Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antimicrobial agent of the group of fluoroquinolones of wide spectrum of action. The bactericidal effect of ofloxacin is associated with the blockade of the DNA-gyrase enzyme in bacterial cells.
Highly active against most Gram-negative bacteria: Escherichia coli, Salmonella spp., Shigella spp., Proteus spp., Morganella morganii, Klebsiella spp. (including Klebsiella pneumoniae), Enterobacter spp., Serratia spp., Citrobacter spp., Yersinia spp., Providencia spp., Haemophilus influenzae, Neisseria gonorrhoeae, Neisseria meningitidis, Mycoplasma spp., Legionella pneumophila, Acinetobacter spp., as well as Chlamydia spp.
It is active against some Gram-positive microorganisms (including Staphylococcus spp., Streptococcus spp., Especially beta-hemolytic streptococci).
To ofloxacin moderately sensitive Enterococcus faecalis, Streptococcus pneumoniae, Pseudomonas spp.
Ofloxacin is not sensitive to anaerobic bacteria (except Bacteroides ureolyticus).
Resistant to the action of? -lactamases.
PHARMACOKINETICS
After ingestion quickly and completely absorbed from the digestive tract. Eating slightly affects the degree of absorption, but it can slow down its speed. C max in blood plasma is achieved after 2 hours.
Binding to proteins - 25%. Ofloxacin widely distributed in tissues and body fluids (organs of the urinary system, genitals, prostate, lungs, ENT organs, gall bladder, bones, skin).
It is excreted unchanged in urine (about 80% in 24 hours). The concentration of ofloxacin in the urine was significantly higher than the MIC of 90 for most microorganisms after the last dose (300 mg 2 times / day for 14 days). A small part of the active substance (about 4%) is excreted with feces. T 1/2 is 6 hours. In elderly patients with SC, an average of 50 ml / min, an increase of T 1/2 to 13.3 hours is possible.
INDICATIONS
Infectious and inflammatory diseases caused by microorganisms sensitive to ofloxacin, including: diseases of the lower respiratory tract, ear, throat, nose, skin, soft tissues, bones, joints, infectious and inflammatory diseases of the abdominal cavity (with the exception of bacterial enteritis ) and small pelvis, infection of the kidneys and urinary tract, prostatitis, gonorrhea.
DOSING MODE
Individual. The daily dose is 200-800 mg, the frequency of application 2 times / day. For patients with impaired renal function (KK 20-50 ml / min), the first dose is 200 mg, then 100 mg every 24 hours. At a CC less than 20 ml / min, the first dose is 200 mg, then 100 mg every 48 hours.
SIDE EFFECT
On the part of the digestive system: nausea, vomiting, diarrhea, pain and cramps in the abdomen, worsening appetite, dry mouth, flatulence, gastrointestinal disturbances, constipation; rarely - violations of the liver, liver necrosis, jaundice, hepatitis, intestinal perforation, pseudomembranous colitis, bleeding from the gastrointestinal tract, mucosal disorders of the oral cavity, heartburn, increased activity of hepatic enzymes, including GGT and LDH, increased serum bilirubin levels.
From the nervous system: insomnia, dizziness, fatigue, drowsiness, nervousness; rarely cramps, anxiety, cognitive changes, depression, pathological dreams, euphoria, hallucinations, paresthesia, syncope, tremor, confusion, nystagmus, suicidal thoughts or attempts, disorientation, psychotic reactions, paranoia, phobia, agitation, aggressiveness, emotional lability, peripheral neuropathy, ataxia, impaired coordination, exacerbation of extrapyramidal disorders, speech impairment.
Allergic reactions: skin rash, itching; rarely - angioedema, hives, vasculitis, allergic pneumonitis, anaphylactic shock, erythema multiforme, Stevens-Johnson syndrome, erythema nodosum, exfoliative dermatitis, toxic epidermal necrolysis, conjunctivitis.
On the part of the reproductive system: itching in the region of the external genitalia in women, vaginitis, discharge from the vagina; rarely - burning, irritation, pain and rash in the genital area of ​​women, dysmenorrhea, menorrhagia, metrorrhagia, vaginal candidiasis.
From the cardiovascular system: rarely - cardiac arrest, edema, arterial hypertension, arterial hypotension, palpitation, vasodilation, cerebral thrombosis, pulmonary edema, tachycardia.
On the part of the urinary system: rarely - dysuria, increased urination, urinary retention, anuria, polyuria formation of kidney stones, kidney failure, nephritis, hematuria, albuminuria, candiduria.
From the musculoskeletal system: rarely - arthralgia, myalgia, tendonitis, muscle weakness, exacerbation of myasthenia gravis.
From the side of metabolism: rarely - thirst, weight loss, hyper- or hypoglycemia (especially in patients with diabetes, receiving insulin or oral hypoglycemic agents), acidosis, increase in serum TG, cholesterol, potassium.
On the part of the respiratory system: rarely - cough, discharge from the nose, stop breathing, dyspnea, bronchospasm, stridor.
From the senses: rarely - hearing impairment, tinnitus, diplopia, nystagmus, impaired clarity of visual perception, violation of taste, smell, photophobia.
Dermatological reactions: rarely - photosensitivity, hyperpigmentation, vesicle-bullous eruptions.
From the hemopoietic system: rarely - anemia, bleeding, pancytopenia, agranulocytosis, leukopenia, reversible suppression of bone marrow hematopoiesis, thrombocytopenia, thrombocytopenic purpura, petechiae, ecchymosis, increased prothrombin time.
Other: pain in the chest, pharyngitis, fever, pain in the body; rarely - asthenia, chills, general malaise, epistaxis, increased sweating.
CONTRAINDICATIONS
Pregnancy, lactation, children and adolescents under 18, hypersensitivity to ofloxacin or other quinolone derivatives.
PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation.
In experimental studies, no negative effect on fertility in rats was detected.
APPLICATION FOR FUNCTIONS OF THE LIVER
Use with caution in patients with impaired renal function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Use with caution in patients with impaired hepatic function.
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 18 years.
SPECIAL INSTRUCTIONS
Use with caution in patients with impaired renal and hepatic function.
During the period of treatment, it is required to monitor blood glucose levels. With prolonged therapy, it is necessary to periodically monitor the functions of the kidneys, liver, and the picture of peripheral blood.
When using ofloxacin should provide sufficient hydration of the body, the patient should not be exposed to ultraviolet radiation.
In experimental studies, a mutagenic potential was not detected. Long-term studies to determine the carcinogenicity of ofloxacin were not performed.
In studies on young animals of several species ofloxacin caused arthropathy and osteochondrosis.
Safety and efficacy in children and adolescents under the age of 18 years have not been established.
Impact on the ability to drive vehicles and manage mechanisms
Use with caution in patients whose activities are associated with the need for high concentration of attention and speed of psychomotor reactions.
DRUG INTERACTION
When used simultaneously with antacids containing calcium, magnesium or aluminum, with sucralfate, with preparations containing bivalent and trivalent cations such as iron, or with multivitamins containing zinc, absorption of quinolones may be impaired, 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 is increased.
With simultaneous application with theophylline it is possible to increase its concentration in the blood plasma (including in the equilibrium state), an increase in T1/2 . This increases the risk of adverse reactions associated with the action of theophylline.
With the simultaneous use of ofloxacin with beta-lactam antibiotics, aminoglycosides and metronidazole, additive interaction is noted.
