Ofloxacin, tab. of 200 mg No. 10, 400 of mg No. 5

General characteristics. Structure:

Active agent: 1 tablet contains an ofloksatsin of 200 mg or 400 mg; excipients: lactose, sodium of a kroskarmelloz, starch corn, magnesium stearate, gidroksipropilmetil-cellulose, hydroxypropyl cellulose, titanium dioxide (Е 171), the talc purified polyethyleneglycol 6000.

Pharmacological properties:

Pharmacodynamics. Antimicrobic means of group of ftorkhinolon of a broad spectrum of activity. Bactericidal a deystviyeofloksatsina it is caused by ability to block bacterial DNK-girazu enzyme owing to what the DNA function of bacteria is broken. The range of antimicrobic action covers the majority gram-negative and some gram-positive microorganisms. Synergy action of an ofloksatsin and rifabutin concerning Mycobacteriumleprae is established.

Pharmacokinetics. After intake it is quickly and easily adsorbed from the zheludochno-a intestinal path (ZIP). The maximum concentration of an ofloksatsin in a blood plasma after reception of orally single dose of 200 mg makes 2,5-3,0 mg/ml and is reached in 1-2 hours. Biological availability of drug makes 96 - 100%. Contacts proteins of plasma about 25%. Ofloxacin gets through a placenta, is emitted in breast milk. About 5% of an ofloksatsin are metabolized. It is removed for 5 - 8 hours. To 80% of an ofloksatsin it is removed by kidneys in not changed look. At patients with a disease of kidneys and a liver a conclusion of an ofloksatsin from an organism can be slowed down.
At patients of advanced age at reception of a peroral single dose of an ofloksatsin increase in an elimination half-life of drug is observed, but the maximum concentration in blood serum does not change. At patients with a renal failure in proportion to decrease in clearance of creatinine the elimination half-life increases, the general and renal clearance decreases.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to an ofloksatsin:
- acute, chronic and recurrent respiratory infections; the bronchitis caused by Haemophilusinfluenzae or other gram-negative multiresistant activators, and also golden staphylococcus; the pneumonia caused by such problem activators as colibacillus, a klebsiyella, enterobakteriya, proteas, staphylococcus;
- persistent and recurrent infections of ENT organs (an ear, a throat and a nose) if they are caused by gram-negative activators or stafilokokka;
- infections of skin, soft tissues, bones, joints;
- infections of kidneys, urinary tract and generative organs: acute and chronic pyelonephritis, surgical infections of uric ways, gonorrhea, uncomplicated prostatitis of a gonorrheal and not gonorrheal etiology, urethritis, cystitis, clamidiosis;
- infectious and inflammatory diseases of abdominal organs including small pelvis;
- bacterial enteritis.
Drug is used also for prevention of infections (prevention of infections by intestines decontamination) at patients with reduced protective properties of an organism (for example, in a condition of a neutropenia).

Route of administration and doses:

The mode of dosing is defined by the doctor individually, depending on weight of process and a type of an infection, function of kidneys of the patient.
Adults with normal function of kidneys. The average single dose makes 200 mg 2 times a day with an interval of 12 hours. Daily dose of 400 mg. The doses which are not exceeding 400 mg can be appointed 1 time a day, is preferential in the morning. If the daily dose exceeds 400 mg, it can be divided into 2 receptions and is received by the patient at regular intervals.
The daily dose can be increased to 600 mg, at patients with heavy infections or in cases of excess body weight: the maximum dose – to 800 mg.
At respiratory infection 2 times a day apply 200 mg of an ofloksatsin.
At infections of kidneys, urinary tract and generative organs appoint 200 mg of an ofloksatsin twice a day.
At treatment of cystitis there can be sufficient a use of an ofloksatsin within 3 days on 200 mg 2 times a day whereas treatment of prostatitis can last several weeks (on 200 mg 2 times a day).
At treatment of uncomplicated gonorrhea of rather single dose of 400 mg.
At infections of skin, soft tissues and bones ofloxacin is accepted on 200 mg by 2 times a day, the daily dose makes 400 mg.
At infections of bones duration of treatment makes 3 – 4 weeks, in some cases – longer.
At infections of an abdominal cavity ofloxacin is accepted on 200 mg by 2 times a day, the daily dose makes 400 mg.
For patients with heavy abnormal liver functions the daily dose should not exceed 400 mg.
Dose adjustment of an ofloksatsin is not required from patients of advanced age.

Features of use:

