Pefloxacin
Pefloxacin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Pefloxacin
ATX code: J01MA03
Active ingredient: Pefloxacin (Pefloxacin)
Manufacturer: JSC "KRASFARMA" (Russia)
Description and photo update: 2019-07-08
Pefloxacin is an antimicrobial drug with a broad spectrum of bactericidal action, a group of fluoroquinolones.
Release form and composition
Dosage forms of the drug:
- Film-coated tablets (10 pcs. In a blister, 1 blister in a cardboard box);
- Solution for infusion (100 ml in bottles, 1 bottle in a cardboard box, for hospitals - in a cardboard box 48 bottles).
Active ingredient content:
- 1 tablet: pefloxacin, in the form of methanesulfonate - 400 mg;
- 1 ml of solution: pefloxacin, in the form of mesylate dihydrate (in terms of pefloxacin) - 4 mg.
Pharmacological properties
Pharmacodynamics
Pefloxacin is a broad spectrum antimicrobial agent. Refers to the group of fluoroquinolones. The drug acts bactericidal, blocking the enzyme DNA gyrase, disrupting the replication of the A-subunit of DNA and RNA, as well as the synthesis of bacterial proteins.
Pefloxacin is active against gram-negative and gram-positive bacteria. Acts on cells that are in the stage of division and rest (in gram-negative bacteria) and on cells in the process of mitosis (in gram-positive bacteria). Resistant to β-lactamases.
Pefloxacin acts on the following microorganisms:
- aerobic gram-negative bacteria: Enterobacter spp., Morganella morganii, Vibrio parahaemolyticus, Vibrio cholerae, Pseudomonas aeruginosa, Pasteurella multocida, Serratia spp., Citrobacter spp., Shigella meori spp., Neisseria gonorrilseria Moraxella catarrhalis, Haemophilus spp., Salmonella spp., Klebsiella spp., Yersinia enterocolitica, Campylobacter spp., Indole-negative and indole-positive Proteus spp.;
- aerobic gram-positive bacteria: Streptococcus spp. (including Streptococcus agalactiae and Streptococcus pyogenes), Listeria monocytogenes, Staphylococcus spp., Corynebacterium diphtheria;
- intracellular bacteria: Brucella spp., Mycoplasma spp., Legionella spp. (including Legionella pneumophila), Chlamydia spp.
Moderate sensitivity to the drug is possessed by: Acinetobacter spp., Pseudomonas spp., Pneumococcus spp., Chlamydia trachomatis and Clostridium perfringens.
Pefloxacin does not act on anaerobic gram-negative bacteria: Mycobacterium tuberculosis, Treponema spp. and Bacteroides spp. (the exception is B.fragilis).
Pharmacokinetics
After oral administration, the drug is rapidly absorbed from the gastrointestinal tract. After oral administration of a single dose of 400 mg, about 90% of the dose taken is absorbed after 20 minutes, and the maximum concentration is reached after 1.5–2 hours and is 4 μg / ml. After repeated administration of the drug, the maximum plasma concentration is 10 μg / ml, the concentration of pefloxacin in the bronchial membrane is 5 μg / ml, and the ratio between the concentration in the blood and mucous membrane is 100%.
After intravenous administration of the drug, the maximum concentration is reached within 1 hour.
Pefloxacin is 25–30% bound to plasma proteins. The volume of distribution is 1.5-1.8 l / kg. The drug penetrates well into all tissues and body fluids (lungs, heart, prostate gland, bone tissue, salivary glands, tonsils, skin, muscles, bronchial secretions, peritoneal fluid, urine, cerebrospinal fluid, bile, phlegm), and the concentration in these tissues and liquids above the concentration of pefloxacin in the blood.
Metabolism occurs in the liver in the following ways: oxidation to N-oxide, methylation to dimethylpefloxacin (pharmacologically active) and conjugation with glucuronic acid, followed by the formation of pefloxacin-glucuronide.
The half-life after taking the drug inside is from 8 to 10 hours, with repeated administration - from 12 to 13 hours. After intravenous administration of Pefloxacin in a single dose, the half-life is from 7 to 13 hours, after repeated administration - from 14 to 15 hours.
It is excreted in feces and urine (about 60%) unchanged, some in the form of metabolites. After 1–2 hours after administration, it is found unchanged in urine at a concentration of 25 μg / ml, and after 12–24 hours, the concentration of pefloxacin in urine in unchanged form is already 15 μg / ml. The drug and its metabolites are found in the urine for up to 84 hours after the last dose. With hemodialysis, the excretion rate of pefloxacin is 23%.
Indications for use
The use of the drug is indicated in the treatment of infections and inflammatory processes of the following localization caused by microorganisms sensitive to pefloxacin:
- Hepatobiliary system (liver, gallbladder and biliary tract);
- Bones and joints;
- ENT organs (ear, throat, nose) and lower respiratory tract;
- Urinary system (kidneys and urinary tract);
- Abdominal cavity and pelvic organs;
- Digestive system (including infections of the mouth, jaws, teeth);
- Skin, soft tissues, mucous membranes;
- Gynecological infections, sexually transmitted diseases (chlamydia, gonorrhea), prostatitis;
- Hospital-acquired and surgical infections;
- Severe systemic infections (bacteremia, septicemia, endocarditis, osteomyelitis, meningoencephalitis).
