Peflostan (Solution) Instructions for Use

Marketing Authorization Holder

Grotex, LLC (Russia)

ATC Code

J01MA03 (Pefloxacin)

Active Substance

Pefloxacin (Rec.INN registered by WHO)

Dosage Form

Peflostan

Infusion solution 4 mg/ml: 100 ml bottle.

Dosage Form, Packaging, and Composition

Infusion solution in the form of a transparent, colorless or slightly colored solution with a brownish-yellow, or yellowish, or brownish, or greenish-yellow, or reddish tint.

Excipients : dextrose monohydrate (calculated as anhydrous substance) – 50 mg, disodium edetate dihydrate (Trilon B) – 0.05 mg, water for injections – up to 1 ml.

100 ml – bottles – cardboard packs.
100 ml – bottles (36) – cardboard boxes (for hospitals).

Clinical-Pharmacological Group

Antibacterial drug of the fluoroquinolone group

Pharmacotherapeutic Group

Systemic antibacterial agents; quinolone derivatives; fluoroquinolones

Pharmacological Action

Antimicrobial agent of the fluoroquinolone group with a broad spectrum of action. It has a bactericidal effect by inhibiting bacterial DNA replication at the level of DNA gyrase, and also affects RNA and bacterial protein synthesis.

It acts on gram-negative bacteria, both in the division stage (growth phase) and in the resting stage. Against gram-positive strains, it acts only on cells in the process of mitotic division. It exhibits activity against intracellular pathogens.

It is active against gram-positive bacteria: Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus; gram-negative bacteria: Escherichia coli, Klebsiella spp., Enterobacter spp., Serratia spp., Proteus mirabilis, Proteus vulgaris, Citrobacter spp., Salmonella spp., Shigella spp., Haemophilus ducreyi, Haemophilus influenzae, Neisseria gonorrhoeae, Neisseria meningitidis, Aeromonas spp., Campylobacter spp., Legionella spp., Moraxella spp., Morganella spp., Pasteurella spp., Providencia spp., Pseudomonas aeruginosa, Yersinia spp., Ureaplasma urealyticum.

Moderately sensitive to pefloxacin: Acinetobacter spp., Gardnerella vaginalis, Mycoplasma spp., Chlamydia spp; weakly sensitive: Streptococcus spp. (including Streptococcus pneumoniae), Enterococcus spp.

Pharmacokinetics

After a single infusion at a dose of 400 mg, the C_max of pefloxacin is 4 µg/ml and is maintained for 12-15 hours. After IV infusion, the pharmacokinetic parameters are the same as after oral administration. The AUC for both methods of administration is the same, which indicates complete absorption of pefloxacin.

After oral administration, Pefloxacin is rapidly absorbed from the gastrointestinal tract. After a single oral dose of 400 mg of pefloxacin, 90% of the dose is absorbed within 20 minutes, with C_max reached in 1-2 hours and is 4 µg/ml after 1.5 hours. Bioavailability is about 100%.

Plasma protein binding is 25-30%. V_d – 1.5-1.8 l/kg. Pefloxacin rapidly penetrates into tissues, organs and body fluids (aortic valves, mitral valve, heart muscle, bones, abdominal cavity, peritoneal fluid, gallbladder, prostate gland, saliva, sputum, pancreatic tissues /including necrotized/). The concentration of pefloxacin in the listed fluids and tissues is higher than the concentration in blood plasma.

T_1/2 is approximately 8-10 hours, with repeated administration – 12-13 hours. It is excreted mainly in the urine (60% within 72 hours). 30% is excreted in the bile unchanged, partially in the form of metabolites: norfloxacin, Pefloxacin-N-oxide and pefloxacin glucuronide. The content of unchanged pefloxacin in urine 1-2 hours after administration is 25 µg/ml, after 12-24 hours – 15 µg/ml. Unchanged Pefloxacin and its metabolites are detected in urine for 84 hours after the last administration of the drug. The extraction coefficient of pefloxacin during hemodialysis is 23%.

Indications

Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to pefloxacin: infections of the liver and biliary tract; sepsis and bacterial endocarditis; staphylococcal meningitis and meningitis caused by gram-negative flora; infections of bones and joints; infections of the lower respiratory tract; infections of the ENT organs; infections of the urinary tract; infections of the abdominal cavity; gynecological infections; infections of the skin and soft tissues; sexually transmitted diseases.

Treatment and prevention of infectious complications after surgical interventions.

ICD codes

Dosage Regimen

It is set individually, depending on the location and severity of the infection, as well as the sensitivity of the microorganism.

When taken orally, the average dose is 800 mg/day in 2 divided doses.

For severe infections, it is administered intravenously by drip: the first dose is 800 mg, then 400 mg every 12 hours. For mild renal impairment, 400 mg is administered every 24 hours, for more severe impairment – every 36 hours.

For patients with liver disease during intravenous drip administration, a single dose is 8 mg/kg; the duration of infusion is 1 hour. The frequency of infusions is for patients with jaundice once every 24 hours; for patients with ascites – once every 36 hours; for patients with jaundice and ascites – once every 48 hours.

Maximum daily dose is 1.2 g/day.

Adverse Reactions

From the digestive system nausea, vomiting, diarrhea, abdominal pain.

From the central nervous system headache, insomnia.

From the musculoskeletal system myalgia, arthralgia.

From the hematopoietic system thrombocytopenia (when used at a dose of 1.6 g/day).

Dermatological reactions photosensitivity.

Allergic reactions skin itching, urticaria.

Contraindications

Glucose-6-phosphate dehydrogenase deficiency, pregnancy, lactation (breastfeeding), children and adolescents under 15 years of age, hypersensitivity to pefloxacin and other fluoroquinolones.

Use in Pregnancy and Lactation

Pefloxacin is contraindicated for use during pregnancy and during lactation (breastfeeding).

In experimental studies, the toxic effect of monofluoroquinolones on cartilage tissue has been established.

Use in Hepatic Impairment

Use with caution in patients with severe liver dysfunction.

Use in Renal Impairment

Use is possible according to the dosage regimen.

Pediatric Use

Contraindicated in children and adolescents under 15 years of age.

Special Precautions

Use with caution in patients with cerebral atherosclerosis, cerebrovascular accidents, epilepsy, convulsive syndrome of unknown etiology, with severe liver dysfunction.

During treatment, ultraviolet radiation should be avoided.

Combined use of pefloxacin with beta-lactam antibiotics and rifampicin is possible to prevent the development of bacterial resistance to the latter.

Drug Interactions

With simultaneous use of pefloxacin and aminoglycosides, synergism is noted against Pseudomonas aeruginosa; with indirect anticoagulants – it is possible to enhance their effect.

The absorption of pefloxacin is slowed down with simultaneous administration with antacids containing aluminum hydroxide and magnesium hydroxide.

Simultaneous administration of pefloxacin and cimetidine leads to a decrease in total clearance and an increase in T_1/2 of pefloxacin.

Pefloxacin inhibits microsomal oxidation in liver cells by affecting cytochrome P450 system enzymes. Therefore, Pefloxacin slows down the metabolism of theophylline in the liver, which leads to an increase in the concentration of theophylline in plasma.

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

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.