Some strains of microorganisms are moderately sensitive to an ofloksatsin therefore drug is not recommended to be used as means of the first row for treatment of the pneumonia caused by pneumococci and also the acute tonsillitis caused by a beta and hemolitic streptococcus. At the hospital and other heavy infections connected with Pseudomonasaeruginosa the combination therapy can be necessary. Specific therapy of the infections caused by Pseudomonasaeruginosa requires resistance definition.
The diseases caused by Clostridiumdifficile. In time or after treatment ofloksatsiny can be displays of the diseases caused by Clostridiumdifficile heavy, persistent and/or blood diarrhea which severe form is pseudomembranous colitis. At suspicion on development of such complication treatment ofloksatsiny has to be immediately stopped, and emergency antibacterial treatment is at the same time appointed. In that case the drugs reducing a peristaltics of intestines are contraindicated.
Tendinitis. In isolated cases at treatment of a hinolonama there can be a tendinitis leading to a rupture of sinews, mainly, of an Achilles sinew. Patients of advanced age are most inclined to tendinites. The risk of a rupture of sinews amplifies at treatment by corticosteroids. At tendency to a tendinitis treatment ofloksatsiny it is necessary to stop and host immediately the relevant activities to sinews (for example, an immobilization).
Patients inclined to spasms. Ofloxacin is contraindicated to patients with the established epilepsy. It is similar to other hinolona, it should be applied with care to the patients inclined to spasms, for example, to patients with the existing damages of the central nervous system at simultaneous treatment fenbufeny, the nonsteroid antipsychotic means or drugs reducing a convulsive threshold such as theophylline.
Patients with an impaired renal function. As ofloxacin is removed, generally by kidneys, patients with an impaired renal function need to regulate a dose or to use drug in other dosage. This form of drug at treatment of a renal failure is not appointed.
Prevention of photosensitivity. Though at use of an ofloksatsin very seldom there is a photosensitivity, patients should avoid solar or artificial Uv-radiation (for example, sunlight lamps, a sunbed) to avoid a photosensitization.
Ofloxacin is taken with caution at atherosclerosis of vessels of a brain, disturbances of cerebral circulation, renal failures.
At treatment ofloksatsiny definition of opiates or porphyrine in urine can yield lozhnopozitivny result.
Drug contains lactose therefore patients with rare hereditary forms of intolerance of a galactose, insufficiency of lactase or a syndrome of glyukozo-galaktozny malabsorption should not apply ofloxacin.

Side effects:

Side reactions arise seldom and quickly disappear after drug withdrawal. Ofloxacin is, as a rule, transferred well, but side effects are possible during treatment.
From system of digestion: abdominal pain, nausea, vomiting, lack of appetite, diarrhea, pseudomembranous colitis.
From a nervous system: headache, fatigue, drowsiness, excitement, goglovokruzheniye, disturbance of peripheral sensitivity (vision disorder, taste), sonitus, spasms, loss of consciousness.
Seldom: psychotonic reactions (with hallucinations), alarming states, dreadful dreams.
The isolated cases: the psychotonic reactions which are followed menacing povedeny for the patient.
From system of blood: seldom - anemia, a neutropenia, thrombocytopenia, a leukopenia.
The isolated cases: agranulocytosis, pancytopenia, oppression of a marrowy hemopoiesis.
From cardiovascular system: tachycardia, arterial hypotension, collapse.
Myshechno - skeletal reactions: the tendinitis, especially at patients of advanced age, a mialgiya, an arthralgia, a gap is (Achilles) sinews – unilateral or bilateral. Such side reaction can be observed within 48 hours after an initiation of treatment.
The isolated cases: the muscular weakness having special value at patients with a heavy pseudoparalytic myasthenia.
Reactions from outside blood serum creatinine pochek:povysheniye, acute renal failure.
The isolated cases: acute intersticial nephrite.
Reactions from outside pecheni:povysheny activities of liver enzymes or bilirubin, cholestatic jaundice.
Allergic reactions: rash on skin, a paraglossa, a Quincke's edema.
Seldom: a small tortoiseshell, a Quincke's disease, a suffocation/bronchospasm, rushes of blood, the strengthened potovydeleniye, pustulopodobny skin rash.
The isolated cases: a multiformny erythema, a toxic epidermal necrolysis, a photosensitization, a vascular purpura, the vasculitis leading as an exception to a necrosis.
Anaphylactic or anaphylactoid reactions arise very seldom in the form of a thermalgia in eyes, the irritating cough or allocations from a nose, a cutaneous dropsy and mucous membranes, the person, language, a throat. In the most hard cases drug is immediately cancelled and carry out the antishock and desensibilizing therapy.
Other side effects: very seldom the mialgiya or weakness, especially at patients with a myasthenia can be noted. There can seldom be a hypoglycemia or a hyperglycemia, especially at patients with a diabetes mellitus.
The isolated cases: a hypoglycemia at patients with a diabetes mellitus, the receiving hypoglycemic drugs.

Interaction with other medicines:

The antacids containing aluminum magnesia hydroxide, zinc, iron can reduce adsorption of an ofloksatsin. In such cases reception of an ofloksatsin is possible in 2 hours after reception of antacids. At simultaneous use of antagonists of vitamin K constant control behind a condition of system of a blood coagulation as decrease of the activity of coumarinic derivatives is possible is necessary. Ofloxacin can slightly increase serumal concentration of Glibenclamidum at simultaneous use. In case of use of high doses of drug, increase in its concentration in serum is possible. At simultaneous use of an ofloksatsin and non-steroidal anti-inflammatory drugs the risk of emergence of spasms increases. At use of an ofloksatsin with caffeine, theophylline, Cimetidinum, cyclosporine, the peroral anticoagulants and drugs metabolizing with the participation of P450 cytochrome strengthening of side effects is possible. During treatment ofloksatsiny pseudo-negative results of definition of opiates and porphyrines in urine are possible.

Contraindications:

Hypersensitivity to an ofloksatsin or other ftorkhinolona, epilepsy, defeats of TsNS with a reduced convulsive threshold, liver diseases, anamnestic damage of sinews after reception of ftorkhinolon, deficit glyukozo-6-fosfatdegidrogenazy, children's age up to 18 years, the period pregnancy and feeding by a breast.

Overdose:

The most important symptoms of overdose are symptoms from a nervous system: dizziness, excitement, spasms, headache.
Reactions from the alimentary system: nausea, vomiting, abdominal pain, diarrhea.
Treatment: the symptomatic, including gastric lavage and correction of a water balance.

Storage conditions:

To store in the dry, protected from light place at a temperature not over 25 of 0C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Ofloxacin on 200 mg on 10 tablets in the blister. Ofloxacin on 400 mg on 5 tablets in the blister.