Instructions for Ofloxacin
Pharmacodynamics Ofloxacin:
The bactericidal effect of ofloxacin is associated with inhibition of DNA gyrase, which leads to impaired bacterial DNA replication and the death of microbial cells. Ofloxacin has a wide spectrum of antimicrobial activity, including microorganisms resistant to other antibiotics, including strains that produce beta-lactamases.
Active (MPC? 0.5 mg / l) against gram-positive microorganisms: Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus spp. (Coagulase-negative); Gram-negative aerobic microorganisms:
Aeromonas hydrophila, Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, producing and not producing beta-lactamases of strains of Haemophilus infl uenzae, Haemophylus parainfluenzae, Haemiergella moriella Mella mella mella moriella Moriophilus morinophilus parainfl uenzae, Haemielli morlius paraffinum Beta-lactamase producing strains of Neisseria gonorrhoeae, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris,
Plesiomonas spp., Salmonella enterica, Shigella spp., Serratia marcescens, Yersinia enterocolitica; other microorganisms: Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma hominis, Legionella pneumophila, Mycoplasma pneumoniae, Ureaplasma urealyticum. Different sensitivity to the drug are: Acinetobacter spp., Gardnerella vaginalis, Pseudomonas aeruginosa, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, Streptococcus pneumonia (penicillin-sensitive, penicillocin-resistant, penicillocin-resistant groups of viridians, Streptococcus bovis, Streptococcus agalactae, Klebsiella pneumoniae, Mycobacterium leprae, Mycobacterium tuberculosis. Ofloxacin resistant: Staphylococcus aureus (methicillin-resistant strains), Nocardia asteroides, Enterococcus spp., Treponema pallidum, Listeria monocytogenes, most anaerobes, including Peptostreptococcus spp., Eubacterium spplo. ,Pppp.
Pharmacokinetics Ofloxacin:
After oral administration, it is rapidly and completely absorbed from the digestive tract. Eating slightly affects the degree of absorption, but can slow its speed. Cmax in blood plasma is reached after 2 hours.
Protein binding is 25%. Ofloxacin is widely distributed in tissues and body fluids (organs of the urinary system, genitals, prostate gland, lungs, ENT organs, gall bladder, bones, skin). It is excreted unchanged in the urine (about 80% in 24 hours). The concentration of ofloxacin in the urine was significantly higher than MPC90 for most microorganisms after taking the last dose (300 mg 2 for 14 days). A small part of the active substance (about 4%) is excreted in the feces. T1 / 2 is 6 hours. In elderly patients with CC on average 50 ml / min, an increase in T1 / 2 to 13.3 hours is possible. Side effects
From the digestive system: nausea, vomiting, diarrhea, abdominal pain and cramps, loss of appetite, dry mouth, flatulence, gastrointestinal tract dysfunction, constipation;
rarely - liver dysfunction, liver necrosis, jaundice, hepatitis, intestinal perforation, pseudomembranous colitis, gastrointestinal bleeding, disturbances in the oral mucosa, heartburn, increased activity of liver enzymes, including GGT and LDH, an increase in serum bilirubin level.
From the side of the central nervous system and peripheral nervous system: insomnia, dizziness, fatigue, drowsiness, nervousness;
rarely - convulsions, anxiety, cognitive changes, depression, pathological dreams, euphoria, hallucinations, paresthesias, syncope, tremors, confusion, nystagmus, suicidal thoughts or attempts, disorientation, psychotic reactions, paranoia, phobia, agitation, aggressiveness, emotional lability peripheral neuropathy, ataxia, impaired coordination, exacerbation of extrapyramidal disorders, impaired speech.
Allergic reactions: skin rash, itching; rarely - angioedema, urticaria, vasculitis, allergic pneumonitis, anaphylactic shock, erythema multiforme, Stevens-Johnson syndrome, erythema nodosum, exfoliative dermatitis, toxic epidermal necrolysis, conjunctivitis.
From the reproductive system: itching in the external genitalia of women, vaginitis, vaginal discharge; rarely - burning, irritation, pain and rash in the genital area of women, dysmenorrhea, menorrhagia, metrorrhagia, Prescription specifics
Indications Ofloxacin:
Infectious and inflammatory diseases caused by microorganisms sensitive to ofloxacin: lower respiratory tract (bronchitis, pneumonia); ENT organs (sinusitis, pharyngitis, otitis media, laryngitis, tracheitis); skin and soft tissues; bones (osteitis, osteomyelitis) and joints; infections of the abdominal cavity and biliary tract; kidney and lower urinary tract; genitals and pelvic organs (pelvioperitonitis, endometritis, salpingitis, oophoritis, tubo-ovarian abscesses, prostatitis); gonorrhea; infection prevention in patients with impaired immune status (including neutropenia).
Contraindications Ofloxacin:
Hypersensitivity to ofloxacin, the components of the drug and other fluoroquinolones; epilepsy (including a history), a decrease in the seizure threshold (including after a head injury, stroke, or inflammatory processes in the central nervous system); chronic renal failure (with creatinine clearance (CC) less than 50 ml / min), children under 18 years of age, pregnancy, lactation, tendon damage with previous treatment with fluoroquinolones.
Drug Interactions Ofloxacin:
With simultaneous use with antacids containing calcium, magnesium or aluminum, with sucralfate, with preparations containing divalent and trivalent cations, such as iron, or with multivitamins containing zinc, a violation of the absorption of quinolones is possible, leading to a decrease in their concentration in the body. These drugs should not be used within 2 hours before or within 2 hours after taking ofloxacin. With the simultaneous use of ofloxacin and NSAIDs, the risk of developing a stimulating effect on the central nervous system and seizures increases. With simultaneous use with theophylline, it is possible to increase its concentration in blood plasma (including in equilibrium), increase the half-life. This increases the risk of adverse reactions associated with theophylline. With the simultaneous use of ofloxacin with beta-lactam antibiotics, aminoglycosides and metronidazole, an additive interaction was noted.
Dosage Ofloxacin:
Inside. Tablets are taken whole, washed down with water, before or during meals. Doses are selected individually depending on the location and severity of the infection, as well as the sensitivity of microorganisms and the general condition of the patient and liver and kidney function. In patients with normal renal function, the drug is prescribed at a dose of 400-800 mg / day, the frequency of administration - 2 times a day. A dose of 400 mg per day is prescribed in one dose, preferably in the morning.
With gonorrhea - 400 mg once. In patients with impaired renal function (with creatinine clearance (CC) less than 50 ml / min), a dose of 400 mg is not recommended. If necessary, use another dosage form in the form of tablets of 200 mg. In case of liver failure, it is not recommended to exceed the dose ofloxacin 400 mg / day.
The duration of treatment depends on the location and severity of the disease; treatment should be continued for a minimum of 48-72 hours after the disappearance of the symptoms of the disease and normalization of body temperature.
In the treatment of uncomplicated and complicated infections of the lower urinary tract, the course of treatment is 7 and 10 days, respectively; with prostatitis up to 6 weeks; with pelvic infections -10-14 days; with infections of the respiratory system and skin - 10 days.
