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

Excipients (core): potato starch - 2,100 mg, microcrystalline cellulose - 93,850 mg, magnesium stearate - 3,000 mg, povidone (polyvinylpyrrolidone) 7.410 mg, croscarmellose sodium - 1,640 mg.

Auxiliary substances (shell): hypromellose - 3,684 mg, macrogol - 1,228 mg, titanium dioxide - 2,088 mg.

Description:

Tablets are round biconvex, covered with a film shell of white or almost white color, slight surface roughness is permissible. On the cross-section, two layers are visible, the inner layer is white or white with a yellowish tinge.

Pharmacotherapeutic group:Antimicrobial agent, fluoroquinolone

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 enzyme DNA hydrase, which ensures super-shrinkage and, thus, the stability of bacterial DNA (the destabilization of DNA chains leads to their death). Has a bactericidal effect.

Highly active against most gram-negative and some gram-positive microorganisms: Aeromonas hydrophila, Branhamella catarrhalis, Brucella spp., Clostridium perfringens, Escherichia coli, Salmonella spp., Enterobacter spp., Serratia spp., Citrobacter spp., Yersinia spp., Providencia spp., Haemophilus influenzae and parainfluenzae, Haemophilus ducreyi, Plesiomonas, Legionella, Shigella spp., Proteus spp., including Proteus mirabilis, Proteus vulgaris (indol +, indol -), Moraxella morganii, Klebsiella spp. (including Klebsiella pneumonia), Helicobacter pylori, Mycoplasma spp., Vibrio spp., Gardnerella vaginalis, Neisseria gonorrhoeae, Neisseria meningitidis, Chlamydia trachomatis, Staphylococcus aureus methi-S, Staphylococcus coagulase negative.

Moderately sensitive to ofloxacin Acinetobacter spp., Ureaplasma urealyticum, Bacteroides fragilis, Mycobacterium tuberculosis, Mycobacterium fortuitum, Chlamidia psittaci, anaerobic Gram-positive cocci, Enterococcus faecalis, Streptococcus pneumoniae, Pseudomonas spp., Streptococcus spp. (especially beta-hemolytic).

To ofloxocin insensitive Acinetobacter braumanmii, Clostridium difficile, Enterococci, Listeria monocytogenes, Staphylococci methi-R, Nocardia spp.

Ofloxacin is inactive with respect to Treponema pallidum.

Pharmacokinetics:

Absorption after oral administration is rapid and complete (95%). Bioavailability is over 96%, the connection with plasma proteins is 25%. Time to reach the maximum concentration (TCmah) with oral intake - 1 -2 hours. Maximum concentration (FROMmOh) after taking the dose of 100, 200, 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. The volume of distribution is 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 blood-brain barrier, the placental barrier, is secreted with the mother's milk. It penetrates into the cerebrospinal fluid (14-60%). Metabolized in the liver (about 5%) with formation NOxygen ofloxacin and dimethylfloxacin. The half-life (T1 / 2) is 4.5-7 hours (regardless of the 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:

Treatment of infectious-inflammatory diseases caused by microorganisms sensitive to ofloxacin:

-infection of the respiratory tract (with the exception of cases of pneumococcal infection); -infection of the ear, throat, nose (except for cases of acute tonsillitis);

-infections of the abdominal cavity and biliary tract;

-infection of the kidneys, urinary tract, prostate, urethra (including gonococcal nature);

-infection of the pelvic organs;

- infection of bones and joints;

-infection of skin and soft tissues;

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

Contraindications:

-Increased sensitivity to ofloxacin, other quinolones or components of the drug;

-epilepsy;

-Corruption of the central nervous system with a lower convulsive threshold (after traumatic brain injury, stroke, inflammatory processes in the central nervous system (CNS);

- the damage of tendons during the previous treatment with quinolones;

- deficiency of glucose-6-phosphate dehydrogenase;

-About 18 years of age;

- Pregnancy and lactation.

Carefully: In patients with atherosclerosis of cerebral vessels, cerebral circulation disorder (in the anamnesis), chronic renal insufficiency, organic lesions of the central nervous system, with lengthening of the interval QT.

Pregnancy and lactation:Contraindicated.

Dosing and Administration:

Inside.

The dose of ofloxacin and the duration of treatment depend on the severity and type of infection, the general condition of the patient and the function of the kidneys.

The average daily intake for adults is from 200 mg to 600 mg. The duration of treatment is 7-10 days.

A dose of up to 400 mg / day can be given in one session, preferably in the morning. Doses over 400 mg / day should be divided into 2 doses with an equal time interval. Tablets should be taken whole, washed down with water before and during meals. It is necessary to avoid simultaneous reception together with antacids.

In severe infections or in the treatment of patients with overweight, the daily dose can be increased to 800 mg.

In uncomplicated infections of the lower urinary tract, the drug is prescribed at a dose of 200 mg / day for 3-5 days. With gonorrhea prescribed 400 mg once.

In patients with impaired renal function, the dose should be reduced depending on the creatinine clearance:

Creatinine clearance	Single dose	Interval between doses
50-20 ml / min	100-200 mg	24 hours
less than 20 ml / min or hemodialysis	100 mg	24 hours
hemodialysis less than 20 ml / min or hemodialysis	200 mg	48 hours

In patients with hepatic insufficiency it is not recommended to exceed the maximum daily dose of 400 mg.

