Ofloxacin - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate 268.8 mg, corn starch 60.0 mg, giprolose 20.0 mg, croscarmellose sodium 15.6 mg, magnesium stearate 15.6 mg; shell: fall off II white (polyvinyl alcohol 9.20 mg, titanium dioxide 5.75 mg, macrogol 4.65 mg, talc 3.4 mg) 23.0 mg.

Description:Oblong, biconvex form of the tablet, covered with a film shell of white or almost white color, on a cross-section a nucleus from white to light yellow color.

Pharmacotherapeutic group:Antimicrobial agent from the group of fluoroquinolones

ATX: & nbsp

S.01.A.E.01 Ofloxacin

J.01.M.A.01 Ofloxacin

Pharmacodynamics:

A broad-spectrum antimicrobial agent from the group of fluoroquinolones,acts on the bacterial DNA-gyrase enzyme, providing super-convoliation and, thus, the stability of bacterial DNA (the destabilization of DNA chains leads to their death). Has a bactericidal effect.

The antimicrobial spectrum includes Gram-positive aerobes: Staphylococcus aureus (methicillin-sensitive), Staphylococcus epidermidis (methicillin-sensitive). Staphylococcus saprophyticus, Streptococcus pneumoniae (penicillin-sensitive). Streptococcus pyogenes.

Rhetoric aerobes: Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter freundii, Citrobacter koseri, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae. Klebsiella oxytoca, Moraxelia catarrhalis, Morganella morganii, Klebsiella pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stucirtii, Pseudomonas aeruginosa (quickly develop resistance), Serratia marcescens.

Anaerobes: Clostridium perfringens.

Other: Chlamydia trachomatis, Chlamydia pneumoniae, Gardnerella vaginalis, Legionella pneumophila. Mycoplasma hominis. Mycoplasma pneumoniae, Ureaplasma urealyticum.

In most cases, they are insensitive: Nocardia asteroides, anaerobic bacteria (including Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile), Enterococcus spp., most Streptococcus spp., does not apply to Treponema pallidum.

Pharmacokinetics:

Absorption after oral administration is rapid and complete (95%). Bioavailability is over 96%. connection with plasma proteins - 25%. The time to reach the maximum concentration (T_C_max) when taken orally - 1-2 hours, the maximum concentration (C_max) after taking the dose of 100, 300 and 600 mg is 1, 3.4 and 6.9 mg / L, respectively, and depends on the dose, after a single dose of 200 and 400 mg, it is 2.5 and 5 μg / ml, respectively. Food can slow absorption, but does not have a significant effect on bioavailability.Apparent volume of distribution - 100 liters. Distribution: cells (leukocytes, alveolar macrophages), skin, soft tissues, bones, abdominal and pelvic organs, respiratory system, urine, saliva, bile, the secret of the prostate gland; well penetrates the hemato-en cephalic barrier, the placental barrier, is secreted with the mother's milk. Penetrates into cerebrospinal fluid with inflamed and non-inflamed meninges (14-60%).

Metabolized in the liver (about 5%) with formation NOxygen ofloxacin and dimethylfloxacin. Half-life (T_1/2) is 4.5-7 hours (regardless of dose). It is excreted by the kidneys - 75-90% (unchanged), about 4% - with bile. The extrarenal clearance is less than 20%.

After a single application in a dose of 200 mg in urine is detected within 20-24 hours. In renal / hepatic insufficiency, excretion can be slowed down. Do not cumulate. With hemodialysis, 10-30% of the drug is removed.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to ofloxacin:

- infections of the upper respiratory tract and LOP-organ (sinusitis, pharyngitis, otitis media, laryngitis except for cases of acute tonsillitis);

- infections of the lower respiratory tract (tracheitis, bronchitis, pneumonia, except for cases of pneumococcal infection);

- infections of the skin, soft tissues, bones and joints;

- infectious and inflammatory diseases of the abdominal cavity and bile ducts, kidneys (pyelonephritis);

- urinary tract infection (cystitis, urethritis, including gonococcal nature);

- infection of genital organs and small organs of gas (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis, colpitis, orchitis, epididymitis), gonorrhea, chlamydia;

- prevention of infections in patients with impaired immune status (including neutropenia).

