations of pefloxacin are reached after 48 hours: the maximum serum concentration varies from 7.9 to 10 μg / ml, the remaining serum concentrations immediately before the next dose are 3.8 μg / ml.

Area under the "drug concentration / time" curve (AUC) when administered orally and intravenously is the same, indicating a complete absorption of pefloxacin and is 29.5 mg / ml / h.

Distribution

The degree of binding to plasma proteins is 20-30%, the volume of distribution is 1.7 l / kg, which ensures a uniform distribution of organs and tissues. Due to the high volume of distribution, it quickly penetrates and is well distributed in the tissues, organs and fluids of the body.

Metabolism

Pefloxacin is metabolized in the liver, with the formation of 5 metabolites, 4 of which are found in the urine.2 major metabolites - pefloxacin-N- oxide, which has minimal antibacterial activity, and N- dimethyl-pefloxacin, which has antibacterial properties.

However, its concentration is minimal and is 2-3% of the concentration of pefloxacin.

Excretion

In patients with normal kidney and liver function, 59% of the accepted dose is excreted by the kidneys unchanged and in the form of two major metabolites.

In general, 60% of the dose is excreted by the kidneys and 40% by the intestine. 20% of the dose was taken as N-dimethyl-pefloxacin and 16.2% in the form of pefloxacin-Noxide.

The drug is reabsorbed in the renal tubules. The renal clearance of pefloxacin is low, depending on the dose, varies from 0.11 to 0.21 ml per second. The half-life (T_1/2) of the drug after a single application is 10.5 hours, and with repeated administration increases to 12.3 hours. but pefloxacin and its metabolites are determined in urine within 48 hours after application.

Also 20-30% of pefloxacin is excreted with bile in the form of pefloxacin-glucuronide and Noxide derivatives. Within 12 hours after ingestion of 400 mg of pefloxacin, its concentration in the bile reached 83 μg / ml.

Pharmacokinetics in special patient groups

In case of impaired renal function plasma concentration of pefloxacin and T_1/2practically do not change due to the fact that hepatic clearance of the drug is the main mechanism of excretion.

When a violation of liver function the plasma clearance of pefloxacin is significantly reduced, and T_1/2, accordingly, increases.

Indications:

The drug Abaktal ® is used for antibacterial therapy of the following diseases caused by microorganisms sensitive to pefloxacin:

- urinary tract infections;

- bacterial prostatitis;

- infection of the lower respiratory tract (exacerbation of chronic bronchitis, exacerbation of cystic fibrosis, nosocomial pneumonia);

- infection of ENT organs (bacterial exacerbation of chronic sinusitis);

- infections of the abdominal cavity and hepatobiliary system;

- bacterial infections of the gastrointestinal tract with severe course, including salmonellosis;

- infection of bones and joints (osteomyelitis caused by gram-negative microorganisms);

- infections of the skin and soft tissues;

- bacterial endocarditis;

- meningitis (in case the pathogen is sensitive only to pefloxacin);

- gonorrhea.

The drug Abaktal ® is used as a monotherapy or as a combination therapy with other antimicrobial agents.

The drug is effective in the therapy and prevention of infections in immunocompromised patients.

Contraindications:

- Hypersensitivity to fluoroquinolones and / or to other components of the drug;

- deficiency of lactase, lactose intolerance, glucose-galactose malabsorption syndrome;

- severe liver dysfunction;

- deficiency of glucose-6-phosphate dehydrogenase;

- lesions of tendons in anamnesis, which occurred with previous treatment with fluoroquinolones;

- Children under 18 years of age (due to the risk of severe forms of arthropathy, especially large joints);

- Pregnancy and the period of breastfeeding.

Carefully:

Neurological disorders (epilepsy, convulsive syndrome of unidentified etiology, severe organic lesions of the central nervous system, cerebral circulation disorders); severe forms of renal and / or liver failure, elderly patients, congenital lengthening interval syndrome QT, heart disease (heart failure, myocardial infarction, bradycardia),electrolyte imbalance (eg, hypokalemia, hypomagnesemia), simultaneous use of drugs that extend the interval QT (including antiarrhythmic IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, imidazole derivatives, some antihistamines), simultaneous use with glucocorticosteroids, isoniazid, hypoglycemic drugs, insulin; porphyria; myasthenia gravis gravis; diabetes.

Pregnancy and lactation:

During pregnancy, the use of Abaktal® is contraindicated.

Pefloxacin penetrates into breast milk in large amounts (75% serum concentration). Therefore, during the use of the drug, it is necessary to stop breastfeeding.

