Abaktal, 400 mg 10 pcs

Antimicrobial agent – fluoroquinolone.

ATX code: J01MA03

Pharmacodynamics

Pefloxacin is a synthetic antimicrobial agent of the group of fluoroquinolones. It acts bactericidally by inhibiting the enzyme DNA-Giase and bacterial DNA replication; it also disrupts ribonucleic acid A-subunit replication and protein synthesis by the bacterial cell. With respect to Gram-negative bacteria, it acts on cells in both resting and dividing phases; with respect to Gram-positive bacteria, it acts only on cells in the process of mitotic division.

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 pneumophilla, Moraxella catarrhalis, Morganella morganii, Pasteurella multocida, Proteus mirabilis, indole positive Proteus, Providencia stuartii, Salmonella spp, Serratia spp., Shigella spp., Vibrio cholerae.

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

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: within 20 minutes after oral administration 90% of pefloxacin is absorbed in the gastrointestinal tract (GIT). After a single oral intake of 200 or 400 mg of pefloxacin per day by healthy volunteers within 1-1.5 hours the maximum plasma concentrations (Cmax) were 2.5 and 4.3 mcg/ml, respectively.

When repeated oral administration of 400 mg of pefloxacin twice daily, maximum and residual concentrations of pefloxacin are reached after 48 hours: maximum serum concentrations range from 7.9 to 10 mcg/ml, residual serum concentrations, just before the next dose, are 3.8 mcg/ml.

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

Distribution

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

Metabolism

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

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

Excretion

In patients with normal renal and hepatic function 59% of the dose taken is excreted by the kidneys unchanged and as two major metabolites. In general, 60% of the dose is excreted by the kidneys and 40% by the intestine. 20% of the administered dose was excreted as N-dimethyl-pefloxacin and 16.2% as pefloxacin-N-oxide.

The drug is reabsorbed in renal tubules. Renal clearance of pefloxacin is low, varying from 0.11 to 0.21 ml per second depending on the dose. The half-life (T½) of the drug after single administration is 10.5 hours, and increases to 12.3 hours with multiple oral administration. However, pefloxacin and its metabolites are detected in the urine within 48 hours after usage.

Also 20-30% of pefloxacin is excreted with the bile as pefloxacin-glucuronide and N-oxide derivatives. Within 12 hours after oral administration of 400 mg of pefloxacin its concentration in bile reached 83 µg/ml.

Pharmacokinetics in special patient groups

In renal disorders plasma concentration of pefloxacin and T½ is almost unchanged due to the fact that hepatic clearance of the drug is the main excretion mechanism.

In impaired liver function, plasma clearance of pefloxacin is significantly reduced and T½ is correspondingly increased.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Contraindications

Side effects

Overdose

Pregnancy use