Contraindications:

Hypersensitivity to ofloxacin, other quinolones or components of the drug, epilepsy (including history), reduction of the convulsive threshold (including after traumatic brain injury, stroke or inflammation in the central nervous system), tendon damage with previous treatment with fluoroquinolones, renal impairment (creatinine clearance less than 50 ml / min), age to 18 years, pregnancy, lactation (breastfeeding), lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Carefully:

Atherosclerosis of cerebral vessels, cerebral circulatory disorders (in the anamnesis), hepatic insufficiency, organic diseases of the central nervous system, predisposition to convulsive reactions, myasthenia gravis, hepatic porphyria, glucose-6-phosphatehydrogase deficiency, congenital lengthening interval syndrome Q-T, heart disease (heart failure, myocardial infarction, bradycardia), psychoses and other mental disorders in the anamnesis; simultaneous reception of drugs that extend the interval Q-T (antiarrhythmic IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, imidazole derivatives, some antihistamines, including astemizole, terfenadine, ebastine), for general anesthesia from the barbiturate group, drugs that lower blood pressure; in patients who are simultaneously receiving medications that reduce the threshold of convulsive brain readiness, such as fenbufen, theophylline; In patients with known risk factors for lengthening the interval Q-T: in elderly patients, in patients with uncorrected electrolyte disorders (eg hypokalemia, hypomagnesemia), in patients with diabetes mellitus receiving hypoglycemic agents for oral administration (eg, glibklamid) or insulin.

Pregnancy and lactation:

See section "Contraindications".

Dosing and Administration:

Inside. Tablets are taken whole, washed down with water, before or during meals. Doses are selected individually depending on the location, the severity of the infection, the sensitivity of microorganisms, as well as the general condition of the patient and the function of the liver and kidneys.

For the prevention of infections in patients with a marked decrease in immunity - 400 mg / day.

Adults - 400-800 mg / day, the course of treatment - 7-10 days, the frequency of application - 2 times a day. A dose of 400 mg / day can be given in one session, preferably in the morning.

With gonorrhea - 400 mg once.

In patients with impaired renal function (when creatinine clearance is less than 50 ml / min), 400 mg dose is not recommended. If necessary, use another dosage form in the form of 200 mg tablets.

The maximum daily dose for liver failure is 400 mg / day.

The duration of treatment is determined by the sensitivity of the pathogen and the clinical picture; treatment should continue for at least 3 more days after the disappearance of the symptoms of the disease and complete normalization of body temperature.

In the treatment of uncomplicated and complicated infections of the lower urinary tract treatment course of 7 and 10 days respectively, with prostatitis - up to 6 weeks, with infections of the pelvic organs - 10-14 days, with infections of the respiratory system and skin - 10 days.

Side effects:

From the digestive system: gastralgia. decline appetizenausea, vomiting, diarrhea, constipation, flatulence, abdominal pain, increased activity of "liver" transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous colitis, dryness of the oral mucosa, enterocolitis, hepatitis, anorexia.

From the nervous system: headache, dizziness, tremor, convulsions, numbness and paresthesia of the limbs, intense dreams, nightmarish dreams, psychotic reactions, anxiety, arousal, phobias, depression, confusion, hallucinations, increased intracranial pressure, insomnia, snotty, extrapyramidal disorders and other disorders of muscle coordination, peripheral sensory or sensory-motor neuropathy, depression with self-harm, up to suicidal thoughts and attempts, tinnitus.

From the side of the locomotor system apparatus: tendonitis, myalgia, arthralgia, tendosynovitis, tendon rupture, pain in the extremities, rhabdomyolysis and / or myopathy.

From the sense organs: violation of color perception, diplopia, violation of taste, smell, hearing and balance.

From the side of the cardiovascular system: tachycardia, increase or decrease in blood pressure.

Allergic reactions: skin rash, itching, hives, allergic pneumonitis, allergic nephritis, eosinophilia. fever, angioedema, bronchospasm; multiforme exudative erythema (including Stevens-Johnson syndrome) and toxic epidermal necrolysis (Lyell's syndrome), photosensitivity, vasculitis. anaphylactic shock. itching of the external genitalia in women.

Co hand dermal integument: point hemorrhage ( petechiae), bullous hemorrhagic dermatitis, papular rash with cortex, indicating the defeat of blood vessels (vasculitis), "tides" of blood to the skin of the face.

On the part of the organs of hematopoiesis: leukopenia, agranulocytosis, anemia (including aplastic and hemolytic), thrombocytopenia, pancytopenia.

From the urinary system: acute interstitial nephritis, impaired renal function, hypercreatininaemia, increased urea concentration, dysuria, urinary retention.

Other: dysbacteriosis of the intestine, superinfection, hypoglycemia (in diabetic patients), vaginitis, chest pain, fatigue, asthenia, general weakness, vaginal discharge, epistaxis, thirst, weight loss, pharyngitis, dyspnea, cough, rhinitis, photophobia, irritation of the mucous membrane of the eye, visual impairment, porphyria attacks in patients with porphyria.

Overdose:

Symptoms: dizziness, confusion, inhibition, disorientation, drowsiness, vomiting.

Treatment: gastric lavage, symptomatic therapy.

Interaction:

Reduces the clearance of theophylline by 25% (with simultaneous use should reduce the dose of theophylline).