Dosing and Administration:

Duration of treatment is determined individually, depending on the localization and severity of the infection, as well as the sensitivity of microorganisms.

Inside, to avoid gastrointestinal disorders, tablets should be taken with food.

The drug is used for 1 tablet (400 mg) twice a day, every 12 hours.

The average daily dose is 800 mg per day, the maximum daily dose is 1200 mg.

With infections of the urinary tract, it is possible to use the drug Abaktal® in a dose of 1 tablet (400 mg) once a day, in the morning or in the evening.

For the treatment of uncomplicated gonorrhea in men and women, 800 mg of the drug Abaktal® is administered once.

Have patients with severe impairment of liver function the removal of pefloxacin significantly slows down, so the recommended daily dose of the drug is 400 mg every 24-48 hours with the determination of its serum concentrations.

Have patients with impaired renal function excretion of pefloxacin remains almost unchanged, since part of the drug is excreted by the liver. In this regard, reducing the average daily dose of pefloxacin for patients with impaired renal function is not required.

Pefloxacin is not excreted during hemodialysis, so there is no need to additionally apply Abaktal® after a hemodialysis session.

Have elderly patients (over 65 years), due to age changes in the processes of distribution and excretion, it is recommended to reduce the dose of pefloxacin.

Side effects:

According to the World Health Organization (WHO), adverse reactions are classified according to their developmental frequency as follows: very often (≥1/10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, < 1/100), rarely (≥1 / 10000, <1/1000) and very rarely (<1/10000); frequency is unknown - according to available data, it was not possible to establish the frequency of occurrence.

From the immune system

frequency is unknown: angioedema, anaphylactic shock.

On the part of the blood and lymphatic system

infrequently: eosinophilia;

rarely: thrombocytopenia;

frequency is unknown: anemia, leukopenia, neutropenia, pancytopenia, agranulocytosis.

From the nervous system and sense organs

often: insomnia;

infrequently: headache, dizziness;

rarely: increased irritability, hallucinations;

frequency is unknown: confusion, convulsions (including epileptic seizures), disorientation, intracranial hypertension (especially in young people after prolonged therapy with nefloxacin, characterized by a favorable prognosis, in most cases resolved after the abolition of therapy and adequate treatment), paresthesia, myoclonia (sudden short-term twitching of individual muscles or muscles of the whole body),Sensory or sensory-motor peripheral neuropathy, fatigue, depression, psychosis, increased convulsive alertness, anxiety, agitation, nightmares, vision disorders, myasthenia gravis, tremor.

From the digestive system

often: nausea, vomiting, pain in the stomach;

infrequently: diarrhea:

rarely: pseudomembranous colitis, transient increase in the activity of "hepatic" transaminases, as well as alkaline phosphatase and bilirubin concentration in the blood plasma;

frequency is unknown: a change in taste, a decrease in appetite, flatulence, cholestatic jaundice, hepatitis, and necrosis of the liver.

From the skin and subcutaneous tissues

often: skin rash, hives;

infrequently: photosensitivity reactions (both to sunlight and ultraviolet radiation (UV));

rarely: skin itching, erythema;

frequency is unknown: exudative erythema multiforme, toxic epidermal necrolysis (Lyell syndrome), Stevens-Johnson syndrome, skin hyperemia, vascular purpura, photoionicholysis.

From the musculoskeletal system

often: myalgia, arthralgia;

frequency is unknown: arthropathy, tendonitis, rupture of tendons, effusion in the joints.

From the genitourinary system

rarely: acute renal insufficiency;

frequency is unknown: crystalluria, glomerulonephritis, dysuria, interstitial nephritis.

From the side of the cardiovascular system

frequency is unknown: interval lengthening QT.

From the respiratory system

frequency is unknown: bronchospasm.

Other

frequency is unknown: candidiasis.

Overdose:

Symptoms: nausea, vomiting, confusion, psychomotor agitation, in severe cases, loss of consciousness, seizures, lengthening of the QT interval.

Treatment: the patient must be under medical supervision. It is necessary to ensure a sufficient supply of fluid in the body. Treatment is symptomatic. Hemodialysis is ineffective.

Interaction:

Synergistic and additive effects are achieved with a combination of pefloxacin with rifampicin (it should be remembered that rifampicin significantly increases the plasma clearance of pefloxacin, so when these medicines are used together, plasma concentrations of pefloxacin in serum should be monitored) beta-lactam antibiotics (in the treatment of staphylococcal infection).

