2010/06/16

Abaktal

Composition, structure and packing

Coated tablets, white or slightly yellowish, oval, biconvex.

1 tab. pefloxacin (in the form mesylate dihydrate) - 400 mg.

Excipients: lactose monohydrate, maize starch, povidone, demineralized water, sodium starch glycolate, talc, silicon dioxide, colloidal anhydrous, magnesium stearate.

The composition of the shell: gipromelloza, titanium dioxide, talc, macrogol 400, carnauba wax. 10 pcs. - Blisters (1) - packs cardboard.

Concentrate for solution for i / in introducing a transparent, light yellow to yellow.

Excipients: ascorbic acid, sodium metabisulfite, disodium edetate, benzyl alcohol, sodium bicarbonate, water, d / and.

Clinico-pharmacological group: antibacterial fluoroquinolone group.

Pharmacological action

Synthetic antibacterial drug of the group of fluoroquinolones.

Has bactericidal activity by inhibiting DNA replication of bacteria at the level of DNA-gyrase. Abaktal active against Staphylococcus aureus, Escherichia coli, Klebsiella spp., Enterobacter spp., Serratia spp., Proteus mirabilis, indole-positive strains of Proteus spp., Sitrobacter spp., Salmonella spp., Shigella spp., Haemophilus influenzae, Neisseria gonorrhoeae . To the drug moderately susceptible Streptococcus spp. (Including Streptococcus pneumoniae), Pseudomonas spp., Acinetobacter spp., Clostridium perfringens, Mycoplasma spp., Chlamydia spp.

To the drug resistant Gram-negative anaerobes, Spirochaeta spp., Mycobacterium tuberculosis.

Pharmacokinetics

Absorption

After oral pefloxacin well absorbed from the gastrointestinal tract. Cmax is achieved through 1-1.5 h after administration. Bioavailability - 100%.

Distribution

The degree of plasma protein binding is 25-30%. Vd - 1.7 L / kg. Pefloxacin rapidly penetrates into tissues, organs and body fluids (aortic valve, mitral valve, cardiac muscle, bone, abdominal cavity, peritoneal fluid, gall bladder, prostate gland, saliva, sputum).

Concentration of pefloxacin in these fluids and tissues of higher concentrations in blood plasma.

Metabolism and excretion

Biotransformiruetsya in the liver. T1 / February is approximately 10.5 h. In the normal liver and kidney function about half the administered dose excreted in the urine as unchanged or as metabolites within 48 h. Approximately 20-30% of pefloxacin excreted in the bile.

Pharmacokinetics in special clinical situations

In case of violation of renal function plasma concentration of pefloxacin and T1 / 2 did not change.

If any function of the liver plasma clearance pefloxacin significantly reduced, and T1 / 2 increases accordingly.

Statement

Treatment of infectious diseases caused by microorganisms sensitive to the drug:
infection of the kidneys and urinary tract infections;
pelvic infections (including adnexitis, prostatitis);
Infection of lower respiratory tract;
infection ENT organs (including chronic sinusitis, severe external otitis);
severe bacterial infections GIT (including salmonella, typhoid fever);
infection of the liver and biliary tract;
infection of the abdominal cavity (intra-abdominal abscesses, peritonitis);
infections of the bones, joints and connective tissue (including bone abscess);
infections of skin and soft tissue (including caused by staphylococci resistant to penicillin);
meningeal infection
sepsis
bacterial endocarditis;
gonorrhea.

It is used as monotherapy or in combination with other antimicrobial drugs. The drug is effective in preventing infections in immunocompromised patients.

Dosage regimen

The average dose for ingestion of 800 mg / day. The drug is prescribed 400 mg (1 tab.) 2 times a day, every 12 h. The maximum daily dose - 1.2 g. When treating certain infections of the genitourinary system can assign Abaktala a dose of 400 mg (1 tab.) 1 times / day in the morning or evening.

For the treatment of uncomplicated gonorrhea in men and women prescribed the drug once a dose of 800 mg. When expressed hepatic failure should appoint a drug at a dose of 400 mg / day (every 24-48 h). The tablets should be taken with food to avoid violations of the gastrointestinal tract.

In / in a drug administered in the form of infusion at a dose of 400 mg every 12 h duration of infusion - 1 pm Pre contents of one ampoule (400 mg) was diluted with 250 ml of 5% dextrose (glucose). Abaktal not dilute solution of sodium chloride or any solvent containing chloride ions. For a more rapid achievement of therapeutic concentrations allowed the introduction of the first dose of 800 mg.