In addition, the solution is prescribed for the prevention and treatment of infectious complications after surgery.
Contraindications
- Deficiency of glucose-6-phosphate dehydrogenase;
- The period of pregnancy and breastfeeding;
- Age up to 15 years;
- Hypersensitivity to pefloxacin and other fluoroquinolones.
In addition, the appointment of tablets to patients with hepatic insufficiency is contraindicated.
The solution is prescribed with caution to patients with severe hepatic dysfunction, cerebrovascular accident, cerebral atherosclerosis, convulsive syndrome of unknown origin, epilepsy.
Instructions for the use of Pefloxacin: method and dosage
Film-coated tablets
The tablets are taken orally, swallowed whole, with meals.
Recommended dosage: 400 mg 2 times a day (morning and evening).
In the absence of the desired therapeutic effect, an increase in the daily dose to 1600 mg is shown.
Solution for infusion
The solution is intended for intravenous drip administration.
The doctor prescribes the dose on the basis of clinical indications individually, taking into account the severity of the course and localization of the infection, as well as the sensitivity of the microorganism to the drug.
Recommended dosage regimen:
- Severe forms of infectious diseases: the initial dose is 800 mg, then 400 mg 2 times a day every 12 hours. Patients with impaired renal function are prescribed 400 mg, with a mild form of pathology - 1 time in 24 hours, with a severe form - with an interval between procedures of 36 hours;
- Liver infections: at the rate of 8 mg per 1 kg of patient's body weight with an infusion duration of 1 hour. Frequency of procedures: for jaundice - 1 time per 24 hours, ascites - 1 time per 36 hours, for patients with jaundice and ascites - 1 time per 48 hours.
The daily dose of Pefloxacin should not exceed 1200 mg.
Side effects
- Digestive system: nausea, abdominal pain;
- Musculoskeletal system: arthralgia, myalgia;
- Nervous system: insomnia, headache;
- Hematopoietic system: thrombocytopenia (with a daily dose of 1600 mg);
- Dermatological reactions: photosensitivity.
In addition, the use of Pefloxacin can cause the following adverse reactions:
- Film-coated tablets: dizziness, dyspeptic symptoms;
- Solution for infusion: vomiting, diarrhea, development of allergic reactions in the form of urticaria, pruritus.
Overdose
To date, no cases of drug overdose have been registered.
In case of accidental intake of doses that significantly exceed the therapeutic ones, symptomatic treatment is prescribed, and if necessary, peritoneal dialysis and hemodialysis are performed. There is no specific antidote to pefloxacin.
special instructions
During the period of application of Pefloxacin, the patient should avoid exposure to ultraviolet radiation.
To prevent the development of bacterial resistance to beta-lactam antibiotics and rifampicin, the solution is prescribed as part of a combination therapy.
Application during pregnancy and lactation
The drug is prohibited for use during pregnancy and lactation.
Pediatric use
According to the instructions, Pefloxacin is contraindicated in children and adolescents under 18 years of age.
With impaired renal function
In case of impaired renal function (if creatinine clearance is less than 20 ml / min), it is necessary to reduce the dose of the drug: when used twice a day, a single dose should be 50% of the average dose, when used once a day, a full single dose is prescribed.
For violations of liver function
In case of violations of the liver function, it is necessary to adjust the dosage regimen of the drug: for mild disorders, 400 mg of Pefloxacin is prescribed per day, for violations of moderate severity - 400 mg every 36 hours, and in case of severe violations, the interval between doses of the drug should be increased to 48 hours. The duration of therapy in patients with impaired liver function should not exceed 30 days.
Drug interactions
With simultaneous use with pefloxacin:
- Aminoglycosides - promote synergism towards Pseudomonas aeruginosa;
- Indirect anticoagulants - can enhance their effect;
- Cimetidine - leads to an increase in T 1 / 2 pefloxacin and lower total clearance;
- Theophylline - slows down its metabolism in the liver and increases the concentration in blood plasma;
- Antacids containing magnesium hydroxide and aluminum hydroxide - slow down the absorption of pefloxacin.
The solution for infusion must not be mixed with preparations containing chlorine ions.
Analogs
Perfloxacin analogues are: Unicpef, Pefloxabol, Abaktal, Pefloxacin-AKOS.
Terms and conditions of storage
Keep out of the reach of children. Store in a dry, cool place protected from light. The storage temperature of the solution is 10-25 ° C (do not freeze).
Shelf life: tablets - 3 years; solution - 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Pefloxacin
The drug is well tolerated by patients and effective against pathogens of a number of infectious diseases. Some reviews of Pefloxacin describe cases of photosensitivity during the period of antimicrobial treatment, as well as the appearance of bitterness in the mouth and mild nausea.
Price for Pefloxacin in pharmacies
Currently, the drug is available only in the form of an infusion solution. The price of Pefloxacin in tablets is unknown, since this form of release has expired the state registration period. If you need to use pefloxacin orally, you can purchase a similar drug Pefloxacin-AKOS for about 75 rubles (film-coated tablets, 400 mg, 10 pcs. Per package). The cost of Pefloxacin-AKOS solution for injections is 125 rubles on average.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