Increases the concentration of glibenclamide in plasma.

Increases serum concentration of cyclosporine.

Cimetidine, furosemide, methotrexate and drugs that block tubular secretion, increase the concentration of ofloxacin in blood plasma.

When taken concomitantly with indirect anticoagulants (coumarin derivatives, including warfarin) it is necessary to control the blood coagulation system.

When used with non-steroidal anti-inflammatory drugs, derivatives of nitroimidazole and methylxanthines, the risk of developing neurotoxic effects, including convulsions, increases.

With simultaneous admission with glucocorticosteroids, the risk of rupture of tendons increases, especially in the elderly.

When used with drugs that alkalinize urine (inhibitors of carbonic anhydrase, citrates, sodium hydrogen carbonate), the risk of crystalluria and nephrotoxic effects increases.

With simultaneous administration with hypoglycemic agents, both hypo- and hyperglycemia are possible, and in this connection it is necessary to monitor the concentration of glucose in the blood plasma.

When combined with drugs that extend the interval QT (IA and III classes of antiarrhythmic drugs, tricyclic antidepressants, macrolides), the risk of lengthening of the interval QT.

With simultaneous use with drugs that can reduce blood pressure, drugs for non-general anesthesia from the barbiturate group, a sharp and significant reduction in blood pressure is possible, so in this case, especially careful monitoring of the functional status of the cardiovascular system is required.

Food products, antacids, containing Al³⁺ , Ca²⁺ , Mg²⁺, or salts Fe decrease the absorption of ofloxacin. forming insoluble complexes (the time interval between the intake of these drugs should be at least 2 hours).

Special instructions:

It is not a drug of choice for pneumonia caused by pneumococci. Not indicated in the treatment of acute tonsillitis.

It is not recommended to be exposed to sunlight, irradiation with UV rays (mercury-quartz lamps, solarium).

To prevent the hyperconcentration of urine and subsequent crystalluria during treatment, it is recommended to conduct adequate hydration.

The appearance of diarrhea, especially in severe form, persistent and / or with an admixture of blood.

during or after treatment of ofloxacin may be a manifestation of pseudomembranous colitis.If suspected to develop pseudomembranous colitis, ofloxacin should be stopped immediately, and appropriate specific antibiotic therapy (for example, vancomycin inside, teicoplanin inside or metronidazole) must be appointed without delay. Drugs that inhibit the intestinal peristalsis are contraindicated.

In the event of side effects from the central nervous system, allergic reactions, it is necessary to cancel the drug.

Rarely developing tendonitis can lead to rupture of tendons (mainly Achilles tendon), especially in elderly patients. In case of signs of tendonitis, it is necessary immediately to stop treatment, to immobilize the Achilles tendon and consult an orthopedist.

During the period of treatment can not be consumed ethanol.

When using the drug, women are not recommended to use hygiene tampons due to the increased risk of thrush development.

Against the backdrop of treatment may worsen the flow of myasthenia, an increase in attacks of porphyria.

Can lead to false-negative results in the bacteriological diagnosis of tuberculosis (prevents the isolation Mycobacterium tuberculosis).

In patients with impaired liver function, it is necessary to monitor the concentration of ofloxacin in plasma. With severe hepatic insufficiency, the risk of toxic effects increases (a decreasing dose correction is required).

In patients who use fluoroquinolones, including ofloxacin, cases of sensory and sensorimotor axonal polyneuropathy, affecting small and (or) large axons, and leading to paresthesia, hypostasis, dysesthesia and weakness. Symptoms may to appear soon after the beginning of application and to be irreversible. If the patient develops symptoms of neuropathy, including pain, burning, tingling, numbness and / or weakness or other sensitivity disorders, including tactile, pain, temperature, vibration sensitivity and a sense of position, the use of the drug ofloxacin must be discontinued immediately.

Taking ofloxacin, especially prolonged, can cause a secondary infection associated with the growth of resistant to the preparation of microorganisms. A reassessment of the patient's condition is necessary.

Effect on the ability to drive transp. cf. and fur:

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions. When such undesirable phenomena as dizziness, drowsiness occur, one should refrain from performing these activities.

Form release / dosage:

Film-coated tablets 400 mg.

Packaging:For 5 or 10 tablets in a contoured cell pack of a polyvinylchloride film and aluminum foil printed lacquered. 1 contour pack together with instructions for use in a cardboard pack.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002957

Date of registration:16.04.2015 / 19.02.2016

Expiration Date:16.04.2020

The owner of the registration certificate:RAFARMA, CJSC RAFARMA, CJSC Russia

Manufacturer: & nbsp

RAFARMA, JSC Russia

Information update date: & nbsp18.06.2017

Illustrated instructions

Instructions

Ofloxacin (Ofloxacin)