The maximum daily dose - 1.2 PM for the prevention of infectious complications in the surgery recommended by a / in the introduction of the drug in doses of 400-800 mg for 1 h before the operation.

For patients with liver disease a single dose for the i / v drip administration of 8 mg / kg body weight, duration of infusion - 1 h. The frequency of infusions of patients with obstructive jaundice 1 times in 24 h in patients with ascites - 1 time in 36 h in patients with jaundice and ascites - 1 times in 48 hours in elderly patients especially with concomitant impaired renal function should be to reduce the dose as when administered, and when i / in the introduction.

Side effect

On the part of the digestive system: loss of appetite, indigestion, diarrhea, nausea, taste changes, vomiting, transient increase in liver enzymes, alkaline phosphatase and bilirubin; very rarely - pseudomembranous colitis.

From the side of the central nervous system: headache, anxiety, dizziness, mental state of heightened excitement, depression, insomnia, blurred vision, confusion, hallucinations, tremors, rare - convulsions.

From the urinary system: crystalluria; rarely - hematuria, interstitial nephritis.

From the Musculoskeletal System: myalgia, arthralgia, tendonitis, and in very rare cases - Achilles tendon rupture.

Local reactions: phlebitis.

Allergic reactions: skin rash, itching, hives, redness of the skin rarely - bronchospasm, photosensitivity. Other: transient changes in patterns of peripheral blood.

Contraindications
Pregnancy
lactation (breastfeeding);
age 18;
Hypersensitivity to quinolones.

With care prescribers in violation of the central nervous system (including epileptic syndrome of unknown etiology), combined renal and hepatic failure, with liver failure and severe.

Pregnancy and lactation

Abaktal contraindicated in pregnancy. If necessary, use during lactation should decide on the termination of breastfeeding.

Be wary prescribers with combined kidney-liver failure, with liver failure and severe.

For patients with liver disease a single dose for the i / v drip administration of 8 mg / kg of body weight, duration of infusion - 1 pm

The frequency of infusions of patients with obstructive jaundice 1 times in 24 h in patients with ascites - 1 times in 36 h in patients with jaundice and ascites - 1 times in 48 hours

Be wary prescribers with combined kidney-liver failure.

Cautions

An injection is used only in a hospital. Because of possible photosensitization during treatment Abaktalom should avoid UV radiation and direct sunlight for 6 days after cessation of therapy. If you have an allergic reaction or changes in the CNS, as well as in suspected tendonitis should immediately remove the drug. Risk factors for the development of tendonitis during therapy with fluoroquinolones include: age over 60 years, renal failure, dialysis, concomitant therapy GCS, dyslipidemia.

Patients should be warned about the need to abolish the drug if the appearance of early signs of tendonitis, eliminate the burden on the affected limb and seek medical advice. There may be false positive results in the determination of glucose in the urine by the method of recovery of copper (using a copper sulfate), and therefore should be used enzymatic methods of analysis. The drug can be used in combination with beta-lactam antibiotics, metronidazole, vancomycin and rifampicin. Be careful while appointing pefloxacin and isoniazid. Effects on ability to drive motor vehicles and management mechanisms on the background of Abaktala caution during the occupation of potentially hazardous activities that require attention and quickness of psychomotor reactions.

Overdose

Symptoms: nausea, vomiting, confusion, mental stimulation, and in severe cases - loss of consciousness, seizures.

Treatment: gastric lavage, activated charcoal. There should be medical supervision of the patient, adequate fluid intake in the patient's body, if necessary, carry symptomatically. Hemodialysis is not an effective method for removal quinolone derivatives of the body.

Drug Interactions

Absorption of pefloxacin slowing at the same time.The with antacids containing aluminum hydroxide and magnesium hydroxide (the interval between doses must be at least 2 h). Simultaneous reception Abaktala with cimetidine and ranitidine led to an increase in T1 / 2 pefloxacin.

Pefloxacin reduces the metabolism of theophylline and NSAIDs in the liver, which leads to an increase in their concentration in blood plasma and CNS. With simultaneous application Abaktala and indirect anticoagulants may be increased by the latter. When the joint application of fluoroquinolones and cyclosporine may increase the concentration of cyclosporine and serum creatinine in the blood. The combination of pefloxacin with tetracyclines and chloramphenicol have antagonistic action.

Pharmaceutical interactions

Pefloxacin not be mixed with solutions containing chloride ions, to avoid precipitation.

Terms and Conditions of storage

The drug should be stored in a dry place protected from light, away from children at or above 25 ° C. Shelf life - 3 years.