Side effects:From the digestive system: gastralgia, decreased appetite, nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity of "liver" transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous enterocolitis.

From the nervous system: headaches, dizziness, motion uncertainty, tremors, convulsions, numbness and paresthesia of the limbs, intense dreams, nightmarish dreams, psychotic reactions, anxiety, arousal, phobias, depression, confusion, hallucinations, increased intracranial pressure.

From the side of the musculoskeletal system: tendonitis, myalgia, arthralgia, tendosynovitis, tendon rupture.

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

From the side of the cardiovascular system: tachycardia, lowering of blood pressure (BP),

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.

From the skin: point hemorrhages (petechiae), bullous hemorrhagic dermatitis, papular rash with a cortex, indicative of vascular lesions (vasculitis).

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

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

Other: dysbacteriosis of the intestine, superinfection, hypoglycemia (in patients with diabetes mellitus), vaginitis.

Overdose:

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

In case of an overdose, it is recommended to perform gastric lavage and symptomatic therapy. There is no specific antidote.

Interaction:

Antacids containing aluminum hydroxide (including sucralfate) and magnesium hydroxide, aluminum phosphate, zinc, iron reduce the absorption of ofloxacin. When you receive antacids and ofloxacin between their intake should be kept approximately two-hour interval.

With the simultaneous use of vitamin K antagonists, control over the blood coagulation system is necessary.

Ofloxacin may slightly increase the serum concentrations of glibenclamide when used concomitantly.

In the case of using high doses of ofloxacin and other drugs released by renal tubular secretion, such as probenecid, cimetidine, furosemide or methotrexate, it is possible to increase the concentration of ofloxacin in the blood serum.

A marked decrease in the threshold of convulsive activity can be observed with the appointment of fluoroquinolones in combination with theophylline, fenbufen or other nonsteroidal anti-inflammatory drugs, as well as other drugs that lower the threshold of seizure activity.

In conjunction with non-steroidal, anti-inflammatory agents, nitroimidazole derivatives and methylxanthines, the risk of neurotoxic effects increases.

At simultaneous appointment with glucocorticosteroids, the risk of rupture of tendons increases, especially in the elderly.

When co-administered with drugs, the lengthening interval QT (IA and III classes of antiarrhythmic drugs, tricyclic antidepressants, macrolides) increases the risk of lengthening the interval QT.

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

Special instructions:

Due to ofloxacin is excreted mainly through the kidneys, patients with renal insufficiency need a dose adjustment of ofloxacin. Due to the risk of photosensitization, exposure to sunlight and ultraviolet rays should be avoided. The appearance of diarrhea, especially in severe, persistent and / or mixed with blood, during or after treatment with ofloxacin may be a manifestation of pseudomembranous colitis. If there is a suspected development of pseudomembranous colitis, ofloxacin should be immediately discontinued and appropriate specific antibiotic therapy should be given promptly. In this clinical situation, drugs that suppress the intestinal peristalsis are contraindicated.

Like other quinolones, ofloxacin must be administered with caution to patients predisposed to development of epileptic seizures (patients with a history of damage to the central nervous system, receiving fenbufen and similar non-steroidal anti-inflammatory drugs or medications that lower seizure threshold, e.g., theophylline).

Tendinitis, which occurs very rarely, can sometimes lead to the rupture of tendons, predominantly Achilles tendon, especially in elderly patients. In case of signs of tendonitis (inflammation of the tendon), it is recommended to immediately stop the treatment, immobilize the Achilles tendon and provide orthopedic consultation.

Some caution is needed when taking fluoroquinolones, including ofloxacin, in patients with known risk factors for lengthening the interval QT, such as:

-elderly age;

- an unbalanced electrolyte imbalance (eg, hypokalemia, hypomagnesemia); -defined interval elongation QT;

- cardiovascular disease (heart failure, myocardial infarction, bradycardia);

- simultaneous reception of drugs that extend the interval QT (IA and III classes of antiarthmics, tricyclic antidepressants, macrolides).

Ofloxacin can lead to a worsening of myasthenia flow. Perhaps more frequent attacks of porphyria. During the treatment with ofloxacin, false-positive results are possible when determining opiates and porphyrins in urine.

Ofloxacin prevents the release of Mycobacterium tuberculosis, leading to false-negative results in the bacteriological diagnosis of tuberculosis. Also during the period of treatment is not recommended to use ethanol. Ofloxacin It is not a drug of choice for pneumonia caused by pneumococci. Not indicated in the treatment of acute tonsillitis.

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated 200 mg.

Packaging:

10 tablets per contour cell package of film polyvinylchloride and aluminum foil printed lacquered.

By 10, 20, 30 tablets into a polymer container for medicines.One container or 1, 2, 3 contour mesh packages together with instructions for use are placed in a pack of cardboard.

Storage conditions:

Store in a dry, dark 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:P N002657 / 01

Date of registration:09.02.2009

Expiration Date:Unlimited

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp17.06.2017

Illustrated instructions

Instructions

Ofloxacin (Ofloxacin)