Aminoglycosides, piperacillin, azlocilin, ceftazidime increase the antibacterial effect (including infection with Pseudomonas aeruginosa).

Pefloxacin reduces metabolism theophylline in the liver, which leads to an increase in its concentration in the blood plasma and CNS. This can lead to an increase in the frequency and / or severity of side effects, which in rare cases may endanger life or be fatal. Therefore, with the simultaneous use of theophylline and pefloxacin, the plasma concentration of theophylline should be controlled and its dose reduced if necessary.

Pefloxacin may reduce the prothrombin index (in patients taking oral (indirect) anticoagulants). The degree of anticoagulant effect may vary depending on the nature of the disease, age and general condition of the patient. Therefore, it is necessary to monitor the International Normalized Ratio (INR) during and for some time after the combined use of pefloxacin and oral anticoagulants.

Cimetidine, ranitidine and other inhibitors of microsomal liver enzymes increase pefloxacin and increase its toxicity.

Antacids (containing aluminum or magnesium) and preparations containing iron and zinc, and didanosine (only didanosine dosage forms containing aluminum or magnesium compounds as a buffer) slow down the absorption of pefloxacin. Concerning pefloxacin should be taken with an interval of at least 2 hours before the application of these drugs or 4-6 hours after.

There was no clinically significant interaction between pefloxacin and calcium carbonate.

With the combined use of fluoroquinolones and cyclosporine it is possible to increase the concentration of creatinine and cyclosporine in the blood plasma.

Care must be taken when using together with isoniazid.

Pefloxacin can be used in combination with metronidazole and vancomycin.

When combined with tetracycline and chloramphenicol antagonism is observed.

When combined with pefloxacin glucocorticosteroids (especially in patients over 60 years old, in patients with impaired renal function and in patients with dyslipidemia), the risk of developing unwanted events (tendonitis and in very rare cases of damage to the Achilles tendon) increases.In view of this, joint use of pefloxacin and glucocorticosteroids should be avoided.

Due to a decrease in the activity of microsomal oxidation in hepatocytes, it increases the concentration and lengthens T_1/2oral hypoglycemic agents.

Pefloxacin can lengthen the interval QT, therefore, care should be taken when using drugs capable of lengthening the interval QT (eg, antiarrhythmic drugs IA and III classes; antipsychotic drugs (pimozide, haloperidol, phenothiazine derivatives); tricyclic antidepressants, some antimicrobials (erythromycin, sparfloxacin, moxifloxacin, anti-malarial drugs, macrolides); some antihistamines (astemizole), as the risk of developing life-threatening arrhythmias increases.

Special instructions:

The drug Abaktal ® is used as a monotherapy or as a combination therapy with other antimicrobial agents.

With mixed infections, with perforated processes in the abdominal cavity, with bacterial infections of the gastrointestinal tract with severe course, the drug Abaktal® is combined with drugs active against anaerobes (metronidazole, clindamycin).

During treatment, patients should receive a large amount of fluid (to prevent crystalluria).

Photosensitivity

Due to the possible appearance of a photosensitivity reaction during treatment, the Abaktal® preparation should not be exposed to UV radiation and prolonged exposure to direct sunlight. If there are any changes on the skin, treatment should be discontinued. Avoid direct sunlight for 4 days after discontinuation of therapy, otherwise it is recommended to use protective clothing or a protective cream (with a high level of UV protection).

Liver failure

For patients with severe liver disease, dose adjustment is required in proportion to the degree of damage (see section "Method of administration and dose").

Musculoskeletal system

Tendinitis, which occurs during treatment with pefloxacin, can lead to rupture of the tendon (for example, the Achilles tendon). Sometimes bilateral bilateral tendonitis may occur within 48 hours after initiation of treatment with Abaktal®, as well as several months after discontinuation of treatment with the drug.

The risk factors for the development of tendonitis against the background of fluoroquinolone therapy include: age over 60 years, renal failure, dialysis, concomitant therapy with glucocorticosteroids, dyslipidemia. In case of initial signs of tendonitis treatment with pefloxacin should be discontinued, the load on the affected limb should be eliminated and the doctor should be consulted.

To reduce the risk of tendonopathy:

- It is recommended to treat elderly patients after a careful assessment of the relationship between benefit and risk. The risk can be reduced through the use of half doses of the drug;

- the use of pefloxacin in patients with tendinitis in a history is contraindicated, it is recommended to avoid the use in patients receiving glucocorticosteroids or engaged in intensive physical exercises.

The risk of rupture is higher in patients who started walking after prolonged compliance with bed rest.

