Da Fu Ming

Da Fu Ming

Pefloxacin

Infectious and inflammatory diseases caused by microorganisms sensitive to pefloxacin: infections of the kidneys and urinary tract, gastrointestinal tract (in t.tsch. salmonellosis, typhoid fever), mouth, teeth, jaws, infections of the gallbladder and biliary tract (cholecystitis, cholangitis, empyema of the gallbladder), infections of the pelvic organs (in the t.tsch. adnexitis and prostatitis), bones, joints, skin and soft tissues, infections of the lower respiratory tract and ENT organs (middle ear, paranasal sinuses, pharynx, larynx), eye infections, intraabdominal abscesses, peritonitis, sepsis, septicemia, endocarditis, meningoencephalitis, osteomyelitis, gonorrhea, chlamydia, epididymitis, soft chancre, surgical and nosocomial infections, prevention of surgical infection

Inside, on an empty stomach. Tablets are swallowed without chewing and washed down with plenty of water. The doses are selected individually, depending on the location and severity of the infection, the sensitivity of microorganisms. For uncomplicated infections-400 mg 2 times a day, the average daily dose is 800 mg in 2 doses.

In/in the drip (for infectious endocarditis, sepsis, osteomyelitis, and severe infections), the 1st dose is 800 mg, then 400 mg every 12 hours. The infusion is carried out for 1 h, the contents of the ampoule are dissolved in 250 ml of 5% glucose solution. The course of treatment is 1-2 weeks (no more).

If abnormal liver function is necessary correction mode: for minor violations, the drug is prescribed in a dose of 400 mg/day, in more severe cases, every 36 h, severe liver disease, the interval between injections was increased to 2 days. The course of treatment — no more than 30 days.

In patients with impaired renal function (with creatinine Cl below 20 ml / min), a single dose is 50% of the average (with a multiplicity of administration 2 times a day) or a full single dose 1 time a day. For the elderly, the dose of the drug is reduced by 1/3.

Hypersensitivity, epilepsy, hemolytic anemia, glucose−6-phosphate dehydrogenase deficiency, pregnancy, lactation, childhood (up to 18 years).

With caution-atherosclerosis of the cerebral vessels, violation of cerebral circulation, organic lesions of the central nervous system, convulsive syndrome of unknown etiology.

From the nervous system and sensory organs: depression, headache, dizziness, increased fatigue, insomnia, increased convulsive readiness, anxiety, agitation, tremor, rarely-convulsions.

From the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain, anorexia, flatulence, pseudomembranous colitis, transient increase in hepatic transaminases, cholestatic jaundice, hepatitis, liver necrosis.

From the genitourinary system: crystalluria, rarely-glomerulonephritis, dysuria.

Allergic reactions: skin rash, itching, urticaria, skin hyperemia, photosensitization, rarely-Quincke's edema, bronchospasm, arthralgia.

From the hematopoietic system: leukopenia, neutropenia. thrombocytopenia (at doses of 1600 mg / day), agranulocytosis, eosinophilia.

Other: tachycardia, myalgia, tendinitis, tendon rupture, candidiasis.

Treatment: symptomatic therapy, if necessary — hemodialysis and peritoneal dialysis. The specific antidote is unknown.

It has a wide spectrum of action. Active against Gram-negative bacteria Escherichia coli, Klebsiella spp., indole-positive and indole-negative Proteus spp., in t.tsch. Proteus mirabilis, Enterobacter spp., Morganella morganii, Yersinia enterocolitica, Vibrio cholerae, Vibrio parahaemolyticus, Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Pseudomonas aeruginosa, Moraxella catarrhalis, Pasteurella multocida, Campylobacter spp., Serratia spp., Citrobacter spp., Salmonella spp., Shigella spp., Haemophilus spp. Aerobic Gram-positive bacteria — Staphylococcus spp. (in t.tsch. producing and not producing penicillinase and methicillin-resistant), Streptococcus spp., in t.tsch. Streptococcus pyogenes, Streptococcus agalactiae, Corynebacterium diphtheriae, Listeria monocytogenes, intracellular bacteria: Legionella pneumophila, Brucella spp., Chlamydia spp., as well as against bacteria that produce beta-lactamases. Suppresses the vital activity of Mycoplasma spp., Helicobacter. Moderately sensitive — Pneumococcus, Acinetobacter spp., Pseudomonas spp. Resistant — gram-negative anaerobic bacteria, Treponema spp., Mycobacterium tuberculosis. With respect to gram-negative strains, it effectively acts both on dividing cells and cells at rest, in the case of Gram-positive strains-only on cells that are in the process of mitotic division

After oral administration at a dose of 400 mg, 90% is absorbed after 20 minutes. C_max it is 4 mcg / ml and is reached after 90-120 minutes, with intravenous administration - within 60 minutes. The therapeutic concentration is maintained for 12-15 hours. After repeated administration With_max in the blood-10 mcg / ml, the concentration in the bronchial mucosa-5 mcg/ml, binding to plasma proteins-25-30%.

It penetrates well into the tissues and body fluids, in t.tsch. into the bronchial secretions, lungs, prostate, cerebrospinal fluid, and bone tissue. The volume of distribution when taken orally — 1.5-1.8 l / kg, the concentration in the cerebrospinal fluid after 3-fold administration of 400 mg-4.5 mcg/ml, with an increase in the dose to 800 mg-9.8 mcg/ml, the ratio between the concentration in plasma and liquid-89%. Concentration in other organs and tissues 12 hours after the last dose: thyroid - 11.4 mcg/g, salivary glands-2.2 mcg/g, skin-7.6 mcg/ g, nasopharyngeal mucosa-6 mcg/ g, tonsils-9 mcg/ g, muscles-5.6 mcg/g. It is metabolized in the liver by methylation to dimethylpefloxacin (has significant antibacterial activity), is oxidized to N-oxide and conjugates with glucuronic acid to form pefloxacin-glucuronide

With the I / V introduction of T_1/2 after one administered dose is 7.2-13 hours, after repeated administration-14-15 hours, when taken orally-8-10 hours, with repeated administration-12-13 hours. In unchanged form and in the form of metabolites, it is excreted by the kidneys (50-60%) and is found in the feces (30%). The content of the unchanged drug in the urine after 1-2 hours after administration is 25 mcg/ml, after 12-24 hours-15 mcg/ml. Unchanged pefloxacin and its metabolites are detected in the urine within 84 hours after the last administration. Poorly amenable to dialysis (extraction coefficient-23%).

• Quinolones/fluoroquinolones

Pefloxacin reduces the metabolism of theophylline in the liver, which leads to an increase in the concentration of theophylline in the plasma and the central nervous system (the dose of theophylline should be reduced).

Cimetidine and other microsomal oxidation inhibitors increase T_1/2, reduce the total clearance, but do not affect the volume of distribution and renal clearance.

Enveloping agents slow down the absorption.

Simultaneous use of beta-lactam antibiotics can prevent the development of resistance during the treatment of staphylococcal infection. Aminoglycosides, piperacillin, azlocillin, ceftazidime enhance the antibacterial effect (including infection caused by Pseudomonas aeruginosa).

Drugs that block tubular secretion slow down the excretion of pefloxacin.