With the beginning of pefloxacin therapy, it is recommended to monitor pain and swelling in the Achilles tendon, especially in patients at risk. If these symptoms are identified, pefloxacin should be discontinued,Eliminate the burden on the affected tendons and support them with a suitable orthosis or orthopedic footwear, even if the lesion is one-sided. You should seek advice from a specialist.

Disglycemia

In patients with diabetes mellitus, taking oral hypoglycemic agents (for example, glibenclamide) or insulin, the use of pefloxacin increases the risk of hypo- / hyperglycemia. Such patients need monitoring of blood glucose concentration.

Disturbances from the nervous system

In patients receiving fluoroquinolones, including pefloxacin, sensory and sensory-motor peripheral neuropathy was noted, the onset of which can be rapid. When a patient develops symptoms of neuropathy, pefloxacin should be discontinued (minimizing the possible risk of irreversible changes). Pefloxacin should be used with caution in patients with pseudo-paralytic myasthenia gravis (myasthenia gravis).

Pefloxacin should be used with caution in elderly patients with impaired cerebral circulation, organic changes in the brain or stroke.

Pefloxacin should be used with caution in patients who have a history of seizures and conditions predisposing to their development in patients with porphyria.

Disturbances on the part of the organ of sight

If visual acuity decreases or other effects from the visual organ are observed, the ophthalmologist should be consulted immediately.

Gastrointestinal tract

Diarrhea (especially in cases of severe, persistent and / or blooded impurities) during or after application of the drug Abaktal^® may be a symptom of the disease caused by Clostridium difficile, the most severe form of which is pseudomembranous colitis. If there is a suspicion of pseudomembranous colitis, the use of Abaktal® should be stopped immediately and symptomatic treatment should be given (eg, vancomycin inside). In this condition, drugs that reduce peristalsis are contraindicated.

Heart Disease

It was reported on the lengthening of the interval QT in patients who received fluoroquinolones. Although pefloxacin can be attributed to a group of fluoroquinolones characterized by very low potential, or lacking sufficient information to assess their potential ability to elicit an interval QT, caution should be exercised while using pefloxacin with drugs that can lengthen the interval QT (for example, antiarrhythmic drugs IA and III classes; antipsychotic drugs (pimozide, haloperidol, phenothiazine derivatives); tricyclic antidepressants, some antimicrobials (erythromycin, sparfloxacin, moxifloxacin, antimalarial drugs, macrolides); some antihistamines (astemizole), as the risk of developing life-threatening arrhythmias increases.

Deficiency of glucose-6-phosphate dehydrogenase

The development of hemolytic reactions with the use of fluoroquinolones in patients with deficiency of glucose-6-phosphate dehydrogenase was reported. Although pefloxacin was not reported for hemolysis, antibiotic use in such patients should be avoided and an alternative treatment option should be avoided, if available.

Sustainability

As with other antibiotics, the use of pefloxacin, especially prolonged, can lead to the propagation of insensitive microorganisms. Repeated evaluation of the patient's condition is mandatory.If a secondary infection develops during treatment, appropriate measures should be taken.

Impact on laboratory tests

There may be false-positive results in determining opioids in urine. It may be necessary to confirm positive results using more specific methods.

Pefloxacin does not affect the tests that determine the level of glucose in the urine.

Hypersensitivity

Hypersensitivity and allergic reactions, including anaphylactic reactions, can be a consequence of the use of pefloxacin and can be life-threatening.

When developing a hypersensitivity reaction, it is necessary to cancel pefloxacin and begin appropriate therapy.

Special precautions for the destruction of unused medicinal product

There is no need for special precautions for the destruction of the unused drug Abaktal®.

Effect on the ability to drive transp. cf. and fur:

During the treatment with the drug Abaktal®, care must be taken when driving vehicles and engaging in other activities requiring concentration of attention and speed of psychomotor reactions.When neurological adverse events such as dizziness, seizures, visual impairment occur, one should refrain from performing these activities.

Form release / dosage:Tablets, film-coated, 400 mg.

Packaging:

For 10 tablets per blister of Al / Pvc.

One blister, along with instructions for medical use, is placed in a cardboard box.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use the product after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N008768 / 02

Date of registration:18.08.2010 / 22.11.2016

Expiration Date:Unlimited

The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia

Manufacturer: & nbsp

LEK d.d. Slovenia

FarmSirma Soteks, ZAO Russia

Representation: & nbspSANDOZ SANDOZ Switzerland

Information update date: & nbsp07.02.2017

Illustrated instructions

Instructions

Abaktal® (Abaktal®)